Entries |
Document | Title | Date |
20080200448 | New Pyridine Analogues VIII 518 - The present invention relates to certain new pyridin analogues of Formula (I) | 08-21-2008 |
20080207587 | Pyridazine Derivatives for Inhibiting Human Stearoyl-Coa-Desaturase - Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I) where x, y, G, J, K, L, M, Q, W, V, R2, R3, R5, R5a, R6, R6a, R7, R7a, R8 and R8a arc defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed. | 08-28-2008 |
20080214519 | Chromane Substituted Benzimidazole Derivatives as Acid Pump Antagonists - This invention relates to compounds of the formula (I): or a pharmaceutically acceptable salt thereof, wherein: A, B, X, R | 09-04-2008 |
20080234249 | CYCLIC 11-BETA HYDROXYSTEROID DEHYDROGENASE TYPE I INHIBITORS - Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-Beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure: | 09-25-2008 |
20080242655 | AZA-INDOLYL COMPOUNDS AND METHODS OF USE - The invention relates to azaindolyl compounds of Formula I with anti-cancer and/or anti-inflammatory activity and more specifically to azaindolyl compounds which inhibit MEK kinase activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth or treating a hyperproliferative disorder, or treating an inflammatory disease in a mammal. The invention also relates to methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions. | 10-02-2008 |
20080249079 | Pyrimidine Derivatives As Kinase Modulators and Method of Use -
The invention provides compounds and methods for inhibition of kinases, more specifically IGF 1 R kinases. The invention also provides compounds and methods for inhibition of wildtype Abl. The invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Compounds of the invention inhibit, regulate and/or modulate kinase receptor signal transduction pathways related to the changes in cellular activities as mentioned above, and the invention includes compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. A compound of formula (I), or a pharmaceutically acceptable salt, hydrate, or prodrug thereof, wherein, V is NR | 10-09-2008 |
20080255085 | Novel Imidazo [4,5-b] Pyridine Derivatives as Inhibitors of Glycogen Synthase Kinase 3 for Use in the Treatment of Dementia and Neurodegenerative Disorders - Compounds of formula I | 10-16-2008 |
20080275021 | PYRROLIDINE DERIVATIVES AS DUAL NK1/NK3 RECEPTOR ANTAGONISTS - The invention relates to pyrrolidine derivatives of formula | 11-06-2008 |
20080280871 | 5-Phenyl-4-Methyl-Thiazol-2-Yl-Amine Derivatives as Inhibitors of Phosphatidylin Ositol 3 Kinase Enzymes (PI13) For Treatment of Inflammatory Diseases - in free or salt form, wherein R | 11-13-2008 |
20080280872 | Benzamide Derivatives and Their Use as Glucokinase Activating Agents - Compounds of Formula (I): wherein: R | 11-13-2008 |
20080280873 | Biaryl Substituted Pyrazinones as Sodium Channel Blockers - Biaryl substituted pyrazinone compounds represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, and bipolar disorder, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds. A method of administering local anesthesia comprises administering an effective amount of a compound of the instant invention, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. | 11-13-2008 |
20080280874 | Phenoxy Benzamide Compounds with Utility in the Treatment of Type 2 Diabetes and Obesity - Compounds of Formula (I): | 11-13-2008 |
20080280875 | FUSED PHENYL AMIDO HETEROCYCLIC COMPOUNDS - The present invention relates to a compound of formula (I): | 11-13-2008 |
20080280876 | Novel oxadiazole compounds - Novel oxadiazole compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions as agonists or antagonists of the S1P family of G protein-coupled receptors for treating diseases associated with modulation of S1P family receptor activity, in particular by affording a beneficial immunosuppressive effect are disclosed. | 11-13-2008 |
20080280877 | Azetidines - The invention relates to EP2 antagonist azetidines of formula (I) | 11-13-2008 |
20080312207 | Compounds - Compounds of Formula (I) wherein: R1 is methyl; R2 is selected from —C (O) NR4R5, SO2NR4R5, S (O) pR4 and HET-2; HET-1 is a 5- or 6-membered, optionally substituted C-linked heteroaryl ring; HET-2 is a 4-, 5- or 6-membered, C- or N-linked optionally substituted heterocyclyl ring; R3 is selected from halo, fluoromethyl, difluoromethyl, trifluoromethyl, methyl, methoxy and cyano; R4 is selected from for example hydrogen, optionally substituted (1-4C) alkyl and HET-2; R5 is hydrogen or (1-4C) alkyl; or R4 and R5 together with the nitrogen atom to which they are attached may form a heterocyclyl ring system as defined by HET-3; HET-3 is for example an optionally substituted N-linked, 4, 5 or 6 membered, saturated or partially unsaturated heterocyclyl ring; p is (independently at each occurrence) 0, 1 or 2; m is 0 or 1; n is 0, 1 or 2; provided that when m is 0, then n is 1 or 2; or a salt, pro drug or solvate thereof, are described. Their use as GLK activators, pharmaceutical compositions containing them and processes for their preparation are also described. | 12-18-2008 |
20080312208 | Pyridine Analogues - The present invention relates to certain new pyridin analogues of Formula (I) Chemical formula should be inserted here. Please see paper copy Formula (I) to processes for preparing such compounds, to their utility as P2Y | 12-18-2008 |
20080312209 | Piperazine Heteroaryl Derivatives as Gpr38 Agonists - The invention provides compounds of formula (I) or pharmaceutically acceptable salts thereof, | 12-18-2008 |
20080318922 | Bicyclic Pyrrole Derivatives - Compounds represented by the general formula (I), prodrugs thereof, or pharmaceutically acceptable salts of both are provided as compounds which have high DPP-IV inhibiting activity and are improved in safety, toxicity and so on: (I) | 12-25-2008 |
20080318923 | 1,3-Dihydro-2H-Indole-2-One Compound and Pyrrolidine-2-One Compound Fused With Aromatic Heterocycle - It is intended to provide a drug which is efficacious against pathological conditions relating to arginine-vasopressin V1b receptor. More particularly speaking, it is intended to provide a drug which has a therapeutic or preventive effect on depression, anxiety, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorders, hypertension, digestive diseases, drug addiction, epilepsy, brain infarction, brain ischemia, brain edema, head injury, inflammation, immune diseases, alopecia and so on. As the results of intensive studies, a novel 1,3-dihydro-2H-indol-2-one compound and a pyrrolidin-2-one compound fused with a heteroaromatic ring, which are highly selective antagonists of arginine-vasopressin V1b receptor, have high metabolic stabilities and show favorable brain penetration and high plasma concentrations, are found, thereby achieving the above objective. | 12-25-2008 |
20080318924 | PHENOXYPYRIDINE DERIVATIVE SALTS AND CRYSTALS THEREOF, AND PROCESS FOR PREPARING THE SAME - The invention provides acid addition salts of the compounds represented by formula (1) or (2), or crystals thereof, and processes for preparing the same. The salts or crystals have HGFR inhibitory activity and excellent physical properties (solubility, safety, etc.) and are therefore useful as anti-tumor agents, angiogenesis inhibitors and inhibitors for metastasis for a various types of tumor. | 12-25-2008 |
20080318925 | Compounds and Uses Thereof - 849 - This invention relates to the use of compounds having the structural formula I below: | 12-25-2008 |
20090005355 | Piperidine Compound and Process for Preparing the Same - The present invention is to provide a piperidine compound represented by the formula [I]: | 01-01-2009 |
20090005356 | SUBSTITUTED PYRROLOPYRIDINES AND PYRAZOLOPYRIDINES AS KINASE MODULATORS - Provided herein are substituted pyrrolopyridine heterocycles and substituted pyrazolopyridine heterocycles, pharmaceutical compositions comprising said heterocycles and methods of using said heterocycles in the treatment of disease. The heterocycles disclosed herein function as kinase modulators and have utility in the treatment of diseases such as cancer, allergy, asthma, inflammation, obstructive airway disease, autoimmune diseases, metabolic disease, infection, CNS disease, brain tumor, obesity, asthma, hematological disorder, degenerative neural disease, cardiovascular disease, or disease associated with angiogenesis, neovascularization, or vasculogenesis. | 01-01-2009 |
20090018112 | Compounds and Uses Thereof - This invention relates to novel compounds having the structural formula I below: | 01-15-2009 |
20090023702 | PYRIDONE GPR119 G PROTEIN-COUPLED RECEPTOR AGONISTS - Novel compounds are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR 119 G protein-coupled receptor modulator therapy. These novel compounds have the structure Formula I or Formula IA. | 01-22-2009 |
20090023703 | Pyrrolopyridine-2-carboxylic acid amide inhibitors of glycogen phosphorylase - Compounds represented by Formula (I): | 01-22-2009 |
20090029965 | Vasopressin V1a Antagonists - The present invention concerns compounds inter alia according to general formula 1 | 01-29-2009 |
20090042854 | Hexahydro-3H-Pyrrolizin-3-Ones Useful as Tachykinin Receptor Antagonists - The present invention is directed to certain hexahydrpyrrolidinone compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety. | 02-12-2009 |
20090042855 | BENZAMIDE mGluR5 POSITIVE ALLOSTERIC MODULATORS AND METHODS OF MAKING AND USING SAME - In one aspect, the invention relates to compounds, including phenylethynylbenzamide derivatives, cycloalkylethynylbenzamide derivatives, styrylbenzamide derivatives, 4-(3-phenyl-1,2,4-oxadiazol-5-yl)benzamide derivatives, 4-(pyridinylethynyl)benzamide derivatives, and N | 02-12-2009 |
20090048226 | Inhibitors of caspases - The present invention relates to novel classes of compounds which are caspase inhibitors, in particular interleukin-1β converting enzyme (“ICE”) inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting caspase activity and consequently, may be advantageously used as agents against interleukin-1-(“IL-1”), apoptosis-, interferon-γ inducing factor-(IGIF), or interferon-γ-(“IFN-γ”) mediated diseases, including inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, and degenerative diseases. This invention also relates to methods for inhibiting caspase activity and decreasing IGIF production and IFN-γ production and methods for treating interleukin-1, apoptosis-, and interferon-γ-mediated diseases using the compounds and compositions of this invention. This invention also relates to methods of preparing the compounds of this invention. | 02-19-2009 |
20090048227 | Substituted-1-Phthalazinamines As Vr- 1 Antagonists - Substituted piperidine compounds represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, and bipolar disorder, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds. | 02-19-2009 |
20090054395 | SULFONYL AMIDE DERIVATIVES FOR THE TREATMENT OF ABNORMAL CELL GROWTH - The present invention relates to a compound of the formula I | 02-26-2009 |
20090062252 | THERAPEUTIC ISOXAZOLE COMPOUNDS - The invention provides a compound of formula I: | 03-05-2009 |
20090069288 | Novel therapeutic compounds - Disclosed herein are novel compounds of Formula (I), | 03-12-2009 |
20090082329 | Novel Sulphur-Containing Cyclic Urea Derivatives, Preparation Thereof and Pharmaceutical Use Thereof as Kinase Inhibitors - The disclosure relates to compounds of formula (I): | 03-26-2009 |
20090082330 | CERTAIN SUBSTITUTED AMIDES, METHOD OF MAKING, AND METHOD OF USE THEREOF - Compounds of Formula I that inhibit Btk are described herein. Pharmaceutical compositions comprising at least one compound of Formula I, together with at least one pharmaceutically acceptable vehicle chosen from carriers, adjuvants, and excipients, are described. Methods of treating patients suffering from certain diseases responsive to inhibition of Btk activity and/or B-cell activity are described. Methods for determining the presence of Btk in a sample are described. | 03-26-2009 |
20090082331 | S1P RECEPTOR MODULATING COMPOUNDS AND USE THEREOF - The present invention relates to amides that have activity as SIP receptor modulating agents and the use of such compounds to treat diseases associated with inappropriate S1P receptor activity. The compounds may be used as immunomodulators, e.g., for treating or preventing diseases such as autoimmune and related immune disorders including systemic lupus erythematosus, inflammatory bowel diseases such as Crohn's disease and ulcerative colitis, type I diabetes, uveitis, psoriasis, myasthenia gravis, rheumatoid arthritis, non-glomerular nephrosis, hepatitis, Behçet's disease, glomerulonephritis, chronic thrombocytopenic purpura, hemolytic anemia, hepatitis and Wegner's granuloma; and for treating other conditions. | 03-26-2009 |
20090093452 | Pyrrole, Thiophene, Furan, Imidazole, Oxazole, and Thiazole Derivatives - Disclosed are compounds and pharmaceutically acceptable salts of Formula I | 04-09-2009 |
20090105209 | BTK protein kinase inhibitors - This application discloses pyridine and pyrimidine compounds according to formula I wherein R | 04-23-2009 |
20090111789 | CHIRAL CIS-IMIDAZOLINES - There are provided compounds of the formula | 04-30-2009 |
20090111790 | HETEROARYL BENZAMIDE DERIVATIVES FOR USE AS GLK ACTIVATORS IN THE TREATMENT OF DIABETES - Compounds of formula (I) | 04-30-2009 |
20090111791 | Soluble Epoxide Hydrolase Inhibitors and Methods of Using Same - Disclosed are compounds active against soluble epoxide hydrolase (sEH), compositions thereof and methods of using and making same. | 04-30-2009 |
20090118254 | HISTAMINE H3 RECEPTOR AGENTS, PREPARATION AND THERAPEUTIC USES - The present invention discloses novel compounds of Formula I or pharmaceutically acceptable salts thereof which have histamine-H3 receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I as well as methods of using these compositions to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases. | 05-07-2009 |
20090131398 | OXINDOLE DERIVATIVE AS FEEDING CONTROL AGENT - Disclosed is a compound represented by the formula (1) below, a prodrug thereof or a pharmaceutically acceptable salt of either, which is useful as a therapeutic, preventive or ameliorating agent for diabetes and the like. | 05-21-2009 |
20090137549 | Novel compounds useful for the treatment of degenerative & inflamatory diseases - The present invention relates to compounds that are inhibitors of PDE1A, a phosphodiesterase that is involved in the modulation of the degradation of cartilage, joint degeneration and diseases involving such degradation and/or inflammation. | 05-28-2009 |
20090143352 | PYRROLO-PYRIDINE KINASE MODULATIORS - The present invention provides novel pyrrolo-pyridine kinase modulators and methods of using the novel pyrrolo-pyridine kinase modulators to treat diseases mediated by kinase activity. | 06-04-2009 |
20090149439 | PYRIDYLMETHYSULFONE DERIVATIVE - The present invention relates to a novel compound having an effect of inhibiting production/secretion of β-amyloid protein. The present invention provides a compound represented by the general formula (1): | 06-11-2009 |
20090156576 | Azetidines as MEK Inhibitors for the Treatment of Proliferative Diseases - Disclosed are compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof. Such compounds are MEK inhibitors and are useful in the treatment of proliferative diseases, such as cancer. Also disclosed are pharmaceutical compositions containing such compounds as well as methods of using the compounds and compositions of the invention in the treatment of cancer. | 06-18-2009 |
20090163467 | New compounds - The present invention encompasses compounds of general formula (1) | 06-25-2009 |
20090163468 | Fused Bicyclic mTor Inhibitors - Compounds represented by Formula (I) | 06-25-2009 |
20090163469 | Organic Compounds - The present invention relates to compounds of formula I | 06-25-2009 |
20090163470 | THIAZOLYLIDINE UREA AND AMIDE DERIVATIVES AND METHODS OF USE THEREOF - The invention relates to novel thiazolylidine urea and amide derivatives that are PAMs of neuronal nicotinic receptors, compositions comprising the same, processes for preparing such compounds, and methods for using such compounds and compositions. | 06-25-2009 |
20090176756 | SUBSTITUTED THIAZOLES AND THEIR USE FOR PRODUCING DRUGS - The present invention relates to substituted thiazoles, to methods for the production thereof, to medicaments containing these compounds and to the use thereof for producing medicaments. | 07-09-2009 |
20090186867 | Substituted Diketopiperazines As Oxytocin Antagonists - A method of treating or preventing diseases or conditions mediated through the action of oxytocin which comprises administering to a human in need thereof of an effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof. | 07-23-2009 |
20090197862 | 2-AMINOPYRIDINE KINASE INHIBITORS - 2-Aminopyridine compounds having the structure of Formula I, and pharmaceutically acceptable salts of these compounds. Compounds of Formula I inhibit the activity of tyrosine kinase enzymes in animals, including humans, and are useful in the treatment and/or prevention of various diseases and conditions. In particular, compounds disclosed herein are inhibitors of kinases, in particular, but not limited to, KDR, Tie-2, Flt3, FGFR3, Ab1, Aurora A, c-Src, IGF-1R, ALK, c-MET, RON, PAK1, PAK2, and TAK1, and can be used in the treatment of proliferative diseases, such as, but not limited to, cancer. The present invention is also directed to a pharmaceutical composition comprising a therapeutically effective amount of a compound of Formula I, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. The present invention is further directed to a method of treating a patient having a condition which is mediated by protein kinase activity by administering to the patient a therapeutically effective amount of the above-mentioned pharmaceutical composition. | 08-06-2009 |
20090215741 | 1H-Pyrimido[4,5-b]indole Derivatives, Their Preparation and Therapeutic Use - The disclosure concerns compounds of general formula (I): | 08-27-2009 |
20090221547 | Immunosuppressant Compounds and Compositions - The present invention relates to immunosuppressants, processes for their production, their uses and pharmaceutical compositions containing them. The invention provides a novel class of compounds useful in the treatment or prevention of diseases or disorders mediated by lymphocyte interactions, particularly diseases associated with EDG receptor mediated signal transduction. This application relates to compounds selected from Formula (Ia), (Ib), (Ic) and (Id). | 09-03-2009 |
20090239838 | PYRROLOTRIAZINE KINASE INHIBITORS - The invention provides compounds of formula I | 09-24-2009 |
20090247501 | PROTEIN KINASE INHIBITORS - Pyrimidine- and triazine-based chemical compounds that are useful, for example, as protein kinase inhibitors for treating cancer, neurological disorders, autoimmune disorders, and other diseases, and methods of using such compounds | 10-01-2009 |
20090247502 | SUBSTITUTED PYRIDOXAZINES - The invention provides compounds having the structure of formula I, | 10-01-2009 |
20090253676 | Heteroaryl Benzamide Derivatives for Use as GLK Activators in the Treatment of Diabetes - Compounds of Formula (I): | 10-08-2009 |
20090253677 | HIV Integrase Inhibitors - The disclosure generally relates to the novel compounds of formula I, including their salts, which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV. | 10-08-2009 |
20090264404 | Derivatives of 4-piperazin-1-yl-4-benzo[b]thiophene suitable for the treatment of cns disorders - A heterocyclic compound or a salt thereof represented by the formula (1): where R | 10-22-2009 |
20090264405 | Cetp Inhibitors - Compounds of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. | 10-22-2009 |
20090270359 | SUBSTITUTED PYRAZOLE DERIVATIVES - The present invention provides a novel pyrazole derivative and an androgen receptor antagonist containing the derivative. The present invention provides a compound represented by the formula (I′) | 10-29-2009 |
20090270360 | DICARBOXAMIDE DERIVATIVES - The invention is concerned with novel dicarboxamide derivatives of formula (I) | 10-29-2009 |
20090270361 | Substituted pyrazole derivatives and use thereof - The present invention aims to provide a novel pyrazole derivative and a pharmaceutical agent containing the same. The present invention provides a compound represented by the formula (I′) | 10-29-2009 |
20090275554 | AMINOCARBOXYLIC ACID DERIVATIVE AND MEDICINAL USE THEREOF - The present invention relates to a compound represented by the formula (I), a salt thereof, an N-oxide form thereof, a solvate thereof, or a prodrug thereof, and a medicament containing the same. The compound represented by the formula (I) has an ability to bind to an S1P receptor (particularly, EDG-1, EDG-6, and/or EDG-8) and is useful for preventing and/or treating for rejection to transplantation, graft-versus-host disease, autoimmune diseases, allergic diseases, neurodegenerating diseases, and the like. | 11-05-2009 |
20090275555 | Substituted indole ligands for the ORL-1 receptor - New ligands for the ORL-1 receptor are described, useful for antagonising the activity of said receptors in a patient in need thereof, and for preventing and treating illnesses dependent on the activation of this receptor. The new compounds conform to structural formula (I) wherein R1, R2, R3, R4 are further defined in the description. | 11-05-2009 |
20090275556 | Aryl sulfonamides useful as inhibitors of chemokine receptor activity - The present invention provides compounds of general formula I: | 11-05-2009 |
20090281074 | DRUG COMPOSITIONS AND METHODS FOR PREVENTING AND TREATING THROMBOSIS OR EMBOLISM - Drug compositions containing a substituted diamine compound represented by formula (1): | 11-12-2009 |
20090298808 | INHIBITORS OF 11-BETA HYDROXYL STEROID DEHYDROGENASE TYPE I AND METHODS OF USING THE SAME - The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-β hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess. | 12-03-2009 |
20090306041 | Inhibitors of Bruton's tyrosine kinase - This application discloses 5-phenyl-1H-pyridin-2-one and 6-phenyl-2H-pyridazin-3-one derivatives according to generic Formulae I-III: | 12-10-2009 |
20090306042 | Novel Compounds 010 - The present invention provides compounds of formula (I) | 12-10-2009 |
20090306043 | PYRROLIDINE ETHER DERIVATIVES AS NK3 RECEPTOR ANTAGONISTS - The present invention relates to compounds of formula I | 12-10-2009 |
20090312303 | Antidiabetic Bicyclic Compounds - Bicyclic compounds containing a phenyl or pyridyl ring fused to a cycloalkyl or heterocyclic ring, to which is attached a 5-membered heterocyclic ring, including pharmaceutically acceptable salts and prodrugs thereof, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia. | 12-17-2009 |
20090318407 | Inhibitors of protein kinases - The present invention is directed to compounds of formula I-II and pharmaceutically acceptable tautomers, salts, or stereoisomers thereof which are inhibitors of syk and/or JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk and/or JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk and/or JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma. | 12-24-2009 |
20090318408 | HALO-SUBSTITUTED PYRIMIDODIAZEPINES - The present invention provides PLK1 inhibitor compounds of formula I: | 12-24-2009 |
20090318409 | PYRROLIDINE INHIBITORS OF IAP - The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: | 12-24-2009 |
20090325924 | GPCR Agonists - Compounds of formula (I): or pharmaceutically acceptable salts thereof, are GPCR agonists and are useful as for the treatment of obesity and diabetes. | 12-31-2009 |
20100009960 | PYRIDONE/HYDROXYPYRIDINE 11-BETA HYDROXYSTEROID DEHYDROGENASE TYPE I INHIBITORS - Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure formula (I) enantiomers, diastereomers, solvates, salts, tautomers or prodrugs thereof wherein, A, W, X, Y and R | 01-14-2010 |
20100009961 | DIPEPTIDYL PEPTIDASE-IV INHIBITORS - The present invention relates generally to pyrrolidine and thiazolidine DPP-IV inhibitor compounds. The present invention also provides synthetic methods for preparation of such compounds, methods of inhibiting DPP-IV using such compounds and pharmaceutical formulations containing them for treatment of DPP-IV mediated diseases, in particular, Type-2 diabetes. | 01-14-2010 |
20100016278 | HETEROARYLCYCLOPROPANECARBOXAMIDES AND THEIR USE AS PHARMACEUTICALS - The present invention relates to heteroarylcyclopropanecarboxamides of the formula I, | 01-21-2010 |
20100022505 | BICYCLIC HETEROCYCLES, DRUGS CONTAINING SAID COMPOUNDS, USE THEREOF, AND METHOD FOR PRODUCTION THEREOF - The present invention relates to bicyclic heterocycles of general formula | 01-28-2010 |
20100022506 | ARYLPROPIONAMIDE, ARYLACRYLAMIDE, ARYLPROPYNAMIDE, OR ARYLMETHYLUREA ANALOGS AS FACTOR XIA INHIBITORS - The present invention provides compounds of Formula (I): | 01-28-2010 |
20100029610 | Heteroaryl Compounds and Uses Thereof - The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same. | 02-04-2010 |
20100048532 | Benzimidazole Derivatives as Selective Acid Pump Inhibitors - This invention relates to compounds of the formula (I): or a pharmaceutically acceptable salt thereof, wherein: R | 02-25-2010 |
20100063024 | Dihydropyrazolopyrimidinone Derivatives - The invention relates to compounds of a general formula (I): | 03-11-2010 |
20100069350 | New Pyridine Analogues III - The present invention relates to certain new pyridin analogues of Formula (I), to processes for preparing such compounds, to their utility as P2Y | 03-18-2010 |
20100075946 | NOVEL THIOPHENE DERIVATIVES - The invention relates to novel thiophene derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunosuppressive agents. | 03-25-2010 |
20100075947 | Methods of Using PI3K and MEK Modulators - The invention provides methods of treating cancer with a combination of compounds which inhibit kinases, more specifically MEK and PI3K. | 03-25-2010 |
20100075948 | Substituted Pyrrolidine-2-Carboxamides - There are provided compounds of the formula | 03-25-2010 |
20100075949 | NOVEL PYRROLIDIN-2-ONES - The present invention provides compounds of formula (I) or (Ia) which are ligands binding to the HDM2 protein, inducing apoptosis and inhibiting proliferation, and having therapeutic utility in cancer therapy and prevention. | 03-25-2010 |
20100087417 | AMINO-PYRIDINE DERIVATIVES AS S1P1 /EDG1 RECEPTOR AGONISTS - The invention relates to novel amino-pyridine derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents. | 04-08-2010 |
20100093692 | PIPERIDINYL-PIPERIDINE AND PIPERAZINYL-PIPERIDINE FOR USE IN THE TREATMENT OF DIABETES OR PAIN - The present invention relates to Compounds of Formula (I), compositions comprising the compounds, and methods of using the compounds to treat or prevent pain, diabetes, a diabetic complication, impaired glucose tolerance (IGT) or impaired fasting glucose (IFG) in a patient. | 04-15-2010 |
20100093693 | MODULATORS OF CELLULAR ADHESION - The present invention provides compounds having formula (I); | 04-15-2010 |
20100093694 | Compounds for the Treatment of Hepatitis C - The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV. | 04-15-2010 |
20100093695 | Substituted N-Arylsulfonylheterocyclic Amines As Gamma-Secretase Inhibitors - This invention discloses novel gamma secretase inhibitors of the formula: | 04-15-2010 |
20100099659 | Inhibitors of Bruton's Tyrosine Kinase - This application discloses 5-phenyl-1H-pyridin-2-one and 6-phenyl-2H-pyridazin-3-one derivatives according to generic Formulae I-III: | 04-22-2010 |
20100099660 | METHOD FOR TREATING THROMBOSIS OR EMBOLISM AND RELATED DISEASES - A method for treating cerebral infarction, cerebral embolism, myocardial infarction, angina pectoris, pulmonary infarction, pulmonary embolism, Buerger's disease, deep venous thrombosis, disseminated intravascular coagulation syndrome, thrombus formation after artificial valve or joint replacement, thrombus formation and reocclusion after angioplasty, multiple organ dysfunction syndrome (MODS), thrombus formation during extracorporeal circulation, or blood clotting upon blood drawing is provided. The method includes administration of an effective amount of a compound represented by formula (1): | 04-22-2010 |
20100105651 | ANTAGONISTS OF SNS SODIUM CHANNELS - Compounds of the formula (I), and pharmaceutically acceptable salts thereof, are found to be antagonists of SNS sodium channels. They are therefore useful as analgesic and neuroprotective agents, formula (I): R | 04-29-2010 |
20100113410 | PYRAZOLOPYRIMIDINE DERIVATIVE - Problem to be Solved To provide a novel compound inhibiting the effect of HSP90, in particular a novel compound inhibiting the function of HSP90 as a chaperone protein and having antitumor activity.
| 05-06-2010 |
20100113411 | Selected CGRP antagonists, processes for preparing them and their use as pharmaceutical compositions - The present invention relates to CGRP antagonists of general formula | 05-06-2010 |
20100113412 | IMIDAZO[1,2-a]PYRIDINES AND THEIR USE AS PHARMACEUTICALS - The present invention relates to derivatives of imidazo[1,2-a]pyridines of formula I, | 05-06-2010 |
20100113413 | MAPK/ERK Kinase Inhibitors - Compounds of the substituted 1,3-dialkyl-2,4-dioxo-6-(arylamino)-1,2,3,4-tetrahydropyrimidine-5-hydroxamic acids, show below: | 05-06-2010 |
20100113414 | THIAZOLYL-DIHYDRO-INDAZOLES - The present invention encompasses compounds of the general formula (1) | 05-06-2010 |
20100120739 | TRIAZOLOPYRIDAZINE PROTEIN KINASE MODULATORS - The present disclosure relates to triazolopyridazine protein kinase modulators of Formula (I), methods of using these compounds to treat diseases mediated by kinase activity. | 05-13-2010 |
20100120740 | PRODRUGS OF FUSED HETEROCYCLIC INHIBITORS OF D-AMINO ACID OXIDASE - The invention relates to prodrugs of fused heterocyclic inhibitors of D-amino oxidase (DAAO) and methods of treating diseases and conditions, wherein modulation of D-amino acid oxidase activity, D-serine levels, D-serine oxidative products and NMDA receptor activity in the nervous system of a mammalian subject is effective. | 05-13-2010 |
20100125061 | NAPHTHYLACETIC ACIDS - The invention is concerned with the compounds of formula I: | 05-20-2010 |
20100130467 | TRIAZOLOTRIAZINES AS KINASE INHIBITORS - The present invention is directed to [1,2,4]triazolo[4,3-b][1,2,4]triazines, and pharmaceutical compositions thereof, which are inhibitors of kinases such as c-Met and are useful in the treatment of cancer and other diseases related to the dysregulation of kinase pathways. | 05-27-2010 |
20100137276 | COMPOUNDS WHICH POTENTIATE AMPA RECEPTOR AND USES THEREOF IN MEDICINE - Compounds of formula (I), and salts and solvates thereof are provided: | 06-03-2010 |
20100137277 | PYRIDINE COMPOUNDS AND THEIR USE AS P2Y12 ANTAGONISTS - The present invention relates to certain new pyridin analogues of Formula (I) to processes for preparing such compounds, to their utility as P2Y | 06-03-2010 |
20100137278 | PYRAZINE COMPOUNDS AS PHOSPHODIESTERASE 10 INHIBITORS - Pyrazine compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like. | 06-03-2010 |
20100137279 | 4-METHYLPYRIDOPYRIMIDINONE COMPOUNDS - The present invention is directed to novel 4-methylpyridopyrimidinone compounds of Formula (I), | 06-03-2010 |
20100144701 | Modulators of CB1 Receptors - Compounds of formula (I) suppress the normal signalling activity CB1 receptors, and are thus useful in the treatment of diseases or conditions which are mediated by CB1 receptor signalling activity, such as treatment of obesity and overweight, prevention of weigh gain, treatment of diseases and conditions directly or indirectly associated with obesity and overweight: wherein A | 06-10-2010 |
20100160286 | HETEROARYLCARBAMOYLBENZENE DERIVATIVES FOR THE TREATMENT OF DIABETES - Compounds of formula (I) | 06-24-2010 |
20100160287 | COMPOUNDS USEFUL AS INHIBITORS OF JANUS KINASES - The present invention relates to compounds useful as inhibitors of protein kinases, particularly of JAK family kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. | 06-24-2010 |
20100160288 | Purine Compounds - A compound of the formula: | 06-24-2010 |
20100173888 | Nicotinamide Derivatives - The present invention relates to compounds of the formula (I) | 07-08-2010 |
20100173889 | Substituted Pyrimidine and Triazine Compounds - Substituted pyrimidine and triazine compounds corresponding to formula I | 07-08-2010 |
20100179120 | NOVEL AMIDE DERIVATIVE FOR INHIBITING THE GROWTH OF CANCER CELLS - The present invention provides a novel amide derivative and a pharmaceutically acceptable salt thereof which selectively and effectively inhibits the growth of cancer cells induced by the overexpression of an epidermal growth factor receptor and also prevents the development of drug resistance caused by the mutation of EGFR tyrosine kinase, and a pharmaceutical composition comprising same as an active ingredient. | 07-15-2010 |
20100179121 | 1,3-DIHYDROXY SUBSTITUTED PHENYLAMIDE GLUCOKINASE ACTIVATORS - Compounds are provided which are glucokinase activators and thus are useful in treating diabetes and related diseases and have the structure wherein in the ring represents one or two double bonds; R | 07-15-2010 |
20100184738 | Uses of cinnoline compounds to treat schizophrenia - This invention relates to the use of compounds having the structural formula I below: | 07-22-2010 |
20100190765 | DIHYDRODIAZEPINES USEFUL AS INHIBITORS OF PROTEIN KINASES - The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions. | 07-29-2010 |
20100190766 | ANTIBACTERIAL AGENTS - Antibacterial compounds of formula (I) are provided: | 07-29-2010 |
20100190767 | Compounds for the treatment of inflammatory diseases - Compounds of formula 1 and hetero derivatives thereof | 07-29-2010 |
20100197654 | TRIAZINE KINASE INHIBITORS - The invention provides compounds of formula I | 08-05-2010 |
20100197655 | SULFONAMIDE DERIVATIVES - The present invention relates to compounds of the formula | 08-05-2010 |
20100204198 | HYDROGENATED BENZO (C) THIOPHENE DERIVATIVES AS IMMUNOMODULATORS - The invention relates to novel thiophene derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunosuppressive agents. | 08-12-2010 |
20100204199 | CYCLIC 11-BETA HYDROXYSTEROID DEHYDROGENASE TYPE I INHIBITORS - Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-Beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure: | 08-12-2010 |
20100204200 | INHIBITORS OF CATHEPSIN S - The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S. More particularly, the present invention provides compounds having Formula 1: | 08-12-2010 |
20100210618 | PIPERIDINE/PIPERAZINE DERIVATIVES - The invention relates to a DGAT inhibitor of formula (I), including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents —O—C(═O)—; —C(═O)—C(═O)—; —NR | 08-19-2010 |
20100210619 | 6-Amino-Pyrimidine-4-Carboxamide Derivatives and Related Compounds Which Bind to the Sphingosine 1-Phosphate (S1P) Receptor for the Treatment of Multiple Sclerosis - The invention relates to compounds of formula (I): | 08-19-2010 |
20100210620 | Substituted Aryl Sulfone Derivatives as Calcium Channel Blockers - A series of substituted aryl sulfone derivatives represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, calcium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, diabetic neuropathy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, sleep disorder, bipolar disorder and stroke, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds. | 08-19-2010 |
20100210621 | CRYSTALLINE POLYMORPHIC FORM 631 - A new polymorphic form of 3-{[5-(azetidin-1-ylcarbonyl)pyrazin-2-yl]oxy}-5-{[(1S)-1-methyl-2-(methyloxy)ethyl]oxy}-N-(5-methylpyrazin-2-yl)benzamide, processes for making it and its use as an activator of glucokinase are described. | 08-19-2010 |
20100216763 | Heteroaryl Amide Derivatives - Heteroaryl amide derivatives are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies. | 08-26-2010 |
20100216764 | Soluble Guanylate Cyclase Activators - This inventions relates to compounds having the structure Formula I | 08-26-2010 |
20100216765 | KINASE INHIBITORS - Compounds, pharmaceutical compositions and kits are provided for use with kinases that comprise a compound selected from the group consisting of: | 08-26-2010 |
20100216766 | Inhibitors of VEGF Receptor and HGF Receptor Signalling - The invention relates to the inhibition of VEGF receptor signaling and HGF receptor signaling. The invention provides compounds and methods for inhibiting VEGF receptor signaling and HGF receptor signaling. The invention also provides compositions and methods for treating cell proliferative diseases and conditions | 08-26-2010 |
20100222320 | TRIAZOLE DERIVATIVES FOR TREATING ALZHEIMER'S DISEASE AND RELATED CONDITIONS - Compounds of formula I: Selectively attenuate production of Aβ(1-42) and hence find use in treatment or prevention of diseases associated with deposition of Aβ in the brain, in particular Alzheimer's disease. | 09-02-2010 |
20100227846 | SUBSTITUTED PYRAZOLE DERIVATIVE - The present invention provides a novel pyrazole derivative and an androgen receptor antagonist containing the derivative. The present invention provides a compound represented by the formula (I′) | 09-09-2010 |
20100227847 | Non-Anilinic Derivatives Of Isothiazol-3(2H)-one 1,1-Dioxides As Liver X Receptor Modulators - The present invention relates to certain novel compounds of the formula (I) to processes for preparing such compounds, to their the utility in modulation of nuclear hormone receptors Liver X Receptor (LXR) α (NR1H3) and/or β (NR1H2) and in treating and/or preventing clinical conditions including cardiovascular diseases such as atherosclerosis; inflammatory diseases, Alzheimer's disease, lipid disorders (dyslipidemias) whether or not associated with insulin resistance, type 2 diabetes and other manifestations of the metabolic syndrome, to methods for their therapeutic use and to pharmaceutical compositions containing them. | 09-09-2010 |
20100234344 | 8-OXY-QUINOLINE DERIVATIVES AS BRADYKININ B2 RECEPTOR MODULATORS - The present invention is related to compound of the formula (I): or a pharmacologically acceptable salt, solvate, or hydrate thereof, wherein A is a 6-membered heteroaryl having from 1 to 3 heteroatoms, each independently selected from N or O and the other substituents are defined as in the claims. | 09-16-2010 |
20100234345 | NOVEL COMPOUNDS AS CANNABINOID RECEPTOR LIGANDS - The present application relates to isothiazolylidene containing compounds of Formula (I) | 09-16-2010 |
20100234346 | NOVEL PYRIMIDINE DERIVATIVES - The invention relates to novel pyrimidine derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents. Formula (I) wherein A represents Formula (II), Formula (III), Formula (IV), Formula (V), Formula (VI), Formula (VII), Formula (VIII) or Formula (IX) | 09-16-2010 |
20100249091 | Amide Compounds Useful in Therapy - A compound of Formula (I), or a pharmaceutically acceptable salt or solvate thereof, | 09-30-2010 |
20100249092 | HETEROARYL COMPOUNDS AND USES THEREOF - The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same. | 09-30-2010 |
20100249093 | Substituted Heteroarylpiperidine Derivatives As Melanocortin-4 Receptor Modulators - The present invention relates to substituted heteroarylpiperidine derivatives as melanocortin-4 receptor modulators. Depending on the structure and the stereochemistry the compounds of the invention are either selective agonists or selective antagonists of the human melanocortin-4 receptor (MC-4R). The agonists can be used for the treatment of disorders and diseases such as obesity, diabetes and sexual dysfunction, whereas the antagonists are useful for the treatment of disorders and diseases such as cancer cachexia, muscle wasting, anorexia, amyotrophic lateral sclerosis (ALS), anxiety and depression. Generally all diseases and disorders where the regulation of the MC-4R is involved can be treated with the compounds of the invention. | 09-30-2010 |
20100249094 | Compounds for the Treatment of Hepatitis C - The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV. | 09-30-2010 |
20100249095 | Substituted Spiro-amide Compounds - Substituted spiro-amide compounds corresponding to formula I | 09-30-2010 |
20100249096 | Azetidines as MEK Inhibitors for the Treatment of Proliferative Diseases - Disclosed are compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof. Such compounds are MEK inhibitors and are useful in the treatment of proliferative diseases, such as cancer. Also disclosed are pharmaceutical compositions containing such compounds as well as methods of using the compounds and compositions of the invention in the treatment of cancer. | 09-30-2010 |
20100261701 | 8-Substituted isoquinoline derivative and the use thereof - The present invention relates to a compound represented by the following formula (1): | 10-14-2010 |
20100261702 | THIOPHENE DERIVATIVES AS AGONISTS OF S1P1/EDG1 - The invention relates to novel thiophene derivatives (1), their preparation and their use as pharmaceutically active compounds.Said compounds particularly act as immunomodulating agents. Formula (I). | 10-14-2010 |
20100267687 | PHENYLPYRAZOLE DERIVATIVES - The present invention provides a prophylactic or therapeutic agent for dementia, Alzheimer's disease, attention-deficit hyperactivity disorder, schizophrenia, eating disorders, obesity, diabetes, hyperlipidemia, sleep disorders, narcolepsy, sleep apnea syndrome, circadian rhythm disorder, depression, allergic rhinitis or other diseases. | 10-21-2010 |
20100286111 | COMBINATION THERAPY FOR THE TREATMENT OF DIABETES AND CONDITIONS RELATED THERETO AND FOR THE TREATMENT OF CONDITIONS AMELIORATED BY INCREASING A BLOOD GLP-1 LEVEL - The present invention concerns combination of an amount of a GPR119 agonist with an amount of a dipeptidyl peptidase IV (DPP-IV) inhibitor such that the combination provides an effect in lowering a blood glucose level or in increasing a blood GLP-1 level in a subject over that provided by the amount of the GPR119 agonist or the amount of the DPP-IV inhibitor alone and the use of such a combination for treating or preventing diabetes and conditions related thereto or conditions ameliorated by increasing a blood GLP-1 level. The present invention also relates to the use of a G protein-coupled receptor to screen for GLP-1 secretagogues. | 11-11-2010 |
20100286112 | COMPOUNDS FOR THE TREATMENT OF METABOLIC DISORDERS - The present invention is directed to therapeutic compounds which have dual activity as agonists of GPR119 and inhibitors of DPP-IV and are useful for the treatment of metabolic disorders including type II diabetes. | 11-11-2010 |
20100286113 | BICYCLIC HETEROCYCLIC COMPOUNDS AS PROTEIN TYROSINE KINASE INHIBITORS - The invention relates to new bicyclic heterocyclic derivative compounds of formula (I): wherein R | 11-11-2010 |
20100286114 | HEDGEHOG PATHWAY ANTAGONISTS AND THERAPEUTIC APPLICATIONS THEREOF - Heterocyclic compounds that modulate the hedgehog signaling pathway, pharmaceutical composition thereof and their therapeutic applications. | 11-11-2010 |
20100286115 | PYRAZOLES - The present invention is concerned with isoxazole-pyrazoles of formula I, having affinity and selectivity for GABA A a5 receptor, their manufacture, pharmaceutical compositions containing them and their use as therapeutics. The active compounds of the present invention are useful as cognitive enhancer or for the therapeutic and/or prophylactic treatment of cognitive disorders like Alzheimer's disease. | 11-11-2010 |
20100286116 | THIAZOLES - The present invention is concerned with isoxazole-thiazole derivatives of formula I, having affinity and selectivity for GABA A α5 receptor, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful as cognitive enhancer or for the therapeutic and/or prophylactic treatment of cognitive disorders like Alzheimer's disease. | 11-11-2010 |
20100286117 | PYRIDINES - The present invention is concerned with novel isoxazoles of formula I | 11-11-2010 |
20100292205 | Pyrimidone Compounds As GSK-3 Inhibitors - The invention pertains to pyrimidone compounds that serve as effective GSK-3 inhibitors. The invention further relates to pharmaceutical compositions and methods comprising such pyrimidone compounds; and the use of such compounds for treating certain disorders. | 11-18-2010 |
20100292206 | HETEROCYCLIC COMPOUND - The present invention relates to | 11-18-2010 |
20100298285 | Biclycloheteroaryl Compounds as P2x7 Modulators and Uses Thereof - Bicycloheteroaryl compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others. | 11-25-2010 |
20100298286 | Organic Compounds - The present invention relates to a compound of formula I | 11-25-2010 |
20100298287 | TRICYCLIC COMPOUNDS HAVING CORTICOTROPIN-RELEASING FACTOR ANTAGONISTIC ACTIVITY AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM - There is provided a compound of the formula (I′): wherein X is a nitrogen or CRx, Rx is a hydrogen, etc., R | 11-25-2010 |
20100305090 | META-SUBSTITUTED PHENYL SULFONYL AMIDES OF SECONDARY AMINO ACID AMIDES, THE PRODUCTION THEREOF, AND USE THEREOF AS MATRIPTASE INHIBITORS - The invention relates to meta-substituted phenyl sulfonyl amides of secondary amino acid amides according to the general formula (I), (II), or (III), the production thereof, and the use thereof as matriptase inhibitors, in particular the use thereof as drugs for inhibiting tumor growth and/or metastasization. | 12-02-2010 |
20100305091 | PYRAZOLO[1,5-a]PYRIMIDINE DERIVATIVES - Compounds of the following formula (I) are inhibitors of microtubule affinity regulating kinase, and hence find use in the treatment of neurodegenerative diseases associated with hyperphosphorylation of tau. | 12-02-2010 |
20100305092 | TRIAZOLE OXADIAZOLES DERIVATIVES - The invention relates to compounds of formula I: | 12-02-2010 |
20100317645 | SUBSTITUTED DIAZEPINE SULFONAMIDES AS BOMBESIN RECEPTOR SUBTYPE-1 MODULATORS - Certain novel substituted diazepine sulfonamides are ligands of the human bombesin receptor and, in particular, are selective ligands of the human bombesin receptor subtype-3 (BRS-3). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of BRS-3, such as obesity, and diabetes. | 12-16-2010 |
20100317646 | COMPOUNDS - A compound of formula I, or a pharmaceutically acceptable salt or ester thereof, | 12-16-2010 |
20100317647 | NOVEL CYCLOPENTANE DERIVATIVES - The invention relates to a compound of formula (I) | 12-16-2010 |
20100317648 | THERAPEUTIC COMPOUNDS - The invention provides a compound of formula I: | 12-16-2010 |
20100317649 | S1P Receptor Modulating Compounds and Use Thereof - The present invention relates to compounds that have activity as S1P receptor modulating agents and the use of such compounds to treat diseases associated with inappropriate S1P receptor activity. In certain embodiments, the compounds of the invention relate to aryl oxoimidazolidinyls. | 12-16-2010 |
20100324010 | AMIDE COMPOUNDS AND USE OF THE SAME - A renin inhibitor comprising a compound represented by the formula: | 12-23-2010 |
20100324011 | AZETIDINYL DIAMIDES AS MONOACYLGLYCEROL LIPASE INHIBITORS - Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: | 12-23-2010 |
20100324012 | AZETIDINYL DIAMIDES AS MONOACYLGLYCEROL LIPASE INHIBITORS - Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: | 12-23-2010 |
20100324013 | AZETIDINYL DIAMIDES AS MONOACYLGLYCEROL LIPASE INHIBITORS - Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: | 12-23-2010 |
20100324014 | AZETIDINYL DIAMIDES AS MONOACYLGLYCEROL LIPASE INHIBITORS - Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: | 12-23-2010 |
20100324015 | HETEROAROMATIC AND AROMATIC PIPERAZINYL AZETIDINYL AMIDES AS MONOACYLGLYCEROL LIPASE INHIBITORS - Disclosed are compounds, compositions and methods for treating diseases, syndromes, conditions and disorders that are affected by the inhibition of MGL, including pain. Such compounds are represented by Formula (I) as follows: | 12-23-2010 |
20100324016 | HETEROAROMATIC AND AROMATIC PIPERAZINYL AZETIDINYL AMIDES AS MONOACYLGLYCEROL LIPASE INHIBITORS - Disclosed are compounds, compositions and methods for treating diseases, syndromes, conditions and disorders that are affected by the inhibition of MGL, including pain. Such compounds are represented by Formula (I) as follows: | 12-23-2010 |
20100331295 | MODULATORS OF LXR - Compounds of the invention, such as compounds of Formulae Ia, Ib, Ic, or Id and pharmaceutically acceptable salts, isomers, and prodrugs thereof, which are useful as modulators of the activity of liver X receptors, where R1, R2, R21, R3, and G are defined herein. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed. | 12-30-2010 |
20100331296 | BICYCLIC HETEROCYCLIC COMPOUNDS AS PROTEIN TYROSINE KINASE INHIBITORS - The invention relates to new bicyclic heterocyclic derivative compounds of formula (I): wherein R | 12-30-2010 |
20100331297 | MODULATION OF PROTEIN TRAFFICKING - Compounds and compositions are provided for treatment or amelioration of one or more disorders characterized by defects in protein trafficking. A method of treating a disorder characterized by impaired protein trafficking includes administering to a subject or contacting a cell with a compound of Formula I: [formula here] or pharmaceutically acceptable salts or derivatives thereof. | 12-30-2010 |
20100331298 | Carboxamide Compounds and Their Use - Chemokine receptor antagonists, in particular, compounds of Formula (I) that act as antagonists of the chemokine CCR2 receptor, including pharmaceutical compositions and uses thereof to treat or prevent diseases associated with monocyte accumulation, lymphocyte accumulation or leukocyte accumulation are described herein. | 12-30-2010 |
20100331299 | AZETIDINYL DIAMIDES AS MONOACYLGLYCEROL LIPASE INHIBITORS - Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: | 12-30-2010 |
20100331300 | AZETIDINYL DIAMIDES AS MONOACYLGLYCEROL LIPASE INHIBITORS - Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: | 12-30-2010 |
20100331301 | AZETIDINE COMPOUND AND PHARMACEUTICAL USE THEREOF - Compounds of formula [I]: | 12-30-2010 |
20100331302 | N-(2-(HETARYL)ARYL) ARYLSULFONAMIDES AND N-(2-(HETARYL)HETARYL ARYLSULFONAMIDES - Compounds are provided that act as potent antagonists of the CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists. | 12-30-2010 |
20100331303 | PROLYL HYDROXYLASE INHIBITORS AND METHODS OF USE - The present disclosure relates to HIF-1α prolyl hydroxylase inhibitors, compositions which comprise the HIF-1α prolyl hydroxylase inhibitors described herein and to methods for controlling, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia. | 12-30-2010 |
20110003785 | Fused Thiazole Derivatives As Kinase Inhibitors - A series of 6,7-dihydro[1,3]thiazolo[5,4-c]pyridin-4(5H)-one derivatives, which are substituted in the 2-position by a substituted morpholin-4-yl moiety, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions. | 01-06-2011 |
20110003786 | 2-Carboxamide Cycloamino Ureas - The present invention relates to compounds of formula I | 01-06-2011 |
20110003787 | NOVEL PHENYLPYRROLE DERIVATIVE - The present invention relates to a compound or a pharmacologically acceptable salt thereof having superior glucokinase activating activity, and is a compound represented by general formula (I), or pharmacologically acceptable salt thereof: | 01-06-2011 |
20110003788 | FUSED HETEROCYCLIC DERIVATIVE AND USE THEREOF - The present invention provides a compound having a superior Smo inhibitory activity and lower toxicity, which is sufficiently satisfactory as a pharmaceutical product. The present invention provides a compound represented by the formula (I) wherein ring A is 5- to 7-membered ring optionally having substituent(s), where substituents are optionally bonded to each other to form a ring; X is O, S or NR | 01-06-2011 |
20110009378 | Heterocyclic compounds, pharmaceutical compositions containing them, and their use in therapy - The present invention relates to heterocyclic compounds of the formula (I) | 01-13-2011 |
20110009379 | INDOLINONE COMPOUND - [Problems] A compound, which is useful as an active ingredient for a pharmaceutical composition, for example a pharmaceutical composition for treating constipation-type irritable bowel syndrome, atonic constipation and/or functional gastrointestinal disorder, is provided. | 01-13-2011 |
20110015170 | AZETIDINYL DIAMIDES AS MONOACYLGLYCEROL LIPASE INHIBITORS - Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: | 01-20-2011 |
20110015171 | AZETIDINYL DIAMIDES AS MONOACYLGLYCEROL LIPASE INHIBITORS - Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: | 01-20-2011 |
20110015172 | PYRROLOPYRAZINE INHIBITORS OF KINASES - The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, | 01-20-2011 |
20110015173 | PYRROLOPYRIDINE INHIBITORS OF KINASES - The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, | 01-20-2011 |
20110021489 | SUBSTITUTED PIPERIDINES - The invention relates to novel substituted piperidines, to processes for preparation thereof, to the use thereof for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially of cardiovascular disorders and tumour disorders. | 01-27-2011 |
20110021490 | Chromene compounds, a process for their preparationand pharmaceutical compositions containing them - The invention relates to compounds of formula (I): | 01-27-2011 |
20110021491 | COMPOUNDS, PHARMACEUTICAL COMPOSITION AND METHODS RELATING THERETO - New compounds are disclosed which have utility in the treatment of a variety of metabolic related conditions in a patient. The compounds of this invention have the structure (I): | 01-27-2011 |
20110021492 | PYRIDAZINE DERIVATIVES AS FACTOR XIA INHIBITORS - The present invention provides compounds of Formula (I): | 01-27-2011 |
20110028445 | Urea derivatives of benzomorphanes and related scaffolds, medicaments containing such compounds and their use - The present invention relates to compounds defined by formula (I) wherein the groups A, B, X, m, n and o are defined as in claim | 02-03-2011 |
20110028446 | ARYLPROPIONAMIDE, ARYLACRYLAMIDE, ARYLPROPYNAMIDE, OR ARYLMETHYLUREA ANALOGS AS FACTOR XIA INHIBITORS - The present invention provides compounds of Formula (I): | 02-03-2011 |
20110028447 | INDAZOLE DERIVATIVES - This invention relates to compounds, pharmaceutical compositions and methods for the treatment of a condition mediated by CB1 receptor activity in a mammalian subject including a human, which comprises administering to a mammal in need of such treatment a therapeutically effective amount of the compound of formula (I) wherein R | 02-03-2011 |
20110028448 | PYRIDINE COMPOUNDS - The invention relates to pyridine compounds, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents. | 02-03-2011 |
20110028449 | NOVEL AMINOMETHYL BENZENE DERIVATIVES - The invention relates to novel aminomethyl benzene derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents. | 02-03-2011 |
20110034432 | BENZAMIDE DERIVATIVES AND THEIR USE AS GLUCOKINASE ACTIVATING AGENTS - Compounds of Formula (I): | 02-10-2011 |
20110034433 | 4-(4-CYANO-2-THIOARYL)DIHYDROPYRIMIDINONES AND THEIR USE - The present invention relates to novel 4-(4-cyano-2-thioaryl)dihydropyrimidin-2-one derivatives, to processes for their preparation, to their use alone or in combination for the treatment and/or prevention of diseases and also to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of disorders of the lung and the cardiovascular system. | 02-10-2011 |
20110034434 | PRODRUGS OF FUSED HETEROCYCLIC INHIBITORS OF D-AMINO ACID OXIDASE - The invention relates to prodrugs of fused heterocyclic inhibitors of D-amino oxidase (DAAO) and methods of treating diseases and conditions, wherein modulation of D-amino acid oxidase activity, D-serine levels, D-serine oxidative products and NMDA receptor activity in the nervous system of a mammalian subject is effective. | 02-10-2011 |
20110034435 | PYRIMIDINE, PYRIDINE AND TRIAZINE DERIVATIVES AS MAXI-K CHANNEL OPENERS - A compound of formula (A); wherein ring A is an aromatic ring or a heteroaromatic ring; R | 02-10-2011 |
20110039820 | LACTAM COMPOUNDS USEFUL AS PROTEIN KINASE INHIBITORS - The present invention provides novel compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases. | 02-17-2011 |
20110039821 | Fused Phenyl Amido Heterocyclic Compounds - The present invention relates to a compound of formula (I): | 02-17-2011 |
20110039822 | HETEROCYCLIC JANUS KINASE 3 INHIBITORS - The present invention provides a compound having an excellent JAK3 inhibition activity and being useful as an active ingredient of an agent for treating and/or preventing various immune diseases including autoimmune diseases, inflammatory diseases, and allergic diseases. | 02-17-2011 |
20110046108 | PYRIMIDINE DERIVATIVES - The invention concerns benzamide compounds of Formula (I), or a pharmaceutically acceptable salt thereof, where R | 02-24-2011 |
20110046109 | 2,4,8-TRISUBSTITUTED-8H-PYRIDO[2,3-D]PYRIMIDIN-7-ONE COMPOUNDS AND COMPOSITIONS FOR USE IN THERAPY - Novel substituted 2,4,8-trisubstituted-8H-pyrido[2,3-d]pyrimidin-7-one compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors. | 02-24-2011 |
20110053904 | CARBOCYCLIC GLYT1 RECEPTOR ANTAGONISTS - The present invention relates to the use of a compound of formula I | 03-03-2011 |
20110053905 | COMPOUNDS AS TYROSINE KINASE MODULATORS - The present invention is directed to novel compounds of Formula I. The compounds of the present invention are potent tyrosine kinase modulators, and are suitable for the treatment and prevention of diseases and conditions related to abnormal activities of tyrosine kinase receptors. | 03-03-2011 |
20110053906 | PROTEIN KINASE INHIBITORS AND USE THEREOF - Disclosed are benzonaphthyridinyl derivative compounds and analogs thereof, pharmaceutical compositions comprising such compounds and processes for preparing the same. The compounds are useful in the treatment of diseases amenable to kinase signal transduction inhibition, regulation or modulation. | 03-03-2011 |
20110053907 | SUBSTITUTED PYRIMIDINES AND TRIAZINES AND THEIR USE IN CANCER THERAPY - Provided herein are substituted pyrimidine and triazine derivatives, including bicyclic pyrimidine derivatives, their pharmaceutical compositions, their preparation, and their use as agents or drugs for cancer therapy, either alone or in combination with radiation and/or other anticancer drugs. In one embodiment, the pyrimidine and triazine derivatives are morpholino-pyrimidine, morpholino-triazine, pyridyl-pyrimidine, and pyridyl-triazine derivatives which are selective irreversible inhibitors of the p110α isoform of PI3K. | 03-03-2011 |
20110059941 | 2-PHENYL SUBSTITUTED IMIDAZOL [4,5B] PYRIDINE/PYRAZINE AND PURINE DERIVATIVES AS GLUCOKINASE MODULATORS - Compounds of Formula (I), wherein R | 03-10-2011 |
20110059942 | Azetidinyl G-Protein Coupled Receptor Agonists - Compounds of formula (I): or pharmaceutically acceptable salts thereof, are agonists of GPR119 and are useful for the treatment of diabetes and as peripheral regulators of satiety, e.g. for the treatment of obesity and metabolic syndrome. | 03-10-2011 |
20110059943 | JAK2 INHIBITORS AND THEIR USE FOR THE TREATMENT OF MYELOPROLIFERATIVE DISEASES AND CANCER - The present invention provides compounds of formula I | 03-10-2011 |
20110059944 | Certain Substituted Amides, Method of Making, and Method of Use Thereof - Compounds of Formula I that inhibit Btk are described herein. Pharmaceutical compositions comprising at least one compound of Formula I, together with at least one pharmaceutically acceptable vehicle chosen from carriers, adjuvants, and excipients, are described. Methods of treating patients suffering from certain diseases responsive to inhibition of Btk activity and/or B-cell activity are described. Methods for determining the presence of Btk in a sample are described. | 03-10-2011 |
20110059945 | S1P Receptor Modulating Compounds and Use Thereof - The present invention relates to compounds of the general formula (I) that have activity as S1P receptor modulating agents and the use of such compounds to treat diseases associated with inappropriate S1P receptor activity. The compounds may be used as immunomodulators, e.g., for treating or preventing diseases such as autoimmune and related immune disorders including systemic lupus erythematosus, inflammatory bowel diseases such as Crohn's disease and ulcerative colitis, type I diabetes, uveitis, psoriasis, myasthenia gravis, rheumatoid arthritis, non-glomerular nephrosis, hepatitis, Behçet's disease, glomerulonephritis, chronic thrombocytopenic purpura, hemolytic anemia, hepatitis and Wegner's granuloma; and for treating other conditions. | 03-10-2011 |
20110065681 | AMIDE COMPOUNDS, COMPOSITIONS AND USES THEREOF - Compounds are provided according to formula 1: | 03-17-2011 |
20110077233 | C-Met Modulators and Method of Use - The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds. | 03-31-2011 |
20110077234 | Urea Glucokinase Activators - The invention provides a compound of general formula (I) | 03-31-2011 |
20110086835 | Pyrrolo[2,3-b]pyridin-4-yl-amines and pyrrolo[2,3-b]pyrimidin-5-yl-amines as janus kinase inhibitors - The present invention provides pyrrolo[2,3-b]pyridine-4-yl amines pyrrolo[2,3-b]pyrimidin-4-yl amines that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases and cancer. | 04-14-2011 |
20110086836 | Substituted Phenylpiperidine Derivatives As Melanocortin-4 Receptor Modulators - The present invention relates to substituted phenylpiperidine derivatives as melanocortin-4 receptor modulators. Depending on the structure and the stereochemistry the compounds of the invention are either selective agonists or selective antagonists of the human melanocortin-4 receptor (MC-4R). The agonists can be used for the treatment of disorders and diseases such as obesity, diabetes and sexual dysfunction, whereas the antagonists are useful for the treatment of disorders and diseases such as cancer cachexia, muscle wasting, anorexia, anxiety and depression. Generally all diseases and disorders where the regulation of the MC-4R is involved can be treated with the compounds of the invention. | 04-14-2011 |
20110086837 | COMBINATIONS OF A PI3K INHIBITOR AND A MEK INHIBITOR - The invention relates methods of treating a patient with locally advanced or metastatic solid tumors with a combination of an inhibitor of phosphatidylinositol 3-kinase (PI 3-kinase or PI3K) and an inhibitor of mitogen activated protein kinase (MEK) described herein. | 04-14-2011 |
20110086838 | NOVEL COMPOUNDS AS CANNABINOID RECEPTOR LIGANDS - The present invention relates to thiophene containing compounds of formula (I) | 04-14-2011 |
20110086839 | COMPOUNDS - The present invention relates to novel oxadiazole derivatives having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders. | 04-14-2011 |
20110092476 | Bicycloheteroaryl compounds as P2X7 modulators and uses thereof - Bicycloheteroaryl compounds are disclosed that have a formula represented by the following: | 04-21-2011 |
20110092477 | SUBSTITUTED IMIDAZOQUINOLINES, IMIDAZOPYRIDINES, AND IMIDAZONAPHTHYRIDINES - Imidazo-quinoline, -pyridine, and -naphthyridine ring systems (particularly quinolines, tetrahydroquinolines, pyridines, [1,5]naphthyridines, [1,5]tetrahydronaphthyridines) substituted at the 1-position with a cyclic substituent, pharmaceutical compositions containing the compounds, methods of making these compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed. | 04-21-2011 |
20110098271 | CHROMENONE DERIVATIVES - The invention concerns chromenone derivatives of Formula I | 04-28-2011 |
20110098272 | Novel Compounds As Casein Kinase Inhibitors - Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I | 04-28-2011 |
20110105459 | AZETIDINES AND CYCLOBUTANES AS HISTAMINE H3 RECEPTOR ANTAGONISTS - The invention relates to compounds of formula (I) wherein R, R | 05-05-2011 |
20110105460 | TRIAZOLE DERIVATIVE OR SALT THEREOF - [Problem] A compound, which can be used for preventing or treating diseases, in which 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) is concerned, in particular, diabetes, insulin resistance, dementia, schizophrenia and depression, is provided. | 05-05-2011 |
20110124621 | BENZOTHIAZOLES AS GHRELIN RECEPTOR MODULATORS - A compound of formula I | 05-26-2011 |
20110124622 | ISOINDOLONES DERIVATIVES AS MEK KINASE INHIBITORS AND METHODS OF USE - The invention relates to isoindolones of formula, (I) with anti-cancer and/or anti-inflammatory activity and more specifically with MEK kinase inhibitory activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth, treating a hyperproliferative disorder, or treating an inflammatory disease in a mammal. The invention also relates to methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions. | 05-26-2011 |
20110124623 | PYRROLOTRIAZINE KINASE INHIBITORS - The invention provides compounds of formula I | 05-26-2011 |
20110124624 | 5-PHENYL-4-METHYL-THIAZOL-2-YL-AMINE DERIVATIVES AS INHIBITORS OF PHOSPHATIDYLINOSITOL 3 KINASE ENZYMES (PI3) FOR THE TREATMENT OF INFLAMMATORY DISEASES - Compounds of Formula I: | 05-26-2011 |
20110124625 | Modulators of Cellular Adhesion - The present invention provides compounds having formula (I): | 05-26-2011 |
20110124626 | BENZAZEPINE DERIVATIVES AND THEIR USE AS HISTAMINE H3 ANTAGONISTS - A compound having the formula (1) wherein: R1 is a group selected from C | 05-26-2011 |
20110130380 | Heteroaryl Kinase Inhibitors - The present invention provides compounds of Formula (I): | 06-02-2011 |
20110130381 | SMALL MOLECULE INHIBITORS OF PLASMODIUM FALCIPARUM DIHYDROOROTATE DEHYDROGENASE - Inhibitors of dihydroorotate dehydrogenase (DHODH) for the | 06-02-2011 |
20110136780 | DIHYDROPYRROLONAPHTYRIDINONE COMPOUNDS AS INHIBITORS OF JAK - Disclosed are JAK inhibitors of formula I | 06-09-2011 |
20110136781 | IMIDAZOTRIAZINES AND IMIDAZOPYRIMIDINES AS KINASE INHIBITORS - The present invention is directed to imidazo[1,2-b][1,2,4]triazines and imidazo[1,2-a]pyrimidines, and pharmaceutical compositions thereof, which are inhibitors of kinases such as c-Met and are useful in the treatment of cancer and other diseases related to the dysregulation of kinase pathways. | 06-09-2011 |
20110152240 | PYRAZOLOPYRIMIDINES AND RELATED HETEROCYCLES AS CK2 INHIBITORS - The invention provides compounds that inhibit protein kinase CK2 activity (CK2 activity), and compositions containing such compounds. These compounds and compositions are useful for treating proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation, pain, and certain immunological disorders, and have the following general formula: | 06-23-2011 |
20110152241 | NOVEL COMPOUNDS AS RECEPTOR MODULATORS WITH THERAPEUTIC UTILITY - The present invention relates to novel cyclic amine and cycloalkyl derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors. | 06-23-2011 |
20110160180 | Cannabinoid Receptor Ligands - Compounds of Formulae (I), or pharmaceutically acceptable salts thereof: wherein R | 06-30-2011 |
20110160181 | SUBSTITUTED PYRAZOLINE COMPOUNDS, THEIR PREPARATION AND USE AS MEDICAMENTS - The present invention relates to substituted pyrazoline compounds, methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animals. | 06-30-2011 |
20110160182 | PYRAZINE COMPOUNDS AS PHOSPHODIESTERASE 10 INHIBITORS - Pyrazine compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like. | 06-30-2011 |
20110166120 | SULFONYL AMIDE DERIVATIVES FOR THE TREATMENT OF ABNORMAL CELL GROWTH - The present invention relates to a compound of the formula I | 07-07-2011 |
20110166121 | FUSED HETEROCYCLIC COMPOUND - The present invention relates to a fused heterocyclic compound having the Formula 1, which is useful as a platelet aggregation inhibitor, a method for preparing the same, and a pharmaceutical composition for inhibiting platelet aggregation comprising the same. | 07-07-2011 |
20110166122 | SUBSTITUTED IMIDAZO[1,2b]PYRIDAZINE COMPOUNDS AS TRK KINASE INHIBITORS - Compounds of Formula (I): in which R | 07-07-2011 |
20110172202 | SELECTIVE SPHINGOSINE 1 PHOSPHATE RECEPTOR MODULATORS AND METHODS OF CHIRAL SYNTHESIS - Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds is provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated. | 07-14-2011 |
20110178056 | SPHINGOSINE 1 PHOSPHATE RECEPTOR MODULATORS AND METHODS OF CHIRAL SYNTHESIS - Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds is provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated. | 07-21-2011 |
20110178057 | HETEROCYCLIC COMPOUND AND USE THEREOF - Compounds represented by the formulas (I) (II) wherein each symbol is as defined in the specification, and a pro-drug thereof have a superior renin inhibitory activity, and are useful as agents for the prophylaxis or treatment of hypertension, various organ damages attributable to hypertension and the like. | 07-21-2011 |
20110178058 | INHIBITORS OF FLAVIVIRIDAE VIRUSES - Provided are compounds of Formula I: | 07-21-2011 |
20110178059 | 1,3-OXAZOLIDIN -2-ONE DERIVATIVES USEFUL AS CETP INHIBITORS - Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. The compounds have 3 cyclic groups connected by single bonds, as for example triphenyl, which are attached directly to the ring of formula I or attached at the position B. | 07-21-2011 |
20110178060 | NITROGEN-CONTAINING HETEROCYCLIC COMPOUND AND USE OF SAME - The present invention relates to a compound represented by the formula | 07-21-2011 |
20110183959 | P38 KINASE INHIBITING AGENTS - Compounds described by the chemical formula (I) or pharmaceutically acceptable salts thereof: | 07-28-2011 |
20110183960 | THIOPHENE-2-CARBOXAMIDE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF - The subject matter of the invention is compounds corresponding to formula (I), in which: R | 07-28-2011 |
20110190257 | BICYCLIC HETEROCYCLES AS MEK KINASE INHIBITORS - The invention relates to bicyclic heterocycles of formulae I and II with anti-cancer and/or anti-inflammatory activity and more specifically with MEK kinase inhibitory activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth, treating a hyperproliferative disorder, or treating an inflammatory disease in a mammal. The invention also relates to methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions. | 08-04-2011 |
20110190258 | ARYL BENZYLAMINE COMPOUNDS - The present invention relates to substituted aryl-benzylamine compounds, to processes for their production, to their use as pharmaceuticals and to pharmaceutical compositions comprising them. | 08-04-2011 |
20110190259 | COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS - The invention provides novel pyrimidine and pyridine derivatives and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine and pyridine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of anaplastic lymphoma kinase (ALK) activity, focal adhesion kinase (FAK), zeta-chain-associated protein kinase 70 (ZAP-70), insulin-like growth factor (IGF-1R), or a combination thereof. | 08-04-2011 |
20110190260 | NOVEL COMPOUNDS USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES - [1,2,4]Triazolo[1,5-a]pyridine compounds are disclosed that have a formula represented by the formula (I). The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, diseases involving cartilage degradation, bone and/or joint degradation, for example osteoarthritis; and/or conditions involving inflammation or immune responses, such as Crohn's disease, rheumatoid arthritis, psoriasis, allergic airways disease (e.g. asthma, rhinitis), juvenile idiopathic arthritis, colitis, inflammatory bowel diseases, endotoxin-driven disease states (e.g. complications after bypass surgery or chronic endotoxin states contributing to e.g. chronic cardiac failure), diseases involving impairment of cartilage turnover (e.g diseases involving the anabolic stimulation of chondrocytes), congenital cartilage malformations, diseases associated with hypersecretion of IL6, transplantation rejection (e.g. organ transplant rejection) and proliferative diseases. | 08-04-2011 |
20110190261 | MAPK/ERK Kinase Inhibitors - Compounds of the substituted 1,3-dialkyl-2,4-dioxo-6-(pyrimidinylamino)-1,2,3,4-tetrahydropyrimidine-5-hydroxamic acids, show below: | 08-04-2011 |
20110195948 | Substituted Pyrazolo[1,5-a]Pyrimidine Compounds as TRK Kinase Inhibitors - Compounds of Formula (I) in which R | 08-11-2011 |
20110201592 | Therapeutic Oxy-Phenyl-Aryl Compounds and Their Use - The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain oxy phenyl aryl compounds (referred to herein as OPA compounds), as described herein, which, inter alia, inhibit Checkpoint Kinase 2 (CHK2) kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit CHK2 kinase function, and in the treatment of diseases and conditions that are mediated by CHK2, that are ameliorated by the inhibition of CHK2 kinase function, etc., including proliferative conditions such as cancer, etc., optionally in combination with another agent, for example, (a) a DNA topoisomerase I or II inhibitor; (b) a DNA damaging agent; (c) an antimetabolite or TS inhibitor; (d) a microtubule targeted agent; and (e) ionising radiation. | 08-18-2011 |
20110201593 | TRICYCLIC HETEROCYCLIC COMPOUNDS, COMPOSITIONS AND METHODS OF USE THEREOF - The invention provides novel compounds of formula I having the general formula: | 08-18-2011 |
20110207712 | Phosphatidylinositol 3-Kinase Inhibitors And Methods Of Their Use - The present invention comprises small molecule inhibitors of phosphatidylinositol 3-kinase (PI3K), which is associated with a number of malignancies such as ovarian cancer, cervical cancer, breast cancer, colon cancer, rectal cancer, and glioblastomas, among others. Accordingly, the compounds of the present invention are useful for treating, preventing, and/or inhibiting these diseases. | 08-25-2011 |
20110212938 | BICYCLIC HETEROCYCLE DERIVATIVES AND THEIR USE AS MODULATORS OF THE ACTIVITY OF GPR119 - The present invention relates to Bicyclic Heterocycle Derivatives, compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of GPR119 in a patient. | 09-01-2011 |
20110212939 | Heterocyclic GPCR Agonists - Compounds of formula (I) or pharmaceutically acceptable salts thereof, are GPCR (GPR119) agonists and are useful as for the treatment of diabetes and obesity. | 09-01-2011 |
20110212940 | S1P Receptor Modulating Compounds and Use Thereof - The present invention relates to compounds of the general formula (I) that have activity as S1P receptor modulating agents and the use of such compounds to treat diseases associated with inappropriate S1P receptor activity. The compounds may be used as immunomodulators, e.g., for treating or preventing diseases such as autoimmune and related immune disorders including systemic lupus erythematosus, inflammatory bowel diseases such as Crohn's disease and ulcerative colitis, type I diabetes, uveitis, psoriasis, myasthenia gravis, rheumatoid arthritis, non-glomerular nephrosis, hepatitis, Behçet's disease, glomerulonephritis, chronic thrombocytopenic purpura, hemolytic anemia, hepatitis and Wegner's granuloma; and for treating other conditions. | 09-01-2011 |
20110212941 | Imidazoisoindole Neuropeptide S Receptor Antagonists - The present invention is directed to imidazoisoindole compounds which are antagonists of neuropeptide S receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which the neuropeptide S receptor is involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the neuropeptide S receptor is involved. | 09-01-2011 |
20110218182 | CHEMICAL COMPOUNDS 251 - The invention relates to chemical compounds of formula (I), and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of PIM-1 and/or PIM-2, and/or PIM-3 protein kinase activity or enzyme function. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein, and their use in the prevention and treatment of PIM kinase related conditions and diseases, preferably cancer. | 09-08-2011 |
20110218183 | Fused Bicyclic mTOR Inhibitors - Compounds represented by Formula (I) | 09-08-2011 |
20110224188 | DERIVATIVES OF 6,7-DIHYDRO-5H-IMIDAZO[1,2-alpha]IMIDAZOLE-3-CARBOXYLIC ACID AMIDES - Derivatives of 6,7-dihydro-5H-imidazo[1,2-α]imidazole-3-carboxylic acid amide exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease. | 09-15-2011 |
20110224189 | SUBSTITUTED CYCLIC HYDROXAMATES AS INHIBITORS OF MATRIX METALLOPROTEINASES - The present invention provides compounds of the formula: | 09-15-2011 |
20110230462 | Pyrrolopyrazine Kinase Inhibitors - The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, | 09-22-2011 |
20110230463 | 2H-CHROMENE COMPOUND AND DERIVATIVE THEREOF - [Object] Provided is a compound which has an excellent S1P | 09-22-2011 |
20110237564 | IMIDAZOPYRIMIDINE DERIVATIVES - The invention is concerned with novel imidazopyrimidine derivatives of formula (I) | 09-29-2011 |
20110245223 | HETEROCYCLIC COMPOUNDS - The present invention provides a compound represented by the following formula [1′] or a salt thereof: | 10-06-2011 |
20110245224 | FUSED, SPIROCYCLIC HETEROAROMATIC COMPOUNDS FOR THE TREATMENT OF BACTERIAL INFECTIONS - The present invention relates to compounds of Formula (I); to pharmaceutically acceptable salts thereof, to methods of using them to treat bacterial infections, and to methods for their preparation. | 10-06-2011 |
20110245225 | QUINAZOLINAMIDE DERIVATIVES - Novel quinazolinamide derivatives of the formula (I), in which R | 10-06-2011 |
20110245226 | PIPERIDINYL DERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY - The present application describes substituted piperidinyl modulators of MIP-1α or CCR-1 or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and transplant rejection using said modulators are disclosed. | 10-06-2011 |
20110245227 | PYRIDONE GPR119 G PROTEIN-COUPLED RECEPTOR AGONISTS - Novel compounds are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. These novel compounds have the structure Formula I or Formula IA. | 10-06-2011 |
20110251172 | PURINE DERIVATIVES FOR TREATMENT OF ALZHEIMER'S DISEASE - The invention encompasses purine derivatives as gamma secretase modulators, useful for treating diseases associated with the deposition of beta-amyloid peptide in the brain, such as Alzheimer's disease, or of preventing or delaying the onset of dementia associated with such diseases. Pharmaceutical compositions and methods of use are included. | 10-13-2011 |
20110251173 | CHEMICAL COMPOUNDS - DGAT-1 inhibitor compounds of formula (I), pharmaceutically-acceptable salts and pro-drugs thereof are described, together with pharmaceutical compositions, processes for making them and their use in treating, for example, diabetes and obesity | 10-13-2011 |
20110251174 | 2,4-DIAMINO-PYRIMIDINES AS AURORA INHIBITORS - The present invention encompasses compounds of general formula (1) | 10-13-2011 |
20110257151 | NOVEL 3,3-DIMETHYL TETRAHYDROQUINOLINE DERIVATIVES - A compound of formula (I) | 10-20-2011 |
20110257152 | PYRROLOPYRIDINE INHIBITORS OF KINASES - The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, | 10-20-2011 |
20110257153 | Aryl-substituted bridged or fused diamines as modulators of leukotriene A4 hydrolase - Aryl-substituted bridged or fused diamine compounds, pharmaceutical compositions containing them, and methods of using the compounds and the pharmaceutical compositions for leukotriene A | 10-20-2011 |
20110257154 | COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS - The invention provides novel pyrimidine and pyridine derivatives and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine and pyridine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of anaplastic lymphoma kinase (ALK) activity, focal adhesion kinase (FAK), zeta-chain-associated protein kinase 70 (ZAP-70), insulin-like growth factor (IGF-1R), or a combination thereof. | 10-20-2011 |
20110257155 | COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS - The invention provides novel pyrimidine and pyridine derivatives and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine and pyridine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of anaplastic lymphoma kinase (ALK) activity, focal adhesion kinase (FAK), zeta-chain-associated protein kinase 70 (ZAP-70), insulin-like growth factor (IGF-1R), or a combination thereof. | 10-20-2011 |
20110263559 | INDAZOLE COMPOUNDS USEFUL AS KETOHEXOKINASE INHIBITORS - The present invention is directed to substituted indazole compounds, pharmaceutical compositions of these compounds and methods of use thereof. The compounds of the present invention are ketohexokinase (KHK) inhibitors, useful for treating or ameliorating a KHK mediated metabolic disorders and/or diseases such as obesity, Type II diabetes mellitus and Metabolic Syndrome X. | 10-27-2011 |
20110263560 | Organic Compounds - 3,4-substituted piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,4-substituted piperidine compound, and/or a method of treatment comprising administering a 3,4substituted piperidine compound, a method for the manufacture of a 3,4-substituted piperidine compound, and novel intermediates and partial steps for their synthesis are disclosed. The 3,4-disubstituted piperidine compounds have the formula (I), wherein the symbols have the meanings defined in the specification. | 10-27-2011 |
20110269737 | 7-(Piperazine-1-Ymethyl)-1H-Indole-2-Carboxylic Acid (Phenyl)-Amide Derivatives and Allied Compounds as P38 Map Kinase Inhibitors for the Treatment of Respiratory Diseases - The present invention provides compounds according to general formula (I) | 11-03-2011 |
20110269738 | COMPOUNDS - The present invention relates to novel compounds having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders. | 11-03-2011 |
20110275609 | BICYCLIC PYRAZOLO-HETEROCYCLES - The present invention provides substituted pyrazolo-heterocycles having the general structure of formula I | 11-10-2011 |
20110275610 | SUBSTITUTED PYRAZOLE COMPOUNDS - Disclosed are compounds of Formula (I) | 11-10-2011 |
20110281840 | N-SUBSTITUTED SATURATED HETEROCYCLIC SULFONE COMPOUNDS WITH CB2 RECEPTOR AGONISTIC ACTIVITY - This invention relates to compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein X, R | 11-17-2011 |
20110288068 | AZA SPIRO ALKANE DERIVATIVES AS INHIBITORS OF METALLOPROTEASES - The present invention provides a compound of Formula I or Formula II: | 11-24-2011 |
20110294776 | Pyrrolo[2,1-F] [1,2,4] Triazin-4-Ylamines IGF-1R Kinase Inhibitors for the Treatment of Cancer and Other Hyperproliferative Diseases - This invention relates to novel compounds of formula (I). Formula (I) in which the variable groups are as defined in the specification and claims, to pharmaceutical compositions containing them, and to a method of treatment using them for treatment of cancer. | 12-01-2011 |
20110294777 | BETA-LACTAMASE INHIBITORS - Substituted bicyclic beta-lactams of Formula I: (I), are β-lactamase inhibitors, wherein a, X, R | 12-01-2011 |
20110294778 | HEPATITIS C INHIBITOR COMPOUNDS - Compounds of Formula (I) | 12-01-2011 |
20110294779 | NOVEL IMIDAZOPYRIDINES - The invention is concerned with novel imidazopyridine derivatives of formula (I) | 12-01-2011 |
20110301142 | ANTAGONISTS OF LYSOPHOSPHATIDIC ACID RECEPTORS - Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases. | 12-08-2011 |
20110301143 | HETEROCYCLIC DERIVATIVES AS INHIBITORS OF STEAROYL-COENZYME A DELTA-9 DESATURASE - Heterocyclic compounds of structural formula (I), or a pharmaceutically acceptable salt thereof, wherein W is a R | 12-08-2011 |
20110306590 | ARYL- AND HETEROARYL- NITROGEN-HETEROCYCLIC COMPOUNDS AS PDE10 INHIBITORS - Aryl- and heteroaryl-nitrogen heterocyclic compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, Huntington's Disease, bipolar disorder, obsessive-compulsive disorder, and the like. | 12-15-2011 |
20110306591 | HETEROARYLOXYCARBOCYCLYL COMPOUNDS AS PDE10 INHIBITORS - Heteroaryloxycarbocyclyl compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, Huntington's Disease, bipolar disorder, obsessive-compulsive disorder, and the like. | 12-15-2011 |
20110312933 | OXYINDOLE DERIVATIVES WITH MOTILIN RECEPTOR AGONISTIC ACTIVITY - The present invention relates to novel oxyindole derivatives of formula (I) or a pharmaceutically acceptable salt thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders which are mediated via the motilin receptor (GPR38). | 12-22-2011 |
20110319379 | Substituted Indazole Amides And Their Use As Glucokinase Activators - The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R | 12-29-2011 |
20120010188 | Imidazopyridine Compounds - The invention relates to compounds of formula (I): and their pharmaceutically acceptable salts and solvates, which are inhibitors of SSAO activity. The invention further relates to pharmaceutical compositions comprising these compounds and to the use of these compounds for the treatment or prevention of medical conditions wherein inhibition of SSAO activity is beneficial, such as inflammatory diseases and immune disorders. | 01-12-2012 |
20120010189 | (3-(4-(AMINOMETHYL)PHENOXY OR PHENYLTHIO)AZETIDIN-1-YL)(5-PHENYL-1,3,4-OXADIAZOL-2-YL)METHANONE COMPOUNDS - Disclosed herein are azetidinyl compounds of formula I, | 01-12-2012 |
20120010190 | 1-HYDROXYIMINO-3-PHENYL-PROPANES - This invention relates to novel 1-hydroxyimino-3-phenyl-propanes of the formula | 01-12-2012 |
20120015930 | SUBSTITUTED IMIDAZOHETEROCYCLE DERIVATIVES - The present invention provides substituted imidazoheterocycles having the general structure of formula I: | 01-19-2012 |
20120015931 | PURINE COMPOUNDS SELECTIVE FOR PI3K P110 DELTA, AND METHODS OF USE - The invention provides compounds having the general formula: | 01-19-2012 |
20120015932 | Pyrazole Derivatives Used as CCR4 Receptor Antagonists - Indazole compounds, processes for their preparation, intermediates usable in these processes, pharmaceutical compositions containing such compounds and their use in therapy. | 01-19-2012 |
20120015933 | Spirocyclic nitriles as protease inhibitors - The invention relates to substituted carbo- and heterocyclic spiro compounds of the formula Ia which inhibit thiol proteases, to processes for their preparation and to the use thereof as medicaments. | 01-19-2012 |
20120022041 | SUBSTITUTED HETEROCYCLIC COMPOUNDS - Disclosed are compounds of Formula (I) | 01-26-2012 |
20120022042 | CARBOCYCLIC GLYT1 RECEPTOR ANTAGONISTS - The present invention relates to the use of a compound of formula I | 01-26-2012 |
20120028953 | Azetidine Derivatives - Compounds of formula (I) are inhibitors of fatty acid amide hydrolase, (FAAH), and which are useful in the treatment of diseases or medical conditions which benefit from inhibition of FAAH activity, such as anxiety, depression pain, inflammation, and eating, sleep, neurodegenerative and movement disorders: Formula (I) Wherein Ar | 02-02-2012 |
20120028954 | Substituted Pyridine, Pyridazine, Pyrazine And Pyrimidine Compounds And Methods For Using The Same - Disclosed are substituted pyridine compounds as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure | 02-02-2012 |
20120035149 | Prokineticin Receptor Antagonists And Uses Thereof - Contemplated compounds, compositions, and methods of prokineticin antagonists are presented where a prokineticin antagonist is used in the treatment and prevention of various conditions and disorders, and especially type II diabetes. | 02-09-2012 |
20120035150 | MIF INHIBITORS AND THEIR USES - The invention relates to MIF inhibitors; compositions comprising an effective amount of a MIF inhibitor; and methods for treating or preventing diseases associated with MIF. | 02-09-2012 |
20120035151 | SUBSTITUTED DIHYDROPYRAZOLONES AND THEIR USE - The present application relates to novel substituted dihydropyrazolone derivatives, processes for their preparation, their use for treatment and/or prophylaxis of diseases and their use for the preparation of medicaments for treatment and/or prophylaxis of diseases, in particular cardiovascular and haematological diseases and kidney diseases, and for promoting wound healing. | 02-09-2012 |
20120035152 | BICYCLIC HETEROCYCLIC COMPOUNDS AS PROTEIN TYROSINE KINASE INHIBITORS - The invention relates to new bicyclic heterocyclic derivative compounds of formula (I): wherein R | 02-09-2012 |
20120035153 | BICYCLIC HETEROCYCLIC COMPOUNDS AS PROTEIN TYROSINE KINASE INHIBITORS - The invention relates to new bicyclic heterocyclic derivative compounds of formula (I): wherein R | 02-09-2012 |
20120040950 | ISOINDOLINONE INHIBITORS OF PHOSPHATIDYLINOSITOL 3-KINASE - The present invention relates to compounds useful as inhibitors of PI3K, particularly of PI3Kγ. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. | 02-16-2012 |
20120040951 | HETEROARYL COMPOUNDS USEFUL AS RAF KINASE INHIBITORS - The present invention provides compounds of formula (I) useful as inhibitors of Raf protein kinase. The present invention also provides compositions thereof, and methods of treating Raf-mediated diseases. | 02-16-2012 |
20120040952 | AZETIDINES AS HISTAMINE H3 RECEPTOR ANTAGONISTS - The invention relates to compounds of formula (I), wherein R, R | 02-16-2012 |
20120040953 | Compounds for the Treatment of Metabolic Disorders - The present invention is directed to therapeutic compounds which have activity as agonists of GPR119 and are useful for the treatment of metabolic disorders including type II diabetes. | 02-16-2012 |
20120040954 | NOVEL ANTI-INFLAMMATORY AGENTS - Disclosed are novel compounds that are useful in regulating the expression of interleukin-6 (IL-6) and/or vascular cell adhesion molecule-1 (VCAM-1), and their use in the treatment and/or prevention of cardiovascular and inflammatory diseases and related disease states, such as, for example, atherosclerosis, asthma, arthritis, cancer, multiple sclerosis, psoriasis, and inflammatory bowel diseases, and autoimmune disease(s). Also, disclosed are compositions comprising the novel compounds, as well as methods for their preparation. | 02-16-2012 |
20120040955 | FLUORO SUBSTITUTED PYRIMIDINE COMPOUNDS AS JAK3 INHIBITORS - The invention relates to compounds of formula (I) | 02-16-2012 |
20120046267 | 7-AMINOFUROPYRIDINE DERIVATIVES - Compounds of Formula 1, as shown below and defined herein: | 02-23-2012 |
20120046268 | Substituted piperidines as Par-1 Antagonists - The invention relates to novel substituted piperidines, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular of cardiovascular disorders and tumour disorders. | 02-23-2012 |
20120058985 | CYCLOPROPYL DICARBOXAMIDES AND ANALOGS EXHIBITING ANTI-CANCER AND ANTI-PROLIFERATIVE ACTIVITIES - The disclosed compounds are useful in the treatment of mammalian cancers and especially human cancers. Compounds, pharmaceutical compositions, and methods of Formula I are disclosed: | 03-08-2012 |
20120058986 | DI-AZETIDINYL DIAMIDE AS MONOACYLGLYCEROL LIPASE INHIBITORS - Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: | 03-08-2012 |
20120058987 | THERAPEUTIC USES OF QUINAZOLINEDIONE DERIVATIVES - The subject matter of the present invention is the use of compounds of formula (I) in the form of a base, a hydrate or a solvate, or of mixtures thereof, as a medicament or for preparing a medicament intended for the treatment and/or prevention of disorders associated with the central nervous system (abbreviated to CNS) and/or associated with the peripheral nervous system (abbreviated to PNS). | 03-08-2012 |
20120065183 | Tetrahydro-Pyrido-Pyrimidine Derivatives - The invention relates to substituted tetrahydro-pyrido-pyrimidine derivatives of the formula (I), | 03-15-2012 |
20120065184 | COMPOUNDS AND COMPOSITIONS AS TRK INHIBITORS - The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated TRK kinase activity. | 03-15-2012 |
20120065185 | SUBSTITUTED ALKYLAMINE DERIVATIVES AND METHODS OF USE - Selected heterocyclic compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. | 03-15-2012 |
20120071460 | PYRAZOLE OXADIAZOLE DERIVATIVES AS S1P1 AGONISTS - The present invention relates to pyrazole oxadiazoles derivatives of Formula (I), and their use for treating multiple sclerosis and other diseases, wherein R | 03-22-2012 |
20120077796 | PHENALKYLAMINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND THEIR USE IN THERAPY - The present invention relates to phenalkylamine derivatives of the formula (I) | 03-29-2012 |
20120077797 | OXOPIPERAZINE-AZETIDINE AMIDES AND OXODIAZEPINE-AZETIDINE AMIDES AS MONOACYLGLYCEROL LIPASE INHIBITORS - Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds, and enantiomers, diastereomers, and pharmaceutically acceptable salts thereof, are represented by Formula (Ia) and Formula (Ib) as follows: | 03-29-2012 |
20120077798 | AZETIDINE AND CYCLOBUTANE DERIVATIVES AS JAK INHIBITORS - The present invention relates to azetidine and cyclobutane derivatives, as well as their compositions, methods of use, and processes for preparation, which are JAK inhibitors useful in the treatment of JAK-associated diseases including, for example, inflammatory and autoimmune disorders, as well as cancer. | 03-29-2012 |
20120083482 | INHIBITORS OF VEGF RECEPTOR AND HGF RECEPTOR SIGNALING - The invention relates to the inhibition of VEGF receptor signaling and HGF receptor signaling. The invention provides compounds of general formula (A) | 04-05-2012 |
20120088747 | SULFONAMIDE CONTAINING COMPOUNDS AND USES THEREOF - Compounds, compositions and methods for treating GHS-R mediated disorders are described herein. | 04-12-2012 |
20120088748 | HETEROCYCLIC COMPOUNDS - Provided is a compound having a monoamine reuptake inhibitory activity, which is represented by the formula (I) | 04-12-2012 |
20120088749 | S1P Receptor Modulating Compounds and Use Thereof - The present invention relates to amides that have activity as S1P receptor modulating agents and the use of such compounds to treat diseases associated with inappropriate S1P receptor activity. The compounds may be used as immunomodulators, e.g., for treating or preventing diseases such as autoimmune and related immune disorders including systemic lupus erythematosus, inflammatory bowel diseases such as Crohn's disease and ulcerative colitis, type I diabetes, uveitis, psoriasis, myasthenia gravis, rheumatoid arthritis, non-glomerular nephrosis, hepatitis, Behçet's disease, glomerulonephritis, chronic thrombocytopenic purpura, hemolytic anemia, hepatitis and Wegner's granuloma; and for treating other conditions. | 04-12-2012 |
20120094973 | CATECHOL-BASED DERIVATIVES FOR TREATING OR PREVENTING DIABETICS - The present invention provides a catechol-based derivative and a pharmaceutical acceptable salt therefrom and a solvate therefrom. A pharmaceutical composition for preventing or treating diabetes and ischemia, comprising a catechol-based derivative of formula (I) and at least one selected from the group consisting of a pharmaceutical excipient, a diluent and a carrier. | 04-19-2012 |
20120101081 | AMINO-PYRROLIDINE-AZETIDINE DIAMIDES AS MONOACYLGLYCEROL LIPASE INHIBITORS - Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds, and enantiomers, diastereomers, and pharmaceutically acceptable salts thereof, are represented by Formula (I) as follows: | 04-26-2012 |
20120101082 | VASOPRESSIN V1A ANTAGONISTS - The present invention concerns compounds inter alia according to general formula 1a. Compounds according to the invention are vasopressin V | 04-26-2012 |
20120101083 | S1P1 AGONISTS COMPRISING A BICYCLIC N-CONTAINING RING - The present invention relates to novel compounds of formula (I) having S1P1 agonist activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders. | 04-26-2012 |
20120108564 | 1,3,4,8-Tetrahydro-2H-Pyrido[1,2-a]Pyradine Derivatives and Use Thereof as HIV Integrase Inhibitor - [Problem] Provided is a novel 1,3,4,8-tetrahydro-2H-pyrido[1,2-a]pyrazine derivative or a pharmaceutically acceptable salt thereof, or a solvate thereof, which is useful as an anti-HIV agent. | 05-03-2012 |
20120108565 | PYRROLE CARBOXYLIC ACID DERIVATIVES AS ANTIBACTERIAL AGENTS - The present invention provides DNA Gyrase and/or Topo IV inhibitors of Formula (I), which can be used as antibacterial agents. Compounds disclosed herein can be used for treating or preventing conditions caused by or contributed by gram positive, gram negative and anaerobic bacteria, more particularly against, for example, | 05-03-2012 |
20120108566 | NICOTINAMIDES AS JAK KINASE MODULATORS - The present invention is directed to compounds of formula I and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma. | 05-03-2012 |
20120108567 | Thiazolyl-Dihydro-Indazoles - The present invention encompasses compounds of general formula (1) | 05-03-2012 |
20120108568 | SUBSTITUTED PYRAZOLO[1,5-a]PYRIMIDINE COMPOUNDS AS TRK KINASE INHIBITORS - Compounds of Formula (I) and salts thereof in which R | 05-03-2012 |
20120115842 | Substituted Oxindole Derivatives, Medicaments Containing Said Derivatives and Use Thereof - The invention relates to novel oxindole derivatives of general formula (I), wherein substituents A, B, X and Y are defined as in claim | 05-10-2012 |
20120115843 | NOVEL PYRROLIDINE DERIVATIVES - The invention relates to a compound of formula (I) | 05-10-2012 |
20120115844 | NOVEL TRIAZOLE COMPOUNDS I - The present invention is concerned with novel triazole compounds of formula (I) | 05-10-2012 |
20120115845 | THERAPEUTIC AGENTS - A compound of formula I | 05-10-2012 |
20120122837 | INHIBITORS OF FATTY ACID BINDING PROTEIN - The present invention relates to novel heterocyclic compounds as Fatty Acid Binding Protein (“FABP”) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. | 05-17-2012 |
20120122838 | HETEROCYCLIC COMPOUNDS AND USES THEREOF - Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein. | 05-17-2012 |
20120122839 | NOVEL PYRROLIDIN-2-ONES - The present invention provides compounds of formula (I) or (Ia) which are ligands binding to the HDM2 protein, inducing apoptosis and inhibiting proliferation, and having therapeutic utility in cancer therapy and prevention. | 05-17-2012 |
20120129827 | NOVEL DERIVATIVES OF 1-ALKYL-6-OXO-PIPERIDINE-3-CARBOXYLIC ACIDS AND 1-ALKYL-5-OXO-PYRROLIDINE-3-CARBOXYLIC ACIDS AND THEIR USES AS COOLING COMPOUNDS - The present invention relates to novel derivatives of 1-alkyl-6-oxo-piperidine-3-carboxylic acids and 1-alkyl-5-oxo-pyrrolidine-3-carboxylic acids represented by Formula I: | 05-24-2012 |
20120129828 | S1P1 RECEPTOR AGONISTS AND USE THEREOF - The present invention relates to compounds of Formula (I) that are have activity as S1P1 receptor modulating agents, more specifically to specifically compounds that are S1P1 receptor agonists. The invention also related to the use of such compounds to treat diseases associated with inappropriate S1P1 receptor activity such as autoimmune diseases. | 05-24-2012 |
20120129829 | NOVEL INDOLE MODULATORS OF S1P RECEPTORS - The present invention relates to novel indole derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors. | 05-24-2012 |
20120129830 | 7-AZA-SPIRO[3.5]NONANE-7-CARBOXYLATE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF - The invention relates to compounds of the general formula (I) where: R | 05-24-2012 |
20120129831 | Substituted 3-(1,2,4-Oxadiazol-5-yl)-5-Phenylpiperidines - The invention relates to novel substituted piperidines, to processes for preparation thereof, to the use thereof for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially of cardiovascular disorders and tumour disorders. | 05-24-2012 |
20120129832 | AMIDE DERIVATIVE - Provided are a compound having an excellent hypoglycemic action, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition having an excellent therapeutic effect and/or prophylactic effect on type 1 diabetes, type 2 diabetes, and the like, which cause an increase in the blood sugar level due to abnormal sugar metabolism. A compound represented by general formula (I), or a pharmaceutically acceptable salt thereof, is disclosed. | 05-24-2012 |
20120135977 | ETHER BENZOTRIAZOLE DERIVATIVES - The present invention is directed to ether benzotriazole derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved. | 05-31-2012 |
20120135978 | 6,7-UNSATURATED-7-CARBAMOYL SUBSTITUTED MORPHINAN DERIVATIVE - A novel compound which is useful as an agent for treating and/or preventing emesis, vomiting and/or constipation. | 05-31-2012 |
20120142663 | NOVEL AZETIDINE DERIVATIVES AS SPHINGOSINE 1-PHOSPHATE (S1P) RECEPTOR MODULATORS - The present invention relates to novel azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors. | 06-07-2012 |
20120142664 | NOVEL BENZYL AZETIDINE DERIVATIVES AS SPHINGOSINE 1-PHOSPHATE (S1P) RECEPTOR MODULATORS - The present invention relates to novel benzyl azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors. | 06-07-2012 |
20120142665 | TRIAZOLOPYRIDINE COMPOUNDS - The invention is concerned with triazolopyridine compounds of formula (I) | 06-07-2012 |
20120142666 | Azetidine 2-Carboxamide Derivatives Which Modulate The CB2 Receptor - Compounds of the formula (I), (II) and (III) which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain. | 06-07-2012 |
20120142667 | PYRIMIDINE DERIVATIVES AS ZAP-70 INHIBITORS - The invention relates to compounds of formula (I) | 06-07-2012 |
20120142668 | CATHEPSIN C INHIBITORS - Disclosed are 4-amino-2-butenamides of Formula (I) having pharmacological activity, pharmaceutical compositions containing them, and methods for the treatment of diseases mediated by the cathepsin C enzyme such as chronic obstructive pulmonary disease. | 06-07-2012 |
20120149679 | Sulfonamide Derivatives - The present invention relates to compounds of the formula | 06-14-2012 |
20120157429 | COMPOUNDS USEFUL AS INHIBITORS OF JANUS KINASES - The present invention relates to compounds useful as inhibitors of protein kinases, particularly of JAK family kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. | 06-21-2012 |
20120157430 | N-(1-(SUBSTITUTED-PHENYL)ETHYL)-9H-PURIN-6-AMINES AS PI3K INHIBITORS - The present invention provides N-(1-(substituted-phenyl)ethyl)-9H-purin-6-amines derivatives that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases. | 06-21-2012 |
20120157431 | Pyrimidine Sulphonamide Derivatives as Chemokine Receptor Modulators - A compound of formula (I), or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof and pharmaceutical compositions comprising these, all for use in the treatment of chemokine mediated diseases and disorders. | 06-21-2012 |
20120157432 | NOVEL PYRROLIDINE DERIVED BETA 3 ADRENERGIC RECEPTOR AGONISTS - The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of β3-adrenoceptor. | 06-21-2012 |
20120157433 | Heteroaryl Compounds as Kinase Inhibitors - The present invention provides a compound of Formula (I): | 06-21-2012 |
20120165304 | 6,7,8,9-Tetrahydro-5H-1,4,7,10a-tetraaza-cyclohept[f]indene derivatives, pharmaceutical compositions containing these compounds, their use and processes for preparing them - The present invention relates to compounds defined by formula (I), wherein the groups X, Y, W and R | 06-28-2012 |
20120165305 | SUBSTITUTED IMIDAZOPYRIDAZINES AND BENZIMIDAZOLES AS INHIBITORS OF FGFR3 - The present invention relates to substituted imidazopyridazines and substituted benzimidazoles, as well as pharmaceutical compositions comprising the same, which are FGFR3 inhibitors useful in the treatment of cancer and other diseases. | 06-28-2012 |
20120165306 | PYRAZINYLPYRIDINES USEFUL FOR THE TREATMENT OF PROLIFERATIVE DISEASES - The present invention provides a compound of Formula (I): | 06-28-2012 |
20120165307 | AZAINDOLES USEFUL AS INHIBITORS OF JANUS KINASES - The present invention relates to compounds useful as inhibitors of protein kinases, particularly of JAK family kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. | 06-28-2012 |
20120172347 | 8-OXODIHYDROPURINE DERIVATIVE - The present invention provides a compound represented by the formula (1) or a pharmaceutically acceptable salt thereof (wherein W represents a hydrogen atom, a halogen atom, or the others; A represents an alkyl group optionally substituted by aryl group or the others, an aryl group, or the others; and one of X and Y represents a di-substituted alkylaminocarbonyl group, or the others, and the other represents a hydrogen atom, an alkyl group, an alkylcarbonyl group, or the others); a medicament or a pharmaceutical composition for treatment or prophylaxis of FAAH-related diseases such as depression, anxiety disorder or pains, comprising the compound or the like as an active ingredient; a use of the compound or the like; and a method for treatment or prophylaxis using the compound or the like. | 07-05-2012 |
20120178733 | FACTOR XA INHIBITORS - The present invention is directed to compounds represented by Formula I and pharmaceutically acceptable salts, solvates, hydrates, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to and intermediates used in making such compounds, pharmaceutical compositions containing such compounds, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample. | 07-12-2012 |
20120178734 | DERIVATIVES OF 6,7-DIHYDRO-5H-IMIDAZO[1,2-a]IMIDAZOLE-3-CARBOXYLIC ACID AMIDES - Derivatives of 6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-carboxylic acid amide exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease. | 07-12-2012 |
20120178735 | 2H-CHROMENE COMPOUND AND DERIVATIVE THEREOF - Provided is a 2H-chromene compound or a derivative thereof which has an excellent S1P1 agonist action. The 2H-chromene compound or derivative is particularly useful for preventing and/or treating a disease induced by undesirable lymphocyte infiltration or a disease induced by abnormal proliferation or accumulation of cells. | 07-12-2012 |
20120178736 | BICYCLIC PYRIMIDINE PI3K INHIBITOR COMPOUNDS SELECTIVE FOR P110 DELTA, AND METHODS OF USE - Formula I (Ia and Ib) compounds wherein (i) X | 07-12-2012 |
20120184522 | THERAPEUTIC APPLICATIONS IN THE CARDIOVASCULAR FIELD OF QUINAZOLINEDIONE DERIVATIVES - A subject-matter of the present invention is the use of compounds of formula (I) | 07-19-2012 |
20120184523 | C-Met Modulators and Method of Use - The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds. | 07-19-2012 |
20120190665 | PYRAZOLOPYRIMIDINE JAK INHIBITOR COMPOUNDS AND METHODS - A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R | 07-26-2012 |
20120196845 | QUINOLINONE-PYRAZOLONE M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS - The present invention is directed to quinolinone-pyrazolone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor. | 08-02-2012 |
20120202784 | ISOINDOLINONE INHIBITORS OF PHOSPHATIDYLINOSITOL 3-KINASE - The present invention relates to compounds useful as inhibitors of PI3K, particularly of PI3Kγ. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. | 08-09-2012 |
20120202785 | HETEROCYCLIC COMPOUNDS AND METHODS OF USE - Formula I compounds, including stereoisomers, geometric isomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological disorders, and cancer. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. | 08-09-2012 |
20120202786 | THERAPEUTIC ISOXAZOLE COMPOUNDS - The invention provides a compound of formula I: | 08-09-2012 |
20120202787 | Novel Heteroaryl Imidazoles And Heteroaryl Triazoles As Gamma-Secretase Modulators - Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I; | 08-09-2012 |
20120208791 | IMIDAZOPYRIDINE DERIVATIVES AS INHIBITORS OF RECEPTOR TYROSINE KINASES - The invention relates to new bicyclic heterocyclic derivative compounds, to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer. | 08-16-2012 |
20120214786 | NEW COMPOUNDS - This invention relates to compounds of formula I | 08-23-2012 |
20120214787 | OXADIAZOLE INHIBITORS OF LEUKOTRIENE PRODUCTION - The present invention relates to compounds of formula (I): | 08-23-2012 |
20120214788 | HETEROARYL-SUBSTITUTED PIPERIDINES - The invention relates to novel heteroaryl-substituted piperidines, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular of cardiovascular diseases and tumour diseases. | 08-23-2012 |
20120214789 | TETRAZOLE-SUBSTITUTED ARYLAMIDES AS P2X3 AND P2X2/3 ANTAGONISTS - Compounds of the formula I: | 08-23-2012 |
20120214790 | N-ACYL CYCLIC AMINE DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF - The present invention provides compounds which show high effectiveness against positive symptoms, negative symptoms and cognitive dysfunction in schizophrenia and reduce conventional side-effect risks as well as have remarkable effects for central neurological diseases associated with cognitive dysfunction other than schizophrenia. N-Acyl cyclic amine derivatives of formula (1): wherein Ar | 08-23-2012 |
20120220563 | Substituted piperidines - The invention relates to novel substituted piperidines, to processes for preparation thereof, to the use thereof for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially of cardiovascular disorders and tumour disorders. | 08-30-2012 |
20120220564 | SELECTIVE CALCIUM CHANNEL MODULATORS - Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted T-type calcium channel activity are disclosed using a series of compounds containing N-acylated cyclic amines linked to an aπl ring as shown in formula (I). | 08-30-2012 |
20120225855 | TRIAZOLOPYRIDINE JAK INHIBITOR COMPOUNDS AND METHODS - A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R | 09-06-2012 |
20120232049 | PYRIDINE OR PYRIMIDINE DERIVATIVE HAVING EXCELLENT CELL GROWTH INHIBITION EFFECT AND EXCELLENT ANTI-TUMOR EFFECT ON CELL STRAIN HAVING AMPLIFICATION OF HGFR GENE - A pyridine or pyrimidine derivative represented by the formula (I) has an excellent HGFR inhibitory activity and exhibits strong cell proliferation inhibitory effect and anti-tumor effect against cancer cell lines with amplified HGFR gene. | 09-13-2012 |
20120232050 | Cyclic Inhibitors of 11 beta-Hydroxysteroid Dehydrogenase 1 - This invention relates to novel compounds of the Formula (I), (II), (II-A), (II-B), (II-C), (II-D), (III). (III-A). (IIII-B). (III-C). (III-D), (III-E) (IV), (IV-A), (IV-B). (IV-C), (IV-D). (V), (V-A), (V-B), (V-C), (V-D), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11β-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell. | 09-13-2012 |
20120232051 | 3-AMINO-PYRIDINES AS GPBAR1 AGONISTS - This invention relates to novel 3-aminopyridines of the formula | 09-13-2012 |
20120232052 | ARYL CARBOXAMIDE DERIVATIVES AS TTX-S BLOCKERS - The present invention relates to aryl carboxamide derivatives of formula (I), wherein Ar | 09-13-2012 |
20120238540 | AMINO-PYRIMIDINE COMPOUNDS AS INHIBITORS OF IKK EPSILON AND/OR TBK1 - The invention relates to certain amino-pyrimidine compounds that inhibit IKK epsilon and/or TBK1, methods of making such compounds, pharmaceutical compositions comprising such compounds, and the use of these compounds in treating a variety of diseases and disorders. | 09-20-2012 |
20120245138 | N-(2-(HETARYL)ARYL)ARYLSULFONAMIDES AND N-(2-(HETARYL)HETARYL ARYLSULFONAMIDES - Compounds are provided that act as potent antagonists of the CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists. | 09-27-2012 |
20120245139 | INHIBITORS OF THE HEDGEHOG PATHWAY - The present invention is directed to a compound of Formula I | 09-27-2012 |
20120245140 | N-CONTAINING HETEROARYL DERIVATIVES AS JAK3 KINASE INHIBITORS - N-containing heteroaryl derivatives of formula I or II, wherein the meanings for the various substituents are as disclosed in the description. These compounds are useful as JAK, particularly JAK3, kinase inhibitors. | 09-27-2012 |
20120264729 | CO-CRYSTALS AND SALTS OF CCR3-INHIBITORS - This invention relates to co-crystals and salts of CCR3 inhibitors of formula 1, | 10-18-2012 |
20120264730 | SUBSTITUTED BICYCLIC METHYL AZETIDINES AS SPHINGOSINE-1 PHOSPHATE RECEPTORS MODULATORS - The present invention relates to novel substituted bicyclic methyl azetidine derivatives which are useful as sphingosine-1-phosphate receptors modulators and useful for treating a wide variety of disorders associated with modulation of sphingosine-1-phosphate receptors. | 10-18-2012 |
20120264731 | CHROMENONE DERIVATIVES - The invention concerns chromenone compounds of Formula I; | 10-18-2012 |
20120264732 | PHENYL BICYCLIC METHYL AZETIDINE DERIVATIVES AS SPHINGOSINE-1 PHOSPHATE RECEPTORS MODULATORS - The present invention relates to novel phenyl bicyclic methyl azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors. | 10-18-2012 |
20120264733 | HETEROCYCLIC COMPOUND AND USE THEREOF - Compounds represented by the formulas | 10-18-2012 |
20120264734 | Aryl- or Heteroaryl-Substituted Benzene Compounds - The present invention relates to aryl- or heteroaryl-substituted benzene compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes. | 10-18-2012 |
20120264735 | TYROSINE KINASE INHIBITORS - The present invention relates to pyridazin-4(1H)-one derivatives, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals. | 10-18-2012 |
20120270852 | PHENYL OR PYRIDINYL-ETHYNYL DERIVATIVES - The present invention relates to ethynyl derivatives of formula I | 10-25-2012 |
20120270853 | ARYLPROPIONAMIDE, ARYLACRYLAMIDE, ARYLPROPYNAMIDE, OR ARYLMETHYLUREA ANALOGS AS FACTOR XIA INHIBITORS - The present invention provides compounds of Formula (I): | 10-25-2012 |
20120277205 | DERIVATIVES OF N-[(1H-PYRAZOL-1-YL)ARYL]-1H-INDOLE OR 1H-INDAZOLE-3-CARBOXAMIDE, PREPARATION THEREOF AND APPLICATIONS THEREOF IN THERAPEUTICS - The present invention relates to compounds corresponding to formula (I): | 11-01-2012 |
20120277206 | REVERSE TRANSCRIPTASE INHIBITORS - Described herein are novel enzyme inhibitors. In some embodiments, the enzyme inhibitors are reverse transcriptase inhibitors, particularly HIV reverse transcriptase inhibitors. Also described herein are compositions containing them and methods of using them. Thus, the compounds and compositions described herein are useful for the in vitro and in vivo inhibition of HIV reverse transcriptase as a method of treating or preventing HIV, AIDS or related disorders. | 11-01-2012 |
20120277207 | NOVEL HETEROCYCLIC ACRYLAMIDES AND THEIR USE AS PHARMACEUTICALS - The invention relates to novel heterocyclic acrylamide compounds (I), to the preparation of the compounds and intermediates used therein, to the use of the compounds as antibacterial medicaments and pharmaceutical compositions containing the compounds. | 11-01-2012 |
20120277208 | BENZAMIDE COMPOUND - [Problem]A compound which is useful as a GK activator is provided. | 11-01-2012 |
20120277209 | PYRAZINE COMPOUNDS AS PHOSPHODIESTERASE 10 INHIBITORS - Pyrazine compounds of formula (I): | 11-01-2012 |
20120289493 | FUSED HETEROCYCLIC COMPOUNDS AS ION CHANNEL MODULATORS - The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: | 11-15-2012 |
20120289494 | SPIRO-OXINDOLE MDM2 ANTAGONISTS - Provided herein are compounds, compositions, and methods in the field of medicinal chemistry. The compounds and compositions provided herein relate to spiro-oxindoles which function as antagonists of the interaction between p53 and MDM2, and their use as therapeutics for the treatment of cancer and other diseases. | 11-15-2012 |
20120289495 | COMPOUNDS AND METHODS - Disclosed are compounds having the formula: | 11-15-2012 |
20120295883 | COMPOUNDS - The present invention relates to substituted pyrazolopyridine compounds, and pharmaceutically acceptable salts or esters thereof. The present invention further relates to therapeutic uses of pharmaceutical compositions comprising the substituted pyrazolopyridine compounds, for example, in cancer and neurodegenerative diseases. | 11-22-2012 |
20120295884 | Complement pathway modulators and uses thereof - The present invention provides a compound of formula I: | 11-22-2012 |
20120302543 | Compounds for the Treatment of Neurological Disorders - Provided are compounds, pharmaceutical compositions and methods of treatment or prophylaxis of certain neurologic disorders, including disorders related to NMDA receptor activation, neuropsychiatric disorders, neurodegenerative disorders and other neurologic diseases, disorders and related conditions. The compounds are of the Formulas I and Ia-Ij as described herein. | 11-29-2012 |
20120302544 | SUBSTITUTED AMINOTHIAZOLONE INDAZOLES AS ESTROGEN RELATED RECEPTOR-ALPHA MODULATORS - The present invention relates to compounds of Formula (I), | 11-29-2012 |
20120302545 | Method of Using PI3K and MEK Modulators - The invention provides methods of treating cancer with a combination of compounds which inhibit kinases, more specifically MEK and PI3K. | 11-29-2012 |
20120309738 | NOVEL COMPOUNDS - This invention relates to compounds of formula I | 12-06-2012 |
20120316148 | Compositions and Methods for Modulating a Kinase - The invention relates to compounds and methods for modulating one or more components of a kinase signaling cascade. | 12-13-2012 |
20120316149 | HETEROCYCLIC SULFONAMIDE DERIVATIVES - The present invention relates to compounds: | 12-13-2012 |
20120316150 | AMIDE COMPOUNDS USEFUL IN THERAPY - A compound of Formula (I), or a pharmaceutically acceptable salt or solvate thereof, | 12-13-2012 |
20120316151 | TRIAZOLONES AS FATTY ACID SYNTHASE INHIBITORS - This invention relates to the use of triazolone derivatives of Formula (I) for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of triazolones in the treatment of cancer. | 12-13-2012 |
20120322785 | SUBSTITUTED 6,6-FUSED NITROGENOUS HETEROCYCLIC COMPOUNDS AND USES THEREOF - The invention provides novel compounds having the general formula: | 12-20-2012 |
20120329774 | THIENO-PYRIDINE DERIVATIVES AS MEK INHIBITORS - A series of thieno[2,3-b]pyridine derivatives which are substituted in the 2-position by a substituted anilino moiety, being selective inhibitors of human MEK (MAPKK) enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, proliferative (including oncological) and nociceptive conditions. | 12-27-2012 |
20130005704 | SUBSTITUTED ARYLIMIDAZOLONE AND TRIAZOLONE AS INHIBITORS OF VASOPRESSIN RECEPTORS - The present application relates to novel, substituted 4-arylimidazol-2-ones and 5-aryl-1,2,4-triazolones, processes for the production thereof, the use thereof alone or in combinations for the treatment and/or prevention of diseases and the use thereof for the production of medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular diseases. | 01-03-2013 |
20130012488 | BENZOXEPIN PI3K INHIBITOR COMPOUNDS AND METHODS OF USE - Benzoxepin compounds of Formula I, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. | 01-10-2013 |
20130012489 | Morpholinylquinazolines - The invention relates to compounds of the formulae (I), (II) and (III) | 01-10-2013 |
20130012490 | Pyrimidine Sulphonamide Derivatives as Chemokine Receptor Modulators - A compound of formula (1), or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof and pharmaceutical compositions comprising these, all for use in the treatment of chemokine mediated diseases and disorders. | 01-10-2013 |
20130012491 | PYRIMIDINE DERIVATIVES FOR USE AS SPHINGOSINE 1-PHOSPHATE 1 (S1P1) RECEPTOR AGONISTS - Disclosed are pyrimidine derivatives for use as a sphingosine 1-phosphate 1 (S1P1) receptor agonists, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of conditions or diseases mediated by S1P1 receptors, particularly multiple sclerosis. | 01-10-2013 |
20130018032 | INHIBITORS OF BRUTON'S TYROSINE KINASE - Described herein are kinase inhibitor compounds, methods for synthesizing such inhibitors, and methods for using such inhibitors in the treatment of diseases. Further described herein are methods, assays and systems for determining an appropriate inhibitor of a protein, including a kinase. | 01-17-2013 |
20130023517 | Therapeutic methods employing substituted piperidines which are CCR3 antagonists - Object of the present invention are novel substituted compounds of the formula 1, | 01-24-2013 |
20130023518 | NOVEL 3,3-DIMETHYL TETRAHYDROQUINOLINE DERIVATIVES - A compound of formula (I) | 01-24-2013 |
20130029964 | [5, 6] HETEROCYCLIC COMPOUND - An object of the present invention is to provide a novel low molecular weight compound exhibiting an osteogenesis-promoting action. This object is achieved by a compound having the general formula (I) or a pharmacologically acceptable salt thereof. In the general formula (I), R | 01-31-2013 |
20130029965 | PHARMACEUTICAL SOLID DISPERSIONS - A composition comprises a solid dispersion comprising a low-solubility drug and at least one polymer. In another aspect of the invention, a composition comprises a solid dispersion comprising a low-solubility drug and a stabilizing polymer. At least a major portion of the drug in the dispersion is amorphous. The composition also includes a concentration-enhancing polymer that increases the concentration of the drug in a use environment. The stabilizing polymer has a glass transition temperature that is greater than the glass transition temperature of the concentration-enhancing polymer at a relative humidity of 50%. | 01-31-2013 |
20130035324 | HETEROCYCLIC COMPOUNDS AND USES THEREOF - Heterocyclic entities that modulate PI3 kinase activity, pharmaceutical compositions containing the heterocyclic entities, and methods of using these chemical entities for treating diseases and conditions associated with PI3 kinase activity are described herein. | 02-07-2013 |
20130035325 | KINASE INHIBITORS - Methods of inhibiting kinases using kinase inhibitors having olefin moieties are disclosed. | 02-07-2013 |
20130040931 | Amino Heteroaryl Compounds as Beta-Secretase Modulators and Methods of Use - The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula (I); wherein ring A, B | 02-14-2013 |
20130040932 | SUBSTITUTED ARYL SULFONE DERIVATIVES AS CALCIUM CHANNEL BLOCKERS - A series of substituted aryl sulfone derivatives represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, calcium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, diabetic neuropathy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, sleep disorder, bipolar disorder and stroke, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds. | 02-14-2013 |
20130040933 | AZAINDOLES AS JANUS KINASE INHIBITORS - The present invention provides compounds of formula I: or a pharmaceutically acceptable salt thereof. Compounds of formula I are inhibitors of Janus kinases and as such are useful for the treatment of various diseases and conditions mediated by said enzymes, such as rheumatoid arthritis, asthma, COPD, ALS, and the like. | 02-14-2013 |
20130045963 | Cyclohexyl Azetidine Derivatives as JAK Inhibitors - The present invention provides cyclohexyl azetidine derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase (JAK) and are useful in the treatment of diseases related to the activity of JAK including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases. | 02-21-2013 |
20130045964 | MANDELAMIDE HETEROCYCLIC COMPOUNDS - Disclosed are compounds of Formula (I) or stereoisomers, salts, or prodrugs thereof, wherein: Q is, or R | 02-21-2013 |
20130053361 | THERAPEUTIC ISOXAZOLE COMPOUNDS - The invention provides a compound of formula I: | 02-28-2013 |
20130053362 | HETEROCYCLIC COMPOUNDS AND USES THEREOF - Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including P13 kinase activity, are described herein. | 02-28-2013 |
20130053363 | IMIDAZO[1,2-a]PYRIDINE DERIVATIVE | 02-28-2013 |
20130059832 | COMPOUNDS AND COMPOSITIONS AS C-KIT KINASE INHIBITORS - The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of c-kit or c-kit and PDGFR (PDGFRα, PDGFRβ) kinases. | 03-07-2013 |
20130059833 | PDE10 MODULATORS - The present invention relates to compounds of formula (I) | 03-07-2013 |
20130059834 | PYRROLOPYRAZINE KINASE INHIBITORS - The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, | 03-07-2013 |
20130059835 | HETEROCYCLYLAMINES AS PI3K INHIBITORS - The present invention provides heterocyclylamine derivatives of Formula I: | 03-07-2013 |
20130065879 | HETEROARYL COMPOUNDS AND USES THEREOF - The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same. | 03-14-2013 |
20130065880 | COMPOUNDS AS TYROSINE KINASE MODULATORS - The present invention is directed to novel compounds of Formula I. The compounds of the present invention are potent tyrosine kinase modulators, and are suitable for the treatment and prevention of diseases and conditions related to abnormal activities of tyrosine kinase receptors. | 03-14-2013 |
20130079324 | PYRROLOPYRIMIDINE AND PURINE DERIVATIVES - The present invention relates to compounds of formula (I) | 03-28-2013 |
20130079325 | PYRIDINE AND PYRIMIDINE DERIVATIVES AS PHOSPHODIESTERASE 10 INHIBITORS - Pyridine and pyrimidine compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like. | 03-28-2013 |
20130079326 | N-PHENYL IMIDAZOLE CARBOXAMIDE INHIBITORS OF 3-PHOSPHOINOSITIDE-DEPENDENT PROTEIN KINASE-1 - The present invention provide Imidazole Carboxamide Compounds of Formula (I): wherein D, T, R | 03-28-2013 |
20130079327 | PURINONE DERIVATIVE - Compounds represented by general formula (I) (all of the symbols in the formula conform to the definitions in the Description) are compounds that, in addition to having a Btk-selective inhibitory activity, exhibit an excellent metabolic stability and can avoid hepatotoxicity or the like, and as a consequence can provide safe therapeutic agents for diseases in which B cells or mast cells participate. | 03-28-2013 |
20130079328 | COMPOSITIONS AND METHODS FOR MODULATING THE WNT SIGNALING PATHWAY - The present invention relates to compositions and methods for modulating the Wnt signaling pathway, using compounds having Formula (1) and (3): wherein A, B, Y and Z all represent rings, and R | 03-28-2013 |
20130085128 | 6-(4-Hydroxy-phenyl)-3-alkyl-1H-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors - The present invention relates to pyrazolo[3,4-b]pyridine compounds of the formula I, | 04-04-2013 |
20130085129 | MONOACYLGLYCEROL LIPASE INHIBITORS FOR THE TREATMENT OF METABOLIC DISEASES AND RELATED DISORDERS - Disclosed are compounds, compositions and methods for treating metabolic diseases, including obesity and diabetes, and for reducing weight gain. Such compounds are represented by formula (I) as follows: | 04-04-2013 |
20130085130 | MONOACYLGLYCEROL LIPASE INHIBITORS FOR THE TREATMENT OF METABOLIC DISEASES AND RELATED DISORDERS - Disclosed are compounds, compositions and methods for treating metabolic diseases, including obesity and diabetes. Such compounds are represented by formula (I) as follows: | 04-04-2013 |
20130085131 | HETEROCYCLIC COMPOUNDS AND THEIR USES - Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with pi 110δ activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia (T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer. | 04-04-2013 |
20130090326 | Antimicrobial Compounds and Methods of Making and Using the Same - The present invention relates generally to the field of antimicrobial compounds and to methods of making and using them. These compounds are useful for treating, preventing, and reducing the risk of microbial infections in humans and animals. | 04-11-2013 |
20130090327 | Inhibitors of Protein Tyrosine Kinase Activity - The present invention provides new compounds and methods for treating a disease responsive to inhibition of kinase activity, for example a disease responsive to inhibition of protein tyrosine kinase activity, for example a disease responsive to inhibition of protein tyrosine kinase activity of growth factor receptors, for example a disease responsive to inhibition of receptor type tyrosine kinase signaling, or for example, a disease responsive to inhibition of VEGF receptor signaling. | 04-11-2013 |
20130096101 | INHIBITORS OF HCV NS5A - Provided herein are compounds, pharmaceutical compositions, and combination therapies for inhibition of hepatitis C. | 04-18-2013 |
20130096102 | AMINOPYRIMIDINE DERIVATIVES AS LRRK2 MODULATORS - Compounds of the formula I: | 04-18-2013 |
20130102584 | PIPERIDIN-4-YL-AZETIDINE DIAMIDES AS MONOACYLGLYCEROL LIPASE INHIBITORS - Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds, and enantiomers, diastereomers, and pharmaceutically acceptable salts thereof, are represented by Formula (I) as follows: | 04-25-2013 |
20130102585 | AZETIDINYL DIAMIDES AS MONOACYLGLYCEROL LIPASE INHIBITORS - Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: | 04-25-2013 |
20130109669 | 6-AMINO-PYRIMIDINE-4-CARBOXAMIDE DERIVATIVES AND RELATED COMPOUNDS WHICH BIND TO THE SPHINGOSINE 1-PHOSPHATE (S1P) RECEPTOR FOR THE TREATMENT OF MULTIPLE SCLEROSIS | 05-02-2013 |
20130109670 | TRIAZINE COMPOUNDS AS PI3 KINASE AND MTOR INHIBITORS | 05-02-2013 |
20130116229 | NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A - The present invention relates to compounds which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders. | 05-09-2013 |
20130116230 | 3-AMINOPYRROLIDINE DERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTORS - The present invention relates to 3-aminopyrrolidine derivatives of the formula I: | 05-09-2013 |
20130116231 | TYROSINE KINASE INHIBITORS - The present invention relates to 1,4-dihydropyridazinone derivatives, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals. | 05-09-2013 |
20130123231 | ACC INHIBITORS AND USES THEREOF - The present invention provides compounds useful as inhibitors of Acetyl CoA Carboxylase (ACC), compositions thereof, and methods of using the same. | 05-16-2013 |
20130123232 | AZETIDINYL DIAMIDES AS MONOACYLGLYCEROL LIPASE INHIBITORS - Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: | 05-16-2013 |
20130123233 | AZETIDINYL DIAMIDES AS MONOACYLGLYCEROL LIPASE INHIBITORS - Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: | 05-16-2013 |
20130123234 | Aryl- or Heteroaryl-Substituted Benzene Compounds - The present invention relates to aryl- or heteroaryl-substituted benzene compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes. | 05-16-2013 |
20130131038 | N-CONTAINING HETEROARYL DERIVATIVES AS JAK3 KINASE INHIBITORS - N-containing heteroaryl derivatives of formula I or II, wherein the meanings for the various substituents are as disclosed in the description. These compounds are useful as JAK, particularly JAK3, kinase inhibitors. | 05-23-2013 |
20130131039 | 5,7-SUBSTITUTED-IMIDAZO[1,2-C]PYRIMIDINES AS INHIBITORS OF JAK KINASES - Compounds of Formula I: (Formula should be inserted here) and stereoisomers and pharmaceutically acceptable salts and solvates thereof in which R | 05-23-2013 |
20130131040 | PYRAZINE KINASE INHIBITORS - Provided are pyrazine compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibition Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity. | 05-23-2013 |
20130131041 | SPIROCYCLIC COMPOUNDS - The present invention relates to a novel class of substituted spirocyclic compounds. These compounds can inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the compounds of the instant invention and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of these compounds in vivo. | 05-23-2013 |
20130131042 | SPIROXAZOLIDINONE COMPOUNDS - Substituted spirocyclic amines of structural formula (I) are selective antagonists of the somatostatin subtype receptor 5 (SSTR5) and are useful for the treatment, control or prevention of disorders responsive to antagonism of SSTR5, such as Type 2 diabetes, insulin resistance, lipid disorders, obesity, atherosclerosis, Metabolic Syndrome, depression, and anxiety. | 05-23-2013 |
20130137673 | INHIBITORS OF JAK - The present invention is directed to compounds of formula I and tautomers and pharmaceutically acceptable salts thereof which are selective inhibitors of JAK. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition JAK activity, and methods to prevent or treat a number of conditions mediated at least in part by JAK activity. | 05-30-2013 |
20130137674 | AZETIDINYL DIAMIDES AS MONOACYLGLYCEROL LIPASE INHIBITORS - Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: | 05-30-2013 |
20130137675 | HETEROCYCLIC COMPOUND AND USE THEREOF - The present invention aims to provide a compound having a PDE inhibitory action and useful as a medicament for the prophylaxis or treatment of schizophrenia and the like. | 05-30-2013 |
20130143862 | CERTAIN AMINO-PYRIDAZINES, COMPOSITIONS THEREOF, AND METHODS OF THEIR USE - Provided are compounds of Formula I: | 06-06-2013 |
20130143863 | NEW BICYCLIC DIHYDROISOQUINOLINE-1-ONE DERIVATIVES - The invention provides novel compounds having the general formula (I) | 06-06-2013 |
20130150340 | 6-(4-Hydroxy-phenyl)-1H-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors - The present invention relates to 1H-pyrazolo[3,4-b]pyridine compounds of the formula I, | 06-13-2013 |
20130150341 | NOVEL COMPOUNDS - This invention relates to compounds of formula I | 06-13-2013 |
20130157996 | TRPM8 ANTAGONISTS AND THEIR USE IN TREATMENTS - Compounds of Formula I are useful as antagonists of TRPM8. Such compounds are useful in treating a number of TRPM8 mediated disorders and conditions and may be used to prepare medicaments and pharmaceutical compositions useful for treating such disorders and conditions. Examples of such disorders include, but are not limited to, migraines and neuropathic pain. Compounds of Formula I have the following structure: | 06-20-2013 |
20130157997 | BENZIMIDAZOLE ANALOGUES FOR THE TREATMENT OR PREVENTION OF FLAVIVIRUS INFECTIONS - Compounds represented by formula I: | 06-20-2013 |
20130157998 | HETEROCYCLIC INHIBITORS OF GLUTAMINASE - The invention relates to novel heterocyclic compounds and pharmaceutical preparations thereof. The invention further relates to methods of treatment using the novel heterocyclic compounds of the invention. | 06-20-2013 |
20130157999 | AMINOPYRIMIDINE DERIVATIVES AS LRRK2 MODULATORS - Specific Compounds of formula I: | 06-20-2013 |
20130158000 | Disubstituted benzothienyl-pyrrolotriazines and uses thereof - This invention relates to novel substituted 5-(1-benzothiophen-2-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives having protein tyrosine kinase inhibitory activities, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for treating proliferative disorders, in particular cancer and tumor diseases. | 06-20-2013 |
20130158001 | SUBSTITUTED 3-PHENYL-1,2,4-OXADIAZOLE COMPOUNDS - Disclosed are compounds of Formula (I): (I) or stereoisomers, salts, or prodrugs thereof, wherein: (i) R1 and R2 are independently C | 06-20-2013 |
20130165422 | HEXAFLUOROISOPROPYL CARBAMATE DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION - The disclosure relates to hexafluoroisopropyl carbamate derivatives of general formula (I): | 06-27-2013 |
20130165423 | SUBSTITUTED BENZIMIDAZOLES AND BENZOPYRAZOLES AS CCR(4) ANTAGONISTS - Benzimidazole, benzopyrazole and benzotriazole compounds are provided which bind to CCR(4) and are useful for the treatment of diseases such as allergic diseases, autoimmune diseases, graft rejection and cancer. | 06-27-2013 |
20130172314 | PYRAZOLO[3,4-d]PYRIMIDINE AND PYRROLO[2,3-d]PYRIMIDINE COMPOUNDS AS KINASE INHIBITORS - Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions. | 07-04-2013 |
20130172315 | SUBSTITUTED ANILINES AS CCR(4) ANTAGONISTS - Aniline compounds are provided which bind to CCR(4) and are useful for the treatment of diseases such as allergic diseases, autoimmune diseases, graft rejection and cancer. | 07-04-2013 |
20130178457 | CANNABINOID RECEPTOR MODULATORS - Compounds of Formula (I) along with processes for their preparation that are useful for treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of cannabinoid (CB) receptors. Methods of treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of cannabinoid (CB) receptors of Formula (I). | 07-11-2013 |
20130178458 | SUBSTITUTED (1-(METHYLSULFONYL)AZETIDIN-3-YL)(HETEROCYCLOALKYL)METHANONE ANALOGS AS ANTAGONISTS OF MUSCARINIC ACETYLCHOLINE M1 RECEPTORS - In one aspect, the invention relates to substituted (1-(methylsulfonyl)azetidin-3-yl)(heterocycloalkyl)methanone analogs, derivatives thereof, and related compounds, which are useful as antagonists of the muscarinic acetylcholine receptor M | 07-11-2013 |
20130184250 | Therapeutic Agents - Disclosed herein are azetidinyl compounds of formula I, | 07-18-2013 |
20130184251 | HETEROAROMATIC AND AROMATIC PIPERAZINYL AZETIDINYL AMIDES AS MONOACYLGLYCEROL LIPASE INHIBITORS - Disclosed are compounds, compositions and methods for treating diseases, syndromes, conditions and disorders that are affected by the inhibition of MGL, including pain. Such compounds are represented by Formula (I) as follows: | 07-18-2013 |
20130184252 | DIHYDROPYRROLONAPHTHYRIDINONE COMPOUNDS AS INHIBITORS OF JAK - Disclosed are JAK inhibitors of formula I | 07-18-2013 |
20130190289 | COMPOUNDS AND METHODS FOR THE TREATMENT OR PREVENTION OF FLAVIVIRUS INFECTIONS - A compound is represented by Structural Formula (I): | 07-25-2013 |
20130196964 | HETEROCYCLICALLY SUBSTITUTED ARYL COMPOUNDS AS HIF INHIBITORS - The present application relates to novel aryl compounds with heterocyclic substituents, processes for their preparation, their use for treatment and/or prevention of diseases and their use for the preparation of medicaments for treatment and/or prevention of diseases, in particular for treatment and/or prevention of hyperproliferative and angiogenic diseases and those diseases which arise from metabolic adaptation to hypoxic states. Such treatments can be carried out as monotherapy or also in combination with other medicaments or further therapeutic measures. | 08-01-2013 |
20130196965 | CYCLIC AMIDES - The invention relates to a compound of formula (I) | 08-01-2013 |
20130196966 | SPHINGOSINE 1 PHOSPHATE RECEPTOR MODULATORS AND METHODS OF CHIRAL SYNTHESIS - Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds are provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated. | 08-01-2013 |
20130196967 | HETEROCYCLIC COMPOUNDS AS INHIBITORS OF LEUKOTRIENE PRODUCTION - The present invention relates to compound of formula (I): | 08-01-2013 |
20130196968 | DI-AZETIDINYL DIAMIDE AS MONOACYLGLCEROL LIPASE INHIBITORS - Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: | 08-01-2013 |
20130196969 | DI-AZETIDINYL DIAMIDE AS MONOACYLGLCEROL LIPASE INHIBITORS - Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: | 08-01-2013 |
20130196970 | AMINO-PYRROLIDINE-AZETIDINE DIAMIDES AS MONOACYLGLYCEROL LIPASE INHIBITORS - Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds, and enantiomers, diastereomers, and pharmaceutically acceptable salts thereof, are represented by Formula (I) as follows: | 08-01-2013 |
20130196971 | FATTY ACID SYNTHASE INHIBITORS - This invention relates to the use of imidazole, triazole, and tetrazole derivatives for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of imidazoles, triazoles, and tetrazoles in the treatment of cancer. | 08-01-2013 |
20130196972 | NOVEL COMPOUND OF A REVERSE-TURN MIMETIC AND A PRODUCTION METHOD AND USE THEREFOR - This invention relates to novel compounds of reverse-turn mimetics, having pyrazino-triazinone as a basic framework, and a method of preparing the same, and the use thereof to treat diseases such as cancer, in particular, acute myeloid leukemia. | 08-01-2013 |
20130203729 | SOLUBLE GUANYLATE CYCLASE ACTIVATORS - The present invention relates to compounds of formula (I): | 08-08-2013 |
20130203730 | BENZOTHIAZOLES AS GHRELIN RECEPTOR MODULATORS - A compound of formula I | 08-08-2013 |
20130210799 | NOVEL AZETIDINE DERIVATIVES - The invention relates to a compound of formula (I) | 08-15-2013 |
20130210800 | PYRIDINE-2-DERIVATIVES AS SMOOTHENED RECEPTOR MODULATORS - The present application relates to compounds of Formula (I), and Formula (II), or pharmaceutically acceptable salt thereof, wherein A, X, Y, Z, e, f, R | 08-15-2013 |
20130217662 | METHOD OF TREATMENT USING SUBSTITUTED IMIDAZO[1,2B]PYRIDAZINE COMPOUNDS - Methods for treating a disease or disorder selected from pain, cancer, inflammation, neurodegenerative disease, Typanosoma cruzi infection and osteolytic disease in a mammal, which comprise administering to said mammal a therapeutically effective amount of a compound of Formula I | 08-22-2013 |
20130217663 | NOVEL S1P RECEPTOR MODULATING AGENT - An object of the present invention is to provide a compound having a modulating activity at an S1P receptor which is useful for preventing and treating autoimmune diseases, allergic diseases, and the like. According to the present invention, a compound represented by formula (I) or a pharmaceutically acceptable salt thereof is provided. | 08-22-2013 |
20130217664 | NOVEL COMPOUNDS USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES - Novel imidazolopyridines according to Formula I, able to inhibit JAK are disclosed, these compounds may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, allergic or inflammatory conditions, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons. | 08-22-2013 |
20130217665 | NOVEL PYRROLIDINE DERIVATIVES - The invention relates to a compound of formula (I) | 08-22-2013 |
20130217666 | TRICYCLIC COMPOUNDS AND METHODS OF USE THEREFOR - The invention relates to novel compounds of Formula I: | 08-22-2013 |
20130217667 | PHENOXY-AZETIDINE DERIVATIVES AS SPHINGOSINE 1-PHOSPHATE (S1P) RECEPTOR MODULATORS - The present invention relates to novel phenoxy-azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors. | 08-22-2013 |
20130217668 | BENZIMIDAZOLE AND AZABENZIMIDAZOLE COMPOUNDS THAT INHIBIT ANAPLASTIC LYMPHOMA KINASE - Compounds of Formula (I) are useful inhibitors of anaplastic lymphoma kinase. Compounds of Formula (I) have the following structure: where the definitions of the variables are provided herein. | 08-22-2013 |
20130217669 | AZETIDINYL DIAMIDES AS MONOACYLGLYCEROL LIPASE INHIBITORS - Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: | 08-22-2013 |
20130217670 | QUINOXALINE DERIVATIVES - Compounds of the formula I in which R, R | 08-22-2013 |
20130225551 | JAK2 INHIBITORS AND THEIR USE FOR THE TREATMENT OF MYELOPROLIFERATIVE DISEASES AND CANCER - The present invention provides compounds of formula I | 08-29-2013 |
20130225552 | HETEROBICYCLIC COMPOUNDS - Heterobicyclic compounds of Formula (I): | 08-29-2013 |
20130225553 | PYRAZOLOQUINOLINE COMPOUND - The present inventors have investigated a compound which has a PDE9-inhibiting action and is useful as an active ingredient for an agent for treating and/or preventing storage dysfunction, voiding dysfunction, bladder/urethral diseases, and the like, and thus, have found that a pyrazoloquinoline compound has a PDE9-inhibiting action, thereby completing the present invention. | 08-29-2013 |
20130231324 | SPIRO BICYCLIC DIAMINE DERIVATIVES AS HIV ATTACHMENT INHIBITORS - Compounds of Formula I, including pharmaceutically acceptable salts thereof: | 09-05-2013 |
20130231325 | ALDH-2 INHIBITORS IN THE TREATMENT OF ADDICTION - Disclosed are novel isoflavone derivatives having the structure of Formula I: | 09-05-2013 |
20130231326 | SELECTIVE SPHINGOSINE 1 PHOSPHATE RECEPTOR MODULATORS AND METHODS OF CHIRAL SYNTHESIS - Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds are provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated. | 09-05-2013 |
20130231327 | Substituted Spiro-Amide Compounds - Substituted spiro-amide compounds corresponding to formula I | 09-05-2013 |
20130237516 | AZAINDOLES USEFUL AS INHIBITORS OF JANUS KINASES - The present invention relates to compounds useful as inhibitors of protein kinases, particularly of JAK family kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. | 09-12-2013 |
20130237517 | AZETIDINYL DIAMIDES AS MONOACYLGLYCEROL LIPASE INHIBITORS - Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: | 09-12-2013 |
20130237518 | NOVEL COMPOUNDS THAT ARE ERK INHIBITORS - Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof, wherein: A is a five membered monocyclic heteroaryl ring; and B is a monocyclic heterocycloalkyl ring, or a monocyclic heterocycloalkenyl ring, or a bridged monocyclic heterocycloalkyl ring, or a fused (monocyclic heterocycloalkyl ring) cyclopropyl ring. Also disclosed are methods of treating cancer using the compounds of formula (1). | 09-12-2013 |
20130244996 | BENZODIOXANE INHIBITORS OF LEUKOTRIENE PRODUCTION - The present invention relates to compounds of formula (I): | 09-19-2013 |
20130244997 | AZETIDINYL DIAMIDES AS MONOACYLGLYCEROL LIPASE INHIBITORS - Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: | 09-19-2013 |
20130244998 | PIPERIDIN-4-YL-AZETIDINE DIAMIDES AS MONOACYLGLCEROL LIPASE INHIBITORS - Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds, and enantiomers, diastereomers, and pharmaceutically acceptable salts thereof, are represented by Formula (I) as follows: | 09-19-2013 |
20130244999 | Substituted Heterocyclic Compounds - The present invention relates to substituted heterocyclic compounds of Formula I: | 09-19-2013 |
20130245000 | BICYCLIC GPR119 MODULATORS - The present invention relates to compounds of Formula (I) that are useful for treating, preventing and/or managing the diseases, disorders, syndromes or conditions associated with the modulation of GPR119 receptor activity. The invention also relates to the process for preparation of the compounds, pharmaceutical compositions thereof. The invention further relates to methods of treating, preventing and/or managing diseases, disorders syndromes or conditions associated with the modulation of GPR119 receptor by using either alone or in combinations of Formula (I). | 09-19-2013 |
20130252936 | PYRAZOLOPYRIDAZINES AND METHODS FOR TREATING RETINAL-DEGENERATIVE DISEASES AND HEARING LOSS ASSOCIATED WITH USHER SYNDROME - Compounds, compositions and methods for the treatment of retinal degenerative diseases, such as retinitis pigmentosa, Leber's congenital Amaurosis, Syndromic retinal degenerations, age-related macular degeneration and Usher Syndrome, and hearing loss associated with Usher Syndrome are described herein. | 09-26-2013 |
20130261101 | BICYCLIC AZAHETEROCYCLOBENZYLAMINES AS PI3K INHIBITORS - The present invention provides bicyclic azaheterocyclobenzylamines of Formula I: | 10-03-2013 |
20130267493 | INDOLE AND INDAZOLE COMPOUNDS THAT ACTIVATE AMPK - The present invention relates to indole and indazole compounds of Formula (I) | 10-10-2013 |
20130267494 | 1,4-OXAZEPANE DERIVATIVES - Provided is a compound having a monoamine reuptake inhibitory activity, which is represented by the formula (I) wherein ring A is an optionally substituted 6-membered aromatic ring, ring B is the substituents on ring A are optionally bonded to form, together with ring A, an optionally substituted 9- or 10-membered aromatic fused ring, and other symbols are as defined in the specification, or a salt thereof. | 10-10-2013 |
20130274240 | FLUORENE COMPOUND AND PHARMACEUTICAL USE THEREOF - The present invention provides an agent for the prophylactic or treatment of diabetes, diabetic complications, insulin resistance syndrome, metabolic syndrome, hyperglycemia, dyslipidemia, atherosclerosis, cardiac failure, cardiomyopathy, myocardial ischemia, brain ischemia, cerebral apoplexy, pulmonary hypertension, hyperlactacidemia, mitochondrial disease, mitochondrial encephalomyopathy or cancer, namely, a PDHK inhibitor and the like. A compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof: | 10-17-2013 |
20130274241 | INDAZOLYL TRIAZOL DERIVATIVES - Compounds of Formula (I) | 10-17-2013 |
20130281428 | Pyridone Derivatives - Novel compounds or salts thereof, or crystals thereof, which inhibit Axl and are useful for treating diseases caused by Axl hyperfunction, diseases associated with Axl hyperfunction and/or diseases accompanied by Axl hyperfunction are provided. Pyridone derivatives represented by the formula (1) having various substituents or salts thereof, or crystals thereof (where R | 10-24-2013 |
20130281429 | 2,4-DIAMINO-PYRIMIDINES AS AURORA INHIBITORS - The present invention encompasses compounds of general formula (1) | 10-24-2013 |
20130281430 | Amino-Indolyl-Substituted Imidazolyl-Pyrimidines and Their Use as Medicaments - The invention relates to new amino-indole-substituted imidazolyl-pyrimidines of formula 1 | 10-24-2013 |
20130281431 | DNA-PK INHIBITORS - The present invention relates to compounds useful as inhibitors of DNA-PK. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. | 10-24-2013 |
20130289014 | Combination therapy in treatment of oncological and fibrotic diseases - The invention relates to new methods for the treatment of oncological and fibrotic disease comprising the combined administration of a cell signalling and/or angiogenesis inhibitor in conjunction with an Aurora kinase inhibitor. | 10-31-2013 |
20130289015 | N-CONTAINING HETEROARYL DERIVATIVES AS JAK3 KINASE INHIBITORS - N-containing heteroaryl derivatives of formula I or II, wherein the meanings for the various substituents are as disclosed in the description. These compounds are useful as JAK, particularly JAK3, kinase inhibitors. | 10-31-2013 |
20130296296 | 2-Carboxamide-7-Piperazinyl-Benzofuran Derivatives - The present invention relates to compounds of formula (I), | 11-07-2013 |
20130296297 | HETEROAROMATIC AND AROMATIC PIPERAZINYL AZETIDINYL AMIDES AS MONOACYLGLYCEROL LIPASE INHIBITORS - Disclosed are compounds, compositions and methods for treating diseases, syndromes, conditions and disorders that are affected by the inhibition of MGL, including pain. Such compounds are represented by Formula (I) as follows: | 11-07-2013 |
20130296298 | TRIAZOLOPYRIDAZINE COMPOUNDS, USE AS INHIBITORS OF THE KINASE LRRK2, AND METHODS FOR PREPARATION THEREOF - The present invention provides novel LRRK2 kinase inhibitors and methods of treating disease states using these inhibitors. | 11-07-2013 |
20130296299 | PYRROLO[2,3-b]PYRIDIN-4-YL-AMINES AND PYRROLO[2,3-b]PYRIMIDIN-5-YL-AMINES AS JANUS KINASE INHIBITORS - The present invention provides pyrrolo[2,3-b]pyridine-4-yl amines pyrrolo[2,3-b]pyrimidin-4-yl amines that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases and cancer. | 11-07-2013 |
20130296300 | QUINOLINES AND AZA-QUINOLINES AS CRTH2 RECEPTOR MODULATORS - The invention provides certain quinolines and aza-quinolines of the Formula (I), and their pharmaceutically acceptable salts, wherein E, J | 11-07-2013 |
20130303508 | NAMPT INHIBITORS - Disclosed are compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed. | 11-14-2013 |
20130303509 | NAMPT INHIBITORS - Disclosed are compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed. | 11-14-2013 |
20130303510 | NAMPT INHIBITORS - Disclosed are compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed. | 11-14-2013 |
20130303511 | NAMPT INHIBITORS - Disclosed are compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed. | 11-14-2013 |
20130303512 | Use of modulators of CCR5 in the treatment of Cancer and cancer metastasis - This disclosure is directed, in part, to a method of determining whether a subject having cancer is at risk for developing metastasis of the cancer. In one embodiment, the method comprises (a) obtaining a biological sample from the subject having cancer; (b) determining CCR5 expression level and/or expression level of at least one of CCR5 ligands in the biological sample; and (c) if the expression level of CCR5 and/or of at least one of CCR5 ligands determined in step (b) is increased compared to CCR5 expression level and/or expression level of at least one of CCR5 ligands in a control sample, then the subject is identified as likely at risk for developing metastasis of the cancer. | 11-14-2013 |
20130303513 | NOVEL AZETIDINE DERIVATIVES AS SPHINGOSINE 1-PHOSPHATE (S1P) RECEPTOR MODULATORS - The present invention relates to novel azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors. | 11-14-2013 |
20130303514 | 2-METHOXY-PYRIDIN-4-YL-DERIVATIVES - The invention relates to pyridine derivatives of Formula (I) | 11-14-2013 |
20130303515 | NOVEL COMPOUNDS USEFUL FOR THE TREATMENT OF METABOLIC AND INFLAMMATORY DISEASES - Compounds are disclosed that have a formula represented by the following: | 11-14-2013 |
20130303516 | NOVEL TRIAZINE COMPOUNDS - The present invention relates to novel triazine compounds of formula (1), methods of their preparation, pharmaceutical compositions containing these compounds and the use of these compounds to treat proliferative disorders such as tumors and cancers and also other conditions and disorders related to or associated with dysregulation of PI3 Kinases, PI3 Kinase pathway, mTOR and/or the mTOR pathway. | 11-14-2013 |
20130303517 | QUINOXALINES AND AZA-QUINOXALINES AS CRTH2 RECEPTOR MODULATORS - The invention provides certain quinoxalines and aza-quinoxalines of the Formula (I), and their pharmaceutically acceptable salts, wherein J | 11-14-2013 |
20130310361 | COMPOUNDS AND COMPOSITIONS AS KINASE INHIBITORS - The invention provides novel pyrimidine derivatives and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of insulin-like growth factor (IGF-1R) or analplastic lymphoma kinase (ALK). | 11-21-2013 |
20130324515 | IMIDAZOTRIAZINES AND IMIDAZOPYRIMIDINES AS KINASE INHIBITORS - The present invention is directed to imidazo[1,2-b][1,2,4]triazines and imidazo[1,2-a]pyrimidines, and pharmaceutical compositions thereof, which are inhibitors of kinases such as c-Met and are useful in the treatment of cancer and other diseases related to the dysregulation of kinase pathways. | 12-05-2013 |
20130324516 | AMINOQUINAZOLINE AND PYRIDOPYRIMIDINE DERIVATIVES - The invention provides novel compounds having the general formula: | 12-05-2013 |
20130324517 | CYCLIC PYRIMIDIN-4-CARBOXAMIDES AS CCR2 RECEPTOR ANTAGONISTS FOR TREATMENT OF INFLAMMATION, ASTHMA AND COPD - The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD. | 12-05-2013 |
20130331371 | Azetidine Derivatives - Compounds of formula (I) are inhibitors of fatty acid amide hydrolase, (FAAH), and which are useful in the treatment of diseases or medical conditions which benefit from inhibition of FAAH activity, such as anxiety, depression pain, inflammation, and eating, sleep, neurodegenerative and movement disorders: | 12-12-2013 |
20130331372 | Cyclic Amine Substituted Oxazolidinone CETP Inhibitor - Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compound of Formula I, A | 12-12-2013 |
20130331373 | SUBSTITUTED BICYCLIC METHYL AZETIDINES AS SPHINGOSINE-1 PHOSPHATE RECEPTORS MODULATORS - The present invention relates to novel substituted bicyclic methyl azetidine derivatives which are useful as sphingosine-1-phosphate receptors modulators and useful for treating a wide variety of disorders associated with modulation of sphingosine-1-phosphate receptors. | 12-12-2013 |
20130338132 | HETEROARYLCARBOXYLIC ACID ESTER DERIVATIVE - Compounds represented by the following formula (I), | 12-19-2013 |
20130338133 | SUBSTITUTED IMIDAZOPYRIDAZINES - The present invention relates to substituted imidazopyridazine compounds of general formula (I), which are Mps-1 (Monopolar Spindle 1) Kinase inhibitors (also known as Tyrosine Threonine Kinase, TTK) in which R | 12-19-2013 |
20130338134 | SUBSTITUTED TRICYCLIC COMPOUNDS AS FGFR INHIBITORS - The present invention relates to tricyclic compounds, and pharmaceutical compositions of the same, that are inhibitors of one or more FGFR enzymes and are useful in the treatment of FGFR-associated diseases such as cancer. | 12-19-2013 |
20130338135 | PHENYL BICYCLIC METHYL AZETIDINE DERIVATIVES AS SPHINGOSINE-1 PHOSPHATE RECEPTORS MODULATORS - The present invention relates to novel phenyl bicyclic methyl azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors. | 12-19-2013 |
20130338136 | NOVEL INDOLE MODULATORS OF S1P RECEPTORS - The present invention relates to novel indole derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors. | 12-19-2013 |
20130345191 | 1,2,4-TRIAZINE-6-CARBOXAMIDE KINASE INHIBITORS - Provided are triazine compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibiting Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity. | 12-26-2013 |
20130345192 | HETEROCYCLIC TYROSINE KINASE INHIBITORS - The present invention provides compounds useful as inhibitors of Tec family kinases, compositions thereof, and methods of using the same. | 12-26-2013 |
20130345193 | COMPOUNDS THAT MODULATE INTRACELLULAR CALCIUM - Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity. | 12-26-2013 |
20130345194 | SUBSTITUTED CYCLOPENTYL-AZINES AS CASR-ACTIVE COMPOUNDS - The invention relates to compounds of general Formula (I), Wherein R | 12-26-2013 |
20140005163 | 1H-IMIDAZO[4,5-C]QUINOLINONE DERIVATIVES | 01-02-2014 |
20140005164 | WNT PATHWAY ANTAGONISTS | 01-02-2014 |
20140005165 | SUBSTITUTED 3-AZABICYCLO[3.1.0]HEXANE DERIVATIVES USEFUL AS CCR2 ANTAGONISTS | 01-02-2014 |
20140011800 | PYRROLOPYRIDAZINE JAK3 INHIBITORS AND THEIR USE FOR THE TREATMENT OF INFLAMMATORY AND AUTOIMMUNE DISEASES - The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of JAK3, thereby making them useful for the treatment of inflammatory and autoimmune diseases. | 01-09-2014 |
20140018343 | IRAK INHIBITORS AND USES THEREOF - The present invention provides arylo-fused thienopyrimidine compounds, compositions thereof, and methods of using the same. | 01-16-2014 |
20140031333 | COMPOUNDS AND COMPOSITIONS AS C-KIT KINASE INHIBITORS - The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of c-kit or c-kit and PDGFR (PDGFRα, PDGFRβ) kinases. | 01-30-2014 |
20140031334 | DERIVATIVES OF 4-PIPERAZIN-1-YL-4-BENZO[B]THIOPHENE SUITABLE FOR THE TREATMENT OF CNS DISORDERS - A heterocyclic compound or a salt thereof represented by the formula (1): | 01-30-2014 |
20140031335 | CYCLOALKENYL ARYL DERIVATIVES FOR CETP INHIBITOR - The present invention relates to cycloalkenyl aryl derivatives, isomers thereof, pharmaceutically acceptable salts thereof, hydrates thereof, or solvates thereof; a method for preparing the derivatives; and pharmaceutical compositions containing the same. The compounds of the present invention show the effect of CETP activity inhibition. It means that the compounds can increase HDL-cholesterol and decrease LDL-cholesterol. | 01-30-2014 |
20140031336 | Tetrahydroquinoline Derivatives Useful As Bromodomain Inhibitors - Tetrahydroquinoline compounds, pharmaceutical compositions containing such compounds and their use in therapy. | 01-30-2014 |
20140038935 | DIHYDRODIAZEPINES USEFUL AS INHIBITORS OF PROTEIN KINASES - The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions. | 02-06-2014 |
20140038936 | ISOINDOLINONE INHIBITORS OF PHOSPHATIDYLINOSITOL 3-KINASE - The present invention relates to compounds useful as inhibitors of PI3K, particularly of PI3Kγ. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. | 02-06-2014 |
20140038937 | Chromenone Derivatives - The invention concerns chromenone compounds of Formula I; | 02-06-2014 |
20140038938 | Substituted dihydropyrazolones and their use - The present application relates to novel substituted dihydropyrazolone derivatives, processes for their preparation, their use for treatment and/or prophylaxis of diseases and their use for the preparation of medicaments for treatment and/or prophylaxis of diseases, in particular cardiovascular and haematological diseases and kidney diseases, and for promoting wound healing. | 02-06-2014 |
20140038939 | TRIAZOLOPYRIDINE JAK INHIBITOR COMPOUNDS AND METHODS - A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R | 02-06-2014 |
20140045811 | AMIDE, UREA OR SULFONE AMIDE LINKED BENZOTHIAZOLE INHIBITORS OF ENDOTHELIAL LIPASE - The present invention provides compounds of Formula (I): | 02-13-2014 |
20140045812 | 5-CYANO-4- (PYRROLO [2,3B] PYRIDINE-3-YL) -PYRIMIDINE DERIVATIVES USEFUL AS PROTEIN KINASE INHIBITORS - The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions. | 02-13-2014 |
20140045813 | HETEROAROMATIC COMPOUNDS AS BTK INHIBITORS - The present invention encompasses compounds of the formula (I) | 02-13-2014 |
20140045814 | PYRAZINE DERIVATIVES AS FGFR INHIBITORS - The present invention relates to pyrazine derivatives, and pharmaceutical compositions including the same, that are inhibitors of one or more FGFR enzymes and are useful in the treatment of FGFR-associated diseases such as cancer. | 02-13-2014 |
20140051675 | MODULATORS OF CELLULAR ADHESION - The present invention provides compounds having formula (I): | 02-20-2014 |
20140051676 | Triazine-oxadiazoles - The invention relates to new derivatives of formula (I), | 02-20-2014 |
20140051677 | NOVEL COMPOUND USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES - Novel pyrrazolopyridines according to Formula I, able to inhibit JAK are disclosed, these compounds may be prepared as a pharmaceutical composition, and may be used for the prophylaxis and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, allergy, inflammatory conditions, autoimmune diseases, proliferative diseases, transplant rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons. | 02-20-2014 |
20140057891 | Substituted 6,5-Fused Bicyclic Heteroaryl Compounds - The present invention relates to substituted 6,5-fused bicyclic heteroaryl compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. | 02-27-2014 |
20140057892 | PROLYL HYDROXYLASE INHIBITORS AND METHODS OF USE - The present disclosure relates to HIF-1α prolyl hydroxylase inhibitors, compositions which comprise the HIF-1α prolyl hydroxylase inhibitors described herein and to methods for controlling, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD) heart failure, ischemia, and anemia. | 02-27-2014 |
20140057893 | SUBSTITUTED CYCLOPROPLY COMPOUNDS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF TREATMENT - Substituted cyclopropyl compounds of the formula I: and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included | 02-27-2014 |
20140066424 | HETEROCYCLIC MODULATORS OF HIF ACTIVITY FOR TREATMENT OF DISEASE - The present invention relates to compounds and methods which may be useful as inhibitors of HIF pathway activity for the treatment or prevention of cancer and other hypoxia-mediated diseases. | 03-06-2014 |
20140066425 | ANDROGEN RECEPTOR ANTAGONISTS AND USES THEREOF - Disclosed are substituted thioimidazolidinone compounds and pharmaceutical compositions comprising such compounds. The compounds and compositions can be used for treatment of androgen receptor-associated diseases or disorders, such as prostate cancer, benign prostatic hypertrophy, male hair loss and hypertrichosis. | 03-06-2014 |
20140066426 | FLUOROMETHYL-SUBSTITUTED PYRROLE CARBOXAMIDES - The invention relates to pyrrole carboxamides bearing a fluoromethyl-moiety as voltage gated calcium channel blockers, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders. | 03-06-2014 |
20140066427 | S1P Receptors Modulators and Their Use Thereof - The invention relates to novel compounds that have SIP receptor modulating activity. Further, the invention relates to a pharmaceutical comprising at least one compound of the invention for the treatment of diseases and/or conditions caused by or associated with inappropriate SIP receptor modulating activity or expression, for example, autoimmune response. A further aspect of the invention relates to the use of a pharmaceutical comprising at least one compound of the invention for the manufacture of a medicament for the treatment of diseases and/or conditions caused by or associated with inappropriate SIP receptor modulating activity or expression such as autoimmune response. | 03-06-2014 |
20140066428 | 6,7,8,9-Tetrahydro-5H-1,4,7,10a-tetraaza-cyclohept[f]indene derivatives, pharmaceutical compositions containing these compounds, their use and processes for preparing them - The present invention relates to compounds defined by formula I | 03-06-2014 |
20140073624 | Biaryl Heterocyclic Compounds and Methods of Making and Using the Same - The present invention relates generally to the field of anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. More particularly, the invention relates to a family of compounds having both a biaryl moiety and at least one heterocylic moiety that are useful as such agents. | 03-13-2014 |
20140073625 | NOVEL N-(4-(AZETIDINE-1-CARBONYL) PHENYL) - (HETERO-) ARYLSULFONAMIDE DERIVATIVES AS PYRUVATE KINASE M2 (PMK2) MODULATORS - Compounds of general Formula (I), and compositions comprising compounds of general formula I that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that modulate PKM2 in the treatment of cancer. | 03-13-2014 |
20140073626 | AZAINDOLE DERIVATIVES AS TYROSINE KINASE INHIBITORS - The present disclosure provides compounds and pharmaceutically acceptable salts that are tyrosine kinase inhibitors, in particular BLK, BMX, EGFR, HER2, HER4, ITK, JAK3, TEC, Btk, and TXK and are therefore useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as cancer and inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and pharmaceutically acceptable salts and processes for preparing such compounds and pharmaceutically acceptable salts. | 03-13-2014 |
20140080803 | NOVEL TRPV3 MODULATORS - Disclosed herein are modulators of TRPV3 of Formula (I) | 03-20-2014 |
20140080804 | NOVEL 6-ARYLAMINO PYRIDONE CARBOXAMIDE AS MEK INHIBITORS - The invention provides novel substituted 6-arylamino pyridone carboxamides represented by Formula I, or a pharmaceutically acceptable salt, solvate, poly-morph, ester, tautomer or prodrug thereof, and a composition comprising these compounds. The compounds provided can be used as inhibitors of MEK and are useful in the treatment of inflammatory diseases, cancer and other hyperproliferative diseases. The invention further provides a method of treatment for inflammatory diseases, cancer and other hyperproliferative diseases in mammals, especially humans. | 03-20-2014 |
20140080805 | PYRROLIDINE INHIBITORS OF IAP - The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: | 03-20-2014 |
20140088075 | DIHYDRONAPHTHYRIDINES AND RELATED COMPOUNDS USEFUL AS KINASE INHIBITORS FOR THE TREATMENT OF PROLIFERATIVE DISEASES - The invention relates to dihydronaphthyridines and related compounds; compositions comprising an effective amount of a dihydronaphthyridine or a related compound; and methods for treating or preventing proliferative diseases comprising the administration of an effective amount of a dihydronaphthyridine or a related compound. | 03-27-2014 |
20140088076 | SUBSTITUTED 6,6-FUSED NITROGENOUS HETEROCYCLIC COMPOUNDS AND USES THEREOF - The invention provides novel compounds having the general formula: | 03-27-2014 |
20140100211 | New pyrrolidine derivatives, pharmaceutical compositions and uses thereof - Pyrrolidine derivatives of the formula | 04-10-2014 |
20140100212 | COMPOUNDS AS TYROSINE KINASE MODULATORS - The present invention is directed to novel compounds of Formula I. The compounds of the present invention are potent tyrosine kinase modulators, and are suitable for the treatment and prevention of diseases and conditions related to abnormal activities of tyrosine kinase receptors. | 04-10-2014 |
20140100213 | TRIAZOLONES AS FATTY ACID SYNTHASE INHIBITORS - This invention relates to the use of triazolone derivatives for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of triazolones in the treatment of cancer. | 04-10-2014 |
20140100214 | HETEROCYCLIC COMPOUNDS AND USES THEREOF - Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including P13 kinase activity, are described herein. | 04-10-2014 |
20140100215 | Methods of Using PI3K and MEK Modulators - The invention provides methods of treating cancer with a combination of compounds which inhibit kinases, more specifically MEK and PI3K. | 04-10-2014 |
20140107094 | METHYLENE LINKED QUINOLINYL MODULATORS OF RORyt - The present invention comprises compounds of Formula I. | 04-17-2014 |
20140113890 | NEW 4-AMINO-4-OXOBUTANOYL PEPTIDES AS INHIBITORS OF VIRAL REPLICATION - The invention provides 4-amino-4-oxobutanoyl peptides of Formula I | 04-24-2014 |
20140121194 | METHOD FOR ADMINISTERING AGENT FOR CONTROLLING ECTOPARASITE TO DOG - There is provided a method for controlling an animal ectoparasite having excellent controlling effects. The method for controlling an ectoparasite of dogs comprises orally administering an ectoparasite-controlling agent comprising as an active ingredient an isoxazoline compound represented by formula (I): | 05-01-2014 |
20140121195 | SUBSTITUTED BENZIMIDAZOLES AND BENZOPYRAZOLES AS CCR(4) ANTAGONISTS - Benzimidazole, benzopyrazole and benzotriazole compounds are provided which bind to CCR(4) and are useful for the treatment of diseases such as allergic diseases, autoimmune diseases, graft rejection and cancer. | 05-01-2014 |
20140121196 | DISPIROPYRROLIDINE DERIVATIVES - A compound that inhibits interaction between, murine double minute 2 (Mdm2) protein and p53 protein and exhibits anti-tumor activity is provided. The present invention provides a dispiropyrrolidine derivative represented by the following formula (1), which has various substituents, inhibits interaction between Mdm2 protein and p53 protein and exhibits anti-tumor activity, wherein R | 05-01-2014 |
20140128365 | PYRIDONE/HYDROXYPYRIDINE 11-BETA HYDROXYSTEROID DEHYDROGENASE TYPE I INHIBITORS - Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure: | 05-08-2014 |
20140128366 | 1,3,4-OXADIAZOLES-2-THIO AZETIDINE DERIVATIVES AS SPHINGOSINE-1 PHOSPHATE RECEPTORS MODULATORS - The present invention relates to substituted 1,3,4-oxadiazoles-2-thio azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors. | 05-08-2014 |
20140128367 | CYCLOALKYL-FUSED TETRAHYDROQUINOLINES AS CRTH2 RECEPTOR MODULATORS - The invention provides certain cycloalkyl-fused tetrahydroquinolines of the Formula (I), and their pharmaceutically acceptable salts and esters, wherein R | 05-08-2014 |
20140128368 | SUBSTITUTED CYCLOPROPYL COMPOUNDS, COMPOSITIONS CONTAINING SUCH COMPOUNDS, AND METHODS OF TREATMENT - Substituted cyclopropyl compounds of the formula I: and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included. | 05-08-2014 |
20140128369 | NOVEL BENZYL AZETIDINE DERIVATIVES AS SPHINGOSINE 1-PHOSPHATE (S1P) RECEPTOR MODULATORS - The present invention relates to novel benzyl azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors. | 05-08-2014 |
20140128370 | Tetrahydro-Pyrido-Pyrimidine Derivatives - The invention relates to substituted tetrahydro-pyrido-pyrimidine derivatives of the formula (I), | 05-08-2014 |
20140128371 | CHEMICAL COMPOUNDS 542 - The present invention relates to compounds of Formula (I): | 05-08-2014 |
20140135306 | HDYROXY SUBSTITUTED ISOQUINOLINONE DERIVATIVES - The invention relates to compounds of formula (I): as defined in the application. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of MDM2 and/or MDM4, or variants thereof. | 05-15-2014 |
20140135307 | CO-CRYSTALS AND SALTS OF CCR3-INHIBITORS - This invention relates to co-crystals and salts of CCR3 inhibitors of formula 1, | 05-15-2014 |
20140135308 | BENZOXEPIN PI3K INHIBITOR COMPOUNDS AND METHODS OF USE - Benzoxepin compounds of Formula I, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, wherein: Z | 05-15-2014 |
20140142084 | NITROGEN-CONTAINING AROMATIC HETEROCYCLIC COMPOUND - Provided is a compound useful as a prophylactic and/or therapeutic agent for bladder cancer. | 05-22-2014 |
20140142085 | COMPOUNDS FOR THE TREATMENT OF HIV - The invention provides compounds of formula (I): or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula (I), processes for preparing compounds of formula (I), intermediates useful for preparing compounds of formula I and therapeutic methods for treating a Retroviridae viral infection including an infection caused by the HIV virus. | 05-22-2014 |
20140148432 | Compounds for the Treatment of Neurological Disorders - Provided are compounds, pharmaceutical compositions and methods of treatment or prophylaxis of certain neurologic disorders, including disorders related to NMDA receptor activation, including neuropsychiatric disorders, neurodegenerative diorders and other neurologic diseases, disorders and conditions including stroke, brain injury, epilepsy, neuropsychiatric disorders, mood disorders, chronic pain and related conditions. The compounds are of the general Formula I, or a pharmaceutically acceptable salt, ester, prodrug or derivative thereof are provided: | 05-29-2014 |
20140155372 | COMBINATIONS OF AKT AND MEK INHIBITOR COMPOUNDS, AND METHODS OF USE - The invention provides combinations comprising a) compound of formula I: (formula I), or a pharmaceutically acceptable salt thereof; and another agent selected from GDC-0973, PD-0325901, or a pharmaceutically acceptable salt thereof. The combinations are particularly useful for treating hyperproliferative disorders, such as cancer. | 06-05-2014 |
20140155373 | NOVEL COMPOUNDS - Compounds of formula (I) described herein are both inhibitors of the phosphodiesterase 4 (PDE4) enzyme and muscarinic M3 receptor antagonists, and are useful for the prevention and/or treatment of diseases of the respiratory tract characterized by airway obstruction. | 06-05-2014 |
20140155374 | METHODS OF USING PYRUVATE KINASE ACTIVATORS - Described herein are methods for using compounds that activate pyruvate kinase. | 06-05-2014 |
20140155375 | NOVEL COMPOUNDS - The present invention relates to novel NADPH oxidase II inhibitors and their use in the treatment of diseases mediated by the NADPH oxidase enzymes. | 06-05-2014 |
20140155376 | PYRROLOPYRAZINE KINASE INHIBITORS - The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, | 06-05-2014 |
20140155377 | 3-CYCLOALKYLAMINOPYRROLIDINE DERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTORS - The present invention relates to 3-cycloalkylaminopyrrolidine derivatives of the formula I: | 06-05-2014 |
20140163000 | COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE - The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. | 06-12-2014 |
20140163001 | HETEROCYCLIC COMPOUND - Provided is a heterocyclic compound having an RORγt inhibitory activity. A compound represented by the formula (I): | 06-12-2014 |
20140163002 | CYCLIC P1 LINKERS AS FACTOR XIA INHIBITORS - The present invention provides compounds of Formula (Ia): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same. | 06-12-2014 |
20140171403 | Autotaxin inhibitors - The present invention relates to novel compounds that are autotaxin inhibitors, processes for their preparation, pharmaceutical compositions and medicaments containing them and to their use in diseases and disorders mediated by autotaxin. | 06-19-2014 |
20140171404 | Autotaxin inhibitors - The present invention relates to novel compounds that are autotaxin inhibitors, processes for their preparation, pharmaceutical compositions and medicaments containing them and to their use in the treatment of an ATX-dependent or ATX-mediated disease or condition. | 06-19-2014 |
20140171405 | Fused Pyrazoles as FGFR Inhibitors - The present invention relates to fused pyrazole derivatives, and pharmaceutical compositions including the same, that are inhibitors of one or more FGFR enzymes and are useful in the treatment of FGFR-associated diseases such as cancer. | 06-19-2014 |
20140171406 | TRPM8 ANTAGONISTS AND THEIR USE IN TREATMENTS - Compounds of Formula I are useful as antagonists of TRPM8. Such compounds are useful in treating a number of TRPM8 mediated disorders and conditions and may be used to prepare medicaments and pharmaceutical compositions useful for treating such disorders and conditions. Examples of such disorders include, but are not limited to, migraines and neuropathic pain. Compounds of Formula I have the following structure: | 06-19-2014 |
20140179666 | BICYCLIC HETEROCYCLE COMPOUNDS AND THEIR USES IN THERAPY - The invention relates to bicyclic heterocycle compounds of formula (I): or tautomeric or stereochemically isomeric forms, N-oxides, pharmaceutically acceptable salts or the solvates thereof; wherein R | 06-26-2014 |
20140179667 | ARYL AND HETEROARYL FUSED LACTAMS - This invention relates to compounds of general formula (I) | 06-26-2014 |
20140179668 | FUSED PYRIMIDINE COMPOUNDS AND USE THEREOF - Fused pyrimidine compounds as kinase inhibitors, such as multi-kinase inhibitors, are provided. Fused pyrimidine compounds as IGF-IR inhibitors are provided. The compounds may be used in a method of treating cancer. Pharmaceutical compositions containing a fused pyrimidine compound and a pharmaceutically acceptable carrier are also provided, as are kits containing a fused pyrimidine compound or salt thereof and instructions for use, e.g., in a method of treating cancer. | 06-26-2014 |
20140179669 | Alicyclic carboxylic acid derivatives of benzomorphans and related scaffolds, medicaments containing such compounds and their use - The present invention relates to compounds defined by formula I | 06-26-2014 |
20140179670 | URACIL DERIVATIVE AND USE THEREOF FOR MEDICAL PURPOSES - The present invention provides: an uracil derivative represented by general formula (I) or a physiologically acceptable salt thereof (in the formula, R | 06-26-2014 |
20140187533 | BENZIMIDAZOLE INHIBITORS OF THE SODIUM CHANNEL - The invention relates to compounds useful in treating conditions associated with voltage-gated ion channel function, particularly conditions associated with sodium channel activity. More specifically, the invention concerns compounds (e.g., compounds according to any of Formulas (I)-(XIII) or Compounds (1)-(236) of Table 1) that are useful in treatment of a variety of diseases and conditions. Formula (I) | 07-03-2014 |
20140187534 | NITROGEN-CONTAINING SPIROCYCLIC COMPOUNDS AND PHARMACEUTICAL USES THEREOF - A compound of the following general formula [I]: | 07-03-2014 |
20140194403 | METHOD OF TREATMENT USING SUBSTITUTED PYRAZOLO[1,5-a]PYRIMIDINE COMPOUNDS - Provided herein are methods for treating pain, cancer, inflammation, neurodegenerative disease or Typanosoma cruzi infection in a mammal, which comprises administering to said mammal in need thereof a therapeutically effective amount of a compound of Formula I: | 07-10-2014 |
20140194404 | AMIDOPYRAZOLE INHIBITORS OF INTERLEUKIN RECEPTOR-ASSOCIATED KINASES - This invention relates to amidopyrazole compounds that are inhibitors of Interleukin receptor-associated kinases, in particular IRAK-4, and are useful in the treatment of cellular proliferative diseases, for example, cancer, hyperplasia, restenosis, cardiac hypertrophy, immune disorders and inflammation. | 07-10-2014 |
20140194405 | CYCLOPROPYL DICARBOXAMIDES AND ANALOGS EXHIBITING ANTI-CANCER AND ANTI-PROLIFERATIVE ACTIVITIES - The disclosed compounds are useful in the treatment of mammalian cancers and especially human cancers. Compounds, pharmaceutical compositions, and methods of Formula I are disclosed: | 07-10-2014 |
20140194406 | ALKYNYL SUBSTITUTED PYRIMIDINYL-PYRROLES ACTIVE AS KINASES INHIBITORS - The present invention relates to alkynyl substituted pyrimidinyl-pyrrole compounds which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular Jak and/or Src family kinases. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such compounds or the pharmaceutical compositions containing them. | 07-10-2014 |
20140200206 | SUBSTITUTED PYRROLOPYRIMIDINE COMPOUNDS, COMPOSITIONS THEREOF, AND METHODS OF TREATMENT THEREWITH - Provided herein are Pyrrolopyrimidine Compounds having the following structure: | 07-17-2014 |
20140200207 | SUBSTITUTED PYRROLOPYRIMIDINE COMPOUNDS, COMPOSITIONS THEREOF, AND METHODS OF TREATMENT THEREWITH - Provided herein are Pyrrolopyrimidine Compounds having the following structure: | 07-17-2014 |
20140206662 | Imidazopyridine Compounds - A method of treating inflammation, an inflammatory disease, an immune or an autoimmune disorder comprising administering to a patient in need thereof compounds of formula (I): | 07-24-2014 |
20140206663 | TRIAZINONE COMPOUNDS - The invention provides a compound of Formula (I) | 07-24-2014 |
20140213572 | UNSATURATED NITROGEN HETEROCYCLIC COMPOUNDS USEFUL AS PDE10 INHIBITORS - Unsaturated nitrogen heterocyclic compounds of formula (I): | 07-31-2014 |
20140213573 | NOVEL BENZYL AZETIDINE DERIVATIVES AS SPHINGOSINE 1-PHOSPHATE (S1P) RECEPTOR MODULATORS - The present invention relates to novel benzyl azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors. | 07-31-2014 |
20140213574 | HETEROARYL COMPOUNDS AND USES THEREOF - The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same. | 07-31-2014 |
20140213575 | 6H-Thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepines - The invention relates to 6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepines, in particular for therapeutic purposes, pharmaceutical agents and use thereof in therapy, in particular for the prevention and treatment of tumour diseases. | 07-31-2014 |
20140221335 | SUBSTITUTED BICYCLIC DIHYDROPYRIMIDINONES AND THEIR USE AS INHIBITORS OF NEUTROPHIL ELASTASE ACTIVITY - This invention relates to substituted bicyclic dihydropyrimidinones of formula 1 | 08-07-2014 |
20140221336 | COMPOUNDS USEFUL AS INHIBITORS OF JANUS KINASES - The present invention relates to compounds useful as inhibitors of protein kinases, particularly of JAK family kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. | 08-07-2014 |
20140221337 | Potassium Channel Blockers - The present invention provides a compound of formula (I) | 08-07-2014 |
20140221338 | NOVEL MACROCYCLES AS FACTOR XIA INHIBITORS - The present invention provides compounds of Formula (Ia): or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same. | 08-07-2014 |
20140221339 | Heterocyclic Derivative and Pharmaceutical Drug - The present invention provides a novel heterocyclic derivative or a pharmaceutically acceptable salt thereof. For example, the present invention provides a heterocyclic derivative of the general formula [1] or its tautomer, or a pharmaceutically acceptable salt thereof: | 08-07-2014 |
20140221340 | CHEMOKINE RECEPTOR ACTIVITY REGULATOR - The invention provides a chemokine receptor activity modulator containing a pyrazolopyrimidine derivative represented by the formula (I) | 08-07-2014 |
20140221341 | BICYCLIC COMPOUNDS AND THEIR USE AS ANTIBACTERIAL AGENTS AND BETALACTAMASE INHIBITORS - A compound of formula (I): | 08-07-2014 |
20140235612 | Azabenzimidazole Compounds - The present invention is directed to compounds of formula I: | 08-21-2014 |
20140235613 | SUBSTITUTED DIARYL AZETIDINE DERIVATIVES AS SPHINGOSINE RECEPTOR MODULATORS - The present invention relates to substituted diaryl azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors. | 08-21-2014 |
20140243305 | AZETIDINYL DIAMIDES AS MONOACYLGLYCEROL LIPASE INHIBITORS - Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: | 08-28-2014 |
20140243306 | NOVEL PYRROLO PYRIMIDINE DERIVATIVES - The present invention describes new pyrrolo pyrimidine derivatives and pharmaceutically acceptable salts thereof which appear to interact with Bruton's tyrosine kinase (Btk). Accordingly, the novel pyrrolo pyrimidines may be effective in the treatment of autoimmune disorders, inflammatory diseases, allergic diseases, airway diseases, such as asthma and chronic obstructive pulmonary disease (COPD), transplant rejection, cancers e.g. of hematopoietic origin or solid tumors. | 08-28-2014 |
20140243307 | PYRAZOLE AZETIDINE DERIVATIVES AS SPHINGOSINE 1-PHOSPHATE (S1P) RECEPTOR MODULATORS - The present invention relates to pyrazole azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors. | 08-28-2014 |
20140243308 | SUBSTITUTED IMIDAZOPYRIDAZINES AND BENZIMIDAZOLES AS INHIBITORS OF FGFR3 - The present invention relates to substituted imidazopyridazines and substituted benzimidazoles, as well as pharmaceutical compositions comprising the same, which are FGFR3 inhibitors useful in the treatment of cancer and other diseases. | 08-28-2014 |
20140243309 | CYCLOALKYLNITRILE PYRAZOLE CARBOXAMIDES AS JANUS KINASE INHIBITORS - The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer. | 08-28-2014 |
20140243310 | BICYCLIC COMPOUND - The present invention provides a compound represented by the formula (I): | 08-28-2014 |
20140249130 | BIPYRIDYLAMINOPYRIDINES AS SYK INHIBITORS - The present invention provides novel pyrimidine amines of formula I which are potent inhibitors of spleen tyrosine kinase, or are prodrugs thereof, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis and cancer. | 09-04-2014 |
20140249131 | Substituted 7-Oxo-Pyrido[2,3-d]Pyrimidines and Methods of Use - The invention encompasses compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions, uses and methods for prophylaxis and treatment of cancer. | 09-04-2014 |
20140249132 | USE OF PYRAZOLOPYRIMIDINE DERIVATIVES FOR THE TREATMENT OF PI3K-DELTA RELATED DISORDERS - The present application provides methods of treating PI3Kδ related disorders using compounds of Formula I: | 09-04-2014 |
20140249133 | SUBSTITUTED BENZYLINDAZOLES FOR USE AS BUB1 KINASE INHIBITORS IN THE TREATMENT OF HYPERPROLIFERATIVE DISEASES - Compounds of formula (I) which are inhibitors of Bub1 kinase, processes for their production and their use as pharmaceuticals. | 09-04-2014 |
20140256700 | CARBAZOLE COMPOUNDS USEFUL AS BROMODOMAIN INHIBITORS - The present invention is directed to carbazole compounds, pharmaceutically acceptable compositions comprising compounds of the invention and methods of using said compositions in the treatment of various disorders. | 09-11-2014 |
20140256701 | PHENALKYLAMINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND THEIR USE IN THERAPY - The present invention relates to phenalkylamine derivatives of the formula (I) | 09-11-2014 |
20140275008 | Compounds and uses thereof for the modulation of hemoglobin - Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation. | 09-18-2014 |
20140275009 | COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE - The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. | 09-18-2014 |
20140275010 | QUATERNARY SALTS - The present invention provides quaternary salts, such as those of Formula I: | 09-18-2014 |
20140275011 | PYRIDINE CDK9 KINASE INHIBITORS - Disclosed are compound of Formula (Ia), | 09-18-2014 |
20140275012 | HETEROAROMATIC COMPOUNDS AS BTK INHIBITORS - The present invention encompasses compounds of the formula (I) | 09-18-2014 |
20140275013 | COMPOUNDS AND COMPOSITIONS FOR THE TREATMENT OF PARASITIC DISEASES - The present invention provides compounds of formula I: | 09-18-2014 |
20140275014 | HETEROAROMATIC COMPOUNDS AS BTK INHIBITORS - The present invention encompasses compounds of the formula (I) | 09-18-2014 |
20140275015 | P2X7 MODULATORS - The present invention is directed to compounds of Formulas (I, IIa and IIb): | 09-18-2014 |
20140275016 | N-Acyl-N'-(pyridin-2-yl) Ureas and Analogs Exhibiting Anti-Cancer and Anti-Proliferative Activities - Described are compounds of Formula 1 | 09-18-2014 |
20140275017 | CGRP RECEPTOR ANTAGONISTS - Compounds of Formula I: | 09-18-2014 |
20140275018 | NITROGEN CONTAINING COMPOUNDS - Compounds of Formula (I), their preparation and use in preventing or treating bacterial infection is disclosed. | 09-18-2014 |
20140275019 | TETRAHYDROPYRIDINE DERIVATIVES AS FABI INHIBITORS - The present invention relates to tetrahydropyridine derivatives of formula (1) which may be therapeutically useful as anti-bacterial agents, more particularly FabI inhibitors. | 09-18-2014 |
20140288043 | PYRAZOLOPYRIDINE COMPOUNDS - A first aspect of the invention relates to a compound of formula (1A) or (1B), or a pharmaceutically acceptable salt thereof, | 09-25-2014 |
20140288044 | COMPOSITIONS AND THERAPEUTIC USES OF IKK-RELATED KINASE EPSILON AND TANKBINDING KINASE 1 INHIBITORS - The invention relates to compounds, pharmaceutical compositions and medicaments comprising such compounds, and the use of these compounds, compositions, and medicaments in methods of treating diseases and disorders. | 09-25-2014 |
20140288045 | COVALENT INHIBITORS OF KRAS G12C - Irreversible inhibitors of G12C mutant K-Ras protein are provided. Also disclosed are methods to modulate the activity of G12C mutant K-Ras protein and methods of treatment of disorders mediated by G12C mutant K-Ras protein. | 09-25-2014 |
20140288046 | NOVEL [1,2,3]TRIAZOLO[4,5-D]PYRIMIDINE DERIVATIVES - The invention relates to a compound of formula (I) | 09-25-2014 |
20140288047 | BENZOXAZEPIN PI3K INHIBITOR COMPOUNDS AND METHODS OF USE - Benzoxazepin compounds of Formula I, including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, wherein: Z | 09-25-2014 |
20140288048 | HETEROCYCLIC COMPOUNDS AND USES THEREOF - Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including P13 kinase activity, are described herein. | 09-25-2014 |
20140288049 | 2-Thiopyrimidinones - Myeloperoxidase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, cardiovascular conditions. | 09-25-2014 |
20140296200 | 6-(5-HYDROXY-1H-PYRAZOL-1-YL)NICOTINAMIDE INHIBITORS OF PHD - The present invention provides compounds of the formula: | 10-02-2014 |
20140296201 | INHIBITORS OF INFLUENZA VIRUSES REPLICATION - Methods of inhibiting the replication of influenza viruses in a biological sample or patient, of reducing the amount of influenza viruses in a biological sample or patient, and of treating influenza in a patient, comprises administering to said biological sample or patient an effective amount of a compound represented by Structural Formula (I): | 10-02-2014 |
20140296202 | SUBSTITUTED PIPERIDINYL COMPOUNDS USEFUL AS GPR119 AGONISTS - Substituted piperidinyl compounds of the formula (I): are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119. | 10-02-2014 |
20140296203 | NOVEL COMPOUNDS THAT ARE ERK INHIBITORS - Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (1). | 10-02-2014 |
20140296204 | CHEMICAL COMPOUNDS - The invention is directed to substituted heteroaryl derivatives. Specifically, the invention is directed to compounds according to Formula Q: | 10-02-2014 |
20140303140 | NOVEL COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF INFLAMMATORY DISORDERS - The present invention discloses compounds according to Formula I: | 10-09-2014 |
20140303141 | TRIAZOLOPYRIDINE COMPOUNDS - The invention is concerned with triazolopyridine compounds of formula (I) | 10-09-2014 |
20140303142 | AZAINDOLES AS JANUS KINASE INHIBITORS - The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer. | 10-09-2014 |
20140309207 | NOVEL SPIROINDOLINE COMPOUND, AND MEDICINAL AGENT COMPRISING SAME - The present invention provides a novel compound represented by a general formula (1) as shown below, which has a glucokinase-activating action in the liver and pancreatic β-cells and which is useful as an agent for preventing and/or treating diseases caused by hyperglycemia, such as diabetes. | 10-16-2014 |
20140309208 | DISUBSTITUTED 3,4-DIAMINO-3-CYCLOBUTENE-1,2-DIONE COMPOUNDS FOR USE IN THE TREATMENT OF CHEMOKINE-MEDIATED PATHOLOGIES - Disubstituted 3,4-diamino-3-cyclobutene-1,2-dione compounds are disclosed that are represented by general formula (I). Also disclosed, are pharmaceutical compositions including these compounds and methods of using these compounds and compositions for the treatment of chemokine-mediated pathologies. | 10-16-2014 |
20140309209 | Pyrazine Kinase Inhibitors - Provided are pyrazine compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibition Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity. | 10-16-2014 |
20140315881 | COMPOUNDS AND METHODS - The present invention relates to novel retinoid-related orphan receptor gamma (RORγ) modulators and their use in the treatment of diseases mediated by RORγ. | 10-23-2014 |
20140315882 | PYRIMIDINE-SUBSTITUTED PYRROLIDINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF - The invention relates to new pyrrolidine derivatives of the formula | 10-23-2014 |
20140315883 | 6H-IMIDAZO[1,5-a]PYRROLO[2,3-e]PYRAZINE COMPOUNDS - The invention provides a compound of Formula (I as defined herein, pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variables are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions. | 10-23-2014 |
20140315884 | AMPK-ACTIVATING HETEROCYCLIC COMPOUNDS AND METHODS FOR USING THE SAME - Disclosed are substituted pyridine compounds as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure | 10-23-2014 |
20140315885 | Therapeutically Active Thiazolo-Pyrimidine Derivatives - A series of thiazolo[5,4-d]pyrimidine derivatives of formula (I) or an N-oxide thereof, or a pharmaceutically acceptable salt or solvate thereof: (I) Q represents a group of formula (Qa), (Qb), (Qc), (Qd) or (Qe) are beneficial in the treatment and/or prevention of various human ailments, including inflammatory, autoimmune and oncological disorders; viral diseases; and organ and cell transplant rejection. | 10-23-2014 |
20140323463 | PYRAZINECARBOXAMIDE COMPOUND | 10-30-2014 |
20140323464 | KINASE INHIBITORS - Provided herein are kinase inhibiting compounds and methods of using the same. | 10-30-2014 |
20140323465 | HCV PROTEASE INHIBITORS AND USES THEREOF - The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same. | 10-30-2014 |
20140323466 | THIENYL [3,2-D] PYRIMIDIN-4-ONE COMPOUNDS, PREPARATION METHOD, PHARMACEUTICAL COMPOSITIONS AND USE THEREOF - Disclosed are new thienyl[3,2-d]pyrimidin-4-one compounds shown as the general formula (I), preparation method, pharmaceutical compositions and pharmacological use thereof. The compounds are strong DPPIV (dipeptide peptidase IV) inhibitors and can treat type II diabetes through well inhibiting DPPIV indirectly increasing the content of GLP-1 in vivo and inducing a series of physiological actions in vivo. Therefore, the compounds could be developed as new promising drugs for treating diabetes. | 10-30-2014 |
20140329794 | PRMT5 INHIBITORS AND USES THEREOF - Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described. | 11-06-2014 |
20140329795 | KYNURENINE-3-MONOOXYGENASE INHIBITORS, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE THEREOF - Certain chemical entities are provided herein. Also provided are pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity. | 11-06-2014 |
20140329796 | HETEROCYCLIC AMIDE DERIVATIVE AND PHARMACEUTICAL PRODUCT CONTAINING SAME - The present invention aims to provide a novel compound having a TRPA1 antagonist activity, and a medicament containing the compound. Moreover, the present invention aims to provide a TRPA1 antagonist and a medicament useful for the prophylaxis or treatment of diseases involving TRPA1. | 11-06-2014 |
20140329797 | SUBSTITUTED OXADIAZOLYL PYRIDINONES AND OXADIAZOLYL PYRIDAZINONES AS HIF INHIBITORS - The present application relates to novel substituted 5-(1,2,4-oxadiazol-5-yl)pyridin-2-ones and 6-(1,2,4-oxadiazol-5-yl)pyridazin-3-ones, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for producing medicaments for treatment and/or prevention of diseases, in particular for treatment and/or prevention of hyperproliferative and angiogenic diseases and those diseases which arise from metabolic adaptation to hypoxic states. Such treatments can be effected in the form of monotherapy or else in combination with other medicaments or further therapeutic measures. | 11-06-2014 |
20140329798 | SUBSTITUTED CYCLOPROPYL COMPOUNDS USEFUL AS GPR119 AGONISTS - Substituted cyclopropyl compounds of the formula (I): and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included | 11-06-2014 |
20140336167 | NAMPT INHIBITORS - Disclosed are compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed. | 11-13-2014 |
20140336168 | NAMPT INHIBITORS - Disclosed are compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed. | 11-13-2014 |
20140336169 | IMIDAZOPYRAZINE SYK INHIBITORS - Certain imidazopyrazines and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample. | 11-13-2014 |
20140336170 | INDAZOLE COMPOUNDS USEFUL AS KETOHEXOKINASE INHIBITORS - The present invention is directed to substituted indazole compounds, pharmaceutical compositions of these compounds and methods of use thereof. The compounds of the present invention are ketohexokinase (KHK) inhibitors, useful for treating or ameliorating a KHK mediated metabolic disorders and/or diseases such as obesity, Type II diabetes mellitus and Metabolic Syndrome X. | 11-13-2014 |
20140336171 | AZAINDOLES USEFUL AS INHIBITORS OF JANUS KINASES - The present invention relates to compounds useful as inhibitors of protein kinases, particularly of JAK family kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. | 11-13-2014 |
20140336172 | Novel 2H-Indazoles as EP2 Receptor Antagonists - The present invention relates to novel 2H-indazoles of the general formula (I), methods for the preparation thereof and the use thereof for the production of pharmaceutical agents for the treatment of diseases and indications which are linked with the EP | 11-13-2014 |
20140336173 | DISUBSTITUTED BENZOTHIENYL-PYRROLOTRIAZINES AND THEIR USE AS FGFR KINASE INHIBITORS - This invention relates to novel substituted 5-(1-benzothiophen-2-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives of formula (I) wherein R | 11-13-2014 |
20140343034 | Skin barrier function improving agent - [PROBLEM] The problem to be solved by the invention is to provide a novel pharmaceutical use of a JAK inhibitor. | 11-20-2014 |
20140343035 | 3,5-DISUBSTITUTED ALKYNYLBENZENE COMPOUND AND SALT THEREOF - The present invention provides a compound represented by Formula (I) | 11-20-2014 |
20140343036 | ISOQUINOLINE AND NAPHTHYRIDINE DERIVATIVES - The invention provides novel compounds having the general formula: | 11-20-2014 |
20140343037 | BENZENE, PYRIDINE, AND PYRIDAZINE DERIVATIVES - Disclosed are compounds and pharmaceutically acceptable salts of Formula I | 11-20-2014 |
20140349989 | COMPOUNDS AND THERAPEUTIC USES THEREOF - The invention relates to compounds, pharmaceutical compositions and methods useful for treating cancer, systemic or chronic inflammation, rheumatoid arthritis, diabetes, obesity, T-cell mediated autoimmune disease, ischemia, and complications associated with these diseases and disorders. | 11-27-2014 |
20140349990 | Pyrazolopyrrolidine Derivatives and their Use in the Treatment of Disease - The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; | 11-27-2014 |
20140357615 | SUBSTITUTED 1H-PYRAZOLO[3',4',4,5]THIENO[2,3-B]PYRIDIN-3-AMINE ANALOGS AS POSITIVE ALLOSTERIC MODULATORS OF THE MUSCARINIC ACETYCHOLINE RECEPTOR M4 - In one aspect, the invention relates to substituted 1H-pyrazolo[3′,4′:4,5]thieno[2,3-b]pyridin-3-amine analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M | 12-04-2014 |
20140357616 | PYRROLOPYRIDINE INHIBITORS OF KINASES - The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, | 12-04-2014 |
20140357617 | NOVEL HETEROCYCLIC ACRYLAMIDES AND THEIR USE AS PHARMACEUTICALS - The invention relates to novel heterocyclic acrylamide compounds (I), to the preparation of the compounds and intermediates used therein, to the use of the compounds as antibacterial medicaments and pharmaceutical compositions containing the compounds. | 12-04-2014 |
20140364409 | SUBSTITUTED PYRAZOLO[3',4':4,5]THIENO[2,3-C]PYRIDAZIN-3-AMINE ANALOGS AS POSITIVE ALLOSTERIC MODULATORS OF THE MUSCARINIC ACETYLCHOLINE RECEPTOR M4 - In one aspect, the invention relates to substituted pyrazolo[3′,4′:4,5]thieno[2,3-c]pyridazine-3-amine analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M | 12-11-2014 |
20140364410 | PYRAZOLOPYRIMIDINE COMPOUNDS AS KINASE INHIBITORS - The present disclosure provides compounds of Formula (IA) and/or pharmaceutically acceptable salts thereof that are tyrosine kinase inhibitors, in particular BTK, and are potentially useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as cancer, inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and/or pharmaceutically acceptable salts thereof and processes for preparing such compounds and pharmaceutically acceptable salts thereof. | 12-11-2014 |
20140371198 | NOVEL COMPOUNDS USEFUL FOR THE TREATMENT OF METABOLIC AND INFLAMMATORY DISEASES - Compounds are disclosed that have a formula represented by the following: | 12-18-2014 |
20140371199 | BICYCLIC HETEROCYCLIC DERIVATIVES AS MNK1 AND MNK2 MODULATORS AND USES THEREOF - The present invention relates to certain compounds (e.g., imidazopyrazine, imidazopyridine, imidazopyridazine and imidazpyrimidine compounds) that act as inhibitors of the MAP kinase interacting kinases MNK2a, MNK2b, MNK1a, and MNK1b. The present invention further relates to pharmaceutical compositions comprising these compounds, and to the use of the compounds for the preparation of a medicament for the prophylaxis and treatment of diseases (e.g., proliferative diseases (e.g., cancer), inflammatory diseases, Alzheimer's disease), as well as methods of treating these diseases. | 12-18-2014 |
20140371200 | ALKENE AZETIDINE DERIVATIVES AS SPHINGOSINE 1-PHOSPHATE (S1P) RECEPTOR MODULATORS - The present invention relates to alkene azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors. | 12-18-2014 |
20140378431 | TRIAZOLO[4,5-D]PYRIMIDINE DERIVATIVES - Compounds of the formula I | 12-25-2014 |
20150011527 | NOVEL GLP-1 RECEPTOR MODULATORS - Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds can act as modulators or potentiators of GLP-1 receptor on their own, or with incretin peptides such as GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “ | 01-08-2015 |
20150011528 | PHENYLIMIDE-CONTAINING BENZOTHIAZOLE DERIVATIVE OF ITS SALT AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME - Provided is a phenylimide-containing benzothiazole derivative or its pharmaceutically acceptable salt, a process for the preparation thereof, and a pharmaceutical composition comprising the same. The phenylimide-containing benzothiazole derivative or its pharmaceutically acceptable salt can selectively inhibit the protein-protein interaction between KRS and a laminin receptor (LR), thereby inhibiting migration of cancer cells. Therefore, the phenylimide-containing benzothiazole derivative or its pharmaceutically acceptable salt may be usefully applied for preventing or treating the diseases associated with cancer cell metastasis. | 01-08-2015 |
20150011529 | AZETIDINE-SUBSTITUTED QUINOXALINE-TYPE PIPERIDINE COMPOUNDS AND USES THEREOF - The disclosure relates to Azetidine-Substituted Quinoxaline-Type Piperidine Compounds of Formula (I): | 01-08-2015 |
20150011530 | CYCLIC MOLECULES AS BRUTON'S TYROSINE KINASE INHIBITORS - The present document describes novel molecules having protein tyrosine kinase inhibitory activity, and methods of synthesizing and using such compounds. More specifically, the present document describes compound of Formula (A): (Formula (A)) or a pharmaceutically acceptable salt, hydrate or solvate thereof, and methods of synthesizing and using such compounds. | 01-08-2015 |
20150018331 | ANTIBACTERIAL AGENTS - Antibacterial compounds of formula (I) are provided: | 01-15-2015 |
20150018332 | Nuclear Transport Modulators and Uses Thereof - The invention generally relates to nuclear transport modulators, e.g CRM1 inhibitors, and more particularly to a compound represented by formula (I): or a pharmaceutically acceptable salt thereof, wherein the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of structural formula (I), or a pharmaceutically acceptable salt or composition thereof, e.g, in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity. | 01-15-2015 |
20150018333 | INHIBITORS OF LEUKOTRIENE PRODUCTION - The present invention relates to compounds of formula (I): | 01-15-2015 |
20150018334 | INHIBITORS OF LEUKOTRIENE PRODUCTION - The present invention relates to aryl pyrazoles, and pharmaceutically acceptable salts thereof. The aryl pyrazoles of the present invention are useful as inhibitors of leukotriene A | 01-15-2015 |
20150018335 | CARBAMATE COMPOUNDS AND OF MAKING AND USING SAME - This disclosure provides compounds and compositions which may be modulators of MAGL and/or ABHD6 and their use as medicinal agents, processes for their preparation, and pharmaceutical compositions that include disclosed compounds as at least one active agent. The disclosure also provides for method of treating a patient in need thereof, where the patient is suffering from indications such as pain, solid tumor cancer and/or obesity comprising administering a disclosed compound or composition. | 01-15-2015 |
20150018336 | PYRAZOLO[3,4-d]PYRIMIDINE AND PYRAZOLO[2,3-d]PYRIMIDINE COMPOUNDS AS KINASE INHIBITORS - Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions. | 01-15-2015 |
20150018337 | N-(2-(HETARYL)ARYL)ARYLSULFONAMIDES AND N-(2-(HETARYL)HETARYL)ARYLSULFONAMIDES - Compounds are provided that act as potent antagonists of the CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists. | 01-15-2015 |
20150025056 | SUBSTITUTED CYCLIC HYDROXAMATES AS INHIBITORS OF MATRIX METALLOPROTEINASES - The present invention provides compounds of the formula I: | 01-22-2015 |
20150025057 | Triazine-oxadiazoles - The invention relates to new derivatives of formula (I), wherein the substituents are as defined in the specification; to processes for the preparation of such derivatives; pharmaceutical compositions comprising such derivatives; such derivatives as a medicament; such derivatives for the treatment of chronic pain. | 01-22-2015 |
20150031667 | Substituted Pyrazolo [1,5-A] Pyrimidine Compounds as TRK Kinase Inhibitors - Compounds of Formula I: | 01-29-2015 |
20150031668 | CHROMAN DERIVATIVES AS TRPM8 INHIBITORS - Chroman compounds and derivatives of Formula I are useful inhibitors of TRPM8. Such compounds are useful in treating a number of TRPM8 mediated disorders and conditions and may be used to prepare medicaments and pharmaceutical compositions useful for treating such disorders and conditions. Examples of such disorders include, but are not limited to, migraines and neuropathic pain. Compounds of Formula I have the following structure: | 01-29-2015 |
20150031669 | ANTICANCER BENZOPYRAZINES VIA THE INHIBITION OF FGFR KINASES - The invention relates to new quinoxaline derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer. | 01-29-2015 |
20150031670 | CYCLIC AMIDES AS METAP-2 INHIBITORS - Compounds of the formula (I), in which R | 01-29-2015 |
20150031671 | NOVEL COMPOUND USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES - A compound is disclosed that has a formula represented by the following: | 01-29-2015 |
20150031672 | HETEROCYCLIC COMPOUNDS AND USES THEREOF - Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein. | 01-29-2015 |
20150038483 | AROMATIC 5-MEMBERED HETEROCYCLIC DERIVATIVE HAVING TRPV4-INHIBITING ACTIVITY - The present invention is related to a compound represented by formula (I) | 02-05-2015 |
20150038484 | INDOLE AND INDAZOLE COMPOUNDS THAT ACTIVATE AMPK - The present invention relates to indole and indazole compounds of Formula (I) | 02-05-2015 |
20150045342 | NOVEL PIPERIDINE COMPOUND OR SALT THEREOF - A novel compound which has an excellent aurora A-selective inhibitory action and is useful as an orally administrable anticancer agent is provided. Also, a novel agent for potentiation of anti-tumor effect of microtubule agonists, which include a taxane anticancer agent, and a combination therapy are provided. A piperidine compound represented by a general formula (I) or a salt thereof:
| 02-12-2015 |
20150045343 | KINASE INHIBITORS - Methods of inhibiting kinases using kinase inhibitors having olefin moieties are disclosed. | 02-12-2015 |
20150045344 | 4-(4-CYANO-2-THIOARYL)DIHYDROPYRIMIDINONES AND USE THEREOF - The present invention relates to novel 4-(4-cyano-2-thioaryl)dihydropyrimidin-2-one derivatives, to processes for their preparation, to their use alone or in combination for the treatment and/or prevention of diseases and also to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of disorders of the lung and the cardiovascular system. | 02-12-2015 |
20150051187 | COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE - The present invention relates to pyrazine compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. | 02-19-2015 |
20150057262 | CYCLIC P1 LINKERS AS FACTOR XIA INHIBITORS - The present invention provides compounds of Formula (Ia): | 02-26-2015 |
20150065479 | METHOD FOR ENHANCING ANTI-TUMOR EFFECT OF A MICROTUBULE-TARGETING DRUG, AND A METHOD FOR TREATMENT OF TUMOR - A method for treating a tumor by combining a piperidine compound of formula (I) or salt thereof and a microtubule-targeting drug, in which the microtubule-targeting drug is administered once per 7 days or more one cycle, and the piperidine compound is administered once or more per day for 4 days or more: | 03-05-2015 |
20150065480 | MIF INHIBITORS AND THEIR USES - The invention relates to MIF inhibitors; compositions comprising an effective amount of a MIF inhibitor; and methods for treating or preventing diseases associated with MIF. | 03-05-2015 |
20150065481 | MICROBIOCIDAL PYRAZOLE DERIVATIVES - Compounds of the formula I wherein the substituents areas defined in claim | 03-05-2015 |
20150065482 | ALKYNYL ALCOHOLS AND METHODS OF USE - The invention relates to compounds of Formula (0): | 03-05-2015 |
20150065483 | Substituted 6,5-Fused Bicyclic Heteroaryl Compounds - The present invention relates to substituted 6,5-fused bicyclic heteroaryl compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. | 03-05-2015 |
20150080364 | CARBAMATE COMPOUNDS AND OF MAKING AND USING SAME - Provided herein are carbamate compounds which may be useful in the treatment of for example, pain, solid tumors and/or obesity. | 03-19-2015 |
20150080365 | HETEROARYL COMPOUNDS WITH CYCLIC BRIDGING UNIT - This invention relates to certain heteroaryl compounds for use as medicaments, more specifically as medicaments for treating animals. The medicament can be used for the treatment of helminth infections and the treatment of parasitosis caused by helminth infections. This invention also relates to uses of the compounds to make medicaments and treatments comprising the administration of the compounds to animals in need of the treatments. This invention also relates to pharmaceutical compositions and kits comprising the compounds. | 03-19-2015 |
20150080366 | CYTOMEGALOVIRUS INHIBITOR COMPOUNDS - Compounds of Formula (I) wherein n, A, R | 03-19-2015 |
20150080367 | SUBSTITUTED DIPYRIDYLAMINES AND USES THEREOF - The present invention provides for compounds of Formula I and various embodiments thereof, and compositions comprising compounds of Formula I and various embodiments thereof. | 03-19-2015 |
20150080368 | SULFONYL AMIDE DERIVATIVES FOR THE TREATMENT OF ABNORMAL CELL GROWTH - The present invention relates to a compound of the formula I | 03-19-2015 |
20150087627 | COMBINATION OF KINASE INHIBITORS AND USES THEREOF - The present invention provides for a method for treating a disease condition associated with PI3-kinase α and/or mTOR in a subject. In another aspect, the invention provides for a method for treating a disease condition associated with PI3-kinase α and/or mTOR in a subject. In yet another aspect, a method of inhibiting phosphorylation of both Akt (S473) and Akt (T308) in a cell is set forth. The present invention also provides a pharmaceutical kit effective for treating a disease condition associated with PI3-kinase α and/or mTOR in a subject. | 03-26-2015 |
20150087628 | COMPOSITIONS AND METHODS FOR TREATING CANCER - K-Ras is the most frequently mutated oncogene in human cancer. Disclosed herein are compositions and methods for modulating K-Ras and treating cancer. | 03-26-2015 |
20150087629 | PIPERIDINE/PIPERAZINE DERIVATIVES - The invention relates to a DGAT inhibitor of formula | 03-26-2015 |
20150094295 | PYRAZOLOPYRIMIDINE COMPOUNDS AS KINASE INHIBITORS - The present disclosure provides compounds of Formula (IA) and or pharmaceutically acceptable salts thereof that are tyrosine kinase inhibitors, in particular BTK, and are potentially useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as cancer, inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and/or pharmaceutically acceptable salts thereof and processes for preparing such compounds and pharmaceutically acceptable salts thereof. | 04-02-2015 |
20150094296 | HETEROCYCLIC COMPOUND - The present invention provides an agent for the prophylaxis or treatment of autoimmune diseases (e.g., psoriasis, rheumatoid arthritis, inflammatory bowel disease, Sjogren's syndrome, Behcet's disease, multiple sclerosis, systemic lupus erythematosus etc.) and the like, which has a superior Tyk2 inhibitory action. | 04-02-2015 |
20150094297 | IMIDAZOTHIADIAZOLE AND IMIDAZOPYRAZINE DERIVATIVES AS PROTEASE ACTIVATED RECEPTOR 4 (PAR4) INHIBITORS FOR TREATING PLATELET AGGREGATION - The present invention provides thiazole compounds of Formula I wherein W, Y, R | 04-02-2015 |
20150094298 | INHIBITORS OF PROTEIN KINASES - The present invention is directed to compounds of formula I-II and pharmaceutically acceptable tautomers, salts, or stereoisomers thereof which are inhibitors of syk and/or JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk and/or JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk and/or JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma. | 04-02-2015 |
20150094299 | PURINONE DERIVATIVE - Compounds represented by general formula (I) (all of the symbols in the formula conform to the definitions in the Description) are compounds that, in addition to having a Btk-selective inhibitory activity, exhibit an excellent metabolic stability and can avoid hepatotoxicity or the like, and as a consequence can provide safe therapeutic agents for diseases in which B cells or mast cells participate. | 04-02-2015 |
20150099730 | IMIDAZOLIN-5-ONE DERIVATIVE USEFUL AS FASN INHIBITORS FOR THE TREATMENT OF CANCER - Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including those mediated by inhibition of fatty acid synthase (FASN) enzyme, such as, cancer, obesity or related discorders, and liver related disorders. Such compounds are represented by formula (I) as follows: | 04-09-2015 |
20150099731 | USE OF PARTHENOLIDE DERIVATIVES AS ANTILEUKEMIC AND CYTOTOXIC AGENTS - The present invention provides compounds of the formula (I) | 04-09-2015 |
20150099732 | 3-ARYL-5-SUBSTITUTED-ISOQUINOLIN-1-ONE COMPOUNDS AND THEIR THERAPEUTIC USE - The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain 3-aryl-5-substituted-2H-isoquinolin-1-one compounds that, inter alia, inhibit PARP (e.g., PARP1, TNKS1, TNKS2, etc.) and/or Wnt signalling. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit PARP (e.g., PARP1, TNKS1, TNKS2, etc.); to inhibit Wnt signalling; to treat disorders that are ameliorated by the inhibition of PARP (e.g., PARP1, TNKS1, TNKS2, etc.); to treat disorders that are ameliorated by the inhibition of Wnt signalling; to treat proliferative conditions such as cancer, etc. | 04-09-2015 |
20150099733 | HETEROARYLCARBOXYLIC ACID ESTER DERIVATIVE - Compounds represented by the following formula (I); | 04-09-2015 |
20150099734 | NEW DIAZASPIROCYCLOALKANE AND AZASPIROCYCLOALKANE - The invention provides novel compounds having the general formula (I) | 04-09-2015 |
20150099735 | TRIAZOLOPYRIDINE COMPOUNDS - The invention is concerned with triazolopyridine compounds of formula (I) | 04-09-2015 |
20150105366 | METHYLENE LINKED QUINOLINYL MODULATORS OF RORyt - The present invention comprises compounds of Formula I. | 04-16-2015 |
20150105367 | RAF INHIBITOR COMPOUNDS - This invention provides compounds of Formula (I) or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising a compound of Formula (I); and use of a compound of Formula (I) for treating specified cancers. | 04-16-2015 |
20150105368 | PYRAZOLYL QUINOXALINE KINASE INHIBITORS - The invention relates to new quinoxaline derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer. | 04-16-2015 |
20150105369 | ALKYL LINKED QUINOLINYL MODULATORS OF RORyt - The present invention comprises compounds of Formula I. | 04-16-2015 |
20150105370 | SELECTIVELY SUBSTITUTED QUINOLINE COMPOUNDS - Embodiments of the disclosure relate to selectively substituted quinoline compounds that act as antagonists or inhibitors for Toll-like receptors 7 and/or 8, and their use in pharmaceutical compositions effective for treatment of systemic lupus erythematosus (SLE) and lupus nephritis. | 04-16-2015 |
20150105371 | CO-CRYSTALS AND SALTS OF CCR3-INHIBITORS - This invention relates to co-crystals and salts of CCR3 inhibitors of formula 1, | 04-16-2015 |
20150111868 | NOVEL 1,3-DIHYDRO-2H-BENZIMIDAZOL-2-ONE DERIVATIVES SUBSTITUTED WITH HETEROCYCLES AS RESPIRATORY SYNCYTIAL VIRUS ANTIVIRAL AGENTS - The present invention is concerned with novel 1,3-dihydro-2H-benzimidazol-2-one derivatives substituted with heterocycles having formula (I) | 04-23-2015 |
20150111869 | USE OF A COMBINATION OF A MEK INHIBITOR AND AN ERK INHIBITOR FOR TREATMENT OF HYPERPROLIFERATIVE DISEASES - The invention provides combinations comprising a MEK inhibitor (such as GDC-0973 or GDC-0623), or a pharmaceutically acceptable salt thereof and an ERK inhibitor (such as GDC-0994). The combinations are particularly useful for treating hyperproliferative disorders, such as cancer. | 04-23-2015 |
20150111870 | QUINOLINYL MODULATORS OF RORyt - The present invention comprises compounds of Formula I. | 04-23-2015 |
20150111871 | DNA-PK INHIBITORS - The present invention relates to compounds useful as inhibitors of DNA-PK. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. | 04-23-2015 |
20150111872 | NOVEL COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF INFLAMMATORY DISORDERS - The present invention discloses compounds according to Formula I: | 04-23-2015 |
20150119376 | CYCLOALKENYL ARYL DERIVATIVES FOR CETP INHIBITOR - The present invention relates to cycloalkenyl aryl derivatives, isomers thereof, pharmaceutically acceptable salts thereof, hydrates thereof, or solvates thereof; a method for preparing the derivatives; and pharmaceutical compositions containing the same. The compounds of the present invention show the effect of CETP activity inhibition. It means that the compounds can increase HDL-cholesterol and decrease LDL-cholesterol. | 04-30-2015 |
20150119377 | AZETIDINE DERIVATIVES AS ANTIPARASITIC AGENTS - This invention recites substituted azetidine derivatives of Formula (1) stereoisomers thereof, veterinarily acceptable salts thereof, compositions thereof, and their use as a parasiticide in animals. The substituents A, B, R | 04-30-2015 |
20150119378 | AZETIDINYLOXY-, PYRROLIDINYLOXY-, AND PIPERIDINYLOXY-SUBSTITUTED METANICOTINES AS NEURONAL NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS - The present invention relates to compounds that bind to and modulate the activity of neuronal nicotinic acetylcholine receptors, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders, including those associated with dysfunction of the central nervous system (CNS). | 04-30-2015 |
20150119379 | 2-(2,4,5-SUBSTITUTED-ANILINO)PYRIMIDINE COMPOUNDS - The present invention relates to certain 2-(2,4,5-substituted-anilino)pyrimidine compounds and pharmaceutically acceptable salts thereof which may be useful in the treatment or prevention of a disease or medical condition mediated through certain mutated forms of epidermal growth factor receptor (for example the L858R activating mutant, the Exon19 deletion activating mutant and the T790M resistance mutant). Such compounds and salts thereof may be useful in the treatment or prevention of a number of different cancers. The invention also relates to pharmaceutical compositions comprising said compounds and salts thereof, especially useful polymorphic forms of these compounds and salts, intermediates useful in the manufacture of said compounds and to methods of treatment of diseases mediated by various different forms of EGFR using said compounds and salts thereof. | 04-30-2015 |
20150126487 | HETEROCYCLIC COMPOUND AND USE THEREFOR - The present invention provides a compound having a cholinergic muscarinic M1 receptor positive allosteric modulator activity, and useful as a prophylactic or therapeutic drug for Alzheimer's disease, schizophrenia, pain, a sleep disorder and the like. The present invention relates to a compound represented by the formula (I): | 05-07-2015 |
20150126488 | NITROGEN-CONTAINING BICYCLIC AROMATIC HETEROCYCLIC COMPOUND - [Problem] On the basis of a cathepsin S inhibitory effect, an excellent agent for treating or preventing autoimmune disease, allergic disease, graft rejection of an organ, bone marrow or tissue, systemic lupus erythematosus, or the like is provided. | 05-07-2015 |
20150126489 | FUMIGILLOL COMPOUNDS AND METHODS OF MAKING AND USING SAME - The disclosure provides fumagillol type compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of using, e.g. in the treatment of obesity are provided. | 05-07-2015 |
20150126490 | AMINOHETEROARYL BENZAMIDES AS KINASE INHIBITORS - The present invention provides a compound of Formula (I) or a salt thereof; | 05-07-2015 |
20150126491 | PYRIDAZINE DERIVATIVES AS RORc MODULATORS - Compounds of the formula I: | 05-07-2015 |
20150133424 | HETEROCYCLYL COMPOUNDS AS MEK INHIBITORS - The present disclosure is related to heteroaryl compounds as MEK inhibitors. These compounds include heteroaryl compounds of formula I, their pharmaceutically acceptable salts, combinations with suitable medicament and pharmaceutical compositions thereof. The present disclosure also includes processes of preparation of the compounds and their use in methods of treatment. The compounds as disclosed herein are of Formula (I) below: | 05-14-2015 |
20150133425 | THIENOPYRIMIDINES - The present invention relates to substituted thienopyrimidine compounds of general formula (I) as described and defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients. | 05-14-2015 |
20150133426 | SUBSTITUTED PYRROLOPYRIMIDINES - The present invention relates to substituted pyrrolopyrimidine compounds general formula I: in which A, X, R | 05-14-2015 |
20150133427 | PRMT5 INHIBITORS AND USES THEREOF - Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described. | 05-14-2015 |
20150133428 | NOVEL SUBSTITUTED PYRAZOLO-PIPERAZINES AS CASEIN KINASE 1 D/E INHIBITORS - The invention provides compounds of Formula (I): | 05-14-2015 |
20150133429 | METHOD OF TREATMENT USING SUBSTITUTED PYRAZOLO[1,5-a] PYRIMIDINE COMPOUNDS - Compounds useful in the synthesis of compounds for treating pain, cancer, inflammation, neurodegenerative disease or | 05-14-2015 |
20150133430 | COMPOUNDS AND USES THEREOF FOR THE MODULATION OF HEMOGLOBIN - Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation. | 05-14-2015 |
20150141396 | PYRIMIDINE PYRAZOLYL DERIVATIVES - The present invention provides compounds of Formula (I) for the treatment of cancer, rheumatoid arthritis and other diseases. | 05-21-2015 |
20150141397 | SUBSTITUTED ANILINES AS CCR(4) ANTAGONISTS - Aniline compounds are provided which bind to CCR(4) and are useful for the treatment of diseases such as allergic diseases, autoimmune diseases, graft rejection and cancer. | 05-21-2015 |
20150141398 | NAMPT INHIBITORS - Disclosed are compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed. | 05-21-2015 |
20150141399 | MEK Inhibitors And Methods Of Their Use - Disclosed are compounds of Formula I: | 05-21-2015 |
20150148327 | SUBSTITUTED PYRIDINE SPLEEN TYROSINE KINASE (SYK) INHIBITORS - The invention provides certain substituted pyridines of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R | 05-28-2015 |
20150148328 | Novel 2,3-Dihydro-1H-imidazopyrimidin-5-one and this 1,2,3,4-tetrahydropyrimidopyrimidin-6-one Derivatives Comprising a Substituted Morpholine, Preparation Thereof and Pharmaceutical Use Thereof - The invention relates to the novel products of formula (I) with p, q=0, 1 or 2; R1=phenyl, pyridyl; —(CH | 05-28-2015 |
20150148329 | PRO-DRUGS OF RILUZOLE AND THEIR METHOD OF USE FOR THE TREATMENT OF AMYOTROPHIC LATERAL SCLEROSIS - Pharmaceutical compositions of the invention include substituted riluzole pro drugs useful for the treatment of amyotrophic lateral sclerosis (ALS) and related disorders through the release of riluzole, especially to avoid patient to patient variability in first pass, hepatic metabolism promoted by Cyp 1A2. Pro-drugs of riluzole have enhanced stability to hepatic metabolism and are delivered into systemic circulation by oral administration, and then cleaved to release riluzole in the plasma via either an enzymatic or general biophysical release process. The invention further includes pro-drugs of riluzole useful for the treatment of disease states that can be treated with riluzole through the release of riluzole from a pro-drug agent. | 05-28-2015 |
20150148330 | CARBAMATE COMPOUNDS AND OF MAKING AND USING SAME - This disclosure provides compounds and compositions which may be modulators of MAGL and/or ABHD6 and their use as medicinal agents, processes for their preparation, and pharmaceutical compositions that include disclosed compounds as at least one active agent. The disclosure also provides for method of treating a patient in need thereof, where the patient is suffering from indications such as pain, solid tumor cancer and/or obesity comprising administering a disclosed compound or composition. | 05-28-2015 |
20150291586 | BICYCLIC HETEROCYCLE COMPOUNDS AND THEIR USES IN THERAPY - The invention relates to bicyclic heterocycle compounds of formula (I): | 10-15-2015 |
20150291592 | HEPATITIS C INHIBITOR COMPOUNDS - Compounds of Formula (I) wherein n, X | 10-15-2015 |
20150299150 | SPHINGOSINE 1 PHOSPHATE RECEPTOR MODULATORS AND METHODS OF CHIRAL SYNTHESIS - Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds are provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated. | 10-22-2015 |
20150299186 | HETEROCYCLYL COMPOUNDS - The present invention is related to heteroaryl compounds as MEK inhibitors. The invention includes heteroaryl compounds of formula I, their tautomers and pharmaceutically acceptable salts, combinations with suitable medicament and pharmaceutical compositions thereof. The present invention also includes process of preparation of the said compounds and intended use in therapy of them. | 10-22-2015 |
20150299198 | Inhibitors of the Renal Outer Medullary Potassium Channel - The present invention provides compounds of Formula I | 10-22-2015 |
20150299201 | BET PROTEIN-INHIBITING 5-ARYL TRIAZOLE AZEPINES - The present invention relates to BET-protein-inhibitory, in particular BRD4-inhibitory 5-aryltriazoloazepines of the general formula (I) | 10-22-2015 |
20150307473 | THERAPEUTIC COMPOUNDS AND COMPOSITIONS AND THEIR USE AS PKM2 MODULATORS - Compositions comprising compounds of general formula (I) that modulate pyruvate kinase are described herein. Also described herein are methods of using the compounds that modulate pyruvate kinase in the treatment of diseases. | 10-29-2015 |
20150307483 | ALKYL-AMIDE-SUBSTITUTED PYRIDYL COMPOUNDS USEFUL AS MODULATORS OF IL-12, IL-23 AND/OR IFN ALPHA RESPONSES - Compounds having the following formula (I): or a stereoisomer or pharmaceutically-acceptable salt thereof, where R | 10-29-2015 |
20150315141 | Thrombin Inhibitors - Compounds of the invention, which may be useful in inhibiting thrombin and associated thrombotic occlusions, have the following structure: | 11-05-2015 |
20150315172 | PYRIDONE COMPOUND - The invention provides a pyridone compound represented by the following formula (I) [wherein, R | 11-05-2015 |
20150315185 | PYRROLO[2,3-b]PYRIDIN-4-YL-AMINES AND PYRROLO[2,3-b]PYRIMIDIN-5-YL-AMINES AS JANUS KINASE INHIBITORS - The present invention provides pyrrolo[2,3-b]pyridine-4-yl amines pyrrolo[2,3-b]pyrimidin-4-yl amines that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases and cancer. | 11-05-2015 |
20150320727 | HETEROCYCLIC COMPOUNDS AND USES THEREOF - Heterocyclic entities that modulate PI3 kinase activity, pharmaceutical compositions containing the heterocyclic entities, and methods of using these chemical entities for treating diseases and conditions associated with PI3 kinase activity are described herein. | 11-12-2015 |
20150320759 | DIHYDRONAPHTHYRIDINES AND RELATED COMPOUNDS USEFUL AS KINASE INHIBITORS FOR THE TREATMENT OF PROLIFERATIVE DISEASES - The invention relates to dihydronaphthyridines and related compounds; compositions comprising an effective amount of a dihydronaphthyridine or a related compound; and methods for treating or preventing proliferative diseases comprising the administration of an effective amount of a dihydronaphthyridine or a related compound. | 11-12-2015 |
20150329558 | FUSED HETEROCYCLIC COMPOUNDS AS ION CHANNEL MODULATORS - The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: | 11-19-2015 |
20150336941 | THERAPEUTIC ISOXAZOLE COMPOUNDS - The invention provides a compound of formula I: | 11-26-2015 |
20150336962 | 5-CHLORO-2-DIFLUOROMETHOXYPHENYL PYRAZOLOPYRIMIDINE COMPOUNDS, COMPOSITIONS AND METHODS OF USE THEREOF - Compounds of Formula (00A) and methods of use as Janus kinase inhibitors are described herein. | 11-26-2015 |
20150342951 | Use of Inhibitors of the Activity or Function of PI3K - The invention relates to new uses of PI3K inhibitors, wherein said inhibitors have an inhibitory action on the PI3K isoform delta for the treatment of immunopathology in a subject suffering from a disease or disorder selected from malaria, leishmaniasis, trypanosomiasis, toxoplasmosis and/or neurocysticercosis, via functional inhibition of TLR9 of the infected subject. | 12-03-2015 |
20150344423 | CARBOXAMIDE OR SULFONAMIDE SUBSTITUTED NITROGEN-CONTAINING 5-MEMBERED HETEROCYCLES AS MODULATORS FOR THE ORPHAN NUCLEAR RECEPTOR ROR GAMMA - The invention provides modulators for the orphan nuclear receptor RORy and methods for treating RORy mediated diseases by administering these novel RORy modulators to a human or a mammal in need thereof. Specifically, the present invention provides carboxamide containing cyclic compounds of Formula (1) to Formula (5) and the enantiomers, diastereomers, tautomers, /V-oxides, solvates and pharmaceutically acceptable salts thereof. | 12-03-2015 |
20150344429 | PYRIDINE-2-AMIDES USEFUL AS CB2 AGONISTS - The invention relates to a compound of formula (I) wherein R | 12-03-2015 |
20150344434 | TETRAHYDRO- AND DIHYDRO-ISOQUINOLINE PRMT5 INHIBITORS AND USES THEREOF - Described herein are compounds of Formula (A), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5 mediated disorders are also described. | 12-03-2015 |
20150344444 | BET-PROTEIN-INHIBITING DIHYDROXYQUINOXALINONES - The present invention relates to BET protein-inhibitory, especially BRD4-inhibitory, dihydroquinoxalinones of the general formula (I) | 12-03-2015 |
20150344457 | METHODS OF INHIBITING PRMT5 - Described herein are compounds of Formula (I) useful for inhibiting PRMT5 activity. The planes of Ring AA and Ring BB are between 75° and 105°. Ring AA-M-Ring BB (I) | 12-03-2015 |
20150344473 | TANK-BINDING KINASE INHIBITOR COMPOUNDS - Compounds having the following formula (I) and methods of their use and preparation are disclosed: | 12-03-2015 |
20150344481 | NOVEL SUBSTITUTED IMIDAZOLES AS CASEIN KINASE 1 D/E INHIBITORS - The invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The compounds of Formula (I) inhibit protein kinase activity thereby making them useful as anticancer agents. | 12-03-2015 |
20150344489 | OXINDOLE COMPOUNDS CARRYING A CO-BOUND SPIRO SUBSTITUENT AND USE THEREOF FOR TREATING VASOPRESSIN-RELATED DISEASES - The present invention relates to novel substituted oxindole derivatives of formula I | 12-03-2015 |
20150352090 | CARBAMATE DERIVATIVES - Compounds of formula (I) defined herein are both phosphodiesterase 4 (PDE4) enzyme inhibitors and muscarinic M3 receptor antagonists and are useful for the prevention and/or treatment of diseases of the respiratory tract. | 12-10-2015 |
20150353494 | ARYL- OR HETEROARYL-SUBSTITUTED BENZENE COMPOUNDS - The present invention relates to aryl- or heteroaryl-substituted benzene compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes. | 12-10-2015 |
20150353505 | PHTHALAZINONES AND ISOQUINOLINONES AS ROCK INHIBITORS - The present invention provides compounds of Formula (I) or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same. | 12-10-2015 |
20150353546 | METALLOENZYME INHIBITOR COMPOUNDS - The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes. | 12-10-2015 |
20150353552 | PURINE INHIBITORS OF HUMAN PHOSPHATIDYLINOSITOL 3-KINASE DELTA - The instant invention provides compounds of formula I which are PI3K-delta inhibitors, and as such are useful for the treatment of PI3K-delta-mediated diseases such as inflammation, asthma, COPD and cancer. | 12-10-2015 |
20150361042 | PRMT5 INHIBITORS AND USES THEREOF - Described herein are compounds of formula (A), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described. | 12-17-2015 |
20150361055 | SULFOXIMINE SUBSTITUTED QUINAZOLINES FOR PHARMACEUTICAL COMPOSITIONS - This invention relates to novel sulfoximine substituted quinazoline derivatives of formula I | 12-17-2015 |
20150361067 | SUBSTITUTED DIHYDROISOQUINOLINONE COMPOUNDS - This invention relates to compounds of general formula (I) | 12-17-2015 |
20150368265 | TETRACYCLIC HETEROCYCLE COMPOUNDS AND METHODS OF USE THEREOF FOR THE TREATMENT OF HEPATITIS C - The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system. I | 12-24-2015 |
20150368266 | CHEMICAL COMPOUNDS 542 - The present invention relates to compounds of Formula (I): | 12-24-2015 |
20150368270 | FLAP MODULATORS - The present invention relates to compounds of Formula (I), or a form thereof wherein ring A, R | 12-24-2015 |
20150374708 | DISUBSTITUTED 3,4-DIAMINO-3-CYCLOBUTENE-1,2-DIONE COMPOUNDS FOR USE IN THE TREATMENT OF CHEMOKINE-MEDIATED PATHOLOGIES - Disubstituted 3,4-diamino-3-cyclobutene-1,2-dione compounds represented by the general formula (I) are described. Also described, are pharmaceutical compositions including these compounds and the use of these compounds and compositions for the treatment of chemokine-mediated pathologies. | 12-31-2015 |
20150376133 | C-Met Modulators and Methods of Use - The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate and/or modulate kinase receptor, particularly c-Met, KDR, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds. | 12-31-2015 |
20150376173 | SPHINGOSINE-1-PHOSPHATE RECEPTOR AGONISTS, METHODS OF PREPARING THE SAME, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME AS AN ACTIVE AGENT - The present invention relates to novel compounds of Formula 1 as sphingosine-1-phosphate receptor agonists which can be effectively used for the treatment of autoimmune diseases, a method for preparing the same, and a pharmaceutical composition comprising the same as an active component. The compounds according to the present invention are effective on extensive autoimmune diseases and chronic inflammatory diseases including relapsing-remitting multiple sclerosis, and can also be used for treating or preventing immunoregulation disorders. | 12-31-2015 |
20150376196 | 4-SUBSTITUTED PYRROLO- AND PYRAZOLO-DIAZEPINES - BET protein-inhibitory, especially BRD2-, BRD3- and BRD4-inhibitory, 4-substituted pyrrolo- and pyrazolodiazepines of the general formula I | 12-31-2015 |
20160002175 | Pyrimidine-2,4-Diamine Derivatives for Treatment of Cancer - A compound of formula (I), or a pharmaceutically-acceptable salt thereof. The compound is useful in the treatment of cancer or other diseases that may benefit from inhibition of MTH1. | 01-07-2016 |
20160002185 | CIS-MORPHOLINONE AND OTHER COMPOUNDS AS MDM2 INHIBITORS FOR THE TREATMENT OF CANCER - The present invention provides MDM2 inhibitor compounds of Formula (I), or the pharmaceutically acceptable salts thereof, wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor. | 01-07-2016 |
20160002219 | IMIDAZOLIN-5-ONE DERIVATIVE USEFUL AS FASN INHIBITORS FOR THE TREATMENT OF CANCER - Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including those mediated by inhibition of fatty acid synthase (FASN) enzyme, such as, cancer, obesity or related discorders, and liver related disorders. Such compounds are represented by formula (I) as follows: | 01-07-2016 |
20160002221 | Substituted Pyridopyrazines as Syk Inhibitors - The present invention relates to pyridopyrazine compounds of formula (I), pharmaceutical compositions thereof and methods of use therefore, wherein R | 01-07-2016 |
20160002228 | 3-SUBSTITUTED PYRAZOLES AND USE AS DLK INHIBITORS - The present invention provides for compounds of Formula (I) and various embodiments thereof, and compositions comprising compounds of Formula (I) and various embodiments thereof. | 01-07-2016 |
20160002241 | INHIBITORS OF BRUTON'S TYROSINE KINASE - Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. In addition, reversible inhibitors of Btk are also described. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions. | 01-07-2016 |
20160002247 | 8-SUBSTITUTED IMIDAZOPYRIMIDINONE DERIVATIVE HAVING AUTOTAXIN INHIBITORY ACTIVITY - A compound of formula (I) wherein variables are as defined herein having an autotaxin inhibitory effect and a pharmaceutical composition comprising the same. | 01-07-2016 |
20160008362 | AGENT FOR PREVENTING AND/OR TREATING OCULAR INFLAMMATORY DISEASE | 01-14-2016 |
20160009659 | PYRIMIDINE CARBOXAMIDES AS SODIUM CHANNEL BLOCKERS | 01-14-2016 |
20160009682 | COMPOUNDS INHIBITING LEUCINE-RICH REPEAT KINASE ENZYME ACTIVITY | 01-14-2016 |
20160009688 | BENZAMIDE DERIVATIVE USEFUL AS FASN INHIBITORS FOR THE TREATMENT OF CANCER | 01-14-2016 |
20160009701 | CARBAZOLE COMPOUNDS USEFUL AS BROMODOMAIN INHIBITORS | 01-14-2016 |
20160009704 | GLS1 INHIBITORS FOR TREATING DISEASE | 01-14-2016 |
20160009725 | PYRROLO- AND PYRAZOLO-TRIAZOLODIAZEPINES AS BET-PROTEIN INHIBITORS FOR TREATING HYPERPROLIFERATIVE DISEASES | 01-14-2016 |
20160009734 | SUBSTITUTED THIAZOLOPYRIMIDINES | 01-14-2016 |
20160015712 | Triazolo[4,5-d]pyrimidine derivatives - Compounds of the formula I | 01-21-2016 |
20160016916 | Exo Olefin-Containing Nuclear Transport Modulators and Uses Thereof - The invention generally relates to nuclear transport modulators, e.g., CRM1 inhibitors, and, more particularly, to a compound represented by structural formula (I), or a pharmaceutically acceptable salt thereof, wherein the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of structural formula I, or a pharmaceutically acceptable salt or composition thereof, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity. | 01-21-2016 |
20160016938 | Novel 2,5-substituted pyrimidines - The invention relates to novel substituted condensed pyrimidine compounds of general formula (I) | 01-21-2016 |
20160016948 | AMINOPYRIMIDINE COMPOUNDS AS INHIBITORS OF T790M CONTAINING EGFR MUTANTS - This invention relates to novel compounds which are inhibitors of T790M containing EGFR mutants, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the prevention or treatment of cancer. | 01-21-2016 |
20160016951 | NOVEL NAPHTHYRIDINES AND ISOQUINOLINES AND THEIR USE AS CDK8/19 INHIBITORS - The present invention relates to naphthyridine and isoquinoline compounds, and pharmaceutically acceptable compositions thereof, useful as inhibitors of CDK8/19, and for the treatment of CDK8/19-related disorders. | 01-21-2016 |
20160016975 | C2-AZASPIRO IMINOTHIAZINE DIOXIDES AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE - In its many embodiments, the present invention provides certain C2-azaspiro substituted iminothiazine dioxide compounds. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed. | 01-21-2016 |
20160022670 | BENZAMIDES - Novel benzamide derivatives of formula (I) | 01-28-2016 |
20160024049 | HETEROCYCLIC COMPOUND - The present invention relates to a compound represented by the formula (I), which is useful as an agent for the prophylaxis or treatment of epilepsy, neurodegenerative disease and the like. In the formula (I), each symbol is as defined in the specification. | 01-28-2016 |
20160024053 | Novel 2,5-Substituted Pyrimidines - The invention relates to novel substituted condensed pyrimidine compounds of general formula (I) | 01-28-2016 |
20160024064 | AZETIDINE AMIDE DERIVATIVES AS OREXIN RECEPTOR ANTAGONISTS - The present invention relates to azetidine amide derivatives derivatives of formula (I) wherein rings A | 01-28-2016 |
20160024072 | Heterocyclic Ring and Carbocyclic Derivative - The present invention provides novel compounds having a P2X | 01-28-2016 |
20160024117 | HETEROCYCLYLAMINES AS PI3K INHIBITORS - The present invention provides heterocyclylamine derivatives of Formula I: | 01-28-2016 |
20160031813 | Nampt Inhibitors - Disclosed are compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed. | 02-04-2016 |
20160031828 | ANTIMICROBIAL COMPOUNDS AND METHODS OF MAKING AND USING THE SAME - The present invention relates generally to the field of antimicrobial compounds and to methods of making and using them. These compounds are useful for treating, preventing, and reducing the risk of microbial infections in humans and animals. | 02-04-2016 |
20160031857 | NOVEL SUBSTITUTED CONDENSED PYRIMIDINE COMPOUNDS - The invention relates to novel substituted condensed pyrimidine compounds of general formula (I) | 02-04-2016 |
20160031872 | HETEROAROMATIC COMPOUNDS AS BTK INHIBITORS - The present invention encompasses compounds of the formula (I) | 02-04-2016 |
20160031880 | Nampt and Rock Inhibitors - Disclosed are compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed. Disclosed are compounds which inhibit the activity of ROCK, compositions containing the compounds and methods of treating diseases during which ROCK is expressed. | 02-04-2016 |
20160031892 | COMPOSITIONS USEFUL FOR TREATING DISORDERS RELATED TO KIT - Compounds and compositions useful for treating disorders related to Kit are described herein. | 02-04-2016 |
20160031903 | sGC STIMULATORS - Compounds of Formulae I′ and I are described, which are useful as stimulators of sGC, particularly NO-independent, heme-dependent stimulators. These compounds are also useful for treating, preventing or managing various disorders that are herein disclosed. | 02-04-2016 |
20160038455 | S1P RECEPTORS MODULATORS AND THEIR USE THEREOF - The invention relates to novel compounds that have S1P receptor modulating activity. Further, the invention relates to a pharmaceutical comprising at least one compound of the invention for the treatment of diseases and/or conditions caused by or associated with inappropriate S1P receptor modulating activity or expression, for example, autoimmune response. A further aspect of the invention relates to the use of a pharmaceutical comprising at least one compound of the invention for the manufacture of a medicament for the treatment of diseases and/or conditions caused by or associated with inappropriate S1P receptor modulating activity or expression such as autoimmune response. | 02-11-2016 |
20160038504 | BIARYL AMIDE COMPOUNDS AS KINASE INHIBITORS - The present invention provides compounds of Formula (I) as described herein, and salts thereof, and therapeutic uses of these compounds for treatment of disorders associated with Raf kinase activity. The invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds and a therapeutic co-agent. | 02-11-2016 |
20160039825 | S1P AND/OR ATX MODULATING AGENTS - Compounds of formula (I), and pharmaceutically acceptable salts thereof, can modulate the activity of one or more SIP receptors and/or the activity of autotaxin (ATX). | 02-11-2016 |
20160039828 | Imidazopyridazine Compounds - The present invention is directed to compounds of Formula I: | 02-11-2016 |
20160045507 | NOVEL USES - The subject matter generally relates to methods of treatment and/or prophylaxis of CNS diseases, disorders, and/or injuries. In one aspect, the subject matter relates to inhibitors of phosphodiesterase 1 (PDE1) as neuroprotective agents and/or neural regenerative agents. In a further aspect, the subject matter relates to individuals that are at risk for the development of CNS disease or disorder. | 02-18-2016 |
20160046597 | RORC2 INHIBITORS AND METHODS OF USE THEREOF - The present invention provides compounds, pharmaceutical compositions, methods of inhibiting RORγ activity and/or reducing the amount of IL-17 in a subject, and methods of treating various medical disorders using such compounds and pharmaceutical compositions. | 02-18-2016 |
20160046601 | HETEROCYCLIC COMPOUND AND USE THEREOF - Compounds represented by the formulas | 02-18-2016 |
20160046612 | Heterocyclic Derivative and Pharmaceutical Drug - The present invention provides a novel heterocyclic derivative or a pharmaceutically acceptable salt thereof. For example, the present invention provides a heterocyclic derivative of the general formula [1] or its tautomer, or a pharmaceutically acceptable salt thereof: | 02-18-2016 |
20160046618 | Cyclopropyl Fused Thiazin-2-Amine Compounds as Beta-Secretase Inhibitors and Methods of Use - The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: | 02-18-2016 |
20160046625 | BENZIMIDAZOLE AND AZABENZIMIDAZOLE COMPOUNDS THAT INHIBIT ANAPLASTIC LYMPHOMA KINASE - Compounds of Formula (I) are useful inhibitors of anaplastic lymphoma kinase. Compounds of Formula (I) have the following structure: where the definitions of the variables are provided herein. | 02-18-2016 |
20160052897 | HETEROCYCLIC COMPOUND - The present invention relates to a compound represented by the formula (I), which is useful as an agent for the prophylaxis or treatment of epilepsy, neurodegenerative disease and the like. In the formula (I), each symbol is as defined in the specification. | 02-25-2016 |
20160052924 | 2-KETO AMIDE DERIVATIVES AS HIV ATTACHMENT INHIBITORS - Compounds of Formula I, including pharmaceutically acceptable salts thereof: I useful as HIV attachment inhibitors. | 02-25-2016 |
20160052940 | BIHETEROARYL COMPOUNDS AND USES THEREOF - The present invention provides for compounds of Formula I-I and embodiments and salts thereof for the treatment of diseases (e.g., neurodegenerative diseases). R | 02-25-2016 |
20160058763 | NOVEL HETEROCYCLIC CARBOXAMIDES AS MODULATORS OF KINASE ACTIVITY - The invention provides novel heterocyclic carboxamide compounds according to Formula (I) their manufacture and use for the treatment of hyperproliferative diseases, such as cancer. | 03-03-2016 |
20160060231 | SUBSTITUTED BICYCLIC DIHYDROPYRIMIDINONES AND THEIR USE AS INHIBITORS OF NEUTROPHIL ELASTASE ACTIVITY - This invention relates to substituted bicyclic dihydropyrimidinones of formula 1 | 03-03-2016 |
20160060262 | Substituted 6,6-Fused Nitrogenous Heterocyclic Compounds and Uses Thereof - The invention provides novel compounds having the general formula: | 03-03-2016 |
20160060267 | PYRAZOLO COMPOUNDS AND USES THEREOF - Provided are compounds useful as inhibitors of one or more histone demethylases, such as KDM5. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using the present composition in the treatment of various disorders. | 03-03-2016 |
20160060273 | HETEROCYCLIC COMPOUND - Provided is a compound represented by the following formula (1) or a salt thereof, which has an SSTR5 antagonistic action: wherein each symbol has the same definition as in the specification. | 03-03-2016 |
20160068544 | NOVEL MACROCYCLES AS FACTOR XIA INHIBITORS - The present invention provides compounds of Formula (Ia): | 03-10-2016 |
20160075686 | NEW 3,4-DIHYDRO-2H-ISOQUINOLINE-1-ONE AND 2,3-DIHYDRO-ISOINDOL-1-ONE COMPOUNDS - The invention provides novel compounds having the general formula (I) | 03-17-2016 |
20160075687 | NEW 3,4-DIHYDRO-2H-ISOQUINOLINE-1-ONE AND 2,3-DIHYDRO-ISOINDOL-1-ONE COMPOUNDS - The invention provides novel compounds having the general formula (I) | 03-17-2016 |
20160075688 | NEW 3,4-DIHYDRO-2H-ISOQUINOLINE-1-ONE AND 2,3-DIHYDRO-ISOINDOL-1-ONE COMPOUNDS - The invention provides novel compounds having the general formula (I) | 03-17-2016 |
20160081986 | LONG-ACTING SPIRO-ISOXAZOLINE ANTIPARASITIC COMPOSITIONS - The invention describes a long-acting composition comprising a spiro-azetidine isoxazoline of Formula (1) or (2) wherein R | 03-24-2016 |
20160081997 | PIPERIDINE/PIPERAZINE DERIVATIVES - The invention relates to a DGAT inhibitor of formula | 03-24-2016 |
20160083348 | COMPOUNDS AND USES THEREOF FOR THE MODULATION OF HEMOGLOBIN - Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation. | 03-24-2016 |
20160083354 | NOVEL COMPOUNDS FOR SELECTIVE HISTONE DEACETYLASE INHIBITORS, AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME - The present invention relates to novel urea derivatives and, more particularly, to novel urea derivatives with histone deacetylase (HDAC) inhibitory activity, isomers thereof, pharmaceutically acceptable salts thereof, their use for the preparation of a medicaments comprising the same, a pharmaceutical composition comprising the same, a treatment method using the composition, and a method for preparing novel urea derivatives. The novel urea derivatives as selective histone deacetylase (HDAC) inhibitors are effective for the treatment of histone deacetylase-mediated diseases such as malignant tumors, inflammatory diseases, rheumatoid arthritis, neurodegeneration, etc. | 03-24-2016 |
20160083357 | NOVEL TETRAZOLONE DERIVATIVES - The invention relates to a compound of formula (I) | 03-24-2016 |
20160090372 | COMPOUNDS AS TYROSINE KINASE MODULATORS - The present invention is directed to novel compounds of Formula I. The compounds of the present invention are potent tyrosine kinase modulators, and are suitable for the treatment and prevention of diseases and conditions related to abnormal activities of tyrosine kinase receptors. | 03-31-2016 |
20160095848 | PHENYLPYRROLE DERIVATIVE - Provided are novel compounds that are useful in the prevention or treatment of such diseases as dementia, Alzheimer's disease, attention-deficient hyperactivity disorder, schizophrenia, epilepsy, central convulsion, obesity, diabetes mellitus, hyperlipidemia, narcolepsy, idiopathic hypersomnia, behaviorally induced insufficient sleep syndrome, sleep apnea syndrome, circadian rhythm disorder, parasomnia, sleep related movement disorder, insomnia, and depression, or allergic rhinitis, or pharmaceutically acceptable salts of such compounds. Specifically, there are provided phenylpyrrole compounds represented by the following formula (I) or pharmaceutically acceptable salts thereof: | 04-07-2016 |
20160096827 | TANK-BINDING KINASE INHIBITOR COMPOUNDS - Compounds having the following formula (I) and methods of their use and preparation are disclosed: | 04-07-2016 |
20160096834 | HETEROARYL COMPOUNDS AS BTK INHIBITORS AND USES THEREOF - The present invention relates to imidazo pyridine compounds, and pharmaceutically acceptable compositions thereof, useful as BTK inhibitors. | 04-07-2016 |
20160096850 | ALKYNYL ALCOHOLS AND METHODS OF USE - The invention relates to compounds of Formula (0): | 04-07-2016 |
20160102075 | UNSATURATED NITROGEN HETEROCYCLIC COMPOUNDS USEFUL AS PDE10 INHIBITORS - Unsaturated nitrogen heterocyclic compounds of formula (I): | 04-14-2016 |
20160115168 | NOVEL FUSED PYRIMIDINE COMPOUND OR SALT THEREOF - Provided is a novel compound having BTK inhibitory action and a cell proliferation suppressing effect. Also provided is a medicine useful for the prevention and/or treatment of a disease associated with BTK, particularly cancer, based on BTK inhibitory action. A compound represented by formula (I) [wherein R | 04-28-2016 |
20160115169 | 6,7-DIHYDROPYRAZOLO[1,5-a]PYRAZIN-4(5H)-ONE COMPOUNDS AND THEIR USE AS NEGATIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS - The present invention relates to novel 6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one derivatives as negative allosteric modulators (NAMs) of the metabotropic glutamate receptor subtype 2 (“mGluR2”). The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention or treatment of disorders in which the mGluR2 subtype of metabotropic receptors is involved. | 04-28-2016 |
20160120841 | SUBSTITUTED CHROMANES AND METHOD OF USE - The invention provides for compounds of formula (I) | 05-05-2016 |
20160122336 | TRIFLUOROMETHYL ALCOHOLS AS MODULATORS OF RORyt - The present invention comprises compounds of Formula I. | 05-05-2016 |
20160122346 | NOVEL 1,3-DIHYDRO-2H-BENZIMIDAZOL-2-ONE DERIVATIVES SUBSTITUTED WITH HETEROCYCLES AS RESPIRATORY SYNCYTIAL VIRUS ANTIVIRAL AGENTS - The present invention is concerned with novel 1,3-dihydro-2H-benzimidazol-2-one derivatives substituted with heterocycles having formula (I) | 05-05-2016 |
20160122358 | NOVEL SUBSTITUTED PYRAZOLO-PIPERAZINES AS CASEIN KINASE 1 D/E INHIBITORS - The invention provides compounds of Formula (I): | 05-05-2016 |
20160128984 | ISOXAZOLE COMPOUNDS AND METHODS FOR THE TREATMENT OF CYSTIC FIBROSIS - The invention relates to a compound of Formula I and methods of treating cystic fibrosis comprising the step of administering a therapeutically effective amount of a compound of Formula I or II to a patient in need thereof: | 05-12-2016 |
20160128996 | BICYCLIC AZA COMPOUNDS AS MUSCARINIC M1 RECEPTOR AGONISTS - This invention relates to compounds (Formula (1)) that are agonists of the muscarinic M1 receptor and which are useful in the treatment of muscarinic M1 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula where R | 05-12-2016 |
20160129011 | BICYCLO 2,3-BENZODIAZEPINES AND SPIROCYCLICALLY SUBSTITUTED 2,3-BENZODIAZEPINES - BET-protein-inhibitory, in particular BRD4-inhibitory bicyclo- and spirocyclically substituted 2,3-benzodiazepines of the general formula (I), | 05-12-2016 |
20160136168 | THERAPEUTIC AGENT FOR FGFR INHIBITOR-RESISTANT CANCER - The problem to be solved by the present invention is to provide an anticancer agent for treating tumors resistant to other antitumor agents that inhibit FGFR, and a method for treating such tumors. The present invention provides an antitumor agent for administration to a tumor patient resistant to an FGFR inhibitor, the antitumor agent comprising a 3,5-disubstituted benzene alkynyl compound represented by Formula (I) below or a salt thereof. The present invention also provides a therapeutic method using the anticancer agent. | 05-19-2016 |
20160137613 | NOVEL ANTI-INFLAMMATORY AGENTS - Disclosed are novel compounds that are useful in regulating the expression of interleukin-6 (IL-6) and/or vascular cell adhesion molecule-1 (VCAM-1), and their use in the treatment and/or prevention of cardiovascular and inflammatory diseases and related disease states, such as, for example, atherosclerosis, asthma, arthritis, cancer, multiple sclerosis, psoriasis, and inflammatory bowel diseases, and autoimmune disease(s). Also, disclosed are compositions comprising the novel compounds, as well as methods for their preparation. | 05-19-2016 |
20160137633 | PHARMACEUTICAL COMPOSITION FOR TREATING DIABETES - Provided is a compound represented by the following general formula (I), or a pharmaceutically acceptable salt thereof. This novel compound has a glycogen-synthase activation ability, but activates a receptor PPAR to a low degree and is highly safe. | 05-19-2016 |
20160137639 | TRIAZOLE-ISOXAZOLE COMPOUND AND MEDICAL USE THEREOF - A compound represented by Formula [I]: | 05-19-2016 |
20160137649 | PYRROLO-PYRROLE CARBAMATE AND RELATED ORGANIC COMPOUNDS, PHARMACEUTICAL COMPOSITIONS, AND MEDICAL USES THEREOF - The invention provides pyrrolo-pyrrole carbamate and related organic compounds, compositions containing such compounds, medical kits, and methods for using such compounds and compositions to treat medical disorders, e.g., solid tumor cancer, obesity, Down's syndrome, Alzheimer's disease, or pain, in a patient. The octahydropyrrolo pyrrole carbamates could be derived from hexafluoroisopropanol, N,N-disuccinimide and such. The activity of carbamates in MAGL, FAAH, and ABHD6 assays are also described. | 05-19-2016 |
20160145237 | PROTEIN TYROSINE KINASE MODULATORS AND METHODS OF USE - Heterocyclic pyrimidine compounds that modulate mutant-selective epidermal growth factor receptor (EGFR) and ALK kinase activity are disclosed. More specifically, the invention provides pyrimidines which inhibit, regulate and/or modulate kinase receptor, particularly in selectively modulation of various EGFR mutant activity and ALK kinase activity have been disclosed. Pharmaceutical compositions comprising the pyrimidine derivative, and methods of treatment for diseases associated with protein kinase enzymatic activity, particularly EGFR or ALK kinase activity including non-small cell lung cancer comprising administration of the pyrimidine derivative are disclosed. | 05-26-2016 |
20160152609 | IMIDAZOLE COMPOUNDS AS MODULATORS OF FSHR AND USES THEREOF | 06-02-2016 |
20160152624 | NOVEL SUBSTITUTED CONDENSED PYRIMIDINE COMPOUNDS | 06-02-2016 |
20160152626 | PYRAZOLE COMPOUNDS AS MODULATORS OF FSHR AND USES THEREOF | 06-02-2016 |
20160152628 | TRICYCLIC PYRIDO-CARBOXAMIDE DERIVATIVES AS ROCK INHIBITORS | 06-02-2016 |
20160159738 | COVALENT INHIBITORS OF KRAS G12C - Irreversible inhibitors of G12C mutant K-Ras protein are provided. Also disclosed are methods to modulate the activity of G12C mutant K-Ras protein and methods of treatment of disorders mediated by G12C mutant K-Ras protein. | 06-09-2016 |
20160159784 | N-CYCLOPROPYL-N-PIPERIDINYL-AMIDES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND USES THEREOF - Compounds of formula I | 06-09-2016 |
20160159789 | SUBSTITUTED PYRAZOLOPYRIDINES - The present invention relates to substituted pyrazolopyridine compounds of general formula I as described and defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyperproliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients. | 06-09-2016 |
20160159790 | Pyrroloquinoline Derivatives as 5-HT6 Antagonists, Preparation Method and Use Thereof - This invention concerns pyrroloquinoline derivatives as antagonists of 5-HT6 receptors, to methods for the preparation of these compounds and to novel intermediates useful for their synthesis. The invention also relates to the uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in schizophrenia, anxiety, depression, maniac depression, epilepsy, obsessive compulsive disorders, mood disorders, migraine, Alzheimer's disease, age related cognitive decline, mild cognitive impairment, sleep disorders, eating disorders, anorexia, bulimia, panic attacks, attention deficit hyperactivity disorder, attention deficit disorder, Parkinson's disease, Huntington's disease, withdrawal from abuse of cocaine, ethanol, nicotine or benzodiazepines, pain, obesity and type-2 diabetes, functional bowel disorder, Irritable Bowel Syndrome. The compounds have the general formula (XIV), wherein the symbols have the meanings given in the description. | 06-09-2016 |
20160159793 | Fused Pyrroledicarboxamides and Their Use as Pharmaceuticals - The present invention relates in fused pyrroledicarboxamides of the formula (I), in which R1 to R9, X, m and n are as defined in claims. The compounds of the formula (I) are inhibitors of the acid-sensitive potassium channel TASK-1 and suitable for the treatment of TASK-1 channel-mediated diseases such as arrhythmias, in particular atrial arrhythmias like atrial fibrillation or atrial flutter, and respiratory disorders, in particular sleep-related respiratory disorders like sleep apnea, for example. | 06-09-2016 |
20160159816 | SUBSTITUTED THIENOPYRIMIDINES AND PHARMACEUTICAL USE THEREOF - The present invention relates to substituted thienopyrimidine compounds of general formula (I) as described and defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients. | 06-09-2016 |
20160168090 | NOVEL INDOLE DERIVATIVES AND THEIR USE IN NEURODEGENERATIVE DISEASES | 06-16-2016 |
20160168156 | FUSED RING HETEROARYL COMPOUNDS AND THEIR USE AS TRK INHIBITORS | 06-16-2016 |
20160175315 | N-PIPERIDINYL ACETAMIDE DERIVATIVES AS CALCIUM CHANNEL BLOCKERS | 06-23-2016 |
20160176850 | AXL INHIBITORS | 06-23-2016 |
20160176864 | NOVEL TRICYCLIC COMPOUNDS AS ANTICANCER AGENTS | 06-23-2016 |
20160184281 | NAMPT INHIBITORS - Disclosed are compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed. | 06-30-2016 |
20160184307 | Heterocyclyl Pyrimidine Analogues As TYK2 Inhibitors - The present invention relates to compounds of formula (I) | 06-30-2016 |
20160184316 | NEPRILYSIN INHIBITORS - In one aspect, the invention relates to compounds having the formula: | 06-30-2016 |
20160184318 | AUTOTAXIN INHIBITORS - The present invention relates to novel compounds that are autotaxin inhibitors, processes for their preparation, pharmaceutical compositions and medicaments containing them and to their use in diseases and disorders mediated by autotaxin. | 06-30-2016 |
20160185725 | c-Met Modulators and Method of Use - The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds. | 06-30-2016 |
20160185756 | SUBSTITUTED BENZIMIDAZOLES AND BENZOPYRAZOLES AS CCR(4) ANTAGONISTS - Benzimidazole, benzopyrazole and benzotriazole compounds are provided which bind to CCR(4) and are useful for the treatment of diseases such as allergic diseases, autoimmune diseases, graft rejection and cancer. | 06-30-2016 |
20160185757 | INDOLE DERIVATIVES AS MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF - Agents of formulas (I)/(II)/(III) for modulating methyl modifying enzymes, compositions and uses thereof are provided herein. | 06-30-2016 |
20160185764 | PREPARATION AND USE OF 7A-AMIDE SUBSTITUTED- 6,6-DIFLUORO BICYCLIC HIMBACINE DERIVATIVES AS PAR-1 RECEPTOR ANTAGONISTS - The present invention relates to bicyclic himbacine derivatives of the formula | 06-30-2016 |
20160185776 | IMIDE AND ACYLUREA DERIVATIVES AS MODULATORS OF THE GLUCOCORTICOID RECEPTOR - Novel non-steroidal compounds are provided which are useful in treating diseases or disorders associated with modulation of the glucocorticoid receptor, AP-1, and/or NF- | 06-30-2016 |
20160185785 | PYRROLO AND PYRAZOLOPYRIMIDINES AS UBIQUITIN-SPECIFIC PROTEASE 7 INHIBITORS - The invention relates to inhibitors of USP7 inhibitors useful in the treatment of cancers, neurodegenerative diseases, immunological disorders, inflammatory disorders, cardiovascular diseases, ischemic diseases, viral infections and diseases, and bacterial infections and diseases, having the Formula: | 06-30-2016 |
20160199383 | 5-ALKYNYL-PYRIMIDINES | 07-14-2016 |
20160200724 | DIHYDROPYRROLOPYRIDINE INHIBITORS OF ROR-GAMMA | 07-14-2016 |
20160200725 | QUINOLONE DERIVATIVES AS FIBROBLAST GROWTH FACTOR RECEPTOR INHIBITORS | 07-14-2016 |
20160200733 | SUBSTITUTED THIENO[2,3-B]PYRIDINE-2-CARBOXAMIDE ANALOGS AS POSITIVE ALLOSTERIC MODULATORS OF THE MUSCARINIC ACETYLCHOLINE RECEPTOR M4 | 07-14-2016 |
20160200739 | ALKYNYL ALCOHOLS AND METHODS OF USE | 07-14-2016 |
20160251337 | 6-(5-HYDROXY-1H-PYRAZOL-1-YL)NICOTINAMIDE INHIBITORS OF PHD | 09-01-2016 |
20160251358 | PYRAZOLOPYRIMIDINE COMPOUNDS AS KINASE INHIBITORS | 09-01-2016 |
20160376254 | SUBSTITUTED DIHYDROISOQUINOLINONE COMPOUNDS - This invention relates to compounds of general formula (I) | 12-29-2016 |
20160376268 | Fused Tricyclic Imidazole Derivatives As Modulators of TNF Activity - A series of fused tricyclic imidazole derivatives, in particular dihydro-1H-cyclopenta[4,5]imidazo[1,2-a]pyridine derivatives, and analogues thereof, being potent modulators of human TNFα activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders. | 12-29-2016 |
20160376278 | FUSED PYRAZOLE DERIVATIVE HAVING AUTOTAXIN INHIBITORY ACTIVITY - The present invention provides a compound of formula (1), wherein R | 12-29-2016 |
20160376289 | NOVEL BICYCLIC OR TRICYCLIC HETEROCYCLIC COMPOUND - The present invention provides a novel bicyclic or tricyclic heterocyclic compound represented by the formula (I) | 12-29-2016 |
20170231991 | Use Of Modulators Of CCR5 In The Treatment Of Cancer And Cancer Metastasis | 08-17-2017 |
20170233368 | ARYL AND HETEROARYL FUSED LACTAMS | 08-17-2017 |
20170233371 | RORC2 INHIBITORS AND METHODS OF USE THEREOF | 08-17-2017 |
20180021345 | AUTOTAXIN INHIBITORS | 01-25-2018 |
20180022726 | MUSCARINIC AGONISTS | 01-25-2018 |
20180022732 | COMPOUNDS USEFUL FOR TREATING DISORDERS RELATED TO RET | 01-25-2018 |
20180022745 | ISOQUINILINE AND NAPTHALENE-SUBSTITUTED COMPOUNDS AS MGLUR4 ALLOSTERIC POTENTIATORS, COMPOSITIONS, AND METHODS OF TREATING NEUROLOGICAL DYSFUNCTION | 01-25-2018 |
20180022747 | Factor IXa Inhibitors | 01-25-2018 |
20180022759 | COMPOUNDS, COMPOSITIONS AND METHODS | 01-25-2018 |
20190144382 | MEK Inhibitors and Methods of Their Use | 05-16-2019 |
20190144403 | 2-(BENZOTHIAZOL-2-YL)-2-CYANO-ACETAMIDE DERIVATIVES AND THEIR USE AS ENDOTHELIAL LIPASE INHIBITORS | 05-16-2019 |
20190144429 | RORC2 INHIBITORS AND METHODS OF USE THEREOF | 05-16-2019 |
20190144442 | ASH1L INHIBITORS AND METHODS OF TREATMENT THEREWITH | 05-16-2019 |
20220135570 | FUSED PYRAZINE DERIVATIVES AS A2A / A2B INHIBITORS - This application relates to compounds of Formula (I): | 05-05-2022 |