Entries |
Document | Title | Date |
20080214520 | 6-N-Linked Heterocycle-Substituted 2,3,4,5-Tetrahydro-1H-Benzo[d]Azepines as 5-Ht2c Receptor Agonists - The present invention provides 6-substituted 2,3,4,5-tetrahydro-1H-benzo[d]azepines of Formula I as selective 5-HT | 09-04-2008 |
20080221077 | Ansamycin formulations and methods of use thereof - Provided herein, inter alia, are solid forms of geldanamycin analogs, pharmaceutical compositions comprising a geldanamycin analog and a crystallization inhibitor, methods of making and using such compositions. Additionally, provided are methods for the treatment of cancer, a neoplastic disease state and/or a hyperproliferative disorder, and methods of inhibiting Heat Shock Protein 90 (“Hsp90”). | 09-11-2008 |
20080221078 | Use of a CB1 Antagonist for Treating Side Effects and Negative Symptoms of Schizophrenia - The present invention discloses and claims a method of treating cognition deficits in a patient suffering from schizophrenia by administering to said patient a therapeutically effective amount of a CB1 receptor antagonist as described herein. In another aspect, this invention also discloses and claims a combination of one or more CB1 receptor antagonists and of one or more antipsychotic agents useful in the treatment of psychiatric disorders. The combination of this invention provides synergistic results in that the combination improves positive and negative symptoms of schizophrenia, weight gain and catalepsy. | 09-11-2008 |
20080227769 | Compounds for the Treatment of Hepatitis C - The invention encompasses compounds of formula I, including pharmaceutically acceptable salts, as well as compositions and methods of using these compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV. | 09-18-2008 |
20080255086 | Heterocyclic Derivatives - The present invention relates to a heterocyclic derivative according to formula I | 10-16-2008 |
20080261943 | PYRROLOPYRIMIDINE A2B SELECTIVE ANTAGONIST COMPOUNDS, THEIR SYNTHESIS AND USE - The subject invention provides compounds having the structure: | 10-23-2008 |
20080261944 | Indole Derivatives as Antiviral Agents - The present invention relates to indole compounds of the formula (I): wherein R | 10-23-2008 |
20080261945 | Compounds Having Activity at Nk3 Receptor and Uses Thereof in Medicine - The present invention relates to compounds of formula (I), a pharmaceutically acceptable salt, solvate or prodrug thereof: | 10-23-2008 |
20080261946 | Pyrimidine Compounds for the Treatment of Inflammatory Disorders - The present invention relates to novel pyrimidine compounds, for the modulation of the histamine H4 receptor and the treatment or prevention of conditions mediated by the histamine H4 receptor. The invention also relates to the preparation of such compounds. | 10-23-2008 |
20080261947 | FUSED PYRIDAZINE DERIVATIVE COMPOUNDS AND DRUGS CONTAINING THESE COMPOUNDS AS THE ACTIVE INGREDIENT - Fused pyridazine derivatives represented by formula (I) or pharmaceutically acceptable salts thereof (wherein each symbol has the meaning as defined in the specification.). | 10-23-2008 |
20080269191 | Compounds for Nonsense Suppression, Use of These Compounds for the Manufacture of a Medicament for Treating Somatic Mutation-Related Diseases - The present invention relates to methods, compounds, and compositions for treating or preventing diseases associated with nonsense mutations in an mRNA by administering the compounds or compositions of the present invention. More particularly, the present invention relates to methods, compounds, and compositions for suppressing premature translation termination associated with a nonsense mutation in an mRNA. | 10-30-2008 |
20080275022 | Substituted Quinazolones as Anti-Cancer Agents - The invention relates to chemical compounds of the formula (I): or pharmaceutically acceptable salts thereof, which possess B Raf inhibitory activity and are accordingly useful for their anti cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm blooded animal such as man. | 11-06-2008 |
20080280878 | Methods and Compositions for Treating Chronic Lymphocytic Leukemia - Novel method of treating chronic lymphocytic leukemia by the administering of HSP90 inhibitors, particularly ansamycins, more particularly I 7-allylamino-I 7-demethoxygetdanarnycin (17-AAG). | 11-13-2008 |
20080280879 | SUBSTITUTED HETEROCYCLIC DERIVATIVES AND THEIR PHARMACEUTICAL USE AND COMPOSITIONS - Compounds of the general Formula I, wherein X | 11-13-2008 |
20080287414 | Mitotic Kinesin Inhibitors - The present invention relates to tricyclic pyrazoles according to Formula (I) that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also relates to compositions which comprise these compounds, and methods of using them to treat cancer in mammals. | 11-20-2008 |
20080287415 | Bicycloheteroaryl compounds as P2X7 modulators and uses thereof - Compounds are disclosed that have a formula represented by the following: | 11-20-2008 |
20080287416 | Organic Compounds - There are provided according to the invention compounds of formula (I) | 11-20-2008 |
20080293688 | AMINOAZACYCLYL-3-SULFONYLINDAZOLES AS 5-HYDROXYTRYPTAMINE-6 LIGANDS - The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of disorders related to or affected by the 5-HT6 receptor. | 11-27-2008 |
20080300234 | PYRIMIDINE DERIVATIVES FOR THE TREATMENT OF ABNORMAL CELL GROWTH - The present invention relates to a compound of the formula 1 | 12-04-2008 |
20080318926 | Methods of Treating Mood Disorders Using Pyridyloxymethyl and Benzisoxazole Azabicyclic Derivatives - An aminomethylpyridyloxymethyl/benzisoxazole substituted azabicyclic compound, a pharmaceutical composition comprising same, and a method of treating a mood disorder selected from the group consisting of Somatization Disorder, Borderline Personality Disorder, Narcissistic Personality Disorder, Suicidal Ideation, and Antisocial Personality Disorder. | 12-25-2008 |
20090012055 | Organic compounds - Novel substituted piperidines of the general formulae (I) and (II) | 01-08-2009 |
20090012056 | Quinoline Compounds Capable of Binding the Cb2 and/or the 5-Ht6 Receptor - The present invention relates to novel quinoline derivatives such as compounds of the formula (I) which possess antagonist potency for the 5-HT | 01-08-2009 |
20090023704 | Novel Compounds 737 - The present invention relates to novel xanthine compounds of the general formula (I) | 01-22-2009 |
20090029966 | COMBINATION THERAPY WITH PARP INHIBITORS - The present invention describes benzimidazole derivatives of Formula (I) which constitute potent PARP inhibitors in combination with temozolomide (TMZ). | 01-29-2009 |
20090042856 | PYRIDAZINONE DERIVATIVES USED FOR THE TREATMENT OF PAIN - A pyridazinone derivative compound shown by the following formula (I): wherein R | 02-12-2009 |
20090048228 | Heterocycle Derivatives As Histone Deacetylase (Hdac) Inhibitors - The present invention relates to compounds of formula I: | 02-19-2009 |
20090054397 | PYRAZOLE COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS COMPRISING THE COMPOUND - The present invention provides a novel compound having an excellent JNK inhibitory effect. That is, it provides a compound represented by the following formula, a salt thereof or a hydrate of them. | 02-26-2009 |
20090069289 | 6-SUBSTITUTED 2-(BENZIMIDAZOLYL)PURINE AND PURINONE DERIVATIVES FOR IMMUNOSUPPRESSION - The present invention provides novel purinones and purines useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection. The compounds are of the general formulae I and II: | 03-12-2009 |
20090075970 | Thieno-and furo-pyrimidine modulators of the histamine H4 receptor - Thieno- and furo-pyrimidine compounds are described, which are useful as H | 03-19-2009 |
20090082332 | PURINE DERIVATIVES FOR THE TREATMENT OF VIRAL OR ALLERGIC DISEASES AND CANCERS - The present invention provides compounds of formula (I) | 03-26-2009 |
20090093454 | Chemical Compounds - The present invention provides compounds of Formula (I) comprising: | 04-09-2009 |
20090093455 | QUINOLONE ANALOGS AND METHODS RELATED THERETO - The present invention provides novel quinolone compounds and pharmaceutical composition thereof which may inhibit cell proliferation and/or induce cell apoptosis. The present invention also provides methods of preparing such compounds and compositions, and methods of making and using the same. | 04-09-2009 |
20090093456 | NOVEL MCH RECEPTOR ANTAGONISTS - The present invention relates to a melanin concentrating hormone antagonist compound of formula (1): wherein R | 04-09-2009 |
20090105210 | Bicyclic Pyrimidines as Dipeptidyl Peptidase-IV Inhibitors for the Treatment or Prevention of Diabetes - The present invention is directed to novel substituted bicyclic pyrimidines which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DPP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. 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 dipeptidyl peptidase-IV enzyme is involved. | 04-23-2009 |
20090105211 | INHIBITORS OF HEDGEHOG PATHWAY - The present invention is directed to a compound of Formula I | 04-23-2009 |
20090105212 | NOVEL ADENINE COMPOUND - A novel adenine compound represented by the formula (1): | 04-23-2009 |
20090105213 | 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. | 04-23-2009 |
20090131399 | Imidazopyridine Derivatives Useful as iNOS Inhibitors - The compounds of formula (I) | 05-21-2009 |
20090131400 | IMMUNOSUPPRESSANT COMPOUNDS AND COMPOSITIONS - The present invention relates to immunosuppressant, process 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. | 05-21-2009 |
20090137550 | Novel Compounds - This invention relates to a novel group of 8-Alkyl/Aryl-4-aryl-2-N-(alkylamino)-N″-substituted-N′-cyanoguanidino-8H-pyrido[2,3-d]pyrimidin-7-one compounds, processes for the preparation thereof, the use thereof in treating CSBP/p38 kinase mediated diseases and pharmaceutical compositions for use in such therapy. | 05-28-2009 |
20090143353 | ANTIFUNGAL BICYCLIC HETERO RING COMPOUNDS - A 1,6-β-glucan synthetase inhibitor is provided, having potent growth inhibition and having excellent safety. | 06-04-2009 |
20090143354 | P2X7 Receptor Antagonists and Their Use - The invention provides compounds of formula (IA), processes for their preparation, pharmaceutical compositions containing them, and their use in therapy. | 06-04-2009 |
20090143355 | Substituted aryl-amine derivatives and methods of use - Selected amines are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds of Formula I and II | 06-04-2009 |
20090149440 | NOVEL PYRIDONECARBOXYLIC ACID DERIVATIVES OR SALTS THEREOF - The present invention provides an agent which exhibits excellent antibacterial activity, low toxicity, improved bioavailability, and low binding rate to serum proteins. The present invention is directed to a pyridonecarboxylic acid derivative represented by formula (1): | 06-11-2009 |
20090149441 | DERIVATIVES OF IMIDAZO[1,2-a]PYRIDINE-2-CARBOXAMIDES, PREPARATION METHOD THEREOF AND USE OF SAME IN THERAPEUTICS - The present invention is related to a compound of formula (I): | 06-11-2009 |
20090156577 | 7-AMINO ALKYLIDENYL-HETEROCYCLIC QUINOLONES AND NAPHTHYRIDONES - The present invention relates to compounds having a structure according to Formula (I) | 06-18-2009 |
20090163471 | Tropane compounds - A compound according to Formula I or II: | 06-25-2009 |
20090163472 | MINERALOCORTICOID RECEPTOR ANTAGONISTS AND METHODS OF USE - The present invention provides a compound of Formula (I): | 06-25-2009 |
20090186869 | Antiviral compounds - The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds. | 07-23-2009 |
20090186870 | Therapeutic Agents - 802 - A compound of formula I | 07-23-2009 |
20090186871 | Tyrosine kinase inhibitors - The present invention relates to compounds that are capable of inhibiting, modulating and/or regulating signal transduction of both receptor-type and non-receptor type tyrosine kinases. The compounds of the instant invention possess a core structure that comprises a sulfonyl indole moiety. The present invention is also related to the pharmaceutically acceptable salts, hydrates and stereoisomers of these compounds. | 07-23-2009 |
20090192138 | COMPOUNDS - The invention provides novel deazaxanthine and deazahypoxanthine compounds. The compounds may be useful in the therapy of diseases and conditions in which dipeptidylpeptidase-IV (DPP-IV) is implicated. | 07-30-2009 |
20090197863 | BENZOXAZOLE CARBOXAMIDE INHIBITORS OF POLY(ADP-RIBOSE)POLYMERASE (PARP) - A compound having the structure set forth in Formula (I) or Formula (II): | 08-06-2009 |
20090197864 | Furo- and Thieno [3,2-c] Pyridines - Furo[3,2-c]Pyridine and Thieno[3,2-c]pyridine compounds of Formula I, and pharmaceutically acceptable salts thereof, preparation, intermediates, pharmaceutical compositions, and use, such as in disease treatment, including cancers, including conditions in which EMT is involved, including conditions mediated by protein kinase activity such as RON and/or MET. | 08-06-2009 |
20090203665 | HETEROCYCLIC-SUBSTITUTED PHENYL METHANONES - The present invention relates to compounds of formula I | 08-13-2009 |
20090247504 | Indazole Derivatives for Treatment of Alzheimer's Disease - Compounds of formula (IA) and (IB) are inhibitors of MARK, and hence are suitable for treatment of Alzheimer's disease. | 10-01-2009 |
20090247505 | SPIRO(5.5)UNDECANE DERIVATIVES - The invention relates to compounds that have an affinity to the μ-opioid receptor and the ORL 1-receptor, methods for their production, medications containing these compounds and the use of these compounds for the treatment of pain and other conditions. | 10-01-2009 |
20090253678 | MACROCYCLIC PYRIMIDINE DERIVATIVES - Macrocyclic pyrimidine compounds, compositions comprising such compounds, methods for making the compounds, and methods of treating and preventing the progression of diseases, conditions, and disorders using such compounds and compositions are described herein. | 10-08-2009 |
20090253679 | NEW IMIDAZOLONE DERIVATIVES, PREPARATION THEREOF AS DRUGS, PHARMACEUTICAL COMPOSITIONS, AND USE THEREOF AS PROTEIN KINASE INHIBITORS, IN PARTICULAR CDC7 - The present invention relates to imidazolone derivatives of formula (I) | 10-08-2009 |
20090258852 | Inhibitors of Checkpoint Kinases - The instant invention provides for compounds which comprise benzoisoquinolinones and aza derivatives that inhibit CHK1 activity. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting CHK1 activity by administering the compound to a patient in need of treatment of cancer. | 10-15-2009 |
20090258853 | Somatostatin Agonists - This invention relates to compounds which are agonists of somatostatin and selective toward somatostatin receptor subtype SSTR2. The compounds are useful in the treatment and prevention of diabetes, and diabetes-related pathologies, including retinopathy, neuropathy and nephropathy. Many of the compounds are orally active. Thus, it is an object of this invention to describe such compounds. It is a further object to describe the specific preferred stereoisomers of the somatostatin agonists. A still further object is to describe processes for the preparation of such compounds. Another object is to describe methods and compositions which use the compounds as the active ingredient thereof. | 10-15-2009 |
20090258854 | Thiazolopyridin-2-yloxy-phenyl and thiazolopyrazin-2-yloxy-phenyl amines as modulators of leukotriene A4 hydrolase - Thiazolopyridin-2-yloxy-phenyl and thiazolopyrazin-2-yloxy-phenyl amine compounds are described, which are useful as LTA4 hydrolase (LTA4H) modulators. Such compounds may be used in pharmaceutical compositions and methods for modulation of LTA4H and for the treatment of disease states, disorders, and conditions mediated by LTA4 hydrolase activity. | 10-15-2009 |
20090258855 | BICYCLIC TRIAZOLES AS PROTEIN KINASE MODULATORS - The present disclosure provides bicyclic triazole protein kinase modulators and methods of using these compounds to treat diseases mediated by kinase activity. | 10-15-2009 |
20090264406 | 3-METHYL-IMIDAZO[1,2-B]PYRIDAZINE DERIVATIVES - The invention relates to compounds of formula (I) and salts thereof | 10-22-2009 |
20090270362 | BICYCLIC MGLUR5 POSITIVE ALLOSTERIC MODULATORS AND METHODS OF MAKING AND USING SAME - In one aspect, the invention relates to bicyclic MGluR5 positive allosteric modulators, for example 6-(phenylethynyl)-3,4-dihydroisoquinolin-1(2H)-one, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. | 10-29-2009 |
20090270363 | 2-Aryl- and 2-Heteroarylthiazolyl Compounds, Methods for Their Preparation and Use Thereof - The present invention discloses fused bicyclic 2-aryl- or 2-heteroarylthiazolyl compounds and their pharmaceutically acceptable salts and esters thereof, which are useful for inhibiting the growth of cancerous cells, inhibiting human breast carcinoma tumor growth in particular and to treat diseases or disorders associated with securin, including elevated securin levels. | 10-29-2009 |
20090270364 | SUBSTITUTED PYRIMIDINE DERIVATIVES - The present application describes substituted pyrimidine compounds of formula (I) | 10-29-2009 |
20090275557 | Novel Composition for Treatment of Diseases Related to Activated Lymphocytes - The present invention relates to inhibiting proliferation and inducing apoptosis in activated lymphocytes, including T cells and B cells. The invention also provides compositions and methods for inhibiting proliferation and inducing apoptosis in activated lymphocytes, as well methods for treating diseases associated with activated lymphocytes by administering 5-HT receptor antagonists. | 11-05-2009 |
20090275558 | SUBSTITUTED SULFONAMIDE COMPOUNDS - Substituted sulfonamide compounds corresponding to formula I | 11-05-2009 |
20090281075 | ISOMERIC PURINONES AND 1H-IMIDAZOPYRIDINONES AS PKC-THETA INHIBITORS - A chemical genus of purinones and 1H-imidazopyridinones, which are useful as PKCθ inhibitors, and their methods of use are disclosed. The genus is represented by the formula I: | 11-12-2009 |
20090281076 | Azetidine Derivatives as G-Protein Coupled Receptor (GPR119) 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. | 11-12-2009 |
20090286767 | SUBSTITUTED QUINOLIN-4-YLAMINE ANALOGUES - Substituted quinolin-4-ylamine analogues are provided. 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 them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies. | 11-19-2009 |
20090286768 | SUBSTITUTED IMIDAZOPYR- AND IMIDAZOTRI-AZINES - Fused pyridine-based bicyclic compounds having the structure of Formula I, as defined herein, pharmaceutically acceptable salts thereof, preparation, compositions, and disease treatment therewith. This abstract does not define or limit the invention. | 11-19-2009 |
20090291937 | 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. | 11-26-2009 |
20090291938 | POLO-LIKE KINASE INHIBITORS - Compounds of the following formula are provided for use with kinases: | 11-26-2009 |
20090312304 | 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 3,4-substituted 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, | 12-17-2009 |
20090312305 | BICYCLIC COMPOUNDS HAVING ACTIVITY AT THE CXCR4 RECEPTOR - A compound represented by the structural formula: | 12-17-2009 |
20090318410 | IMIDAZOPYRIDAZINES AS LIPID KINASE INHIBITORS - The invention relates to novel compounds of the formula I, | 12-24-2009 |
20090318411 | PURINE PI3K INHIBITOR COMPOUNDS AND METHODS OF USE - Purine 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. | 12-24-2009 |
20090325926 | PYRROLO[3,2-D] PYRIMIDINES AS DPP-IV INHIBITORS FOR THE TREATMENT OF DIABETES MELLITUS - The present invention relates to substituted pyrrolo[3,2-d]pyrimidines of formula (I), wherein R1 and R2 are defined as in claim | 12-31-2009 |
20090325927 | Benzofuro- and benzothienopyrimidine modulators of the histamine H4 receptor - Benzofuro- and benzothienopyrimidine compounds are described, which are useful as H | 12-31-2009 |
20090325928 | 6,6-Bicyclic Ring Substituted Heterobicyclic Protein Kinase Inhibitors - Compounds of the formula | 12-31-2009 |
20100004220 | Indenoisoquinolinone Analogs and Methods of Use Thereof - The present invention relates to Indenoisoquinolinone Analogs, compositions comprising an effective amount of an Indenoisoquinolinone Analog and methods for treating or preventing an inflammatory disease, a reperfusion injury, diabetes mellitus, a diabetic complication, reoxygenation injury resulting from organ transplantation, an ischemic condition, a neurodegenerative disease, renal failure, a vascular disease, a cardiovascular disease, cancer, a complication of prematurity, cardiomyopathy, retinopathy, nephropathy, neuropathy, erectile dysfunction or urinary incontinence, comprising administering to a subject in need thereof an effective amount of an Indenoisoquinolinone Analog. | 01-07-2010 |
20100009962 | Benzyl-substituted quinolone m1 receptor positive allosteric modulators - The present invention is directed to benzyl-substituted quinolone compounds of general formula (I) | 01-14-2010 |
20100009963 | KINASE ANTAGONISTS - The present invention provides novel compounds that are antagonists of PI3 kinase, PI3 kinase and tyrosine kinase, PI3 kinase and mTOR, or PI33 kinase, mTOR and tyrosine kinase. | 01-14-2010 |
20100016279 | BICYCLIC DERIVATIVES FOR USE IN THE TREATMENT OF ANDROGEN RECEPTOR ASSOCIATED CONDITIONS-155 - The invention concerns bicyclic compounds of Formula I | 01-21-2010 |
20100016280 | Low Dosage Serotonin 5-HT2A Receptor Agonist To Suppress Inflammation - Activation of 5-HT | 01-21-2010 |
20100022507 | AMINOPYRIMIDINES 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. | 01-28-2010 |
20100029611 | S1P1 receptor agonists and use thereof - The present invention relates to compounds of Formula (I): | 02-04-2010 |
20100035858 | Novel Compositions and Methods for Binding and Inhibiting 5-HT4 Receptor - The present invention relates to compositions that bind to 5-HT4 receptors and inhibit proliferation of activated lymphocytes. The invention also provides methods for inhibiting proliferation and inducing cell death in activated immune cells, as well methods for treating diseases associated with activated immune cells by administering 5-HT4 receptor ligands. | 02-11-2010 |
20100041634 | N-(amino-heteroaryl)-1H-pyrrolopyridine-2-carboxamides derivatives preparation thereof and their use in therapy - The invention relates to compounds of the general formula (I): | 02-18-2010 |
20100041635 | OXINDOLE COMPOUNDS - The invention provides compounds that inhibit PIM kinases and Flt3 kinase, 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. | 02-18-2010 |
20100041636 | NOVEL KINASE INHIBITORS - The present invention provides compounds of Formula (I), and pharmaceutically acceptable salts thereof. The Formula (I) compounds inhibit the tyrosine kinase activity of growth factor receptors such as VEGFR-2, FGFR-1 and IGFR-1, thereby making them useful as anti-cancer agents. The formula (I) compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors. | 02-18-2010 |
20100056491 | 4'-AMINO CYCLIC COMPOUNDS HAVING 5-HT6 RECEPTOR AFFINITY - The present disclosure provides compounds having affinity for the 5-HT | 03-04-2010 |
20100063025 | Substituted isoquinoline and isoquinolinone derivatives as inhibitors of RHO-Kinase - The invention relates to 6-substituted isoquinoline and isochinolone derivatives of the formula (I) | 03-11-2010 |
20100063026 | ANTIBACTERIAL QUINOLINE DERIVATIVES - The present invention relates to novel substituted quinoline derivatives according to the general Formula (Ia) or Formula (Ib): | 03-11-2010 |
20100069351 | SPIRO COMPOUND AND USE THEREOF - The present invention aims to provide a novel SCD inhibitor. | 03-18-2010 |
20100069352 | 5- [4-(AZETIDIN-3-YLOXY)-PHENYL]-2-PHENYL-5H-THIAZOLO[5,4-C] PYRIDIN-4-ONE DERIVATIVES AND THEIR USE AS MCH RECEPTOR ANTAGONISTS - The present invention relates to a melanin concentrating hormone antagonist compound of formula I: wherein “ - - - ” is absent or is optionally a bond; q is 1 or 2; R | 03-18-2010 |
20100069353 | INHIBITORS OF HIV REPLICATION - The present invention relates to compounds of formula (I) wherein R | 03-18-2010 |
20100069354 | 7-AZAINDOLE DERIVATIVES AND THEIR USE IN THE INHIBITION OF C-JUN N-TERMINAL KINASE - The present invention provides a compound of formula (I); or a pharmaceutically acceptable salt thereof, the use of a compound of formula (I) or a pharmaceutically acceptable salt thereof in the inhibition of c-Jun N-terminal kinase (JNK) activity and the use in medicine and particularly in the treatment of neurodegenerative disorders, inflammatory diseases and/or and autoimmune diseases. The invention also provides processes for the manufacture of said compounds of formula (I) or a pharmaceutically acceptable salt thereof and compositions containing them. | 03-18-2010 |
20100069355 | Analogs of Indole-3-Carbinol and Their Use as Agents Against Infection - Compounds useful as antibacterial agents are provided. The compounds are analogs of indole-3-carbinol and have a backbone selected from dihydroindolo[2,3-b]carbazole, 2,2′-diindolylmethane, 2′,3-diindolylmethane, and 3,3′-diindolylmethane. The compounds are useful therapeutic and prophylactic treatment of bacterial infections in mammals. Methods of synthesis of the compounds are provided, as are pharmaceutical compositions containing the compounds. | 03-18-2010 |
20100093696 | 2-AMINO PYRIMIDINE COMPOUNDS - The present invention is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, their synthesis, and their use as HSP-90 inhibitors. | 04-15-2010 |
20100093697 | Substituted Imidazopyridine Derivatives As Melanocortin-4 Receptor Antagonists - The present invention relates to substituted imidazopyridine derivatives as melanocortin-4 receptor (MC-4R) modulators, in particular as melanocortin-4 receptor antagonists. The antagonists are useful for the treatment of disorders and diseases such as cancer cachexia, muscle wasting, anorexia, amytrophic lateral sclerosis (ALS), anxiety and depression. | 04-15-2010 |
20100093698 | AMINOTRIAZOLOPYRIDINES, COMPOSITIONS THEREOF, AND METHODS OF TREATMENT THEREWITH - Provided herein are Heteroaryl Compounds of formula (I): | 04-15-2010 |
20100105652 | PURINES AS CYSTEINE PROTEASE INHIBITORS - Substituted heteroaryl nitrile salt of Formula I, | 04-29-2010 |
20100105653 | PYRROLOPYRIMIDINE COMPOUNDS AND THEIR USES - The disclosed compounds relate to treatments and therapies for protein kinase-associated disorders. There is also a need for compounds useful in the treatment or prevention or amelioration of one or more symptoms of cancer, transplant rejections, and autoimmune diseases. Furthermore, there is a need for methods for modulating the activity of protein kinases, such as CDK1, CDK2, CDK4, CDK5, CDK6, CDK7, CDK8 and CDK9, using the compounds provided herein. | 04-29-2010 |
20100105654 | SUBSTITUTED QUINAZOLINONE COMPOUNDS - A variety of small molecule, guanidine-containing molecules capable of acting as MC4-R agonists are provided. The compounds are useful in treating MC4-R mediated diseases when administered to subjects. The compounds have the structures VA, VB, VIIA and VIIB where the values of the variables are defined herein. | 04-29-2010 |
20100105655 | NOVEL COMPOUNDS 515 - There is provided novel pyrimidine derivatives of formula (I) | 04-29-2010 |
20100105656 | TRIAZOLOPYRAZINE DERIVATIVES - The invention relates to compounds of the formula I | 04-29-2010 |
20100113415 | EPHA4 RTK INHIBITORS FOR TREATMENT OF NEUROLOGICAL AND NEURODEGENERATIVE DISORDERS AND CANCER - The present invention is directed to compounds of generic formula (I) | 05-06-2010 |
20100113416 | JANUS KINASE INHIBITORS FOR TREATMENT OF DRY EYE AND OTHER EYE RELATED DISEASES - Methods, kits, and compositions for treating dry eye disorders and other related eye diseases are provided, wherein the methods, kits, and compositions utilize a JAK inhibitor. | 05-06-2010 |
20100113417 | Substituted Spiroamine Compounds - Substituted spiroamine compounds corresponding to the formula (I) | 05-06-2010 |
20100120741 | HETEROCYCLIC INHIBITORS OF HISTAMINE RECEPTORS FOR THE TREATMENT OF DISEASE - The present invention relates to compounds and methods which may be useful as inhibitors of H | 05-13-2010 |
20100125062 | 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. | 05-20-2010 |
20100130468 | INDOLE CARBOXAMIDES AS IKK2 INHIBITORS - The invention is directed to novel indole carboxamide derivatives. Specifically, the invention is directed to compounds according to formula (I): | 05-27-2010 |
20100130469 | 2, 6-NAPHTHRIDINE DERIVATIVES - The present invention relates to novel organic compounds comprising a naphthyridine which may be mediators of a selective subset of kinases belonging to the AGC kinase family, such as for example PKC, PKD, PKN-1/2, CDK-9, MRCK-beat, PASK, PRKX, ROCK-I/II or mediators of other kinases, the selectivity of which would be depending on the structural variation thereof. | 05-27-2010 |
20100137280 | AZETIDIN COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE SEROTONIN 5-HT6 RECEPTOR - The present invention relates to compounds of formula (I) | 06-03-2010 |
20100144702 | INDOLE COMPOUND - The purpose of the present invention is to provide a glucokinase activator useful as a pharmaceutical agent such as an agent for the prophylaxis or treatment of diabetes, obesity and the like. The present invention provides a glucokinase activator containing a compound represented by the formula (I): wherein R | 06-10-2010 |
20100152158 | Substituted Disulfonamide Compounds - Substituted disulfonamide compounds corresponding to formula I: | 06-17-2010 |
20100152159 | 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. | 06-17-2010 |
20100152160 | NOVEL BENZODIOXANE AND BENZOXAZINE DERIVATIVES USEFUL AS CC CHEMOKINE RECEPTOR LIGANDS - The present invention relates to benzodioxane and benzoxazine derivatives that act as ligands for CC chemokine receptors, such as CCR1. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds. | 06-17-2010 |
20100179122 | Non-Nucleoside Reverse Transcriptase Inhibitors - Compounds of Formula (I): are HIV reverse transcriptase inhibitors, wherein R | 07-15-2010 |
20100179123 | THIENOPYRIMIDINES USEFUL AS AURORA KINASE INHIBITORS - The present invention provides compounds having the formula: | 07-15-2010 |
20100179124 | 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. | 07-15-2010 |
20100184739 | Modulators of ATP-Binding Cassette Transporters - The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators. | 07-22-2010 |
20100190768 | NOVEL FUSED PYROLE DERIVATIVE - The present invention relates to a compound represented by the formula (1) which is useful as a glucocorticoid receptor function regulating agent, an anti-inflammatory agent or an antidiabetic agent, or a pharmaceutically acceptable salt thereof: | 07-29-2010 |
20100190769 | THIAZOLOPYRIMIDINES AND THEIR USE AS INHIBITORS OF PHOSPHATIDYLINOSITOL-3 KINASE - Thiazolopyrimidines of formula (I): wherein W represents a thiazole ring; R | 07-29-2010 |
20100190770 | COMPOSITIONS AND METHODS FOR INHIBITION OF THE JAK PATHWAY - Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful. | 07-29-2010 |
20100190771 | AMINO-HETEROCYCLIC COMPOUNDS - The invention provides PDE9-inhibiting compounds of Formula (I), | 07-29-2010 |
20100197656 | COMPOUNDS FOR THE TREATMENT OF INFLAMMATORY DISEASES - Dihydrothienopyrimidines of formula 1 | 08-05-2010 |
20100210622 | HETEROCYCLIC COMPOUNDS AND METHODS OF USE - In one aspect, the present invention provides for a compound of Formula I | 08-19-2010 |
20100210623 | THERAPEUTIC COMPOUNDS - The present invention relates to pyrazine substituted pyrrolopyridines which are inhibitors of JAK kinases (JAK1, JAK2, JAK3 and/or TYK2) and/or PDK1 and are thus useful for the treatment of myeloproliferative disorders or cancer. | 08-19-2010 |
20100216767 | QUINAZOLINES FOR PDK1 INHIBITION - The invention provides novel compounds that are inhibitors of PDK1. Also provided are pharmaceutical compositions including the compounds, and methods of treating proliferative diseases, such as cancers, with the compounds or compositions. | 08-26-2010 |
20100216768 | N-SUBSTITUTED AZAINDOLES AND METHODS OF USE - The invention relates to N-substituted azaindolyl compounds of Formula I with anti-cancer and/or anti-inflammatory activity and more specifically to N-substituted 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. | 08-26-2010 |
20100222321 | Inhibitors of akt activtiy - The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer. | 09-02-2010 |
20100222322 | Non-Nucleoside Reverse Transcriptase Inhibitors - Indole compounds of Formula (I) are HIV reverse transcriptase inhibitors, wherein R | 09-02-2010 |
20100222323 | 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. | 09-02-2010 |
20100222324 | Substituted Indole Compounds - Substituted indole compounds corresponding to the formula I: | 09-02-2010 |
20100222325 | Inhibitors of Bruton's Tyrosine Kinase - This application discloses 5-phenyl-1H-pyridin-2-one, 6-phenyl-2H-pyridazin-3-one, and 5-Phenyl-1H-pyrazin-2-one derivatives according to generic Formulae I-III: | 09-02-2010 |
20100234347 | Substituted Pteridines substituted with a Four-Membered Heterocycle - The invention relates to novel pteridines of formula (1), | 09-16-2010 |
20100249098 | OXYPIPERIDINE DERIVATIVES AND METHODS OF USE THEREOF - The present invention relates to novel Oxypiperidine Derivatives, pharmaceutical compositions comprising the Oxypiperidine Derivatives and the use of the Oxypiperidine Derivatives for treating or preventing treating allergy, an allergy-induced airway response, congestion, hypotension, a cardiovascular disease, a gastrointestinal disorder, obesity, a sleep disorder, pain, diabetes, a diabetic complication, impaired glucose tolerance, impaired fasting glucose or a central nervous system (CNS) disorder. | 09-30-2010 |
20100249099 | PYRIMIDINYL AND 1,3,5-TRIAZINYL BENZIMIDAZOLE SULFONAMIDES AND THEIR USE IN CANCER THERAPY - Provided herein are pyrimidinyl and 1,3,5-triazinyl benzimidazole sulfonamides, e.g., compounds of Formulae IA, IB, and IC, and their pharmaceutical compositions, preparation, and use as agents or drugs for cancer therapy, either alone or in combination with radiation and/or other anticancer drugs. | 09-30-2010 |
20100249100 | QUINAZOLINES USEFUL AS MODULATORS OF ION CHANNELS - The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels and calcium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders. | 09-30-2010 |
20100261703 | SALT AND CRYSTALLINE FORMS THEREOF OF A DRUG - A crystalline form of a drug, ways to make it, compositions containing it and methods of treatment of diseases and inhibition of adverse physiological events using it are disclosed. | 10-14-2010 |
20100261704 | THERAPEUTIC AGENTS 928 - A compound (2S)-2-[1-(2,6-dichlorophenyl)pyrazolo[4,5-e]pyrimidin-4-yl]oxy-3-(3-hydroxyazetidin-1-yl)-N-(5-methylpyrazin-2-yl)propanamide is useful in the treatment or prevention of a disease or medical condition mediated through glucokinase (GLK or GK), leading to a decreased glucose threshold for insulin secretion. | 10-14-2010 |
20100267688 | 4-AZETIDINYL-1-HETEROARYL-CYCLOHEXANE ANTAGONISTS OF CCR2 - The present invention comprises compounds of Formula (I). | 10-21-2010 |
20100267689 | 4-AZETIDINYL-1-PHENYL-CYCLOHEXANE ANTAGONISTS OF CCR2 - The present invention comprises compounds of Formula (I): | 10-21-2010 |
20100273765 | Rifamycin analogs and uses thereof - The present invention features rifamycin analogs that can be used as therapeutics for treating or preventing a variety of microbial infections. In one form, the analogs are acetylated at the 25-position, as is rifamycin. In another form, the analogs are deacetylated at the 25-position. In yet other forms, benzoxazinorifamycin, benzthiazinorifamycin, and benzdiazinorifamycin analogs are derivatized at various positions of the benzene ring, including 3′-hydroxy analogs, 4′- and/or 6′ halo and/or alkoxy analogs, and various 5′ substituents that incorporate a cyclic amine moiety. | 10-28-2010 |
20100273766 | SUBSTITUTED OXINDOL DERIVATIVES, MEDICAMENTS CONTAINING SAID DERIVATIVES AND USE THEREOF - The invention relates to novel oxindole derivatives of general formula (I), wherein the substituents R | 10-28-2010 |
20100280001 | IMIDAZOQUINOLINES WITH IMMUNO-MODULATING PROPERTIES - The present invention provides compounds of formula (I) | 11-04-2010 |
20100280002 | AMINOPYRIDINE-DERIVATIVES AS INDUCTIBLE NO-SYNTHASE INHIBITORS - The compounds of Formula (I) | 11-04-2010 |
20100286119 | N-(Aminoheteroaryl)-1H-indole-2-carboxamide derivatives, and preparation and therapeutic application thereof - The invention concerns compounds of general formula (I): | 11-11-2010 |
20100292207 | SUBSTITUTED INDAZOLE DERIVATIVES ACTIVE AS KINASE INHIBITORS - Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer. | 11-18-2010 |
20100292208 | COMPOUNDS WITH TWO FUSED BICYCLIC HETEROARYL MOIETIES AS MODULATORS OF LEUKOTRIENE A4 HYDROLASE - Compounds with two fused bicyclic heteroaryl moieties and their pharmaceutical compositions, and methods of using them as leukotriene A | 11-18-2010 |
20100298288 | CETP INHIBITORS DERIVED FROM BENZOXAZOLE ARYLAMIDES - Compounds having the structure of Formula I1 including pharmaceutically acceptable salts of the compounds, are potent CETP (cholesterol ester transfer protein) inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis Atherosclerosis and its clinical consequences, coronary heart disease (CHD), stroke and penpheral vascular disease, represent a truly enormous burden to the health care systems of the industrialized world In formula I, A-B is an arylamide moiety | 11-25-2010 |
20100298289 | HETEROBICYCLIC COMPOUNDS AS HISTAMINE H4-RECEPTOR ANTAGONISTS - The present invention concerns heterobicyclic compounds of formula (I) processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals. | 11-25-2010 |
20100298290 | Benzoxazepines as Inhibitors of PI3K/mTOR and Methods of Their Use and Manufacture - The invention is directed to Compounds of Formula I: | 11-25-2010 |
20100298291 | FUSED BICYCLIC-SUBSTITUTED AMINES AS HISTAMINE-3 RECEPTOR LIGANDS - Compounds of formula (I) | 11-25-2010 |
20100305093 | Inhibitors of mTOR and Methods of Making and Using - The invention is directed to Compounds of Formula I: | 12-02-2010 |
20100311713 | Novel Azetidine Compounds Useful in the Treatment of Functional Gastrointestinal Disorders, Ibs and Functional Dyspepsia - The present invention relates to new azetidine compounds, to pharmaceutical compositions containing them and the use of said compounds in the treatment of functional gastrointestinal disorders, IBS and functional dyspepsia. The compounds are neurokinin (NK) antagonists. The present invention further relates to processes for the preparation of the compounds. | 12-09-2010 |
20100311714 | 1H-IMIDAZO[4,5-c]QUINOLINONE COMPOUNDS - The invention relates to the use of 1H-imidazo[4,5-c]quinolinone compounds and salts thereof in the treatment of protein and/or lipid kinase dependent diseases and for the manufacture of pharmaceutical preparations for the treatment of said diseases; 1H-imidazo[4,5-c]quinolinone compounds for use in the treatment of protein and/or lipid kinase dependent diseases; a method of treatment against said diseases, comprising administering the 1H-imidazo[4,5-c]quinolinone compounds to a warm-blooded animal, especially a human; pharmaceutical preparations comprising an 1H-imidazo[4,5-c]quinolinone compounds, especially for the treatment of a protein and/or lipid kinase dependent disease; novel 1H-imidazo[4,5-c]quinolinone compounds; and a process for the preparation of the novel 1H-imidazo[4,5-c]quinolinone compounds. | 12-09-2010 |
20100311715 | ALPHA CARBOLINES AND USES THEREOF - This invention provides alpha-carboline compounds of formula I: | 12-09-2010 |
20100317650 | IMIDAZOPYRIDINE DERIVATIVES USEFUL AS INOS INHIBITORS - The compounds of formula (I) | 12-16-2010 |
20100324017 | ACYLGUANIDINE DERIVATIVE - An object of the present invention is to provide a novel and excellent agent for treating or preventing dementia, schizophrenia and the like, based on the 5-HT | 12-23-2010 |
20100324018 | PHARMACEUTICAL COMPOSITIONS HAVING IMPROVED DISSOLUTION PROFILES FOR POORLY SOLUBLE DRUGS - Pharmaceutical compositions having improved dissolution profiles for drugs therein is disclosed. | 12-23-2010 |
20100331304 | Compounds Which Modulate The CB2 Receptor - Compounds of formula (I) 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. | 12-30-2010 |
20100331305 | OXO-HETEROCYCLE FUSED PYRIMIDINE COMPOUNDS, COMPOSITIONS AND METHODS OF USE - Disclosed are compounds of Formula I, including steroisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, that are useful in modulating PIKK related kinase signaling, e.g., mTOR, and for the treatment of diseases (e.g., cancer) that are mediated at least in part by the dysregulation of the PIKK signaling pathway (e.g., mTOR). | 12-30-2010 |
20100331306 | 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 p110δ 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. | 12-30-2010 |
20100331307 | THERAPEUTIC COMPOUNDS AND COMPOSITIONS - Compounds and compositions comprising compounds 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. | 12-30-2010 |
20100331308 | OXAZOLIDINONE DERIVATIVES - The invention relates to compounds of Formula (I) | 12-30-2010 |
20110003789 | 5-AMINOCYCLYLMETHYL-OXAZOLIDIN-2-ONE DERIVATIVES - The invention relates to antibacterial compounds of formula I | 01-06-2011 |
20110003790 | PYRIDO [4, 3-D] PYRIMIDINONE DERIVATIVES AS KINASE INHIBITORS - The invention provides a class of compounds of Formula (I), pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly Syk, ZAP70, KDR, FMS, FLT3, c-Kit, RET, TrkA, TrkB, TrkC, IGR-IR, AIk, c-FMS, or combinations thereof. | 01-06-2011 |
20110009380 | QUINOLINE COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE SEROTONIN 5-HT6 RECEPTOR - The present invention relates to novel quinoline compounds. The compounds possess valuable therapeutic properties and are particularly suitable, for treating diseases that respond to modulation of the serotonin 5-HT | 01-13-2011 |
20110009381 | SOLUBILIZED THIAZOLOPYRIDINES - Provided herein are novel sirtuin-modulating compounds Structural Formula (I): and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent. | 01-13-2011 |
20110009382 | Substituted Benzimidazoles, Benzothiazoles and Benzoxazoles - Substituted benzimidazoles, benzothiazoles and benzoxazoles, processes for their preparation, pharmaceutical compostions containing these compounds and the use of these compounds for treating or inhibiting disorders or disease states mediated at least in part by bradykinin receptor 1 (BR1). | 01-13-2011 |
20110015175 | Bicyclic Compounds for the Reduction of Beta-Amyloid Production - The present disclosure provides a series of compounds of the formula (I) | 01-20-2011 |
20110021493 | SUBSTITUTED TRICYCLIC COMPOUNDS AND METHODS OF USE THEREOF - This invention relates to novel compounds and processes for their preparation, methods of treating diseases, particularly cancer, comprising administering said compounds, and methods of making pharmaceutical compositions for the treatment or prevention of disorders, particularly cancer. | 01-27-2011 |
20110021494 | NOVEL TETRAHYDRO-FUSED PYRIDINES AS HISTONE DEACETYLASE INHIBITORS - The compounds of formula (I), wherein ring D and ring E together form a fused ring system selected from formula (II), (III), (IV), (V), (VI), (VII), and the salts of these compounds are novel, effective inhibitors of histone deacetylases. | 01-27-2011 |
20110021495 | QUINAZOLES USEFUL AS MODULATORS OF ION CHANNELS - The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels and calcium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders. | 01-27-2011 |
20110021496 | THIENOPYRIMIDINE DERIVATIVES AS P13K INHIBITORS - Thienopyrimidines of formula (I) wherein W and R | 01-27-2011 |
20110021497 | AMINO TRIAZOLES AS PI3K INHIBITORS - The invention relates to compounds of formula (I) | 01-27-2011 |
20110021498 | INDOLYL- PYRIDONE DERIVATIVES HAVING CHECKPOINT KINASE 1 INHIBITORY ACTIVITY - Compounds of formula (I) have checkpoint kinase 1 (CHK1) inhibitory activity: wherein R | 01-27-2011 |
20110028450 | Ring-annulated dihydropyrrolo[2,1-alpha]isoquinolines - The invention relates to ring-annulated dihydropyrrolo[2,1-a]isoquinoline compounds according to general Formula I | 02-03-2011 |
20110028451 | Dihydrobenzoindazoles - The invention relates to benzoindazole derivatives according to general Formula I | 02-03-2011 |
20110028452 | PYRIDO[4,3-d]PYRIMIDIN-4(3H)-ONE DERIVATIVES AS CALCIUM RECEPTOR ANTAGONISTS - The present invention is directed to novel pyrido[4,3-d]pyrimidin-4(3H)-one derivatives and pharmaceutically acceptable salts thereof of structural formula I | 02-03-2011 |
20110039823 | OXAZOLIDINONE ANTIBIOTICS - The invention relates to compounds of formula (I) wherein U, V, W, X, R1, R2, R3, R4, R5, R6, A, B, D, E, G, m, and n are as defined in the description, to pharmaceutically acceptable salts of such compounds for use in the manufacture of a medicament for the prevention or treatment of a bacterial infection. Certain compounds of formula (I) are new and are also part of this invention. | 02-17-2011 |
20110046110 | QUINOLINES AND RELATED ANALOGS AS SIRTUIN MODULATORS - Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent. | 02-24-2011 |
20110053909 | Compounds - 801 - Spirocyclic amide derivatives of formula I | 03-03-2011 |
20110059946 | DUAL ACTION ANTIBIOTICS - The present invention relates to compounds of the Formula (I) that are useful antimicrobial agents and effective against a variety of multi-drug resistant bacteria: | 03-10-2011 |
20110071130 | 2-AMINOBENZIMIDAZOLES FOR TREATING NEURODEGENERATIVE DISEASES - The invention relates to 2-aminobenzimidazoles useful in treating disorders that are mediated by A | 03-24-2011 |
20110071131 | Substituted Spirocyclic Piperidine Derivatives as Histamine-3 (H3) Receptor Ligands - The present invention provides compounds of Formula (I): | 03-24-2011 |
20110071132 | SUBSTITUTED OXINDOLE DERIVATIVES, DRUGS CONTAINING SAID DERIVATIVES AND THE USE THEREOF - The invention relates to novel oxindol derivative of general formula (I), wherein substituents R | 03-24-2011 |
20110071133 | BICYCLIC ARYL AND BICYCLIC HETEROARYL SUBSTITUTED TRIAZOLES USEFUL AS AXL INHIBITORS - Bicyclic aryl substituted triazoles or heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed. | 03-24-2011 |
20110077235 | APOPTOSIS SIGNAL-REGULATING KINASE 1 INHIBITORS - The present invention relates to apoptosis signal-regulating kinase 1 (“ASK1”) inhibiting compounds of the formula (I); wherein the variables are as defined herein. The invention also relates to pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds. | 03-31-2011 |
20110086840 | N-7 SUBSTITUTED PURINE AND PYRAZOLOPYRIMINE COMPOUNDS, COMPOSITIONS AND METHODS OF USE - The present invention relates to compounds of Formula I: | 04-14-2011 |
20110086841 | N-9 SUBSTITUTED PURINE COMPOUNDS, COMPOSITIONS AND METHODS OF USE - The present invention relates to compounds of Formula I: | 04-14-2011 |
20110092478 | DIAZABENZO[DE] ANTHRACEN-3-ONE COMPOUNDS AND METHODS FOR INHIBITING PARP - The present invention relates to diazabenzo[de]anthracen-3-one compounds which inhibit poly(ADP-ribose) polymerase (“PARP”), compositions containing these compounds and methods for using these PARP inhibitors to treat, prevent and/or ameliorate the effects of the conditions described herein. | 04-21-2011 |
20110092479 | PYRAZOLE [3, 4-B] PYRIDINE RAF INHIBITORS - Compounds of Formula I are useful for inhibition of Raf kinases. Methods of using compounds of Formula I and stereoisomers, tautomers, prodrugs and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed. | 04-21-2011 |
20110092480 | Substituted Heterocyclic Derivatives and Their Pharmaceutical Use and Compositions - Compounds of the general Formula I, wherein X | 04-21-2011 |
20110092481 | QUINOLINE OR ISOQUINOLINE SUBSTITUTED P2X7 ANTAGONISTS - The present invention is related to novel compounds of formula (I) having P2X7 antagonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment or prophylaxis of diseases associated with P2X7 receptor activity in animals, in particular humans. (I) | 04-21-2011 |
20110105464 | PHOSPHOINOSITIDE 3-KINASE INHIBITOR COMPOUNDS AND METHODS OF USE - Methods of using compounds of Formula Ia and Ib for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. | 05-05-2011 |
20110124627 | MODULATORS OF TOLL-LIKE RECEPTORS - The present application includes novel modulators of TLRs, compositions containing such compounds, therapeutic methods that include the administration of such compounds. | 05-26-2011 |
20110124628 | APOPTOSIS-INDUCING AGENTS FOR THE TREATMENT OF CANCER AND IMMUNE AND AUTOIMMUNE DISEASES - Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein. | 05-26-2011 |
20110144083 | Xanthine Derivatives, the Preparation Thereof and Their Use as Pharmaceutical Compositions - The present invention relates to substituted xanthines of general formula | 06-16-2011 |
20110144084 | 6 SUBSTITUTED 2- HETEROCYCLYLAMINO PYRAZINE COMPOUNDS AS CHK-1 INHIBITORS - The present invention is directed to compounds of formula (I), | 06-16-2011 |
20110144085 | TRIAZOLOPYRIDINE COMPOUNDS AS PIM KINASE INHIBITORS - Compounds of Formula (I), in which A, B, R | 06-16-2011 |
20110152242 | 2,3-Substituted Fused Pyrimidin -4 (3H)-Ones as VR1 Antagonists - A compound of formula (I), wherein W is formula (1); A is a benzene ring, a fÊve-membered heteroaromatic ring containing 1, 2 or 3 heteroatoms independently chosen from O, N and S, providing that no more than one O or S atom is present, or a six-membered heteroaromatic ring containing 1, 2 or 3 N atoms; n is zero, one, two or three; when n is zero or one, V is CH | 06-23-2011 |
20110152243 | NOVEL THIENOPYRROLE COMPOUNDS - The invention provides a compound of Formula (I) | 06-23-2011 |
20110152244 | PYRROLOPYRIMIDINE COMPOUNDS AND THEIR USES - The disclosed compounds relate to treatments and therapies for protein kinase-associated disorders. There is also a need for compounds useful in the treatment or prevention or amelioration of one or more symptoms of cancer, transplant rejections, and autoimmune diseases. Furthermore, there is a need for methods for modulating the activity of protein kinases, such as CDK1, CDK2, CDK4, CDK5, CDK6, CDK7, CDK8 and CDK9, using the compounds provided herein. | 06-23-2011 |
20110160183 | INHIBITORS OF AKT ACTIVITY - The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer. | 06-30-2011 |
20110166123 | NOVEL COMPOSITIONS AND METHODS OF USE - Described herein are novel enzyme inhibitors. In some embodiments the enzyme inhibitors are integrase inhibitors, particularly HIV integrase 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 integrase as a method of treating or preventing HIV, AIDS or related disorders. | 07-07-2011 |
20110166124 | TRICYCLIC SPIROCYCLE DERIVATIVES AND METHODS OF USE - The present invention relates to novel Tricyclic Spirocycle Derivatives, pharmaceutical compositions comprising the Tricyclic Spirocycle Derivatives and the use of these compounds for treating or preventing allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disorder, a metabolic disorder, obesity or an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or aired fasting glucose. | 07-07-2011 |
20110172203 | Substituted Imidazopyridinyl-Aminopyridine Compounds - The present invention relates to substituted imidazopyridinyl-aminopyridine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted imidazopyridinyl-aminopyridine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof. | 07-14-2011 |
20110172204 | COMPOUNDS AND THEIR USE - A compound of the formula: | 07-14-2011 |
20110190262 | Aryl-and Heteroarylcarbonyl derivatives of benzomorphanes and related scaffolds, medicaments containing such compounds and their use - The present invention relates to compounds defined by formula I | 08-04-2011 |
20110190263 | COMPOUNDS AND COMPOSITIONS AS MODULATORS OF GPR119 ACTIVITY - The invention provides compounds of Formula (I): pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of GPR119. | 08-04-2011 |
20110190264 | COMPOUNDS AND COMPOSITIONS AS KINASE INHIBITORS - The invention relates to triazine and pyrimidine derivatives having Formula (1) or (2), and methods for using such compounds. For example, the compounds of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of anaplastic lymphoma kinase (ALK) activity, c-ros oncogene (ROS), insulin-like growth factor (IGF-IR), and/or insulin receptor (InsR) or a combination thereof. | 08-04-2011 |
20110190265 | METHODS AND COMPOSITIONS FOR TREATING BACTERIAL INFECTIONS BY INHIBITING QUORUM SENSING - The present invention provides methods for treating bacterial infections in a subject comprising administering to the subject a sub-growth inhibiting amount of a 5′-Methylthioadenosine/S-adenosyl homocysteine nucleosidase (MTAN) inhibitor. The present invention further provides pharmaceutical compositions comprising a sub-bacterial-growth inhibiting amount of a 5′-Methylthioadenosine/S-adenosyl homocysteine nucleosidase (MTAN) inhibitor and a pharmaceutically acceptable carrier. | 08-04-2011 |
20110190266 | 5,6,6a,7,8,9-HEXAHYDRO-2H-PYRIDOPHTHALAZINONE INHIBITORS OF POLY(ADP-RIBOSE)POLYMERASE (PARP) - Provided herein are compounds having the structure set forth in Formula (I): | 08-04-2011 |
20110195949 | 2-BENZOTHIOPHENYL- AND 2-NAPHTHYL-OXAZOLIDINONES AND THEIR AZAISOSTERE ANALOGUES AS ANTIBACTERIAL AGENTS - The invention relates to antibacterial compounds of formula (I) | 08-11-2011 |
20110201594 | PYRIDO [2,3-D] PYRIMIDINES AND THEIR USE AS KINASE INHIBITORS - The present invention provides derivatives of pyrido[2,3-d]pyrimidin-7-one. These compounds are kinase inhibitors, including compounds that show anti-proliferative activity, including against tumor cells, and are useful in the treatment of diseases including cancer. | 08-18-2011 |
20110201595 | OXAZOLIDINYL ANTIBIOTICS - The invention relates to antibacterial compounds of formula I | 08-18-2011 |
20110207713 | PYRIDO[3,2-d]PYRIMIDINE PI3K DELTA INHIBITOR 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. | 08-25-2011 |
20110207714 | SEROTONIN RECEPTOR MODULATORS - The biphenyic compounds of formula (I) are serotonin modulators useful in the treatment of serotonin-mediated diseases. | 08-25-2011 |
20110218184 | QUINOLONE ANALOGS AND METHODS RELATED THERETO - The present invention provides novel quinolone compounds and pharmaceutical composition thereof which may inhibit cell proliferation and/or induce cell apoptosis. The present invention also provides methods of preparing such compounds and compositions, and methods of making and using the same. | 09-08-2011 |
20110218185 | AZOLOTRIAZINONE MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS - The present application provides compounds that are useful as MCHR1 antagonists, especially for the treatment of obesity, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I | 09-08-2011 |
20110224190 | PIPERIDIN-4-YL AZETIDINE DERIVATIVES AS JAK1 INHIBITORS - The present invention provides piperidin-4-yl azetidine derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase 1 (JAK1) and are useful in the treatment of diseases related to the activity of JAK1 including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases. | 09-15-2011 |
20110224191 | Substituted Pyrrolo[2,3-b]-Pyridines and -Pyrazines - Compounds of Formula I, as shown below and defined herein: (I) pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers mediated at least in part by Ron and/or Met. | 09-15-2011 |
20110230464 | PURINE DERIVATIVES USEFUL AS P13 KINASE INHIBITORS - This invention provides a compound which is a purine of formula (Ia) or (Ib): and the pharmaceutically acceptable salts thereof that are inhibitors of PI3K and a selective for the p110δ isoform, which is a class Ia PI3 kinase, over other class Ia PI3 kinases and over class Ib kinases. The compounds may be used to treat diseases and disorders arising from abnormal cell growth, function or behaviour associated with PI3 kinase such as cancer immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine function disorders and neurological disorders. | 09-22-2011 |
20110230465 | VIRAL POLYMERASE INHIBITORS - Compounds of formula I: | 09-22-2011 |
20110237565 | HETEROCYCLIC INHIBITORS OF HISTAMINE RECEPTORS FOR THE TREATMENT OF DISEASE - The present invention relates to compounds and methods which may be useful as inhibitors of H | 09-29-2011 |
20110245229 | DIHYDROPYRAZOLOPYRIMIDINONE DERIVATIVES - The invention relates to compounds represented by the general formula (I) and the like. In the formula, Ar | 10-06-2011 |
20110245230 | PYRIMIDYL CYCLOPENTANES AS AKT PROTEIN KINASE INHIBITORS - The present invention provides compounds of Formula I, including tautomers, resolved enantiomers, diastereomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof. | 10-06-2011 |
20110257156 | GAMMA SECRETASE MODULATORS - In its many embodiments, the present invention provides novel heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions. | 10-20-2011 |
20110263561 | Novel pyrrolidone derivatives for use as MetAP-2 inhibitors - Compounds of the formula (I), in which R, X, Y, Z, R | 10-27-2011 |
20110263562 | BICYCLIC COMPOUND - The present invention provides to a compound having an ACC inhibitory action, which is useful as an agent for the prophylaxis or treatment of obesity, diabetes, hypertension, hyperlipidemia, cardiac failure, diabetic complications, metabolic syndrome, sarcopenia, cancer and the like, and has superior efficacy. | 10-27-2011 |
20110263563 | Ansamycin Hydroquinone Compositions - Aspects of the present invention provide compositions comprising a sulfur containing compound and a compound of the formula (I); and also provide methods of their preparation and use. | 10-27-2011 |
20110263564 | PYRIDINE, BICYCLIC PYRIDINE AND RELATED ANALOGS AS SIRTUIN MODULATORS - Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent. | 10-27-2011 |
20110263565 | COMPOUNDS - The present invention encompasses compounds of general formula (1), wherein R | 10-27-2011 |
20110263566 | 7-Hydroxy-benzoimidazole-4-yl-methanone Derivatives and PBK Inhibitors Containing the Same - 7-Hydroxy-benzoimidazole-4-yl-methanone Derivatives, which are useful for PBK inhibitors, are provided. | 10-27-2011 |
20110269739 | KINASE INHIBITORS - The present invention provides a new group of protein kinase inhibitors, pyrido[4,3,-d]pyrimidin-5-one derivatives, and pharmaceutically acceptable salts thereof that are useful for intreating cell proliferative disease and disorder such as cancer, autoimmune diseases, infection, cardiovascular disease and neurodegenerative disease and disorder. The present invention provides methods for synthesizing and administering the protein kinase inhibitor compounds. The present invention also provides pharmaceutical formulations comprising at least one of the protein kinase inhibitor compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor. The invention also provides useful intermediates generated during the syntheses of the pyrido[4,3,-d]pyrimidin-5-one derivatives. | 11-03-2011 |
20110269740 | JAK KINASE MODULATING COMPOUNDS AND METHODS OF USE THEREOF - Provided herein are pyrrolotriazine compounds for treatment of JAK kinase, including JAK2 kinase mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions. | 11-03-2011 |
20110269741 | NOVEL COMPOSITIONS AND METHODS OF USE - Described herein are novel enzyme inhibitors. In some embodiments the enzyme inhibitors are integrase inhibitors, particularly HIV integrase 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 integrase as a method of treating or preventing HIV, AIDS or related disorders. | 11-03-2011 |
20110269742 | Serotonin 5-HT2B Receptor Inhibitors - Disclosed are Serotonin 5-HT2B receptor inhibitors of the formula I. Also disclosed are methods of making and methods of using these compounds. | 11-03-2011 |
20110275611 | CHEMICAL COMPOUNDS - The invention is directed to 6-(4-pyrimidinyl)-1H-indazole derivatives. Specifically, the invention is directed to compounds according to Formula (I) wherein R | 11-10-2011 |
20110281841 | Kinase Inhibitors - The present invention provides a new group of protein kinase inhibitors, pyrropyrimidine and pyrazolopyrimidine derivatives, and pharmaceutically acceptable salts and prodrugs thereof that are useful for treating cell proliferative disease and disorder such as cancer, autoimmune diseases, infection, cardiovascular disease and neurodegenerative disease and disorder. The present invention provides methods for synthesizing and administering the protein kinase inhibitor compounds. The present invention also provides pharmaceutical formulations comprising at least one of the protein kinase inhibitor compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor. The invention also provides useful intermediates generated during the syntheses of the pyrropyrimidine and pyrazolopyrimidine derivatives. | 11-17-2011 |
20110281842 | PYRROLOPYRIDINE AND PYRROLOPYRIMIDINE INHIBITORS OF KINASES - The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, | 11-17-2011 |
20110281843 | SUBSTITUTED INDAZOLE DERIVATIVES ACTIVE AS KINASE INHIBITORS - Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer. | 11-17-2011 |
20110288069 | Benzodiazepine and Pyridodiazepine Derivatives - The present application relates to benzodiazepine and pyridodiazepine derivatives of formula (I) | 11-24-2011 |
20110294780 | SUBSTITUTED THIAZOLIDINEDIONE INDAZOLES, INDOLES AND BENZOTRIAZOLES AS ESTROGEN-RELATED RECEPTOR-a MODULATORS - The present invention relates to compounds of Formula (I), | 12-01-2011 |
20110294781 | PYRAZOLO-PYRIMIDINE COMPOUNDS - The present invention has searched for a variety of compounds which show IL-12/IL-23 production-inhibitory activities and herein provides a pharmaceutical composition and an agent for preventing or treating IL-12/IL-23 excess production-related diseases, which comprise the compound. | 12-01-2011 |
20110301144 | Kinase Antagonists - The present invention provides novel compounds that are antagonists of PI3 kinase, PI3 kinase and tyrosine kinase, PI3 kinase and mTOR, or PI33 kinase, mTOR and tyrosine kinase. | 12-08-2011 |
20110301145 | PYRIDAZINONES, 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. | 12-08-2011 |
20110301146 | GLYCOGEN SYNTHASE KINASE-3 BETA INHIBITORS CONTAINING 7-HYDROXY-BENZOIMIDAZOLE-4-YL-METHANONE DERIVATIVES - GSK-3beta inhibitors comprising 7-Hydroxy-benzoimidazole-4-yl-methanone Derivatives are provided. For example, the inhibitors have following general formula (I). | 12-08-2011 |
20110306592 | CYCLOHEXYL-AZETIDINYL ANTAGONISTS OF CCR2 - The present invention comprises compounds of Formula (I). | 12-15-2011 |
20110312934 | 2-ALKYL-6-CYCLOAMINO-3-(PYRIDIN-4-YL)IMIDAZO[1,2-B]-PYRIDAZINE DERIVATIVES, PREPARATION THEREOF, AND THERAPEUTIC APPLICATION THEREOF - The invention relates to 2-alkyl-6-cycloamino-3-(pyridin-4-yl)imidazo[1,2-b]pyridazine derivatives of the general formula (I) where: R | 12-22-2011 |
20110312935 | 1H-Benz Imidazole-5-Carboxamides As Anti-Inflammatory Agents - There are provided compounds of formula (I), wherein R | 12-22-2011 |
20110312936 | CYCLOHEXYL-AZETIDINYL ANTAGONISTS OF CCR2 - The present invention comprises compounds of Formula I. | 12-22-2011 |
20110319380 | Compounds for Treating Disorders Mediated by Metabotropic Glutamate Receptor 5, and Methods of Use Thereof - Provided herein are compounds and methods of synthesis thereof. The compounds set forth herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders, neurodegenerative disorders, neuropsychiatric disorders, disorders of cognition, learning or memory, gastrointestinal disorders, lower urinary tract disorder, and cancer. Compounds set forth herein modulate the activity of metabotropic glutamate receptor 5 (mGluR5) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein. | 12-29-2011 |
20110319381 | DERIVATIVES OF AZASPIRANYL-ALKYLCARBAMATES OF 5-MEMBER HETEROCYCLIC COMPOUNDS, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF - The invention relates to a compound of the general formula (I) in which R | 12-29-2011 |
20120010191 | PYRIDONE AND AZA-PYRIDONE COMPOUNDS AND METHODS OF USE - Pyridone and aza-pyridone compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. | 01-12-2012 |
20120010192 | 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: | 01-12-2012 |
20120010193 | CGRP RECEPTOR ANTAGONISTS - Compounds of Formula (I) (wherein variables A | 01-12-2012 |
20120022043 | PYRAZOLOPYRIMIDINE JAK INHIBITOR COMPOUNDS AND METHODS - The invention provides JAK kinase inhibitors of Formula Ia, enantiomers, diasteriomers or pharmaceutically acceptable salts thereof, wherein R | 01-26-2012 |
20120028955 | BICYCLIC MGLUR5 POSITIVE ALLOSTERIC MODULATORS AND METHODS OF MAKING AND USING SAME - In one aspect, the invention relates to bicyclic mGluR5 positive allosteric modulators, for example 6-(phenylethynyl)-3,4-dihydroisoquinolin-1(2H)-one, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. | 02-02-2012 |
20120028956 | BICYCLIC MGLUR5 POSITIVE ALLOSTERIC MODULATORS AND METHODS OF MAKING AND USING SAME - In one aspect, the invention relates to bicyclic mGluR5 positive allosteric modulators, for example 6-(phenylethynyl)-3,4-dihydroisoquinolin-1(2H)-one, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. | 02-02-2012 |
20120035154 | Modulators of Cellular Adhesion - The present invention provides compounds having formula (I): | 02-09-2012 |
20120035155 | INDOLE-2-CARBOXAMIDE DEIVATIVE - To provide an indole compound having a human QRFP receptor antagonistic activity and useful as a preventive or a remedy for various disorders. A compound of a formula (I) or a pharmaceutically-acceptable salt thereof is provided: [wherein, R | 02-09-2012 |
20120040957 | Novel Bicyclic Antibiotics - Compounds of formula (I) wherein X1, X3; X4 and X6, each independently of the others, represents a nitrogen atom or CR2, with the proviso that at least one of X1, X3; X4 and X6 represents a nitrogen atom; X2 represents C—H, C—(C1-C6alkyl), C—(C1-C6alkoxy), C-halogen, C—COOH; X5 represents C—H or C—(C1-C6alkyl), C-halogen; R1 and R2, independently of one another, represent hydrogen or a substituent selected from hydroxy, halogen, carboxy, amino, C1-C6alkylamino, di(C1-C6alkyl)amino, mercapto, cyano, nitro, C1-C6alkyl, C1-C6alkoxy, C1-C6alkylthio, C1-C6alkylamino-carbonyloxy, C2-C6alkenyl, C2-C6alkynyl, C1-C6alkylcarbonyloxy, C1-C6alkyl-sulfonyloxy, C1-C6heteroalkylcarbonyloxy, C5-C6heterocyclyl-carbonyloxy, C1-C6heteroalkyl, C1-C6heteroalkoxy, wherein heteroalkyl, heteroalkoxy groups or heterocyclyl comprise 1, 2 or 3 heteroatoms selected from nitrogen, oxygen and sulphur, in which substituents the alkyl moieties are unsubstituted or further substituted by halogeno, cyano, hydroxy, C1-C4alkoxy, C1-C4alkylcarbonyl, C1-C4alkoxycarbonyl, unsubstituted or substituted phenoxy or phenylcarbonyl, unsubstituted or substituted C5-C6heterocyclyl or carboxy; A1 represents a divalent group of one of the formulae —O—(CH | 02-16-2012 |
20120040958 | INDOLE CARBOXAMIDES AS IKK2 INHIBITORS - The invention is directed to novel indole carboxamide compounds. Specifically, the invention is directed to compounds according to formula (I): | 02-16-2012 |
20120040959 | 8-METHOXY-9H-ISOTHIAZOLO[5,4-B]QUINOLINE-3,4-DIONES AND RELATED COMPOUNDS AS ANTI-INFECTIVE AGENTS - The invention provides compound and salts of Formula I and II, disclosed herein, which includes compounds of Formula A and Formula B: | 02-16-2012 |
20120040960 | 4-AZETIDINYL-1-PHENYL-CYCLOHEXANE ANTAGONISTS OF CCR2 - The present invention comprises compounds of Formula (I): | 02-16-2012 |
20120046269 | Novel Amino Azaheterocyclic Carboxamides - The invention provides novel substituted amino azaheterocyclic carboxamide compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer. | 02-23-2012 |
20120058988 | CARBAZOLE AND CARBOLINE KINASE INHIBITORS - The present invention provides compounds of Formula (I) | 03-08-2012 |
20120065186 | ANTIMICROBIAL COMPOSITIONS - The present invention relates to antimicrobial compositions and more specifically compositions of quinolone carboxylic acid derivatives. These compositions have improved solubility, stability, and tolerability. These compositions are useful for intravenous administration for treating, preventing, or reducing the risk of infection. | 03-15-2012 |
20120065187 | HETEROCYCLIC INHIBITORS OF HISTAMINE RECEPTORS FOR THE TREATMENT OF DISEASE - The present invention relates to compounds and methods which may be useful as inhibitors of H | 03-15-2012 |
20120065188 | SUBSTITUTED HETEROCYCLIC DERIVATIVES AND THEIR PHARMACEUTICAL USE AND COMPOSITIONS - Compounds of the general Formula I, wherein X | 03-15-2012 |
20120071461 | Substituted Benzamide Compounds - Substituted benzamide compounds corresponding to formula (I) | 03-22-2012 |
20120077799 | HETEROCYCLIC COMPOUND AND USE THEREOF - Provided is a compound represented by the formula (I): | 03-29-2012 |
20120094974 | SMOOTHENED RECEPTOR MODULATORS - The present invention relates, in general, to the Smoothened receptor and, in particular, to a method of modulating Smoothened receptor activity and to compounds and compositions suitable for use in such a method. | 04-19-2012 |
20120094975 | PYRIDO [5, 4-D] PYRIMIDINES AS CELL PROLIFERATION INHIBITORS - The present invention encompasses compounds of general formula (1) wherein the groups R | 04-19-2012 |
20120094976 | NEW CHEMICAL COMPOUNDS - The present invention encompasses compounds of general formula (1) | 04-19-2012 |
20120101084 | Biological Markers Predictive of Anti-Cancer Response to Insulin-Like Growth Factor-1 Receptor Kinase Inhibitors - The present invention provides diagnostic and prognostic methods for predicting the effectiveness of treatment of a cancer patient with an IGF-1R kinase inhibitor. Methods are provided for predicting the sensitivity of tumor cell growth to inhibition by an IGF-1R kinase inhibitor, comprising assessing whether the tumor cell has undergone an epithelial to mesenchymal transition (EMT), by determining the expression level of epithelial and/or mesenchymal biomarkers, wherein tumor cells that have undergone an EMT are substantially less sensitive to inhibition by IGF-1R kinase inhibitors. Improved methods for treating cancer patients with IGF-1R kinase inhibitors that incorporate the above methodology are also provided. Additionally, pErk, HER | 04-26-2012 |
20120108569 | 8-AZA Tetracycline Compounds - The present invention is directed to a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. The variables for Structural Formula I are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula I and its therapeutic use. | 05-03-2012 |
20120115846 | QUINAZOLINEDIONE DERIVATIVES, PREPARATION THEREOF AND VARIOUS THERAPEUTIC USES THEREOF. - The subject matter of the invention is quinazolinedione derivatives of formula (I), methods for obtaining same and therapeutic uses thereof, such as cancer, diabetes, muscle diseases, bone diseases, cardiovascular diseases, central nervous system diseases, peripheral nervous system diseases, inter alia. | 05-10-2012 |
20120122840 | COMPOUNDS AND THERAPEUTIC USES THEREOF - The invention relates to compounds, pharmaceutical compositions, and uses thereof, including therapeutic uses thereof, such as methods useful for treating cancer. | 05-17-2012 |
20120122841 | Biological Markers Predictive Of Anti-Cancer Response To Insulin-like Growth Factor-1 Receptor Kinase Inhibitors - The present invention provides diagnostic and prognostic methods for predicting the effectiveness of treatment of a cancer patient with an IGF-1R kinase inhibitor. Methods are provided for predicting the sensitivity of tumor cell growth to inhibition by an IGF-1R kinase inhibitor, comprising assessing whether the tumor cell has undergone an epithelial to mesenchymal transition (EMT), by determining the expression level of epithelial and/or mesenchymal biomarkers, wherein tumor cells that have undergone an EMT are substantially less sensitive to inhibition by IGF-1R kinase inhibitors. Improved methods for treating cancer patients with IGF-1R kinase inhibitors that incorporate the above methodology are also provided. | 05-17-2012 |
20120122842 | 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. | 05-17-2012 |
20120142669 | N-(amino-heteroaryl)-1H-pyrrolopyridine-2-carboxamides derivatives preparation thereof and their use in therapy - The invention relates to compounds of the general formula (I): | 06-07-2012 |
20120142670 | N-(amino-heteroaryl)-1H-pyrrolopyridine-2-carboxamides derivatives preparation thereof and their use in therapy - The invention relates to compounds of the general formula (I): | 06-07-2012 |
20120149680 | 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. | 06-14-2012 |
20120149681 | CYCLOBUTYL SUBSTITUTED PYRROLOPYRIDINE AND PYRROLOPYRIMIDINE DERIVATIVES AS JAK INHIBITORS - The present invention provides cyclobutyl substituted pyrrolopyrimidines and pyrrolopyridines of Formula I: | 06-14-2012 |
20120149682 | HETEROCYCLIC-SUBSTITUTED PYRROLOPYRIDINES AND PYRROLOPYRIMIDINES AS JAK INHIBITORS - The present invention provides heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines of Formula I: | 06-14-2012 |
20120149683 | SUBSTITUTED AMINOPIPERIDINES AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS FOR THE TREATMENT OF DIABETES - The present invention is directed to novel substituted aminopiperidines of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-ÏV enzyme is involved, such as diabetes and particularly Type 2 diabetes. 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 dipeptidyl peptidase-IV enzyme is involved. | 06-14-2012 |
20120149684 | AKT INHIBITORS - The present invention provides AKT inhibitors of the formula: Formula I The present invention also provides pharmaceutical compositions comprising compounds of Formula I, uses of compounds of Formula I and method of using compounds of Formula I. | 06-14-2012 |
20120157434 | Antimicrobial heterocyclic compounds for treatment of bacterial infections - The present invention provides heterocyclic compounds of the following formula I: | 06-21-2012 |
20120157435 | Antiviral Compounds - Compounds and methods for preventing and treating viral infections are provided. In some embodiments, novel compounds broad-spectrum antiviral activity are provided. In more specific embodiments, the compounds and methods are effective against viruses such as Venezuelan Equine Encephalitis, West Nile Virus, and respiratory viruses including the common cold. | 06-21-2012 |
20120157436 | 5,6,7,8-TETRAHYDRO[1,2,4]TRIAZOLO[4,3-a]PYRAZINE DERIVATIVES AS P2X7 MODULATORS - The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof: | 06-21-2012 |
20120157437 | VLA-4 INHIBITORY DRUG - This invention relates to a VLA-4 inhibitory drug, having good oral absorbability and exhibiting sufficient anti-inflammatory effects when administered orally, wherein an active ingredient is represented by formula (I), or a salt thereof: | 06-21-2012 |
20120157438 | PYRANYL ARYL METHYL BENZOQUINAZOLINONE M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS - The present invention is directed to pyranyl aryl methyl benzoquinazolinone 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. | 06-21-2012 |
20120157439 | RAF INHIBITOR COMPOUNDS AND METHODS OF USE THEREOF - Compounds of Formula I are useful for inhibition of Raf kinases. Methods of using compounds of Formula I and stereoisomers, tautomers, prodrugs and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed. | 06-21-2012 |
20120165309 | HETERO RING DERIVATIVE | 06-28-2012 |
20120165310 | ETHER DERIVATIVES OF BICYCLIC HETEROARYLS - The invention relates to compounds of formula I, | 06-28-2012 |
20120165311 | 1H-THIENO[2,3-C]PYRAZOLE DERIVATIVES USEFUL AS KINASE INHIBITORS - Thieno[2,3-c]pyrazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer. | 06-28-2012 |
20120178737 | Tricyclic Heterocyclic Compounds as Phosphoinositide 3-Kinase Inhibitors - Compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein: W is O, N—H, N-(C | 07-12-2012 |
20120184524 | PYRAZOLOPYRIDINE 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. | 07-19-2012 |
20120184525 | 1,2,3-TRIAZOLO [4,3-A] PYRIDINE DERIVATIVES AND THIER USE FOR THE TREATMENT OF PREVENTION OF NEUROLOGICAL AND PSYCHIATRIC DISORDERS - The present invention relates to novel triazolo[4,3- | 07-19-2012 |
20120184526 | COMPOUNDS AND COMPOSITIONS AS SYK KINASE INHIBITORS - Provided herein are a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated Syk kinase activity. | 07-19-2012 |
20120190666 | Heteroaryl Compounds as PIKK Inhibitors - The present invention provides compounds that are PIKK inhibitors, more specifically, mTOR and/or PI3Kα kinase inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of kinases, specifically PI3 kinases, more specifically, mTOR and/or PI3Kα, such as cancer. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds. | 07-26-2012 |
20120196846 | ANTI-RSV COMPOUNDS - The present invention relates to anti-RSV compounds of Formula (I) and methods for use of the compounds in the treatment and prevention of RSV infection. | 08-02-2012 |
20120196847 | 6,6-Bicyclic Ring Substituted Heterobicyclic Protein Kinase Inhibitors - Compounds of the formula | 08-02-2012 |
20120202788 | AZABENZOTHIAZOLE COMPOUNDS, COMPOSITIONS AND METHODS OF USE - Provided are compounds of Formula I, stereoisomers, tautomers, solvates, prodrugs and pharmaceutically acceptable salts thereof, wherein A, X, R | 08-09-2012 |
20120208792 | PROTEIN KINASE MODULATORS - The invention relates in part to molecules having certain biological activities that include, but are not limited to, inhibiting cell proliferation, modulating protein kinase activity and modulating polymerase activity. Molecules of the invention can modulate Pim kinase activity and/or FMS-like tyrosine kinase (Flt) activity. The invention also relates in part to methods for using such molecules. | 08-16-2012 |
20120208793 | THIENO- AND FURO-PYRIMIDINE MODULATORS OF THE HISTAMINE H4 RECEPTOR - Thieno- and furo-pyrimidine compounds are described, which are useful as H | 08-16-2012 |
20120214791 | Imidazo[5,1-f][1,2,4]Triazines for the Treatment of Neurological Disorders - The present invention relates to compounds of the Formula | 08-23-2012 |
20120214792 | THIENO- ADN FURO-PYRIMIDINE MODULATORS OF THE HISTAMINE H4 RECEPTOR - Thieno- and furo-pyrimidine compounds are described, which are useful as H | 08-23-2012 |
20120220565 | PYRIDYL-AMINE FUSED AZADECALIN MODULATORS - The present invention provides a novel class of pyridyl-amine fused azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators. | 08-30-2012 |
20120220566 | 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. | 08-30-2012 |
20120225856 | FUSED RING AZADECALIN GLUCOCORTICOID RECEPTOR MODULATORS - The present invention provides a novel class of fused ring azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators. | 09-06-2012 |
20120232054 | PYRROLOTRIAZINE COMPOUNDS - A compound of formula (I): | 09-13-2012 |
20120232055 | HYDROXYLATED AND METHOXYLATED PYRIMIDYL CYCLOPENTANES AS AKT PROTEIN KINASE INHIBITORS - The present invention provides compounds, including resolved enantiomers, resolved diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula I: | 09-13-2012 |
20120232056 | HETEROCYCLIC COMPOUNDS FOR THE INHIBITION OF PASK - Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus. | 09-13-2012 |
20120238542 | AMINOPYRAZOLOQUINAZOLINES - Compounds of general formula (I) | 09-20-2012 |
20120238543 | Antiviral Compounds - Novel compounds, methods, and compositions for treating various viral infections are described. In some embodiments the novel compounds of the invention are 3-oxo-phenothiazine derivatives; more specific embodiments include 3-oxo-phenothiazine derivatives having substituents at the 1-, 7-, and 9-positions of the phenothiazine parent ring. In other embodiments, the invention provides compositions and methods for treating viral infections, especially HIV. | 09-20-2012 |
20120238544 | THIENO- AND FURO-PYRIMIDINE MODULATORS OF THE HISTAMINE H4 RECEPTOR - Thieno- and furo-pyrimidine compounds are described, which are useful as H | 09-20-2012 |
20120238545 | TRICYCLIC PYRAZOL AMINE DERIVATIVES - This invention relates to compounds of Formula (I*) as Pi3k inhibitors for treating autoimmune diseases, inflammatory disorders, multiple sclerosis and other diseases like cancers. | 09-20-2012 |
20120245142 | 3-OXO-2,3-DIHYDRO-1H-ISOINDOLE-4-CARBOXAMIDES AS PARP INHIBITORS - There are provided substituted 3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide derivatives (I) which selectively inhibit the activity of poly (ADP-ribose) polymerase PARP-1 with respect to poly (ADP-ribose) polymerase PARP-2. The compounds of this invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating, diseases utilizing pharmaceutical compositions comprising these compounds. | 09-27-2012 |
20120245143 | 3-0X0-2,3-DIHYDRO-1H-ISOINDOLE-4-CARBOXAMIDES WITH SELECTIVE PARP-1 INHIBITION - There are provided substituted 3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide derivatives (I) which selectively inhibit the activity of poly (ADP-ribose) polymerase PARP-1 with respect to poly (ADP-ribose) polymerase PARP-2. The compounds of this invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds. | 09-27-2012 |
20120245144 | BENZOXAZEPIN COMPOUNDS SELECTIVE FOR PI3K P110 DELTA AND METHODS OF USE - Benzoxazepin 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. | 09-27-2012 |
20120252777 | THIAZOLOPYRIMIDINE COMPOUNDS - The present invention relates to the use of novel pyrrolopyrazine derivatives of formula I: | 10-04-2012 |
20120252778 | PYRAZOLO PYRIMIDINE DERIVATIVES - The present invention relates to pyrazolo pyrimidine derivatives, to methods of preparing these, to combinations and pharmaceutical composition comprising these, and to their use in the treatment of diseases and disorders which may for example involve autoimmune diseases, angiogenesis, pain, and/or inflammatory diseases. | 10-04-2012 |
20120252779 | HETEROCYCLYL PYRAZOLOPYRIMIDINE ANALOGUES AS JAK INHIBITORS - The invention relates to compounds of formula (I) | 10-04-2012 |
20120252780 | BICYCLIC PYRIDINES AND ANALOGS AS SIRTUIN MODULATORS - Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent. | 10-04-2012 |
20120252781 | Benzodiazepine Bromodomain Inhibitor - Benzodiazepine compounds of formula (I) | 10-04-2012 |
20120252782 | Xanthine Derivatives, the Preparation Thereof and Their Use as Pharmaceutical Compositions - The present invention relates to substituted xanthines of general formula | 10-04-2012 |
20120252783 | Xanthine derivatives, the preparation thereof and their use as pharmaceutical compositions - The present invention relates to substituted xanthines of general formula | 10-04-2012 |
20120258950 | PYRROLO[2,3-d]PYRIMIDINE TROPOMYSIN-RELATED KINASE INHIBITORS - The present invention relates to compounds of Formula (I) | 10-11-2012 |
20120258951 | NOVEL ANTIPLATELET AGENT - The present invention relates to a novel antiplatelet agent and a novel compound which is an active ingredient for the agent. The present invention provides the antiplatelet agent comprising a compound represented by the formula I: | 10-11-2012 |
20120258952 | Substituted N-(1H-Indazol-4-yl)Imidazo[1,2-a]Pyridine-3-Carboxamide Compounds as cFMS Inhibitors - Compounds of Formula (I): and pharmaceutically acceptable salts thereof in which R | 10-11-2012 |
20120264737 | Heterocyclic Modulators of Lipid Synthesis - Compounds that are fatty acid synthesis modulators are provided. The compounds may be used to treat disorders characterized by disregulation of the fatty acid synthase function by modulating the function and/or the fatty acid synthase pathway. Methods are provided for treating such disorders including viral infections, such as hepatitis C infection, cancer and metabolic disorders. | 10-18-2012 |
20120264738 | 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 | 10-18-2012 |
20120264739 | CERTAIN TRIAZOLOPYRIDINES AND TRIAZOLOPYRAZINES, COMPOSITIONS THEREOF AND METHODS OF USE THEREFOR - Provided are certain triazolopyridines and triazolopyrazines, compositions thereof and methods of use therefor. | 10-18-2012 |
20120270854 | Antiviral Compounds - Compounds and methods for preventing and treating viral infections are provided. In some embodiments, novel compounds broad-spectrum antiviral activity are provided. In more specific embodiments, the compounds and methods are effective against viruses such as Venezuelan Equine Encephalitis, West Nile Virus, and Hepatitis C. | 10-25-2012 |
20120270855 | THIENO- AND FURO-PYRIMIDINE MODULATORS OF THE HISTAMINE H4 RECEPTOR - Thieno- and furo-pyrimidine compounds are described, which are useful as H | 10-25-2012 |
20120270856 | HETEROARYLOXY QUINAZOLINE DERIVATIVES - Disclosed are compounds of the following formula and their pharmaceutically-acceptable salts, which have an effect of glucokinase activation and are useful in the field of medicines for treatment for diabetes, obesity, etc. | 10-25-2012 |
20120277210 | SOLID DISPERSIONS CONTAINING AN APOPTOSIS-INDUCING AGENT - A pro-apoptotic solid dispersion comprises, in essentially non-crystalline form, a Bcl-2 family protein inhibitory compound of Formula I as defined herein, dispersed in a solid matrix that comprises (a) a pharmaceutically acceptable water-soluble polymeric carrier and (b) a pharmaceutically acceptable surfactant. A process for preparing such a solid dispersion comprises dissolving the compound, the polymeric carrier and the surfactant in a suitable solvent, and removing the solvent to provide a solid matrix comprising the polymeric carrier and the surfactant and having the compound dispersed in essentially non-crystalline form therein. The solid dispersion is suitable for oral administration to a subject in need thereof for treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer. | 11-01-2012 |
20120283238 | IRAK INHIBITORS AND USES THEREOF - The present invention provides compounds, compositions thereof, and methods of using the same. | 11-08-2012 |
20120283239 | 1H-[1,2,3]TRIAZOLO[4,5-c]PYRIDINE-4-CARBONITRILE DERIVATIVES - The invention relates to 1H-[1,2,3]triazolo[4,5-c]pyridine-4-carbonitrile derived Cathepsin S inhibitors of Formula (I), wherein R | 11-08-2012 |
20120283240 | Analogs of Indole-3-Carbinol and Their Use as Agents Against Infection - Compounds useful as antibacterial agents are provided. The compounds are analogs of indole-3-carbinol and have a backbone selected from dihydroindolo[2,3-b]carbazole, 2,2′-diindolylmethane, 2′,3-diindolylmethane, and 3,3′-diindolylmethane. The compounds are useful therapeutic and prophylactic treatment of bacterial infections in mammals. Methods of synthesis of the compounds are provided, as are pharmaceutical compositions containing the compounds. | 11-08-2012 |
20120283241 | IMIDAZOPYRIDAZINECARBONITRILES USEFUL AS KINASE INHIBITORS - The invention provides compounds of Formula (I) | 11-08-2012 |
20120289496 | NOVEL COMPOUNDS AS MODULATORS OF PROTEIN KINASES - The present invention provides PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them. | 11-15-2012 |
20120289497 | FUSED PYRIDINE DERIVATIVES - Fused pyridine derivatives shown as the general formula (I), and their pharmaceutically acceptable salts, stereoisomers or solvates thereof are disclosed, which belong to the technical field of medicines. The R | 11-15-2012 |
20120295885 | INHIBITORS OF BRUTON'S TYROSINE KINASE - This application discloses compounds according to generic Formula I: | 11-22-2012 |
20120302547 | NOVEL MCH RECEPTOR ANTAGONISTS - The present invention relates to a melanin concentrating hormone antagonist compound of formula (I) wherein R | 11-29-2012 |
20120309739 | AKT / PKB INHIBITORS - The invention relates to a series of compounds with particular activity as inhibitors of the serine-threonine kinase AKT. Also provided are pharmaceutical compositions comprising same as well as methods for treating cancer. | 12-06-2012 |
20120309740 | Pharmaceutical Compositions Having Improved Dissolution Profiles For Poorly Soluble Drugs - Pharmaceutical compositions having improved dissolution profiles for drugs therein is disclosed. | 12-06-2012 |
20120309741 | QUINOXALINE CARBOXAMIDE DERIVATIVES AS PROTEIN TYROSINE KINASE INHIBITORS - The invention relates to compounds of formula (I) | 12-06-2012 |
20120316152 | SUBSTITUTED ISOQUINOLINEAND ISOQUINOLINONE DERIVATIVES - A method for the treatment or prevention in a mammal of a disease associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase comprising administering to the mammal in need thereof at least one compound of the formula (I) | 12-13-2012 |
20120322788 | Compouds - The present invention relates to spirocyclic amide derivatives of the formula I, | 12-20-2012 |
20120329776 | HETEROCYCLIC COMPOUNDS AND USES THEREOF - Heterocyclic entities that modulate PI3 kinase activity, pharmaceutical compositions containing the isoquinolone entities, and methods of using these chemical entities for treating diseases and conditions associated with PI3 kinase activity are described herein. | 12-27-2012 |
20120329777 | Amino-Heterocyclic Compounds - The invention provides PDE9-inhibiting compounds of Formula (I), | 12-27-2012 |
20120329778 | BICYCLIC HETEROCYCLES, PHARMACEUTICAL COMPOSITIONS CONTAINING THESE COMPOUNDS, THEIR USE AND PROCESSES FOR PREPARING THEM - The present invention relates to bicyclic heterocycles of general formula | 12-27-2012 |
20130005705 | NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A - The present invention relates to novel carboxamide compounds, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating or controlling 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. | 01-03-2013 |
20130005706 | 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: | 01-03-2013 |
20130005707 | AMINOTRIAZOLOPYRIDINES, COMPOSITIONS THEREOF, AND METHODS OF TREATMENT THEREWITH - Provided herein are Heteroaryl Compounds of formula (I): | 01-03-2013 |
20130012492 | 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: | 01-10-2013 |
20130012493 | NOVEL SPIRO IMIDAZOLONE DERIVATIVES AS GLUCAGON RECEPTOR ANTAGONISTS, COMPOSITIONS, AND METHODS FOR THEIR USE - The present invention relates to compounds of the general formula (I): wherein ring A, ring B, G, R | 01-10-2013 |
20130018033 | RAF INHIBITOR COMPOUNDS AND METHODS OF USE THEREOF - Compounds of Formula I are useful for inhibition of Raf kinases. Methods of using compounds of Formula I and stereoisomers, tautomers, prodrugs and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed. | 01-17-2013 |
20130018034 | AZETIDINYL PHENYL, PYRIDYL OR PYRAZINYL CARBOXAMIDE DERIVATIVES AS JAK INHIBITORS - The present invention provides azetidinyl phenyl, pyridyl, or pyrazinyl carboxamide derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase (JAKs) 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. | 01-17-2013 |
20130018035 | COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE - The present invention relates to pyrrolopyrazines 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. | 01-17-2013 |
20130018036 | SUBSTITUTED INDAZOLE DERIVATIVES ACTIVE AS KINASE INHIBITORS - Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer. | 01-17-2013 |
20130018037 | Compounds - 801 - Spirocyclic amide derivatives of formula I | 01-17-2013 |
20130018038 | CHEMICAL COMPOUNDS - The invention is directed to substituted indoline derivatives. Specifically, the invention is directed to compounds according to Formula I: | 01-17-2013 |
20130018039 | IMIDAZOLYL-IMIDAZOLES AS KINASE INHIBITORS - Disclosed are compounds having the formula: wherein R | 01-17-2013 |
20130029966 | SUBSTITUTED OXINDOLE DERIVATIVES, MEDICAMENTS CONTAINING SAID DERIVATIVES AND USE THEREOF - The invention relates to novel oxindole derivatives of general formula (I), wherein the substituents R | 01-31-2013 |
20130029967 | Fused Imidazo [3,2 - D] Pyrazines as P13 Kinase Inhibitors - There is provided compounds of formula (I), wherein A | 01-31-2013 |
20130029968 | INDAZOLES - The present invention relates to compounds of formula (I): | 01-31-2013 |
20130029969 | HETEROCYCLIC COMPOUND - Provided is a compound useful for the prophylaxis or treatment of cancer. | 01-31-2013 |
20130040934 | SPIROCYCLIC COMPOUNDS AND THEIR USE AS THERAPEUTIC AGENTS AND DIAGNOSTIC PROBES - The invention relates to new triazines (G=Q=U are N), pyrimidines (two out of G, Q and U are N), and pyridopyrimidines (one of G and U together with R2 forms an anullated pyridine ring) of formula (I) carrying a spirocyclic substituent, wherein E | 02-14-2013 |
20130045965 | INHIBITORS OF BRUTON'S TYROSINE KINASE - This application discloses compounds according to generic Formula I: | 02-21-2013 |
20130053365 | DIHYDROPYRIDOPHTHALAZINONE INHIBITORS OF POLY(ADP-RIBOSE)POLYMERASE (PARP) - Provided are inhibitors of poly(ADP-ribose)polymerase according to Formula (M): | 02-28-2013 |
20130059836 | PYRAZOLOPYRIMIDINE COMPOUNDS FOR THE TREATMENT OF CANCER - Compound of Formula (I): are described, along with pharmaceutically acceptable salts thereof, compositions containing the same, and methods of use thereof in the treatment of cancer. | 03-07-2013 |
20130065881 | Tricyclic Compounds for Use as Kinase Inhibitors - There is provided compounds of formula (I), wherein R | 03-14-2013 |
20130065882 | VLA-4 inhibitory drug - This invention relates to a VLA-4 inhibitory drug, having good oral absorbability and exhibiting sufficient anti-inflammatory effects when administered orally, wherein an active ingredient is represented by formula (I), or a salt thereof: | 03-14-2013 |
20130065883 | Triazolo [4, 5- B] Pyridin Derivatives - There is provided compounds of formula (I), wherein R | 03-14-2013 |
20130072470 | NOVEL TRICYCLIC COMPOUNDS - The invention provides compounds of Formula (I) | 03-21-2013 |
20130079329 | INDAZOLE-3-CARBOXAMIDES AND THEIR USE AS WNT/Beta-CATENIN SIGNALING PATHWAY INHIBITORS - Indazole-3-carboxamide compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole-3-carboxamide compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states. | 03-28-2013 |
20130079330 | 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. | 03-28-2013 |
20130096103 | IMIDAZOQUINOLINE COMPOUNDS - The invention provides novel compositions comprising imidazoquinoline compounds. Also provided are methods of administering the compositions in an effective amount to enhance the immune response of a subject. Further provided are novel compositions and methods of administering the compositions in combination with (an)other agent(s). | 04-18-2013 |
20130096104 | IMIDAZOPYRIDINE COMPOUNDS, COMPOSITIONS AND METHODS OF USE - The invention provides compounds of Formulas Ia-Ib, stereoisomers or pharmaceutically acceptable salts thereof, wherein A, X, R | 04-18-2013 |
20130102586 | SUBSTITUTED 5-(PYRAZIN-2-YL)-1H-PYRAZOLO [3, 4-B] PYRIDINE AND PYRAZOLO [3, 4-B] PYRIDINE DERIVATIVES AS PROTEIN KINASE INHIBITORS - Substituted 5-(pyrazin-2-yl)-1H-pyrazolo[3,4-b]pyridine, 5-(pyrazin-2-yl)-1H-pyrrolo[2,3-b]pyridine and pyrazolo[3,4-b]pyridine derivatives according to formula I, II and VII, and methods for making same, which are inhibitors of constitutively activated Tyrosine Kinase-Like (TKL), CMGC protein kinases family members and can be useful in the treatment of Parkinson's disease, Alzheimer's disease, Down's Syndrome, Huntington's disease, other neurodegenerative and central nervous system disorders, cancer, metabolic disorders and inflammatory diseases. Also disclosed are pharmaceutical compositions including the compounds and methods of inhibiting wild type and/or mutated protein kinase activities of these families and the treatment of disorders associated therewith using compounds and pharmaceutical compositions including the compounds. | 04-25-2013 |
20130116233 | NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A - The present invention relates to novel compounds of the formula I 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 |
20130116234 | ARYL-QUINOLINE DERIVATIVES - The invention provides novel compounds having the general formula (I) | 05-09-2013 |
20130116235 | HETEROARYL PYRIDONE AND AZA-PYRIDONE COMPOUNDS - Heteroaryl pyridone and aza-pyridone compounds of Formula I are provided, where one or two of X | 05-09-2013 |
20130116236 | NOVEL [1,2,3]TRIAZOLO[4,5-D]PYRIMIDINE DERIVATIVES - The invention relates to a compound of formula (I) | 05-09-2013 |
20130123236 | SUBSTITUTED BENZYLSPIROINDOLIN-2-ONE ANALOGS AS POSITIVE ALLOSTERIC MODULATORS OF THE MUSCARINIC ACETYLCHOLINE RECEPTOR M1 - In one aspect, the invention relates to substituted benzylspiroindolin-2-one analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M | 05-16-2013 |
20130123237 | NOVEL CYCLIC AZABENZIMIDAZOLE DERIVATIVES USEFUL AS ANTI-DIABETIC AGENTS - Novel compounds of structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension. | 05-16-2013 |
20130131043 | PYRAZOLE COMPOUNDS AS JAK INHIBITORS - The invention relates to compounds of formula (I) | 05-23-2013 |
20130131044 | SELECTIVE GLYCOSIDASE INHIBITORS AND USES THEREOF - The invention provides compounds of Formula (I) for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc. | 05-23-2013 |
20130137676 | NOVEL [1,2,3]TRIAZOLO[4,5-D]PYRIMIDINE DERIVATIVES - The invention relates to a compound of formula (I) | 05-30-2013 |
20130137677 | Bicyclic Azaheterocyclic Carboxamides - The invention provides novel bicyclic azaheterocyclic carboxamide compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer. | 05-30-2013 |
20130143864 | (6,7-DIHYDRO-2-NITRO-5H-IMIDAZOL[2,1-B][1,3]OXAZIN-6YL) AMIDE COMPOUNDS, PREPARATION METHODS AND USES THEREOF - (6,7-Dihydro-2-nitro-5H-imidazo[2,1-b][1,3]oxazin-6-yl)amide compounds of formula (I), and their pharmaceutically acceptable salts, preparation methods and pharmaceutical compositions thereof are disclosed, wherein m and R are defined as in the description. The uses of the compounds in preparing medicaments for treating infectious diseases caused by | 06-06-2013 |
20130143865 | PYRIMIDYL CYCLOPENTANES AS AKT PROTEIN KINASE INHIBITORS - The present invention provides compounds of Formula I, including tautomers, resolved enantiomers, diastereomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof. | 06-06-2013 |
20130150342 | PYRROLOPYRIMIDINE COMPOUNDS AS INHIBITORS OF CDK4/6 - The invention is directed to novel pyrrolopyrimidine compounds of formula (I) wherein R | 06-13-2013 |
20130158002 | POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 - The present invention is directed to 5-substituted 1,3-dihydro-2,1,3-benzothiadiazole 2,2-dioxide and 1,3-dihydro[1,2,5]thiadiazolo[3,4-b]pyridine 2,2,-dioxide 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. | 06-20-2013 |
20130158003 | HETEROARYL COMPOUNDS AND METHODS OF USE THEREOF - Provided herein are heteroaryl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and metabolic disorders, including, but not limited to, e.g., neurological disorders, psychosis, schizophrenia, obesity, and diabetes. | 06-20-2013 |
20130158004 | Azetidine Derivatives - Azetidine derivatives of which the following is exemplary | 06-20-2013 |
20130158005 | PYRIMIDINE DERIVATIVES AS FAK INHIBITORS - Compounds of the formula (I), in which R | 06-20-2013 |
20130165424 | 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 | 06-27-2013 |
20130172316 | New azetidine derivatives, pharmaceutical compositions and uses thereof - The invention relates to new azetidine derivatives of the formula I | 07-04-2013 |
20130172317 | TRIAZINE DERIVATIVE AND PHARMACEUTICAL COMPOSITION HAVING AN ANALGESIC ACTIVITY COMPRISING THE SAME - The present invention provides novel compounds having a P2X | 07-04-2013 |
20130178459 | TRICYCLIC COMPOUNDS AND PBK INHIBITORS CONTAINING THE SAME - Tricyclic compounds are provided. These compounds are PBK inhibitors, and are useful for the treatment of PBK related diseases, including cancer. | 07-11-2013 |
20130178460 | THIENOPYRIMIDINE COMPOUNDS - The present invention relates to the use of novel compounds of Formula I: | 07-11-2013 |
20130178461 | INHIBITORS OF BRUTON'S TYROSINE KINASE - This application discloses 6-(2-Hydroxymethyl-phenyl)-2-methyl-2H-pyridazin-3-one derivatives according to generic Formula I: | 07-11-2013 |
20130178462 | COMPOUNDS FOR THE REDUCTION OF BETA-AMYLOID PRODUCTION - The present disclosure provides a series of compounds of the formula (I) | 07-11-2013 |
20130184253 | TETRAHYDROPYRIDO-PYRIDINE AND TETRAHYDROPYRIDO-PYRIMIDINE COMPOUNDS AND USE THEREOF AS C5A RECEPTOR MODULATORS - The present invention provides a compound of formula I: | 07-18-2013 |
20130184254 | AZAINDAZOLE COMPOUNDS - Disclosed are azaindazole compounds of Formula (I), or pharmaceutically acceptable salts thereof, wherein W is CR | 07-18-2013 |
20130190290 | Substituted phenylimidazopyrazoles and their use - The present application relates to novel 1-phenyl-1H-imidazo[1,2-b]pyrazole derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular angiogenic disorders and hyperproliferative disorders, where neovascularization plays a role, such as, for example, neoplastic disorders and tumour disorders. Such treatments can be carried out as monotherapy or else in combination with other medicaments or further therapeutic measures. | 07-25-2013 |
20130190291 | HETEROCYCLIC COMPOUND AND USE THEREOF - Provided is a compound represented by the formula (I): | 07-25-2013 |
20130190292 | HETEROCYCLYL PYRAZOLOPYRIMIDINE ANALOGUES AS SELECTIVE JAK INHIBITORS - The present invention relates to compounds of formula (I) | 07-25-2013 |
20130196973 | BENZODIOXANE INHIBITORS OF LEUKOTRIENE PRODUCTION - The present invention relates to compounds of formula (I): | 08-01-2013 |
20130196974 | COMPOUNDS FOR THE TREATMENT AND PROPHYLAXIS OF RESPIRATORY SYNCYTIAL VIRUS DISEASE - A compound of formula (I) | 08-01-2013 |
20130203731 | APOPTOSIS SIGNAL-REGULATING KINASE 1 INHIBITORS - The present invention relates to apoptosis signal-regulating kinase 1 (“ASK1”) inhibiting compounds of the formula | 08-08-2013 |
20130210801 | 2-QUINOLINYL-ACETIC ACID DERIVATIVES AS HIV ANTIVIRAL COMPOUNDS - 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 the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds of formula (I). | 08-15-2013 |
20130210802 | IMIDAZOPYRIDINES SYK INHIBITORS - Certain imidazopyridines (I) 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. | 08-15-2013 |
20130217671 | QUINOLINE DERIVATIVES AND MELK INHIBITORS CONTAINING THE SAME - The present invention directs a compound represented by formula (I). | 08-22-2013 |
20130225554 | NEW BICYCLIC COMPOUNDS AND THEIR USE AS ANTIBACTERIAL AGENTS AND BETA-LACTAMASE INHIBITORS - A compound of formula (I): | 08-29-2013 |
20130225555 | Imidazoquinolines with Immuno-Modulating Properties - The present invention provides compounds of formula (I) | 08-29-2013 |
20130225556 | 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. | 08-29-2013 |
20130225557 | PYRIDO[3,2-d]PYRIMIDINE PI3K DELTA INHIBITOR 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. | 08-29-2013 |
20130231328 | IRAK INHIBITORS AND USES THEREOF - The present invention provides compounds, compositions thereof, and methods of using the same. | 09-05-2013 |
20130231329 | Benzazole Derivatives as Histamine H4 Receptor Ligands - The present patent application concerns new ligands of the H4-receptor of formula (I), their process of preparation and their therapeutic use. | 09-05-2013 |
20130231330 | IMIDAZOPYRIZINE 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. | 09-05-2013 |
20130237519 | BICYCLIC HETEROCYCLE DERIVATIVES FOR THE TREATMENT OF PULMONARY ARTERIAL HYPERTENSION - Bicyclic heterocyclic derivatives of formula I useful in inhibiting PDGF receptor mediated biological activity. | 09-12-2013 |
20130237520 | 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. | 09-12-2013 |
20130237521 | IMIDAZOPYRIZINE 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. | 09-12-2013 |
20130245001 | HETEROCYCLIC INHIBITORS OF HISTAMINE RECEPTORS FOR THE TREATMENT OF DISEASE - The present invention relates to salts, hydrates, and polymorphs of bicyclic heteroaryl compounds, and pharmaceutical compositions thereof, which may be useful as inhibitors of H | 09-19-2013 |
20130245002 | Triazolopyridine Compounds - The invention relates to compounds of formula (I) and salts thereof: | 09-19-2013 |
20130245003 | CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS - The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. | 09-19-2013 |
20130252938 | Antibacterial Compounds - The present invention provides a compound of the following formula, salts, racemates, diastereomers, enantiomers, esters, carbamates, phosphates, sulfates, deuterated forms and prodrugs thereof. | 09-26-2013 |
20130252939 | TRI-CYCLIC PYRAZOLOPYRIDINE 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. | 09-26-2013 |
20130252940 | 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. | 09-26-2013 |
20130252941 | PYRAZOLOPYRIDINE COMPOUNDS, COMPOSITIONS AND METHODS OF USE - The invention provides compounds of Formula I, stereoisomers or pharmaceutically acceptable salts thereof, wherein A, X, R | 09-26-2013 |
20130252942 | QUINAZOLINE CARBOXAMIDE AZETIDINES - The invention provides novel quinazoline carboxamide azetidine compounds according to Formula (I) and use for the treatment of hyperproliferative diseases, such as cancer. | 09-26-2013 |
20130261102 | 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. | 10-03-2013 |
20130261103 | PYRIDAZINONES, METHOD OF MAKING, AND METHOD OF USE THEREOF - Pyridazinone compounds of Formula I including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. | 10-03-2013 |
20130261104 | METHODS OF USE OF DIAZACARBAZOLES FOR TREATING CANCER - Methods of use of compounds of formula (I) for treating cancer: | 10-03-2013 |
20130267495 | INDAZOLE INHIBITORS OF THE WNT SIGNAL PATHWAY AND THERAPEUTIC USES THEREOF - Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states. | 10-10-2013 |
20130267496 | 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. | 10-10-2013 |
20130267497 | KINASE INHIBITORS - The present invention relates to drug delivery systems comprising ocular implant, which include organic molecules, capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation, in combination with a polymer, which polymer serves to control, modify, modulate and/or slow the release of the therapeutic component into the environment of the eye in which said composite is placed. | 10-10-2013 |
20130274242 | SUBSTITUTED PYRIMIDINE COMPOUNDS AND THEIR USE AS SYK INHIBITORS - Compounds of Formula (I) and methods for inhibiting kinases, including spleen tyrosine kinases, are disclosed. Also disclosed are methods for treating a kinase-mediated disease or condition by administering to a subject a therapeutically effective amount of the compound of Formula (I). | 10-17-2013 |
20130274243 | Chemical Compounds - The invention relates to benzimidazole and imidazopyridine derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to new Na | 10-17-2013 |
20130274244 | SUBSTITUTED N-(1H-INDAZOL-4-YL)IMIDAZO[1,2-]PYRIDINE-3-CARBOXAMIDE COMPOUNDS AS TYPE III RECEPTOR TYROSINE KINASE INHIBITORS - Compounds of Formula I: and pharmaceutically acceptable salts thereof in which R | 10-17-2013 |
20130281432 | PYRIDINONES/PYRAZINONES, METHOD OF MAKING, AND METHOD OF USE THEREOF - Pyridone and pyrazinone compounds of Formula I including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. | 10-24-2013 |
20130281433 | THERAPEUTIC COMPOUNDS - Compounds disclosed herein including compounds of formula I′: | 10-24-2013 |
20130281434 | THERAPEUTIC COMPOUNDS - Compounds of formula I′: | 10-24-2013 |
20130289016 | PYRIMIDINYL AND 1,3,5-TRIAZINYL BENZIMIDAZOLE SULFONAMIDES AND THEIR USE IN CANCER THERAPY - Provided herein are pyrimidinyl and 1,3,5-triazinyl benzimidazole sulfonamides, e.g., compounds of Formulae IA, IB, and IC, and their pharmaceutical compositions, preparation, and use as agents or drugs for cancer therapy, either alone or in combination with radiation and/or other anticancer drugs. | 10-31-2013 |
20130289017 | 5 (1,2,3-TRIAZOL-4-YL)-7H-PYRROLO[2,3-D]PYRIMIDINE DERIVATIVES - Compounds of the formula (I), in which R | 10-31-2013 |
20130296301 | SELECTIVE GLYCOSIDASE INHIBITORS AND USES THEREOF - The invention is directed to compounds for selectively inhibiting glycosidases, uses of the compounds and pharmaceutical compositions including the compounds, and methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, and/or accumulation or deficiency of O-GlcNAc. | 11-07-2013 |
20130296302 | 1H-PYRAZOLO[3,4-B]PYRIDINES AND THERAPEUTIC USES THEREOF - Provided herein are compounds according to Formulas (I) or (II) and pharmaceutically acceptable salts thereof, and compositions comprising the same, for use in various methods, including treating cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease, osteoarthritis, idiopathic pulmonary fibrosis and neurological conditions/disorders/diseases. | 11-07-2013 |
20130296303 | 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. | 11-07-2013 |
20130310362 | FUSED PYRIMIDINES - The present invention relates to compounds of formula (I), | 11-21-2013 |
20130310363 | IMIDAZOPYRIZINE SYK INHIBITORS - Certain imidazopyrazines of Formula (I): | 11-21-2013 |
20130310364 | COMPOSITIONS AND METHODS FOR INHIBITION OF THE JAK PATHWAY - Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful. | 11-21-2013 |
20130310365 | CYCLOHEXYL-AZETIDINYL ANTAGONISTS OF CCR2 - The present invention comprises compounds of Formula I. | 11-21-2013 |
20130317002 | FUSED PYRIMIDINES - Compounds of formula (I) | 11-28-2013 |
20130317003 | Histone Deacetylase Inhibitors - This invention relates to generally inhibiting histone deacetylase (“HDAC”) enzymes (e.g., HDAC1, HDAC2, and HDAC3). | 11-28-2013 |
20130317004 | AMINOALCOHOL SUBSTITUTED 2,3-DIHYDROIMIDAZO[1,2-C]QUINAZOLINE DERIVATIVES USEFUL FOR TREATING HYPER-PROLIFERATIVE DISORDERS AND DISEASES ASSOCIATED WITH ANGIOGENESIS - This invention relates to novel 2,3-dihydroimidazo[1,2-c]quinazoline compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for phosphotidylinositol-3-kinase (PI3K) inhibition and treating diseases associated with phosphotidylinositol-3-kinase (PI3K) activity, in particular treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients. | 11-28-2013 |
20130324518 | ARYLMETHOXY ISOINDOLINE DERIVATIVES AND COMPOSITIONS COMPRISING AND METHODS OF USING THE SAME - Provided are 4′-arylmethoxy isoindoline compounds, and pharmaceutically acceptable salts, solvates, clathrates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed. | 12-05-2013 |
20130324519 | QUINOXALINE CARBOXAMIDE DERIVATIVES AS PROTEIN TYROSINE KINASE INHIBITORS - The invention relates to compounds of formula (I) | 12-05-2013 |
20130331374 | Protein Kinase C Inhibitors and Uses Thereof - This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes. | 12-12-2013 |
20130331375 | PYRROLOPYRIMIDONE AND PYRROLOPYRIDONE INHIBITORS OF TANKYRASE - There are provided compounds of the formula (I) | 12-12-2013 |
20130338137 | Substituted annellated pyrimidines and use thereof - The present application relates to novel substituted annellated pyrimidines, methods for production thereof, use thereof alone or in combinations for treating and/or preventing diseases and use thereof for the production of medicinal products for treating and/or preventing diseases, in particular for treating and/or preventing cardiovascular diseases. | 12-19-2013 |
20130338138 | AZETIDINE AND PIPERIDINE COMPOUNDS USEFUL AS PDE10 INHIBITORS - Azetidine and piperidine compounds of formula (I): | 12-19-2013 |
20130338139 | THERAPEUTIC THIOPHENE-, FURAN-, AND PYRIDINE-FUSED AZOLOPYRIMIDIN-5-(6H)-ONES - Described herein are compounds of Formula I and Formula II, methods of their synthesis, compositions comprising the compounds, and use of the compounds and compositions in treating numerous diseases and disorders, including cognitive deficits associated with CNS diseases and disorders. | 12-19-2013 |
20130338140 | SERINE/THREONINE KINASE INHIBITORS - Compounds having the formula I wherein Z, Z | 12-19-2013 |
20140005166 | PIPERIDINYLCYCLOBUTYL SUBSTITUTED PYRROLOPYRIDINE AND PYRROLOPYRIMIDINE DERIVATIVES AS JAK INHIBITORS | 01-02-2014 |
20140005167 | KINASE INHIBITORS AND METHOD OF TREATING CANCER WITH SAME | 01-02-2014 |
20140005168 | 5-AZAINDAZOLE COMPOUNDS AND METHODS OF USE | 01-02-2014 |
20140005169 | BROMODOMAIN INHIBITORS AND USES THEREOF | 01-02-2014 |
20140005170 | INDAZOLE INHIBITORS OF THE WNT SIGNAL PATHWAY AND THERAPEUTIC USES THEREOF | 01-02-2014 |
20140011801 | HETEROARYL QUINAZOLINE DERIVATIVES - Disclosed are compounds of the following formula and their pharmaceutically-acceptable salts, which have an effect of glucokinase activation and are useful in the field of medicines for treatment for diabetes, obesity, etc. | 01-09-2014 |
20140018344 | AZAINDOLE DERIVATIVES - Disclosed are compounds of Formula 1, | 01-16-2014 |
20140018345 | INHIBITION OF ENZYMES - Compounds of formula (I): | 01-16-2014 |
20140024634 | INDAZOLES - A method of treating a disease or condition for which a JAK inhibitor is indicated in a subject in need of such treatment, comprising administering to the subject a therapeutically effective amount of a compound of formula (I) | 01-23-2014 |
20140031337 | AZOLOTRIAZINONE MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS - The present application provides compounds that are useful as MCHR1 antagonists, especially for the treatment of obesity, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I | 01-30-2014 |
20140038940 | NOVEL EGFR MODULATORS AND USES THEREOF - The present invention relates to certain pyrrolopyrimidine derivatives, pharmaceutical compositions containing them, and methods of using them, including methods for the treatment of tumors and related diseases related to the dysregulation of kinase (such as EGFR (including HER), Alk, PDGFR, but not limited to) pathways. | 02-06-2014 |
20140038941 | RING-FUSED HETEROCYCLIC DERIVATIVE - A ring-fused heterocyclic derivative represented by the following general formula (I) or a pharmaceutically acceptable salt thereof having a T-type calcium channel regulatory effect and useful as a pruritus therapeutic and/or preventive agent, and the like are provided. In the general formula (I), R | 02-06-2014 |
20140038942 | RORgammaT INHIBITORS - The present invention relates to compounds according to Formula (I) or a pharmaceutically acceptable salt or solvate thereof. Such compounds can be used in the treatment of RORgammaT-mediated diseases or condition. | 02-06-2014 |
20140038943 | SEROTONIN RECEPTOR MODULATOR - Certain biphenyic compounds are serotonin modulators useful in the treatment of serotonin-mediated diseases. | 02-06-2014 |
20140045815 | INDAZOLE-3-CARBOXAMIDES AND THEIR USE AS WNT/BETA-CATENIN SIGNALING PATHWAY INHIBITORS - Indazole-3-carboxamide compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole-3-carboxamide compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states. | 02-13-2014 |
20140045816 | Cyclopropyl Fused Indolobenzazepine HCV NS5B Inhibitors - The invention encompasses compounds of formula I as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV. | 02-13-2014 |
20140045817 | TRIAZOLOPYRIDINE COMPOUNDS AS PIM KINASE INHIBITORS - Provided herein is a method of treating a PIM-1 and/or PIM-2 and/or PIM-3 kinase-mediated condition in a mammal, which comprises administering to said mammal a therapeutically effective amount of a compound of Formula I: | 02-13-2014 |
20140045818 | BENZOTHIAZOLE COMPOUNDS AND THEIR PHARMACEUTICAL USE - 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 the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds of formula I. | 02-13-2014 |
20140045819 | ALDOSTERONE SYNTHASE INHIBITORS - This invention relates to tricyclic triazole analogues of the formula I or their pharmaceutically acceptable salts, wherein the variable are defined herein. The inventive compounds selectively inhibit aldosterone synthetase. This invention also provides for pharmaceutical compositions comprising the compounds of Formula I or their salts as well as to methods for the treatment, amelioration or prevention of conditions that could be treated by inhibiting aldosterone synthetase. | 02-13-2014 |
20140051679 | KINASE INHIBITORS AND METHOD OF TREATING CANCER WITH SAME - The present teachings provide a compound represented by Structural Formula (I): | 02-20-2014 |
20140051680 | Histone Deacetylase Inhibitors - This invention relates to generally inhibiting histone deacetylase (HDAC) enzymes (e.g., HDAC1, HDAC2, and HDAC3). | 02-20-2014 |
20140057894 | PYRAZOLOPYRIDINE AND PYRAZOLOPYRIMIDINE DERIVATIVES AS MELANOCORTIN-4 RECEPTOR MODULATORS - Disclosed herein is a compound of Formula I: wherein X, R | 02-27-2014 |
20140057895 | INDAZOLE- AND PYRROLOPYRIDINE-DERIVATIVE AND PHARMACEUTICAL USE THEREOF - The present invention relates to a novel indazole- or pyrrolopyridine-derivative comprising a 5 membered heterocyclic substituent at 1 position thereof which has an agonistic action or a partial agonistic action against serotonin-4 receptor, and a pharmaceutical composition comprising the same. | 02-27-2014 |
20140057896 | PYRIDONE AND AZA-PYRIDONE COMPOUNDS AND METHODS OF USE - Pyridone and aza-pyridone compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. | 02-27-2014 |
20140066429 | DIHYDROPYRIDOPHTHALAZINONE INHIBITORS OF POLY(ADP-RIBOSE)POLYMERASE (PARP) FOR USE IN TREATMENT OF DISEASES ASSOCIATED WITH A PTEN DEFICIENCY - A compound having the structure set forth in Formula (I) and Formula (II): | 03-06-2014 |
20140066430 | AURORA KINASE MODULATORS AND METHOD OF USE - The present invention relates to chemical compounds having a general formula I | 03-06-2014 |
20140073628 | BENZOXAZEPINES ASN INHIBITORS OF P13K/M TOR AND METHODS OF THEIR USE AND MANUFACTURE - The invention is directed to inhibitors of mTOR and pharmaceutically acceptable salts or solvates thereof, as well as methods of using them. The inhibitors are generally of structural formula I and pharmaceutically acceptable salts thereof, wherein the variables are as defined herein. | 03-13-2014 |
20140080806 | PYRAZOLO[3,4-D]PYRIMIDINE COMPOUNDS AND THEIR USE AS PDE2 INHIBITORS AND/OR CYP3A4 INHIBITORS - The present invention provides, inter alia, compounds of Formula (I) and pharmaceutically acceptable salts thereof, to processes for the preparation of, intermediates used in the preparation of and compositions containing such compounds and the uses of such compounds as a method for the treatment of a disease or condition selected from the group consisting of central nervous system disorders, cognitive disorders, schizophrenia, dementia and other disorders in a mammal. The present invention further provides compounds of Formula (Id) and pharmaceutically acceptable salts thereof as CYP3A4 selective inhibitors. | 03-20-2014 |
20140080807 | SUBSTITUTED INDAZOLE DERIVATIVES ACTIVE AS KINASE INHIBITORS - The present invention relates to substituted indazole compounds which modulate the activity of protein kinases and are therefore useful in treating diseases caused by degulated protein kinase activity, like cancer. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such these compounds or the pharmaceutical compositions containing them. | 03-20-2014 |
20140088080 | IMIDAZOPYRIDINE COMPOUNDS | 03-27-2014 |
20140088081 | Amino-Heterocyclic Compounds - The invention provides PDE9-inhibiting compounds of Formula (I), | 03-27-2014 |
20140107096 | HETEROARYL LINKED QUINOLINYL MODULATORS OF RORyt - The present invention comprises compounds of Formula I. | 04-17-2014 |
20140107097 | HETEROARYL LINKED QUINOLINYL MODULATORS OF RORyt - The present invention comprises compounds of Formula I. | 04-17-2014 |
20140107098 | IMIDAZOLO-, OXAZOLO-, AND THIAZOLOPYRIMIDINE MODULATORS OF TRPV1 - Certain TRPV1-modulating imidazolo-, oxazolo-, and thiazolopyrimdine compounds are described. The compounds may be used in pharmaceutical compositions and methods for treating disease states, disorders, and conditions mediated by TRPV1 activity, such as pain, arthritis, itch, cough, asthma, or inflammatory bowel disease. | 04-17-2014 |
20140107099 | PYRAZOLOPYRIMIDINE JAK INHIBITOR COMPOUNDS AND METHODS - The invention provides JAK kinase inhibitors of Formula Ia, enantiomers, diasteriomers or pharmaceutically acceptable salts thereof, wherein R | 04-17-2014 |
20140121197 | 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. | 05-01-2014 |
20140121198 | TRICYCLIC FUSED THIOPHENE DERIVATIVES AS JAK INHIBITORS - The present invention provides tricyclic fused thiophene 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. | 05-01-2014 |
20140128372 | Amino-substituted imidazo[1,2-a]pyridinecarboxamides and their use - The present application relates to novel substituted imidazo[1,2-a]pyridine-3-carboxamides, to processes for their preparation, to their use alone or in combinations 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 for the treatment and/or prophylaxis of cardiovascular disorders. | 05-08-2014 |
20140128373 | COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR - Compounds active on protein kinases are described, as well as methods of making and using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases. | 05-08-2014 |
20140128374 | HETEROAROMATIC COMPOUNDS AND THEIR USE AS DOPAMINE D1 LIGANDS - The present invention provides, in part, compounds of Formula I: | 05-08-2014 |
20140135309 | SULFOXIMINE SUBSTITUTED QUINAZOLINES FOR PHARMACEUTICAL COMPOSITIONS - This invention relates to novel sulfoximine substituted quinazoline derivatives of formula I | 05-15-2014 |
20140135310 | SULPHONAMIDE DERIVATIVES OF ALICYCLIC AMINES FOR THE TREATMENT OF CENTRAL NERVOUS SYSTEM DISEASES - Sulphonamide derivatives of alicyclic amines of formula (I), wherein A represents naphthyl or 9- or 10-membered bicyclic group, consisting of benzene ring fused with 5- or 6-membered heterocyclic ring; D represents phenyl, naphthyl, 5-membered aromatic heterocyclic group, bicyclic group consisting of a ring selected from benzene and pyridine, fused with aromatic or non-aromatic 5-membered heterocyclic ring; p, r independently represent 0 or 1; x, z independently represent 1 or 2; n is 2 or 3; | 05-15-2014 |
20140135311 | TETRAHYDRO-PYRIMIDOAZEPINES AS MODULATORS OF TRPV1 - Certain tetrahydro-pyrimidoazepine compounds are described, which are useful as TRPV1 modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by TRPV1. Thus, the compounds may be administered to treat, e.g., pain, itch, cough, asthma, or inflammatory bowel disease. | 05-15-2014 |
20140135312 | PYRROLOPYRIMIDINE COMPOUNDS AND THEIR USES - The disclosed compounds relate to treatments and therapies for protein kinase-associated disorders. There is also a need for compounds useful in the treatment or prevention or amelioration of one or more symptoms of cancer, transplant rejections, and autoimmune diseases. Furthermore, there is a need for methods for modulating the activity of protein kinases, such as CDK1, CDK2, CDK4, CDK5, CDK6, CDK7, CDK8 and CDK9, using the compounds provided herein. | 05-15-2014 |
20140148433 | BICYCLIC AZA HETEROCYCLES, AND USE THEREOF - The present application relates to novel bicyclic azaheterocycles, to processes for preparation thereof, to the use thereof, alone or in combinations, for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially for treatment and/or prophylaxis of cardiovascular disorders. | 05-29-2014 |
20140148434 | PYRAZOLOPYRIDINE 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. | 05-29-2014 |
20140148435 | AZETIDINE AND PIPERIDINE COMPOUNDS USEFUL AS PDE10 INHIBITORS - Azetidine and piperidine compounds of formula (I): | 05-29-2014 |
20140148436 | AKT PROTEIN KINASE INHIBITORS - The present invention provides compounds, including resolved enantiomers, diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula: | 05-29-2014 |
20140155378 | 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. | 06-05-2014 |
20140155379 | HETEROCYCLE AMINES AND USES THEREOF - Compounds and methods in the fields of chemistry and medicine are disclosed. Some of the disclosed embodiments include compounds, compositions and methods of using heterocycle amines. Some of the disclosed embodiments include heterocycle amines useful to treat inflammatory disorders. | 06-05-2014 |
20140155380 | Salt and Crystalline Forms Thereof of a Drug - A crystalline form of a drug, ways to make it, compositions containing it and methods of treatment of diseases and inhibition of adverse physiological events using it are disclosed. | 06-05-2014 |
20140163003 | Pyrido-[2,3-D] Pyrimidines and Their Use as Kinase Inhibitors - The present invention provides derivatives of pyrido[2,3-d]pyrimidin-7-one. These compounds are kinase inhibitors, including compounds that show anti-proliferative activity, including against tumor cells, and are useful in the treatment of diseases including cancer. | 06-12-2014 |
20140163004 | Pyrido-[2,3-D] Pyrimidines and Their Use as Kinase Inhibitors - The present invention provides derivatives of pyrido[2,3-d]pyrimidin-7-one. These compounds are kinase inhibitors, including compounds that show anti-proliferative activity, including against tumor cells, and are useful in the treatment of diseases including cancer. | 06-12-2014 |
20140163005 | Pyrido-[2,3-D] Pyrimidines and Their Use as Kinase Inhibitors - The present invention provides derivatives of pyrido[2,3-d]pyrimidin-7-one. These compounds are kinase inhibitors, including compounds that show anti-proliferative activity, including against tumor cells, and are useful in the treatment of diseases including cancer. | 06-12-2014 |
20140163006 | Pyrido-[2,3-D] Pyrimidines and Their Use as Kinase Inhibitors - The present invention provides derivatives of pyrido[2,3-d]pyrimidin-7-one. These compounds are kinase inhibitors, including compounds that show anti-proliferative activity, including against tumor cells, and are useful in the treatment of diseases including cancer. | 06-12-2014 |
20140163007 | Pyrido-[2,3-D] Pyrimidines and Their Use as Kinase Inhibitors - The present invention provides derivatives of pyrido[2,3-d]pyrimidin-7-one. These compounds are kinase inhibitors, including compounds that show anti-proliferative activity, including against tumor cells, and are useful in the treatment of diseases including cancer. | 06-12-2014 |
20140163008 | DIBENZOOXEPIN DERIVATIVE - A dibenzoxepin derivative represented by the following general formula (I) wherein Y is a hydrogen atom and the like, R | 06-12-2014 |
20140171407 | 1,7-DIAZACARBAZOLES AND METHODS OF USE - The invention relates to 1,7-diazacarbazole compounds of Formula (I), (I-a) and (I-b) which are useful as kinase inhibitors, more specifically useful as checkpoint kinase 1 (chk1) inhibitors, thus useful as cancer therapeutics. The invention also relates to compositions, more specifically pharmaceutical compositions comprising these compounds and methods of using the same to treat various forms of cancer and hyperproliferative disorders, as well as methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions. | 06-19-2014 |
20140171408 | AZABENZOTHIAZOLE COMPOUNDS, COMPOSITIONS AND METHODS OF USE - Provided are compounds of Formula I, stereoisomers, tautomers, solvates, prodrugs and pharmaceutically acceptable salts thereof, wherein A, X, R | 06-19-2014 |
20140171409 | AZETIDINYL PHENYL, PYRIDYL OR PYRAZINYL CARBOXAMIDE DERIVATIVES AS JAK INHIBITORS - The present invention provides azetidinyl phenyl, pyridyl, or pyrazinyl carboxamide derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase (JAKs) 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. | 06-19-2014 |
20140179671 | FUSED RING AZADECALIN GLUCOCORTICOID RECEPTOR MODULATORS - The present invention provides a novel class of fused ring azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators. | 06-26-2014 |
20140179672 | Amino-substituted imidazo[1,2-a]pyridinecarboxamides and their use - The present application relates to novel substituted imidazo[1,2-a]pyridine-3-carboxamides, to processes for their preparation, to their use alone or in combinations 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 for the treatment and/or prophylaxis of cardiovascular disorders. | 06-26-2014 |
20140179673 | PHOSPHATIDYLINOSITOL 3-KINASE INHIBITORS - The present disclosure provides phosphatidylinositol 3-kinase (PI3K) inhibitors of formula (I), | 06-26-2014 |
20140179674 | IMIDAZOPYRIDAZINECARBONITRILES USEFUL AS KINASE INHIBITORS - The invention provides compounds of Formula (I) | 06-26-2014 |
20140179675 | QUINOLONE COMPOUND - The present invention provides a compound represented by the formula (I) | 06-26-2014 |
20140187535 | SUBSTITUTED BENZIMIDAZOLE-TYPE PIPERIDINE COMPOUNDS AND USES THEREOF - The disclosure relates to Substituted Benzimidazole-Type Piperidine Compounds of Formula (I): | 07-03-2014 |
20140194407 | NOVEL ANTIPLATELET AGENT - The present invention relates to a novel antiplatelet agent and a novel compound which is an active ingredient for the agent. The present invention provides the antiplatelet agent comprising a compound represented by the formula I: | 07-10-2014 |
20140194408 | HETEROARYL PYRIDONE AND AZA-PYRIDONE COMPOUNDS - Heteroaryl pyridone and aza-pyridone compounds of Formula I are provided, where one or two of X | 07-10-2014 |
20140206664 | Heterocycle Amido Alkyloxy Substituted Quinazoline Derivative and Use Thereof - Heterocycle amino alkyloxy substituted quinazoline derivatives as represented by the structural Formula (I) and pharmaceutically acceptable salts thereof, capable of inhibiting the activity of receptor tyrosine kinase EGFR, and being used to treat cancers related to the expression of the receptor tyrosine kinase of the ErbB family are provided. | 07-24-2014 |
20140206665 | SELECTIVE GLYCOSIDASE INHIBITORS AND USES THEREOF - The invention is directed to compounds for selectively inhibiting glycosidases, uses of the compounds and pharmaceutical compositions including the compounds, and methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, and/or accumulation or deficiency of O-GlcNAc. | 07-24-2014 |
20140213576 | NOVEL COMPOUND USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES - A novel compound according to Formula I, able to inhibit JAK as disclosed, this compound 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. | 07-31-2014 |
20140221343 | FUSED AMINO PYRIDINE AS HSP90 INHIBITORS - The present invention relates to HSP90 inhibitors containing fused amino pyridine core that are useful as inhibitors of HSP90 and their use in the treatment of HSP90 related diseases and disorders such as cancer, an autoimmune disease, or a neurodegenerative disease. | 08-07-2014 |
20140221344 | Bicyclic Pyridazine Compounds as PIM Inhibitors - The invention relates to bicyclic compounds of formulas I and 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. | 08-07-2014 |
20140221345 | 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. | 08-07-2014 |
20140221346 | THERAPEUTIC COMPOUNDS - Compounds of formula I: | 08-07-2014 |
20140221347 | THERAPEUTIC COMPOUNDS - Compounds of formula I: | 08-07-2014 |
20140221348 | NOVEL BICYCLIC ANTIBIOTICS - The antibacterial compound of formula I | 08-07-2014 |
20140235614 | MONOCYCLIC PYRIDINE DERIVATIVE - The present invention provides a novel compound having FGFR inhibitory activity or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the same. Specifically, the present invention provides a compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof: | 08-21-2014 |
20140235615 | HETEROCYCLIC COMPOUND - Provided is a compound useful for the prophylaxis or treatment of cancer. | 08-21-2014 |
20140235616 | PYRAZOLOQUINOLINONE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF - The invention relates to compounds corresponding to formula (I), in which R1, R2 and R3 are as defined in Claim | 08-21-2014 |
20140243311 | NOVEL OCTAHYDROTHIENOQUINOLINE DERIVATIVE, PHARMACEUTICAL COMPOSITION COMPRISING DERIVATIVE, AND USE OF THESE - The present invention provides compounds represented by the general formula (I): or pharmaceutical acceptable salts thereof, wherein R | 08-28-2014 |
20140243312 | PYRROLO[2,3-D]PYRIMIDINE DERIVATIVES - Described herein are pyrrolo{2,3-d}pyrimidine derivatives, their use as Janus Kinase (JAK) inhibitors, and pharmaceutical compositions containing them. | 08-28-2014 |
20140243313 | TRICYCLIC COMPOUNDS USEFUL AS NEUROGENIC AND NEUROPROTECTIVE AGENTS - The invention disclosed herein is direct to compounds of Formula I and pharmaceutically acceptable salts thereof, which are useful in treating neurodegenerative diseases and promoting the generation or survival of neurons in the mammalian brain. The invention also comprises pharmaceutical compositions comprising a therapeutically effective amount of compound of Formula I or a pharmaceutically acceptable salt thereof. The invention disclosed herein is also directed to a method of promoting the generation or survival of neurons in a patient in need thereof in neurodegenerative and related diseases. | 08-28-2014 |
20140243314 | QUINOLINONE CARBOXAMIDE INHIBITORS OF ENDOTHELIAL LIPASE - The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments. | 08-28-2014 |
20140243315 | PYRROLOPYRIMIDINE COMPOUNDS FOR THE TREATMENT OF CANCER - The ectopic expression of Mer receptor tyrosine kinase (Mer) has been identified as a tumor cell survival gene product in Acute Lymphoblastic Leukemia (ALL) cells and a potential cause of ALL chemoresistance. Hence, we investigated whether the development of small molecule Mer inhibitors was possible. A first aspect of the present invention is a compound (sometimes referred to as an “active compound” herein) of Formula I, IA, or IB. | 08-28-2014 |
20140249134 | TRIAZOLYL PDE10 INHIBITORS - The present invention is directed to substituted triazolyl compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction. | 09-04-2014 |
20140256703 | AMINOPYRIMIDINES 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. | 09-11-2014 |
20140256704 | Substituted 1H-Pyrrolo [2, 3-b] pyridine and 1H-Pyrazolo [3, 4-b] pyridine Derivatives as Salt Inducible Kinase 2 (SIK2) Inhibitors - The present invention relates to compounds according to Formulas I, IA or IB: | 09-11-2014 |
20140256705 | BROMODOMAIN INHIBITORS - The present invention provides for compounds of formula (I) | 09-11-2014 |
20140256706 | BET BROMODOMAIN INHIBITORS AND THERAPEUTIC METHODS USING THE SAME - Inhibitors of BET bromodomains and compositions containing the same are disclosed. Methods of using the BET bromodomain inhibitors in the treatment of diseases and conditions wherein inhibition of BET bromodomain provides a benefit, like cancers, also are disclosed. | 09-11-2014 |
20140256707 | Heteroaryl Sodium Channel Inhibitors - The present invention provides compounds of Formula I or II, or pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav 1.7. The compounds are useful for the treatment of diseases treatable by inhibition of channels such as pain disorders. Also provided are pharmaceutical compositions containing compounds of the present invention. | 09-11-2014 |
20140256708 | 1,3 SUBSTITUTED AZETIDINE PDE10 INHIBITORS - The present invention is directed to substituted azetidinecompounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction. | 09-11-2014 |
20140275021 | 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 |
20140275022 | SELECTIVE GLYCOSIDASE INHIBITORS AND USES THEREOF - The invention provides compounds for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc. | 09-18-2014 |
20140275023 | Substituted Tricyclic Pyrazolo-Pyrimidine Compounds - The present invention relates to substituted tricyclic pyrazolo-pyrimidine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted tricyclic pyrazolo-pyrimidine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof. | 09-18-2014 |
20140275024 | 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. | 09-18-2014 |
20140275025 | SUBSTITUTED 2-AZA-BICYCLO[2.2.1]HEPTANE-3-CARBOXYLIC ACID (BENZYL-CYANO-METHYL)-AMIDES INHIBITORS OF CATHEPSIN C - This invention relates to 2-Aza-bicyclo[2.2.1]heptane-3-carboxylic acid(benzyl-cyano-methyl)-amides of formula 1 | 09-18-2014 |
20140275026 | DIHYDRO-PYRROLOPYRIDINONE INHIBITORS - The present invention provides for compounds of formula (I) | 09-18-2014 |
20140275027 | PYRROLO[2,3-B]PYRIDINE CDK9 KINASE INHIBITORS - Disclosed are compounds of Formula (IIIa), | 09-18-2014 |
20140275028 | 1,2,5-SUBSTITUTED BENZIMIDAZOLES AS FLAP MODULATORS - The present invention relates to compounds of Formula (I), | 09-18-2014 |
20140275029 | 1,2,6-SUBSTITUTED BENZIMIDAZOLES AS FLAP MODULATORS - The present invention relates to compounds of Formula (I), | 09-18-2014 |
20140275030 | TRICYCLIC HETEROCYCLES AS BET PROTEIN INHIBITORS - The present invention relates to tricyclic heterocycles which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer. | 09-18-2014 |
20140275031 | PIPERIDIN-4-YL AZETIDINE DERIVATIVES AS JAK1 INHIBITORS - The present invention provides piperidin-4-yl azetidine derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase 1 (JAK1) and are useful in the treatment of diseases related to the activity of JAK1 including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases. | 09-18-2014 |
20140288051 | BICYCLIC COMPOUNDS AND THEIR USE AS ANTIBACTERIAL AGENTS AND BETA-LACTAMASE INHIBITORS - New bicyclic compounds, their preparation, and their use as antibacterial agents, either alone or in combination with an antibiotic for the treatment of infections caused by β-lactamase-producing pathogenic bacteria, are described. | 09-25-2014 |
20140288052 | SUBSTITUTED BICYCLIC AZA-HETEROCYCLES AND ANALOGUES AS SIRTUIN MODULATORS - Provided herein are novel substituted bicyclic aza-heterocycle sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent. | 09-25-2014 |
20140288053 | ANTICANCER PYRIDOPYRAZINES VIA THE INHIBITION OF FGFR KINASES - The invention relates to new pyridopyrazine 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. | 09-25-2014 |
20140296205 | SELECTIVE GLYCOSIDASE INHIBITORS AND USES THEREOF - The invention provides compounds with enhanced permeability for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc. | 10-02-2014 |
20140296206 | COMPOSITIONS USEFUL FOR TREATING DISORDERS RELATED TO KIT - Compounds and compositions useful for treating disorders related to Kit are described herein. | 10-02-2014 |
20140296207 | HETEROCYCLIC COMPOUNDS AND USES THEREOF - Heterocyclic entities that modulate PI3 kinase activity, pharmaceutical compositions containing the isoquinolone entities, and methods of using these chemical entities for treating diseases and conditions associated with P13 kinase activity are described herein. | 10-02-2014 |
20140303143 | BENZOXAZOLINONE COMPOUNDS WITH SELECTIVE ACTIVITY IN VOLTAGE-GATED SODIUM CHANNELS - Disclosed are compounds of Formula (A) or a salt thereof, wherein “Het”, R | 10-09-2014 |
20140309210 | INDAZOLE COMPOUNDS, COMPOSITIONS AND METHODS OF USE THEREOF - A compound of formula I: | 10-16-2014 |
20140309211 | SUBSTITUTED 5-(PYRAZIN-2-YL)-1H-PYRAZOLO [3, 4-B] PYRIDINE AND PYRAZOLO [3, 4-B] PYRIDINE DERIVATIVES AS PROTEIN KINASE INHIBITORS - Substituted 5-(pyrazin-2-yl)-1H-pyrazolo[3,4-b]pyridine, 5-(pyrazin-2-yl)-1H-pyrrolo[2,3-b]pyridine and pyrazolo[3,4-b]pyridine derivatives according to formula I, II and VII, and methods for making same, which are inhibitors of constitutively activated Tyrosine Kinase-Like (TKL), CMGC protein kinases family members and can be useful in the treatment of Parkinson's disease, Alzheimer's disease, Down's Syndrome, Huntington's disease, other neurodegenerative and central nervous system disorders, cancer, metabolic disorders and inflammatory diseases. Also disclosed are pharmaceutical compositions including the compounds and methods of inhibiting wild type and/or mutated protein kinase activities of these families and the treatment of disorders associated therewith using compounds and pharmaceutical compositions including the compounds. | 10-16-2014 |
20140309212 | BRUTON'S TYROSINE KINASE INHIBITORS - The present invention provides compounds useful as inhibitors of Btk, compositions thereof, and methods of using the same. | 10-16-2014 |
20140315886 | QUINAZOLINES AS THERAPEUTIC COMPOUNDS AND RELATED METHODS OF USE - Methods of treating disorders using compounds (I) that modulate stri-atal-enriched tyrosine phosphatase (STEP) are described herein. Exemplary disorders include schizophrenia and cognitive deficit. Formula (I). | 10-23-2014 |
20140315887 | PYRIMIDYL CYCLOPENTANES AS AKT PROTEIN KINASE INHIBITORS - The present invention provides compounds of Formula I, including tautomers, resolved enantiomers, diastereomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof. | 10-23-2014 |
20140315888 | NOVEL HETEROCYCLIC DERIVATIVES AND THEIR USES - The present invention relates to novel heterocyclic compounds useful in preparing drugs for treatment of diseases associated with various functions of the histamine 4 receptor. Especially, the said drugs are useful for treatment of inflammatory diseases, allergy, pain, nasal polyps, rhinitis, chronic sinusitis, nasal congestion, nasal itch, asthma, chronic obstructive pulmonary disease, rheumatoid arthritis, atopic dermatitis, psoriasis, eczema, pruritus, itchy skin, urticaria, idiopathic chronic urticaria, scleroderma, conjunctivitis, keratoconjunctivitis, ocular inflammation, dry eye, cardiac dysfunction, arrhythmia, atherosclerosis, multiple sclerosis, inflammatory bowel disease (including colitis, Crohn's disease, ulcerative colitis), inflammatory pain, neuropathic pain, osteoarthritic pain, autoimmune thyroid disease, immune-mediated (also known as type I) diabetes, lupus, post-operative adhesions, vestibular disorders and cancer. | 10-23-2014 |
20140315889 | HYDROXAMATE DERIVATIVES FOR HDAC INHIBITOR, AND THE PHARMACEUTICAL COMPOSITION COMPRISING THEREOF - The present invention relates to a novel hydroxamate derivatives, more specifically, to novel hydroxamate derivatives having inhibitory activity against Histone Deacetylase (HDAC), isomers thereof, pharmaceutically acceptable salts thereof, hydrates or solvates thereof, use for preparing pharmaceutical compositions, pharmaceutical compositions comprising the same, treatment method using said composition, and a preparing method of novel hydroxamate derivatives. The novel selective hydroxamate derivatives having inhibitory activity against Histone Deacetylase (HDAC) compositions can be used for treatment of inflammatory disease, rheumatoid arthritis, or degenerative disease. | 10-23-2014 |
20140323467 | THERAPEUTIC COMPOUNDS AND COMPOSITIONS - Compounds and compositions comprising compounds 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. | 10-30-2014 |
20140329799 | AMINOPYRIMIDINONES AS INTERLEUKIN RECEPTOR-ASSOCIATED KINASE INHIBITORS - This invention relates to aminopyrimidinone compounds of Formula (I) that are inhibitors of Interleukin receptor-associated kinases, in particular IRAK-4, and are useful in the treatment or prevention of inflammatory diseases, including rheumatoid arthritis and inflammatory bowel disease. | 11-06-2014 |
20140329800 | TRI-HETEROCYCLIC DERIVATIVES, PREPARATION PROCESS AND USES THEREOF - The present invention relates to a tri-heterocyclic derivatives, preparation process and uses thereof, specifically relates to a tri-heterocyclic derivatives of the formula (I) or a pharmaceutically acceptable salt thereof, preparation process, and further relates to a pharmaceutically acceptable composition comprising compounds of formula (I), or a pharmaceutically acceptable salt thereof, and their pharmaceutical use as inhibitors of kinase. | 11-06-2014 |
20140329801 | SULPHONYLAMINOPYRROLIDINONE DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION - The invention relates to new sulphonylaminopyrrolidinone compounds having antithrombotic activity which, in particular, inhibit blood clotting factor IXa and/or factor Xa, to processes for their preparation and to use thereof as drugs. | 11-06-2014 |
20140336175 | PURINE DERIVATIVES FOR USE IN THE TREATMENT OF ALLERGIC, INFLAMMATORY AND INFECTIOUS DISEASES - The present invention relates to compounds of formula (I): | 11-13-2014 |
20140336176 | HETEROAROMATIC COMPOUNDS AND THEIR USE AS DOPAMINE D1 LIGANDS - The present invention provides, in part, compounds of Formula I: | 11-13-2014 |
20140343038 | 1,2,4-TRIAZINE-6-CARBOXAMIDE DERIVATIVE - The present invention provides a compound represented by the following general formula (I) or a salt thereof which has a Syk inhibitory effect (in the formula R | 11-20-2014 |
20140349992 | COMPOUNDS FOR TREATING DISORDERS MEDIATED BY METABOTROPIC GLUTAMATE RECEPTOR 5, AND METHODS OF USE THEREOF - Provided herein are compounds and methods of synthesis thereof. The compounds set forth herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders, neurodegenerative disorders, neuropsychiatric disorders, disorders of cognition, learning or memory, gastrointestinal disorders, lower urinary tract disorder, and cancer. Compounds set forth herein modulate the activity of metabotropic glutamate receptor 5 (mGluR5) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein. | 11-27-2014 |
20140349993 | SUBSTITUTED BICYCLIC AZA-HETEROCYCLES AND ANALOGUES AS SIRTUIN MODULATORS - Provided herein are novel substituted bicyclic aza-heterocycle sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent. | 11-27-2014 |
20140349994 | Novel 2-Amino-4,5,6,8-Tetrahydropyrazolo[3,4-b]Thiazolo [4,5-d]Azepine Derivatives and Their Use as Allosteric Modulators of Metabotropic Glutamate Receptors - The present invention relates to novel compounds of Formula (I), wherein M and R | 11-27-2014 |
20140349995 | TETRAHYDROPYRIDO-PYRIDINE AND TETRAHYDROPYRIDO-PYRIMIDINE COMPOUNDS AND USE THEREOF AS C5A RECEPTOR MODULATORS - The present invention provides a compound of formula I: | 11-27-2014 |
20140349996 | PYRIMIDYL CYCLOPENTANES AS AKT PROTEIN KINASE INHIBITORS - The present invention provides compounds of Formula I, including tautomers, resolved enantiomers, diastereomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof. | 11-27-2014 |
20140349997 | HYDROXYLATED AND METHOXYLATED PYRIMIDYL CYCLOPENTANES AS AKT PROTEIN KINASE INHIBITORS - The present invention provides compounds, including resolved enantiomers, resolved diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula I: | 11-27-2014 |
20140364411 | KINASE INHIBITORS - Compounds of formula (I) described herein are p38 MAPK inhibitors and are useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract. | 12-11-2014 |
20140364412 | KINASE INHIBITORS - Compounds of formula (I) described herein are p38 MAPK inhibitors and are useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract | 12-11-2014 |
20140364413 | PDE 10a Inhibitors for the Treatment of Type II Diabetes - Disclosed are compounds, compositions and methods for treating Type II diabetes. Such compounds are represented by Formula (I) as follows: | 12-11-2014 |
20140364414 | PDE 10a Inhibitors for the Treatment of Type II Diabetes - Disclosed are compounds, compositions and methods for treating Type II diabetes. Such compounds are represented by Formula (I) as follows: | 12-11-2014 |
20140364415 | PYRROLO[2,3-d]PYRIMIDINE TROPOMYSIN-RELATED KINASE INHIBITORS - The present invention relates to compounds of Formula (I) | 12-11-2014 |
20140371201 | BICYCLIC SULFONAMIDE COMPOUNDS AS SODIUM CHANNEL INHIBITORS - The present invention provides compounds of Formula I, | 12-18-2014 |
20140371202 | INDAZOLE COMPOUNDS AS KINASE INHIBITORS AND METHOD OF TREATING CANCER WITH SAME - The present teaching provide indazole compounds represented by Structural Formulae (I) or (I′) or a pharmaceutically acceptable salt thereof. Also described are pharmaceutical compositions and methods of use thereof as protein kinase inhibitors, such as TTK protein kinase, polo-like kinase 4 (PLK4) and Aurora kinases having anticancer activity against breast cancer cells, colon cancer cells, and ovarian cancer cells. | 12-18-2014 |
20140371203 | Thieno- and furo - pyrimidines and pyridines, useful as potassium channel inhibitors - The present invention provides compounds of formula (I): (Formula (I); wherein A, R | 12-18-2014 |
20140371204 | 4-(Benzoimidazol-2-yl)-thiazole Compounds and Related Aza Derivatives - The invention relates to compounds of Formula (I) wherein ring A, X, (R | 12-18-2014 |
20140378432 | HETEROARYL PYRIDONE AND AZA-PYRIDONE COMPOUNDS - Heteroaryl pyridone and aza-pyridone compounds are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using heteroaryl pyridone and aza-pyridone compounds for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. | 12-25-2014 |
20150011531 | INHIBITORS OF HIV REPLICATION - Compounds of formula (I) and pharmaceutical compositions thereof: wherein A | 01-08-2015 |
20150011532 | HETEROCYCLIC-SUBSTITUTED PYRIDYL COMPOUNDS USEFUL AS KINASE INHIBITORS - Compounds having the following formula: wherein A is, or; and X is N or C—R | 01-08-2015 |
20150011533 | 1H-PYRROLO[2,3-B] PYRIDINE DERIVATIVES AND THEIR USE AS KINASE INHIBITORS - The inventions relates to compounds of (I) and therapeutic uses thereof: (I) The terms Z, Y, and R | 01-08-2015 |
20150025058 | 8 - SUBSTITUTED 2 -AMINO - [1,2,4] TRIAZOLO [1, 5 -A] PYRAZINES AS SYK TRYROSINE KINASE INHIBITORS AND GCN2 SERIN KINASE INHIBITORS - Compounds of the formula I | 01-22-2015 |
20150025059 | BICYCLIC HETEROCYCLE DERIVATIVES FOR THE TREATMENT OF PULMONARY ARTERIAL HYPERTENSION - Bicyclic heterocyclic derivatives of formula I useful in inhibiting PDGF receptor mediated biological activity. | 01-22-2015 |
20150031673 | PYRROLE COMPOUNDS, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM - Compounds of formula (I): | 01-29-2015 |
20150031674 | SERINE/THREONINE KINASE INHIBITORS - Compounds having the formula I wherein R | 01-29-2015 |
20150031675 | DIAZABICYCLO[3.3.1]NONANES, METHODS OF SYNTHESIS, AND USES THEREOF - 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). | 01-29-2015 |
20150031676 | SUBSTITUTED 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. | 01-29-2015 |
20150038485 | HETEROCYCLYL AMINOIMIDAZOPYRIDAZINES - The present invention relates to heterocyclyl aminoimidazopyridazine compounds of general formula (I): in which A, R1, R2, R3 and R4 are as defined in the claims, to methods of 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. | 02-05-2015 |
20150038486 | PYRIMIDINYL AND 1,3,5-TRIAZINYL BENZIMIDAZOLE SULFONAMIDES AND THEIR USE IN CANCER THERAPY - Provided herein are pyrimidinyl and 1,3,5-triazinyl benzimidazole sulfonamides, e.g., compounds of Formulae IA, IB, and IC, and their pharmaceutical compositions, preparation, and use as agents or drugs for cancer therapy, either alone or in combination with radiation and/or other anticancer drugs. | 02-05-2015 |
20150045346 | SELECTIVE GLYCOSIDASE INHIBITORS AND USES THEREOF - The invention provides compounds for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc. | 02-12-2015 |
20150045347 | TRIAZOLYL-SUBSTITUTED PYRIDYL COMPOUNDS USEFUL AS KINASE INHIBITORS - Compounds having the following formula: (I) wherein: A is an optionally substituted triazole, or a stereoisomer or a pharmaceutically-acceptable salt thereof, are useful as kinase modulators, including IRAK-4 modulation. | 02-12-2015 |
20150045348 | PDE9 inhibitors with imidazo triazinone backbone - This invention is directed to compounds, which are PDE9 enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula (I). The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula (I). The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula (I). | 02-12-2015 |
20150045349 | 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. | 02-12-2015 |
20150051188 | 2-OXO-OXAZOLIDIN-3,5-DIYL ANTIBIOTIC DERIVATIVES - The invention relates to antibacterial compounds of formula I | 02-19-2015 |
20150051189 | INDOLIZINE COMPOUNDS, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM - Compounds of formula (I): | 02-19-2015 |
20150051190 | IMIDAZO[1,2-b]PYRIDAZINE DERIVATIVES AS KINASE INHIBITORS - The present invention is intended to provide a compound or a pharmacologically acceptable salt thereof which is useful in the treatment of a tumor through its ROS1 kinase enzyme activity inhibitory effect and NTRK kinase enzyme inhibitory effect. The present invention provides a compound having an imidazo[1,2-b]pyridazine structure represented by the general formula (I) or a pharmacologically acceptable salt thereof, and a pharmaceutical composition comprising the compound. In the formula, R | 02-19-2015 |
20150057263 | Quinazoline Compounds And Their Use In Therapy - This invention relates to quinazoline compounds of Formula (I) which are inhibitors of the histone lysine methyltransferase (HKMTase) EZH2, and to uses of such compounds as medicaments, in particular in the treatment of a disease or disorder in which inhibition of EZH2 provides a therapeutic or prophylactic effect. | 02-26-2015 |
20150057264 | BICYCLIC PYRAZINONE DERIVATIVES - Compounds of the formula I | 02-26-2015 |
20150057265 | FURO- AND THIENO-PYRIDINE CARBOXAMIDE COMPOUNDS USEFUL AS PIM KINASE INHIBITORS - The present disclosure describes furo- and thieno-pyridine carboxamide compounds, as well as their compositions and methods of use. The compounds inhibit the activity of the Pim kinases, and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases. | 02-26-2015 |
20150057266 | Pharmaceutical Composition Having Improved Dissolution Profiles For Poorly Soluble Drugs - Pharmaceutical compositions having improved dissolution profiles for drugs therein are disclosed. | 02-26-2015 |
20150065484 | SUSTAINED RELEASE DOSAGE FORMS FOR A JAK1 INHIBITOR - This invention relates to sustained release dosage forms comprising {1-{1-[3-fluoro-2-(trifluoromethyl)isonicotinoyl]piperidin-4-yl}-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]azetidin-3-yl}acetonitrile, or a pharmaceutically acceptable salt thereof, and doses and methods related thereto. | 03-05-2015 |
20150065485 | SUBSTITUTED POLYCYCLIC CARBAMOYLPYRIDONE DERIVATIVE - This invention provides compounds having antiviral activities especially inhibiting activity for influenza virus, more preferably provides substituted 3-hydroxy-4-pyridone derivatives having cap-dependent endonuclease inhibitory activity. | 03-05-2015 |
20150080370 | 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: | 03-19-2015 |
20150080371 | SUBSTITUTED BENZOTHIENYL - PYRROLOTRIAZINES AND USES THEREOF IN THE TREATMENT CANCER - This invention relates to novel substituted 5-(1-benzothiophen-2-yl)pyrrolo[2,1-fJ[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. | 03-19-2015 |
20150080372 | COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR - Compounds and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof are active on each of B-Raf, B-Raf V600E and c-Raf-1 protein kinase. In certain aspects and embodiments, the described compounds are active in inhibiting proliferation of a Ras mutant cell line. Also described are methods of use thereof to treat diseases and conditions, including melanoma, glioma, glioblastoma, pilocytic astrocytoma, liver cancer, biliary tract cancer, cholangiocarcinoma, colorectal cancer, lung cancer, bladder cancer, gallbladder cancer, breast cancer, pancreatic cancer, thyroid cancer, kidney cancer, ovarian cancer, adrenocortical cancer, prostate cancer, gastrointestinal stromal tumors, medullary thyroid cancer, tumor angiogenesis, acute myeloid leukemia, chronic myelomonocytic leukemia, childhood acute lymphoblastic leukemia, plasma cell leukemia, and multiple myeloma. | 03-19-2015 |
20150080373 | NOVEL BICYCLIC ANTIBIOTICS - The antibacterial compound of formula I | 03-19-2015 |
20150080374 | AMINOALCOHOL SUBSTITUTED 2,3-DIHYDROIMIDAZO[1,2-C]QUINAZOLINE DERIVATIVES USEFUL FOR TREATING HYPER-PROLIFERATIVE DISORDERS AND DISEASES ASSOCIATED WITH ANGIOGENESIS - This invention relates to novel 2,3-dihydroimidazo[1,2-c]quinazoline compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for phosphotidylinositol-3-kinase (PI3K) inhibition and treating diseases associated with phosphotidylinositol-3-kinase (PI3K) activity, in particular treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients. | 03-19-2015 |
20150087630 | METHODS OF USE OF DIAZACARBAZOLES FOR TREATING CANCER - Methods of use of compounds of formula (I) for treating cancer: | 03-26-2015 |
20150087631 | AMINO-SUBSTITUTED IMIDAZOPYRIDAZINES - The present invention relates to amino-substituted imidazopyridazine compounds of general formula (I), in which A, R1, R2, R3, R4, R5 and n are as defined in the claims, 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. | 03-26-2015 |
20150087632 | CYCLOBUTYL SUBSTITUTED PYRROLOPYRIDINE AND PYRROLOPYRIMIDINES DERIVATIVES AS JAK INHIBITORS - The present invention provides cyclobutyl substituted pyrrolopyrimidines and pyrrolopyridines of Formula I: | 03-26-2015 |
20150094300 | AMINO-SUBSTITUTED IMIDAZOPYRIDAZINES - The present invention relates to amino-substituted imidazopyridazine compounds of general formula (I); in which A, R1, R2, R3, R4, R5 and n are as defined in the claims, 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. | 04-02-2015 |
20150099736 | Indolyl-Pyridone Derivatives Having Checkpoint Kinase 1 Inhibitory Activity - Compounds of formula (I) have checkpoint kinase 1 (CHK1) inhibitory activity: | 04-09-2015 |
20150099737 | PYRROLOPYRIMIDINE COMPOUNDS AS INHIBITORS OF CDK4/6 - The invention is directed to novel pyrrolopyrimidine compounds of formula (1) wherein R | 04-09-2015 |
20150105372 | SECONDARY ALCOHOL QUINOLINYL MODULATORS OF RORyt - The present invention comprises compounds of Formula I. | 04-16-2015 |
20150105373 | NITROGENATED HETEROCYCLIC COMPOUND - The present invention provides a compound having a PDE2A selective inhibitory action, which is useful as an agent for the prophylaxis or treatment of schizophrenia, Alzheimer's disease and the like. | 04-16-2015 |
20150105374 | Substituted annellated pyrimidines and use thereof - The present application relates to novel substituted annellated pyrimidines, methods for production thereof, use thereof alone or in combinations for treating and/or preventing diseases and use thereof for the production of medicinal products for treating and/or preventing diseases, in particular for treating and/or preventing cardiovascular diseases. | 04-16-2015 |
20150105375 | METHODS FOR TREATING PULMONARY EMPHYSEMA USING SUBSTITUTED 2-AZA-BICYCLO[2.2.1]HEPTANE-3-CARBOXYLIC ACID (BENZYL-CYANO-METHYL)-AMIDES INHIBITORS OF CATHEPSIN C - This invention relates to 2-Aza-bicyclo[2.2.1]heptane-3-carboxylic acid (benzyl-cyano-methyl)-amides of formula 1 | 04-16-2015 |
20150105376 | QUINOLINONE CARBOXAMIDE INHIBITORS OF ENDOTHELIAL LIPASE - The present invention provides compounds of Formula (I): | 04-16-2015 |
20150111873 | PHARMACEUTICALLY ACTIVE PYRAZOLO-TRIAZINE DERIVATIVES - Pyrazolo[1,5-a][1,3,5]triazine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of infectious diseases, including opportunistic diseases, immunological diseases, autoimmune diseases, cardiovascular diseases, cell proliferative diseases, inflammation, erectile dysfunction and stroke, and pharmaceutical compositions containing at least one of said pyrazolo[1,5-a][1,3,5]triazine derivatives and/or pharmaceutically acceptable salts thereof. Furthermore, the present invention relates to the use of said pyrazolo[1,5-a][1,3,5]triazine derivatives as inhibitors for a protein kinase. | 04-23-2015 |
20150111874 | 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. | 04-23-2015 |
20150111875 | Aminotetraline and aminoindane derivatives, pharmaceutical compositions containing them, and their use in therapy - The present invention relates to aminotetraline and aminoindane derivatives of the formula (I) | 04-23-2015 |
20150111876 | SULFUR-CONTAINING BICYCLIC COMPOUND - A sulfur-containing bicyclic compound having a PAM action of GABA | 04-23-2015 |
20150119380 | COMPOUNDS FOR TREATING SPINAL MUSCULAR ATROPHY - Provided herein are compounds, compositions thereof and uses therewith for treating spinal muscular atrophy. In a specific embodiment, provided herein are compounds of a form that may be used to modulate the inclusion of exon 7 of SMN2 into mRNA that is transcribed from the SMN2 gene. In another specific embodiment, provided herein are compounds of a form that may be used to modulate the inclusion of exon 7 of SMN1 into mRNA that is transcribed from the SMN1 gene. In yet another embodiment, provided herein are compounds of a form that may be used to modulate the inclusion of exon 7 of SMN1 and SMN2 into mRNA that is transcribed from the SMN1 and SMN2 genes, respectively. | 04-30-2015 |
20150119381 | USE OF GHRELIN RECEPTOR INVERSE AGONISTS OR ANTAGONISTS FOR TREATING SLEEP DISORDERS - The present invention relates to methods of treating sleep disorders in patients comprising administration of a ghrelin receptor inverse agonist or antagonist. The invention also includes methods of treating sleep disorders comprising the administration of a pharmaceutical composition comprising a ghrelin receptor inverse agonist or antagonist and at least one pharmaceutically acceptable carrier, diluent, or excipient. | 04-30-2015 |
20150119382 | 1,2,6-SUBSTITUTED BENZIMIDAZOLES AS FLAP MODULATORS - The present invention relates to compounds of Formula (I), | 04-30-2015 |
20150126492 | Complement Pathway Modulators and Uses Thereof - The present invention provides a compound of formula I a method for manufacturing the compounds of the invention, and its therapeutic uses as inhibitor of the complement alternative pathway and particularly as inhibitor of Factor B for the treatment of e.g. age-related macular degeneration and diabetic retinopathy. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition. | 05-07-2015 |
20150141400 | QUINAZOLINEDIONE DERIVATIVE - The present invention relates to quinazolinedione derivatives represented by formula (I) or pharmaceutically acceptable salts thereof. | 05-21-2015 |
20150141401 | NOVEL BETA-LACTAMASE INHIBITOR AND PROCESS FOR PREPARING THE SAME - A diazabicyclooctane compound, which is a beta-lactame inhibitor, represented by the following formula (I): | 05-21-2015 |
20150141402 | PURINE DERIVATIVES - The present invention relates to compounds of formula (I) | 05-21-2015 |
20150141403 | 1,2,4-Triazolo [4,3-A] Pyridine Derivatives and Their Use For The Treatment of Prevention of Neurological and Psychiatric Disorders - The present invention relates to novel triazolo[4,3-a]pyridine derivatives of Formula (I) | 05-21-2015 |
20150148331 | MELT-EXTRUDED SOLID DISPERSIONS CONTAINING AN APOPTOSIS-INDUCING AGENT - A pro-apoptotic solid dispersion comprises, in essentially non-crystalline form, a Bcl-2 family protein inhibitory compound of Formula I as defined herein, dispersed in a solid matrix that comprises (a) a pharmaceutically acceptable water-soluble polymeric carrier and (b) a pharmaceutically acceptable surfactant. A process for preparing such a solid dispersion comprises subjecting to elevated temperature the compound of Formula I, the water-soluble polymeric carrier and the surfactant, to provide an extrudable semi-solid mixture; extruding the semi-solid mixture; and cooling the resulting extrudate to provide a solid matrix comprising the polymeric carrier and the surfactant and having the compound dispersed in essentially non-crystalline form therein. The solid dispersion is suitable for oral administration to a subject in need thereof for treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer or an immune or autoimmune disease. | 05-28-2015 |
20150148332 | TRIAZOLO COMPOUNDS AS PDE10 INHIBITORS - The present invention provides compounds of formula (Ia) and (Ib) | 05-28-2015 |
20150290192 | INHIBITORS OF BRUTON'S TYROSINE KINASE - This application discloses the Btk inhibitor compounds 6-tert-Butyl-8-fluoro-2-{3-hydroxymethyl-4-[1-methyl-5-(1′-methyl-1′,2′,3′,4′,5′,6′-hexahydro-[3,4′]bipyridinyl-6-ylamino)-6-oxo-1,6-dihydro-pyridazin-3-yl]-pyridin-2-yl}-2H-phthalazin-1-one, 2-(2-{3-[5-(5-Azetidin-1-ylmethyl-1-methyl-1H-pyrazol-3-ylamino)-1-methyl-6-oxo-1,6-dihydro-pyridazin-3-yl]-2-hydroxy methyl-phenyl}-8-fluoro-1-oxo-1,2-dihydro-isoquinolin-6-yl)-2-methyl-propionitrile, and 6-tert-Butyl-2-[2-hydroxymethyl-3-(5-{5-[(2-methoxy-ethylamino)-methyl]-pyridin-2-ylamino}-6-oxo-1,6-dihydro-pyridin-3-yl)-phenyl]-3,4-dihydro-2H-isoquinolin-1-one, formulations thereof, and methods of treatment of asthma, as described herein. | 10-15-2015 |
20150290212 | THERAPEUTIC USES OF SELECTED PYRAZOLOPYRIMIDINE COMPOUNDS WITH ANTI-MER TYROSINE KINASE ACTIVITY - Pyrazolopyrimidine compounds, methods of use, and processes for making compounds with anti-Mer tyrosine kinase activity comprising Formula I, II, III, IV, or a pharmaceutically acceptable composition, salt, isotopic analog, or prodrug thereof, are provided. The pyrazolopyrimidine compounds described herein have Mer tyrosine kinase (MerTK) inhibitory activity and are useful as anti-infective agents, immunostimulatory and immunomodulatory agents, anti-cancer agents (including against MerTK −/− tumors and ITD and TKD mutant forms of Acute Myeloid Leukemia (AML)), and as adjunctive agents in combination with chemotherapeutic, radiation or other standard of care for neoplasms. | 10-15-2015 |
20150291564 | SUBSTITUTED INDOL-5-OL DERIVATIVES AND THEIR THERAPEUTICAL APPLICATIONS - The present invention relates generally to the use of compounds to treat a variety of disorders, diseases and pathologic conditions and more specifically to the use of substituted indol-5-ol derivatives to modulate protein kinases and for treating protein kinase-mediated diseases. | 10-15-2015 |
20150291593 | NOVEL HETEROARYL AND HETEROCYCLE COMPOUNDS, COMPOSITIONS AND METHODS - Provided are novel heteroaryl and heterocycle compounds of formula (I-1), (I-2) or (I-3) and pharmaceutical compositions comprising them, uses and methods thereof for inhibiting the activity of PI | 10-15-2015 |
20150291606 | MERTK-SPECIFIC PYRROLOPYRIMIDINE COMPOUNDS - The present invention includes pyrrolopyrimidine compounds that selectively inhibit Mer tyrosine kinase (MerTK) activity and/or Tyro3 tyrosine kinase activity, and use of these pyrrolopyrimidine compounds as anti-cancer agents, immunostimulatory and immunomodulatory agents, anti-platelet agents, anti-infective agents, and as adjunctive agents in combination with chemotherapeutic, radiation or other standard of care for neoplasms. | 10-15-2015 |
20150291625 | Heteroaromatic Compounds and their Use as Dopamine D1 Ligands - The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof and N-oxides thereof; processes and intermediates for preparation of; and compositions and uses thereof. The present invention further provides D1 agonists with reduced D1R desensitization, D1 agonists with a reduced β-arrestin recruitment activity relative to Dopamine, D1 agonists interacting significantly with the Ser188 but not significantly with the Ser202 of a D1R when binding to the D1R, D1 agonists interacting less strongly with the Asp103 and interacting less strongly with the Ser198 of a D1R when binding to the D1R, and their uses. | 10-15-2015 |
20150299203 | PYRAZOLOPYRIMIDINE COMPOUNDS - The present teachings provide a compound represented by structural formula (1-0), or a pharmaceutically acceptable salt thereof. Also described are pharmaceutical compositions and methods of use thereof. | 10-22-2015 |
20150299205 | 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. | 10-22-2015 |
20150299220 | NOVEL PYRAZINE DERIVATIVES AS CB2 RECEPTOR AGONISTS - The invention relates to a compound of formula (I) wherein R | 10-22-2015 |
20150299224 | INHIBITORS OF IRAK4 ACTIVITY - The present invention relates to compounds which modulate interleukin-1 (IL-1) receptor-associated kinase 4 (IRAK4) and are useful in the prevention or treatment of inflammatory, cell proliferative and immune-related conditions and diseases. Specifically, provided herein are inhibitors of IRAK4 of Formula I and pharmaceutical compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases. | 10-22-2015 |
20150307520 | NOVEL HETEROARYL AND HETEROCYCLE COMPOUNDS, COMPOSITIONS AND METHODS THEREOF - Disclosed are novel heteroaryl and heterocycle compounds of formula I-1, I-2 or I-3 and pharmaceutical compositions comprising them, uses and methods thereof for inhibiting the activity of PI | 10-29-2015 |
20150320733 | INDAZOLE COMPOUNDS AS ALDOSTERONE SYNTHASE INHIBITORS - This invention relates to indazole compounds of the structural formula: (structure represented) or their pharmaceutically acceptable salts, wherein the variable are defined herein. The inventive compounds selectively inhibit aldosterone synthase. This invention also provides for pharmaceutical compositions comprising the compounds of Formula I or their salts as well as potentially to methods for the treatment or amelioration of conditions that could be treated by inhibiting aldosterone synthase. | 11-12-2015 |
20150322008 | INDOLE CARBOXAMIDE DERIVATIVES AS P2X7 RECEPTOR ANTAGONIST - The invention relates to indole carboxamide derivatives of formula (I), | 11-12-2015 |
20150322056 | Factor IXa Inhibitors - The present invention provides a compound of Formula (I) | 11-12-2015 |
20150322066 | SUBSTITUTED BENZIMIDAZOLE-TYPE PIPERIDINE COMPOUNDS AND USES THEREOF - The disclosure relates to Substituted Benzimidazole-Type Piperidine Compounds of Formula (I): | 11-12-2015 |
20150329497 | SMALL MOLECULE AGONISTS OF NEUROTENSIN RECEPTOR 1 - Provided herein are small molecule neurotensin receptor agonists, compositions comprising the compounds, and methods of using the compounds and compositions comprising the compounds. | 11-19-2015 |
20150329536 | SUBSTITUTED NORIBOGAINE - This invention relates noribogaine derivatives, compositions and methods of use thereof. | 11-19-2015 |
20150329538 | AMIDES AS PIM INHIBITORS - The invention relates to amide-containing compounds of formula (1), 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. | 11-19-2015 |
20150329542 | PYRAZOLOPYRIDINES AND PYRAZOLOPYRIMIDINES - A compound having the structure: | 11-19-2015 |
20150329551 | OXINDOLE COMPOUNDS CARRYING A NITROGEN-BOUND SPIRO SUBSTITUENT AND USE THEREOF FOR TREATING VASOPRESSIN-RELATED DISEASES - The present invention relates to novel substituted oxindole derivatives of the formula I | 11-19-2015 |
20150336952 | Imidazo[4,5-c]quinolin-2-one Compounds and Their Use in Treating Cancer - The specification generally relates to compounds of Formula (I): | 11-26-2015 |
20150336967 | Novel Benzimidazole Derivatives as Kinase Inhibitors - The present invention relates to derivatives of benzimidazoles of formula (I) as disclosed herein as well as pharmaceutical compositions comprising said derivatives. The derivates according to the present invention are serine/threonine and tyrosine kinase-inhibitors, particularly of PIM1-3- and DYRK1A-kinases and may particularly be used in the treatment of diseases linked to these kinases, such as e.g. leukemias, lymphomas, solid tumors and autoimmune disorders. | 11-26-2015 |
20150336975 | COMPOUNDS FOR THE REDUCTION OF BETA-AMYLOID PRODUCTION - The present disclosure provides a series of compounds of the formula (I) | 11-26-2015 |
20150336982 | Five-And-Six-Membered Heterocyclic Compound, And Preparation Method, Pharmaceutical Composition And Use Thereof - A five-and-six-membered heterocyclic compound as represented by general formula I, pharmaceutically acceptable salt, metabolite, metabolic precursors or drug precursors thereof, preparation method, pharmaceutical composition, and use thereof; the five-and-six-membered heterocyclic compound has activity as a Janus kinase (JAK) inhibitor, and can be used to prepare drugs for treating diseases caused by the abnormal activity of kinase, such as cell proliferation diseases like cancer. | 11-26-2015 |
20150342952 | TREATMENT OF CHRONIC NEUTROPHILIC LEUKEMIA (CNL) AND ATYPICAL CHRONIC MYELOID LEUKEMIA (aCML) BY INHIBITORS OF JAK1 - This invention relates to JAK selective inhibitors for use in treatment of chronic neutrophilic leukemia and atypical chronic myeloid leukemia in patients. | 12-03-2015 |
20150344433 | PRMT5 INHIBITORS CONTAINING A DIHYDRO- OR TETRAHYDROISOQUINOLINE 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 |
20150344468 | 6-SUBSTITUTED-3H-1,3-BENZOTHIAZOL-2-ONE COMPOUNDS AS TARP-GAMMA 8 DEPENDENT AMPA RECEPTOR ANTAGONISTS - A TARP γ8 dependant AMPA receptor antagonist of the formula: | 12-03-2015 |
20150344474 | HETEROAROMATIC COMPOUNDS AND THEIR USE AS DOPAMINE D1 LIGANDS - The present invention provides, in part, compounds of Formula I: | 12-03-2015 |
20150344490 | Heteroaromatic Compounds and their Use as Dopamine D1 Ligands - The present invention provides, in part, compounds of Formula I: | 12-03-2015 |
20150353497 | NOVEL QUINOLINE DERIVATIVES AND THEIR USE IN NEURODEGENERATIVE DISEASES - The present invention relates to quinoline compounds, and pharmaceutically acceptable compositions thereof, useful as antagonists of P2X7, and for the treatment of P2X7-related disorders. | 12-10-2015 |
20150353553 | 2,6,7,8 SUBSTITUTED PURINES AS HDM2 INHIBITORS - The present invention provides 2,6,7,8 Substituted Purines as described herein or a pharmaceutically acceptable salt thereof. The representative compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same. | 12-10-2015 |
20150353561 | NOVEL COMPOUNDS - Compounds of formula (I), described herein, exhibit human neutrophil elastase inhibitory properties, and are useful for the treatment of diseases and conditions in which HNE is implicated. | 12-10-2015 |
20150353570 | BTK INHIBITORS - The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula I or a pharmaceutically acceptable salt thereof or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds in the treatment of Btk mediated disorders. | 12-10-2015 |
20150353578 | HETEROCYCLIC COMPOUND AND USE THEREOF - Provided is a compound represented by the formula (I): | 12-10-2015 |
20150361054 | PHOSPHATIDYLINOSITOL 3-KINASE INHIBITORS - The present application provides the compounds of formula (J), | 12-17-2015 |
20150361080 | SUBSTITUTED NORIBOGAINE - This invention relates noribogaine derivatives, compositions and methods of use thereof. | 12-17-2015 |
20150361100 | INDOLIZINE DERIVATIVES AS PHOSHOINOSITIDE 3-KINASES INHIBITORS - Compounds of formula (I), defined herein, inhibit phosphoinositide 3-kinases (PI3K) and are useful for the treatment of disorders associated with PI3K enzymes. | 12-17-2015 |
20150361101 | 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. | 12-17-2015 |
20150368245 | TRICYCLIC PYRROLOPYRIDINE COMPOUND, AND JAK INHIBITOR - To provide a novel tricyclic pyrrolopyridine compound having a JAK inhibitory activity and useful for prevention, treatment and/or improvement of particularly autoimmune diseases, inflammatory diseases and allergic diseases. | 12-24-2015 |
20150368256 | NEW BICYCLICPYRIDINE DERIVATIVES - The invention provides novel compounds having the general formula (I) | 12-24-2015 |
20150368271 | CERTAIN TRIAZOLOPYRIDINES AND TRIAZOLOPYRAZINES, COMPOSITIONS THEREOF AND METHODS OF USE THEREFOR - Provided are certain triazolopyridines and triazolopyrazines, compositions thereof and methods of use therefor. | 12-24-2015 |
20150376181 | MNK INHIBITORS AND METHODS RELATED THERETO - The present invention relates to compounds according to Formula (I): | 12-31-2015 |
20160000785 | Novel Imidazole Amines as Modulators of Kinase Activity - The invention provides novel imidazole amine compounds according to Formula (I) and Formula (II) their manufacture and use for the treatment of hyperproliferative diseases, such as cancer. | 01-07-2016 |
20160000795 | TREATMENT OF B-CELL MALIGNANCIES BY A COMBINATION JAK AND PI3K INHIBITORS - This invention relates to methods of treating B-cell malignancies using a combination of inhibitors of JAK1 and/or JAK2 and inhibitors of PI3Kδ. | 01-07-2016 |
20160002246 | NOVEL COMPOUNDS AS DUAL INHIBITORS OF PHOSPHODIESTERASES AND HISTONE DEACETYLASES - It relates to certain compounds having a polycyclic structure and a hydroxamic acid moiety, wherein the polycyclic structure comprises at least three ring systems, wherein one ring system is a polycyclic ring system comprising from 2 to 4 rings; at least one ring is an aromatic ring; and wherein the structure comprises at least 3 nitrogen atoms and 1 oxygen atom. It also relates to a process for their preparation, as well as to pharmaceutical compositions containing them, and to their use in medicine, in particular in the treatment and/or prevention of neurological disorders coursing with a cognition deficit or impairment, or neurodegenerative diseases. wherein B | 01-07-2016 |
20160009681 | COMPOUNDS INHIBITING LEUCINE-RICH REPEAT KINASE ENZYME ACTIVITY | 01-14-2016 |
20160009689 | COMPOUNDS INHIBITING LEUCINE-RICH REPEAT KINASE ENZYME ACTIVITY | 01-14-2016 |
20160009696 | COMPOUNDS INHIBITING LEUCINE-RICH REPEAT KINASE ENZYME ACTIVITY | 01-14-2016 |
20160009710 | SUBSTITUTED TRIAZOLOPYRIDINES AND METHODS OF USE THEREOF | 01-14-2016 |
20160009714 | BICYCLIC AROMATIC CARBOXAMIDE COMPOUNDS USEFUL AS PIM KINASE INHIBITORS | 01-14-2016 |
20160009720 | IMIDAZOPYRAZINES AS LSD1 INHIBITORS | 01-14-2016 |
20160015690 | THERAPEUTIC COMPOUNDS - Compounds disclosed herein including compounds of formula I′: | 01-21-2016 |
20160016914 | SPIROCYCLOHEPTANES AS INHIBITORS OF ROCK - The present invention provides compounds of Formula (I): | 01-21-2016 |
20160016936 | NOVEL HETEROCYCLES AS MODULATORS OF KINASE ACTIVITY - The invention provides novel heterocyclic amines according to Formula (I) their manufacture and use for the treatment of hyperproliferative diseases, such as cancer. | 01-21-2016 |
20160016937 | Novel substituted pyrimidine compounds - The invention relates to novel substituted pyrimidine compounds of general formula (I) | 01-21-2016 |
20160016945 | SUBSTITUTED INDOL-5-OL DERIVATIVES AND THEIR THERAPEUTIC APPLICATIONS - The present invention relates generally to the use of compounds to treat a variety of disorders, diseases and pathologic conditions and more specifically to the use of substituted indol-5-ol derivatives to modulate protein kinases and for treating protein kinase-mediated diseases. | 01-21-2016 |
20160016953 | KINASE INHIBITORS - Compounds of formula (I) described herein are p38 MAPK inhibitors and are useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract | 01-21-2016 |
20160016963 | Piperazino[1,2-a]indol-1-ones and [1,4]diazepino[1,2-a]indol-one - The present invention relates to compounds of general formula I | 01-21-2016 |
20160024054 | PHOSPHATIDYLINOSITOL 3-KINASE INHIBITORS - The present disclosure provides phosphatidylinositol | 01-28-2016 |
20160024090 | BETA-LACTAMASE INHIBITOR AND PROCESS FOR PREPARING THE SAME - A diazabicyclooctane compound, which is a beta-lactame inhibitor, represented by the following formula (I): | 01-28-2016 |
20160024095 | HEDGEHOG PATHWAY SIGNALING INHIBITORS AND THERAPEUTIC APPLICATIONS THEREOF - The hedgehog (Hh) signaling pathway is a pathway which regulates patterning, growth and cell migration during embryonic development, but in adulthood is limited to tissue maintenance and repair. Mutational inactivation of the inhibitory pathway components leads to constitutive ligand-independent activation of the Hh signaling pathway, results in cancers such as basal cell carcinoma and medulloblastoma. Ligand-dependent activation of Hh signaling is involved in prostate cancer, pancreatic cancer, breast cancer and some blood cancers. Therefore, inhibition of the aberrant Hh signaling represents a promising approach toward novel anticancer therapy. The present invention provides novel molecules of formula I that inhibit hedgehog pathway signaling and provides therapeutic applications for the treatment of malignancies (basal cell carcinoma, medulloblastoma, glioblastoma, non-small cell lung cancer, prostate cancer, pancreatic cancer, blood cancers, mesenchymal cancers, etc.), prevention of tumor regrowth, sensitization of radio-chemo therapies, and other diseases (inflammation, fibrosis and immune disorders) related to hedgehog signaling. | 01-28-2016 |
20160024109 | TRICYCLIC FUSED THIOPHENE DERIVATIVES AS JAK INHIBITORS - The present invention provides tricyclic fused thiophene 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. | 01-28-2016 |
20160030395 | SUBSTITUTED 5-(3,5-DIMETHYLISOXAZOL-4-YL)INDOLINE-2-ONES - Disclosed are substituted 5-(3,5-dimethylisoxazol-4-yl)indoline-2-one compounds, pharmaceutical compositions comprising at least one such 4 substituted 5-(3,5-dimethylisoxazol-4-yl)indoline-2-one compound processes for the preparation thereof, and the use thereof for inhibiting BET family of bromodomains and for treating disorders mediated thereby, such as certain cancers. | 02-04-2016 |
20160031893 | 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 |
20160031901 | SUBSTITUTED THIOPHENE- AND FURAN-FUSED AZOLOPYRIMIDINE-5-(6H)-ONE COMPOUNDS - Described herein are compounds and chemical entities of Formula (I), methods of their synthesis, compositions comprising them, and their use in treating numerous diseases and disorders, including cognitive deficits associated with CNS diseases and disorders. | 02-04-2016 |
20160031908 | CHEMOKINE RECEPTOR ANTAGONISTS AND METHODS OF USE THEREOF - Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by: | 02-04-2016 |
20160039790 | 1,2,6-SUBSTITUTED BENZIMIDAZOLES AS FLAP MODULATORS - The present invention relates to compounds of Formula (I), | 02-11-2016 |
20160039811 | HETEROCYCLIC COMPOUND - Provided is a compound or a salt thereof, which has an excellent JAK inhibitory action, and is useful as a prophylactic or therapeutic agent for autoimmune diseases (rheumatoid arthritis, psoriasis, inflammatory bowel disease, Sjogren's syndrome, Behcet's syndrome, multiple sclerosis, systemic lupus erythematosus, etc.), cancer (leukemia, uterine leiomyosarcoma, prostate cancer, multiple myeloma, cachexia, myelofibrosis, etc.) and the like. The present invention relates to a compound represented by the formula (I) | 02-11-2016 |
20160039846 | AZABENZIMIDAZOLE DERIVATIVES - The present invention relates to compounds of general formula I, | 02-11-2016 |
20160046600 | 1,2,5-SUBSTITUTED BENZIMIDAZOLES AS FLAP MODULATORS - The present invention relates to compounds of Formula (I), | 02-18-2016 |
20160046603 | Crystalline Forms of D-Glucitol, 1-Deoxy-1-(Methylamino)-, 1-(6-Amino-3,5-Difluoropyridine-2-Yl)-8-Chloro-6-Fluoro-1,4-Dihydro-7-(3-- Hydroxyazetidin-1-Yl)-4-Oxo-3-Quinolinecarboxylate - The present disclosure relates generally to crystalline forms of anhydrous D-glucitol, 1-deoxy-1-(methylamino)-, 1-(6-amino-3,5-difluoropyridin-2-yl)-8-chloro-6-fluoro-1,4-dihydro-7-(3-hydroxyazetidin-1- yl)-4-oxo-3-quinolinecarboyxlate, compositions comprising the same, and methods of making the same. Delafloxacin is an fluoroquinolone antibiotic with the chemical structure and the chemical name 1-deoxy-1-(methylamino)-, 1-(6-amino-3,5-difluoropyridin-2-yl)-8-chloro-6-fluoro-1,4-dihydro-7-(3-hydroxyazetidin-1-yl)-4-oxo-3-quinolinecarboyxlate. Studies have indicated the existence of three anhydrous polymorphs of delafloxacin, as well as a trihydrate and methanol and ethanol solvates. | 02-18-2016 |
20160046627 | ITK and JAK Kinase Inhibitors - The present invention relates to compounds described by Formula I: | 02-18-2016 |
20160046631 | PURINE DERIVATIVES AS CB2 RECEPTOR AGONISTS - The invention relates to a compound of formula (I) | 02-18-2016 |
20160046637 | PYRROLO[2,3-D]PYRIMIDINE DERIVATIVES AS CB2 RECEPTOR AGONISTS - The invention relates to a compound of formula (I) | 02-18-2016 |
20160046639 | IMIDAZO[1,2-b]PYRIDAZINE DERIVATIVES AS KINASE INHIBITORS - The present invention is intended to provide a compound or a pharmacologically acceptable salt thereof which is useful in the treatment of a tumor through its ROS1 kinase enzyme activity inhibitory effect and NTRK kinase enzyme inhibitory effect. The present invention provides a compound having an imidazo[1,2-b]pyridazine structure represented by the general formula (I) or a pharmacologically acceptable salt thereof, and a pharmaceutical composition comprising the compound. In the formula, R | 02-18-2016 |
20160046650 | TRICYCLIC HETEROCYCLES AS BET PROTEIN INHIBITORS - The present invention relates to tricyclic heterocycles which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer. | 02-18-2016 |
20160052913 | SUBSTITUTED BENZIMIDAZOLES AS NOCICEPTIN RECEPTOR MODULATORS - The invention provides modulators of the nociceptin receptor (NOP), including both agonists and antagonists. A compound of the invention can be a selective modulator of NOP with respect to the μ- and κ-opioid receptors (MOP and KOP), thus providing a therapeutic method for the treatment of conditions wherein selective NOP modulation is medically indicated and MOP or KOP modulation may be less desirable. A compound of the invention can be a NOP full agonist, partial agonist, inverse agonist, positive or negative allosteric modulator, or a functionally biased agonist. A compound of the invention can be used for the treatment of an anxiety state, post-traumatic stress disorder, addictive disorders (including overuse of alcohol, tobacco, and drugs of abuse such as cocaine, amphetamines, and opitates), misregulated food intake and/or energy expenditure, cough, sleep disorders, grain, pain, depression, or neurodegenerative disorders such as Parkinsons disease or Alzheimers disease. | 02-25-2016 |
20160058742 | FUSED AMINO PYRIDINE AS HSP90 INHIBITORS - The present invention relates to HSP90 inhibitors containing fused amino pyridine core that are useful as inhibitors of HSP90 and their use in the treatment of HSP90 related diseases and disorders such as cancer, an autoimmune disease, or a neurodegenerative disease. | 03-03-2016 |
20160058750 | METHODS OF TREATING INFECTIONS IN OVERWEIGHT AND OBESE PATIENTS USING ANTIBIOTICS - The present disclosure relates generally to methods of treating infections in overweight or obese patients using antibiotics. According to statistics compiled by National Health and Nutrition Examination Survey conducted by the National Center for Health Statistics (NCHS) of the U.S. Centers for Disease Control and Prevention (CDC), in 2009-2010, 35.7% of adults in the United States were found to be obese. Ogden, C.L. NCHS Data Brief 2012, 82, available at http://www.cdc.gov/nchs/data/databiefs/db82.pdf (last visited Mar. 2, 2013). | 03-03-2016 |
20160058764 | METHODS FOR TREATING HAIR LOSS DISORDERS - The invention provides for methods for treating a hair loss disorder in a subject by administering a Janus Kinase/Signal Transducers and Activators of Transcription inhibitor. | 03-03-2016 |
20160058765 | METHODS FOR TREATING HAIR LOSS DISORDERS - The invention provides for methods for treating a hair loss disorder in a subject by administering a Janus Kinase/Signal Transducers and Activators of Transcription inhibitor. | 03-03-2016 |
20160060261 | SUBSTITUTED 5-(PYRAZIN-2-YL)-1H-PYRAZOLO [3, 4-B] PYRIDINE AND PYRAZOLO [3, 4-B] PYRIDINE DERIVATIVES AS PROTEIN KINASE INHIBITORS - Substituted 5-(pyrazin-2-yl)-1H-pyrazolo[3,4-b]pyridine, 5-(pyrazin-2-yl)-1H-pyrrolo[2,3-b]pyridine and pyrazolo[3,4-b]pyridine derivatives according to formula I, II and VII, and methods for making same, which are inhibitors of constitutively activated Tyrosine Kinase-Like (TKL), CMGC protein kinases family members and can be useful in the treatment of Parkinson's disease, Alzheimer's disease, Down's Syndrome, Huntington's disease, other neurodegenerative and central nervous system disorders, cancer, metabolic disorders and inflammatory diseases. Also disclosed are pharmaceutical compositions including the compounds and methods of inhibiting wild type and/or mutated protein kinase activities of these families and the treatment of disorders associated therewith using compounds and pharmaceutical compositions including the compounds. | 03-03-2016 |
20160060270 | New Aryl-Quinoline Derivatives - The invention provides novel compounds having the general formula (I) | 03-03-2016 |
20160068494 | FUSED HETEROCYCLIC OR CARBOCYCLIC COMPOUNDS CARRYING A SUBSTITUTED CYCLOALIPHATIC RADICAL AND USE THEREOF FOR TREATING VASOPRESSIN-RELATED DISEASES - The present invention relates to novel fused heterocyclic or carbocyclic compounds of formula I | 03-10-2016 |
20160068529 | 3-(1H-BENZO[D]IMIDAZOL-2-YL)-1H-PYRAZOLO[3,4-C]PYRIDINE AND THERAPEUTIC USES THEREOF - Azaindazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an azaindazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states. | 03-10-2016 |
20160068547 | 3-(1H-IMIDAZO[4,5-C]PYRIDIN-2-YL)-1H-PYRAZOLO[3,4-C]PYRIDINE AND THERAPEUTIC USES THEREOF - Azaindazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an azaindazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states. | 03-10-2016 |
20160068548 | 3-(3H-IMIDAZO[4,5-C]PYRIDIN-2-YL)-1H-PYRAZOLO[3,4-C]PYRIDINE AND THERAPEUTIC USES THEREOF - Azaindazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an azaindazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states. | 03-10-2016 |
20160068549 | 3-(1H-IMIDAZO[4,5-C]PYRIDIN-2-YL)-1H-PYRAZOLO[3,4-B]PYRIDINE AND THERAPEUTIC USES THEREOF - Azaindazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an azaindazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states. | 03-10-2016 |
20160068550 | 3-(3H-IMIDAZO[4,5-B]PYRIDIN-2-YL)-1H-PYRAZOLO[3,4-B]PYRIDINE AND THERAPEUTIC USES THEREOF - Azaindazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an azaindazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states. | 03-10-2016 |
20160068551 | 3-(3H-IMIDAZO[4,5-B]PYRIDIN-2-YL)-1H-PYRAZOLO[3,4-C]PYRIDINE AND THERAPEUTIC USES THEREOF - Azaindazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an azaindazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states. | 03-10-2016 |
20160074395 | SUBSTITUTED 5-(PYRAZIN-2-YL)-1H-PYRAZOLO [3, 4-B] PYRIDINE AND PYRAZOLO [3, 4-B] PYRIDINE DERIVATIVES AS PROTEIN KINASE INHIBITORS - Substituted 5-(pyrazin-2-yl)-1H-pyrazolo[3, 4-b]pyridine, 5-(pyrazin-2-yl)-1H-pyrrolo[2,3-b]pyridine and pyrazolo[3,4-b]pyridine derivatives according to formula I, II and VII, and methods for making same, which are inhibitors of constitutively activated Tyrosine Kinase-Like (TKL), CMGC protein kinases family members and can be useful in the treatment of Parkinson's disease, Alzheimer's disease, Down's Syndrome, Huntington's disease, other neurodegenerative and central nervous system disorders, cancer, metabolic disorders and inflammatory diseases. Also disclosed are pharmaceutical compositions including the compounds and methods of inhibiting wild type and/or mutated protein kinase activities of these families and the treatment of disorders associated therewith using compounds and pharmaceutical compositions including the compounds. | 03-17-2016 |
20160075692 | Indazole Ureas and Method of Use - Compounds of formula (I) | 03-17-2016 |
20160075699 | 3-(2-AMINOPYRIMIDIN-4-YL)-5-(3-HYDROXYPROPYNYL)-1H-PYRROLO[2,3-C]PYRIDINE DERIVATIVES AS NIK INHIBITORS FOR THE TREATMENT OF CANCER - The present invention relates to compounds of formula (I) which are inhibitors of NF- | 03-17-2016 |
20160075701 | 2-(1H-INDAZOL-3-YL)-1H-IMIDAZO[4,5-C]PYRIDINE AND THERAPEUTIC USES THEREOF - Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states. | 03-17-2016 |
20160075704 | NOVEL SUBSTITUTED SPIROCYCLES - This invention relates to a compound of formula I | 03-17-2016 |
20160075715 | SUBSTITUTED TETRAHYDROISOQUINOLINE COMPOUNDS AS FACTOR XIA INHIBITORS - The present invention provides compounds of Formula (I): | 03-17-2016 |
20160083368 | THERAPEUTIC COMPOUNDS - Compounds of formula I: | 03-24-2016 |
20160083392 | Fused heterocyclic compounds as protein kinase inhibitors - The invention is fused heterocyclic compounds of formula (I), and salts thereof, compositions thereof, and methods of use therefor. In particular, disclosed herein are certain fused heterocyclic compounds that can be useful for inhibiting protein kinase, including Bruton's tyrosine kinase (Btk), and for treating disorders mediated thereby. | 03-24-2016 |
20160090380 | 2-(1H-INDAZOL-3-YL)-3H-IMIDAZO[4,5-B]PYRIDINE AND THERAPEUTIC USES THEREOF - Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states. | 03-31-2016 |
20160090382 | Substituted 1 H-Pyrrolo [2, 3-b] pyridine and 1 H-Pyrazolo [3, 4-b] pyridine Derivatives as Salt Inducible Kinase 2 (SIK2) Inhibitors - Compounds according to Formulas I, IA or IB: | 03-31-2016 |
20160096846 | 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: | 04-07-2016 |
20160102055 | INDOLINONE COMPOUNDS AND USES THEREOF - Indolinone derivative compounds that act as EWS-FLI1 transcription factor inhibitors are provided. Also provided are pharmaceutical compositions of the indolinone derivatives, methods of synthesizing the same, methods of treating using same, and assays for identifying the inhibitors of EWS-FLI1 oncoprotein. | 04-14-2016 |
20160102091 | HETEROCYCLIC MODULATORS OF LIPID SYNTHESIS - Compounds that are fatty acid synthesis modulators are provided. The compounds may be used to treat disorders characterized by disregulation of the fatty acid synthase function by modulating the function and/or the fatty acid synthase pathway. Methods are provided for treating such disorders including viral infections, such as hepatitis C infection, cancer and metabolic disorders. | 04-14-2016 |
20160108028 | 1,2,5-SUBSTITUTED BENZIMIDAZOLES AS FLAP MODULATORS - The present invention relates to compounds of Formula (I), | 04-21-2016 |
20160108057 | TRICYCLIC HETEROCYCLIC COMPOUNDS AS PHOSPHOINOSITIDE 3-KINASE INHIBITORS - Compounds of formula (I) or a pharmaceutically acceptable sail thereof, wherein: W is O, N—H, N—(C | 04-21-2016 |
20160122341 | 3-ARYL-SUBSTITUTED IMIDAZO[1,2-A]PYRIDINES AND THEIR USE - The present application relates to novel 3-aryl-substituted imidazo[1,2-a]pyridines, to processes for preparation thereof, to the use thereof, alone or in combinations, for treatment and/or prophylaxis of diseases, and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially for treatment and/or prophylaxis of cardiovascular disorders. | 05-05-2016 |
20160122342 | ENHANCER OF ZESTE HOMOLOG 2 INHIBITORS - This invention relates to novel compounds according to Formula (I) which are inhibitors of Enhancer of Zeste Homolog 2 (EZH2), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment of cancers. | 05-05-2016 |
20160122343 | Novel Pyridopyrimidinone Compounds for Modulating the Catalytic Activity of Histone Lysine Demethylases (KDMs) - The present invention provides a compound of Formula (I) being capable of modulating the activity of histone lysine demethylase (KDM), pharmaceutical compositions thereof, methods to prepare the said compounds, and the use of such compounds as a medicament. The compound of Formula (I) acts as KDM inhibitor with marked potency, thereby having an outstanding potential for a pharmaceutical intervention of cancer and any other diseases related to KDM dysregulation. | 05-05-2016 |
20160137636 | Bicyclic Sulfonamide Compounds as Sodium Channel Inhibitors - The present invention provides compounds of Formula I or pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav1.7. The compounds are useful for the treatment of diseases treatable by inhibition of sodium channels such as pain disorders. Also provided are pharmaceutical compositions containing compounds of the present invention. | 05-19-2016 |
20160137648 | TETRAAZA-CYCLOPENTA[A]INDENYL DERIVATIVES - The present invention provides compounds of Formula (I) as M1 receptor positive allosteric modulators for the treatment of diseases mediated by the muscarinic M1 mediator. | 05-19-2016 |
20160137668 | NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A - The present invention relates to novel compounds of the formula I 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. | 05-19-2016 |
20160145263 | TETRAHYDROISOQUINOLINES CONTAINING SUBSTITUTED AZOLES AS FACTOR XIA 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 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. | 05-26-2016 |
20160145270 | COMPOUNDS FOR TREATING SPINAL MUSCULAR ATROPHY - The present invention provides compounds of formula (I) wherein A, B, X, Y, R1 and R2 are as described herein, as well as pharmaceutically acceptable salts thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments. | 05-26-2016 |
20160152576 | AKT PROTEIN KINASE INHIBITORS | 06-02-2016 |
20160152582 | THERAPEUTIC COMPOUNDS | 06-02-2016 |
20160152606 | HYDROXYLATED AND METHOXYLATED PYRIMIDYL CYCLOPENTANES AS AKT PROTEIN KINASE INHIBITORS | 06-02-2016 |
20160158234 | BIHETEROARYL COMPOUNDS AND USES THEREOF - The present invention provides for compounds of Formula I and embodiments and salts thereof for the treatment of diseases (e.g., neurodegenerative diseases). R | 06-09-2016 |
20160159801 | NOVEL BICYCLIC BROMODOMAIN INHIBITORS - The invention relates to substituted bicyclic compounds, which are useful for inhibition of BET protein function by binding to bromodomains, pharmaceutical compositions comprising these compounds, and use of the compounds and compositions in therapy. | 06-09-2016 |
20160159804 | PYRIDINES, PYRIMIDINES, AND PYRAZINES, AS BTK INHIBITORS AND USES THEREOF - The present invention relates to pyridine, pyrimidine, and pyrazene compounds, and pharmaceutically acceptable compositions thereof, useful as BTK inhibitors. | 06-09-2016 |
20160159808 | HETEROCYCLIC COMPOUND - A compound represented by the formula (I): | 06-09-2016 |
20160159809 | HETEROCYCLIC COMPOUNDS AS BIOGENIC AMINE TRANSPORT MODULATORS - The present disclosure relates to certain amine derivatives of fused bicyclic heterocycles that inhibit the amine reuptake function of the biogenic amine transporters, dopamine transporter (DAT), serotonin transporter (SERT) and norepinephrine transporter (NET). Compounds of the present disclosure are potent inhibitors of the reuptake of dopamine (DA), serotonin (5-hydroxytryptamine, 5-HT) and norepinephrine (NE) with full or partial maximal efficacy. The compounds with partial maximal efficacy in inhibiting reuptake of all three biogenic amines are herein referred to as partial triple uptake inhibitors (PTRIs). Compounds of the present disclosure are useful for treating depression, pain and substance abuse and relapse to substance abuse and addiction to substances such as cocaine, methamphetamine, nicotine and alcohol. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. | 06-09-2016 |
20160168125 | WNT SIGNALING INHIBITOR | 06-16-2016 |
20160168129 | QUINAZOLINE DERIVATIVES, COMPOSITIONS THEREOF, AND USE AS PHARMACEUTICALS | 06-16-2016 |
20160168158 | NOVEL TRIAZOLO[4,5-D]PYRIMIDINE DERIVATIVES | 06-16-2016 |
20160175284 | ESTROGEN RECEPTOR MODULATORS AND USES THEREOF | 06-23-2016 |
20160176841 | SELECTIVELY SUBSTITUTED QUINOLINE COMPOUNDS | 06-23-2016 |
20160176867 | MODIFIED BET-PROTEIN-INHIBITING DIHYDROQUINOXALINONES AND DIHYDROPYRIDOPYRAZINONES | 06-23-2016 |
20160176871 | TGF BETA R ANTAGONISTS | 06-23-2016 |
20160176882 | TRIAZOLOPYRIMIDINE COMPOUNDS AND USES THEREOF | 06-23-2016 |
20160184305 | 1,4-DISUBSTITUTED PYRIDAZINE QUINOLNE ANALOGS THERE OF AND METHODS FOR TREATING SMN-DEFICIENCY-RELATED CONDITIONS - The present invention provides a compound of formula IA or a pharmaceutically acceptable salt thereof; 5 (IA) a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition. | 06-30-2016 |
20160184308 | AMINOPYRIMIDINE DERIVATIVES FOR USE AS MODULATORS OF KINASE ACTIVITY - The invention provides novel heterocyclic amine compounds according to Formula (I) and their manufacture and use for the treatment of hyperproliferative diseases, such as cancer. | 06-30-2016 |
20160193206 | BET-PROTEIN-INHIBITING DIHYDROPYRIDOPYRAZINONES | 07-07-2016 |
20160193216 | IRAK INHIBITORS AND USES THEREOF | 07-07-2016 |
20160194328 | SELECTIVE GRP94 INHIBITORS AND USES THEREOF | 07-07-2016 |
20160194329 | Therapeutically Active Pyrazolo-Pyrimidine Derivatives | 07-07-2016 |
20160200722 | COMPOUNDS INHIBITING LEUCINE-RICH REPEAT KINASE ENZYME ACTIVITY | 07-14-2016 |
20160200729 | NEW CHEMICAL COMPOUNDS (DERIVATIVES) AND THEIR APPLICATION FOR THE TREATMENT OF ONCOLOGICAL DISEASES | 07-14-2016 |
20160200741 | Novel indazoles for the treatment and prophylaxis of respiratory syncytial virus infection | 07-14-2016 |
20160376240 | 6 Phenyl or 6 Pyridin 3 YL Indazole Derivatives and Methods of Use - Compounds of formula (I) and pharmaceutically acceptable salts, esters, amides, or radiolabelled forms thereof, wherein R | 12-29-2016 |
20160376275 | Imidazopyridazine Derivatives as Modulators of TNF Activity - A series of substituted imidazo[1,2-b]pyridazine derivatives of formula (I), being potent modulators of human TNFa 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 |
20160376291 | IMIDAZOLO-, OXAZOLO-, AND THIAZOLOPYRIMIDINE MODULATORS OF TRPV1 - Certain TRPV1-modulating imidazolo-, oxazolo-, and thiazolopyrimdine compounds are described. The compounds may be used in pharmaceutical compositions and methods for treating disease states, disorders, and conditions mediated by TRPV1 activity, such as pain, arthritis, itch, cough, asthma, or inflammatory bowel disease. | 12-29-2016 |
20180021235 | METHODS FOR TREATING HAIR LOSS DISORDERS | 01-25-2018 |
20180022758 | BICYCLIC HETEROCYCLYL DERIVATIVES AS IRAK4 INHIBITORS | 01-25-2018 |
20190144444 | KRAS G12C INHIBITORS | 05-16-2019 |
20220135566 | CRYSTALLINE SOLID FORMS OF BARICITINIB - The present disclosure relates to cocrystals/salts of baricitinib, processes for preparation thereof as well as a pharmaceutical composition comprising the same. | 05-05-2022 |