Entries |
Document | Title | Date |
20080200457 | 4-Cyclopropyl-1,2,3,-Thiadiazole Compound, Agrohorticultural Plant Disease Controlling Agent And Method Of Using The Same - The present invention relates to 1,2,3 -thiadiazole compounds represented by formula (I): | 08-21-2008 |
20080221092 | Heterobicyclic metalloprotease inhibitors - The present invention relates generally to amide containing heterobicyclic containing pharmaceutical agents, and in particular, to amide containing heterobicyclic metalloprotease inhibiting compounds. More particularly, the present invention provides a new class of heterobicyclic MMP-3 and/or MMP-13 inhibiting compounds that exhibit an increased potency and selectivity in relation to currently known MMP-13 and MMP-3 inhibitors. | 09-11-2008 |
20080221093 | Metalloprotease inhibitors containing a heterocyclic moiety - The present invention relates generally to pharmaceutical agents containing a heterocyclic moiety, and in particular, to heterocyclic metalloprotease inhibiting compounds. More particularly, the present invention provides a new class of heterocyclic MMP-13 inhibiting compounds with a benzoxazinone moiety, that exhibit an increased potency and selectivity in relation to currently known MMP-13 inhibitors. | 09-11-2008 |
20080221094 | Metalloprotease inhibitors containing a squaramide moiety - The present invention relates generally to pharmaceutical agents containing a heterocyclic moiety, and in particular, to heterocyclic metalloprotease inhibiting compounds. More particularly, the present invention provides a new class of heterocyclic MMP-13 inhibiting compounds with a squaramide moiety, that exhibit an increased potency and selectivity in relation to currently known MMP-13 inhibitors. | 09-11-2008 |
20080221095 | Metalloprotease inhibitors containing a heterocyclic moiety - The present invention relates generally to pharmaceutical agents containing a heterocyclic moiety, and in particular, to heterocyclic metalloprotease inhibiting compounds. More particularly, the present invention provides a new class of heterocyclic MMP-3, MMP-8 and/or MMP-13 inhibiting compounds with a squaramide or benzoxazinone moiety, that exhibit an increased potency and selectivity in relation to currently known MMP-13, MMP-8 and MMP-3 inhibitors. | 09-11-2008 |
20080227776 | INHIBITORS OF HEMEPROTEIN-CATALYZED LIPID PEROXIDATION - Methods and compounds for the treatment or prevention of oxidative damage in a mammalian subject. The treatment and/or prevention may be on inhibiting heme-induced lipid peroxidation. Also discloses are methods and compounds for treating or preventing isoprostane-mediated tissue damage. | 09-18-2008 |
20080234257 | SUBSTITUTED PHENETHYLAMINES WITH SEROTONINERGIC AND/OR NOREPINEPHRINERGIC ACTIVITY - Chemical syntheses and medical uses of novel inhibitors of the uptake of monoamine neurotransmitters and pharmaceutically acceptable salts and prodrugs thereof, for the treatment and/or management of psychotropic disorders, anxiety disorder, generalized anxiety disorder, depression, post-traumatic stress disorder, obsessive-compulsive disorder, panic disorder, hot flashes, senile dementia, migraine, hepatopulmonary syndrome, chronic pain, nociceptive pain, neuropathic pain, painful diabetic retinopathy, bipolar depression, obstructive sleep apnea, psychiatric disorders, premenstrual dysphoric disorder, social phobia, social anxiety disorder, urinary incontinence, anorexia, bulimia nervosa, obesity, ischemia, head injury, calcium overload in brain cells, drug dependence, attention deficit hyperactivity disorder, fibromyalgia, irritable bowel syndrome, and/or premature ejaculation are described. | 09-25-2008 |
20080242662 | Organic Compounds - The invention relates to substituted 3,4- or higher substituted piperazine compounds, the use thereof 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; 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; pharmaceutical formulations or products comprising said compounds, and/or a method of treatment comprising administering said compounds, a method for the manufacture of said compounds as well as novel intermediates, starting materials and/or partial steps for their synthesis. The compounds are especially of the formula I, | 10-02-2008 |
20080249086 | Novel Oxabispidine Compounds And Their Use In The Treatment Of Cardiac Arrhythmias -
There is provided compounds of formula I, wherein R | 10-09-2008 |
20080249087 | Heterocylic antiviral compounds - This invention relates to piperidine derivatives of formula I wherein R | 10-09-2008 |
20080255108 | NOVEL THIOPHENE SULFOXIMINES, COMPOSITIONS THEREOF, AND METHODS OF TREATING COMPLEMENT-MEDIATED DISEASES AND CONDITIONS - Disclosed are compounds for treating the symptoms of an acute or chronic disorder mediated by the classical pathway of the complement cascade. Said compounds are of Formula I | 10-16-2008 |
20080255109 | Non-peptide GnRH antagonists - Compounds according to general formula 1, wherein A | 10-16-2008 |
20080261965 | KINASE INHIBITORS USEFUL FOR THE TREATMENT OF MYLEOPROLIFIC DISEASES AND OTHER PROLIFERATIVE DISEASES - Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant, melanomas, glioblastomas, ovarian cancer, pancreatic cancer, prostate cancer, lung cancers, breast cancers, kidney cancers, cervical carcinomas, metastasis of primary tumor sites, myeloproliferative diseases, leukemias, papillary thyroid carcinoma, non small cell lung cancer, mesothelioma, hypereosinophilic syndrome, gastrointestinal stromal tumors, colonic cancers, ocular diseases characterized by hyperproliferation leading to blindness including various retinopathies, rheumatoid arthritis, asthma, chronic obstructive pulmonary disease, mastocyclosis, mast cell leukemia, a disease caused by c-Abl kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof, or a disease caused by c-Kit kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof. | 10-23-2008 |
20080269208 | Pyridine Derivatives and Their Use in the Treatment of Psychotic Disorders - There are provided according to the invention novel compounds of formula (I) or a pharmaceutically acceptable salt or solvate thereof: | 10-30-2008 |
20080275035 | Nitroimidazole Compounds - The present invention relates to certain nitroimidazole compounds, which have interesting pharmaceutical properties. In particular, the compounds are useful in the treatment and/or prevention of infections such as those caused by | 11-06-2008 |
20080280895 | 5-Amino-4-Hydroxy-7-(1H-Indolmethyl)-8-Methylnonamide Derivatives as Renin Inhibitors for the Treatment of Hypertension - The application relates to novel alkanamides of the general formula (I) where X is —CH | 11-13-2008 |
20080280896 | Dipyrrole Compounds, Compositions, and Methods For Treating Cancer or Viral Diseases - The present invention relates to novel Dipyrrole Compounds, compositions comprising a Dipyrrole Compound, and methods useful for treating or preventing cancer or a neoplastic disorder comprising administering a Dipyrrole Compound. The compounds, compositions, and methods of the invention are also useful for inhibiting the growth of a cancer cell or neoplastic cell, treating or preventing a viral infection, or inhibiting the replication and/or infectivity of a virus. The invention also provides screening assays for compounds that can be used in combination with Dipyrrole Compounds for the treatment of cancer or neoplastic disease, inhibition of cancer cell growth, or treatment of viral infections. | 11-13-2008 |
20080280897 | Aerosol Formulation for Inhalation - The present invention relates to a propellant-free aerosol formulation which contains one or more compounds of general formula 1. | 11-13-2008 |
20080287427 | Bicyclic Amides as Kinase Inhibitors - The invention relates to compounds of formula (I) and their use in the treatment of the animal or human body, to pharmaceutical compositions comprising en a compound of formula I and to the use of a compound of formula I for the preparation of pharmaceutical compositions for use in the treatment of protein kinase dependent diseases, especially of proliferative diseases, such as in particular tumour diseases. | 11-20-2008 |
20080287428 | Novel Heterocyclidene Acetamide Derivative - A compound represented by formula (I′): | 11-20-2008 |
20080287429 | Dissolution of Arterial Cholesterol Plaques by Pharmacologically Induced Elevation of Endogenous Bile Salts - A group of pharmaceutical substances induce elevation of endogenous bile salts and acids via different mechanisms. The elevated circulating bile salts exert a beneficial effect in atherosclerosis by acting both as atherolytic and antiatherogenic agents. The result of the elevated circulating endogenous bile salt is the dissolution of cholesterol/lipidic aggregates of the atherosclerotic plaques. | 11-20-2008 |
20080293708 | Pyrimidine Derivatives - Novel pyrimidine derivatives of formula I | 11-27-2008 |
20080293709 | Novel 2-Amino-Heterocycles Useful in the Treatment of Abeta-Related Pathologies - This invention relates to novel compounds having the structural formula I below: and to their pharmaceutically acceptable salts, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia. | 11-27-2008 |
20080293710 | Aerosol formulation for the inhalation of beta-agonists - The present invention relates to a propellant-free aerosol formulation which [contains] one or more compounds of general formula 1 | 11-27-2008 |
20080300243 | Amide Derivatives as Ion-Channel Ligands and Pharmaceutical Compositions and Methods of Using the Same - Compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others. | 12-04-2008 |
20080306057 | P13K Inhibitors for the Treatment of Endometriosis - This invention relates to a method of treating and/or preventing endometriosis comprising administering a PI3K inhibitor. The PI3K inhibitor can also be administered combined with a hormonal suppressor. The invention further relates to the treatment of endometriosis-related infertility. | 12-11-2008 |
20080306058 | Combinations Comprising a Vegf Receptor Inhibitor - A composition comprising a VEGF receptor inhibitor and a penetration enhancer and uses thereof. | 12-11-2008 |
20080306059 | Pyrimido [4,5-B] -Oxazines For Use as Dgat Inhibitors - Compounds of formula (I) or salts thereof, wherein A, and R | 12-11-2008 |
20080312222 | 4-Benzyledene-Piperidin Derivatives - The present invention relates to new 4-benzylidene-piperidin derivatives of formula (I), useful as NMDA, in a particular NR2B subunit containing receptor antagonists and analgesica. | 12-18-2008 |
20080318941 | 4' SUBSTITUTED COMPOUNDS HAVING 5-HT6 RECEPTOR AFFINITY - The present disclosure provides compounds having affinity for the 5-HT | 12-25-2008 |
20090012073 | N-AROYL CYCLIC AMINES - Disclosed are N-aroyl cyclic amine derivatives having the formula: | 01-08-2009 |
20090023716 | Benzoxazines and Related Nitrogen-Containing Heterobicyclic Compounds Useful as Mineralocorticoid Receptor Modulating Agents - The present invention relates to a compound, useful as a mineralocorticoid receptor-modulating agent, of the following formula [I]: | 01-22-2009 |
20090023717 | MORPHINE-BRIDGED INDAZOLE DERIVATIVES - The present invention relates to novel morpholine-bridged indazole derivatives which stimulate soluble guanylate cyclase, to process for the preparation thereof, and to the use thereof for producing medicaments, in particular medicaments for the treatment of disorders of the central nervous system. | 01-22-2009 |
20090029981 | SUBSTITUTED 4-PHENYLPIPERIDINES - The application relates to substituted 4-phenylpiperidines of the general formula and their salts, preferably their pharmaceutically acceptable salts, in which R | 01-29-2009 |
20090036438 | FIVE-MEMBERED HETEROCYCLES USEFUL AS SERINE PROTEASE INHIBITORS - The present invention provides a method for treating a thrombotic or an inflammatory disorder administering to a patient in need thereof a therapeutically effective amount of at least one compound of Formula (I) or Formula (V): | 02-05-2009 |
20090042874 | ANTIDEPRESSANT HETEROARYL DERIVATIVES OF HETEROCYCLE-FUSED BENZODIOXANS - The invention provides compounds of the Formula: | 02-12-2009 |
20090042875 | SUBSTITUTED HETEROCYCLIC COMPOUNDS AND USES THEREOF - The present invention relates to substituted heterocyclic compounds and compositions comprising a substituted heterocyclic compound. The present invention also relates to methods for preventing or treating various diseases and disorders by administering to a subject in need thereof one or more substituted heterocyclic compounds. In particular, the invention relates to methods for preventing or treating cancer or an inflammatory disorder by administering to a subject in need thereof one or more substituted heterocyclic compounds. The present invention further relates to articles of manufacture and kits comprising one or more substituted heterocyclic compounds. | 02-12-2009 |
20090054421 | Pyrimidothiophene Compounds Having HSP90 Inhibitory Activity - Compounds of formula (I) are HSP90 inhibitors, of utility in the treatment of, for example, cancers: wherein R | 02-26-2009 |
20090054422 | New Oxabispidine Compounds For The Treatment Of Cardiac Arrhythmias - There is provided compounds of formula I, wherein R | 02-26-2009 |
20090054423 | Niacin receptor agonists, compositions containing such compounds and methods of treatment - The present invention encompasses compounds of Formula I: as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating dyslipidemias. Pharmaceutical compositions and methods of use are also included. | 02-26-2009 |
20090054424 | Optically active pyridine derivative and a medicament containing the same - An optically active (−)-7-[2-(cyclopropylmethoxy)-6-hydroxyphenyl]-5-[(3S)-3-piperidinyl]-1,4-dihydro-2H-pyrido[2,3-d][1,3]oxazin-2-one of the formula: | 02-26-2009 |
20090054425 | PROTEIN KINASE INHIBITORS - Compounds, particularly compounds having spleen tyrosine kinase (Syk) inhibition activity, having the following structure: | 02-26-2009 |
20090062267 | L-ALANINE DERIVATIVES AS a5beta1 ANTAGONISTS - The present invention relates to compounds that inhibit a5b1 function, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment in warm-blooded animals such as humans of diseases that have a significant angiogenesis or vascular component such as for treatment of solid tumours. The present invention also relates to compounds that inhibit a5b1, and also that exhibit appropriate selectivity profile(s) against other integrins. | 03-05-2009 |
20090062268 | NOVEL INHIBITORS OF POLY(ADP-RIBOSE)POLYMERASE (PARP) - A compound having the structure set forth in Formula (I): | 03-05-2009 |
20090062269 | Niacin Receptor Agonists, Compositions Containing Such Compounds and Methods of Treatment - The present invention encompasses compounds of Formula I: as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating atherosclerosis, dyslipidemias and the like. Pharmaceutical compositions and methods of use are also included. | 03-05-2009 |
20090062270 | SPIRO 2,4 PYRIMIDINEDIAMINE COMPOUNDS AND THEIR USES - The present invention provides methods of treating or preventing autoimmune diseases with spiro 2,4-pyrimidinediamine compounds, as well as methods of treating, preventing or ameliorating symptoms associated with such diseases. Specific examples of autoimmune diseases that can be treated or prevented with the compounds include rheumatoid arthritis and/or its associated symptoms, systemic lupus erythematosis and/or its associated symptoms and multiple sclerosis and/or its associated symptoms. | 03-05-2009 |
20090069312 | Potassium Channel Inhibitors - The present invention relates to dipyridin-3-ylmethoxy compounds and derivatives thereof having the structure I useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like. | 03-12-2009 |
20090075989 | NON-STEROIDAL PROGESTERONE RECEPTOR MODULATORS - The present invention relates to non-steroidal progesterone receptor modulators of the general formula 1, | 03-19-2009 |
20090075990 | Aerosol Formulation for Inhalation Containing an Anticholinergic Agent - The invention relates to specific aqueous aerosol formulations that are devoid of propellant, containing one or more anticholinergic agents of formula (1), in which X | 03-19-2009 |
20090075991 | DEUTERIUM-ENRICHED EFAVIRENZ - The present application describes deuterium-enriched efavirenz, pharmaceutically acceptable salt forms thereof, and methods of treating using the same. | 03-19-2009 |
20090075992 | Pteridine Derivatives as Nitric Oxide Synthase Activators - The present invention relates to the use of pteridine derivatives as nitric oxide synthase activators. In particular, the derivatives find use in the treatment of diseases associated with endothelial dysfunction such as cardiovascular diseases. | 03-19-2009 |
20090082344 | Methods and systems for treating disease - Methods and systems described herein are applicable to the identification of pathogens, pathogenic variants and applicable treatments or remedies. In some embodiments, the pathogen or pathogens bears a causal relationship to a disease state. | 03-26-2009 |
20090088424 | METHODS AND COMPOSITIONS FOR CONTROLLING THE BIOAVAILABILITY OF POORLY SOLUBLE DRUGS - Provided are methods and compositions for controlling the bioavailability of poorly soluble drugs, including, for example, efravirenz. | 04-02-2009 |
20090088425 | GLUCOCORTICOID RECEPTOR ANTAGONISTS - The present invention relates to compounds of formula I | 04-02-2009 |
20090088426 | Substituted 4-Phenyl Piperidines for Use as Renin Inhibitors - Compounds of the general formula (I) and the salts thereof, preferably the pharmaceutically acceptable salts thereof; in which R | 04-02-2009 |
20090093472 | ORTHO PYRROLIDINE, BENZYL-SUBSTITUTED HETEROCYCLE CCR1 ANTAGONISTS FOR AUTOIMMUNE DISEASES & INFLAMMATION - Compounds of the formula | 04-09-2009 |
20090099162 | Novel Oxabispidine Compounds And Their Use In The Treatment Of Cardiac Arrhythmias -
There is provided compounds of formula I,
| 04-16-2009 |
20090099163 | GLUCOKINASE ACTIVATORS - Compounds are provided for use with glucokinase that comprise the formula: | 04-16-2009 |
20090099164 | Phenylaminopropanol Derivatives and Methods of Their Use - The present invention is directed to phenylaminopropanol derivatives of formula I: | 04-16-2009 |
20090111801 | SUBSTITUTED PYRAZINONE DERIVATIVES FOR USE AS A MEDICINE - The present invention concerns substituted pyrazinone derivatives according to the general Formula (I), a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof, an N-oxide form thereof or a quaternary ammonium salt thereof, wherein the variables are defined in Claim | 04-30-2009 |
20090111802 | CYCLOCARBAMATE DERIVATIVES AS PROGESTERONE RECEPTOR MODULATORS - This invention provides compounds of Formula (I): | 04-30-2009 |
20090124608 | CB2 Receptor Modulators In Neurodegenerative Diseases And Applications Of The Same - Compositions for the treatment of neurodegenerative diseases are disclosed. Methods of treating and monitoring progression of a neurodegenerative disease are disclosed. According to the present invention, a selective CB2 receptor modulator may be administered to a mammal for the treatment of a neurodegenerative disease. | 05-14-2009 |
20090124609 | Fused heterocyclic derivatives and methods of use - Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes. | 05-14-2009 |
20090124610 | PHARMACEUTICAL COMPOUNDS - Compounds of the formula (I), and salts, solvates, tautomers and N-oxide thereof, wherein TG is selected from groups (1) and (2): wherein the asterisk (*) represents the point of attachment of the group E to the group X; R | 05-14-2009 |
20090137576 | Novel Piperidine Derivative - Disclosed is a substance having an antagonistic effect on the binding of histamine to a histamine H3 receptor or an inhibitory effect on the activity which a histamine H3 receptor constantly exhibits. A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof; (I) | 05-28-2009 |
20090137577 | HETEROCYCLIC COMPOUNDS - Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I | 05-28-2009 |
20090137578 | ENANTIOMERICALLY PURE BETA AGONISTS, PROCESS FOR THE MANUFACTURE THEREOF AND USE THEREOF AS MEDICAMENTS - Enantiomerically pure compounds of general formula 1 | 05-28-2009 |
20090149454 | Benzomorpholine derivatives and methods of use - Selected benzomorpholine compounds are effective for prophylaxis and treatment of diseases, such as VEGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes. | 06-11-2009 |
20090156588 | 3,4-DIHYDRO-BENZO[E][1,3]OXAZIN-2-ONES - The present invention relates 3,4-dihydro-benzo[e][1,3]oxazin-2-ones which are substituted at the nitrogen atom by unsubstituted or substituted (C | 06-18-2009 |
20090156589 | 1,2-DI(CYCLIC GROUP)SUBSTITUTED BENZENE DERIVATIVE - A compound represented by the following general formula (1) or (100), a salt thereof or a hydrate of the foregoing has excellent cell adhesion inhibitory action and cell infiltration inhibitory action. | 06-18-2009 |
20090156590 | Vanilloid Receptor Ligands, Pharmaceutical Compositions Containing Them, Process for Making Them, and Use Thereof for Treating Pain and Other Conditions - Vanilloid receptor ligand compounds corresponding to formula I: | 06-18-2009 |
20090163486 | Novel 2-arylthiazole-4-carboxamide derivatives, their preparation and use as pharmaceuticals - The present invention relates to 2-arylthiazole-4-carboxamide derivatives of the formula (I), the use thereof as medicament for the treatment of various disorders, and processes for the preparation thereof | 06-25-2009 |
20090170839 | AEROSOL FORMULATION FOR INHALATION CONTAINING AN ANTICHOLINERGIC AGENT - The invention relates to specific aqueous aerosol formulations that are devoid of propellant, containing one or more anticholinergic agents of formula (1), in which X represents an anion, and containing at least one pharmacologically compatible organic acid and optionally additional pharmacologically compatible adjuvants and/or complexing agents. The cation of formula (1′) is contained in the preparation at a concentration of between 830.22 and 904.2 mg per 100 ml of medicament preparation. | 07-02-2009 |
20090170840 | NS1 protein inhibitors - The present invention generally relates to compounds to treat viral infections and methods of their use. In particular, compounds of the present invention inhibit the activity of NS1 protein, thereby mitigating viral infection and, in particular, influenza virus infection. Accordingly, NS1 protein inhibitors and methods of treatment that employ such inhibitors are contemplated by the present invention. | 07-02-2009 |
20090176773 | Non-Peptidic Inhibitors of AKAP/PKA Interaction - The invention relates to non-peptidic molecules which modulate, especially inhibit, the interaction of protein kinase A (PKA) and A kinase anchor proteins (AKAP) and to a host or target organism that comprises said non-peptidic compounds or recognition molecules directed to said compounds, such as e.g. antibodies or chelating agents. The invention also relates to a pharmaceutical agent, especially for use in the treatment of diseases that are associated with a disturbance of the cAMP signal path, especially insipid diabetes, hypertonia, pancreatic diabetes, duodenal ulcer, asthma, heart failure, obesity, AIDS, edema, hepatic cirrhosis, schizophrenia and others. The invention also relates to the use of the inventive molecules. | 07-09-2009 |
20090176774 | Compounds and methods of use - Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes. | 07-09-2009 |
20090176775 | DERIVATIVES OF UREAS OF PIPERIDINE OR PYRROLIDINE, THEIR PREPARATION AND THEIR THERAPEUTICAL USE - The present invention is related to a compound of formula (I): | 07-09-2009 |
20090192148 | Organic Compounds - The invention relates to 3,5-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 3,5-substituted piperidine compound, and/or a method of treatment comprising administering a 3,5-substituted piperidine compound, a method for the manufacture of a 3,5-substituted piperidine compound, and novel intermediates and partial steps for its synthesis. | 07-30-2009 |
20090192149 | Imidazo Compounds - The application relates to novel heterocyclic compounds of the general formula (I) and salts, preferably pharmaceutically acceptable salts, thereof, in which R, R | 07-30-2009 |
20090192150 | IMINO-IMIDAZO-PYRIDINE DERIVATIVES HAVING ANTITHROMBOTIC ACTIVITY - The invention relates to compounds of the formula I | 07-30-2009 |
20090197877 | Antibacterial Compositions - Compounds of formula (I) have antibacterial activity: wherein: m is 0 or 1; Q is hydrogen or cyclopropyl; AIk is an optionally substituted, divalent C | 08-06-2009 |
20090197878 | SUBSTITUTED BENZO[d][1,3]OXAZIN-2(4H)-ONES AND RELATED DERIVATIVES AND THEIR USES FOR MODULATING THE PROGESTERONE RECEPTOR - Compounds of formula (I), or pharmaceutically acceptable salts thereof, are provided, wherein R | 08-06-2009 |
20090197879 | VANILLOID RECEPTOR LIGANDS AND THEIR USE IN TREATMENTS - Compounds having the general structure | 08-06-2009 |
20090209528 | SUBSTITUTED TETRAHYDROISOQUINOLINE COMPOUND, THEIR PREPARATION AND USE IN MEDICAMENTS - The present invention relates to substituted tetrahydroisoquinoline compounds of general formula (I), a process for their preparation, medicaments comprising said substituted tetrahydroisoquinoline compounds as well as the use of said substituted tetrahydroisoquinoline compounds for the preparation of medicaments, which are particularly suitable for the prophylaxis and/or treatment of disorders or diseases that are at least partially mediated via 5-HT | 08-20-2009 |
20090209529 | 4,5-DIHYDRO-OXAZOL-2-YL AMINE DERIVATIVES - The present invention relates to a compounds of formula I | 08-20-2009 |
20090215763 | SUBSTITUTED BENZOXAZINONES - The present invention provides substituted oxazinone compounds, such as substituted benzoxazinones, which exhibit potent renin inhibition activities. | 08-27-2009 |
20090221566 | INHIBITORS OF PHOSPHODIESTERASE TYPE-IV - The present invention relates to oxazine derivatives, which can be used as selective inhibitors of phosphodiesterase (PDE) type IV. Compounds disclosed herein can be useful in the treatment of CMS disorders, AIDS, asthma, arthritis, bronchitis, chronic obstructive pulmonary disease (COPD), psoriasis, allergic rhinitis, shock, atopic dermatitis, Crohn's disease, adult respiratory distress syndrome (ARDS), eosinophilic granuloma, allergic conjunctivitis, osteoarthritis, ulcerative colitis and other inflammatory diseases especially in humans. Processes for the preparation of disclosed compounds are provided, as well as pharmaceutical compositions containing the disclosed compounds, and their use as phosphodiesterase (PDE) type IV inhibitors. | 09-03-2009 |
20090221567 | MUSCARINIC RECEPTOR AGONISTS, COMPOSITIONS, METHODS OF TREATMENT THEREOF, AND PROCESSES FOR PREPARATION THEREOF 177 - Compounds of Formula I, or pharmaceutically acceptable salts thereof: | 09-03-2009 |
20090239856 | Use of Pyrrolopyridine Compounds for Activating PPAR Receptors and Treatment of Conditions Involving Such Receptors - A method of activating PPAR receptors in a subject, said method comprising administering to said subject an effective PPAR receptor activating amount of a pyrrolopyridine compound corresponding to formula (I): | 09-24-2009 |
20090247512 | MACROCYLIC INHIBITORS OF HEPATITIS C VIRUS - Inhibitors of HCV replication of formula (I) | 10-01-2009 |
20090253691 | TRISUBSTITUTED 1,2,4-TRIAZOLES - The present invention relates to 3-aniline-5-aryl triazole derivatives and analogues or pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, according to Formula (I). | 10-08-2009 |
20090253692 | CRYSTALLINE FORM OF N-[[4-FLUORO-2-(5-METHYL-1H-1,2,4-TRIAZOL-1-YL)PHENYL]METHYL]-4,6,7,9-TET- RAHYDRO-3-HYDROXY-9,9-DIMETHYL-4-OXO-PYRIMIDO[2,1-C][1,4]OXAZINE-2-CARBOXA- MIDE, SODIUM SALT MONOHYDRATE - Disclosed is a crystalline form of N-[[4-fluoro-2-(5-methyl-1H-1,2,4-triazol-1-yl)phenyl]methyl]-4,6,7,9-tetrahydro-3-hydroxy-9,9-dimethyl-4-oxo-pyrimido[2,1-c][1,4]oxazine-2-carboxamide, sodium salt monohydrate. Also disclosed are at least one pharmaceutical composition comprising at least one crystalline form of N-[[4-fluoro-2-(5-methyl-1H-1,2,4-triazol-1-yl)phenyl]methyl]-4,6,7,9-tetrahydro-3-hydroxy-9,9-dimethyl-4-oxo-pyrimido[2,1-c][1,4]oxazine-2-carboxamide, sodium salt monohydrate, and at least one method of using at least one crystalline form of N-[[4-fluoro-2-(5-methyl-1H-1,2,4-triazol-1-yl)phenyl]methyl]-4,6,7,9-tetrahydro-3-hydroxy-9,9-dimethyl-4-oxo-pyrimido[2,1-c][1,4]oxazine-2-carboxamide, sodium salt monohydrate to treat AIDS or HIV infection. | 10-08-2009 |
20090253693 | 2H-BENZO[b][1,4]OXAZIN-3(4H)-ONE DERIVATIVES FOR USE AS STEAROYL CoA DESATURASE INHIBITORS - The present invention discloses 2H-benzo[b][1,4]oxazin-3(4H)-one derivatives for use as inhibitors of stearoyl-CoA desaturase having the structure of Formula I: | 10-08-2009 |
20090264424 | VANILLOID RECEPTOR LIGANDS AND THEIR USE IN TREATMENTS - Compounds having the general structure | 10-22-2009 |
20090270380 | 3,4,5-Substituted Piperidines as Renin Inhibitors - The application relates to novel substituted piperidines of the general formula (II) in which R | 10-29-2009 |
20090270381 | Non-steroidal progesterone receptor modulators - The present invention relates to non-steroidal progesterone receptor modulators of the general formula I, | 10-29-2009 |
20090270382 | Soluble epoxide hydrolase inhibitors - Disclosed are amide, thioamide, urea and thiourea compounds and compositions that inhibit soluble epoxide hydrolase (sEH), methods for preparing the compounds and compositions, and methods for treating patients with such compounds and compositions. The compounds, compositions, and methods are useful for treating a variety of sEH mediated diseases, including hypertensive, cardiovascular, inflammatory, and diabetic-related diseases. | 10-29-2009 |
20090270383 | Novel Oxabispidine Compounds And Their Use In The Treatment Of Cardiac Arrhythmias - There is provided compounds of formula (I), wherein R | 10-29-2009 |
20090275570 | SUBSTITUTED HETEROCYCLES AND THEIR USE AS CHK1, PDK1 AND PAK INHIBITORS - The invention relates to novel compounds of Formula (I) and to their pharmaceutical compositions and to their methods of use. These novel compounds possess CHK1 kinase inhibitory activity, PDK1 inhibitory activity and Pak kinase inhibitory activity and are accordingly useful in the treatment and/or prophylaxis of cancer. | 11-05-2009 |
20090275571 | MORPHOLINYL AND PYRROLIDINYL ANALOGS - The present invention relates to morpholinyl, and pyrrolidinyl analogs, pharmaceutical compositions containing them, and their use as antagonists of urotensin II. | 11-05-2009 |
20090275572 | FAB I INHIBITORS - Compounds of the formula (I) are disclosed which are Fab I inhibitors and are useful in the treatment of bacterial infections. | 11-05-2009 |
20090275573 | Imidazolidinone Derivatives as 11B-HSD1 Inhibitors - Compounds of formula | 11-05-2009 |
20090275574 | NOVEL COMPOUNDS-300 - Compounds of Formula I, or pharmaceutically acceptable salts thereof: | 11-05-2009 |
20090281096 | CYCLOTHIOCARBAMATE DERIVATIVES AS PROGESTERONE RECEPTOR MODULATORS - Methods of using compounds which are progesterone receptor agonists for contraception and the treatment of progesterone-related maladies alone or in combination with an estrogen receptor agonist or progesterone receptor antagonist are provided. These compounds have the structure: | 11-12-2009 |
20090286774 | PURINONE DERIVATIVES AS HM74A AGONISTS - The present invention relates to purinone derivatives which are agonists of the HM74a receptor. Further provided are compositions and methods of using the compounds herein, and their pharmaceutically acceptable salts for the treatment of disease. | 11-19-2009 |
20090291947 | PROLINE ANALOGS AS LIGANDS FOR CANNABINOID RECEPTORS - The present invention relates to Proline Analog Compounds that are ligands for cannabinoid receptors, compositions comprising a Proline Analog Compound and a pharmaceutically-acceptable carrier, methods of making such Proline Analog Compounds, and methods for treating or preventing a Condition comprising administering an effective amount of a Proline Analog Compound to an animal in need thereof. | 11-26-2009 |
20090291948 | SULFONAMIDE PERI-SUBSTITUTED BICYCLICS FOR OCCLUSIVE ARTERY DISEASE - Acyl sulfonamide, peri-substituted, fused bicyclic ring compounds useful for the treatment or prophylaxis of a prostaglandin-mediated disease or condition are disclosed. The compounds are of the general formula | 11-26-2009 |
20090298817 | ANTI-AMNESIC COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS COMPRISING THEM - The present invention relates to the use of at least one compound of formula (I) as follows: | 12-03-2009 |
20090298818 | PHARMACEUTICAL COMPOUNDS - The invention provides the use of a compound for the manufacture of a medicament for the treatment of pain, wherein the compound is a compound of the formula (VI): | 12-03-2009 |
20090298819 | Compositions, Synthesis, And Methods Of Using Piperazine Based Antipsychotic Agents - The present invention provides novel piperazine derivatives which can be advantageously used for treating schizophrenia and related psychoses such as acute manic, bipolar disorder, autistic disorder and depression. | 12-03-2009 |
20090298820 | 3-SUBSTITUTED-1H-PYRROLO[2,3-B]PYRIDINE AND 3-SUBSTITUTED-1H-PYRROLO[3,2-B]PYRIDINE COMPOUNDS, THEIR USE AS MTOR KINASE AND PI3 KINASE INHIBITORS, AND THEIR SYNTHESES - The invention relates to 3-substituted-1H-pyrrolo[2,3-b]pyridine, and 3-substituted-1H-pyrrolo[3,2-b]pyridine compounds of the Formula 1: | 12-03-2009 |
20090306064 | Substituted Piperidines as Renin Inhibitors - Compounds of the general formula (I) in which the meanings of the substituents R | 12-10-2009 |
20090306065 | AEROSOL FORMULATION FOR INHALATION CONTAINING AN ANTICHOLINERGIC AGENT - The invention relates to specific aqueous aerosol formulations that are devoid of propellant, containing one or more anticholinergic agents of formula (1), in which X represents an anion, and containing at least one pharmacologically compatible organic acid and optionally additional pharmacologically compatible adjuvants and/or complexing agents. The cation of formula (1′) is contained in the preparation at a concentration of between 83 and 94.5 mg per 100 ml of medicament preparation. | 12-10-2009 |
20090306066 | PEPTIDE DEFORMYLASE INHIBITORS - The present invention is directed to certain {2-(alkyl)-3-[2-(5-fluoro-4-pyrimidinyl)hydrazino]-3-oxopropyl}hydroxyformamide derivatives, compositions containing them, the use of such compounds in the inhibition of bacterial peptide deformylase (PDF) activity, and in the treatment of bacterial infections. Specifically, the invention is directed to compounds of formula (I): | 12-10-2009 |
20090306067 | 2, 4-DIAMINOPYRIMIDIDE DERIVATES AND THEIR USE FOR THE TREATMENT OF CANCER - The present invention encompasses compounds of general formula (1) wherein Q and R | 12-10-2009 |
20090306068 | NOVEL ENANTIOMERIC PURE BETA AGONISTS, MANUFACTURING AND USE AS A MEDICAMENTS THEREOF - The present invention relates to enantiomerically pure compounds of formula 1 | 12-10-2009 |
20090306069 | AZOLIDINONE-VINYL FUSED-BENZENE DERIVATIVES - The present invention is related to azolidinedione-vinyl fused-benzene derivatives of formula (I) for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, graft rejection or lung injuries. | 12-10-2009 |
20090312312 | Heterobicyclic Metalloprotease Inhibitors - The present invention relates generally to amide group containing pharmaceutical agents, and in particular, to amide containing heterobicyclic metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of heterobicyclic MMP-13 inhibiting and MMP-3 inhibiting compounds, that exhibit an increased potency in relation to currently known MMP-13 and MMP-3 inhibitors. | 12-17-2009 |
20090312313 | COMPOUND HAVING TGFBETA INHIBITORY ACTIVITY AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME - The present invention provides compounds represented by formula (I) and pharmaceutically acceptable salts and solvates thereof: | 12-17-2009 |
20090312314 | HETEROAROMATIC MONOAMIDES AS OREXININ RECEPTOR ANTAGONISTS - The present invention is concerned with novel sulfonamides of formula | 12-17-2009 |
20090318431 | BENZOXAZINONE AND BENZOXAZEPINONE OXAZOLIDINONES AS ANTIBACTERIAL AGENTS - The present invention provides a compound of formula (I) wherein X is a structure of the following formula (i), (ii) (iii), or iv G is O, or S; U is —(CR | 12-24-2009 |
20090318432 | Nitrate esters of aminoalcohols - The application relates to novel nitrate ester derivatives of substituted aminoalcohols of the general formula (I), wherein R | 12-24-2009 |
20090325947 | NITRATE ESTERS OF PIPERIDINES - The application relates to novel nitrate ester derivatives of substituted piperidines of the general formula (I), wherein R | 12-31-2009 |
20090325948 | INHIBITORS OF UNDECAPRENYL PYROPHOSPHATE SYNTHASE - The present invention relates to compounds that are selective and/or potent inhibitors of UPPS. In addition to compounds which inhibit UPPS, the invention also provides pharmaceutical compositions comprising these compounds and methods of using these compounds for treating bacterial disease, such as bacterial infection. | 12-31-2009 |
20090325949 | 5 HT RECEPTOR MEDIATED NEUROGENESIS - The instant disclosure describes methods for treating diseases and conditions of the central and peripheral nervous system by stimulating or increasing neurogenesis. The disclosure includes compositions and methods based on use of a 5HTR agent, optionally in combination with one or more other neurogenic agents, to stimulate or activate the formation of new nerve cells. | 12-31-2009 |
20090325950 | Benzoxazine derivatives and uses thereof - The present invention provides a compound of the formula: | 12-31-2009 |
20100004233 | NOVEL COUMARIN DERIVATIVE HAVING ANTITUMOR ACTIVITY - The present invention provides a compound represented by general formula (1) below or a pharmaceutically acceptable salt thereof: | 01-07-2010 |
20100009983 | 5 HT RECEPTOR MEDIATED NEUROGENESIS - The instant disclosure describes methods for treating diseases and conditions of the central and peripheral nervous system by stimulating or increasing neurogenesis. The disclosure includes compositions and methods based on use of a 5HTR agent, in combination with one or more other neurogenic agents, or anti-astrogenic agent, to stimulate or activate the formation of new nerve cells. | 01-14-2010 |
20100009984 | AEROSOL FORMULATIONS FOR THE INHALATION OF BETA-AGONISTS - A pharmaceutical formulation, comprising:
| 01-14-2010 |
20100016296 | HETEROARYL COMPOUNDS AND USES THEREOF - The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same. | 01-21-2010 |
20100016297 | ALKYL-SUBSTITUTED 3' COMPOUNDS HAVING 5-HT6 RECEPTOR AFFINITY - The present disclosure provides compounds having affinity for the 5-HT | 01-21-2010 |
20100022525 | Arginine Derivatives with NP-I Antagonistic Activity - The present invention is a compound of formula (I) or formula (II) which are suitable as NP-1 antagonists. | 01-28-2010 |
20100029628 | 2,4,5-Substituted Piperidines as Renin Inhibitors - SP-P2140 ATE-132—Abstract Novel substituted piperidines of the general formula (I) and (II) with the substituent definitions as explained in detail in the description are described. The compounds are suitable in particular as renin inhibitors and are highly potent. | 02-04-2010 |
20100029629 | ACYCLIC COMPOUNDS HAVING 5-HT6 RECEPTOR AFFINITY - The present disclosure provides compounds having affinity for the 5-HT | 02-04-2010 |
20100029630 | REVERSE-TURN MIMETICS AND METHOD RELATING THERETO - Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetic structures have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis. | 02-04-2010 |
20100029631 | CARBOXYLIC ACID COMPOUNDS AND MEDICINAL COMPOSITIONS CONTAINING THE SAME AS THE ACTIVE INGREDIENT - A compound represented by formula (I) | 02-04-2010 |
20100029632 | BROADSPECTRUM 2-AMINO-BENZOXAZOLE SULFONAMIDE HIV PROTEASE INHIBITORS - The present invention concerns the compounds having the formula | 02-04-2010 |
20100029633 | IMIDAZO[1,2-A]PYRIDINE COMPOUNDS AS RECEPTOR TYROSINE KINASE INHIBITORS - Compounds of Formula I: in which A, B, R | 02-04-2010 |
20100035871 | BENZOXAZINE DERIVATIVES AND USES THEREOF - Compounds of formula (I) or pharmaceutically acceptable salts thereof are provided, wherein each of Z, X, R | 02-11-2010 |
20100035872 | PDE10 INHIBITORS AND RELATED COMPOSITIONS AND METHODS - Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette's syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. Pharmaceutically acceptable salts, stereoisomers, solvates and prodrugs of the compounds are also provided. Also disclosed are compositions containing a compound in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same. | 02-11-2010 |
20100048547 | PI 3-KINASE INHIBITORS AND METHODS OF THEIR USE - Phosphatidylinositol (PI) 3-kinase inhibitor compounds, their pharmaceutically acceptable salts, and prodrugs thereof; compositions of the new compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier; and uses of the new compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of diseases characterized by the abnormal activity of growth factors, protein serine/threonine kinases, and phospholipid kinases, including proliferative diseases, inflammatory and obstructive airways diseases, allergic conditions, autoimmune and cardiovascular diseases. | 02-25-2010 |
20100056507 | PHENYL DERIVATIVES AND THEIR USE AS A MEDICAMENT - The present invention relates to new phenylic derivatives exhibiting a good affinity for certain sub-types of cannabinoid receptors, in particular the CB2 receptors. These derivatives are of particular interest in a method for treating pathological conditions and diseases in which one or more cannabinoid receptors are involved. The invention also relates to pharmaceutical compositions containing said new phenylic derivatives and to methods for the preparation and use thereof. | 03-04-2010 |
20100056508 | AMINE DERIVATIVES AND THEIR USE IN BETA-2-ADRENORECEPTOR MEDIATED DISEASES - The present invention provides compounds of formula (I), wherein k, Ar, R | 03-04-2010 |
20100056509 | HETEROARYL SULFONAMIDES AND CCR2 - Compounds are provided that act as potent antagonists of the CCR2 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, and as controls in assays for the identification of CCR2 antagonists. | 03-04-2010 |
20100063040 | Sulfonamide Derivative Having PGD2 Receptor Antagonistic Activity - The present invention provides an sulfonamide derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further a therapeutic agent for treating allergic diseases. | 03-11-2010 |
20100063041 | NOVEL PHENYLPROPIONIC ACID DERIVATIVES AS PEROXISOME PROLIFERATOR-ACTIVATED GAMMA RECEPTOR MODULATORS, METHOD OF THE SAME, AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME - The present invention provides a novel phenylpropionic acid derivative and a PPAR-γ modulator comprising the same as an active ingredient. The phenylpropionic acid derivative of the present invention has modulatory action on function of PPAR-γ and then exhibits hypoglycemic, hypolipidemic and insulin resistance-reducing effects on PPAR-mediated diseases or disorders. Therefore, the present invention is prophylactically or therapeutically effective for diabetes and metabolic diseases. | 03-11-2010 |
20100063042 | 5-SUBSTITUTED BENZOXAZINES - The present invention is concerned with 5-substituted benzoxazine derivatives of formula (I) | 03-11-2010 |
20100069378 | SUBSTITUTED INDANYL SULFONAMIDE COMPOUNDS, THEIR PREPARATION AND USE AS MEDICAMENTS - The present invention refers to new indanyl sulphonamide compounds with general formula (I), as well as to their preparation procedure, their application as medicine and the pharmaceuticals composition which they are made up of. The new compounds of formula (I) show affinity for 5-HT | 03-18-2010 |
20100069379 | Bicyclic androgen and progesterone receptor modulator compounds and methods - The present invention is directed to compounds, pharmaceutical compositions, and methods for modulating processes mediated by AR and PR. More particularly, the invention relates to nonsteroidal compounds and compositions that are high affinity, high specificity agonists, partial agonists (i.e., partial activators and/or tissue-specific activators) and antagonists for AR and PR. Also provided are methods of making such compounds and pharmaceutical compositions, as well as critical intermediates used in their synthesis. | 03-18-2010 |
20100081655 | REVERSE-TURN MIMETICS AND METHOD RELATING THERETO - Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetic structures have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis. | 04-01-2010 |
20100087427 | PYRROLIDINE DERIVATIVES FOR THE TREATMENT OF A DISEASE DEPENDING ON THE ACTIVITY OF RENIN - Novel 3-mono-, 3,4-di- and 3,4,4,-tri-substituted pyrrolidine 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 inappropriate 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 inappropriate activity of renin; the use of a compound of that class in the treatment of a disease that depends on inappropriate activity of renin; pharmaceutical formulations comprising a said substituted pyrrolidine compound, and/or a method of treatment comprising administering a said substituted pyrrolidine compound, a method for the manufacture of said substituted pyrrolidine compounds, and novel intermediates and partial steps for their synthesis are described. The substituted pyrrolidine compounds are especially of the formula I | 04-08-2010 |
20100087428 | Novel Potassium Channel Blockers - The present invention provides a compound of formula (I) | 04-08-2010 |
20100093717 | TRIAZOLE COMPOUNDS THAT MODULATE HSP90 ACTIVITY - The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of treating or inhibiting angiogenesis in a subject in need thereof and methods for blocking, occluding, or otherwise disrupting blood flow in neo vasculature, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound. | 04-15-2010 |
20100099670 | Benzoquinazoline derivatives - A compound of formula (I) or a pharmaceutically acceptable salt or prodrug ester thereof: | 04-22-2010 |
20100105670 | FUNGICIDAL MIXTURES - Disclosed is a fungicidal mixture comprising (a) at least one compound selected from the compounds of Formula 1 N-oxides, and salts thereof, | 04-29-2010 |
20100120758 | REVERSE-TURN MIMETICS AND METHOD RELATING THERETO - Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetic structures have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis. | 05-13-2010 |
20100120759 | AZADECALIN GLUCOCORTICOID RECEPTOR MODULATORS - The present invention provides a novel class of azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators. | 05-13-2010 |
20100125069 | Methods of Treating or Preventing Autoimmune Diseases with 2,4-Pyrimidinediamine Compounds - The present invention provides methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds, as well as methods of treating, preventing or ameliorating symptoms associated with such diseases. Specific examples of autoimmune diseases that can be treated or prevented with the compounds include rheumatoid arthritis and/or its associated symptoms, systemic lups erythematosis and/or its associated symptoms and multiple sclerosis and/or its associated symptoms. | 05-20-2010 |
20100137297 | SPIROINDALONES - The present invention relates to spiroindalone compounds useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions. | 06-03-2010 |
20100152175 | Pyridine Derivatives and Their Use in The Treatment of Psychotic Disorders - There are provided according to the invention novel compounds of formula (I) or a pharmaceutically acceptable salt thereof: | 06-17-2010 |
20100152176 | Modulators of Muscarinic Receptors - The present invention relates to modulators of muscarinic receptors. The present invention also provides compositions comprising such modulators, and methods therewith for treating muscarinic receptor mediated diseases. | 06-17-2010 |
20100152177 | COMPOUNDS HAVING 5-HT6 RECEPTOR AFFINITY - The present disclosure provides compounds having affinity for the 5HT6 receptor which are of the formula (I): | 06-17-2010 |
20100160304 | AROMATIC SULFONE COMPOUND AS ALDOSTERONE RECEPTOR MODULATOR - The present invention provides a compound represented by the following formula (I): | 06-24-2010 |
20100160305 | 3, 4, 5 - Substituted Piperidine Compounds - 3,4,5-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 3,4,5-substituted piperidine compound, and/or a method of treatment comprising administering a 3,4,5-substituted piperidine compound, a method for the manufacture of a 3,4,5-substituted piperidine compound, and novel intermediates and partial steps for its synthesis. | 06-24-2010 |
20100160306 | Acylated Piperidine Derivatives as Melanocortin-4 Receptor Agonists - Certain novel 4 alkyl substituted N acylated piperidine derivatives are ligands of the human melanocortin receptor(s) and, in particular, are selective ligands of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of MC-4R, such as obesity, diabetes, nicotine addiction, alcoholism, sexual dysfunction, including erectile dysfunction and female sexual dysfunction. | 06-24-2010 |
20100160307 | METHOD FOR CONTROLLING PARTICULAR INSECT PESTS BY APPLYING ANTHRANILAMIDE COMPOUNDS - This invention pertains to a method for controlling lepidopteran, homopteran, hemipteran, thysanopteran and coleopteran insect pests comprising contacting the insects or their environment with an arthropodicidally effective amount of a compound of Formula I, its N-oxide or an agriculturally suitable salt thereof | 06-24-2010 |
20100168093 | SUBSTITUTED 3-AMINO-4 -HYDROXY PYRROLIDINES COMPOUNDS, THEIR PREPARATION AND USE AS MEDICAMENTS - The present invention relates to substituted pyrrolidine compounds of general formula (I), methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animal. | 07-01-2010 |
20100168094 | MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR - 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 diseases using such CFTR modulators. | 07-01-2010 |
20100168095 | MULTI-CYCLIC CINNAMIDE DERIVATIVES - The present invention provides a compound represented by the formula (I): | 07-01-2010 |
20100173901 | Substituted Heterocyclic Compounds - The present invention relates to substituted heterocyclic compounds of Formula I: | 07-08-2010 |
20100173902 | Bicyclic amide derivatives for enhancing glutamatergic synaptic responses - This invention relates to compounds, pharmaceutical compositions and methods for use in the prevention and treatment of cerebral insufficiency, including enhancement of receptor functioning in synapses in brain networks responsible for basic and higher order behaviors. These brain networks, which are involved in cognitive abilities related to memory impairment, such as is observed in a variety of dementias, in imbalances in neuronal activity between different brain regions, as is suggested in disorders such as Parkinson's disease, schizophrenia, sleep apneas, attention deficit hyperactivity disorder and affective or mood disorders, and in disorders wherein a deficiency in neurotrophic factors is implicated, as well as conditions such as stroke-induced central sleep apnea, obstructive sleep apnea, congenital hypoventilation syndrome, obesity hypoventilation syndrome, sudden infant death syndrome, Rett syndrome, spinal cord injury, traumatic brain injury, Cheney-Stokes respiration, Ondines curse, Prader-Willi's syndrome and drowning. In a particular aspect, the invention relates to bicyclic amide compounds useful for treatment of such conditions, and methods of using these compounds for such treatment. | 07-08-2010 |
20100173903 | Bicyclic amide derivatives for the treatmet of respiratory disorders - This invention relates to compounds, pharmaceutical compositions and methods for use in the prevention and treatment of disorders of respiration such as overdose of an alcohol, an opiate, an opioid, a barbiturate, an anesthetic, or a nerve toxin. In a particular aspect, the invention relates to bicyclic amide compounds useful for treatment of such conditions, and methods of using these compounds for such treatment. | 07-08-2010 |
20100190782 | COMPOUNDS AND METHODS OF USE - In one aspect, the present invention provides for a compound of Formula I | 07-29-2010 |
20100190783 | TRIAZOLONE DERIVATIVES - A Compound represented by the following general formula (1): | 07-29-2010 |
20100197678 | Glucocorticoid Mimetics, Methods of Making Them, Pharmaceutical Compositions and Uses Thereof - Compounds of Formula (IA) | 08-05-2010 |
20100197679 | COMPOUNDS - Bicyclic nitrogen containing compounds and their use as antibacterials | 08-05-2010 |
20100204218 | FUSED BICYCLIC COMPOUND - The present invention provides a novel fused bicyclic compound having an affinity to a receptor of mineral corticoid (MR), shown by the formula [I]: | 08-12-2010 |
20100210635 | RENIN INHIBITORS - Compounds, pharmaceutical compositions, kits and methods are provided for use with Renin that comprise a compound selected from the group consisting of: wherein the variables are as defined herein. | 08-19-2010 |
20100210636 | BENZOXAZINONE DERIVATIVE | 08-19-2010 |
20100216782 | HYDROXYBENZAMIDE DERIVATIVES AND THEIR USE AS INHIBITORS OF HSP90 - This invention provides methods for treating, alleviating or reducing the incidence of a disease or condition comprising or arising from abnormal cell growth in a mammal, which comprise administering to the mammal a compound, salt, hydrate, tautomer or N-oxide according to formula (I): | 08-26-2010 |
20100216783 | COMPOSITIONS, SYNTHESIS, AND METHODS OF UTILIZING ARYLPIPERAZINE DERIVATIVES - The present invention provides arylpiperazine derivatives which can be advantageously used for treating schizophrenia and related psychoses such as acute manic, bipolar disorder, autistic disorder and depression. | 08-26-2010 |
20100216784 | Compounds for Inhibiting Beta-Amyloid Production and Methods of Identifying the Compounds - Provided are compounds useful for treating diseases associated with a cerebral accumulation of Alzheimer's amyloid, such as Alzheimer's disease. Also provided are methods for screening for such compounds, by measuring capacitative calcium entry in cells which optionally overexpress APP or a fragment thereof. Also provided are methods of treating or reducing the risk of developing β-amyloid production, β-amyloid deposition, β-amyloid neurotoxicity (including abnormal hyperphosphorylation of tau) and microgliosis associated with cerebral accumulation of Alzheimer's amyloid by administering therapeutically effective amounts of compounds which decrease β-amyloid production and capacitative calcium entry in cells. Further provided are methods for diagnosing diseases associated with cerebral accumulation of Alzheimer's amyloid in animals or humans by administering diagnostically effective amounts of compounds which inhibit capacitative calcium entry in cells. | 08-26-2010 |
20100222335 | Process For The Preparation Of N,N'-Disubstituted Oxabispidines - There is provided a process for the preparation of a sulfonic acid salt of formula I, or a solvate thereof, which process comprises hydrogenating a sulfonic acid salt of formula II, or a solvate thereof; in the presence of a solvent system consisting essentially of water, a C | 09-02-2010 |
20100222336 | SINGLE ENANTIOMER BETA-AGONISTS, METHODS FOR THE PRODUCTION THEREOF AND THE USE THEREOF AS MEDICATION - The present invention relates to single enantiomer compounds of formula (1), where the moieties n, A, R | 09-02-2010 |
20100227857 | 3,4-DIHYDRO-2H-BENZO[1,4]OXAZINE AND THIAZINE DERIVATIVES AS CETP INHIBITORS - The invention is directed to compounds of Formula (I) described herein useful as CETP inhibitors, compositions containing them, and methods of using them. | 09-09-2010 |
20100234368 | CONDENSED RING COMPOUND AND USE THEREOF - The present invention relates to a compound of formula (I) | 09-16-2010 |
20100240644 | MORPHOLINE DERIVATIVE - The present invention provides a morpholine derivative of the formula [I]; | 09-23-2010 |
20100249122 | Kinase Inhibitors for Preventing or Treating Pathogen Infection and Method of Use Thereof - The present invention provides compositions and methods of use thereof to prevent and/or treat pathogenic infection. In particular, the present invention provides the use of kinase inhibitors to inhibit kinases that involve in pathogen-host cell interactions that are associated with or cause pathogenic infections, therefore, to effectively prevent and/or treat pathogenic infections with far less likely to engender resistance as compared to conventional antibiotics and anti-viral drugs. The present invention further provides the use of kinase inhibitors for the treatment of acute pathogenic infections for a short period of time to avoid toxicities that may caused by long term use of these kinase inhibitors. | 09-30-2010 |
20100249123 | NOVEL BENZAMIDE DERIVATIVES AS MODULATORS OF THE FOLLICLE STIMULATING HORMONE - The present invention provides new compounds of formula I, wherein Q, R | 09-30-2010 |
20100249124 | 2,3-DIARYL- OR HETEROARYL-SUBSTITUTED 1,1,1-TRIFLUORO-2-HYDROXYPROPYL COMPOUNDS - The present invention relates to compounds of formula I | 09-30-2010 |
20100261719 | CHEMICAL COMPOUNDS - In one aspect, the present invention relates to compounds of Formula (I) and to pharmaceutically acceptable salts thereof, wherein: n is 1 to 4; and R | 10-14-2010 |
20100267712 | ISOINDOLINE COMPOUNDS FOR THE TREATMENT OF SPINAL MUSCULAR ATROPHY AND OTHER USES - Disclosed is a compound of Formula (I) in which W and R | 10-21-2010 |
20100267713 | 4,4-DISUBSTITUTED PIPERIDINES - The application relates to 4,4-disubstituted piperidines of the general formula (I) and their salts, preferably their pharmaceutically acceptable salts, in which R | 10-21-2010 |
20100267714 | MIF MODULATORS - The invention provides novel heterocyclic compounds, pharmaceutical compositions and methods of treatment that modulate levels of MIF expression and treat disorders associated with high or low levels of MIF expression. | 10-21-2010 |
20100267715 | Polymorph Form II of Tanaproget - Tanaproget polymorph Form II, processes for preparing tanaproget polymorph Form II, pharmaceutical compositions including tanaproget polymorph Form II, micronized tanaproget polymorph Form II, and processes for converting Form II to tanaproget Form I are provided. Also provided are methods of contraception, hormone replacement therapy, stimulation of food intake and treating or preventing uterine myometrial fibroids, benign prostatic hypertrophy, benign and malignant neoplastic disease, dysfunctional bleeding, uterine leiomyomata, endometriosis, polycystic ovary syndrome, or carcinomas and adenocarcinomas comprising administering polymorph Form II to a mammalian subject. | 10-21-2010 |
20100273788 | FUSED HETEROCYCLIC DERIVATIVE AND USE THEREOF - The present invention provides a fused heterocyclic derivative having a potent kinase inhibitory activity and use thereof. | 10-28-2010 |
20100280023 | THIAZOLE DERIVATIVES - It is intended to provide an adenosine A | 11-04-2010 |
20100280024 | RENIN INHIBITORS - The present invention relates to renin inhibitors of formula (I), their pharmaceutically acceptable salts and pharmaceutical compositions containing them. The present invention also relates to a process of preparing compounds of general formula (I), their tautomeric forms, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and novel intermediates involved in their synthesis. | 11-04-2010 |
20100280025 | EQUILIBRATIVE NUCLEOSIDE TRANSPORTER ENT1 INHIBITORS - The present invention is related to novel compounds of formula (I) having equilibrative nucleoside transporter ENT1 inhibiting properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment of diseases linked to the inhibition of ENT1 receptors in animals, in particular humans. | 11-04-2010 |
20100286135 | HETEROCYCLIC AMIDE COMPOUNDS AS PROTEIN KINASE INHIBITORS - The present invention relates to novel heterocyclic amide compounds of Formula I: as disclosed herein or a pharmaceutically acceptable salt, solvate, ester, prodrug or stereoisomer thereof. Also disclosed are compositions comprising said compounds, and methods for using said compounds for treating or preventing a proliferative disease, an anti-proliferative disorder, inflammation, arthritis, a neurological or neurodegenerative disease, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral disease or a fungal disease. | 11-11-2010 |
20100286136 | DIHYDRONAPHTHYRIDINYL AND RELATED COMPOUNDS FOR USE IN TREATING OPHTHALMOLOGICAL DISORDERS - The invention provides methods of using dihydronaphthyridinyl and related compounds to treat opthalmological disorders, such as, wet age-related macular degeneration, diabetic retinopathy, and high myopia. Pharmaceutical compositions and methods of synthesizing the dihydronaphthyridinyl and related compounds are provided. | 11-11-2010 |
20100286137 | Method of Treating Conditions Involving PPAR-Receptors with Indole Compounds - Indole compounds corresponding to the formula (I): | 11-11-2010 |
20100292228 | SUBSTITUTED OXA-DIAZA-SPIRO-[5.5]-UNDECANONE DERIVATIVES AND THEIR USE AS NEUROKININ ANTAGONISTS - This invention concerns substituted oxa-diaza-spiro-[5.5]-undecanone derivatives having neurokinin antagonistic activity, in particular an NK | 11-18-2010 |
20100292229 | TRYPHOSTIN-ANALOGS FOR THE TREATMENT OF CELL PROLIFERATIVE DISEASES - The present invention concerns compounds and their use to treat cell proliferative diseases such as cancer. In general aspects, compounds of the present invention are tyrphostin-like in structure. Compounds of the present invention, in certain embodiments, display significant potency by causing, for example, inhibition of Stat3 activation, reduction in c-myc protein levels and/or induction of apoptosis in tumor cells. In general aspects, compounds of the present invention induce one or more of these activities at nanomolar concentrations and typically function through a unique mechanism involving the induction of stress granules that bind specific signaling molecules and prevent them from participating in signal transduction and oncogenesis. | 11-18-2010 |
20100298310 | Thiazole Derivatives as Kinase Inhibitors - A series of thiazole 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. | 11-25-2010 |
20100298311 | TETRAHYDRONAPHTHALENE DERIVATES, PROCESS FOR PREPARING THEM AND THEIR USE AS ANTIINFLAMMATORY AGENTS - The invention relates to multiply substituted tetrahydronaphthalene derivatives of the formula (Ia) | 11-25-2010 |
20100305115 | INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION - The present invention relates to compounds of formula (I) wherein c, X, Y, R | 12-02-2010 |
20100311737 | PYRIMIDO [4,5-B] -OXAZINES FOR USE AS DGAT INHIBITORS - Compounds of formula (I) or salts thereof, wherein A, and R | 12-09-2010 |
20100317657 | 1H-IMIDAZO[4,5-c]QUINOLINONE DERIVATIVES - The invention relates to the use of 1H-imidazo[4,5-c]quinolinone derivatives 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 derivatives 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 derivatives to a warm-blooded animal, especially a human; pharmaceutical preparations comprising an 1H-imidazo[4,5-c]quinolinone derivative, especially for the treatment of a protein and/or lipid kinase dependent disease; novel 1H-imidazo[4,5-c]quinolinone derivatives; and a process for the preparation of the novel 1H-imidazo[4,5-c]quinolinone derivatives. | 12-16-2010 |
20100324034 | Methods of Using SAHA for Treating HIV Infection - The present invention relates to pharmaceutical preparations and methods for treating individuals infected with the human immunodeficiency virus (HIV). The pharmaceutical preparations comprise SAHA and another anti-viral agent. The invention also relates to methods for treating HIV infected patients, particularly patients with persistent, latent HIV infection of CD4 | 12-23-2010 |
20100324035 | Carboxamide Compounds and Their Use - Chemokine receptor antagonists, in particular, compounds of Formula (I-A) that act as antagonists of the chemokine CCR2 receptor, including pharmaceutical compositions and uses thereof to treat or prevent diseases associated with monocyte accumulation, lymphocyte accumulation or leukocyte accumulation are described herein. | 12-23-2010 |
20100324036 | 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 cachexia induced by e.g. cancer, chronic kidney disease (CKD) or chronic heart failure (CHF), muscle wasting, anorexia induced by e.g. chemotherapy or radiotherapy, anorexia nervosa, amyotrophic lateral sclerosis (ALS), pain, neuropathic pain, anxiety and depression. | 12-23-2010 |
20100331321 | Bis-(Sulfonylamino) derivatives for use in therapy - The invention provides compounds of formula (I) wherein R | 12-30-2010 |
20100331322 | SUBSTITUTED PIPERIDINES AS RENIN INHIBITORS - The present invention relates to compounds of the general formula (I) and the salts thereof, preferably the pharmaceutically acceptable salts thereof; in which R has the meaning explained in the description, a process for their preparation and the use of these compounds as medicines, especially as renin inhibitors. | 12-30-2010 |
20100331323 | SYNTHESIS AND REGIOSELECTIVE SUBSTITUTION OF 6-HALO- AND 6-ALKOXY NICOTINE DERIVATIVES - The present invention provides active compounds for modulating nicotinic acetylcholine receptors and methods of making the same. The methods of preparing the active compounds utilize different intermediate compounds. | 12-30-2010 |
20110003803 | COMPOSITIONS AND METHODS FOR TREATING OPHTHALMIC, OTIC, OR NASAL INFECTIONS - The present invention relates to methods for treating an ophthalmic, otic, or nasal infection comprising treating the infected tissue with a composition comprising finafloxacin or a finafloxacin derivative. The present invention also relates to antimicrobial compositions comprising finafloxacin or a finafloxacin derivative. The compositions are suitable for the treatment of ophthalmic, otic, or nasal infections. | 01-06-2011 |
20110009397 | TRIAZONE COMPOUNDS THAT MODULATE HSP90 ACTIVITY - The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound. | 01-13-2011 |
20110009398 | p27 Protein Inducer - The present invention provides a p27 protein inducing agent comprising a compound represented by general formula (11) below or pharmaceutically acceptable salt thereof as an active ingredient: | 01-13-2011 |
20110009399 | ORGANIC COMPOUNDS - The application relates to trisubstituted piperidines of the general formula (I) and their salts, preferably their pharmaceutically acceptable salts, in which R | 01-13-2011 |
20110009400 | BICYCLIC DERIVATIVES OF AZABICYCLIC CARBOXAMIDES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF - The disclosure relates to compounds of formula (I): | 01-13-2011 |
20110009401 | 2-AZA-BICYCLO[2.2.1]HEPTANE DERIVATIVES - The invention relates to novel 2-aza-bicyclo[2.2.1]heptane derivatives of formula (I), | 01-13-2011 |
20110015189 | METHODS OF MAKING EFAVIRENZ AND INTERMEDIATES THEREOF - The present invention provides a process for the preparation of Efavirenz. A compound of Formula 1 may be prepared by a process comprising cyclizing, in the presence of a first base, a compound of Formula 5 with a haloformate of Formula 6. Other processes are also provided as well as novel compounds prepared by and used in such processes. | 01-20-2011 |
20110015190 | GAMMA SECRETASE MODULATORS - This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (I) wherein R | 01-20-2011 |
20110021513 | MODULATORS OF INTERLEUKIN-1 RECEPTOR-ASSOCIATED KINASE - The present invention relates to modulators of IRAK kinase and provides compositions comprising such modulators, as well as methods therewith for treating conditions or diseases mediated by or associated with IRAK kinase. | 01-27-2011 |
20110021514 | AMIDE DERIVATIVES AS ION-CHANNEL LIGANDS AND PHARMACEUTICAL COMPOSITIONS AND METHODS OF USING THE SAME - Compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others. | 01-27-2011 |
20110021515 | DIHYROFUROPYRMINDINE COMPOUNDS - The present invention provides mTOR inhibitors of the formula | 01-27-2011 |
20110021516 | MONOCYCLIC CGRP RECEPTOR ANTAGONISTS - The present invention is directed to compounds of the formula (I): (wherein variables A | 01-27-2011 |
20110028462 | Niacin Receptor Agonists, compositions Containing Such Compounds and Methods of Treatment - A method of treating atherosclerosis and related conditions using compounds of formula I: as well as pharmaceutically acceptable salts and solvates is disclosed. The compounds are useful for treating dyslipidemias, and in particular, reducing serum LDL, VLDL and triglycerides, and raising HDL levels. | 02-03-2011 |
20110028463 | AMIDE COMPOUNDS - [Problems] To provide a compound that is useful as an agent for treating chronic renal insufficiency or an agent for treating diabetic nephropathy.
| 02-03-2011 |
20110028464 | INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION - Compounds of formula I: wherein c, R | 02-03-2011 |
20110028465 | AMIDE DERIVATIVES AS ION-CHANNEL LIGANDS AND PHARMACEUTICAL COMPOSITIONS AND METHODS OF USING THE SAME - Compounds are disclosed that have a formula represented by the following: | 02-03-2011 |
20110028466 | NITROIMIDAZOOXAZINE AND NITROIMIDAZOOXAZOLE ANALOGUES AND THEIR USES - The current invention pertains to nitroimidazooxazine and nitroimidazooxazole analogues, their methods of preparation, and uses of the compounds as treatment for | 02-03-2011 |
20110028467 | HETEROCYCLIC DERIVATIVES - The present invention relates to heterocyclic derivatives, and more particularly, to novel heterocyclic derivatives useful for the preparation of medicaments for treating diseases related to uric acid. | 02-03-2011 |
20110028468 | COMPOUNDS HAVING NPY Y5 RECEPTOR ANTAGONISTIC ACTIVITY - This invention provides a compound of the formula (I): | 02-03-2011 |
20110034451 | TRIAZOLOPYRIDAZINES AS PAR1 INHIBITORS, PRODUCTION THEREOF, AND USE AS MEDICAMENTS - The invention relates to novel compounds of formula I | 02-10-2011 |
20110034452 | TRIAZOLIUM SALTS AS PAR1 INHIBITORS, PRODUCTION THEREOF, AND USE AS MEDICAMENTS - The invention relates to novel compounds of formula I | 02-10-2011 |
20110039838 | PYRROLOTRIAZINE COMPOUNDS AS KINASE INHIBITORS - The present invention provides compounds of formula I | 02-17-2011 |
20110039839 | Cyanopyrroles - This invention provides a progesterone receptor antagonist of formula 1 having the structure | 02-17-2011 |
20110039840 | SPIROCYCLIC DERIVATIVES AS HISTONE DEACETYLASE INHIBITORS - This invention is related to new histone deacetylase inhibitors according to the general formula (I) wherein: the dotted line is an optional additional bond; n is zero or an integer from 1 to 4; R | 02-17-2011 |
20110046125 | METHOD FOR TREATING INFECTIONS - The present invention relates to compounds for treating or preventing infection that inhibit the activity of Hsp90. | 02-24-2011 |
20110046126 | Use of 2,4-Pyrimidinediamines For the Treatment of Atherosclerosis - Novel methods and compositions for the prevention and treatment of all forms of atherosclerosis with 2,4-pyrimidinediamine compounds are described. Also disclosed is the coating of prosthetic devices, such as stents, with the compounds of the invention for the prevention and/or treatment of restenosis. | 02-24-2011 |
20110053923 | CHEMICAL COMPOUNDS 610 - There is provided pyrimidinyl indole compounds of Formula (I), | 03-03-2011 |
20110053924 | SUBSTITUTED PIPERIDINES AS RENIN INHIBITORS - The present invention relates to compounds of the general formula (I) and the salts thereof, preferably the pharmaceutically acceptable salts thereof; in which R has the meaning explained in the description, a process for their preparation and the use of these compounds as medicines, especially as renin inhibitors. | 03-03-2011 |
20110053925 | Hydroxamate-Based Inhibitors of Deacetylases - The present teachings relate to compounds of Formula I: | 03-03-2011 |
20110053926 | New Pharmaceutically-Active Compounds for the Treatment of Respiratory Diseases - The present invention relates to the use of the compounds of general formula 1 | 03-03-2011 |
20110059957 | BENZENE OR THIOPHENE DERIVATIVE AND USE THEREOF AS VAP-1 INHIBITOR - The present invention provides a novel benzene derivative or thiophene derivative useful as a VAP-1 inhibitor, or a medicament for the prophylaxis or treatment of a VAP-1 associated disease and the like, namely, a compound represented by the formula (I): wherein each symbol is as defined in the present specification, or a pharmaceutically acceptable salt thereof. | 03-10-2011 |
20110065696 | IMIDAZOYL PYRIDINE COMPOUNDS AND SALTS THEREOF - A compound represented by the formula (I): | 03-17-2011 |
20110065697 | 2-OXY-BENZOXAZINONE DERIVATIVES FOR THE TREATMENT OF OBESITY - The use of a compound comprising formula (I): | 03-17-2011 |
20110071145 | Raf Modulators And Methods Of Use - The present invention relates to compounds of the Formula I, wherein G, A, X1, X2, X3, Z, E, Y, and X are defined herein. The compounds modulate protein kinase enzymatic activity to modulate cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Compounds of the invention inhibit, regulate and/or modulate kinases, particularly Raf. Methods of using and preparing the compounds, and pharmaceutical compositions thereof, to treat kinase-dependent diseases and conditions are also an aspect of the invention. | 03-24-2011 |
20110071146 | 17BetaHSD Type 5 Inhibitor - To provide a novel and excellent method for treating and/or preventing prostatic cancer, benign prostatic hyperplasia, acne, seborrhea, hirsutism, baldness, alopecia, precocious puberty, adrenal hypertrophy, polycystic ovary syndrome, breast cancer, lung cancer, endometriosis, leiomyoma and the like based on selective inhibitory activity against 17βHSD type 5. | 03-24-2011 |
20110077241 | HETEROARYL-SUBSTITUTED 1,3-DIHYDROINDOL-2-ONE DERIVATIVES AND MEDICAMENTS CONTAINING THEM - The present invention relates to novel 1,3-dihydroindol-2-one (oxindole) derivatives of the formula (I) in which A, R | 03-31-2011 |
20110077242 | DIAMINOPYRIMIDINES AS P2X3 AND P2X2/3 ANTAGONISTS - Compounds and methods for treating diseases mediated by a P2X | 03-31-2011 |
20110086849 | NOVEL BENZOXAZINE BENZIMIDAZOLE DERIVATIVE, A PHARMACEUTICAL COMPOSITION COMPRISING THE SAME, AND AUSE THEREOF - The present invention relates to a novel benzoxazine benzimidazole derivative of formula (1) as an antagonist against a vanilloid receptor-1, a pharmaceutical composition comprising the same as an active ingredient, and a use thereof. The benzoxazine benzimidazole derivative of the present invention may be useful for preventing or treating a disease associated with antagonistic activity of vanilloid receptor-1: | 04-14-2011 |
20110092495 | COMPOUNDS FOR THE TREATMENT OF MULTI-DRUG RESISTANT BACTERIAL INFECTIONS - The present invention relates to compounds that demonstrate antibacterial activity, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment of bacterial infections in warm-blooded animals such as humans. In particular this invention relates to compounds useful for the treatment of bacterial infections in warm-blooded animals such as humans, more particularly to the use of these compounds in the manufacture of medicaments for use in the treatment of bacterial infections in warm-blooded animals such as humans. | 04-21-2011 |
20110098288 | SULFONAMIDES AS ZAP-70 INHIBITORS - The invention relates to compounds of formula (I) | 04-28-2011 |
20110105490 | 2,3-DIHYDRO-1H-ISOINDOL-1-IMINE DERIVATIVES USEFUL AS THROMBIN PAR-1 RECEPTOR ANTAGONIST - The present invention is directed to novel 2,3-dihydro-1H-isoindol-1-imine derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the thrombin PAR-1 receptor antagonists. | 05-05-2011 |
20110105491 | THIAZOLIDINE COMPOUNDS AS OREXIN RECEPTOR ANTAGONISTS - The invention relates to thiazolidine derivatives of the formula (I) wherein A, B, and R | 05-05-2011 |
20110112084 | Bicyclic androgen and progesterone receptor modulator compounds and methods - The present invention is directed to compounds, pharmaceutical compositions, and methods for modulating processes mediated by AR and PR. More particularly, the invention relates to nonsteroidal compounds and compositions that are high affinity, high specificity agonists, partial agonists (i.e., partial activators and/or tissue-specific activators) and antagonists for AR and PR. Also provided are methods of making such compounds and pharmaceutical compositions, as well as critical intermediates used in their synthesis. | 05-12-2011 |
20110118248 | Heteroaryl sulfonamides and CCR2/CCR9 - Compounds are provided that act as potent antagonists of the CCR2 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, and as controls in assays for the identification of CCR2 antagonists. | 05-19-2011 |
20110118249 | INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION - Compounds of formula (I): wherein c, X, Y, R | 05-19-2011 |
20110118250 | BETA-SECRETASE MODULATORS AND METHODS OF USE - The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I | 05-19-2011 |
20110124636 | 2-AZA-BICYCLO[3.1.0]HEXANE DERIVATIVES AS OREXIN RECEPTOR ANTAGONISTS - The invention relates to novel 2-aza-bicyclo[3.1.0]hexane derivatives of Formula (I) wherein A, B, n and R | 05-26-2011 |
20110124637 | BENZIMIDAZOLES AND RELATED ANALOGS AS SIRTUIN MODULATORS - Provided herein are sirtuin-modulating compounds of formula (II). 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 relating 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. | 05-26-2011 |
20110130395 | P13K ISOFORM SELECTIVE INHIBITORS - 2-Morpholin-4-yl-9H-purine and 5-Morpholin-4-yl-3H-[1,2,3]triazolo[4,5-d]pyrimidine derivatives, especially those substituted by 6-heteroaryl, are unexpected PI3 kinase isoform selective inhibitors with good drug properties and are useful in treating disorders related to abnormal PI3K activities such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders. | 06-02-2011 |
20110136798 | Crystalline Forms Of A Pyridine Derivative - The invention relates to 4-methylbenzenesulfonate salt of the compound of formula (I) | 06-09-2011 |
20110144098 | AMINO OXAZINE DERIVATIVES - This invention relates to 5,6-dihydro-4H-[1,3]oxazin-2-ylamine compounds of the formula | 06-16-2011 |
20110166132 | Gamma Secretase Modulators - The present invention provides compounds that are gamma secretase modulators and are therefore useful for the treatment of diseases treatable by modulation of gamma secretase such as Alzheimer's disease. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds. | 07-07-2011 |
20110172220 | DISCODERMOLIDE ANALOGUES AND METHODS OF THEIR USE - 6- and 7-substituted coumarin and related 6- and 7-substituted 1H-quinolin-2-one compounds, pharmaceutical compositions containing these compounds, and methods for their pharmaceutical use are disclosed. In certain embodiments, the 7-substituted coumarin and related 7-substituted 1H-quinolin-2-one compounds mimic or exceed the high level of pharmacological activity of discodermolide. In other embodiments, their preparation involves more readily available materials, higher yield processes and/or simpler synthetic sequences. In yet other embodiments, the compounds of the invention represent structurally simpler, therapeutically active analogues of discodermolide than heretofore known and may be useful as microtubule stabilizers and, inter alia, for treating and/or preventing cancer and other diseases, disorders, and/or conditions mediated by the stabilization of microtubules. | 07-14-2011 |
20110172221 | ANNELLATED 4-(INDAZOLYL)-1,4-DIHYDROPYRIDINE DERIVATIVES AND METHODS OF USE THEREOF - This invention relates to novel annellated 4-(indazolyl)-1,4-dihydropyridine derivatives having protein tyrosine kinase inhibitory activity, to a process for the manufacture thereof and to the use thereof for the treatment of c-Met-mediated diseases or c-Met-mediated conditions, particularly cancer and other proliferative disorders. | 07-14-2011 |
20110190283 | Fab I Inhibitors - Compounds of the Formula (I) are disclosed which are Fab I inhibitors and are useful in the treatment of bacterial infections. | 08-04-2011 |
20110190284 | AEROSOL FORMULATIONS FOR THE INHALATION OF BETA-AGONISTS - A pharmaceutical formulation, comprising:
| 08-04-2011 |
20110195963 | NOVEL CARBAMOYLOXY ARYLALKANOYL ARYLPIPERAZINE COMPOUND, PHARMACEUTICAL COMPOSITIONS COMPRISING THE COMPOUND AND METHOD FOR TREATING PAIN, ANXIETY AND DEPRESSION BY ADMINISTERING THE COMPOUND - There is provided a novel carbamoyloxy arylalkanoyl arylpiperazine derivative compound having abundant racemic or enantiomeric characteristics, represented by the Formula 1, and pharmaceutically available salts or hydrates thereof. Also, there are provided a pharmaceutical composition for treating pain, anxiety or depression including an effective amount of the compound, and a method for treating pain, anxiety or depression in mammals by administering an effective amount of the compound to the mammals in need of treatment thereof. | 08-11-2011 |
20110201605 | HETEROARYL SUBSTITUTED PIPERIDINES - The invention relates to compounds of formula | 08-18-2011 |
20110201606 | PYRIMIDINE DERIVATIVES - Novel pyrimidine derivatives of formula I | 08-18-2011 |
20110201607 | FUSED HETEROCYCLIC M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS - The present invention is directed to fused heterocyclic compounds of formula (I): which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor. | 08-18-2011 |
20110207726 | Inhibitors of Human Cathepsin L, Cathepsin B, and Cathepsin S - The present invention is directed to novel protease inhibitors that are specific for cathepsin L, cathepsin B, and cathepsin S. Accordingly, the present invention encompasses compositions and methods for treating and preventing diseases and disorders associated with cathepsin L, cathepsin B, or cathepsin S function or activity. | 08-25-2011 |
20110212950 | 4,4-DISUBSTITUTED PIPERIDINES - The application relates to 4,4-disubstituted piperidines of the general formula (I) and their salts, preferably their pharmaceutically acceptable salts, in which R | 09-01-2011 |
20110212951 | HUMAN PROTEIN TYROSINE PHOSPHATASE INHIBITORS AND METHODS OF USE - The present disclosure relates to compounds effective as human protein tyrosine phosphatase beta (HPTP-β) inhibitors thereby regulating angiogenesis. The present disclosure further relates to compositions comprising said human protein tyrosine phosphatase beta (HPTP-β) inhibitors, and to methods for regulating angiogenesis. | 09-01-2011 |
20110212952 | 3,4-DIHYDROBENZOXAZINE COMPOUNDS AND INHIBITORS OF VANILLOID RECEPTOR SUBTYPE 1 (VRI) ACTIVITY - A 3,4-dihydrobenzoxazine compound of the present invention is represented by the following formula [1] (wherein X is a nitrogen atom or CR | 09-01-2011 |
20110212953 | Polymorph Form II of Tanaproget - Tanaproget polymorph Form II, processes for preparing tanaproget polymorph Form II, pharmaceutical compositions including tanaproget polymorph Form II, micronized tanaproget polymorph Form II, and processes for converting Form II to tanaproget Form I are provided. Also provided are methods of contraception, hormone replacement therapy, stimulation of food intake and treating or preventing uterine myometrial fibroids, benign prostatic hypertrophy, benign and malignant neoplastic disease, dysfunctional bleeding, uterine leiomyomata, endometriosis, polycystic ovary syndrome, or carcinomas and adenocarcinomas comprising administering polymorph Form II to a mammalian subject. | 09-01-2011 |
20110230476 | PI3 KINASE INHIBITORS AND USES THEREOF - The present invention provides compounds, compositions thereof, and methods of using the same. | 09-22-2011 |
20110230477 | COMPOUNDS, PHARMACEUTICAL COMPOSITION AND METHODS FOR USE IN TREATING METABOLIC DISORDERS - The present invention is directed to novel compounds of formula (I) and their use in treating metabolic diseases. | 09-22-2011 |
20110237576 | 2-AMINOPYRIMIDIN-4-ONE AND 2-AMINOPYRIDINE DERIVATIVES BOTH HAVING BACE1-INHIBITING ACTIVITY - The present invention provides a compound which has an effect of inhibiting amyloid-β production and is useful as a therapeutic agent for diseases induced by production, secretion and/or deposition of amyloid-β proteins. The present invention relates to a compound represented by formula (I) or a pharmaceutically acceptable salt or solvate thereof: | 09-29-2011 |
20110237577 | BICYCLIC PEPTIDOMIMETIC INHIBITORS OF ASPARTYL-PROTEASES FOR THE TREATMENT OF INFECTIOUS DISEASES - The present invention refers to 3-aza-bicyclo[3.2.1]octane derivatives of general formula (I) their preparation, use and pharmaceutical compositions useful in the treatment of pathologies associated with microbial pathogens expressing aspartyl-protease activity. | 09-29-2011 |
20110245241 | HIV Integrase Inhibitors - The disclosure generally relates to the novel compounds of formula I, including their salts, which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV. | 10-06-2011 |
20110251189 | HYPOXIA TARGETED COMPOUNDS FOR CANCER DIAGNOSIS AND THERAPY - The present invention generally relates to oxazine derivative compounds and related compositions and methods for inducing hypoxic tumor cell death, treating cancer and locating a hypoxic tumor in a subject. | 10-13-2011 |
20110251190 | SPIRO-TETRACYCLIC RING COMPOUNDS AS BETA-SECRETASE MODULATORS AND METHODS OF USE - The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and other related conditions. In one embodiment, the compounds have a general Formula I | 10-13-2011 |
20110257168 | DERIVATIVES OF OXABISPIDINE AS NEURONAL NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS - The present invention relates to compounds of formula (I) 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). | 10-20-2011 |
20110257169 | NOVEL HYDROXY-6-HETEROARYLPHENANTHRIDINES AND THEIR USE AS PDE4 INHIBITORS - Compounds of the formula Ia***** | 10-20-2011 |
20110263588 | TRICYCLIC COMPOUNDS AS GLUTAMATE RECEPTOR MODULATORS - The present invention relates to compounds that may be negative allosteric modulators of metabotropic receptors-subtype 5, and methods of making and using same. | 10-27-2011 |
20110263589 | Method for preventing or treating a glucocorticoid receptor-related disease - A method of preventing or treating a glucocorticoid receptor-related disease involving administering a therapeutically effective amount of a 1,2-dihydroquinoline compound or a pharmaceutically acceptable salt thereof. | 10-27-2011 |
20110263590 | Antibacterial Compositions - Compounds of formula (I) have antibacterial activity: | 10-27-2011 |
20110275622 | BI-FUNCTIONAL QUINOLINE ANALOGS - Provided are compounds of Formula I: | 11-10-2011 |
20110275623 | BI-FUNCTIONAL PYRAZOLOPYRIDINE COMPOUNDS - This invention provides compounds of the formula: | 11-10-2011 |
20110275624 | INDOLE AND BENZOMORPHOLINE DERIVATIVES AS MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS - The present invention relates to novel compounds, in particular novel indole and benzomorpholine derivatives according to Formula (I) wherein all radicals are as defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic receptors-subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved. | 11-10-2011 |
20110281857 | PI3K/MTOR KINASE INHIBITORS - 6-morpholin-4-yl-pyrazolo[3,4-d]pyrimidine and 2-morpholin-4-yl-7H-pyrrolo[2,3-d]pyrimidine derivatives have unexpected drug properties as inhibitors of PI3 and/or mTOR kinases and are useful in treating disorders related to abnormal PI3K/mTOR activities such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders. | 11-17-2011 |
20110281858 | AEROSOL FORMULATION FOR THE INHALATION OF BETA AGONISTS - The present invention relates to a propellant-free aerosol formulation which [contains] one or more compounds of general formula (1) wherein the groups R | 11-17-2011 |
20110281859 | NOVEL HETEROCYCLIC COMPOUNDS AS METAP-2 INHIBITORS - Compounds of the formula I, in which D, X, Y, Z, R and R | 11-17-2011 |
20110288082 | METHODS AND COMPOSITIONS FOR INHIBITION OF THE TRANSITIONAL ENDOPLASMIC RETICULUM ATPASE - Compounds of Formulas I-XLIII are identified as direct inhibitors of p97 ATPase or of the degradation of a p97-dependent ubiquitin-proteasome system (UPS) substrate. Methods and compositions are disclosed for inhibiting p97 ATPase and the degradation of a p97-dependent UPS substrate, and for identifying inhibitors thereof | 11-24-2011 |
20110288083 | METHOD OF TREATING CANCER BY INHIBITION OF PROTEIN KINASE-LIKE ENDOPLASMIC RETICULUM PROTEIN KINASE - The present invention relates to a method of identifying compounds useful in inhibiting protein kinase-like endoplasmic reticulum protein kinase (PERK). The method comprises providing a first model comprising PERK active domains, where the said active domains are selected from the group consisting of the peptide spanning from amino acid residue Asp144 to amino acid residue Ser191 of SEQ ID NO: 1 and a peptide comprising the amino acid residue at position 7 of SEQ ID NO: 1, providing one or more candidate compounds, evaluating contact between the candidate compounds and the first model to determine which of the one or more candidate compounds have an ability to bind to and/or fit in the first model, and identifying the compounds which, based on said evaluating, have the ability to bind to and/or fit in the first model as compounds potentially useful for inhibiting PERK. The present invention further relates to compounds that can be used for inhibition of PERK, for example human PERK, and methods related to treatment of PERK-mediated diseases. | 11-24-2011 |
20110288084 | [4-( 1-AMINO-ETHYL) - CYCLOHEXYL ] - METHYL - AMINES AS ANTIBACTERIALS - The present invention relates to compounds of Formula (I) and pharmaceutically acceptable salts thereof, to their use in the treatment of bacterial infections, and to their methods of preparation. | 11-24-2011 |
20110294797 | REVERSE-TURN MIMETICS AND METHOD RELATING THERETO - Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetic structures have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis. | 12-01-2011 |
20110301156 | Vanilloid Receptor Ligands, Pharmaceutical Compositions Containing Them, Process For Making Them, and Use Thereof to Treat Pain and Other Conditions - Vanilloid receptor ligand compounds corresponding to formula I: | 12-08-2011 |
20110301157 | BICYCLIC AMIDES AS KINASE INHIBITORS - The invention relates to compounds of formula (I) and their use in the treatment of the animal or human body, to pharmaceutical compositions comprising a compound of formula I and to the use of a compound of formula I for the preparation of pharmaceutical compositions for use in the treatment of protein kinase dependent diseases, especially of proliferative diseases, such as in particular tumour diseases. | 12-08-2011 |
20110312951 | C-Ring Modified Tricyclic Benzonaphthiridinone Protein Kinase Inhibitors and Use Thereof - Disclosed are C-ring modified tricyclic benzonaphthiridinone compounds and analogs thereof, pharmaceutical compositions comprising such compounds and processes for preparing the same. The compounds are useful in the treatment of diseases amenable to protein kinase signal transduction inhibition, regulation and/or modulation. | 12-22-2011 |
20110312952 | NOVEL SPIRO COMPOUNDS USEFUL AS INHIBITORS OF STEAROYL-COENZYME A DELTA-9 DESATURASE - Heteroaromatic compounds of structural formula (I) are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis. | 12-22-2011 |
20110312953 | ANTHRANILIC ACID DERIVATIVES - The present invention relates to novel anthranilic acid derivatives of the general formula (I) | 12-22-2011 |
20110312954 | MINERALOCORTICOID RECEPTOR ANTAGONIST AND METHODS OF USE - The present invention provides a compound of the formula: Compound (I) or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising Compound (I) in combination with a suitable carrier, diluent, or excipient; and methods for treating physiological disorders, particularly congestive heart failure, hypertension, diabetic nephropathy, or chronic kidney disease, comprising administering Compound (I), or a pharmaceutically acceptable salt thereof. | 12-22-2011 |
20110319402 | AEROSOL FORMULATION FOR THE INHALATION OF BETA AGONISTS - The present invention relates to a propellant-free aerosol formulation which [contains] one or more compounds of general formula (1) wherein the groups R | 12-29-2011 |
20110319403 | BICYCLIC COMPOUNDS AS INHIBITORS OF DIACYLGLYCEROL ACYLTRANSFERASE - The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase (“DGAT”) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the invention is shown below: formula (I). | 12-29-2011 |
20110319404 | METHOD FOR TREATING NON-HODKIN'S LYMPHOMA - The present invention relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for treating non-Hodgkin's lymphoma, in a subject in need thereof. | 12-29-2011 |
20120004221 | Antibacterial Compositions - Compounds of formula (I) have antibacterial activity: | 01-05-2012 |
20120010202 | POLYMERIZABLE BENZOXAZINE COMPOUNDS WITH INTERFACIAL ACTIVE OR SURFACE ACTIVE PROPERTIES - The invention relates to polymerizable benzoxazine compounds with interfacial active or surface active properties, having at least one polyalkylene oxide structural element, and to a method for producing said compounds. The invention also relates to benzoxazine (co)polymers comprising at least one of said benzoxazine compounds in the polymerized form. | 01-12-2012 |
20120015940 | NOVEL AMINOPYRIDINE DERIVATIVES HAVING AURORA A SELECTIVE INHIBITORY ACTION - The present invention relates to a compound of Formula (I): wherein: n is 0 or 1; X is O or CH | 01-19-2012 |
20120022057 | BICYCLIC COMPOUNDS AS INHIBITORS OF DIACYGLYCEROL ACYLTRANSFERASE - The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase (“DGAT”) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the invention is shown below (I). | 01-26-2012 |
20120022058 | 4,5-DIHYDRO-1H-PYRAZOLE COMPOUNDS AND THEIR PHARMACEUTICAL USES - Mineralocorticoid receptor antagonists (MRa), pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, diabetic nephropathy and hypertension in mammals, including humans. | 01-26-2012 |
20120028973 | NITROIMIDAZOOXAZINES AND THEIR USES IN ANTI-TUBERCULAR THERAPY - The present invention relates to novel nitroimidazooxazines, to their preparation, and to their use as drugs for treating | 02-02-2012 |
20120035167 | INDOLE AND BENZOXAZINE DERIVATIVES AS MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS - The present invention relates to novel indole and benzoxazine derivatives which are positive allosteric modulators of the metabotropic glutamate receptor subtype 2 (“mGluR2”) and which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, and to the use of such compounds for the prevention or treatment of neurological and psychiatric disorders and diseases in which mGluR2 is involved. | 02-09-2012 |
20120035168 | N-((6-AMINO-PYRIDIN-3-YL)METHYL)-HETEROARYL-CARBOXAMIDES - The invention relates to compound of the formula I | 02-09-2012 |
20120035169 | AEROSOL FORMULATION FOR THE INHALATION OF BETA-AGONISTS - The present invention relates to a propellant-free aerosol formulation which [contains] one or more compounds of general formula 1 | 02-09-2012 |
20120040974 | MIF MODULATORS - The invention provides novel heterocyclic compounds, pharmaceutical compositions and methods of treatment that modulate levels of MIF expression and treat disorders associated with high or low levels of MIF expression. | 02-16-2012 |
20120040975 | BRIDGED BICYCLIC HETEROCYCLE DERIVATIVES AND METHODS OF USE THEREOF - The present invention relates to Bridged Bicyclic Heterocycle Derivatives, compositions comprising a Bridged Bicyclic Heterocycle Derivative, and methods of using the Bridged Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a GPCR in a patient. | 02-16-2012 |
20120065197 | Pyridinylcarboxylic Acid Derivatives as Fungicides - Pyridinylcarboxylic acid derivatives of the formula (I) | 03-15-2012 |
20120071471 | NOVEL BENZOXAZINONE DERIVATIVES USEFUL FOR THE TREATMENT OF CNS DISORDERS - The present invention encompasses novel 1,4-dihydro-3,1-benzoxazin-2-one derivatives, which are surprisingly found to be efficacious in animal models of CNS disorders and, as such, are valuable candidates for the prevention or treatment of CNS (Central Nervous System) diseases or disorders. | 03-22-2012 |
20120094990 | PHENYLACETIC ACID COMPOUND - A compound represented by formula (I), | 04-19-2012 |
20120094991 | 1, 4-Benzoxazine Compounds and Derivatives Thereof as Therapeutic Drugs for the Treatment of Neurodegenerative Conditions - The present invention includes compositions and methods for inhibiting kinase activity to protect against neurodegeneration including diseases such as Alzheimer's disease, Parkinson's disease, or Huntington's disease, and conditions such as ischemic stroke comprising the step of providing the subject with a therapeutically affective amount of 1,4-benzoxazine compounds and derivatives thereof. | 04-19-2012 |
20120094992 | POLY (ADP-RIBOSE) POLYMERASE (PARP) INHIBITORS - Compounds of the following formula are provided for use in inhibiting Poly (ADP-ribose) Polymerase (PARP): | 04-19-2012 |
20120094993 | N-PYRIDIN-3-YL OR N-PYRAZIN-2-YL CARBOXAMIDES - The present invention relates to compounds of formula I, | 04-19-2012 |
20120101090 | CRYSTAL OF A BENZOXAZINONE COMPOUND - Disclosed is a crystal of 2-hexadecyloxy-6-methyl-4H-3,1-benzoxazin-4-one useful as a preventive or therapeutic agent for obesity and the like. Specifically disclosed is a crystal of 2-hexadecyloxy-6-methyl-4H-3, 1-benzoxazin-4-one having a powder X-ray diffraction pattern in which characteristic peaks appear at powder X-ray diffraction interplanar spacings (d) of around 16.54±0.2, 13.26±0.2, 4.70±0.2, 4.38±0.2, and 3.67±0.2A. | 04-26-2012 |
20120115857 | Novel Polymorphs of Efavirenz - The present invention relates to novel amorphous and crystalline forms of efavirenz, processes for their preparation and pharmaceutical compositions containing them. In accordance with the present invention efavirenz crude is dissolved in acetone at 25° C.-30° C., the solution is slowly added to water for 30 minutes at 0° C.-5° C., stirred for 1 hour at the same temperature, the separated solid is filtered, washed with water and dried at 55° C.-60° C. for 5 hours to give amorphous efavirenz. | 05-10-2012 |
20120115858 | Polymorph Form II of Tanaproget - Tanaproget polymorph Form II, processes for preparing tanaproget polymorph Form II, pharmaceutical compositions including tanaproget polymorph Form II, micronized tanaproget polymorph Form II, and processes for converting Form II to tanaproget Form I are provided. Also provided are methods of contraception, hormone replacement therapy, stimulation of food intake and treating or preventing uterine myometrial fibroids, benign prostatic hypertrophy, benign and malignant neoplastic disease, dysfunctional bleeding, uterine leiomyomata, endometriosis, polycystic ovary syndrome, or carcinomas and adenocarcinomas comprising administering polymorph Form II to a mammalian subject. | 05-10-2012 |
20120115859 | 3,4,5-SUBSTITUTED PIPERIDINES AS RENIN INHIBITORS - The application relates to novel substituted piperidines of the general formula (II) in which R | 05-10-2012 |
20120115860 | NOVEL DERIVATIVES OF ARYL--METHANONE, THEIR METHOD OF PREPARATION AND THEIR USE AS MEDICINAL PRODUCTS - The present invention concerns compounds of general formula (1) (I) wherein R | 05-10-2012 |
20120115861 | AMINOPYRIDINE DERIVATIVES FOR TREATING TUMORS AND INFLAMMATORY DISEASES - Compounds of the formula (I), in which R | 05-10-2012 |
20120122859 | METHODS OF USING DIAMINOPYRIMIDINE AS P2X3 AND P2X2/3 RECEPTOR MODULATORS FOR TREATMENT OF RESPIRATORY AND GASTROINTESTINAL DISEASES - Methods for treating respiratory and gastrointestinal diseases mediated by a P2X | 05-17-2012 |
20120122860 | SOLID FORMS OF SULFONAMIDES AND AMINO ACIDS - Solid forms of phenyl sulfonamide compounds of formula (I) active on protein kinases, including Raf protein kinases, are described, as well as methods of using such solid forms to treat diseases and conditions associated with activity of protein kinases, e.g. Raf protein kinases, including pain, polycystic kidney disease, melanoma and colorectal cancer. | 05-17-2012 |
20120122861 | BICYCLIC AMIDE DERIVATIVES FOR ENHANCING GLUTAMATERGIC SYNAPTIC RESPONSES - This invention relates to compounds, pharmaceutical compositions and methods for use in the prevention and treatment of cerebral insufficiency, including enhancement of receptor functioning in synapses in brain networks responsible for basic and higher order behaviors. These brain networks, which are involved in cognitive abilities related to memory impairment, such as is observed in a variety of dementias, in imbalances in neuronal activity between different brain regions, as is suggested in disorders such as Parkinson's disease, schizophrenia, sleep apneas, attention deficit hyperactivity disorder and affective or mood disorders, and in disorders wherein a deficiency in neurotrophic factors is implicated, as well as conditions such as stroke-induced central sleep apnea, obstructive sleep apnea, congenital hypoventilation syndrome, among others. In a particular aspect, the invention relates to bicyclic amide compounds useful for treatment of such conditions, and methods of using these compounds for such treatment. | 05-17-2012 |
20120122862 | ARGININE DERIVATIVES WITH NP-I ANTAGONISTIC ACTIVITY - The present invention is a compound of formula (I) or formula (II) which are suitable as NP-1 antagonists. | 05-17-2012 |
20120129847 | COMPOSITIONS AND METHODS FOR TREATING OCULAR EDEMA, NEOVASCULARIZATION AND RELATED DISEASES - Disclosed are methods for the treatment of diseases or conditions of the eye, especially retinopathies, ocular edema and ocular neovascularization. Non-limiting examples of these diseases or conditions include diabetic macular edema, age-related macular degeneration (wet form), choroidal neovascularization, diabetic retinopathy, retinal vein occlusion (central or branch), ocular trauma, surgery induced edema, surgery induced neovascularization, cystoid macular edema, ocular ischemia, uveitis, and the like. | 05-24-2012 |
20120129848 | Benzo [E] [1,3] Oxazin-4-One Derivatives as Phosphoinositide 3-Kinase Inhibitors - Compounds of formula (I): wherein: W is O, N—H, N-alkyl, N-alkenyl, N-alkynyl, N-aryl, N-heteroaryl or S; each X is independently CH or N; R | 05-24-2012 |
20120149698 | NOUVEL COMPOUNDS - The present invention relates to new CGRP-antagonists of general formulae Ia and Ib | 06-14-2012 |
20120157450 | Anhydrate Forms Of A Pyridine Derivative - The invention relates to the compound of formula (I) in a crystalline anhydrate form, | 06-21-2012 |
20120165324 | THERAPEUTIC COMPOSITIONS AND RELATED METHODS OF USE - 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. | 06-28-2012 |
20120178749 | NS1 PROTEIN INHIBITORS - The present invention generally relates to compounds to treat viral infections and methods of their use. In particular, compounds of the present invention inhibit the activity of NS1 protein, thereby mitigating viral infection and, in particular, influenza virus infection. Accordingly, NS1 protein inhibitors and methods of treatment that employ such inhibitors are contemplated by the present invention. | 07-12-2012 |
20120178750 | Niacin Receptor Agonists, Compositions Containing Such Compounds and Methods of Treatment - The present invention encompasses compounds of Formula I: | 07-12-2012 |
20120184541 | COMPOUNDS AND METHODS OF USE - In one aspect, the present invention provides for a compound of Formula I | 07-19-2012 |
20120184542 | PYRIDO PYRIMIDINES - Compounds of formula | 07-19-2012 |
20120184543 | DIHYDROPTERIDINONE DERIVATIVES, PREPARATION PROCESS AND PHARMACEUTICAL USE THEREOF - Dihydroperidinone derivatives, preparation process and pharmaceutical use thereof are disclosed. Specially, new dihydroperidinone derivatives represented by general formula (I), wherein each substituent of the general formula (I) is defined as in the description, their preparation process, pharmaceutical compositions comprising said derivatives and their use as therapeutical agents, especially as Plk kinase inhibitors are disclosed. | 07-19-2012 |
20120202803 | N-[3-(5-AMINO-3,3A,7,7A-TETRAHYDRO-1H-2,4-DIOXA-6-AZA-INDEN-7-YL)-PHENYL]-- AMIDES AS BACE1 AND/OR BACE2 INHIBITORS - The present invention relates to N-[3-(5-Amino-3,3a,7,7a-tetrahydro-1H-2,4-dioxa-6-aza-inden-7-yl)-phenyl]-amides of formula I | 08-09-2012 |
20120202804 | FUSED AMINODIHYDRO-OXAZINE DERIVATIVES - A compound represented by the general formula (I) or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein Ring A is a C | 08-09-2012 |
20120202805 | PI3K (delta) SELECTIVE INHIBITORS - Novel PI3K, especially PI3K delta isoform, selective inhibitors are disclosed. The compounds are useful in treating disorders related to abnormal PI3K or PI3Kδ activities such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders. | 08-09-2012 |
20120208805 | TRIAZOLIUM SALTS AS PAR1 INHIBITORS, PRODUCTION THEREOF, AND USE AS MEDICAMENTS - The invention relates to novel compounds of formula I | 08-16-2012 |
20120208806 | Hsp90 Inhibitors - The present application provides compounds useful in the inhibition of Hsp90, and hence in the treatment of disease. | 08-16-2012 |
20120214805 | BRIDGED BICYCLIC PIPERIDINE DERIVATIVES AND METHODS OF USE THEREOF - The present invention relates to Bridged Bicyclic Piperidine Derivatives, compositions comprising a Bridged Bi-cyclic Piperidine Derivative, and methods of using the Bridged Bicyclic Piperidine Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of GPR119 in a patient. | 08-23-2012 |
20120220576 | Novel Heterocyclic Derivatives - The invention relates to novel heterocyclic compounds of the formula | 08-30-2012 |
20120220577 | GLYCINE B ANTAGONISTS - The invention relates to naphthalene derivatives as well as their pharmaceutically acceptable salts. The invention further relates to a process for the preparation of such compounds. The compounds of the invention are glycine B antagonists and are therefore useful for the control and prevention of various disorders, including neurological disorders. | 08-30-2012 |
20120220578 | GUM RESIN AS A CARRIER FOR TOPICAL APPLICATION OF PHARMACOLOGICALLY ACTIVE AGENTS - Described are pharmacological compositions comprising a gum resin; a pharmacologically active agent and a topically acceptable volatile solvent for the gum resin and active agent. Also described are methods for the transdermal or transmucosal delivery of a pharmacologically active agent using such compositions. | 08-30-2012 |
20120220579 | METHODS OF UTILIZING ARYLPIPERAZINE DERIVATIVES - The present invention provides arylpiperazine derivatives which can be advantageously used for treating schizophrenia and related psychoses such as acute manic, bipolar disorder, autistic disorder, and depression. | 08-30-2012 |
20120225867 | ANDROGEN RECEPTOR MODULATING COMPOUNDS - The present disclosure relates to compounds of formula (I), and pharmaceutically acceptable salts thereof. The present disclosure also relates to compositions and methods of treating comprising compounds of formula (I), and pharmaceutically acceptable salts thereof. | 09-06-2012 |
20120232069 | PROCESS FOR PREPARING EFAVIRENZ POLYMORPH - The present invention relates to a process for the preparation of crystalline non-hygroscopic form H1 of efavirenz, and pharmaceutical compositions containing it. In accordance with the present invention efavirenz was dissolved in acetone at 25° C.-30° C., the solution was slowly added to water at 0° C.-5° C., the separated solid was filtered, washed with mixture of acetone and water and dried at 25° C.-35° C. under below 65% relative humidity for 18 hours to give crystalline non-hygroscopic efavirenz form H1. | 09-13-2012 |
20120232070 | Use of Indole Derivatives as Nurr-1 Activators for the Application Thereof as a Medicament for the Treatment of Parkinson's Disease - Compounds derived from indole, notably useful in therapeutics, selected from:
| 09-13-2012 |
20120232071 | 2,3-DIARYL- OR HETEROARYL-SUBSTITUTED 1,1,1-TRIFLUORO-2-HYDROXYPROPYL COMPOUNDS - The present invention relates to compounds of formula I | 09-13-2012 |
20120232072 | IMIDAZOPYRIDINE DERIVATIVES - The present invention relates to compounds of formula (I), | 09-13-2012 |
20120232073 | FUSED BICYCLIC PYRIMIDINE DERIVATIVES AND METHODS OF USE THEREOF - The present invention relates to Fused Bicyclic Pyrimidine Derivatives, compositions comprising a Fused Bicyclic Pyrimidine Derivative, and methods of using the Fused Bicyclic Pyrimidine Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G-protein coupled receptor (GPCR) in a patient. | 09-13-2012 |
20120238561 | MORPHOLINOTHIAZOLES AS ALPHA 7 POSITIVE ALLOSTERIC MODULATORS - The present invention relates to morpholinothiazole derivatives and pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy. The invention particularly relates to positive allosteric modulators of nicotinic acetylcholine receptors, such positive allosteric modulators having the capability to increase the efficacy of nicotinic receptor agonists. | 09-20-2012 |
20120245162 | OXADIAZOLE INHIBITORS OF LEUKOTRIENE PRODUCTION - The present invention relates to compounds of formula (I): | 09-27-2012 |
20120245163 | TRPV1 Antagonists - Disclosed herein are compounds of formula (I) or pharmaceutically acceptable salts, solvates, or combinations thereof, | 09-27-2012 |
20120252800 | BICYCLIC THIAZOLES AS ALLOSTERIC MODULATORS OF MGLUR5 RECEPTORS - The present invention relates to novel bicyclic thiazoles which are positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (“mGluR5”) and which are useful for the treatment or prevention of disorders associated with glutamate dysfunction and diseases in which the mGluR5 subtype of receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which mGluR5 is involved. | 10-04-2012 |
20120264748 | DIAZA-SPIRO[5.5]UNDECANES - The invention relates to compound of the formula (I), in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it. | 10-18-2012 |
20120270867 | NOVEL (6-OXO-1,6-DIHYDROPYRIMIDIN-2-YL)AMIDE DERIVATIVES, PREPARATION THEREOF AND PHARMACEUTICAL USE THEREOF AS AKT(PKB) PHOSPHORYLATION INHIBITORS - The invention relates to the novel materials of formula (I), where: R1 is an optionally substituted aryl or heteroaryl; R is an H or, when formed with R1, a 5- or 6-member ring fused with an aryl or heretoaryl group optionally containing one or more of O, S, N, NH, and Nalk, being optionally substituted; R2 and R3 are, independently, an H, Hal, or alkyl optionally substituted by one or more Hal; R4 is H; and R5 is an H or alkyl optionally substituted by one or more halogen atoms. Said materials being in any isomeric form and the salts thereof, and are intended for drugs, particularly AKT(PKB) phosphorylation inhibitors. | 10-25-2012 |
20120277223 | INHIBITORS OF DIACYLGLYCEROL O-ACYLTRANSFERASE TYPE 1 ENZYME - The present invention relates to compounds of formula (I): | 11-01-2012 |
20120295900 | 1,3-OXAZINES AS BACE 1 AND/OR BACE2 INHIBITORS - The present invention provides compounds of formula I | 11-22-2012 |
20120295901 | NOVEL SUBSTITUTED BICYCLIC TRIAZOLE DERIVATIVES AS GAMMA SECRETASE MODULATORS - The present invention is concerned with novel substituted bicyclic triazole derivatives of Formula (I) | 11-22-2012 |
20120295902 | Hetaryl-[1,8]naphthyridine derivatives - Novel hetaryl-[1,8]naphthyridine derivatives of formula (I) | 11-22-2012 |
20120302560 | Novel Benzoic Pyrrolopyridine Derivatives - The present invention relates to compounds of formula: | 11-29-2012 |
20120316159 | BICYCLIC RING SYSTEM SUBSTITUTED SULFONAMIDE FUNCTIONALISED PHENOLS AS MEDICAMENTS - This invention relates to bicyclic ring system substituted sulfonamide functionalized phenols of general formula 1, | 12-13-2012 |
20120316160 | XINAFOATE SALT OF N4-(2,2-DIFLUORO-4H-BENZO[1,4]OXAZIN-3-ONE)-6-YL]-5-FLUORO-N2-[3-(METHYLA- MINOCARBONYLMETHYLENEOXY)PHENYL]2,4-PYRIMIDINEDIAMINE - The present invention relates to the xinafoate salt of N4-[(2,2-difluoro-4H-benzo[1,4]oxazin-3-one)-6-yl]-5-fluoro-N2-[3-(methylaminocarbonylmethyleneoxy)phenyl]-2,4-pyrimidinediamine. This compound is a suitable drug substance and is useful in the treatment of conditions including asthma. | 12-13-2012 |
20120316161 | NOVEL ANTIVIRAL COMPOUNDS - The present invention relates to compounds of formula (A) as defined herein having antiviral activity, more specifically HIV (Human Immunodeficiency Virus) replication inhibiting properties. The invention also relates to pharmaceutical compositions comprising an effective amount of such compounds as active ingredients. This invention further relates to the use of such compounds as medicines or in the manufacture of a medicament useful for the treatment of animals suffering from viral infections, in particular HIV infection. This invention further relates to methods for the treatment of viral infections in animals by the administration of a therapeutical amount of such compounds, optionally combined with one or more other drugs having antiviral activity. | 12-13-2012 |
20120329791 | 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. | 12-27-2012 |
20130012504 | BI-FUNCTIONAL QUINOLINE ANALOGS - Provided are compounds of Formula I: | 01-10-2013 |
20130018049 | Azaindole Compounds and Methods for Treating HIV - Provided are compounds and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and their use for treating viral infections mediated by a member of the retrovirus family of viruses such as the Human Immunodeficiency Virus (HIV). | 01-17-2013 |
20130018050 | BI-FUNCTIONAL PYRAZOLOPYRIDINE COMPOUNDS - This invention provides compounds of the formula: | 01-17-2013 |
20130023529 | Methods Involving Aldose Reductase Inhibitors - Embodiments of the invention include methods and compositions involving aldose reductase inhibitors for the treatment of inflammation, including uveitis and asthma. | 01-24-2013 |
20130029978 | NOVEL ARYL UREA DERIVATIVE - There is a need for FAAH inhibitors capable of oral administration and having excellent efficacy, particularly agents for the prevention and treatment of pain. Disclosed are novel arylurea compounds represented by formula (I), salts or solvates thereof, and pharmaceutical compositions comprising the same as an active ingredient. The pharmaceutical composition is used primarily for FAAH inhibitors, or agents for prevention and treatment of pain. | 01-31-2013 |
20130029979 | FUSED BICYCLIC COMPOUND - Fused bicyclic compound having an affinity to mineral corticoid receptor (MR), of formula [I]: | 01-31-2013 |
20130040944 | MGLUR4 ALLOSTERIC POTENTIATORS, COMPOSITIONS, AND METHODS OF TREATING NEUROLOGICAL DYSFUNCTION - Pyrrole compounds useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease state associated with glutamate dysfunction. | 02-14-2013 |
20130045972 | GLUCOCORTICOID RECEPTOR ANTAGONISTS - The present invention relates to compounds of formula I | 02-21-2013 |
20130045973 | AMIDE DERIVATIVES AS ION-CHANNEL LIGANDS AND PHARMACEUTICAL COMPOSITIONS AND METHODS OF USING THE SAME - Compounds are disclosed that have a formula represented by the following: | 02-21-2013 |
20130065892 | HETEROARYL COMPOUNDS AND USES THEREOF - The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same. | 03-14-2013 |
20130072478 | N-(3-(2-AMINO-6,6-DIFLUORO-4,4A,5,6,7,7A-HEXAHYDRO-CYCLOPENTA[E][1,3]OXAZI- N-4-YL)-PHENYL-AMIDES AS BACE1 INHIBITORS - The present invention provides N-(3-(2-amino-6,6-difluoro-4,4a,5,6,7,7a-hexahydro-cyclopenta[e][1,3]oxazin-4-yl)-phenyl)-amides of formula I | 03-21-2013 |
20130072480 | Cyclothiocarbamate Derivatives as Progesterone Receptor Modulators - Methods of using compounds which are progesterone receptor agonists for contraception and the treatment of progesterone-related maladies alone or in combination with an estrogen receptor agonist or progesterone receptor antagonist are provided. These compounds have the structure: | 03-21-2013 |
20130079337 | PYRAZOLOQUINOLINONE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF - The invention relates to compounds corresponding to formula (I) | 03-28-2013 |
20130079338 | Selective NR2B Antagonists - The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands, antagonists of the NR2B receptor and may be useful for the treatment of various disorders of the central nervous system. | 03-28-2013 |
20130079339 | TRPV1 VANILLOID RECEPTOR ANTAGONISTS WITH A BICYCLIC PORTION - The invention discloses compounds of formula I | 03-28-2013 |
20130085138 | Selective NR2B Antagonists - The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands, antagonists of the NR2B receptor and may be useful for the treatment of various disorders of the central nervous system. | 04-04-2013 |
20130090333 | BENZOXAZINE DERIVATIVES AS CRAC MODULATORS - Compounds of the formula (I): | 04-11-2013 |
20130090334 | AZABENZOXAZINE DERIVATIVES AS CRAC MODULATORS - Compounds of the formula (I): | 04-11-2013 |
20130096110 | Pyrazolopyridine, Pyrazolopyrazine, Pyrazolopyrimidine, Pyrazolothiophene and Pyrazolothiazole Compounds as MGLUR4 Allosteric Potentiators, Compositions, and Methods of Treating Neurological Dysfunction - Pyrazolopyridine, pyrazolopyrazine, pyrazolopyrimidine, pyrazolothiophene and pyrazolothiazole compounds which are useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease state associated with glutamate dysfunction. | 04-18-2013 |
20130096111 | Methods Involving Aldose Reductase Inhibitors - Embodiments of the invention include methods and compositions involving aldose reductase inhibitors for the treatment of inflammation, including uveitis and asthma. | 04-18-2013 |
20130102595 | TREATMENT OF CANCERS HAVING K-RAS MUTATIONS - The present invention provides a method of treating a cancer associated with a K-ras mutation in a subject in need thereof. The method comprises the steps of: (1) identifying a subject with a cancer associated with a K-ras mutation; and (2) administering to the subject (i) an inhibitor of PI3 kinase and (ii) an HDAC inhibitor, wherein the PI3 kinase inhibitor and the HDAC inhibitor are administered in amounts which together are therapeutically effective. | 04-25-2013 |
20130102596 | METHOD AND DEVICE FOR ADMINISTERING XINAFOATE SALT OF N4-(2,2-DIFLUORO-4H-BENZO [1,4]OXAZIN-3-ONE)-6-YL]-5-FLUORO-N2-[3- (METHYLAMINOCARBONYLMETHYLENEOXY) PHENYL]2,4-PYRIMIDINEDIAMINE - Disclosed embodiments concern a device for administering a xinafoate salt of N4-[(2,2-difluoro-4H-benzo[1,4]oxazin-3-one)-6-yl]-5-fluoro-N2-[3-(methylaminocarbonylmethyleneoxy)phenyl]-2,4-pyrimidinediamine, or compositions thereof, and a method for making and using the device. Particular disclosed embodiments concern formulating the xinafoate salt for administration via the device. | 04-25-2013 |
20130109684 | GRP94 INHIBITORS | 05-02-2013 |
20130109685 | 1-PHENYL-SUBSTITUTED HETEROCYCLYL DERIVATIVES AND THEIR USE AS PROSTAGLANDIN D2 RECEPTOR MODULATORS | 05-02-2013 |
20130116245 | ALKYLATED PIPERAZINE COMPOUNDS - Alkylated piperazine 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. | 05-09-2013 |
20130116246 | 8-FLUOROPHTHALAZIN-1(2H)-ONE COMPOUNDS - 8-Fluorophthalazin-1(2h)-one compounds of Formula II where one or two of X | 05-09-2013 |
20130123250 | SPIRO (PIPERIDINE-4,2'-PYRROLIDINE)-1-(3,5-TRIFLUOROMETHYLPHENYL) METHYLCARBOXAMIDES AS NK1 TACHIKYNIN RECEPTOR ANTAGONISTS - Compounds of formula (I) or pharmaceutically acceptable salts thereof | 05-16-2013 |
20130123251 | BENZOXAZINE DERIVATIVES AND USES THEREOF - The present invention provides a compound of the formula: | 05-16-2013 |
20130131055 | FUROPYRIDINYL-SUBSTITUTED 1,4-DIHYDROPYRIDINE DERIVATIVES AND METHODS OF USE THEREOF - This invention relates to novel 4-(furo[3,2-c]pyridin-2-yl)-1,4-dihydropyridine derivatives having protein tyrosine kinase inhibitory activity, to a process for the manufacture thereof and to the use thereof for the treatment of c-Met-mediated diseases or c-Met-mediated conditions, particularly cancer and other proliferative disorders. | 05-23-2013 |
20130137684 | HAEMATOPOIETIC-PROSTAGLANDIN D2 SYNTHASE INHIBITORS - The present invention generally relates to compounds that inhibit haematopoietic-prostaglandin D | 05-30-2013 |
20130150354 | NEW SELECTIVE CCR2 ANTAGONISTS - The present invention relates to novel and selective antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD as well as pain. | 06-13-2013 |
20130150355 | NOVEL COMPOUNDS - This invention relates to compounds of formula I | 06-13-2013 |
20130150356 | Acyl Piperazine Derivatives as TTX-S Blockers - The present invention relates to acyl piperazine derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved. | 06-13-2013 |
20130158021 | AMINO ACID-, PEPTIDE-AND POLYPEPTIDE-LIPIDS, ISOMERS, COMPOSITIONS, AND USES THEREOF - Described herein are compounds and compositions characterized, in certain embodiments, by conjugation of various groups, such as lipophilic groups, to an amino or amide group of an amino acid, a linear or cyclic peptide, a linear or cyclic polypeptide, or structural isomer thereof, to provide compounds of the present invention, collectively referred to herein as “APPLs”. Such APPLs are deemed useful for a variety of applications, such as, for example, improved nucleotide delivery. Exemplary APPLs include, but are not limited to, compounds of Formula (I), (II), (III), (IV), (V), and (VI), and salts thereof, as described herein: | 06-20-2013 |
20130165436 | Dihydro-Benzo-Oxazine and Dihydro-Pyrido-Oxazine Derivatives - The invention relates to dihydro-benzo-oxazine and dihydro-pyrido-oxazine compounds of the formula (I) and/or pharmaceutically acceptable salts and/or solvates thereof, | 06-27-2013 |
20130172333 | FORMULATION AND DOSING OF HSP90 INHIBITORY COMPOUNDS - Provided is a pharmaceutical composition comprising a pharmaceutically acceptable organic solvent, a pharmaceutically acceptable surfactant, and a compound according to the following formula: wherein the variables are defined herein. Optionally, the pharmaceutical composition further comprises a co-solvent. Also provided is a method of using the pharmaceutical composition disclosed herein for the treatment of a patient in need thereof. | 07-04-2013 |
20130172334 | TRPV1 ANTAGONISTS - Disclosed herein are compounds of formula (I): | 07-04-2013 |
20130172335 | 2,3-DIARYL- OR HETEROARYL-SUBSTITUTED 1,1,1-TRIFLUORO-2-HYDROXYPROPYL COMPOUNDS - The present invention relates to compounds of formula I | 07-04-2013 |
20130196982 | MORPHOLINO SUBSTITUTED UREA DERIVATIVES AS MTOR INHIBITORS - The invention relates to compounds of formula (I) | 08-01-2013 |
20130196983 | MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR - 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 diseases using such CFTR modulators. | 08-01-2013 |
20130203748 | Inhibitors of Human Immunodeficiency Virus Replication - The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection. | 08-08-2013 |
20130203749 | Tetrahydroisoquinolines, pharmaceutical compositions containing them, and their use in therapy - The present invention relates to tetrahydroisoquinoline of the formula (I) | 08-08-2013 |
20130203750 | N,N-SUBSTITUTED 3-AMINOPYRROLIDINE COMPOUNDS USEFUL AS MONOAMINES REUPTAKE INHIBITORS - The present invention provides a pyrrolidine compound of General Formula (1) | 08-08-2013 |
20130210818 | Novel Heterocyclic Compounds and Uses Thereof - New substituted heterocyclic compounds, compositions containing them, and methods of using them for the inhibition of Raf kinase activity are provided. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer. | 08-15-2013 |
20130210819 | QUINAZOLINE DERIVATIVES - Compounds of the formula I in which R, X, L | 08-15-2013 |
20130225567 | 5-Alkynyl Pyridine - 5-alkynyl-pyridine of general formula (I) | 08-29-2013 |
20130225568 | TRIAZOLOPYRAZINE DERIVATIVES - Compounds of the formula I | 08-29-2013 |
20130225569 | FUROPYRIDINE DERIVATIVES - Compounds of the formula I | 08-29-2013 |
20130225570 | METHODS OF USING DIAMINOPYRIMIDINE P2X3 AND P2X2/3 RECEPTOR MODULATORS FOR TREATMENT OF RESPIRATORY AND GASTROINTESTINAL DISEASES - Methods for treating respiratory and gastrointestinal diseases mediated by a P2X | 08-29-2013 |
20130245009 | NOVEL COMPOUNDS - The present invention relates to new CGRP-antagonists of general formulae Ia and Ib | 09-19-2013 |
20130261112 | Cyclothiocarbamate Derivatives as Progesterone Receptor Modulators - Methods of using compounds which are progesterone receptor agonists for contraception and the treatment of progesterone-related maladies alone or in combination with an estrogen receptor agonist or progesterone receptor antagonist are provided. These compounds have the structure: | 10-03-2013 |
20130267510 | HYDANTOIN DERIVATIVES USEFUL AS KV3 INHIBITORS - The invention provides compounds of formula (I): Said compounds being inhibitors of Kv3 channels and of use in the prophylaxis or treatment of related disorders. | 10-10-2013 |
20130274253 | NOVEL PYRIMIDINE DERIVATIVES, PREPARATION THEREOF, AND PHARMACEUTICAL USE THEREOF AS AKT(PKB) PHOSPHORYLATION INHIBITORS - The present invention relates to novel chemical compounds derived from pyrimidines, to the method for preparing same, to the novel intermediates obtained, to the use thereof as drugs, to the pharmaceutical compositions containing same, and to the therapeutic use thereof as AKT inhibitors. | 10-17-2013 |
20130281444 | PREPARATION AND PHARMACEUTICALS OF BIPHENYL BENZAMIDE-DERIVED DERIVATIVES - The present invention provides a biphenyl benzamide-derived derivatives, which structure is selected from formula I or formula II: | 10-24-2013 |
20130281445 | COMPOUNDS USEFUL AS INHIBITORS OF CHOLINE KINASE - The present invention relates to compounds useful as inhibitors of choline 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. | 10-24-2013 |
20130281446 | XINAFOATE SALT OF N4-(2,2-DIFLUORO-4H-BENZO[1,4]OXAZIN-3-ONE)-6-YL]-5-FLUORO-N2-[3-(METHYLA- MINOCARBONYLMETHYLENEOXY)PHENYL]2,4-PYRIMIDINEDIAMINE - The present invention relates to the xinafoate salt of N4-[(2,2-difluoro- | 10-24-2013 |
20130296314 | GASTRIC AND COLONIC FORMULATIONS AND METHODS FOR MAKING AND USING THEM - In alternative embodiments, the invention provides compositions, e.g., formulations, used for gastric, gastrointestinal and/or colonic treatments or lavage, e.g., orthostatic lavage, e.g., for inducing the purgation (e.g., cleansing) of a gastrointestinal (GI) tract, including a colon; and methods for making and using them. In alternative embodiments, compositions and methods of the invention are used for the amelioration, treatment and/or prevention of constipation, for the treatment of abdominal pain, particularly non-specific abdominal pain, and diarrhea, including diarrhea caused by a drug side effect, a psychological condition, a disease or a condition such as Crohn's Disease, a poison, a toxin or an infection, e.g., a toxin-mediated traveler's diarrhea. In alternative embodiments, the invention provides pharmaceuticals and products (articles) of manufacture for delivering these compositions and formulations to an individual, e.g., a human or an animal. | 11-07-2013 |
20130303529 | FUSED HETEROCYCLIC DERIVATIVES AND METHODS OF USE - Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes. | 11-14-2013 |
20130303530 | METHODS FOR TREATING CHRONIC PELVIC PAIN SYNDROME WITH ANTIBODIES THAT BINDS MCP-1 OR MIP-1A - The present invention provides methods and compositions for treating chronic pelvic pain syndrome. In particular, the present invention provides methods and compositions for treating chronic pelvic pain syndrome with an agent that targets MCP-1, MIP-1α, or the CCR-2 receptor. | 11-14-2013 |
20130324523 | TAU IMAGING PROBE - An object of the present invention is to provide a probe for imaging a β-sheet structure protein which can be used for the diagnosis of conformational diseases, particularly disease (tauopathy) having a cardinal symptom such as intracerebral accumulation of tau protein, for example, Alzheimer's disease. Another object of the present invention is to provide a compound which is highly specific to tau and can image tau with satisfactory sensitivity, and also has high brain transition, low or non-recognized bone-seeking properties and low or non-recognized toxicity. | 12-05-2013 |
20130324524 | 2,4-PYRIMIDINEDIAMINE COMPOUNDS AND THEIR USES - The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades. | 12-05-2013 |
20130331385 | COMPOSITIONS AND METHODS FOR TREATING OPHTHALMIC, OTIC, OR NASAL INFECTIONS - The present invention relates to methods for treating an ophthalmic, otic, or nasal infection comprising treating the infected tissue with a composition comprising finafloxacin or a finafloxacin derivative. The present invention also relates to antimicrobial compositions comprising finafloxacin or a finafloxacin derivative. The compositions are suitable for the treatment of ophthalmic, otic, or nasal infections. | 12-12-2013 |
20130331386 | METHODS FOR TREATING VASCULAR LEAK SYNDROME - Disclosed are methods for treating Vascular Leak Syndrome. Further disclosed are methods for treating vascular leakage due to inflammatory diseases, inter alia, sepsis, lupus, irritable bowel disease. Yet further disclosed are methods for treating renal cell carcinoma and melanoma. Still further disclosed are methods for reducing metastasis of malignant cells and/or preventing the proliferation of carcinoma cells via spreading due to vascular leakage. | 12-12-2013 |
20130338154 | MGLUR4 ALLOSTERIC POTENTIATORS, COMPOSITIONS, AND METHODS OF TREATING NEUROLOGICAL DYSFUNCTION - Pyrrole compounds useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease state associated with glutamate dysfunction. | 12-19-2013 |
20130338155 | METHOD FOR TREATING INFECTIONS - The present invention relates to compounds that inhibit the activity of Hsp90 and methods of using these compounds for treating or preventing infection. | 12-19-2013 |
20130345211 | Pyridine Compounds as Sodium Channel Blockers - The invention relates to substituted pyridine compounds of Formula I: (I) or a pharmaceutically acceptable salt, prodrug, or solvate thereof wherein A | 12-26-2013 |
20130345212 | QUINOLINONE DERIVATIVES - The present invention relates to compounds of the formula (I), | 12-26-2013 |
20140005186 | ANDROGEN RECEPTOR MODULATOR COMPOUNDS AND METHODS | 01-02-2014 |
20140005187 | OXIDOSQUALENE CYCLASE AS A PROTEIN TARGET FOR ANTICANCER THERAPEUTICS | 01-02-2014 |
20140011804 | BICYCLIC PKM2 ACTIVATORS - Compounds and compositions comprising compounds including formula (I) that activate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that activate PKM2 in the treatment of cancer. | 01-09-2014 |
20140018356 | FUSED CYCLOPENTYL ANTAGONISTS OF CCR2 - The present invention comprises compounds of Formula (I). | 01-16-2014 |
20140018357 | IRAK INHIBITORS AND USES THEREOF - The present invention provides thienopyridine compounds, compositions thereof, and methods of using the same. | 01-16-2014 |
20140018358 | BENZO [B] [1,4] OXAZIN DERIVATIVES AS CALCIUM SENSING RECEPTOR MODULATORS - Compounds of Formula (I) along with processes for their preparation that are useful for treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of calcium sensing (CaSR) receptors. Methods of treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of calcium sensing (CaSR) receptors of Formula (I). | 01-16-2014 |
20140024644 | 5-HT3 RECEPTOR ANTAGONISTS - The present invention provides 5-HT3 receptor antagonists of Formula (I): | 01-23-2014 |
20140031348 | HETEROARYL SULFONAMIDES AND CCR2/CCR9 - Compounds are provided that act as potent antagonists of the CCR2 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, and as controls in assays for the identification of CCR2 antagonists. | 01-30-2014 |
20140031349 | INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL - The present invention provides compounds of Formula I | 01-30-2014 |
20140031350 | 2,4-Pyrimidinediamine Compounds and Their Uses - The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades. | 01-30-2014 |
20140038951 | PDE10 INHIBITORS AND RELATED COMPOSITIONS AND METHODS - Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette's syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. Pharmaceutically acceptable salts, stereoisomers, solvates and prodrugs of the compounds are also provided. Also disclosed are compositions containing a compound in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same. | 02-06-2014 |
20140038952 | Substituted Amino-Pyrimidine Derivatives - The present application provides novel substituted quinazoline and pyrido-pyrimidine compounds and pharmaceutically acceptable salts, prodrugs, and solvates thereof. Also provided are methods for preparing these compounds. These compounds are useful in co-regulating PI3K and/or mTOR activity by administering a therapeutically effective amount of one or more of the compounds to a patient. By doing so, these compounds are effective in treating conditions associated with the dysregulation of the PI3K/AKT/mTOR pathway. Advantageously, these compounds perform as dual PI3K/mTOR inhibitors. A variety of conditions can be treated using these compounds and include diseases which are characterized by inflammation or abnormal cellular proliferation. In one embodiment, the disease is cancer. | 02-06-2014 |
20140045830 | CYCLIC UREA- OR LACTAM-SUBSTITUTED QUINOXALINE-TYPE PIPERIDINE COMPOUNDS AND USES THEREOF - The disclosure relates to Cyclic Urea- or Lactam-Substituted Quinoxaline-Type Piperidine Compounds of Formula (I): | 02-13-2014 |
20140045831 | BICYCLIC HETEROCYCLE COMPOUNDS AND THEIR USES IN THERAPY - The invention relates to bicyclic heterocycle compounds of formula (I): or tautomeric or stereochemically isomeric forms, N-oxides, pharmaceutically acceptable salts or the solvates thereof; wherein R | 02-13-2014 |
20140066442 | Pyridinylcarboxylic Acid Derivatives as Fungicides - Pyridinylcarboxylic acid derivatives of the formula (I) | 03-06-2014 |
20140073636 | NOVEL HYDROXY-6-HETEROARYLPHENANTHRIDINES AND THEIR USE AS PDE4 INHIBITORS - Compounds of the formula Ia***** | 03-13-2014 |
20140080823 | SPIROCYCLIC DERIVATIVES AS HISTONE DEACETYLASE INHIBITORS - This invention is related to new histone deacetylase inhibitors according to the general formula (I) wherein: the dotted line is an optional additional bond; n is zero or an integer from 1 to 4; R | 03-20-2014 |
20140088094 | N-SULFONYLATED TETRAHYDROQUINOLINES AND RELATED BICYCLIC COMPOUNDS FOR INHIBITION OF RORgamma ACTIVITY AND THE TREATMENT OF DISEASE - The invention provides tetrahydroquinoline and related compounds, pharmaceutical compositions, methods of inhibiting RORγ activity, reducing the amount of IL-17 in a subject, and treating immune disorders and inflammatory disorders using such tetrahydroquinoline and related compounds are provided. | 03-27-2014 |
20140088095 | METHOD FOR TREATING PAIN, ANXIETY OR DEPRESSION USING CARBAMOYLOXY ALKANOYL PIPERAZINE COMPOUND - There is provided a novel carbamoyloxy arylalkanoyl arylpiperazine derivative compound having abundant racemic or enantiomeric characteristics, represented by the Formula 1, and pharmaceutically available salts or hydrates thereof. Also, there are provided a pharmaceutical composition for treating pain, anxiety or depression including an effective amount of the compound, and a method for treating pain, anxiety or depression in mammals by administering an effective amount of the compound to the mammals in need of treatment thereof. | 03-27-2014 |
20140094457 | PHARMACEUTICAL COMPOSITIONS AND TREATMENT OF GENETIC DISEASES ASSOCIATED WITH NONSENSE MEDIATED RNA DECAY - The present invention relates to pharmaceutical compositions comprising a compound and a pharmaceutically acceptable carrier. The present invention is also directed to a method of treating a genetic disease caused by premature termination codons, or other conditions that render messenger ribonucleic acid (mRNA) susceptible to nonsense mediated RNA decay, in a subject. Also disclosed is a method of inhibiting nonsense mediated RNA decay and/or induction of autophagy. The present invention also relates to a method of identifying inhibitors of nonsense mediated RNA decay and/or inducing autophagy. The present invention further relates to a method of inhibiting nonsense mediated RNA decay and/or induction of autophagy in a subject. | 04-03-2014 |
20140094458 | Cyclic Progestin Regimens and Kits - A method of contraception is provided which involves delivery of 21 to 27 consecutive days of a progestin in the absence of an estrogen or other steroidal compound, followed by 1 to 7 days without an effective amount of an active agent. Also described is a pharmaceutically useful kit to facilitate delivery of this regimen. | 04-03-2014 |
20140100221 | 1H-Pyrrolo[2,3-b]Pyridine Derivatives - 1H-Pyrrolo[2,3-b]pyridine compounds are inhibitors of cell proliferation/cell vitality and can be employed for the treatment of tumours. | 04-10-2014 |
20140100222 | Beta2-ADRENOCEPTOR AGONIST FOR THE TREATMENT OF COUGH - This invention relates to the β2-adrenoceptor agonist Olodaterol or a pharmaceutically acceptable salt thereof, | 04-10-2014 |
20140107113 | PHARMACEUTICAL COMPOSITION COMPRISING A TRPA1 ANTAGONIST AND A BETA-2 AGONIST - The present patent application relates to a pharmaceutical composition comprising a transient receptor potential ankyrin-1 receptor (“TRPA1”) antagonist and a beta-2 adrenergic receptor agonist (“beta-2 agonist”). | 04-17-2014 |
20140128383 | INHIBITORS OF VIRAL REPLICATION, THEIR PROCESS OF PREPARATION AND THEIR THERAPEUTICAL USES - The present invention relates to compounds, their use in the treatment or the prevention of viral disorders, including HIV. | 05-08-2014 |
20140128384 | TUMOR TARGETED DRUG COMBRETASTATIN A4 DERIVATIVE - The present invention relates to imidazole, oxazole and thiazole derivatives of tumor-targeted drug combretastatin A4, and phosphate esters, sulfonate esters or pharmaceutically acceptable salts, glycoside derivatives, solvates thereof, wherein the A-ring comprises a 3,5-dimethoxyphenyl group having a substituent at the 4-position. The pharmacological activity assays have demonstrated that the compounds of the present invention have good in vitro anti-tumor activity and excellent tubulin inhibitory effect. | 05-08-2014 |
20140135320 | HETEROARYL DERIVATIVES AND USES THEREOF - The present invention relates to antimalarial compounds and their use against protozoa of the genus | 05-15-2014 |
20140148449 | HIGHLY LOADED AMORPHOUS EFAVIRENZ COMPOSITION AND PROCESS FOR PREPARING THE SAME - A stable and high loading ternary solid dispersion composition comprising (a) about 50% wt. to about 90% wt. of amorphous Efavirenz; (b) about 10% wt. to about 50% wt. of polyvinyl pyrrolidone (PVP), a first polymer; (c) about 1% wt. to about 30% wt. of a water-soluble second polymer; and (d) optionally about 0.1% wt. to about 50% wt. of at least one pharmaceutically acceptable excipient. Also discloses a high loading ternary composition comprising (a) a solid dispersion composition comprising (i) about 50% wt. to about 90% wt. of amorphous Efavirenz; (ii) about 10% wt. to about 50% wt. of polyvinyl pyrrolidone, a first polymer; (b) about 1% wt. to about 30% wt. of a water-soluble second polymer blended with solid dispersion of composition of (a); and (c) optionally about 0.1% wt. to about 50% wt. of at least one pharmaceutically acceptable excipient. Additionally discloses a method for preparing solid dosage forms comprising (i) amorphous Efavirenz and (ii) polyvinyl pyrrolidone (PVP), a first polymer; (iii) a water-soluble second polymer; and (iv) optionally, at least one pharmaceutical excipients. | 05-29-2014 |
20140148450 | NOVEL SUBSTITUTED INDOLE DERIVATIVES AS GAMMA SECRETASE MODULATORS - The present invention is concerned with novel substituted indole derivatives of Formula (I) wherein R | 05-29-2014 |
20140155392 | METHODS OF UTILIZING ARYLPIPERAZINE DERIVATIVES - The present invention provides arylpiperazine derivatives which can be advantageously used for treating schizophrenia and related psychoses such as acute manic, bipolar disorder, autistic disorder, and depression. | 06-05-2014 |
20140163023 | DIHYDROPYRROLO PYRIMIDINE DERIVATIVES AS MTOR INHIBITORS - The invention relates to compounds of formula (I) | 06-12-2014 |
20140179693 | METHODS FOR TREATING VASCULAR LEAK SYNDROME - Disclosed are methods for treating Vascular Leak Syndrome. Further disclosed are methods for treating vascular leakage due to inflammatory diseases, inter alia, sepsis, lupus, inflammatory bowel disease. Yet further disclosed are methods for treating renal cell carcinoma and melanoma. Still further disclosed are methods for reducing metastasis of malignant cells and/or preventing the proliferation of carcinoma cells via spreading due to vascular leakage. | 06-26-2014 |
20140179694 | PYRUVATE KINASE ACTIVATORS FOR USE FOR INCREASING LIFETIME OF THE RED BLOOD CELLS AND TREATING ANEMIA - Described herein are methods for using compounds that activate pyruvate kinase. | 06-26-2014 |
20140187542 | AMINO GROUP-CONTAINING PYRROLIDINONE DERIVATIVE - A compound represented by the following formula (I) or a salt thereof: | 07-03-2014 |
20140187543 | HETEROARYL-SUBSTITUTED 1,3-DIHYDROINDOL-2-ONE DERIVATIVES AND MEDICAMENTS CONTAINING THEM - The present invention relates to novel 1,3-dihydroindol-2-one (oxindole) derivatives of the formula (I) | 07-03-2014 |
20140187544 | OXIME-SUBSTITUTED-QUINOXALINE-TYPE PIPERIDINE COMPOUNDS AND USES THEREOF - The present disclosure relates to Oxime-Substituted Quinoxaline-Type Piperidine Compounds, such as those of Formula (I): | 07-03-2014 |
20140206678 | INHIBITORS OF MTOR KINASE AS ANTI -VIRAL AGENT - The present invention provides methods for treating or preventing viral infections using modulators of host cell enzymes relating to mTOR. The invention also provides methods for treating or preventing viral infections using modulators of host cell enzymes relating to mTOR and modulators of the unfolded protein response. | 07-24-2014 |
20140206679 | HETEROCYCLIC PYRIDONE COMPOUND, AND INTERMEDIATE, PREPARATION METHOD AND USE THEREOF - The present invention relates to a heterocyclic pyridone compound represented by General Formula (I), where the heterocyclic pyridone compound is used as a tyrosine kinase inhibitor, and particularly a c-Met inhibitor. The present invention also relates to intermediates for preparing heterocyclic pyridone compound and a preparation method. The present invention further relates to a pharmaceutical composition containing the heterocyclic pyridone compound as an active ingredient, and a use of the pharmaceutical composition in treatment of diseases associated with tyrosine kinase c-Met, especially cancer associated with c-Met, as a medicament. | 07-24-2014 |
20140206680 | SUBSTITUTED 6-AZA-ISOINDOLIN-1-ONE DERIVATIVES - Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein G, p, R | 07-24-2014 |
20140206681 | BTK INHIBITORS - The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula I | 07-24-2014 |
20140213582 | 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. | 07-31-2014 |
20140221364 | TETRAHYDROQUINOLINE ANALOGUES AS MUSCARINIC AGONISTS - The present invention relates to tetrahydroquinoline compounds as muscarinic receptor agonists; compositions comprising the same; methods of inhibiting an activity of a muscarinic receptor with said compounds; methods of treating a disease condition associated with a muscarinic receptor using said compounds; and methods for identifying a subject suitable for treatment using said compounds. | 08-07-2014 |
20140221365 | ALKYLATED PIPERAZINE COMPOUNDS - Alkylated piperazine compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating cancer mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of cancer in mammalian cells, or associated pathological conditions, are disclosed. | 08-07-2014 |
20140235627 | 2-ADRENOCEPTOR AGONIST FOR IMPROVEMENT OF EXERCISE TOLERANCE - This invention relates to the β2-adrenoceptor agonist Olodaterol or a pharmaceutically acceptable salt thereof, | 08-21-2014 |
20140235628 | Inhibitors of the Renal Outer Medullary Potassium Channel - This invention relates to compounds having structural Formula I: | 08-21-2014 |
20140275057 | NOVEL COMPOUNDS AND COMPOSITIONS FOR THE INHIBITION OF NAMPT - The present invention relates to compounds and composition for inhibition of NAMPT, their synthesis, applications and antidotes. An illustrative compound of the invention is shown below. | 09-18-2014 |
20140275058 | PERFLUORINATED CYCLOPROPYL FUSED 1,3-OXAZIN-2-AMINE COMPOUNDS AS BETA-SECRETASE INHIBITORS AND METHODS OF USE - The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: | 09-18-2014 |
20140275059 | 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 |
20140275060 | COMPOUNDS FOR THE TREATMENT OF NEUROLOGIC DISORDERS - Provided are compounds, pharmaceutical compositions and methods of treatment or prophylaxis of certain neurologic disorders, including disorders related to NMDA receptor activity, including neuropsychiatric disorders, neurodegenerative disorders and other neurologic diseases, disorders and conditions including stroke, brain injury, epilepsy, neuropsychiatric disorders, mood disorders, chronic pain and related conditions. | 09-18-2014 |
20140288063 | Heterocyclic Substituted Pyrimidine Compound - The present invention pertains to the field of medical technology, and particularly relates to a heterocyclic substituted pyrimidine compound represented by General Formula (I) and its pharmaceutically acceptable salt thereof, wherein R | 09-25-2014 |
20140288064 | Nitrogen containing heterocyclic compounds - Compounds of Formula (I), their preparation and use in preventing or treating bacterial infections are disclosed. | 09-25-2014 |
20140288065 | N,N-SUBSTITUTED 3-AMINOPYRROLIDINE COMPOUNDS USEFUL AS MONOAMINES REUPTAKE INHIBITORS - The present invention provides a pyrrolidine compound of General Formula (1) | 09-25-2014 |
20140288066 | MORPHOLINO SUBSTITUTED BICYCLIC PYRIMIDINE UREA OR CARBAMATE DERIVATIVES AS MTOR INHIBITORS - The invention relates to compounds of formula (I) | 09-25-2014 |
20140296230 | DIHYDROQUINAZOLINONE ANALOGUES - The present invention encompasses compounds of general formula (I) | 10-02-2014 |
20140303156 | NOVEL (6-OXO-1,6-DIHYDROPYRIMIDIN-2-YL)AMIDE DERIVATIVES, PREPARATION THEREOF AND PHARMACEUTICAL USE THEREOF AS AKT(PKB) PHOSPHORYLATION INHIBITORS - The invention relates to the novel materials of formula (I), where: R1 is an optionally substituted aryl or heteroaryl; R is an H or, when formed with R1, a 5- or 6-member ring fused with an aryl or heretoaryl group optionally containing one or more of O, S, N, NH, and Nalk, being optionally substituted; R2 and R3 are, independently, an H, Hal, or alkyl optionally substituted by one or more Hal; R4 is H; and R5 is an H or alkyl optionally substituted by one or more halogen atoms. Said materials being in any isomeric form and the salts thereof, and are intended for drugs, particularly AKT(PKB) phosphorylation inhibitors. | 10-09-2014 |
20140303157 | METALLOENZYME INHIBITOR COMPOUNDS - The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes. | 10-09-2014 |
20140323475 | EP1 RECEPTOR LIGANDS - The present invention belongs to the field of EP1 receptor ligands. More specifically it refers to compounds of general formula (I) having great affinity and selectivity for the EP1 receptor. The invention also refers to the process for their preparation, to their use as medicament for the treatment and/or prophylaxis of diseases or disorders mediated by the EP1 receptor as well as to pharmaceutical compositions comprising them. | 10-30-2014 |
20140323476 | PEPTIDE DEFORMYLASE INHIBITORS - The present invention relates to {2-(alkyl)-3-[2-(5-fluoro-4-pyrimidinyl)hydrazino]-3-oxopropyl}hydroxyformamide compounds of Formula (I): | 10-30-2014 |
20140350005 | D2 ANTAGONISTS, METHODS OF SYNTHESIS AND METHODS OF USE - Provided are D | 11-27-2014 |
20140350006 | Pyrazolopyridine Derivatives, Preparation Process Therefor And Therapeutic Use Thereof - The invention relates to FGF-inhibiting pyrazolopyrimidine derivatives of general formula (I) to a process for preparing them and to the therapeutic use thereof. | 11-27-2014 |
20140357627 | 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. | 12-04-2014 |
20140357628 | THERAPEUTIC COMPOUNDS - Substituted cinnamoyl anthranilate compounds exhibiting anti-fibrotic activity; or derivatives thereof, analogues thereof, pharmaceutically acceptable salts thereof, and metabolites thereof, with the proviso that the compound is no Tranilast. | 12-04-2014 |
20140357629 | DIAMINOPYRIMIDINES AS P2X3 AND P2X2/3 ANTAGONISTS - Compounds and methods for treating diseases mediated by a P2X | 12-04-2014 |
20140357630 | Phenylacetic Acid Compound - A compound represented by formula (I), | 12-04-2014 |
20140357631 | SUCCINIMIDE COMPOUND - A compound represented by formula (1): | 12-04-2014 |
20140371215 | 1-H-Pyrrolo[2,3-b]Pyridine Derivatives - 1H-Pyrrolo[2,3-b]pyridine compounds are inhibitors of cell proliferation/cell vitality and can be employed for the treatment of tumours. | 12-18-2014 |
20140378445 | METHODS FOR TREATING VASCULAR LEAK SYNDROME - Disclosed are methods for treating Vascular Leak Syndrome. Further disclosed are methods for treating vascular leakage due to inflammatory diseases, inter alia, sepsis, lupus, inflammatory bowel disease. Yet further disclosed are methods for treating renal cell carcinoma and melanoma. Still further disclosed are methods for reducing metastasis of malignant cells and/or preventing the proliferation of carcinoma cells via spreading due to vascular leakage. | 12-25-2014 |
20140378446 | PURINONE COMPOUNDS AS KINASE INHIBITORS - Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. In addition, reversible inhibitors of Btk are also described. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions. | 12-25-2014 |
20150011541 | PIPECOLATE-SULFONAMIDES FOR TREATMENT OF PSYCHIATRIC DISORDERS - The present invention relates to compounds having a pipecolate sulfonamide scaffold, pharmaceutically acceptable salts of these compounds and pharmaceutical compositions containing at least one of these compounds together with pharmaceutically acceptable carrier, excipient and/or diluents. Said pipecolate sulfonamide compounds can be used for prophylaxis and/or treatment of psychiatric disorders and neurodegenerative diseases, disorders and conditions. | 01-08-2015 |
20150038502 | ISOXAZOLOPYRIDINE OREXIN RECEPTOR ANTAGONISTS - The present invention is directed to isoxazolopyndine compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the isoxazolopyndine compounds described herein in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved. | 02-05-2015 |
20150045355 | FUSED TRICYCLIC COMPOUNDS AS RAF KINASE INHIBITORS - Provided are certain fused tricyclic compounds and salts thereof, compositions thereof, and methods of use therefor. | 02-12-2015 |
20150051199 | PHARMACEUTICAL COMPOUNDS - The invention provides compounds that are useful in the treatment of hepatitis C virus (HCV) infections. The compounds have the formula (1): | 02-19-2015 |
20150051200 | GUM RESIN AS A CARRIER FOR TOPICAL APPLICATION OF PHARMACOLOGICALLY ACTIVE AGENTS - Described are pharmacological compositions comprising a gum resin; a pharmacologically active agent and a topically acceptable volatile solvent for the gum resin and active agent. Also described are methods for the transdermal or transmucosal delivery of a pharmacologically active agent using such compositions. | 02-19-2015 |
20150051201 | BICYCLIC PYRAZOLE LRRK2 SMALL MOLECULE INHIBITORS - Compounds of formula I: | 02-19-2015 |
20150057271 | DIHYDROBENZOXAZINE AND TETRAHYDROQUINOXALINE 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 Nav 1.7. 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. | 02-26-2015 |
20150057272 | BENZIMIDAZOLES 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. | 02-26-2015 |
20150065497 | MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS - Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention. | 03-05-2015 |
20150080388 | COMPOUNDS FOR THE TREATMENT OF ISCHEMIA-REPERFUSION-RELATED DISEASES - The present invention relates to compounds of formula (I) useful in the treatment of ischemia-reperfusion-related pathologies. | 03-19-2015 |
20150080389 | HETEROARYL-KETONE FUSED AZADECALIN GLUCOCORTICOID RECEPTOR MODULATORS - The present invention provides heteroaryl ketone fused azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators. | 03-19-2015 |
20150087641 | HETEROCYCLIC CGRP RECEPTOR ANTAGONISTS - The present invention is directed to heterocyclic compounds which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. 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 CGRP is involved. | 03-26-2015 |
20150094302 | ALKYLATED PIPERAZINE COMPOUNDS - Alkylated piperazine compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating cancer mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of cancer in mammalian cells, or associated pathological conditions, are disclosed. | 04-02-2015 |
20150111885 | BROMODOMAIN INHIBITORS - The present invention relates to substituted heterocyclic derivative compounds, compositions comprising said compounds, and the use of said compounds and compositions for epigenetic regulation by inhibition of bromodomain-mediated recognition of acetyl lysine regions of proteins, such as histones. Said compositions and methods are useful for the treatment of cancer and neoplastic disease. | 04-23-2015 |
20150111886 | NOVEL ADAMANTYL DERIVATIVES AS CANNABINOID RECEPTOR 2 AGONISTS - The invention relates to a compound of formula (I) | 04-23-2015 |
20150126503 | SUBSTITUTED NAPHTHYRIDINES AND THEIR USE AS MEDICAMENTS - The invention relates to new substituted naphthyridines of formula 1, as well as pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates or solvates thereof, | 05-07-2015 |
20150126504 | 2,4-Pyrimidinediamine Compounds and Their Uses - The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades. | 05-07-2015 |
20150133440 | DIFLUORO-HEXAHYDRO-CYCLOPENTAOXAZINYLS AND DIFLUORO-HEXAHYDRO-BENZOOXAZINYLS AS BACE1 INHIBITORS - The present invention provides difluoro-cyclopentaoxazinyls and difluoroenzooxazinyls of formula (I) having BACE1 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease. | 05-14-2015 |
20150148340 | BICYCLICALLY SUBSTITUTED URACILS AND THE USE THEREOF - The present application relates to novel bicyclically substituted uracil derivatives, 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. | 05-28-2015 |
20150148341 | OCTAHYDRO FUSED AZADECALIN GLUCOCORTICOID RECEPTOR MODULATORS - The present invention provides octahydro fused azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators. | 05-28-2015 |
20150148342 | BICYCLIC HETEROCYCLES AS BET PROTEIN INHIBITORS - The present invention relates to bicyclic 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. | 05-28-2015 |
20150291521 | PYRROL-1-YL BENZOIC ACID DERIVATIVES USEFUL AS MYC INHIBITORS - The present invention provides compounds of Formula (I-A), (I-B), and (I-C), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting Myc (e.g., c-Myc) activity. The present invention further provides methods of using the compounds described herein for treating Myc-mediated disorders (e.g., cancer and other proliferative diseases). The present invention also provides assays for identifying Myc inhibitors. | 10-15-2015 |
20150291551 | INGENOL-3-ACYLATES III AND INGENOL-3-CARBAMATES - The invention relates to compounds of general formula I | 10-15-2015 |
20150291617 | Thiazole Derivatives as Alpha 7 nAChR Modulators - Disclosed is a compound of formula (I) wherein Y, Ring D, m and R | 10-15-2015 |
20150299189 | NOVEL AMINE DERIVATIVE OR SALT THEREOF - A novel amine derivative expressed by general formula (1) | 10-22-2015 |
20150307493 | 1H-PYRROLO[2,3-c]PYRIDIN-7(6H)-ONES AND PYRAZOLO[3,4-c]PYRIDIN-7(6H)-ONES AS INHIBITORS OF BET PROTEINS - The present invention relates to substituted pyrrolopyridinones and substituted pyrazolopyridinones 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. | 10-29-2015 |
20150328229 | COMPOSITIONS AND METHODS FOR TREATING OPHTHALMIC, OCTIC, OR NASAL INFECTIONS - The present invention relates to methods for treating an ophthalmic, otic, or nasal infection comprising treating the infected tissue with a composition comprising finafloxacin or a finafloxacin derivative. The present invention also relates to antimicrobial compositions comprising finafloxacin or a finafloxacin derivative. The compositions are suitable for the treatment of ophthalmic, otic, or nasal infections. | 11-19-2015 |
20150329532 | 2,4-PYRIMIDINEDIAMINE COMPOUNDS AND THEIR USES - The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades. | 11-19-2015 |
20150336983 | ANTIMICROBIAL COMPOUNDS - Provided are compounds which are useful for controlling microorganisms in aqueous or water-containing systems or in systems which are exposed to moisture, including at elevated temperature. The antimicrobial compounds are of the formula I: | 11-26-2015 |
20150344463 | PRMT5 INHIBITORS AND USES THEREOF - Described herein are compounds of Formula (A), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described. | 12-03-2015 |
20150344465 | PYRIDINE COMPOUNDS AS SODIUM CHANNEL BLOCKERS - The invention relates to substituted pyridine compounds of Formula I: (I) or a pharmaceutically acceptable salt, prodrug, or solvate thereof, wherein A | 12-03-2015 |
20150344471 | COMPOUNDS AND COMPOSITIONS FOR THE TREATMENT OF PARASITIC DISEASES - The present invention provides compounds of formula I: | 12-03-2015 |
20150344479 | NOVEL HETEROCYCLIC DERIVATIVES - The invention relates to novel heterocyclic compounds of the formula | 12-03-2015 |
20150361053 | 2 AMINO-3,4-DIHYDRCQUINAZOLINE DERIVATIVES AND THE USE THEREOF AS CATHEPSIN D INHIBITORS - The present invention relates to compounds of the formula (I) and in particular to medicaments comprising at least one compound of the formula (I) for use in the treatment and/or prophylaxis of physiological and/or pathophysiological conditions in the triggering of which cathepsin D is involved, in particular for use in the treatment and/or prophylaxis of osteoarthritis, traumatic cartilage injuries, arthritis, pain, allodynia or hyperalgesia. | 12-17-2015 |
20150361079 | Spiro-Quinazolinone Derivatives and their Use as Positive Allosteric Modulators of mGluR4 - The present invention relates to novel spiro-quinazolinone derivatives as positive allosteric modulators for modulating metabotropic glutamate receptor subtype 4 (mGluR4) and/or altering glutamate level or glutamatergic signalling. | 12-17-2015 |
20150366871 | Increased Dosage of Efavirenz for the Treatment of Cancer - The invention is based on the finding that an increased daily dose of Efavirenz should be used for the treatment of cancer compared to the daily dose used in the treatment of AIDS. The invention thus relates to the use of Efavirenz for preparing a medicament intended for the treatment of cancer, wherein Efavirenz is administered at a dose generating an Efavirenz plasma concentration in said patient superior to 3000 ng/ml. It further relates to the use of Efavirenz for preparing a medicament intended for the treatment of cancer, wherein Efavirenz is administered at a daily dose of at least 1800 mg, in particular between 1800 and 2200 mg. It also relates to the use of Efavirenz for preparing a medicament intended for the treatment of cancer, in which the daily dose of Efavirenz is optimized after administration of a preliminary daily dose and measure or Efavirenz plasma concentration. It also relates to a unique dosage form of Efavirenz, comprising Efavirenz in an amount generating an Efavirenz plasma concentration in said patient superior to 3000 ng/ml, and a pharmaceutically acceptable carrier. | 12-24-2015 |
20150366977 | PHARMACEUTICAL COMPOSITIONS COMPRISING NITROXYL DONORS - The present disclosure provides nitroxyl donating pharmaceutical compositions comprising N-substituted hydroxylamine derivatives. The compositions are highly efficacious in treating cardiovascular diseases (e.g., heart failure), have a suitable toxicological profile, and are sufficiently stable for intravenous or oral administration. | 12-24-2015 |
20150368241 | INHIBITORS OF HEMEPROTEIN-CATALYZED LIPID PEROXIDATION - Compounds, compositions and methods related to the prevention or treatment of isoprostane-mediated tissue damage in a mammalian subject in need thereof. | 12-24-2015 |
20150368273 | IMIDAZO PYRIDINE COMPOUNDS - The present invention provides compounds of the formula I, wherein X is a bond or CH | 12-24-2015 |
20150368274 | Pyridopyrimidine Or Pyrimidopyrimidine Compound, Prepration Method, Pharmaceutical Composition, And Use Thereof - The present invention belongs to the field of pharmaceutical Chemistry. In particular, the present invention relates to a pyridopyrimidine or pyrimidopyrimidine compound as represented by general formula (I), or an isomer thereof or a pharmaceutically acceptable salt, ester, prodrug or solvate thereof, a preparation method, a pharmaceutical composition and uses thereof in preparing a mTOR inhibitor. As a mTOR inhibitor, the compound or the pharmaceutical composition thereof can be used for treating a disease or condition due to PI3K-AKT-mTOR signalling pathway malfunction. | 12-24-2015 |
20150376170 | BENZOXAZINONE AMIDES AS MINERALOCORTICOID RECEPTOR MODULATORS - Disclosed are certain derivatives of benzoxazinone amides of formula (I), or pharmaceutically acceptable salts thereof, | 12-31-2015 |
20150376205 | 1-ARYLCARBONYL-4-OXY-PIPERIDINE COMPOUNDS USEFUL FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES - The present invention provides a compound useful as an agent for the prophylaxis or treatment of neurodegenerative disease and the like, or a salt thereof. The present invention relates to a compound represented by the formula (I) wherein each symbol is as defined in the specification, or a salt thereof. | 12-31-2015 |
20160009712 | IMIDAZOPYRIDINES AND IMIDAZOPYRAZINES AS LSD1 INHIBITORS | 01-14-2016 |
20160016908 | 2,3-DISUBSTITUTED 1 -ACYL-4-AMINO-1,2,3,4-TETRAHYDROQUINOLINE DERIVATIVES AND THEIR USE AS BROMODOMAIN INHIBITORS - The present invention relates to novel compounds, pharmaceutical compositions containing such compounds and to their use in therapy. | 01-21-2016 |
20160016952 | SUBSTITUTED AMINO-PYRIMIDINE DERIVATIVES - The present application provides novel substituted quinazoline and pyrido-pyrimidine compounds and pharmaceutically acceptable salts, prodrugs, and solvates thereof. Also provided are methods for preparing these compounds. These compounds are useful in co-regulating PI3K and/or mTOR activity by administering a therapeutically effective amount of one or more of the compounds to a patient. By doing so, these compounds are effective in treating conditions associated with the dysregulation of the PI3K/AKT/mTOR pathway. Advantageously, these compounds perform as dual PI3K/mTOR inhibitors. A variety of conditions can be treated using these compounds and include diseases which are characterized by inflammation or abnormal cellular proliferation. In one embodiment, the disease is cancer. | 01-21-2016 |
20160024007 | OCTAHYDROCYCLOPENTAPYRROLES, THEIR PREPARATION AND USE - The present invention provides Octahydrocyclopentapyrrole compounds having the structure: (structurally represented) wherein psi is absent or present, and when present is a bond; R1, R2, R3, R4, and R5 are each independently H, halogen, CF, or C1-C4 alkyl; R6 is absent or present, and when present is H, OH, or halogen; A is absent or present, and when present is C(O) or C(O)NH; B is substituted or unsubstituted monocycle, bicycle, heteromonocycle, heterobicycle, benzyl, CO2H or (C1-C4 alkyl)-CO2H, wherein when B is CO2H, then A is present and is C(O); and when psi is present, then R6 is absent and when psi is absent, then R6 is present, or a pharmaceutically acceptable salt thereof, for treatment of diseases characterized by excessive lipofuscin accumulation in the retina. | 01-28-2016 |
20160024077 | INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION - The disclosure generally relates to compounds of formula (I), including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection. | 01-28-2016 |
20160031838 | SMYD2 INHIBITORS - The present disclosure generally relates to compounds having cellular anti-proliferative activities, and more particularly relates to compounds which inhibit the activity of human SMYD2, a SET and MYND domain-containing protein lysine methyltransferase. | 02-04-2016 |
20160039745 | HISTONE DEACETYLASE INHIBITORS AND COMPOSITIONS AND METHODS OF USE THEREOF - Provided are certain histone deacetylase (HDAC) inhibitors of Formula I, compositions thereof, and methods of their use. | 02-11-2016 |
20160039788 | DEOXYURIDINE TRIPHOSPHATASE INHIBITORS - Provided herein are dUTPase inhibitors, compositions comprising such compounds and methods of using such compounds and compositions. | 02-11-2016 |
20160046649 | N-ALKYL-2-PHENOXYETHANAMINES, THEIR PREPARATION AND USE - The present invention provides a compound having the structure: (structurally represented) wherein R1, R2, R3, R4, and R5 are each independently H, halogen, CF3 or C1-C4 alkyl; R6 is alkyl; A is absent or present, and when present is —C(O)— or —C(O)NH—; B is substituted or unsubstituted monocycle, bicycle, heteromonocycle, heterobicycle, benzyl, CO2H or (C1-C4 alkyl)-CO2H, wherein when B is CO2H, then A is present and is —C(O)—, or a pharmaceutically acceptable salt thereof. | 02-18-2016 |
20160052922 | 1-PHENOXY-3-(ALKYLAMINO)-PROPAN-2-OL DERIVATIVES AS CARM1 INHIBITORS AND USES THEREOF - Provided herein are compounds of Formula (I): and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein X, R | 02-25-2016 |
20160058770 | USE OF SUBSTITUTED 2,3-DIHYDROIMIDAZO[1,2-C]QUINAZOLINES FOR TREATING LYMPHOMAS - —use of a 2,3-dihydroimidazo[1,2-c]quinazoline compound, or of a pharmaceutical composition containing same, as a sole active agent, or of a combination of a) said compound or a pharmaceutical composition containing said compound and b) one or more further active agents, for the preparation of a medicament for the treatment or prophylaxis of non-Hodgkin's lymphoma (NHL), particularly 1st line, 2nd line, relapsed, refractory, indolent or aggressive non-Hodgkin's lymphoma (NHL), in particular follicular lymphoma (FL), chronic lymphocytic leukaemia (CLL), marginal zone lymphoma (MZL), diffuse large B-cell lymphoma (DLBCL), mantle cell lymphoma (MCL), transformed lymphoma (TL), or peripheral T-cell lymphoma (PTCL); —combinations of a) said compound and b) one or more further active agents; —a pharmaceutical composition comprising said compound as a sole active agent for the treatment of non-Hodgkin's lymphoma (NHL), particularly 1st line, 2nd line, relapsed, refractory, indolent or aggressive non-Hodgkin's lymphoma (NHL), in particular follicular lymphoma (FL), chronic lymphocytic leukaemia (CLL), marginal zone lymphoma (MZL), diffuse large B-cell lymphoma (DLBCL), mantle cell lymphoma (MCL), transformed lymphoma (TL), or peripheral T-cell lymphoma (PTCL); —a pharmaceutical composition comprising a combination of a) said compound and b) one or more further active agents; —use of biomarkers involved in the modification of the expression of PI3K isoforms, BTK and IKK, BCR activation, BCR downstream activation of NFKB pathway, c-Myc, EZH2, for predicting the sensitivity and/or resistance of a cancer patient to said compound and providing a rationale-based synergistic combination as defined herein to increase sensitivity and/or to overcome resistance; and —a method of determining the level of a component of one or more of the expression of PI3K isoforms, BTK and IKK, BCR activation, BCR downstream activation of NFKB pathway, c-Myc, EZH2. | 03-03-2016 |
20160067256 | Inhibitors of Hemeprotein-Catalyzed Lipid Peroxidation - Methods and compounds for the treatment or prevention of oxidative damage in a mammalian subject. The treatment and/or prevention may be on inhibiting heme-induced lipid peroxidation. Also discloses are methods and compounds for treating or preventing isoprostane-mediated tissue damage. | 03-10-2016 |
20160074410 | Beta2-ADRENOCEPTOR AGONIST FOR THE TREATMENT OF COUGH - This invention relates to the β2-adrenoceptor agonist Olodaterol or a pharmaceutically acceptable salt thereof, | 03-17-2016 |
20160083383 | Novel 6-fused heteroaryldihydropyrimidines for the treatment and prophylaxis of hepatitis B virus infection - The invention provides novel compounds having the general formula: | 03-24-2016 |
20160083401 | ARYLQUINAZOLINES - The invention relates to novel compounds of the formula (I) which can be used for the inhibition of serine-threonine protein kinases and for the sensitisation of cancer cells to anticancer agents and/or ionising radiation. | 03-24-2016 |
20160089377 | THERAPEUTIC TARGETING OF THE MTOR PATHWAY IN NEURODEVELOPMENTAL AND NEUROPSYCHIATRIC DISEASE - The present invention relates to methods of treating various neurodevelopmental and neuropsychiatric diseases which employ inhibition of the mTOR pathway, particularly using mTOR kinase inhibitors. It is based, at least in part, on extensive phenotypic characterization of a knock-out mouse model of Caspr2, the murine ortholog of CNTNAP2, which indicate that the mechanism via which CNTNAP2 deficits lead to neuropsychiatric disorders is overactivation of the mTOR pathway. Accordingly, the present invention provides for methods of treating subjects suffering from neurodevelopmental and/or neuropsychiatric disorders comprising administering, to the subject, an agent that inhibits the mTOR pathway. In particular non-limiting embodiments, the inhibitor of the mTOR pathway is a mTOR kinase inhibitor such as, but not limited to, WYE125132 and analogous compounds. In a non-limiting subset of embodiments, subjects may be tested to determine whether they have a copy number variation or mutation in CNTNAP2 and where such a copy number variation or mutation is present treatment with a mTOR pathway inhibitor may be initiated. | 03-31-2016 |
20160106753 | Dihydro-Benzo-Oxazine and Dihydro-Pyrido-Oxazine Derivatives - The invention relates to dihydro-benzo-oxazine and dihydro-pyrido-oxazine compounds of the formula (I) and/or pharmaceutically acceptable salts and/or solvates thereof, | 04-21-2016 |
20160136172 | SUBSTITUTED BENZOFURAN COMPOUNDS AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES - 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. | 05-19-2016 |
20160137631 | PRMT5 INHIBITORS AND USES THEREOF - Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described. | 05-19-2016 |
20160143915 | NEW CYCLOHEXYLAMINE DERIVATIVES HAVING 2 ADRENERGIC AGONIST AND M3 MUSCARINIC ANTAGONIST ACTIVITIES - The present invention relates to novel compounds having β2 adrenergic agonist and M3 muscarinic antagonist dual activity, to pharmaceutical compositions containing them, to the process for their preparation and to their use in respiratory therapies. | 05-26-2016 |
20160145267 | HETEROARYL SUBSTITUTED PYRAZOLES - Compounds of formula (I), which are inhibitors of Bub1 kinase, processes for their production and their use as pharmaceuticals. | 05-26-2016 |
20160145268 | SUBSTITUTED HETEROCYCLIC COMPOUNDS AS CRAC MODULATORS - The invention relates to compounds of Formula (I) and their pharmaceutically acceptable salts, wherein the substituents are as described herein, and their use in medicine for the treatment of diseases, disorders associated with the modulation of calcium release-activated calcium (CRAC) channel. The invention also relates to pharmaceutical compositions containing such compounds in treating diseases disorders associated with calcium release-activated calcium (CRAC) channel modulators. wherein, ring D is Formula (a) or Formula (b): A and B, which may be same or different, are independently CR | 05-26-2016 |
20160158229 | Mixtures of Heteropolycycles - A mixture of heteropolycycles has preferably two particular heteropolycycles and more preferably, no more than 10 wt. %, 5 wt. %, 2.5 wt. %, 1 wt. %, 0.5 wt. %, 0.1 wt. %, 0.01 wt. %, 0.001 wt. %, or no more than a detectable amount of one of the two. | 06-09-2016 |
20160159757 | OXAZINE DERIVATIVES - The present invention provides, for example, a compound mentioned below as a medicament for treating or preventing the diseases induced by production, secretion or deposition of amyloid-β proteins.
| 06-09-2016 |
20160159820 | FUSED TRICYCLIC AMIDE COMPOUNDS AS MULTIPLE KINASE INHIBITORS - Provided are fused tricyclic amide compounds, pharmaceutical compositions comprising at least one such fused tricyclic compound, processes for the preparation thereof, and the use thereof in therapy. Disclosed herein are certain tricyclic amide compounds that can be useful for inhibiting multiple (specifically BRAF and/or EGFR-T790M) kinases and for treating disorders mediated thereby. | 06-09-2016 |
20160168123 | INHIBITORS OF PLASMA KALLIKREIN | 06-16-2016 |
20160193214 | SMALL MOLECULES TO ENHANCE P53 ACTIVITY | 07-07-2016 |
20160251373 | 5-HT3 RECEPTOR ANTAGONISTS | 09-01-2016 |
20170231998 | Pyrazolopyridine Derivatives, Preparation Process Therefor And Therapeutic Use Thereof | 08-17-2017 |
20170233391 | FUSED TRICYCLIC UREA COMPOUNDS AS RAF KINASE AND/OR RAF KINASE DIMER INHIBITORS | 08-17-2017 |
20170233406 | CRYSTALLINE FORM OF 1-(1-METHYL-1H-PYRAZOL-4-YL)-N-((1R,5S,7S)-9-METHYL-3-OXA-9-AZABICYCLO[3.- 3.1]NONAN-7-YL)-1H-INDOLE-3-CARBOXAMIDE | 08-17-2017 |
20190142838 | METHODS FOR TREATING PARKINSON'S DISEASE | 05-16-2019 |
20190144446 | FUSED TRICYCLIC UREA COMPOUNDS AS RAF KINASE AND/OR RAF KINASE DIMER INHIBITORS | 05-16-2019 |
20190144467 | ANTI-FIBROTIC PYRIDINONES | 05-16-2019 |