Entries |
Document | Title | Date |
20080207611 | Pharmaceutical compounds - Fused pyrimidines of formula (I): | 08-28-2008 |
20080214541 | COMPOSITIONS AND METHODS FOR INDUCING OSTEOGENESIS - The present invention provides compositions and methods for differentiating and transdifferentiating mammalian cells into cells of an osteoblast lineage. | 09-04-2008 |
20080221097 | Imidazopyridine Derivatives as Cannabinoid Receptor Ligands - The present invention relates to novel imidazopyridine derivatives, pharmaceutical compositions containing these compounds and their use in the treatment of diseases, particularly pain, which diseases are caused directly or indirectly by an increase or decrease in activity of the cannabinoid receptor. | 09-11-2008 |
20080221098 | COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS - The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, BCR-Abl, Bmx, c-Raf, Csk, Fes, FGFR, Flt3, Ikk, IR, JNK, Lck, Mkk, PKC, PKD, Rsk, SAPK, Syk, Trk, BTK, Src, EGFR, IGF, Mek, Ros and Tie2 kinases. | 09-11-2008 |
20080221099 | DIHYDROPTERIDINONES FOR THE TREATMENT OF CANCER DISEASES - Disclosed is the use of a compound of general Formula (1), | 09-11-2008 |
20080227777 | Pyrazolopyridine derivatives as inhibitors of beta-Adrenergic Receptor Kinase 1 - The invention relates to 6-amido substituted pyrazolopyridine derivatives of the formula (I) | 09-18-2008 |
20080234261 | Preparation of 1,6-Disubstituted Azabenzimidazoles as Kinase Inhibitors - Novel inhibitors of Rho-kinases are disclosed. | 09-25-2008 |
20080234262 | PYRAZOLOPYRIMIDINE ANALOGS AND THEIR USE AS MTOR KINASE AND PI3 KINASE INHIBITORS - The present invention relates to Pyrazolopyrimidine Analogs, methods of making Pyrazolopyrimidine Analogs, compositions comprising a Pyrazolopyrimidine Analog, and methods for treating mTOR-related disorders comprising administering to a subject in need thereof an effective amount of a Pyrazolopyrimidine Analog. The invention also relates to treating PI3K-related disorders comprising administering to a subject in need thereof an effective amount of a Pyrazolopyrimidine Analog. | 09-25-2008 |
20080242665 | PHOSPHOINOSITIDE 3-KINASE INHIBITOR COMPOUNDS AND METHODS OF USE - Compounds of Formulas Ia-d where X is S or O, mor is a morpholine group, and R | 10-02-2008 |
20080249089 | 8-[3-AMINO-PIPERIDIN-1-YL]-XANTHINES, THE PREPARATION THEREOF AND THEIR USE AS PHARMACEUTICAL COMPOSITIONS - The present invention relates to substituted xanthines of general formula | 10-09-2008 |
20080261972 | Cgrp Receptor Antagonists - Compounds of Formula (I), (where variables R | 10-23-2008 |
20080261973 | Sulphonamidoaniline Derivatives Being Janus Kinase Inhibitors - The invention relates to sulphonamidoanilines of formula I, | 10-23-2008 |
20080269210 | PHOSPHOINOSITIDE 3-KINASE INHIBITOR COMPOUNDS AND METHODS OF USE - Compounds of Formulas Ia-d where X is S or O, mor is a morpholine group, and R | 10-30-2008 |
20080275037 | 2-Cyanophenyl fused heterocyclic compounds, and compositions and uses thereof - Fused heterocyclic compounds are provided according to formula 1: | 11-06-2008 |
20080275038 | Imidazopyridine Derivatives as A2b Adenosine Receptor Antagonists - The present disclosure relates to imidazopyridine derivatives of formula (I): | 11-06-2008 |
20080293714 | Tec Kinase Inhibitors - Disclosed are compounds of formula (I): (F) wherein Ri, R2, X and Ar are defined herein. The compounds of the invention inhibit Itk kinase and are therefore useful for treating diseases and pathological conditions involving inflammation, immunological disorders and allergic disorders. Also disclosed are processes for preparing these compounds and to pharmaceutical compositions comprising these compounds. | 11-27-2008 |
20080300246 | Compounds and Compositions as Protein Kinase Inhibitors - The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, Bcr-Abl, BMX, BTK, CHK2, b-RAF, c-RAF, CSK, c-SRC, Fes, FGFR3, Flt3, IKKα, IKKβ, JNK2α 2, Lck, Met, MKK4, MKK6, MST2, NEK2, p70S6K, PDGFRβ, PKA, PKBα, PKD2, Rsk1, SAPK2α, SAPK2β, SAPK3, SGK, Tie2 and TrkB kinases. | 12-04-2008 |
20080306063 | PHENYLAMINO ISOTHIAZOLE CARBOXAMIDINES AS MEK INHIBITORS - The invention concerns compounds which inhibit MEK and which have activity as anti-neoplastic agents. These compounds include N-substituted-3-hydroxy-5-arylamino-isothiazole-4-carboxamidines. Also included are the tautomeric isothiazol-3(2H)-ones. | 12-11-2008 |
20080312227 | Substituted Pyrido(2,3-D) Pyrimidine Derivatives Useful as Medicines for the Treatment of Autoimmune Disorders - This invention relates to a group of trisubstituted pyrido(2,3-d)pyrimidine derivatives, their pharmaceutically acceptable salts, N-oxides, solvates and enantiomers, possessing unexpectedly desirable pharmaceutical properties, in particular which are highly active immunosuppressive agents, and as such are useful in the treatment in transplant rejection and/or in the treatment of certain inflammatory diseases. These derivatives are also useful in preventing or treating cardiovascular disorders, disorders of the central nervous system, TNF-α related disorders and cell proliferative disorders. | 12-18-2008 |
20080312228 | PYRIMIDINE COMPOUND AND MEDICAL USE THEREOF - The present invention relates to a pyrimidine compound or a pharmaceutically acceptable salt thereof represented by the following formula [I] | 12-18-2008 |
20080318947 | Inhibitors of Akt Activity - Invented are novel 1H-imidazo[4,5-c]pyridin-2-yl compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis. | 12-25-2008 |
20080318948 | Organic Compounds - The present invention provides compounds of the formula | 12-25-2008 |
20080318949 | Pyrazolopyrimidinone Derivatives, Their Preparation And Their Use - The invention discloses a series of pyrazolopyrimidinone derivatives, which have the following chemical structure, their preparation methods and use, | 12-25-2008 |
20090005376 | 1-Alkoxy 1H-Imidazo Ring Systems and Methods - Imidazo-containing compounds (e.g., imidazonaphthyridines, imidazopyridines, imidazoquinolines, and imidazote-trahydroquinolines) with an alkoxy substituent at the 1-position, pharmaceutical compositions containing the compounds and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed. | 01-01-2009 |
20090005377 | Pyrazolopyridine Derivates - New compounds of formula (I) and the salts thereof, wherein the meanings for the various substituents are as disclosed in the description, are useful as p38 kinase inhibitors. | 01-01-2009 |
20090018129 | SUBSTITUTED AMINOPYRAZOLOPYRIDINES AND SALTS THEREOF, PHARMACEUTICAL COMPOSITIONS COMPRISING SAME, METHODS OF PREPARING SAME AND USES OF SAME - The invention relates to substituted aminopyrazolopyridines according to the general formula (I): | 01-15-2009 |
20090023723 | Purinone derivatives for treating neurodegenerative diseases - The invention relates to purinone derivatives useful in treating disorders that are mediated by adenosine receptor function, including neurodegenerative diseases and inflammation. The compounds are of the general formula: | 01-22-2009 |
20090023724 | Heteroaryl compounds, compositions thereof, and methods of treatment therewith - Provided herein are Heteroaryl Compounds having the following structure: | 01-22-2009 |
20090029988 | Hydroxyalkyl Substituted Imidazoquinolines - Certain imidazoquinolines with a hydroxymethyl or hydroxyethyl substituent at the 2-position, pharmaceutical compositions containing the compounds, intermediates, methods of making and methods of use of these compounds as immunomodulators, for preferentially inducing IFN-α biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed. | 01-29-2009 |
20090029989 | SUBSTITUTED PYRAZOLOPYRIMIDINES - Pyrazolo-pyrimidine derivatives are described herein. The described invention also includes methods of making such derivatives as well as methods of using the same in the treatment of diseases. | 01-29-2009 |
20090029990 | Dihydropteridinones in the treatment of respiratory diseases - The present invention relates to the use of dihydropteridinones of formula 1 | 01-29-2009 |
20090029991 | BENZAMIDE DERIVATIVES USEFUL AS HISTONE DEACETYLASE INHIBITORS - The invention concerns a compound of the formula (I) | 01-29-2009 |
20090036445 | KINASE INHIBITORS - The present invention provides kinase inhibitors of Formula I. | 02-05-2009 |
20090042878 | THIENOPYRIMIDYLAMINES AS MODULATORS OF THE EP2 RECEPTOR - The present invention relates to thienopyrimidylamines of the general formula I, to processes for their preparation and to their use for production of pharmaceutical compositions for treatment of disorders and indications connected to the EP | 02-12-2009 |
20090048249 | 3-benzoimidazolyl-pyrazolopyridines useful in treating kinase disorders - The present invention is directed to novel 3-benzoimidazolyl-pyrazolopyridine compounds of formula (I): | 02-19-2009 |
20090062273 | 3-H-pyrazolopyridines and salts thereof, pharmaceutical compositions comprising same, methods of preparing same and uses of same. - The invention relates to 3-H-pyrazolopyridines according to the general formula (I): | 03-05-2009 |
20090062274 | Pyridopyrimidinone inhibitors of pi3kalpha - The invention is directed to Compounds of Formula I and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds. | 03-05-2009 |
20090062275 | N-Substituted Imidazopyridine c-Kit Inhibitors - Compounds represented by Formula (I): | 03-05-2009 |
20090062276 | PYRIDOPYRIMIDINE PROTEIN TYROSINE PHOSPHATASE INHIBITORS - The present invention comprises pyridopyrimidinediamine compounds of the general formula I: | 03-05-2009 |
20090069318 | Novel Compounds - Novel substituted 2,4,8-trisubstituted 8H-pyrido[2,3-d]pyrimidin-7-one containing compounds and compositions, and their use in therapy as CSBP/RK/p38 kinase inhibitors. | 03-12-2009 |
20090069319 | IMIDAZOPYRIDINE ANALOGS AND THEIR USE AS AGONISTS OF THE WNT-BETA-CATENIN CELLULAR MESSAGING SYSTEM - The present invention relates to imidazopyridine analogs, methods of making imidazopyridine analogs, compositions comprising an imidazopyridine analog, and methods for treating canonical Wnt-β-catenin cellular messaging system-related disorders comprising administering to a subject in need thereof an effective amount of an imidazopyridine analog. | 03-12-2009 |
20090076001 | Substituted 4,5,6,7 -Tetrahydro-Isoxazolo[4,5-C]Pyridine Compounds and Use Thereof for Producing Medicaments - The present invention relates to substituted 4,5,6,7-tetrahydro-isoxazolo[4,5-c]pyridine compound corresponding to formula I, methods for producing them, to medicaments containing these compounds, the use of these compounds for producing medicaments and related treatment methods | 03-19-2009 |
20090076002 | NOVEL AMINO ALCOHOL-SUBSTITUTED ARYLTHIENOPYRIMIDINONES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS MEDICAMENTS - The invention relates to amino alcohol-substituted arylthienopyrimidinones and their derivatives, and their physiologically tolerated salts and physiologically functional derivatives, their preparation, medicaments comprising at least one amino alcohol-substituted arylthienopyrimidinone of the invention or its derivative, and the use of the amino alcohol-substituted arylthienopyrimidinones of the invention and their derivatives as MCH antagonists. | 03-19-2009 |
20090082346 | Substituted Pyrrolo-Pyrazole Derivatives as Kinase Inhibitors - Compounds represented by formula (Ia) or (Ib) and wherein R and R | 03-26-2009 |
20090082347 | PYRROLO[3,2-D]PYRIMIDINES THAT ARE SELECTIVE ANTAGONISTS OF A2B ADENOSINE RECEPTORS - The present invention provides compounds of the following formula and pharmaceutical compositions that are selective antagonists of A | 03-26-2009 |
20090093477 | TETRAHYDROPYRROLOPYRIMIDINEDIONES AND THEIR USE IN THERAPY - Compounds of formula (I) and multimers thereof are inhibitors of human neutrophil elastase activity, and of utility in the treatment of, e.g., COPD: | 04-09-2009 |
20090099170 | Sirtuin modulating compounds - 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. | 04-16-2009 |
20090099171 | Diazaquinolones that inhibit prolyl hydroxylase activity - Compounds of Formula I are useful inhibitors of HIF prolyl hydroxylases. Compounds of Formula I have the following structure: | 04-16-2009 |
20090099172 | 6-PHENYL-1H-IMIDAZO[4,5-c]PYRIDINE-4-CARBONITRILE DERIVATIVES - The present invention relates to 6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives having the general Formula I | 04-16-2009 |
20090099173 | Pyridopyridazine compounds, compositions and methods of use - The present invention relates generally to compounds represented in Formula I, pharmaceutical compositions comprising them and methods of treating of diseases or disorders such as cancer. | 04-16-2009 |
20090099174 | COMBINATION 059 - This invention relates to a combination product, as defined herein, comprising a MEK inhibitor and a mTOR-selective inhibitor, and to methods for the production of an anti-cancer effect in a patient, which is accordingly useful in the treatment of cancer in a patient. More specifically the present invention relates to; a combination product, as defined herein, comprising a MEK inhibitor and a mTOR-selective inhibitor; a combination product, as defined herein, comprising a kit of parts comprising a MEK inhibitor and a mTOR-selective inhibitor; use of the combination product, as defined herein, in the treatment of cancer; a method of treating cancer comprising administering the combination product, as defined herein, to a patient. The combination product, as defined herein, and methods of the invention are also useful in the treatment of other diseases associated with the activity of MEK, and/or mTOR. | 04-16-2009 |
20090105246 | Sirtuin modulating compounds - 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. | 04-23-2009 |
20090111805 | BICYCLIC HETEROAROMATIC DERIVATIVES USEFUL AS ANTICANCER AGENTS - The invention relates to compounds of the formula I: | 04-30-2009 |
20090118273 | Compounds and Compositions as Protein Kinase Inhibitors - The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of Abl, Bcr-Abl, Bmx, BTK, b-RAF, c RAF, CSK, cSRC, Fes, FGFR3, Flt3, IKKα, IKKβ, JNK1α1, JNK2α2, Lck, Met, MKK4, MKK6, p70S6K, PAK2, PDGFRα, PKA, PKCα, PKD2, ROCK-II, Ros, Rsk1, SAPK2α, SAPK2β, SAPK3, SAPK4, SGK, Syk, Tie2 and TrkB kinases. | 05-07-2009 |
20090118274 | MONOCYCLIC AMINOPROPYL TETRAHYDRO-PYRAZOLO-PYRIDINE MODULATORS OF CATHEPSIN S - Monocyclic aminopropyl tetrahydro-pyrazolo-pyridine compounds are described, which are useful as cathepsin S modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by cathepsin S activity, such as psoriasis, pain, multiple sclerosis, atherosclerosis, and rheumatoid arthritis. | 05-07-2009 |
20090118275 | THIAZOLOPYRIMIDINE P13K INHIBITOR COMPOUNDS AND METHODS OF USE - Compounds of Formulas Ia and Ib, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia and Ib for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. | 05-07-2009 |
20090118276 | THIENOPYRIMIDINES, THIENOPYRIDINES, AND PYRROLOPYRIMIDINES AS B-RAF INHIBITORS - The present invention relates to compounds of formula la: | 05-07-2009 |
20090118277 | 3 Unsubstituted N-(aryl- or heteroaryl)-pyrazolo[1,5-a]pyrimidines as Kinase Inhibitors - The invention relates to 3-unsubstituted N-(aryl- or heteroaryl)-pyrazolo[1,5-a]pyrimidine compounds, their use as kinase inhibitors, new pharmaceutical formulations comprising said compounds, said compounds for use in the diagnostic or therapeutic treatment of warm-blooded animals, especially humans, their use in the treatment of diseases or for the manufacture of pharmaceutical formulations useful in the treatment of diseases that respond to modulation of kinase, especially tie-2 kinase, activity, methods of treatment comprising administration of said compounds to a warm-blooded animal, especially a human, and processes for the manufacture of said compounds. | 05-07-2009 |
20090118278 | COMPOSITIONS USEFUL AS INHIBITORS OF GSK-3 - The present invention provides a compound of formula I: | 05-07-2009 |
20090124614 | HYDROXY ALKYL SUBSTITUTED 1,3,8-TRIAZASPIRO[4.5]DECAN-4-ONE DERIVATIVES USEFUL FOR THE TREATMENT OF ORL-1 RECEPTOR MEDIATED DISORDERS - The present invention is directed to novel hydroxy alkyl substituted 1,3,8-triazaspiro[4.5]decan-4-one derivatives of the general formula | 05-14-2009 |
20090131429 | Pharmaceutical compounds - Fused pyrimidines of formula (I): | 05-21-2009 |
20090131430 | PYRIDO'2,3-DIPYRIMIDINES AS ANTI-INFLAMMATORY AGENTS - The present invention relates to novel azabicyclo derivatives as anti-inflammatory agents. The compounds provided herein can be useful for inhibition and prevention of inflammation and associated pathologies including inflammatory and autoimmune diseases such as sepsis, rheumatoid arthritis, inflammatory bowel disease, type-1 diabetes, asthma, chronic obstructive pulmonary disorder, organ transplant rejection and psoriasis. Also provided herein are pharmacological compositions containing compounds provided herein and associated methods of treating sepsis, rheumatoid arthritis, inflammatory bowel disease, type-1 diabetes, asthma, chronic obstructive pulmonary disorder, organ transplant rejection and psoriasis, and other inflammatory and/or autoimmune disorders, using the compounds. | 05-21-2009 |
20090131431 | Pyrazolo[3,4-b]pyridine compounds, and their use as a PDE4 inhibitors - The invention provides a compound of formula (I) or a salt thereof: | 05-21-2009 |
20090137580 | Fused Heterocyclic Derivatives and Use Thereof - The present invention provides a fused heterocyclic derivative showing a potent kinase inhibitory activity and use thereof. A compound represented by the formula: | 05-28-2009 |
20090137581 | Heterocyclic compounds and their uses - Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110δ activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia (T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer. | 05-28-2009 |
20090137582 | Pyrazolo-pyridinone derivatives and methods of use - The present invention comprises a new class of compounds useful for the prophylaxis and treatment of pro-inflammatory cytokine mediated diseases, and in particular, p38 activity mediated inflammation and related conditions. The compounds have a general Formula I | 05-28-2009 |
20090143377 | METHODS AND COMPOSITIONS FOR TREATING DISORDERS - Compounds and compositions for treating disorders related to TRPA1 are described herein. | 06-04-2009 |
20090143378 | THIENOPYRIMIDINE AND THIENOPYRIDINE KINASE MODULATORS - The invention is directed to thienopyrimidines and thienopyridines compounds of Formula I and Formula II: | 06-04-2009 |
20090143379 | Storage stable perfusion solution for dihydropteridinones - Disclosed are storage stable aqueous infusible or injectable solutions containing an active substance of general formula (I) | 06-04-2009 |
20090149457 | 1H-Thieno[2,3-c]Pyrazole Compounds Useful as Kinase Inhibitors - There are provided thieno[2,3-c]pyrazole derivatives of formula (I), wherein A is an aryl or heteroaryl ring, on which the substituent-NHZR | 06-11-2009 |
20090149458 | PYRROLO[3,2-d]PYRIMIDINE COMPOUNDS AND THEIR USE AS PI3 KINASE AND mTOR KINASE INHIBITORS - A pyrrolo[3,2-d]pyrimidine compound, such as a compound of the formula (I): | 06-11-2009 |
20090156595 | Pteridines useful as HCV inhibitors and methods for the preparation thereof - The present invention relates to the use of pteridines as inhibitors of HCV replication as well as their use in pharmaceutical compositions aimed to treat or combat HCV infections. In addition, the present invention relates to compounds per se and their use as medicines. The present invention also concerns processes for the preparation of such compounds, pharmaceutical compositions comprising them, and combinations of said compounds with other anti-HCV agents. | 06-18-2009 |
20090156596 | Unsaturated Heterocyclic Derivatives - This invention relates to compounds of the general formula: | 06-18-2009 |
20090156597 | Novel Compounds - Novel substituted 2,4,8-trisubstituted 8H-pyrido[2,3-d]pyrimidin-7-one containing compounds and compositions, and their use in therapy as CSBP/RK/p38 kinase inhibitors. | 06-18-2009 |
20090156598 | Imidazolopyrimidine modulators of TRPV1 - Certain TRPV1-modulating imidazolopyrimidine compounds are described. The compounds may be used in pharmaceutical compositions and methods for treating disease states, disorders, and conditions mediated by TRPV1 activity, such as pain, arthritis, itch, cough, asthma, or inflammatory bowel disease. | 06-18-2009 |
20090156599 | Imidazolo-, oxazolo-, and thiazolopyrimidine modulators of TRPV1 - Certain TRPV1-modulating imidazolo-, oxazolo-, and thiazolopyrimdine compounds are described. The compounds may be used in pharmaceutical compositions and methods for treating disease states, disorders, and conditions mediated by TRPV1 activity, such as pain, arthritis, itch, cough, asthma, or inflammatory bowel disease. | 06-18-2009 |
20090163490 | Pyrrolopyrimidine Derivatives Used As HSP90 Inhibitors - Compounds of formula (I) have HSP90 inhibitory activity and are therefore useful in the treatment of, inter alia, cancer: Formula (I) wherein R | 06-25-2009 |
20090163491 | SUBSTITUTED 8-[6-AMINO-3PYRIDYL]XANTHINES - The present invention provides substituted 8-[6-amino-3-pyridyl]xanthines and pharmaceutical compositions that are selective antagonists of A | 06-25-2009 |
20090176779 | PYRAZOLO[4,3-D]THIAZOLE DERIVATIVES, AND PREPARATION AND THERAPEUTIC APPLICATION THEREOF - The disclosure relates to a compound of formula (I): | 07-09-2009 |
20090181963 | 3H-[1,2,3]TRIAZOLO[4,5-D]PYRIMIDINE COMPOUNDS, THEIR USE AS mTOR KINASE AND PI3 KINASE INHIBITORS, AND THEIR SYNTHESES - The invention relates to 3H-[1,2,3]triazolo[4,5-d]pyrimidine compounds of the Formula 1: | 07-16-2009 |
20090186889 | SPIRO-SUBSTITUTED PYRROLOPYRIMIDINES - The invention provides compounds of formula I or a pharmaceutically acceptable salt or ester thereof formula I | 07-23-2009 |
20090192153 | NOVEL ADENINE COMPOUND - An adenine compound or its pharmaceutically acceptable salt as a medicament as shown following formula (1): | 07-30-2009 |
20090192154 | SULTAM DERIVATIVES - A sultam derivative of Formula (1) described below having inhibitory action for aggrecanase activity is provided. The sultam derivative of Formula (1) and a salt thereof exhibit strong inhibitory action for aggrecanase activity in a living body of a mammalian animal including human, and is useful, for example, as an active ingredient of a pharmaceutical agent for preventing and/or treating various diseases caused by degradation of aggrecan. | 07-30-2009 |
20090197880 | ANTI-VIRAL COMPOUNDS, COMPOSITIONS, AND METHODS OF USE - Disclosed are compounds of Formula (I), pharmaceutically acceptable salts and solvates thereof, compositions thereof, and methods for their preparation and uses for treating viral infections mediated at least in part by a virus in the Flaviviridae family of viruses. | 08-06-2009 |
20090203687 | FUSED RING HETEROCYCLE KINASE MODULATORS - The present invention provides novel fused ring heterocycle kinase modulators and methods of using the novel fused ring heterocycle kinase modulators to treat diseases mediated by kinase activity. | 08-13-2009 |
20090203688 | HETEROCYCLIC COMPOUNDS - The invention relates to compounds of formula I and salts thereof | 08-13-2009 |
20090203689 | ABCA-1 ELEVATING COMPOUNDS AND METHODS - Disclosed are novel compounds of Formula I | 08-13-2009 |
20090209535 | 6-ETHER/THIOETHER-PURINES AS TOPOISOMERASE II CATALYTIC INHIBITORS AND THEIR USE IN THERAPY - The present invention relates to certain purines of the following formulae, which act as topoisomerase II catalytic inhibitors: wherein: J is independently: —H or —NR | 08-20-2009 |
20090215769 | Use of soluble guanylate cyclase activators for the treatment of Raynaud's Phenomenon - The present invention relates to a method for prevention or treatment of primary and secondary Raynaud's phenomenon comprising administration of an effective amount of a compound selected from compounds of formulae I-IV, and to pharmaceutical compositions containing these compounds. | 08-27-2009 |
20090221573 | Use of Activators of Soluble Guanylate Cyclase for Promoting Wound Healing - The present invention relates to a method for promoting wound healing by administering one or more compounds identified in the claims, and to pharmaceutical compositions containing such compounds. | 09-03-2009 |
20090247517 | COMPOUNDS AND COMPOSITIONS AS INHIBITORS OF CANNABINOID RECEPTOR 1 ACTIVITY - The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of Cannabinoid Receptor 1 (CB1). | 10-01-2009 |
20090247518 | 6-(2-ALKYL-PHENYL)-PYRIDO[2,3-D]PYRIMIDINES USEFUL AS PROTEIN KINASE INHIBITORS - Objects of the present invention are the compounds of formula I | 10-01-2009 |
20090253696 | SUBSTITUTED PYRIDO(3,2-D) PYRIMIDINES AND PHARMACEUTICAL COMPOSITIONS FOR TREATING VIRAL INFECTIONS - This invention provides di-, tri- and tetra-substituted pyrido(3,2-d)pyrimidine derivatives with specific substituting patterns, their pharmaceutically acceptable salts, N-oxides, solvates, pro-drugs and enantiomers, possessing unexpectedly desirable pharmaceutical properties, in particular being highly active antiviral agents. The invention also provides use of such derivatives in the treatment of viral infections and pathologic conditions associated therewith, including hepatitis C. | 10-08-2009 |
20090258874 | PYRAZOLO-HETEROARYL COMPOUNDS - A compound of formula I | 10-15-2009 |
20090270389 | Pyrimidinyl pyridone inhibitors of kinases - This application discloses novel pyrimidinyl pyridone derivatives according to formula I, wherein A, R | 10-29-2009 |
20090286781 | Use of Suluble Guanylate Cyclase Acitvators for Treating Acute and Chronic Lung Diseases - The present invention relates to the use of compounds of the formulae I-VI for manufacturing a pharmaceutical for the treatment of acute and chronic lung disorders such as the respiratory distress syndromes [acute lung injury (ALI), acute respiratory distress syndrome (ARDS)] and the treatment of COPD. | 11-19-2009 |
20090286782 | COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR - Compounds and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof are active on at least one of Fms protein kinase or Kit protein kinase. Also described are methods of use thereof to treat diseases and conditions, including diseases and conditions associated with activity of Fms protein kinases and/or Kit protein kinases, including rheumatoid arthritis, osteoarthritis, osteoporosis, peri-prosthetic osteolysis, systemic sclerosis, demyelinating disorders, multiple sclerosis, Charcot Marie Tooth syndrome, amyotrophic lateral sclerosis, Alzheimer's disease, Parkinson's disease, ulcerative colitis, Crohn's disease, immune thrombocytopenic purpura, myelopreparation for autologous transplantation, transplant rejection, nephritis, nephropathy, type I diabetes, acute pain, inflammatory pain, neuropathic pain, breast cancer, prostate cancer, pancreatic cancer, lung cancer, ovarian cancer, gliomas, glioblastomas, neurofibromatosis, osteolytic bone metastases, and giant cell tumors. | 11-19-2009 |
20090286783 | COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR - Compounds and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof derivatives thereof, forms thereof are active on at least one Raf protein kinase. Also described are methods of use thereof to treat diseases and conditions, including diseases and conditions associated with activity of Raf protein kinases, including melanoma, colorectal cancer, thyroid cancer, ovarian cancer, cholangiocarcinoma, pain or polycystic kidney disease. | 11-19-2009 |
20090298822 | Use of Activators of Soluble Guanylate Cyclase for Treating Reperfusion Damage - The present invention relates to the use of compounds for manufacturing a pharmaceutical product/medicament for the prophylaxis and/or treatment of reperfusion damage. | 12-03-2009 |
20090298823 | Inhibitors of protein kinases - The present invention is directed to compounds of formula I-II and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk and/or JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk and/or JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk and/or JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma. | 12-03-2009 |
20090312319 | CERTAIN CHEMICAL ENTITIES, COMPOSITIONS AND METHODS - Chemical entities that modulate PI3 kinase activity, pharmaceutical compositions containing the chemical entities, and methods of using these chemical entities for treating diseases and conditions associated with PI3 kinase activity are described herein. | 12-17-2009 |
20090312320 | METHODS OF TREATMENT COMPRISING THE ADMINISTRATION OF HALOARYL SUBSTITUTED AMINOPURINES OR COMPOSITIONS THEREOF - Provided herein are Aminopurine Compounds having the following structure: | 12-17-2009 |
20090318440 | CARBONYLAMINO PYRROLOPYRAZOLES, POTENT KINASE INHIBITORS - Carbonylamino Pyrrolopyrazole compounds of formula I, compositions including these compounds and methods of their use are provided. Preferred compounds of formula I have activity as protein kinase inhibitors, including as inhibitors of PAK4. | 12-24-2009 |
20090318441 | Pyrrolopyrimidine Compounds and Their Uses - The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of diseases, particularly pyrrolopyrimidine compounds and derivatives are described which inhibit protein kinases. The organic compounds are useful in treating proliferative disease. | 12-24-2009 |
20090318442 | THIAZOLYL-AND OXAZOLYL-ISOQUINOLINONES AND METHODS FOR USING THEM - The present invention relates to substituted thiazolyl- and oxazoyl-isoquinolinones that act, for example, as modulators of poly(ADP-ribose) polymerase (PARP). The present invention also relates to processes for the preparation of substituted thiazolyl- and oxazolyl-isoquinolinones and to their use in treating various diseases and disorders. | 12-24-2009 |
20090318443 | KINASE INHIBITORS - The present invention provides kinase inhibitors of Formula I. | 12-24-2009 |
20090325952 | PYRAZOLO[3,4-B]PYRIDINE COMPOUNDS, AND THEIR USE AS PDE4 INHIBITORS - The invention provides a compound of formula (I) or a salt thereof: | 12-31-2009 |
20090325953 | P38 KINASE INHIBITING AGENTS - Compounds described by the chemical formula (I) or pharmaceutically acceptable salts thereof: | 12-31-2009 |
20100004235 | Heterocyclic Substituted, Anellated Pyrazole Derivative and its uses - The present application relates to novel heterocyclyl-substituted fused pyrazole derivatives, to processes for their preparation, to their use, alone or in combination, for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular disorders. | 01-07-2010 |
20100004236 | PHOSPHODIESTERASE 4 INHIBITORS - PDE4 inhibition is achieved by novel compounds of the Formula I: | 01-07-2010 |
20100004237 | 2-Amino-7,8-dihydro-6H-pyrido[4,3-D]pyrimidin-5-ones - Disclosed are 2-amino-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one compounds, their stereoisomers, tautomers, pharmaceutically acceptable salts, and prodrugs thereof; compositions that include a pharmaceutically acceptable carrier and one or more of the 2-amino-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one compounds, either alone or in combination with at least one additional therapeutic agent. Disclosed also are methods of using the 2-amino-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of cellular proliferative, viral, autoimmune, cardiovascular, and central nervous system diseases. | 01-07-2010 |
20100004238 | FUSED HETEROCYCLIC COMPOUND - The present invention provides a fused heterocyclic compound having a tyrosine kinase inhibitory action, which is represented by the formula: | 01-07-2010 |
20100016305 | novel use of activators and stimulators of soluble guanylate cyclase for the prevention or treatment of renal disorders - The present invention relates generally to a method for the treatment of renal failure or renal hypertension and, more particularly, for improving the recovery from acute renal failure or renal hypertension by treatment with activators of soluble guanylate cyclase or stimulators of guanylate cyclase. | 01-21-2010 |
20100016306 | PYRIMIDINE DERIVATIVES AS PI3K INHIBITORS - Thienopyrimidines of formula (Ia) or (Ib): | 01-21-2010 |
20100022531 | NOVEL COMPOUNDS AS P2X7 MODULATORS AND USES THEREOF - Compounds are disclosed that have a formula represented by the following (1), 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. | 01-28-2010 |
20100022532 | USE OF A KINASE INHIBITOR FOR THE TREATMENT OF PARTICULAR RESISTANT TUMORS - The invention provides low molecular weight compounds, namely 1H-thieno[2,3-c]pyrazoles, showing a high affinity for the ATP pocket of ABL tyrosine kinase. These compounds are thus ATP-competitive tyrosine kinase inhibitors displaying a significant inhibitory potency also, and in particular, towards BCR-ABL inhibitor-resistant T315I ABL mutants. The compounds of the invention find a useful application in the treatment of BCR-ABL inhibitor-resistant ABL-mediated diseases, such as Imatinib-resistant chronic myelogenous leukemia. Moreover, the invention provides a screening method for the identification of compounds capable of binding the ATP pocket of a kinase protein, in particular of the T315I mutant ABL kinase. | 01-28-2010 |
20100022533 | COMPOSITIONS AND METHODS FOR INDUCING CELL DEDIFFERENTIATION - The present invention provides compounds, compositions and methods for dedifferentiating lineage committed mammalian cells into stem cells. The present invention also provides methods of inducing dedifferentiation of lineage committed mammalian cells into stem cells, which can be further differentiated into various lineage committed cells. Methods of identifying additional compounds useful for inducing dedifferentiation of lineage committed cells into stem cells are also provided. | 01-28-2010 |
20100029641 | ARYL SULFAMIDE DERIVATIVES AND METHODS OF THEIR USE - The present invention is directed to aryl sulfamide derivatives of formula I: | 02-04-2010 |
20100029642 | Methods of Using Pyridodihydropyrazinones - Disclosed are pyridodihydropyrazinone compounds, processes for preparing them and their use as pharmaceutical compositions. The compounds according to the invention correspond to general formula (I), | 02-04-2010 |
20100035876 | Use of a Kinase Inhibitor for the Treatment of Particular Resistant Tumors - The invention provides low molecular weight compounds, namely tetrahydropyrrolo[3,4-c]pyrazoles, showing a high affinity for the ATP pocket of ABL tyrosine kinase. These compounds are thus ATP-competitive tyrosine kinase inhibitors displaying a significant inhibitory potency also, and in particular, towards BCR-ABL inhibitor-resistant T315I ABL mutants. The compounds of the invention find a useful application in the treatment of BCR-ABL inhibitor-resistant ABL-mediated diseases, such as Imatinib-resistant chronic myelogenous leukemia. Moreover, the invention provides a screening method for the identification of compounds capable of binding the ATP pocket of a kinase protein, in particular of the T315I mutant ABL kinase. | 02-11-2010 |
20100035877 | METHODS AND COMPOSITIONS FOR TREATING PATHOLOGIES ASSOCIATED WITH BDNF SIGNALING - A method of treating ncm-neurødegenerative pathologies associated with derangement in brain-derived neurotrophic factor signaling in the brain stem includes administering to the subject an amount of at least one arnpakine effective to increase brain-derived neurotrophic factor nodose sensory neurons of the subject. | 02-11-2010 |
20100041650 | PURINE COMPOUNDS AS CANNABINOID RECEPTOR BLOCKERS - The present invention relates to purine-based cannabinoid receptor blockers and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, dyslipidemias, cardiovascular disorders, inflammatory disorders, hepatic disorders, and a combination thereof. | 02-18-2010 |
20100041651 | TRIAZOLOPYRIDINE CARBOXAMIDE DERIVATIVES AND TRIAZOLOPYRIMIDINE CARBOXAMIDE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF - The invention relates to the triazolopyridine carboxamide derivatives and triazolopyrimidine carboxamide derivatives of general formula (I): | 02-18-2010 |
20100048559 | PYRIDO(3,2-d)PYRIDMIDINES USEFUL FOR TREATING VIRAL INFECTIONS - This invention provides pyrido(3,2-d)pyrimidine derivatives represented by the structural formula (I), wherein: R | 02-25-2010 |
20100048560 | PYRAZOLO PYRIDINE DERIVATIVES AS NADPH OXIDASE INHIBITORS - The present invention is related to pyrazolo pyridine derivatives of Formula (I), pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase). | 02-25-2010 |
20100056514 | THIENOPYRAZOLES - Thienopyrazoles, their preparation, pharmaceutical compositions comprising these compounds, and their pharmaceutical uses in the treatment of disease states capable of being modulated by the inhibition of the protein kinases, in particular interleukin-2 inducible tyrosine kinase (ITK). | 03-04-2010 |
20100063047 | AMINOPYRIMIDINE INHIBITORS OF HISTAMINE RECEPTORS FOR THE TREATMENT OF DISEASE - The present invention relates to compounds and methods which may be useful as inhibitors of H | 03-11-2010 |
20100093720 | MACROCYCLIC ANTAGONISTS OF THE MOTILIN RECEPTOR FOR TREATMENT OF GASTROINTESTINAL DYSMOTILITY DISORDERS - The present invention provides conformationally-defined macrocyclic compounds that bind to and/or are functional modulators of the motilin receptor including subtypes, isoforms and/or variants thereof. These macrocyclic compounds, at a minimum, possess adequate pharmacological properties to be useful as therapeutics for a range of disease indications. In particular, these compounds are useful for treatment and prevention of disorders characterized by hypermotilinemia and/or gastrointestinal hypermotility, including, but not limited to, diarrhea, cancer treatment-related diarrhea, cancer-induced diarrhea, chemotherapy-induced diarrhea, radiation enteritis, radiation-induced diarrhea, stress-induced diarrhea, chronic diarrhea, AIDS-related diarrhea, | 04-15-2010 |
20100093721 | PHENYL AND HETEROARYL SUBSTITUTED THIENO[2,3-d]PYRIMIDINES AND THEIR USE AS ADENOSINE A2a RECEPTOR ANTAGONISTS - This invention relates to a novel thieno[2,3-d]pyrimidine, Z, and its therapeutic and prophylactic uses, wherein X, R | 04-15-2010 |
20100093722 | HETEROARYL AND PHENYL SUBSTITUTED THIENO[2,3-d]PYRIMIDINES AND THEIR USE AS ADENOSINE A2a RECEPTOR ANTAGONISTS - This invention relates to a novel thieno[2,3-d]pyrimidine, Z, and its therapeutic and prophylactic uses, wherein R | 04-15-2010 |
20100093723 | HETEROCYCLYL AND CYCLOALKYL SUBSTITUTED THIENO[2,3 d]PYRIMIDINE AND THEIR USE AS ADENOSINE A2a RECEPTOR ANTAGONISTS - This invention relates to a novel thieno[2,3-d]pyrimidine, Z, and its therapeutic and prophylactic uses, wherein X, R | 04-15-2010 |
20100093724 | Azaindazole Compounds As CCR1 Receptor Antagonists - Disclosed are compounds of the formula (I), useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. | 04-15-2010 |
20100120764 | DI-SUBSTITUTED AMIDES 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 regulation of breathing, and 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, respiratory depression, 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 in disorders of respiration such as overdose of an alcohol, an opiate, an opioid, a barbiturate, an anesthetic, or a nerve toxin, or where the respiratory depression results form a medical condition such as central sleep apnea, 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 compounds useful for treatment of such conditions, and methods of using these compounds for such treatment. | 05-13-2010 |
20100120765 | PYRAZOLYL SUBSTITUTED XANTHINES - The present invention provides compounds and pharmaceutical compositions that are selective antagonists of A | 05-13-2010 |
20100120766 | Substituted Pteridines - The invention relates to new pteridines which are suitable for treating respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin or eyes, diseases of the peripheral or central nervous system and cancers. This invention also relates to pharmaceutical compositions containing these compounds. | 05-13-2010 |
20100120767 | Pyrimidothiophene Compounds - Compounds of formula (1) are inhibitors of HSP90 activity in vitro or in vivo, and of use in the treatment of inter alia, cancer: wherein R | 05-13-2010 |
20100125074 | Thieno-[2,3-d]Pyrimidine and Thieno-Pyridazine Compounds and Methods of Use - The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I | 05-20-2010 |
20100130491 | 9-SUBSTITUTED-8-OXO-ADENINE COMPOUNDS AS TOLL-LIKE RECEPTOR (TLR7 ) MODULATORS - The present invention provides compounds of formula (I) | 05-27-2010 |
20100130492 | MORPHOLINOPURINE DERIVATIVES - There is provided a novel compound that inhibits phosphatidylinositol 3-kinase (PI3K) and/or the mammalian target of rapamycin (mTOR) and exhibits anti-tumor activity. The present invention provides a compound represented by the following formula (1) having various substituents that inhibits PI3K and/or mTOR and exhibits anti-tumor activity: | 05-27-2010 |
20100137302 | Fused Thiazole Derivatives as Kinase Inhibitors - A series of 6,7-dihydro[1,3]thiazolo[5,4-c]pyridin-4(5H)-one derivatives, and analogues thereof, which are substituted in the 2-position by an optionally 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. | 06-03-2010 |
20100137303 | NEW COMPOUND 255 - Compounds of formula (I) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described. | 06-03-2010 |
20100160313 | DISCOVERY OF NOVEL ANTICANCER COMPOUNDS BASED ON CONFORMATIONAL SAMPLING OF QUINOXALINHYDRAZIDE PHARMACOPHORE - The present invention relates in general to anti-cancer drug design. More specifically, the invention provides methods of mapping and screening for anti-cancer agents using pharmacophore models. The invention demonstrates that, conformational sampling of a small lead molecule, followed by representative pharmacophore model development, is an efficient approach for rational design of novel anticancer agents with similar or better potency than the original lead but with different physicochemical properties. | 06-24-2010 |
20100184759 | PYRANO-PYRAZOLE-AMINES - The present invention relates to compounds having the structural formula below and pharmacological activity towards the sigma (σ) receptor, and more particularly to pyrano-pyrazole-amines, to processes of preparing such compounds, to pharmaceutical compositions comprising them, and to their use in therapy and prophylaxis, in particular for the treatment of psychosis. | 07-22-2010 |
20100184760 | Benzoxazole kinase inhibitors and methods of use - The present invention provides chemical entities or compounds and pharmaceutical compositions thereof that are capable of modulating certain protein kinases such as mTor, tyrosine kinases, and/or lipid kinases such as PI3 kinase. Also provided in the present invention are methods of using these compositions to modulate activities of one or more of these kinases, especially for therapeutic applications. | 07-22-2010 |
20100184761 | 6-PHENYL-1H-IMIDAZO[4,5-c]PYRIDINE-4-CARBONITRILE DERIVATIVES - The present invention relates to 6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives having the general Formula I | 07-22-2010 |
20100190787 | Modulators of Mitotic Kinases - The invention relates to compounds of Formula (I), a prodrug, a polymorph, a tautomer, an enantiomer, a stereoisomer, a solvate, an N-oxide, or a pharmaceutically acceptable salt thereof: (formula should be inserted here) which have inhibitory effect on one or more protein kinases that are involved in cell mitosis. | 07-29-2010 |
20100204221 | Pyrrolopyrimidinyl axl kinase inhibitors - Compounds represented by Formula (I): | 08-12-2010 |
20100204222 | PYRIDOPYRIMIDINE DERIVATIVES AS P13 KINASE INHIBITORS - Invented is a method of inhibiting the activity/function of PI3 kinases using pyridopyrimidine derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of pyridopyrimidine derivatives. | 08-12-2010 |
20100204223 | 2-Substituted phenyl-5,7-dihydrocarbyl-3,7-dihydropyrrolo[2,3-d] pyrimidin-4-one derivatives, the preparation and the pharmaceutical use thereof - The invention relates to the compounds of formula I, their preparation and the pharmaceutical compositions containing the compounds. The invention also relates to the use of the compounds of formula I in preparing medicines, which can treat sexual dysfunction of animals including human (male and female), especially erectile dysfunction of male and the diseases in which the function of phospholipase 5 (cGMP PDE5) is involved. | 08-12-2010 |
20100210643 | sGC STIMULATORS, sGC ACTIVATORS AND COMBINATIONS FOR THE TREATMENT OF UROLOGICAL DISORDERS - The invention provides pharmacological compositions comprising a stimulator or activator of the soluble guanylate cyclase alone (sGC) or in combination with a PDE5 inhibitor for the treatment of urological disorders comprising of Benign Prostate Syndrome (BPS), Benign Prostate Hyperplasia (BPH), Benign Prostate Enlargement (BPE), Bladder Outlet Obstruction (BOO), Lower Urinary Tract Symptoms (LUTS), genitourinary disorders comprising neurogenic bladder syndrome (OAB) and (IC), urinary incontinence (UI) like mixed-, urge-, stress-, or overflow incontinence (MUI, UUI, SUI, OUI) and pelvic pain (PP). | 08-19-2010 |
20100210644 | CHEMICAL COMPOUNDS - The present invention encompasses compounds of general formula (1) wherein the groups R | 08-19-2010 |
20100210645 | Certain Chemical Entities, Compositions and Methods - Provided are certain chemical entities, and methods of use to modulate skeletal myosin, skeletal actin, skeletal tropomyosin, skeletal troponin C, skeletal troponin I, skeletal troponin T, and skeletal muscle, including fragments and isoforms thereof, as well as the skeletal sarcomere, and methods of use in the treatment of obesity, sarcopenia, wasting syndrome, frailty, cachexia, muscle spasm, post-surgical and post-traumatic muscle weakness, neuromuscular disease, and other indications. | 08-19-2010 |
20100216788 | FUSED HETEROCYCLIC COMPOUND - The present invention provides a compound represented by the formula: | 08-26-2010 |
20100216789 | RHO-KINASE INHIBITORS - Disclosed are compounds and derivatives thereof, their synthesis, and their use as Rho-kinase inhibitors. These compounds of the present invention are useful for inhibiting tumor growth, treating erectile dysfunction, and treating other indications mediated by Rho-kinase, e.g., coronary heart disease. | 08-26-2010 |
20100216790 | IMIDAZOPYRIDINE-DERIVATIVES AS INDUCIBLE NO-SYNTHASE INHIBITORS - The compounds of formula (I) | 08-26-2010 |
20100222342 | PYRROLOPYRAZOLE, POTENT KINASE INHIBITORS - Pyrrole pyrazole compounds of formula I, compositions including these compounds and methods of their use are provided. Preferred compounds of formula I have activity as protein kinase inhibitors, including as inhibitors of PAK4. | 09-02-2010 |
20100222343 | PHOSPHOINOSITIDE 3-KINASE INHIBITORS WITH A ZINC BINDING MOIETY - The instant application relates to deazapurines, thienopyrimidines and furopyrimidines with zinc-binding moiety based derivatives and their use in the treatment of phosphoinositide 3-kinase related diseases and disorders such as cancer. The instant application further relates to the the treatment of histone deacetylase related disorders and diseases related to both histone deacetylase and phosphoinositide 3-kinase. | 09-02-2010 |
20100234370 | PHARMACEUTICAL COMPOUNDS - Fused pyrimidines of formula (I): | 09-16-2010 |
20100249128 | NOVEL 3-AMIDO-PYRROLO[3,4-C]PYRAZOLE-5(1H,4H,6H) CARBALDEHYDE DERIVATIVES - The present invention relates to compounds and pharmaceutically acceptable salts of Formula (I): wherein X, R | 09-30-2010 |
20100280027 | PHARMACEUTICAL COMPOUNDS - Provided herein are methods of treating diseases or disorders arising from abnormal cell growth, function or behavior associated with PI3 kinase, which method includes administering to a patient in need thereof a compound that is a fused pyrimidine of formula (I): | 11-04-2010 |
20100292234 | TRIAZOLE FUSED HETEROARYL COMPOUNDS AND METHODS OF USE THEREOF - The present invention comprises a new class of compounds useful for modulating the activity of p38 MAP kinase. The compounds have a general Formula I | 11-18-2010 |
20100298318 | METHODS AND COMPOSITIONS FOR STIMULATING NEUROGENESIS AND INHIBITING NEURONAL DEGENERATION USING ISOTHIAZOLOPYRIMIDINONES - The present invention provides methods and compositions comprising compounds useful for stimulating neurogenesis. The methods and compositions comprising compounds are also useful for inhibiting neuronal degeneration. Thus, the present invention can be used in the treatment of diseases and conditions characterized by neuronal loss and reduced neurogenesis including Alzheimer's disease, stroke, traumatic brain injury, traumatic nerve injury, and depression. This invention is useful for resear products including single agents or mixtures of agents to promote, proliferate, differentiate, or maintain neurons from stem or progenitor cells. | 11-25-2010 |
20100298319 | PYRIMIDINE SUBSTITUTED PURINE DERIVATIVES - The present invention relates to purine compounds that are useful as kinase inhibitors. More particularly, the present invention relates to purine compounds, methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment of proliferative conditions or disorders. These compounds may be useful as medicaments for the treatment of a number of proliferative conditions or disorders including tumours and cancers as well as other disorders or conditions related to or associated with PI3 and/or mTOR kinases. | 11-25-2010 |
20100298320 | Pyrido[2,3-b]pyrazin-8-substituted Compounds and Their Use - The present invention pertains generally to the field of therapeutic compounds for treating proliferative disorders, cancer, etc., and more specifically to certain pyrido[2,3-b]pyrazin-8-substituted compounds, as described herein, which, inter alia, inhibit RAF (e.g., B-RAF) activity. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit RAF (e.g., BRAF) activity, to inhibit receptor tyrosine kinase (RTK) activity, to inhibit cell proliferation, and in the treatment of diseases and disorders that are ameliorated by the inhibition of RAF, RTK, etc., proliferative disorders such as cancer (e.g., colorectal cancer, melanoma), etc. | 11-25-2010 |
20100324040 | 9-(PYRAZOL-3-YL)-9H-PURINE-2-AMINE AND 3-(PYRAZOL-3-YL) -3H-IMIDAZO[4,5-B] PYRIDIN-5- AMINE DERIVATIVES AND THEIR USE FOR THE TREATMENT OF CANCER - The present invention relates to compounds of Formula (I): and to their pharmaceutical compositions, and to their methods of use. These compounds provide a treatment for myeloproliferative disorders and cancer. | 12-23-2010 |
20110003809 | IMIDAZO [4,5-B] PYRIDINE DERIVATIVES USED AS RAF INHIBITORS - Compounds of Formula I are useful for inhibition of Raf kinases. Methods of using compounds of Formula I and stereoisomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed. | 01-06-2011 |
20110009405 | PYRIMIDINYL AND 1,3,5-TRIAZINYL BENZIMIDAZOLES AND THEIR USE IN CANCER THERAPY - Provided herein are pyrimidinyl and 1,3,5-triazinyl benzimidazoles of Formula I, and their pharmaceutical compositions, preparation, and use as agents or drugs for cancer therapy, either alone or in combination with radiation and/or other anticancer drugs. | 01-13-2011 |
20110015193 | 1, 5-DIHYDRO-PYRAZOLO (3, 4-D) PYRIMIDIN-4-ONE DERIVATIVES AND THEIR USE AS PDE9A MUDULATORS FOR THE TREATMENT OF CNS DISORDERS - The invention relates to novel substituted pyrazolopyrimidines. Chemically, the compounds are characterised by general Formula (I): with R | 01-20-2011 |
20110028472 | THIENOPYRIMIDINES - Novel thienopyrimidines of the formula (I), in which R | 02-03-2011 |
20110034458 | PYRIDINE METHYLENE AZOLIDINONES AND USE THEREOF PHOSPHOINOSITIDE INHIBITORS - The present invention is related to pyridine methylene azolidinone derivatives of Formula (I) in particular 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, transplantation, graft rejection or lung injuries. | 02-10-2011 |
20110046131 | PURINES AS PKC-THETA INHIBITORS - A chemical genus of purines, which are useful as PKCθ inhibitors, is disclosed. The genus is represented by the formula (I); A representative example is: (II) | 02-24-2011 |
20110059961 | 4-SUBSTITUTED PYRIDIN-3-YL-CARBOXAMIDE COMPOUNDS AND METHODS OF USE - The invention relates to compounds of formula (I) which are useful as kinase inhibitors, more specifically useful as PIM kinase inhibitors, thus useful as cancer therapeutics. The invention also relates to compositions, more specifically pharmaceutical compositions comprising these compounds and methods of using the same, either alone or in combination, to treat various forms of cancer and hyperproliferative disorders, as well as methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions. | 03-10-2011 |
20110065701 | PHARMACEUTICAL COMPOUNDS - A thienopyrimidine of formula (I): | 03-17-2011 |
20110082137 | NEW COMPOUNDS FOR THE TREATMENT OF CNS DISORDERS - The invention relates to novel 1,6-disubstituted pyrazolopyrimidinones of formula (I), | 04-07-2011 |
20110082138 | IMIDAZOPYRIDIN-2-ONE DERIVATIVES - A compound represented by formula (I) having mTOR inhibitory activity or a pharmacologically acceptable salt thereof. | 04-07-2011 |
20110082139 | SUBSTITUTED 8-[6-AMINO-3-PYRIDYL]XANTHINES - The present invention provides substituted 8-[6-amino-3-pyridyl]xanthines and pharmaceutical compositions that are selective antagonists of A | 04-07-2011 |
20110092499 | N-CONTAINING HETEROCYCLIC COMPOUNDS - The present invention relates to N-containing heterocyclic compounds that are inhibitors of protein kinases including JAK kinases. In particular, the compounds are selective for JAK1, JAK2, JAK3 or TYK2 kinases and combinations thereof such as JAK1 and JAK2. The kinase inhibitors can be used in the treatment of kinase associated diseases such as immunological and inflammatory diseases including organ transplants; hyperproliferative diseases including cancer and myeloproliferative diseases; viral diseases; metabolic diseases; and vascular diseases. | 04-21-2011 |
20110092500 | SGC STIMULATORS, SGC ACTIVATORS AND COMBINATIONS THEREOF FOR THE TREATMENT OF HEARING IMPAIRMENT - The invention provides pharmacological compositions comprising a stimulator or activator of the soluble guanylate cyclase (sGC) either alone or in combination for the treatment of hearing impairment i.e. hearing loss and tinnitus. | 04-21-2011 |
20110098294 | PURINE ANALOGS - The present invention provides a new patentable class of purine analog compounds, as well as compositions and methods of using them, for example, to prevent or treat various diseases and disorders in human and non-human animals. | 04-28-2011 |
20110098295 | METHODS OF TREATING ANXIETY, ITCHING AND PSYCHIATRIC DISORDERS - A method of treating an undesirable AC8-related condition in a mammal is provided comprising the step of inhibiting AC8 in the mammal | 04-28-2011 |
20110105498 | Pyrazolo-pyridinone and pyrazolo-pyrazinone compounds as P38 modulators and methods of use thereof - The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I | 05-05-2011 |
20110105499 | Pyrazolo-Pyrazinone Compounds and Methods of Use Thereof - The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I | 05-05-2011 |
20110105500 | PYRAZINE SUBSTITUTED PURINES - The present invention relates to purine compounds of formula (I) that are useful as kinase inhibitors. More particularly, the present invention relates to purine compounds, methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment of proliferative conditions or disorders. These compounds may be useful as medicaments for the treatment of a number of proliferative conditions or disorders including tumours and cancers as well as other disorders or conditions related to or associated with PI3K and/or mTOR kinases. | 05-05-2011 |
20110112090 | Depsipeptides and Their Therapeutic Use - A Compound of structure (IX) or (X) or a pharmaceutically acceptable salt thereof, wherein: X is —C(═O)N(R | 05-12-2011 |
20110124641 | BENZOTHIAZOLE KINASE INHIBITORS AND METHODS OF USE - The present invention provides chemical entities or compounds and pharmaceutical compositions thereof that are capable of modulating lipid kinases such PI3 kinases, tryosine kinases and protein kinases such as mTOR. Also provided in the present invention are methods of using these compositions to modulate these kinases especially for therapeutic applications. | 05-26-2011 |
20110130397 | PYRROLINONE COMPOUNDS AS INHIBITORS OF BACTERIAL PEPTIDYL TRNA HYDROLASE AND USES THEREOF - Provided herein are compounds that modulate the activity of a bacterial peptidyl tRNA hydrolase, including compositions and dosage forms comprising the compounds. Further provided herein are methods for preventing or inhibiting bacterial proliferation as well as methods for preventing, treating, and/or managing a bacterial infection using such compounds and compositions. | 06-02-2011 |
20110144104 | PYRROLIDINYL-ALKYL-AMIDE DERIVATIVES, THEIR PREPARATION, AND THEIR THERAPEUTIC APPLICATION AS CCR3 RECEPTOR LIGANDS - The present invention relates to pyrrolidinyl-alkyl-amide derivatives of formula (I) or (IA) | 06-16-2011 |
20110152258 | Compounds and Methods for Kinase Modulation, and Indications Therefor - Compounds and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof are active on at least one Raf protein kinase. In certain aspects and embodiments, the described compounds are active in inhibiting proliferation of a Ras mutant cell line. Also described are methods of use thereof to treat diseases and conditions, including diseases and conditions associated with activity of B-Raf V600E mutant protein kinase, including melanoma, glioma, glioblastoma multiforme, pilocytic astrocytoma, colorectal cancer, thyroid cancer, lung cancer, ovarian cancer, prostate cancer, liver cancer, gallbladder cancer, gastrointestinal stromal tumors, biliary tract cancer, and cholangiocarcinoma. Also described are methods of use thereof to treat diseases and conditions, including diseases and conditions associated with activity of c-Raf-1 protein kinase, including acute pain, chronic pain or polycystic kidney disease. | 06-23-2011 |
20110152259 | NITROGEN-CONTAINING HETEROCYCLIC COMPOUNDS AND METHODS OF USE THEREOF - The present invention provides compounds of Formula (I): | 06-23-2011 |
20110160203 | Substituted Pyrrolo-Aminopyrimidine Compounds - The present invention relates to substituted pyrrolo-aminopyrimidine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted pyrrolo-aminopyrimidine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof. | 06-30-2011 |
20110166135 | AROMATIC NITROGEN-CONTAINING 6-MEMBERED RING COMPOUNDS AND THEIR USE - The present invention provides aromatic nitrogen-containing 6-membered ring compounds having excellent PDE10 inhibitory activity. The present invention relates to an aromatic nitrogen-containing 6-membered ring compound represented by the following formula [I | 07-07-2011 |
20110172228 | KINASE INHIBITORS AND METHODS OF USE - The present invention provides chemical entities or compounds and pharmaceutical compositions thereof that are capable of modulating certain protein kinases such as mTor, tyrosine kinases, and/or lipid kinases such as PI3 kinase. Also provided in the present invention are methods of using these compositions to modulate activities of one or more of these kinases, especially for therapeutic applications. | 07-14-2011 |
20110178080 | Melanocortin Receptor-Specific Spiro-Piperidine Compounds - Melanocortin receptor-specific compounds of formula I below: | 07-21-2011 |
20110178081 | PYRAZOLO PYRIDINE DERIVATIVES AS NADPH OXIDASE INHIBITORS - The present invention is related to pyrazolo pyridine derivatives of Formula (I), pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase). | 07-21-2011 |
20110178082 | PYRAZOLO PYRIDINE DERIVATIVES AS NADPH OXIDASE INHIBITORS - The present invention is related to pyrazolo pyridine derivatives of Formula (I), pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase). | 07-21-2011 |
20110183972 | AROMATIC RING FUSED TRIAZINE DERIVATIVES AND USES THEREOF - The invention belongs to pharmaceutical field. The invention relates to the compounds according to Formula I, including their optically active forms, pharmaceutically acceptable salts or hydrates, and the pharmaceutical composition comprising thereof as active ingredient; uses in the preparation of vascular endothelial growth factor receptor tyrosine kinase inhibitors, and uses in the preparation of medicament for the treatment and/or prevention of cancer. | 07-28-2011 |
20110190290 | 1H-PYRAZOLO[3,4-B]PYRIDINES AND THERAPEUTIC USES THEREOF - Provided herein are compounds according to Formula I and pharmaceutically acceptable salts thereof, and compositions comprising the same, for use in various methods, including treating cancers such as colon, ovarian, pancreatic, breast, liver, prostate and hematologic cancers: | 08-04-2011 |
20110190291 | Prodrug and Fluoregenic Compositions and Methods for Using the Same - Methods and compositions for treating disease caused by increased iron levels are disclosed Fluoregenic compounds and methods of using the same are also described. | 08-04-2011 |
20110190292 | HETEROBICYCLIC COMPOUNDS USEFUL AS KINASE INHIBITORS - A compound of Formula (I) | 08-04-2011 |
20110212960 | NEW COMPOUNDS FOR THE TREATMENT OF CNS DISORDER - The invention relates to novel pyrazolopyrimidinones according to formula (I). | 09-01-2011 |
20110218197 | SUBSTITUTED AZA-BICYCLIC IMIDAZOLE DERIVATIVES USEFUL AS TRPM8 RECEPTOR MODULATORS - The present invention is directed to substituted aza-bicyclic imidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by TRP M8, including for example, inflammatory pain, inflammatory hyperalgesia, inflammatory hypersensitivity condition, neuropathic pain, neuropathic cold allodynia, inflammatory somatic hyperalgesia, inflammatory visceral hyperalgesia, cardiovascular disease aggravated by cold and pulmonary disease aggravated by cold. | 09-08-2011 |
20110230479 | NEUROTROPHIN MIMETICS AND USES THEREOF - The present application is related to compounds which are novel neurotrophin mimetics. The application also discloses the treatment of disorders associated with p75 expression, such as degradation or dysfunction of cells expressing p75 in a mammal by administering an effective amount of such compounds. | 09-22-2011 |
20110230480 | 8-HETEROARYLPURINE MNK2 INHIBITORS FOR TREATING METABOLIC DISORDERS - Compounds of the formula | 09-22-2011 |
20110237583 | 2, 5-DIAMINO-SUBSTITUTED PYRIDO [4, 3-D] PYRIMIDINES AS AUTOTAXIN INHIBITORS AGAINST CANCER - The present invention relates to pyridopyrimidine derivatives according to formula (I) as autotaxin inhibitors and the use of such compounds for the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by increased lysophosphatic acid levels and/or the activation of autotaxin, in particular of different cancers. | 09-29-2011 |
20110245245 | METHODS OF TREATMENT COMPRISING THE ADMINISTRATION OF HETEROARYL COMPOUNDS - Provided herein are Heteroaryl Compounds having the following structure: | 10-06-2011 |
20110263595 | COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR - Compounds and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof are active on one or more of Fms, Kit, Flt3, TrkA, TrkB and TrkC kinase protein. Also described are methods of use thereof to treat diseases and conditions, including diseases and conditions associated with activity of one or more of Fms, Kit, Flt3, TrkA, TrkB and TrkC, including rheumatoid arthritis, osteoarthritis, osteoporosis, peri-prosthetic osteolysis, systemic sclerosis, demyelinating disorders, multiple sclerosis, Charcot Marie Tooth syndrome, amyotrophic lateral sclerosis, Alzheimer's disease, Parkinson's disease, global ischemia, ulcerative colitis, Crohn's disease, immune thrombocytopenic purpura, atherosclerosis, systemic lupus erythematosis, myelopreparation for autologous transplantation, transplant rejection, glomerulonephritis, interstitial nephritis, Lupus nephritis, tubular necrosis, diabetic nephropathy, renal hypertrophy, type I diabetes, acute pain, inflammatory pain, neuropathic pain, acute myeloid leukemia, melanoma, multiple myeloma, breast cancer, prostate cancer, pancreatic cancer, lung cancer, ovarian cancer, gliomas, glioblastoma, neurofibromatosis, osteolytic bone metastases, brain metasteses, gastrointestinal stromal tumors, and giant cell tumors. | 10-27-2011 |
20110263596 | 2-OXO-3-BENZYLBENZOXAZOL-2-ONE DERIVATIVES AND RELATED COMPOUNDS AS MET KINASE INHIBITORS FOR THE TREATMENT OF TUMOURS - Described are compounds which inhibit, regulate and/or modulate kinase signal transduction, for example of Met kinase. The compounds are of the formulae A1 to A148 and B1 described herein, including 2-oxobenzoxazol-3-ylmethyl]phenyl}carbamate and 2-oxooxazolo[4,5-b]pyridin-3-ylmethyl)phenyl]carbamate compounds, and pharmaceutically usable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. Also described are compositions containing these compounds. Also described are methods for the treatment of diseases in which the inhibition, regulation and/or modulation of kinase signal transduction plays a role by administering these compounds. | 10-27-2011 |
20110263597 | SUBSTITUTED PYRIDINES AND PYRIDAZINES WITH ANGIOGENESIS INHIBITING ACTIVITY - Methods of treating a mammal having a condition characterized by abnormal angiogenesis or hyperpermiability processes using substituted pyridazines having angiogenesis inhibiting activity and the generalized structural formula | 10-27-2011 |
20110269757 | PYRAZOLO PYRIDINE DERIVATIVES AS NADPH OXIDASE INHIBITORS - The present invention is related to pyrazolo pyridine derivatives of Formula (I), pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase). | 11-03-2011 |
20110275629 | Pyridazino-pyridinone Compounds and Methods of Use - The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I | 11-10-2011 |
20110281864 | Pyrido[3,2-d]Pyridazine-2(1H)-One Compounds as p38 Modulators and Methods of Use Thereof - The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I | 11-17-2011 |
20110281865 | NOVEL 3,5-DISUBSTITUTED-3H-IMIDAZO[4,5-B]PYRIDINE AND 3,5- DISUBSTITUTED -3H-[1,2,3]TRIAZOLO[4,5-B] PYRIDINE COMPOUNDS AS MODULATORS OF PROTEIN KINASES - The present invention provides, inter alia, compounds of formula I as protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them. | 11-17-2011 |
20110281866 | HETEROCYCLIC KINASE INHIBITORS - The present invention provides heterocyclic compounds for use as kinase inhibitors and in other applications. Also provided are pharmaceutical compositions and methods of treatments of diseases and conditions associated with P13 kinase activity. | 11-17-2011 |
20110288088 | SUBSTITUTED PYRROLO-PYRAZOLE DERIVATIVES ACTIVE AS KINASE INHIBITORS - Substituted pyrrolo-pyrazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with dysregulated protein kinase activity, like cancer. | 11-24-2011 |
20110288089 | INSECTICIDAL COMPOUNDS - A compound of Formula (I): wherein A | 11-24-2011 |
20110288090 | Inhibitors of AKT Activity - The instant invention provides for compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer. | 11-24-2011 |
20110294802 | PHARMACEUTICALLY ACCEPTABLE SALTS OF METHYL (3-{ [[3-(6- AMINO- 2-BUTOXY-8-OXO-7, 8-DIHYDRO-9H-PURIN-9-YL) PROPYL] (3- MORPHOLIN-4-YLPROPYL) AMINO] METHYL }PHENYL) ACETATE AND THEIR USE IN THERAPY - The present invention concerns hydrochloric acid, hydrobromic acid and maleic acid salts of methyl (3-{[[3-(6-amino-2-butoxy-8-oxo-7,8-dihydro-9H-purin-9-yl)propyl](3-morpholin-4-ylpropyl)amino]methyl}phenyl)acetate, compositions comprising them and their use in therapy. | 12-01-2011 |
20110294803 | PHOSPHATIDYLINOSITOL-3-KINASE P110 DELTA-TARGETED DRUGS IN THE TREATMENT OF CNS DISORDERS - Methods for treating CNS disorders such as schizophrenia, psychosis and cognitive disorders using specific inhibitors of phosphatidylinositol-3-kinase p110 delta (PIK3CD) expression and/or activity are described. Methods of determining risk of CNS disorders and methods of determining treatment response are also described. An integrative systems biology approach to identify a signaling mechanism and genetic network associated with schizophrenia and with schizophrenia-associated risk variation in ErbB4. A risk pathway associated with ErbB4 genetic variation involving increased expression of a PI3K-linked ErbB4 receptor CYT-1 and a specific PI3K enzyme, PIK3CD has been identified. | 12-01-2011 |
20110294804 | NOVEL BICYCLIC HETEROCYCLIC COMPOUND - The invention provides a compound for the treatment or prophylaxis of pathology involving SNS, specifically diseases such as neuropathic pain, nociceptive pain, dysuria, multiple sclerosis and the like. The compound is represented by formula (1) or a pharmaceutically acceptable salt thereof wherein R | 12-01-2011 |
20110294805 | PYRAZOLO-PYRIDINONE AND PYRAZOLO-PYRAZINONE COMPOUNDS AS P38 MODULATORS AND METHODS OF USE THEREOF - The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I | 12-01-2011 |
20110306609 | THIAZOLOPYRIDINE SIRTUIN MODULATING COMPOUNDS - Provided herein are novel sirtuin-modulating compounds of Structural Formula (Ia) 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. | 12-15-2011 |
20110306610 | 9-SUBSTITUTED 8-OXOADENINE COMPOUND - The present invention provides an 8-oxoadenine compound having immunemodulating activities such as an interferon inducing activity and useful as an antiviral agent and antiallergic agent, which is represented by the following formula (1): | 12-15-2011 |
20110319409 | 7-AZA-QUINAZOLINE PDE10 INHIBITORS - The present invention is directed to 7-aza-quinazoline compounds of general structural formula I | 12-29-2011 |
20120035173 | DI-SUBSTITUTED AMIDES 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 regulation of breathing, and 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, respiratory depression, sleep apneas, attention deficit hyperactivity disorder and affective or mood disorders, among numerous others. In a particular aspect, the invention relates to compounds useful for treatment of such conditions, and methods of using these compounds for such treatment. | 02-09-2012 |
20120040981 | THIENOPYRIMIDINE AS CDC7 KINASE INHIBITORS - The present invention relates to a compound represented by the formula (I): | 02-16-2012 |
20120040982 | Xanthine derivatives, the preparation thereof and their use as pharmaceutical compositions - The present invention relates to substituted xanthines of general formula | 02-16-2012 |
20120046283 | COMPOUNDS FOR TREATING NEUROPSYCHIATRIC CONDITIONS - Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of neuropsychiatric conditions. | 02-23-2012 |
20120059000 | CHEMICAL COMPOUNDS, COMPOSITIONS AND METHODS FOR KINASE MODULATION - Chemical compounds that modulate kinase activity, including PI3 kinase activity, and chemical compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including P13 kinase activity, are described herein. | 03-08-2012 |
20120059001 | NOVEL KINASE MODULATORS - The present invention provides PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them. | 03-08-2012 |
20120065200 | INHIBITORS OF NOTUM PECTINACETYLESTERASE AND METHODS OF THEIR USE - Compounds are disclosed for the treatment, management and prevention of diseases and disorders affecting the bone. Particular compounds are potent inhibitors of Notum Pectinacetylesterase, and are of the formula: | 03-15-2012 |
20120065201 | INHIBITORS OF BRUTON'S TYROSINE KINASE - Described herein are irreversible kinase inhibitor compounds, methods for synthesizing such irreversible inhibitors, and methods for using such irreversible inhibitors in the treatment of diseases. Further described herein are methods, assays and systems for determining an appropriate irreversible inhibitor of a protein, including a kinase. | 03-15-2012 |
20120065202 | PYRIMIDINE DERIVATIVES AS mTOR INHIBITORS - The invention relates to compounds of formula (I) | 03-15-2012 |
20120071475 | UREA DERIVATIVES HAVING PI3K-INHIBITING ACTIVITY - Provided is a compound or a pharmaceutically acceptable salt thereof which inhibits the activity of PI3K to regulate many biological processes including the growth, differentiation, survival, proliferation, migration, metabolism, and the like of cells and is therefore useful for the prophylaxis/therapy of diseases including inflammatory diseases, arteriosclerosis, vascular/circulatory diseases, cancer/tumors, immune system diseases, cell proliferative diseases, infectious diseases, and the like. The above problem was solved by providing a urea derivative shown in the present specification, or a pharmaceutically acceptable salt thereof. | 03-22-2012 |
20120071476 | MORPHOLINOPURINE DERIVATIVES - There is provided a novel compound that inhibits phosphatidylinositol 3-kinase (PI3K) and/or the mammalian target of rapamycin (mTOR) and exhibits anti-tumor activity. The present invention provides a compound represented by the following formula (1) having various substituents that inhibits PI3K and/or mTOR and exhibits anti-tumor activity: | 03-22-2012 |
20120088764 | PHOSPHOINOSITIDE 3-KINASE INHIBITORS WITH A ZINC BINDING MOIETY - The instant application relates to deazapurines, thienopyrimidines and furopyrimidines with zinc-binding moiety based derivatives and their use in the treatment of phosphoinositide 3-kinase related diseases and disorders such as cancer. The instant application further relates to the treatment of histone deacetylase related disorders and diseases related to both histone deacetylase and phosphoinositide 3-kinase. | 04-12-2012 |
20120088765 | PURINE DERIVATIVE AND ANTITUMOR AGENT USING SAME - Disclosed are: a novel purine derivative, a composition thereof, a method for treating tumor using the purine derivative, and an antitumor agent using the purine derivative. Specifically disclosed is a compound represented by formula (I), or a pharmaceutically acceptable salt, solvate or hydrate thereof, or a prodrug thereof. | 04-12-2012 |
20120088766 | FUSED HETEROCYCLIC COMPOUNDS AND THEIR USES - The present application relates to therapeutic organic compounds, compositions comprising an effective amount of a therapeutic organic compound; and methods for treating and preventing disease comprising administering and effective amount of a therapeutic organic compound to a subject in need thereof. | 04-12-2012 |
20120101095 | ALKOXY-THIENOPYRIMIDINES AS TGF-BETA RECEPTOR KINASE MODULATORS - Novel alkoxy-thienopyrimidine derivatives of formula (I) | 04-26-2012 |
20120108587 | Aza- and Diaza-Phthalazine Compounds as P38 Map Kinase Modulators and Methods of Use Thereof - The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula (I) wherein A | 05-03-2012 |
20120108588 | NOVEL 3-AMIDO-PYRROLO[3,4-C]PYRAZOLE-5(1H, 4H,6H) CARBALDEHYDE DERIVATIVES - The present invention relates to compounds and pharmaceutically acceptable salts of Formula (I): | 05-03-2012 |
20120108589 | AZABICYCLO COMPOUND AND SALT THEREOF - It is intended to provide a novel azabicyclo compound which exhibits both HSP90 inhibitory activity and cell proliferation inhibitory effect. Specifically disclosed is a compound represented by the following general formula (I) or a salt thereof: wherein X | 05-03-2012 |
20120115863 | COMPOUNDS FOR THE TREATMENT OF CNS DISORDERS - The invention relates to novel cycloalkyl- or cycloalkenyl-substituted pyrazolopyrimidinones of formula (I), wherein Ā is selected from the group A | 05-10-2012 |
20120115864 | Substituted Fused Pyrimidine Compounds - The present invention discloses substituted fused pyrimidine compounds of formula (I), their tautomers, polymorphs, stereoisomers, solvates, pharmaceutically acceptable salts, or pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by adenosine receptor (AR) activity. The compounds of the present invention are useful in the treatment, prevention or suppression of diseases and disorders that may be susceptible to improvement by antagonism of the adenosine receptor, such as asthma, chronic obstructive pulmonary disorder, angiogenesis, pulmonary fibrosis, emphysema, allergic diseases, inflammation, reperfusion injury, myocardial ischemia, atherosclerosis, hypertension, congestive heart failure, retinopathy, diabetes mellitus, obesity, inflammatory gastrointestinal tract disorders, and/or autoimmune diseases. | 05-10-2012 |
20120129851 | Substituted Quinazoline and Pyrido-Pyrimidine Derivatives - The present application provides novel substituted quinazoline and pyrido-pyrimidine compounds and pharmaceutically acceptable salts 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. | 05-24-2012 |
20120129852 | AZAINDAZOLES AS KINASE INHIBITORS AND USE THEREOF - Compounds having the formula (I), and enantiomers, and diastereomers, pharmaceutically-acceptable salts, thereof, (I) are useful as kinase modulators, including Btk modulation, wherein A | 05-24-2012 |
20120135988 | PURINE PI3K INHIBITOR COMPOUNDS AND METHODS OF USE - Purine compounds of Formula I, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. | 05-31-2012 |
20120142683 | PYRIMIDINE SUBSTITUTED PURINE COMPOUNDS AS KINASE (S) INHIBITORS - The present invention relates to a purine compound useful as a kinase inhibitor. The compound has the structure (I) or a pharmaceutically acceptable salt thereof | 06-07-2012 |
20120142684 | COMPOUNDS AND METHODS FOR SKIN REPAIR - The disclosure provides compositions and methods for treating a skin blemish. The compositions comprise a therapeutically effective amount of a compound useful for treating skin blemishes such as wounds, scars and wrinkles. | 06-07-2012 |
20120149700 | 2-CYANOPHENYL FUSED HETEROCYCLIC COMPOUNDS, AND COMPOSTIONS AND USES THEREOF - Fused heterocyclic compounds are provided according to formula 1: | 06-14-2012 |
20120149701 | CERTAIN CHEMICAL ENTITIES, COMPOSITIONS AND METHODS - Chemical entities that modulate PI3 kinase activity, pharmaceutical compositions containing the chemical entities, and methods of using these chemical entities for treating diseases and conditions associated with P13 kinase activity are described herein. | 06-14-2012 |
20120157452 | 1H-PYRAZOLO[3,4-B] PYRIDINE COMPOUNDS FOR INHIBITING RAF KINASE - Compounds of Formula I are useful for inhibition of Raf kinases. Methods of using compounds of Formula I and stereoisomers, tautomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed. [FORMULA I] | 06-21-2012 |
20120157453 | RAF INHIBITOR COMPOUNDS AND METHODS OF USE THEREOF - Compounds of Formula II are useful for inhibition of Raf kinases. Methods of using compounds of Formula II and stereoisomers, tautomers, prodrugs and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed. | 06-21-2012 |
20120165328 | INHIBITORS OF B LYMPHOCYTE KINASE - Described herein are irreversible kinase inhibitor compounds, methods for synthesizing such irreversible inhibitors, and methods for using such irreversible inhibitors in the treatment of diseases. Further described herein are methods, assays and systems for determining an appropriate irreversible inhibitor of a protein, including a kinase. | 06-28-2012 |
20120165329 | COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR - Compounds and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof are active on at least one of Fms protein kinase or Kit protein kinase. Also described are methods of use thereof to treat diseases and conditions, including diseases and conditions associated with activity of Fms protein kinases and/or Kit protein kinases, including rheumatoid arthritis, osteoarthritis, osteoporosis, peri-prosthetic osteolysis, systemic sclerosis, demyelinating disorders, multiple sclerosis, Charcot Marie Tooth syndrome, amyotrophic lateral sclerosis, Alzheimer's disease, Parkinson's disease, ulcerative colitis, Crohn's disease, immune thrombocytopenic purpura, myelopreparation for autologous transplantation, transplant rejection, nephritis, nephropathy, type I diabetes, acute pain, inflammatory pain, neuropathic pain, breast cancer, prostate cancer, pancreatic cancer, lung cancer, ovarian cancer, gliomas, glioblastomas, neurofibromatosis, osteolytic bone metastases, and giant cell tumors. | 06-28-2012 |
20120178753 | INHIBITORS OF BRUTON'S TYROSINE KINASE - Described herein are irreversible kinase inhibitor compounds, methods for synthesizing such irreversible inhibitors, and methods for using such irreversible inhibitors in the treatment of diseases. Further described herein are methods, assays and systems for determining an appropriate irreversible inhibitor of a protein, including a kinase. | 07-12-2012 |
20120178754 | Furazano '3, 4-B! Pyrazines and Their Use as Anti-Tumor Agents - The present invention provides novel compounds and pharmaceutical compositions thereof, as well as methods for using the compounds and pharmaceutical compositions for treating tumors. Examples of specific tumor types that the compounds may be used to treat include, but are not limited to sarcomas, melanomas, neuroblastomas, carcinomas (including but not limited to lung, renal cell, ovarian, liver, bladder, and pancreatic carcinomas), and mesotheliomas. | 07-12-2012 |
20120184547 | METHODS FOR TREATING SCHIZOPHRENIA - Provided herein are PAK inhibitors. Also provided herein are compositions and methods for treating an individual suffering from schizophrenia. | 07-19-2012 |
20120190679 | Novel Protein Kinase B Inhibitors - 060 - The invention relates to a novel group of compounds of Formula (I) or salts thereof: | 07-26-2012 |
20120202809 | NOVEL N-PYRIMIDIN-4-YL-3-AMINO-PYRROLO[3,4-C]PYRAZOLE DERIVATIVES AS PKC KINASE INHIBITORS - The present invention relates to compounds and pharmaceutically acceptable salts of Formulas A and B: | 08-09-2012 |
20120220584 | HETEROCYCLIC COMPOUNDS AND METHODS OF USE - Heterocyclic compounds derived from benzotriazine, triazines, triazoles and oxadiazoles are disclosed. The methods of synthesis and of use of such heterocyclic compounds are also provided. | 08-30-2012 |
20120220585 | HETEROCYCLIC COMPOUNDS AND THEIR USES - Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110δ activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia (T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer. | 08-30-2012 |
20120220586 | HETEROCYCLIC COMPOUNDS AND THEIR USES - Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110δ activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia (T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer. | 08-30-2012 |
20120225869 | COMPOUNDS AND COMPOSITIONS AS INHIBITORS OF CANNABINOID RECEPTOR 1 ACTIVITY - The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of Cannabinoid Receptor 1 (CB1). | 09-06-2012 |
20120232077 | SELECTIVE ANTIBACTERIALS FOR CLOSTRIDIUM DIFFICILE INFECTIONS - The invention features compounds of formula (I): The compounds are useful as antibacterial agents, especially again | 09-13-2012 |
20120238568 | Pyrido[2,3-b]pyrazin-8-substituted Compounds and Their Use - The present invention pertains generally to the field of therapeutic compounds for treating proliferative disorders, cancer, etc., and more specifically to certain pyrido[2,3-b]pyrazin-8-substituted compounds, as described herein, which, inter alia, inhibit RAF (e.g., B-RAF) activity. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit RAF (e.g., BRAF) activity, to inhibit receptor tyrosine kinase (RTK) activity, to inhibit cell proliferation, and in the treatment of diseases and disorders that are ameliorated by the inhibition of RAF, RTK, etc., proliferative disorders such as cancer (e.g., colorectal cancer, melanoma), etc. | 09-20-2012 |
20120245168 | Composition, Synthesis, and Use of New Substituted Pyran and Pterin Compounds - The present invention relates to substituted pterin compounds, their synthesis and use. In particular, the present invention relates to a new precursor compound and its analogs for synthesizing a new substituted pterin compound and its analogs. These new compounds are particularly suitable for treating molybdenum cofactor deficiency. | 09-27-2012 |
20120245169 | CERTAIN CHEMICAL ENTITIES, COMPOSITIONS AND METHODS - Chemical entities that modulate PI3 kinase activity, pharmaceutical compositions containing the chemical entities, and methods of using these chemical entities for treating diseases and conditions associated with PI3 kinase activity are described herein. | 09-27-2012 |
20120245170 | PYRAZOLOPYRIDINE DERIVATIVES AS ANTICANCER AGENT - The present invention concerns compounds of following general formula (I): (Formula I) and their pharmaceutically acceptable salts, their method of preparation and their uses, notably as anticancer agent. | 09-27-2012 |
20120245171 | BENZPYRAZOLE DERIVATIVES AS INHIBITORS OF PI3 KINASES - The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): | 09-27-2012 |
20120264751 | PYRROLOPYRAZOLES, POTENT KINASE INHIBITORS - Pyrrole pyrazole compounds of formula I, compositions including these compounds and methods of their use are provided. Preferred compounds of formula I have activity as protein kinase inhibitors, including as inhibitors of PAK4. | 10-18-2012 |
20120270870 | Indazole and Pyrazolopyridine Compounds As CCR1 Receptor Antagonists - Diclosed are CCR1 receptor antagonists of the formula (I) | 10-25-2012 |
20120302567 | BICYCLIC HETEROARYL DERIVATIVES HAVING INHIBITORY ACTIVITY FOR PROTEIN KINASE - The present invention relates to a novel bicyclic heteroaryl derivative, a pharmaceutically acceptable salt thereof, a hydrate thereof, and a solvate thereof having an improved inhibitory activity for protein kinases, and a pharmaceutical composition for preventing or treating an abnormal cell growth disorder comprising same as an active ingredient. | 11-29-2012 |
20120309755 | NOVEL COMPOUNDS - This invention relates to compounds of formula I | 12-06-2012 |
20120316163 | Pyrazolo Piperidine Derivatives as NADPH Oxidase Inhibitors - The present invention is related to pyrazolo piperidine derivatives of Formula (I), pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase). | 12-13-2012 |
20120322799 | DEUTERATED COMPOUNDS USEFUL FOR TREATING NEURODEGENERATIVE DISEASES - The present application is related to deuterated compounds which are novel neurotrophin mimetics. The application also discloses the treatment of disorders involving degradation or dysfunction of cells expressing p75 in a mammal by administering an effective amount of such deuterated compounds. | 12-20-2012 |
20120329793 | Substituted Imidazopyridinyl Compounds - The present invention relates to substituted imidazopyridinyl compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted imidazopyridinyl 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 |
20130012507 | SUBSTITUTED PYRROLO-PYRAZOLE DERIVATIVES AS KINASE INHIBITORS - Compounds represented by formula (Ia) or (Ib) and wherein R and R | 01-10-2013 |
20130023531 | PYRIMIDO[5,4-D]PYRIMIDYLAMINO PHENYL SULFONAMIDES AS SERINE/THREONINE KINASE INHIBITORS - The present invention encompasses compounds of general formula (I) | 01-24-2013 |
20130023532 | INDAZOLYL-PYRIMIDINES AS KINASE INHIBITORS - Disclosed are compounds having the formula: or a salt thereof, wherein A, n, R | 01-24-2013 |
20130029983 | AMINOTHIENOPYRIDAZINE INHIBITORS OF TAU ASSEMBLY - The present invention is directed to methods of inhibiting a tauopathy in a patient by administration of a compound of formula I: | 01-31-2013 |
20130029984 | HETEROCYCLIC COMPOUNDS AND USES THEREOF - Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein. | 01-31-2013 |
20130035334 | INHIBITORS OF BRUTON'S TYROSINE KINASE - Described herein are irreversible kinase inhibitor compounds, methods for synthesizing such irreversible inhibitors, and methods for using such irreversible inhibitors in the treatment of diseases. Further described herein are methods, assays and systems for determining an appropriate irreversible inhibitor of a protein, including a kinase. | 02-07-2013 |
20130035335 | 8-ETHYL-6-(ARYL)PYRIDO[2,3-D]PYRIMIDIN-7(8H)-ONES FOR THE TREATMENT OF CNS DISORDERS - Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of CNS disorders such as neuropsychiatric disorders. | 02-07-2013 |
20130035336 | COMBINATION COMPRISING A CYCLIN DEPENDENT KINASE 4 OR CYCLIN DEPENDENT KINASE (CDK4/6) INHIBITOR FOR TREATING CANCER - A combination of a CDK4/8 inhibitor and an mTOR inhibitor for the treatment of cancer. | 02-07-2013 |
20130059847 | SUBSTITUTED N-(3-(PYRIMIDIN-4-YL)PHENYL)ACRYLAMIDE ANALOGS AS TYROSINE RECEPTOR KINASE BTK INHIBITORS - In one aspect, the invention relates to substituted N-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs, derivatives thereof, and related compounds, which are useful as inhibitors of the BTK kinase; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the BTK kinase. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. | 03-07-2013 |
20130059848 | CANNABINOID-2 AGONISTS - The present specification discloses cannabinoid-2 agonists, compositions comprising such cannabinoid-2 agonists, and methods of treating an individual suffering from a disease by administering compositions comprising such cannabinoid-2 agonists. (Formula I and III) | 03-07-2013 |
20130059849 | AZAINDAZOLES - Herein are disclosed azaindazoles of formula (I) | 03-07-2013 |
20130065894 | 6-(4-HYDROXY-PHENYL)-3-STYRYL-1H-PYRAZOLO[3,4-b]PYRIDINE-4-CARBOXYLIC ACID AMIDE DERIVATIVES AS KINASE INHIBITORS - The present invention relates to pyrazolo[3,4-b]pyridine compounds of the formula I, | 03-14-2013 |
20130065895 | 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. | 03-14-2013 |
20130072481 | mTOR SELECTIVE KINASE INHIBITORS - The 4-urea-phenyl substituted 6-morpholin-4-yl-pyrazolo[3,4-d]pyrimidine derivatives are potent and selective inhibitors of mTOR kinase and are useful in treating disorders related to abnormal mTOR activities such as cancer, immune disorders, cardiovascular disease, ocular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders. | 03-21-2013 |
20130072482 | ANTI-INFLAMMATORY COMPOUND HAVING INHIBITORY ACTIVITY AGAINST MULTIPLE TYROSINE KINASES AND PHARMACEUTICAL COMPOSITION CONTAINING SAME - The present invention is for the anti-inflammatory compounds that have an inhibitory activity against protein tyrosine kinases and their pharmaceutical composition(s) containing the compound as the active ingredient. Since the compounds of the present invention can inhibit multiple protein kinases associated with inflammatory diseases and immune disorders, they are useful for their prevention or treatment. | 03-21-2013 |
20130079341 | THIENO (2, 3B) PYRAZINE COMPOUNDS AS B-RAF INHIBITORS - The invention relates to compounds according to general Formula (I) or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of cancer. | 03-28-2013 |
20130079342 | HETEROCYCLIC COMPOUNDS AND THEIR USES - Substituted bicyclic heteroaryls of the following formulae and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110 activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia (T-ALL) B-cell Acute Lymphoblastic leukaemia ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer. | 03-28-2013 |
20130090335 | PHOSPHOINOSITIDE 3-KINASE INHIBITOR WITH A ZINC BINDING MOIETY - The invention provides a compound of Formula I, | 04-11-2013 |
20130090336 | N-CONTAINING HETEROCYCLIC COMPOUNDS - The present invention relates to N-containing heterocyclic compounds that are inhibitors of protein kinases including JAK kinases. In particular, the compounds are selective for JAK1, JAK2, JAK3 or TYK2 kinases and combinations thereof such as JAK1 and JAK2. The kinase inhibitors can be used in the treatment of kinase associated diseases such as immunological and inflammatory diseases including organ transplants; hyperproliferative diseases including cancer and myeloproliferative diseases; viral diseases; metabolic diseases; and vascular diseases. | 04-11-2013 |
20130096115 | METHODS FOR TREATING AUTISM - Provided herein are PAK inhibitors. Also provided herein are compositions and methods for treating an individual suffering from autism. | 04-18-2013 |
20130096116 | TREATMENT OF PHARMACOLOGICAL-INDUCED HYPOCHLORHYDRIA - Changes in gastric pH due to oral co-administration of acid-reducing agents, such as proton pump inhibitors, and oncology drugs can have a marked impact on the absorption and oral bioavailability of the oncology drug if the pH decreases the maximal absorbable dose. Moreover, there is a potential for specific drug-drug interactions between some of the acid-reducing agents and these drugs. Methods are described for treating patients on gastric acid-reducing therapy with orally-administered PI3K inhibitor compound GDC-0941. Treatment with a re-acidification compound during treatment with GDC-0941 improves bioavailability of GDC-0941. | 04-18-2013 |
20130102600 | Heteroaryl hydroxamic acid derivatives and their use in the treatment, amelioration or prevention of a viral disease - The present invention relates to a compound having the general formula I, optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, | 04-25-2013 |
20130102601 | Pyrimidin-4-one derivatives and their use in the treatment, amelioration or prevention of a viral disease - The present invention relates to a compound having the general formula II, optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, | 04-25-2013 |
20130123255 | COMBINATION OF A PI3K INHIBITOR AND A MEK INHIBITOR - The invention relates to a method for the treatment of a patient with a proliferative disease including solid tumors, hematological malignancies and hyperplasia comprising administering a therapeutic combination to said patient wherein the therapeutic combination comprises a therapeutically effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of a compound of formula (II) or a pharmaceutically acceptable salt thereof. | 05-16-2013 |
20130123256 | Pyrazolo Pyridine Derivatives as NADPH Oxidase Inhibitors - The present invention is related to pyrazolo pyridine derivatives of Formula (I), pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase). | 05-16-2013 |
20130131058 | 2-SUBSTITUTED-8-ALKYL-7-OXO-7,8-DIHYDROPYRIDO[2,3-D] PYRIMIDINE-6-CARBONITRILES AND USES THEREOF - Compounds according to Formula (I), as well salts thereof: wherein R | 05-23-2013 |
20130137685 | 2,5,7-SUBSTITUTED OXAZOLOPYRIMIDINE DERIVATIVES - The invention relates to oxazolopyrimidine compounds of formula (I), where A, R | 05-30-2013 |
20130143879 | PYRAZOLO PYRIDINE DERIVATIVES AS NADPH OXIDASE INHIBITORS - The present invention is related to pyrazolo pyridine derivatives of Formula (I), pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase). | 06-06-2013 |
20130158027 | PYRAZOLO PYRIDINE DERIVATIVES AS NADPH OXIDASE INHIBITORS - The present invention is related to pyrazolo pyridine derivatives of Formula (I), pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase). | 06-20-2013 |
20130158028 | USE OF STIMULATORS AND ACTIVATORS OF SOLUBLE GUANYLATE CYCLASE FOR TREATING SICKLE-CELL ANEMIA AND CONSERVING BLOOD SUBSTITUTES - The present invention relates to the novel use of stimulators and activators of soluble guanylate cyclase for the treatment of sickle cell anemia and for the preservation of blood substitutes. The present invention furthermore relates to the use of stimulators and activators of soluble guanylate cyclase in combination with PDE5 inhibitors for the treatment of sickle cell anemia and for the preservation of blood substitutes. | 06-20-2013 |
20130165439 | CHEMICAL COMPOUNDS - The present invention encompasses compounds of general formula (I) | 06-27-2013 |
20130172340 | SUBSTITUTED 2-(9H-PURIN-9-YL) ACETIC ACID ANALOGUES AS INHIBITORS OF STAT3 - In one aspect, the invention relates to substituted purine analogs, derivatives thereof, and related compounds, which are useful as inhibitors of STAT protein activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders of uncontrolled cellular proliferation associated with a STAT protein activity dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. | 07-04-2013 |
20130172341 | FUSED PYRAZOLE DERIVATIVES AS NOVEL ERK INHIBITORS - Disclosed are the ERK inhibitors of Formula (I): (Formula (I)) and the pharmaceutically acceptable salts thereof. All substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of Formula (I). | 07-04-2013 |
20130184274 | Protein Kinase Inhibitors and Methods of Treatment - The present invention relates to chemical compounds of formula (I) and methods for their use and preparation. In particular, the invention relates to substituted pyrazolo[3,4-d]pyrimidine based compounds which can be used in treating proliferative disorders, use of these compounds in methods of therapy and the manufacture of medicaments as well as compositions containing these compounds. | 07-18-2013 |
20130196988 | Dihydrothienopyrimidines - The present invention relates to dihydrothienopyrimidines, their use as modulators of γ-secretase and to pharmaceutical compositions containing said compounds. In particular, the present invention relates to compounds which interfere with γ-secretase and/or its substrate and therefore modulate the formation of Aβ peptides. | 08-01-2013 |
20130196989 | COMPOSITIONS AND METHODS FOR INDUCING CELL DEDIFFERENTIATION - The present invention provides compounds, compositions and methods for dedifferentiating lineage committed mammalian cells into stem cells. The present invention also provides methods of inducing dedifferentiation of lineage committed mammalian cells into stem cells, which can be further differentiated into various lineage committed cells. Methods of identifying additional compounds useful for inducing dedifferentiation of lineage committed cells into stem cells are also provided. | 08-01-2013 |
20130203755 | BICYCLIC HETEROARYL KINASE INHIBITORS AND METHODS OF USE - Provided are compounds having an inhibitory effect on kinases including Mixed Lineage Kinases. Also provided are pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions that are affected by Mixed Lineage Kinase inhibition. Also provided are methods of treatment of neuropsychiatric disorders that comprise the inhibition of Mixed Lineage Kinases. | 08-08-2013 |
20130225575 | METHODS FOR TREATING NEUROLOGICAL CONDITIONS - Provided herein are PAK inhibitors. Also provided herein are compositions and methods for treating an individual suffering from certain neurological conditions. | 08-29-2013 |
20130225576 | 1H-PYRAZOLO[3,4-B]PYRIDINES AND THERAPEUTIC USES THEREOF - Provided herein are compounds according to Formula I and pharmaceutically acceptable salts thereof, and compositions comprising the same, for use in various methods, including treating cancers such as colon, ovarian, pancreatic, breast, liver, prostate and hematologic cancers: | 08-29-2013 |
20130225577 | BICYCLIC DIAMINES AS JANUS KINASE INHIBITORS - The instant invention provides compounds of formula I which are Jak inhibitors, and as such are useful for the treatment of Jak-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer. | 08-29-2013 |
20130245012 | 6-(ETHYNYL)PYRIDO[2,3-D]PYRIMIDIN-7(8H)-ONES FOR THE TREATMENT OF CNS DISORDERS - Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of CNS disorders. | 09-19-2013 |
20130245013 | STORAGE STABLE PERFUSION SOLUTION FOR DIHYDROPTERIDINONES - Disclosed are storage stable aqueous infusible or injectable solutions containing an active substance of general formula (I) | 09-19-2013 |
20130252953 | Targeting Human Thymidylate Kinase Induces DNA Repair Toxicity in Malignant Tumor Cells - The present invention relates to novel TMPK inhibitor compositions and their methods of use. In particular, it relates to novel TMPK inhibitor compositions and therapeutics that lead to dUTP-mediated DNA repair in tumor cells and acts as a novel chemosensitizer, which are useful in methods for treating or preventing cancers. | 09-26-2013 |
20130261116 | NOVEL 3,5-DISUBSTITUTED-3H-IMIDAZO[4,5-B]PYRIDINE AND 3,5-DISUBSTITUTED -3H-[1,2,3]TRIAZOLO[4,5-B] PYRIDINE COMPOUNDS AS MODULATORS OF PROTEIN KINASES - The present invention provides, inter alia, compounds of formula I as protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them. | 10-03-2013 |
20130267513 | PYRAZOLOPYRIDINES AS INHIBITORS OF THE KINASE LRRK2 - A compound of formula Ia or formula Ib, or a pharmaceutically acceptable salt or ester thereof, wherein R | 10-10-2013 |
20130296318 | COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS - The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of B-Raf. | 11-07-2013 |
20130303533 | AZOLOPYRIDINE AND AZOLOPYRIMIDINE COMPOUNDS AND METHODS OF USE THEREOF - Provided herein are azolopyridine and azolopyrimidine compounds for treatment of JAK kinase mediated diseases, including JAK2 kinase-, JAK3 kinase- or TYK2 kinase-mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions. | 11-14-2013 |
20130317021 | HETEROCYCLIC PYRIMIDINE CARBONIC ACID DERIVATIVES WHICH ARE USEFUL IN THE TREATMENT, AMELIORATION OR PREVENTION OF A VIRAL DISEASE - The present invention relates to a compound having the general formula (C), optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, codrug, cocrystal, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, | 11-28-2013 |
20130317022 | 7-OXO-THIAZOLOPYRIDINE CARBONIC ACID DERIVATIVES AND THEIR USE IN THE TREATMENT, AMELIORATION OR PREVENTION OF A VIRAL DISEASE - The present invention relates to a compound having the general formula (A), optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, codrug, cocrystal, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, | 11-28-2013 |
20130317023 | NOVEL PURINYLPYRIDINYLAMINO-2,4-DIFLUOROPHENYL SULFONAMIDE DERIVATIVE, PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION WITH INHIBITORY ACTIVITY AGAINST RAF KINASE, CONTAINING SAME AS ACTIVE INGREDIENT - A novel purinylpyridinylamino-2,4-difluorophenyl sulfonamide derivative, a pharmaceutically acceptable salt thereof, a preparation method thereof, and a pharmaceutical composition with an inhibitory activity against Raf kinase, containing the same as an active ingredient are provided. The purinylpyridinylamino-2,4-difluorophenyl sulfonamide derivative of the present invention effectively regulates the activity of B-Raf kinase, and thus may be useful for preventing or treating cancers induced by the over-activation of Raf kinase, especially various melanoma, colorectal cancer, prostate cancer, thyroid cancer, ovarian cancer and the like. | 11-28-2013 |
20130324528 | PYRAZOLO[4,3-B]PYRIDINE-7-AMINE INHIBITORS OF ALK5 - The present invention provides ALK5 inhibitors of the formula | 12-05-2013 |
20130338157 | AZAINDAZOLE COMPOUNDS AND METHODS OF USE - Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists. | 12-19-2013 |
20130345215 | PYRAZOLOPYRIMIDONE AND PYRAZOLOPYRIDONE INHIBITORS OF TANKYRASE - There are provided compounds of the formula | 12-26-2013 |
20130345216 | CERTAIN CHEMICAL ENTITIES, COMPOSITIONS AND METHODS - Chemical entities that modulate PI3 kinase activity, pharmaceutical compositions containing the chemical entities, and methods of using these chemical entities for treating diseases and conditions associated with PI3 kinase activity are described herein. | 12-26-2013 |
20130345217 | COMBINATIONS OF PHOSPHOINOSITIDE 3-KINASE INHIBITOR COMPOUNDS AND CHEMOTHERAPEUTIC AGENTS, AND METHODS OF USE - Combinations of PI3K inhibitor compounds having Formulas I and II and chemotherapeutic agents, including stereoisomers, geometric isomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for treating hyperproliferative disorders such as cancer. Methods of using such combinations for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. | 12-26-2013 |
20140005191 | SELECTIVE GLYCOSIDASE INHIBITORS AND USES THEREOF | 01-02-2014 |
20140005192 | INHIBITORS OF INFLUENZA VIRUSES REPLICATION | 01-02-2014 |
20140018361 | IRAK INHIBITORS AND USES THEREOF - The present invention provides furano- and pyrrolo-pyrimidine and pyridine compounds, compositions thereof, and methods of using the same. | 01-16-2014 |
20140038956 | Use of sGC stimulators, sGC activators, alone and combinations with PDE5 inhibitors for the treatment of systemic sclerosis (SSc). - The use of sGC stimulators, sGC activators alone, or in combination with PDE5 inhibitors for the prevention and treatment of fibrotic diseases, such as systemic sclerosis, scleroderma, and the concomitant fibrosis of internal organs. | 02-06-2014 |
20140038957 | ASK 1 INHIBITING PYRROLOPYRIMIDINE DERIVATIVES - This invention relates to pyrrolopyrimidine derivatives of formula (I): where R | 02-06-2014 |
20140045837 | 9-Substituted 8-Oxoadenine Compound - The present invention provides an 8-oxoadenine compound having immunomodulating activities such as an interferon inducing activity and useful as an antiviral agent and antiallergic agent, which is represented by the following formula (1): | 02-13-2014 |
20140051698 | Pyrazolo [3,4-D] Pyrimidine Derivatives Useful to Treat Respiratory Disorders - The present invention concerns a compound of formula (I) | 02-20-2014 |
20140051699 | 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. | 02-20-2014 |
20140057907 | INHIBITORS OF BRUTON'S TYROSINE KINASE - Described herein are irreversible kinase inhibitor compounds, methods for synthesizing such irreversible inhibitors, and methods for using such irreversible inhibitors in the treatment of diseases. Further described herein are methods, assays and systems for determining an appropriate irreversible inhibitor of a protein, including a kinase. | 02-27-2014 |
20140066443 | AMINOMETHYL BIARYL BENZOTRIAZOLE DERIVATIVES - The present invention is directed to aminomethyl biaryl benzotriazole derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved. | 03-06-2014 |
20140073639 | INHIBITION OF ANTIMICROBIAL TARGETS WITH REDUCED POTENTIAL FOR RESISTANCE - The application describes targets and methods that can inhibit bacterial growth in Gram-positive and Gram-negative bacteria. A bacterial enzyme, 2-epimerase, is common to both Gram-positive and Gram-negative bacteria and contains an allosteric site that can be targeted to disrupt the enzyme. The allosteric site is present on the bacterial 2-epimerase, but the analogous mammalian enzyme does not contain the allosteric site, providing a route for attacking bacterial infections without affecting the mammalian enzyme. | 03-13-2014 |
20140073640 | APOPTOSIS-INDUCING AGENTS FOR THE TREATMENT OF CANCER AND IMMUNE AND AUTOIMMUNE DISEASES - Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-xL protein. | 03-13-2014 |
20140073641 | 1-HETEROCYCLYL-1,5-DIHYDRO-PYRAZOLO[3,4-D] PYRIMIDIN-4-ONE DERIVATIVES AND THEIR USE AS PDE9A MODULATORS - The invention relates to novel 1,6-disubstituted pyrazolopyrimidinones, wherein i.) the nitrogen atom of the pyrazolo-group that is next to the pyrimidino-group is attached to a non-aromatic, organic heterocycle having at least one ring hetero atom selected from O, N and S and ii.) to the C-atom between the two nitrogen atoms of the pyrimidinone-ring a second substituent is bound via an optionally substituted methylene-bridge. According to one aspect of the invention the new compounds are for the manufacture of medicaments, in particular medicaments for the treatment of conditions concerning deficits in perception, concentration, learning or memory. The new compounds are also for the manufacture of medicaments for the treatment of Alzheimer's disease. | 03-13-2014 |
20140080827 | NOVEL KINASE MODULATORS - The present invention provides PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them. | 03-20-2014 |
20140088099 | CHEMICAL COMPOUNDS, COMPOSITIONS AND METHODS FOR KINASE MODULATION - Chemical compounds that modulate kinase activity, including PI3 kinase activity, and chemical compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including P13 kinase activity, are described herein. | 03-27-2014 |
20140094459 | Tyrosine Kinase Inhibitors - The present disclosure provides compounds and pharmaceutically acceptable salts thereof that are tyrosine kinase inhibitors, in particular BLK, BMX, EGFR, HER2, HER4, ITK, TEC, BTK, and TXK and are therefore useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as cancer and inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and pharmaceutically acceptable salts thereof and processes for preparing such compounds and pharmaceutically acceptable salts thereof. | 04-03-2014 |
20140100224 | NEUROTROPHIN MIMETICS AND USES THEREOF - The present application is related to compounds which are novel neurotrophin mimetics. The application also discloses the treatment of disorders associated with p75 expression, such as degradation or dysfunction of cells expressing p75 in a mammal by administering an effective amount of such compounds. | 04-10-2014 |
20140107118 | Novel Heterocyclic Derivatives and Their Use in the Treatment of Neurological Disorders - The invention relates to novel heterocyclic compounds of the formula | 04-17-2014 |
20140121205 | PYRAZOLOPYRIDAZINES AND METHODS FOR TREATING RETINAL-DEGERATIVE DISEASES AND HEARING LOSS ASSOCIATED WITH USHER SYNDROME - Compounds, compositions and methods for the treatment of retinal degenerative diseases, such as retinitis pigmentosa, Leber's congenital Amaurosis, Syndromic retinal degenerations, age-related macular degeneration and Usher Syndrome, and hearing loss associated with Usher Syndrome are described herein. | 05-01-2014 |
20140128388 | TARGETING AN HIV-1 NEF-HOST CELL KINASE COMPLEX - Drug candidates for inhibition of HIV-1 replication can target Src family kinases (SFK), such as Hck, that interact with Nef protein of the virus. Compounds characterized by such inhibitory activity were identified via an assay for kinase activity of an SFK in a Nef:SFK complex. Illustrative of inhibitors identified using the kinase assay are various 2,3-diaminoquinaxolines and furo[2,3-d]pyrimidines. The inventive inhibitors were found to arrest HIV-1 viral replication in vitro. | 05-08-2014 |
20140128389 | DERIVATIVES OF PURINE OR DEAZAPURINE USEFUL FOR THE TREATMENT OF (INTER ALIA) VIRAL INFECTIONS - The present application includes novel modulators of TLRs, compositions containing such compounds, therapeutic methods that include the administration of such compounds. | 05-08-2014 |
20140128390 | COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR - Compounds active on c-kit protein kinases or mutant c-kit protein kinases having any mutations are described, as well as methods of making and using such compounds to treat diseases and conditions associated with aberrant activity of the c-kit protein kinases and mutant c-kit protein kinases. | 05-08-2014 |
20140142098 | TRIAZOLOPYRAZINE - Disclosed are compounds of the formula (I) | 05-22-2014 |
20140142099 | Purinone Derivatives as Tyrosine Kinase Inhibitors - The present disclosure provides compounds and pharmaceutically acceptable salts thereof that are tyrosine kinase inhibitors, in particular BLK, BMX, EGFR, HER2, HER4, ITK, TEC, BTK, and TXK and are therefore useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as autoimmune diseases, cancer and inflammatory diseases. Also provided are pharmaceutical compositions containing such compounds and pharmaceutically acceptable salts thereof and processes for preparing such compounds and pharmaceutically acceptable salts thereof. | 05-22-2014 |
20140142100 | NEW MACROLIDES AND THEIR USE - The invention relates to macrolide compounds of formula (I), | 05-22-2014 |
20140155393 | 1,2,4-TRIAZOLO[4,3-a]PYRIDINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS - The present invention relates to novel triazolo[4,3-a]pyridine derivatives of Formula (I) | 06-05-2014 |
20140155394 | Chemical Compounds - 759 - The present invention relates to compounds of Formula (I): | 06-05-2014 |
20140155395 | SUBSTITUTED AZA-BICYCLIC IMIDAZOLE DERIVATIVES USEFUL AS TRPM8 RECEPTOR MODULATORS - The present invention is directed to substituted aza-bicyclic imidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by TRP M8, including for example, inflammatory pain, inflammatory hyperalgesia, inflammatory hypersensitivity condition, neuropathic pain, neuropathic cold allodynia, inflammatory somatic hyperalgesia, inflammatory visceral hyperalgesia, cardiovascular disease aggravated by cold and pulmonary disease aggravated by cold. | 06-05-2014 |
20140163026 | 8-ETHYL-6-(ARYL)PYRIDO[2,3-D]PYRIMIDIN-7(8H)-ONES FOR THE TREATMENT OF NERVOUS SYSTEM DISORDERS AND CANCER - Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of CNS disorders such as neuropsychiatric disorders or neurofibromatosis. Also described herein are methods of utilizing PAK inhibitors for the treatment of cancer. | 06-12-2014 |
20140163027 | INHIBITORS OF BRUTON'S TYROSINE KINASE - Described herein are irreversible kinase inhibitor compounds, methods for synthesizing such irreversible inhibitors, and methods for using such irreversible inhibitors in the treatment of diseases. Further described herein are methods, assays and systems for determining an appropriate irreversible inhibitor of a protein, including a kinase. | 06-12-2014 |
20140171428 | METHODS AND COMPOSITIONS FOR STIMULATING NEUROGENESIS AND INHIBITING NEURONAL DEGENERATION USING ISOTHIAZOLOPYRIMIDINONES - The present invention provides methods and compositions comprising compounds useful for stimulating neurogenesis. The methods and compositions comprising compounds are also useful for inhibiting neuronal degeneration. Thus, the present invention can be used in the treatment of diseases and conditions characterized by neuronal loss and reduced neurogenesis including Alzheimer's disease, stroke, traumatic brain injury, traumatic nerve injury, and depression. This invention is useful for research products including single agents or mixtures of agents to promote, proliferate, differentiate, or maintain neurons from stem or progenitor cells. | 06-19-2014 |
20140179696 | INDAZOLE INHIBITORS OF THE WNT SIGNAL PATHWAY AND THERAPEUTIC USES THEREOF - Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states. | 06-26-2014 |
20140194420 | AZABENZIMIDAZOLE DERIVATIVE HAVING AMPK-ACTIVATING ACTIVITY - Disclosed is a compound which is useful as an AMPK activator. | 07-10-2014 |
20140206684 | CERTAIN CHEMICAL ENTITIES, COMPOSITIONS AND METHODS - Chemical entities that modulate PI3 kinase activity, and chemical entities, pharmaceutical compositions, and methods of treatments of diseases and conditions associated with P13 kinase activity are described herein. | 07-24-2014 |
20140206685 | HETEROCYCLIC KINASE INHIBITORS - The present invention provides heterocyclic compounds for use as kinase inhibitors and in other applications. Also provided are pharmaceutical compositions and methods of treatments of diseases and conditions associated with P13 kinase activity. | 07-24-2014 |
20140213584 | SELECTIVE GLYCOSIDASE INHIBITORS AND USES THEREOF - The invention provides compounds for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc. | 07-31-2014 |
20140221367 | PHARMACEUTICAL COMPOUNDS - Provided herein is a pharmaceutical composition that comprises a pharmaceutically acceptable carrier or diluent and, as an active ingredient, the compound 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine bismesylate. | 08-07-2014 |
20140235632 | PYRAZOLO [3,4-D] PYRIMIDINE DERIVATIVES USEFUL TO TREAT RESPIRATORY DISORDERS - The present invention concerns a compound of formula (I) | 08-21-2014 |
20140243330 | PHOSPHOINOSITIDE 3-KINASE INHIBITOR WITH A ZINC BINDING MOIETY - The invention provides a compound of Formula I, | 08-28-2014 |
20140275069 | Novel inhibitor compounds of phosphodiesterase type 10A - The present invention relates to compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof: | 09-18-2014 |
20140275070 | COMPOSITIONS COMPRISING THIENOPYRIMIDINE AND THIENOPYRIDINE COMPOUNDS AND METHODS OF USE THEREOF - The present invention relates generally to thienopyrimidine and thienopyridine class compounds and methods of use thereof. In particular embodiments, the present invention provides compositions comprising thienopyrimidine class compounds and methods of use to inhibit the interaction of menin with MLL1, MLL2 and MLL-fusion oncoproteins (e.g., for the treatment of leukemia, solid cancers and other diseases dependent on activity of MLL1 and MLL2 or menin). | 09-18-2014 |
20140275071 | SUBSTITUTED XANTHINES AND METHODS OF USE THEREOF - Compounds, compositions and methods are described for inhibiting the TRPC5 ion channel and disorders related to TRPC5. | 09-18-2014 |
20140275072 | MORPHOLINYLBENZOTRIAZINES FOR USE IN CANCER THERAPY - The invention relates to compounds of the formula (I) in which R1, L and m have the meaning indicated in the claims, and/or physiologically acceptable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. | 09-18-2014 |
20140288070 | COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR - Compounds and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof are active on at least one Raf protein kinase. In certain aspects and embodiments, the described compounds are active in inhibiting proliferation of a Ras mutant cell line. Also described are methods of use thereof to treat diseases and conditions, including diseases and conditions associated with activity of B-Raf V600E mutant protein kinase, including melanoma, glioma, glioblastoma multiforme, pilocytic astrocytoma, colorectal cancer, thyroid cancer, lung cancer, ovarian cancer, prostate cancer, liver cancer, gallbladder cancer, gastrointestinal stromal tumors, biliary tract cancer, and cholangiocarcinoma. Also described are methods of use thereof to treat diseases and conditions, including diseases and conditions associated with activity of c-Raf-1 protein kinase, including acute pain, chronic pain or polycystic kidney disease. | 09-25-2014 |
20140288071 | INHIBITORS OF NOTUM PECTINACETYLESTERASE AND METHODS OF THEIR USE - Compounds are disclosed for the treatment, management and prevention of diseases and disorders affecting the bone. Particular compounds are potent inhibitors of Notum Pectinacetylesterase, and are of the formula: | 09-25-2014 |
20140288072 | 5 - BENZYLAMINOMETHYL - 6 - AMINOPYRAZOLO [3, 4 -B] PYRIDINE DERIVATIVES AS CHOLESTERYL ESTER-TRANSFER PROTEIN (CETP) INHIBITORS USEFUL FOR THE TREATMENT OF ATHEROSCLEROSIS - The present application relates to a series of substituted pyra-zolopyridin-6-amines having the general formula (I), including their stereoisomers and/or their pharmaceutically acceptable salts. Wherein R, R | 09-25-2014 |
20140296233 | HETEROARYL COMPOUNDS AND USES THEREOF - The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same. | 10-02-2014 |
20140296234 | PYRIMIDINE DERIVATIVES AS MTOR INHIBITORS - The invention relates to compounds of formula (I) | 10-02-2014 |
20140303161 | TYROSINE KINASE INHIBITORS - The present disclosure provides compounds and pharmaceutically acceptable salts thereof that are tyrosine kinase inhibitors, in particular BLK, BMX, EGFR, HER2, HER4, ITK, TEC, BTK, and TXK and are therefore useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as cancer and inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and pharmaceutically acceptable salts thereof and processes for preparing such compounds and pharmaceutically acceptable salts thereof. | 10-09-2014 |
20140303162 | AZABICYCLO COMPOUND AND SALT THEREOF - It is intended to provide a novel azabicyclo compound which exhibits both HSP90 inhibitory activity and cell proliferation inhibitory effect. Specifically disclosed is a compound represented by the following general formula (I) or a salt thereof: wherein X | 10-09-2014 |
20140309222 | Therapeutically Active Fused Pyrimidine Derivatives - A series of monocyclic or bicyclic diamine-substituted thieno[2,3-d]pyrimidine and isothiazolo[5,4-d]pyrimidine derivatives are beneficial in the treatment and/or prevention of various human ailments, including inflammatory, autoimmune and oncological disorders; viral diseases; and organ and cell transplant rejection. | 10-16-2014 |
20140309223 | TYROSINE KINASE INHIBITORS - The present disclosure provides compounds and pharmaceutically acceptable salts thereof that are tyrosine kinase inhibitors, in particular BLK, BMX, EGFR, HER2, HER4, ITK, TEC, BTK, and TXK and are therefore useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as cancer and inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and pharmaceutically acceptable salts thereof and processes for preparing such compounds and pharmaceutically acceptable salts thereof. | 10-16-2014 |
20140315900 | METHODS FOR TREATING CANCER USING DIHYDROPYRAZINO-PYRAZINE COMPOUND COMBINATION THERAPY - Provided herein are methods for treating or preventing a cancer, comprising administering an effective amount of a Dihydropyrazino-Pyrazine Compound and an effective amount of an androgen receptor antagonist to a patient having a cancer. | 10-23-2014 |
20140323477 | SERINE/THREONINE KINASE INHIBITORS - Compounds having the formula I, or a pharmaceutically acceptable salt thereof, wherein R | 10-30-2014 |
20140323478 | SERINE/THREONINE KINASE INHIBITORS - Compounds having the formula I, or a pharmaceutically acceptable salt thereof, wherein R | 10-30-2014 |
20140323479 | 1H-PYRAZOLO[3,4-B]PYRIDINES AND THERAPEUTIC USES THEREOF - Provided herein are compounds according to Formula I and pharmaceutically acceptable salts thereof, and compositions comprising the same, for use in various methods, including treating cancers such as colon, ovarian, pancreatic, breast, liver, prostate and hematologic cancers: | 10-30-2014 |
20140323480 | Imidazopyridine Derivatives As PI3 Kinase - This invention relates to the use of imidizopyridine derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3′ OH kinase family (hereinafter PI3 kinases), suitably, PI3Kα, PI3Kδ, PI3Kβ, and/or PI3Kγ. Suitably, the present invention relates to the use of imidizopyridines in the treatment of one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries. More suitably, the present invention relates to PI3Kβ selective imidizopyridine compounds for treating cancer. | 10-30-2014 |
20140343056 | AZAINDAZOLES - Herein are disclosed azaindazoles of formula (I) | 11-20-2014 |
20140343057 | TREATMENT OF LUPUS, FIBROTIC CONDITIONS, AND INFLAMMATORY MYOPATHIES AND OTHER DISORDERS USING PI3 KINASE INHIBITORS - Provided herein are methods, kits, and pharmaceutical compositions that include a PI3 kinase inhibitor for treating lupus, a fibrotic condition, or inflammatory myopathies and other conditions (e.g., skin conditions). | 11-20-2014 |
20140350010 | Pyrazolopyrrolidine Compounds - The invention relates to compounds of formula (I) as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds. | 11-27-2014 |
20140350011 | Imidazo[4,5-b]pyridine Derivatives as ALK and JAK Modulators for the Treatment of Proliferative Disorders - This application relates to compounds of the Formula I | 11-27-2014 |
20140350012 | PIPERIDINE/PIPERAZINE DERIVATIVES - The invention further relates to a DGAT inhibitor of formula | 11-27-2014 |
20140364430 | METHODS FOR TREATING SCHIZOPHRENIA - Provided herein are PAK inhibitors. Also provided herein are compositions and methods for treating an individual suffering from schizophrenia | 12-11-2014 |
20140371219 | THIENO[3,2-D]PYRIMIDINE DERIVATIVES HAVING INHIBITORY ACTIVITY FOR PROTEIN KINASES - Provided are a thieno[3,2-d]pyrimidine derivative of formula (I) or a pharmaceutically acceptable salt thereof having inhibitory activity for protein kinase, and a pharmaceutical composition comprising same for prevention and treatment of abnormal cell growth diseases. | 12-18-2014 |
20140378451 | Cannabinoid-2-Receptor Agonists - The present invention relates to cannabinoid-2-receptor (CB2R) agonist compounds. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them and to their use as therapeutic agents for the treatment and/or prevention of diseases or conditions in which CB2R stimulation is beneficial (especially inflammatory conditions). | 12-25-2014 |
20140378452 | Treatment of Neurodegenerative Diseases Through Inhibition of HSP90 - Treatment of neurodegenerative diseases is achieved using small molecule purine scaffold compounds that inhibit Hsp90 and that possess the ability to cross the blood-brain barrier or are other wise delivered to the brain. | 12-25-2014 |
20150011545 | Chemical Compounds - 759 - The present invention relates to compounds of Formula (I): | 01-08-2015 |
20150011546 | MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF - Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein. | 01-08-2015 |
20150011547 | SUBSTITUTED QUINAZOLINE AND PYRIDO-PYRIMIDINE DERIVATIVES - The present application provides novel substituted quinazoline and pyrido-pyrimidine compounds and pharmaceutically acceptable salts 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. | 01-08-2015 |
20150018349 | SUBSTITUTED N-(3-(PYRIMIDIN-4-YL)PHENYL)ACRYLAMIDE ANALOGS AS TYROSINE RECEPTOR KINASE BTK INHIBITORS - In one aspect, the invention relates to substituted N-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs, derivatives thereof, and related compounds, which are useful as inhibitors of the BTK kinase; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the BTK kinase. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. | 01-15-2015 |
20150018350 | N-CONTAINING HETEROCYCLIC COMPOUNDS - The present invention relates to N-containing heterocyclic compounds that are inhibitors of protein kinases including JAK kinases. In particular, the compounds are selective for JAK1, JAK2, JAK3 or TYK2 kinases and combinations thereof such as JAK1 and JAK2. The kinase inhibitors can be used in the treatment of kinase associated diseases such as immunological and inflammatory diseases including organ transplants; hyperproliferative diseases including cancer and myeloproliferative diseases; viral diseases; metabolic diseases; and vascular diseases. | 01-15-2015 |
20150025070 | NOVEL 2-PIPERIDIN-1-YL-ACETAMIDE COMPOUNDS FOR USE AS TANKYRASE INHIBITORS - The present invention provides for compounds of formula (I): | 01-22-2015 |
20150031693 | PAK INHIBITORS FOR THE TREATMENT OF FRAGILE X SYNDROME - Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of Fragile X syndrome. | 01-29-2015 |
20150031694 | ANTIMICROBIAL AGENTS - The invention provides compounds of formula (I): wherein R | 01-29-2015 |
20150045359 | MORPHOLINE COMPOUNDS AND USES THEREOF - The present invention relates to compounds of formula | 02-12-2015 |
20150045360 | 1H-PYRAZOLO[3,4-B]PYRIDINES AND THERAPEUTIC USES THEREOF - Provided herein are compounds according to Formula I and pharmaceutically acceptable salts thereof, and compositions comprising the same, for use in various methods, including treating cancers such as colon, ovarian, pancreatic, breast, liver, prostate and hematologic cancers: | 02-12-2015 |
20150045361 | HETEROCYCLIC COMPOUNDS AND THEIR USES - Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110δ activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia (T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer. | 02-12-2015 |
20150051208 | PYRIDINONES - The present invention encompasses compounds of general formula (I) | 02-19-2015 |
20150065501 | N-substituted hetero-bicyclic furanone derivatives for combating animal - The invention relates to N-substituted hetero-bicyclic furanone compounds of formula (I), to the enantiomers, diastereomers and salts thereof and to compositions comprising such compounds. The invention also relates to methods and uses of these N-substituted hetero-bicyclic furanone compounds, and of compositions comprising thereof, for combating and controlling animal pests. Furthermore the invention relates also to pesticidal methods of applying such N-substituted hetero-bicyclic furanone compounds. | 03-05-2015 |
20150072981 | 1H-PYRAZOLO[3,4-B]PYRIDINES AND THERAPEUTIC USES THEREOF - Provided herein are compounds according to Formulas (I) or (II) and pharmaceutically acceptable salts thereof, and compositions comprising the same, for use in various methods, including treating cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease, osteoarthritis, idiopathic pulmonary fibrosis and neurological conditions/disorders/diseases. | 03-12-2015 |
20150072982 | AZA-PYRIDONE COMPOUNDS AND USES THEREOF - Disclosed herein are aza-pyridone compounds, pharmaceutical compositions that include one or more aza-pyridone compounds, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a disease and/or a condition, including an orthomyxovirus infection, with an aza-pyridone compounds. Examples of an orthomyxovirus viral infection include an influenza infection. | 03-12-2015 |
20150080391 | NOVEL COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF PROLIFERATIVE DISORDERS - The present invention discloses compounds according to Formula I: | 03-19-2015 |
20150087643 | Substituted Fused Pyrimidine Compounds - The present invention discloses substituted fused pyrimidine compounds of formula (I), their tautomers, polymorphs, stereoisomers, solvates, pharmaceutically acceptable salts, or pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by adenosine receptor (AR) activity; the compounds of the present invention are useful in the treatment, prevention or suppression of diseases and disorders that may be susceptible to improvement by antagonism of the adenosine receptor, such as asthma, chronic obstructive pulmonary disorder, angiogenesis, pulmonary fibrosis, emphysema, allergic diseases, inflammation, reperfusion injury, myocardial ischemia, atherosclerosis, hypertension, congestive heart failure, retinopathy, diabetes mellitus, obesity, inflammatory gastrointestinal tract disorders, and/or autoimmune diseases. | 03-26-2015 |
20150087644 | PYRROLIDINO HETEROCYCLES - The invention relates to compounds of formula I | 03-26-2015 |
20150094305 | IRAK INHIBITORS AND USES THEREOF - The present invention provides compounds, compositions thereof, and methods of using the same. | 04-02-2015 |
20150099743 | NOVEL N-PYRIMIDIN-4-YL-3-AMINO-PYRROLO[3,4-C]PYRAZOLE DERIVATIVES AS PKC KINASE INHIBITORS - The present invention relates to compounds and pharmaceutically acceptable salts of Formulas A and B: | 04-09-2015 |
20150099744 | COMBINATIONS OF HISTONE DEACETYLASE INHIBITORS AND EITHER HER2 INHIBITORS OR PI3K INHIBITORS - The invention relates to combinations comprising an HDAC inhibitor and a Her2 inhibitor for the treatrent of breast cancer in a subject in need thereof. The invention also relates to combinations comprising an HDAC inhibitor and a PI3K inhibitor for the treatment of breast cancer in a subject in need thereof. Also provided herein are methods for treating breast cancer in a subject in need thereof comprising administering to the subject an effective amount of one of the above combinations. Further provided are methods for inhibiting migration and/or invasion of a breast cancer cell in a subject by administering to the subject a HDAC6 specific inhibitor. | 04-09-2015 |
20150105382 | PYRIMIDINE SUBSTITUTED PURINE COMPOUNDS AS KINASE (S) INHIBITORS - The present invention relates to a purine compound useful as a kinase inhibitor. The compound has the structure: | 04-16-2015 |
20150105383 | HDAC Inhibitors, Alone Or In Combination With PI3K Inhibitors, For Treating Non-Hodgkin's Lymphoma - The invention relates to HDAC inhibitors, or combinations comprising an HDAC inhibitor and a PI3K inhibitor for the treatment of non-hodgkin's lymphoma in a subject in need thereof. Also provided herein are methods for treating non-hodgkin's lymphoma in a subject in need thereof comprising administering to the subject a therapeutically effective amount of an HDAC inhibitor, or a combination comprising an HDAC inhibitor and a PI3K inhibitor. | 04-16-2015 |
20150119392 | RAF INHIBITOR COMPOUNDS - This invention provides compounds of Formula I: (Formula I should be inserted here) or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising a compound of Formula I; and use of a compound of Formula I for treating specified cancers. | 04-30-2015 |
20150119393 | NEW AZABENZIMIDAZOLE DERIVATIVES - The present invention relates to compounds of general formula I, | 04-30-2015 |
20150126508 | PTERIDINE KETONE DERIVATIVE AND APPLICATIONS THEREOF AS EGFR, BLK, AND FLT3 INHIBITOR - Provided are a pteridine ketone derivative used as an EGFR, BLK, and FLT3 inhibitor and applications thereof. Specifically, provided are a compound of the following formula I, a pharmaceutical composition containing the compound of the formula I, and use of compound in preparing medicine for treating diseases mediated by EGFR, BLK, or FLT3 or inhibiting EGFR, BLK, and FLT3. | 05-07-2015 |
20150126509 | DERIVATIVES OF PURINE OR DEAZAPURINE USEFUL FOR THE TREATMENT OF (INTER ALIA) VIRAL INFECTIONS - The present application includes novel modulators of TLRs, compositions containing such compounds, therapeutic methods that include the administration of such compounds. | 05-07-2015 |
20150133449 | NOVEL 3,5-DISUBSTITUTED-3H-IMIDAZO[4,5-B]PYRIDINE AND 3,5-DISUBSTITUTED -3H-[1,2,3]TRIAZOLO[4,5-B] PYRIDINE COMPOUNDS AS MODULATORS OF PROTEIN KINASES - The present invention provides, inter alia, compounds of formula I as protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them. | 05-14-2015 |
20150290208 | PYRAZOLO PYRIDINE DERIVATIVES AS NADPH OXIDASE INHIBITORS - The present invention is related to pyrazolo pyridine derivatives of Formula (I), pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase). | 10-15-2015 |
20150291582 | PYRAZOLOPYRIDINE DERIVATIVES AS TTX-S BLOCKERS - The present invention relates to pyrazolopyridine 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. | 10-15-2015 |
20150297605 | METHODS FOR TREATING CANCER USING TOR KINASE INHIBITOR COMBINATION THERAPY - Provided herein are methods for treating or preventing a cancer, comprising administering an effective amount of a TOR kinase inhibitor and an effective amount a second active agent to a patient having a cancer. | 10-22-2015 |
20150299185 | NOVEL IMIDAZOPYRIDINE DERIVATIVES AS A TYROSINE KINASE INHIBITOR - Provided is a novel imidazopyridine derivative having irreversible tyrosine kinase inhibiting activities, and a pharmaceutical composition comprising the same which can be useful for prevention or treatment of inflammatory diseases, autoimmune diseases, proliferative diseases or hyperproliferative diseases, immunologically mediated diseases, cancers or tumors. | 10-22-2015 |
20150307516 | 2,5,6,7-tetrasubstituted Thiazolo[4,5-b]pyridine Derivatives and Use Thereof - Provided are a pharmaceutical composition containing a 2,5,6,7-tetrasubstituted thiazolo[4,5-b]pyridine derivative represented by Formula 1 as an active ingredient and a use thereof effective on a vascular inflammation-related infectious disease triggered by activity of HMGB1 protein. | 10-29-2015 |
20150315191 | 4-Position Substituted Pyrazolopyrimidine Derivative, And Use Thereof In Drug Preparation - The invention belongs to the technical field of organic synthetic drugs, and particularly relates to a pyrazolopyrimidine derivative and a preparation method and medical uses thereof. The invention provides a new pyrazolopyrimidine derivative mainly having position 4 substituted, i.e., position substituted by Y in formula I. The pyrazolopyrimidine derivative of the invention has a structural formula I as follows: | 11-05-2015 |
20150322088 | PIPERIDINE/PIPERAZINE DERIVATIVES - The invention further relates to a DGAT inhibitor of formula | 11-12-2015 |
20150353557 | TYROSINE KINASE INHIBITORS - The present disclosure provides compounds and pharmaceutically acceptable salts thereof that are tyrosine kinase inhibitors, in particular BLK, BMX, EGFR, HER2, HER4, ITK, TEC, BTK, and TXK and are therefore useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as cancer and inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and pharmaceutically acceptable salts thereof and processes for preparing such compounds and pharmaceutically acceptable salts thereof. | 12-10-2015 |
20150353562 | TYROSINE KINASE INHIBITORS - The present disclosure provides compounds and pharmaceutically acceptable salts thereof that are tyrosine kinase inhibitors, in particular BLK, BMX, EGFR, HER2, HER4, ITK, TEC, BTK, and TXK and are therefore useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as cancer and inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and pharmaceutically acceptable salts thereof and processes for preparing such compounds and pharmaceutically acceptable salts thereof. | 12-10-2015 |
20150361068 | PHOSPHATIDYLINOSITOL 3-KINASE INHIBITORS - The present application provides the compounds of formula (J), | 12-17-2015 |
20150361097 | HETEROCYCLIC AMIDE DERIVATIVES AS P2X7 RECEPTOR ANTAGONISTS - The invention relates to heterocyclic amide derivatives of formula (I), | 12-17-2015 |
20150366874 | Novel 4-(Substituted Amino)-7H-Pyrrolo[2,3-d]Pyrimidines As LRRK2 Inhibitors - The present invention provides novel 4,5-disubstituted-7H-pyrrolo[2,3-d]pyrimidine derivatives of Formula I, and the pharmaceutically acceptable salts thereof | 12-24-2015 |
20150368259 | Polycyclic Substituted Pyrazole Kinase Activity Inhibitors and Use Thereof - The present invention relates to the field of medicinal chemistry, and in particular relates to 4-(five-membered heterocyclic pyrimidine/pyridine substituted) amino-1H-3-pyrazolecarboxamide derivatives, the preparation method thereof, pharmaceutical compositions containing these compounds and the medicinal use thereof, especially as protein kinase inhibitors for anti-tumour use. | 12-24-2015 |
20160000799 | PHARMACEUTICAL COMPOSITIONS OF CETP INHIBITORS - The present application discloses a pharmaceutical composition comprising a class of cholesteryl ester transfer protein (CETP) inhibitors with improved oral bioavailability. The application further discloses compositions comprising a class of CETP inhibitor and at least one surfactant in the form of a solution, suspension, emulsion or a pre-concentrate. | 01-07-2016 |
20160002230 | PYRIDO[2,3-B]PYRAZIN-8-SUBSTITUTED COMPOUNDS AND THEIR USE - The present invention pertains generally to the field of therapeutic compounds for treating proliferative disorders, cancer, etc., and more specifically to certain pyrido[2,3-b]pyrazin-8-substituted compounds, as described herein, which, inter alia, inhibit RAF (e.g., B-RAF) activity. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit RAF (e.g., BRAF) activity, to inhibit receptor tyrosine kinase (RTK) activity, to inhibit cell proliferation, and in the treatment of diseases and disorders that are ameliorated by the inhibition of RAF, RTK, etc., proliferative disorders such as cancer (e.g., colorectal cancer, melanoma), etc. | 01-07-2016 |
20160002252 | SUBSTITUTED PYRROLO[2,3-d]PYRIMIDINES FOR THE TREATMENT OF CANCER AND PROLIFERATIVE DISORDERS - Disclosed are substituted pyrrolo[2,3-d]pyrimidine compounds. The disclosed compounds are shown to be useful in inhibiting the growth of cancer cell lines and treating cancer and cell proliferative disorders. | 01-07-2016 |
20160016949 | MICROBICIDALLY ACTIVE IMIDAZOPYRIDINE DERIVATIVES - The present invention provides compounds of formula (I) wherein Y | 01-21-2016 |
20160016957 | CHEMICAL COMPOUNDS, COMPOSITIONS AND METHODS FOR KINASE MODULATION - Chemical compounds that modulate kinase activity, including PI3 kinase activity, and chemical compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including P13 kinase activity, are described herein. | 01-21-2016 |
20160022682 | Methods and Compositions For Stimulating Neurogenesis And Inhibiting Neuronal Degeneration Using Isothiazolopyrimidinones - The present invention provides methods and compositions comprising compounds useful for stimulating neurogenesis. The methods and compositions comprising compounds are also useful for inhibiting neuronal degeneration. Thus, the present invention can be used in the treatment of diseases and conditions characterized by neuronal loss and reduced neurogenesis including Alzheimer's disease, stroke, traumatic brain injury, traumatic nerve injury, and depression. This invention is useful for research products including single agents or mixtures of agents to promote, proliferate, differentiate, or maintain neurons from stem or progenitor cells. | 01-28-2016 |
20160024097 | N-(4-(AZAINDAZOL-6-YL)-PHENYL)-SULFONAMIDES AND THEIR USE AS PHARMACEUTICALS - The present invention relates to N-(4-(azaindazol-6-yl)-phenyl)-sulfonamides of the formula I, | 01-28-2016 |
20160024099 | KINASE INHIBITORS AND METHODS OF USE - The present invention provides chemical entities or compounds and pharmaceutical compositions thereof that are capable of modulating certain protein kinases such as mTor, tyrosine kinases, and/or lipid kinases such as PI3 kinase. Also provided in the present invention are methods of using these compositions to modulate activities of one or more of these kinases, especially for therapeutic applications. | 01-28-2016 |
20160031875 | IMIDAZO(4,5-B) PYRIDIN-2-YL AMIDES AS KV7 CHANNEL ACTIVATORS - Compounds represented by formula 1 can be potent and/or partially selective for the Kv7.2/7.3 heteromultimer. They may be useful in treating disorders related to seizures, pain, neurotransmitter release, etc. | 02-04-2016 |
20160039808 | HISTONE DEMETHYLASE INHIBITORS - The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted pyrido[3,4-d]pyrimidin-4-one derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like. | 02-11-2016 |
20160046586 | SUBSTITUTED N-(3-(PYRIMIDIN-4-YL)PHENYL)ACRYLAMIDE ANALOGS AS TYROSINE RECEPTOR KINASE BTK INHIBITORS - In one aspect, the invention relates to substituted N-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs, derivatives thereof, and related compounds, which are useful as inhibitors of the BTK kinase; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the BTK kinase. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. | 02-18-2016 |
20160046634 | HETEROARYL COMPOUNDS AND USES THEREOF - The present invention relates to compounds useful as inhibitors of protein kinases, containing a cysteine residue in the ATP binding site. The invention further provides for pharmaceutically acceptable compositions comprising therapeutically effective amounts of one or more of the protein kinase inhibitor compounds and methods of using said compositions in the treatment of cancers and carcinomas. | 02-18-2016 |
20160060259 | Substituted 4,5,6,7-Tetrahydro-1H-Pyrazolo[4,3-C]Pyridines, Their Use as Medicament, and Pharmaceutical Preparations Comprising Them - The invention relates to substituted 4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridines of formula (I), their use as medicament, and pharmaceutical preparations comprising them. The compounds of formula (I) act on the TASK-1 potassium channel. The compounds are particularly suitable for the treatment or prevention of atrial arrhythmias, for example atrial fibrillation (AF) or arterial flutter. | 03-03-2016 |
20160067251 | ASK 1 INHIBITING PYRROLOPYRIMIDINE DERIVATIVES - This invention relates to pyrrolopyrimidine derivatives of formula (I): where R | 03-10-2016 |
20160075710 | PYRIDAZINONE DERIVATIVES AS PHOSHOINOSITIDE 3-KINASES INHIBITORS - Compounds of formula (I) described herein inhibit phosphoinositide 3-kinases (PI3K) and useful for the treatment of disorders associated with PI3K enzymes. | 03-17-2016 |
20160089376 | MODULATION OF REACTIVATION OF A LATENT VIRUS - The disclosure relates to methods of controlling the state of a virus (lytic or lysogenic) in an individual, such as a method of reactivating a latent virus in an individual, comprising administering one or more agents that modulates the activity of signal transducer and activator of transcription 3 (STAT3) or any of p300, CBP or p300/CBP. Also contemplated are methods further comprising administering an HDAC modulating agent, such as an HDAC inhibiting agent or an HDAC activating agent. | 03-31-2016 |
20160090386 | Purine Diones As Wnt Pathway Modulators - The invention relates to the use of compounds of general structure (I) in modulation of the Wnt pathway [Formula should be inserted here] wherein R | 03-31-2016 |
20160096847 | SUBSTITUTED BICYCLIC HETEROARYL COMPOUNDS - Disclosed are azaindazole compounds of Formula (I): | 04-07-2016 |
20160101092 | 1H-PYRAZOLO[3,4-B]PYRIDINES AND THERAPEUTIC USES THEREOF - Provided herein are compounds according to Formula I and pharmaceutically acceptable salts thereof, and compositions comprising the same, for use in various methods, including treating cancers such as colon, ovarian, pancreatic, breast, liver, prostate and hematologic cancers: | 04-14-2016 |
20160102366 | METHOD FOR PREDICTING THERAPEUTIC EFFICACY OF PI3K/AKT/mTOR INHIBITOR ON BASIS OF PHLDA1 OR PIK3C2B EXPRESSION - An object of the present invention is to provide a chemotherapy using a PI3K/AKT/mTOR inhibitor that produces an excellent antitumor effect on a cancer patient. The present invention provides a method for predicting the therapeutic efficacy of the chemotherapy using the antitumor agent comprising a PI3K/AKT/mTOR inhibitor on a cancer patient on the basis of the expression level of PHLDA1 and/or PIK3C2B in a biological sample containing tumor cells isolated from the cancer patient. | 04-14-2016 |
20160108047 | IMIDAZOPYRROLIDINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF DISEASE - The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition. | 04-21-2016 |
20160137665 | COMPOSITIONS COMPRISING THIENOPYRIMIDINE AND THIENOPYRIDINE COMPOUNDS AND METHODS OF USE THEREOF - The present disclosure relates generally to thienopyrimidine and thienopyridine compounds and methods of use thereof. In particular embodiments, the present disclosure provides compositions comprising thienopyrimidine and thienopyridine compounds of Formula 2: | 05-19-2016 |
20160145220 | NITROGEN-CONTAINING SATURATED HETEROCYCLIC COMPOUND - The present invention provides a nitrogen-containing saturated heterocyclic compound of the formula [I]: | 05-26-2016 |
20160145257 | SUBSTITUTED XANTHINES AND METHODS OF USE THEREOF - Compounds, compositions and methods are described for inhibiting the TRPC5 ion channel and disorders related to TRPC5. | 05-26-2016 |
20160151372 | PYRROLOPYRIMIDINE COMPOUNDS FOR THE TREATMENT OF CANCER | 06-02-2016 |
20160152634 | THIENO- AND FURO - PYRIMIDINES AND PYRIDINES, USEFUL AS POTASSIUM CHANNEL INHIBITORS | 06-02-2016 |
20160153049 | METHODS AND COMPOSITIONS FOR DETECTING AND TREATING DRUG RESISTANT AKT MUTANT | 06-02-2016 |
20160159803 | Pteridines Useful As HCV Inhibitors And Methods For The Preparation Thereof - The present invention relates to the use of pteridines as inhibitors of HCV replication as well as their use in pharmaceutical compositions aimed to treat or combat HCV infections. In addition, the present invention relates to compounds per se and their use as medicines. The present invention also concerns processes for the preparation of such compounds, pharmaceutical compositions comprising them, and combinations of said compounds with other anti-HCV agents. | 06-09-2016 |
20160168149 | PURINONE COMPOUNDS AS KINASE INHIBITORS | 06-16-2016 |
20160168157 | HETEROCYCLIC KINASE INHIBITORS | 06-16-2016 |
20160176866 | 4-AMINO-6-(2,6-DICHLOROPHENYL)-2-(PHENYLAMINO)-PYRIDO[2,3-d]PYRIMIDIN-7(8H- )-ONE DERIVATIVES, SYNTHESIS AND USES THEREOF | 06-23-2016 |
20160185796 | PHOSPHOINOSITIDE 3-KINASE INHIBITOR WITH A ZINC BINDING MOIETY - The invention provides a compound of Formula I, | 06-30-2016 |
20160185798 | HETEROCYCLYLALKYNE DERIVATIVES AND THEIR USE AS MODULATORS OF mGluR5 RECEPTORS - This invention relates to compounds of formula I, | 06-30-2016 |
20160200693 | Trisubstituted Benzotriazole Derivatives as Dihydroorotate Oxygenase Inhibitors | 07-14-2016 |
20160200728 | IMIDAZOLE-DERIVED MODULATORS OF THE GLUCOCORTICOID RECEPTOR | 07-14-2016 |
20160376286 | Pyrimidin-4-one derivatives and their use in the tratement, amelioration or prevention of a viral disease - The present invention relates to a compound having the general formula II, optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, | 12-29-2016 |
20180021311 | TRISUBSTITUTED BENZOTRIAZOLE DERIVATIVES AS DIHYDROOROTATE OXYGENASE INHIBITORS | 01-25-2018 |
20180022713 | HETEROARYL COMPOUNDS AND USES THEREOF | 01-25-2018 |
20190144441 | BICYCLIC FUSED PYRAZOLE DERIVATIVES FOR THE TREATMENT OF RSV | 05-16-2019 |
20190144451 | PURINONE COMPOUNDS AS KINASE INHIBITORS | 05-16-2019 |
20220135559 | NOVEL PYRIDO[3,4-D]PYRIMIDIN-8-ONE DERIVATIVE HAVING PROTEIN KINASE INHIBITORY ACTIVITY, AND PHARMACEUTICAL COMPOSITION FOR PREVENTING, ALLEVIATING, OR TREATING CANCER, COMPRISING SAME - The present disclosure relates to a pyrido[3,4-d]pyrimidin-8-one derivative compound exhibiting excellent anti-proliferative effects against cancer cells, a pharmaceutically acceptable salt thereof, a hydrate thereof, or a stereoisomer thereof, a production method therefor, a pharmaceutical composition for preventing, alleviating or treating cancer metastasis and proliferative disease containing the same as an active ingredient, and an anticancer composition against cancer cells. The compound exhibits excellent cancer cell inhibitory activity and anti-proliferative effects, and thus is effective in inhibiting cancer cells, preventing cancer metastasis and proliferative diseases or treating cancer. | 05-05-2022 |