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Three or more ring hetero atoms in the bicyclo ring system

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514 - Drug, bio-affecting and body treating compositions

514001000 - DESIGNATED ORGANIC ACTIVE INGREDIENT CONTAINING (DOAI)

514183000 - Heterocyclic carbon compounds containing a hetero ring having chalcogen (i.e., O,S,Se or Te) or nitrogen as the only ring hetero atoms DOAI

514228800 - Hetero ring is six-membered and includes at least nitrogen and oxygen as ring hetero atoms (e.g., monocyclic 1,2- and 1,3-oxazines, etc.)

514231200 - Morpholines (i.e., fully hydrogenated 1,4- oxazines)

514231500 - Additional hetero ring attached directly or indirectly to the morpholine ring by nonionic bonding

514232800 - Polycyclo ring system having the additional hetero ring as one of the cyclos

514233500 - Bicyclo ring system having the additional hetero ring as one of the cyclos

514233800 - Plural ring hetero atoms in the bicyclo ring system

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Entries
DocumentTitleDate
20130029984HETEROCYCLIC 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
20130029983AMINOTHIENOPYRIDAZINE 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
20090318443KINASE INHIBITORS - The present invention provides kinase inhibitors of Formula I.12-24-2009
20100022533COMPOSITIONS 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
20120184547METHODS 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
20080214541COMPOSITIONS 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
20090023724Heteroaryl compounds, compositions thereof, and methods of treatment therewith - Provided herein are Heteroaryl Compounds having the following structure:01-22-2009
20090192154SULTAM 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
20090192153NOVEL ADENINE COMPOUND - An adenine compound or its pharmaceutically acceptable salt as a medicament as shown following formula (1):07-30-2009
20120178754Furazano '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
20120178753INHIBITORS 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
20120245171BENZPYRAZOLE 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
20120245168Composition, 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
20130035336COMBINATION 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
201300353358-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
20130079341THIENO (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
20130079342HETEROCYCLIC 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
20090118273Compounds 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
20100004235Heterocyclic 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
200901819633H-[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
20130035334INHIBITORS 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
20090163490Pyrrolopyrimidine 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 R06-25-2009
20100041650PURINE 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
20090156598Imidazolopyrimidine 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
20090156599Imidazolo-, 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
20090156597Novel 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
20090156596Unsaturated Heterocyclic Derivatives - This invention relates to compounds of the general formula:06-18-2009
20080234262PYRAZOLOPYRIMIDINE 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
20090082347PYRROLO[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 A03-26-2009
20100093723HETEROCYCLYL 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, R04-15-2010
20090124614HYDROXY 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 formula05-14-2009
20130090336N-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
20090023723Purinone 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
20130090335PHOSPHOINOSITIDE 3-KINASE INHIBITOR WITH A ZINC BINDING MOIETY - The invention provides a compound of Formula I,04-11-2013
20090325953P38 KINASE INHIBITING AGENTS - Compounds described by the chemical formula (I) or pharmaceutically acceptable salts thereof:12-31-2009
20090318440CARBONYLAMINO 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
20100130492MORPHOLINOPURINE 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
20090093477TETRAHYDROPYRROLOPYRIMIDINEDIONES 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
20130072482ANTI-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
20130072481mTOR 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
20130059848CANNABINOID-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
20130059847SUBSTITUTED 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
20130059849AZAINDAZOLES - Herein are disclosed azaindazoles of formula (I)03-07-2013
201100151931, 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 R01-20-2011
20110065701PHARMACEUTICAL COMPOUNDS - A thienopyrimidine of formula (I):03-17-2011
20090270389Pyrimidinyl pyridone inhibitors of kinases - This application discloses novel pyrimidinyl pyridone derivatives according to formula I, wherein A, R10-29-2009
20120225869COMPOUNDS 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
201300658946-(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
20130065895Pyrazolopyridine, 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
20120115864Substituted 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
20090029990Dihydropteridinones in the treatment of respiratory diseases - The present invention relates to the use of dihydropteridinones of formula 101-29-2009
20090005377Pyrazolopyridine 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
20120238568Pyrido[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
20130165439CHEMICAL COMPOUNDS - The present invention encompasses compounds of general formula (I)06-27-2013
20090143377METHODS AND COMPOSITIONS FOR TREATING DISORDERS - Compounds and compositions for treating disorders related to TRPA1 are described herein.06-04-2009
20120088764PHOSPHOINOSITIDE 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
20090099173Pyridopyridazine 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
20110281864Pyrido[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 I11-17-2011
200902095356-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 —NR08-20-2009
20090312319CERTAIN 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
20130023531PYRIMIDO[5,4-D]PYRIMIDYLAMINO PHENYL SULFONAMIDES AS SERINE/THREONINE KINASE INHIBITORS - The present invention encompasses compounds of general formula (I)01-24-2013
20110281865NOVEL 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
20110281866HETEROCYCLIC 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
20080318949Pyrazolopyrimidinone 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
20130023532INDAZOLYL-PYRIMIDINES AS KINASE INHIBITORS - Disclosed are compounds having the formula: or a salt thereof, wherein A, n, R01-24-2013
20110294804NOVEL 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 R12-01-2011
20110294803PHOSPHATIDYLINOSITOL-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
20110294802PHARMACEUTICALLY 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
20090286783COMPOUNDS 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
20110294805PYRAZOLO-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 I12-01-2011
20100093721PHENYL 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, R04-15-2010
20100035876Use 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
20090099174COMBINATION 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
20090099171Diazaquinolones 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
20090099170Sirtuin 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
200900991726-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 I04-16-2009
20090149458PYRROLO[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
200901494571H-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-NHZR06-11-2009
201102635962-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
20110124641BENZOTHIAZOLE 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
20080306063PHENYLAMINO 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
20100280027PHARMACEUTICAL 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
20120035173DI-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
20100120767Pyrimidothiophene 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 R05-13-2010
20100120764DI-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
20100249128NOVEL 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, R09-30-2010
200900622733-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
20110172228KINASE 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
20100125074Thieno-[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 I05-20-2010
20090163491SUBSTITUTED 8-[6-AMINO-3PYRIDYL]XANTHINES - The present invention provides substituted 8-[6-amino-3-pyridyl]xanthines and pharmaceutical compositions that are selective antagonists of A06-25-2009
20090286781Use 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
20090298822Use 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
20090042878THIENOPYRIMIDYLAMINES 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 EP02-12-2009
20090298823Inhibitors 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
20110269757PYRAZOLO 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
20080275038Imidazopyridine Derivatives as A2b Adenosine Receptor Antagonists - The present disclosure relates to imidazopyridine derivatives of formula (I):11-06-2008
200802750372-Cyanophenyl fused heterocyclic compounds, and compositions and uses thereof - Fused heterocyclic compounds are provided according to formula 1:11-06-2008
20080312228PYRIMIDINE 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
20080207611Pharmaceutical compounds - Fused pyrimidines of formula (I):08-28-2008
20080293714Tec 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
20090156595Pteridines 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
20080269210PHOSPHOINOSITIDE 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 R10-30-2008
20100137303NEW 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
20100137302Fused 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
20090062276PYRIDOPYRIMIDINE PROTEIN TYROSINE PHOSPHATASE INHIBITORS - The present invention comprises pyridopyrimidinediamine compounds of the general formula I:03-05-2009
20090062274Pyridopyrimidinone 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
20090137582Pyrazolo-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 I05-28-2009
20090137580Fused 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
20090137581Heterocyclic 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
20090286782COMPOUNDS 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
20080318948Organic Compounds - The present invention provides compounds of the formula12-25-2008
200900053761-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
20090143379Storage 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
20090143378THIENOPYRIMIDINE AND THIENOPYRIDINE KINASE MODULATORS - The invention is directed to thienopyrimidines and thienopyridines compounds of Formula I and Formula II:06-04-2009
20080318947Inhibitors 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
201000042372-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
20090082346Substituted Pyrrolo-Pyrazole Derivatives as Kinase Inhibitors - Compounds represented by formula (Ia) or (Ib) and wherein R and R03-26-2009
20110230479NEUROTROPHIN 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
20090105246Sirtuin 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
20080261973Sulphonamidoaniline Derivatives Being Janus Kinase Inhibitors - The invention relates to sulphonamidoanilines of formula I,10-23-2008
201102304808-HETEROARYLPURINE MNK2 INHIBITORS FOR TREATING METABOLIC DISORDERS - Compounds of the formula09-22-2011
20080261972Cgrp Receptor Antagonists - Compounds of Formula (I), (where variables R10-23-2008
20090197880ANTI-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
200902475186-(2-ALKYL-PHENYL)-PYRIDO[2,3-D]PYRIMIDINES USEFUL AS PROTEIN KINASE INHIBITORS - Objects of the present invention are the compounds of formula I10-01-2009
20090253696SUBSTITUTED 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
20090221573Use 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
20090258874PYRAZOLO-HETEROARYL COMPOUNDS - A compound of formula I10-15-2009
20120142683PYRIMIDINE 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 thereof06-07-2012
200900482493-benzoimidazolyl-pyrazolopyridines useful in treating kinase disorders - The present invention is directed to novel 3-benzoimidazolyl-pyrazolopyridine compounds of formula (I):02-19-2009
20100190787Modulators 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
20100184760Benzoxazole 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
201001847616-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 I07-22-2010
201100599614-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
20100016306PYRIMIDINE DERIVATIVES AS PI3K INHIBITORS - Thienopyrimidines of formula (Ia) or (Ib):01-21-2010
20100184759PYRANO-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
20130123255COMBINATION 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
20130123256Pyrazolo 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
20100222342PYRROLOPYRAZOLE, 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
20100216790IMIDAZOPYRIDINE-DERIVATIVES AS INDUCIBLE NO-SYNTHASE INHIBITORS - The compounds of formula (I)08-26-2010
20100216788FUSED HETEROCYCLIC COMPOUND - The present invention provides a compound represented by the formula:08-26-2010
20100210643sGC 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
20090076001Substituted 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 methods03-19-2009
20100210645Certain 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
20100210644CHEMICAL COMPOUNDS - The present invention encompasses compounds of general formula (1) wherein the groups R08-19-2010
20100222343PHOSPHOINOSITIDE 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
20100041651TRIAZOLOPYRIDINE 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
20100048560PYRAZOLO 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
20120245170PYRAZOLOPYRIDINE 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
20120245169CERTAIN 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
20090318442THIAZOLYL-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
20090318441Pyrrolopyrimidine 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
20110130397PYRROLINONE 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
20090111805BICYCLIC HETEROAROMATIC DERIVATIVES USEFUL AS ANTICANCER AGENTS - The invention relates to compounds of the formula I:04-30-2009
20110112090Depsipeptides and Their Therapeutic Use - A Compound of structure (IX) or (X) or a pharmaceutically acceptable salt thereof, wherein: X is —C(═O)N(R05-12-2011
20100298318METHODS 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
20100298320Pyrido[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
201301310582-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 R05-23-2013
201301376852,5,7-SUBSTITUTED OXAZOLOPYRIMIDINE DERIVATIVES - The invention relates to oxazolopyrimidine compounds of formula (I), where A, R05-30-2013
20090036445KINASE INHIBITORS - The present invention provides kinase inhibitors of Formula I.02-05-2009
20090069319IMIDAZOPYRIDINE 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
20110009405PYRIMIDINYL 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
20110003809IMIDAZO [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
20110034458PYRIDINE 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
20110245245METHODS OF TREATMENT COMPRISING THE ADMINISTRATION OF HETEROARYL COMPOUNDS - Provided herein are Heteroaryl Compounds having the following structure:10-06-2011
20110212960NEW COMPOUNDS FOR THE TREATMENT OF CNS DISORDER - The invention relates to novel pyrazolopyrimidinones according to formula (I).09-01-2011
20110144104PYRROLIDINYL-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
20090312320METHODS OF TREATMENT COMPRISING THE ADMINISTRATION OF HALOARYL SUBSTITUTED AMINOPURINES OR COMPOSITIONS THEREOF - Provided herein are Aminopurine Compounds having the following structure:12-17-2009
20100216789RHO-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
20100035877METHODS 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
20090203687FUSED 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
20100004236PHOSPHODIESTERASE 4 INHIBITORS - PDE4 inhibition is achieved by novel compounds of the Formula I:01-07-2010
20100063047AMINOPYRIMIDINE INHIBITORS OF HISTAMINE RECEPTORS FOR THE TREATMENT OF DISEASE - The present invention relates to compounds and methods which may be useful as inhibitors of H03-11-2010
20100056514THIENOPYRAZOLES - 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
20110178080Melanocortin Receptor-Specific Spiro-Piperidine Compounds - Melanocortin receptor-specific compounds of formula I below:07-21-2011
20090215769Use 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
20110098295METHODS 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 mammal04-28-2011
20110082138IMIDAZOPYRIDIN-2-ONE DERIVATIVES - A compound represented by formula (I) having mTOR inhibitory activity or a pharmacologically acceptable salt thereof.04-07-2011
20110082139SUBSTITUTED 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 A04-07-2011
20110082137NEW COMPOUNDS FOR THE TREATMENT OF CNS DISORDERS - The invention relates to novel 1,6-disubstituted pyrazolopyrimidinones of formula (I),04-07-2011
20120149701CERTAIN 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
20110152258Compounds 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
20120202809NOVEL 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
20110152259NITROGEN-CONTAINING HETEROCYCLIC COMPOUNDS AND METHODS OF USE THEREOF - The present invention provides compounds of Formula (I):06-23-2011
20110178082PYRAZOLO 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
20100004238FUSED 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
20090029988Hydroxyalkyl 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
20090029991BENZAMIDE DERIVATIVES USEFUL AS HISTONE DEACETYLASE INHIBITORS - The invention concerns a compound of the formula (I)01-29-2009
20090029989SUBSTITUTED 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
20090247517COMPOUNDS 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
20090118278COMPOSITIONS USEFUL AS INHIBITORS OF GSK-3 - The present invention provides a compound of formula I:05-07-2009
20090118275THIAZOLOPYRIMIDINE 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
200901182773 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
20090118276THIENOPYRIMIDINES, THIENOPYRIDINES, AND PYRROLOPYRIMIDINES AS B-RAF INHIBITORS - The present invention relates to compounds of formula la:05-07-2009
20090118274MONOCYCLIC 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
20110288090Inhibitors 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
20110288089INSECTICIDAL COMPOUNDS - A compound of Formula (I): wherein A11-24-2011
20110288088SUBSTITUTED 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
20110028472THIENOPYRIMIDINES - Novel thienopyrimidines of the formula (I), in which R02-03-2011
20110263597SUBSTITUTED 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 formula10-27-2011
20110263595COMPOUNDS 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
20100298319PYRIMIDINE 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
20120302567BICYCLIC 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
201003240409-(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
20100120765PYRAZOLYL SUBSTITUTED XANTHINES - The present invention provides compounds and pharmaceutical compositions that are selective antagonists of A05-13-2010
20110098294PURINE 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
20110178081PYRAZOLO 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
20120309755NOVEL COMPOUNDS - This invention relates to compounds of formula I12-06-2012
201201497002-CYANOPHENYL FUSED HETEROCYCLIC COMPOUNDS, AND COMPOSTIONS AND USES THEREOF - Fused heterocyclic compounds are provided according to formula 1:06-14-2012
20090176779PYRAZOLO[4,3-D]THIAZOLE DERIVATIVES, AND PREPARATION AND THERAPEUTIC APPLICATION THEREOF - The disclosure relates to a compound of formula (I):07-09-2009
20110190292HETEROBICYCLIC COMPOUNDS USEFUL AS KINASE INHIBITORS - A compound of Formula (I)08-04-2011
20110190291Prodrug 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
201101902901H-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
20110160203Substituted 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
20100029641ARYL SULFAMIDE DERIVATIVES AND METHODS OF THEIR USE - The present invention is directed to aryl sulfamide derivatives of formula I:02-04-2010
20100022532USE 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
20110218197SUBSTITUTED 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
20090062275N-Substituted Imidazopyridine c-Kit Inhibitors - Compounds represented by Formula (I):03-05-2009
20100029642Methods 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
20090325952PYRAZOLO[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
20090069318Novel 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
20120040981THIENOPYRIMIDINE AS CDC7 KINASE INHIBITORS - The present invention relates to a compound represented by the formula (I):02-16-2012
201103066109-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
20090076002NOVEL 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
20120040982Xanthine derivatives, the preparation thereof and their use as pharmaceutical compositions - The present invention relates to substituted xanthines of general formula02-16-2012
20120065200INHIBITORS 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
20090203689ABCA-1 ELEVATING COMPOUNDS AND METHODS - Disclosed are novel compounds of Formula I08-13-2009
20080312227Substituted 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
20120065201INHIBITORS 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
20110105499Pyrazolo-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 I05-05-2011
20120046283COMPOUNDS FOR TREATING NEUROPSYCHIATRIC CONDITIONS - Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of neuropsychiatric conditions.02-23-2012
20120065202PYRIMIDINE DERIVATIVES AS mTOR INHIBITORS - The invention relates to compounds of formula (I)03-15-2012
20120115863COMPOUNDS 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 A05-10-2012
20090186889SPIRO-SUBSTITUTED PYRROLOPYRIMIDINES - The invention provides compounds of formula I or a pharmaceutically acceptable salt or ester thereof formula I07-23-2009
20110166135AROMATIC 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 [I07-07-2011
20120059001NOVEL 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
20120059000CHEMICAL 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
201201574521H-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
20120157453RAF 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
20120108588NOVEL 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
20120108589AZABICYCLO 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 X05-03-2012
20120108587Aza- 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 A05-03-2012
20120071476MORPHOLINOPURINE 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
20120071475UREA 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
20110092500SGC 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
20110092499N-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
20110105500PYRAZINE 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
20110105498Pyrazolo-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 I05-05-2011
20120135988PURINE 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
20100093724Azaindazole 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
20100093722HETEROARYL 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 R04-15-2010
20100093720MACROCYCLIC 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
20120316163Pyrazolo 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
20090131430PYRIDO'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
20090131429Pharmaceutical compounds - Fused pyrimidines of formula (I):05-21-2009
20090131431Pyrazolo[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
20110183972AROMATIC 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
20120220586HETEROCYCLIC 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
20120165328INHIBITORS 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
20120129852AZAINDAZOLES 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 A05-24-2012
20120165329COMPOUNDS 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
20100048559PYRIDO(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: R02-25-2010
20100016305novel 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
20120220584HETEROCYCLIC 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
20100120766Substituted 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
20100292234TRIAZOLE 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 I11-18-2010
20120220585HETEROCYCLIC 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
20120190679Novel Protein Kinase B Inhibitors - 060 - The invention relates to a novel group of compounds of Formula (I) or salts thereof:07-26-2012
20090018129SUBSTITUTED 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
20120264751PYRROLOPYRAZOLES, 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
20120232077SELECTIVE ANTIBACTERIALS FOR CLOSTRIDIUM DIFFICILE INFECTIONS - The invention features compounds of formula (I): The compounds are useful as antibacterial agents, especially again 09-13-2012
20080300246Compounds 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
201001304919-SUBSTITUTED-8-OXO-ADENINE COMPOUNDS AS TOLL-LIKE RECEPTOR (TLR7 ) MODULATORS - The present invention provides compounds of formula (I)05-27-2010
20090203688HETEROCYCLIC COMPOUNDS - The invention relates to compounds of formula I and salts thereof08-13-2009
20110046131PURINES 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
20120322799DEUTERATED 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
20120270870Indazole and Pyrazolopyridine Compounds As CCR1 Receptor Antagonists - Diclosed are CCR1 receptor antagonists of the formula (I)10-25-2012
201102375832, 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
20120129851Substituted 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
20100234370PHARMACEUTICAL COMPOUNDS - Fused pyrimidines of formula (I):09-16-2010
20120329793Substituted 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
201002042232-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
20100204222PYRIDOPYRIMIDINE 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
20100204221Pyrrolopyrimidinyl axl kinase inhibitors - Compounds represented by Formula (I):08-12-2010
201103194097-AZA-QUINAZOLINE PDE10 INHIBITORS - The present invention is directed to 7-aza-quinazoline compounds of general structural formula I12-29-2011
20120101095ALKOXY-THIENOPYRIMIDINES AS TGF-BETA RECEPTOR KINASE MODULATORS - Novel alkoxy-thienopyrimidine derivatives of formula (I)04-26-2012
20120142684COMPOUNDS 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
20130012507SUBSTITUTED PYRROLO-PYRAZOLE DERIVATIVES AS KINASE INHIBITORS - Compounds represented by formula (Ia) or (Ib) and wherein R and R01-10-2013
20100160313DISCOVERY 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
20130172341FUSED 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
200802490898-[3-AMINO-PIPERIDIN-1-YL]-XANTHINES, THE PREPARATION THEREOF AND THEIR USE AS PHARMACEUTICAL COMPOSITIONS - The present invention relates to substituted xanthines of general formula10-09-2008
20080242665PHOSPHOINOSITIDE 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 R10-02-2008
20080234261Preparation of 1,6-Disubstituted Azabenzimidazoles as Kinase Inhibitors - Novel inhibitors of Rho-kinases are disclosed.09-25-2008
20080227777Pyrazolopyridine 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
20130184274Protein 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
20080221099DIHYDROPTERIDINONES FOR THE TREATMENT OF CANCER DISEASES - Disclosed is the use of a compound of general Formula (1),09-11-2008
20080221098COMPOUNDS 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
20080221097Imidazopyridine 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
20130143879PYRAZOLO 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
20130172340SUBSTITUTED 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
20130102601Pyrimidin-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
20130096116TREATMENT 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
20110275629Pyridazino-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 I11-10-2011
20100022531NOVEL 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
20130158027PYRAZOLO 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
20130158028USE 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
20110306609THIAZOLOPYRIDINE 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
20130196989COMPOSITIONS 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
20130196988Dihydrothienopyrimidines - 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
20130102600Heteroaryl 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
20130203755BICYCLIC 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
20130096115METHODS 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
20120088766FUSED 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
20120088765PURINE 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

Patent applications in class Three or more ring hetero atoms in the bicyclo ring system