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Exactly four ring nitrogens in the bicyclo ring system

Subclass of:

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

514247000 - Hetero ring is six-membered consisting of two nitrogens and four carbon atoms (e.g., pyridazines, etc.)

514256000 - 1,3-diazines (e.g., pyrimidines, etc.)

514257000 - Polycyclo ring system having 1,3-diazine as one of the cyclos

514258100 - Bicyclo ring system having the 1,3-diazine as one of the cyclos

Patent class list (only not empty are listed)

Deeper subclasses:

Class / Patent application numberDescriptionNumber of patent applications / Date published
514263100 Purine (including hydrogenated) 261
Entries
DocumentTitleDate
20120184567INHIBITORS 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.07-19-2012
20090062313Pde5 inhibitor compositions and methods for treating cardiac indications - The invention features methods and compositions featuring a PDE5 inhibitor for treating or preventing a cardiac indication in a subject.03-05-2009
20100160350PYRAZOLOPYRIMIDINONE KINASE INHIBITOR - The present invention provides a novel pyrazolo[3,4-d]pyrimidin-4-one, specifically a derivative of 1-(pyridine-4-yl)-pyrazolo[3,4-d]pyrimidin-4-one. This compound is a kinase inhibitor that shows unexpected anti-proliferative activity against cells, including against tumor cells, and anti-tumor activity in xenograft tumor models. The compound or a suitable salt or prodrug thereof is useful for the treatment of individuals suffering from a cancer or another proliferative disorder or disease.06-24-2010
20130035348ANTIMETASTATIC COMPOUNDS - Screening methods for identifying compounds and compounds and pharmaceutical compositions for treating and preventing cancer are disclosed. The compounds affect signal transduction downstream of the MET receptor.02-07-2013
20130035349PYRAZOLOPYRIMIDINONE KINASE INHIBITOR - The present invention provides a novel pyrazolo[3,4-d]pyrimidin-4-one, specifically a derivative of 1-(pyridine-4-yl)-pyrazolo[3,4-d]pyrimidin-4-one. This compound is a kinase inhibitor that shows unexpected anti-proliferative activity against cells, including against tumor cells, and anti-tumor activity in xenograft tumor models. The compound or a suitable salt or prodrug thereof is useful for the treatment of individuals suffering from a cancer or another proliferative disorder or disease.02-07-2013
20130040972USE OF c-Src INHIBITORS IN COMBINATION WITH A PYRIMIDYLAMINOBENZAMIDE COMPOUND FOR THE TREATMENT OF LEUKEMIA - The invention relates to a combination which comprises (a) at least one compound decreasing the c-Src activity and (b) a pyrimidylaminobenzamide compound; to pharmaceutical compositions comprising said combinations; and to a method of treating a warm-blooded animal having leukemia, especially chronic myelogenous leukemia, comprising administering to the animal at least one compound inhibiting the activity of a member of the Src kinase family, the Btk kinase family, the Tec kinase family or a Raf kinase inhibitor, in particular inhibiting the c-Src protein tyrosine kinase activity or inhibiting simultaneously the c-Src protein tyrosine kinase activity and the Bcr-Abl tyrosine kinase activity, in combination with a pyrimidylaminobenzamide compound, in particular 4-Methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]-N-[5-(4-methyl-1H-imidazol-1-yl)-3-(trifluoromethyl)phenyl]benzamide.02-14-2013
201300409716-CYCLOALKYL-PYRAZOLOPYRIMIDINONES FOR THE TREATMENT OF CNS DISORDERS - The invention relates to novel pyrazolopyrimidinones according to formula (I)02-14-2013
20100041677INHIBITORS OF BRUTON'S TYROSINE KINASE - Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.02-18-2010
20100041678COMPOSITIONS AND METHODS FOR TREATING INFLAMMATORY DISORDERS - The present disclosure relates to methods of treating inflammatory disorders by administering a Syk inhibitory 2,4-pyrimidinediamine compound and a second agent.02-18-2010
200901566181-(1- (2-Ethoxyethyl)-3-Ethyl-7-(4-Methylpyridin-2-Ylamino) - 1H-Pyrazolo [4,3-D] Pyrimidin-5-YL) Piperidine-4-Carboxylic acid and salts thereof - The present invention comprises 1-(1-(2-ethoxyethyl)-3-ethyl-7-(4-methylpyridin-2-ylamino)-1H-pyrazolo[4,3-d]pyrimidin-5-yl)piperidine-4-carboxylic acid and its salts. The invention further comprises pharmaceutical compositions, methods of treatment, and synthetic methods relating to 1-(1-(2-ethoxyethyl)-3-ethyl-7-(4-methylpyridin-2-ylamino)-1H-pyrazolo[4,3-d]pyrimidin-5-yl)piperidine-4-carboxylic acid and its salts.06-18-2009
201001057047-(3',4'-Dialkoxyphenyl)-[1,2,4]-Triazolo[1,5-A]Pyrimidine Compounds, Process for Preparing Thereof, and Pharmaceutical Composition for Treating or Preventing Asthma, Chronic Obstructive Pulmonary Disease, Arthritis, Atopic Dermatitis, Tumor and Degenerative Brain Diseases Comprising the Same - The present invention relates to novel {7-(3′,4′-dialkoxyphenyl)-[1,2,4]-triazolo[1,5-a]pyrimidine compounds or pharmaceutically acceptable salts thereof, a process for preparing the same, and pharmaceutical compositions for treating or preventing inflammatory diseases including asthma and chronic obstructive pulmonary disease, arthritis, atopic dermatitis, cancers including leukemia, and degenerative brain diseases including Alzheimer's disease, depression and memory impairment, which comprises the same as an active ingredient.04-29-2010
20090124638ANTI-INFLAMMATORY PYRAZOLOPYRIMIDINES - The present invention provides anti-inflammatory compounds useful in the treatment of diseases and conditions in which inflammation is involved in disease progression or the manifestation of symptoms of the disease or condition.05-14-2009
20090306097Use of allopurinol for the treatment of palmar plantar erythrodysesthesia - Allopurinol or a pharmaceutically acceptable salt thereof can be used for the treatment or prevention of palmar plantar erythrodysesthesia induced by chemotherapy. The allopurinol or its salt may be administered topically to the affected areas, palms and soles, preferably in the form of a cream.12-10-2009
20080280925Amines as Small Molecule Inhibitors - The present invention relates to compounds that are useful as inhibitors of protein arginine methyltransferase that have a formula selected from Formula (I), Formula (II) and Formula (III), as well as racemic mixtures, diastereomers, enantiomers and tautomers thereof and N-oxides, hydrates, solvates, pharmaceutically acceptable salts, prodrugs and complexes thereof as defined herein. Said compound are useful as inhibitors of PRMTs and/or CARM-I. The invention further relates to compositions comprising such compounds and methods for their use.11-13-2008
20130059868TREATMENT OF GOUT - Sodium 2-(5-bromo-4-(4-cyclopropyl-naphthalen-1-yl)-4H-1,2,4-triazol-3-ylthio)acetate is described. In addition, pharmaceutical compositions and uses such compositions for the treatment of a variety of diseases and conditions.03-07-2013
201100657306-CYCLYLMETHYL-AND 6-ALKYLMETHYL-SUBSTITUTED PYRAZOLEPYRIMIDINES - The invention relates to novel 6-cyclylmethyl- and 6-alkylmethyl-substituted pyrazolopyrimidines, process for their preparation and their use for producing medicaments for improving perception, concentration, learning and/or memory.03-17-2011
20090270426P13 Kinase Antagonists - The present invention provides novel PI3-Kinase antagonists and methods of use thereof.10-29-2009
200902704253-(DIHYDRO-1H-PYRAZOLO[4,3-D]PYRIMIDIN-5-YL)-4-PROPOXYBENZENESULFONAMIDE DERIVATIVES AND METHODS OF USE - This invention relates to novel 3-(dihydro-1H-pyrazolo[4,3-d]pyrimidin-5-yl)-4-propoxybenzenesulfonamide compounds, their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering inhibitors of cyclic guanosine 3′,5′-monophosphate specific phosphodiesterase (cGMP-specific PDE), in particular PDE5.10-29-2009
20110021542Use of a Combination of Udenafil and Alfuzosin or Oxybutynin for the Treatment of Overactive Bladder - The invention relates to a specific combination of two active agents: udenafil and one of alfuzosin and oxybutynin and its use for the treatment of overactive bladder.01-27-2011
20120115889INHIBITORS OF BRUTON'S TYROSINE KINASE - Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.05-10-2012
20080293746COMBINATIONS COMPRISING PREGABALIN - The invention relates to a combination of pregabalin and 1-(2-ethoxyethyl)-5-[ethyl(methyl)amino]-N-mesyl-7-[(4-methyl-2-pyridyl)amino]-1H-pyrazolo[4,3-d]pyrimidine-3-carboxamide, to pharmaceutical compositions containing the combination, and to the use of the combination in the treatment of pain.11-27-2008
20130165454COMPOUNDS AND COMPOSITIONS FOR TREATING CHEMICAL WAREFARE AGENT-INDUCED INJURIES - Compounds and compositions for treating injuries caused by exposure to chemical warfare agents are described herein.06-27-2013
20100004270INHIBITORS OF BRUTON'S TYROSINE KINASE - Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.01-07-2010
20100160351PHARMACEUTICAL COMPOSITIONS AND METHODS FOR TREATING HYPERURICEMIA AND RELATED DISORDERS - Disclosed is a pharmaceutical composition comprising (a) a first therapeutic agent, wherein the first therapeutic agent is a compound of formula II:06-24-2010
20080318982Pharmaceutical Combination for the Treatment of Luts - This invention relates to the combined use of a PDE5 inhibitor and a muscarinic antagonist in the treatment of lower urinary tract symptoms (LUTS), such as urgency, frequency, nocturia and urge incontinence.12-25-2008
20120108612INHIBITORS OF BRUTON'S TYROSINE KINASE - Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.05-03-2012
20110294833Methods for Healthy Aging - Genome-wide association studies have been used to elucidate genes and/or pathways related to diseases; however, this methodology has yet to be used to understand the phenotype of healthy aging and/or healthspan in humans.12-01-2011
201000359006-Arylmethyl-substituted pyrazolopyrimidines - The invention relates to novel 6-arylmethyl-substituted pyrazolopyrimidines, process for their preparation and their use for producing medicaments for improving perception, concentration, learning and/or memory.02-11-2010
20090099211TREATMENTS FOR CONGESTIVE HEART FAILURE - Methods and pharmaceutical preparations for treating heart failure by administering to a human or animal subject a therapeutically effective amount of at least one substance selected from the group consisting of a) SOD mimics (e.g., Tempol), b) NADPH oxidase inhibitors (e.g., Apocynin) and c) other substance that inhibit or reduce the amount of superoxide present in the affected tissues (e.g., the subjects heart and/or blood vessels) and/or increase levels of nitric oxide.04-16-2009
20100113486USE OF PDE7 INHIBITORS FOR THE TREATMENT OF MOVEMENT DISORDERS - A method of treating a movement abnormality associated with the pathology of a neurological movement disorder, such as Parkinson's disease or Restless Leg(s) Syndrome by administering a therapeutically effective amount of a PDE7 inhibitory agent. An aspect of the invention provides for the administration of a PDE& inhibitory agent in conjunction with a dopamine agonist or precursor, such as levodopa. In another aspect of the invention, the PDE7 inhibitory agent may be selective for PDE7 relative to other molecular targets (i) known to be involved with the pathology of Parkinson's disease or (ii) at which other drug(s) that are therapeutically effective to treat Parkinson's disease act.05-06-2010
20080207646Agent For the Prevention and Treatment of Liver Diseases Containing Pyrazolopyrimidine Derivative - The present invention relates to the pharmaceutical composition for prevention and treatment of liver diseases containing pyrazolopyrimidine derivative as all active ingredient. According to the present invention, pyrazolopyrimidine derivative has an excellent effect on inhibiting collagen synthesis in hepatic stellate cells and acts directly on the portal vein. Particularly, it may increase the diameter and the amount of blood flow of the portal vein, and finally decrease the pressure thereof. Therefore, pyrazolopyrimidine derivative can be used advantageously for prevention and treatment of hepatic fibrosis, liver cirrhosis caused by hepatic fibrosis, portal hypertension and various complications caused by portal hypertension. In addition, pyrazolopyrimidine derivative according to the present invention can reduce dosing frequency because of its long half-life, and therefore, has an advantage to improve the drug compliance of patients suffering from chronical liver diseases.08-28-2008
20100249153SUBSTITUTED INDOLO-PIPERIDINE COMPOUNDS - The present invention relates to substituted indolo-piperidine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted indolo-piperidine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds or pharmaceutical compositions to subjects in need thereof.09-30-2010
20100249152NEW 4-SUBSTITUTED DERIVATIVES OF PYRAZOLO[3,4-D PYRIMIDINE AND PYRROLO[2,3-D]PYRIMIDINE AND USES THEREOF - The present invention relates to a compound 4-substituted derivative of pyrazolo[3,4-d]pyrimidine or of pyrrolo[2,3-d]pyrimidine having the formula (I) and uses thereof, in particular for the treatment of bone related diseases and tumours.09-30-2010
20110207752P70 S6 KINASE INHIBITOR AND EGFR INHIBITOR COMBINATION THERAPY - The present invention provides a combination therapy comprising the compound 4-[4-[4-(4-fluoro-3-trifluoromethyl-phenyl)-1-methyl-1H-imidazol-2-yl]-piperidin-1-yl]-1H-pyrazolo[3,4-d]pyrimidine, or a pharmaceutically acceptable salt thereof, and an EGFR inhibitor for use in the treatment of glioblastoma multiforme, adenocarcinomas of the colon, non-small-cell lung cancer, small-cell lung cancer, cisplatin-resistant small-cell lung cancer, ovarian cancer, leukemia, pancreatic cancer, prostate cancer, mammary carcinoma, renal cell carcimoma, multiple myeloma, Kaposis Sarcoma, Hodgkins lymphoma, lymphangioleiomyomatosis, Non-Hodgkins lymphoma or sarcoma.08-25-2011
20090163521Novel Pyrazolopyrimidinone Derivatives - The present invention relates to novel pyrazolopyrimidinones of the general formula (I), their derivatives, their analogs, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them. The present invention more particularly provides novel pyrazolopyrimidinones derivatives of the general formula (I).06-25-2009
20110224237USE OF ALLOPURINOL FOR THE TREATMENT OF PALMAR PLANTAR ERYTHRODYSESTHESIA - Use of allopurinol or a pharmaceutically acceptable salt thereof for the treatment or prevention of palmar plantar erythrodysesthesia induced by chemotherapy. The allopurinol or its salt is administered topically to the affected areas, palms and soles, preferably in the form of a cream.09-15-2011
201000100184-Amino-3-Arylamino-6-Arylpyrazolo[3,4-D) Pyrimidine Derivatives, Methods for their Preparation and their Use as Antiviral Agents - 4-amino-3-arylamino-6-arylpyrazolo[3,4-d]pyrimidine derivatives of general formula (I), pharmaceutically acceptable salts thereof, method for preparation of the aforesaid compounds and their use as antiviral agents.01-14-2010
20090163520MNK1 or MNK2 Inhibitors - The present invention relates to the use of pyrazolopyrimidine compounds for the production of pharmaceutical compositions for the prophylaxis and/or treatment of diseases which can be influenced by the inhibition of the kinase activity of Mnk1 and/or Mnk2 (Mnk2a or Mnk2b) and/or variants thereof.06-25-2009
20110224236TREATMENT FOR PULMONARY HYPERTENSION - One embodiment relates to a method of treating pulmonary hypertension based upon co-administering to a subject in need thereof a pharmaceutically effective amount of an oral therapeutic agent for treating pulmonary hypertension and a pharmaceutically effective amount of an inhaled therapeutic agent for treating pulmonary hypertension. The benefit of the co-administration of these agents is to eliminate or reduce one or more side effects associated with mono-therapy of either agent, as well as one or more side effects associated with other administration routes such as subcutaneous or intravenous administration.09-15-2011
200901978993-(Dihydro-1H-pyrazolo[4,3-d]pyrimidin-5-yl)-4-propoxybenzenesulfonamide Derivatives and Methods of Use - This invention relates to novel 3-(dihydro-1H-pyrazolo[4,3-d]pyrimidin-5-yl)-4-propoxybenzenesulfonamide compounds, their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering inhibitors of cyclic guanosine 3′,5′-monophosphate specific phosphodiesterase (cGMP-specific PDE), in particular PDE5.08-06-2009
20090239883Treatment of Pulmonary Hypertension - This invention relates to the use of certain cyclic guanosine 3′,5′-monophosphate phosphodiesterase type five (cGMP PDE5) inhibitors, including in particular the compound sildenafil, for the treatment of pulmonary hypertension.09-24-2009
20100190805PREPARATION FOR THE TREATMENT OF EQUINE LAMINITIS - Disclosed is the use of active substances known from human medicine for treating gout in order to pharmaceutically treat equine laminitis, especially the use of a preparation containing at least allopurinol and/or hydrocortisone and/or powdered opium and/or prednisolone and/or prednisone.07-29-2010
20100152209Compounds for Modulating TRPV3 Function - The present application relates to compounds and methods for treating pain and other conditions related to TRPV3.06-17-2010
20100210668COMPOSITION AND METHOD FOR TREATMENT OR PREVENTION OF BENIGN PROSTATIC HYPERPLASIA AND LOWER URINARY TRACT SYMPTOMS - The present invention relates to a composition and a method for treating or preventing benign prostatic hyperplasia (BPH) and lower urinary tract symptoms (LUTS) without showing the side effect, by dramatically relaxing the smooth muscle in prostate and bladder.08-19-2010
20090076037BICYCLIC PYRIMIDINE KINASE INHIBITORS - The present invention is directed to novel bicyclic pyrimidine compounds of Formula (I) or a form or composition thereof03-19-2009
20130131088TREATING CANCER WITH STATINS AND COMPOUNDS HAVING DIPYRIDAMOLE ACTIVITY - The disclosure pertains to methods of treating a cancer comprising administering to a subject in need thereof an effective amount of a statin in combination with an effective amount of a dipyridamole and/or a compound that has dipyridamole activity.05-23-2013
20130137709Compounds that modulate EGFR activity and methods for treating or preventing conditions therewith - Provided are compounds and methods for treating or preventing kinase-mediated disorders therewith.05-30-2013
20110039868INHIBITORS OF BRUTON'S TYROSINE KINASE - Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.02-17-2011
20110212977P70 S6 KINASE INHIBITOR AND MTOR INHIBITOR COMBINATION THERAPY - The present invention provides a combination therapy comprising the compound 4-[4-[4-(4-fluoro-3-trifluoromethyl-phenyl)-1-methyl-1H-imidazol-2-yl]-piperidin-1-yl]-1H-pyrazolo[3,4-d]pyrimidine, or a pharmaceutically acceptable salt thereof, and an mTOR inhibitor for use in the treatment of glioblastoma multiforme, adenocarcinomas of the colon, non-small-cell lung cancer, small-cell lung cancer, cisplatin-resistant small-cell lung cancer, ovarian cancer, leukemia, pancreatic cancer, prostate cancer, mammary carcinoma, renal cell carcimoma, multiple myeloma, Kaposis Sarcoma, Hodgkins lymphoma, lymphangioleiomyomatosis, Non-Hodgkins lymphoma or sarcoma.09-01-2011
20110245276PHOTOSTABILIZED PHARMACEUTICAL COMPOSITIONS - A crosslinking reaction and a reaction for reducing molecular weight that take place in a hyaluronic acid-methotrexate conjugate upon irradiation with light are suppressed to improve the photostability of the conjugate. Specifically, a substance having a quenching effect and/or a radical scaveng effect is added to a pharmaceutical composition containing the hyaluronic acid-methotrexate conjugate.10-06-2011
20110092520PROCESS FOR PRODUCING BICYCLOANILINE DERIVATIVES - The present invention relates to a process for producing a hydrate of 3-(2,6-dichlorophenyl)-4-imino-7-[(2′-methyl-2′,3′-dihydro-1′H-spiro[cyclopropane-1,4′-isoquinolin]-7′-yl)amino]-3,4-dihydropyrimido[4,5-d]pyrimidin-2(1H)-one (Compound A) or of a pharmaceutically acceptable salt of Compound A and a crystalline form of Compound A or of a pharmaceutically acceptable salt of Compound A, which are useful in the field of treatment of various cancers as a kinase inhibitor, especially as a Weel kinase inhibitor.04-21-2011
20100069409"NOVEL COMPOUNDS" - Novel substituted 2,4,8-trisubstituted-8H-pyrido[2,3-d]pyrimidin-7-one compounds, and 1,5,7-trisubstituted-3,4-dihydro-pyrimido[4,5-d]pyrimidin-2-(M)-one compounds and compositions, and their use in therapy as CSBP/RK/p38 kinase inhibitors.03-18-2010
20100016339FUNGICIDAL COMPOUNDS AND COMPOSITIONS - The present invention relates, inter alia, to a compound having the formula (I):—wherein (R)n is selected from the group consisting of 4-Br, 4-OCH01-21-2010
20110071168NITRIC OXIDE DONORS FOR INDUCING NEUROGENESIS - There is provided a method of promoting neurogenesis by administering a therapeutic amount of a nitric oxide donor compound to a patient in need of neurogenesis promotion. Also provided is a compound for providing neurogenesis having an effective amount of a nitric oxide donor sufficient to promote neurogenesis. A nitric oxide compound for promoting neurogenesis is also provided. Further, a method of augmenting the production of brain cells and facilitating cellular structural and receptor changes by administering an effective amount of a nitric oxide donor compound to a site in need of augmentation is provided. There is provided a method of increasing both neurological and cognitive function by administering an effective amount of a nitric oxide donor compound to a patient.03-24-2011
20110257203INHIBITORS OF BRUTON'S TYROSINE KINASE - Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.10-20-2011
20100261737Method of Treating Erectile Dysfunction - A combined therapy for treatment of a patient having erectile dysfunction at least in part caused by vascular disease within a pelvic vessel is disclosed that includes placement of a stent within a stenosed region of the pelvic vessel in conjunction with the administration of a drug for treatment of erectile dysfunction.10-14-2010
20090286812GPR119 Receptor Agonists - Provided herein are compounds of the formula (I):11-19-2009
201202028296-Cycloalkyl-pyrazolopyrimidinones for the Treatment of CNS Disorders - The invention relates to novel 6-Cycloalkyl-pyrazolopyrimidinones according to formula (I).08-09-2012
20110263617Combination therapy for the treatment of diabetes and related conditions - The present invention relates to combinations of DPP-4 inhibitors with GPR119 agonists, as well as to the use of these combinations for treating and/or preventing metabolic diseases, particularly diabetes (especially type 2 diabetes mellitus) and conditions related thereto.10-27-2011
20110257202Therapeutic Compositions and Methods for Treating Chronic Kidney Disease Associated with a Metabolic Imbalance - Disclosed herein are compositions and methods for treating chronic kidney disease and/or a metabolic imbalance. Specifically exemplified herein are methods involving the coadministration of a RAS inhibitor with a conjunctive agent that improves endothelial NO or endothelial function. Also disclosed are methods of treating a patient exhibiting symptoms of a stage of chronic kidney disease and at least one symptom of a metabolic imbalance, such as one or more diagnostic criteria of the metabolic syndrome.10-20-2011
20100298351NOVEL PYRAZOLO [3, 4 -D] PYRIMIDINE DERIVATIVES AS ANTI-CANCER AGENTS - The invention relates to substituted pyrazolo[3,4-d]pyrimidine derivatives of the Formula-(I), or pharmaceutically-acceptable salts thereof, which possess anti-proliferative activity such as anti-cancer activity and are accordingly useful in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of substituted pyrazolo[3,4-d]pyrimidine derivatives, to pharmaceutical compositions containing the compound and to its use in the manufacture of medicaments for the production of an anti-proliferative effect in a warm-blooded animal such as man.11-25-2010
20110136835COMBINATION FORMULATIONS OF TRANILAST AND ALLOPURINOL AND METHODS RELATED THERETO - Disclosed is a pharmaceutical composition comprising tranilast or a pharmaceutically acceptable salt thereof and allopurinol or a pharmaceutically acceptable salt thereof, wherein the amount by weight of said allopurinol or pharmaceutically acceptable salt thereof in said composition is greater than the amount by weight of said tranilast or pharmaceutically acceptable salt thereof in said composition.06-09-2011
20110144134Anti-Inflammatory Pyrazolopyrimndines - The present invention provides anti-inflammatory compounds useful in the treatment of diseases and conditions in which inflammation is involved in disease progression or the manifestation of symptoms of the disease or condition.06-16-2011
20100022561INHIBITORS OF BRUTON'S TYROSINE KINASE - Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.01-28-2010
201100599931-(1-(2-Ethoxyethyl)-3-Ethyl-7-(4-Methylpyridin-2-Ylamino)-1H-Pyrazolo[4,3- -D]Pyrimidin-5-YL) Piperidine-4-Carboxylic Acid And Salts Thereof - The present invention comprises 1-(1-(2-ethoxyethyl)-3-ethyl-7-(4-methylpyridin-2-ylamino)-1H-pyrazolo[4,3-d]pyrimidin-5-yl)piperidine-4-carboxylic acid and its salts. The invention further comprises pharmaceutical compositions, methods of treatment, and synthetic methods relating to 1-(1-(2-ethoxyethyl)-3-ethyl-7-(4-methylpyridin-2-ylamino)-1H-pyrazolo[4,3-d]pyrimidin-5-yl)piperidine-4-carboxylic acid and its salts.03-10-2011
20100280051USE OF ALLOPURINOL FOR THE TREATMENT OF HAND FOOT SKIN REACTION - Use of allopurinol or a pharmaceutically acceptable salt thereof for the treatment or prevention of Hand Foot Skin Reaction (HFSR) induced by Multitargeted Kinase Inhibitor (MKI) therapy. The allopurinol or its salt is administered topically to the affected areas, palms and soles, preferably in the form of a cream.11-04-2010
20110144135Compounds for Modulating TRPV3 Function - The present application relates to compounds and methods for treating pain and other conditions related to TRPV3.06-16-2011
20110086866INHIBITORS OF BRUTON'S TYROSINE KINASE - Described herein are kinase inhibitor compounds, methods for synthesizing such inhibitors, and methods for using such inhibitors in the treatment of diseases. Further described herein are methods, assays and systems for determining an appropriate inhibitor of a protein, including a kinase.04-14-2011
20090253717Inhibitors of p97 - One aspect of the invention relates to compounds that inhibit the activity of p97, such as by binding covalently to a cysteine residue in the active site. In certain embodiments, the invention relates to the treatment of disease, such as cancer, comprising administering a compound of the invention.10-08-2009
20090048274PYRAZOLO[3,4-d]PYRIMIDINE DERIVATIVES - Disclosed are novel pyrazolo[3,4-d]pyrimidine derivatives that are inhibitors of Raf kinase. These compounds and their pharmaceutically-acceptable salts and esters are anti-proliferative agents useful in the treatment or control of proliferative disorders such as solid tumors, in particular breast tumor, colon tumor, lung tumor, prostate tumor, and melanoma. Also disclosed are a composition and a unit dose formulation comprising such a compound, or a pharmaceutically-acceptable salt or ester thereof, methods for making such compounds, and methods for using such compounds, or their pharmaceutically-acceptable salts or esters, in the treatment of proliferative disorders.02-19-2009
20120041005USE OF ALKANOYL L-CARNITINE FOR THE TREATMENT OF ERECTILE DYSFUNCTION - Erectile dysfunction is treated with a combination of propionyl L-carnitine in combination with sildenafil, apomorphine prostaglandin El, pentolamine and papaverine.02-16-2012
20120041004FUSED PYRIMIDINE-DIONE DERIVATIVES AS TRPAI MODULATORS - The invention described herein relates to novel fused pyrimidinediones derivatives of formula (I) which are TRPA (Transient Receptor Potential subfamily A) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPA1 (Transient Receptor Potential subfamily A, member 1). This invention also provides processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1.02-16-2012
20100144764PYRIMIDINEDIONE DERIVATIVES AND METHODS OF USE THEREOF - The present invention relates to Pyrimidinedione Derivatives, compositions comprising a Pyrimidinedione Derivative and methods for using the Pyrimidinedione Derivatives for treating or preventing a metabolic disorder, dyslipidemia, a cardiovascular disease, a neurological disorder, a hematological disease, cancer, inflammation, a respiratory disease, a gastroenterological disease, diabetes, a diabetic complication, obesity, an obesity-related disorder or non-alcoholic fatty liver disease.06-10-2010
201200102246-CYCLYLMETHYL-AND 6-ALKYLMETHYL-SUBSTITUTED PYRAZOLEPYRIMIDINES - The invention relates to novel 6-cyclylmethyl- and 6-alkylmethyl-substituted pyrazolopyrimidines, process for their preparation and their use for producing medicaments for improving perception, concentration, learning and/or memory.01-12-2012
20110166165BICYCLIC HETEROCYCLE DERIVATIVES AND USE THEREOF AS GPR119 MODULATORS - The present invention relates to Bicyclic Heterocycle Derivatives of Formula (I), compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G-protein coupled receptor (GPCR) such as GPR119 in a patient.07-07-2011
20120015963NOVEL PYRAZOLO[3,4-d]PYRIMIDINE COMPOUNDS - The present disclosure is directed to novel compounds of Formula (I)01-19-2012
20100184784PHARMACEUTICAL COMPOSITIONS COMPRISING A MULTIFUNCTIONAL PHOSPHODIESTERASE INHIBITOR AND AN ADENOSINE UPTAKE INHIBITOR - The present invention relates to pharmaceutical compositions comprising at least one multifunctional phosphodiesterase inhibitor (MPDEI) and at least one adenosine uptake inhibitor. The present invention also relates to compositions comprising cilostazol and dipyridamole and their use.07-22-2010
20090281125Heterocyclic Compounds Useful in Treating Diseases and Conditions - The present invention relates to compounds of formula (I)11-12-2009
20120059018NOVEL CHLORIN E6-FOLIC ACID CONJUGATE, PREPARATION METHOD THEREOF, AND A PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF CANCER COMPRISING THE SAME - The present invention relates to a novel chlorin e6-folic acid conjugate, a preparation method thereof, and a pharmaceutical composition for the treatment of cancer comprising the same, and more particularly, to a novel compound prepared by linking chlorin e6 to folic acid, which effectively produces singlet oxygen in various media and has much better tumor selectivity than the known porphyrin-based photosensitizers, thereby being used effectively in photodynamic therapy for malignant tumors, a preparation method thereof, and a pharmaceutical composition for photodynamic treatment of solid tumors comprising the compound.03-08-2012
20120071497METHODS OF TREATING ABC-DLBCL USING INHIBITORS OF BRUTON'S TYROSINE KINASE - Disclosed herein are methods for treating an individual diagnosed with ABC-DLBCL. The methods include administering to the individual an inhibitor of Bruton's tyrosine kinase (Btk).03-22-2012
20120208830Anhydrous Crystalline Forms of N-[1-(2-ethoxyethyl)-5-(N-ethyl-N-methylamino)-7-(4-methylpyridin-2-yl-am- ino)-1H-pyrazolo[4,3-d]pyrimidine-3-carbonyl]methanesulfonamide - The invention comprises (1) anhydrous crystalline forms of N-[1-(2-ethoxyethyl)-5-(N-ethyl-N-methylamino)-7-(4-methylpyridin-2-yl-amino)-1H-pyrazolo[4,3-d]pyrimidine-3-carbonyl]methanesulfonamide, (2) pharmaceutical compositions comprising at least one such form, (3) methods for the treatment of a phosphodiesterase-5-mediated condition using at least one such form, and (4) methods for preparing such forms. The compound N-[1-(2-ethoxyethyl)-5-(N-ethyl-N-methylamino)-7-(4-methylpyridin-2-yl-amino)-1H-pyrazolo[4,3-d]pyrimidine-3-carbonyl]methanesulfonamide has the following structure (I).08-16-2012
20100120796COMPOSITIONS AND METHODS FOR TREATMENT AND PREVENTION OF HYPERURICEMIA RELATED HEALTH CONSEQUNECES - Disclosed herein are methods of delaying the onset or treating diabetes that comprises administering a uric acid lowering agent. The inventors have made the remarkable discovery that elevated uric acid levels are not a corollary to insulin resistance, but rather a primary mediator of insulin resistance. Specifically exemplified are methods that involve administering to a patient susceptible to development of diabetes a composition comprising a uric acid lowering agent in a regimen that maintains serum uric acid levels below at least 5.5 mg/dl, or below at least 5.2 mg/dl.05-13-2010
20090105281Methods of treating inflammation - The invention features compositions and methods for treating inflammation and other immune-related disorders.04-23-2009
20120077827ZAP-70 ACTIVE COMPOUNDS - 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 protein kinases, including a Zeta-chain-associated protein kinase 70 (ZAP-70), and any mutations thereof.03-29-2012
20110065729METHODS AND COMPOSITIONS FOR AMELIORATING THE UNDESIRABLE EFFECTS OF CHEMOTHERAPY - In one aspect, the present invention provides chemoprotectant compositions that each comprise at least two of the chemoprotectants disclosed herein. The chemoprotectant compositions of the invention are useful, for example, for ameliorating at least one adverse effect of chemotherapy. In another aspect, the present invention provides methods of ameliorating at least one adverse effect of chemotherapy, the methods each comprising the step of administering to a subject undergoing chemotherapy an amount of a chemoprotectant composition that is effective to ameliorate at least one adverse effect of the chemotherapy.03-17-2011
20120122893METHODS OF TREATING CANCER - Described are methods and compositions for treating epithelial tumors with a folate-vinca conjugate in combination with at least one other chemotherapeutic agent in which the tumors include ovarian, endometrial or non-small cell lung cancer tumors, including platinum-resistant ovarian tumors and platinum-sensitive ovarian tumors.05-17-2012
20090018147Compounds for modulating TRPV3 function - The present application relates to compounds and methods for treating pain and other conditions related to TRPV3.01-15-2009
20120122894INHIBITORS OF BRUTON'S TYROSINE KINASE - Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.05-17-2012
20100093766NOVEL COMPOUNDS - Novel substituted 1,5,7-trisubstituted-3,4-dihydro-pyrimido[4,5-d]pyrimidin-2-(1H)-one compounds and compositions, and their use in therapy as CSBP/RK/p38 kinase inhibitors.04-15-2010
20100093765NOVEL COMPOUNDS - Novel substituted 1,5,7-trisubstituted-3,4-dihydro-pyrimido[4,5-d]pyrimidin-2-(1H)-one compounds and compositions, and their use in therapy as CSBP/RK/p38 kinase inhibitors.04-15-2010
20090131457Pyrazolo [3,4-D] Pyrimidine Derivatives Useful to Treat Respiratory Disorders - The present invention concerns a compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof, where R05-21-2009
20110184001INHIBITORS OF BRUTON'S TYROSINE KINASE - Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.07-28-2011
201101840001-HETEROCYCLYL-1,5-DIHYDRO-PYRAZOLO[3,4-D] PYRIMIDIN-4-ONE DERIVATES AND THEIR USE AS PDE9A MODULATORS - The invention relates to novel 1,6-disubstituted pyrazolopyrimidinones, Formula (I) with is a mono-, bi- or tri-cyclic heterocyclyl group, the ring members of which are carbon atoms and at least 1, preferably 1, 2 or 3, heteroatom(s), which are selected from the group of nitrogen, oxygen and sulphur, which is in the form of —S(O)07-28-2011
20120165349Phenyl-Substituted Pyrazolopyrimidines - The invention relates to novel phenyl-substituted pyrazolopyrimidines, process for their preparation, and their use for producing medicaments for improving perception, concentration, learning and/or memory.06-28-2012
20120214826INHIBITORS OF BRUTON'S TYROSINE KINASE - Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.08-23-2012
20120214825mTOR/JAK INHIBITOR COMBINATION THERAPY - Provided herein is a combination therapy comprising an mTOR inhibitor and a JAK inhibitor. The combination therapy is useful for the treatment of a variety of cancers, including MPNs. The combination therapy is also useful for the treatment of any number of JAK-associated diseases.08-23-2012
20120214827Anhydrous Crystalline Forms of N-[1-(2-ethoxyethyl)-5-(N-ethyl-N-methylamino)-7-(4-methylpyridin-2-yl-am- ino)-1H-pyrazolo[4,3-d]pyrimidine-3-carbonyl]methanesulfonamide - The invention comprises (1) anhydrous crystalline forms of N-[1-(2-ethoxyethyl)-5-(N-ethyl-N-methylamino)-7-(4-methylpyridin-2-yl-amino)-1H-pyrazolo[4,3-d]pyrimidine-3-carbonyl]methanesulfonamide, (2) pharmaceutical compositions comprising at least one such form, (3) methods for the treatment of a phosphodiesterase-5-mediated condition using at least one such form, and (4) methods for preparing such forms. The compound N-[1-(2-ethoxyethyl)-5-(N-ethyl-N-methylamino)-7-(4-methylpyridin-2-yl-amino)-1H-pyrazolo[4,3-d]pyrimidine-3-carbonyl]methanesulfonamide has the following structure (I).08-23-2012
201201723794 SUBSTITUTED PYRAZOLOPYRIMIDINES - The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.07-05-2012
20100010019Reactive Oxygen Generating Enzyme Inhibitor With Nitric Oxide Bioactivity and Uses Thereof - A reactive oxygen generating enzyme inhibitor with NO donor bioactivity, e.g., nitrated allopurinol, is useful to treat heart failure, stable angina, ischemic disorder, ischemic reperfusion injury, atherosclerosis, sickle cell disease, diabetes, Alzheimer's disease, Parkinson's disease, ALS and asthma and to obtain proper contraction of heart, skeletal and smooth muscle.01-14-2010
20120220607COMPOSITIONS AND METHODS FOR TREATMENT AND PREVENTION OF HYPERURICEMIA RELATED HEALTH CONSEQUENCES - Disclosed herein are methods of delaying the onset or treating diabetes that comprises administering a uric acid lowering agent. The inventors have made the remarkable discovery that elevated uric acid levels are not a corollary to insulin resistance, but rather a primary mediator of insulin resistance. Specifically exemplified are methods that involve administering to a patient susceptible to development of diabetes a composition comprising a uric acid lowering agent in a regimen that maintains serum uric acid levels below at least 5.5 mg/dl, or below at least 5.2 mg/dl.08-30-2012
20120322814METHODS OF INHIBITING IRE1 - Disclosed herein are, inter alia, methods for inhibiting Ire1 activity.12-20-2012
20120129873INHIBITORS OF BRUTON'S TYROSINE KINASE - Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.05-24-2012
20100234400COMPOUNDS THAT MAINTAIN PLURIPOTENCY OF EMBRYONIC STEM CELLS - The present invention relates to methods and compositions for culturing embryonic stem (ES) cells. The methods relate to growing the ES cells in the presence of small molecules of formula (I) that maintain the pluripotency/self-renewal of the cells without feeder cells and LIF in serum-free conditions. These methods in part facilitate much more consistency in embryonic stem cell production, providing, for example, new avenues in the practical applications of embryonic stem cells in regenerative medicine.09-16-2010
20120277255INHIBITORS 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.11-01-2012
20120277254INHIBITORS OF BRUTON'S TYROSINE KINASE - Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.11-01-2012
20120101114INHIBITORS 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.04-26-2012
20120101113INHIBITORS 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.04-26-2012
20100168138Anti-Viral Compounds - Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.07-01-2010
20130012525INHIBITORS OF BRUTON'S TYROSINE KINASE FOR THE TREATMENT OF SOLID TUMORS - Described herein are irreversible Btk inhibitor compounds, and methods for using such irreversible inhibitors in the treatment of diseases and disorders characterized by the presence or development of solid tumors.01-10-2013
20100173915PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT OF CHRONIC HEART FAILURE COMPRISING PYRAZOLOPYRIMIDINONE DERIVATIVE COMPOUND - Disclosed herein is a therapeutic agent for chronic heart failure comprising, as an effective ingredient, 5-[2-propyloxy-5-(1-methyl-2-pyrrolidinyl-ethylamidosulfonyl)phenyl]-1-methyl-propyl-1,6-dihydro-7H-pyrazolo(4,3-d)pyrimidine-7-one. The compound inhibits phosphodiesterase-5 (PDE-5), which catalyzes the intracellular degradation of cyclic guanosine monophosphatase (cGMP), thereby mitigating several signs of chronic heart failure, that is, thereby preventing left ventricular dilatation, decreasing ventricular wall thinning, lowering elevated cardiac and circulating levels of atrial natriuretic peptide (ANP), and inhibiting ventricular fibrosis. Also, the compound has advantages in that it reaches the maximal plasma level in a short time, has an in vivo half-life longer than conventional PDE-5 inhibitors, allowing decreased administration frequency, and has fewer side effects, thus ensuring safety. Thus, the compound is useful as a therapeutic agent for chronic heart failure.07-08-2010
20130018060INHIBITORS 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.01-17-2013
20090239884Methods of Treating Inflammation - The invention features compositions and methods for treating inflammation and other immune-related disorders.09-24-2009
20130172369PROCESSES FOR THE PREPARATION OF DIPYRIDAMOLE - The present invention relates to the active pharmaceutical ingredient dipyridamole. In particular, it relates to efficient processes for the preparation of dipyridamole which are amenable to large scale commercial production and provide the required product with improved yield and purity. The present invention also relates to a novel crystallization method for the purification of dipyridamole.07-04-2013
20130178483Methods and Compositions for Inhibition of Bone Resorption - Disclosed herein are methods and compounds for inhibiting bone and/or cartilage resorption in an individual. The methods comprise administering to the individual a composition comprising a therapeutically effective amount of a compound that is an irreversible inhibitor of a Bruton's tyrosine kinase (BTK), or a pharmaceutically acceptable salt thereof. Also described are irreversible inhibitors of Btk and methods for the preparation of the compounds. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the inhibition of cancer metastasis, and for inhibition of bone or cartilage resorption in cancer patients.07-11-2013
20130178484TREATMENT OF GOUT AND HYPERURICEMIA - Sodium 2-(5-bromo-4-(4-cyclopropylnaphthalen-1-yl)-4H-1,2,4-triazol-3-ylthio)acetate is described. In addition, pharmaceutical compositions and uses of such compositions for the treatment of a variety of diseases and conditions are described.07-11-2013
20130172368Methods for Treating Hyperuricemia in Patients with Gout Using Halofenate or Halogenic Acid and A Second Urate-Lowering Agent - Disclosed herein are pharmaceutical compositions, methods and kits for lowering the serum uric acid level of a subject and for the treatment of a condition associated with elevated serum uric acid levels comprising administering a composition comprising a first urate-lowering agent and a second urate-lowering agent. In some aspects the first urate-lowering agent is (−)-halofenate, (−)-halofenic acid, or a pharmaceutically acceptable salts thereof. In some aspects the second urate-lowering agent is an inhibitor of uric acid production, a uricosuric agent, a uricase, or a pharmaceutically acceptable salt thereof.07-04-2013
20120252822INHIBITORS OF BRUTON'S TYROSINE KINASE - Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.10-04-2012
20120252821INHIBITORS OF BRUTON'S TYROSINE KINASE - Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.10-04-2012
20110269779METHODS AND COMPOSITIONS FOR TREATMENT OF OPHTHALMIC CONDITIONS - The present invention provides chemical entities or compounds and pharmaceutical compositions thereof that are capable of modulating signal transduction by certain protein kinases such as mTor, tyrosine kinases, and/or lipid kinases such as PB kinase in an ocular tissue. 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.11-03-2011
20130096142METHODS FOR HEALTHY AGING - Genome-wide association studies have been used to elucidate genes and/or pathways related to diseases; however, this methodology has yet to be used to understand the phenotype of healthy aging and/or healthspan in humans.04-18-2013
20080200481Method of treatment of myocardial infarction - Myocardial infarction in a mammal is treated by administering to the mammal a therapeutically effective amount of a chemical Src family tyrosine kinase protein inhibitor and the use of such inhibitor compounds for the preparation of a medicament for treating myocardial infarction. Myocardial infarction can be prevented by administering to the mammal a prophylactic amount of the inhibitor. The inhibitor preferably is an inhibitor of Src protein selected from the group consisting of a pyrazolopyrimidine class Src family tyrosine kinase inhibitor, a macrocyclic dienone class Src family tyrosine kinase inhibitor, a pyrido[2,3-d]pyrimidine class Src family tyrosine kinase inhibitor, a 4-anilino-3-quinolinecarbonitrile class Src family tyrosine kinase inhibitor, and a mixture thereof. The Src family tyrosine kinase inhibitors can be used to prepare medicaments for the treatment of myocardial infarction. Also disclosed are articles of manufacture containing a chemical Src family tyrosine kinase inhibitor.08-21-2008
20110224235INHIBITORS OF BRUTON'S TYROSINE KINASE FOR THE TREATMENT OF SOLID TUMORS - Described herein are irreversible Btk inhibitor compounds, and methods for using such irreversible inhibitors in the treatment of diseases and disorders characterized by the presence or development of solid tumors.09-15-2011
20110275651FUSED RING HETEROARYL KINASE INHIBITORS - Provided herein are fused ring heteroaryl compounds useful in a variety of methods, including reducing the activity of certain kinases and treating certain disease states.11-10-2011
20130150381PHENYLTHIOACETATE COMPOUNDS, COMPOSITIONS AND METHODS OF USE - Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of using them. In some embodiments, the compounds described herein are used in the treatment or prevention of dis orders related to aberrant levels of uric acid.06-13-2013
20130137708METHODS AND COMPOSITIONS FOR KINASE INHIBITION - The present invention sets forth a new chemical genetic approach for engineering kinase enzymes with a cysteine gatekeeper residue as well as for developing electrophilic inhibitors thereto. The present invention also provides a Src proto-oncogenic tyrosine kinase with a cysteine gatekeeper that recapitulates wild type activity and can be irreversibly inhibited both in vitro and in cells. The present invention also provides methods and compositions for modulating kinases and for treating kinase-associated diseases.05-30-2013
20120283277INHIBITORS OF BRUTON'S TYROSINE KINASE - Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.11-08-2012
20120283276INHIBITORS OF BRUTON'S TYROSINE KINASE - Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.11-08-2012
20110294834Alkyl-substituted pyrazolopyrimidines - The invention relates to novel alkyl-substituted pyrazolopyrimidines, process for their preparation, and the use thereof for producing medicaments for improving perception, concentration, learning and/or memory.12-01-2011
20130203779THIOACETATE COMPOUNDS, COMPOSITIONS AND METHODS OF USE - Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.08-08-2013
20120095026INHIBITORS OF BRUTON'S TYROSINE KINASE - Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.04-19-2012

Patent applications in class Exactly four ring nitrogens in the bicyclo ring system

Patent applications in all subclasses Exactly four ring nitrogens in the bicyclo ring system