Entries |
Document | Title | Date |
20080200481 | Method 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 |
20080207646 | Agent 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 |
20080280925 | Amines 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 |
20080293746 | COMBINATIONS 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 |
20080318982 | Pharmaceutical 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 |
20090018147 | Compounds for modulating TRPV3 function - The present application relates to compounds and methods for treating pain and other conditions related to TRPV3. | 01-15-2009 |
20090048274 | PYRAZOLO[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 |
20090062313 | Pde5 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 |
20090076037 | BICYCLIC PYRIMIDINE KINASE INHIBITORS - The present invention is directed to novel bicyclic pyrimidine compounds of Formula (I) or a form or composition thereof | 03-19-2009 |
20090099211 | TREATMENTS 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 |
20090105281 | Methods of treating inflammation - The invention features compositions and methods for treating inflammation and other immune-related disorders. | 04-23-2009 |
20090124638 | ANTI-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 |
20090131457 | Pyrazolo [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 R | 05-21-2009 |
20090156618 | 1-(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 |
20090163520 | MNK1 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 |
20090163521 | Novel 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 |
20090197899 | 3-(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 |
20090239883 | Treatment 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 |
20090239884 | Methods of Treating Inflammation - The invention features compositions and methods for treating inflammation and other immune-related disorders. | 09-24-2009 |
20090253717 | Inhibitors 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 |
20090270425 | 3-(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 |
20090270426 | P13 Kinase Antagonists - The present invention provides novel PI3-Kinase antagonists and methods of use thereof. | 10-29-2009 |
20090281125 | Heterocyclic Compounds Useful in Treating Diseases and Conditions - The present invention relates to compounds of formula (I) | 11-12-2009 |
20090286812 | GPR119 Receptor Agonists - Provided herein are compounds of the formula (I): | 11-19-2009 |
20090306097 | Use 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 |
20100004270 | INHIBITORS 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 |
20100010018 | 4-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 |
20100010019 | Reactive 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 |
20100016339 | FUNGICIDAL 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-OCH | 01-21-2010 |
20100022561 | INHIBITORS 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 |
20100035900 | 6-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 |
20100041677 | INHIBITORS 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 |
20100041678 | COMPOSITIONS 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 |
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 |
20100093765 | NOVEL 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 |
20100093766 | NOVEL 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 |
20100105704 | 7-(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 |
20100113486 | USE 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 |
20100120796 | COMPOSITIONS 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 |
20100144764 | PYRIMIDINEDIONE 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 |
20100152209 | Compounds for Modulating TRPV3 Function - The present application relates to compounds and methods for treating pain and other conditions related to TRPV3. | 06-17-2010 |
20100160350 | PYRAZOLOPYRIMIDINONE 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 |
20100160351 | PHARMACEUTICAL 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 |
20100168138 | Anti-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 |
20100173915 | PHARMACEUTICAL 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 |
20100184784 | PHARMACEUTICAL 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 |
20100190805 | PREPARATION 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 |
20100234400 | COMPOUNDS 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 |
20100249152 | NEW 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 |
20100249153 | SUBSTITUTED 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 |
20100280051 | USE 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 |
20100298351 | NOVEL 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 |
20110021542 | Use 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 |
20110039868 | INHIBITORS 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 |
20110059993 | 1-(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 |
20110065729 | METHODS 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 |
20110065730 | 6-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 |
20110071168 | NITRIC 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 |
20110086866 | INHIBITORS 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 |
20110092520 | PROCESS 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 |
20110136835 | COMBINATION 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 |
20110144134 | Anti-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 |
20110144135 | Compounds for Modulating TRPV3 Function - The present application relates to compounds and methods for treating pain and other conditions related to TRPV3. | 06-16-2011 |
20110166165 | BICYCLIC 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 |
20110184000 | 1-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 |
20110184001 | INHIBITORS 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 |
20110207752 | P70 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 |
20110212977 | P70 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 |
20110224235 | INHIBITORS 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 |
20110224236 | TREATMENT 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 |
20110224237 | USE 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 |
20110245276 | PHOTOSTABILIZED 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 |
20110257202 | Therapeutic 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 |
20110257203 | INHIBITORS 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 |
20110263617 | Combination 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 |
20110269779 | METHODS 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 |
20110275651 | FUSED 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 |
20110294833 | Methods 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 |
20110294834 | Alkyl-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 |
20120010224 | 6-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 |
20120015963 | NOVEL PYRAZOLO[3,4-d]PYRIMIDINE COMPOUNDS - The present disclosure is directed to novel compounds of Formula (I) | 01-19-2012 |
20120041004 | FUSED 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 |
20120059018 | NOVEL 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 |
20120071497 | METHODS 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 |
20120077827 | ZAP-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 |
20120095026 | INHIBITORS 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 |
20120101113 | INHIBITORS OF BRUTON'S TYROSINE KINASE - Described herein are irreversible kinase inhibitor compounds, methods for synthesizing such irreversible inhibitors, and methods for using such irreversible inhibitors in the treatment of diseases. Further described herein are methods, assays and systems for determining an appropriate irreversible inhibitor of a protein, including a kinase. | 04-26-2012 |
20120101114 | INHIBITORS OF BRUTON'S TYROSINE KINASE - Described herein are irreversible kinase inhibitor compounds, methods for synthesizing such irreversible inhibitors, and methods for using such irreversible inhibitors in the treatment of diseases. Further described herein are methods, assays and systems for determining an appropriate irreversible inhibitor of a protein, including a kinase. | 04-26-2012 |
20120108612 | INHIBITORS 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 |
20120115889 | INHIBITORS 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 |
20120122893 | METHODS 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 |
20120122894 | INHIBITORS 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 |
20120129873 | INHIBITORS 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 |
20120165349 | Phenyl-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 |
20120172379 | 4 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 |
20120184567 | INHIBITORS OF BRUTON'S TYROSINE KINASE - Described herein are irreversible kinase inhibitor compounds, methods for synthesizing such irreversible inhibitors, and methods for using such irreversible inhibitors in the treatment of diseases. Further described herein are methods, assays and systems for determining an appropriate irreversible inhibitor of a protein, including a kinase. | 07-19-2012 |
20120202829 | 6-Cycloalkyl-pyrazolopyrimidinones for the Treatment of CNS Disorders - The invention relates to novel 6-Cycloalkyl-pyrazolopyrimidinones according to formula (I). | 08-09-2012 |
20120208830 | Anhydrous 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 |
20120214825 | mTOR/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 |
20120214826 | INHIBITORS 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 |
20120214827 | Anhydrous 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 |
20120220607 | COMPOSITIONS 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 |
20120252821 | INHIBITORS 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 |
20120252822 | INHIBITORS 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 |
20120277254 | INHIBITORS 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 |
20120277255 | INHIBITORS OF BRUTON'S TYROSINE KINASE - Described herein are irreversible kinase inhibitor compounds, methods for synthesizing such irreversible inhibitors, and methods for using such irreversible inhibitors in the treatment of diseases. Further described herein are methods, assays and systems for determining an appropriate irreversible inhibitor of a protein, including a kinase. | 11-01-2012 |
20120283276 | INHIBITORS 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 |
20120283277 | INHIBITORS 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 |
20120322814 | METHODS OF INHIBITING IRE1 - Disclosed herein are, inter alia, methods for inhibiting Ire1 activity. | 12-20-2012 |
20130005745 | INHIBITORS 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. | 01-03-2013 |
20130005746 | INHIBITORS OF BRUTONS 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. | 01-03-2013 |
20130012525 | INHIBITORS 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 |
20130018060 | INHIBITORS OF BRUTON'S TYROSINE KINASE - Described herein are irreversible kinase inhibitor compounds, methods for synthesizing such irreversible inhibitors, and methods for using such irreversible inhibitors in the treatment of diseases. Further described herein are methods, assays and systems for determining an appropriate irreversible inhibitor of a protein, including a kinase. | 01-17-2013 |
20130035348 | ANTIMETASTATIC 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 |
20130035349 | PYRAZOLOPYRIMIDINONE 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 |
20130040971 | 6-CYCLOALKYL-PYRAZOLOPYRIMIDINONES FOR THE TREATMENT OF CNS DISORDERS - The invention relates to novel pyrazolopyrimidinones according to formula (I) | 02-14-2013 |
20130040972 | USE 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 |
20130059868 | TREATMENT 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 |
20130096142 | METHODS 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 |
20130131088 | TREATING 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 |
20130137708 | METHODS 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 |
20130137709 | Compounds 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 |
20130150381 | PHENYLTHIOACETATE 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 |
20130165454 | COMPOUNDS 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 |
20130172368 | Methods 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 |
20130172369 | PROCESSES 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 |
20130178483 | Methods 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 |
20130178484 | TREATMENT 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 |
20130203779 | THIOACETATE 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 |
20130225610 | ANTIMETASTATIC 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. | 08-29-2013 |
20130231355 | QUINAZOLIN-4 (3H)- ONE DERIVATIVES USED AS P13 KINASE INHIBITORS - The present invention relates to the compound of formula (I) | 09-05-2013 |
20130245045 | SELECTIVE PHOSPHODIESTERASE 9A INHIBITORS AS MEDICAMENTS FOR IMPROVING COGNITIVE PROCESSES - The invention relates to the use of selective phosphodiesterase 9A (PDE9A) inhibitors for producing medicaments for improving perception, concentration, cognitive processes, learning and/or memory. | 09-19-2013 |
20130281469 | THIOACETATE 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. | 10-24-2013 |
20130296345 | METHODS FOR TREATING HYPERURICEMIA AND RELATED DISEASES - Provided herein are methods of treating gout, treating hyperuricemia, lowering serum uric acid, or the like with compounds of formula (I) have the following structure Further, provided herein are compositions comprising a compound of formula (I). | 11-07-2013 |
20130303552 | NOVEL INHIBITORS OF SECRETION OF HEPATITIS B VIRUS ANTIGENS - Pharmaceutical compositions of the invention comprise triazolopyrimidines useful for the treatment of hepatitis virus in a patient. | 11-14-2013 |
20130310402 | USE OF INHIBITORS OF BRUTON'S TYROSINE KINASE (BTK) - Disclosed herein are methods for treating a cancer comprising: a. administering a Btk inhibitor to a subject sufficient to result in an increase or appearance in the blood of a subpopulation of lymphocytes defined by immunophenotyping; b. determining the expression profile of one or more biomarkers from one or more subpopulation of lymphocytes; and c. administering a second agent based on the determined expression profile. | 11-21-2013 |
20130338172 | CRYSTALLINE FORMS OF A BRUTON'S TYROSINE KINASE INHIBITOR - Described herein is the Bruton's tyrosine kinase (Btk) inhibitor 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one, including crystalline forms, solvates and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions that include the Btk inhibitor, as well as methods of using the Btk inhibitor, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions. | 12-19-2013 |
20140011819 | NOVEL SELECTIVE PI3K DELTA INHIBITORS - The present invention relates to selective inhibitors of PI3K delta protein kinases, methods of preparing them, pharmaceutical compositions containing them and methods of treatment and/or prevention of kinase mediated diseases or disorders with them. | 01-09-2014 |
20140011820 | USE 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. | 01-09-2014 |
20140066461 | METHODS FOR DIAGNOSING AND TREATING SCHIZOPHRENIA - Genetic markers of schizophrenia (SCZ) are presented herein, as are methods for using same for assessing risk of developing SCZ and diagnosing SCZ. Methods for choosing a therapeutic regimen and predicting and/or determining efficacy of a therapeutic regimen based on these genetic markers are also encompassed herein. | 03-06-2014 |
20140080843 | METHODS FOR INHIBITING FASCIN - Provided are compositions and methods for treating a condition or disorder mediated by fascin activity in a subject in need thereof which method comprises administering to the subject a therapeutically effective amount of at least one compound of any one of Formula I-a to I-n, II, II-a, II-b or III or a pharmaceutically acceptable salt thereof. | 03-20-2014 |
20140080844 | INHIBITORS 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. | 03-20-2014 |
20140080845 | USE 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. | 03-20-2014 |
20140107136 | COMPOSITIONS AND METHODS FOR TREATMENT AND DELAYING THE ONSET OF DIABETES - 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 5.2 to 5.5 mg/dl. | 04-17-2014 |
20140128413 | INHIBITORS 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. | 05-08-2014 |
20140128414 | INHIBITORS 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. | 05-08-2014 |
20140135347 | INHIBITORS 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. | 05-15-2014 |
20140142123 | INHIBITORS 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. | 05-22-2014 |
20140155417 | COMPOUNDS FOR MODULATING TRPV3 FUNCTION - The present application relates to compounds and methods for treating pain and other conditions related to TRPV3. | 06-05-2014 |
20140163045 | Small Molecule Xanthine Oxidase Inhibitors and Methods of Use - Small molecule xanthine oxidase inhibitors are provided, as well as methods for their use in treating gout or hyperuricemia. | 06-12-2014 |
20140163046 | INHIBITORS 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. | 06-12-2014 |
20140171453 | INHIBITORS 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. | 06-19-2014 |
20140179717 | Use 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. | 06-26-2014 |
20140187564 | INHIBITORS 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. | 07-03-2014 |
20140187565 | INHIBITORS 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. | 07-03-2014 |
20140194446 | USE OF INHIBITORS OF BRUTON'S TYROSINE KINASE (BTK) - Disclosed herein are methods for treating a cancer comprising: a. administering a Btk inhibitor to a subject sufficient to result in an increase or appearance in the blood of a subpopulation of lymphocytes defined by immunophenotyping; b. determining the expression profile of one or more biomarkers from one or more subpopulation of lymphocytes; and c. administering a second agent based on the determined expression profile. | 07-10-2014 |
20140221398 | PYRAZOLOPYRIMIDINE DERIVATIVES AS TYROSINE KINASE INHIBITORS - The present disclosure provides compounds and pharmaceutically acceptable salts that are tyrosine kinase inhibitors, in particular BLK, BMX, EGFR, HER2, HER4, ITK, Jak3, TEC, Btk, and TXK and are therefore useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as cancer and inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and pharmaceutically acceptable salts and processes for preparing such compounds and pharmaceutically acceptable salts. | 08-07-2014 |
20140243355 | INHIBITORS 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. | 08-28-2014 |
20140243356 | USE OF TRANSLATIONAL PROFILING TO IDENTIFY TARGET MOLECULES FOR THERAPEUTIC TREATMENT - The present invention provides methods of identifying an agent that modulates an oncogenic signaling pathway in a biological sample by generating a translational profile of gene translational levels in the biological sample. The present invention also provides diagnostic and therapeutic methods using the translational profiling methods described herein. | 08-28-2014 |
20140243357 | SUBSTITUTED PYRAZOLO[3,4-D]PYRIMIDINES AND USES THEREOF - Presented herein are novel therapeutic compounds and methods of using the same for the treatment of cancers. | 08-28-2014 |
20140249164 | COMPOUNDS - The present invention relates to compounds of formula (I) | 09-04-2014 |
20140256748 | 3,4-DI-SUBSTITUTED PYRIDINE COMPOUND, METHODS OF USING AND COMPOSITIONS COMPRISING THE SAME - 2-((3-(4-cyanonaphthalen-1-yl)pyridin-4-yl)thio)-2-methylpropanoic acid is useful in the modulation of blood or serum uric acid levels. In some embodiments, 2-((3-(4-cyanonaphthalen-1-yl)pyridin-4-yl)thio)-2-methylpropanoic acid is used in the treatment or prevention of disorders related to aberrant levels of uric acid. In some embodiments, 2-((3-(4-cyanonaph-thalen-1-yl)pyridin-4-yl)thio)-2-methylpropanoic acid is used for reducing serum uric acid levels in a human. Also described herein are compositions comprising 2-((3-(4-cyanonaphthalen-1-yl)pyridin-4-yl)thio)-2-methylpropanoic acid, and their use in the modulation of blood or serum uric acid levels. | 09-11-2014 |
20140275124 | METHODS FOR TREATING EYE DISORDERS USING DIPYRIDAMOLE - The present invention discloses methods for treating eye disorders. The methods include the step of administering an effective amount of a topically-administered dipyridamole. Preferably, the topically-administered dipyridamole is formulated as a solution. Preferably, the topically-administered dipyridamole is at least one agent selected from the group consisting of: dipyridamole, and a pharmaceutically-acceptable salt thereof. Preferably, the effective amount corresponds to a concentration of at least about 10 | 09-18-2014 |
20140275125 | INHIBITORS 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. | 09-18-2014 |
20140275126 | PROCESSES AND INTERMEDIATES FOR PREPARING A MEDICAMENT - Disclosed is a process for the preparation of the following compounds: | 09-18-2014 |
20140288096 | P13 KINASE ANTAGONISTS - The present invention provides novel PI3-Kinase antagonists and methods of use thereof. | 09-25-2014 |
20140288097 | USE OF TRANSLATIONAL PROFILING TO IDENTIFY TARGET MOLECULES FOR THERAPEUTIC TREATMENT - The present invention provides methods of identifying an agent or drug candidate molecule, validating a target, and identifying normalizing therapeutics that modulates translation, such as in an oncogenic signaling pathway, in a biological sample as determined by translational profiling of one or more genes in the biological sample. The present invention also provides diagnostic and therapeutic methods using the translational profiling methods described herein. | 09-25-2014 |
20140288098 | Bruton's Tyrosine Kinase As Anti-Cancer Drug Target - Receptor protein kinases (RPTKs) transmit extracellular signals across the plasma membrane to cytosolic proteins, stimulating formation of complexes that regulate key cellular functions. Over half of the known tyrosine kinases are implicated in human cancers and are therefore highly promising drug targets. A large-scale loss-of-function analysis of tyrosine kinases using RNA interference in the clinically relevant Erb-B2 positive, BT474 breast cancer cell line showed that Bruton's tyrosine kinase (BTK), a cytosolic, non-receptor tyrosine kinase that has been extensively studied for its role in B cell development, is required, in altered form, for BT474 breast cancer survival. This alternative form contains an amino-terminal extension that is also present in tumorigenic breast cells at significantly higher levels than in normal breast cells. | 09-25-2014 |
20140296259 | 4-Amino-3-phenylamino-6-phenylpyrazolo[3,4-d]pyrimidine derivatives, their manufacture and their use as antiviral active substances - The present invention relates to 5-amino-3-phenylamino-6-phenylpyrazolo[3,4-d]pyrimidine derivatives of the general formula I | 10-02-2014 |
20140303190 | TYROSINE KINASE INHIBITORS - The present disclosure provides compounds and pharmaceutically acceptable salts thereof that are tyrosine kinase inhibitors, in particular BLK, BMX, EGFR, HER2, HER4, ITK, TEC, BTK, and TXK and are therefore useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as cancer and inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and pharmaceutically acceptable salts thereof and processes for preparing such compounds and pharmaceutically acceptable salts thereof. | 10-09-2014 |
20140303191 | USE OF INHIBITORS OF BRUTON'S TYROSINE KINASE (BTK) - Methods are provided for treating a hematologic cancer comprising administering an anticancer agent to a subject identified as having an increased mobilization of a subpopulation of lymphocytes from a malignancy following administration of an irreversible Btk inhibitor. Methods also are provided for identification of subjects for treatment and the analysis of cells mobilized from a hematologic malignancy following administration of an irreversible Btk inhibitor. | 10-09-2014 |
20140309241 | SALT AND POLYMORPH OF PYRAZOLOPYRIMIDINONE COMPOUND, AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME, PREPARATION METHOD AND USE THEREOF - The present invention relates to new salts of pyrazolopyrimidinone represented by formula (I), and pharmaceutically acceptable polymorph, solvate, hydrate, dehydrate, co-crystallization, anhydrous, or amorphous form thereof, the pharmaceutical compositions, and a pharmaceutical unit dosage form containing the same, wherein x represents organic or inorganic acids, preferable maleic acid, succinic acid, methanesulfonic acid, hydrochloric acid, etc. The invention further relates to co-crystals or complexes of compounds of pyrazolopyrimidinone and pharmaceutical compositions containing the same. The present invention also relates to a process for the preparation, use thereof and pharmaceutical preparation containing the salts or crystalline forms. | 10-16-2014 |
20140323504 | Pyrazolo[4,3-c]Pyridine Derivatives As Kinase Inhibitors - The present invention relates to compounds of formula (I) | 10-30-2014 |
20140336203 | CRYSTALLINE FORMS OF A BRUTON'S TYROSINE KINASE INHIBITOR - Described herein is the Bruton's tyrosine kinase (Btk) inhibitor 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one, including crystalline forms, solvates and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions that include the Btk inhibitor, as well as methods of using the Btk inhibitor, 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. | 11-13-2014 |
20140336204 | METHODS OF INHIBITING XANTHINE OXIDASE ACTIVITY IN A CELL - Small molecule xanthine oxidase inhibitors are provided, as well as methods for their use in treating gout or hyperuricemia. | 11-13-2014 |
20140336205 | Small Molecule Xanthine Oxidase Inhibitors and Methods of Use - Small molecule xanthine oxidase inhibitors are provided, as well as methods for their use in treating gout or hyperuricemia. | 11-13-2014 |
20140336206 | INHIBITORS OF BRUTON'S TYROSINE KINASE - Disclosed herein are pyrazolo[3,4-d]pyrimidines 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. | 11-13-2014 |
20140357651 | COMBINATION PHARMACEUTICAL COMPOSITIONS AND USES THEREOF - The present invention provides for methods and pharmaceutical compositions for treating proliferative disorders. In one aspect, the method comprises administration of two cell-cycle suppressors having a synergistic effect. In another aspect, two cell-cycle suppressors having a synergistic effect are provided in a pharmaceutical composition. | 12-04-2014 |
20140371241 | TEC FAMILY KINASE INHIBITOR ADJUVANT THERAPY - Described herein are methods and compositions comprising a covalent TEC family kinase inhibitor for use in adjuvant therapy, including adjuvant cancer therapy, vaccination and treatment of immune disorders and pathogenic infections. | 12-18-2014 |
20140378478 | Small Molecule Xanthine Oxidase Inhibitors and Methods of Use - Small molecule xanthine oxidase inhibitors are provided, as well as methods for their use in treating gout or hyperuricemia. | 12-25-2014 |
20150025088 | 6-CYCLOALKYL-PYRAZOLOPYRIMIDINONES FOR THE TREATMENT OF CNS DISORDERS - The invention relates to novel 6-Cycloalkyl-pyrazolopyrimidinones according to formula (I). | 01-22-2015 |
20150031710 | USE OF INHIBITORS OF BRUTON'S TYROSINE KINASE (BTK) - Disclosed herein are methods for treating a cancer comprising: a. administering a Btk inhibitor to a subject sufficient to result in an increase or appearance in the blood of a subpopulation of lymphocytes defined by immunophenotyping; b. determining the expression profile of one or more biomarkers from one or more subpopulation of lymphocytes; and c. administering a second agent based on the determined expression profile. | 01-29-2015 |
20150031711 | USE OF INHIBITORS OF BRUTON'S TYROSINE KINASE (BTK) - Disclosed herein are methods for treating a cancer comprising: a. administering a Btk inhibitor to a subject sufficient to result in an increase or appearance in the blood of a subpopulation of lymphocytes defined by immunophenotyping; b. determining the expression profile of one or more biomarkers from one or more subpopulation of lymphocytes; and c. administering a second agent based on the determined expression profile. | 01-29-2015 |
20150031712 | Therapeutic Compositions Containing Dipyridamole and Treatment Packs Including Such Compositions and Methods for Producing Same - A treatment pack comprising: (a) multiple doses of a composition containing dipyridamole as an active ingredient; (b) packaging material; and (c) instructions for topical administration of said composition to the anterior segment of the eye to treat an anterior segment eye disorder. | 01-29-2015 |
20150038518 | METHODS FOR THE TREATMENT OF SOLID TUMORS - Described herein are combinations of ACK inhibitors and HDAC inhibitors in the treatment of diseases and disorders characterized by the presence or development of solid tumors. | 02-05-2015 |
20150038519 | ORGANIC COMPOUNDS - The invention provides a new method of treating diseases or conditions characterized by reduced dopamine D1 receptor signaling activity, such as Parkinson's disease, depression, and cognitive impairment of schizophrenia, comprising administering an effective amount of a 1,3,5,-substituted, 6,7-dihydro-1H-pyrazolo[4,3-d]pyrimidin-7-one to a patient in need thereof. | 02-05-2015 |
20150065524 | KINASE INHIBITOR POLYMORPHS - Polymorphs, hydrates, and solvates of chemical compounds that modulate kinase activity, including mTOR activity, and chemical compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including mTOR activity, are described herein. | 03-05-2015 |
20150094319 | INHIBITORS 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. In addition, reversible inhibitors of Btk are also described. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions. | 04-02-2015 |
20150094320 | PROCESSES 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. | 04-02-2015 |
20150105408 | CRYSTALLINE Pl3 KINASE INHIBITORS - There is provided inter alia 6-(2-((4-amino-3-(3-hydroxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)methyl)-3-(2-chlorobenzyl)-4-oxo-3,4-dihydroquinazolin-5-yl)-N,N-bis(2-methoxyethyl)hex-5-ynamide in the form of a solid crystalline hydrate and in solid crystalline anhydrous form. There are also provided dry powder pharmaceutical compositions for inhalation containing such solid crystalline forms. | 04-16-2015 |
20150105409 | HDAC INHIBITORS, ALONE OR IN COMBINATION WITH BTK INHIBITORS, FOR TREATING NONHODGKIN'S LYMPHOMA - The invention relates to HDAC inhibitors, or combinations comprising an HDAC inhibitor and a BTK inhibitor for the treatment of non-hodgkin's lymphoma in a subject in need thereof. Also provided herein are methods for treating non-hodgkin's lymphoma in a subject in need thereof comprising administering to the subject a therapeutically effective amount of an HDAC inhibitor, or a combination comprising an HDAC inhibitor and a BTK inhibitor. | 04-16-2015 |
20150105410 | POLYMORPHIC FORMS OF 2-(5-BROMO-4-(4-CYCLOPROPYLNAPHTHALEN-1-YL)-4H-1,2,4-TRIAZOL-3-YLTHIO)ACE- TIC ACID AND USES THEREOF - Crystalline polymorph forms of 2-(5-bromo-4-(4-cyclopropyl naphthalen-1-yl)-4H-1,2,4-triazol-3-ylthio)acetic acid are described. Pharmaceutical compositions and the uses of such compounds, compound forms, and compositions for the treatment of a variety of diseases and conditions are also presented. | 04-16-2015 |
20150119405 | INHIBITORS OF THE FIBROBLAST GROWTH FACTOR RECEPTOR - Described herein are inhibitors of FGFR-4, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions. | 04-30-2015 |
20150126532 | Identification of Stabilizers of Multimeric Proteins - Disclosed herein are compounds and compositions thereof which find use in increasing stability of TTR tetramers reducing its tendency to misfold and form aggregates. Also provided herein are methods for using these compounds and compositions for increasing stability of TTR and thereby decreasing aggregate formation by TTR. Also disclosed herein are methods to screen for candidate compounds that increase stability of TTR. Also disclosed herein are heterobifunctional compounds that include a TTR binding compound connected to a targeting moiety via a linker, for use in disrupting PPIs of a target protein. | 05-07-2015 |
20150141438 | METHODS FOR DELAYING OR PREVENTING THE ONSET OF TYPE 1 DIABETES - Described herein are methods for preventing or delaying the onset of Type 1 Diabetes, or inhibiting the maturation of anti-insulin B cells, in an individual in need thereof. The methods include administering to an individual in need thereof ibrutinib, alone or in combination with other Type 1 Diabetes treatments. | 05-21-2015 |
20150306054 | THE USE OF BUCILLAMINE IN THE TREATMENT OF GOUT - Disclosed are pharmaceutical compositions comprising, bucillamine, including bucillamine and allopurinol or colchicine, or pharmaceutically acceptable salts or solvates thereof, together with one or more pharmaceutically acceptable carriers, diluents and excipients. Methods for use of the said compositions in the treatment of gout and metabolic syndrome are also disclosed. | 10-29-2015 |
20150306105 | BENZOXAZOLE KINASE INHIBITORS AND METHODS OF USE - The present invention provides chemical entities or compounds and pharmaceutical compositions thereof that are capable of modulating certain protein kinases such as mTor, tyrosine kinases, and/or lipid kinases such as PI3 kinase. Also provided in the present invention are methods of using these compositions to modulate activities of one or more of these kinases, especially for therapeutic applications. | 10-29-2015 |
20150315192 | SUBSTITUTED PYRAZOLO[3,4-d]PYRIMIDINE COMPOUNDS, THEIR PREPARATION AND USE AS SIGMA RECEPTORS LIGANDS - The present invention relates to new substituted pyrazolo[3,4-d]pyrimidine compounds, having a great affinity for sigma receptors, especially sigma-1 receptor, as well as to the process for the preparation thereof, to compositions comprising them, and to their use as medicaments. | 11-05-2015 |
20150315198 | PYRAZOLOPYRIDINE PYRAZOLOPYRIMIDINE AND RELATED COMPOUNDS - In one aspect this invention relates generally to compounds of Formula: | 11-05-2015 |
20150329550 | INHIBITORS 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. | 11-19-2015 |
20150344478 | PROTEIN KINASE INHIBITORS - The present invention relates to a novel family of inhibitors of protein kinase of formula 1 and process for their production and pharmaceutical compositions thereof. In particular, the present invention relates to inhibitors of the members of the Tec, Src and Btk protein kinase families. | 12-03-2015 |
20150353563 | PYRAZOLO[3,4-D]PYRIMIDINONE COMPOUNDS AS INHIBITORS OF THE P53/MDM2 INTERACTION - The invention relates to compounds of formula (I): as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds. | 12-10-2015 |
20150361083 | NOVEL SELECTIVE PI3K DELTA INHIBITORS - The present invention relates to selective inhibitors of PI3K delta protein kinases, methods of preparing them, pharmaceutical compositions containing them and methods of treatment and/or prevention of kinase mediated diseases or disorders with them. | 12-17-2015 |
20150361504 | BIOMARKER FOR PREDICTING RESPONSE OF CLL TO TREATMENT WITH A BTK INHIBITOR - Disclosed herein are methods for treating an individual diagnosed with a solid tumor or a hematological malignancy, such as chronic lymphocytic leukemia (CLL), for treatment with a Bruton's tyrosine kinase (BTK) inhibitor (e.g., ibrutinib) based on the expression level of miR-155. Also disclosed herein are methods for assessing whether an individual having a solid tumor or a hematological malignancy such as chronic lymphocytic leukemia (CLL) is responsive or likely to be responsive to therapy with a BTK inhibitor (e.g., ibrutinib). Further disclosed herein are methods of monitoring whether an individual receiving a BTK inhibitor (e.g., ibrutinib) for treatment of a solid tumor or a hematological malignancy such as chronic lymphocytic leukemia (CLL) has relapsed or is likely to have a relapse to therapy. Also disclosed herein are methods of selecting an individual having a solid tumor or a hematological malignancy such as chronic lymphocytic leukemia (CLL) for therapy with a BTK inhibitor (e.g., ibrutinib). | 12-17-2015 |
20150374699 | NOVEL USES - The invention relates to the administration of inhibitors of phosphodiesterase 1 (PDE1) for the treatment of diseases or disorders characterized by disruption of or damage to various cGMP/PKG mediated pathways. In one embodiment the invention relates to inhibitors of phosphodiesterase 1 (PDE1) for treatment of cardiovascular disease and related disorders, e.g., congestive heart disease, atherosclerosis, myocardial infarction, and stroke. | 12-31-2015 |
20150376188 | SELECTIVE DUAL INHIBITORS OF PI3 DELTA AND GAMMA PROTEIN KINASES - The present invention relates to a selective dual delta (δ) and gamma (γ) PI3K protein kinase modulator (S)—N-(5-(4-amino-1-(1-(5-fluoro-3-(3-fluorophenyl)-4-oxo-4H-chromen-2-yl)ethyl)-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-2-methoxyphenyl) methane sulfonamide, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of PI3K kinase mediated diseases or disorders with them. | 12-31-2015 |
20150376192 | NOVEL PYRAZOL DERIVATIVES - The invention relates to a compound of formula (I) | 12-31-2015 |
20150376193 | PROCESSES AND INTERMEDIATES FOR PREPARING A MEDICAMENT - Disclosed is a process for the preparation of the following compounds: | 12-31-2015 |
20160000738 | USE OF BUCILLAMINE IN THE TREATMENT OF GOUT - Disclosed are pharmaceutical compositions comprising, bucillamine, including bucillamine and allopurinol or colchicine, or pharmaceutically acceptable salts or solvates thereof, together with one or more pharmaceutically acceptable carriers, diluents and excipients. Methods for use of the said compositions in the treatment of gout and metabolic syndrome are also disclosed. | 01-07-2016 |
20160000789 | MTOR MODULATORS AND USES THEREOF - The present invention provides methods and compositions for selective modulation of certain protein kinases, and especially mTor complexes. The methods and compositions are particularly useful in inhibiting mTor selectively for therapeutic applications. | 01-07-2016 |
20160002245 | SUBSTITUTED PYRAZOLOPYRIMIDINYLAMINO-INDAZOLES - The present invention relates to substituted pyrazolopyrimidinylamino-indazole compounds of general formula I as described and defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients. | 01-07-2016 |
20160008366 | BTK INHIBITORS FOR THE TREATMENT OF CNS MALIGNANCIES | 01-14-2016 |
20160022685 | HETEROCYCLYLAMINES AS PI3K INHIBITORS - The present invention provides heterocyclylamine derivatives of Formula I: | 01-28-2016 |
20160031891 | INHIBITORS OF BRUTON'S TYROSINE KINASE - Disclosed herein are amido compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. 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. | 02-04-2016 |
20160032404 | BIOMARKERS FOR PREDICTING RESPONSE OF DLBCL TO TREATMENT WITH A BTK INHIBITOR - Disclosed herein, are methods, systems, compositions, arrays, and kits for using biomarkers, biomarker genes (e.g. EP300, MLL2, BCL-2, RB1, LRP1B, PIM1, TSC2, TNFRSF11A, SMAD4, PAX5, CARD11, ACTG2, LOR, GAPT, CCND2, SELL, GEN1, HDAC9, CD79B, MYD88, and ROS1) or biomarker gene expression levels for stratifying a patient having a hematological malignancy such as DLBCL for treatment, and administering a TEC inhibitor to selected patients. Also disclosed herein are methods, systems, compositions, arrays, and kits for using biomarkers, biomarker genes, or biomarker gene expression levels for monitoring a patient during treatment of a hematological malignancy such as DLBCL or FL or for optimizing a treatment regimen with a TEC inhibitor. | 02-04-2016 |
20160038494 | NOVEL COMBINATION - The invention relates to the combination of inhibitors of phosphodiesterase 1 (PDE1) and inhibitors of Neprilysin (NEP) useful for the treatment of certain cardiovascular diseases or related disorders, e.g., hypertension, congestive heart disease, and post-myocardial infarction. In another embodiment, the invention relates to the combination of inhibitors of PDE1 and inhibitors of NEP for the treatment of diseases or disorders characterized by disruption of or damage to various cGMP/PKG mediated pathways in the cardiovascular system (e.g., in cardiac tissue or in arterial smooth muscle). | 02-11-2016 |
20160038496 | NOVEL FORMULATIONS OF A BRUTON'S TYROSINE KINASE INHIBITOR - Described herein is the Bruton's tyrosine kinase (Btk) inhibitor 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one, including novel pharmaceutical formulations thereof. Also disclosed are pharmaceutical compositions that include the Btk inhibitor, as well as methods of using the Btk inhibitor, 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. | 02-11-2016 |
20160038595 | XANTHINE OXIDASE INHIBITOR FORMULATIONS - Disclosed herein are methods and compositions for involving a xanthine oxidase inhibitor that has enhanced solubility. The compositions described herein include a xanthine oxidase inhibitor combined with an organic base. The compositions can be used to treat a disease or medical condition that involves elevated uric acid levels. | 02-11-2016 |
20160039829 | ORGANIC COMPOUNDS - The invention relates to novel inhibitors of phosphodiesterase 1 (PDE1), useful for the treatment of diseases or disorders characterized by disruption of or damage to certain cGMP/PKG mediated pathways (e.g., in cardiac tissue). The invention further relates to pharmaceutical composition comprising the same and methods of treatment of cardiovascular disease and related disorders, e.g., congestive heart disease, atherosclerosis, myocardial infarction, and stroke. | 02-11-2016 |
20160089342 | METHOD OF INHIBITING XANTHINE OXIDASE ACTIVITY IN A CELL - Small molecule xanthine oxidase inhibitors are provided, as well as methods for their use in treating gout or hyperuricemia. | 03-31-2016 |
20160108035 | CYCLOALKYL ACID DERIVATIVE, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL APPLICATION THEREOF - Cycloalkyl acid derivatives, a preparation method thereof, and a pharmaceutical application thereof are described. In particular, a cycloalkyl acid derivative represented by general formula (I) and a medical salt thereof, a preparation method thereof, and an application of the cycloalkyl acid derivative and the medical salt thereof as URAT1 inhibitors, and particularly as therapeutic agents for diseases related to an abnormal uric acid level are described, wherein definitions of substituent groups in general formula (I) are the same as the definitions in the specification. | 04-21-2016 |
20160120868 | SUBSTITUTED PYRAZOLOPYRIMIDINES AS KINASES INHIBITORS - The present invention is directed to novel pyrazolopyrimidines, their derivatives, pharmaceutically acceptable salts, solvates and hydrates thereof. The compounds and compositions of the present invention have protein kinases inhibitory activities against BTK and/or EGFR T790M and are useful for the treatment of protein kinases mediated diseases and conditions. | 05-05-2016 |
20160136170 | USE OF A TETRASUBSTITUTED PYRAZOLO[4, 3-D]PYRIMIDINE COMPOUND FOR TREATING DIABETIC NEPHROPATHY - The present invention relates to methods of delaying progression to end stage renal disease (ESRD) in patients comprising administration of 1-(2-ethoxyethyl)-5-(ethyl(methyl)amino)-7-((4-methylpyridin-2-yl)amino)-N-(methylsulfonyl)-1H-pyrazolo[4,3-d]pyrimidine-3-carboxamide. The present invention also includes administration of pharmaceutical compositions for delaying progression to ESRD. | 05-19-2016 |
20160137610 | Compounds 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. | 05-19-2016 |
20160166573 | COMPOSITIONS AND METHODS FOR TREATMENT AND PREVENTION OF HYPERURICEMIA RELATED HEALTH CONSEQUENCES | 06-16-2016 |
20160168151 | PYRAZOLO PYRIMIDINE DERIVATIVES AND METHODS OF USE THEREOF | 06-16-2016 |
20160193191 | ANTAGONISTS OF CHEMOKINE RECEPTORS | 07-07-2016 |
20160193210 | ANTITUMOR DRUG FOR INTERMITTENT ADMINISTRATION OF FGFR INHIBITOR | 07-07-2016 |
20160193211 | COMBINATIONS OF A BTK INHIBITOR AND FLUOROURACIL FOR TREATING CANCERS | 07-07-2016 |
20160199376 | METHODS OF TREATING FIBROSIS | 07-14-2016 |
20160200730 | POLYFLUORINATED COMPOUNDS ACTING AS BRUTON TYROSINE KINASE INHIBITORS | 07-14-2016 |
20160250193 | POLYMORPHIC FORMS OF 2-(5-BROMO-4-(4-CYCLOPROPYLNAPHTHALEN-1-YL)-4H-1,2,4-TRIAZOL-3-YLTHIO)ACE- TIC ACID AND USES THEREOF | 09-01-2016 |
20160374993 | TREATMENT OF GOUT - 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 such compositions for the treatment of a variety of diseases and conditions. | 12-29-2016 |
20160375027 | PROTEIN KINASE INHIBITORS - The present invention relates to a novel family of inhibitors of protein kinase of formula 1 and process for their production and pharmaceutical compositions thereof. In particular, the present invention relates to inhibitors of the members of the Tec, Src and Btk protein kinase families. | 12-29-2016 |
20190142740 | Methods of Eye Treatment Using Therapeutic Compositions Containing Dipyridamole | 05-16-2019 |