Entries |
Document | Title | Date |
20080200486 | Combination Of Organic Compounds - The invention provides a pharmaceutical combination comprising:
| 08-21-2008 |
20080200487 | Salts of 4-Methyl-N-[3-(4-Methyl-Imidazol-1-Yl)-5-Trifluoromethyl-Phenyl]-3-(4-Pyridin-3-Yl-Pyrimidin-2-Ylamino)-Benzamide - Salts of 4-methyl-N-[3-(4-methyl-imidazol-1-yl)-5-trifluoromethyl-phenyl]-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-benzamide are prepared by various processes. | 08-21-2008 |
20080200488 | Combinations Comprising a Protein Kinase Inhibitor Being a Pyrimidylaminobenzamide Compound and a Hsp90 Inhibitor Such as 17-Aag - The invention provides a pharmaceutical combination comprising:
| 08-21-2008 |
20080200489 | Combination of Organic Compounds - The invention provides a pharmaceutical combination comprising:
| 08-21-2008 |
20080207657 | Use Of Minoxidil Sulfate As An Anti-Tumor Drug - The invention relates to compositions, methods and kits for the treatment of cancer. ATP-dependent potassium channel agonists, salts thereof, or chemical analogs thereof, for example, minoxidil sulfate, have been found to possess anti-neoplastic properties. Administering minoxidil sulfate may prolong the life of a cancer patient; for example, a patient with a brain tumor. | 08-28-2008 |
20080207658 | Pharmaceutical Combination of Bcr-Abl and Raf Inhibitors - The invention provides a pharmaceutical combination comprising: a) a pyrimidylaminobenzamide compound, and b) a RAF kinase inhibitor and a method for treating or preventing a proliferative disease using such a combination, wherein compound a) has the following general Formula: (I). | 08-28-2008 |
20080207659 | INHIBITORS OF PHOSPHODIESTERASE TYPE 4 - The present invention relates to inhibitors of phosphodiesterase (PDE) type 4. | 08-28-2008 |
20080207660 | PHOSPHODIESTERASE 4 INHIBITORS - Selective PDE4 inhibition is achieved by aryl and heteroaryl pyrazole compounds. The compounds exhibit improved PDE4 inhibition as compared to compounds such as rolipram and show selectivity with regard to inhibition of other classes of PDEs. | 08-28-2008 |
20080227799 | CXCR4 Antagonists Including Heteroatoms for the Treatment of Medical Disorders - The invention provides compounds, pharmaceutical compositions and methods of use of certain compounds that are antagonists of the chemokine CXCR4 receptor for the treatment of proliferative conditions mediated by CXCR4 receptors. The compounds provided interfere with the binding of SDF1 to the receptor. These compounds are particularly useful for treating or reducing the severity of hyperproliferative diseases by inhibiting metastasis. | 09-18-2008 |
20080227800 | Pyrimidylaminobenzamide Derivatives for Hypereosinophilic Syndrome - The present invention relates to the use of pyrimidylaminobenzamide derivatives for the preparation of a drug for the treatment of FIP1L1-PDGFRα-induced or TEL-PDGFRβ-induced myeloproliferative diseases, especially for the curative and/or prophylactic treatment of hypereosinophilic syndrome and hypereosinophilic syndrome with resistance to imatinib, and to a method of treating hypereosinophilic syndrome, chronic eosinophilic leukemia and hypereosinophilic syndrome with resistance to imatinib, or other diseases associated with FIP1L1-PDGFRα, TEL-PDGFRβ or similar mutations that activate PDGFR. | 09-18-2008 |
20080234302 | Novel Processes for Preparing Amorphous Rosuvastatin Calcium and a Novel Polymorphic Form of Rosuvastatin Sodium - Provided are processes for preparing amorphous rosuvastatin calcium from crystalline rosuvastatin calcium by simple precipitation processes. Also provided is a novel polymorphic form of rosuvastatin sodium, processes for preparing thereof and pharmaceutical compositions thereof. | 09-25-2008 |
20080249120 | Pharmaceutical compositions - A pharmaceutical composition in solid form containing at least a therapeutically effective amount of one or more statins in the free acid form is disclosed. | 10-09-2008 |
20080249121 | INTERMEDIATES AND A PROCESS EMPLOYING THE INTERMEDIATES FOR THE PREPARATION OF (3-TRIFLUOROMETHYLSULFONYL)-N-[4-METHYL-3-(4-PYRIDIN-3YL-PYRIMIDIN-2YLAMINO)-PHENYL]-BENZAMIDE - This invention relates to a process for the preparation of (3-trifluoromethylsulfonyl)-N-[4-methyl-3-(4-pyridin-3yl-pyrimidin-2ylamino)-phenyl]-benzamide (formula (I)) starting from 4-methyl-2-nitro-aniline (formula (II)) through intermediates (3-trifluoromethylsulfonyl)-N-[4-methyl-3-nitrophenyl]-benzamide (formula (III)), (3-trifluoromethylsulfonyl)-N-[3-amino-4-methylphenyl]-benzamide (formula (IV)) and (3-trifluoromethylsulfonyl)-N-[3-guanidino-4-methylphenyl]-benzamide (formula (V)). This invention also relates to processes for the preparation of these intermediates. The compound of formula (I), also known as AN-024, is: | 10-09-2008 |
20080255169 | Sulphonamide Derivatives - The invention relates to sulphonamide derivatives of formula (I), | 10-16-2008 |
20080255170 | Process for the Synthesis of Rosuvastatin Calcium - Present invention represents process for the preparation of HMG-CoA reductase inhibitors, in particular rosuvastatin calcium introducing L-malic acid as the source of chirality for the side chain. | 10-16-2008 |
20080255171 | Combination of Nilotinib with Farnesyl Transferase Inhibitors - The invention provides a pharmaceutical combination comprising:
| 10-16-2008 |
20080255172 | PYRIMIDINE DERIVATIVES - A compound of the following formula: | 10-16-2008 |
20080262007 | Hiv Inhibiting 5-Substituted Pyrimidines - HIV replication inhibitors of formula | 10-23-2008 |
20080262008 | CRYSTALLINE FORMS AND POLYMORPHS OF N-(3-(DIMETHYLAMINO)PROPYL)-4-(4-(3-FLUORO-4-METHOXYPHENYL) PYRIMIDIN-2-YLAMINO) BENZENESULFONAMIDE AS SUCCINATE SALTS - The present invention relates to methods for preparing and manufacturing a crystalline form or polymorph of a compound of formula I: | 10-23-2008 |
20080262009 | CRYSTALLINE POLYMORPHS OF N-(3-(DIMETHYLAMINO)PROPYL)-4-(4-(3-FLUORO-4-METHOXYPHENYL) PYRIMIDIN-2-YLAMINO) BENZENESULFONAMIDE AS ACETATE SALTS - The present invention relates to methods for preparing one or more crystalline forms and polymorphs of a compound of formula I: | 10-23-2008 |
20080262010 | CRYSTALLINE POLYMORPHS OF N-(3-(DIMETHYLAMINO)PROPYL)-4-(4-(3-FLUORO-4-METHOXYPHENYL) PYRIMIDIN-2-YLAMINO) BENZENESULFONAMIDE AS D-GLUCORONATE SALTS - The present invention relates to methods for preparing one or more crystalline polymorphs of a compound of formula I: | 10-23-2008 |
20080269268 | Substituted Phenylamino-Pyrimidines - The invention relates to substituted phenylaminopyrimidines, to a process for their preparation and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases in humans and animals, in particular cardiovascular disorders. | 10-30-2008 |
20080269269 | Crystalline Forms of 4-Methyl-N- [3-(4-Methyl-Imidazol-1-Yl)-5-Trifluoromethyl-Phenyl]-3- (4-Pyridin-3-Yl-Pyrimidin-2-Ylamino) -Benzamide - Polymorphic forms of 4-methyl-N-[3-(4-methyl-imidazol-1-yl)-5-trifluoromethyl-phenyl]-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-benzamide free base and salts thereof are prepared by various processes. | 10-30-2008 |
20080269270 | Triol form of rosuvastatin and synthesis of rosuvastatin - Provided is a rosuvastatin triol and its use as a reference standard for analysis of rosuvastatin. Also provided are methods for preparation of rosuvastatin. | 10-30-2008 |
20080275073 | CRYSTALLINE FORMS AND POLYMORPHS OF N-(3-(DIMETHYLAMINO)PROPYL)-4-(4-(3-FLUORO-4-METHOXYPHENYL) PYRIMIDIN-2-YLAMINO) BENZENESULFONAMIDE AS PHARMACEUTICALLY ACCEPTABLE SALTS - The present invention relates to one or more crystalline forms and polymorphs of compounds of formula I: | 11-06-2008 |
20080280932 | COMPOSITIONS AND METHODS FOR TREATING VASCULAR, AUTOIMMUNE, AND INFLAMMATORY DISEASES - The disclosure provides methods and compositions for the treatment of vascular, autoimmune and inflammatory diseases using a combination of an inosine monophosphate dehydrogenase (IMPDH) inhibitor and a HMG CoA reductase inhibitor. | 11-13-2008 |
20080287477 | Novel Compounds as Modulators of Ppar - Compounds as modulators of peroxisome proliferator activated receptors, pharmaceutical compositions comprising the same, and methods of treating disease using the same are disclosed. | 11-20-2008 |
20080293750 | Susceptibility Gene for Myocardial Infarction, Stroke, Paod and Methods of Treatment - Linkage of myocardial infarction (MI) and a locus on chromosome 13q12 is disclosed. In particular, the FLAP gene within this locus is shown by genetic association analysis to be a susceptibility gene for MI and ACS, as well as stroke and PAOD. Pathway targeting for treatment and diagnostic applications in identifying those who are at risk of developing MI, ACS, stroke or PAOD, in particular are described. The invention also provides for compositions comprising a leukotriene synthesis inhibitor and a stating and methods of using these compositions to reduce C-reactive protein in a human subject at risk of MI, ACS, stroke and/or PAOD. | 11-27-2008 |
20080293751 | Tetralin and indane derivatives and uses thereof - Compounds of the formula I: | 11-27-2008 |
20080300266 | 1-(Hetero)Aryl-3-Amino-Pyrrolidine Derivatives for Use as Mglur3 Antagonists - The present invention relates to compounds of the Formula (I) which are useful for treating conditions associated with mGluR3 receptors, such as depression, schizophrenia and migraine, pharmaceutical compositions thereof, and methods of using the same. | 12-04-2008 |
20080300267 | Compounds and Compositions as Protein Kinase Inhibitors - The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the CDKs, Aurora, Jak2, Rock, CAMKII, FLT3, Tie2, TrkB, FGFR3 and KDR kinases. | 12-04-2008 |
20080300268 | HETEROCYCLIC COMPOUNDS AND USES THEREOF - The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same. | 12-04-2008 |
20080306099 | COMPOSITIONS AND METHODS FOR INHIBITION OF THE JAK PATHWAY - The invention encompasses compounds having formula I-V and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, may be therapeutically useful. | 12-11-2008 |
20080306100 | PHENYLAMINOPYRIMIDINE DERIVATIVES AS INHIBITORS OF BCR-ABL KINASE - The present invention relates to novel intermediates useful for the preparation of novel phenylaminopyrimidine derivatives, novel phenylaminopyrimidine derivatives. Pharmaceutical composition containing the novel phenylaminopyrimidine derivatives and processes for their preparation. The invention particularly relates to novel Phenyl pyrimidine amine derivatives of the general formula (I). The novel compounds of the formula 1 can be used in the therapy of Chronic Myeloid Leukemia (CML). Since the IC | 12-11-2008 |
20080312263 | PHARMACEUTICAL COMPOSITIONS FOR THE PREVENTION AND TREATMENT OF ATHEROSCLEROSIS - The present invention relates to the use,
| 12-18-2008 |
20080318988 | Pyrimidylaminobenzamide Derivatives For the Treatment of Neurofibromatosis - The present invention relates to the use of pyrimidylaminobenzamide derivatives for the preparation of a drug for the treatment of non-cancerous, benign brain tumors, especially for the curative and/or prophylactic treatment of NF, and to a method of treating non-cancerous, benign brain tumors, especially for the curative and/or prophylactic treatment of NF. | 12-25-2008 |
20080318989 | Pyrimidine Kinase Inhibitors - The invention provides novel kinase inhibitors that are useful as therapeutic agents for example in the treatment malignancies where the compounds have the general formula (I) wherein ring A, X, Y, Z, R | 12-25-2008 |
20090005406 | Cancer Treatment Method - The present invention relates to a method of treating cancer in a mammal by administration of pyrimidine derivatives. In particular, the method relates to a method of treating cancer by administration of 5-[[4-[(2,3-Dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methylbenzenesulfonamide or a salt or solvate thereof. | 01-01-2009 |
20090005407 | PARTICULATE (3'-CHLOROBIPHENYL-4-YL)(1-(PYRIMIDIN-2-YL)PIPERIDIN-4-YL)METHANONE AND METHODS OF ITS USE - Particulate (3′-chlorobiphenyl-4-yl)(1-(pyrimidin-2-yl)piperidin-4-yl)methanone is disclosed. Also disclosed are pharmaceutical formulations and dosage forms comprising particulate (3′-chlorobiphenyl-4-yl)(1-(pyrimidin-2-yl)piperidin-4-yl) and methods of their use. | 01-01-2009 |
20090012107 | Antiviral Compounds and Methods of Using Thereof - Disclosed herein are compounds which exhibit antiviral activity against a plurality of viruses belonging to different families such as Bornaviridae, Filoviridae, Paramyxoviridae, Rhabdoviridae, Arenaviridae, Bunyaviridae, Orthomyxoviridae, and Poxviridae. Thus, methods of preventing, inhibiting, or reducing the viral activity of various viruses are provided as well as methods of treating viral infections. | 01-08-2009 |
20090012108 | SALT OF 4-[[4-[[4-(2-CYANOETHENYL)-2,6-DIMETHYLPHENYL]AMINO]-2-PYRIMIDINYL]AMINO]BENZONITRILE - The present invention relates to a pharmaceutical composition comprising as active ingredient the hydrochloric acid salt of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethyl-phenyl]amino]-2-pyrimidinyl]amino]benzonitrile and to processes for their preparation. | 01-08-2009 |
20090018150 | 5-Ht2b Receptor Antagonists - Compounds of formulae: (I), (II), (IIIa), (IIIb), (IVa) and (IVb): or a pharmaceutically acceptable salt thereof, for use as pharmaceuticals, in particular for the treatment of a condition alleviated by antagonism of a 5-HT | 01-15-2009 |
20090018151 | Topical Treatment of Peripheral diabetic complications - This invention relates to agents for treating, ameliorating, or preventing diabetic complications specifically diabetic neuropathy and skin ulceration by topical application of materials containing one or more arterial or venous dilation components and one or more fast sodium channel inhibitors. Particularly, the invention relates to treating or ameliorating agents that contain minoxidil and its related congeners, which have both potassium channel agonist properties and nitric oxide agonist properties as an active ingredient and which are effective against diabetic complications such as neuropathy, peripheral circulation disorders and skin ulcerations. Unique methods of delivery including delivery through impregnated socks or gloves to match the distribution of pain are also noted. | 01-15-2009 |
20090018152 | Aminophenyl Derivatives as Novel Inhibitors of Histone Deacetylase - This invention comprises the novel compounds of formula (I) | 01-15-2009 |
20090018153 | Substituted Indolyl-Alkyl-Amino-Derivatives as Inhibitors of Histone Deacetylase - This invention comprises the novel compounds of formula (I) wherein R | 01-15-2009 |
20090030023 | PYRIMIDINE COMPOUNDS AND MEDICINAL COMPOSITION THEREOF - A compound represented by the following formula (I), a salt, or a solvate thereof: | 01-29-2009 |
20090030024 | THIAZOLES AS FUNGICIDES - Use of compounds of the formula (I), | 01-29-2009 |
20090036476 | BENZIMIDAZOLE DERIVATIVES AND THEIR USE FOR MODULATING THE GABAA RECEPTOR COMPLEX - This invention relates to novel benzimidazole derivatives, pharmaceutical compositions containing these compounds, and methods of treatment therewith. | 02-05-2009 |
20090042918 | Pyridopyrimidinone Inhibitors of PIM-1 and/or PIM-3 - Compounds of formula (I), useful for inhibiting PIM-I and/or PIM-3: and pharmaceutically acceptable salts thereof, wherein Y, Z, R | 02-12-2009 |
20090042919 | METHOD FOR MODULATING GPR119 G PROTEIN-COUPLED RECEPTOR AND SELECTED COMPOUNDS - A method of modulating the activity of the GPR119 G protein-coupled receptor comprising administering to a mammalian patient in need thereof a therapeutically effective amount of at least one compound of Formula I or Formula IA and, optionally, an additional therapeutic agent. | 02-12-2009 |
20090042920 | CARBONYLAMINO-DERIVATIVES AS NOVEL INHIBITORS OF HISTONE DEACETYLASE - This invention comprises the novel compounds of formula (I) | 02-12-2009 |
20090048281 | Organic Compounds - Compounds of Formula (I); in salt or zwitterionic form wherein R | 02-19-2009 |
20090048282 | PYRIMIDINE SULFONAMIDE ANALOGS AND THEIR USE AS AGONISTS OF THE WNT-BETA-CATENIN CELLULAR MESSAGING SYSTEM - The present invention relates to pyrimidine sulfonamide analogs, methods of making pyrimidine sulfonamide analogs, compositions comprising a pyrimidine sulfonamide analog, and methods for treating canonical Wnt-β-catenin cellular messaging system-related disorders comprising administering to a subject in need thereof an effective amount of a pyrimidine sulfonamide analog. | 02-19-2009 |
20090054474 | Novel pyrimidine compound having benzyl(pyridylmethyl)amine structure and medicament comprising the same - A compound represented by the following general formula (I) or a salt thereof, or a solvate thereof: | 02-26-2009 |
20090054475 | HETEROCYCLIC RECEPTOR AGONISTS FOR THE TREATMENT OF DIABETES AND METABOLIC DISORDERS - Compounds and methods are provided for the treatment of, inter alia, Type II diabetes and other diseases associated with poor glycemic control. The compounds of the invention are orally active. | 02-26-2009 |
20090062320 | Method of Treating Disorders Mediated by the Fibroblast Growth Factor Receptor - The disclosure includes a method of treating a warm-blooded animal having a disorder mediated by the fibroblast growth factor receptor (FGFR), in particular 8p11 myelo-proliferative syndrome (EMS), pituitary tumors, retinoblastoma, synovial sarcoma, chronic obstructive pulmonary disease (COPD), seborrheic keratosis, obesity, diabetes and related disorders, autosomal dominant hypophosphatemic Rickets (ADHR), X-chromosome linked hypophosphatemic rickets (XLH), tumor-induced osteomalacia (TIO) and fibrous dysplasia of the bone (FD), as well as to a method of promoting localized neochondrogenesis, as well as a method of treating hepatocellular carcinoma, lung cancer, especially pulmonary adnocarcinoma, oral squameous cell carcinoma, or esophageal squameous cell carcinoma, or any combination of two or more such diseases. | 03-05-2009 |
20090069356 | USE OF ANILINOPYRIMIDINES IN WOOD PROTECTION - The present invention relates to the use of the anilinopyrimidines pyrimethanil, cyprodinil and mepanipyrim for the protection of wood and wood materials against wood destroying and wood discolouring fungi. | 03-12-2009 |
20090069357 | DEUTERIUM-ENRICHED ICLAPRIM - The present application describes deuterium-enriched iclaprim, pharmaceutically acceptable salt forms thereof, and methods of treating using the same. | 03-12-2009 |
20090069358 | Use of IKappaB-Kinase Inhibitors in Pain Therapy - The present invention relates to the use of IκB-kinase Inhibitors and methods for the prophylaxis and therapy for treating pain comprising administering such compounds. | 03-12-2009 |
20090069359 | Topical and transdermal treatments using urea formulation - Various medical conditions, some previously treated by injection or surgery, are effectively treated by a topical application of a composition of urea and a chemotherapeutic agent. Such agents include sclerosing agents, vasodilators, botulinum toxin and minoxidil. Conditions as diverse as spider veins, erectile dysfunction, facial wrinkles, hair loss and baldness can be effectively treated with the compositions. | 03-12-2009 |
20090069360 | Organic Compounds - The present invention relates to the discovery that certain compounds inhibit, regulate and/or modulate tyrosine and serine/threonine kinase and kinase-like proteins, such as RAF kinase, a serine/threonine kinase that functions in the MAP kinase signaling pathway, and is concerned with compositions which contain these compounds, and methods of using them to treat tyrosine and serine/threonine kinase and kinase-like dependent diseases, such as angiogenesis, cancer and cardiac hypertrophy. | 03-12-2009 |
20090076046 | Compounds modulating c-fms and/or c-kit activity and uses therefor - Compounds active on the receptor protein tyrosine kinases c-kit and/or c-fms are provided herewith. Also provided herewith are compositions useful for treatment of c-kit mediated diseases or conditions and/or c-fms-mediated diseases or conditions, and methods for the use thereof. | 03-19-2009 |
20090076047 | 2-Substituted Hydroxylaminopyrimidine, Method for the Production and the Use Thereof in the Form of Pesticides - 2-Substituted pyrimidines of the formula I, | 03-19-2009 |
20090082379 | Novel Cyclic Urea Derivatives, Preparation Thereof and Pharmaceutical Use Thereof as Kinase Inhibitors - Compounds of formula (I): | 03-26-2009 |
20090082380 | DEUTERIUM-ENRICHED ROSUVASTATIN - The present application describes deuterium-enriched rosuvastatin, pharmaceutically acceptable salt forms thereof, and methods of treating using the same. | 03-26-2009 |
20090093505 | Imazalil compositions comprising alkoxylated amines - The present invention relates to the use of alkoxylated amines to enhance the activity of fungicidal formulations comprising the fungicidal compound imazalil. It also relates to formulations comprising imazalil and alkoxylated amines. These formulations are useful to protect materials, plants, fruits or seeds against fungi. | 04-09-2009 |
20090093506 | Copper antagonist compositions - Pharmaceutical compositions having a pharmaceutically acceptable copper antagonist compound(s) or a pharmaceutically acceptable salt or prodrug thereof, including copper (II) antagonists, and a pharmaceutically acceptable 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitor or a pharmaceutically acceptable salt or prodrug thereof, articles and kits and delivery devices containing such compositions, tablets and capsules and formulations containing such compositions, and methods of use for treatment of subjects, including humans, who have or are at risk for various diseases, disorders, and conditions. | 04-09-2009 |
20090093507 | CDK INHIBITORS CONTAINING A ZINC BINDING MOIETY - The present invention relates to CDK inhibitors and their use in the treatment of cell proliferative diseases such as cancer. The compounds of the invention may further act as HDAC inhibitors. | 04-09-2009 |
20090093508 | THERAPEUTIC OR PROPHYLACTIC AGENT FOR ALLERGIC DERMATITIS - A therapeutic or prophylactic agent for allergic dermatitis is disclosed. The therapeutic or prophylactic agent comprises as an effective ingredient a glycine derivative having a specific structure or a pharmaceutically acceptable salt thereof, for example, the below-described compound [(E)-2-(2,6-dichlorobenzamido)-5-[4-(isopropyl-pyrimidin-2-ylamino)phenyl]pent-4-enoic acid]. The therapeutic or prophylactic agent for allergic dermatitis according to the present invention has high therapeutic or prophylactic effect. | 04-09-2009 |
20090099219 | ALKYNYLPYRIMIDINES AND SALTS THEREOF, PHARMACEUTICAL COMPOSITIONS COMPRISING SAME, METHODS OF PREPARING SAME AND USES OF SAME - The invention relates to alkynylpyrimidines according to the general formula (I): | 04-16-2009 |
20090099220 | ANTIMALARIAL COMPOUNDS WITH FLEXIBLE SIDE-CHAINS - The present invention relates to novel compounds that are inhibitors of wild type and mutant dihydrofolate reductase (DHFR) of | 04-16-2009 |
20090099221 | PYRIDYL-AND PYRIMIDINYL-SUBSTITUTED PYRROLE-, THIOPHENE-AND FURANE-DERIVATIVES AS KINASE INHIBITORS - The present invention provides compounds of the formula (I), or the pharmaceutically acceptable salts thereof, wherein G, W, R | 04-16-2009 |
20090105287 | Inhibitors of Dihydrofolate Reductase With Antibacterial Antiprotozoal, Antifungal and Anticancer Properties - The compositions and methods described herein discloses the design, synthesis and testing of compounds that act as inhibitors of DHFR. The basic scaffold of these inhibitors includes a 2,4-diaminopyrimidine ring with a propargyl linker to another substituted aryl, bicyclo or heteroaryl ring. These DHFR inhibitors are potent and selective for many different pathogenic organisms, including the DHFR enzyme from bacteria such as | 04-23-2009 |
20090111839 | Process for Preparing Amorphous Rosuvastatin Calcium of Impurities - A pure amorphous form of rosuvastatin calcium substantially free from alkali metal impurities is disclosed. A process of preparing a pure amorphous form of rosuvastatin calcium is disclosed, which comprises hydrolysis of C | 04-30-2009 |
20090118316 | Methods for Augmenting Bone - The present invention relates to methods of stimulating osteoblast function with a PYK2 inhibitor in subjects with osteoporosis, bone fractures, non-unions, pseudoarthroses, periodontal disease or other disorders of bone metabolism. Optionally, the method further comprises administration of a second therapeutic bone agent. The present invention also relates to methods to identify a PYK2 inhibitor effective as a therapeutic bone agent comprising administering a test agent to an osteoblast-like cell and determining if osteoblast function is stimulated. Optionally, the identifying method further comprises contacting the test agent with PYK2 and determining if PYK2 activity is inhibited. | 05-07-2009 |
20090124646 | SUBSTITUTED INDOLYL ALKYL AMINO DERIVATIVES AS NOVEL INHIBITORS OF HISTONE DEACETYLASE - This invention comprises the novel compounds of formula (I) | 05-14-2009 |
20090124647 | Indole Derivatives as Antitumoral Compounds - Antitumoural compounds of general formula (I); wherein Ar is an heterocyclic group of formula (a) and R | 05-14-2009 |
20090131463 | NOVEL COMPOUNDS - The invention provides compounds of formula | 05-21-2009 |
20090137617 | USE OF HAPTOGLOBIN GENOTYPING IN DIAGNOSIS AND TREATMENT OF CARDIOVASCULAR DISEASE - This invention is directed to methods and compositions for the treatment of cardiovascular disorders. Specifically, the invention is directed to compositions comprising vitamin E, statins and/or glutathione peroxidase mimetics; methods of treating diabetic patients expressing the Hp-2-2 haptoglobin genotype; a method of inhibiting or suppressing a cardiovascular disorder in a diabetic subject, treating cardiovascular disease in subjects exhibiting the Haptoglobin Hp-2-2 genotype; and methods of treating cardiovascular disease in subjects exhibiting the Haptoglobin Hp-2-2 genotype. | 05-28-2009 |
20090149487 | 4,5-DIPHENYL-PYRIMIDINYLAMINO SUBSTITUTED CARBOXYLIC ACIDS, METHOD FOR THE PRODUCTION AND USE THEREOF AS MEDICAMENTS - This invention relates to a compound of formula I, | 06-11-2009 |
20090156621 | HCV INHIBITORS - The present invention relates to compounds that are useful in the treatment of viruses belonging to Flaviviridae, including flaviviruses, pestiviruses, and hepaciviruses. The invention includes compounds useful for the treatment or prophylaxis of dengue fever, yellow fever, West Nile virus, and HCV. | 06-18-2009 |
20090156622 | 2,4-PYRIMIDINEDIAMINE COMPOUNDS AND THEIR USES - The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades. | 06-18-2009 |
20090156623 | N-ARYL PIPERIDINE SUBSTITUTED BIPHENYLCARBOXAMIDES - N-aryl piperidine substituted biphenylcarboxamides compounds of formula (I) | 06-18-2009 |
20090170884 | FUNGICIDAL ACTIVE SUBSTANCE COMBINATION - Active compound combinations comprising an oxime ether derivative of the formula (I) | 07-02-2009 |
20090170885 | NAPHTHYRIDINE DERIVATIVES AS POTASSIUM CHANNEL MODULATORS - This invention provided compounds of formula I | 07-02-2009 |
20090176813 | AQUEOUS SUSPENSIONS OF TMC278 - This invention concerns pharmaceutical compositions for administration via intramuscular or subcutaneous injection, comprising micro- or nanoparticles of the NNRTI compound TMC278, suspended in an aqueous pharmaceutically acceptable carrier, and the use of such pharmaceutical compositions in the treatment and prophylaxis of HIV infection. | 07-09-2009 |
20090181993 | HIV INHIBITING 5-HETEROCYCLYL PYRIMIDINES - HIV replication inhibitors of formula (I), N-oxides, pharmaceutically acceptable addition salts, quaternary amines or stereoisomeric forms thereof, wherein -a | 07-16-2009 |
20090181994 | TRIAZOLE DERIVATIVES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE-1 - Triazole derivatives of structural formula I are selective inhibitors of the 11β-hydroxysteroid dehydrogenase-1. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Metabolic Syndrome, and other symptoms associated with NIDDM. | 07-16-2009 |
20090181995 | 2-ANILINO-4-AMINOALKYLENEAMINOPYRIMIDINES - The present invention relates to 2-arylamino-4-(aminoalkylene)aminopyrimidines inhibitors which are inhibitors and therefore inhibit Protein Kinase C-alpha (PKC-α). The PKC-α inhibitors of the present invention are important for improving myocardial intracellular calcium cycling, resulting in improved myocardial contraction and relaxation performance and thereby slowing the progression of heart failure. The present invention further relates to compositions comprising said 2-arylamino-4-(aminoalkylene)amino-pyrimidines and to methods for controlling, abating, or otherwise slowing the progression of heart failure. | 07-16-2009 |
20090192180 | Alpha-7 Nicotinic Receptor Agonists and Statins In Combination - Combinations of α7-nAChR agonists and statins, pharmaceutical compositions containing the same and methods of using the same useful for treatment or prophylaxis of neurological degenerative diseases. | 07-30-2009 |
20090192181 | PYRIMIDINYL AMIDE COMPOUNDS WHICH INHIBIT LEUKOCYTE ADHESION MEDIATED BY VLA-4 - Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a human or animal subject such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis. | 07-30-2009 |
20090203720 | Methods for inhibiting cell growth - Cell growth is inhibited and/or cell death is induced in a cell by administering an RXR agonist and an inhibitor of casein kinase 1α. A cell or a tissue can be screened for enhanced susceptibility to cell death or interference with cell growth. Conditions characterized by uncontrolled cell growth or proliferation, such as a cancer, can be treated with inhibitors of casein kinase 1α. | 08-13-2009 |
20090209566 | Spirocyclic Compounds - The present invention relates to a novel class of substituted spirocyclic compounds, represented by the following structural Formula: I Wherein A, B and D are independently selected from CR | 08-20-2009 |
20090209567 | Rosuvastatin and salts thereof free of rosuvastatin alkylether and a process for the preparation thereof - The present invention provides rosuvastatin and intermediates thereof having a low level of alkylether impurity and processes for the preparation thereof. | 08-20-2009 |
20090215804 | FUMARATE OF 4- [[4- [[4- (2-CYANOETHENYL) -2,6-DIMETHYLPHENYL)AMINO] -2-PYRIMIDINYL]AMINO]BENZONITRILE - The present invention relates to the fumarate salt of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]benzonitrile, pharmaceutical compositions comprising as active ingredient said salt and to processes for their preparation. | 08-27-2009 |
20090215805 | 4-Heteroaryl Pyrimidine Derivatives and use thereof as Protein Kinase Inhibitors - The present invention relates to compounds of formula (I) or formula (II), or pharmaceutically acceptable salts thereof. Further aspects relate to pharmaceutical compositions comprising compounds according to the invention, and the use of said compounds in the preparation of a medicament for treating a variety of disorders, including proliferative disorders, viral disorders, stroke, etc. | 08-27-2009 |
20090215806 | Rosuvastatin calcium with a low salt content - Provided is rosuvastatin calcium with a low salt by product content and processes for preparing such rosuvastatin calcium. | 08-27-2009 |
20090221619 | NOVEL MATERIALS AND METHODS FOR THE PRODUCTION THEREOF - The present invention relates to, inter alia, methods for the treatment of wallboards with fungicides and the treated wallboards. In particular, the invention relates to the treatment of wallboards with synergistic combinations of an anilinopyrimidine fungicide and other fungicides. The invention also provides the treatment of building materials with synergistic mixtures containing an anilinopyrimidine fungicide. More specifically the anilinopyrimidine fungicide is cyprodinil. | 09-03-2009 |
20090221620 | GENTIC POLYMORPHISMS ASSOCIATED WITH STROKE, METHODS OF DETECTION AND USES THEREOF - The present invention provides compositions and methods based on genetic polymorphisms that are associated with vascular diseases such as stroke. In particular, the present invention relates to genetic polymorphisms that have utility for such uses as predicting disease risk or predicting an individual's response to a treatment such as statins, including groups of polymorphisms that may be used as a signature marker set for such uses, as well as nucleic acid molecules containing the polymorphisms, variant proteins encoded by such nucleic acid molecules, reagents for detecting the polymorphic nucleic acid molecules and proteins, and methods of using the nucleic acid and proteins as well as methods of using reagents for their detection. | 09-03-2009 |
20090253722 | AQUEOUS PHARMACEUTICAL FORMULATION - The invention concerns a stable aqueous pharmaceutical composition comprising 5-[(2RS)-2-cyclopropyl-7,8-dimethoxy-2H-1-benzopyran-5-ylmethyl]-pyrimidine-2,4-diamine in form of the water soluble methanesulfonic acid salt, a physiological sodium chloride solution, ethanol and Povidone 12 PF, the liquid having a pH of over and above 4.8, but not higher than 5.2, and wherein the oxygen amount is controlled to be 0.8 ppm or less; which can be sterilized by filtration and/or by heated treatment, stored for longer time periods and which can be use for bolus injection or diluted for i.v. infusion. | 10-08-2009 |
20090253723 | PROTEIN KINASE INHIBITORS - Compounds that inhibit protein kinases, compositions containing the compounds and methods of treating diseases using the compounds are disclosed. | 10-08-2009 |
20090253724 | THERAPEUTIC OR PROPHYLACTIC AGENT FOR LEUKEMIA - A therapeutic or prophylactic agent for leukemia is disclosed. The therapeutic or prophylactic agent comprises as an effective ingredient a glycine derivative having a specific structure or a pharmaceutically acceptable salt thereof, for example, the below-described compound [(E)-2-(2,6-dichlorobenzamido)-5-[4-(isopropyl-pyrimidin-2-ylamino)phenyl]pent-4-enoic acid]. The therapeutic or prophylactic agent for leukemia according to the present invention shows the excellent absorbability and in vivo stability when orally administered, and exhibits prominent therapeutic or prophylactic effects. | 10-08-2009 |
20090258888 | Pyrimidine Derivatives - This invention relates to novel compounds and processes for their preparation, methods of treating diseases, particularly cancer, comprising administering said compounds, and methods of making pharmaceutical compositions for the treatment or prevention of disorders, particularly cancer. | 10-15-2009 |
20090264452 | 2-(Phenylamino)-Pyrimidin-5-Amides As Cannabinoid 2 Receptors Modulators for the Treatment of Immune or Inflammatory Disorders - The present invention relates to novel pyrimidine derivatives such as compounds of the formula (I): | 10-22-2009 |
20090270433 | 2,3-DIHYDRO-IMINOISOINDOLE DERIVATIVES - A compound represented by the following general formula (1), or a salt thereof has serine protease inhibiting activity, and particularly excellent inhibiting activity against clotting factor VIIa. This compound or a salt thereof is useful as therapeutic and/or prophylactic agents for diseases associated with thrombus formation. | 10-29-2009 |
20090270434 | AZACYCLOALKANE DERIVATIVES AS INHIBITORS OF STEAROYL-COENZYME A DELTA-9 DESATURASE - Azacycloalkane derivatives of structural formula I are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis. | 10-29-2009 |
20090286819 | Process for Preparing the Calcium Salt of Rosuvastatin - An improved process for manufacture of (E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl](3R,5S)-3,5-dihydroxyhept-6-enoic acid calcium salt, which is useful for the production of a pharmaceutical useful in the treatment of, inter alia, hypercholesterolemia, hyperlipoproteinemia and atherosclerosis, is described. | 11-19-2009 |
20090286820 | (R)-PHENYL(HETEROCYCLE)METHANOL-BASED COMPOUNDS, COMPOSITIONS COMPRISING THEM AND METHODS OF THEIR USE - Multicyclic compounds, pharmaceutical compositions comprising them, and methods of their use are described. Compounds described include those of formula I: | 11-19-2009 |
20090286821 | INHIBITORS OF TYROSINE KINASES - The invention relates to compounds of formula | 11-19-2009 |
20090298860 | ANTIFUNGAL WALLBOARDS AND BUILDING MATERIALS AND METHODS FOR THE PRODUCTION THEREOF - The present invention relates to, inter alia, methods for the treatment of wallboards with fungicides and the treated wallboards. In particular, the invention relates to the treatment of wallboards with a fungicidally effective amount of difenoconazole. The invention also provides for the treatment of wallboards with synergistic combinations of difenoconazole and other fungicides. The invention also provides the treatment of building materials with difenoconazole and synergistic mixtures containing difenoconazole. | 12-03-2009 |
20090306115 | Phenyl ethyne compounds - In accordance with the present invention, there is provided a novel class of heterocyclic compounds. Compounds of the invention contain a substituted or unsubstituted six membered heterocyclic ring that includes at least two nitrogen atoms. The ring additionally includes four carbon atoms. The heterocyclic ring has at least one substituent located at a ring position adjacent to a ring nitrogen atom. This mandatory substituent of the ring includes a moiety (B), linked to the heterocyclic ring via a carbon-carbon triple bond. The mandatory substituent is positioned adjacent to the ring nitrogen atom. Invention compounds are capable of a wide variety of uses. For example heterocyclic compounds can act to modulate physiological processes by functioning as agonists and antagonists of receptors in the nervous system. Invention compounds may also act as insecticides, and as fungicides. Pharmaceutical compositions containing invention compounds also have wide utility. | 12-10-2009 |
20090306116 | PYRIMIDINE DERIVATIVES FOR THE INHIBITION OF IGF-IR TYROSINE KINASE ACTIVITY - A compound of formula (I) wherein the substituents are as defined in the text for use in inhibiting insulin-like growth factor 1 receptor activity in a warm blooded animal such as man. | 12-10-2009 |
20090306117 | ROSUVASTATIN ZINC SALT - The present invention is related to rosuvastatin zinc salt of the Formula (I), process for preparation thereof and medicinal products containing said salt. Rosuvastatin zinc salt according to the present invention is prepared by reacting rosuvastatin with a zinc alcoholate, zinc enolate or an inorganic or organic zinc salt and isolating the thus obtained rosuvastatin zinc salt (2:1). | 12-10-2009 |
20090312353 | Methods and compositions for treating liquid tumors - The application relates to a method of using compositions having anti-alpha-4 integrin and/or anti-alpha-9 integrin activity to inhibit liquid tumor growth, malignancies thereof and/or development of metastases thereof that involve expression of an alpha-4 integrin and/or alpha-9 integrin. Pharmaceutical compositions and combination therapies (for example, with chemotherapies) for the inhibition of liquid tumor growth, malignancies thereof and/or development of metastases thereof are also provided. | 12-17-2009 |
20090318484 | Inhibitors of JNK - The invention relates to prodrugs of JNK inhibitors and corresponding methods, formulations, and compositions for inhibiting JNK and treating JNK-mediated disorders. The application discloses prodrugs of JNK inhibitors, as described below in formula I: | 12-24-2009 |
20090325989 | INDAZOLYL DERIVATIVES USEFUL AS POTASSIUM CHANNEL MODULATING AGENTS - This invention relates to novel indazolyl derivatives useful as potassium channel modulating agents, and their use in the preparation of pharmaceutical compositions. | 12-31-2009 |
20100004274 | Stable pharmaceutical compositions comprising a pyrimidine-sulfamide - Stable pharmaceutical compositions include the compound of the below formula, or pharmaceutically acceptable salts, solvates, hydrates or morphological forms thereof: | 01-07-2010 |
20100010025 | Pyrimidine Derivatives - Disclosed are pyrimidine derivatives having interesting pharmacological properties. | 01-14-2010 |
20100010026 | STATIN AND OMEGA-3 FATTY ACIDS FOR REDUCTION OF APO-B LEVELS - Methods of utilizing a combined administration or a unit dosage of a combination of an HMG-CoA inhibitor and omega-3 fatty acids for the reduction of apolipoprotein-B levels. The methods are especially useful in the treatment of patients with hypertriglyceridemia or hypercholesterolemia or mixed dyslipidemia, coronary heart disease (CHD), vascular disease, atherosclerotic disease and related conditions, and for the prevention or reduction of cardiovascular, cardiac, and vascular events. | 01-14-2010 |
20100016344 | AMINO HETEROCYCLIC LINKED PYRIMIDINE DERIVATIVES - Macrocyclic benzofused pyrimidine compounds, compositions comprising such compounds, methods for making the compounds, and methods of treating and preventing the progression of diseases, conditions and disorders using such compounds and compositions are described herein. | 01-21-2010 |
20100016345 | PYRIMIDINYL SULFONAMIDE COMPOUNDS WHICH INHIBIT LEUKOCYTE ADHESION MEDIATED BY VLA-4 - Disclosed are compounds, which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a human or animal subject such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, Crohn's disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis. | 01-21-2010 |
20100022569 | INHIBITORS OF TYROSINE KINASES - The present invention relates to the use of pyrimidylaminobenzamide compounds for the preparation of a drug for the treatment of diseases that respond to modulation of Ephrin receptor kinase, especially EphB4, activity, especially for the curative and/or prophylactic treatment of proliferative diseases, and to a method of treating diseases that respond to modulation of kinase activity, especially Ephrin receptor kinase activity. | 01-28-2010 |
20100035906 | Dipyridyl-dihydropyrazolones and their use - The present application relates to novel dipyridyl-dihydropyrazolones, processes for their preparation, their use for treatment and/or prophylaxis of diseases and their use for the preparation of medicaments for treatment and/or prophylaxis of diseases, in particular cardiovascular and hematological diseases and kidney diseases, and for promoting wound healing. | 02-11-2010 |
20100035907 | NEW 2,4-DIANILINOPYRIMIDINES, PREPARATION THEREOF AS DRUGS, PHARMACEUTICAL COMPOSITIONS AND USE THEREOF ESSENTIALLY AS IKK INHIBITORS - The disclosure relates to a compound of formula (I): | 02-11-2010 |
20100041687 | HYDROBROMIDE SALT OF AN ANTI-HIV COMPOUND - Solid dispersions and dosage forms comprising the hydrobromide salt of a diarylpyrimidine derivative, useful as an anti-HIV agent. | 02-18-2010 |
20100041688 | REVAPRAZAN-CONTAINING SOLID DISPERSION AND PROCESS FOR THE PREPARATION THEREOF - The present invention provides a solid dispersion in which revaprazan particles are surface-modified with a water-soluble polymer, a water-soluble saccharide, a surfactant, or a mixture thereof and a process for preparing the same. The present invention also provides a pharmaceutical composition containing the solid dispersion and a process for preparing the pharmaceutical composition. | 02-18-2010 |
20100048595 | USE OF ARCHAEA TO MODULATE THE NUTRIENT HARVESTING FUNCTIONS OF THE GASTROINTESTINAL MICROBIOTA - The invention generally relates to the use of archaea to modulate nutrient harvesting in a subject. In particular, the invention provides methods that use archaea to modulate the nutrient harvesting functions of the microbiota in the subject's gastrointestinal tract. | 02-25-2010 |
20100048596 | Indole Derivatives as Antitumoral Compounds - Antitumoural compounds of general formula (I); wherein Ar is an heterocyclic group of formula (a) and R | 02-25-2010 |
20100048597 | Organic Compounds and Their Uses - The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of diseases. | 02-25-2010 |
20100048598 | TOPICAL COMPOSITIONS COMPRISING 5-ALPHA REDUCTASE INHIBITORS - The present invention relates to topical compositions comprising 5α-reductase inhibitors. The present invention also includes processes for preparation of such topical compositions and methods of using them. | 02-25-2010 |
20100056552 | COMBINATION FOR USE IN THE TREATMENT OF INFLAMMATORY DISORDERS - There is provided combination products comprising (a) suplatast, or a pharmaceutically-acceptable salt or solvate thereof; and (b) a statin, or a pharmaceutically-acceptable salt or solvate thereof. Such combination products find particular utility in the treatment of atherosclerosis and related conditions. | 03-04-2010 |
20100063081 | CPCR Agonists - Compounds of formula (I): or pharmaceutically acceptable salts thereof, are GPCR agonists and are useful as for the treatment of obesity and diabetes. | 03-11-2010 |
20100069417 | NOVEL PHENYL(4-PHENYLPYRIMIDIN-2-YL)AMINE DERIVATIVES, THEIR PREPARATION, AS MEDICAMENTS, PHARMACEUTICAL COMPOSITIONS AND IN PARTICULAR AS IKK INHIBITORS - The disclosure relates to a compound of formula (I): | 03-18-2010 |
20100069418 | 3-HETEROARYL (AMINO OR AMIDO)-1-(BIPHENYL OR PHENYLTHIAZOLYL) CARBONYLPIPERIDINE DERIVATIVES AS OREXIN RECEPTOR INHIBITORS - The invention relates to piperidine compounds of formula (I) wherein X-R | 03-18-2010 |
20100076001 | IMIDAZOLIDINONYL AMINOPYRIMIDINE COMPOUNDS FOR THE TREATMENT OF CANCER - The present invention provides novel imidazolidinonyl aminopyrimidine compounds believed to have clinical use for treatment of cancer through inhibiting Plk1. wherein: R | 03-25-2010 |
20100076002 | Method of Treating Atherosclerosis, Dyslipidemias and Related Conditions and Pharmaceutical Compositions - A method of treating atherosclerosis is disclosed wherein nicotinic acid or another nicotinic acid receptor agonist is administered to the patient in combination with a DP receptor antagonist. The DP receptor antagonist is administered to reduce, prevent or eliminate flushing that may otherwise occur. | 03-25-2010 |
20100081679 | DIAMINOPYRIMIDINES AS FUNGICIDES - Use of diaminopyrimidines of the formula (I) | 04-01-2010 |
20100087462 | METHODS FOR PREDICTING AND DETECTING INTOLERANCE TO AN HYPOLIPIDEMIC AGENT - The invention describes methods and tools for the identification of drug intolerance into subjects receiving an hypolipidemic agent. The invention further describes methods and tools for the prediction of drug intolerance in subjects in need of hypolipidemic agents. Some aspects of the invention are based on the assessment of the subject plasma glycerol concentrations. Some aspects of the invention are based on the assessment of the subject HDL-triglycerides concentration. Some other aspects are based on the identification of hepatic lipase gene variants in a subject genome. | 04-08-2010 |
20100087463 | PHARMACEUTICAL COMPOSITIONS COMPRISING NILOTINIB OR ITS SALT - A pharmaceutical composition, especially capsules. comprising granules containing nilotinib or a salt thereof with at least one pharmaceutically acceptable excipient. The granules may be produced by a wet granulation process. | 04-08-2010 |
20100087464 | PROTEIN KINASE INHIBITORS AND METHODS FOR USING THEREOF - The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, and methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of TrkA, TrkB, TrkC, Abl, Bcr-Abl, cSrc, TPR-Met, Tie2, MET, FGFR3, Aurora, Axl, Bmx, BTK, c-kit, CHK2, Flt3, MST2, p70S6K, PDGFR, PKB, PKCα, Raf, ROCK-II, Rsk1, and SGK kinases, or a combination thereof. | 04-08-2010 |
20100087465 | HETEROCYCLIC RECEPTOR AGONISTS FOR THE TREATMENT OF DIABETES AND METABOLIC DISORDERS - Compounds and methods are provided for the treatment of, inter alia, Type II diabetes and other diseases associated with poor glycemic control. The compounds of the invention are orally active. | 04-08-2010 |
20100087466 | NOVEL SMALL MOLECULE DNAK INHIBITORS - Methods of inhibiting HSP70 proteins, agents causing the inhibition of HSP70 proteins, and the effects of such inhibition on cell proliferation. Anti-microbial agents comprising small molecules, or pharmaceutical salts thereof, disclosed herein and further methods of use thereof are also disclosed. The disclosed small molecules, or pharmaceutical salts thereof, are effective in inhibiting microbial chaperone activity in microbes, such as homologs of HSP70. The disclosed small molecules, or pharmaceutical salts thereof, are also effective for the therapeutic treatment of cancer. | 04-08-2010 |
20100087467 | Compositions Useful As Inhibitors of Protein Kinases - The present invention provides compounds of formula I: | 04-08-2010 |
20100093776 | Organic Compounds and Their Uses - The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of diseases. | 04-15-2010 |
20100099693 | NEW COMBINATION FOR USE IN THE TREATMENT OF INFLAMMATORY DISORDERS - There is provided combination products comprising (a) ramatroban, or a pharmaceutically-acceptable salt or solvate thereof and (b) a statin, or a pharmaceutically-acceptable salt or solvate thereof. Such combination products find particular utility in the treatment of atherosclerosis and related conditions. | 04-22-2010 |
20100099694 | 2-ANILINO-4-HETEROARYL PYRIMIDINE DERIVATIVES, AND PREPARATION THEREOF AS MEDICAMENTS, PHARMACEUTICAL COMPOSITIONS, AND IN PARTICULAR IKK INHIBITORS - The disclosure relates to a compound of formula (I): | 04-22-2010 |
20100105711 | Organic Compounds - The present invention relates to a compound of formula (I) | 04-29-2010 |
20100105712 | CHEMICAL COMPOUNDS - Pyrimidine derivatives, which are useful as VEGFR2 inhibitors are described herein. The described invention also includes methods of making such pyrimidine derivatives as well as methods of using the same in the treatment of hyperproliferative diseases. | 04-29-2010 |
20100113492 | Substituted Aminopyrimidines as Cholecystokinin-1 Receptor Modulators - Certain novel substituted aminopyrimidines are ligands of the human cholecystokinin receptor and, in particular, are selective ligands of the human cholecystokinin-1 receptor (CCK-1R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of CCK-1R, such as obesity, and diabetes. | 05-06-2010 |
20100120807 | COMPOUNDS AND COMPOSITIONS AS MODULATORS OF GPR119 ACTIVITY - The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of GPR119. | 05-13-2010 |
20100130522 | COMPOUNDS FOR INFLAMMATION AND IMMUNE-RELATED USES - The invention relates to certain compounds according to Formula (I): | 05-27-2010 |
20100130523 | MONO-HYDROCHLORIC SALTS OF AN INHIBITOR OF HISTONE DEACETYLASE - This invention provides novel crystalline forms of mono-HCl salts and a mono-HCl salt hydrate of JNJ-26481585, an inhibitor of histone deacetylases. The invention also relates to processes for production of these forms, to intermediates used in these processes, to pharmaceutical compositions comprising these forms, and to the use of these forms in medical treatment for instance as a medicine to inhibit proliferative conditions, such as cancer and leukemia. | 05-27-2010 |
20100144772 | 2,2,2-TRI-SUBSTITUTED ACETAMIDE DERIVATIVES AS GLUCOKINASE ACTIVATORS, THEIR PROCESS AND PHARMACEUTICAL APPLICATION - Compounds of the present disclosure are 2,2,2-tri-substituted acetamide derivatives of formula (I), its polymorphs, stereoisomers, prodrugs, solvates, pharmaceutically acceptable salts and formulations thereof, useful as Glucokinase activator. Processes of their preparation are also described in the disclosure. The disclosure also describes method to characterize partial glucokinase activators. | 06-10-2010 |
20100152218 | COMPOSITIONS AND METHODS FOR INHIBITION OF THE JAK PATHWAY - The invention encompasses compounds having formula I and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, are therapeutically useful. | 06-17-2010 |
20100152219 | PYRAZOLE DERIVATIVES AS INHIBITORS OF RECEPTOR TYROSINE KINASES - Compounds of formula (I): and their use in the inhibition of Trk activity are described. | 06-17-2010 |
20100160360 | JNK MODULATORS - Compounds of formula I modulate JNK: | 06-24-2010 |
20100160361 | TREATMENT OF MAJOR ADVERSE CARDIAC EVENTS AND ACUTE CORONARY SYNDROME USING SECRETORY PHOSPHOLIPASE A2 (SPLA2) INHIBITOR OR SPLA2 INHIBITOR COMBINATION THERAPIES - Administration of sPLA | 06-24-2010 |
20100168144 | INHIBITORS OF PROTEIN KINASES - The present invention relates to inhibitors of cyclin-dependent kinases and therapeutic applications thereof. Furthermore, the invention relates to methods of preventing and/or treating any type of pain, inflammatory disorders, immunological diseases, proliferative diseases, infectious diseases, cardiovascular diseases and neurodegenerative diseases comprising the administration of an effective amount of at least one inhibitor of cyclin-dependent kinases. formula (I). | 07-01-2010 |
20100173923 | 4 (PYRROLOPYRIDINYL)PYRIMIDINYL-2-AMINE DERIVATIVES - Compounds of the formula I in which R | 07-08-2010 |
20100173924 | NOVEL HETEROCYCLE COMPOUNDS AND USES THEREOF - The invention relates to chemical compounds, or pharmaceutically acceptable salts thereof of the formula (I): which penetrate the blood-brain barrier, inhibit the formation and accumulation of beta-amyloid, and are useful in the treatment of neurodegenerative diseases, particularly Alzheimer's disease. Further, the compounds of the present invention inhibit certain kinases, thereby being useful for the treatment of cancers of the central nervous system. | 07-08-2010 |
20100179178 | PYRIMIDINE DERIVATIVES AS POSH AND POSH-AP INHIBITORS - Pyrimidine deriviatives are ubiquination inhibitors that inhibit the ubiquitin ligase activity, particularly of POSH polypeptides, are useful for the treatment of viral infections and neurological disorders. | 07-15-2010 |
20100179179 | INHIBITORS OF THE MUTANT FORM OF KIT - The present invention relates to the treatment of KIT dependent diseases that are characterized by a mutant form of KIT whereby the mutant KIT is identified and an appropriate inhibitor of the mutant KIT is administered. | 07-15-2010 |
20100184789 | INHIBITORS OF PROTEIN KINASES - The present invention relates to inhibitors of cyclin-dependent kinases and therapeutic applications thereof. Furthermore, the invention relates to methods of preventing and/or treating any type of pain, inflammatory disorders, immunological diseases, proliferative diseases, infectious diseases, cardiovascular diseases and neurodegenerative diseases comprising the administration of an effective amount of at least one inhibitor of cyclin-dependent kinases. | 07-22-2010 |
20100184790 | PYRROLO[2,3-B]PYRIDINE COMPOUNDS, AZAINDOLE COMPOUNDS USED FOR SYNTHESIZING SAID PYRROLO[2,3-B]PYRIDINE COMPOUNDS, METHODS FOR THE PRODUCTION THEREOF, AND USES THEREOF - The invention relates to pyrrolo[2,3-b]pyridine compounds and azaindole compounds used for the synthesis thereof. The invention also relates to methods for the production thereof and the uses thereof. Said novel pyrrolo[2,3-b]pyridine compounds according to the invention have great antiproliferative, apoptotic, and neuroprotective activities. The invention particularly applies to the pharmaceutical field. | 07-22-2010 |
20100184791 | COMPOUNDS AND COMPOSITIONS AS C-KIT AND PDGFR KINASE INHIBITORS - The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of c-kit, PDGFRα and PDGFRβ kinases. | 07-22-2010 |
20100184792 | Co-Crystals of Pyrimethanil and Dithianon - The present invention relates to co-crystals of pyrimethanil and dithianon, which, in a X-ray powder diffractogram at 25° C. show at least three of the following reflexes:
| 07-22-2010 |
20100190811 | PYRIMIDINE DERIVATIVES AND COMPOSITIONS AS C-KIT AND PDGFR KINASE INHIBITORS - The invention provides a novel class of pyrimidine derivatives, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of c-kit, PDGFRα and PDGFRβ kinases. | 07-29-2010 |
20100190812 | NILOTINIB HCL CRYSTALLINE FORMS - Crystalline forms of Nilotinib HCl are described. | 07-29-2010 |
20100204254 | Use of statins in the prevention and treatment of radiation injury and other disorders associated with reduced endothelial thrombomodulin - The present invention discloses statins (3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitors) consistently and significantly increased endothelial cell thrombomodulin protein and functional activity. Statins also abrogated the downregulation of thrombomodulin that occurs in response to radiation injury. These results indicate that preserving or restoring endothelial thrombomodulin expression and function by statins may be useful in a variety of disorders associated with widespread endothelial dysfunction such as sepsis, adult respiratory distress syndrome, and normal tissue radiation injury. | 08-12-2010 |
20100204255 | BICYCLIC DERIVATIVES AS MODULATORS OF ION CHANNELS - The present invention relates to bicyclic compounds useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders. | 08-12-2010 |
20100210673 | PYRIMIDYLAMINOBENZAMIDE DERIVATIVES FOR SYSTEMIC MASTOCYTOSIS - The present invention relates to the use of pyrimidylaminobenzamide derivatives for the preparation of a drug for the treatment of systemic mastocytosis. | 08-19-2010 |
20100216827 | ARYL GPR120 RECEPTOR AGONISTS AND USES THEREOF - Aryl GPR120 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control. | 08-26-2010 |
20100216828 | METHODS AND COMPOSITIONS FOR TREATING CANCERS - This invention provides a combination of antagonists of the hedgehog signaling pathway with a BCR-ABL inhibitor. The combination of the present invention may be used for treating cancers known to be associated with protein tyrosine kinases such as, for example, Src, BCR-ABL and c-kit. | 08-26-2010 |
20100222373 | Crystalline Form of Bis [(E)-7-[4-(4-fluoro-phenyl)-6-isopropyl-2-[methyl(methyl-sulfonyl)amino] pyrimidin-5-yl] (3R,5S)-3,5-dihydroxyhept-6-enoic acid] Calcium Salt - Two polymorphic forms of bis[(E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl](3R,5S)-3,5-dihydroxyhept-6-enoic acid] calcium salt, processes for making them and their use as HMG Co-A reductase inhibitors are described. | 09-02-2010 |
20100234406 | COMPOUNDS AND COMPOSITIONS AS C-KIT AND PDGFR KINASE INHIBITORS - The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of c-kit, PDGFR and PDGFR kinases. | 09-16-2010 |
20100234407 | PREVENTIVES/REMEDIES FOR MYELOMA TUMOR AND METHOD FOR DIAGNOSING THE SAME - The present invention provides a preventive or therapeutic drug for a myeloma tumor and osteoclastic bone loss associating therewith, the drug containing as an active ingredient an osteopontin-production regulator or inhibitor; a screening method for a preventive or therapeutic drug for a myeloma tumor, characterized by determining osteopontin production regulatory or inhibitory effect; as well as a diagnostic kit for a myeloma tumor, characterized by including a reagent for measuring blood osteopontin level, and a diagnostic method. | 09-16-2010 |
20100234408 | PYRIMIDYLAMINOBENZAMIDE DERIVATIVES FOR THE TREATMENT OF NEUROFIBROMATOSIS - The present invention relates to the use of pyrimidylaminobenzamide derivatives for the preparation of a drug for the treatment of non-cancerous, benign brain tumors, especially for the curative and/or prophylactic treatment of NF, and to a method of treating non-cancerous, benign brain tumors, especially for the curative and/or prophylactic treatment of NF. | 09-16-2010 |
20100240686 | CHEMICAL COMPOUNDS - Compounds of formula (I): | 09-23-2010 |
20100240687 | METHOD FOR CHECKING AND CONTROLLING THE MAMMALIAN LACTIC ACID FERMENTATION PROCESS/AEROBIC GLUCOSE FERMENTATION METABOLIC PATHWAY IN MAMMALIAN ORGANISM - The method for qualitative and quantitative detecting of the extend of use and the correct process flow of the mammalian aerobic glucose fermentation metabolic pathway (mam-aGF) in a mammalian individual is characterized in that the enzyme TKTL1 is used as indicator and target molecule and the structural and/or functional parameter of said TKTL1 in a biological sample of said individual (patient) are taken as indication for the qualitative and quantitative run of the mam-aGF in the cells and/or tissue of said individual (patient). In combination with the use of inhibitors and activators of the mam-aGF the method is further suitable for checking and controlling the mam-aGF in an individual (patient). | 09-23-2010 |
20100249164 | MODULATION OF SLEEP WITH NR2B RECEPTOR ANTAGONISTS - An NR2B receptor antagonist is useful, alone or in combination with other agents, for promoting wakefulness, treating narcolepsy, excessive daytime sleepiness, enhancing cognition, treating sleepiness associated with Alzheimer's disease, Parkinson's disease, fibromyalgia, chronic pain, sleep disorders, autism and attention deficit hyperactivity disorder. | 09-30-2010 |
20100261743 | NOVEL SEH INHIBITORS AND THEIR USE - The invention is directed to novel sEH inhibitors and their use in the treatment of diseases mediated by the sEH enzyme. Specifically, the invention is directed to compounds according to Formula I: | 10-14-2010 |
20100267755 | PYRIMIDINE DERIVATIVES - The invention provides the compounds of formula (I) | 10-21-2010 |
20100280056 | IDENTIFICATION OF SUBJECTS LIKELY TO BENEFIT FROM STATIN THERAPY - Methods are provided herein to determine if a subject is a candidate for treatment with an inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMGCR). The method includes determining the presence of at least one polymorphism in the HMGCR gene in a sample from a subject. The presence of at least one polymorphism indicates that the subject is a candidate for treatment with a statin, for example to decrease risk of or treat cancer, cardiovascular disease, diabetes, obesity, inflammatory disease, or auto-immune disease. | 11-04-2010 |
20100292262 | 4 (PYRROLO[2,3-C]PYRIDINE-3-YL)PYRIMIDIN-2-AMINE DERIVATIVES - Compounds of the formula (I), in which R | 11-18-2010 |
20100298364 | SALTS 756 - The invention provides salts of 4-(dimethylamino)butyl 2-(4-((2-amino-4-methyl-6-(pentylamino)pyrimidin-5-yl)methyl)phenyl)acetate, pharmaceutical compositions containing them and their use in therapy. | 11-25-2010 |
20100298365 | TOPICAL ADMINISTRATION CARRIER COMPOSITION AND THERAPEUTIC FORMULATIONS COMPRISING SAME - A topical administration carrier composition including water, glycerin and polysorbate, suitable for use in formulations with active ingredient compositions containing active ingredients such as minoxidil that are susceptible to systemic penetration, and solvents that are susceptible to evaporative loss, when the active ingredient composition is topically applied to the body. The carrier formulation retards the evaporative losses of the solvent component(s) and systemic migration losses of the active ingredient composition, to provide sustained topical action, in relation to formulations lacking the carrier composition of the invention. | 11-25-2010 |
20100298366 | CHEMOKINE RECEPTOR BINDING COMPOUNDS - The present invention relates to chemokine receptor binding compounds, pharmaceutical compositions and their use. More specifically, the present invention relates to modulators of chemokine receptor activity, preferably modulators of CCR5. These compounds demonstrate protective effects against infection of target cells by a human immunodeficiency virus (HIV). | 11-25-2010 |
20100311775 | Novel sEH Inhibitors and Their Use - The invention is directed to novel sEH inhibitors and their use in the treatment of diseases mediated by the sEH enzyme. Specifically, the invention is directed to compounds according to Formula I: | 12-09-2010 |
20100311776 | Novel sEH Inhibitors and their Use - The invention is directed to novel sEH inhibitors and their use in the treatment of diseases mediated by the sEH enzyme. Specifically, the invention is directed to compounds according to Formula I: | 12-09-2010 |
20100317678 | HYDROXAMATES AS INHIBITORS OF HISTONE DEACETYLASE - Compounds of formula (I), and salts, N-oxides, hydrates and solvates thereof are histone deacetylase inhibitors and are useful in the treatment of cell proliferative diseases, including cancers: | 12-16-2010 |
20100317679 | SUBSTITUTED ARYL-FUSED SPIROCYCLIC AMINES - Substituted Aryl-fused Spirocyclic Amines of the formula (I): are provided, as are methods for their preparation and use. Such compounds may generally be used to modulate ligand binding to histamine H3 receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and therapeutic methods are provided, as are methods for using such ligands for detecting histamine H3 receptors (e.g., receptor localization studies). | 12-16-2010 |
20100317680 | PYRIMIDINE INHIBITORS OF KINASES - The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, | 12-16-2010 |
20100324075 | THERAPEUTIC USE OF CARBOXYL ESTER LIPASE INHIBITORS - Compounds, pharmaceutical compositions, and their methods of use in raising serum HDL levels in subjects in need thereof are provided. Also provided are compounds, pharmaceutical compositions, and their methods of use in increasing reverse cholesterol transport in subjects in need thereof. Finally, methods for treating disease by raising serum HDL levels and increasing reverse cholesterol transport are provided. | 12-23-2010 |
20100324076 | Novel sEH Inhibitors and their Use - The invention is directed to novel sEH inhibitors and their use in the treatment of diseases mediated by the sEH enzyme. Specifically, the invention is directed to compounds according to Formula I: | 12-23-2010 |
20100324077 | COMBINATIONS OF ANILINOPYRIMIDINES AND PYRION COMPOUNDS - The present invention relates to combinations of an anilinopyrimidine, or a salt thereof, and a pyrion compound, or a salt thereof, which provide an improved biocidal effect. More particularly, the present invention relates to compositions comprising a combination of an anilinopyrimidine, or a salt thereof, selected from the group consisting of pyrimethanil, cyprodinil or mepanipyrim, together with a pyrion compound selected from 1-hydroxy-2-pyridinone, ciclopirox, ciclopirox olamine, piroctone, piroctone olamine, rilopirox, pyrion disulfide, sodium pyrithione and zinc pyrithione in respective proportions to provide a synergistic biocidal effect. Compositions comprising these combinations are useful for the protection of any living or non-living material, such as crops, plants, fruits, seeds, objects made of wood, thatch or the like, engineering material, biodegradable material and textiles against deterioration due to the action of microorganisms such as bacteria, fungi, yeasts, algae, virusses, and the like. | 12-23-2010 |
20110003836 | Pro-Neurogenic Compounds - This invention relates generally to stimulating neurogenesis (e.g., post-natal neurogenesis, e.g., post-natal hippocampal neurogenesis) and protection from neuron cell death. | 01-06-2011 |
20110003837 | MODIFIED RELEASE FORMULATIONS OF HMG COA REDUCTASE INHIBITORS - Modified release formulations of HMG Co-A reductase inhibitors, which provide reduced incidence of rhabdomyolysis, renal toxicity and other side effects by increasing hepatic bioavailability and decreasing systemic availability upon oral administration. The modified release pharmaceutical formulation comprises a therapeutically effective amount of HMG CoA reductase inhibitor or a pharmaceutically acceptable salt(s), polymorph(s), solvate(s), hydrate(s), prodrug or metabolite thereof, one or more release modifying agent(s) and one or more pharmaceutically acceptable excipient(s), wherein the modified release formulation provides reduced incidence of adverse effects and improved efficacy when compared to the immediate release formulation upon oral administration. | 01-06-2011 |
20110003838 | Whitening Agent And Skin External Preparation - The present invention provides a compound having an excellent inhibitory action on melanin production and being useful as a whitening agent, and a skin external preparation containing the compound. The whitening agent of the present invention comprises, as an active ingredient, a compound represented by formula (1) or a pharmacologically acceptable salt thereof: | 01-06-2011 |
20110015217 | Pro-Neurogenic Compounds - This invention relates generally to stimulating neurogenesis (e.g., post-natal neurogenesis, e.g., post-natal hippocampal neurogenesis) and protecting from neuron cell death. | 01-20-2011 |
20110015218 | AZA-BICYCLOHEXYL SUBSTITUTED INDOLYL ALKYL AMINO DERIVATIVES AS NOVEL INHIBITORS OF HISTONE DEACETYLASE - This invention comprises the novel compounds of formula (I) | 01-20-2011 |
20110028503 | COMPOSITIONS AND METHODS FOR INHIBITION OF THE JAK PATHWAY - Compounds I and II as well as salts and pharmaceutical compositions containing them are useful for treating diseases and/or disorders of the eye. | 02-03-2011 |
20110034495 | Method of Modulating Stress-Activated Protein Kinase System - A series of thieno[2,3-b]pyridin-6(7H)-one derivatives, substituted in the 2-position by a carbonyl- or sulfonyl-linked pyrrolidin-1-yl or related moiety, being inhibitors of p38 MAP kinase, are accordingly of use in medicine, for example in the treatment and/or prevention of immune or inflammatory disorders. | 02-10-2011 |
20110034496 | POST-HARVEST TREATMENT - The present invention relates to methods for the protection of harvested fruit, cutflowers or vegetables against decay caused by certain storage diseases or disorders expressed in storage conditions. In particular the invention relates to the application of certain fungicidal active compounds to protect harvested fruit, cutflowers or vegetables against phytopathogenic fungi. | 02-10-2011 |
20110034497 | INDAZOLE INHIBITORS OF THE WNT SIGNAL PATHWAY AND THERAPEUTIC USES THEREOF - Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases due to mutations in Wnt signaling components. Also provided are methods for treating Wnt-related disease states. | 02-10-2011 |
20110039873 | SUBSTITUTED PYRAZOLO[1,5-a] PYRIDINE COMPOUNDS HAVING MULTI-TARGET ACTIVITY - The substituted pyrazolo[1,5-a]pyridine compounds in accordance with Formula 1 are strong inhibitors of phosphodiesterase and c-Jun N-terminal kinase activity. | 02-17-2011 |
20110046170 | NOVEL PYRIMIDINE-PYRIDINE DERIVATIVES - The invention relates to novel pyrimidine-pyridine derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents. | 02-24-2011 |
20110053968 | AMINOPYRIMIDINE INHIBITORS OF TYROSINE KINASE - The present invention relates to new aminopyrimidine inhibitors of tyrosine kinase activity, pharmaceutical compositions thereof, and methods of use thereof | 03-03-2011 |
20110071176 | PHARMACEUTICAL COMPOSITION COMPRISING OMEGA-3 FATTY ACID AND HYDROXY-DERIVATIVE OF A STATIN AND METHODS OF USING SAME - In various embodiments, the present invention provides compositions and methods for treating and/or preventing a cardiovascular-related disease in subject in need thereof. | 03-24-2011 |
20110071177 | FUNGICIDAL ACTIVE SUBSTANCE COMBINATION - Methods of controlling fungi with an active compound combination that includes trifloxystrobin and pyrimethanil. | 03-24-2011 |
20110077261 | PREVENTION OF HIV-INFECTION - This invention relates to the use of a parenteral formulation comprising the NNRTI TMC278 for the long term prevention of HIV infection in a subject at risk of being infected by HIV, which comprises the intermittent administration of the said formulation at long time intervals. | 03-31-2011 |
20110082164 | POLYCYCLIC COMPOUNDS AS LYSOPHOSPHATIDIC ACID RECEPTOR ANTAGONISTS - Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases. | 04-07-2011 |
20110082165 | PYRROLIDINE GPR40 MODULATORS - The present invention provides compounds of Formula (I): | 04-07-2011 |
20110092527 | 4 (Pyrrolopyridinyl)pyrimidin-2-ylamine derivatives - Compounds of the formula (I), in which R | 04-21-2011 |
20110092528 | PIPERIDINYL COMPOUNDS THAT SELECTIVELY BIND INTEGRINS - The invention is directed to piperidinyl compounds that selectively bind integrin receptors and methods for treating an integrin mediated disorder. | 04-21-2011 |
20110098314 | STATINS FOR THE TREATMENT OF OCULAR HYPERTENSION AND GLAUCOMA - The use of HMG-CoA reductase inhibitors (e.g., statins) to treat glaucoma, control intraocular pressure, preserve the trabecular meshwork, protect against ocular neurodegeneration and/or protect against glaucomatous retinopathy is described. The preferred HMG-CoA reductase inhibitors, which are statins having an RI value of 0.2 to 0.7 (e.g., pravastatin), are administered via topical application to the affected eye(s) of the patient. | 04-28-2011 |
20110098315 | PHARMACEUTICAL COMPOSITIONS OF ROSUVASTATIN CALCIUM - This invention is related to pharmaceutical compositions of rosuvastatin or pharmaceutically acceptable salts thereof especially calcium salt with sodium carbonate anhydrous which has effects on dissoltion profiles in 0.1 N HCI medium provided that using of sodium carbonate anhydrous should be presence in the range of from about 0.5% to about 2% by weight. | 04-28-2011 |
20110105543 | NOVEL TRIARYL DERIVATIVES USEFUL AS MODULATORS OF NICOTINIC ACETYLCHOLINE RECEPTORS - This invention relates to novel triaryl derivatives, formula (I), a stereoisomer thereof or a mixture of its stereoisomers, or a pharmaceutically acceptable salt thereof, wherein all of X, Y and Z represent CH; or one or two of X, Y and Z represent N; and the others of X, Y and Z represent CH; and R | 05-05-2011 |
20110112125 | Novel hair growth composition - A water-soluble minoxidil composition for topical use significantly enhances the transdermal delivery of the drug in comparison with that of Rogaine. The composition contains minoxidil, water, enhancer, and polymer. The percentage of water in the composition may be up to 95%. | 05-12-2011 |
20110112126 | ENZYME INHIBITING COMPOUNDS - The present invention is directed to compounds that are specifically structured to provide enzyme inhibition. In specific embodiments, the enzyme inhibiting compounds exhibit antifolate activity. Particularly, the inventive compounds are formed of an antifolate residue that is active in inhibiting one or more of TS, DHFR, GAR, FPGS, and AICAR Tfase. The enzyme inhibiting compounds are useful in a variety of methods of treatment, including treating abnormal cell proliferation and treating inflammation. | 05-12-2011 |
20110112127 | COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR - Compounds and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, or forms thereof are active on Fms protein kinase, or on Fms and Kit protein kinase, or on Fms and Flt-3 protein kinase. Also described are methods of use thereof to treat diseases and conditions, including diseases and conditions associated with activity of Fms protein kinase, Kit protein kinase, or Flt-3 protein kinase including rheumatoid arthritis, osteoarthritis, multiple sclerosis, Alzheimer's disease, Parkinson's disease, glomerulonephritis, interstitial nephritis, Lupus nephritis, tubular necrosis, diabetic nephropathy, renal hypertrophy, acute myeloid leukemia, melanoma, multiple myeloma, metastatic breast cancer, prostate cancer, pancreatic cancer, neurofibromatosis, brain metastases, and gastrointestinal stromal tumors. | 05-12-2011 |
20110118291 | SUBSTITUTED INDOLYL-ALKYL-AMINO-DERIVATIVES AS INHIBITORS OF HISTONE DEACETYLASE - This invention comprises the novel compounds of formula (1) | 05-19-2011 |
20110118292 | METHOD OF TREATING ATHEROSCLEROSIS, DYSLIPIDEMIAS AND RELATED CONDITIONS - A method of treating atherosclerosis is disclosed wherein nicotinic acid or another nicotinic acid receptor agonist is administered to the patient in combination with a DP receptor antagonist. The DP receptor antagonist is administered to reduce, prevent or eliminate flushing that may otherwise occur. | 05-19-2011 |
20110124669 | Modulators of Cellular Adhesion - The present invention provides compounds having formula (I): | 05-26-2011 |
20110124670 | Use of Pyrimidylaminobenzamide Derivatives for the Treatment of Fibrosis - The invention relates to the use of a pyrimidylaminobenzamides of formula I | 05-26-2011 |
20110130415 | PROTEIN KINASE C INHIBITORS AND USES THEREOF - This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes. | 06-02-2011 |
20110130416 | PHARMACEUTICAL COMPOSITION FOR TREATING HYPERTENSION AND METABOLIC SYNDROME AND USE THEREOF - The present invention provides a pharmaceutical composition comprising the following active ingredients: 1) amlodipine or a pharmaceutically acceptable salt thereof, 2) pioglitazone or a pharmaceutically acceptable salt thereof, and 3) rosuvastatin or a pharmaceutically acceptable salt thereof. The present invention also provides use of the pharmaceutical composition in preparing a medicament for treating hypertension or metabolic syndrome. The pharmaceutical composition of the present invention can treat hypertension or metabolic syndrome, while effectively controlling the incidence of associated cardiovascular diseases and more potently improving survival prognosis in hypertensive patients. When blood pressure is lowered to desired level, the risk factors such as cardiovascular diseases are rectified, metabolic disorders and prognosis of patients are improved, and survival rate of hypertensive patients is raised. | 06-02-2011 |
20110136840 | ANTI-INFECTIVE AGENTS - The present invention relates to the use of molecules having a spacer unit, linker and recognition unit(s) for the treatment and prevention of various diseases, disorders and conditions. In particular, the present invention provides compounds useful in preventing or treating infectious diseases and diseases, disorders or conditions related thereto. Further, the present invention relates to methods for preventing or treating diseases, disorders or conditions involving recognition and binding of carbohydrate structures. | 06-09-2011 |
20110136841 | SUBSTITUTED INDOLYL ALKYL AMINO DERIVATIVES AS NOVEL INHIBITORS OF HISTONE DEACETYLASE - This invention comprises the novel compounds of formula (I) | 06-09-2011 |
20110136842 | Substituted Dihydroisoquinolinone and Isoquinolinedione Derivatives as Calcium Channel Blockers - A series of disubstituted dihydroisoquinolinone and isoquinolinedione derivatives represented by Formula I, or pharmaceutically acceptable salts thereof are presented. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, calcium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, diabetic neuropathy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, sleep disorder, bipolar disorder and stroke, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds. | 06-09-2011 |
20110144141 | Hair Growth and/or Regrowth Compositions - The present disclosure relates to compositions containing certain pyrimidine compounds such as minoxidil and/or certain pyrimidine sulfate (inner salt) compounds such as minoxidil sulfate and especially compositions containing pyrimidine compounds in combination with an admixtures comprising at least one antioxidant, at least one organic acid and a select fatty acid mixture. The present disclosure also relates to use of the compositions to grow and/or regrow hair and/or prevent hair loss in mammals and particularly in humans. | 06-16-2011 |
20110144142 | Methods of Reducing Hair Loss and/or Facilitating Hair Growth and/or Regrowth - The present disclosure relates to methods of retarding hair loss or facilitating hair growth and/or regrowth. More specifically, the present disclosure relates to methods of using the disclosed compositions to increase the rate of terminal hair growth and/or regrowth in a mammal. | 06-16-2011 |
20110152302 | Novel dicyclanil-based shelf stable aqueous suspension and non-aqueous solution pour-on and spray-on formulations useful for the prevention and treatment of insect infestation in animals - This invention relates to topically active compositions, including pour-on and spray-on formulations, comprising insect growth regulator (IGR) insecticides prepared as aqueous suspension formulations, or as non-aqueous solution formulations, and to the methods of making these formulations, and to methods of using these formulations for the treatment and/or prevention of insect infestation in animals. | 06-23-2011 |
20110152303 | Chemical Compounds - Novel diarylpyrimidine derivatives and pharmaceutically acceptable salts, solvates or hydrates thereof, designed to inhibit HIV reverse transcriptase, are provided, and a pharmaceutical composition containing the same, especially an anti-HIV agent. More specifically, novel diarylpyrimidine derivatives that are derivatives of the HIV reverse transcriptase inhibitor TMC278 of formula (1 | 06-23-2011 |
20110160236 | Treating Vascular Events with Statins by Inhibiting PAR-1 and PAR-4 - The present invention relates to new methods for treating and/or preventing vascular events by inhibiting G-coupled Protease Activating Receptor (PAR)-1 and/or PAR-4 with the administration of statins. In one embodiment, individuals who are at risk for vascular events, but have cholesterol levels (e.g., total cholesterol or Low Density Lipoprotein) in normal ranges, are treated with statins. | 06-30-2011 |
20110160237 | Substituted Heterocyclic Compounds - The present invention relates to substituted heterocyclic compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted heterocyclic compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof. | 06-30-2011 |
20110166169 | NOVEL HSP90 INHIBITORY CARBAZOLE DERIVATIVES, COMPOSITIONS CONTAINING SAME AND USE THEREOF - The invention relates to the novel substances in Formula (I): wherein Het is a heterocycle optionally substituted by one or a plurality of radicals R1 or R′1; R is selected from the group comprising Formula (A′), (B), (C), (D), or (E), with R1 and/or R′1 selected from H, halogen, CF3, nitro, cyano, alkyl, hydroxyl, mercapto, amino, alkylamino, dialkylamino, alkoxy, phenylalcoxy, alkylhio, or carboxy that is free or esterified by an alkyl, carboxamide, CO—NH(alkyl), CON(alkyl)2, NH—CO-alkyl, sulfonamide, NH—S02-alkyl, S(0)2-NHalkyl, or S(02)-N(alkyl)2 radical; all these radicals are optionally substituted; W1, W2, and W3 independently are CH or N; X is 0, S, NR2, C(O), S(O), or S(0)2; Z is optionally substituted H, Hal, -0-R2 or —NH—R2 with R2 being H, alkyl, cycloalkyl, or heterocycloalkyl; and these substances are all isomeric forms and salts thereof, used as drugs. | 07-07-2011 |
20110178111 | LONG-TERM TREATMENT OF SYMPTOMATIC HEART FAILURE - The main object here is the use of omega-3 polyunsaturated fatty acids (as ethyl esters, hereinafter called “n-3 PUFA”) as a medicament, either alone or in combination with other therapeutic agents, for reducing mortality for a cardiovascular cause, in particular arrhythmia or for reducing hospitalization for any cause, in particular a cardiovascular cause and for the daily administration to patients with symptomatic heart failure (HF) for more than 3.5 years. | 07-21-2011 |
20110190327 | METHOD FOR MODULATING GPR119 G PROTEIN-COUPLED RECEPTOR AND SELECTED COMPOUNDS - A method of modulating the activity of the GPR119 G protein-coupled receptor comprising administering to a mammalian patient in need thereof a therapeutically effective amount of at least one compound of Formula I or Formula IA and, optionally, an additional therapeutic agent. | 08-04-2011 |
20110190328 | ACID ADDITION SALTS OF (3,5-BIS TRIFLUOROMETHYL)-N-[4-METHYL-3-(4-PYRIDIN-3YL-PYRIMIDIN-2YLAMINO)-PHENYL]- -BENZAMIDE - The present invention relates to acid addition salts of the pharmaceutically active compound (3,5-Bistrifluoromethyl)-N-[4-methyl-3-(4-pyridin-3yl-pyrimidin-2ylamino)-phenyl]-benzamide(I): | 08-04-2011 |
20110195985 | COMPOUNDS FOR THE TREATMENT OF LYSOSOMAL STORAGE DISEASES - A method of treating a lysosomal storage disease comprises administering a pyrimethamine derivative to a subject in need thereof. | 08-11-2011 |
20110195986 | PYRROLONE MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS - The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I | 08-11-2011 |
20110207759 | METHOD FOR TREATMENT OF ATHEROSCLEROTIC DISEASE - A method of effecting regression of atherosclerotic disease in a patient whose plasma lipid concentrations are at levels considered normal or optimal. The method involves treating the patient with a combination of a 3-hydroxy-3-methylglutaryl-coenzyme A reductase inhibitor and niacin. Disease regression has been observed over periods as short as 14 months, preferably 8 months. | 08-25-2011 |
20110212983 | PLATELET ADP RECEPTOR INHIBITORS - Novel compounds of formula (I) to (VI), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I)-(VI), or a pharmaceutically acceptable salt thereof. | 09-01-2011 |
20110224244 | Adamantyl Benzamide Derivatives - Embodiments of the present invention provide adamantyl benzamide derivtives and pharmaceutical compositions comprising adamantyl benzamide derivatives. Methods of use of such compounds and compositions to modulate the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) in a subject are also provided. | 09-15-2011 |
20110230507 | Piperidine GPCR Agonists - Compounds of formula (I): or pharmaceutically acceptable salts thereof, are GPCR agonists and are useful as for the treatment of diabetes and obesity. | 09-22-2011 |
20110230508 | Novel Forms of a Fused Pyrrolocarbazole Compound - Alternative chemical and/or solid state forms of Compound I, processes to reproducibly make them and methods of treating patients using them. | 09-22-2011 |
20110237612 | Thienylamino pyrimidines for use as Fungicides - Thienylaminopyrimidines of the formula (I) | 09-29-2011 |
20110245283 | Methods for predicting the response to statins - The invention provides methods for optimizing therapeutic efficacy for treating hypercholesterolemia in a subject having a cardiovascular disease (CVD), comprising (a) determining subject characteristics that affect the likelihood of reaching a goal level of low density lipoprotein (LDL); and (b) obtaining success probabilities of a variety of statin treatments for reaching said goal level of LDL using said subject characteristics and a multivariate model; and (c) administrating the optimal statin treatment with the highest success probability of step (b) to said subject thereby optimizing therapeutic efficacy for treating hypercholesterolemia in said subject. | 10-06-2011 |
20110245284 | Alkoxy- and Alkylthio-Substituted Anilinopyrimidines - Alkoxy- and alkylthio-substituted anilinopyrimidines of the formula (I) | 10-06-2011 |
20110245285 | PROCESS FOR PREPARATION OF ROSUVASTATIN ACETONIDE CALCIUM - The present invention is in relation to a process for preparation of HMG-CoA reductase inhibitor. More particularly, the present invention provides a process for preparation of (3R,5S,6E) 6-{2-[4-(4-Fluoro-phenyl)-6-isopropyl-2-(methanesulfonyl-methyl-amino)-pyrimidin-5-yl]-vinyl}-2,2-dimethyl-[1,3]dioxan-4-yl)-acetic acid, calcium salt (Rosuvastatin acetonide calcium) which is used for treating hypercholesterolemia. | 10-06-2011 |
20110251221 | PYRIMIDINYLPIPERIDINYLOXYPYRIDINONE ANALOGUES AS GPR119 MODULATORS - Novel compounds of structure Formula I: | 10-13-2011 |
20110251222 | SULFONE-SUBSTITUTED ANILINOPYRIMIDINE DERIVATIVES AS CDK INHIBITORS, THE PRODUCTION THEREOF, AND USE AS A MEDICINE - The invention relates to sulphone-substituted anilinopyrimidine derivatives of the formula (I), | 10-13-2011 |
20110257211 | Small-Molecule Choline Kinase Inhibitors as Anti-Cancer Therapeutics - Small molecule choline kinase inhibitors having the following formula: | 10-20-2011 |
20110263628 | N-HYDROXYAMIDE DERIVATIVES AND USE THEREOF - The present invention is related to N-hydroxyamide derivatives of Formula (I) and use thereof in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis. | 10-27-2011 |
20110275654 | LONG TERM TREATMENT OF HIV-INFECTION WITH TMC278 - This invention relates to the use of a parenteral formulation comprising an anti-virally effective amount of TMC278 or a pharmaceutically acceptable acid-addition salt thereof, and a carrier, for the manufacture of a medicament for the treatment of a subject being infected with HIV, wherein the formulation is to be administered intermittently at a time interval of at least one week. | 11-10-2011 |
20110275655 | PYRIMIDINECARBOXAMIDE DERIVATIVES AS INHIBITORS OF SYK KINASE - The present invention relates to the compound of formula (I): | 11-10-2011 |
20110281901 | PHARMACEUTICAL COMPOSITIONS AND METHODS OF MAKING SAME - Pharmaceutical compositions that include an amount of an acid addition salt of pazopanib equivalent to about 5 mg/mL pazopanib, about 2.0 to about 13.0% w/w of a modified cyclodextrin suitable for use in an ophthalmic formulation, and pH adjusting agent as well as methods of making the same are described. | 11-17-2011 |
20110281902 | COMBINATIONS COMPRISING A PROTEIN KINASE INHIBITOR BEING A PYRIMIDYLAMINOBENZAMIDE COMPOUND AND A HSP90 INHIBITOR SUCH AS 17-AAG - The invention provides a pharmaceutical combination comprising:
| 11-17-2011 |
20110288110 | METHODS FOR TREATING DISORDERS ASSOCIATED WITH HYPERLIPIDEMIA IN A MAMMAL - The invention is directed to methods for treating hyperlipidemia in a mammal. The methods involve combination therapies using a microsomal triglyceride transfer protein (MTP) inhibitor (for example, BMS-201038 and implitapide) and a HMG-CoA reductase inhibitor (for example simvastatin or atorvastatin). Co-administration of the MTP inhibitor with the HMG-CoA reductase inhibitor produces a therapeutic benefit, for example, a reduction in the concentration of cholesterol and/or triglycerides in the blood stream, but with fewer or reduced side effects than when higher dosages of the MTP inhibitor are used during monotherapy to provide the same or similar therapeutic benefit. | 11-24-2011 |
20110294840 | HYDRAZIDE COMPOUND AND USE OF THE SAME IN PEST CONTROL - There is provided a hydrazide compound having a controlling effect on pests represented by the formula (1): wherein, G is a 5-membered heterocyclic group, M is an oxygen atom or a sulfur atom, Q | 12-01-2011 |
20110294841 | NOVEL STATIN PHARMACEUTICAL COMPOSITIONS AND RELATED METHODS OF TREATMENT - The invention provides novel omega-3 oil formulations of one or more statins. These formulations are readily bioavailable. Notably, because the formulations of the invention contain an omega-3 oils as the major ingredient, they not only provide an antihypercholesterolemic effect due to the statin active ingredient, they also provide recommended daily dosages of omega-3 oils (i.e., approximately 1 gram of omega-3 oil per day), or a portion thereof. The invention also provides novel salts of one or more statins. | 12-01-2011 |
20110301186 | USE OF HAPTOGLOBIN GENOTYPING IN DIAGNOSIS AND TREATMENT OF CARDIOVASCULAR DISEASE - This invention is directed to methods and compositions for the treatment of cardiovascular disorders. Specifically, the invention is directed to compositions comprising vitamin E, statins and/or glutathione peroxidase mimetics; methods of treating diabetic patients expressing the Hp-2-2 haptoglobin genotype; a method of inhibiting or suppressing a cardiovascular disorder in a diabetic subject, treating cardiovascular disease in subjects exhibiting the Haptoglobin Hp-2-2 genotype; and methods of treating cardiovascular disease in subjects exhibiting the Haptoglobin Hp-2-2 genotype. | 12-08-2011 |
20110306625 | COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS - The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of B-Raf. | 12-15-2011 |
20110312985 | NARINGENIN COMPLEXES AND METHODS OF USE THEREOF - The invention relates to methods of treatment of hepatitis C, dyslipidemia, insulin resistance, and inflammation, with flavonoid-sugar complexes. | 12-22-2011 |
20120004253 | Novel Fused Pyrrolocarbazoles - The present invention relates generally to selected fused pyrrolocarbazoles, including pharmaceutical compositions thereof and methods of treating diseases therewith. The present invention is also directed to intermediates and processes for making these fused pyrrolocarbazoles. | 01-05-2012 |
20120015967 | PYRIMIDINE AND PYRIDINE DERIVATIVES AS POSH AND POSH-AP INHIBITORS - Pyridine and pyrimidine derivatives inhibit ubiquitination of human polypeptides, particularly of POSH and POSH-associated proteins such as HERPUD1, and can be used as medicaments for treatment of viral infections caused by virus such as HIV and for treatment of neurological disorders or diseases. | 01-19-2012 |
20120015968 | USE OF PYRIMIDYLAMINOBENZAMIDE DERIVATIVES FOR THE TREATMENT OF DISORDERS MEDIATED BY THE LEUCINE ZIPPER-AND STERILE ALPHA MOTIF-CONTAINING KINASE (ZAK) - The invention relates to the use of a pyrimidylaminobenzamide derivative of formula I | 01-19-2012 |
20120015969 | NOVEL AMINOPYRIDINE DERIVATIVES HAVING AURORA A SELECTIVE INHIBITORY ACTION - The present invention relates to a compound of Formula (I): wherein: R | 01-19-2012 |
20120022090 | NOVEL SUBSTITUTED BENZOXAZOLE, BENZIMIDAZOLE, OXAZOLOPYRIDINE AND IMIDAZOPYRIDINE DERIVATIVES AS GAMMA SECRETASE MODULATORS - The present invention is concerned with novel substituted benzoxazole, benzimidazole, oxazolopyridine and imidazopyridine derivatives of Formula (I) | 01-26-2012 |
20120022091 | KEY INTERMEDIATES FOR THE SYNTHESIS OF ROSUVASTATIN OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF - The present invention relates in general to the field of organic chemistry and in particular to the preparation of N-(4-(4-fluorophenyl)-6-isopropyl-5-methylpyrimidin-2-yl)-N-methylmethanesulfonamide (I), N-(4-(4-fluorophenyl)-5-(bromomethyl)-6-isopropylpyrimidin-2-yl)-N-methylmethanesulfonamide (II) and N-(4-(4-fluorophenyl)-5-(hydroxymethyl)-6-isopropylpyrimidin-2-yl)-N-methylmethanesulfonamide (III), key intermediates in preparation of Rosuvastatin. | 01-26-2012 |
20120022092 | PROTEIN KINASE C INHIBITORS AND USES THEREOF - This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes. | 01-26-2012 |
20120029001 | METHOD OF TREATMENT OF NEPHROGENIC DIABETES INSIPIDUS - Nephrogenic diabetes insipidus is treated with statins. | 02-02-2012 |
20120029002 | BENZIMIDAZOLE AND PYRAZOLOPYRIDINE DERIVATIVES FOR TREATING AND/OR PREVENTING CARDIOVASCULAR DISEASES - The present application relates to novel fused, heteroatom-bridged pyrazole and imidazole derivatives, to processes for their preparation, to their use, alone or in combination, for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular disorders. | 02-02-2012 |
20120029003 | GALECTIN-3 AND STATIN THERAPY - Described herein are materials and methods for predicting and monitoring a heart failure patient's physiological response to treatment with a statin. More specifically, the present invention relates to the endogenous protein galectin-3 and its use as a predictor of response to treatment with 3-hydroxy-3-methylglutaryl coenzyme-A reductase inhibitors, or statins. | 02-02-2012 |
20120029004 | NOVEL AMINOPYRIDINE DERIVATIVES HAVING AURORA A SELECTIVE INHIBITORY ACTION - The present invention relates to a compound of Formula (I): wherein: R | 02-02-2012 |
20120035197 | Novel Use of Fibrates - The present invention, which is applicable in the pharmaceutical industry, relates to the use of fibrates, in particular fenofibrate, especially in the form of a solid oral composition, for the manufacture of a drug for the treatment of sleep apnea, sleep apnea syndrome, in particular obstructive sleep apnea or obstructive sleep apnea syndrome. | 02-09-2012 |
20120035198 | Antiviral Compounds and Methods of Using Thereof - Disclosed herein are compounds which exhibit antiviral activity against a plurality of viruses belonging to different families such as Bornaviridae, Filoviridae, Paramyxoviridae, Rhabdoviridae, Arenaviridae, Bunyaviridae, Orthomyxoviridae, and Poxviridae. Thus, methods of preventing, inhibiting, or reducing the viral activity of various viruses are provided as well as methods of treating viral infections. | 02-09-2012 |
20120041010 | PHARMACEUTICAL COMBINATION OF (E)-7-[4-(4-FLUOROPHENYL)-6-ISOPROPYL-2-[METHYL(METHYLSULFONYL)AMINO]PYRI- MIDIN-5-YL] (3R,5S)-3,5-DIHYDROXYHEPT-6-ENOIC ACID AND CANDESARTAN - The present invention relates to a new use of a statin drug in the improvement of diabetic neuropathy, specifically in improving nerve conduction velocity and nerve blood flow in patients suffering diabetes, in particular to pharmaceutical combinations of the statin drug and other agents known to improve diabetic neuropathy such as an aldose reductase inhibitor (ARI), an angiotensin converting enzyme (ACE) inhibitor or an angiotensin II (AII) antagonist which combinations are useful in the prevention and treatment of the complications of diabetes | 02-16-2012 |
20120041011 | SUBSTITUTED BENZOFUSED DERIVATIVES AND THEIR USE AS VANILLOID RECEPTOR LIGANDS - The present invention relates to substituted benzofused derivatives, which can he used as vanilloid receptor ligands, method of treating diseases, conditions and/or disorders modulated by vanilloid receptors with them, and processes for preparing them. | 02-16-2012 |
20120041012 | SUBSTITUTED SPIROCYCLIC AMINES USEFUL AS ANTIDIABETIC COMPOUNDS - Substituted spirocyclic amines of structural formula I are selective antagonists of the somatostatin sub-type receptor 5 (SSTR5) and are useful for the treatment, control or prevention of disorders responsive to antagonism of SSTR5, such as Type 2 diabetes, insulin resistance, lipid disorders, obesity, atherosclerosis, metabolic syndrome, depression, and anxiety. | 02-16-2012 |
20120059022 | Crystalline Form of Bis[(E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]- pyrimidin-5-yl](3R,5S)-3,5-dihydroxyhept-6-enoicacid] Calcium Salt - Two polymorphic forms of bis[(E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl](3R,5S)-3,5-dihydroxyhept-6-enoic acid] calcium salt, processes for making them and their use as HMG Co-A reductase inhibitors are described. | 03-08-2012 |
20120077832 | BESYLATE SALT OF A BTK INHIBITOR - The present invention provides a salt form, and compositions thereof, useful as an inhibitor of one or more protein kinases and which exhibits desirable characteristics for the same. | 03-29-2012 |
20120077833 | ACID ADDITION SALTS OF (3,5-BIS TRIFLUOROMETHYL)-N-[4-METHYL-3-(4-PYRIDIN-3YL-PYRIMIDIN-2YLAMINO)-PHENYL]- -BENZAMIDE - The present invention relates to acid addition salts of the pharmaceutically active compound (3,5-Bistrifluoromethyl)-N-[4-methyl-3-(4-pyridin-3yl-pyrimidin-2ylamino)-phenyl]-benzamide(I): | 03-29-2012 |
20120083504 | Reverse Amide Compounds As Protein Deacetylase Inhibitors And Methods Of Use Thereof - The present invention relates to novel “reverse amide” compounds comprising a zinc chelator group, and the use of such compounds in the inhibition of HDAC6 and in the treatment of various diseases, disorders or conditions related to HDAC6. | 04-05-2012 |
20120108617 | METHODS AND COMPOSITIONS INVOLVING (S)-BUCINDOLOL - Disclosed is bucindolol substantially free of its R-stereoisomer. Also disclosed are pharmaceutical compositions that include bucindolol substantially free of its R-stereoisomer or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. Also disclosed are methods of treating a patient that involve administering to the patient a therapeutically effective amount of a composition of the present invention. Formula (I). | 05-03-2012 |
20120136018 | QUINOLINES - The present invention relates to 2-aminoquinolines of formula I | 05-31-2012 |
20120165354 | TREATMENT METHOD - The present invention relates to methods of treating age-related macular degeneration in a patient by administration of pazopanib or pharmaceutically acceptable salts or solvates thereof. | 06-28-2012 |
20120165355 | METHODS AND COMPOSITIONS FOR TREATING CANCERS - This invention provides a combination of antagonists of the hedgehog signaling pathway with a BCR-ABL inhibitor. The combination of the present invention may be used for treating cancers known to be associated with protein tyrosine kinases such as, for example, Src, BCR-ABL and c-kit. | 06-28-2012 |
20120172384 | HETEROCYCLYLAMINOPYRIMIDINES AS KINASE INHIBITORS - The invention relates to compounds of formula (I) | 07-05-2012 |
20120172385 | ORTHO SUBSTITUTED PYRIMIDINE COMPOUNDS AS JAK INHIBITORS - The invention relates to compounds of formula (I) | 07-05-2012 |
20120172386 | Combinations Comprising a VEGF Receptor Inhibitor - A composition comprising a VEGF receptor inhibitor and a penetration enhancer and uses thereof. | 07-05-2012 |
20120178770 | SUBSTITUTED PYRIMIDINYLPYRROLOPYRIDINONE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS KINASE INHIBITORS - Pyrimidinylpyrrolopyridinone derivatives of formula (I) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer. | 07-12-2012 |
20120184574 | INDOLE DERIVATIVES AND METHODS FOR ANTIVIRAL TREATMENT - The present invention is directed to compounds and forms and pharmaceutical compositions thereof useful for treating a viral infection, or for affecting viral activity by modulating viral replication. | 07-19-2012 |
20120184575 | TOPICAL ADMINISTRATION CARRIER COMPOSITION AND THERAPEUTIC FORMULATIONS COMPRISING SAME - A topical administration carrier composition including water, glycerin and polysorbate, suitable for use in formulations with active ingredient compositions containing active ingredients such as minoxidil that are susceptible to systemic penetration, and solvents that are susceptible to evaporative loss, when the active ingredient composition is topically applied to the body. The carrier formulation retards the evaporative losses of the solvent component(s) and systemic migration losses of the active ingredient composition, to provide sustained topical action, in relation to formulations lacking the carrier composition of the invention. | 07-19-2012 |
20120190700 | NOVEL 4-AMINO-N-HYDROXY-BENZAMIDES FOR THE TREATMENT OF CANCER - The present invention provides compounds of formula | 07-26-2012 |
20120196885 | NEW HISTONE DEACETYLASE INHIBITORS BASED SIMULTANEOUSLY ON TRISUBSTITUTED 1H-PYRROLES AND AROMATIC AND HETEROAROMATIC SPACERS - The present invention refers to compounds derived from trisubstituted 1H-pyrrole rings and aromatic rings, which have the following formula (I): | 08-02-2012 |
20120196886 | COMBINATION - The present invention relates to a method of treating cancer in a human and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method that includes administering N-{3-[5-(2-Amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-1,3-thiazol-4-yl]-2-fluorophenyl}-2,6-difluorobenzenesulfonamide or a pharmaceutically acceptable salt thereof, and N-{(1S)-2-amino-1-[(3,4-difluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-furancarboxamide, or a pharmaceutically acceptable salt thereof, to a human in need thereof. | 08-02-2012 |
20120202834 | GLUCAGON RECEPTOR MODULATORS - The present invention provides a compound of Formula (I) | 08-09-2012 |
20120202835 | COMBINATION - The present invention relates to a method of treating cancer in a human and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method that includes administering N-{3-[5-(2-Amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-1,3-thiazol-4-yl]-2-fluorophenyl}-2,6-difluorobenzenesulfonamide or a pharmaceutically acceptable salt thereof, and N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecarboxamide, or a pharmaceutically acceptable salt thereof, to a human in need thereof. | 08-09-2012 |
20120202836 | METHOD OF TREATING PROLIFERATIVE DISORDERS AND OTHER PATHOLOGICAL CONDITIONS MEDIATED BY BCR-ABL, C-KIT, DDR1, DDR2 OR PDGF-R KINASE ACTIVITY - The present invention relates to a regimen for the administration of a pyrimidylaminobenzamide of formula I as defined herein for the treatment of proliferative disorders, particularly solid and liquid tumors, and other pathological conditions mediated by the Bcr-AbI oncoprotein, the cell transmembrane tyrosine kinase receptor c-Kit, DDR1 (discoidin domain receptor 1), DDR2 (discoidin domain receptor 2) or PDGF-R (platelet derived growth factor receptor) kinase activity. | 08-09-2012 |
20120220615 | SUBSTITUTED INDOLYL ALKYL AMINO DERIVATIVES AS NOVEL INHIBITORS OF HISTONE DEACETYLASE - This invention comprises the novel compounds of formula (I) | 08-30-2012 |
20120225897 | HAIR GROWTH AND/OR REGROWTH COMPOSITIONS - The present disclosure relates to compositions containing certain pyrimidine compounds such as minoxidil and/or certain pyrimidine sulfate (inner salt) compounds such as minoxidil sulfate and especially compositions containing pyrimidine compounds in combination with an admixtures comprising at least one antioxidant, at least one organic acid and a select fatty acid mixture. The present disclosure also relates to use of the compositions to grow and/or regrow hair and/or prevent hair loss in mammals and particularly in humans. | 09-06-2012 |
20120225898 | HAIR GROWTH AND/OR REGROWTH COMPOSITIONS - The present disclosure relates to compositions containing certain pyrimidine compounds such as minoxidil and/or certain pyrimidine sulfate (inner salt) compounds such as minoxidil sulfate and especially compositions containing pyrimidine compounds in combination with an admixtures comprising at least one antioxidant, at least one organic acid and a select fatty acid mixture. The present disclosure also relates to use of the compositions to grow and/or regrow hair and/or prevent hair loss in mammals and particularly in humans. | 09-06-2012 |
20120225899 | Compounds and Compositions as Protein Kinase Inhibitors - The present invention provides compounds of Formula I or II: | 09-06-2012 |
20120232105 | PHARMACEUTICAL COMPOSITION FOR INHIBITING OSTEOCLAST GROWTH - A pharmaceutical composition for inhibiting osteoclast growth is disclosed in the present invention. The pharmaceutical composition includes a compound represented by a formula (I), and a pharmaceutically acceptable salt and carrier: | 09-13-2012 |
20120232106 | TREATMENT FOR DISCOID LUPUS - Compounds I and II as well as salts and pharmaceutical compositions containing them are useful for treating diseases and/or disorders of the skin, such as cutaneous lupus, for example acute cutaneous lupus erythematosus, subacute cutaneous lupus erythematosus, or discoid lupus erythematosus. In certain embodiments, the compounds are provided in topical compositions. | 09-13-2012 |
20120232107 | NON-PEPTIDE ANTAGONISTS OF GASTRIN RELEASING PEPTIDE - This invention relates, e.g., to methods for inhibiting or stimulating an activity of an adrenomedullin (AM) or gastrin releasing peptide (GRP) peptide hormone, comprising contacting the peptide with a small molecule, non-peptide, modulatory agent of the invention. Complexes of these modulatory agents with other components, such as the peptides or blocking antibodies specific for the peptides, are also described, as are pharmaceutical compositions comprising the modulatory agents, and methods for using the modulatory agents to diagnose or treat patients. | 09-13-2012 |
20120238593 | HETEROCYCLIC COMPOUNDS AND USES THEREOF - The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same. | 09-20-2012 |
20120245189 | CRYSTALLINE CDC7 INHIBITOR SALTS - The present invention relates to novel crystalline salts of a CDC7 or CDC7/CDKs inhibitor, to a novel crystal form of the corresponding free base, to a process for their preparation, to hydrates, solvates and polymorphs of such new salt forms, to their use in therapy and to pharmaceutical compositions containing them. Such crystal salts are selected from L-asparate, hemifumarate, hydrochloride, maleate, mesylate, sulfate, L-tartrate or phosphate salts of 5-(2-amino-pyrimidin-4-yl)-2-(2,4-dichloro-phenyl)-1H-pyrrole-3-carboxylic acid amide. | 09-27-2012 |
20120264773 | ORGANIC COMPOUNDS - The present invention provides a compound of formula (I): | 10-18-2012 |
20120270891 | Salts of 4-Methyl-N-[3-(4-methyl-imidazol-1-yl)-5-trifluoromethyl-phenyl]-- 3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-benzamide - Salts of 4-methyl-N-[3-(4-methyl-imidazol-1-yl)-5-trifluoromethyl-phenyl]-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-benzamide are prepared by various processes. | 10-25-2012 |
20120270892 | Aminopyrimidine Kinase Inhibitors - Disclosed are compounds, pharmaceutical compositions containing those compounds, and uses of the compounds and compositions as modulators of casein kinase 1 (e.g., CK1γ), casein kinase 2 (CK2), Pim-1, Pim-2, Pim-3, the TGFβ pathway, the Wnt pathway, the JAK/STAT pathway, and/or the mTOR pathway. Uses are also disclosed for the treatment or prevention of a range of therapeutic indications due at least in part to aberrant physiological activity of casein kinase 1 (e.g., CK1γ), casein kinase 2 (CK2), Pim-1, Pim-2, Pim-3, the TGFβ pathway, the Wnt pathway, the JAK/STAT pathway, and/or the mTOR pathway. | 10-25-2012 |
20120277258 | Chemical Compounds - Pyrimidine derivatives, which are useful as VEGFR2 inhibitors are described herein. The described invention also includes methods of making such pyrimidine derivatives as well as methods of using the same in the treatment of hyperproliferative diseases. | 11-01-2012 |
20120277259 | SUBSTITUTED BENZOFUSED DERIVATIVES AND THEIR USE AS VANILLOID RECEPTOR LIGANDS - The present invention relates to substituted benzofused derivatives, which can be used as vanilloid receptor ligands, method of treating diseases, conditions and/or disorders modulated by vanilloid receptors with them, and processes for preparing them. | 11-01-2012 |
20120289527 | MONO-HYDROCHLORIC SALTS OF AN INHIBITOR OF HISTONE DEACETYLASE - This invention provides novel crystalline forms of mono-HCl salts and a mono-HCl salt hydrate of JNJ-26481585, an inhibitor of histone deacetylases. The invention also relates to processes for production of these forms, to intermediates used in these processes, to pharmaceutical compositions comprising these forms, and to the use of these forms in medical treatment for instance as a medicine to inhibit proliferative conditions, such as cancer and leukemia. | 11-15-2012 |
20120289528 | METHOD OF TREATING PROLIFERATIVE DISORDERS AND OTHER PATHOLOGICAL CONDITIONS MEDIATED BY BCR-ABL, C-KIT, DDR1, DDR2 OR PDGF-R KINASE ACTIVITY - The present invention relates to a regimen for the administration of a pyrimidylaminobenzamide of formula I | 11-15-2012 |
20120302588 | METHOD OF ENHANCING HAIR GROWTH - Methods and compositions for stimulating the growth of hair are disclosed wherein said compositions include bimatoprost and minoxidil in a vehicle for topical application to the skin of a mammal, e.g. a human, whereby the combination of bimatoprost and minoxidil produces a faster onset of hair growth in humans or other mammals and wherein said composition brings about a synergestic result of faster onset of hair growth as compared to compositions comprising bimatoprost and minoxidil, alone. | 11-29-2012 |
20120302589 | PHARMACEUTICAL COMPOSITIONS COMPRISING EPA AND A CARDIOVASCULAR AGENT AND METHODS OF USING THE SAME - The present invention relates to, inter alia, pharmaceutical compositions comprising EPA and one or more cardiovascular agents, and to therapeutic methods for treating various diseases and disorders using the same. | 11-29-2012 |
20130005757 | PHARMACEUTICAL COMPOSITIONS COMPRISING EPA AND A CARDIOVASCULAR AGENT AND METHODS OF USING THE SAME - The present invention relates to, inter alia, pharmaceutical compositions comprising EPA and one or more cardiovascular agents, and to therapeutic methods for treating various diseases and disorders using the same. | 01-03-2013 |
20130012531 | TREATMENT METHOD - The present invention is directed to methods of treating disorders of ocular angiogenesis or vascular leakage in a patient by administration of suitable inhibitors, including pazopanib or pharmaceutically acceptable salts or hydrates thereof. | 01-10-2013 |
20130012532 | CYCLOPROPANECARBOXYLIC ACID DERIVATIVE - A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof, wherein R | 01-10-2013 |
20130018065 | PROCESSES FOR THE PREPARATION OF KEY INTERMEDIATE FOR THE SYNTHESIS OF ROSUVASTATIN OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOFAANM Andrensek; SamoAACI LjubljanaAACO SIAAGP Andrensek; Samo Ljubljana SIAANM Anzel; JolandaAACI LjubljanaAACO SIAAGP Anzel; Jolanda Ljubljana SIAANM Hocevar; MarjetaAACI LjubljanaAACO SIAAGP Hocevar; Marjeta Ljubljana SIAANM Casar; ZdenkoAACI LjubljanaAACO SIAAGP Casar; Zdenko Ljubljana SI - The present invention relates in general to the field of organic chemistry and in particular to a process for the preparation of 5-((E)-2-((2S,4R)-4-hydroxy-6-oxotetrahydro-2H-pyran-2-yl)vinyl)-4-(4-fluorophenyl)-6-isopropyl-2-(N-methyl-methanesulfonylamino)pyrimidine (RSVL) as well as a process for preparing crystalline 5-((E)-2-((2S,4R)-4-(tert-butyldimethylsilyloxy)-6-oxotetrahydro-2H-pyran-2-yl)vinyl)-4-(4-fluorophenyl)-6-isopropyl-2-(N-methylmethanesulfonylamino)pyrimidine (RSVLTBS) useful as key intermediates for the preparation of rosuvastatin or pharmaceutically acceptable salts thereof. | 01-17-2013 |
20130018066 | HETEROCYCLIC ASPARTYL PROTEASE INHIBITORS - Disclosed are compounds of the formula I | 01-17-2013 |
20130023548 | Crystalline Forms of 4-Methyl-N-[3-(4-methyl-imidazol-1-yl)-5-trifluoromethyl-phenyl]-3-(4-pyr- idin-3-yl-pyrimidin-2-ylamino)-benzamide - Crystalline forms of 4-methyl-N-[3-(4-methyl-imidazol-1-yl)-5-trifluoromethyl-phenyl]-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-benzamide free base and salts thereof are prepared by various processes. | 01-24-2013 |
20130023549 | Pharmaceutical Compositions Comprising Nilotinib or Its Salt - A pharmaceutical composition, especially capsules, comprising granules containing nilotinib or a salt thereof with at least one pharmaceutically acceptable excipient. The granules may be produced by a wet granulation process. | 01-24-2013 |
20130023550 | PHARMACEUTICAL COMPOSITIONS AND METHODS OF MAKING SAME - Pharmaceutical compositions that include about 10 mg pazopanib/mL of the composition and about 2 to about 13% w/w of a modified cyclodextrin as well as methods of making the same are described. | 01-24-2013 |
20130040976 | INDAZOLE INHIBITORS OF THE WNT SIGNAL PATHWAY AND THERAPEUTIC USES THEREOF - Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases due to mutations in Wnt signaling components. Also provided are methods for treating Wnt-related disease states. | 02-14-2013 |
20130040977 | Pro-Neurogenic Compounds - This technology relates generally to compounds and methods for stimulating neurogenesis (e.g., post-natal neurogenesis, including post-natal hippocampal and hypothalamic neurogenesis) and/or protecting neuronal cell from cell death. Various compounds are disclosed herein. In vivo activity tests suggest that these compounds may have therapeutic benefits in neuropsychiatric and/or neurodegenerative diseases such as schizophrenia, major depression, bipolar disorder, normal aging, epilepsy, traumatic brain injury, post-traumatic stress disorder, Parkinson's disease, Alzheimer's disease, Down syndrome, spinocerebellar ataxia, amyotrophic lateral sclerosis, Huntington's disease, stroke, radiation therapy, chronic stress, abuse of a neuro-active drug, retinal degeneration, spinal cord injury, peripheral nerve injury, physiological weight loss associated with various conditions, as well as cognitive decline associated with normal aging, chemotherapy, and the like. | 02-14-2013 |
20130045986 | NOVEL COMPOUNDS AS MODULATORS OF GPR-119 - The present invention relates to novel compounds of formula (A) and (B) as modulators of GPR-119, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of GPR-119 mediated diseases or disorders with them. | 02-21-2013 |
20130059873 | PHARMACEUTICAL COMPOSITIONS AS INHIBITORS OF DIPEPTIDYL PEPTIDASE-IV (DPP-IV) - The present invention relates to compounds which inhibit dipeptidyl peptidase IV (DPP-IV) and are useful for the prevention or treatment of diabetes, especially type II diabetes, as well as hyperglycemia, Syndrome X, hyperinsulinemia, obesity, atherosclerosis, and various immunomodulatory diseases. | 03-07-2013 |
20130072509 | PTEROSTILBENE AND STATIN COMBINATION FOR TREATMENT OF METABOLIC DISEASE, CARDIOVASCULAR DISEASE, AND INFLAMMATION - A pharmaceutical composition is provided comprising a therapeutically effective amount of pterostilbene, a therapeutically effective amount of a statin compound, and a pharmaceutically acceptable carrier. The embodiments of the pharmaceutical compositions can have lipid lowering properties, or alternatively can have properties that can treat oxidative stress, by decreasing inflammation or inflammatory processes contributing to neurodegenerative diseases. A method of lowering lipid levels in an individual is also provided, comprising administering to the individual in need of such treatment a pharmaceutical composition including a therapeutically effective amount of pterostilbene, a therapeutically effective amount of a statin compound, and a pharmaceutically acceptable carrier, wherein lipid levels are decreased. | 03-21-2013 |
20130072510 | Benzoimidazol-2-yl pyrimidines and pyrazines as modulators of the histamine H4 receptor - Benzoimidazol-2-yl pyrimidines and pyrazines, pharmaceutical compositions and methods for H | 03-21-2013 |
20130079363 | COMBINATIONS OF PYRIMETHANIL AND MONOTERPENES - The present invention relates to combinations of pyrimethanil, or a salt thereof, and a monoterpene, or a salt thereof, which provide an improved biocidal effect. More particularly, the present invention relates to compositions comprising a combination of pyrimethanil, or a salt thereof, together with a monoterpene selected from thymol and β-thujaplicin in respective proportions to provide a synergistic biocidal effect. Compositions comprising these combinations are useful for the protection of any living or non-living material, such as crops, plants, fruits, seeds, objects made of wood, thatch or the like, engineering material, biodegradable material and textiles against deterioration due to the action of microorganisms such as bacteria, fungi, yeasts, algae, virusses, and the like. | 03-28-2013 |
20130090347 | ETHYNYL DERIVATIVES - The present invention relates to ethynyl derivatives of formula I | 04-11-2013 |
20130096149 | HETEROARYL COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS - The present invention provides compounds of Formula I: | 04-18-2013 |
20130109709 | METHODS OF TREATING A BRUTON'S TYROSINE KINASE DISEASE OR DISORDER | 05-02-2013 |
20130123289 | CERTAIN AMINO-PYRIMIDINES, COMPOSITIONS THEREOF, AND METHODS FOR THEIR USE - Provided are compounds of Formula I: | 05-16-2013 |
20130123290 | Pyrimidylaminobenzamide Derivatives for Treatment of Neurofibromatosis - The present invention relates to the use of pyrimidylaminobenzamide derivatives for the preparation of a drug for the treatment of non-cancerous, benign brain tumors, especially for the curative and/or prophylactic treatment of NF, and to a method of treating non-cancerous, benign brain tumors, especially for the curative and/or prophylactic treatment of NF. | 05-16-2013 |
20130131094 | PYRIMIDINE DERIVATIVES AS POSH AND POSH-AP INHIBITORS - Pyrimidine deriviatives are ubiquination inhibitors that inhibit the ubiquitin ligase activity, particularly of POSH polypeptides, are useful for the treatment of viral infections and neurological disorders. | 05-23-2013 |
20130131095 | ADMINISTRATION OF PYRIDINEDICARBOXYLIC ACID COMPOUNDS FOR STIMULATING OR INDUCING THE GROWTH OF HUMAN KERATINOUS FIBERS AND/OR ARRESTING THEIR LOSS - The invention relates to the use in a composition for caring for human hair or eyelashes of an effective amount of a pyridinedicarboxylic acid derivative of general formula (I) or of one of its salts, | 05-23-2013 |
20130131096 | 8-HYDROXY-QUINOLINE DERIVATIVES - The invention relates to compounds of the general formula (I) and their pharmaceutically acceptable salts (in which formula R | 05-23-2013 |
20130131097 | TOPICAL TREATMENT FOR CHEMOTHERAPY INDUCED EYELASH LOSS OR HYPOTRICHOSIS USING PROSTAMIDE F2 ALPHA AGONISTS - The present invention is directed to compositions and methods for the treatment of post-chemotherapeutic hypotrichosis. More specifically, the present invention is directed to the use of compositions comprising bimatoprost for the treatment of post-chemotherapeutic hypotrichosis which may be applied before, during and after receiving chemotherapeutic treatment. | 05-23-2013 |
20130137712 | Salts of 4-Methyl-N-[3-(4-methyl-imidazol-1-yl)-5-trifluoromethyl-phenyl]-- 3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-benzamide - Salts of 4-methyl-N-[3-(4-methyl-imidazol-1-yl)-5-trifluoromethyl-phenyl]-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-benzamide are prepared by various processes. | 05-30-2013 |
20130143908 | METHOD FOR PREPARING ROSUVASTATIN CALCIUM INTERMEDIATE - A method for preparing a rosuvastatin calcium intermediate represented by formula I. The method includes: hydrolyzing an ester compound represented by formula II (in which, R represents C1-C5) in the presence of a metal compound to obtain a carboxylic acid compound represented by formula III; and reducing the carboxylic acid compound in the presence of a reductant. | 06-06-2013 |
20130150393 | Statin Bioavailability Enhancement Delivery Composition - A composition for increasing the bioavailability of a statin active pharmaceutical ingredient (“API”) in humans and animals, wherein that composition includes a statin API selected from the group consisting of atorvastatin, fluvastatin, lovastatin, pitavastatin, pravastatin, rosuvastatin, and simvastatin, a first water soluble surfactant having a cloud point greater than about 37° C., a second water soluble surfactant having a cloud point greater than about 37° C., wherein a mixture of the first surfactant and the second surfactant comprises a cloud point less than about 37° C. | 06-13-2013 |
20130158057 | AMINOPYRIMIDINE DERIVATIVES AS LRRK2 MODULATORS - Compounds of the formula I: | 06-20-2013 |
20130158058 | HYPERCHOLESTEROLEMIA AND TENDINOUS INJURIES - This invention provides compositions and methods of inhibiting, suppressing, or treating a tendinous or musculoskeletal soft tissue injury. The invention further provides a method of ameliorating symptoms associated with a tendinous or musculoskeletal soft tissue injury. Additionally, the invention provides methods for evaluating the risk of developing a tendinous or musculoskeletal soft tissue injury. | 06-20-2013 |
20130158059 | NILOTINIB SALTS AND CRYSTALLINE FORMS THEREOF - Nilotinib salts and crystalline forms thereof have been prepared and characterized. | 06-20-2013 |
20130165461 | METHODS OF TREATING HEART FAILURE - Methods of treating heart failure by administration of beneficial agents to the heart. | 06-27-2013 |
20130165462 | HETEROARYL COMPOUNDS AND USES THEREOF - The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same. | 06-27-2013 |
20130165463 | INHIBITION OF FOCAL ADHESION KINASE FOR CONTROL OF SCAR TISSUE FORMATION - The formation of scars at a wound site is reduced by contacting the wound site with an effective dose of an inhibitor of focal adhesion kinase (FAK) activity or expression. Blockade of FAK is sufficient to prevent mechanical and inflammatory stimuli from activating MCP-1 pathways. In addition to these chemokine-mediated mechanisms, inhibition of FAK may control fibrosis by blocking fibroblast collagen production. Pharmacologic blockade of FAK significantly reduces scar formation in vivo. | 06-27-2013 |
20130165464 | HETEROARYLS AND USES THEREOF - This invention provides compounds of formula IB: | 06-27-2013 |
20130165465 | Crystalline Forms of 4-Methyl-N-[3-(4-methyl-imidazol-1-yl)-5-trifluoromethyl-phenyl]-3-(4-pyr- idin-3-yl-pyrimidin-2-ylamino)-benzamide - Crystalline forms of 4-methyl-N-3-(4-methyl-imidazol-1-yl)-5-trifluoromethyl-phenyl-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-benzamide free base and salts thereof are prepared by various processes. | 06-27-2013 |
20130172378 | Combination of BRAF and VEGF Inhibitors - A novel combination comprising the VEGFR inhibitor 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methylbenzenesulfonamide, or a pharmaceutically acceptable salt thereof, with a B-Raf inhibitor, particularly N-(3-[5-(2-Amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-1,3-thiazol-4-yl]-2-fluorophenyl)-2,6-difluorobenzenesulfonamide or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the same and methods of using such combinations and compositions in the treatment of conditions in which the inhibition of VEGFR and/or B-Raf is beneficial. | 07-04-2013 |
20130178491 | FUNGICIDAL COMPOSITION - A composition comprising (i) a compound of formula (I) | 07-11-2013 |
20130184300 | Methods of Treating Traumatic Brain Injury Using Pro-Neurogenic Compounds - This invention relates generally to stimulating neurogenesis (e.g., post-natal neurogenesis, e.g., post-natal hippocampal neurogenesis) and protecting from neuron cell death. | 07-18-2013 |
20130184301 | Methods of Treating Post-Traumatic Stress Disorder Using Pro-Neurogenic Compounds - This invention relates generally to stimulating neurogenesis (e.g., post-natal neurogenesis, e.g., post-natal hippocampal neurogenesis) and protecting from neuron cell death. | 07-18-2013 |
20130190339 | Pro-Neurogenic Compounds - This invention relates generally to stimulating neurogenesis (e.g., post-natal neurogenesis, e.g., post-natal hippocampal neurogenesis) and protecting from neuron cell death. | 07-25-2013 |
20130190340 | Small-Molecule-Targeted Protein Degradation - Certain aspects of the invention relate to compounds, compositions and methods that are useful for treating or preventing a disease in a subject by enhancing the degradation of a protein. In other aspects, said compounds can be useful research tools for investigating protein degradation. In other aspects, said compounds are useful research tools for investigating protein function. In certain embodiments, the degraded protein is implicated in a disease or disorder whose pathology is related at least in part to the excessive expression of the protein or the expression of a mutant form of the protein. | 07-25-2013 |
20130197017 | COMBINATIONS COMPRISING A PROTEIN KINASE INHIBITOR BEING A PYRIMIDYLAMINOBENZAMIDE COMPOUND AND A HSP90 INHIBITOR SUCH AS 17-11G - The invention provides a pharmaceutical combination comprising:
| 08-01-2013 |
20130197018 | Synergistic Fungicidal Active Substance Combinations - Novel active compound combinations comprising a carboxamide of the general formula (I) (group 1) | 08-01-2013 |
20130203792 | CO-CRYSTALS OF PYRIMETHANIL OR CYPRODINIL - The present invention relates to co-crystals of cyprodinil or pyrimethanil and a co-crystal forming compound which has at least one imide and/or oxime functional group. | 08-08-2013 |
20130210847 | PROCESS FOR THE PREPARATION OF NILOTINIB - The present invention relates a process for the preparation of a compound of formula (I): | 08-15-2013 |
20130210848 | NEW SALT OF A PYRIMIDIN DERIVATIVE - The present invention relates to a salt of a pyrimidin derivative of the acid (3R,5S,6E)-7-[4-(4-fluorophenyl)-2-(N-methylmethanesulfonamide)-6-(propan-2-yl)pyrimidin-5-yl]-3,5-dihydroxyhept-6-enoic, to a method for preparing same and to the use thereof in formulating pharmaceutical formulations. | 08-15-2013 |
20130217714 | Non-Flushing Niacin Analogues, and Methods of Use Thereof - One aspect of the present invention relates to substituted pyridines and pharmaceutically acceptable salts thereof that are active against a range of mammalian maladies. Another aspect of the invention relates to a pharmaceutical composition, comprising a compound of the present invention or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable excipient. The present invention also relates to methods of treating a range of mammalian maladies or conditions, including but not limited to hyperlipidemia, hypercholesterolemia, atherosclerosis, coronary artery disease, congestive heart failure, cardiovascular disease, hypertension, coronary heart disease, angina, pellagra, Hartnup's syndrome, carcinoid syndrome, arterial occlusive disease, obesity, hypothyroidism, vasoconstriction, osteoarthritis, rheumatoid arthritis, diabetes, Alzheimer's disease, lipodystrophy, or dyslipidemia, raising serum high-density lipoprotein (HDL) levels, and lowering serum low-density lipoprotein (LDL) levels. | 08-22-2013 |
20130217715 | DERIVATIVES OF PYRAZOLOPHENYL-BENZENESULFONAMIDE COMPOUNDS AND USE THEREOF AS ANTITUMOR AGENTS - Substituted pyrazolophenyl-benzenesulfonamide compounds of formula (I) are described, wherein m, R1, R2, R3, and R4 are defined in the description, which modulate the activity of protein kinases, These compounds find utility in treating diseases caused by deregulated protein kinase activity, such as cancer and cell proliferative disorders. | 08-22-2013 |
20130225620 | SERINE/THREONINE KINASE INHIBITORS - Compounds having the formula I wherein A, Z, R | 08-29-2013 |
20130225621 | SUBSTITUTED 2-HYDROXY-4-(2-(PHENYLSULFONAMIDO)ACETAMIDO)BENZOIC ACID ANALOGS AS INHIBITORS OF STAT PROTEIN - In one aspect, the invention relates to substituted 2-hydroxy-4-(2-(phenylsulfonamido)acetamido)benzoic acid analogs, derivatives thereof, and related compounds, which are useful as inhibitors of STAT protein activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders of uncontrolled cellular proliferation associated with a STAT protein activity dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. | 08-29-2013 |
20130225622 | Crystalline Form of Bis[(E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]- pyrimidin-5-yl](3R,5S)-3,5-dihydroxyhept-6-enoic acid] Calcium Salt - Two polymorphic forms of bis[(E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl](3R,5S)-3,5-dihydroxyhept-6-enoic acid] calcium salt, processes for making them and their use as HMG Co-A reductase inhibitors are described. | 08-29-2013 |
20130237553 | MULTICOMPONENT SYSTEM OF RESUVASTATIN CALCIUM SALT AND SORBITOL - A novel solid form of Rosuvastatin comprises as the active ingredient a salt of bis[(E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)-amino]pyrimidin-5-yl]-(3R,5S)-3,5-dihydroxyhept-6-enoic acid] and sorbitol. The crystal comprising the two components, and minor amounts of water, shows improved properties such as crystal-lization behaviour and stability. | 09-12-2013 |
20130237554 | COMBINATION - The present invention relates to a method of treating cancer in a human and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method that includes administering 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methylbenzenesulfonamide, or a pharmaceutically acceptable salt thereof, and N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecarboxamide, or a pharmaceutically acceptable salt thereof, to a human in need thereof. | 09-12-2013 |
20130245052 | NOVEL POLYMORPH OF NILOTINIB HYDROCHLORIDE - The present invention provides a novel crystalline form of nilotinib hydrochloride, process for its preparation and pharmaceutical compositions comprising it. | 09-19-2013 |
20130252987 | METHOD OF REGULATING PLASMA LIPOPROTEINS - A method of modulating the level of lipoproteins in human cells comprising the step of inhibiting resistin in the cells or cellular environment. The method is useful to treat cardiovascular disease. | 09-26-2013 |
20130252988 | COMPOSITIONS AND METHODS FOR TREATING MYELOFIBROSIS - Provided herein are compositions and methods for treating myelofibrosis in a subject. The methods comprise administering to the subject an effective amount of compound which is which is N-tert-butyl-3-[(5-methyl-2-{[4-(2-pyrrolidin-1-ylethoxy)phenyl]amino}pyrimidin-4-yl)amino]benzenesulfonamide or a pharmaceutical salt thereof or a hydrate thereof. | 09-26-2013 |
20130252989 | STABLE PHARMACEUTICAL COMPOSITION AND METHODS OF USING SAME - The present invention relates to, inter alia, pharmaceutical compositions comprising a polyunsaturated fatty acid and to methods of using the same to treat or prevent cardiovascular-related diseases. | 09-26-2013 |
20130252990 | STABLE PHARMACEUTICAL COMPOSITION AND METHODS OF USING SAME - The present invention relates to, inter alia, pharmaceutical compositions comprising a polyunsaturated fatty acid and to methods of using the same to treat or prevent cardiovascular-related diseases. | 09-26-2013 |
20130252991 | Combination - The present invention relates to methods of treating neuroblastoma, osteosarcoma, and rhabdomyosarcoma in a human and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a neuroblastoma treatment method that includes administering 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methylbenzenesulfonamide, or a pharmaceutically acceptable salt thereof, and (S)-10-[(dimethylamino)methyl]-4-ethyl-4,9-dihydroxy-1H-pyrano[3′,4′:6,7]indolizino[1,2-b]quinoline-3,14-(4H,12H)-dione, or a pharmaceutically acceptable salt thereof, to a human in need thereof. | 09-26-2013 |
20130261141 | NOVEL HETEROCYCLIC COMPOUNDS AS PESTICIDES - The present application relates to novel heterocyclic compounds, to processes for preparation thereof and to the use thereof for controlling animal pests, which also include arthropods and especially insects. | 10-03-2013 |
20130267548 | SUBSTITUTED 6-FLUORO-1H-PYRAZOLO[4,3-B]PYRIDINES AND USE THEREOF - The present application relates to novel substituted 6-fluoro-1H-pyrazolo[4,3-b]pyridines, to processes for preparation thereof, to the use thereof, alone or in combinations, for treatment and/or prophylaxis of diseases and to the use thereof for preparing Medicaments for the treatment and/or prophylaxis of diseases, especially for treatment and/or prophylaxis of cardiovascular disorders. | 10-10-2013 |
20130267549 | Use of Pyrimidylaminobenzamide Derivatives for the Treatment of Fibrosis - The invention relates to the use of a pyrimidylaminobenzamides of formula I | 10-10-2013 |
20130274276 | METHODS AND COMPOSITIONS FOR DETERMINING VIRUS SUSCEPTIBILITY TO NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS - Methods and compositions for the efficient and accurate determination of HIV susceptibility to a non-nucleoside reverse transcriptase inhibitor (NNRTI) are provided. In certain aspects, the methods involve detecting in a biological sample a nucleic acid encoding an HIV reverse transcriptase that comprises a mutation at codon 188, wherein the presence of the reverse transcriptase-encoding nucleic acid in the biological sample indicates that the HIV has a decreased susceptibility to an NNRTI. In certain embodiments, the HIV also contains one or more secondary mutations in reverse transcriptase. Also provided are methods for selecting a treatment for an HIV patient and methods for determining the selective advantage of a mutation or mutation profile. | 10-17-2013 |
20130274277 | TREATMENT FOR DISCOID LUPUS - Compounds I and II as well as salts and pharmaceutical compositions containing them are useful for treating diseases and/or disorders of the skin, such as cutaneous lupus, for example acute cutaneous lupus erythematosus, subacute cutaneous lupus erythematosus, or discoid lupus erythematosus. In certain embodiments, the compounds are provided in topical compositions. | 10-17-2013 |
20130274278 | IAP INHIBITORS - The present invention describes compounds, processes for their preparation, pharmaceutical compositions containing them, and their use in therapy. | 10-17-2013 |
20130274279 | CRYSTALLINE FORMS OF 5-CHLORO-N2-(2-ISOPROPOXY-5-METHYL-4-PIPERIDIN-4-YL-PHENYL)-N4-[2-(PROPAN- E-2-SULFONYL)-PHENYL]-PYRIMIDINE-2, 4-DIAMINE - The present invention describes specific crystalline forms of 5-chloro-N-(2-isopropoxy-5-methyl-4-(piperidin-4-ylphenyl)-N-2-(isopropylsulfonyl)phenyl)-2,4-diamine. The present invention further relates to methods for preparing said crystalline forms, pharmaceutical compositions comprising said crystalline forms, and methods of using said crystalline forms and pharmaceutical compositions to treat disease. | 10-17-2013 |
20130281475 | INHIBITORS OF C-FMS KINASE - The invention is directed to compounds of Formula I: | 10-24-2013 |
20130289058 | CYCLIC BRIDGEHEAD ETHER DGAT1 INHIBITORS - The invention relates to compounds of formula (I): | 10-31-2013 |
20130296353 | CRYSTALLINE PHARMACEUTICALLY ACTIVE INGREDIENTS - The present invention is related to crystalline forms of rosuvastatin zinc (2:1) salt. The polymorphs are suitable for use as pharmaceutically active ingredients in the treatment of the diseases of the lipid metabolism including hypercholesterolemia, hyperlipidemia, dyslipidemia or atherosclerosis. | 11-07-2013 |
20130296354 | 2,3-DIHYDROFURO[2,3-c]PYRIDINES, THEIR USE AS MODULATORS OF THE G-PROTEIN-COUPLED RECEPTOR GPR119 AND PHARMACEUTICAL COMPOSITIONS THEREOF - The present invention relates to compounds of general formula I, | 11-07-2013 |
20130296355 | GLUCAGON RECEPTOR MODULATORS - The present invention provides a compound of Formula (I) | 11-07-2013 |
20130296356 | COMBINATIONS - The present invention relates to a method of treating ovarian cancer in a female human and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a ovarian cancer treatment method that includes administering 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methylbenzenesulfonamide, or a pharmaceutically acceptable salt thereof, and 2-[(5-chloro-2-[[3-methyl-1-(1-methylethyl)-1H-pyrazol-5-yl]amino]-4-pyridinyl)amino]-N-methoxybenzamide, or a pharmaceutically acceptable salt thereof, and optionally 1,7β,10β-trihydroxy-9-oxo-5β,20-epoxytax-11-ene-2α,4,13α-triyl 4-acetate 2-benzoate 13-{(2R,3S)-3-[(tert-butoxycarbonyl)amino]-2-hydroxy-3-phenylpropanoate}, to a human in need thereof. | 11-07-2013 |
20130296357 | METHODS OF USING ALK INHIBITORS - The invention provides methods for using compounds of Formula (I) for treating an EML4-ALK | 11-07-2013 |
20130303558 | GENETIC POLYMORPHISMS ASSOCIATED WITH STROKE, METHODS OF DETECTION AND USES THEREOF - The present invention provides compositions and methods based on genetic polymorphisms that are associated with vascular diseases such as stroke. In particular, the present invention relates to genetic polymorphisms that have utility for such uses as predicting disease risk or predicting an individual's response to a treatment such as statins, including groups of polymorphisms that may be used as a signature marker set for such uses, as well as nucleic acid molecules containing the polymorphisms, variant proteins encoded by such nucleic acid molecules, reagents for detecting the polymorphic nucleic acid molecules and proteins, and methods of using the nucleic acid and proteins as well as methods of using reagents for their detection. | 11-14-2013 |
20130303559 | BENZIMIDAZOLE AND PYRAZOLOPYRIDINE DERIVATIVES FOR TREATING AND/OR PREVENTING CARDIOVASCULAR DISEASES - The present application relates to novel fused, heteroatom-bridged pyrazole and imidazole derivatives, to processes for their preparation, to their use, alone or in combination, for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular disorders. | 11-14-2013 |
20130303560 | Combination - The present invention relates to a method of treating breast cancer in a human and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a breast cancer treatment method that includes administering 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methylbenzenesulfonamide, or a pharmaceutically acceptable salt thereof, and (S)-10-[(dimethylamino)methyl]-4-ethyl-4,9-dihydroxy-1H-pyrano[3′,4′:6,7]indolizino[1,2-b]quinoline-3,14-(4H,12H)-dione, or a pharmaceutically acceptable salt thereof, to a human in need thereof. | 11-14-2013 |
20130310408 | Pesticidal Arylpyrrolidines - The invention is directed to arylpyrrolidines compounds which exhibit excellent insecticidal efficacy and which may be used as in the agrochemical field or in the vield of veterinary medicine. The compounds are represented by formula (I): | 11-21-2013 |
20130324567 | RESTORATION OF HAIR - A nonirritant composition which is useful in restoring hair and which comprises a normally solid, water-insoluble hair restorer, for example, minoxidil, a normally solid Hsieh dermal penetration-facilitator for the hair restorer, for example, pentadecalactone, and a solvent or co-solvent in which the hair restorer and the facilitator are solubilized and which does not impart to the composition irritant properties, and wherein, upon application to the surface of the skin of a recipient, the hair restorer penetrates the dermal layer of the skin and with minimal systemic delivery of the hair restorer into the blood stream of the recipient. | 12-05-2013 |
20130324568 | SUBSTITUTED INDOLYL ALKYL AMINO DERIVATIVES AS NOVEL INHIBITORS OF HISTONE DEACETYLASE - This invention comprises the novel compounds of formula (I) | 12-05-2013 |
20130331407 | INHIBITORS OF PROTEIN KINASES - The present invention relates to inhibitors of cyclin-dependent kinases and therapeutic applications thereof. Furthermore, the invention relates to methods of preventing and/or treating any type of pain, inflammatory disorders, immunological diseases, proliferative diseases, infectious diseases, cardiovascular diseases and neurodegenerative diseases comprising the administration of an effective amount of at least one inhibitor of cyclin-dependent kinases. | 12-12-2013 |
20130338179 | DIAMINOPYRIMIDINE DERIVATIVES AND PROCESSES FOR THE PREPARATION THEREOF - The present invention provides a diaminopyrimidine derivative or its pharmaceutically acceptable salt, a process for the preparation thereof, a pharmaceutical composition comprising the same, and a use thereof. The diaminopyrimidine derivative or its pharmaceutically acceptable salt functions as a 5-HT | 12-19-2013 |
20130338180 | FORMULATION COMPRISING PHENYLAMINOPYRIMIDINE DERIVATIVE AS ACTIVE AGENT - An oral pharmaceutical formulation containing an effective amount of NRC-AN-019 including its pharmaceutically acceptable salts and polymorphs such as Form I, Form II and Form III thereof to improve the bioavailability intended for self-emulsification upon its contact with the gastro-intestinal fluid. The invention also relates to a process for the preparation of oral solution containing NRC-AN-019 in an effective concentration for the better therapy against Chronic Myeloid Leukemia as BCR-ABL tyrosine kinase inhibitor and against other tumors such as head and neck cancer, prostate cancer and the like. | 12-19-2013 |
20130345245 | SUBSTITUTED PYRIMIDINYLPYRROLOPYRIDINONE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS KINASE INHIBITORS - Pyrimidinylpyrrolopyridinone derivatives of formula (I) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer. | 12-26-2013 |
20140011825 | Compounds and Compositions as Protein Kinase Inhibitors - The present invention provides compounds of Formula I or II: | 01-09-2014 |
20140018379 | PYRIMIDINE DERIVATIVES - The present invention provides a compound of Formula I or Formula VI: | 01-16-2014 |
20140018380 | BICYCLIC HETEROARYL COMPOUNDS AS GPR119 RECEPTOR AGONISTS - The present invention provides a new class of bicyclic heteroaryl compounds represented by Formula I, pharmaceutical compositions containing these compounds, and their use for modulating the activity of GPR119 in the treatment of metabolic disorders and complications thereof, as well as methods for the treatment of the metabolic disorders and complications thereof. | 01-16-2014 |
20140018381 | Use of Rosuvastatin Lactols as Medicaments - This invention relates to the discovery of novel rosuvastatin analogues. More specifically, the invention relates to novel rosuvastatin analogues which have utility in treating conditions treatable by the inhibition of HMG-CoA reductase. | 01-16-2014 |
20140024667 | FUNGICIDAL COMPOSITIONS - A composition for control of phytopathogenic diseases on useful plants or on propagation material thereof, that, in addition to customary inert formulation adjuvants, comprises as active ingredient a mixture of component (A) and a synergistically effective amount of component (B), wherein
| 01-23-2014 |
20140024668 | FUNGICIDAL COMPOSITIONS - A composition for control of phytopathogenic diseases on useful plants or on propagation material thereof, that, in addition to customary inert formulation adjuvants, comprises as active ingredient a mixture of component (A) and a synergistically effective amount of component (B), wherein | 01-23-2014 |
20140031377 | MULTICOMPONENT CRYSTALLINE SYSTEM OF ROSUVASTATIN CALCIUM SALT AND VANILLIN - A novel solid form of Rosuvastatin comprises as the active ingredient a salt of bis[(E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)-amino]pyrimidin-5-yl]-(3R,5S)-3,5-dihydroxyhept-6-enoic acid] and vanillin or vanillin derivatives. The crystal comprising the two components, and minor amounts of water, shows improved properties such as crystallization behavior stability and decreased hydroscopic behavior. | 01-30-2014 |
20140038994 | Salts of 4-Methyl-N-[3-(4-methyl-imidazol-1-yl)-5-trifluoromethyl-phenyl]-- 3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-benzamide - Salts of 4-methyl-N-[3-(4-methyl-imidazol-1-yl)-5-trifluoromethyl-phenyl]-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-benzamide are prepared by various processes. | 02-06-2014 |
20140038995 | Benzoimidazol-2-yl pyrimidines and pyrazines as modulators of the histamine H4 receptor - Benzoimidazol-2-yl pyrimidines and pyrazines, pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H | 02-06-2014 |
20140038996 | Freeze Dried Drug Nanosuspensions - The present invention relates to a freeze-dried (also called lyophilized) drug nanosuspension. The present freeze-dried drug nanosuspension composition has an acceptable stability of the particle size distribution during storage, including long term storage. | 02-06-2014 |
20140051716 | COMPOUNDS AND METHODS FOR IMPROVING IMPAIRED ENDOGENOUS FIBRINOLYSIS USING HISTONE DEACETYLASE INHIBITORS - There is provided a compound which is a histone deacetylase (HDAC) inhibitor, or a pharmaceutically acceptable ester, amide, solvate or salt thereof, for use in: (I) treating or preventing a pathological condition associated with excess fibrin deposition and/or thrombus formation; and/or (II) potentiating the degradation of fibrin deposits and preventing such deposits associated with pathological conditions or which may lead to such conditions, wherein the HDAC inhibitor, and the dose thereof, is as described in the description. There is also provided valproic acid, or a pharmaceutically acceptable salt thereof, for use in improving or normalizing endogenous fibrinolysis impaired by local or systemic inflammation. | 02-20-2014 |
20140057929 | BESYLATE SALT OF A BTK INHIBITOR - The present invention provides a salt form, and compositions thereof, useful as an inhibitor of one or more protein kinases and which exhibits desirable characteristics for the same. | 02-27-2014 |
20140066469 | TREATMENT OF DISEASES ASSOCIATED WITH INFLAMMATION - Compositions and methods are provided for preventing or treating the pre-clinical early-stages of inflammatory diseases, including autoimmune diseases, degenerative inflammatory diseases, metabolic inflammatory diseases, chronic infection associated with inflammation, cancer associated with inflammation, and other inflammatory diseases by administration to an individual of an effective dose of a synergistic combination of active agents comprising or consisting essentially of an aminoquinoline, e.g. hydroxychloroquine, and a statin, e.g. atorvastatin. Each or both of the active agents can be formulated in various ways, including without limitation a solid oral dosage form. | 03-06-2014 |
20140073659 | TREATMENT FOR VITILIGO - Compounds I and II, as well as prodrugs, hydrates, solvates, N-oxides, salts and pharmaceutical compositions containing them, are useful for treating vitiligo. In certain embodiments, the compounds are provided in topical compositions. | 03-13-2014 |
20140073660 | Pyrimidylaminobenzamide Derivatives for Treatment of Neurofibromatosis - The present invention relates to the use of pyrimidylamlnobenzamide derivatives for the preparation of a drug for the treatment of non-cancerous, benign brain tumors, especially for the curative and/or prophylactic treatment of NF, and to a method of treating non-cancerous, benign brain tumors, especially for the curative and/or prophylactic treatment of NF. | 03-13-2014 |
20140073661 | HETEROCYCLIC COMPOUNDS AND USES THEREOF - The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same. | 03-13-2014 |
20140080850 | PHARMACEUTICAL COMPOSITION COMPRISING AN OMEGA-3 FATTY ACID AND A HYDROXY-DERIVATIVE OF A STATIN AND METHODS OF USING SAME - In various embodiments, the present invention provides compositions and methods for treating and/or preventing a cardiovascular-related disease in subject in need thereof. | 03-20-2014 |
20140080851 | Benzene Sulfonamide Thiazole and Oxazole Compounds - The present invention provides thiazole sulfonamide and oxazole sulfonamide compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents. | 03-20-2014 |
20140088126 | Rosuvastatin Enantiomer Compounds - The invention discloses a method for the treatment of diseases, particularly those diseases characterized by diminished or aberrant cellular function, including AIDS, cancer, and Alzheimer's Disease. The method comprises administering a therapeutically effective amount of rosuvastatin enantiomer compounds in their (3R, 5R), (3S, 5R), or (3S, 5S) configurations, or pharmaceutically acceptable salts thereof. Biologically-active rosuvastatin enantiomer compounds with (3R, 5R), (3S, 5R), and (3S, 5S) stereochemistry are also disclosed. | 03-27-2014 |
20140094480 | Pro-Neurogenic Compounds - This invention relates generally to stimulating neurogenesis (e.g., post-natal neurogenesis, e.g., post-natal hippocampal neurogenesis) and protection from neuron cell death. | 04-03-2014 |
20140113923 | NOVEL ANTIVIRAL THERAPIES - The field of the invention relates to the use of carbohydrate binding compounds as a medicine, their use to treat or prevent viral infections, their use to manufacture a medicine to treat or prevent viral infections and their use in a vaccination strategy. The present invention relates to the use of said compounds to manufacture a medicine to treat or prevent viral infections of subject, more in particular infections with viruses having glycosilated envelope proteins such as Retroviridae (i.e., Lentivirinae), like HIV (human immunodeficiency virus), Flaviviridae, like HCV (hepatitis C virus), Hepadnaviridae, like HBV (hepatitis B virus), Coronaviridae, like SARS corona virus, and Orthomyxoviridae, like influenza A, B, or C. | 04-24-2014 |
20140121229 | COMBINATION COMPRISING S-[2-([[1-(2-ETHYLBUTYL)CYCLOHEXYL] CARBONYL]AMINO)PHENYL] 2-METHYLPROPANETHIOATE AND AN HMG COA REDUCTASE INHIBITOR - The invention provides a combination comprising (a) S-[2-([[1-(2-ethylbutyl)cyclohexyl]carbonyl]amino)phenyl]2-methylpropanethioate or prodrug of the active form thereof, and (b) at least one HMG CoA reductase inhibitor. Also provided are a pharmaceutical composition, package, and a kit comprising the aforementioned active ingredients, as well as a method for treatment and prophylaxis of a cardiovascular disorder involving the use of the aforementioned active ingredients. | 05-01-2014 |
20140121230 | TOPICAL PARASITICIDAL FORMULATION - The present invention relates to topical parasiticidal formulations comprising a parasiticide, an organo-silicone surfactant and a topically acceptable liquid carrier, and methods of preventing or treating parasites on an animal. | 05-01-2014 |
20140128418 | PYRAZOLE DERIVATIVES, PREPARATION METHOD THEREOF, AND COMPOSITION FOR PREVENTING AND TREATING OSTEOPOROSIS CONTAINING SAME - The present invention provides a pyrazole derivative compound and a pharmaceutically acceptable salt thereof. The compound of the invention is remarkably effective for preventing and treating osteoporosis. | 05-08-2014 |
20140142127 | Stable Compositions of HMG-COA Reductase Inhibitors and Omega-3 Oils - Disclosed are stable formulations of omega-3 oils and HMG-CoA reductase inhibitors. The invention comprises an omega-3 oil, a salt form of an HMG-CoA reductase inhibitor, and a salt. These compositions are stable in liquid form useful for combination therapy. | 05-22-2014 |
20140142128 | METHODS OF TREATING A DISEASE OR DISORDER ASSOCIATED WITH BRUTON'S TYROSINE KINASE - The present invention provides methods of treating, stabilizing or lessening the severity or progression of a disease or disorder associated with BTK. | 05-22-2014 |
20140142129 | METHODS OF TREATING A DISEASE OR DISORDER ASSOCIATED WITH BRUTON'S TYROSINE KINASE - The present invention provides methods of treating, stabilizing or lessening the severity or progression of a disease or disorder associated with BTK. | 05-22-2014 |
20140142130 | COMBINATIONS OF PYRIMETHANIL AND MONOTERPENES - The present invention relates to combinations of pyrimethanil, or a salt thereof, and a monoterpene, or a salt thereof, which provide an improved biocidal effect. More particularly, the present invention relates to compositions comprising a combination of pyrimethanil, or a salt thereof, together with a monoterpene selected from thymol and β-thujaplicin in respective proportions to provide a synergistic biocidal effect. Compositions comprising these combinations are useful for the protection of any living or non-living material, such as crops, plants, fruits, seeds, objects made of wood, thatch or the like, engineering material, biodegradable material and textiles against deterioration due to the action of microorganisms such as bacteria, fungi, yeasts, algae, viruses, and the like. | 05-22-2014 |
20140155421 | SUBSTITUTED PYRIMIDINYL-PYRROLES ACTIVE AS KINASE INHIBITORS - The present invention relates to substituted pyrimidinyl-pyrrole compounds of formula (I) which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular Janus kinases. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such compounds or the pharmaceutical compositions containing them. | 06-05-2014 |
20140187570 | NOVEL FORMULATIONS OF PYRIMETHANIL, AND THEIR USE IN TREATMENT OF CROPS - Solutions and emulsions of pyrimethanil and essential oils, and their use in fungicidal treatment of crops. | 07-03-2014 |
20140194450 | TOPICAL TREATMENT FOR CHEMOTHERAPY INDUCED EYELASH LOSS OR HYPOTRICHOSIS USING PROSTAMIDE F2 ALPHA AGONISTS - The present invention is directed to compositions and methods for the treatment of post-chemotherapeutic hypotrichosis. More specifically, the present invention is directed to the use of compositions comprising bimatoprost for the treatment of post-chemotherapeutic hypotrichosis which may be applied before, during and after receiving chemotherapeutic treatment. | 07-10-2014 |
20140194451 | Cdc42 Inhibitor and Uses Thereof - Compounds which inhibit the small G protein Rho GTPase cell division cycle protein Cdc42 are provided. Morphological analyses of filopodia, western blots of Ccd42 phosphorylation, and effects on cellular wound healing and on growth cone formation all demonstrate that the described compounds are able to inhibit all tested Cdc42-mediated processes. The compounds effectively inhibit, the effects of Cdc42 and effectively inhibit Cdc42-related cellular functions involving actin, such as Golgi organization and cell movement. Furthermore, the described Cdc42 inhibitor compounds may be provided as a medicament for the treatment of various conditions. | 07-10-2014 |
20140194452 | Pyrazolyl-Based Carboxamides II - The invention relates to pyrazolyl-based carboxamide compounds useful as ICRAC inhibitors, to pharmaceutical compositions containing these compounds and to these compounds for the use in the treatment and/or prophylaxis of diseases and/or disorders, in particular inflammatory diseases and/or inflammatory disorders. | 07-10-2014 |
20140194453 | MULTICOMPONENT CRYSTALLINE SYSTEM OF ROSUVASTATIN CALCIUM SALT AND VANILLIN - A novel solid form of Rosuvastatin comprises as the active ingredient a salt of bis[(E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)-amino]pyrimidin-5-yl]-(3R,5S)-3,5-dihydroxyhept-6-enoic acid] and vanillin or vanillin derivatives. The crystal comprising the two components, and minor amounts of water, shows improved properties such as crystallization behavior stability and decreased hydroscopic behavior. | 07-10-2014 |
20140206708 | COMPOSITION FOR OPHTHALMIC ADMINISTRATION - Disclosed herein are embodiments of a composition useful for treating and/or preventing dry eye disorders. The disclosed composition comprises components that maintain the composition's chemical and/or physical properties thereby providing a composition suitable for use. | 07-24-2014 |
20140206709 | CERTAIN AMINO-PYRIMIDINES, COMPOSITIONS THEREOF, AND METHODS FOR THEIR USE - Provided are compounds of Formula I: | 07-24-2014 |
20140221411 | 2-HYDROXYARYLAMIDE DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING CANCER CONTAINING SAME AS ACTIVE INGREDIENT - The present invention relates to a 2-hydroxyarylamide derivative or a pharmaceutically acceptable salt thereof, a preparation method thereof, and a pharmaceutical composition for preventing or treating cancer comprising the same as an active ingredient. The 2-hydroxyarylamide derivative prepared by the present invention is excellent in the inhibition of the activity of TMPRSS4 serine protease and the suppression of the infiltration of TMPRSS4-expressed cancer cells, and thus can be useful as a composition for preventing or treating cancer by inhibiting TMPRSS4 over-expressed in cancer cells, particularly, colorectal cancer, lung cancer, breast cancer, prostate cancer, ovarian cancer, pancreatic cancer, or stomach cancer cells. | 08-07-2014 |
20140256758 | METHODS FOR REDUCING THE RISK OF AN ADVERSE TERIFLUNOMIDE AND ROSUVASTATIN INTERACTION IN MULTIPLE SCLEROSIS PATIENTS - This invention relates to a method for managing the risk of an adverse interaction between teriflunomide and a substrate of breast cancer resistance protein (BCRP) and/or organic anion transporting polypeptide B1 and B3 (OATP1B1/B3). | 09-11-2014 |
20140256759 | KINASE INHIBITOR AND METHOD FOR TREATMENT OF RELATED DISEASES - Disclosed is a compound of (aminophenylamino) pyrimidyl benzamides and a synthesis method thereof. The compound has Btk-inhibition activity and can be used to treat autoimmune diseases, heteroimmune diseases, cancers or thromboembolic diseases. | 09-11-2014 |
20140275135 | SALTS AND SOLID FORMS OF ISOQUINOLINONES AND COMPOSITION COMPRISING AND METHODS OF USING THE SAME - Solid forms of chemical compounds that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein. Also provided herein are processes for preparing compounds, solid forms thereof, and pharmaceutical compositions thereof. | 09-18-2014 |
20140275136 | Method of Treating a Proliferative Disease - The present invention relates to a method of treating a patient with a serine/threonine kinase inhibitor wherein resistance to the treatment with a serine/threonine kinase inhibitor is suppressed by administering the serine/threonine kinase inhibitor on an intermittent dosing schedule. | 09-18-2014 |
20140288109 | MK2 INHIBITORS - The present invention relates to compounds of general Formula (I) or a pharmaceutically acceptable salt thereof. The compounds can be used in the treatment of immune, autoimmune, inflammatory diseases, cardiovascular diseases, infectious diseases, bone resorption disorders, neurodegenerative diseases or proliferative diseases. | 09-25-2014 |
20140309247 | Systems And Methods For Detecting Scalp Follicular Inflammation In Humans - Methods, processes, systems, and apparatuses are disclosed for detecting biomarkers associated with the inflammation response in the pilosebaceous unit of the human scalp using plucked human hair and an enzyme activity assay which may for example be colorimetric or fluorometric. | 10-16-2014 |
20140309248 | SUBSTITUTED INDOLYL ALKYL AMINO DERIVATIVES AS INHIBITORS OF HISTONE DEACETYLASE - This invention comprises the novel compounds of formula (I) | 10-16-2014 |
20140309249 | INHIBITORS OF C-JUN-N-TERMINAL KINASE (JNK) - The present invention provides novel compounds according to Formula (I): where Ring A, Ring B, X, L | 10-16-2014 |
20140309250 | Pharmaceutical Formulations - This invention relates to solid oral pharmaceutical formulations of (S)-methyl (1-((4-(3-(5-chloro-2-fluoro-3-(methylsulfonamido)phenyl)-1-isopropyl-1H-pyrazol-4-yl)pyrimidin-2-yl)amino)propan-2-yl)carbamate (COMPOUND A) and the use of the formulations for treating proliferative diseases, such as solid tumor diseases. | 10-16-2014 |
20140323509 | 2-HETEROCYCLYLAMINOALKYL-(P-QUINONE) DERIVATIVES FOR TREATMENT OF OXIDATIVE STRESS DISEASES - Methods of treating or suppressing oxidative stress disorders including mitochondrial diseases, impaired energy processing disorders, neurodegenerative diseases and diseases of aging are disclosed, as well as compounds useful in the methods of the invention, such as 2-heterocyclylaminoalkyl-(p-quinone) derivatives. | 10-30-2014 |
20140329842 | Protein Kinase C Inhibitors and Uses Thereof - This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes. | 11-06-2014 |
20140336211 | Crystalline forms of 2-(2-methylamino-pyrimidin-4-yl)-1H-Indole-5-carboxylic acid [ (S)-1-carbamoyl-2-(phenyl-pyrimidin-2-yl-amino) -ethyl ] -amide - The present invention relates to polymorphs and hydrates of 2-(2-methylamino-pyrimidin-4-yl)-1H-indole-5-carboxylic acid [(S)-1-carbamoyl-2-(phenyl-pyrimidin-2-yl-amino)-ethyl]-amide, processes for their preparation and their use, in particular in pharmaceutical compositions. | 11-13-2014 |
20140343085 | USE OF ARYL DERIVATIVES FOR CONTROLLING ECTOPARASITES - The present invention relates to the use of compounds of formula (I), wherein the variables are as defined in the description, in the free form or in salt form, for the manufacture of a medicament for controlling ectoparasites on a warm-blooded animal, wherein said medicament is administered orally to the animal at a dose of from 0.1 to 100 mg/kg from 30 minutes before to 3 hours after feeding the animal with an animal food. | 11-20-2014 |
20140343086 | COMPOUNDS AND COMPOSITIONS FOR INHIBITING THE ACTIVITY OF ABL1, ABL2 AND BCR-ABL1 - The present invention relates to compounds of formula (I): | 11-20-2014 |
20140343087 | Crystalline Forms of 4-Methyl-N-[3-(4-methyl-imidazol-1-yl)-5-trifluoromethyl-phenyl]-3-(4-pyr- idin-3-yl-pyrimidin-2-ylamino)-benzamide - Crystalline forms of 4-methyl-N-[3-(4-methyl-imidazol-1-yl)-5-trifluoromethyl-phenyl]-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-benzamide free base and salts thereof are prepared by various processes. | 11-20-2014 |
20140350037 | METHOD OF TREATING PROLIFERATIVE DISORDERS AND OTHER PATHOLOGICAL CONDITIONS MEDIATED BY BCR-ABL, C-KIT, DDR1, DDR2 OR PDGF-R KINASE ACTIVITY - The present invention relates to a regimen for the administration of a pyrimidylaminobenzamide of formula I as defined herein for the treatment of proliferative disorders, particularly solid and liquid tumors, and other pathological conditions mediated by the Bcr-Abl oncoprotein, the cell transmembrane tyrosine kinase receptor c-Kit, DDR1 (discoidin domain receptor 1), DDR2 (discoidin domain receptor 2) or PDGF-R (platelet derived growth factor receptor) kinase activity. | 11-27-2014 |
20140350038 | RILPIVIRINE HYDROCHLORIDE - The present invention provides a novel process for the preparation of rilpivirine. The present invention also provides a novel process for the preparation of rilpivirine hydrochloride. The present invention further provides a rilpivirine hydrochloride monohydrate, process for its preparation and pharmaceutical compositions comprising it. | 11-27-2014 |
20140350039 | COMBINATION - The present invention relates to a method of treating cancer in a human and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method that includes administering N-{3-[5-(2-Amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-1,3-thiazol-4-yl]-2-fluorophenyl}-2,6-difluorobenzenesulfonamide or a pharmaceutically acceptable salt thereof, and N-{(1S)-2-amino-1-[(3,4-difluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-furancarboxamide, or a pharmaceutically acceptable salt thereof, to a human in need thereof. | 11-27-2014 |
20140357653 | CHEMICAL COMPOUNDS - The invention relates to a novel compound of formula (I) or a stereoisomer, or a racemate or a mixture or a pharmaceutically acceptable salt thereof: wherein: R is phenyl or a 5- or 6-membered heteroaryl ring containing 1 to 3 heteroatoms selected from S, N and O, such rings may be optionally substituted with n groups Q; Q is selected from a group consisting of: C1-C4 alkyl, halogen, halo C1-C4 alkyl, C1-C4 alkoxy, CN, SO | 12-04-2014 |
20140371251 | METHOD OF INHIBITING DYRK1B - The present invention relates to a DYRK1B inhibitor for use in the treatment of cancer, wherein in said cancer and/or in cells of said cancer the hedgehog signaling pathway is activated, and in particular the activation of the hedgehog signaling pathway is independent of signaling by the G protein-coupled receptor Smoothened. | 12-18-2014 |
20140378493 | Fused Bicyclic Oxazolidinone CETP Inhibitor - Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. | 12-25-2014 |
20150011575 | METHODS AND COMPOSITIONS FOR MODULATING IRE1, SRC, AND ABL ACTIVITY - Disclosed herein are, inter alia, compositions for modulating Ire1, Src, or Abl, methods for identifying modulating activity in test compounds, and methods for treating diseases caused by the activity or inactivity of Ire1, Src, or Abl. | 01-08-2015 |
20150011576 | Inhibitors of Protein Kinases - The present invention relates to inhibitors of cyclin-dependent kinases and therapeutic applications thereof. Furthermore, the invention relates to methods of preventing and/or treating any type of pain, inflammatory disorders, immunological diseases, proliferative diseases, infectious diseases, cardiovascular diseases and neurodegenerative diseases comprising the administration of an effective amount of at least one inhibitor of cyclin-dependent kinases. | 01-08-2015 |
20150018378 | FADS REGULATION - The present invention relates methods to increase the expression of fatty acid desaturases (FADS) and increase cellular and tissue levels of highly unsaturated fatty acids (HUFA) by modulating one or more of the FADS via the action of specific classes of drugs (e.g., statins and LXR agonists). The present invention also relates to methods of treating conditions (e.g., tumor and cancer) involving deficient function of FADS by administering statins and/or LXR agonists. The present invention further relates to methods of determining the need for statins or dietary LCPUFA in subjects. | 01-15-2015 |
20150025095 | Diaminopyrimidines And Uses Thereof - This disclosure relates to: (a) compounds and salts thereof that, inter alia, inhibit RSV infection and/or replication; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions. | 01-22-2015 |
20150025096 | SMALL MOLECULE COMPOUNDS TO TREAT HEARING LOSS - The invention is directed, in part, to compositions comprising small molecule compounds to treat or prevent hearing loss. Compositions of the present invention also promote sensory hair cell regeneration. Particular compositions comprise ellipticine derivatives, and optionally one or more small molecules that increase Atoh1 expression or activity, and optionally one or more growth factors. | 01-22-2015 |
20150025097 | METHODS OF REDUCING HAIR LOSS AND/OR FACILITATING HAIR GROWTH AND/OR REGROWTH - The present disclosure relates to methods of retarding hair loss or facilitating hair growth and/or regrowth. More specifically, the present disclosure relates to methods of using the disclosed compositions to increase the rate of terminal hair growth and/or regrowth in a mammal. | 01-22-2015 |
20150038523 | INTEGRIN ANTAGONIST CONJUGATES FOR TARGETED DELIVERY TO CELLS EXPRESSING ALPHA-V-BETA-3 - The invention relates to compounds of formula (I): wherein R | 02-05-2015 |
20150045379 | INDAZOLE INHIBITORS OF THE WNT SIGNAL PATHWAY AND THERAPEUTIC USES THEREOF - Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases due to mutations in Wnt signaling components. Also provided are methods for treating Wnt-related disease states. | 02-12-2015 |
20150045380 | REVERSE AMIDE COMPOUNDS AS PROTEIN DEACETYLASE INHIBITORS AND METHODS OF USE THEREOF - The present invention relates to novel “reverse amide” compounds comprising a zinc chelator group, and the use of such compounds in the inhibition of HDAC6 and in the treatment of various diseases, disorders or conditions related to HDAC6. | 02-12-2015 |
20150051235 | Compositions and Methods for Treating Cardiovascular Diseases - The present specification discloses pharmaceutical compositions, methods of preparing such pharmaceutical compositions, and methods and uses of treating a cardiovascular disease in an individual using such pharmaceutical compositions. | 02-19-2015 |
20150051236 | Combinations Useful for the Treatment of Chronic Lymphocytic Leukemia - The invention relates to a combination which comprises (a) a DNA damaging agent; and (b) 4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidioyl]amino]-N-[5-(4-methyl-1H-imidazol-1-yl)-3-(trifluoromethyl)phenyl]benzamide (“nilotinib”); a pharmaceutical composition comprising such a combination and optionally at least one pharmaceutical acceptable carrier for simultaneous, separate or sequential use, in particular for the treatment chronic lymphocytic leukemia (CLL); the use of such a combination for the preparation of a medicament for the treatment of CLL; a commercial package or product comprising such a combination; and to a method of treatment of a warm-blooded animal, especially a human. | 02-19-2015 |
20150051237 | PYRIDYL-AND PYRIMIDINYL-SUBSTITUTED PYRROLE-, THIOPHENE- AND FURANE-DERIVATIVES AS KINASE INHIBITORS - The present invention provides compounds of the formula (I), or the pharmaceutically acceptable salts thereof, wherein G, W, R | 02-19-2015 |
20150051238 | PYRAZOLE AMINOPYRIMIDINE DERIVATIVES AS LRRK2 MODULATORS - Pyrazole compounds that are modulators of LRRK2, methods of making the compounds, and methods for using the compounds for treatment of diseases associated with LRRK2 receptor, such as Parkinson's disease. | 02-19-2015 |
20150057301 | Pro-Neurogenic Compounds - This invention relates generally to stimulating neurogenesis (e.g., post-natal neurogenesis, e.g., post-natal hippocampal neurogenesis) and protectiong from neuron cell death. | 02-26-2015 |
20150065533 | Benzyl-substituted carbamates and use thereof - The present application relates to novel benzyl-substituted carbamates, to processes for their preparation, to their use, alone or in combinations, for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prophylaxis of cardiovascular disorders. | 03-05-2015 |
20150065534 | INTEGRIN ANTAGONIST CONJUGATES FOR TARGETED DELIVERY TO CELLS EXPRESSING LFA-1 - The invention relates to compounds of formula (I), wherein R1, R2, and n are defined in the detailed description and claims. In particular, the present invention relates to the compounds of formula I for use in the manufacture and delivery of conjugated moieties such as small molecules, peptides, nucleic acids, fluorescent moieties, and polymers which are linked to LFA-1 integrin antagonists to target cells expressing LFA-1. | 03-05-2015 |
20150073005 | COMPOSITION FOR HAIR GROWTH - To provide a composition for hair growth (hair growth agent) which has high hair growing effects and can be used for prevention or treatment of alopecia. The composition for hair growth comprises as an active ingredient at least one member selected from the group consisting of a compound represented by the formula (1) and a salt thereof. In the formula, R is a carboxy group or an alkoxycarbonyl group. | 03-12-2015 |
20150073006 | OLIGOMER-PROTEIN TYROSINE KINASE INHIBITOR CONJUGATES - The invention relates to (among other things) oligomer-PTK inhibitor conjugates and related compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits advantages over PTK inhibitor compounds lacking a water-soluble, non-peptidic oligomer. | 03-12-2015 |
20150094322 | SUSTAINED-RELEASE FORMULATIONS OF COLCHICINE AND METHODS OF USING SAME - Pharmaceutical compositions of colchicine for once-a-day oral administration are provided. The formulations comprise a sustained-release component and an optional immediate-release component, the compositions of which can be selectively adjusted, respectively, to release the active ingredient along a pre-determined or desired release profile. Methods of treating or preventing cardiovascular disease and/or inflammatory disease in mammalian subjects comprising the administration of the novel formulations disclosed herein are also provided. | 04-02-2015 |
20150094323 | METHODS OF TREATING AND/OR PREVENTING CARDIOVASCULAR DISEASE - Methods of treating or preventing cardiovascular disease and/or inflammatory disease in mammalian subjects comprising the administration of the novel formulations disclosed herein are provided. | 04-02-2015 |
20150099770 | CARBOXYLIC ACID COMPOUNDS - The present disclosure concerns at least one entity chosen from compounds of Formula (I) and pharmaceutically acceptable salts thereof: (I) wherein the variable groups X, R1, R2, R3 m, n and p are as defined herein. The present disclosure also relates to methods for the preparation of at least one such entity, and intermediates useful in the preparation thereof, to pharmaceutical compositions containing at least one such entity, to the use of at least one such entity in the preparation of medicaments, and to the use of at least one such entity in the treatment of conditions such as, for example, allergic diseases, autoimmune diseases, viral diseases, and cancer. | 04-09-2015 |
20150105413 | THERAPEUTIC COMPOUNDS - The present invention relates to compounds of formula (I): wherein R | 04-16-2015 |
20150105414 | HAIR GROWTH AND/OR REGROWTH COMPOSITIONS - The present disclosure relates to compositions containing certain pyrimidine compounds such as minoxidil and/or certain pyrimidine sulfate (inner salt) compounds such as minoxidil sulfate and especially compositions containing pyrimidine compounds in combination with an admixtures comprising at least one antioxidant, at least one organic acid and a select fatty acid mixture. The present disclosure also relates to use of the compositions to grow and/or regrow hair and/or prevent hair loss in mammals and particularly in humans. | 04-16-2015 |
20150111912 | 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. | 04-23-2015 |
20150111913 | METHOD AND APPARATUS FOR DELIVERY OF A MEASURED DOSAGE OF A NON-AEROSOL, NON-SPRAY FOAM COMPOSITION OF MINOXIDIL - A non-pressurized container that contains one or more of: a foamable composition of minoxidil, or a pharmaceutically acceptable salt thereof, and a dihydrotestosterone blocker in a formulation with a precise density and viscosity to yield a foam with a temperature sensitivity and shear strength designed for inverted application and immediate targeted release at body temperature under a minimal hand applied pressure to the scalp. | 04-23-2015 |
20150119413 | TREATMENT OF POLYCYSTIC DISEASES WITH AN HDAC6 INHIBITOR - An HDAC6-specific inhibitor (i.e., a compound of Formula I or II) is shown to reduce the pathogenesis associated with polycystic disease. Administration of an HDAC6-specific inhibitor attenuated many of the symptoms characteristic of polycystic liver disease including cyst formation, cyst growth and cholangiocyte proliferation. Treatment with a HDAC6-specific inhibitor also increased the amount of bile duct acetylated tubulin and β-catenin phosphorylation and/or acetylation while reducing bile duct β-catenin synthesis. These results demonstrate that HDAC6 is overexpressed in cystic cholangiocytes and that its pharmacological inhibition reduces cholangiocyte proliferation and cyst growth. | 04-30-2015 |
20150119414 | STATIN AND OMEGA 3 FATTY ACIDS FOR REDUCTION OF APOLIPOPROTEIN-B LEVELS - A composition and a method of treatment utilizing a combination of statins (or HMG-CoA reductase inhibitors), a class of drug used to lower cholesterol levels by inhibiting the enzyme HMG-CoA reductase, with mixtures of an omega-3 fatty acid formulation containing about 90% or more omega 3 fatty acids by weight including a combination of Eicosapentaenoic acid (EPA), Docosapentaenoic acid (DPA) and Docosahexaenoic acid (DHA) in a weight ratio of EPA:DHA of from 5.7 to 6.3, wherein the sum of the EPA, DHA and DPA represent about 82% by weight of the total formulation and about 92% of the total omega 3 fatty acid content of the composition are taught. | 04-30-2015 |
20150133478 | C-RAF MUTANTS THAT CONFER RESISTANCE TO RAF INHIBITORS - Nucleic acids and proteins having a mutant C-RAF sequence, and methods of identifying patients having cancer who are likely to benefit from a combination therapy and methods of treatment are provided. | 05-14-2015 |
20150133479 | PYRIMIDINYLPIPERIDINYLOXYPYRIDONE ANALOGUES AS GPR119 MODULATORS - Novel compounds of structure Formula I: (I) or an enantiomer, a diastereomer, or a pharmaceutically acceptable salt thereof, wherein R1, R2 and R3 are defined herein, are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. Thus, the disclosure also concerns compositions comprising these novel compounds and methods of treating diseases or conditions related to the activity of the GPR119 G protein-coupled receptor by using any of these novel compounds or a composition comprising any of such novel compounds. | 05-14-2015 |
20150141448 | Topical Ophthalmological Pharmaceutical Composition containing Pazopanib - The present invention relates to topical ophthalmological pharmaceutical compositions containing pazopanib, a hydrate, solvate or pharmaceutically acceptable salt thereof or a polymorph thereof and its process of preparation and its use for treating ophthalmological disorders. | 05-21-2015 |
20150141449 | KEY INTERMEDIATES FOR THE SYNTHESIS OF ROSUVASTATIN OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF - The present invention relates in general to the field of organic chemistry and in particular to the preparation of N-(4-(4-fluorophenyl)-6-isopropyl-5-methylpyrimidin-2-yl)-N-methylmethanesulfonamide (I), N-(4-(4-fluorophenyl)-5-(bromomethyl)-6-isopropylpyrimidin-2-yl)-N-methylmethanesulfonamide (II) and N-(4-(4-fluorophenyl)-5-(hydroxymethyl)-6-isopropylpyrimidin-2-yl)-N-methylmethanesulfonamide (III), key intermediates in preparation of Rosuvastatin. | 05-21-2015 |
20150148360 | 3,5,N-TRIHYDROXY-ALKANAMIDE AND DERIVATIVES: METHOD FOR MAKING SAME AND USE THEREOF - The present invention provides novel compounds of Formula (I), and pharmaceutically compositions thereof. Compounds of Formula (I) are inhibitors of histone deacetylases (HDACs) and 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase (HMGR). Also provided are methods of using the compounds and pharmaceutical compositions for inhibiting the activity of HDACs and HMGR, treating diseases associated with HDACs or HMGR (e.g., cancer, hypercholesterolemia, an acute or chronic inflammatory disease, autoimmune disease, allergic disease, pathogen infection, neurodegenerative disease, and a disease associated with oxidative stress), or inhibiting drug resistance of cancer cells. | 05-28-2015 |
20150148361 | Benzoimidazol-2-yl pyrimidines and pyrazines as modulators of the histamine H4 receptor - Benzoimidazol-2-yl pyrimidines and pyrazines, pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H | 05-28-2015 |
20150290104 | METHOD OF ENHANCING HAIR GROWTH - Methods and compositions for stimulating the growth of hair are disclosed wherein said compositions include bimatoprost and minoxidil in a vehicle for topical application to the skin of a mammal, e.g. a human, whereby the combination of bimatoprost and minoxidil produces a faster onset of hair growth in humans or other mammals and wherein said composition brings about a synergestic result of faster onset of hair growth as compared to compositions comprising bimatoprost and minoxidil, alone. | 10-15-2015 |
20150290195 | PRO-NEUROGENIC COMPOUNDS - This invention relates generally to stimulating neurogenesis (e.g., post-natal neurogenesis, e.g., post-natal hippocampal neurogenesis) and protecting from neuron cell death. | 10-15-2015 |
20150291537 | 4-(ORTHO)-FLUOROPHENYL-5-FLUOROPYRIMIDIN-2-YL AMINES CONTAINING A SULFOXIMINE GROUP - The present invention relates to 4-(ortho)-fluorophenyl-5-fluoropyrimidin-2-yl amine derivatives containing a sulfoximine group of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I). | 10-15-2015 |
20150297595 | INHIBITORS OF SYK AND JAK PROTEIN KINASES - The present invention is directed to compounds of formula I-V and tautomers thereof or pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma. | 10-22-2015 |
20150299139 | ALKYL AMIDE-SUBSTITUTED PYRIMIDINE COMPOUNDS USEFUL IN THE MODULATION OF IL-12, IL-23 AND/OR IFN ALPHA - Compounds having the following formula (I): or a stereoisomer or pharmaceutically-acceptable salt thereof, where R | 10-22-2015 |
20150305337 | COMBINATIONS OF PYRIMETHANIL AND MONOTERPENES - The present invention relates to combinations of pyrimethanil, or a salt thereof, and a monoterpene, or a salt thereof, which provide an improved biocidal effect. More particularly, the present invention relates to compositions comprising a combination of pyrimethanil, or a salt thereof, together with a monoterpene selected from thymol and β-thujaplicin in respective proportions to provide a synergistic biocidal effect. Compositions comprising these combinations are useful for the protection of any living or non-living material, such as crops, plants, fruits, seeds, objects made of wood, thatch or the like, engineering material, biodegradable material and textiles against deterioration due to the action of microorganisms such as bacteria, fungi, yeasts, algae, virusses, and the like. | 10-29-2015 |
20150306099 | COMBINATION - The present invention relates to a method of treating cancer and pre-cancerous syndromes in a human and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method that includes administering 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methylbenzenesulfonamide, or a pharmaceutically acceptable salt thereof, and 3′-[(2Z)-[1-(3,4-dimethylphenyl)-1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene]hydrazino]-2′-hydroxy-[1,1′-biphenyl]-3-carboxylic acid, or a pharmaceutically acceptable salt thereof, to a human in need thereof. | 10-29-2015 |
20150307479 | CYCLOBUTYL BENZIMIDAZOLES AS PDE 10 INHIBITORS - The present invention is directed to substituted cyclobutyl benzimidazole compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction. | 10-29-2015 |
20150307484 | Crystal Form of Dabrafenib and Preparation Method and Use Thereof - The invention relates to a new crystal form of dabrafenib and preparation method thereof. With respect to known crystal forms, the new crystal form has the advantage of being more stable at room temperature or in aqueous systems, and has low hygroscopicity, and thus is more suitable for a wet granulation process or being prepared into a suspension. The present invention also relates to a pharmaceutical composition and formulations comprising the new crystal form, and their use in the treatment of Raf family kinase-related diseases. | 10-29-2015 |
20150313900 | METHOD OF TREATING PROLIFERATIVE DISORDERS AND OTHER PATHOLOGICAL CONDITIONS MEDIATED BY BCR-ABL, C-KIT, DDR1, DDR2 OR PDGF-R KINASE ACTIVITY - The present invention relates to a regimen for the administration of a pyrimidyl-aminobenzamide of formula I as defined herein for the treatment of proliferative disorders, particularly solid and liquid tumors, and other pathological conditions mediated by the Bcr-Abl oncoprotein, the cell transmembrane tyrosine kinese receptor c-Kit, DDR1 (discoidin domain receptor 1), DDR2 (discoidin domain receptor 2) or PDGF-R (platelet derived growth factor receptor) kinase activity. | 11-05-2015 |
20150315181 | CERTAIN AMINO-PYRIMIDINES, COMPOSITIONS THEREOF, AND METHODS FOR THEIR USE - Provided are compounds of Formula I: | 11-05-2015 |
20150322058 | Oxytocin receptor agonists for the treatment of CNS diseases - The invention relates to the use of a compound of formula I | 11-12-2015 |
20150329531 | AMINO-PYRIMIDINE-CONTAINING SPLEEN TYROSINE KINASE (SYK) INHIBITORS - The invention provides certain amino-pyrimidine-containing compounds. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase. | 11-19-2015 |
20150335609 | COMBINATIONS OF HISTONE DEACETYLASE INHIBITOR AND PAZOPANIB AND USES THEREOF - Dosing regimens, methods of treatment, controlled release formulations, and combination therapies that include an HDAC inhibitor, or a pharmaceutically acceptable salt thereof, and pazopanib (or a salt thereof, e.g., pazopanib HCI) are described. | 11-26-2015 |
20150335643 | PERSONALIZED TREATMENT OF CANCER USING FGFR INHIBITORS - The present invention relates to a method for predicting the responsiveness of cancer cells to FGFR1 inhibitors, which comprises the evaluation of the status of FGFR1 gene and the status of MYC. A kit useful for carrying out the method is also provided. In addition, a method of treating cancer such as lung cancer is also provided which includes determining the status of FGFR1 gene and the status of MYC gene, and administering to the cancer patient an FGFR1 inhibitor if the tumor tissue or cells exhibit an increased expression or amplification of the FGFR1 gene, as well as an increased expression or amplification of the MYC gene. | 11-26-2015 |
20150335645 | Combination of BRAF and VEGF Inhibitors - A novel combination comprising the VEGFR inhibitor 5[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methylbenzenesulfonamide, or a pharmaceutically acceptable salt thereof, with a B-Raf inhibitor, particularly N-{3-[5-(2-Amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-1,3-thiazol-4-yl]-2-fluorophenyl}-2,6-difluorobenzenesulfonamide or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the same and methods of using such combinations and compositions in the treatment of conditions in which the inhibition of VEGFR and/or B-Raf is beneficial. | 11-26-2015 |
20150336901 | SUBSTITUTED DIAMINOCARBOXAMIDE AND DIAMINOCARBONITRILE PYRIMIDINES, COMPOSITIONS THEREOF, AND METHODS OF TREATMENT THEREWITH - Provided herein are Diaminopyrimidine Compounds having the following structures: | 11-26-2015 |
20150336902 | Phosphatidylcholine Transfer Protein Inhibitors - This invention relates to compounds of Formulas I, II, and III, and their use as inhibitors of phosphatidylcholine transfer protein (PC-TP). The invention further relates to pharmaceutical compositions and methods of treatment of disorders related to the inhibition of PC-TP using the compounds of Formulas I, II, and III. Such disorders include obesity and disorders associated with obesity. | 11-26-2015 |
20150342950 | SUBSTITUTED INDOLYL ALKYL AMINO DERIVATIVES AS NOVEL INHIBITORS OF HISTONE DEACETYLASE - This invention comprises the novel compounds of formula (I) | 12-03-2015 |
20150344957 | MONITORING TREATMENT OF HISTIOCYTOSIS WITH VEMURAFENIB AND DABRAFENIB - Provided are methods of determining the amount of a BRAF V600E mutation over time in a subject with Langerhans Cell Histiocytosis (LCH) or Erdheim-Chester Disease (ECD) who is being treated with vemurafenib or dabrafenib. | 12-03-2015 |
20150359794 | IMPAIRMENT OF THE LARGE RIBOSOMAL SUBUNIT PROTEIN RPL24 BY DEPLETION OR ACETYLATION - Provided herein are compositions of histone deacetylase (HDAC) inhibitors for the treatment of cancers overexpressing the large ribosomal subunit protein 24 (RPL24) in a subject in need thereof. Provided herein are methods for treating RPL24-overexpressing cancers in a subject in need thereof, comprising administering to the subject an effective amount of an HDAC inhibitor. Also provided herein are methods for inhibiting the viability of an RPL24-overexpressing cancer cell with an HDAC inhibitor. Also provided herein are methods for assessing the efficacy of an HDAC inhibitor against a cancer. | 12-17-2015 |
20150366980 | Mineral Amino-Acid Complexes of Fatty Acids - The present invention relates to compound of Formula III comprising an amino acid component, a divalent metal component, and a counter-ion component, compositions containing same, and methods of use. | 12-24-2015 |
20150368229 | MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF - Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein. | 12-24-2015 |
20150374603 | HAIR GROWTH COMPOSITION AND METHOD - The present invention relates to compositions for and methods of retarding hair loss or facilitating hair growth comprising a hair growth active and a C | 12-31-2015 |
20150374690 | HETEROARYL COMPOUNDS AND USES THEREOF - The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same. | 12-31-2015 |
20160000782 | PHARMACEUTICAL COMPOSITION CONTAINING ANTIBACTERIAL AGENT - [Problem] The purpose of the present invention is to provide a pharmaceutical composition containing an antibacterial agent, which is effective in elucidating one cause of dementia, and in treatment thereof. | 01-07-2016 |
20160008304 | Methods for Alleviating Statin Myopathy | 01-14-2016 |
20160015034 | Co-Crystals of Pyrimethanil and Selected Dithiine Tetracarboximide - Co-crystals comprising
| 01-21-2016 |
20160024051 | SALTS AND SOLID FORMS OF ISOQUINOLINONES AND COMPOSITION COMPRISING AND METHODS OF USING THE SAME - Solid forms of chemical compounds that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein. Also provided herein are processes for preparing compounds, solid forms thereof, and pharmaceutical compositions thereof. | 01-28-2016 |
20160030426 | HETEROARYL COMPOUNDS AND USES THEREOF - The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same. Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful for treating a variety of diseases, disorders or conditions, associated with abnormal cellular responses triggered by protein kinase-mediated events. Compounds provided by this invention are also useful for the study of kinases in biological and pathological phenoma, the study of intracellular signal transduction pathways mediated by such kinases and the comparative evaluation of new kinase inhibitors. | 02-04-2016 |
20160030427 | METHODS FOR REDUCING THE RISK OF AN ADVERSE TERIFLUNOMIDE AND ROSUVASTATIN INTERACTION IN MULTIPLE SCLEROSIS PATIENTS - This invention relates to a method for managing the risk of an adverse interaction between teriflunomide and a substrate of breast cancer resistance protein (BCRP) and/or organic anion transporting polypeptide B1 and B3 (OATP1B1/B3). | 02-04-2016 |
20160038488 | Stable and Soluble Formulations of Receptor Tyrosine Kinase Inhibitors, and Methods of Preparation Thereof - The present disclosure relates to stable formulations of receptor tyrosine kinase inhibitors (TKI), e.g., pazopanib; methods of preparation thereof; and use of the disclosed formulations in sustained delivery of the active agent to a target site. The disclosure further relates to methods of converting one polymorphic Form of a TKI to another polymorphic Form and/or an amorphous form. | 02-11-2016 |
20160046615 | Novel Crystal Form of Dabrafenib Mesylate and Preparation Method Thereof - Disclosed are a novel crystal form of Dabrafenib mesylate and preparation method thereof. The novel crystal form of the present invention is more stable in water or an aqueous system, and has greater solubility and dissolution in water, thus having better stability and bioavailability compared with the existing crystal forms. | 02-18-2016 |
20160046632 | OCTAHYDROPYRROLOPYRROLES THEIR PREPARATION AND USE - The present invention provides compounds comprising variously substituted octahydropyrrolopyrroles, their synthesis, methods of making, methods of using, compositions and formulations thereof. | 02-18-2016 |
20160058760 | Protein Kinase C Inhibitors and Uses Thereof - This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes. | 03-03-2016 |
20160067248 | COMBINATIONS - The present invention relates to a method of treating ovarian cancer in a female human and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a ovarian cancer treatment method that includes administering 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methylbenzenesulfonamide, or a pharmaceutically acceptable salt thereof, and 2-[(5-chloro-2-[[3-methyl-1-(1-methylethyl)-1H-pyrazol-5-yl]amino]-4-pyridinyl)amino]-N-methoxybenzamide, or a pharmaceutically acceptable salt thereof, and optionally 1,7β,10β-trihydroxy-9-oxo-5β,20-epoxytax-11-ene-2α,4,13α-triyl 4-acetate 2-benzoate 13-{(2R,3S)-3-[(tert-butoxycarbonyl)amino]-2-hydroxy-3-phenylpropanoate}, to a human in need thereof. | 03-10-2016 |
20160074361 | PRO-NEUROGENIC COMPOUNDS - This technology relates generally to compounds and methods for stimulating neurogenesis (e.g., post-natal neurogenesis, including post-natal hippocampal and hypothalamic neurogenesis) and/or protecting neuronal cell from cell death. Various compounds are disclosed herein. In vivo activity tests suggest that these compounds may have therapeutic benefits in neuropsychiatric and/or neurodegenerative diseases such as schizophrenia, major depression, bipolar disorder, normal aging, epilepsy, traumatic brain injury, post-traumatic stress disorder, Parkinson's disease, Alzheimer's disease, Down syndrome, spinocerebellar ataxia, amyotrophic lateral sclerosis, Huntington's disease, stroke, radiation therapy, chronic stress, abuse of a neuro-active drug, retinal degeneration, spinal cord injury, peripheral nerve injury, physiological weight loss associated with various conditions, as well as cognitive decline associated with normal aging, chemotherapy, and the like. | 03-17-2016 |
20160075665 | COMPOUNDS AND METHODS OF TREATING INFECTIONS - The invention provides compounds of Formula (I), and methods of treating or preventing a bacterial infection in a subject using a compound of Formula (I). The invention also provides the use of a compound of Formula (I) in the manufacture of a medicament for the treatment of a bacterial infection in a subject. The invention further provides a medical device when used in a method of treating or preventing a bacterial infection in a subject and to a medical device comprising the composition of the invention. | 03-17-2016 |
20160081936 | SUSTAINED-RELEASE FORMULATIONS OF COLCHICINE AND METHODS OF USING SAME - Pharmaceutical compositions of colchicine for once-a-day oral administration are provided. The formulations comprise a sustained-release component and an optional immediate-release component, the compositions of which can be selectively adjusted, respectively, to release the active ingredient along a pre-determined or desired release profile. Method of treating or preventing cardiovascular disease and/or inflammatory disease in mammalian subjects comprising the administration of the novel formulations disclosed herein is also provided. | 03-24-2016 |
20160096825 | Furanone Compounds as Kinase Inhibitors - The present disclosure provides novel furanone compounds, or pharmaceutically acceptable salts, solvates or prodrugs thereof, as Raf kinase, especially BRAF kinase, inhibitors, which are useful therapeutic agents for treatment of Raf kinase related diseases or disorders, such as melanomas, cancers, and leukemia. The disclosure also provides methods and processes for preparing these novel furanone compounds, pharmaceutical compositions containing these furanone compounds, and methods of treatment using these furanone compounds. | 04-07-2016 |
20160106748 | PHARMACEUTICAL GASTRO-RETENTIVE SOLID ORAL DOSAGE FORM OF NILOTINIB - The present invention relates to a pharmaceutical gastro-retentive solid oral dosage form comprising nilotinib as the active ingredient. The invention is further related to methods of preparing said dosage form. | 04-21-2016 |
20160108021 | PYRIDONE DERIVATIVES FOR THE TREATMENT OF VIRAL INFECTIONS AND FURTHER DISEASES - This invention relates to pyridone derivatives, processes for their preparation, phamaceutical compositions, and their use in therapy. | 04-21-2016 |
20160120866 | COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS - The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of B-Raf. | 05-05-2016 |
20160151276 | PREVENTION OF HIV-INFECTION | 06-02-2016 |
20160151343 | NON-FLUSHING NIACIN ANALOGUES, AND METHODS OF USE THEREOF | 06-02-2016 |
20160158231 | PYRIMIDINE HYDROXY AMIDE COMPOUNDS FOR TREATING PERIPHERAL NEUROPATHY - The invention relates to HDAC inhibitors for the treatment of peripheral neuropathy in a subject in need thereof. Also provided herein are methods for treating peripheral neuropathy in a subject in need thereof comprising administering to the subject a therapeutically effective amount of an HDAC inhibitor. | 06-09-2016 |
20160158232 | COMBINATIONS OF HISTONE DEACETYLASE INHIBITORS AND BENDAMUSTINE - The invention relates to pharmaceutical combinations comprising an HDAC inhibitor and bendamustine; pharmaceutical compositions comprising the same; and methods of using such combinations and compositions for treating lymphoma in a subject in need thereof. | 06-09-2016 |
20160166531 | METHODS AND COMPOSITIONS FOR TREATING CARDIOVASCULAR DISORDERS | 06-16-2016 |
20160168105 | FORMULATIONS OF 2-(TERT-BUTYLAMINO)-4-((1R,3R,4R)-3-HYDROXY-4-METHYLCYCLOHEXYLAMINO)-PYRI- MIDINE-5-CARBOXAMIDE | 06-16-2016 |
20160169908 | METHODS FOR MEASUREMENT OF INHIBITION OF C-JUN N-TERMINAL KINASE IN SKIN | 06-16-2016 |
20160175305 | CRYSTALLINE FORMS OF 5-CHLORO-N2-(2-ISOPROPOXY-5-METHYL-4-PIPERIDIN-4-YL-PHENYL)-N4-[2-(PROPAN- E-2-SULFONYL)-PHENYL]-PYRIMIDINE-2, 4-DIAMINE | 06-23-2016 |
20160185753 | DEUTERATED DIAMINOPYRIMIDINE COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS COMPRISING SUCH COMPOUNDS - Deuterated diaminopyrimidine compounds and pharmaceutical compositions containing such compounds are described. In particular, disclosed are deuterated diaminopyrimidine compounds of formula (I), and pharmaceutical compositions containing such compounds or crystal forms, pharmaceutically acceptable salt, hydrates or solvates thereof. The disclosed deuterated diaminopyrimidine compounds can be used for treating and/or preventing protein kinase-associated diseases, such as cell proliferative disease, cancer, immune disease and the like. | 06-30-2016 |
20160192654 | COMBINATIONS OF PYRIMETHANIL AND MONOTERPENES | 07-07-2016 |
20160199354 | METHODS FOR OLMESARTAN DOSING BY AUC | 07-14-2016 |
20160199385 | Mineral Amino-Acid Complexes of Active Agents | 07-14-2016 |
20160250211 | AURORA KINASE INHIBITORS | 09-01-2016 |
20160251319 | CARBOXYLIC ACID COMPOUNDS | 09-01-2016 |
20160375020 | USE OF A STATIN COMPOUND AS TOPICAL DRUG FOR TREATING OBESITY, DIABETES, HYPERTENSION AND HYPERLIPEMIA - The invention discloses a use of a statin compound in the preparation of local drugs for improving lipid metabolism and treating obesity, hypertension, hyperlipidemia, fatty liver and hyperglycemia; and statin compound local compositions for improving lipid metabolism and treating obesity, hypertension, fatty liver, hyperlipidemia, atherosclerosis, coronary heart disease, apoplexy and other cardiovascular and cerebrovascular diseases, and drug formulation and preparation method thereof. | 12-29-2016 |
20160376266 | ANTI-ALPHAVBETA1 INTEGRIN COMPOUNDS AND METHODS - Provided herein, inter alia, are methods and compositions for inhibiting αvβ1 integrin and for treating fibrosis. | 12-29-2016 |
20170233372 | NOVEL SALTS OF NILOTINIB AND POLYMORPHS THEREOF | 08-17-2017 |
20180021335 | HETEROCYCLIC RECEPTOR AGONISTS FOR THE TREATMENT OF DIABETES AND METABOLIC DISORDERS | 01-25-2018 |
20180022710 | ISOTOPOLOGUES OF 2-(TERT-BUTYLAMINO)-4-((1R,3R,4R)-3-HYDROXY-4-METHYLCYCLOHEXYLAMINO)-PYRI- MIDINE-5-CARBOXAMIDE | 01-25-2018 |
20220133722 | PHARMACEUTICAL COMPOSITIONS - The present invention relates to pharmaceutical compositions for the treatment or prevention of symptoms associated with endocrine disturbances, such as hot flashes. The pharmaceutical compositions comprise a tricyclic amino containing compound of formula (I), such as MSX-122 (also known as “Q-122”) (N,N′-(1,4-phenylenebis(methylene))bis(pyrimidin-2-amine)), and one or more pharmaceutically acceptable excipients. The pharmaceutical compositions may be given in certain doses and/or dosing regimens, preferably twice daily. | 05-05-2022 |
20220135536 | 2,4,5-TRISUBSTITUTED 1,2,4-TRIAZOLONES USEFUL AS INHIBITORS OF DHODH - The present invention provides triazolone compounds of general formula (I): | 05-05-2022 |