Entries |
Document | Title | Date |
20080200458 | Methods and compositions for the treatment of body composition disorders - This invention relates to methods of treating, managing and preventing body composition disorders, and to compounds and pharmaceutical compositions useful in such methods. | 08-21-2008 |
20080207612 | Benzimidazole Derivatives, Compositions Containing Them, Preparation Thereof and Uses Thereof - Compounds of Formula (I) or pharmaceutically acceptable salts thereof; wherein R | 08-28-2008 |
20080207613 | Selective Kinase Inhibitors - A compound of the general formula (I) or pharmaceutically acceptable prodrugs, salts, hydrates, solvates, crystal forms or diastereomers thereof, wherein A represents a variety of six membered nitrogen containing heterocyclic rings, Q is a bond, halogen, C | 08-28-2008 |
20080207614 | QUINAZOLINE DERIVATIVES FOR THE TREATMENT AND PREVENTION OF DIABETES AND OBESITY - The present invention relates to novel quinazoline derivatives effective in lowering blood glucose level and body weight, and a medicine for treatment and/or prevention of diabetes and/or obesity, which comprises the compound as an active ingredient. | 08-28-2008 |
20080207615 | Method to determine responsiveness of cancer to epidermal growth factor receptor targeting treatments - The present invention is directed to a method for determining the responsiveness of cancer to an epidermal growth factor receptor (EGFR) treatment. In a preferred embodiment, the presence of at least one variance in the kinase domain of the erbB1 gene confers sensitivity to the tyrosine kinase inhibitor gefitinib. Thus, a diagnostic assay for these mutations will allow for the administration of gefitinib, erlotinib and other tyrosine kinase inhibitors to those patients most likely to respond to the drug. | 08-28-2008 |
20080234263 | Quinazoline Derivatives - The invention concerns quinazoline derivatives of Formula (I) wherein each of R | 09-25-2008 |
20080234264 | Method to determine responsiveness of cancer to epidermal growth factor receptor targeting treatments - The present invention is directed to a method for determining the responsiveness of cancer to an epidermal growth factor receptor (EGFR) treatment. In a preferred embodiment, the presence of at least one variance in the kinase domain of the erbB1 gene confers sensitivity to the tyrosine kinase inhibitor gefitinib. Thus, a diagnostic assay for these mutations will allow for the administration of gefitinib, erlotinib and other tyrosine kinase inhibitors to those patients most likely to respond to the drug. | 09-25-2008 |
20080234265 | Histone Deacetylase Inhibitors Sensitize Cancer Cells to Epidermal Growth Factor Inhibitors - Disclosed is the use of a combination of histone deacetylase inhibitors and epidermal growth factor receptor (EGFR) inhibitors to treat cancer. | 09-25-2008 |
20080234266 | Squaric Acid Derivatives II -
Compounds of the formula (I), in which R, X, X′ and R | 09-25-2008 |
20080249090 | Substituted pyridone compounds and methods of use - The present invention comprises a new class of compounds capable of modulating the c-kit receptor and, accordingly, useful for treatment of c-kit mediated diseases, including various inflammatory, fibrotic and/or mast cell mediated diseases such as mastocytosis. The compounds have a general Formula I | 10-09-2008 |
20080255111 | Tissue Factor Production Inhibitor - A medicament which has an activity of inhibiting production of tissue factor and comprises an LXR ligand as an active ingredient; and a medicament for treatment and/or prophylaxis of vascular restenosis following angioplasty, endarterectomy, percutaneous transluminal coronary angioplasty (PTCA) or stent implantation, or treatment and/or prophylaxis of blood coagulation diseases, diseases induced by platelet aggregation including stable or unstable angina pectoris, cardiovascular and cerebrovascular diseases including thromboembolism formation diseases accompanying diabetes, rethrombosis following thrombolysis, cerebral ischemic attack, infarction, stroke, ischemia-derived dementia, peripheral artery disease, thromboembolism formation diseases during use of an aorta-coronary artery bypass, glomerulosclerosis, renal embolism, tumor or cancer metastasis, which comprises an LXR ligand as an active ingredient. | 10-16-2008 |
20080255112 | Pyrimidine-Substituted Benzimidazole Derivatives 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 Alk, Abl, BRK, Blk, BMX, CSK, c-Src, c-Raf, EGFR, Fes, FGFR3, Fms, Fyn, IGF-IR, IR, IKKα, IKKβ, JAK2, JAK3, KDR, Lck, Met, p70S6k, Ros, Rsk1, SAPK2α, SAPK2β, SAPK3, SIK, Tie2, TrkB and/or WNK3 kinases. | 10-16-2008 |
20080261974 | Novel Chemical Compounds - This invention relates to newly identified compounds for inhibiting hYAK3 proteins and methods for treating diseases associated with the imbalance or inappropriate activity of hYAK3 proteins. | 10-23-2008 |
20080261975 | Tec Kinase Inhibitors - Disclosed are compounds of formula (I): | 10-23-2008 |
20080269211 | Indazole Derivatives - This invention relates to compounds of the formula (I): | 10-30-2008 |
20080275039 | Geldanamycin Derivatives and the Method for Biosynthesis Thereof - The present invention relates to geldanamycin derivatives, benzoquinone ansamycin biosynthesized by gene manipulation of | 11-06-2008 |
20080280899 | Inhibitors of Akt Activity - The present invention is directed to compounds which contain substituted napthyridines which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention. | 11-13-2008 |
20080280900 | BICYCLIC PYRIMIDINE DERIVATIVES AS CALCIUM CHANNEL BLOCKERS - Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted T-type calcium channel activity are disclosed. Specifically, a series of compounds containing thienopyrimidine or oxoquinazoline derivatives are disclosed of the general formula (1) or formula (2) where X is a linker and Y is an aromatic moiety or N(R5)(R6). | 11-13-2008 |
20080293715 | Therapeutic Pyrazolo[3,4-b]Pyridines and Indazoles - The present invention provides for compounds of Formula I: | 11-27-2008 |
20080300247 | Benzimidazole Thiophene Compounds - The present invention provides benzimidazole thiophene compounds pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents. | 12-04-2008 |
20080300248 | Quinazoline Derivatives, Preparation Methods and Uses Thereof - The present invention has disclosed a compound of formula I and a pharmaceutically acceptable salt or a solvate thereof, wherein the substituents are as defined in the description. The invention has also disclosed a method for preparing the compound of formula I, the pharmaceutical compositions comprising the same and their uses in the preparation of an anti-tumor medicament. | 12-04-2008 |
20080306064 | Benzimidazole Derivatives - Benzimidazole derivatives, methods of preparing the same and their pharmaceutical uses for the treatment of inflammatory diseases including COPD. | 12-11-2008 |
20080312229 | Organic Compounds - There are provided according to the invention compounds of formula (I) | 12-18-2008 |
20080312230 | Organic Compounds - There are provided according to the invention compounds of formula (I), | 12-18-2008 |
20080318950 | Quinazoline Derivatives as a Multiplex Inhibitor and Method For the Preparation Thereof - The present invention relates to a novel quinazoline derivative and a pharmaceutically acceptable salt thereof as a multiplex inhibitor, a method for the preparation thereof, and a pharmaceutical composition and a therapeutic composition comprising same as an active ingredient. The inventive quinazoline derivative as a multiplex inhibitor can selectively and effectively inhibit diseases caused by the overactivity of a tyrosine kinase. | 12-25-2008 |
20080318951 | Dual-acting benzoimidazole antihypertensive agents - The invention is directed to compounds having the formula: | 12-25-2008 |
20090005378 | PYRROLO-PYRIDINE KINASE MODULATORS - The present invention provides novel pyrrolo-pyridine kinase modulators and methods of using the novel pyrrolo-pyridine kinase modulators to treat diseases mediated by kinase activity. | 01-01-2009 |
20090005379 | Azaindole-2-Carboxamide Derivatives - The present invention relates to compounds of formula (I) wherein R | 01-01-2009 |
20090012082 | Mediators of Hedgehog Signaling Pathways, Compositions and Uses Related Thereto - The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function comprising contacting the cell with a hedgehog antagonist, such as a small molecule, in a sufficient amount to aberrant growth state, e.g., to agonize a normal ptc pathway or antagonize smoothened or hedgehog activity. | 01-08-2009 |
20090012083 | N-AROYL CYCLIC AMINE DERIVATIVES AS OREXIN RECEPTOR ANTAGONISTS - Disclosed are N-aroyl cyclic amine derivatives having the formula: | 01-08-2009 |
20090012084 | 3-CINNOLINECARBOXAMIDE DERIVATIVES AND THEIR USE FOR TREATING CANCER - The invention relates to chemical compounds of formula (I): | 01-08-2009 |
20090018130 | Derivatives of 5-Aryl-1H-Pyrrolo [2, 3B] Pyridine-3-Carboxamide or 5-Aryl-1H-Pyrrolo [2, 3B] Pyridine-3-Carboxylic Acid - The present invention relates to new compounds of formula I as a free base or a pharmaceutically acceptable salt, solvate or solvate of salt thereof, a process for their preparation and new intermediates used therein, pharmaceutical formulations containing said therapeutically active compounds and to the use of said active compounds in therapy. | 01-15-2009 |
20090018131 | QUINAZOLINE DERIVATIVES AS P13 KINASE INHIBITORS - Invented is a method of inhibiting the activity/function of PI3 kinases using quinazoline derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of quinazoline derivatives. | 01-15-2009 |
20090018132 | Substituted Heterocyclic Ethers and Their Use in CNS Disorders - The invention encompasses compounds of Formula I, including pharmaceutically acceptable salts, their pharmaceutical compositions, and their use in treating CNS disorders. | 01-15-2009 |
20090023725 | Fused Heteroaryl Derivatives for Use as P38 Kinase Inhibitors - Compounds of formula (I): | 01-22-2009 |
20090023726 | Heterocyclylalkyl Derivatives as Novel Inhibitors of Histone Deacetylase - This invention comprises the novel compounds of formula (I) | 01-22-2009 |
20090023727 | PHTHALAZINONE DERIVATIVES - A compound of the formula (I): | 01-22-2009 |
20090042879 | PHTHALAZINONE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME - The present invention provides a novel compound having an excellent PDE4 inhibitory activity and TNF-α production-suppressing activity, and also provides a preventive and therapeutic agent for atopic dermatitis or the like. The present invention includes a novel phthalazinone derivative of the following general structural formula [1] or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising it as an active ingredient. | 02-12-2009 |
20090042880 | NOVEL 4-BENZIMIDAZOL-2-YLPYRIDAZIN-3-ONE DERIVATIVES - Disclosed are compounds of the general formula (I), where the definition of the substituents A, B, D, E, R | 02-12-2009 |
20090048250 | INDAZOLINONE COMPOSITIONS USEFUL AS KINASE INHIBITORS - The present invention provides compounds of formula I: | 02-19-2009 |
20090048251 | 4-(1H-INDAZOL-5-YL-AMINO)-QUINAZOLINE COMPOUNDS AS ERBB RECEPTOR TYROSINE KINASE INHIBITORS FOR THE TREATMENT OF CANCER - A quinazoline derivative of the Formula I: | 02-19-2009 |
20090048252 | THIAZOLONES FOR USE AS PI3 KINASE INHIBITORS - Invented is a method of inhibiting the activity/function of PI3 kinases using substituted thiazolones. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of substituted thiazolones. | 02-19-2009 |
20090054432 | 2-(2-Hydroxybiphenyl-3-yl)-1H-Benzoimidazole-5-Carboxamidine Derivatives as Factor VIIA Inhibitors - The present invention relates to novel inhibitors of Factors VIIa, IXa, Xa, XIa, in particular Factor VIIa, pharmaceutical compositions comprising these inhibitors, and methods for using these inhibitors for treating or preventing thromboembolic disorders, cancer or rheumatoid arthritis. Processes for preparing these inhibitors are also disclosed. | 02-26-2009 |
20090062277 | PHOSPHODIESTERASE 10 INHIBITORS - The present invention is directed to certain compounds useful as phosphodiesterase 10 (PDE10) inhibitors that have the formula | 03-05-2009 |
20090062278 | 5- OR 6-SUBSTITUTED BENZIMIDAZOLE DERIVATIVES AS INHIBITORS OF RESPIRATORY SYNCYTIAL VIRUS REPLICATION - The present invention concerns 5- or 6-substituted-benzimidazole derivatives having inhibitory activity on the replication of the respiratory syncytial virus and having the formula | 03-05-2009 |
20090069320 | Substituted 4-Amino-Quinazoline Compounds with Metabotropic Glutamate Receptor Regulating Activity and Uses Thereof - Substituted 4-amino-quinazoline compounds corresponding to formula I | 03-12-2009 |
20090076003 | Phthalazine Derivatives with Angiogenesis Inhibiting Activity - The invention relates to new phthalazine derivatives, processes for the preparation thereof, the application thereof in a process for the treatment of the human or animal body, the use thereof alone or in combination with one or more other pharmaceutically active compounds for the treatment of a disease, especially of a disease that responds to the inhibition of tyrosine kinases, more especially the inhibition of the vascular endothelial growth factor (VEGF) receptor kinase, preferably the treatment of a proliferative disease, such as a tumour disease. | 03-19-2009 |
20090082348 | INDAZOLE DERIVATIVES - The present invention provides a compound represented by Formula (I): | 03-26-2009 |
20090082349 | THIAZOLONES FOR USE AS PI3 KINASE INHIBITORS - Invented is a method of inhibiting the activity/function of PI3 kinases using substituted thiazolones. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of substituted thiazolones. | 03-26-2009 |
20090088428 | CYCLOHEXYLIMIDIAZOLE LACTAM DERIVATIVES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1 - The present invention discloses novel compounds of Formula I: (I) having 11β-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11β-HSD type 1 activity. | 04-02-2009 |
20090099175 | Phosphodiesterase 10 inhibitors - The present invention if directed to certain cinnoline compounds that are PDE10 inhibitors, pharmaceutical compositions containing such compounds and processes for preparing such compounds. The invention is also directed to methods of treating diseases mediated by PDE10 enzyme, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like. | 04-16-2009 |
20090099176 | PYRROLOPYRIDINE-2-CARBOXYLIC ACID AMIDES - Compounds represented by Formula (I) or pharmaceutically acceptable salts thereof, are useful in the prophylactic or therapeutic treatment of diabetes, hyperglycemia, hypercholesterolemia, hyperinsulinemia, hyperlipidemia, hypertension, atherosclerosis or tissue ischemia e.g. myocardial ischemia, and as cardioprotectants. | 04-16-2009 |
20090099177 | PYRIDYL COMPOUNDS - Compounds of formula (I) or a pharmaceutically acceptable derivative thereof: wherein R | 04-16-2009 |
20090099178 | INDAZOLE COMPOUNDS AND METHODS OF USE THEREOF - This invention is directed to Indazole Compounds or pharmaceutically acceptable salts, solvates and hydrates thereof. The Indazole Compounds have utility in the treatment or prevention of a wide range of diseases and disorders that are responsive to the inhibition, modulation or regulation of kinases, such as inflammatory diseases, abnormal angiogenesis and diseases related thereto, cancer, atherosclerosis, a cardiovascular disease, a renal disease, an autoimmune condition, macular degeneration, disease-related wasting, an asbestos-related condition, pulmonary hypertension, diabetes, obesity, pain and others. Thus, methods of treating or preventing such diseases and disorders are also disclosed, as are pharmaceutical compositions comprising one or more of the Indazole Compounds. This invention is based, in part, upon the discovery of a novel class of 5-triazolyl substituted indazole molecules that have potent activity with respect to the modulation of protein kinases. Thus, the invention encompasses orally active molecules as well as parenterally active molecules which can be used at lower doses or serum concentrations for treating diseases or disorders associated with protein kinase signal transduction. | 04-16-2009 |
20090105247 | QUINAZOLINE AND QUINOLINE DERIVATIVES AS IRREVERSIBLE PROTEIN TYROSINE KINASE INHIBITORS - A compound of formula (I), a pharmaceutically acceptable salt, or hydrate thereof, and a method of preparing the same. A method of treating or preventing a physiological disorder caused by abnormal protein tyrosine kinase activity in a mammal comprising administering to said mammal a pharmaceutical composition comprising a compound of formula (I). | 04-23-2009 |
20090111806 | Azaquinolone based compounds exhibiting prolyl hydroxylase Inhibitory activity, compositions, and uses thereof - are useful as inhibitors of HIF prolyl hydroxylases where the definitions of the variables are provided herein. | 04-30-2009 |
20090118279 | COMPOUND CONTAINING BASIC GROUP AND USE THEREOF - The present invention relates to a compound represented by formula (I): | 05-07-2009 |
20090118280 | Compounds Which Potentiate AMPA Receptor and Uses Thereof in Medicine - Compounds of formula (I) and salts are provided: | 05-07-2009 |
20090124615 | Benzimidazole Thiophene Compounds - The present invention provides benzimidazole thiophene compounds pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents. | 05-14-2009 |
20090131432 | XANTHINE DERIVATES, THEIR PREPARATION AND THEIR USE IN PHARMACEUTICAL COMPOSITIONS - Compounds of formula (I) | 05-21-2009 |
20090137583 | 2-AMINOQUINAZOLINE DERIVATIVES - The present invention provides 2-aminoquinazoline derivatives represented by formula (I): | 05-28-2009 |
20090137584 | SULFONYL BENZIMIDAZOLE DERIVATIVES - This invention relates to compounds of the formula (I): or a pharmaceutically acceptable salt thereof, wherein A, R | 05-28-2009 |
20090137585 | N-ACYLSULFONAMIDE APOPTOSIS PROMOTERS - N-Benzoyl arylsulfonamides having the formula | 05-28-2009 |
20090143380 | 2H- OR 3H-BENZO[E]INDAZOL-1-YL CARBAMATE DERIVATIVES, THE PREPARATION AND THERAPEUTIC USE THEREOF - Compounds corresponding to the formula (I) | 06-04-2009 |
20090149459 | P38 INHIBITORS AND METHODS OF USE THEREOF - This invention relates to inhibitors of p38 and methods of utilizing the inhibitors and pharmaceutical compositions thereof in the treatment and prevention of various disorders mediated by p38. | 06-11-2009 |
20090170846 | INHIBITORS OF THE HIV INTEGRASE ENZYME - The present invention is directed to compounds of formula (I), and pharmaceutically acceptable salts and solvates thereof, their synthesis, and their use as modulators or inhibitors of the human immunodeficiency virus “HIV” integrase enzyme. Formula (I). | 07-02-2009 |
20090170847 | Imidazopyridine Derivatives Inhibiting Protein Kinase Activity, Method for the Preparation Thereof and Pharmaceutical Composition Containing Same - The inventive imidazopyridine derivative can be used in a pharmaceutical composition for preventing or treating diseases such as diabetes, obesity, dementia, cancer, and inflammation, since it can efficiently inhibit the activities of several protein kinases including glycogen synthase kinase-3 (GSK-3), aurora kinase, extracellular signal-regulated kinase (ERK), protein kinase B (AKT), and the likes, to control signal transductions thereof. | 07-02-2009 |
20090176780 | NITROGENOUS HETEROCYCLIC COMPOUNDS - The present invention relates to nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention is also related to a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases. In a particular aspect the present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which inhibit phosphorylation of a PDGF receptor to hinder abnormal cell growth and cell wandering, and a method for preventing or treating cell-proliferative diseases such as arteriosclerosis, vascular reobstruction, cancer and glomerulosclerosis. | 07-09-2009 |
20090181964 | Propane-1,3-Dione Derivative or Salt Thereof - It is intended to provide a compound useful as a GnRH receptor antagonist. The inventors further investigated propane-1,3-dione derivatives. As a result, they confirmed that a compound having a benzene ring or a thiophene ring substituted with a group represented by —SO | 07-16-2009 |
20090181965 | MODULATORS FOR AMYLOID BETA - The invention relates to compounds of formula | 07-16-2009 |
20090186890 | Pharmaceutical Formulation of Iressa Comprising a Water-Soluble Cellulose Derivative - A pharmaceutical composition comprising 4-(3′-chloro-4′-fluoroanilino)-7-methoxy-6-(3-morpholinopropoxy)quinazoline or a pharmaceutically acceptable salt thereof (the Agent) and a water-soluble cellulose ether or an ester of a water-soluble cellulose ether. The water-soluble cellulose ether or ester of a water-soluble cellulose ether present in the composition inhibits the rate of precipitation of the Agent from solution. | 07-23-2009 |
20090186891 | ORGANIC COMPOUNDS - The present invention provides compounds of the following structure; | 07-23-2009 |
20090186892 | METHODS FOR TREATING LUNG CANCERS - The present invention provided methods for treating lung cancers using therapeutic agents for lung cancers comprising erbB receptor inhibitors as active ingredients. Methods for examining the responsiveness of lung cancer patients to erbB receptor inhibitors by using blood amphiregulin (AREG) as an indicator were provided. Furthermore, methods for treating lung cancers in which responsiveness to an erbB receptor inhibitor is determined based on blood AREG concentration, and in which therapeutic agents are selectively administered to patients expected to be responsive, were also provided. Advanced therapeutic effects can be expected by administering an erbB receptor inhibitor to patients predicted to be responsive. The present invention contributes to the improvement of therapeutic effects of gefitinib (Product name: Iressa®) and such on lung cancers. | 07-23-2009 |
20090192155 | Identification of Compounds Suitable for Treating Ad - The invention provides a method of screening for compounds which inhibit the hyperphosphorylation of tau, and hence are suitable for treating AD and related conditions. | 07-30-2009 |
20090192156 | PHTHALAZINONE DERIVATIVES - A compound of the formula (I): | 07-30-2009 |
20090197881 | Azaindole Derivative Having PGD2 Receptor Antagonistic Activity - The present invention creates an azaindole derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further providing a therapeutic agent for treating allergic diseases. | 08-06-2009 |
20090197882 | INDAZOLE DERIVATIVES FOR THE TREATMENT OF HSP90-INDUCED DISEASES - Novel indazole derivatives of the formula (I), in which R | 08-06-2009 |
20090203690 | 5-SUBSTITUTED INDAZOLES AS KINASE INHIBITORS - The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, | 08-13-2009 |
20090203691 | Novel 1H-indazole compounds - The present invention provides a novel 1H-indazole compound having an excellent JNK inhibitory action. More specifically, it provides a compound represented by the following formula, a salt thereof or a hydrate of them. | 08-13-2009 |
20090209536 | AMINOQUINAZOLINE CANNABINOID RECEPTOR MODULATORS FOR TREATMENT OF DISEASE - The present invention relates to compounds and methods useful as modulators of CB2 for the treatment or prevention of disease states including, but not limited to pain, autoimmune disease, malabsorption syndrome, pulmonary disease, osteoporosis, muscle spasm in cancer, neuromuscular disorder, and atherosclerosis progression. | 08-20-2009 |
20090209537 | AURORA INHIBITORS - The present invention provides an Aurora inhibitor which comprises, as an active ingredient, an indazole derivative represented by Formula (I) (wherein R | 08-20-2009 |
20090215770 | Substituted Quinazoline Derivatives as Inhibitors of Aurora Kinases - The invention provides quinazoline derivatives of formula (I): | 08-27-2009 |
20090215771 | JNK INHIBITORS - The present invention provides novel compounds of formula I and their use in the inhibition of c-Jun N-terminal kinases. The present invention further provides the use of these compounds in medicine, in particular in the prevention and/or treatment of neurodegenerative disorders related to apoptosis and/or inflammation. | 08-27-2009 |
20090239861 | QUINAZOLINE DERIVATIVES AS ANTICANCER AGENTS - A quinazoline derivative of the Formula I: | 09-24-2009 |
20090247519 | AMINO-ETHYL-AMINO-ARYL (AEAA) COMPOUNDS AND THEIR USE - The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain amino-ethyl-amino-aryl (AEAA) compounds which, inter alia, inhibit protein kinase D (PKD) (e.g., PKD1, PKD2, PKD3). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit PKD, and in the treatment of diseases and conditions that are mediated by PKD, that are ameliorated by the inhibition of PKD, etc., including proliferative conditions such as cancer, etc. | 10-01-2009 |
20090247520 | INHIBITORS OF ANTIGEN RECEPTOR-INDUCED NF-kappa B ACTIVATION - A method to identify selective inhibitors of antigen receptor-mediated NF-κB activation is provided, as well as compositions having one or more of those inhibitors and methods of using those inhibitors. | 10-01-2009 |
20090253697 | Novel Indole Derivatives, Preparation Thereof as Medicinal Products and Pharmaceutical Compositions, and Especially as KDR Inhibitors - The disclosure relates to compounds of formula (I): | 10-08-2009 |
20090270390 | PYRIMIDINE DERIVATIVES - The invention concerns pyrimidine derivatives of Formula (I) wherein each of p, R | 10-29-2009 |
20090281098 | BENZOIMIDAZOLE COMPOUND CAPABLE OF INHIBITING PROSTAGLANDIN D SYNTHETASE - The present invention provides a benzimidazole compound represented by Formula (I) | 11-12-2009 |
20090286784 | INDAZOLE, BENZISOXAZOLE, AND BENZISOTHIAZOLE KINASE INHIBITORS - Compounds having the formula | 11-19-2009 |
20090298824 | Organic compounds - Compounds of formula I | 12-03-2009 |
20090312321 | COMPOSITIONS AND METHODS FOR FGF RECEPTOR KINASES INHIBITORS - Described are compounds, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat or prevent disease or disordered associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activity of kinases such as Abl, ALK, AMPK, Aurora, Axl, Bcr-Abl, BIK, Bmx, BRK, BTK, c-Kit, CSK, cSrc, CDK1, CHK2, CK1, CK2, CaMKII, CaMKIV, DYRK2, EGFR, EphB1, FES, FGFR1, FGFR2, FGFR3, Flt1, Flt3, FMS, Fyn, GSK3β, IGF-1R, IKKα, IKKβ, IR, IRAK4, ITK, JAK2, JAK3, JNK1α1, JNK2α, KDR, Lck, LYN, MAPK1, MAPKAP-K2, MEK1, MET, MKK4, MKK6, MST2, NEK2, NLK, p70S6K, PAK2, PDGFR, PDGFRα, PDK1, Pim-2, Plk3, PKA, PKBα, PKCα, PKCtheta, PKD2, c-Raf, RET, ROCK-I, ROCK-II, Ron, Ros, Rsk1, SAPK2a, SAPK2b, SAPK3, SAPK4, SGK, SIK, Syk, Tie2, TrkB, WNK3, and ZAP-70. | 12-17-2009 |
20090312322 | Use of Oxindole Derivatives in the Treatment of Dementia Related Diseases, Alzheimer's Disease and Conditions Associated with Glycogen Synthase Kinase-3 - The present invention relates to a new use of oxindole derivatives of formula I, as a free base or a pharmaceutically acceptable salt thereof, [Chemical formula should be inserted here. Please see paper copy.] wherein R | 12-17-2009 |
20090318444 | TETRAHYDRO- AND DIHYDROQUINAZOLINONES - The present invention relates to the use of tetrahydro- and dihydroquinazolinones of formula I as protein kinase activators or inhibitors, a method for their manufacture, their use for the preparation of a medicament for the treatment of diseases, their use for the manufacture of a pharmaceutical composition and new tetrahydro- and dihydroquinazolinones. | 12-24-2009 |
20090318445 | PDF INHIBITORS - The invention relates to novel compounds that are inhibitors of peptidyl deformylase (PDF). The compounds are useful as antimicrobials and antibiotics. The compounds of the invention display selective inhibition of peptidyl deformylase versus other metalloproteinases such as MMPs. Methods of preparation and uses of the compounds are also disclosed. | 12-24-2009 |
20090325954 | 2-BENZIMIDAZOLYL-6-MORPHOLINO-4-PHENYLPYRIMIDINE DERIVATIVES AS PI3K AND MTOR INHIBITORS FOR THE TREATMENT OF PROLIFERATIVE DISORDERS - The invention concerns pyrimidine derivatives of Formula (I), wherein each of p, R | 12-31-2009 |
20090325955 | GYRASE INHIBITORS AND USES THEREOF - The present invention relates to methods of treating, preventing, or lessening the severity of resistant bacterial infections in mammals, utilizing compounds of formula I or formula VII or pharmaceutically salts thereof. The present invention also relates to methods of using compounds of formula I or formula VII in combination with one or more additional antibacterial agents and/or one or more additional therapeutic agents that increase the susceptibility of bacterial organisms to antibiotics. | 12-31-2009 |
20100004239 | Pyrrolo [3,2-C] Pyridine-4-One 2-Indolinone Protein Kinase Inhibitors - The present invention relates to pyrrolo[3,2-c]pyridine-4-one 2-indolinone compounds of Formula (I) and their pharmaceutically acceptable salts thereof, wherein R | 01-07-2010 |
20100016307 | NOVEL COMPOUNDS - The present invention relates to compounds of formula (I): | 01-21-2010 |
20100022534 | 2-BENZIMIDAZOLYL-6-MORPHOLINO-4- (AZETIDINE, PYRROLIDINE, PIPERIDINE OR AZEPINE) PYRIMIDINE DERIVATIVES AS PI3K AND MTOR INHIBITORS FOR THE TREATMENT OF PROLIFERATIVE DISORDERS - The invention concerns pyrimidine derivatives of Formula (I) wherein each of p, R | 01-28-2010 |
20100029643 | HETEROCYCLYC SULFONAMIDES HAVING EDG-1 ANTAGONISTIC ACTIVITY - The invention relates to chemical compounds of formula (I), (Ia) and (Ib) or pharmaceutically acceptable salts thereof, which possess Edg-1 antagonistic activity and are accordingly useful for their anti-cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments for use in the production of an anti-cancer effect in a warm-blooded animal, such as man. | 02-04-2010 |
20100035878 | INHIBITORS OF C-JUN N-TERMINAL KINASES FOR THE TREATMENT OF NEURODEGENERATIVE DISORDERS RELATING TO APOPTOSIS AND/OR INFLAMMATION - The present invention provides novel compounds of formula I and their use in the inhibition of c-Jun N-terminal kinases. The present invention further provides the use of these compounds in medicine, in particular in the prevention and/or treatment of neurodegenerative disorders related to apoptosis and/or inflammation. | 02-11-2010 |
20100048561 | QUINAZOLINES FOR PDK1 INHIBITION - The invention provides quinazoline compounds that are inhibitors of PDK1. Also provided are pharmaceutical compositions including the compounds, and methods of treating proliferative diseases, such as cancers, with the compounds or compositions. | 02-25-2010 |
20100048562 | ORGANIC COMPOUNDS - The present invention provides a compound of formula I: | 02-25-2010 |
20100048563 | SUBSTITUTED INDOLEPYRIDINIUM AS ANTI-INFECTIVE COMPOUNDS - The present invention concerns the compounds of formula (I) | 02-25-2010 |
20100048564 | FUSED BICYCLIC HETEROARYL DERIVATIVE - The present invention relates to a novel fused bicyclic heteroaryl derivative or a pharmacologically acceptable salt thereof, which has an excellent hypoglycemic effect or treats and/or prevents the onset of a disorder of carbohydrate or lipid metabolism or a disease mediated by peroxisome proliferator-activated receptor (PPAR) γ. | 02-25-2010 |
20100048565 | BENZIMIDAZOLE DERIVATIVES - Compounds, pharmaceutical compositions and methods are provided that are useful in the treatment of inflammatory and immune-related conditions or disorders. In particular, the invention provides compounds which modulate the expression and/or function of proteins involved in inflammation, immune response regulation and cell proliferation. The subject compounds are 2-amino-imidazole derivatives. | 02-25-2010 |
20100056515 | BENZIMIDAZOLE COMPOUNDS - There is provided a compound of the formula (I): | 03-04-2010 |
20100056516 | 1-HYDROXY NAPHTHYRIDINE COMPOUNDS AS ANTI-HIV AGENTS - 1-Hydroxy naphthyridine compounds (e.g., 1-hydroxy naphthyridin-2(1H)-one compounds of Formula I are inhibitors of HIV integrase and/or HIV RNase H and inhibitors of HIV replication: (I) wherein X and R1-R6 are as defined herein. The compounds are useful in the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other anti-HIV agents such as HIV antivirals, immunomodulators, antibiotics and vaccines. | 03-04-2010 |
20100056517 | ARYLSULFONAMIDE COMPOUNDS - The invention relates generally to small molecules that mimic the biological activity of certain peptides and proteins, to compositions containing them and to their use. In particular, the invention relates to compounds of the general formula (I) that mimic the biological activity of BH3-only proteins and are capable of binding to and neutralizing pro-survival Bcl-2 proteins: | 03-04-2010 |
20100069382 | Agent for prophylaxis or treatment of alcohol dependence or drug dependence - The present invention provides an agent for the prophylaxis or treatment of substance abuse and dependence, which contains a compound of the formula (I) represented by (R)-2-{3-[1-(acenaphthen-1-yl)piperidin-4-yl]-2,3-dihydro-2-oxo-benzimidazol-1-yl}-N-methylacetamide, or a pharmaceutically acceptable salt thereof as an active ingredient. | 03-18-2010 |
20100069383 | COMPOUNDS AND THERAPEUTICAL USE THEREOF - Disclosed are 4-arylamino-quinazolines and analogs thereof that are effective as activators of caspases and inducers of apoptosis. The compounds of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs. | 03-18-2010 |
20100075960 | BENZIMIDAZOLE THIOPHENE COMPOUNDS - The present invention provides bezimidazole thiophene compounds pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents. | 03-25-2010 |
20100075961 | MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-kB ACTIVITY AND USE THEREOF - Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity including inflammatory and immune diseases, obesity and diabetes having the structure of formula (I), its enantiomers, diastereomers, or a pharmaceutically acceptable salt, or hydrate, thereof, wherein X is (Ia); or X is (Ib); or X is (Ic); (Id) is heterocycle or heteroaryl; E is —N—, —NR | 03-25-2010 |
20100081656 | COMPOSITIONS AND METHODS FOR MODULATING C-KIT AND PDGFR RECEPTORS - The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as 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 c-kit, PDGFRα, PDGFRβ, CSF1R, Abl, BCR-Abl, CSK, JNK1, JNK2, p38, p70S6K, TGFβ, SRC, EGFR, trkB, FGFR3, FLT3, Fes, Lck, Syk, RAF, MKK4, MKK6, SAPK2β, BRK, KDR, c-raf or b-raf kinase, or mutant forms thereof. | 04-01-2010 |
20100105678 | NOVEL ANXIOLYTIC COMPOUNDS - The present invention relates to chemical compounds of general formula (I) which may possess useful therapeutic activity in a range of central nervous system disorders, and in particular, anxiety disorders. | 04-29-2010 |
20100105679 | 5-PYRIDINONE SUBSTITUTED INDAZOLES - Various 5-substituted 1-substituted indazoles are described, as are pharmaceutical compositions containing these compounds and methods of treatment of diseases using these compounds. Other embodiments are also described. | 04-29-2010 |
20100120768 | METHODS, KITS, AND COMPOSITIONS FOR GENERATING NEW HAIR FOLLICLES AND GROWING HAIR - The invention features methods, kits, and compositions for generating new hair follicles and growing hair on a subject. | 05-13-2010 |
20100130493 | COMBINATION OF VEGF RECEPTOR TYROSINE KINASE INHIBITORS FOR TREATMENT OF CANCER - The present invention relates to a method for the production of an antiangiogenic and/or vascular permeability reducing effect in a warm-blooded animal such as a human which is optionally being treated with ionising radiation, particularly a method for the treatment of a cancer, particularly a cancer involving a solid tumour, which comprises the administration of ZD6474 in combination with ZD1839; to a pharmaceutical composition comprising ZD6474 and ZD1839; to a combination product comprising ZD6474 and ZD1839 for use in a method of treatment of a human or animal body by therapy; to a kit comprising ZD6474 and ZD1839; to the use of ZD6474 and ZD1839 in the manufacture of a medicament for use in the production of an antiangiogenic and/or vascular permeability reducing effect in a warm-blooded animal such as a human which is optionally being treated with ionising radiation. | 05-27-2010 |
20100137304 | NOVEL CRYSTALLINE FORMS OF THE ANTI-CANCER COMPOUND ZD1839 - The invention concerns certain crystalline solvates and hydrates of the compound of the Formula I | 06-03-2010 |
20100137305 | AMINOPYRIMIDINES USEFUL AS KINASE INHIBITORS - The present invention relates to compounds useful as inhibitors of Aurora protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention. | 06-03-2010 |
20100137306 | HETEROCYCLIC TRPV1 RECEPTOR LIGANDS - The invention relates to compounds of formulae I(a)-I(d): | 06-03-2010 |
20100144730 | PYRIDINONYL PDK1 INHIBITORS - The present invention provides pyridinonyl PDK1 inhibitors and methods of treating cancer using the same. | 06-10-2010 |
20100144731 | Novel Biccyclic Compounds As GATA Modulators - Novel bicyclic compounds, stereoisomers, and/or pharmaceutically acceptable salts of the novel bicyclic compounds, and/or pharmaceutically acceptable salts of the stereoisomers of the novel bicyclic compounds are provided. Additionally, methods of forming novel bicyclic compounds, stereoisomers, and/or pharmaceutically acceptable salts of the novel bicyclic compounds, and/or pharmaceutically acceptable salts of the stereoisomers of the novel bicyclic compounds are provided. | 06-10-2010 |
20100152183 | BCL-2-SELECTIVE APOPTOSIS-INDUCING AGENTS FOR THE TREATMENT OF CANCER AND IMMUNE DISEASES - Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 or Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which are expressed anti-apoptotic Bcl-2 protein. | 06-17-2010 |
20100160314 | Small Molecule Inhibitors of Toll-Like Receptor 9 - Small molecule compounds and compositions containing said compounds useful for inhibiting signaling by certain Toll-like receptors (TLRs), particularly TLR9, are provided. The compounds and compositions can be used to inhibit immune responses, including unwanted immune responses in particular. Compounds, compositions, and methods are provided to treat a variety of conditions involving unwanted immune responses, including for example autoimmune disease, inflammation, transplant rejection, and sepsis. | 06-24-2010 |
20100160315 | NOVEL 2, 3-DIAMINO-QUINAZOLINONE DERIVATIVES AND THEIR MEDICAL USE - This invention relates to novel 2,3-diamino-quinazolinone derivatives having medical utility, to use of the 2,3-diamino-quinazolinone derivatives of the invention for the manufacture of a medicament, to pharmaceutical compositions comprising the 2,3-diamino-quinazolinone derivatives of the invention, and to methods of treating a disorder, disease or a condition of a subject, which disorder, disease or condition is responsive to activation of K | 06-24-2010 |
20100160316 | QUINAZOLINES USEFUL AS MODULATORS OF ION CHANNELS - The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels and calcium 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. | 06-24-2010 |
20100160317 | 2-(2-OXOINDOLINE-3-YLIDENE)METHYL-5-(2-HYDROXY-3-MORPHOLIN-4-YL-PROPYL)-6,- 7-DIHYDRO-1H-PYRROL[3,2-C]PYRIDINE-4(5H)-ONE COMPOUNDS AND USE AS PROTEIN KINASE INHIBITORS - Pyrrolo[3,2-c]pyridine-4-one-2-indolinone compounds, especially 2-(2-oxoindoline-3-ylidene)methyl-5-(2-hydroxy-3-morpholin-4-yl-propyl)-6,7-dihydro-1H-pyrrol[3,2-c]pyridine-4(5H)-one compounds. Their preparation and pharmaceutical composition, and pharmaceutical use as protein kinase inhibitors. | 06-24-2010 |
20100179142 | Cancer Combination Therapy Comprising AZD2171 and ZD1839 - The present invention relates to a method for the production of an antiangiogenic and/or vascular permeability reducing effect in a warm-blooded animal such as a human which is optionally being treated with ionising radiation, particularly a method for the treatment of a cancer, particularly a cancer involving a solid tumour, which comprises the administration of AZD2171 in combination with ZD1839; to a pharmaceutical composition comprising AZD2171 and ZD1839; to a combination product comprising AZD2171 and ZD1839 for use in a method of treatment of a human or animal body by therapy; to a kit comprising AZD2171 and ZD1839; to the use of AZD2171 and ZD1839 in the manufacture of a medicament for use in the production of an antiangiogenic and/or vascular permeability reducing effect in a warm-blooded animal such as a human which is optionally being treated with ionising radiation. | 07-15-2010 |
20100179143 | NAPHTHYRIDINE, DERIVATIVES AS P13 KINASE INHIBITORS - Invented is a method of inhibiting the activity/function of PI3 kinases using naphthyridine derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of naphthyridine derivatives. | 07-15-2010 |
20100179144 | QUINAZOLINE DERIVATIVES AS P13 KINASE INHIBITORS - Invented is a method of inhibiting the activity/function of PI3 kinases using quinazoline derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of quinazoline derivatives. | 07-15-2010 |
20100204224 | AZACYCLIC COMPOUNDS AS INHIBITORS OF SENSORY NEURONE SPECIFIC SODIUM CHANNELS - Compounds of the formula (I), and pharmaceutically acceptable salts thereof, are found to be antagonists of SNS sodium channels. They are therefore useful as analgesic and neuroprotective agents; wherein (1) represents (A), (B) or (C); R | 08-12-2010 |
20100204225 | Organic compounds - There are provided according to the invention compounds of formula (I), in free or salt form, wherein R | 08-12-2010 |
20100204226 | QUINAZOLINONES AS PROLYL HYDROXYLASE INHIBITORS - Quinazolinone compounds of formula (I) are described, | 08-12-2010 |
20100216791 | PYRIDINYLQUINAZOLINAMINE DERIVATIVES AND THEIR USE AS B-RAF INHIBITORS - The invention relates to chemical compounds of the formula (I) or pharmaceutically acceptable salts thereof, which possess B-Raf inhibitory activity and are accordingly useful for their anti cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm blooded animal such as man. | 08-26-2010 |
20100222344 | 4-ANILINO-SUBSTITUTED QUINAZOLINE DERIVATIVES AS TYROSINE KINASE INHIBITORS - A quinazoline derivative of the Formula (I): | 09-02-2010 |
20100227862 | DIAZA-SPIRO [4.5] DECANES USEFUL AS PESTICIDES - A method of combating and controlling insects, acarines, nematodes or molluscs which comprises applying to a pest, to a locus of a pest, or to a plant susceptible to attack by a pest an insecticidally, acaricidally, nematicidally or molluscicidally effective amount of a compound of formula (I) wherein Y is a single bond, C═O, C═S or S(O) | 09-09-2010 |
20100240649 | QUINAZOLINE AND QUINOLINE DERIVATIVES AS IRREVERSIBLE PROTEIN TYROSINE KINASE INHIBITORS - A compound of formula (I), | 09-23-2010 |
20100267717 | Novel Heterocyclic NF-kB Inhibitors - The present invention relates in one embodiment to compounds of formula (Ih) and/or a pharmaceutically acceptable salt thereof with an acid or a base, and/or a pharmaceutically acceptable prodrug and/or a stereoisomer thereof, | 10-21-2010 |
20100267718 | Bicyclic heterocycles, pharmaceutical compositions containing these compounds, their use and processes for preparing them - The present invention relates to bicyclic heterocycles of general formula | 10-21-2010 |
20100273793 | 6-ARYL/HETEROALKYLOXY BENZOTHIAZOLE AND BENZIMIDAZOLE DERIVATIVES, METHOD FOR PREPARING SAME, APPLICATION THEREOF AS DRUGS, PHARMACEUTICAL COMPOSITIONS AND NOVEL USE IN PARTICULAR AS c-MET INHIBITORS - The disclosure relates to compounds of formula (I): | 10-28-2010 |
20100273794 | Benzimidazolone Compounds Having 5-HT4 Receptor Agonistic Activity - This invention provides a compound of the formula (I): | 10-28-2010 |
20100280028 | CXCR3 RECEPTOR ANTAGONISTS - The present invention relates to compounds of formula (I): | 11-04-2010 |
20100280029 | NOVEL COMPOUNDS - The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): | 11-04-2010 |
20100286142 | 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, and forms thereof are active on each of BRaf and c-Raf-1 protein kinase, and may also be active on either or both of A-Raf and B-Raf V600E protein kinase. Also described are methods of use thereof to treat diseases and conditions, including melanoma, colorectal cancer, thyroid cancer, ovarian cancer, and biliary tract cancer. | 11-11-2010 |
20100286143 | Methods and materials for genetic analysis of tumors - This invention relates generally to methods and materials for rapid detection of mutations for tumor genotyping. | 11-11-2010 |
20100298321 | BCL-2-SELECTIVE APOPTOSIS-INDUCING AGENTS FOR THE TREATMENT OF CANCER AND IMMUNE DISEASES - Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 or Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which are expressed anti-apoptotic Bcl-2 protein. | 11-25-2010 |
20100298322 | Quinazolines and Related Heterocyclic Compounds, and Their Therapeutic Use - A compound of the formula (I) wherein X is CR | 11-25-2010 |
20100305119 | Method for the treatment of anthrax infections - A method of treating an anthrax infection wherein a compound of formula I | 12-02-2010 |
20100305120 | COMPOUNDS FOR TREATING MUSCULAR DYSTROPHY - Compounds of formula (I): wherein X, L | 12-02-2010 |
20100305121 | NOVEL ANTAGONISTS OF THE HUMAN FATTY ACID SYNTHASE THIOESTERASE - The present invention provides for compounds of formula (I)-(XIII), as well as pharmaceutically acceptable salts thereof, metabolites thereof, pro-drugs thereof, and pharmaceutical kits that include such compounds. The present invention also provides for the compounds of formula (I)-(XIII) for use in medical therapy or diagnosis. The present invention also provides for the use of the compounds of formula (I)-(XIII) in treating cancer in mammals (e.g., humans), as well inhibiting tumor cell growth in such mammals. The present invention also provides for methods of inhibiting FAS. The methods include contacting FAS with an effective amount of a compound of formula (I)-(XIII). The present invention also provides for methods of inhibiting the TE domain of the FAS. The methods include contacting the thioesterase TE domain of the FAS with an effective amount of a compound of formula (I)-(XIII). The present invention also provides for methods of treating cancer in mammals, as well as methods of inhibiting tumor cell growth in such mammals. The methods include administering a compound of formula (I)-(XIII) to a mammal in need of such treatment. | 12-02-2010 |
20100305122 | APOPTOSIS INDUCING AGENTS FOR THE TREATMENT OF CANCER AND IMMUNE AND AUTOIMMUNE DISEASES - Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein. | 12-02-2010 |
20100317659 | JAK KINASE MODULATING COMPOUNDS AND METHODS OF USE THEREOF - Provided herein are quinazoline compounds for treatment of JAK kinase mediated diseases, including JAK2 kinase-, JAK3 kinase- or TYK2 kinase-mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions. | 12-16-2010 |
20100317660 | Mediators of hedgehog signaling pathways, compositions and uses related thereto - The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function comprising contacting the cell with a hedgehog antagonist of formula (I) in a sufficient amount to aberrant growth state, e.g., to agonize a normal ptc pathway or antagonize smoothened or hedgehog activity. | 12-16-2010 |
20100324041 | PYRROLOPYRIDINES AS KINASE INHIBITORS - Compounds of Formula (I) are useful for inhibition of CHK1 and/or CHK2. Methods of using compounds of Formula (I) and stereoisomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed. Formula, (I). | 12-23-2010 |
20110003810 | HETEROCYCLIC COMPOUNDS AND THEIR USE AS GLYCOGEN SYNTHASE KINASE-3 INHIBITORS - The present invention relates to novel heterocyclic compounds which are useful for inhibiting glycogen synthase kinase 3 (GSK-3), methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds. | 01-06-2011 |
20110009406 | TETRAHYDRO-1H-PYRROLO FUSED PYRIDONES - The present invention relates to tetrahydro-1H-pyrrolo fused pyridone compounds useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions. | 01-13-2011 |
20110028473 | METHODS OF TREATING DRUG RESISTANT AND OTHER TUMORS BY ADMINISTERING 6,7-DIALKOXY QUINAZOLINE DERIVATIVES - Methods employing and uses of a compound of formula (I) in inhibiting the growth of a tumor cell in a subject in need thereof. Methods employing and uses of a compound of formula (I) in treating pancreatic cancer in a subject in need of treatment for pancreatic cancer. Methods employing and uses of a compound of formula (I) in treating HER-2 positive breast cancer in a subject in need of treatment for HER-2 positive breast cancer. Methods employing and uses of a compound of formula (I) in treating drug resistant non-small cell lung cancer in a subject in need of treatment for drug resistant non-small cell lung cancer. Each of these methods can include administering to the subject an effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof. | 02-03-2011 |
20110034459 | 6,7-DIALKOXY QUINAZOLINE DERIVATIVES AND METHODS OF TREATING DRUG RESISTANT AND OTHER TUMORS - Compounds of formula (I) | 02-10-2011 |
20110039844 | 6-7,DIALKOXY QUINAZOLINE DERIVATIVES USEFUL FOR TREATMENT OF CANCER RELATED DISORDERS - In view of the great potential the quinazoline class of compounds offer, we started the synthesis and screening of a large number of new chemical entities with novel structural features. It has been surprisingly and unexpectedly found that quinazolines having 3-Ethynyl anilino group at the 4th position and specifically substituted alkoxy groups in the 6 and 7 positions, impart much enhanced and special anti-proliferative properties when compared to other prominent members of the quinazoline class of drugs. Also, surprisingly the compounds of this invention are much less toxic and the safety profile is exceedingly beneficial for therapeutic applications. The novel chemical entities described in this invention are designated by the general structure (I) and have not been synthesized earlier nor investigated for their therapeutic benefits and safety profile. Compound (I) is NRC-2694, when structure (A). | 02-17-2011 |
20110039845 | 2-AMINOQUINAZOLINE DERIVATIVE - A 2-aminoquinazoline derivative represented by formula (I) {wherein R | 02-17-2011 |
20110046132 | BENZOIMIDAZOLES AS PROLYL HYDROXYLASE INHIBITORS - The present invention is directed to benzoimidazole compounds of the formula (1) and enantiomers, diastereomers, racemates, and pharmaceutically acceptable salts thereof. Compounds of the present invention are useful in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions modulated by prolyl hydroxylase activity. | 02-24-2011 |
20110053931 | QUINOLINE COMPOUNDS AND METHODS OF USE - Compounds of Formula (I), and stereoisomers, geometric isomers, tautomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof, are useful for inhibiting receptor tyrosine kinases and for treating hyperproliferative disorders mediated thereby. Methods of using compounds of Formula (I), and stereoisomers, geometric isomers, tautomers, solvates and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed. | 03-03-2011 |
20110053932 | 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 Alk, Abl, Aurora-A, B-Raf, C-Raf, Bcr-Abl, BRK, Blk, Bmx, BTK, C-Kit, C-Raf, C-Src, EphB1, EphB2, EphB4, FGFR1, FGFR2, FGFR3, FLT1, Fms, Flt3, Fyn, FRK3, JAK2, KDR, Lck, Lyn, PDGFRα, PDGFRβ, PKCα, p38, Src, SIK, Syk, Tie2 and TrkB kinases. | 03-03-2011 |
20110059962 | TRANSCRIPTION FACTOR MODULATING COMPOUNDS AND METHODS OF USE THEREOF - Substituted benzoimidazole compounds useful as anti-infectives that decrease resistance, virulence, or growth of microbes are provided. Methods of using substituted benzimidazole compounds, in, e.g., reducing virulence and infectivity, inhibiting biofilms and treating bacterial infections, are also provided. | 03-10-2011 |
20110059963 | COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR - Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases. | 03-10-2011 |
20110065702 | INDAZOLYL, BENZIMIDAZOLYL, BENZOTRIAZOLYL SUBSTITUTED INDOLINONE DERIVATIVES AS KINASE INHIBITORS USEFUL IN THE TREATMENT OF CANCER - The present invention is directed to a compound is represented by Structural Formula (A):or a pharmaceutically acceptable salt therof. The present invention is also directed to a pharmaceutical composition comprising a compound represented by Structural Formula (A) described above or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or diluent. Also disclosed is a method of treating a subject having cancer, wherein the method comprises administering a therapeutically effective amount of a compound represented by Structural Formula (A) described above or a pharmaceutically acceptable salt thereof. | 03-17-2011 |
20110071148 | COMPOUNDS AS THE ESTROGEN RELATED RECEPTORS MODULATORS AND THE USES THEREOF - The compounds according to formula VIII, their pharmaceutically acceptable acid or base addition salts, and the uses thereof is disclosed. These compounds and their pharmaceutically acceptable acid or base addition salts can be used for the preparing a medicament for modulating estrogen related receptor (ERR), and treating metabolic diseases, such as high blood fat, fatty liver, hyperglycemia, diabetes, obesity, etc. The definition of the groups of the formula is defined as the description. | 03-24-2011 |
20110077245 | SUBSTITUTED 2-ALKYL QUINAZOLINONE DERIVATIVES AS PARP INHIBITORS - The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) | 03-31-2011 |
20110077246 | BICYCLIC HETEROCYCLIC COMPOUNDS PHARMACEUTICAL COMPOSITIONS CONTAINING THESE COMPOUNDS, THEIR USE AND PROCESS FOR PREPARING THE SAME - The present invention relates methods for treating disease conditions selected from the list consisting of benign or malignant tumors, diseases of the airways and lungs, diseases of the gastrointestinal tract, the bile duct and the gall bladder by administration to a patient in need thereof of a therapeutically effective amount of a bicyclic heterocyclic groups of general formula | 03-31-2011 |
20110082140 | 6-(PYRROLOPYRIDINYL) PYRIMIDIN-2-YLAMINE DERIVATIVES AND THE USE THEREOF FOR THE TREATMENT OF CANCER AND AIDS. - Compounds of the formula (I), in which R | 04-07-2011 |
20110082141 | 1-BENZYL-3-HYDROXYMETHYLINDAZOLE DERIVATIVES AND USE THEREOF IN THE TREATMENT OF DISEASES BASED ON THE EXPRESSION OF MCP-1, CX3CR1 AND P40 - The present invention relates to novel 1-benzyl-3-hydroxymethylindazole derivatives according to Formula (I) described in the claims, and to a pharmaceutical composition comprising them, together with a pharmaceutically acceptable vehicle. In addition, the present invention relates to the use of 1-benzyl-3-hydroxymethylindazole derivatives for the preparation of a pharmaceutical composition that is active in the treatment of diseases based on the expression of MCP-1, CX3CR1 and p40, and to their use in a method for treating or preventing diseases based on the expression of MCP-1, CX3CR1 and p40. | 04-07-2011 |
20110082142 | SELECTIVE KINASE INHIBITORS - A compound of the general formula (I) or pharmaceutically acceptable prodrugs, salts, hydrates, solvates, crystal forms or diastereomers thereof, wherein A represents a variety of six membered nitrogen containing heterocyclic rings, Q is a bond, halogen, C | 04-07-2011 |
20110082143 | Bicyclic Heteroaryl Compounds - Bicyclic heteroaryl compounds of formula (I) shown below are disclosed. Each variable in formula (I) is defined in the specification. Also disclosed is treatment of cancer with these compounds. | 04-07-2011 |
20110086853 | Therapeutic Compounds - Compounds of formula I or pharmaceutically acceptable salts thereof: | 04-14-2011 |
20110092501 | NOVEL INHIBITORS - The invention relates to novel pyrrolidine derivatives of formula (I): | 04-21-2011 |
20110092502 | DIAMINOTHIAZOLES USEFUL AS AXL INHIBITORS - Diaminothiazoles and pharmaceutical compositions containing them are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the diaminothiazoles in treating diseases or conditions associated with Axl activity are also disclosed. | 04-21-2011 |
20110112091 | DERIVATIVES OF TETRABROMOBENZIMIDAZOLE, A PROCESS FOR THE PREPARATION THEREOF, A PHARMACEUTICAL COMPOSITION COMPRISING THE SAME, A METHOF OF USING THE SAME, A METHOD FOR MODULATING OR REGULATING SERINE/THREONINE KINASES, AND SERINE/THREONINE KINASES MODULATING AGENT - A derivative of tetrabromobenzimidazole, a process for the preparation thereof, a pharmaceutical composition, a method for using the same, a method for modulating or regulating serine/threonine kinases, and a serine/threonine kinases modulating agent. The invention relates to novel small-molecule compounds with kinase inhibitory activity, having superior properties as pharmaceutical agents, production method thereof and uses thereof. In particular, this invention relates to new derivatives of tetrabromobenzimidazole with Pim kinases inhibitory properties, which exhibits superior pharmacological actions, and can be useful for the treatment of disease conditions, especially cancers depending on Pim kinases, such as leukemias and prostate cancer. | 05-12-2011 |
20110118258 | QUINAZOLIN-OXIME DERIVATIVES AS HSP90 INHIBITORS - Compounds of general formula (I); or a stereoisomers, tautomers, pharmaceutically acceptable salts, or prodrugs thereof, wherein R1, R2, R3, R4, R5, R6, R8 and R9 are as defined herein, are useful for the treatment of diseases and conditions which are mediated by excessive or inappropriate Hsp90 activity such as cancers, viral infection and inflammatory diseases or conditions. | 05-19-2011 |
20110118259 | 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. | 05-19-2011 |
20110124642 | POTASSIUM CHANNEL MODULATORS - Disclosed herein are KCNQ potassium channels modulators of formula (I) | 05-26-2011 |
20110124643 | PYRIDINOPYRIDINONE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF - The present invention relates to pyridopyridone derivatives of formula (I): | 05-26-2011 |
20110130398 | SPIROINDOLINONE PYRROLIDINES - There are provided compounds of the formula | 06-02-2011 |
20110130399 | Phthalazine Derivatives with Angiogenesis Inhibiting Activity - The invention relates to new phthalazine derivatives of formula I, | 06-02-2011 |
20110130400 | TRPV4 ANTAGONISTS - The present invention relates to diazabicyclo[2.2.1]hept-2-yl analogs, pharmaceutical compositions containing them and their use as TRPV4 antagonists. | 06-02-2011 |
20110136805 | BICYCLIC HETEROCYCLES, MEDICAMENTS CONTAINING SAID COMPOUNDS, USE THEREOF, AND METHOD FOR PRODUCTION OF SAME - The present invention relates to bicyclic heterocycles of general formula | 06-09-2011 |
20110136806 | Bicyclic heterocycles, pharmaceutical compositions containing these compounds, the use thereof and processes for the preparation thereof - The invention relates to bicyclic heterocycles of general formula (I), in which R | 06-09-2011 |
20110144105 | AZAINDOLE GLUCOKINASE ACTIVATORS - Provided herein are compounds of the formula (I): | 06-16-2011 |
20110152260 | Indazole derivatives as modulators of interleukin-1 receptor-associated kinase - The present invention relates to modulators of IRAK kinases of formula (I) and provides compositions comprising such modulators, as well as methods therewith for treating IRAK-mediated or IRAK-associated conditions or diseases. | 06-23-2011 |
20110160204 | PYRIDOPYRAZINES AND DERIVATIVES THEREOF AS ALK AND c-MET INHIBITORS - The present invention provides a compound of Formula I | 06-30-2011 |
20110160205 | NOVEL 1-BENZYL-3-HYDROXYMETHYLINDAZOLE DERIVATIVES AND USE THEREOF IN THE TREATMENT OF DISEASES BASED ON THE EXPRESSION OF MCP-1, CX3CR1 AND P40 - The present invention relates to novel 1-benzyl-3-hydroxymethylindazole derivatives according to formula (I) described in the claims, and to a pharmaceutical composition comprising them, together with a pharmaceutically acceptable vehicle. In addition, the present invention relates to the use of 1-benzyl-3-hydroxymethylindazole derivatives for the preparation of a pharmaceutical composition that is active in the treatment of diseases based on the expression of MCP-1, CX3CR1 and p40, and to their use in a method for treating or preventing diseases based on the expression of MCP-1, CX3CR1 and p40. | 06-30-2011 |
20110178083 | PDE-10 INHIBITORS - Vicinal substituted cyclopropyl compounds which are inhibitors of phosphodiesterase 10 are described as are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function, for example neurological, neurodegenerative and psychiatric disorders including, but not limited to, those comprising cognitive deficits or schizophrenic symptoms. | 07-21-2011 |
20110183973 | Novel Compounds - The invention is directed to certain novel compounds directed to compounds of formula (I) and salts thereof. The compounds of the invention are inhibitors of PI3-kinase activity. | 07-28-2011 |
20110183974 | 1,2,4-OXADIAZOLE SUBSTITUTED PIPERIDINE AND PIPERAZINE DERIVATIVES AS SMO ANTAGONISTS - The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts, stereoisomers or tautomers thereof which are inhibitors of the Sonic Hedgehog pathway, in particular Smo antagonists. Thus the compounds of this invention are useful for the treatment of diseases associated with abnormal hedgehog pathway activation, including cancer, for example basal cell carcinoma, medulloblastoma, prostate, pancreatic, breast, colon, bone and small cell lung cancers, and cancers of the upper GI tract. | 07-28-2011 |
20110183975 | NOVEL 6-AZAINDOLE AMINOPYRIMIDINE DERIVATIVES HAVING NIK INHIBITORY ACTIVITY - The present invention relates to a compound of formula I: wherein: R | 07-28-2011 |
20110195964 | NOVEL CYCLIC BENZIMIDAZOLE DERIVATIVES USEFUL AS ANTI-DIABETIC AGENTS - Novel compounds of the structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension. | 08-11-2011 |
20110201608 | SUBSTITUTED NAPHTHYRIDINES AND USE THEREOF AS MEDICINES - The invention relates to new substituted naphthyridines of formula 1, as well as pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates or solvates thereof, | 08-18-2011 |
20110207731 | SUBSTITUTED 4-(INDAZOLYL)-1,4-DIHYDROPYRIDINES AND METHODS OF USE THEREOF - This invention relates to novel 4-(indazolyl)-1,4-dihydropyridine og the following formula (I) derivatives having protein tyrosine kinase inhibitory activity, to a process for the manufacture thereof and to the use thereof for the treatment of c-Met-mediated diseases or c-Met-mediated conditions, particularly cancer and other proliferative disorders. | 08-25-2011 |
20110207732 | AZAINDOLE DERIVATIVES - Compounds of the formula (I), in which X | 08-25-2011 |
20110212961 | Pyrazole Derivatives as Kinase Inhibitors - The present invention provides compounds having the general structure I, or a pharmaceutically acceptable salt thereof: | 09-01-2011 |
20110218198 | Pyrrolopyridinylpyrimidin-2-ylamine derivatives - Compounds of the formula I in which X, R | 09-08-2011 |
20110224205 | USE OF CURCUMIN OR ITS ANALOGUES IN CANCER THERAPY UTILIZING EPIDERMAL GROWTH FACTOR RECEPTOR TYROSINE KINASE INHIBITOR - Provided is combined use of an epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) and curcumin or its analogue in cancer therapy, which reduces side effects resulting from the EGFR-TKI and reduces doses of the EGFR-TKI needed for the therapy, particular in a patient resistant to the treatment with the EGFR-TKI alone. | 09-15-2011 |
20110230482 | COMPOUNDS MODULATING C-FMS AND/OR C-KIT ACTIVITY - 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. | 09-22-2011 |
20110245246 | Quinazoline Derivatives Useful as Anti-Tumor Medicament - he present invention has disclosed a compound of formula I and a pharmaceutically acceptable salt or a solvate thereof, wherein the substituents are as defined in the description. The invention has also disclosed a method for preparing the compound of formula I, the pharmaceutical compositions comprising the same and their uses in the preparation of an anti-tumor medicament. | 10-06-2011 |
20110251194 | ANTINEOPLASTIC DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF - The disclosure concerns heterobicyclic compounds of general formula (I) and acid addition salts, hydrates and solvates thereof, as well as enantiomers, diastereoisomers and mixtures thereof. Methods for preparing the compounds, pharmaceutical compositions, and methods of treatment also are disclosed. | 10-13-2011 |
20110263598 | KINASE INHIBITORS AND METHOD OF TREATING CANCER - The invention is directed to a compound represented by the following structural formula and pharmaceutically acceptable salts thereof: | 10-27-2011 |
20110269758 | NAPHTHYRIDINONES AS PROTEIN KINASE INHIBITORS - Naphthyridinone derivative compounds that inhibit Aurora kinase enzymes are disclosed along with pharmaceutical compositions comprising these compounds and methods for synthesizing the same. Such compounds have utility in the treatment of proliferative diseases resulting from unregulated and/or disturbed Aurora kinases such as cancers, psoriasis, viral and bacterial infections, inflammatory and autoimmune diseases. | 11-03-2011 |
20110281867 | COMPOSITIONS AND METHODS OF USE FOR TYROSINE KINASE INHIBITORS TO TREAT PATHOGENIC INFECTION - Compositions and methods are provided for using tyrosine kinase inhibitors to treat pathogenic infection. In particular, methods for using Abl-family tyrosine kinase inhibitors to treat pathogenic infection are provided. Infections to be treated according to the present invention include, particularly, those caused by microbial pathogens such as bacteria and viruses. | 11-17-2011 |
20110281868 | INDAZOLE INHIBITORS OF KINASE - The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, | 11-17-2011 |
20110294806 | AZAINDOLE DERIVATIVES AS KINASE INHIBITORS - This invention relates to compounds of the general formula (I) in which the variable groups are as defined herein, and to their preparation and use. | 12-01-2011 |
20110294807 | COMPOUNDS FOR THE PREVENTION AND TREATMENT OF CARDIOVASCULAR DISEASE - Disclosed are novel compounds that are useful for regulating the expression of apolipoprotein A-I (ApoA-I), and their use for the treatment and prevention of cardiovascular disease and related disease states, including cholesterol- or lipid-related disorders, such as, for example, atherosclerosis. Also disclosed are pharmaceutical compositions comprising the novel compounds. Formula (I) | 12-01-2011 |
20110294808 | Indazole Compounds As CCR1 Receptor Antagonists - Disclosed indazoles compounds that are useful as antagonists of CCR1 activity and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are 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. | 12-01-2011 |
20110301161 | BENZIMIDAZOLE INHIBITORS OF LEUKOTRIENE PRODUCTION - The present invention relates to compounds of formula (I): | 12-08-2011 |
20110301162 | AURORA KINASE MODULATORS AND METHODS OF USE - The present invention relates to chemical compounds having a general formula I | 12-08-2011 |
20110306611 | Transcription factor modulating compounds and methods of use thereof - Substituted benzoimidazole compounds useful as anti-infectives that decrease resistance, virulence, or growth of microbes are provided. Methods of making and using substituted benzoimidazole compounds, as well as pharmaceutical preparations thereof, in, e.g., reducing antibiotic resistance and inhibiting biofilms. | 12-15-2011 |
20110306612 | QUINAZOLINONE, QUINOLONE AND RELATED ANALOGS AS SIRTUIN MODULATORS - Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent. | 12-15-2011 |
20110306613 | CHEMICAL COMPOUNDS - There is provided pyrimidinyl compounds of Formula (I), | 12-15-2011 |
20110312959 | Derivatives of Azaindoles as Inhibitors of Protein Kinases ABL and SRC - The present invention relates to compounds of general formula I and use thereof as inhibitors of protein kinases AbI and Src and the method of production thereof. The present invention also relates to pharmaceutical compositions and medici-nal products comprising these compounds. | 12-22-2011 |
20120010204 | Phthalazinone Derivatives - Compounds of the formula (I): | 01-12-2012 |
20120040983 | Phthalazine Compounds as P38 Map Kinase Modulators and Methods of Use Thereof - The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I wherein A | 02-16-2012 |
20120046284 | Salts and hydrates of 4-[(3-chloro-4-fluoro-phenyl)amino]-6-(cis-4--cyclohexan-1-yloxy)-7-metho- xy-quinazoline, their use as a medicament and the preparation thereof - The present invention relates to a compound of formula (I), | 02-23-2012 |
20120046285 | BRADYKININ RECEPTOR AGONISTS AND USES THEREOF TO TREAT OCULAR HYPERTENSION AND GLAUCOMA - The invention provides compositions and methods for treating and/or preventing ocular disorders associated with increased intraocular pressure. In particular, the compounds are bradykinin agonists. | 02-23-2012 |
20120046286 | Novel Compounds - The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): | 02-23-2012 |
20120059002 | NOVEL ANTI-INFLAMMATORY AGENTS - Disclosed are methods of regulating interleukin-6 (IL-6) and/or vascular cell adhesion molecule-1 (VCAM-1) and methods of treating and/or preventing cardiovascular and inflammatory diseases and related disease states, such as, for example, atherosclerosis, asthma, arthritis, cancer, multiple sclerosis, psoriasis, and inflammatory bowel diseases, and autoimmune disease(s) by administering a naturally occurring or synthetic quinazolone derivative. The invention provides novel synthetic quinazolone compounds, as well as pharmaceutical compositions comprising those compounds. | 03-08-2012 |
20120059003 | INHIBITORS OF INV(16) LEUKEMIA - This invention describes the development of targeted small molecule inhibitors of the inv(16) fusion, the causative agent in ˜12% of acute myeloid leukemia (AML). The inv(16) fusion results in expression of the CBFβ-SMMHC fusion protein in the blood cells of afflicted patients. The present invention provides compounds which inhibit the function of both CBFβ and the CBFβ-SMMHC fusion. These compounds block the growth of an inv(16) leukemia cell line as well as increase its apoptosis, while showing minimal effects against non inv(16) cell lines. As a mechanism to develop inhibitors with selectivity for the CBFβ-SMMHC fusion protein, the present invention further provides dimeric derivatives of these compounds which show both increased potency as well selectivity for CBFβ-SMMHC. These compounds show potent inhibition of an inv(16) leukemia cell line with minimal effects on non inv(16) cell lines. Analysis of the pharmacokinetics of the developed compounds has made it possible to improve the lifetime of the compound in the plasma of mice to a level commensurate with long-term treatment. | 03-08-2012 |
20120071477 | CDKI PATHWAY INHIBITORS AND USES THEREOF - The invention relates to the compounds and methods for inhibiting the Cyclin-Dependent Kinase Inhibitor (CDKI) pathway. More particularly, the invention relates to compounds and methods for inhibiting the CDKI pathway for studies of and intervention in senescence-related and other CDKI-related diseases. | 03-22-2012 |
20120077811 | PRODRUG FORMS OF KINASE INHIBITORS AND THEIR USE IN THERAPY - The invention provides novel prodrug compounds comprising a kinase inhibitor and a reductively-activated fragmenting aromatic nitroheterocycle or aromatic nitrocarbocycle trigger, where the compound carries a positive charge. In preferred embodiments, the compounds are of Formula I: | 03-29-2012 |
20120083493 | SMALL-MOLECULE MODULATORS OF TRP-P8 ACTIVITY - Provided are small-molecule Trp-p8 modulators, including Trp-p8 agonists and Trp-p8 antagonists, and compositions comprising small-molecule Trp-p8 agonists as well as methods for identifying and characterizing novel small-molecule Trp-p8 modulators and methods for decreasing viability and/or inhibiting growth of Trp-p8 expressing cells, methods for activating Trp-p8-mediated cation influx, methods for stimulating apoptosis and/or necrosis, and related methods for the treatment of diseases, including cancers such as lung, breast, colon, and/or prostate cancers as well as other diseases, such as benign prostatic hyperplasia, that are associated with Trp-p8 expression. | 04-05-2012 |
20120088767 | BENZIMIDAZOLE DERIVATIVES AS PI3 KINASE INHIBITORS - This invention relates to the use of benzimidazole derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3′ OH kinase family (hereinafter PI3 kinases), suitably, PI3Kα, PI3Kβ, PI3Kβ, and/or PI3Kγ. Suitably, the present invention relates to the use of benzimidazoles in the treatment of one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries. More suitably, the present invention relates to PI3Kβ selective benzimidazoles compounds for treating cancer. | 04-12-2012 |
20120094997 | SUBSTITUTED HYDROXAMIC ACIDS AND USES THEREOF - This invention provides compounds of formula (I): | 04-19-2012 |
20120101096 | Compounds and Methods for Treating Mammalian Gastrointestinal Microbial Infections - Described herein are compounds, and pharmaceutically acceptable salts and prodrugs thereof, which are useful as inhibitors of IMPDH. In certain embodiments, a compound of the invention selectively inhibits a parasitic IMPDH versus a host IMPDH. Further, the invention provides pharmaceutical compositions comprising one or more compounds of the invention. The invention also relates to methods of treating various parasitic and bacterial infections in mammals. Moreover, the compounds may be used alone or in combination with other therapeutic or prophylactic agents, such as anti-virals, anti-inflammatory agents, antimicrobials and immunosuppressants. | 04-26-2012 |
20120108590 | MELT-EXTRUDED SOLID DISPERSIONS CONTAINING AN APOPTOSIS-INDUCING AGENT - A pro-apoptotic solid dispersion comprises, in essentially non-crystalline form, a Bcl-2 family protein inhibitory compound of Formula I as defined herein, dispersed in a solid matrix that comprises (a) a pharmaceutically acceptable water-soluble polymeric carrier and (b) a pharmaceutically acceptable surfactant. A process for preparing such a solid dispersion comprises subjecting to elevated temperature the compound of Formula I, the water-soluble polymeric carrier and the surfactant, to provide an extrudable semi-solid mixture; extruding the semi-solid mixture; and cooling the resulting extrudate to to provide a solid matrix comprising the polymeric carrier and the surfactant and having the compound dispersed in essentially non-crystalline form therein. The solid dispersion is suitable for oral administration to a subject in need thereof for treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer or an immune or autoimmune disease. | 05-03-2012 |
20120122863 | Quinazolinedione Chymase Inhibitors - Disclosed are small molecule inhibitors which are useful in treating various diseases and conditions involving Chymase. | 05-17-2012 |
20120122864 | INHIBITORS OF HCV NS5A - Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C. | 05-17-2012 |
20120129853 | METHODS OF TREATMENT USING SELECTIVE BCL-2 INHIBITORS - This invention pertains to methods of treating systemic lupus erythematosus, lupus nephritis or Sjogren's Syndrome with compounds that selectively inhibit the activity of Bcl-2 anti-apoptotic proteins. Specifically, the current invention is directed to treatment with compounds that selectively inhibit the activity of Bcl-2 proteins, with a lesser affinity for inhibiting the activity of other BCL-2 family proteins, including Bcl-x | 05-24-2012 |
20120129854 | 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 yield of veterinary medicine. The compounds are represented by formula (I): wherein the respective substituents are defined in the specification. | 05-24-2012 |
20120129855 | PHTHALAZINONE DERIVATIVES - A compound of the formula (I): | 05-24-2012 |
20120135989 | AZAINDOLE DERIVATIVE - The present invention provides a (di)azaindole derivative represented by the formula (I). A compound of the present invention inhibits a Cdc7 protein kinase activity and suppresses cell proliferation. | 05-31-2012 |
20120135990 | IAP INHIBITORS - The present invention describes compounds, processes for their preparation, pharmaceutical compositions containing them, and their use in therapy. | 05-31-2012 |
20120142685 | ORGANIC COMPOUNDS - The present invention provides a compound formula I: (formula I) said compound is inhibitor of selective subset of kinases belonging to the AGC or calmodulin kinase family, such as for example MARK1/2/3, PKD-1/2/3, PKN-1/2, CDK-9, CaMKII, ROCK-I/II, inhibitors of histone deacetylase (HDAC) phosphorylation, or inhibitors of other kinases. Finally, the present invention also provides a pharmaceutical composition. | 06-07-2012 |
20120142686 | VIRAL POLYMERASE INHIBITORS - The present invention relates to viral polymerase inhibitors of formula (I), salts, N-oxides, solvates, hydrates, racemates, enantiomers or isomers thereof, processes for their preparation and their use in the treatment of Flaviviridae viral infections such as Hepatitis C virus (HCV) infections: | 06-07-2012 |
20120165330 | QUINAZOLINONE AND RELATED ANALOGS AS SIRTUIN MODULATORS - Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent. | 06-28-2012 |
20120190680 | Heteroaryl Amide Analogues - Compounds, pharmaceutical compositions, and methods of use are disclosed for heteroaryl amide analogues of formula Ia and/or Ib: | 07-26-2012 |
20120196856 | ARYL AMINOPYRIDINE PDE10 INHIBITORS - The present invention is directed to aryl aminopyridine 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. | 08-02-2012 |
20120208811 | Aminopyrazole Derivative - A compound represented by formula (I) or a pharmacologically acceptable salt thereof, which can inhibit a fibroblast growth factor receptor (FGFR) family kinase in cancer tissues. (In the formula, A represents a 5- to 10-membered heteroaryl group, or a C | 08-16-2012 |
20120208812 | DISUBSTITUTED OCTAHYDROPYRROLO[3,4-c]PYRROLES AS OREXIN RECEPTOR MODULATORS - Disubstituted octahydropyrrolo[3,4-c]pyrrole compounds are described, which are useful as orexin receptor modulators. Such compounds may be useful in pharmaceutical compositions and methods for the treatment of diseased states, disorders, and conditions mediated by orexin activity, such as insomnia. | 08-16-2012 |
20120220587 | PYRIDINYLIMIDAZOLONE DERIVATIVES FOR THE INHIBITION OF PI3 KINASES - Compounds of the formula (I), in which X | 08-30-2012 |
20120220588 | QUINAZOLINE COMPOUNDS - Disclosed are compounds having the formula: wherein R | 08-30-2012 |
20120225870 | METHODS FOR TREATING CANCER RESISTANT TO ERBB THERAPEUTICS - Provided herein are methods for treating cancer that is resistant to treatment with an anti-ErbB therapeutic agent and which is associated with an activating MET gene mutation or a MET gene amplification. The methods involve administering to a subject a combination of an anti-ErbB therapeutic and an anti-MET therapeutic. Also provided are methods for reducing ErbB mediated signaling or PI3 kinase mediated signaling in a cancer cell. | 09-06-2012 |
20120225871 | SMALL-MOLECULE MODULATORS OF TRP-P8 ACTIVITY - Provided are small-molecule Trp-p8 modulators, including Trp-p8 agonists and Trp-p8 antagonists, and compositions comprising small-molecule Trp-p8 agonists as well as methods for identifying and characterizing novel small-molecule Trp-p8 modulators and methods for decreasing viability and/or inhibiting growth of Trp-p8 expressing cells, methods for activating Trp-p8-mediated cation influx, methods for stimulating apoptosis and/or necrosis, and related methods for the treatment of diseases, including cancers such as lung, breast, colon, and/or prostate cancers as well as other diseases, such as benign prostatic hyperplasia, that are associated with Trp-p8 expression. | 09-06-2012 |
20120225872 | METHODS OF PREPARING AND USING QUINAZOLINE AND QUINOLINE DERIVATIVES - A method of preparing a compound of formula (I), | 09-06-2012 |
20120238569 | THIAZOLE AND THIOPHENE COMPOUNDS - Provided herein are compounds of the formula (I): | 09-20-2012 |
20120238570 | INHIBITORS OF THE HEDGEHOG PATHWAY - The present invention is directed to a compound of Formula I | 09-20-2012 |
20120238571 | INDAZOLE DERIVATIVES AS PI 3-KINASE - The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): | 09-20-2012 |
20120245172 | HETEROCYCLIC AMINE DERIVATIVES - The present invention relates to compounds of formula I | 09-27-2012 |
20120245173 | INHIBITION OF ACTIVATED CDC42-ASSOCIATED KINASE 1 - Compounds, compositions, and methods for specific inhibition of activated cdc42-associated kinase 1 (Ack1) are provided. | 09-27-2012 |
20120245174 | 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, and forms thereof are active on each of BRaf and c-Raf-1 protein kinase, and may also be active on either or both of A-Raf and B-Raf V600E protein kinase. Also described are methods of use thereof to treat diseases and conditions, including melanoma, colorectal cancer, thyroid cancer, ovarian cancer, and biliary tract cancer. | 09-27-2012 |
20120245175 | 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. | 09-27-2012 |
20120252806 | INHIBITORS OF AKT ACTIVITY - The instant invention provides for compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer. | 10-04-2012 |
20120258968 | 4-PHENYLAMINO-PYRIMIDINE DERIVATIVES HAVING PROTEIN KINASE INHIBITOR ACTIVITY - The invention relates compounds of general formula (I) and pharmaceutically acceptable salts and solvates thereof wherein
| 10-11-2012 |
20120270871 | PYRROLOPYRIDINYLPYRIMIDIN-2-YLAMINE DERIVATIVES - Pyrrolopyridinylpyrimidin-2-ylamine derivatives of the formula (I), in which R | 10-25-2012 |
20120277226 | BENZIMIDAZOLE INHIBITORS OF LEUKOTRIENE PRODUCTION - The present invention relates to compounds of formula (IA) and (IB): | 11-01-2012 |
20120277227 | BENZIMIDAZOLE INHIBITORS OF LEUKOTRIENE PRODUCTION - The present invention relates to compounds of formula (IA), (IB) and (IC): | 11-01-2012 |
20120277228 | Novel Azaheterocyclic Compounds - The invention provides novel substituted azaheterocyclic compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer. | 11-01-2012 |
20120277229 | SUBSTITUTED 3-(1H-BENZO[D]IMIDAZOL-2-YL)-1H-INDAZOLE ANALOGS AS INHIBITORS OF THE PDK1 KINASE - In one aspect, the invention relates to substituted 3-(1H-benzo[d]imidazol-2-yl)-1H-indazole analogs, derivatives thereof, and related compounds, which are useful as inhibitors of the PDK1 kinase; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions for treating disorders associated with dysfunction of the PDK1 kinase. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. | 11-01-2012 |
20120283258 | MEDIATORS OF HEDGEHOG SIGNALING PATHWAYS, COMPOSITIONS AND USES RELATED HERETO - The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function comprising contacting the cell with a hedgehog antagonist of formula (I) in a sufficient amount to aberrant growth state, e.g., to agonize a normal ptc pathway or antagonize smoothened or hedgehog activity. | 11-08-2012 |
20120283259 | NOVEL INHIBITORS - Novel heterocyclic derivatives as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water. | 11-08-2012 |
20120283260 | BRADYKININ RECEPTOR AGONISTS AND USES THEREOF TO TREAT OCULAR HYPERTENSION AND GLAUCOMA - The invention provides compositions and methods for treating and/or preventing ocular disorders associated with increased intraocular pressure. In particular, the compounds are bradykinin agonists. | 11-08-2012 |
20120289504 | Benzoimidazole Compounds and Uses Thereof - This invention generally relates to substituted benzoimidazole compounds, particularly methyl 2-((2-(2,6-difluoro-4-(methylcarbamoyl)phenyl)-5-methyl-1H-benzo[d]imidazol-1-yl)methyl)morpholine-4-carboxylate and salts thereof. This invention also relates to pharmaceutical compositions and kits comprising such a compound, uses of such a compound (including, for example, treatment methods and medicament preparations), processes for making such a compound, and intermediates used in such processes. | 11-15-2012 |
20120295904 | HEMATOPOIETIC GROWTH FACTOR MIMETIC SMALL MOLECULE COMPOUNDS AND THEIR USES - The present embodiments relate to compounds with physiological effects, such as the activation of hematopoietic growth factor receptors. The present embodiments also relate to use of the compounds to treat a variety of conditions, diseases and ailments such as hematopoietic conditions and disorders. | 11-22-2012 |
20120309756 | 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. | 12-06-2012 |
20120316164 | METHOD FOR INHIBITING THE GROWTH OF CANCER STEM CELLS - The present invention provides a method for inhibiting the growth of cancer stem cells, particularly colorectal cancer stem cells, liver cancer stem cells, lung cancer stem cells or breast cancer stem cells, comprising administering to a subject in need thereof a therapeutically effective amount of a compound of antimycin A or a pharmaceutically acceptable salt thereof, together with a pharmaceutically acceptable carrier. | 12-13-2012 |
20120316165 | SUBSTITUTED BENZAMIDE DERIVATIVES - The present invention relates to compounds of formula | 12-13-2012 |
20120316166 | HETARYLAMINONAPHTHYRIDINES - Novel hetarylaminonaphthyridine derivatives of formula (I) | 12-13-2012 |
20120329794 | Ab1 KINASE INHIBITORS - The present invention provides an Abelson kinase (Abl kinase) inhibitor which comprises, as an active ingredient, an indazole derivative represented by Formula (I) (wherein R | 12-27-2012 |
20120329795 | QUINAZOLINE DERIVATIVES - The invention concerns quinazoline derivatives of Formula I: | 12-27-2012 |
20130005724 | PYRIDINO-PYRIDINONE DERIVATIVES, PREPARATION AND THERAPEUTIC USE THEREOF - The present invention relates to derivatives of pyridino-pyridinones, and to their preparation and use thereof, having activity as inhibitors of kinase activity of receptors for PDGF (platelet derived growth factors) ligands and optionally of receptors for the FLT3 (fms-like tyrosine kinase receptor) ligand receptors, said derivatives comprising compounds of formula (I): | 01-03-2013 |
20130005725 | CHEMICAL COMPOUNDS - There is provided pyrimidinyl compounds of Formula (I), | 01-03-2013 |
20130005726 | COMPOSITIONS AND METHODS FOR TREATING INFLAMMATORY DISORDERS - A method for treating in a subject with an inflammatory disorder and/or immunological disorder associated with NOD2 activation includes administering to the subject a therapeutically effective amount of at least one tyro sine kinase inhibitor that substantially inhibits nucleotide-binding oligomerization domain containing 2 (NOD2):receptor-interacting protein 2 (RIP2) signaling in a NOD2-bearing cell and is not cytotoxic to the cell. | 01-03-2013 |
20130005727 | QUINAZOLINE DERIVATIVES - The invention concerns quinazoline derivatives of Formula I | 01-03-2013 |
20130012508 | NOVEL ANXIOLYTIC COMPOUNDS - The present invention relates to chemical compounds of general formula (I) | 01-10-2013 |
20130012509 | NOVEL ANXIOLYTIC COMPOUNDS - The present invention relates to chemical compounds of general formula (I) | 01-10-2013 |
20130012510 | 1-BENZYL-3-HYDROXYMETHYLINDAZOLE DERIVATIVES AND USE THEREOF IN THE TREATMENT OF DISEASES BASED ON THE EXPRESSION OF MCP-1 AND CX3CR1 - The present invention relates to novel 1-benzyl-3-hydroxymethylindazole derivatives according to formula (I) described in the claims, and to a pharmaceutical composition comprising them, together with a pharmaceutically acceptable vehicle. In addition, the present invention relates to the use of novel 1-benzyl-3-hydroxymethylindazole derivatives for the preparation of a pharmaceutical composition that is active in the treatment of diseases based on the expression of MCP-1 and CX3CR1, and to their use in a method for treating or preventing diseases based on the expression of MCP-1 and CX3CR1. | 01-10-2013 |
20130012511 | SOLUBLE GUANYLATE CYCLASE ACTIVATORS - The invention relates to compounds having the structure of Formula (I) and pharmaceutically acceptable salts thereof, which are soluble guanylate cyclase activators. The compounds are capable of modulating the body's production of cyclic guanosine monophosphate (“cGMP”) and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The compounds are useful for treatment or prevention of cardiovascular diseases, endothelial dysfunction, diastolic dysfunction, atherosclerosis, hypertension, pulmonary hypertension, angina pectoris, thromboses, restenosis, myocardial infarction, strokes, cardiac insufficiency, pulmonary hypertonia, erectile dysfunction, asthma bronchiale, chronic kidney insufficiency, diabetes, or cirrhosis of the liver. | 01-10-2013 |
20130029985 | Novel Compounds - The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): | 01-31-2013 |
20130035337 | FUSED BICYCLIC HETEROARYL DERIVATIVE - The present invention relates to a novel fused bicyclic heteroaryl derivative or a pharmacologically acceptable salt thereof, which has an excellent hypoglycemic effect or treats and/or prevents the onset of a disorder of carbohydrate or lipid metabolism or a disease mediated by peroxisome proliferator-activated receptor (PPAR) γ. | 02-07-2013 |
20130053381 | 2,4-DIOXO-1,4-DIHYDRO-2H-QUINAZOLIN-3-YL-SULFONAMIDE DERIVATIVES - The invention relates to a 2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl-sulfonamide derivative being (A) a compound of the formula (I) in which the substituents are as defined in the specification; in free form or in salt form; or (B) a compound selected from a certain group of 2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl-sulfonamide derivatives disclosed in the specification; in free form or in salt form; to their preparation, to their use as medicament and to medicaments comprising them. In a first aspect, the invention provides prodrugs of AMPA receptor antagonists which potentially useful in the treatment of a wide range of disorders, particularly epilepsy. | 02-28-2013 |
20130053382 | Inhibitors of Phosphoinositide Dependent Kinase 1 (PDK1) - The instant invention provides for compounds that inhibit PDK1 activity. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting PDK1 activity by administering the compound to a patient in need of treatment of cancer. | 02-28-2013 |
20130053383 | INDAZOLES - Herein are disclosed indazoles of formula (I) | 02-28-2013 |
20130059850 | AZA-INDOLE DERIVATIVES USEFUL AS MODULATORS OF FAAH - The present invention is directed to certain Aza-Indole derivatives which are useful as modulators of Fatty Acid Amide Hydrolase (FAAH) and as FAAH imaging agents. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzheimer Disease, and Parkinson's Disease. | 03-07-2013 |
20130065896 | FUSED IMIDAZOLE DERIVATIVE - Provided is a novel compound which shows an antagonistic effect against T-type calcium channels, and is useful as a pharmaceutical product. | 03-14-2013 |
20130072483 | SUBSTITUTED HYDROXYETHYL AMINE COMPOUNDS AS BETA-SECRETASE MODULATORS AND METHODS OF USE - The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I | 03-21-2013 |
20130072484 | TYROSINE KINASE INHIBITORS AS ANTI-KINETOPLASTID AND ANTI-APICOMPLEXAN AGENTS - The present invention provides methods of killing, inhibiting the growth, and/or inhibiting the reproduction of kinetoplastid or apicomplexan protozoan with tyrosine kinase inhibitors. | 03-21-2013 |
20130090337 | CRYSTAL OF AMIDE COMPOUND - Provision of crystal of 1-(4-methoxybutyl)-N-(2-methylpropyl)-N-[(3S,5R)-5-(morpholin-4-ylcarbonyl)piperidin-3-yl]-1H-benzimidazole-2-carboxamide hydrochloride which has a superior rennin inhibitory activity and is useful as a prophylactic or therapeutic agent for hypertension and various organ disorders caused by hypertension, and the like. Crystal of 1-(4-methoxybutyl)-N-(2-methylpropyl)-N-[(3S,5R)-5-(morpholin-4-ylcarbonyl)piperidin-3-yl]-1H-benzimidazole-2-carboxamide hydrochloride having an X-ray powder diffraction pattern showing characteristic peaks at interplanar spacings (d) of around 26.43±0.2, 7.62±0.2 and 4.32±0.2 angstroms. | 04-11-2013 |
20130096117 | Novel Compounds - The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): | 04-18-2013 |
20130096118 | CARBOLINE CARBOXAMIDE COMPOUNDS USEFUL AS KINASE INHIBITORS - Compounds having formula (I), and enantiomers, and diastereomers, stereoisomers, pharmaceutically-acceptable salts thereof, formula (I) are useful as kinase modulators, including Btk modulation. | 04-18-2013 |
20130102602 | 2-Aryl-4-Quinazolinones And Their Pharmaceutical Compositions - Provided is a compound of the formula I or a pharmaceutically acceptable salt, solvate or stereoisomer thereof: | 04-25-2013 |
20130102603 | 2,4-DIARYL - SUBSTITUTED [1,8] NAPHTHYRIDINES AS KINASE INHIBITORS FOR USE AGAINST CANCER - The present invention relates to novel [1,8]naphthyridine derivatives of formula (I) and to the use of such compounds in which the inhibition, regulation and/or modulation of signal transduction by ATP consuming proteins like kinases plays a role, particularly to inhibitors of TGF-beta receptor kinases, and to the use of such compounds for the treatment of kinase-induced diseases, in particular for the treatment of tumors. | 04-25-2013 |
20130109688 | Naphthridine derivatives as PI3K inhibitors for the treatment of cancer and immune-inflammatory disease | 05-02-2013 |
20130131059 | METHOD FOR TREATING OPHTHALMIC DISEASES USING KINASE INHIBITOR COMPOUNDS IN PRODRUG FORMS - This invention is directed to prodrugs of rho kinase (ROCK) inhibitors. These prodrugs are in general the ester or the amide derivatives of the parent compounds. These prodrugs are often weak inhibitors of ROCK, but their parent compounds have good activities. Upon instillation into the eyes, the ester or the amide group of these prodrugs is rapidly hydrolyzed into alcohol, amine, or acid, and the prodrugs are converted into the active base compounds. The prodrugs of ROCK inhibitors provide several advantages such as delivery of higher concentrations of the active species into the target site and reduction of ocular discomfort. The invention is also directed to a method of treating ophthalmic diseases such as glaucoma, allergic conjunctivitis, macular edema, macular degeneration, and blepharitis, by administering an effective amount of a ROCK prodrug compound of Formula I to the eyes of the patient in need of. | 05-23-2013 |
20130143880 | POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 - The present invention is directed to benzimidazolone derivatives which are positive allosteric modulators of the mGluR | 06-06-2013 |
20130150363 | Method of Treating Cancer Using a cMET and AXL Inhibitor and an ErbB Inhibitor - The present invention relates to a method of treating cancer in a patient comprising administering to the patient therapeutically effective amounts of:
| 06-13-2013 |
20130150364 | HETEROCYCLIC COMPOUND | 06-13-2013 |
20130165440 | JAK1 Inhibitors - JAK1 inhibitors of structural formula (I), wherein Ar | 06-27-2013 |
20130165441 | Novel Polymorphs and Salts - The present invention is directed to novel polymorphs and salts of a compound which is an inhibitor of kinase activity. | 06-27-2013 |
20130172342 | BENZIMIDAZOLE DERIVATIVES AS SELECTIVE BLOCKERS OF PERSISTENT SODIUM CURRENT - The present invention is directed to methods of treating diseases or conditions mediated by elevated persistent sodium channel, such as ocular disorders, pain, multiple sclerosis, and seizure disorders utilizing a compound of Formula I | 07-04-2013 |
20130172343 | Derivatives of 1H-isoindol-3-amine, 1H-iso-aza-indol-3amine, 3,4-dihydroisoquinolin-1-amine, and 1,4-dihydroisoquinolin-3-amine as Beta-secretase Inhibitors - The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I: (I). In another embodiment, the compounds have a general Formula II: (II). In another embodiment, the compounds have a general Formula III: (III). Variables A | 07-04-2013 |
20130178472 | ARYLSULFONAMIDE PYRIDINE-PYRIDINONE DERIVATIVES, PREPARATION OF SAME, AND THERAPEUTIC USE THEREOF - The invention relates to pyridine-pyridinone derivatives general formula (I): | 07-11-2013 |
20130178473 | 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. | 07-11-2013 |
20130190309 | PHTHALAZINONE AND RELATED ANALOGS AS SIRTUIN MODULATORS - Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent. | 07-25-2013 |
20130190310 | MIG6 AND THERAPEUTIC EFFICACY - We identify markers capable of guiding the decision to incorporate epidermal growth factor receptor (EGFR) inhibitors, in particular EGFR tyrosine kinase inhibitors (TKIs), into chemotherapeutic regimens. Mitogen-inducible gene 6 (Mig6), a negative regulator of EGFR, is selectively upregulated during the development of resistance to the EGFR tyrosine kinase inhibitor (TKI) erlotinib, resulting in decreased EGFR phosphorylation. The ratio of Mig6/EGFR expression highly correlates with erlotinib sensitivity. A low Mig6/EGFR ratio correlates with a high response rate to gefitinib and a marked increase in progression-free survival for patients. The ratio of Mig6 to EGFR is a major predictor of biologic and clinical responses to EGFR inhibitors. | 07-25-2013 |
20130196990 | Benzimidazole Derivatives As PI3 Kinase Inhibitors - This invention relates to the use of benzimidazole derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3′ OH kinase family (hereinafter PI3 kinases), suitably, PI3Kα, PI3Kδ, PI3Kβ, and/or PI3Kγ. Suitably, the present invention relates to the use of benzimidazoles in the treatment of one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries. More suitably, the present invention relates to PI3Kβ selective benzimidazoles compounds for treating cancer. | 08-01-2013 |
20130210821 | Methods for Treating Obesity - The disclosure provides for methods of treating obesity and related disorders. Pharmaceutical compositions and methods of using, e.g. in the treatment of obesity are provided. | 08-15-2013 |
20130217684 | NOVEL BIARYL BENZOIMIDAZOLE DERIVATIVES AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME - Disclosed are biaryl benzoimidazole derivatives. They have an inhibitory effect on calcium influx in HEK cells, thereby showing a powerful antagonistic effect on a vanilloid receptor, and further have an analgesic effect, thereby being useful for preventing or treating pain, acute pain, chronic pain, neuropathic pain, postoperative pain, migraine, arthralgia, neuropathies, nerve injury, diabetic neuropathy, neurological illness, neurodermatitis, stroke, bladder hypersensitivity, irritable bowel syndrome, a respiratory disorder such as cough, asthma, and chronic obstructive pulmonary disease, burning, psoriasis, itching, vomiting, irritation of the skin, eyes, and mucous membranes, gastric-duodenal ulcers, inflammatory intestinal diseases, and inflammatory diseases. | 08-22-2013 |
20130225578 | 7-CYCLYLQUINAZOLINE DERIVATIVES AND METHODS OF USE THEREOF - Provided herein are 7-cyclylquinazoline compounds for treatment of JAK kinase mediated diseases, including JAK2 kinase-, JAK3 kinase- or TYK2 kinase-mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions. | 08-29-2013 |
20130237537 | METHOD OF TREATING CONDITIIONS WITH KINASE INHIBITORS - The present invention relates to a method of treating ophthalmic diseases and conditions, e.g. diabetic retinopathy, age-related macular degeneration, retinopathy of prematurity, etc., in a subject comprising administering to said subject a therapeutically effective amount of at least one compound of formula I | 09-12-2013 |
20130237538 | KINASE INHIBITORS - The present invention relates to compounds of formulae I and II | 09-12-2013 |
20130245014 | JAK KINASE MODULATING COMPOUNDS AND METHODS OF USE THEREOF - Provided herein are quinazoline compounds for treatment of JAK kinase mediated diseases, including JAK2 kinase-, JAK3 kinase- or TYK2 kinase-mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions. | 09-19-2013 |
20130245015 | INDAZOLE, BENZISOXAZOLE, AND BENZISOTHIAZOLE KINASE INHIBITORS - Compounds having the formula | 09-19-2013 |
20130252954 | CRYSTAL OF AMIDE COMPOUND - Provision of crystal of 1-(4-methoxybutyl)-N-(2-methylpropyl)-N-[(3S,5R)-5-(morpholin-4-ylcarbonyl)piperidin-3-yl]-1H-benzimidazole-2-carboxamide hydrochloride which has a superior rennin inhibitory activity and is useful as a prophylactic or therapeutic agent for hypertension and various organ disorders caused by hypertension, and the like. Crystal of 1-(4-methoxybutyl)-N-(2-methylpropyl)-N-[3S,5R)-5-(morpholin-4-ylcarbonyl)piperidin-3-yl]-1H-benzimidazole-2-carboxamide hydrochloride having an X-ray powder diffraction pattern showing characteristic peaks at interplanar spacings (d) of around 26.43±0.2, 7.62±0.2 and 4.32±0.2 angstroms. | 09-26-2013 |
20130261117 | COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR - Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases. | 10-03-2013 |
20130267514 | APOPTOSIS-INDUCING AGENTS FOR THE TREATMENT OF CANCER AND IMMUNE AND AUTOIMMUNE DISEASES - Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein. | 10-10-2013 |
20130267515 | COMBINATION COMPRISING AN ATP ANALOG AND AN ADENOSINE RECEPTOR ANTAGONIST OR A NUCLEOBASE/NUCLEOSIDE ANALOG FOR THE TREATMENT OF CANCER - A method for treating an ATP analog-induced side effect in a subject comprises administering an effective amount of an adenosine receptor antagonist to the subject. A method for treating cancer in a subject comprises administering a nucleobase and/or nucleoside prior to administering an ATP analog. | 10-10-2013 |
20130274259 | KINASE MODULATION AND INDICATIONS THEREFOR - Compounds, compositions and methods useful for treatment of Flt3-mediated diseases or conditions are provided herewith. Also provided herewith are methods for modulating the receptor protein tyrosine like kinase 3(Flt3). | 10-17-2013 |
20130281448 | SMALL MOLECULE COMPOUNDS FOR TARGETING INFLAMMATORY CONDITIONS - Provided herein are small molecule compounds for the treatment of inflammatory conditions, and pharmaceutical compositions and methods relating thereto. For example, provided herein are compositions comprising small molecule compounds for the treatment of conditions such as multiple sclerosis, type 2 diabetes, psoriasis, rheumatoid arthritis, Hashimoto's thyroiditis, and Crohn's disease. In some embodiments, the pharmaceutical composition and methods described herein pertain to small molecule compounds previously known for the treatment of another condition, such as non-small-cell lung cancer (NSCLC). | 10-24-2013 |
20130281449 | Oxazine Derivatives and their Use in the Treatment of Neurological Disorders - The invention relates to novel heterocyclic compounds of the formula (I), in which all of the variables are as defined in the specification, in free form or in pharmaceutically acceptable salt form, to their preparation, to their medical use and to medicaments comprising them. | 10-24-2013 |
20130289032 | ESTERS OF BENDAMUSTINE AND RELATED COMPOUNDS, AND MEDICAL USE THEREOF - The present invention relates to particular esters of bendamustine and related compounds, and medical uses thereof. | 10-31-2013 |
20130296319 | N1-PYRAZOLOSPIROKETONE ACETYL-CoA CARBOXYLASE INHIBITORS - The invention provides a compound of Formula (I) | 11-07-2013 |
20130303534 | COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR - Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases. | 11-14-2013 |
20130303535 | NOVEL BICYCLIC HETEROCYCLIC COMPOUND - The invention provides a compound for the treatment or prophylaxis of pathology involving SNS, specifically diseases such as neuropathic pain, nociceptive pain, dysuria, multiple sclerosis and the like. The compound is represented by formula (1) or a pharmaceutically acceptable salt thereof wherein R | 11-14-2013 |
20130303536 | Combination of 10-Propargyl-10-Deazaaminopterin and Erlotinib for the Treatment of Non-Small Cell Lung Cancer - The present invention relates to compositions comprising a combination of 10-propargyl-10-deazaaminopterin and an EGFR Kinase inhibitor, including erlotinib, for treatment of non-small cell lung cancer, and methods of treatment for non-small cell lung cancer in a patient in need thereof comprising administering for combination of 10-propargyl-10-deazaaminopterin and an EGFR Kinase inhibitor, including erlotinib, for treatment of non-small cell lung cancer. | 11-14-2013 |
20130310376 | 2-ARYL-4-QUINAZOLINONES AND THEIR PHARMACEUTICAL COMPOSITIONS - Provided is a compound of the formula I or a pharmaceutically acceptable salt, solvate or stereoisomer thereof: | 11-21-2013 |
20130317024 | PYRROLOPYRROLIDINONE COMPOUNDS - The invention relates to compounds of formula (I): | 11-28-2013 |
20130317025 | PDE-10 INHIBITORS - Vicinal substituted cyclopropyl compounds which are inhibitors of phosphodiesterase 10 are described as are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function, for example neurological, neurodegenerative and psychiatric disorders including, but not limited to, those comprising cognitive deficits or schizophrenic symptoms. | 11-28-2013 |
20130317026 | SUBSTITUTED 6,5-FUSED BICYCLIC HETEROARYL COMPOUNDS - The present invention relates to substituted 6,5-fused bicyclic heteroaryl compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. | 11-28-2013 |
20130324529 | BENZIMIDAZOLE CANNABINOID AGONISTS BEARING A SUBSTITUTED HETEROCYCLIC GROUP - The present invention is related to novel benzimidazole compounds of formula (I) having cannabinoid receptor agonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals, in particular humans. | 12-05-2013 |
20130345218 | INHIBITORS OF INFLUENZA VIRUSES REPLICATION - Methods of inhibiting the replication of influenza viruses in a biological sample or patient, of reducing the amount of influenza viruses in a biological sample or patient, and of treating influenza in a patient, comprises administering to said biological sample or patient an effective amount of a compound represented by Structural Formula (I): | 12-26-2013 |
20140005193 | BENZOIMIDAZOLES AS PROLYL HYDROXYLASE INHIBITORS | 01-02-2014 |
20140005194 | BENZIMIDAZOLE DERIVATIVES: PREPARATION AND PHARMACEUTICAL APPLICATIONS | 01-02-2014 |
20140018363 | 2-ARYL-4-QUINAZOLINONES AND THEIR PHARMACEUTICAL COMPOSITIONS - Provided is a compound of the formula I or a pharmaceutically acceptable salt, solvate or stereoisomer thereof: | 01-16-2014 |
20140018364 | CHEMICAL COMPOUNDS - There is provided pyrimidinyl compounds of Formula (I), | 01-16-2014 |
20140024646 | OCTAHYDRO-CYCLOPENTAPYRROLYL ANTAGONISTS OF CCR2 - The present invention comprises compounds of Formula (I). | 01-23-2014 |
20140031352 | SOLID FORMS OF TYROSINE KINASE INHIBITORS, PROCESS FOR THE PREPARATION AND THEIR PHARMACEUTICAL COMPOSITION THEREOF - The present invention generally relates to solid forms of tyrosine kinase inhibitors, in particular combinations of tyrosine kinase inhibitors with anti-oxidative acids, processes for its preparation and a pharmaceutical compositions containing the same. | 01-30-2014 |
20140038958 | CDK8-CDK19 SELECTIVE INHIBITORS AND THEIR USE IN ANTI-METASTATIC AND CHEMOPREVENTATIVE METHODS FOR CANCER - The invention relates to the compounds and methods for inhibiting the Cyclin-Dependent Kinase Inhibitor (CDKI) pathway. More particularly, the invention relates to compounds and methods for inhibiting the CDKI pathway for studies of and intervention in senescence-related and other CDKI-related diseases. The invention provides new compounds having improved solubility and/or potency, and methods for their use. In various aspects, the invention relates to the treatment of cancer. The invention provides methods for chemoprevention and prevention of tumor recurrence or metastasis. The invention further provides diagnostic techniques for treatment for certain cancer types. The invention utilizes specific inhibitors of CDK8/19 and/or measurement of CDK8 levels in a patient. | 02-06-2014 |
20140038959 | METHODS OF TREATING TUMORS - The present invention relates to a method of treating tumors wherein PAK1 is over-expressed or amplified by co-administering a PAK1 inhibitor and a second anti-hyper-proliferative agent | 02-06-2014 |
20140038960 | Hetaryl-[1,8]naphthyridine derivatives - Novel hetaryl-[1,8]naphthyridine derivatives of formula (I) | 02-06-2014 |
20140045838 | KINASE INHIBITORS AND METHOD OF TREATING CANCER - The invention is directed to a compound represented by the following structural formula and pharmaceutically acceptable salts thereof: | 02-13-2014 |
20140045839 | NOVEL ANXIOLYTIC COMPOUNDS - The present invention relates to chemical compounds of general formula (I) | 02-13-2014 |
20140045840 | 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. | 02-13-2014 |
20140045841 | METHOD FOR INHIBITING THE GROWTH OF CANCER STEM CELL - The present invention provides a method for inhibiting the growth of cancer stem cells, particularly colorectal cancer stem cells, liver cancer stem cells, lung cancer stem cells or breast cancer stem cells, comprising administering to a subject in need thereof a therapeutically effective amount of a compound of antimycin A or a pharmaceutically acceptable salt thereof, together with a pharmaceutically acceptable carrier. | 02-13-2014 |
20140051700 | Small-molecule agonists for type-2 orexin receptor - Methods and compositions for agonizing a type-2 orexin receptor (OX2R) in a cell determined to be in need thereof, including the general method of (a) administering to a subject a cyclic guanidinyl OX2R agonist and (b) detecting a resultant enhanced wakefulness or increased resistance to diet-induced accumulation of body fat, or abbreviated recovery from general anesthesia or jet lag. | 02-20-2014 |
20140051701 | METHODS OF TREATING A DISEASE OR CONDITION OF THE CENTRAL NERVOUS SYSTEM - The present invention provides methods of treating central nervous system disorders, such as mood disorders (e.g., depression) and neurodegenerative diseases using compounds of formula (I). The subject disclosure enables the manufacture of medicaments as well as compositions containing same for use in methods of therapy and prophylaxis of central nervous system disorders. | 02-20-2014 |
20140073642 | QUINAZOLINE DERIVATIVES FOR THE TREATMENT OF VIRAL INFECTIONS AND FURTHER DISEASES - This invention relates to quinazoline derivatives, processes for their preparation, pharmaceutical compositions, and their use in therapy of disorders in which the modulation of toll-like-receptors is involved. | 03-13-2014 |
20140080828 | IMIDAZOLYL AMIDE COMPOUNDS AND USES RELATED THERETO - This disclosure relates to antiviral compounds disclosed herein and uses related thereto. In certain embodiments, the disclosure relates to pharmaceutical compositions comprising 2-((benzo[d]imidazol-2-yl)thio)-N-phenylpropanamide derivatives, N-phenyl-2-((1-phenyl-benzo[d]imidazol-2-yl)thio)propanamide derivatives, or 2-((benzo[d]imidazol-2-yl)thio)-N-(2-chloro-4-methylphenyl)propanamide derivatives. The derivatives may be substituted with one or more substituents. Typically, the pharmaceutical composition comprises a compound of Formula (I), or salt, prodrug, or ester thereof wherein X, Y, and R1 to R7 are described herein. | 03-20-2014 |
20140080829 | PYRIMIDYL CYCLOPENTANES AS AKT PROTEIN KINASE INHIBITORS - The present invention provides compounds of Formula I, including tautomers, resolved enantiomers, diastereomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof. | 03-20-2014 |
20140080830 | Novel Compounds - The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): | 03-20-2014 |
20140088100 | INHIBITORS OF THE FIBROBLAST GROWTH FACTOR RECEPTOR - Described herein are inhibitors of FGFR, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions to inhibit the activity of tyrosine kinases. | 03-27-2014 |
20140088101 | NAPHTHYRIDINE DERIVATIVES AS INHIBITORS OF HYPOXIA INDUCIBLE FACTOR (HIF) HYDROXYLASE - The present disclosure relates to novel compounds, methods, and compositions capable of inhibiting HIF hydroxylase enzyme activity, thereby increasing the stability and/or activity of hypoxia inducible factor (HIF). | 03-27-2014 |
20140088102 | (ALPHA-SUBSTITUTED CYCLOALKYLAMINO AND HETEROCYCLYLAMINO) PYRIMIDINYL AND 1,3,5-TRIAZINYL BENZIMIDAZOLES, PHARMACEUTICAL COMPOSITIONS THEREOF, AND THEIR USE IN TREATING PROLIFERATIVE DISEASES - Provided herein are (alpha-substituted cycloalkylamino or heterocyclylamino) pyrimidinyl and 1,3,5-triazinyl benzimidazoles, e.g., a compound of Formula I, and their pharmaceutical compositions, preparation, and use as agents or drugs for treating proliferative diseases. | 03-27-2014 |
20140088103 | (FUSED RING ARYLAMINO AND HETEROCYCLYLAMINO) PYRIMIDINYL AND 1,3,5-TRIAZINYL BENZIMIDAZOLES, PHARMACEUTICAL COMPOSITIONS THEREOF, AND THEIR USE IN TREATING PROLIFERATIVE DISEASES - Provided herein are (fused ring arylamino and heterocyclylamino) pyrimidinyl and 1,3,5-triazinyl benzimidazoles, e.g., a compound of Formula (I), and their pharmaceutical compositions, preparation, and use as agents or drugs for treating proliferative diseases. | 03-27-2014 |
20140107119 | BCL-2-SELECTIVE APOPTOSIS-INDUCING AGENTS FOR THE TREATMENT OF CANCER AND IMMUNE DISEASES - Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 or Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which are expressed anti-apoptotic Bcl-2 protein. | 04-17-2014 |
20140107120 | DUAL-ACTING BENZOIMIDAZOLE ANTIHYPERTENSIVE AGENTS - The invention is directed to compounds having the formula: | 04-17-2014 |
20140121206 | TRPV4 ANTAGONISTS - The present invention relates to spirocarbamate compounds of Formula (I) in which R1, (R2)Y, R3, R4, X and A have the meanings given in the specification. The invention further provides pharmaceutical compositions containing the compounds or pharmaceutically acceptable salts thereof and relates to their use of these compounds as TRPV4 antagonists in treating or preventing conditions associated with TRPV4 imbalance. | 05-01-2014 |
20140128391 | SELECTIVE HDAC1 AND HDAC2 INHIBITORS - Provided herein are compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with HDAC activity, particularly diseases or disorders that involve activity of HDAC1 and/or HDAC2. Such diseases include cancer, sickle-cell anemia, beta-thalassemia, and HIV. | 05-08-2014 |
20140142101 | CORRELATION OF MOLECULAR MARKERS WITH CLINICAL OUTCOME IN GBM PATIENTS RADIATION TREATED WITH OR WITHOUT GEFITINIB - Interestingly, for prognosis, the significant biomarkers for Gefitinib-treated GBM patients (RTOG 0211) appeared to differ compared to historical, RT and non-Gefitinib-treated GBM patients. In Gefitinib-treated patients, those with higher levels of nuclear pAKT driven by PTEN loss, higher levels of nuclear pMAPK, and lower levels of nuclear pmTOR had significantly worse clinical outcomes. In contrast, in non-Gefitinib-treated patients, patients with PTEN-deficiency, and higher levels of EGFRvIII, total EGFR, IGFR1, NFkB and lower levels of nuclear Survivin appeared to have adverse clinical outcomes, highlighting the treatment-dependency of these biomarkers. | 05-22-2014 |
20140142102 | CYCLIC AMINES AS BROMODOMAIN INHIBITORS - The present disclosure relates to compounds, which are useful for inhibition of BET protein function by binding to bromodomains, and their use in therapy. | 05-22-2014 |
20140155396 | C-Met Modulators and Method of Use - The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds. | 06-05-2014 |
20140155397 | EMT SIGNATURES AND PREDICTIVE MARKERS AND METHOD OF USING THE SAME - EMT signatures and markers useful for characterizing the status of epithelial cancers and for predicting drug responses in patients having non-small cell lung cancer are provided together with methods of using the same. | 06-05-2014 |
20140155398 | HETEROCYCLIC COMPOUNDS AS PROTEIN KINASE INHIBITORS - The present invention provides a heterocyclic compound of formula (I), a pharmaceutically acceptable salt thereof, a prodrug thereof or a hydrate thereof, wherein A, A′ B, D, R | 06-05-2014 |
20140155399 | BRAF Mutations Conferring Resistance to BRAF Inhibitors - The present invention relates to methods, compositions and kits concerning resistance to treatment with an anti-cancer agent, specifically an inhibitor of BRAF. In particular embodiments, the invention concerns mutations in a BRAF sequence that confer resistance to a BRAF inhibitor. Identification of such mutations in a BRAF sequence allows the identification and design of second-generation BRAF inhibitors. Methods and kits for detecting the presence of a mutant BRAF sequence in a sample are also provided. | 06-05-2014 |
20140163028 | INHIBITION OF ACTIVATED CDC42-ASSOCIATED KINASE 1 - Compounds, compositions, and methods for specific inhibition of activated cdc42-associated kinase 1 (Ack1) are provided. | 06-12-2014 |
20140171429 | BICYCLIC INHIBITORS OF ALK - The present invention relates to compounds of formula (1) or pharmaceutical acceptable salts, Formula (1) wherein R | 06-19-2014 |
20140171430 | DISUBSTITUTED OCTAHYDROPYRROLO [3,4-C] PYRROLES AS OREXIN RECEPTOR MODULATORS - Disubstituted octahydropyrrolo[3,4-c]pyrrole compounds are described, which are useful as orexin receptor modulators. Such compounds may be useful in pharmaceutical compositions and methods for the treatment of diseased states, disorders, and conditions mediated by orexin activity, such as insomnia. | 06-19-2014 |
20140171431 | AZOLE HETEROCYCLIC COMPOUND, PREPARATION METHOD, PHARMACEUTICAL COMPOSITION AND USE - The present invention relates to the field of pharmaceutical chemistry, and in particular, to a novel class of azole compounds represented by general formula (I), (II) or (III) and a preparation method thereof, a pharmaceutical composition with the compounds as active components, and a use of the azole compounds and the pharmaceutical composition in the preparation of a medicament for treatment of diseases associated with Lp-PLA | 06-19-2014 |
20140171432 | HISTONE DEMETHYLASE INHIBITORS - The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted 3-aminopyridine derivative compounds, substituted 3-aminopyridazine derivative compounds, and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like. | 06-19-2014 |
20140179697 | DISUBSTITUTED OCTAHYDROPYRROLO[3,4-c]PYRROLES AS OREXIN RECEPTOR MODULATORS - Disubstituted octahydropyrrolo[3,4-c]pyrrole compounds are described, which are useful as orexin receptor modulators. Such compounds may be useful in pharmaceutical compositions and methods for the treatment of diseased states, disorders, and conditions mediated by orexin activity, such as insomnia. | 06-26-2014 |
20140187550 | BICYCLIC ORGANIC COMPOUNDS SUITABLE FOR THE TREATMENT OF INFLAMMATORY OR ALLERGIC CONDITIONS - A compound of formula (I): | 07-03-2014 |
20140187551 | 7-AZAINDOLE DERIVATIVES SUITABLE FOR TREATMENT OF CANCERS - Compounds of the formula (I) in which R | 07-03-2014 |
20140194421 | HETEROCYCLIC GLUTAMINASE INHIBITORS - The invention relates to novel heterocyclic compounds and pharmaceutical preparations thereof. The invention further relates to methods of treatment using the novel heterocyclic compounds of the invention. | 07-10-2014 |
20140206686 | PHTHALAZINONES AND ISOQUINOLINONES AS ROCK INHIBITORS - The present invention provides compounds of Formula (I): | 07-24-2014 |
20140206687 | QUINAZOLINE DERIVATIVE, PREPARATION METHOD THEREFOR, INTERMEDIATE, COMPOSITION AND APPLICATION THEREOF - Disclosed are as represented by Formula (I) a quinazoline derivative and a pharmaceutical acceptable salt thereof, or, an enantiomer, a non-enantiomer, a tautomer, a racemate, a solvate, a metabolic precursor, or a prodrug of both. Also disclosed are a preparation method therefor, an intermediate, a pharmaceutical composition having the quinazoline derivative, and an application thereof. The quinazoline derivative of the present invention is provided with improved anti-tumor activity. | 07-24-2014 |
20140206688 | AMINO QUINAZOLINES AS KINASE INHIBITORS - Disclosed are compounds having the formula (Formula I)): wherein R | 07-24-2014 |
20140213585 | PYRIMIDINE-2-AMINE COMPOUNDS AND THEIR USE AS INHIBITORS OF JAK KINASES - This invention is directed to methods of treating diseases or conditions associated with JAK2 activity in a mammal comprising the administration of a compound of formula (I): | 07-31-2014 |
20140221368 | BIOMARKERS OF THERAPEUTIC RESPONSIVENESS - The present invention relates to methods of diagnosing breast cancer in a patient, as well as methods of monitoring the progression of breast cancer and/or methods of monitoring a treatment protocol of a therapeutic agent or a therapeutic regimen. The invention also relates to assay methods used in connection with the diagnostic methods described herein. | 08-07-2014 |
20140221369 | 5-DEUTERO-2,4-THIAZOLIDINEDIONE AND 5-DEUTERO-2,4-OXAZOLIDINEDIONE DERIVATIVES AND COMPOSITIONS COMPRISING AND METHODS OF USING THE SAME - The invention provides 5-deuterium enriched 2,4-thiazolidinediones and 2,4-oxazolidinediones, such as 5-(4-((6-(4-amino-3,5-dimethylphenoxy)-1-methyl-1H-benzo[d]imidazol-2-yl)methoxy)benzyl)-5-deutero-thiazolidine-2,4-dione, deuterated derivatives thereof, stereoisomers thereof, pharmaceutically acceptable salt forms thereof, and methods of treating medical disorders, such as cancer, using the same. | 08-07-2014 |
20140221370 | PYRROLOPYRIDINES AS KINASE INHIBITORS - Compounds of Formula (I) are useful for inhibition of CHK1 and/or CHK2. Methods of using compounds of Formula (I) and stereoisomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed. | 08-07-2014 |
20140235633 | 4-Aminoquinazoline Derivatives and Uses Thereof - The present invention provides a 4-aminoquinazoline derivative having the chemical structure of the following formula, and the use thereof. It is demonstrated by the pharmacological experiment that, the compound or a salt thereof according to the present invention not only has distinct inhibitory effect on histone deacetylases, but also has stronger differentiation induction and anti-proliferative activities for certain tumor cells. It can be used in the treatment of cancers and diseases related to cell differentiation and proliferation. Excellent efficacy is observed especially for leukemia and a solid tumor. As demonstrated by the animal test, the compound or a salt thereof according to the present invention is less toxic. | 08-21-2014 |
20140235634 | THERAPEUTIC COMPOUNDS AND USES THEREOF - Described herein are compounds of Formula (I) or Formula (VI), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Also provided are particles (e.g., nanoparticles) comprising compounds of Formula (I) or Formula (VI) and pharmaceutical compositions thereof that are mucus penetrating. Methods of using the compounds or pharmaceutical compositions thereof for treating diseases are also provided. | 08-21-2014 |
20140243331 | INHIBITORS OF INV(16) LEUKEMIA - This invention describes the development of targeted small molecule inhibitors of the inv(16) fusion, the causative agent in ˜12% of acute myeloid leukemia (AML). The inv(16) fusion results in expression of the CBFβ-SMMHC fusion protein in the blood cells of afflicted patients. The present invention provides compounds which inhibit the function of both CBFβ and the CBFβ-SMMHC fusion. These compounds block the growth of an inv(16) leukemia cell line as well as increase its apoptosis, while showing minimal effects against non inv(16) cell lines. As a mechanism to develop inhibitors with selectivity for the CBFβ-SMMHC fusion protein, the present invention further provides dimeric derivatives of these compounds which show both increased potency as well as selectivity for CBFβ-SMMHC. These compounds show potent inhibition of an inv(16) leukemia cell line with minimal effects on non inv(16) cell lines. Analysis of the pharmacokinetics of the developed compounds has made it possible to improve the lifetime of the compound in the plasma of mice to a level commensurate with long-term treatment. | 08-28-2014 |
20140249148 | SELECTIVE HDAC3 INHIBITORS - Provided herein are inhibitors of HDAC3, as well as methods of treatment comprising administering those compounds to a subject in need thereof. | 09-04-2014 |
20140256721 | Novel Polymorphs and Salts - The present invention is directed to novel polymorphs and salts of a compound which is an inhibitor of kinase activity. | 09-11-2014 |
20140256722 | BENZOIMIDAZOLES AS PROLYL HYDROXYLASE INHIBITORS - The present invention is directed to benzoimidazole compounds of the formula: | 09-11-2014 |
20140256723 | MINERALOCORTICOID RECEPTOR ANTAGONISTS - The present invention is directed to compounds of the Formula (I) as well as pharmaceutically acceptable salts thereof that are aldosterone receptor antagonists which might be useful for treating aldosterone-mediated diseases. The invention furthermore relates to processes for preparing compounds of the Formula (I), to their possible use for the treatment of the above-mentioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical compositions which comprise compounds of the Formula (I). | 09-11-2014 |
20140275073 | METHODS OF TREATING CANCER SENSITIVE TO ANTI-EGFR THERAPY AND MODIFYING TREATMENT USING BLOOD BIOMARKERS - The present disclosure provides methods of treating cancer and modifying a cancer treatment for a cancer with an anti-EGFR drug by creating PRDX6 expression profiles and using the profiles to evaluate and optionally modify treatment. The present disclosure also provides assays and systems for assessing sensitivity of a cancer to an anti-EGFR therapy. | 09-18-2014 |
20140275074 | HETEROCYCLIC DERIVATIVE HAVING PGD2 RECEPTOR ANTAGONIST ACTIVITY - The present invention is related to a compound represented by formula (I), | 09-18-2014 |
20140296235 | 1H-BENZIMIDAZOLE-4-CARBOXAMIDES SUBSTITUTED WITH PHENYL AT THE 2-POSITION ARE POTENT PARP INHIBITORS - Compounds having formula (I) | 10-02-2014 |
20140303163 | USE OF KINASE INHIBITORS IN PREVENTING AND TREATING INFLAMMATORY DISORDER - The present invention discloses use of compounds of formula (I) in preventing and treating inflammatory disorder. | 10-09-2014 |
20140303164 | THERAPEUTIC COMPOUNDS - Compounds of formula I: | 10-09-2014 |
20140309224 | TREATMENT OF DISEASES OR DISORDERS CAUSED BY INDUCED NFkB TRANSCRIPTIONAL ACTIVITY - The invention provides a method for treating a disease or disorder in a mammal which is caused by induced NFkB transcriptional activity in cells of the mammal, the method comprising administering to the mammal a compound that specifically inhibits one or more of CDK8 and CDK19. | 10-16-2014 |
20140315901 | Arylpyrrolopyridine derived compounds as LRRK2 inhibitors - The present invention is directed to arylpyrrolopyridine derivatives of formula (A) | 10-23-2014 |
20140315902 | BICYCLIC HETEROCYCLES AS FGFR INHIBITORS - The present invention relates to bicyclic heterocycles, and pharmaceutical compositions of the same, that are inhibitors of one or more FGFR enzymes and are useful in the treatment of FGFR-associated diseases such as cancer. | 10-23-2014 |
20140323481 | 3-CYANOARYL-1H-PYRROLO[2,3-B]PYRIDINE DERIVATIVES - Compounds of the formula (I) in which R | 10-30-2014 |
20140336190 | BENZIMIDAZOLE DERIVATIVES AS BROMODOMAIN INHIBITORS - This application relates to chemical compounds which may act as inhibitors of; or which may otherwise modulate the activity of, a bromodomain-containing protein, including bromodomain-containing protein 4 (BRD4), and to compositions and formulations containing such compounds, and methods of using and making such compounds. Compounds include compounds of Formula (I) | 11-13-2014 |
20140350013 | INDAZOLES - Herein are disclosed indazoles of formula (I) | 11-27-2014 |
20140364431 | Quinoline and cinnoline derivatives and their applications - The present invention relates to a series of quinoline and cinnoline derivatives of general formula I, pharmaceutically acceptable salts, hydrates, solvates or prodrugs thereof. And the compounds of general formula I show potent inhibitory activity gainst c-Met kinase. The present invention further relates to the uses of the compounds, pharmaceutically acceptable salts and hydrates for the preparation of medicaments for the treatment and/or prevention of diseases caused by abnormal expression of c-Met kinase, especially for treatment and/or prevention of cancer. | 12-11-2014 |
20140378453 | 2-(2-HYDROXYBIPHENYL-3-YL)-1H-BENZOIMIDAZOLE-5-CARBOXAMIDINE DERIVATIVES AS FACTOR VIIA INHIBITORS - The present invention relates to novel inhibitors of Factors VIIa, IXa, Xa, XIa, in particular Factor VIIa, pharmaceutical compositions comprising these inhibitors, and methods for using these inhibitors for treating or preventing thromboembolic disorders, cancer or rheumatoid arthritis. Processes for preparing these inhibitors are also disclosed. | 12-25-2014 |
20140378454 | NOVEL METHODS - The present invention relates to the field of methods for providing components of pharmaceutical compositions comprising poorly water-soluble drugs. In particular the present invention relates to methods for providing stable, amorphous hybrid nanoparticles, comprising at least one protein kinase inhibitor and at least one polymeric stabilizing and matrix-forming component, useful in pharmaceutical compositions. | 12-25-2014 |
20140378455 | NEW USE OF 1H-INDAZOLE-3-CARBOXAMIDE COMPOUNDS AS GLYCOGEN SYNTHASE KINASE 3 BETA INHIBITORS - 1H-indazole-3-carboxamide compounds as glycogen synthase kinase 3 beta inhibitors. The present invention relates to the 1H-indazole-3-carboxamide compounds for use as glycogen synthase kinase 3 beta (GSK-33) inhibitors and to their use in the treatment of GSK-3p-related disorders such as, for example, (i) insulin-resistance disorders; (ii) neurodegenerative diseases; (iii) mood disorders; (iv) schizophrenic disorders; (v) cancerous disorders; (vi) inflammation, (vii) substance abuse disorders; and (viii) epilepsies. | 12-25-2014 |
20140378456 | Benzimidazole Derivatives As PI3 Kinase Inhibitors - This invention relates to the use of benzimidazole derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3′ OH kinase family (hereinafter PI3 kinases), suitably, PI3Kα, PI3Kδ, PI3Kβ, and/or PI3Kγ. Suitably, the present invention relates to the use of benzimidazoles in the treatment of one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries. More suitably, the present invention relates to PI3Kβ selective benzimidazoles compounds for treating cancer. | 12-25-2014 |
20150011548 | PROTEIN KINASE INHIBITORS - A compound of formula (I), wherein R | 01-08-2015 |
20150011549 | TABLET - Provided is a tablet showing improved hygroscopicity, which contains, as a pharmaceutically active ingredient, a compound showing deliquescence at a relative humidity of not less than 80% at 25 degrees C. A tablet containing a compound showing deliquescence at a relative humidity of not less than 80% at 25 degrees C. and an additive showing an equilibrium moisture absorption rate at relative humidity 75% at 25 degrees C. of not less than 7 wt % relative to its dry weight. | 01-08-2015 |
20150018351 | PYRIDINONYL PDK1 INHIBITORS - The present invention provides pyridinonyl PDK1 inhibitors and methods of treating cancer using the same. | 01-15-2015 |
20150025071 | TETRAHYDRO-QUINAZOLINONE DERIVATIVES AS TANK AND PARP INHIBITORS - Compounds of the formula I | 01-22-2015 |
20150025072 | QUINAZOLINONE COMPOUNDS - The present invention relates to quinazolinone compounds, processes for their preparation and their use as pharmaceutical agents for the treatment of Parkinson's disease (PD). The quinazolinone compounds are of general formula (I). | 01-22-2015 |
20150031695 | SMALL MOLECULE COMPOUNDS FOR TARGETING INFLAMMATORY CONDITIONS - Small molecule compounds for the treatment of inflammatory conditions, and pharmaceutical compositions and methods relating thereto. The compositions may be used for the treatment of conditions such as multiple sclerosis, type 2 diabetes, psoriasis, rheumatoid arthritis, Hashimoto's thyroiditis, and Crohn's disease. In some embodiments, the pharmaceutical composition and methods pertain to small molecule compounds previously known for the treatment of another condition, such as non-small-cell lung cancer (NSCLC). | 01-29-2015 |
20150038509 | Chemokine Receptor Binding Heterocyclic Compounds With Enhanced Efficacy - The invention relates to heterocyclic compounds consisting of a core nitrogen atom surrounded by three pendant groups, wherein two of the three pendant groups are preferably benzimidazolyl methyl and tetrahydroquinolyl, and the third pendant group contains N and optionally contains additional rings. The compounds bind to chemokine receptors, including CXCR4 and CCR5, and demonstrate protective effects against infection of target cells by a human immunodeficiency virus (HIV). | 02-05-2015 |
20150038510 | CINNOLINE DERIVATIVES - Disclosed are compounds of Formula 1, | 02-05-2015 |
20150057275 | METHODS AND MATERIALS FOR GENETIC ANALYSIS OF TUMORS - This invention relates generally to methods and materials for rapid detection of mutations for tumor genotyping. | 02-26-2015 |
20150080392 | QUINAZOLINE DERIVATIVE, COMPOSITION HAVING THE DERIVATIVE, AND USE OF THE DERIVATIVE IN PREPARING MEDICAMENT - A class of quinazoline derivatives or pharmaceutically acceptable salts or solvates thereof with novel structures is provided; meanwhile, a pharmaceutical composition comprising a pharmaceutically effective amount of said quinazoline derivatives or pharmaceutically acceptable salts or solvates thereof, and pharmaceutically acceptable excipients or additives is also provided. By modifying and transforming the quinazoline and screening of the transformed compounds on the activity of tyrosine kinase inhibition, most of the compounds have been found to possess inhibitory activity against one or several of EGFR, VEGFR-2, c-erbB-2, c-erbB-4, c-met, tie-2, PDGFR, c-src, lck, Zap70 and fyn kinases. The present invention has the advantages of reasonable design, broad source of and easy access to the raw materials, simple and easy operation of the preparation methods, mild reaction conditions, high yield of the products and being beneficial for industrial-scale production. | 03-19-2015 |
20150080393 | SPIROCYCLIC COMPOUNDS AS TRYPTOPHAN HYDROXYLASE INHIBITORS - The present invention is directed to spirocyclic compounds which are inhibitors of tryptophan hydroxylase (TPH), particularly isoform 1 (TPH1), that are useful in the treatment of diseases or disorders associated with peripheral serotonin including, for example, gastrointestinal, cardiovascular, pulmonary, inflammatory, metabolic, and low bone mass diseases, as well as serotonin syndrome, and cancer. | 03-19-2015 |
20150094306 | PYRROLOPYRIDINONE DERIVATIVES AS TTX-S BLOCKERS - The present invention relates to pyrrolopyridinone derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved. | 04-02-2015 |
20150119394 | Insulin-Like Growth Factor-1 Receptor Inhibitors - The present invention relates to compounds that are capable of inhibiting, modulating and/or regulating Insulin-Like-Growth Factor I Receptor and Insulin Receptor. The compounds of the instant invention possess a core structure that comprises a sulfonyl indole moiety. The present invention is also related to the pharmaceutically acceptable salts, hydrates and stereoisomers of these compounds. | 04-30-2015 |
20150141421 | 6,7-DIALKOXY QUINAZOLINE DERIVATIVES AND METHODS OF TREATING DRUG RESISTANT AND OTHER TUMORS - Compounds of formula (I) | 05-21-2015 |
20150290205 | COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR - Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases. | 10-15-2015 |
20150291584 | GPR40 RECEPTOR AGONIST, METHODS OF PREPARING THE SAME, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME AS AN ACTIVE AGENT - The present invention relates to a novel compound having GPR40 receptor agonist activity that promotes insulin secretion and inhibits blood sugar rise after glucose loading, and is thereby useful for the treatment of diabetes and complications thereof, the preparation method thereof and pharmaceutical composition containing them as an active ingredient. | 10-15-2015 |
20150292012 | BIOMARKERS FOR NOD2 AND/OR RIP2 ACTIVITY RELATED APPLICATION - A method of predicting RIP2 inhibitor efficacy in treating a subject with an inflammatory disorder includes obtaining a bodily sample from the subject, determining in the bodily sample the expression level(s) of at least one gene selected from the group consisting of cd40, Clec4E, clec5a, CxCL10, gpr84, Icam1, Irgl, Marcks11, pde4b, Ptges, Rasgrp1, and slc2a6,comparing the expression levels of the at least one gene with the corresponding control value(s), and characterizing the subject as being responsive to RIP2 inhibitor treatment if the expression levels of the at least one gene is increased compared to the corresponding control value(s). | 10-15-2015 |
20150297604 | Combination Products with Tyrosine Kinase Inhibitors and their Use - The present invention relates to pharmaceutical products comprising a combination of (i) a MET inhibitor and (ii) an EGFR inhibitor, or a pharmaceutically acceptable salt thereof, respectively, or a prodrug thereof, which are jointly active in the treatment of proliferative diseases, corresponding pharmaceutical formulations, uses, methods, processes commercial packages and related invention embodiments. | 10-22-2015 |
20150299130 | SELECTIVE HDAC3 INHIBITORS - Provided herein are HDAC3 inhibitors, as well as methods of treatment comprising administering these compounds to a subject in need thereof. | 10-22-2015 |
20150299197 | APOPTOSIS-INDUCING AGENTS FOR THE TREATMENT OF CANCER AND IMMUNE AND AUTOIMMUNE DISEASES - Disclosed herein are compounds that inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases using the compounds. | 10-22-2015 |
20150306078 | ANTIFIBROTIC COMPOUNDS AND USES THEREOF - The present invention provides compounds having the general structural formula (I) | 10-29-2015 |
20150313907 | PYRROLE COMPOUNDS, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM - Compounds of formula (I): | 11-05-2015 |
20150328225 | 1,5-NAPHTHYRIDINE DERIVATIVES AND MELK INHIBITORS CONTAINING THE SAME - The present invention directs a compound represented by formula (I). | 11-19-2015 |
20150328226 | Novel Compounds - The invention provides a combination comprising compounds of formula (I) or salts thereof, and one or more therapeutic agents. | 11-19-2015 |
20150329498 | IRAK INHIBITORS AND USES THEREOF - The present invention provides quinazoline and quinoline compounds, compositions thereof, and methods of using the same. Also disclosed is the activity of such compounds as inhibitors of IRAK enzymes. | 11-19-2015 |
20150335651 | DISUBSTITUTED OCTAHYDROPYRROLO[3,4-c]PYRROLES AS OREXIN RECEPTOR MODULATORS - Disubstituted octahydropyrrolo[3,4-c]pyrrole compounds are described, which are useful as orexin receptor modulators. Such compounds may be useful in pharmaceutical compositions and methods for the treatment of diseased states, disorders, and conditions mediated by orexin activity, such as insomnia. | 11-26-2015 |
20150342957 | 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
| 12-03-2015 |
20150352121 | COMBINATION - A novel combination comprising the PI3K-β inhibitor 2-methyl-1-{[2-methyl-3-(trifluoromethyl)phenyl]methyl}-6-(4-morpholinyl)-1H-benzimidazole-4-carboxylic acid, 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 PI3K-β and/or B-Raf is beneficial, eg. cancer. | 12-10-2015 |
20150353540 | AZAINDOLE DERIVATIVES AS INHIBITORS OF PROTEIN KINASES - The present invention relates to compounds of the following formula (I) and/or the pharmaceutically acceptable addition salts, solvates, enantiomers, diastereoisomers thereof, as well as mixtures thereof. The subject matter of the present invention thus also includes the preparation of compounds of formula (I), their uses, in particular in the inhibition of protein kinases which are implicated for example in numerous diseases such as cancers or immune system disorders. | 12-10-2015 |
20150359796 | QUINAZOLINONE COMPOUNDS - The present invention relates to quinazolinone compounds, processes for their preparation and their use as pharmaceutical agents for the treatment of Parkinson's disease (PD). The quinazolinone compounds are of general formula I | 12-17-2015 |
20150368205 | POLY (ADP-RIBOSE) POLYMERASE INHIBITOR - Disclosed are a phthalic hydrazide (phthalazine ketone) compound, and a pharmaceutical composition comprising the same. As a DNA repair enzyme poly (ADP-ribozyme) polymerase inhibitor, the compound and the pharmaceutical composition can effectively treat diseases involving PARP enzymatic activity, including cancer, neural degenerative diseases, inflammation and the like. | 12-24-2015 |
20160002206 | INHIBITORS OF BRUTON'S TYROSINE KINASE - This application discloses compounds according to generic Formula I: (I) wherein all variables are defined as described herein, which inhibit BTK. The compounds disclosed herein are useful to modulate the activity of BTK and treat diseases associated with excessive BTK activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formula I and at least one carrier, diluent or excipient. | 01-07-2016 |
20160002212 | DUAL MEK/PI3K INHIBITORS AND THERAPEUTIC METHODS USING THE SAME - Dual inhibitors of MEK and PI3K and compositions containing the same are disclosed. Methods of using the dual MEK/PI3K inhibitors in the treatment of diseases and conditions wherein inhibition of MEK and PI3K provides a benefit, like cancers, also are disclosed. | 01-07-2016 |
20160002222 | PRODRUG FORMS OF KINASE INHIBITORS AND THEIR USE IN THERAPY - The invention provides novel prodrug compounds comprising a kinase inhibitor and a reductively-activated fragmenting aromatic nitroheterocycle or aromatic nitrocarbocycle trigger, where the compound carries a positive charge. In preferred embodiments, the compounds are of Formula I: | 01-07-2016 |
20160017431 | Methods for Predicting EGFR Tyrosine Kinase Inhibitor Efficacy - Provided herein are compositions and methods for predicting whether a subject with cancer will be responsive to treatment with an EGFR TKI and for the treatment of cancer in a subject. | 01-21-2016 |
20160017440 | Methods Of Classifying Biological Samples For Predicting Response To Tyrosine Kinase Inhibitor Treatment - Gene copy numbers of signaling components downstream of EGFR identify non-small cell lung cancer (NSCLC) patients with poor outcomes on 2nd/3rd line gefitinib therapy. | 01-21-2016 |
20160024080 | NEW COMPOUNDS - The compound of formula (I) are inhibitors of SSAO activity (Formula (I)) wherein the terms Y, Z, W, R | 01-28-2016 |
20160031855 | PROTEIN KINASE INHIBITORS - A compound of formula (I) | 02-04-2016 |
20160039789 | SUBSTITUTED HYDROXAMIC ACIDS AND USES THEREOF - This invention provides compounds of formula (I): | 02-11-2016 |
20160039794 | PYRAZOLYLBENZO[D]IMIDAZOLE DERIVATIVES - A compound represented by the general Formula (I), wherein hydrogen atoms shown as attached to pyrazole and benzimidazole rings are attached to one of nitrogen atoms of the pyrazole or benzimidazole ring, respectively; R | 02-11-2016 |
20160039798 | NOVEL N-(2,3-DIHYDRO-1H-PYRROLO[2,3-b]PYRIDIN-5-YL)-4-QUINAZOLINAMINE AND N-(2,3-DIHYDRO-1H-INDOL-5-YL)-4-QUINAZOLINAMINE DERIVATIVES AS PERK INHIBITORS - The present invention relates to N-(2,3-dihydro-1H-pyrrolo[2,3-b]pyridin-5-yl)-4-quinazolinamine and N-(2,3-dihydro-1H-indol-5-yl)-4-quinazolinamine derivatives of Formula (I) | 02-11-2016 |
20160039810 | A CRYSTALLINE FORM OF AN ANXIOLYTIC COMPOUND - A crystalline Form B of compound 1 can be used in pharmaceutically compositions. The pharmaceutical compositions can be used in methods of treating a disease (e.g., a disease of the central nervous system). | 02-11-2016 |
20160045485 | NEW USE OF 1H-INDAZOLE-3-CARBOXAMIDE COMPOUNDS AS GLYCOGEN SYNTHASE KINASE 3 BETA INHIBITORS - The present invention relates to the new use of 1H-indazole-3-carboxamide compounds as glycogen synthase kinase 3 beta (GSK-3β) inhibitors and to their use in the treatment of GSK-3β-related disorders such as, for example, (i) insulin-resistance disorders; (ii) neurodegenerative diseases; (iii) mood disorders; (iv) schizophrenic disorders; (v) cancerous disorders; (vi) inflammation, (vii) substance abuse disorders; and (viii) epilepsies. | 02-18-2016 |
20160045511 | KINASE INHIBITORS AND METHOD OF TREATING CANCER - The invention is directed to a compound represented by the following structural formula and pharmaceutically acceptable salts thereof: | 02-18-2016 |
20160060247 | HISTONE DEMETHYLASE INHIBITORS - The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted 3-aminopyridine derivative compounds, substituted 3-aminopyridazine derivative compounds, and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like. | 03-03-2016 |
20160060257 | PYRROLO [2,3-B] PYRIDINE CDK9 KINASE INHIBITORS - Disclosed are compounds of Formula (IIa), | 03-03-2016 |
20160060260 | BROMODOMAIN INHIBITORS FOR TREATING DISEASE - Disclosed herein are compounds and compositions useful in the treatment of bromodomain-containing protein-mediated diseases, such as cancer, having the structure of Formula I: | 03-03-2016 |
20160067259 | SELECTIVE HDAC1 AND HDAC2 INHIBITORS - Provided herein are compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with HDAC activity, particularly diseases or disorders that involve activity of HDAC1 and/or HDAC2. Such diseases include cancer, sickle-cell anemia, beta-thalassemia, and HIV. | 03-10-2016 |
20160074412 | Chemical Compounds - There is provided pyrimidinyl compounds of Formula (I), | 03-17-2016 |
20160075695 | BENZIMIDAZOLE DERIVATIVES AS BROMODOMAIN INHIBITORS - This application relates to chemical compounds which may act as inhibitors of, or which may otherwise modulate the activity of, a bromodomain-containing protein, including bromodomain-containing protein 4 (BRD4), and to compositions and formulations containing such compounds, and methods of using and making such compounds. Compounds include compounds of Formula (I) wherein R | 03-17-2016 |
20160083382 | COMPOUNDS FOR INHIBITING DRUG-RESISTANT STRAINS OF HIV-1 INTEGRASE - A method of inhibiting drug-resistant HIV-1 integrase in a subject comprising administering to a subject in need thereof a therapeutically effective amount of a compound of formula I, or a pharmaceutically acceptable salt or ester thereof, having a structure of: | 03-24-2016 |
20160090364 | PHTHALAZINONES AND ISOQUINOLINONES AS ROCK INHIBITORS - The present invention provides compounds of Formula (I): | 03-31-2016 |
20160096820 | INHIBITORS OF INV(16) LEUKEMIA - This invention describes the development of targeted small molecule inhibitors of the inv(16) fusion, the causative agent in ˜12% of acute myeloid leukemia (AML). The inv(16) fusion results in expression of the CBFβ-SMMHC fusion protein in the blood cells of afflicted patients. The present invention provides compounds which inhibit the function of both CBFβ and the CBFβ-SMMHC fusion. These compounds block the growth of an inv(16) leukemia cell line as well as increase its apoptosis, while showing minimal effects against non inv(16) cell lines. As a mechanism to develop inhibitors with selectivity for the CBFβ-SMMHC fusion protein, the present invention further provides dimeric derivatives of these compounds which show both increased potency as well as selectivity for CBFβ-SMMHC. These compounds show potent inhibition of an inv(16) leukemia cell line with minimal effects on non inv(16) cell lines. Analysis of the pharmacokinetics of the developed compounds has made it possible to improve the lifetime of the compound in the plasma of mice to a level commensurate with long-term treatment. | 04-07-2016 |
20160102089 | Arylpyrrolopyridine derived compounds as LRRK2 inhibitors - The present invention is directed to arylpyrrolopyridine derivatives of formula (A) (A). The compounds are considered useful for the treatment of diseases associated with LRRK2 such as Lewy body dementia, Parkinson's disease cancer. | 04-14-2016 |
20160108030 | THERAPEUTIC COMPOUNDS - Compounds of formula (I) or salts thereof are disclosed. Also disclosed are pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating a Retroviridae viral infection including an infection caused by the HIV virus. | 04-21-2016 |
20160108032 | HISTONE DEMETHYLASE INHIBITORS - The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted pyrrolopyridine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like. | 04-21-2016 |
20160113928 | HETEROCYCLIC COMPOUNDS AS HEDGEHOG SIGNALING PATHWAY INHIBITORS - This invention relates to novel compounds of formula (I). The compounds of the invention are hedgehog pathway antagonists. Specifically, the compounds of the invention are useful as Smoothened (SMO) inhibitors. The invention also contemplates the use of the compounds for treating conditions treatable by the inhibition of the Hedgehog pathway and SMO, for example cancer. | 04-28-2016 |
20160115164 | BICYCLIC HETEROCYCLES AS FGFR4 INHIBITORS - The present invention relates to bicyclic heterocycles, and pharmaceutical compositions of the same, that are inhibitors of the FGFR4 enzyme and are useful in the treatment of FGFR4-associated diseases such as cancer. | 04-28-2016 |
20160137637 | 2,3-DIHYDROBENZOFURAN-5YL COMPOUNDS AS DYRK KINASE INHIBITORS - The present invention relates to compounds of below Formula (I), physiologically functional derivatives or salts thereof, where the groups R | 05-19-2016 |
20160137643 | 1,7-NAPHTHYRIDINE DERIVATIVES - The present invention relates to compounds of general formula I wherein R | 05-19-2016 |
20160152601 | PYRIMIDYL CYCLOPENTANES AS AKT PROTEIN KINASE INHIBITORS | 06-02-2016 |
20160152608 | BENZIMIDAZOLE DERIVATIVES AS SELECTIVE PROTEINE KINASE INHIBITORS | 06-02-2016 |
20160159751 | NOVEL QUINAZOLINES AS BIOGENIC AMINE TRANSPORT MODULATORS - The present disclosure relates to certain amine derivatives of fused bicyclic heterocycles that inhibit the amine reuptake function of the biogenic amine transporters, dopamine transporter (DAT), serotonin transporter (SERT) and norepinephrine transporter (NET). Compounds of the present disclosure are potent inhibitors of the reuptake of dopamine (DA), serotonin (5-hydroxytryptamine, 5-HT) and norepinephrine (NE) with full or partial maximal efficacy. The compounds with partial maximal efficacy in inhibiting reuptake of all three biogenic amines are herein referred to as partial triple uptake inhibitors (PTRIs). Compounds of the present disclosure are useful for treating depression, pain and substance abuse and relapse to substance abuse and addiction to substances such as cocaine, methamphetamine, nicotine and alcohol. 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. | 06-09-2016 |
20160159776 | BENZIMIDAZOLE-2-PIPERAZINE HETEROCYCLIC COMPOUND, PHARMACEUTICAL COMPOSITION CONTAINING THE SAME, PREPARATION METHOD AND USE THEREOF - The present invention relates to a class of benzimidazole-2-piperazine heterocyclic derivatives, a preparation method and medical use thereof. Specifically, the present invention relates to a new benzimidazole-2-piperazine heterocyclic derivative of general Formula (I), a preparation method, a pharmaceutical composition containing the same, and use thereof as a therapeutic agent and especially as a poly(ADP-ribose)polymerase (PARP) inhibitor. | 06-09-2016 |
20160159791 | COMPOUNDS AS MODULATORS OF RORC - The present invention encompasses compounds of the formula (I), wherein the variables are defined herein which are suitable for the modulation of RORC and the treatment of diseases related to the modulation of RORC. The present invention also encompasses processes of making compounds of formula (I) and pharmaceutical preparations containing them. | 06-09-2016 |
20160168140 | HETEROCYCLIC COMPOUNDS AS ANTIBIOTIC POTENTIATORS | 06-16-2016 |
20160176848 | INDOLIZINE COMPOUNDS, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM | 06-23-2016 |
20160185770 | SALTS, CO-CRYSTALS, AND POLYMORPHS OF AN ANXIOLYTIC COMPOUND - The present invention provides amorphous arid crystalline forms of 1-ethyl-6-(indan-2-ylamino)-3-(morpholine-4-carbonyl)-1,8-naphthyridin-4-one (compound 1), and salts, co-crystals, and pharmaceutical compositions thereof. The invention also provides methods of treating and/or preventing a disease, such as a central nervous system disease (e.g., an anxiety disorder), using the amorphous and crystalline forms, and salts, co-crystals, and pharmaceutical compositions thereof. | 06-30-2016 |
20160193218 | NOVEL QUINAZOLINONES AS BROMODOMAIN INHIBITORS | 07-07-2016 |
20160194291 | STYRYL QUINAZOLINE DERIVATIVES AS PHARMACEUTICALLY ACTIVE AGENTS | 07-07-2016 |
20160376261 | BENZIMIDAZOLE DERIVATIVES AS BROMODOMAIN INHIBITORS - This application relates to chemical compounds which may act as inhibitors of, or which may otherwise modulate the activity of, a bromodomain-containing protein, including bromodomain-containing protein 4 (BRD4), and to compositions and formulations containing such compounds, and methods of using and making such compounds. Compounds include compounds of Formula (I) | 12-29-2016 |
20170232000 | METHODS OF TREATMENT USING SELECTIVE BCL-2 INHIBITORS | 08-17-2017 |
20170233375 | CANCER THERAPEUTICS | 08-17-2017 |