Entries |
Document | Title | Date |
20080207682 | Phenylurea Derivatives As Inhibitors Of Tyrosine Kinases For The Treatment Of Tumour Diseases - Compounds of the formula (I), in which R | 08-28-2008 |
20080207683 | BIARYL-SUBSTITUTED TETRAHYDRO-PYRAZOLO-PYRIDINE MODULATORS OF CATHEPSIN S - Biaryl-substituted tetrahydro-pyrazolo-pyridine compounds are described, which are useful as cathepsin S modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by cathepsin S activity, such as psoriasis, pain, multiple sclerosis, atherosclerosis, and rheumatoid arthritis. | 08-28-2008 |
20080207684 | Kinase inhibitors and methods for using the same - Compounds of formula I: | 08-28-2008 |
20080221154 | HIV-INTEGRASE INHIBITORS, PHARMACEUTICAL COMPOSITIONS, AND METHODS FOR THEIR USE - Bicyclic hydroxamate compounds represented by the Formula I: | 09-11-2008 |
20080234314 | FUSED AMINO PYRIDINE AS HSP90 INHIBITORS - The present invention relates to HSP90 inhibitors containing fused amino pyridine core that are useful as inhibitors of HSP90 and their use in the treatment of HSP90 related diseases and disorders such as cancer, an autoimmune disease, or a neurodegenerative disease. | 09-25-2008 |
20080242695 | Certain Chemical Entities, Compositions, and Methods - Provided are certain chemical entities, and methods of use to modulate skeletal myosin, skeletal actin, skeletal tropomyosin, skeletal troponin C, skeletal troponin I, skeletal troponin T, and skeletal muscle, including fragments and isoforms thereof, as well as the skeletal sarcomere, and methods of use in the treatment of muscle weakness and/or cachexia, as part of a rehabilitation or conditioning exercise regimen, or in the treatment of fraility, post-polio syndrome, obesity, sarcopenia, wasting syndrome, muscle spasm, and other indications. | 10-02-2008 |
20080255185 | 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. | 10-16-2008 |
20080255186 | Pyrazolo[3,4-B]Pyridine Compound, and Its Use as a Pde4 Inhibitor - The invention provides N-{[1,6-diethyl-4-(tetrahydro-2H-pyran-4-ylamino)-1H-pyrazolo[3,4-b]pyridin-5-yl]methyl}-3-methyl-5-isoxazolecarboxamide | 10-16-2008 |
20080269280 | OXO-IMIDAZOLIDINES AS MODULATORS OF CHEMOKINE RECEPTORS - Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally monocyclic and bicyclic compounds and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists. | 10-30-2008 |
20080269281 | Novel Beta-Agonists, Method for Producing Them and Their Use as Drugs - Compounds of the formula | 10-30-2008 |
20080275078 | Pyrazolo[3,4-B] Pyridine Compounds and Their Use as Pde4 Inhibitors - The invention provides a compound of formula (I) or a salt thereof: | 11-06-2008 |
20080312271 | AZABENZIMIDAZOLYL COMPOUNDS - Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I | 12-18-2008 |
20080312272 | ARYLOAZOL-2-YL CYANOETHYLAMINO COMPOUNDS, METHOD OF MAKING AND METHOD OF USING THEREOF - The present invention relates to novel aryloazol-2-yl-cyanoethylamino derivatives of formula (I): | 12-18-2008 |
20080319005 | Phenylacetamides Suitable as Protein Kinase Inhibitors - The invention relates to compounds of the formula (I) wherein the moieties R1, R2, R3, R9, R10 and Q and X, Y and Z are as defined in the specification, and salts thereof, as well as their use, methods of use for them and method of their synthesis, and the like. The compounds are protein kinase inhibitors and can, inter alia, be used in the treatment of various proliferative diseases. | 12-25-2008 |
20090018158 | CRYSTAL FORMS OF AN IMIDAZOLE DERIVATIVE - The invention relates to the essentially pure Λ/-[({2-[4-(2-Ethyl-4,6-dimethyl-1H-imidazo[4,5-c]pyridin-1 -yl)phenyl]ethyl}amino)carbonyl]-4-methylbenzenesulfonamide Polymorph Forms A and B and to processes for the preparation of, compositions containing and to the uses of, such crystal forms. | 01-15-2009 |
20090023771 | PHARMACEUTICAL COMPOSITION COMPRISING A PROTON PUMP INHIBITOR AND PROTEIN COMPONENT - The present disclosure relates to, inter alia, pharmaceutical compositions comprising a H | 01-22-2009 |
20090036482 | Imidazopyridine-derivatives as inductible no-synthase inhibitors - The compounds of Formula (I) | 02-05-2009 |
20090042931 | Tricyclic Angiotensin II Agonists - There is provided compounds of formula I, | 02-12-2009 |
20090062330 | TREATMENT OF PROGRESSIVE NEURODEGENERATIVE DISEASE WITH IBUDILAST - Compositions and methods for treating progressive neurodegenerative diseases, and their associated symptoms by administration of ibudilast (3-isobutyryl-2-isopropylpyrazolo[1,5-a]pyridine). | 03-05-2009 |
20090076069 | DEUTERIUM-ENRICHED APIXABAN - The present application describes deuterium-enriched apixaban, pharmaceutically acceptable salt forms thereof, and methods of treating using the same. | 03-19-2009 |
20090076070 | HETERO COMPOUND - [Problems] To provide a useful compound as an active ingredient for a preventing and/or treating agent for rejection in the transplantation of an organ, bone marrow, or a tissue, an autoimmune disease, or the like, which has an excellent S1P | 03-19-2009 |
20090082392 | Substituted Carboxylic Acids - The present invention relates to compounds and pharmaceutically acceptable salts of formula (I): | 03-26-2009 |
20090093516 | TRIAZOLOPYRIDINE 11-BETA HYDROXYSTEROID DEHYDROGENASE TYPE I INHIBITORS - Novel compounds are provided which are 11 -beta-hydroxysteroid dehydrogenase type I inhibitors. 11-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds of formula I: | 04-09-2009 |
20090099228 | PYRAZOLO-TETRAHYDRO PYRIDINE DERIVATIVES AS OREXIN RECEPTOR ANTAGONISTS - The invention relates to novel pyrazolo-tetrahydropyridines compounds and their use as orexin receptor antagonists. | 04-16-2009 |
20090111848 | Halogenated Pyrazolo[1,5-A]Pyrimidines, Processes, Uses, Compositions and Intermediates - The invention provides novel halogenated pyrazolo[1,5-a]pyrimidines of formula (I) wherein R, R | 04-30-2009 |
20090118325 | 5-Thioxylopyranose Compounds - 5-thioxylose compounds, especially 5-thioxylopyranose compounds, a process for their preparation, and their use for treating and/or inhibiting thromboses, especially venous thromboses. The compounds correspond to formula I: | 05-07-2009 |
20090137624 | Chemical Compounds - This invention relates to novel compounds having the formula (I): and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment for cancer. | 05-28-2009 |
20090143422 | 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. | 06-04-2009 |
20090163539 | ENANTIOMER OF TENATOPRAZOLE AND THE USE THEREOF IN THERAPY - This invention relates to optically active substances of tenatoprazole, (+) and (−) -5-methoxy-2-{(4-methoxy-3,5-dimethyl-2-pyridyl)methyl]sulfinyl}-1H-imidazo[4,5-b]pyridine. The compound and pharmaceutical compositions thereof are useful for anti-ulcer agent. | 06-25-2009 |
20090197910 | NOVEL VIRAL REPLICATION INHIBITORS - The present invention relates to a pharmaceutical composition for the treatment or prevention of viral infections comprising as an active principle at least one benzimidazole conjugates derivative having the general formula (I). The invention also relates to processes for the preparation of compounds according to the invention having above mentioned general formula and their use as a medicine or to treat or prevent viral infections. | 08-06-2009 |
20090197911 | LONIDAMINE ANALOGUES AND TREATMENT OF POLYCYSTIC KIDNEY DISEASE - Lonidamine derivatives can be useful in methods of treating, inhibiting, and/or preventing polycystic kidney disease (PKD). Accordingly, lonidamine derivatives can be administered in a therapeutically effective amount for inhibiting, and/or preventing polycystic kidney disease (PKD) in the subject. This can include administering a therapeutically effective amount of the lonidamine derivatives for inhibiting CFTR and/or Hsp90 or biological pathway thereof. Also, the method can include administering the lonidamine derivatives in a therapeutically effective amount for inhibiting ErbB2, Src, Raf-1, B-Raf, MEK, Cdk4, NKCC1, or combinations thereof. For example, the therapeutically effective amount of the lonidamine derivatives can be configured so as to provide a concentration in or adjacent to a kidney cell of about 0.25 uM or more or less. | 08-06-2009 |
20090203732 | Thiazolones for Use as P13 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. | 08-13-2009 |
20090209577 | Novel Triazolopyridine Compounds - This invention is directed generally to triazolopyridine compounds that generally inhibit p38 kinase, TNF, and/or cyclooxygenase activity. Such triazolopyridine include compounds generally corresponding in structure to the following formula: | 08-20-2009 |
20090209578 | CHEMICAL COMPOUNDS - The present invention provides compounds of formula (I) wherein R | 08-20-2009 |
20090215817 | Novel Triazolopyridine Compounds for the Treatment of Inflammation - This invention is directed generally to triazolopyridine compounds that generally inhibit p38 kinase, TNF, and/or cyclooxygenase activity. Such triazolopyridine include compounds generally corresponding in structure to the following formula: | 08-27-2009 |
20090215818 | THIOZOLIDINEDIONE DERIVATIVES AS PI3 KINASE INHIBITORS - Invented is a method of inhibiting the activity/function of PI3 kinases using thiozolidinedione 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 thiozolidinedione derivatives. | 08-27-2009 |
20090221631 | IMIDAZOPYRIDINONES - The invention relates to imidazopyridinones, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. | 09-03-2009 |
20090221632 | Bicyclo-Pyrazoles and Pharmaceutical Compositions Comprising Them - Bicyclo-pyrazole compounds of formula (I), as herein defined, are useful for treating diseases linked to disregulated protein kinases. | 09-03-2009 |
20090239899 | Triazolopyridinylsulfanyl Derivatives As P38 Map Kinase Inhibitors - A compound of formula (I), or a pharmaceutical acceptable salt and/or solvate (including hydrate) thereof; | 09-24-2009 |
20090247570 | PHARMACEUTICALS - The present invention relates to the use of a CCR5 antagonist in an HIV infected patient to enhance their immune reconstitution and so treat to HIV related opportunistic conditions resulting from the immunocompromised state of the HIV patient. The invention also allows treatment with a CCR5 antagonist of patients having a CXCR4 using viral population since such patients will also benefit from an increase in their CD4 and/or CD8 cell count. | 10-01-2009 |
20090247571 | Certain Chemical Entities, Compositions and Methods - Provided are certain chemical entities, and methods of use to modulate skeletal myosin, skeletal actin, skeletal tropomyosin, skeletal troponin C, skeletal troponin I, skeletal troponin T, and skeletal muscle, including fragments and isoforms thereof, as well as the skeletal sarcomere, and methods of use in the treatment of obesity, sarcopenia, wasting syndrome, frailty, cachexia, muscle spasm, post-surgical and post-traumatic muscle weakness, neuromuscular disease, and other indications. | 10-01-2009 |
20090253737 | CERTAIN CHEMICAL ENTITIES, COMPOSITIONS, AND METHODS - Provided are certain chemical entities, and methods of use to modulate skeletal myosin, skeletal actin, skeletal tropomyosin, skeletal troponin C, skeletal troponin I, skeletal troponin T, and skeletal muscle, including fragments and isoforms thereof, as well as the skeletal sarcomere, and methods of use in the treatment of neuromuscular disorders, conditions having muscle wasting, claudication, frailty, metabolic syndrome, muscle atrophy associated with disuse, and muscle fatigue, and other indications. | 10-08-2009 |
20090253738 | TRIAZOLOPYRIDINONE DERIVATIVES FOR USE AS STEAROYL CoA DESATURASE INHIBITORS - The present invention discloses triazolopyridinone derivatives for use as inhibitors of stearoyl-CoA desaturase having the structure of Formula I: | 10-08-2009 |
20090258897 | Substituted benzimidazoles - Disclosed herein are substituted benzimidazole-based proton pump modulators of Formula I, processes of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof. | 10-15-2009 |
20090286827 | NOVEL BI-ARYL AMINES - The present invention relates to novel bi-aryl amines of formula (I) and to pharmaceutically acceptable prodrugs, salts, solvates, hydrates, and N-oxides thereof and to pharmaceutical compositions comprising them, methods of their use, and methods of their preparation. | 11-19-2009 |
20090298866 | Indole Compounds - The present application relates to compounds of formula (I) or a pharmaceutically acceptable derivative thereof: formula (I) wherein X, R | 12-03-2009 |
20090306129 | SUBSTITUTED PYRAZOLO [3,4-B] PYRIDINES AS PHOSPHODIESTERASE INHIBITORS - The present invention relates to phosphodiesterase (PDE) type IV selective inhibitors. Processes for the preparation of disclosed compounds, pharmaceutical compositions containing the disclosed compounds and their use as PDE type IV selective inhibitors are provided. Prepared compounds correspond to structure XIV Formula (XIV). | 12-10-2009 |
20090318494 | PYRAZOLO[3,4-B]PYRIDINE COMPOUNDS, AND THEIR USE AS PDE4 INHIBITORS - The invention provides a compound of formula (I) or a salt thereof: | 12-24-2009 |
20090326003 | PYRAZOLO (3, 4-B) PYRIDINE DERIVATIVES AS PDE4 INHIBITORS - The present invention provides a compound of formula (I) or a salt thereof (in particular, a pharmaceutically acceptable salt thereof): | 12-31-2009 |
20100004280 | Substituted imidazoles as bombesin receptor subtype-3 modulators - Certain novel substituted imidazoles are ligands of the human bombesin receptor and, in particular, are selective ligands of the human bombesin receptor subtype-3 (BRS-3). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of BRS-3, such as obesity, and diabetes. | 01-07-2010 |
20100004281 | VIRAL INHIBITORS - The present invention relates to imidazo[4,5-c]pyridine compounds and pharmaceutical compositions for the treatment or prevention of viral infections, wherein the imidazo[4,5-c]pyridine compounds have the formula: | 01-07-2010 |
20100029709 | NOVEL COMPOUNDS USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES - A novel [1,2,4]triazolo[1,5-a]pyridine compound is disclosed that has a formula represented by the following: | 02-04-2010 |
20100029710 | COMPOUNDS HAVING BOTH ANGIOTENSIN II RECEPTOR ANTAGONISM AND PPARy ACTIVATING ACTIVITIES - Compounds of following formula (I) are provided that have both angiotensin II receptor antagonist activity and PPARy agonist activity. Also provided are pharmaceutical compositions comprising the compounds and methods of treatment of diseases with the compounds including type 2 diabetes, insulin resistance, hyperinsulinemia, hyperlipidemia, hypertriglyceridemia, metabolic syndrome, congestive heart failure, and hypertension. | 02-04-2010 |
20100048611 | TETRAHYDROPYRROLOPYRIDINE, TETRAHYDROPYRAZOLOPYRIDINE, TETRAHYDRO-IMIDAZOPYRIDINE AND TETRAHYDROTRIAZOLOPYRIDINE DERIVATIVES AND USE THEREOF - The invention relates to novel tetrahydropyrrolopyridine, tetrahydropyrazolopyridine, tetrahydroimidazopyridine and tetrahydrotriazolopyridine derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular of thromboembolic disorders | 02-25-2010 |
20100048612 | BICYCLIC HETEROCYCLES AS CANNABINOID-1 RECEPTOR MODULATORS - The present application describes compounds according to Formula I, pharmaceutical compositions comprising at least one compound according to Formula I and optionally one or more additional therapeutic agents and methods of treatment using the compounds according to Formula I both alone and in combination with one or more additional therapeutic agents. The compounds have the following general formula: | 02-25-2010 |
20100063088 | Raf Kinase Inhibitors - Methods of treating tumors mediated by raf kinase, with substituted urea compounds, and such compounds per se. | 03-11-2010 |
20100069431 | IMIDAZOPYRIDINE COMPOUNDS - Compounds, pharmaceutical compositions, kits and methods are provided for use with glucokinase that comprise a compound selected from the group consisting of formula (I) wherein the variables are as defined herein. | 03-18-2010 |
20100076014 | 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, and/or 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 (Ia) is heterocycle or heteroaryl; J, Ja, E, F, G, Ma, M, Q, Za and Z are as defined herein. Also provided are pharmaceutical compositions and methods of treating inflammatory- or immune-associated diseases and obesity and diabetes employing said compounds. | 03-25-2010 |
20100087477 | SELECTIVE GLYCOSIDASE INHIBITORS - The present invention provides glucoimidazole derivatives and methods of making them. The compounds can be used to inhibit the activity of O-GlcNAcase enzymes, including both bacterial OGA (bOGA) and human OGA (hOGA) and can be selective, showing low inhibition of hexosaminidases. The compounds can be used to study the role of the O-GlcNAcase modification in human or animal cells. Furthermore the compounds can have therapeutic uses in the treatment of diseases mediated by the activity of O-GlcNAcase enzymes including type II diabetes, Alzheimers disease, and cancer. | 04-08-2010 |
20100087478 | HIF-1 Inhibitors - HIF-1 inhibitors and methods of their use are provided. In particular, 2,2-dimethylbenzopyran based compounds and methods of their use, for example in the treatment or prevention of hypoxia-related pathologies are provided. | 04-08-2010 |
20100093788 | HETEROCYCLIC BENZIMIDAZOLES AS TRPM8 MODULATORS - Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: | 04-15-2010 |
20100105723 | 5-PHENYL-6-PYRIDIN-4-YL-1,3-DIHYDRO-2H-IMIDAZO[4,5-b]PYRIDIN-2-ONE DERIVATIVES USEFUL AS A2B ADENOSINE RECEPTOR ANTAGONISTS - The present disclosure relates to compounds of formula (I): | 04-29-2010 |
20100113507 | 3-Tetrazolyl Indazoles, 3-Tetrazolyl Pyrazolopyridines, and use Thereof - The present application relates to novel 3-tetrazolylindazole and 3-tetrazolylpyrazolo[3,4-b]-pyridine derivatives, processes for their preparation, their use alone or in combination for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prevention of cardiovascular disorders. | 05-06-2010 |
20100120840 | Heterocyclic benzylamino derivatives, their manufacture and use as pharmaceutical agents - Objects of the present invention are the compounds of formula (I) their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, pharmaceutical compositions containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer. | 05-13-2010 |
20100120841 | BENZIMIDAZOLE COMPOUND AND PHARMACEUTICAL USE THEREOF - Provided is an ORL-1 receptor agonist having improved bioavailability based on superior metabolic stability and strong and high selectivity, as compared to conventional compounds. A compound represented by the formula (I) | 05-13-2010 |
20100125089 | ENANTIOMERICALLY ENRICHED ARYLOAZOL-2-YL CYANOETHYLAMINO COMPOUNDS, METHOD OF MAKING AND METHOD OF USING THEREOF - The present invention relates to novel aryloazol-2-yl-cyanoethylamino derivatives substantially enriched in an enantiomer of formula (I): | 05-20-2010 |
20100130542 | Composition Comprising a Combination of Omeprazole and Lansoprazole, and a Buffering Agent, and Methods of Using Same - The present disclosure relates to pharmaceutical compositions comprising omeprazole, lansoprazole and sodium bicarbonate. Methods of using such compositions are also provided | 05-27-2010 |
20100130543 | PYRAZOLE CARBOXAMIDE INHIBITORS OF FACTOR XA - The present invention relates to new pyrazole carboxamide inhibitors of factor Xa, pharmaceutical compositions thereof, and methods of use thereof. | 05-27-2010 |
20100152230 | HYDROXY SUBSTITUTED 1H-IMIDAZOPYRIDINES AND METHODS - Hydroxy substituted 1H-imidazo[4,5-c]pyridin-4-amines, with a hydroxy substituent at the 2-position, pharmaceutical compositions containing these compounds, methods of making the compounds, intermediates, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed. | 06-17-2010 |
20100168159 | HETERO COMPOUND | 07-01-2010 |
20100173934 | COMBINATIONS OF THERAPEUTIC AGENTS FOR TREATING CANCER - The invention relates to a combination comprising a microtubule active agent; and one or more pharmaceutically active agents; pharmaceutical compositions comprising said combination; methods of treatment comprising said combination; processes for making said combination; and a commercial package comprising said combination. | 07-08-2010 |
20100184801 | FUSED AMINO PYRIDINES FOR THE TREATMENT OF BRAIN TUMORS - The present invention relates to the use of compounds with fused amino pyridine core for the treatment of malignancies associated with brain and lung. The oral administration of compounds of the instant application results in effective brain penetration and provides for non-intrusive treatment of brain and lung tumors. | 07-22-2010 |
20100190820 | 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, and/or 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 the group X is O or (R | 07-29-2010 |
20100216835 | Method For Modulating Microbial Quorum Sensing - The present invention provides compositions and methods for modulating bacterial quorum sensing using antagonist or agonist compounds. Further, the present invention provides methods of treating or preventing microbial damages and diseases, in particular for diseases where there is an advantage in inhibiting quorum sensing regulated phenotypes of pathogens. | 08-26-2010 |
20100249181 | HIV Protease Inhibiting Compounds - A compound of the formula | 09-30-2010 |
20100280065 | PERHARIDINES AS CDK INHIBITORS - The invention relates to trisubstituted or tetrasubstituted imidazo[4,5b]pyridines, to their uses as well as to a process for manufacturing them. | 11-04-2010 |
20100286191 | 2-Arylthiazole Derivatives as CXCR3 Receptor Modulators - The invention encompasses compounds of Formula I or pharmaceutically acceptable salts thereof, which are modulators of the CXCR3 chemokine receptor function useful for the treatment or prevention of pathogenic inflammatory processes, autoimmune diseases or graft rejection processes. Methods of use and pharmaceutical compositions are also encompassed. | 11-11-2010 |
20100286192 | NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS - Compounds of Formula I: | 11-11-2010 |
20100317689 | Prodrugs of proton pump inhibitors including the 1h-imidazo[4,5-b] pyridine moiety - The compounds of formulas (I), (II), (III) and (IV), where the symbols are as defined in the specification are prodrugs of proton pump inhibitors. The R | 12-16-2010 |
20100331359 | NOVEL COMPOUND USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES - A compound is disclosed that has a formula represented by the following: | 12-30-2010 |
20110003848 | Polymorphic Form Of A [1,2,4]Triazole[4,3-A] Pyridine Derivative For Treating Inflammatory Diseases - The present invention relates to a polymorphic form B of Λ/[3-tert-butyl-1-(3-chloro-4-hydroxyphenyl)-1H-pyrazol-5-yl]-N-{2-[(3-{2-[(2-hydroxyethyl)sulfanyl]phenyl}[1,2,4]triazolo[4,3-a]pyridin-6-yl)sulfanyl]benzyl}urea (I) as de-fined herein. This polymorph is useful in the treatment of various conditions, particularly in the treatment of inflammatory conditions such as chronic obstructive pulmonary disease. | 01-06-2011 |
20110009444 | N-AZABICYCLIC CARBOXAMIDE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF - This disclosure relates to compounds of formula (I): | 01-13-2011 |
20110009445 | NEUROPROTECTANTS - Methods of protecting cells against cytotoxic insults are provided. The methods involve administering a composition including a CpG oligonucleotide to a subject. The methods are applicable to the protection of neural and non-neural cells. For example, methods of protecting a neural cell against excitotoxic brain injury are provided. Methods for preparing medicaments for the prophylactic treatment of excitotoxic injury, ischemia and/or hypoxia are also provided. Also provided are compositions for use in the described methods. | 01-13-2011 |
20110021559 | AMINOPYRIDINES USEFUL AS INHIBITORS OF PROTEIN KINASES - The present invention relates to compounds useful as inhibitors of 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. | 01-27-2011 |
20110034506 | TRIAZOLOPYRIDINE COMPOUNDS USEFUL AS DGAT1 INHIBITORS - Disclosed are triazolopyridine compounds of the following Formula (I); or stereoisomers or salts thereof. Also, disclosed are methods of using the compound in the treatment of obesity, dyslipidemia, diabetes and atherosclerosis, and to pharmaceutical compositions comprising at least one compound of Formula (I) or a stereoisomer or pharmaceutically acceptable salt thereof. | 02-10-2011 |
20110039884 | Imidazopyridinones - The invention relates to imidazopyridinones, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. | 02-17-2011 |
20110060002 | CONGLOMERATES OF TENATOPRAZOLE POTASSIUM SALTS - The invention relates to conglomerates of tenatoprazole potassium salts of the following general formula (I), that consist of an equimolar mixture of enantiomers having R and S configurations and capable of crystallisation in the form of a conglomerate, wherein said salts are selected from tenatoprazole dehydrated potassium salt, tenatoprazole potassium dimethanolate, tenatoprazole potassium diethanolate and tenatoprazole potassium ethylene-glycolate. The invention also relates to a pharmaceutical composition containing such salt, and to the use of said salt. | 03-10-2011 |
20110060003 | LONIDAMINE ANALOGUES FOR FERTILITY MANAGEMENT - Fertility management can include: administering to the subject one or more doses of a compound according to Formula I so as to reduce fertility in the subject. Fertility management can also include administering an effective amount of the compound to: impair Sertoli cell function in a male subject; inhibit spermatogenesis in the subject; reduce testis weight in the subject; reduce ovary weight in a female subject; reduce serum progesterone in the female subject; impair ovarian follicle function in the female subject; causing reversible fertility in the subject. In order to return fertility, the method can include ceasing administration of the compound to the subject so as to return fertility in the subject. The compound can be administered for irreversibly sterilizing the subject. | 03-10-2011 |
20110060004 | Imidazo-Pyridine Derivatives as Activin-Like Receptor Kinase (ALK4 or ALK5) Inhibitors - Compounds of formula (I): in free or salt or solvate form, where X, R | 03-10-2011 |
20110077267 | TRIAZOLOPYRIDINE COMPOUND, AND ACTION THEREOF AS PROLYL HYDROXYLASE INHIBITOR OR ERYTHROPOIETIN PRODUCTION-INDUCING AGENT - The present invention provides a triazolopyridine compound having a prolyl hydroxylase inhibitory action and an erythropoietin production-inducing ability. The present invention relates to a compound represented by the following formula [I]: | 03-31-2011 |
20110077268 | KINASE INHIBITORS AND METHODS OF USE - The present invention provides chemical entities or compounds and pharmaceutical compositions thereof that are capable of modulating lipid kinases such PB kinases, tryosine kinases and protein kinases such as mTOR. Also provided in the present invention are methods of using these compositions to modulate these kinases especially for therapeutic applications. | 03-31-2011 |
20110092539 | INDANE DERIVATIVES AS AMPA RECEPTOR MODULATORS - The present invention relates to a heterocyclic derivative according to formula (I); wherein the variables are defined as in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to a pharmaceutical composition comprising said heterocyclic derivatives and to their use in therapy, for instance in the treatment or prevention of psychiatric diseases where an enhancement of synaptic responses mediated by AMPA receptors is required, including schizophrenia, depression and Alzheimer's disease. | 04-21-2011 |
20110112138 | MULTI-CYCLIC CINNAMIDE DERIVATIVES - The present invention provides a compound represented by the formula (I): | 05-12-2011 |
20110152313 | SYNTHESIS OF AGELADINE A AND ANALOGS THEREOF - The invention describes a one pot process for synthesizing a compound of structure (I), or a tautomer thereof. A compound of structure (II), or a tautomer thereof, and an aldehyde of structure R | 06-23-2011 |
20110152314 | USE OF TENATOPRAZOLE FOR THE TREATMENT OF GASTROESOPHAGEAL REFLUX DISEASE - The invention relates to a novel therapeutic application of tenatoprazole. Tenatoprazole and the salts thereof can be used in the production of a medicament for the treatment of atypical and esophageal symptoms of gastroesophageal reflux, gastrorrhagia and dyspepsia. | 06-23-2011 |
20110172266 | PYRAZOLO PYRIDINE DERIVATIVES AS NADPH OXIDASE INHIBITORS - The present invention is related to pyrazolo pyridine derivatives of Formula (I), pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase). | 07-14-2011 |
20110184015 | NOVEL DERIVATIVES OF PYRROLOINDOLE WHICH ARE INHIBITORS OF HSP90, COMPOSITIONS CONTAINING SAME, AND USE THEREOF - Pyrroloindoles of formula (I) are provided wherein Het is an aromatic or partially unsaturated, monocyclic or bicyclic heterocycle containing between 1 and 4 heteroatoms N, O or S, optionally substituted by R1 or R′1 which are the same or different; R is X-(A-B)n-CONH2, X-(A-B)n-O—CONH2, X-(A-B)n-NH—CONH2, X—(CH2)m-heterocycloalkyl, X(CH2)m-aryl and X—(CH2)m-heteroaryl wherein X is —O—C(O), —NH—C(O), NH—CS, —NH—CO—CH2-O—; —NH—COCH2-S—CH2-CO—NH—; —NH—CO—(CH2)2-SO2-; and —NH—CO—CH2-N(CH3)-CO—; A and B are the same or different and are each independently a single bond, CH2, CH-alkyl, and CH-aralkyl; n=1,2 and m=0, 1; R1 and/or R′1 are H, halogen, CF3, nitro, cyano, alkyle, hydroxy, mercapto, amino, alkylamino, dialkylamino, alkoxy, alkylthio, and carboxy, free or esterified by an alkyl, carboxamide, CONH(alkyl), CON(alkyl)2, NH—CO-alkyl, sulfonamide, NH—SO2-alkyl, S(O)2-NHalkyl, and S(O2)-N(alkyl)2 group, all of said alkyl, alcoxy and alkylthio groups being optionally substituted themselves, said products being in all isomer forms and salts, as medicaments. | 07-28-2011 |
20110184016 | PREVENTION AND TREATMENT OF ITCH WITH CYSTEINE PROTEASE INHIBITION - Embodiments of the invention relates to methods of preventing itch in a subject using a therapeutically effective amount of a cysteine protease inhibitor. The itch is not associated with psoriasis and atopic dermatitis. The itch is also a non-histamine mediated itch. The inhibitor are directed to the cathepsin selected from the group consisting of cathepsin B, C, F, J, K, H, L, P, Q, S, W, X, V, and Z. | 07-28-2011 |
20110190335 | NITROGENATED 5-MEMBERED HETEROCYCLIC COMPOUND - The purpose of the present invention is to provide a glucokinase activator which is useful as a pharmaceutical agent such as agents for the prophylaxis or treatment of diabetes, obesity and the like, and the like. | 08-04-2011 |
20110190336 | AZABENZIMIDAZOLONES - Compounds are provided having the general structure of formula I: | 08-04-2011 |
20110190337 | SUBSTITUTED PYRAZOLOPYRIDINES, COMPOSITIONS CONTAINING THEM, METHOD FOR THE PRODUCTION THEREOF, AND THEIR USE - The disclosure relates to substituted pyrazolo-pyridines, compositions containing them, methods for the production thereof, and to their use as medicaments, in particular, as anticancer agents. | 08-04-2011 |
20110195992 | NEW COMPOUNDS II - The present invention relates to compounds of formula (I), | 08-11-2011 |
20110312992 | Inhibitors of C-Kit and Uses Thereof - Compounds and methods useful as inhibitors of c-Kit are presented. Pharmaceutical compositions containing these compounds, methods of using these compounds as inhibitors of c-Kit and processes for synthesizing these compounds are also described herein. | 12-22-2011 |
20120035208 | PYRAZOLOPYRIDINE PI3K INHIBITOR COMPOUNDS AND METHODS OF USE - Compounds of Formula (I), and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer or inflammation mediated by lipid kinases. Methods of using compounds of Formula (I) for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. | 02-09-2012 |
20120035209 | Hydroxy Substituted 1H-Imidazopyridines and Methods - Hydroxy substituted 1H-imidazo[4,5-c]pyridin-4-amines, with a hydroxy substituent at the 2-position, pharmaceutical compositions containing these compounds, methods of making the compounds, intermediates, and methods of use of these compounds as immunomodulators for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed. | 02-09-2012 |
20120059029 | SELECTIVE INTEGRIN INHIBITORS - This invention provides methods for selectively antagonizing the α4β1 integrin heterodimer in a subject in need thereof, and preferably in a human subject. The methods of the invention utilize conjugates comprising two or more α4β1 small molecule antagonists covalently attached to a biocompatible polymer. These methods of selectively inhibiting α4β1 may be used modulate both normal and pathological biological processes mediated at least in part through α4β1 activity. | 03-08-2012 |
20120059030 | HETEROCYCLIC COMPOUND AND USE THEREOF - The present invention provides a heterocycle derivative having a superior amyloid β production inhibitory activity and/or a superior γ-secretase modulation activity, and use thereof. A compound represented by the formula (I): | 03-08-2012 |
20120065227 | TRIAZOLOPYRIDINONE DERIVATIVES FOR USE AS STEAROYL CoA DESATURASE INHIBITORS - The present invention discloses triazolopyridinone derivatives for use as inhibitors of stearoyl-CoA desaturase having the structure of Formula I: | 03-15-2012 |
20120077841 | METHODS FOR CANCER THERAPY AND STEM CELL MODULATION - The present invention relates to a method of modulating pluripotency and/or self-renewing characteristics of a stem/progenitor cell. The method comprises administering to the respective cell a compound of the general formula (I) | 03-29-2012 |
20120088788 | SUBSTITUTED IMIDAZOLES AS BOMBESIN RECEPTOR SUBTYPE-3 MODULATORS - Certain novel substituted imidazoles are ligands of the human bombesin receptor and, in particular, are selective ligands of the human bombesin receptor subtype-3 (BRS-3). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of BRS-3, such as obesity, and diabetes. | 04-12-2012 |
20120095036 | NOVEL SUBSTITUTED INDAZOLE AND AZA-INDAZOLE DERIVATIVES AS GAMMA SECRETASE MODULATORS - The present invention is concerned with novel substituted indazole and aza-indazole derivatives of Formula (I) | 04-19-2012 |
20120095037 | SYNTHESIS AND ANTI-PROLIFERATIVE EFFECT OF BENZIMIDAZOLE DERIVATIVES - This invention provides for compounds, compositions, and methods that involve anti-proliferative and anti-neoplastic activity in cancer cells. In particular, a series of benzimidazole, purine, imidazopyridine, and imidazopyrizine compounds having selected substitution patterns are disclosed, and the activity of various subject compounds is demonstrated. In particular, the disclosure provides for substituted imidazo[4,5-b]pyridine compounds having the general formula | 04-19-2012 |
20120095038 | SYNTHESIS AND ANTI-PROLIFERATIVE EFFECT OF BENZIMIDAZOLE DERIVATIVES - This invention provides for compounds, compositions, and methods that involve anti-proliferative and anti-neoplastic activity in cancer cells. In particular, a series of benzimidazole, purine, imidazopyridine, and imidazopyrizine compounds having selected substitution patterns are disclosed, and the activity of various subject compounds is demonstrated. In particular, the disclosure provides for substituted imidazo[4,5-c]pyridine compounds having the general formula | 04-19-2012 |
20120115902 | 3H-Imidazo [4, 5-B] Pyridine- 6 -Carboxamides As Anti-Inflammatory Agents - There are provided compounds of formula (I), wherein R | 05-10-2012 |
20120115903 | Substituted Heteroaromatic Carboxamide and Urea Compounds as Vanilloid Receptor Ligands - Substituted heteroaromatic carboxamide and urea compounds corresponding to formula (i) | 05-10-2012 |
20120122919 | PHARMACEUTICAL COMPOSITION COMBINING TENATOPRAZOLE AND A HISTAMINE H2-RECEPTOR ANTAGONIST - The invention relates to a novel pharmaceutical combination. The inventive pharmaceutical composition, which is intended for the treatment of pathologies linked to gastric hyperacidity, comprises a combination of tenatoprazole and one or more histamine H2-receptor antagonists preferably selected from cimetidine, ranitidine, famotidine and nizatidine. The invention is particularly suitable for the treatment of duodenal and gastric ulcers and the symptoms of, and lesions caused by, gastroesophageal reflux. | 05-17-2012 |
20120165367 | AZAINDAZOLES USEFUL AS INHIBITORS OF KINASES - The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions. | 06-28-2012 |
20120165368 | PYRAZOLOPYRIDINE KINASE INHIBITORS - The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions. | 06-28-2012 |
20120172392 | AMINE-BASED AND AMIDE-BASED INHIBITORS OF SEMICARBAZIDE-SENSITIVE AMINE OXIDASE (SSAO) ENZYME ACTIVITY AND VAP-1 MEDIATED ADHESION USEFUL FOR TREATMENT OF DISEASES - Compositions and methods are disclosed for inhibiting semicarbazide-sensitive amine oxidase (SSAO), also known as vascular adhesion protein-1 (VAP-1). The compounds disclosed are amine-containing and amide-containing compounds. The compounds and compositions are useful for treatment of diseases, including inflammation, inflammatory diseases and autoimmune disorders. | 07-05-2012 |
20120178778 | PYRAZOLOPYRIDINES - The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions. | 07-12-2012 |
20120178779 | FUSED HETEROCYCLIC COMPOUND AND USE THEREOF - A fused heterocyclic compound of formula (1): | 07-12-2012 |
20120178780 | RAF KINASE INHIBITORS - Methods of treating tumors mediated by raf kinase, with substituted urea compounds, and such compounds per se. | 07-12-2012 |
20120202846 | MOLECULAR TARGET OF NEUROTOXICITY - The present invention relates to the fields of biology, genetics and medicine. In particular it concerns new methods for the detection, characterisation and/or treatment (or management) of neurodegenerative diseases, particularly amyotrophic lateral sclerosis. The invention equally concerns methods for identifying or screening compounds active in these diseases. The invention further concerns the compounds, genes, cells, plasmids or compositions useful for implementing the hereinabove methods. In particular, the invention describes the role of PDE4B in these diseases and its use as a therapeutic, diagnostic or experimental target. | 08-09-2012 |
20120208839 | NEW COMPOUNDS - This invention relates to compounds of formula I | 08-16-2012 |
20120208840 | Condensed Ring Pyridine Compounds As Subtype-Selective Modulators Of Sphingosine-1-Phosphate-2 (S1P2) Receptors - The invention provides compounds represented by the formula I, each of which compounds may have sphingosine-1-phosphate receptor agonist and or antagonist biological activity, wherein these compounds selected from the group consisting of wherein A, B, C, D, X, Y, Z and R | 08-16-2012 |
20120220623 | THE ENANTIOMER OF TENATOPRAZOLE AND THE USE THEREOF IN THERAPY - This invention relates to optically active substances of tenatoprazole, (+) and (−)-5-methoxy-2-{(4-methoxy-3,5-dimethyl-2-pyridyl)methyl]sulfinyl}-1H-imidazo[4,5-b]pyridine. The compound and pharmaceutical compositions thereof are useful for anti-ulcer agent. | 08-30-2012 |
20120220624 | PYRAZOLO [3,4-B] PYRIDIN-4-ONE KINASE INHIBITORS - The present invention is directed to novel kinase inhibitors of general formula (I) and pharmaceutically acceptable salts thereof, and to the use of the kinase inhibitors of general formula (I) for treating diseases or disorders in which tau phosphorylation and cell cycle regulation is implicated, such as Alzheimer's Disease and cancer. | 08-30-2012 |
20120225904 | New 7-Phenyl-[1,2,4]triazolo[4,3-a]Pyridin-3(2H)-One Derivatives - This disclosure is directed to, inter alis, new inhibitors of the p38 mitogen-activated protein kinase having the general formula (I), to processes for their preparation, to pharmaceutical compositions comprising them, and to their use in therapy. | 09-06-2012 |
20120252838 | TETRAHYDROTRIAZOLOPYRIDINE COMPOUNDS AS SELECTIVE MGLU5 RECEPTOR POTENTIATORS USEFUL FOR THE TREATMENT OF SCHIZOPHRENIA - The present invention provides certain tetrahydrotriazolopyridine derivatives, pharmaceutical compositions thereof, methods of using the same and processes for preparing the same. Formula (I) wherein R | 10-04-2012 |
20120283288 | 1-(5-TERT-BUTYL-2-PHENYL-2H-PYRAZOL-3-YL)-3-[2-FLUORO-4-(1-METHYL-2-OXO-2,- 3-DIHYDRO-1H-IMIDAZO[4,5-B]PYRIDIN-7-YLOXY)-PHENYL]-UREA AND RELATED COMPOUNDS AND THEIR USE IN THERAPY - The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain compounds of the following formula (I) (for convenience, collectively referred to herein as “IP compounds”), which, inter alia, are useful in the treatment of cancer, e.g., cancer characterised by (e.g., driven by) mutant RAS (“mutant RAS cancer”). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions in the treatment of cancer, e.g., mutant RAS cancer. | 11-08-2012 |
20120302598 | IMIDAZOPYRIDINONES - The invention relates to imidazopyridinones, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. | 11-29-2012 |
20120302599 | KAT ll INHIBITORS - Compounds of Formula I: | 11-29-2012 |
20120309784 | TRIAZOLOPYRIDINE KINASE INHIBITORS USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES - A novel [1,2,4]triazolo[1,5-a]pyridine compound is disclosed that has a formula represented by the following: | 12-06-2012 |
20120316197 | USE OF EP4 RECEPTOR ANTAGONISTS IN THE TREATMENT OF IL-23 MEDIATED DISEASES - This invention relates to a compound with EP4 antagonistic activity, or a pharmaceutically acceptable salt with EP4 receptor antagonistic activities, which is useful in the treatment of immune disease or allergy. This invention also relates to a compound of formula (I), (II), (III), (IV), (Va) or (Vb), or a pharmaceutically acceptable salt thereof with EP4 receptor antagonistic activities, which is useful in the treatment of immune disease or allergy. This invention also relates to a pharmaceutical composition for the treatment of immune disease or allergy which comprises a therapeutically effective amount of a compound of formula (I), (II), (III), (IV), (Va) or (Vb), or a pharmaceutically acceptable salt thereof. Further this invention relates to a method for the treatment of immune disease or allergy in an animal subject including a mammalian subject, which comprises administering to the animal subject including a mammalian subject a compound of the formula (I), (II), (III), (IV), (Va) or (Vb), or a pharmaceutically acceptable salt thereof. | 12-13-2012 |
20120322821 | GHRELIN RECEPTOR AGONIST FOR TREATMENT OF CACHEXIA - The present invention relates to use of a compound of the present invention or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising the compound or the salt, for the manufacture of a medicament for the treatment of cachexia. The invention also relates to a method for the treatment of cachexia, comprising administering the compound of the present invention or a pharmaceutical composition comprising the same to a human or an animal. The invention further relates to use of said compound, or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising the compound or the salt, in combination with one or more second active agents. Moreover, the invention relates to a pharmaceutical composition and a kit comprising the compound of the present invention or a pharmaceutically acceptable salt thereof, for the treatment of said disease. | 12-20-2012 |
20130085156 | NOVEL 2-PYRIDINECARBOXAMIDE DERIVATIVES - The present invention relates to a compound which has a glucokinase-activating effect and is useful as a therapeutic agent for diabetes mellitus, being represented by a formula (I): | 04-04-2013 |
20130096155 | TRIAZOLOPYRIDINE COMPOUND, AND ACTION THEREOF AS PROLYL HYDROXYLASE INHIBITOR OR ERYTHROPOIETIN PRODUCTION-INDUCING AGENT - The present invention provides a triazolopyridine compound having a prolyl hydroxylase inhibitory action and an erythropoietin production-inducing ability. The present invention relates to a compound represented by the following formula [I]: | 04-18-2013 |
20130102629 | ANALOGUES FOR THE TREATMENT OR PREVENTION OF FLAVIVIRUS INFECTIONS - Compounds represented by formula (I) | 04-25-2013 |
20130123296 | LONIDAMINE ANALOGUES FOR FERTILITY MANAGEMENT - Fertility management can include: administering to the subject one or more doses of a compound according to Formula I so as to reduce fertility in the subject. Fertility management can also include administering an effective amount of the compound to: impair Sertoli cell function in a male subject; inhibit spermatogenesis in the subject; reduce testis weight in the subject; reduce ovary weight in a female subject; reduce serum progesterone in the female subject; impair ovarian follicle function in the female subject; causing reversible fertility in the subject. In order to return fertility, the method can include ceasing administration of the compound to the subject so as to return fertility in the subject. The compound can be administered for irreversibly sterilizing the subject. | 05-16-2013 |
20130123297 | PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING OSTEOPOROSIS OR OBESITY COMPRISING PHENYLTETRAZOLE DERIVATIVE - A pharmaceutical composition comprising a phenyltetrazole derivative of formula (I) or a pharmaceutical acceptable salt thereof is effective in preventing or treating osteoporosis, obesity, diabetes, or hyperlipidemia, by regulating protein TAZ. | 05-16-2013 |
20130131103 | Methods and Compositions For Improved Nerve Conduction Velocity - The present invention provides methods and compositions for the effective treatment of impaired nerve signal conduction. Compositions including selective AT | 05-23-2013 |
20130143914 | UREA DERIVATIVES AND THEIR THERAPEUTIC USE IN THE TREATMENT OF, INTER ALIA, DISEASES OF THE RESPIRATORY TRACT - Compounds of formula (I) are p38 MAPK inhibitors, useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory wherein R | 06-06-2013 |
20130143915 | TRIAZOLOPYRIDINES AS TYK2 INHIBITORS - The present invention relates to compounds of Formula (I), wherein R | 06-06-2013 |
20130165478 | PYRAZOLOPYRIDINONE DERIVATIVES AS LPA RECEPTOR ANTAGONISTS - The present invention relates to novel pyrazolopyridinone derivatives according to formula (I) and a process of manufacturing thereof. These pyrazolopyridinone derivatives can be used as LPA receptor antagonists for the treatment of various herein disclosed diseases. | 06-27-2013 |
20130178497 | FUSED TRIAZOLES FOR THE TREATMENT OR PROPHYLAXIS OF MILD COGNITIVE IMPAIRMENT - The present invention provides a heterocycle derivative having a superior amyloid β production inhibitory activity and/or a superior γ-secretase modulation activity, and use thereof. A compound represented by the formula (I): wherein each symbol is as defined in the present specification, or a salt thereof. | 07-11-2013 |
20130190350 | 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. | 07-25-2013 |
20130203803 | Azaindazole Amide Compounds As CCR1 Receptor Antagonists - Disclosed are CCR1 inhibitor compounds of the formula (I): which are useful in the treatment of autoimmune and other diseases. Also disclosed a pharmaceutical compositions containing the same, and methods of making and using same. | 08-08-2013 |
20130217722 | NOVEL COMPOUND USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES - A novel imidazolopyridine according to Formula I, able to inhibit JAK as disclosed, this compound may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, allergic or inflammatory conditions, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons. | 08-22-2013 |
20130217723 | Pharmaceutical Composition Combining Tenatoprazole and an Anti-Inflammatory Agent - The invention relates to a novel pharmaceutical combination. The inventive pharmaceutical composition comprises a combination of tenatoprazole and one or more anti-inflammatory agents selected from non-steroid anti-inflammatory agents and cyclooxygenase-2 inhibitors. The invention is suitable for the treatment of painful and inflammatory manifestations. | 08-22-2013 |
20130225636 | N-(5S,6S,9R)-5-AMINO-6-(2,3-DIFLUOROPHENYL)-6,7,8,9-TETRAHYDRO-5H-CYCLOHEP- TA[B]PYRIDIN-9-YL-4-(2-OXO-2,3-DIHYDRO-1H-IMIDAZO[4,5-B]PYRIDIN-1-YL)PIPER- IDINE-1-CARBOXYLATE SALT - Disclosed is a hemisulfate salt of Compound (I): | 08-29-2013 |
20130261151 | AZABENZIMIDAZOLES AS RESPIRATORY SYNCYTIAL VIRUS ANTIVIRAL AGENTS - A compound satisfying formula I, a prodrug, N-oxide, addition salt, quaternary amine, metal complex, or a stereochemically isomeric form thereof; | 10-03-2013 |
20130267555 | INDOLES AS RESPIRATORY SYNCYTIAL VIRUS ANTIVIRAL AGENTS - Indoles having inhibitory activity on RSV replication and having the formula I | 10-10-2013 |
20130267556 | AZAINDOLES AS RESPIRATORY SYNCYTIAL VIRUS ANTIVIRAL AGENTS - Azaindoles having inhibitory activity on RSV replication and having the formula I | 10-10-2013 |
20130296361 | Condensed Ring Pyridine Compounds As Subtype-Selective Modulators Of Sphingosine-1-Phosphate-2 (S1P2) Receptors - The invention provides compounds represented by the formula I, each of which compounds may have sphingosine-1-phosphate receptor agonist and or antagonist biological activity, wherein these compounds selected from the group consisting of | 11-07-2013 |
20130296362 | PYRAZOLO PYRIDINE DERIVATIVES AS NADPH OXIDASE INHIBITORS - The present invention is related to pyrazolo pyridine derivatives of Formula (I), pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase). | 11-07-2013 |
20130310418 | Azaindazoles useful as inhibitors of kinases - The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions. | 11-21-2013 |
20130338185 | 1,2,4-TRIAZOLO[4,3-a]PYRIDINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS - The present invention relates to novel triazolo[4,3-a]pyridine derivatives of Formula (I) | 12-19-2013 |
20140005221 | RING-FUSED COMPOUND | 01-02-2014 |
20140039004 | METHOD OF TREATING OF GASTROESOPHAGEAL REFLUX DISEASE - The development of agents for gastroesophageal reflux disease, in which existing treatment is not effective, is strongly demanded. An object of the present invention is to provide an agent for preventing or relapse-preventing, treating or ameliorating such gastroesophageal reflux disease. 4-[({6-[Isobutyl(1,3-thiazol-2-ylsulfonyl)amino]-2,3-dihydro-1H-inden-5-yl}oxy)methyl]-3-methyl benzoic acid, a salt thereof or a prodrug thereof is effective in the prevention or relapse prevention, treatment or amelioration of gastroesophageal reflux disease. | 02-06-2014 |
20140057937 | ANTAGONISTS OF CHEMOKINE RECEPTORS - Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists. | 02-27-2014 |
20140057938 | KAT ll INHIBITORS - Compounds of Formula I: | 02-27-2014 |
20140080862 | ARYLOAZOL-2-YL CYANOETHYLAMINO COMPOUNDS, METHOD OF MAKING AND METHOD OF USING THEREOF - The present invention relates to novel aryloazol-2-yl-cyanoethylamino derivatives of formula (I): | 03-20-2014 |
20140088138 | CRYSTALLINE FORMS OF FUSED AMINO PYRIDINES AS HSP90 INHIBITORS - This invention relates to the discovery of novel forms of Compound 1, including solvates, hydrates, and other crystalline forms. These novel forms of Compound 1 may impart advantages in pharmaceutical formulations incorporating them, including improved stability and bioavailability. | 03-27-2014 |
20140088139 | COMPOSITIONS AND METHODS OF USE OF AN INAPPETANCE-CONTROLLING COMPOUND - The invention provides for a method of treating inappetance-induced weight loss in one or more companion animals or livestock. The method provides for administering a therapeutically effective amount of a capromorelin-containing composition to the companion animal or livestock. Optionally, one or more flavoring agents or flavor-masking agents can be added to the capromorelin-containing composition to enhance or mask the flavoring of the composition for the companion animal or livestock. | 03-27-2014 |
20140100245 | Antiviral Drugs for Treatment of Arenvirus Infection - Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by the | 04-10-2014 |
20140107150 | New Compounds II - The present invention relates to compounds of formula (I), | 04-17-2014 |
20140107151 | TYROSINE KINASE INHIBITORS - The present disclosure provides compounds and pharmaceutically acceptable salts that are tyrosine kinase inhibitors, in particular BLK, BMX, EGFR, HER2, HER4, ITK, JAK3, TEC, BTK, and TXK and are therefore useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as cancer and inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and pharmaceutically acceptable salts and processes for preparing such compounds and pharmaceutically acceptable salts. | 04-17-2014 |
20140113932 | CRYSTAL OF FUSED HETEROCYCLIC COMPOUND - The present invention relates to a crystal of 1-ethyl-7-methyl-3-{4-[(3-methyl-3H-imidazo[4,5-b]pyridin-2-yl)oxy]phenyl}-1,3-dihydro-2H-imidazo[4,5-b]pyridin-2-one useful as a prophylactic or therapeutic agent for schizophrenia and the like, which shows an X-ray powder diffraction pattern having characteristic peaks at interplaner spacings (d) of 13.59 plus or minus 0.2 and 6.76 plus or minus 0.2 Angstroms in powder X-ray diffraction. | 04-24-2014 |
20140206717 | USE OF INORGANIC MATRIX AND ORGANIC POLYMER COMBINATIONS FOR PREPARING STABLE AMORPHOUS DISPERSIONS - The present invention relates to methods for processing pharmaceutically active substances having poor water solubility in the presence of an inorganic matrix, e.g., magnesium aluminometasilicate, and a secondary polymer as a means of converting the crystalline API to substantially amorphous and stable form, i.e., the crystallinity is less than 5%. The methods of the invention result in more complete amorphization, increased solubility, drug loading and stability as compared to typical amorphization or literature methods. | 07-24-2014 |
20140243366 | COMPOUNDS THAT MODULATE INTRACELLULAR CALCIUM - Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity. | 08-28-2014 |
20140243367 | ANTIVIRAL DRUGS FOR TREATMENT OF ARENAVIRUS INFECTION - Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by the Arenavirus family such as Lassa fever, Argentine hemorrhagic fever, Bolivian hemorrhagic fever, and Venezuelan hemorrhagic fever. | 08-28-2014 |
20140329852 | N-(IMIDAZOLIDIN-2-YLIDENE)QUINOLINE DERIVATIVES AS MODULATORS OF ALPHA 2 ADRENERGIC RECEPTORS - The present invention relates to novel N-(imidazolidin-2-ylidene)quinoline derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals. | 11-06-2014 |
20140329853 | [1,2,4]TRIAZOLOPYRIDINES AND THEIR USE AS PHOSPHODIESTERASE INHIBITORS - The present invention relates to novel [1,2,4]triazolopyridine compounds with phosphodiesterase inhibitory activity, as well as to their use as therapeutic agents in the treatment of inflammatory diseases and conditions. | 11-06-2014 |
20140350046 | PYRAZOLOPYRIDINONE DERIVATIVES AS LPA RECEPTOR ANTAGONISTS - The present invention relates to novel pyrazolopyridinone derivatives according to formula (I) and a process of manufacturing thereof. These pyrazolopyridinone derivatives can be used as LPA receptor antagonists for the treatment of various herein disclosed diseases. | 11-27-2014 |
20140357663 | 1-(5-TERT-BUTYL-2-PHENYL-2H-PYRAZOL-3-YL)-3-[2-FLUORO-4-(1-METHYL-2-OXO-2,- 3-DIHYDRO-1H-IMIDAZO[4,5-B]PYRIDIN-7-YLOXY)-PHENYL]-UREAAND RELATED COMPOUNDS AND THEIR USE IN THERAPY - The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain compounds of the following formula (for convenience, collectively referred to herein as “IP compounds”), which, inter alia, are useful in the treatment of cancer, e.g., cancer characterised by (e.g., driven by) mutant RAS (“mutant RAS cancer”). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions in the treatment of cancer, e.g., mutant RAS cancer. | 12-04-2014 |
20140364450 | AMINOPYRIDINES USEFUL AS INHIBITORS OF PROTEIN KINASES - The present invention relates to compounds useful as inhibitors of 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. | 12-11-2014 |
20140371263 | COMPOUNDS AND METHODS FOR THE TREATMENT OF CYSTIC FIBROSIS - The invention relates to a compound of Formula I and methods of treating CFTR (cystic fibrosis transmembrane conductance regulator) mediated diseases, in particular cystic fibrosis, comprising the step of administering a therapeutically effective amount of a compound of Formula I or IA to a patient in need thereof: | 12-18-2014 |
20150018385 | FUSED AMINO PYRIDINES FOR THE TREATMENT OF BRAIN TUMORS - The present invention relates to the use of compounds with fused amino pyridine core for the treatment of malignancies associated with brain and lung. The oral administration of compounds of the instant application results in effective brain penetration and provides for non-intrusive treatment of brain and lung tumors. | 01-15-2015 |
20150018386 | AMORPHOUS FORM OF APIXABAN, PROCESS OF PREPARATION AND COMPOSITIONS THEREOF - The present invention discloses an amorphous form of apixaban, process of preparation and compositions thereof. | 01-15-2015 |
20150057309 | NOVEL 3,5-DISUBSTITUTED-3H-IMIDAZO[4,5-B]PYRIDINE AND 3,5- DISUBSTITUTED -3H-[1,2,3]TRIAZOLO[4,5-B] PYRIDINE COMPOUNDS AS MODULATORS OF C-MET PROTEIN, ETC - The present invention provides compounds useful as c-Met protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of c-Met kinase mediated disease or disorders with them. | 02-26-2015 |
20150073012 | AZABENZIMIDAZOLES AS RESPIRATORY SYNCYTIAL VIRUS ANTIVIRAL AGENTS - A compound satisfying formula I, a prodrug, N-oxide, addition salt, quaternary amine, metal complex, or a stereochemically isomeric form thereof; | 03-12-2015 |
20150073013 | INDOLES AS RESPIRATORY SYNCYTIAL VIRUS ANTIVIRAL AGENTS - Indoles having inhibitory activity on RSV replication and having the formula I | 03-12-2015 |
20150105420 | [1,2,4]TRIAZOLOPYRIDINES AND THEIR USE AS PHOSPHODIESTERASE INHIBITORS - The present invention relates to novel [1,2,4]triazolopyridine compounds with phosphodiesterase inhibitory activity, as well as to their use as therapeutic agents in the treatment of inflammatory diseases and conditions. | 04-16-2015 |
20150111920 | SELECTIVE EP4 RECEPTOR ANTAGONISTIC SUBSTANCE FOR TREATMENT OF CANCER - This invention provides a medicament for the treatment of cancer, which cause a reduction of cancer. This invention relates to use of a compound which has inhibitory activities against prostaglandin E2 receptor (EP4 receptor) and is represented by the following general formula (I), (II), (III), or (IV), or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising the compound or the salt for the manufacture of a medicament for the treatment of cancer. The invention relates to a method for treatment of cancer comprising administering the compound or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising the compound or the salt to humans or animals. The compound or a pharmaceutically acceptable salt thereof, or the pharmaceutical composition may be used in combination with one or more second active agents. | 04-23-2015 |
20150133490 | INHIBITOR OF JAK1 AND JAK2 - The present invention provides an amino pyrazole compound, which is 3-[(1R)-6-fluoro-2,3-dihydro-1H-inden-1-yl]-N-(3-methyl-1H-pyrazol-5-yl)-3H-imidazo[4,5-b]pyridin-5-amine, or a pharmaceutically acceptable salt thereof, that inhibits JAK1 and JAK2 and, therefore may be useful in treating cancer. | 05-14-2015 |
20150141455 | COMPLEMENT PATHWAY MODULATORS AND USES THEREOF - The present invention provides a compound of formula I: (I) a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition. | 05-21-2015 |
20150148373 | HETEROCYCLIC GUANIDINE F1F0-ATPASE INHIBITORS AND THERAPEUTIC USES THEREOF - The invention provides heterocyclic guanidine compounds that inhibit F | 05-28-2015 |
20150148374 | COMPLEMENT PATHWAY MODULATORS AND USES THEREOF - The present invention provides a compound of formula I: a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition. | 05-28-2015 |
20150148375 | BICYCLIC HETEROCYCLES AS BET PROTEIN INHIBITORS - The present invention relates to bicyclic heterocycles which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer. | 05-28-2015 |
20150297566 | RORgammaT INHIBITORS - The present invention relates to compounds according to Formula I | 10-22-2015 |
20150299191 | COMPOUNDS AND METHODS FOR INHIBITING FASCIN - Provided are compounds, compositions and methods for inhibiting fascin activity or treating a condition or disorder mediated by fascin activity in a subject in need thereof. | 10-22-2015 |
20150299195 | SALTS AND POLYMORPHS OF A SUBSTITUTED IMIDAZOPYRIDINYL-AMINOPYRIDINE COMPOUND - The present application relates to salts of Compound A, 3-(3-(4-(1-aminocyclobutyl) phenyl)-5-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amine, solid state forms of Compound A free base or of salts of Compound A, amorphous forms of Compound A free base or of salts of Compound A, crystalline forms of Compound A free base or of salts of Compound A, polymorphs of Compound A free base or of salts of Compound A, and mesomorphs of Compound A free base or of salts of Compound A. The present application also relates to pharmaceutical compositions comprising these salts, solid state forms, amorphous forms, crystalline forms, polymorphs, or mesomorphs of Compound A free base or of salts of Compound A. The present application provides methods for preparing these salts, solid state forms, amorphous forms, crystalline forms, polymorphs, or mesomorphs of Compound A free base or of salts of Compound A. | 10-22-2015 |
20160015693 | METHODS AND COMPOUNDS FOR PREVENTING AND TREATING A TUMOUR - The invention relates to a method of preventing, inhibiting, arresting or reversing tumourigenesis in a cell as well as a method of inducing apoptosis in a tumour cell. The method includes increasing the amount and/or the activity of a DACT protein, or a functional fragment thereof, in the cell. Also provided is a pharmaceutical composition that comprises a compound of general formula (I) | 01-21-2016 |
20160024079 | Complement Factor B inhibitors and uses there of - The present invention provides a compound of formula (I): wherein X is N or CH, Y is NH, O or S, methods for manufacturing these compounds, and their uses as Factor B inhibitors for the treatment of conditions and diseases associated with complement alternative pathway activation such as age-related macular degeneration, diabetic retinopathy and related ophthalmic diseases. The present invention further provides pharmaceutical compositions and combinations of pharmacologically active agents. | 01-28-2016 |
20160030405 | 1-(5-TERT-BUTYL-2-PHENYL-2H-PYRAZOL-3-YL)-3-[2-FLUORO-4-(1-METHYL-2-OXO-2,- 3-DIHYDRO-1H-IMIDAZO[4,5-B]PYRIDIN-7-YLOXY)-PHENYL]-UREA AND RELATED COMPOUNDS AND THEIR USE IN THERAPY - The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain compounds of the following formula (for convenience, collectively referred to herein as “IP compounds”), which, inter alia, are useful in the treatment of cancer, e.g., cancer characterised by (e.g., driven by) mutant RAS (“mutant RAS cancer”). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions in the treatment of cancer, e.g., mutant RAS cancer. | 02-04-2016 |
20160039817 | TRIAZOLOPYRIDYL COMPOUNDS AS ALDOSTERONE SYNTHASE INHIBITORS - This invention relates to triazolopyridyl compounds of the structural formula: | 02-11-2016 |
20160060264 | UREA DERIVATIVES AND USES THEREOF - The present invention provides novel compounds of any one of Formulae (I)-(III), and pharmaceutical compositions thereof. Also provided are particles (e.g., nanoparticles) comprising compounds of Formula (I)-(III) and pharmaceutical compositions thereof that are mucus penetrating. The invention also provides methods and kits for using the inventive compounds, and pharmaceutical compositions thereof, for treating and/or preventing diseases associated with abnormal or pathological angiogenesis and/or aberrant signaling of a growth factor (e.g., vascular endothelial growth factor (VEGF)), such as proliferative diseases (e.g., cancers, benign neoplasms, inflammatory diseases, autoimmune diseases) and ocular diseases (e.g., macular degeneration, glaucoma, diabetic retinopathy, retinoblastoma, edema, uveitis, dry eye, blepharitis, and post-surgical inflammation) in a subject in need thereof. | 03-03-2016 |
20160083381 | POLYMORPH FORMS - The present invention relates to novel crystal forms of 2-amino-N-[2-(3a-(R)-benzyl-2-methyl-3-oxo-2,3,3a,4,6,7-hexahydro-pyrazolo[4,3-c]pyridin-5-yl)-1-(R)-benzyloxymethyl-2-oxo-ethyl]-isobutyramide L-tartrate. More particularly, the invention relates to polymorph forms, and to processes for the preparation of compositions containing and to uses of such polymorph forms. | 03-24-2016 |
20160095843 | PYRAZOLOPYRROLIDINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF DISEASE - The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition. | 04-07-2016 |
20160108037 | HETEROCYCLIC AMIDE COMPOUND - The present invention provides a heterocyclic amide compound of Formula (1), and an agricultural chemical containing it, particularly a herbicide: | 04-21-2016 |
20160113912 | AN IMPROVED PROCESS FOR THE PREPARATION OF APIXABAN AND INTERMEDIATES THEREOF - The present invention relates to an improved process for the preparation of apixaban and intermediates thereof. In particular, the invention relates to an improved process for the preparation of an amorphous form of apixaban. The invention also relates to a pharmaceutical composition comprising an amorphous form of apixaban for oral administration as an antithrombotic agent. | 04-28-2016 |
20160114044 | COMPOSITON BASED ON BIOCOMPATIBLE ANIONIC POLYMER FOR DRUG DELIVERY AND PREPARING METHOD THEREOF - A composition for drug delivery based on a biocompatible anionic polymer and a producing method thereof are provided. | 04-28-2016 |
20160120854 | PHARMACEUTICAL COMPOSITIONS - The present invention relates to pharmaceutical compositions of substituted triazolopyridine compounds of general formula (I) as described and defined herein, to methods of preparing said compositions, and to the use of the compositions for the treatment or prophylaxis of a disease. | 05-05-2016 |
20160128991 | INDAZOLE INHIBITORS OF THE WNT SIGNAL PATHWAY AND THERAPEUTIC USES THEREOF - Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases due to mutations in Wnt signaling components. Also provided are methods for treating Wnt-related disease states. | 05-12-2016 |
20160143894 | PROCESS FOR THE PREPARATION OF APIXABAN - A crystalline Form N-1 of apixaban substantially free from one or more of: 1-(4-methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxylic acid; 7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-1-phenyl-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide; or methyl 1-(4-methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxylate, relative to apixaban by area percentage of HPLC and having a mean particle size equal to or greater than 100 μm. | 05-26-2016 |
20160145254 | TRIAZOLOPYRIDINE COMPOUND, AND ACTION THEREOF AS PROLYL HYDROXYLASE INHIBITOR OR ERYTHROPOIETIN PRODUCTION-INDUCING AGENT - The present invention provides a triazolopyridine compound having a prolyl hydroxylase inhibitory action and an erythropoietin production-inducing ability. The present invention relates to a compound represented by the following formula [I]: | 05-26-2016 |
20160194318 | 1,2,4-TRIAZOLO[4,3-a]PYRIDINE COMPOUNDS AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS | 07-07-2016 |
20160250191 | SEPARASE INHIBITORS AND USES THEREOF | 09-01-2016 |
20160251377 | AZAINDOLES AS RESPIRATORY SYNCYTIAL VIRUS ANTIVIRAL AGENTS | 09-01-2016 |
20170231967 | Bach1 Inhibitors in Combination with Nrf2 Activators and Pharmaceutical Compositions Thereof | 08-17-2017 |
20180021312 | BENZOISOXAZOLE-SUBSTITUTED COMPOUNDS AS MGLUR4 ALLOSTERIC POTENTIATORS, COMPOSITIONS, AND METHODS OF TREATING NEUROLOGICAL DYSFUNCTION | 01-25-2018 |
20190144396 | 9-MEMBERED FUSED RING DERIVATIVE | 05-16-2019 |