Entries |
Document | Title | Date |
20080200494 | Imidazopyridine Derivatives - The invention provides imidazopyridine derivatives represented by the general formula [I] [in which R | 08-21-2008 |
20080200495 | Pyrrolopyridine Compounds, Method of Making Them and Uses Thereof - Pyrrolopyridine compounds corresponding to formula (I): | 08-21-2008 |
20080200496 | SUBSTITUTED 1H-PYRROLO[3,2-b, 3,2-c, and 2,3-c]PYRIDINE-2-CARBOXAMIDES AND RELATED ANALOGS AS INHIBITORS OF CASEIN KINASE Ie - The present invention discloses and claims compounds of formula (I) | 08-21-2008 |
20080207677 | Napthyridine Compounds As Rock Inhibitors - The present invention relates to compounds having a naphthyridine scaffold, and stereoisomeric forms, prodrugs, solvates, hydrates and/or pharmaceutically acceptable salts of these compounds as well as pharmaceutical compositions containing at least one of these naphthyridine derivatives together with pharmaceutically acceptable carrier, excipient and/or diluents. Said naphthyridine compounds have been identified as inhibitors of the protein kinase ROCK2, also known as Rho-kinase, and are useful for the treatment of cancers (tumor growth and metastases), erectile dysfunction, cardiovascular diseases, hypertension, angina pectoris, cerebral ischaemia, cerebral vasospasm, myocardial ischaemia, coronary vasospasm, heart failure, myocardial hypertrophy, atherosclerosis, restenosis, spinal cord injuries, neuronal degeneration, thrombotic disorders, asthma, glaucoma, inflammation, anti-viral diseases (e.g. HIV), and osteoporosis. | 08-28-2008 |
20080207678 | VIRAL INHIBITORS - Pyrrolo[2,3-c]pyridine or pyrrolo[3,2-c]pyridine compounds having the general formula (A), | 08-28-2008 |
20080207679 | Glutathione peroxidase mimetics for the treatment of dermatoses - This invention relates to compositions and methods for the treatment of dermatological conditions with a glutathione peroxidase mimetic. | 08-28-2008 |
20080207680 | 7-Azaindoles, their use as inhibitors of phosphodiesterase 4, and a method for synthesizing them - 7-azaindoles inhibit phosphodiesterase 4 (PDE4). Methods for preparing these compounds and methods of treating arthritis and other conditions with the compounds are also provided. | 08-28-2008 |
20080214598 | Novel Piperidine Carboxylic Acid Amide Derivatives - The invention relates to novel piperidine carboxylic acid amide derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of these novel compounds, pharmaceutical compositions comprising such compounds and especially the use of such compounds as inhibitors of renin. | 09-04-2008 |
20080221148 | 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. | 09-11-2008 |
20080221149 | Novel 2-Heteroaryl Substituted Benzothiophenes and Benzofuranes 709 - The present invention relates to novel 2-heteroaryl substituted benzothiophene and benzofuran derivatives, precursors thereof, and therapeutic uses of such compounds, having the structural formula (Ia) below: | 09-11-2008 |
20080221150 | Prevention of Neurodegeneration by Macrolide Antibiotics - The present disclosure describes the use of macrolide antibiotics to prevent neurodegeneration and to treat or prevent disease and conditions which involve neurodegeneration. While not being limited to a specific mechanism of action, in one embodiment, the macrolide antibiotics inhibit neurodegeneration caused by lysosomal and/or mitochondrial dysfunction. The present disclosure contemplates the use of any macrolide antibiotic and pharmaceutically acceptable derivatives thereof. In a specific embodiment, the macrolide antibiotics include bafilomycin A1, bafilomycin B1 and concanamycin. | 09-11-2008 |
20080221151 | 3-AMINO-2-PHENYLPYRROLIDINE DERIVATIVES - 3-amino-2-phenylpyrrolidine compounds useful as NK-1 antagonists, with pharmaceutical compositions and methods of treatment comprising same, are disclosed. | 09-11-2008 |
20080221152 | 4-(HETEROARYL-METHYL AND SUBSTITUTED HETEROARYL-METHYL)-IMIDAZOLE-2-THIONES ACTING AS ALPHA2 ADRENERGIC AGONISTS - Compounds of Formula 1 | 09-11-2008 |
20080227806 | Novel Drugs for Dementia - The invention is directed to compounds that are prodrugs containing a chemical delivery system (CDS) moiety and a cysteine protease inhibitor moiety. The CDS moiety targets the prodrug to the brain or central nervous system. The cysteine protease inhibitor inhibits cysteine proteases upon release from the prodrug. Cysteine protease inhibitors are effective for treating dementia, Alzheimer's disease and vascular dementia. Targeting the brain or central nervous system offers significant advantages in treating these conditions and diseases. A preferred CDS prodrug is a dihydrotrigoneline CDS moiety coupled to an epoxysuccinyl peptide cysteine protease inhibitor moiety. | 09-18-2008 |
20080227807 | 5-LIPOXYGENASE-ACTIVATING PROTEIN (FLAP) INHIBITORS - Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of 5-lipoxygenase-activating protein (FLAP). Also described herein are methods of using such FLAP modulators, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other leukotriene-dependent or leukotriene mediated conditions or diseases. | 09-18-2008 |
20080234313 | NOVEL INHIBITORS - Compounds of formula (I), combinations and uses thereof for disease therapy, | 09-25-2008 |
20080242694 | Amino-substituted heterocycles, compositions thereof, and methods of treatment therewith - Provided herein are Heterocyclic Compounds having the following structure: | 10-02-2008 |
20080249126 | 1,3-SUBSTITUTED CYCLOALKYL DERIVATIVES HAVING ACIDIC, MOSTLY HETEROCYCLIC GROUPS, PROCESSES FOR THEIR PREPARATION AND THEIR USE AS PHARMACEUTICALS - The invention relates to 1,3-substituted cycloalkyl derivatives having acidic, mostly heterocyclic groups and to their physiologically acceptable salts and physiologically functional derivatives. | 10-09-2008 |
20080255182 | Certain chemical entities, compositions, and methods - Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of one or more mitotic kinesins are disclosed. | 10-16-2008 |
20080255183 | N-[HETEROARYLCARBONYL]-3-THIENYL-L-ALANINE DERIVATIVES AS a5beta1 ANTAGONISTS - The present invention relates to compounds that inhibit of a5b1 function, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment in warm-blooded animals such as humans of diseases that have a significant angiogenesis or vascular component such as for treatment of solid tumours. The present invention also relates to a5b1 antagonists that also exhibit appropriate selectivity profile(s) against other integrins. | 10-16-2008 |
20080262025 | Processes for the Preparation of Zolpidem and its Hemitartrate - The invention relates to the preparation of a non-hygroscopic polymorphic form of zolpidem hemitartrate, designated as Form I, and pharmaceutical compositions including it. The invention also relates to use of the compositions for treating anxiety, sleep disorders and convulsions. The invention also relates to a process for the preparation of zolpidem or pharmaceutically acceptable salts thereof by condensing 3-bromo-N,N-dimethyl-4-oxo-4-p-tolyl-butyramide with 2-amino-5-methylpyridine in a polar aprotic solvent. | 10-23-2008 |
20080262026 | Therapeutic Agents 684 - Certain 4,5,6,7-tetrahydropyrrolo[3,2-c]pyridin-4-one and 4,5-dihydropyrrolo[3,2-c]pyridin-4-one compounds of formula I, processes for preparing such compounds, their use in the treatment of obesity, psychiatric and neurological disorders, methods for their therapeutic use and pharmaceutical compositions containing them are described. | 10-23-2008 |
20080262027 | Novel Chemical Compounds - This invention relates to newly identified compounds for inhibiting YAK3 proteins and methods for treating diseases associated with the imbalance or inappropriate activity of YAK3 proteins. | 10-23-2008 |
20080269277 | Pyrrolopyridine-2-Carboxylic Acid Hydrazides - Compounds of Formula (I) or pharmaceutically acceptable salts thereof, are inhibitors of glycogen phosphorylase and are useful in the prophylactic or therapeutic treatment of diabetes, hyperglycemia, hypercholesterolemia, hyperinsulinemia, hyperlipidemia, hypertension, atherosclerosis or tissue ischemia e.g. myocardial ischemia, or as cardioprotectants or inhibitors of abnormal cell growth. | 10-30-2008 |
20080280946 | Azaindole-Derivatives As Factor Xa Inhibitors - Indazole-derivatives as factor Xa inhibitors The present invention relates to compounds of the formula I | 11-13-2008 |
20080280947 | ANTI-INSOMNIA COMPOSITIONS AND METHODS - Compositions of zolpidem, and methods for their manufacture and use for treating insomnia. The compositions are formulated as oral sprays for transmucosal absorption of zolpidem. The methods of treatment in some cases involve night-time dosing administration to achieve therapeutic zolpidem blood levels within 20 minutes or less, tapering off to less than 20 ng/ml within less than five hours, in some cases less than four hours, post dosing. | 11-13-2008 |
20080293760 | Gemifloxacin Process and Polymorphs - The present invention provides a novel process for the preparation of gemifloxacin and its pharmaceutically acceptable acid addition salts in high yield. The present invention also relates to novel polymorphs of gemifloxacin free base and its hydrates to the processes for their preparation and to pharmaceutical compositions comprising them. The present invention also relates to infusion solutions of gemifloxacin and to processes for their preparation. Thus, 7-chloro-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid is reacted with a mixture of acetic anhydride, acetic acid and boric acid to give borane compound, which is then treated with 4-Aminomethyl-3-methoxyimino-pyrrolidinium dimethanesulfonate in presence of triethylamine, followed by treatment with 3.5% sodium hydroxide solution to give gemifloxacin free base. | 11-27-2008 |
20080293761 | Pyrrolopyridine-2-Carboxylic Acid Amide Derivative Useful as Inhibitor of Glycogen Phosphorylase - The present invention is directed to a novel form of a pyrrolopyridine-2-carboxylic acid amide of formula (I), which is an inhibitor of glycogen phosphorylase, compositions containing it and their use in therapy. The invention is also directed to processes for production of the novel form, novel intermediates used in said processes and processes for the production of said intermediates. | 11-27-2008 |
20080306105 | DEUTERIUM-ENRICHED MOXIFLOXACIN - The present application describes deuterium-enriched moxifloxacin, pharmaceutically acceptable salt forms thereof, and methods of treating using the same. | 12-11-2008 |
20080306106 | 1-HETEROCYCLYLALKYL-3-SULFONYLAZAINDOLE OR -AZAINDAZOLE DERIVATIVES AS 5-HYDROXYTRYPTAMINE-6 LIGANDS - The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor. | 12-11-2008 |
20080312269 | Therapeutic Agents - The present invention relates to 4,5,6,7-tetrahydropyrrolo[3,2-c]pyridin-4-one and 4,5-dihydropyrrolo[3,2-c]pyridin-4-one compounds of formula (I) and processes for preparing such compounds, their use in the treatment of obesity, psychiatric and neurological disorders, to methods for their therapeutic use and to pharmaceutical compositions containing them. | 12-18-2008 |
20080312270 | COMPOUNDS AND METHODS USEFUL FOR TREATING ASTHMA AND ALLERGIC INFLAMMATION - Compounds, compositions and methods that are useful in the treatment of inflammatory and immune-related diseases and conditions are provided herein. In particular, the invention provides compounds which modulate the function and/or expression of proteins involved in atopic diseases, inflammatory conditions and cancer. The subject compounds are carboxylic acid derivatives. | 12-18-2008 |
20090005409 | Pyrrolo[3,2-C] Pyrdine Derivatives and Processes for the Preparation Thereof - The present invention provides novel pyrrolo[3,2-c]pyridine derivatives or pharmaceutically acceptable salts thereof, processes for the preparation thereof, and compositions comprising the same. The pyrrolo[3,2-c]pyridine derivatives or pharmaceutically acceptable salts thereof of the present invention have excellent proton pump inhibition effects and possess the ability to attain a reversible proton pump inhibitory effect. | 01-01-2009 |
20090005410 | N-(2-(HETARYL)ARYL) ARYLSULFONAMIDES AND N-(2-(HETARYL) HETARYL ARYLSULFONAMIDES - Compounds are provided that act as potent antagonists of the CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists. | 01-01-2009 |
20090005411 | Combinations of Organic Compounds - The invention provides a pharmaceutical combination comprising:
| 01-01-2009 |
20090018156 | Pyrrolo [2,3,B] Pyridine Derivatives Useful As RAF Kinase Inhibitors - The present invention provides pyrrolo pyridine compounds, compositions containing the same, as well as processes for the preparation and their use as pharmaceutical agents. | 01-15-2009 |
20090023769 | Organic Compounds - Compounds of formula I | 01-22-2009 |
20090023770 | Novel 1,2,3-Substituted Indolizine Derivatives, Inhibitors of FGFs, Method for Preparing Them and Pharmaceutical Compositions Containing Them - The present invention relates to novel 1,2,3-substituted indolizine derivative which are inhibitors of fibroblast growth factors, to methods or preparing such derivatives, to pharmaceutical compositions comprising such derivatives, and to methods of treatment comprising such derivatives. | 01-22-2009 |
20090036481 | Novel Azaindole Inhibitors of Mtp and Apob - The present invention relates to 7-azaindole-based compounds, to processes for the preparation thereof, to pharmaceutical compositions comprising them, and to the use thereof in the preparation of medicaments that are useful as inhibitors of MTP and of ApoB secretion. | 02-05-2009 |
20090042927 | Salts, Prodrugs and Polymorphs of Fab I Inhibitors - In part, the present invention is directed to antibacterial compounds and salts thereof. | 02-12-2009 |
20090042928 | Modulators of muscarinic receptors - The modulator compounds described herein modulate muscarinic receptors and are useful for treating muscarinic receptor mediated diseases. | 02-12-2009 |
20090048285 | Pyrrolopyridines Useful in the Treatment of Inflammation - There is provided compounds of formula (I), wherein X | 02-19-2009 |
20090054477 | 4-thio substituted quinoline and naphthyridine compounds - The present invention relates to 4-thio substituted quinoline and naphthyridine derivatives and processes for their preparation. The invention also related to methods for treating infection of Hepatitis C virus by administering a 4-thio substituted quinoline or naphthyridine derivative. | 02-26-2009 |
20090054478 | AZOLOPYRIDIN-3-ONE DERIVATIVES AS INHIBITORS OF LIPASES AND PHOSPHOLIPASES - The present invention relates to azolopyridin-3-one derivatives of the general formula I with the meanings indicated in the description, their pharmaceutically usable salts and their use as medicinal substances. | 02-26-2009 |
20090069368 | FGF-RECEPTOR AGONIST DIMERIC COMPOUNDS - FGF receptor agonist compounds corresponding to the general formula: M1-L-M2 are disclosed in which M1 and M2, which may be identical or different, each represent, independently of one another, a monomer unit M, and L represents a linker group, wherein the monomer unit is of the general formula I. | 03-12-2009 |
20090076065 | DEUTERIUM-ENRICHED MK-0812 - The present application describes deuterium-enriched MK-0812, pharmaceutically acceptable salt forms thereof, and methods of treating using the same. | 03-19-2009 |
20090076066 | DEUTERIUM-ENRICHED ZOLPIDEM - The present application describes deuterium-enriched zolpidem, pharmaceutically acceptable salt forms thereof, and methods of treating using the same. | 03-19-2009 |
20090082390 | PIPERIDINE COMPOUNDS FOR USE AS OREXIN RECEPTOR ANTAGONIST - This invention relates to N-aroyl cyclic amine derivatives and their use as pharmaceuticals, specifically as orexin receptor antagonists. | 03-26-2009 |
20090093515 | Substituted pyrroline kinase inhibitors - The present invention is directed to novel substituted pyrroline compounds useful as kinase or dual-kinase inhibitors and methods for treating or ameliorating a kinase or dual-kinase mediated disorder. | 04-09-2009 |
20090105297 | Compounds Modulating C-Kit Activity - Compounds with 7-azaindole core structure with activity toward the receptor protein tyrosine kinase c-kit, compositions useful for treatment c-kit-mediate diseases or conditions, and methods of use thereof, are provided. Further provided are methods of c-kit ligand identification and design. | 04-23-2009 |
20090111847 | PREPARATION METHOD AND USE OF COMPOUNDS HAVING HIGH INSECTICIDAL ACTIVITIES - The present invention discloses a kind of nitromethylene derivatives as well as their preparation method and their uses. The insecticidal activity tests show that the nitromethylene derivatives of the present invention not only show high insecticidal activities against insects with piercing-sucking type or scratching type mouthparts, such as aphid, leafhopper, plant hopper, thrips and white fly and their resistant strains, but also show high insecticidal activities against | 04-30-2009 |
20090118322 | Agent for repairing corneal sensitivity containing amide compound - The amide compound of the formula (I) [each symbol is as defined in the description] has a promoting action on neuritogenesis of trigeminal nerve cells, and the compound is useful as a corneal neuritogenesis promoter, an agent for recovering corneal sensitivity by promotion of corneal neuritogenesis, and an agent for treating dry eye. | 05-07-2009 |
20090143420 | 2-BENZOYLIMIDAZOPYRIDINE DERIVATIVES, PREPARATION AND THERAPEUTIC USE THEREOF - The present invention is related to a compound of formula (I) | 06-04-2009 |
20090143421 | USE OF 2-BENZOYL-IMIDAZOPYRIDINES IN THERAPEUTICS - The present invention is related to the use of a compound of formula (I): | 06-04-2009 |
20090149492 | 7,8-DIHYDRO-1,6-NAPHTHYRIDIN-5(6H)-ONES AND RELATED BICYCLIC COMPOUNDS AS INHIBITORS OF DIPEPTIDYL PEPTIDASE IV AND METHODS - The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I. Additionally, the present application provides pharmaceutical compositions containing at least one compound according to Formula I and optionally at least one additional therapeutic agent. Finally, the present application provides methods for treating a patient suffering from an DPP4 modulated disease or disorder such as, for example, diabetes, by administration of a therapeutically effective dose of a compound according to Formula I. | 06-11-2009 |
20090149493 | INHIBITORS OF THE INTERACTION BETWEEN MDM2 AND P53 - The present invention provides compounds of formula (I), their use as an inhibitor of a p53-MDM2 interaction as well as pharmaceutical compositions comprising said compounds of formula (I) wherein n, m, p, s, t, R | 06-11-2009 |
20090149494 | THERAPEUTIC USE OF IMIDAZO[1,2-a]PYRIDINE-2-CARBOXAMIDE DERIVATIVES - The present invention is related to the use of a compound of formula (I): | 06-11-2009 |
20090156631 | Controlled Release Compositions Containing Zolpidem - The present invention relates to controlled release compositions of Zolpidem or pharmaceutically acceptable salts thereof adapted to release Zolpidem over a predetermined time period, according to a monophasic and/or a biphasic profile of dissolution. The present invention also relates to monolithic matrix based formulations of Zolpidem or pharmaceutically acceptable salts thereof. | 06-18-2009 |
20090163535 | Substituted Heteroarylalkanoic Acids - Disclosed are substituted heteroarylalkanoic acids of the following formula D-A-C(O)R′, where D, A, and R′ are defined herein. These compounds are useful in the treatment of chronic complications arising from diabetes mellitus. Also disclosed are pharmaceutical compositions containing the compounds and methods of treatment employing the compounds, as well as methods for their synthesis. | 06-25-2009 |
20090170893 | NOVEL HYDRATE FORM - The present invention relates to a novel hydrate form of moxifloxacin monohydrochloride, processes for preparing the form, pharmaceutical compositions comprising the form and uses of the form and compositions. | 07-02-2009 |
20090176824 | 7- (4-substituted-3-cyclopropylaminomethyl-1-pyrrolidinyl) quinolonecarboxylic acid derivative technical field - Object To provide novel quinolonecarboxylic acid compounds serving as safe, strong antibacterial agents that are effective against drug-resistant bacteria that are less susceptible to conventional antibacterial agents.
| 07-09-2009 |
20090197909 | Bis-Heterocyclic Imidazolyl Compounds - The patent application relates to new heterocyclic compounds of the general formula (I) in which R, R | 08-06-2009 |
20090209573 | COMPOUNDS AND COMPOSITIONS AS HEDGEHOG PATHWAY MODULATORS - The invention provides a method for modulating the activity of the hedgehog signaling pathway. In particular, the invention provides a method for inhibiting aberrant growth states resulting from phenotypes such as Ptc loss-of-function, hedgehog gain-of-function, smoothened gain-of-function or Gli gain-of-function, comprising contacting a cell with a sufficient amount of a compound of Formula I. | 08-20-2009 |
20090209574 | FLUOROQUINOLONE DERIVATIVES FOR OPHTHALMIC APPLICATIONS - The present invention relates to fluoroquinolone derivatives having enhanced ocular penetration characteristics and/or antimicrobial activity, and to compositions comprising such derivatives. The derivatives and compositions are particularly well suited for treating ophthalmic bacterial infections. The present invention more particularly relates to the discovery that a 2-methyl substitution on a diazabicyclo group attached to a fluoroquinolone ring system produces improved permeability characteristics, and that a 5-amino substitution on a fluoroquinolone ring system results in improved anti-microbial activity. | 08-20-2009 |
20090209575 | Method for treating neuropathic pain and associated syndromes - The present invention is directed to the use of ibudilast for treating neuropathic pain. | 08-20-2009 |
20090215816 | Imidazo(1,2-a)Pyridine Derivatives Useful as Peptide Deformylase (PDF) Inhibitors - The present invention relates to compounds of formula (I). These compounds are a novel type of peptide deformylase (PDF) inhibitors, and are therefore of great interest especially as new antibiotics. | 08-27-2009 |
20090221629 | Method for antagonizing MIF activity - Methods of antagonizing MIF activity using ibudilast are described. Also described are methods of screening for MIF antagonists. These agents can be used for treating addictions, including drug and behavioral addictions, as well as for treating neuropathic pain. | 09-03-2009 |
20090239896 | AZAINDOLE COMPOUNDS AND USE THEREOF AS PHOSPHOLIPASE-A2 INHIBITORS - Indole and indole-related compounds, compositions and methods are disclosed. The compounds of the invention are useful as phospholipase inhibitors. The compounds and compositions of the invention are useful for treatment of phospholipase-related conditions, such as insulin-related, weight-related and/or cholesterol-related conditions in an animal subject. The compounds include azaindoles of the formula below [insert FIG. | 09-24-2009 |
20090239897 | NOVEL COMPOUNDS - Novel substituted 1,5,7-trisubstituted-1,8-napthyridin-2(1H)-one compounds; 1,5,7 trisubstituted-1,6-napthyridine-2-(1H)-one compounds and 1,5,7-trisubstituted quinoline-2(1H)-one compounds, processes for the preparation thereof, the use thereof in treating CSBP/p38 kinase mediated diseases and pharmaceutical compositions for use in such therapy. | 09-24-2009 |
20090239898 | FURTHER THERAPEUTIC USE OF ZOLPIDEM - An imidazo[1,2-a] pyridine-3-acetamide such as zolpidem is useful in the treatment of a condition of the brain which has a lesion and exhibits diaschisis/dormant cells at the contralateral and other sites, more particularly trauma-induced injury, spinocerebellar ataxia, cerebellar or cerebral infarct and Ramsey-Hunt syndrome. | 09-24-2009 |
20090253735 | 2-ARYL-6-PHENYLIMIDAZO[1,2-a]PYRIDINE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF - The present invention is related to a compound of formula (I) | 10-08-2009 |
20090253736 | AZAINDOLE DERIVATIVES AS CFTR MODULATORS - The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators. | 10-08-2009 |
20090264459 | Organic Compounds - Compounds of formula (I) in free or a pharmaceutically acceptable salt form, wherein X | 10-22-2009 |
20090270444 | 1,7-Naphthyridines - There are provided according to the invention novel compounds of formula (I) and pharmaceutically acceptable salts and solvates thereof, | 10-29-2009 |
20090286826 | PHARMACEUTICAL COMPOSITIONS HAVING CARBOXYVINYL POLYMER AND POVIDONE POLYMER - The present invention is directed to pharmaceutical compositions, such as ophthalmic gels. The compositions typically include a carboxyvinyl polymer. A povidone polymer is also typically included to stabilize the carboxyvinyl polymer against agents or ingredients (e.g., therapeutic agent) that can otherwise cause instability to the carboxyvinyl polymer. | 11-19-2009 |
20090291977 | Chromane Derivatives Useful As Acid Pump Antagonists - This invention relates to compounds of the formula (I): or a pharmaceutically acceptable salt thereof, wherein: R′, R | 11-26-2009 |
20090291978 | Enzyme Inhibitors - Compounds of formula (I) are inhibitors of histone deacetylase activity, and are useful in the treatment of, for example, cancers, wherein R | 11-26-2009 |
20090298865 | Derivatives of pyrrolopyridine-2-carboxamides, preparation thereof and therapeutic application thereof - The invention relates to compounds of formula (I): | 12-03-2009 |
20090306123 | Bicyclononene derivaties - The invention relates to novel bicyclononene derivatives of Formula (I); and the use thereof as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as inhibitors of renin. | 12-10-2009 |
20090306124 | 3-(INDOLYL)-4-ARYLMALEIMIDE DERIVATIVES AND THEIR USE AS ANGIOGENESIS INHIBITORS - The present invention relates to a compound of formula (I) wherein R | 12-10-2009 |
20090306125 | Mitochondria-Targeted Antioxidant Prodrugs and Methods of Use - The present invention is a mitochondria-targeted antioxidant prodrug useful for the prevention or treatment of diseases or conditions associated with mitochondrial dysfunction resulting from changes in the mitochondrial redox environment. Antioxidant prodrugs of the invention are produced by modifying an antioxidant to a fatty acid so that the resulting prodrug is targeted to and activated by an enzyme of mitochondrial fatty acid beta-oxidation. | 12-10-2009 |
20090306126 | Indole Derivatives - The invention concerns indole derivatives of Formula I | 12-10-2009 |
20090306127 | Certain Chemical Entities, Compositions and Methods - Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of one or more mitotic kinesins are disclosed. | 12-10-2009 |
20090306128 | PHARMACEUTICAL COMPOSITIONS CONTAINING A FLUOROQUINOLONE ANTIBIOTIC DRUG - Pharmaceutical compositions containing a fluoroquinolone antibiotic drug are disclosed. The compositions exhibit improved homogeneity, improved bioavailability, lower turbidity or a combination thereof. The composition can be use as otic or nasal compositions, but are particularly useful as ophthalmic compositions. | 12-10-2009 |
20090312365 | Certain Chemical Entities, Compositions, and Methods - Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of one or more mitotic kinesins are disclosed. | 12-17-2009 |
20090312366 | NOVEL P2X7R ANTAGONISTS AND THEIR USE - The present application is directed to novel P2X7R antagonists that are indol-3-carboxamide or azaindole-3-carboxamide compounds, pharmaceutical compositions comprising the same and their use for the prophylactic or therapeutic treatment of diseases mediated by P2X7R activity. | 12-17-2009 |
20090318492 | INDOLE COMPOUNDS HAVING C4-ACIDIC SUBSTITUENTS AND USE THEREOF AS PHOSPHOLIPASE-A2 INHIBITORS - Indole and indole-related compounds, compositions and methods are disclosed. The compounds of the invention are useful as phospholipase inhibitors. The compounds and compositions of the invention are useful for treatment of phospholipase-related conditions, such as insulin-related, weight-related and/or cholesterol-related conditions in an animal subject. | 12-24-2009 |
20090318493 | Aryl pyrrolidinyl and piperidinyl ketone derivatives and uses thereof - Aryl and heteroaryl ketone compounds substituted with pyrrolidines and piperidines, that modulate serotonin norepinephrine and/or dopamine neurotransmission. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds. | 12-24-2009 |
20100010035 | Novel Dual Action Receptors Antagonists (Dara) at the Ati and Eta Receptors - The present invention relates to new compounds of the formula [Chemical formula should be inserted here. Please see paper copy] wherein R1, R2, R3, and R31 are as specified herein. The invention also relates to a method for preparation thereof, as well as combinations of the new compounds with previously known agents. The invention also relates to the use of the above-mentioned compounds and combinations for the preparation of a medicament for treating hypertension of different kinds, alleviating organ damage of different kinds, treating or preventing diabetic nephropathy, treating endothelin and angiotensin mediated disorders, and treating prostate cancer. | 01-14-2010 |
20100010036 | DRUGS FOR THE TREATMENT OF SARCOGLYCANOPATHIES - Inhibitors of the endoplasmic reticulum associated degradation (ERAD) pathway, particularly inhibitors of mannosidase I, are used for the preparation of a medicinal product intended to treat sarcoglycanopathies. | 01-14-2010 |
20100010037 | 1H-PYRROLO[2,3-B]PYRIDINE DERIVATIVES USEFUL AS HSP90 INHIBITORS - Compounds of formula (I) have HSP90 inhibitory activity: | 01-14-2010 |
20100010038 | TRICYCLIC COMPOUND AND PHARMACEUTICAL USE THEREOF - The present invention provides a compound represented by the formula | 01-14-2010 |
20100022581 | PYRROLIDINE-SUBSTITUTED AZAINDOLE COMPOUNDS HAVING 5-HT6 RECEPTOR AFFINITY - The present disclosure provides compounds having affinity for the 5-HT | 01-28-2010 |
20100029708 | COMPOUNDS AND COMPOSITIONS FOR TREATMENT OF CANCER - Compounds and compositions for treating, preventing or managing cancer are disclosed. The compositions provided herein comprise SNS-595 and N-desmethyl-SNS-595. Also provided are pharmaceutical compositions comprising the compounds and methods of treatment using the compounds and compositions. | 02-04-2010 |
20100035917 | PYRROLO[2,3-B]PYRIDIN-4-YL-BENZENESULFONAMIDE COMPOUNDS AS 1KK2 INHIBITORS - The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds according to Formula (1) and salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular 1KK2 activity. | 02-11-2010 |
20100035918 | Imidazolone Compounds and Methods of Making and Using the Same - In one aspect, the invention features a compound of the general Formula (I). Compounds of Formula (I) possess high affinity for Alk 5 and/or AIk 4, and can be useful as antagonists thereof for preventing and/or treating numerous diseases, including fibrotic disorders. | 02-11-2010 |
20100035919 | COMPOUNDS USEFUL AS INHIBITORS OF PROTEIN KINASES - Disclosed herein are compounds of formula (I) or pharmaceutical acceptable salts thereof, | 02-11-2010 |
20100035920 | SUBSTITUTED PYRAZOLO[1,5-a] PYRIDINE COMPOUNDS AND THEIR METHODS OF USE - The present invention is directed to substituted pyrazolo[1,5-a]pyridines and related methods for their synthesis and use. | 02-11-2010 |
20100041693 | INDOLYLMALEIMIDE DERIVATIVES - A compound of formula (I) | 02-18-2010 |
20100041694 | AGRICULTURAL COMPOSITION FOR CONTROLLING OR PREVENTING PLANT DISEASES CAUSED BY PLANT PATHOGENIC MICROBES - An agricultural composition comprising an amide compound represented by the following formula (I), | 02-18-2010 |
20100048609 | PHARMACEUTICAL DOSAGE FORMS FOR (+)-1,4-DIHYDRO-7-[(3S,4S)-3-METHOXY-4-(METHYLAMINO)-1-PYRROLIDINYL]-4-OX- O-1-(2-THIAZOLYL)-1,8-NAPHTHYRIDINE-3-CARBOXYLIC ACID - Provided herein are light protective pharmaceutical packages for enantiomerically pme (+)-1,4-dihydro-7-[(3S,4S)-3-methoxy-4-(methylamino)-1-pyrrolidinyl]-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acid. In certain embodiments, the pharmaceutical packages comprise a glass vial containing SNS-595 drug product within a secondary container. | 02-25-2010 |
20100056563 | NOVEL 1.8-NAPHTHYRIDINE COMPOUNDS - The present invention relates to naphthyridine compounds useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions. | 03-04-2010 |
20100063087 | 5-Amino-4-Hydroxy-7-(Imidazo [1,2-A] Pyridin-6-Ylmethyl)-8-Methyl-Nonamide Derivatives and Related Compounds as Renin Inhibitors for the Treatment of Hypertension - Compounds of the general formula (I) or its salt or a compound in which one or more atoms are replaced by their stable, nonradio-active isotopes, in particular its pharmaceutically acceptable salt; in which X is —CH | 03-11-2010 |
20100069430 | PYRROLO[2,3-C]PYRIDINE DERIVATIVES AND PROCESSES FOR THE PREPARATION THEREOF - The present invention provides novel pyrrolo[2,3-c]pyridine derivatives or pharmaceutically acceptable salts thereof, processes for the preparation thereof, and compositions comprising the same. The pyrrolo[2,3-c]pyridine derivatives or pharmaceutically acceptable salts thereof of the present invention have excellent proton pump inhibition effects and possess the ability to attain a reversible proton pump inhibitory effect. | 03-18-2010 |
20100076013 | Methods of Treatment - The present invention relates to methods of treating hematological malignancies, including acute myeloid leukemia (AML), comprising the use of compounds that inhibit the binding of the Smac protein to IAPs (“IAP inhibitor”). The present invention also relates to the use of IAP inhibitors for the preparation of a medicament to treat hematological malignancies, including AML. | 03-25-2010 |
20100081683 | NICOTINIC ACETYLCHOLINE RECEPTOR SUB-TYPE SELECTIVE AMIDES OF DIAZABICYCLOALKANES - Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are amide compounds which can be prepared from certain heteoraryl carboxylic acids and certain diazabicycloalkanes. The compounds exhibit selectivity for, and bind with high affinity to, neuronal nicotinic receptors of the a4β2 subtype in the central nervous system (CNS). The compounds and compositions can be used to treat and/or prevent a wide variety of conditions or disorders, particularly CNS disorders. The compounds can: (i) alter the number of nicotinic cholinergic receptors of the brain of the patient, (ii) exhibit neuroprotective effects, and (iii) when employed in effective amounts, not result in appreciable adverse side effects (e.g. side effects such as significant increases in blood pressure and heart rate, significant negative effects upon the gastrointestinal tract, and significant effects upon skeletal muscle). | 04-01-2010 |
20100093784 | NOVEL HETEROCYCLIC NITROGENOUS COMPOUNDS, THEIR PREPARATION AND THEIR USE AS ANTIBACTERIAL MEDICAMENTS - The invention relates to nitrogenous heterocyclic compounds of formula | 04-15-2010 |
20100105720 | PREPARATION AND UTILITY OF SUBSTITUTED IMIDAZOPYRIDINE COMPOUNDS WITH HYPNOTIC EFFECTS - The present disclosure is directed to modulators of GABA | 04-29-2010 |
20100105721 | IMIDAZO[1,2-a]PYRIDINE DERIVATIVES: PREPARATION AND PHARMACEUTICAL APPLICATIONS - The present invention relates to hydroxamate compounds which are inhibitors of histone deacetylase. More particularly, the present invention relates to imidazo[1,2-a]pyridine containing compounds and methods for their preparation. These compounds may be useful as medicaments for the treatment of proliferative disorders as well as other diseases involving, relating to or associated with enzymes having histone deacetylase activities (HDAC). | 04-29-2010 |
20100113505 | AMINO-NAPHTHYRIDINE DERIVATIVES - The present invention relates to new compounds having an amino-naphthyridine group. In particular, the present invention relates to new compounds, its stereoisomers and pharmaceutically acceptable salts or solvates thereof having a first unit (moiety) selected from the group of a phenyl derivative, a biphenyl derivative or a diphenyl alkane derivative and at least one amino-naphthyridine group linked with the first unit via a linking group. In specific embodiments, the present invention relates to compounds having a phenyl derivative unit and three amino-naphthyridine groups bound to the phenyl derivative unit via a linking group as well as salts or solvates thereof, in particular, pharmaceutically acceptable salts or solvates thereof. Further, the present invention relates to pharmaceutical compositions comprising said compounds. The compounds are particularly useful for treating or preventing infections, like viral infections. | 05-06-2010 |
20100120838 | COMPOUNDS FOR THE TREATMENT OF INFLAMMATORY DISORDERS - This invention relates to compounds of the Formula (I): | 05-13-2010 |
20100125086 | USE OF ISOQC INHIBITORS - The present invention relates in general to an inhibitor of a glutaminyl peptide cyclotransferase-like protein (QPCTL), and the use thereof for the treatment and/or prevention of an inflammatory disease or disorder selected from the group consisting of (a) chronic and acute inflammations, e.g. rheumatoid arthritis, atherosclerosis, restenosis, pancreatitis; (b) other inflammatory diseases, e.g. neuropathic pain, graft rejection/graft failure/graft vasculopathy, HIV infections/AIDS, gestosis, tuberous sclerosis, Guillain-Barré syndrome, chronic inflammatory demyelinising polyradiculoneuropathy and multiple sclerosis; (c) neuroinflammation; and (d) neurodegenerative diseases, e.g. mild cognitive impairment (MCI), Alzheimer's disease, neurodegeneration in Down Syndrome, Familial British Dementia, and Familial Danish Dementia, which may result from neuroinflammation. | 05-20-2010 |
20100125087 | NEW COMPOUNDS 575 - The present invention relates to novel compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of Aβ-related pathologies such as Downs syndrome, β-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer Disease, memory loss, attention deficit symptoms associated with Alzheimer disease, neurodegeneration associated with diseases such as Alzheimer disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration. | 05-20-2010 |
20100130538 | BICYCLIC COMPOUND AND PHARMACEUTICAL USE THEREOF - The present invention provides a compound represented by the formula | 05-27-2010 |
20100130539 | IMIDAZOPYRIDINE INHIBITORS OF IAP - The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein Q, X | 05-27-2010 |
20100130540 | AZAQUINOLINONE DERIVATIVES AND USES THEREOF - The present invention provides compounds and methods for treating or preventing the development of a disease, disorder, or condition in a subject or patient. | 05-27-2010 |
20100137355 | NITROGENOUS HETEROCYCLIC COMPOUNDS, PREPARATION THEREOF AND USE THEREOF AS ANTIBACTERIAL MEDICAMENTS - The invention concerns nitrogenated heterocyclic compounds, their preparation and use as antibacterial drugs, compounds of general formula (I) | 06-03-2010 |
20100137356 | AZAINDOLE-INDOLE COUPLED DERIVATIVES, PREPARATION METHODS AND USES THEREOF - A novel class of azaindole-indole coupled derivatives, their preparation methods, pharmaceutical compositions containing the same and the uses thereof. The common structural feature of these derivatives is that they are coupled by azaindole and indole bi-molecule at different positions, forming extended pi-conjugated systems. Such derivatives inhibited cell growth and proliferation by various mechanisms. The present compounds have improved solubility, increased bioavailability, and thus have enhanced drug actions, and reduced medical dosages and undesired responses. | 06-03-2010 |
20100144781 | METHODS OF TREATING PSYCHOSIS AND SCHIZOPHRENIA BASED ON POLYMORPHISMS IN THE ERBB4 GENE - The present application is directed to the use of genetic polymorphism in the ErbB4 gene to predict whether a patient is likely to respond to psychotic medication Paliperidone. The polymorphism in the ErbB4 gene is also used to predict whether a patient is likely to display placebo effect among patients in need of psychotic treatment. A method of treating patients with antipsychotic medication Paliperidone using the polymorphism in the ErbB4 gene and a kit of are also provided. | 06-10-2010 |
20100144782 | DERIVATIVES OF 7-ALKYNYL-1,8-NAPHTHYRIDONES, PREPARATION METHOD THEREOF AND USE OF SAME IN THERAPEUTICS - The disclosure relates to compounds of formula (I): | 06-10-2010 |
20100152229 | Process for the Synthesis of Moxifloxacin Hydrochloride - A new polymorph of moxifloxacin hydrochloride is described, together with a method for making the polymorph. In addition, new intermediates in the formation of moxifloxacin hydrochloride are described, having formulas (1) and (II): | 06-17-2010 |
20100160369 | S1P1 Agonists and Methods of Making And Using - The invention is directed to Compounds of Formula I: | 06-24-2010 |
20100168155 | DERIVATIVES OF IMIDAZO[1,2-a]PYRIDINE-2-CARBOXAMIDES, PREPARATION METHOD THEREOF AND USE OF SAME IN THERAPEUTICS - The present invention is related to a compound of formula (I): | 07-01-2010 |
20100173930 | Certain Chemical Entities, Compositions and Methods - Provided are certain chemical entities, and methods of use to modulate diskeletal 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, muscle spasm, neuromuscular disease, and other indications. | 07-08-2010 |
20100173931 | HARMINE DERIVATIVES FOR REDUCING BODY WEIGHT - The present invention provides a method of reducing body weight in a subject in need thereof, by administering to the subject a therapeutically effective amount of a compound of Formula I. The present invention also provides methods for the treatment of obesity and disorders related to obesity and higher than recommended percentage body fat, such as type II diabetes. | 07-08-2010 |
20100173932 | SUB-TYPE SELECTIVE AMIDES OF DIAZABICYCLOALKANES - Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are amide compounds which can be prepared from certain heteroaryl carboxylic acids and certain diazabicycloalkanes. The compounds exhibit selectivity for, and bind with high affinity to, neuronal nicotinic receptors of the α4β2 subtype in the central nervous system (CNS). The compounds and compositions can be used to treat and/or prevent a wide variety of conditions or disorders, particularly CNS disorders. The compounds can: (i) alter the number of nicotinic cholinergic receptors of the brain of the patient, (ii) exhibit neuroprotective effects, and (iii) when employed in effective amounts, not result in appreciable adverse side effects (e.g. side effects such as significant increases in blood pressure and heart rate, significant negative effects upon the gastrointestinal tract, and significant effects upon skeletal muscle). | 07-08-2010 |
20100184800 | Compounds for the Treatment of Hepatitis C - The disclosure provides compounds of formula I, II, III, IV, and V, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV. | 07-22-2010 |
20100190819 | alpha-7 Nicotinic Acetylcholine Receptor Allosteric Modulators, Their Derivatives and Uses Thereof - The present application is related to compounds represented by Formula I, which are novel allosteric modulators of α7nAChR. The application also discloses the treatment of disorders that are responsive to modulation of acetylcholine action on α7nAChR in a mammal by administering an effective amount of a compound of Formula I. | 07-29-2010 |
20100197723 | BICYCLIC COMPOUNDS AND METHODS OF MAKING AND USING SAME - Disclosed herein are compounds that may be modulators of 5-HT receptors, and methods of making and using same. | 08-05-2010 |
20100197724 | 6.5 -PYRROLOPIPERIDINE TACHYKININ RECEPTOR ANTAGONISTS - The present invention is directed to certain hydroxymethyl ether hydroisoindoline compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. 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 emesis, urinary incontinence, LUTS, depression, and anxiety. | 08-05-2010 |
20100204265 | Certain Nitrogen Containing Bicyclic Chemical Entities for Treating Viral Infections - Provided are certain chemical entities, pharmaceutical compositions, and methods of treatment of a member of the flaviviradae family of viruses such as hepacivirus (Hepatitis C or HCV). | 08-12-2010 |
20100204266 | COMPOSITIONS FOR USE IN IDENTIFICATION OF MIXED POPULATIONS OF BIOAGENTS - The present invention provides oligonucleotide primers, compositions, and kits containing the same for rapid identification of bacterial bioagents and populations of bioagents which are members of the | 08-12-2010 |
20100227880 | CHEMICAL COMPOUNDS - The present invention provides compounds of formula (I): | 09-09-2010 |
20100227881 | 1,7-NAPHTHYRIDINE DERIVATIVES AS P38 MAP KINASE INHIBITORS - New inhibitors of the p38 mitogen-activated protein kinase having the general formula (I) are disclosed, as well as processes for their preparation, pharmaceutical compositions comprising them, and their use in therapy. | 09-09-2010 |
20100234417 | THYROTROPIN RELEASING HORMONE RECEPTOR-OREXIN RECEPTOR HETERO-DIMERS/-OLIGOMERS - A hetero-dimeric or hetero-oligomeric receptor, comprising at least one thyrotropin releasing hormone receptor subunit associated with at least one orexin receptor subunit. | 09-16-2010 |
20100234418 | COMPOUNDS AND USES THEREOF - N-[3-(4-Cyano-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluoro-phenyl]-4-trifluoromethyl-benzenesulfonamide, N-[3-(4-ethynyl-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluoro-phenyl]-4-trifluoromethyl-benzenesulfonamide, and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof are active on at least one Raf protein kinase. Also described are methods of use thereof to treat diseases and conditions, including diseases and conditions associated with activity of Raf protein kinases, including pain and polycystic kidney disease. | 09-16-2010 |
20100240694 | SALT OF NAPHTHYRIDINE CARBOXYLIC ACID DERIVATIVE - 7-(3-Aminomethyl-4-methoxyiminopyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid methanesulfonate and hydrates thereof, processes for their preparation, pharmaceutical compositions comprising them, and their use in antibacterial therapy. | 09-23-2010 |
20100240695 | STABILIZED ZOLPIDEM PHARMACEUTICAL COMPOSITIONS - Pharmaceutical compositions for buccal delivery of zolpidem comprising an effective amount of zolpidem and a carbonate and bicarbonate buffer system in an amount sufficient to raise the pH of saliva to at least 8.5, and wherein the carbonate forms a coating on the bicarbonate wherein the amount of carbonate coating is at least 30% (w/w) of the total buffer amount are described. Pharmaceutical compositions for buccal delivery of zolpidem comprising an effective amount of zolpidem and a binary buffer system of carbonate and bicarbonate, wherein the carbonate and bicarbonate are co-located in a single particle, wherein the bicarbonate is coated with the carbonate, and wherein the amount of carbonate coating is at least 30% (w/w) of the binary buffer system are also described. | 09-23-2010 |
20100249175 | Dicationic compounds which selectively recognize G-quadruplex DNA - Dicationic compounds that are highly selective for binding G-quadruplex DNA are described. Several compounds exhibit groove binding toward G-quadruplex DNA and in vitro and in vivo activity versus | 09-30-2010 |
20100249176 | HETEROCYCLE AMIDE T-TYPE CALCIUM CHANNEL ANTAGONISTS - The present invention is directed to heterocycle amide compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved. | 09-30-2010 |
20100249177 | COMPOSITIONS AND METHODS FOR TREATING MIDDLE-OF-THE-NIGHT INSOMNIA - The present invention provides compositions for treating middle-of-the-night insomnia without residual sedative effects upon awakening by administering low doses (about 5 mg or less) of zolpidem or a salt thereof. | 09-30-2010 |
20100249178 | COMPOSITIONS AND METHODS FOR TREATING MIDDLE-OF-THE-NIGHT INSOMNIA - The present invention provides compositions having a therapeutically effective amount of zolpidem, carbonate buffer, bicarbonate buffer, and a mixture comprising large and fine particles of silicon dioxide. Compositions having a therapeutically effective amount of zolpidem, carbonate buffer, bicarbonate buffer, and sodium stearyl fumarate are also described. | 09-30-2010 |
20100261750 | Modulators of Cystic Fibrosis Transmembrane Conductance Regulator - The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators. | 10-14-2010 |
20100261751 | METHOD FOR DETERMINING ONE OF THE TWO HUMAN IMMUNODEFICIENCY VIRUS (HIV) INTEGRASE ENZYMATIC ACTIVITIES - The invention concerns a method for determining one of the two Human Immunodeficiency Virus (HIV) integrase enzymatic activities, in particular 3′-end processing, in an in vitro assay. | 10-14-2010 |
20100267761 | 7-Azaindole Derivatives as Selective 11-Beta-Hydroxysteroid Dehydrogenase Type 1 Inhibitors - The present invention relates to 7-azaindole derivatives of formula I as selective inhibitors of the enzyme 11-beta-hydroxysteroid dehydrogenase type 1 (11β-HSD-1) and the use of such compounds for the treatment and prevention of metabolic syndrome, diabetes, insulin resistance, obesity, lipid disorders, glaucoma, osteoporosis, cognitive disorders, anxiety, depression, immune disorders, hypertension and other diseases and conditions. | 10-21-2010 |
20100267762 | NOVEL P2X7R ANTAGONISTS AND THEIR USE - The present application is directed to novel P2X7R antagonists that are N-indol-3-yl-acetamide and N-azaindol-3-yl-acetamide compounds, pharmaceutical compositions comprising the same and their use for the prophylactic or therapeutic treatment of diseases mediated by P2X7R activity. | 10-21-2010 |
20100267763 | Method of Decreasing Pro-ADAM10 Secretase and/or Beta Secretase Levels - The present invention provides a method of decreasing the level of pro-ADAM10 and/or BACE protein in a subject, the method comprising administering a heterocyclic compound or a pharmaceutically acceptable salt, hydrate or prodrug thereof to a subject in need thereof. | 10-21-2010 |
20100280063 | 8-ANILINOIMIDAZOPYRIDINES AND THEIR USE AS ANTI-CANCER AND/OR ANTI-INFLAMMATORY AGENTS - The invention relates to imidazopyridines of formula I with anti-cancer and/or anti-inflammatory activity and more specifically to imidazopyridines which inhibit MEK kinase activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth or treating a hyperproliferative disorder, or treating an inflammatory disease in a mammal. The invention also relates to methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions. | 11-04-2010 |
20100286189 | (AZA)INDOLE DERIVATIVE SUBSTITUTED IN POSITION 5, PHARMACEUTICAL COMPOSITION COMPRISING IT, INTERMEDIATE COMPOUNDS AND PREPARATION PROCESS THEREFOR - An (aza)indole derivative substituted in position 5, of formula (I) in which X, Y, Z, G1, G2, G3, R1, W, and R2 have the meanings given in the description, a pharmaceutical composition comprising it, and also intermediate compounds and a preparation process therefor. | 11-11-2010 |
20100286190 | CERTAIN SUBSTITUTED UREAS, AS MODULATORS OF KINASE ACTIVITY - Certain chemical entities chosen from compounds of Formula 1 and pharmaceutically acceptable salts, solvates, chelates, non-covalent complexes, and prodrugs thereof, are provided herein. Pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicles chosen from carriers, adjuvants, and excipients, are also provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to angiogenic kinase modulation, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include cancer, including breast neoplasia, endometrial cancer, colon cancer, and neck squamous cell carcinoma. Methods of treatment include administering at least one chemical entity as a single active agent or administering such at least one chemical entity in combination with one or more other therapeutic agents. A method for determining the presence or absence of an angiogenic kinase in a sample comprising contacting the sample with at least one chemical entity under conditions that permit detection of activity of the angiogenic kinase, detecting a level of the activity of the angiogenic kinase, and therefrom determining the presence or absence of the angiogenic kinase in the sample. | 11-11-2010 |
20100317685 | N-PHENYL-IMIDAZO[1,2-a]PYRIDINE-2-CARBOXAMIDE DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION - Compounds of formula (I): | 12-16-2010 |
20100317686 | N-HETEROCYCLIC-6-HETEROCYCLIC-IMIDAZO[1,2-a]PYRIDINE-2-CARBOXAMIDE DERIVATIVES, PREPARATION AND THERAPEUTIC USE THEREOF - Compounds of formula (I): | 12-16-2010 |
20100317687 | 2-BENZOYLIMIDAZO[1,2-a]PYRIDINE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF - Compounds of formula (I) | 12-16-2010 |
20100317688 | 2-HETEROAROYLIMIDAZOL[1,2-a]PYRIDINE DERIVATIVES, PREPARATION AND THERAPEUTIC USE THEREOF - Compounds of formula (I): | 12-16-2010 |
20100324081 | PREVENTIVE, INHIBITOR OR REMEDY FOR CEREBRAL ANEURYSM COMPRISING IBUDILAST AS AN ACTIVE INGREDIENT - Herein provided is an agent for the prevention of cerebral aneurysm, for the control of the formation thereof or for the treatment thereof, which comprises Ibudilast as an effective component. | 12-23-2010 |
20100324082 | ENANTIOMERIC COMPOSITIONS OF 2-AMINO-1-(2-ISOPROPYLPYRAZOLO[1,5-a]PYRIDIN-3-YL)PROPAN-1-ONE AND RELATED METHODS - Enantiomerically pure (S)-2-amino-1-(2-isopropylpyrazolo[1,5-a]pyridin-3-yl)propan-1-one, (S)-AV1013, is a candidate therapeutic for treating neuroathic pain, addiction behavior and drug withdrawal symptoms. Also described are methods for preparing and using (S)-AV1013, its pharmaceutically acceptable salts as well as pharmaceutically acceptable formulations of the same. | 12-23-2010 |
20100324083 | Combinations of Organic Compounds - The invention provides a pharmaceutical combination comprising:
| 12-23-2010 |
20110003845 | SUBSTITUTED AZABICYCLIC COMPOUNDS AND THE USE THEREOF - The present application relates to novel substituted pyrrolopyridine, pyrazolopyridine and isoxazolopyridine derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, preferably for the treatment and/or prevention of cardiovascular disorders. | 01-06-2011 |
20110021556 | PYRROLIDINYL DERIVATIVES AND USES THEREOF - The invention relates to 3,3 disubstituted pyrrole derivatives useful for treatment of diseases associated with monoamine reuptake inhibitors. Also provided pharmaceutical compositions, methods of using, and methods of preparing the compounds. | 01-27-2011 |
20110028510 | Compositions, Methods, and Kits for Treating Influenza Viral Infections - The present invention provides compositions, methods, and kits for treating or preventing a viral infection (e.g., an infection caused by an influenza virus). | 02-03-2011 |
20110028511 | PROCESS FOR THE MANUFACTURE OF PHARMACEUTICALLY ACTIVE COMPOUNDS - According to the present invention there are provided novel processes for the manufacture of the compound of formula 1 | 02-03-2011 |
20110028512 | BIS-HETEROCYCLIC IMIDAZOLYL COMPOUNDS - Heterocyclic compounds of the general formula (I) are provided in which R, R | 02-03-2011 |
20110028513 | METHOD FOR TREATING NEUROLOGICAL DISORDERS WITH IMIDAZOLIUM AND IMIDAZOLINIUM COMPOUNDS - There is presently provided methods for delivering a neuroprotective agent to a neural cell. The methods comprise contacting a neural cell with an imidazolium or imidazolinium compound as described herein, including an imidazolium or imidazolinium salt. | 02-03-2011 |
20110039878 | METHODS FOR REDUCING BLOOD PRESSURE - The present invention provides methods and medicaments for reducing blood pressure. Methods and medicaments for treating or preventing hypertension are also provided. | 02-17-2011 |
20110039879 | METHODS FOR INCREASING WHITE BLOOD CELLS - The present invention relates to methods and compounds useful for increasing white blood cell levels in blood and bone marrow. Methods and compounds for increasing hematopoietic progenitor cells are also provided. | 02-17-2011 |
20110039880 | ARYL SUBSTITUTED SULFONAMIDE COMPOUNDS AND THEIR USE AS ANTICANCER AGENTS - Aryl substituted sulfonamide compounds of formula (I): | 02-17-2011 |
20110039881 | COMPOSITIONS AND METHODS FOR TREATING MIDDLE-OF-THE-NIGHT INSOMNIA - The present invention provides compositions and methods for treating middle-of-the-night insomnia without residual sedative effects upon awakening by dosing an amount of zolpidem or a salt thereof to a subject who awakens from sleep and desires to resume sleep for less than 5 hours. The step of dosing is performed after the subject awakens from sleep and the amount permits the subject to awaken at a time about four hours after dosing without residual sedative effects. | 02-17-2011 |
20110039882 | PHOSPHODIESTERASE 10A INHIBITOR - A phosphodiesterase 10A inhibitor serving as an effective prophylactic or therapeutic agent for Parkinson's disease, Huntington's disease, Alzheimer's disease, and schizophrenia. | 02-17-2011 |
20110065745 | POLYSUBSTITUTED 2-ARYL-6-PHENYLIMIDAZO[1,2-A]PYRIDINE DERIVATIVES, AND PREPARATION AND THERAPEUTIC USE THEREOF - Compounds of formula (I): | 03-17-2011 |
20110082169 | Stable SNS-595 Compositions and Methods of Preparation - Methods of preparing substantially pure SNS-595 substance are disclosed. Also provided are compositions comprising SNS-595 substance that are substantially pure and essentially free of visible particles. | 04-07-2011 |
20110086876 | STABLE SNS-595 COMPOSITIONS AND METHODS OF PREPARATION - Methods of preparing substantially pure SNS-595 substance are disclosed. Also provided are compositions comprising SNS-595 substance that are substantially pure and essentially free of visible particles. | 04-14-2011 |
20110092536 | NOVEL ANTI-INFECTIOUS DERIVATIVES, METHOD FOR THE PRODUCTION THEREOF, PHARMACEUTICAL COMPOSITIONS CONTAINING SAME AND USES OF SAID DERIVATIVES IN TREATMENT - The invention relates to bi-substrate inhibitor molecules associating (i) a pyridine, pyridinium or dihydropyridine-type structure allied to active metabolites of isoniazide, or related structures, and (ii) a hydrophobic substituent. The invention also relates to the method for producing said molecules, to the pharmaceutical compositions containing said molecules, and to the use thereof as inhibitors of enoyl reductase for the preparation of a medicament, especially an anti-infectious medicament for the treatment of tuberculosis. | 04-21-2011 |
20110092537 | 2,6-Diaminopyridine Compounds Suitable For Treating Diseases Associated With Amyloid Or Amyloid-Like Proteins Or For Treating Or Preventing Ocular Diseases Or Conditions Associated With A Pathological Abnormality/Change In The Tissue Of The Visual System - The present invention relates to 2,6-diaminopyridine compounds that can be employed in the treatment of a group of disorders and abnormalities associated with amyloid protein and of diseases or conditions associated with amyloid-like proteins. The compounds of the present invention can also be used in the treatment of ocular diseases associated with pathological abnormalities/changes in the tissues of the visual system. | 04-21-2011 |
20110092538 | 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. | 04-21-2011 |
20110112135 | Imidazo [1,2-A] Pyridine Compounds - This invention relates generally to imidazo[1,2-a]pyridine-based modulators of Liver X receptors (LXRs) having formula (I) and related methods: | 05-12-2011 |
20110112136 | NOVEL PROCESS FOR THE MANUFACTURE OF PHARMACEUTICAL PREPARATIONS - The present invention is related to an improved method for the manufacture of Micro-precipitated Bulk Powder (MBP) containing the active pharmaceutical ingredient Propane-1-sulfonic acid {3-[5-(4-chloro-phenyl)-1H-pyrrolo[2,3- | 05-12-2011 |
20110136855 | GEMIFLOXACIN PROCESS AND POLYMORPHS - The present invention provides a novel process for the preparation of gemifloxacin and its pharmaceutically acceptable acid addition salts in high yield. The present invention also relates to novel polymorphs of gemifloxacin free base and its hydrates to the processes for their preparation and to pharmaceutical compositions comprising them. The present invention also relates to infusion solutions of gemifloxacin and to processes for their preparation. Thus, 7-chloro-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8-naphth-yridine-3-carboxylic acid is reacted with a mixture of acetic anhydride, acetic acid and boric acid to give borane compound, which is then treated with 4-Aminomethyl-3-methoxyimino-pyrrolidinium dimethanesulfonate in presence of triethylamine, followed by treatment with 3.5% sodium hydroxide solution to give gemifloxacin free base. | 06-09-2011 |
20110136856 | Novel imidazo[1,5-a]pyridine derivatives, method for preparing same and pharmaceutical compositions containing same - The invention concerns compounds of formula I, a method for preparing said compounds, pharmaceutical compositions containing same and the theraprutic uses thereof. | 06-09-2011 |
20110136857 | PYRROLE[2,3-B]PYRIDINE DERIVATIVES ACTIVE AS KINASE INHIBITORS - Compounds which are pyrrolo[2,3-b]pyridine derivatives or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, cell proliferative disorders, Alzheimer's disease, viral infections, auto-immune diseases and neurodegenerative disorders; also disclosed is a process under SPS conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them. | 06-09-2011 |
20110144149 | GEMIFLOXACIN PROCESS AND POLYMORPHS - The present invention provides a novel process for the preparation of gemifloxacin and its pharmaceutically acceptable acid addition salts in high yield. The present invention also relates to novel polymorphs of gemifloxacin free base and its hydrates to the processes for their preparation and to pharmaceutical compositions comprising them. The present invention also relates to infusion solutions of gemifloxacin and to processes for their preparation. Thus, 7-chloro-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8-naphth-yridine-3-carboxylic acid is reacted with a mixture of acetic anhydride, acetic acid and boric acid to give borane compound, which is then treated with 4-Aminomethyl-3-methoxyimino-pyrrolidinium dimethanesulfonate in presence of triethylamine, followed by treatment with 3.5% sodium hydroxide solution to give gemifloxacin free base. | 06-16-2011 |
20110152311 | NOVEL CRYSTALLINE FORMS OF TRANS-7-OXO-6-(SULPHOOXY)-1,6-DIAZABICYCLO[3,2,1]OCTANE-2-CARBOXAMIDE SODIUM SALT - The present invention relates to novel crystalline forms of sodium salt of trans-7-oxo-6-(sulphooxy)-1,6-diazabicyclo[3,2,1]octane-2-carboxamide (e.g., NXL-104) thereof. The present invention relates to compositions comprising a crystalline form of sodium salt of trans-7-oxo-6-(sulphooxy)-1,6-diazabicyclo[3,2,1]octane-2-carboxamide (e.g., NXL-104) alone or in combination with an antibacterial agent (e.g., ceftaroline fosamil). Processes for the preparation of the crystalline forms and methods of treating bacterial infections by administering the crystalline forms alone or in combination with an antibacterial agent (e.g., ceftaroline fosamil) are also described. | 06-23-2011 |
20110152312 | ANTIPARISITIC DIHYDROAZOLE COMPOUNDS AND COMPOSITIONS COMPRISING SAME - The present invention relates to novel dihydroazole of formula (I) and salts thereof: | 06-23-2011 |
20110166173 | 3,5-DISUBSTUTUTED 1H-PYRROLO [2,3-B] PYRIDINES AS JNK INHIBITORS - The present invention provides novel compounds of forumula (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. | 07-07-2011 |
20110166174 | COMPOUNDS MODULATING C-KIT AND C-FMS ACTIVITY AND USES THEREFOR - Compounds active on the receptor protein tyrosine kinases c-kit and c-fms are provided herewith. Also provided herewith are compositions useful for treatment of c-kit mediated diseases or condition and c-fms-mediated diseases or condition, and methods for the use thereof. | 07-07-2011 |
20110166175 | 7-AZAINDOLE DERIVATIVES - Novel 7-azaindole derivatives of the formula (I), in which U, L, R, Y, X | 07-07-2011 |
20110172265 | Fused pyrrolidino-cyclopropane derivatives as selective 11-beta-hydroxysteroid dehydrogenase type 1 inhibitors - The present invention relates to fused pyrrolidino-cyclopropane derivatives according to formulae (I) to (IV) as selective inhibitors of the enzyme 11-beta-hydroxysteroid dehydrogenase type 1 (11-β-HSD-1) and the use of such compounds for the treatment and/or prevention of metabolic syndrome, diabetes, insulin resistance, obesity, lipid disorders, glaucoma, osteoporosis, cognitive disorders, anxiety, depression, immune disorders, hypertension and other diseases and conditions. | 07-14-2011 |
20110184012 | METHODS AND COMPOSITIONS FOR ALLEVIATING STUTTERING - Methods of treating stuttering include treating people with gamma-aminobutyric acid (GABA) receptor modulators, including cyclopyrrolones. A second active agent may be used with GABA receptor modulators. Active enantiomers, active metabolites, and pharmaceutically acceptable salts of garnma-aminobutyric acid receptor modulators, including cyclopyrrolones, are acceptable components of the compositions. The cyclopyrrolone class of modulators includes pagoclone, suriclone, zopiclone, 2-(7-chloro-2-naphthyridin-1,8-yl)-3-(5-methyl-2-oxohexy))isoindolin-1-one, 2-(7-chloro-2-naphthyridin-1,8-yl)isoindolin-1-yl-4- acetamidobutyrate, and 2-(7-chloro-1,8-naphthyridin-2y1)-3-(5-methyl-5-hydroxy-2-oxohexyl)-1-isoindolinone. | 07-28-2011 |
20110184013 | Imidazo[1,2-a]Pyridine Compounds As Receptor Tyrosine Kinase Inhibitors - Compounds of Formula I and II: I II having the chemical names cis-6-fluoro-8-(3-fluoropiperidin-4-yloxy)-2-(7-(2-methoxyethoxy)imidazo[1,2-a]pyridin-3-yl)quinoline and 6-fluoro-8-(trans-3-fluoropiperidin-4-yloxy)-2-(7-(2-methoxyethoxy)imidazo[1,2-a]pyridin-3-yl)quinoline, respectively, and enantiomers and pharmaceutically acceptable salts thereof, are receptor tyrosine inhibitors useful in the treatment of diseases mediated by class 3 and class 5 receptor tyrosine kinases. The compounds of this invention have also been found to be inhibitors of Pim-1. | 07-28-2011 |
20110190334 | Heterocyclic Sulfonamide Derivatives - The present invention relates to compounds of Formula I | 08-04-2011 |
20110195991 | 3-AMINOIMIDAZO [1,2-A] PYRIDINE DERIVATIVES AS SGLT INHIBITORS - Novel compounds of the formula I, in which X, Y, R, R′, R | 08-11-2011 |
20110201642 | Bioactive Compounds - The invention relates to bioactive compounds derived from an endophytic | 08-18-2011 |
20110212990 | NOVEL POLYMORPH OF MOXIFLOXACIN HYDROCHLORIDE - The present invention relates to novel polymorph of moxifloxacin hydrochloride, processes for its preparation and to pharmaceutical compositions containing it. Thus, for example moxifloxacin hydrochloride is suspended in methanol and water and the p | 09-01-2011 |
20110212991 | Diagnostic Test for Susceptibility to B-RAF Kinase Inhibitors - The present invention provides methods and reagents for the detection of a mutation in BRAF and methods of selecting, patients for treatment if a B-Raf kinase inhibitor, such as a selective B-Raf kinase inhibitor. | 09-01-2011 |
20110212992 | NOVEL P2X7R ANTAGONISTS AND THEIR USE - The present application is directed to novel P2X7R antagonists that are N-indol-3-yl-acetamide and N-azaindol-3-yl-acetamide compounds, pharmaceutical compositions comprising the same and their use for the prophylactic or therapeutic treatment of diseases mediated by P2X7R activity. | 09-01-2011 |
20110218214 | Inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme - The present invention relates to compounds which are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome and other diseases and conditions that are mediated by excessive glucocorticoid action. | 09-08-2011 |
20110224247 | AZAISOQUINOLINONE DERIVATIVES AS NK3 ANTAGONISTS - The invention relates to compounds useful in therapy, in particular in the treatment of psychosis, to compositions comprising said compounds, and to methods of treating diseases comprising the administration of said compounds. | 09-15-2011 |
20110224248 | AZAQUINOLONES THAT INHIBIT PROLYL HYDROXYLASE - Compounds of Formula I are useful inhibitors of HIF prolyl hydroxylases. Compounds of Formula I have the following structure: | 09-15-2011 |
20110224249 | Novel Hydrate Form - The present invention relates to a novel hydrate form of moxifloxacin monohydrochloride, processes for preparing the form, pharmaceutical compositions comprising the form and uses of the form and compositions. | 09-15-2011 |
20110224250 | ISOQUINOLINE DERIVATIVE, AND PDE INHIBITOR COMPRISING SAME AS ACTIVE INGREDIENT - The present invention provides a novel isoquinoline derivative which is useful as a pharmaceutical agent having a phosphodiesterase inhibitory activity. | 09-15-2011 |
20110237619 | IMIDAZOPYRIDINE DERIVATIVES WHICH INHIBIT THE SECRETION OF GASTRIC ACID - The present invention relates to substituted imidazo[1,2-a]pyridines of formula I where R is —CH | 09-29-2011 |
20110245290 | Alternative Forms of the Phosphodiesterase-4 Inhibitor N-Cyclopropyl-1--4-Oxo-1,4-Dihydro-1,8-Naphthyridine-3-Carboxyamide - The present invention is directed to alternative forms of the title phosphodiesterase 4 inhibitor which has the structural formula shown immediately below: | 10-06-2011 |
20110257222 | COMPOUNDS AND METHODS FOR THE TREATMENT OF PAIN AND OTHER DISEASES - The present invention relates generally to alkyne containing pharmaceutical agents, and in particular, to phenylethynyl-thiophene based metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of MMP inhibiting compounds that exhibit increased potency, metabolic stability and/or reduced toxicity in relation to currently known MMP inhibitors for the treatment of pain and other diseases such as cancer. Additionally, the present invention relates to methods for treating pain in a patient comprising administering to the patient a pain-reducing effective amount of a present compound. | 10-20-2011 |
20110263638 | Therapeutic agent for glaucoma comprising rho kinase inhibitor and - blocker - A therapeutic agent for glaucoma including a combination of pharmaceutically effective amounts of a Rho kinase inhibitor and a β-blocker, wherein the Rho kinase inhibitor is (R)-(+)-N-(1H-pyrrolo[2,3-b]pyridin-4-yl)-4-(1-aminoethyl)benzamide and the β-blocker is befunolol, carteolol, nipradilol, betaxolol, levobunolol or metipranolol. A method of treating glaucoma including administering effective amounts of a Rho kinase inhibitor and a β-blocker to a patient, wherein the Rho kinase inhibitor is (R)-(+)-N-(1H-pyrrolo[2,3-b]pyridin-4-yl)-4-(1-aminoethyl)benzamide and the β-blocker is befunolol, carteolol, nipradilol, betaxolol, levobunolol or metipranolol. | 10-27-2011 |
20110275663 | N-Acylthiourea and N-Acylurea Inhibitors of the Hedgehog Protein Signalling Pathway - The present invention relates to the use of acylthiourea or acylurea derivatives for the treatment of pathologies involving a tissue dysfunction associated with a deregulation of the Hedgehog protein signalling pathway, and also to novel acylthiourea or acylurea derivatives as such, to their use as a medicinal product, and to pharmaceutical compositions containing them. | 11-10-2011 |
20110275665 | GLUCOKINASE ACTIVATORS - Compounds are provided for use with hexokinases that comprise: | 11-10-2011 |
20110288116 | IAP INHIBITORS - The present invention describes compounds of the following formula: processes for their preparation, pharmaceutical compositions containing them, and their use in therapy. The compounds of the present invention inhibit IAPs (inhibitors of apoptosis proteins) and thus are useful in the treatment of cancer, autoimmune diseases and other disorders where a defect in apoptosis is implicated. | 11-24-2011 |
20110288117 | SUBSTITUTED HYDROXAMIC ACIDS AND USES THEREOF - This invention provides compounds of formula (I): | 11-24-2011 |
20110312987 | SALT OF NAPHTHYRIDINE CARBOXYLIC ACID DERIVATIVE - 7-(3-Aminomethyl-4-methoxyiminopyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid methanesulfonate and hydrates thereof, processes for their preparation, pharmaceutical compositions comprising them, and their use in antibacterial therapy. | 12-22-2011 |
20110312988 | SNS-595 AND METHODS OF USING THE SAME - The present invention relates to SNS-595 and methods of treating cancer using the same. | 12-22-2011 |
20110312989 | INDOLES, 1H-INDAZOLES, 1,2-BENZISOXAZOLES, AND 1,2-BENZISOTHIAZOLES, AND PREPARATION AND USES THEREOF - The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nAChR), activation of nAChRs, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds for example, indoles, 1H-indazoles, 1,2-benzisoxazoles, and 1,2-benzisothiazoles, which act as ligands for the α7 nAChR subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof. | 12-22-2011 |
20110319443 | INHIBITORS OF AKT ACTIVITY - The instant invention provides for substituted naphthyridine 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. | 12-29-2011 |
20120015973 | MEK MUTATIONS CONFERRING RESISTANCE TO MEK INHIBITORS - The present invention relates to methods, compositions and kits concerning resistance to treatment with an anti-cancer agent, specifically an inhibitor of MEK. In particular embodiments, the invention concerns mutations in a MEK sequence that confer resistance to a MEK inhibitor. Identification of such mutations in a MEK sequence allows the identification and design of second-generation MEK inhibitors. Methods and kits for detecting the presence of a mutant MEK sequence in a sample are also provided. | 01-19-2012 |
20120015974 | IMIDAZOPYRIDINE INHIBITORS OF IAP - The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: | 01-19-2012 |
20120015975 | FUSED HETEROCYCLIC COMPOUND AND USE THEREOF - A fused heterocyclic compound of formula (1): wherein, A | 01-19-2012 |
20120022098 | 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. | 01-26-2012 |
20120065224 | PYRROLO[3,2-C) PYRIDINE DERIVATIVES AND PROCESSES FOR THE PREPARATION THEREOF - The present invention provides novel pyrrolo[3,2-c]pyridine derivatives or pharmaceutically acceptable salts thereof, processes for the preparation thereof, and compositions comprising the same. The pyrrolo[3,2-c]pyridine derivatives or pharmaceutically acceptable salts thereof of the present invention have excellent proton pump inhibition effects and possess the ability to attain a reversible proton pump inhibitory effect. | 03-15-2012 |
20120065225 | HETEROARYL PYRROLIDINYL AND PIPERIDINYL KETONE DERIVATIVES AND USES THEREOF - Compounds of the formula: | 03-15-2012 |
20120077840 | 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. | 03-29-2012 |
20120095034 | PIPERIDINE DERIVATIVES USEFUL AS OREXIN RECEPTOR ANTAGONISTS - This invention relates to imidazo[1,2-a]pyridin-2-ylmethyl substituted piperidine derivatives of formula (I) and their use as pharmaceuticals, in the treatment of obesity and diabetes. | 04-19-2012 |
20120101122 | IMIDAZO[1,2 A] PYRIDINE 6 CARBOXAMIDE DERIVATIVES, THEIR USE FOR THE TREATMENT OF COLON CANCER AND THEIR METHOD OF MANUFACTURE - This invention relates to the manufacture of novel chemical compounds which have biological activity, particularly to novel chemical compounds that are cytotoxic against colon cancer cells and colon cancer cell lines. The manufacturing of said chemical compounds displaying anti-cancer properties employs the use of multi-component chemical reactions. The object of this invention is to manufacture and isolate analogues of imidazo[1,2-a]pyridine, namely compounds of Formula 1, which are cytotoxic against colon cancer cells, while concomitantly being relatively inactive against white blood cells. | 04-26-2012 |
20120101123 | COMPOUNDS - The present invention relates to novel compounds having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders. | 04-26-2012 |
20120101124 | 1,2,4-OXADIAZOL DERIVATIVES, THEIR PHARMACEUTICAL COMPOSITIONS AND THEIR USE AS SPHINGOSINE 1-PHOSPHATE 1 RECEPTOR AGONISTS - 1,2,4-Oxadiazol derivatives represented by formula (I) useful as sphingosine 1-phosphate 1 (S1P1) receptor agonists, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders mediated via S1P1 receptor are disclosed. | 04-26-2012 |
20120115899 | NAPHTHYRIDIN-2 (1 H)-ONE COMPOUNDS USEFUL AS ANTIBACTERIALS - Compounds of Formula (I), | 05-10-2012 |
20120115900 | SUBSTITUTED NAPHTHYRIDINE DERIVATIVES AND THEIR MEDICAL USE - The present application discloses novel substituted naphthyridine derivatives of Formula (I) and their use as modulators of the voltage gated K | 05-10-2012 |
20120129884 | PHOTOCHEMOTHERAPEUTIC HETEROCYCLIC AGENTS HAVING ANTIPROLIFERATIVE AND ANTINEOPLASTIC ACTIVITY - The present invention concerns the synthesis of new analogs of angelicins, pyrrolo [3,2-h]quinoline, for the treatment of pathologies having hyperproliferative character included those having neoplastic nature. The treatment is based on the combined action of pyrrolo [3,2-h]quinolines and UV-A light, through a clinical approach defined as PUVA (psoralen-UVA light). The most important feature of these compounds is that they exert their remarkable photoxicity without any DNA damage, which is the main origin of the side effects of the PUVA therapy. | 05-24-2012 |
20120165366 | COMPOUNDS AND USES THEREOF - N-[3-(4-Cyano-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluoro-phenyl]-4-trifluoromethyl-benzenesulfonamide, N-[3-(4-ethynyl-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluoro-phenyl]-4-trifluoromethyl-benzenesulfonamide, and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof are active on at least one Raf protein kinase. Also described are methods of use thereof to treat diseases and conditions, including diseases and conditions associated with activity of Raf protein kinases, including pain and polycystic kidney disease. | 06-28-2012 |
20120172390 | METHOD OF TREATING SLEEP DISORDERS USING THE COMBINATION OF EPLIVANSERIN AND ZOLPIDEM - The instant invention relates to a method of treating sleep disorders by using eplivanserin or pharmaceutically acceptable salts or esters thereof and Zolpidem by evaluating the effect of eplivanserin combined with the sleep-inducing agent Zolpidem on psychomotor/cognitive performance. | 07-05-2012 |
20120172391 | NAPHTHYRIDINONE ANALOGS AS MGLUR5 POSITIVE ALLOSTERIC MODULATORS - In one aspect, the invention relates to naphthyridinone analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. | 07-05-2012 |
20120178776 | DIHYDRONAPHTHYRIDINYL(ORGANO)METHANONE ANALOGS AS POSITIVE ALLOSTERIC MGLUR5 MODULATORS - In one aspect, the invention relates to dihydronaphthyridinyl(organo)methanone analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. | 07-12-2012 |
20120190707 | SELECTIVE INHIBITORS OF AKT AND METHODS OF USING SAME - The present invention describes an improved method for screening compounds for activity in inhibiting the enzymatic activity of Akt1 protein kinase. In general, the method comprises: (1) providing a plurality of compounds suspected of having Akt1 kinase inhibitory activity; (2) modeling the docking of each of the plurality of the compounds with a target binding site; (3) ranking the docked compounds by goodness of fit; (4) further selecting compounds; (5) optionally, visually analyzing structures of compounds selected in step (4) to remove any compounds with improbable docking geometry; and (6) experimentally testing the selected compounds from step (4) or step (5), if step (5) is performed, to determine their inhibitory activity against Akt1. The invention also encompasses pharmaceutical compositions including compounds whose inhibitory activity against Akt1 is discovered by the screening method, as well as methods of use of the pharmaceutical compositions to prevent and treat cancer and other conditions. | 07-26-2012 |
20120208837 | SUBSTITUTED AZAINDOLES - This invention relates to novel substituted azaindoles and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a compound showing selective inhibitory activity of oncogenic B-Raf | 08-16-2012 |
20120214839 | 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). | 08-23-2012 |
20120214840 | INDOLIZINE INHIBITORS OF 5-LIPOXYGENASE - Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of 5-lipoxygenase (5-LO). Also described herein are methods of using such 5-LO inhibitors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other leukotriene-dependent or leukotriene mediated conditions, diseases, or disorders. | 08-23-2012 |
20120220622 | HETEROCYCLIC DERIVATIVES | 08-30-2012 |
20120232108 | GAMMA SECRETASE MODULATORS - This invention provides novel compounds that are modulators of gamma secretase. The compounds have the Formula I: Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of Formula I. | 09-13-2012 |
20120238597 | Inhibiting EPH B-3 Kinase - EphB3 kinase inhibitor compounds, including certain pyrazolo[1,5-a]pyridine and imidazo[1,2-a]pyridine compounds, inhibit EphB3 kinase. The EphB3 kinase inhibitor compounds can have greater potency for the inhibition of EphB3 kinase than general kinase inhibitors. Pharmaceutical compositions, such as neuroprotective agents, comprising the EphB3 kinase inhibitor compounds are also provided. The EphB3 kinase inhibitor compounds and pharmaceutical compositions are useful, for example, to provide neuroprotection and/or repair of neuronal tissue damaged during an ischemic event, such as a stroke. | 09-20-2012 |
20120238598 | DERIVATIVES OF 7 ALKYNYL-1,8 NAPHTHYRIDONES, PREPARATION METHOD THEREOF AND USE OF SAME IN THERAPEUTICS - The disclosure relates to method of treating a disease in which VEGFR-3 is involved, comprising administering a therapeutically effective amount of a compound of the formula | 09-20-2012 |
20120245197 | PHARMACEUTICAL COMPOSITION CONTAINING TOSUFLOXACIN OR SALT THEREOF - A pharmaceutical composition containing tosufloxacin or a salt thereof, which is excellent in stability and preservative effect and contamination preventing effect is provided. A pharmaceutical composition containing tosufloxacin or a salt thereof, a metal compound comprising aluminum, borax, an alkali metal chloride and a preservative is excellent in stability and preservative effect and contamination preventing effect, and useful especially as eye drops, nasal drops and ear drops. | 09-27-2012 |
20120245198 | COMPOUNDS AND COMPOSITIONS FOR TREATMENT OF CANCER - Compounds and compositions for treating, preventing or managing cancer are disclosed. The compositions provided herein comprise SNS-595 and N-desmethyl-SNS-595. Also provided are pharmaceutical compositions comprising the compounds and methods of treatment using the compounds and compositions. | 09-27-2012 |
20120245199 | [4 [4-(AMINOMETHYL-2-FLUORO-PHENYL)-PIPERIDIN-1-YL]-(1H-PYRROLO-PYRIDIN-YL- )-METHANONES AND SYNTHESIS THEREOF - The present invention relates herein to compounds and compositions for the treatment and amelioration of inflammatory disease. Specifically the present invention relates to compounds that having a tryptase inhibition activity and the intermediates thereof, pharmaceutical compositions comprising such compounds, and a method of treating subjects suffering from a condition disease or disorder that can be ameliorated by the administration of an inhibitor of tryptase. | 09-27-2012 |
20120258982 | ADAMANTYL COMPOUNDS - The invention relates to JNK inhibitors and corresponding methods, formulations, and compositions for inhibiting JNK and treating JNK-mediated disorders. The application discloses JNK inhibitors, as described below in Formula I: | 10-11-2012 |
20120270897 | ACETYLENE DERIVATIVES OF 5-PHENYL-PYRAZOLOPYRIDINE, PREPARATION THEREOF, AND THERAPEUTIC USE THEREOF - Compounds of formula (I): | 10-25-2012 |
20120277261 | PHARMACEUTICAL FORMULATIONS USEFUL IN THE TREATMENT OF INSOMNIA - There is provided a formulation suitable for transmucosal administration comprising a short acting hypnotic drug, which formulation provides a measurable plasma concentration of drug within 10 minutes of administration. The formulation is capable of providing sleep on demand, and preferably comprises particles of drug, for example zolpidem or a pharmaceutically-acceptable salt thereof and a mucoadhesion promoting agent, such as sodium carboxymethylcellulose, which particles of drug and mucoadhesive are presented upon the surface of larger carrier particles. | 11-01-2012 |
20120277262 | NEW AMINOTETRALINE DERIVATIVES - The present application relates to compounds of formula (I): and pharmaceutically acceptable salts and solvates thereof, wherein the substituents are as defined herein, compositions containing such compounds and the uses of such compounds in producing medicaments for the treatment of various diseases and conditions, such as of the central nervous system. | 11-01-2012 |
20120277263 | POLYMORPHS OF 1-CYCLOPROPYL-7-([S,S])-2,8-DIAZADICYCLO[4.3.0]NON-8-YL)-6-FLUORO-1,4-DIH- YDRO -8-METHOXY-4-OXO-3-QUINOLINE CARBOXYLIC ACID HYDROCHLORIDE AND METHODS FOR THE PREPARATION THEREOF - Two novel crystalline forms, designated form A and form B of the antibacterial agent 1-cyclopropyl-7-([S,S])-2,8-diazabicyclo[4.3.0]non-8-yl)-6-fluoro-1,4-dihydro-8-methoxy-4-oxo-3-quinoline carboxylic acid hydrochloride of formula, | 11-01-2012 |
20120283287 | CERTAIN CHEMICAL ENTITIES, COMPOSITIONS, AND METHODS - Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of one or more mitotic kinesins are disclosed. | 11-08-2012 |
20120289540 | KINASE INHIBITORS USEFUL FOR THE TREATMENT OF PROLIFERATIVE DISEASES - The present invention relates to novel kinase inhibitors and modulator compounds useful for the treatment of various diseases. More particularly, the invention is concerned with such compounds, kinase/compound adducts, methods of treating diseases, and methods of synthesis of the compounds. Preferrably, the compounds are useful for the modulation of kinase activity of Raf kinases and disease polymorphs thereof. Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant melanoma, colorectal cancer, ovarian cancer, papillary thyroid carcinoma, non small cell lung cancer, and mesothelioma. Compounds of the present invention also find utility in the treatment of rheumatoid arthritis and retinopathies including diabetic retinal neuropathy and macular degeneration. | 11-15-2012 |
20120289541 | METHODS AND COMPOSITIONS FOR APPLYING MOXIFLOXACIN TO THE EAR - Methods and materials useful for applying moxifloxacin to the ear are described. The methods involve delivering a composition that contains at least one viscogenic agent and moxifloxacin or a salt thereof to the epidermal surface of the tympanic membrane via the ear canal. The composition is delivered to the tympanic membrane in a flowable form and, after delivery to the tympanic membrane, becomes sufficiently viscous such that the moxifloxacin is localized against the tympanic membrane. Such compositions can be used to prophylactically and/or therapeutically treat middle and inner ear conditions, including otitis media. | 11-15-2012 |
20120295934 | New Hexahydrocyclopentapyrrolone, Hexahydropyrrolopyrrolone, Octahydropyrrolopyridinone and Octahydropyridinone Compounds - The invention provides novel compounds having the general formula (I) | 11-22-2012 |
20120302596 | AZAINDOLES HAVING SEROTONIN RECEPTOR AFFINITY - Described herein are compounds with affinity for the 5-HT | 11-29-2012 |
20120302597 | NOVEL P2X7R ANTAGONISTS AND THEIR USE - The present application is directed to novel P2X7R antagonists that are indol-3-carboxamide or azaindole-3-carboxamide compounds, pharmaceutical compositions comprising the same and their use for the prophylactic or therapeutic treatment of diseases mediated by P2X7R activity. | 11-29-2012 |
20120316194 | APOPTOSIS SIGNAL-REGULATING KINASE 1 INHIBITORS - The present invention relates to apoptosis signal-regulating kinase 1 (“ASK1”) inhibiting compounds of the formula | 12-13-2012 |
20120322820 | METHODS TO INHIBIT TUMOR CELL GROWTH BY USING PROTON PUMP INHIBITORS - Methods of treating one or more growth deregulated cells are disclosed. An effective amount of a pharmaceutical composition including a proton pump inhibitor is administered thereby treating a growth deregulated cell outside of the gastric lumen of a subject. | 12-20-2012 |
20120329826 | SUBSTITUTED-5-AMINOPYRROLO/PYRAZOLOPYRIDINES - Compounds of Formula I, as shown below and defined herein: pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers mediated at least in part by RON and/or MET. | 12-27-2012 |
20130005760 | HETEROCYCLIC COMPOUND HAVING AZOLE GROUP - A heterocyclic compound of formula (I) or a salt thereof: | 01-03-2013 |
20130005761 | PROCESS FOR THE MANUFACTURE OF PHARMACEUTICALLY ACTIVE COMPOUNDS - The present invention relates to a composition comprising the compound of formula (1), | 01-03-2013 |
20130018070 | MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR - The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators. | 01-17-2013 |
20130023554 | 5-PHENYLPYRAZOLOPYRIDINE DERIVATIVES, PREPARATION AND THERAPEUTIC USE THEREOF - Compounds of formula (I): | 01-24-2013 |
20130035353 | DRUGS FOR THE TREATMENT OF SARCOGLYCANOPATHIES - Inhibitors of the endoplasmic reticulum associated degradation (ERAD) pathway, particularly inhibitors of mannosidase I, are used for the preparation of a medicinal product intended to treat sarcoglycanopathies. | 02-07-2013 |
20130035354 | ARYL PYRIDINE AS ALDOSTERONE SYNTHASE INHIBITORS - The present invention provides a compound of formula I; | 02-07-2013 |
20130040983 | RAF KINASE INHIBITORS - Described herein are compounds, pharmaceutical compositions and methods for the inhibition of RAF kinae mediated signaling. Said compounds, pharmaceutical compositions and methods have utility in the treatment of human disease and disorders. | 02-14-2013 |
20130040984 | 7-(lH-PYRAZOL-4-YL)-1,6-NAPHTHYRIDINE COMPOUNDS AS SYK INHIBITORS - The present invention relates to a compound of formula (I): | 02-14-2013 |
20130053412 | Cyclopentanecarboxamide derivatives, medicaments containing such compounds and their use - The invention relates to cyclopentanecarboxamide derivatives of formula 1, to their use as Fatty Acid Synthase inhibitors, to methods for their therapeutic use and to pharmaceutical compositions containing them, wherein R | 02-28-2013 |
20130059880 | MOXIFLOXACIN HYDROCHLORIDE COMPOUNDS AND INTERMEDIATES AND METHODS FOR MAKING SAME - Methods for producing moxifloxacin hydrochloride compounds having very low levels of impurities are provided. Compounds produced using such methods and pharmaceutical compositions including such compounds are also provided. | 03-07-2013 |
20130059881 | COMPOSITIONS AND METHODS FOR TREATING VIRAL DISEASES - Substituted perhydro pyrrolopyridines and methods for their use in the treatment of viral diseases including hepatitis C viral infections are described herein. | 03-07-2013 |
20130065917 | SALT OF NAPHTHYRIDINE CARBOXYLIC ACID DERIVATIVE - 7-(3-Aminomethyl-4-methoxyiminopyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid methanesulfonate and hydrates thereof, processes for their preparation, pharmaceutical compositions comprising them, and their use in antibacterial therapy. | 03-14-2013 |
20130079365 | NEW BICYCLIC DIHYDROQUINOLINE-2-ONE DERIVATIVES - The invention provides novel compounds having the general formula (I) | 03-28-2013 |
20130085153 | COMBINATION OF AN IAP INHIBITOR AND A TAXANE FOR THE TREATMENT OF A PROLIFERATIVE DISEASE - The invention provides a pharmaceutical combination comprising:
| 04-04-2013 |
20130090351 | ANALOGUES FOR THE TREATMENT OR PREVENTION OF FLAVIVIRUS INFECTIONS - Compounds represented by formula I | 04-11-2013 |
20130090352 | TETRAHYDROQUINOLINE AMIDE M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS - The present invention is directed to tetrahydroquinoline amide compounds of formula (I) (Formula should be inserted here) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor. | 04-11-2013 |
20130102628 | CRYSTAL OF FUSED PYRIDINE COMPOUND SALT - [Problem] A salt or crystal of a compound which is highly stable in a solid state and useful as a bulk material for the preparation of a pharmaceutical product is provided. | 04-25-2013 |
20130109714 | NEURODEGENERATIVE DISEASE THERAPEUTIC AGENT | 05-02-2013 |
20130131102 | 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. | 05-23-2013 |
20130137715 | Pharmaceutical Compositions Containing A Fluoroquinolone Antibiotic Drug - Pharmaceutical compositions containing a fluoroquinolone antibiotic drug are disclosed. The compositions exhibit improved homogeneity, improved bioavailability, lower turbidity or a combination thereof. The composition can be use as otic or nasal compositions, but are particularly useful as ophthalmic compositions. | 05-30-2013 |
20130143910 | Fructose-1,6-biphosphatases as new targets for diagnosing and treating breast cancer brain metastasis - A method and composition for treating cancer cells that targets fructose-1,6-biphosphataseenzymes (FBPs, type 1 and type 2) and/or their respective pathways. In one embodiment, inhibitors of FBPs or FBPs pathways are administered to a patient to treat brain cancer metastasis. In another embodiment, the present invention is particularly well suited for treating cancer cells that generally survive under glucose-independent conditions, or any other condition where cancer cells produce glucose via FBPs mediated pathways. | 06-06-2013 |
20130143911 | MEK1 Mutation Conferring Resistance to RAF and MEK Inhibitors - Nucleic acids and proteins having a mutant MEK sequence, and methods concerning identification of patients having resistance to treatment with anti-cancer agents, specifically inhibitors of RAF or MEK are provided. Methods of treatment and for optimizing treatment for patients having a mutation in a MEK1 sequence are also provided. | 06-06-2013 |
20130143912 | SUBLINGUAL ZOLPIDEM FORMULATIONS - The present disclosure provides pharmaceutical compositions for the delivery of a hypnotic agent across the oral mucosa. In particular, the compositions devoid of buffer and in the presence of alkaline oxides capable of raising the pH of saliva to a pH greater than about 7.0 thereby facilitate the substantially complete conversion of the hypnotic agent from its ionized to its un-ionized form. As a result, the dose of hypnotic agent is rapidly and efficiently absorbed by the oral mucosa with surprisingly low inter-subject variability. Furthermore, delivery of the hypnotic agent across the oral mucosa advantageously bypasses hepatic first pass metabolism of the drug and avoids enzymatic degradation of the drug within the gastrointestinal tract. Methods for using the compositions of the present invention for treating sleep disorders such as insomnia are also provided. | 06-06-2013 |
20130143913 | PROPHYLACTIC OR THERAPEUTIC AGENT FOR NON-ALCOHOLIC STEATOHEPATITIS - An object of the present invention is to provide an agent for prevention or treatment of a fatty liver disease, preferably NAFLD, more preferably NASH. The present invention provides an agent for prevention or treatment of a fatty liver disease containing ibudilast as an active agent. | 06-06-2013 |
20130150400 | SALTS, PRODRUGS AND POLYMORPHS OF FAB I INHIBITORS - In part, the present invention is directed to antibacterial compounds and salts thereof. | 06-13-2013 |
20130158066 | 4-AZAINDOLE INHIBITORS OF CRAC - Disclosed are compounds of Formula (I): | 06-20-2013 |
20130158067 | TRPV1 Antagonists - Disclosed herein are compounds of formula (I): | 06-20-2013 |
20130158068 | DICARBOXIMIDE DERIVATIVES OF BERBAMINE, THE PREPARATION AND USE THEREOF - The present invention relates to a novel dicarboximide derivative of berbamine represented by formula I, including, but not limited to, a phthalimide derivative of berbamine and an aromatic heterocyclic dicarboximide derivative of berbamine, or a pharmaceutically acceptable salt thereof, to a process for preparation of the same, to a pharmaceutical composition comprising said compound and to use thereof in manufacture of an antitumor medicament. | 06-20-2013 |
20130165473 | Azaquinolinone Derivatives and Uses Thereof - The present invention provides compounds and methods for treating or preventing the development of a disease, disorder, or condition in a subject or patient. | 06-27-2013 |
20130165474 | COMPOUNDS THAT INHIBIT TAU PHOSPHORYLATION - The present invention provides methods and compositions for enhancing working memory impaired in a tau pathological condition associated with AD or Down's syndrome. | 06-27-2013 |
20130165475 | DEUTERIUM-ENRICHED HETEROCYCLIC COMPOUNDS AS KINASE INHIBITORS - The present invention provides deuterium-enriched heteroaryl-containing urea compounds (I) and use of the same for treating conditions mediated by protein kinase such as | 06-27-2013 |
20130178495 | IBUDILAST FOR RELIEVING NEGATIVE EFFECTS OF MEDICATION OVERUSE HEADACHE - Certain negative effects of medication overuse headache (MOH) are relieved by administering ibudilast or a pharmaceutically acceptable salt thereof. | 07-11-2013 |
20130178496 | MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR - The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators. | 07-11-2013 |
20130190349 | THERAPEUTIC COMPOSITIONS FOR INTRANASAL ADMINISTRATION OF ZOLPIDEM - The invention provides sprayable aqueous compositions containing zolpidem or single stereoisomer, mixtures of stereoisomers, pharmaceutically acceptable salts or prodrugs thereof, a solubilizing agent, a water soluble polymer with bioadhesive property. When administered intranasally using a spray device, zolpidem is rapidly absorbed with prolonged intranasal residence time and improved bioavailability. The compositions can be applied for the treatment of insomnia-related disorders such as difficulties with sleep initiation or middle of the night awakenings. | 07-25-2013 |
20130203802 | 3 -AMINO- PYRAZOLE DERIVATIVES USEFUL AGAINST TUBERCULOSIS - A compound of Formula (I) or a pharmaceutically acceptable salt thereof: | 08-08-2013 |
20130210856 | COMPOSITIONS AND METHODS FOR TREATING SLEEP DISORDERS - The present invention provides liquid dosage forms for treating narcolepsy. The liquid dosage form includes zolpidem or a pharmaceutically acceptable salt thereof, a carbonate salt, a metal oxide, and a borate salt. The present invention also provides methods for treating somnambulism. The methods include administering an emulsion that includes zolpidem, a bicarbonate salt, a citrate salt, and a phosphate salt. | 08-15-2013 |
20130210857 | Inhibitors of Human Immunodeficiency Virus Replication - The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection. | 08-15-2013 |
20130210858 | SULFAMOYL BENZOIC ACID HETEROBICYCLIC DERIVATIVES AS TRPM8 ANTAGONISTS - The present invention relates to sulfamoyl benzoic acid heterobicyclic derivatives of the formula (I) or a pharmaceutically acceptable salt thereof or a prodrug thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders which are mediated via the TRPM8 receptor. | 08-15-2013 |
20130217718 | TREATMENT OF PROGRESSIVE NEURODEGERATIVE 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). | 08-22-2013 |
20130217719 | Combination of Organic Compounds - The invention provides a pharmaceutical combination comprising:
| 08-22-2013 |
20130217720 | IMIDAZOLIDINE-2,4-DIONE DERIVATIVES AS N-FORMYL PEPTIDE RECEPTOR 2 MODULATORS - The present invention relates to novel imidazolidine-2,4-dione derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor 2 (FPR2). | 08-22-2013 |
20130217721 | COMPOSITIONS AND METHODS FOR DETECTION AND TREATMENT OF B-RAF INHIBITOR-RESISTANT MELANOMAS - Specific, targetable molecules mediating acquired resistance of B-RAF-mutant melanomas to a B-RAF inhibitor, thereby providing materials and methods for the treatment and detection of B-RAF inhibitor resistant cancers, such as melanoma. A method of identifying a patient to be treated with an alternative to B-RAF inhibitor therapy is described. Also described is a method of treating a patient having cancer. The patient is administered a MEK inhibitor, optionally in conjunction with vemurafenib therapy, or an inhibitor of the MAPK pathway (RAF, MEK, ERK) in conjunction with an inhibitor of the RTK-PI3K-AKT-mTOR pathway. | 08-22-2013 |
20130225635 | FUSED BICYCLIC DIAMINE DERIVATIVES AS HIV ATTACHMENT INHIBITORS - Compounds of Formula I, including pharmaceutically acceptable salts thereof: | 08-29-2013 |
20130231363 | ALTERNATIVE FORMS OF THE PHOSPHODIESTERASE-4 INHIBITOR N-CYCLOPROPYL-1--4-OXO-1,4-DIHYDRO-1,8-NAPHTHYRIDINE-3-CARBOXYAMIDE - The present invention is directed to alternative forms of the title phosphodiesterase 4 inhibitor which has the structural formula shown immediately below: | 09-05-2013 |
20130245062 | NITRILE DERIVATIVES AND THEIR PHARMACEUTICAL USE AND COMPOSITIONS - Disclosed are nitrile derivatives and pharmaceutical compositions comprising nitrile derivatives. The pharmaceutical compositions comprise compounds of the formula I | 09-19-2013 |
20130310417 | Small Molecules For Endothelial Cell Activation - The present invention provides small molecules for endothelial cell activation and compositions thereof and methods of making and using the same. | 11-21-2013 |
20130317057 | ALDOSTERONE SYNTHASE INHIBITORS - The invention involves compounds of structural Formula (I) and the pharmaceutically acceptable salts thereof. The compounds of the invention are effective at selectively inhibiting CYP11B2, and are therefore useful for the treatment or prophylaxis of disorders that are associated with elevated aldosterone levels, including, but not limited to, hypertension and heart failure. | 11-28-2013 |
20130338184 | 2-AMINO-NAPHTHYRIDINE DERIVATIVES - The invention in one embodiment is directed to a compound of Formula A: | 12-19-2013 |
20130345254 | CYCLOHEXANE SUBSTITUTED AMINO CYCLOPENTANE DERIVATIVES AS USEFUL CCR2 ANTAGONISTS - Disclosed are the CCR2 antagonists of Formula I: I or pharmaceutically acceptable salts thereof, wherein A, B, R, and R6 are as defined herein. Also disclosed are pharmaceutical compositions containing the compounds, methods of treatment using the compounds, and compositions to treat diseases or disorders associated with CCR2 activity. | 12-26-2013 |
20140024671 | COMPOSITIONS AND METHODS FOR INHIBITING CYTOCHROME P450 - Methods of inhibiting cytochrome P450 enzymes are provided that can be used for improving the treatment of diseases by preventing degradation of drugs or other molecules by cytochrome P450. Pharmaceutical compositions are provided that can act as boosters to improve the pharmacokinetics, enhance the bioavailability, and enhance the therapeutic effect of drugs that undergo in vivo degradation by cytochrome P450 enzymes. | 01-23-2014 |
20140024672 | AZAINDOLE DERIVATIVES AS CFTR MODULATORS - The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators. | 01-23-2014 |
20140031383 | METHODS FOR TREATMENT OF MELANOMA - The present invention is directed to methods for treatment of melanoma using an inhibitor of dihydroorotate dehydrogenase (DHODH) and to combination therapies that involve administering to a subject an inhibitor of oncogenic BRAF (e.g. BRAF(V600E)), as well as an inhibitor of dihydroorotate dehydrogenase (DHODH). Assays for identifying compounds useful for the treatment of melanoma are also provided. The methods herein are directed to screening for compounds or agents that inhibit neural crest progenitor formation in a zebra fish model of melanoma. | 01-30-2014 |
20140031384 | THERAPEUTIC AGENT FOR TUMOR - A therapeutic agent for tumor for combined use of a compound or pharmaceutically acceptable salt thereof represented by Formula (I) and a compound represented by Formula (II): | 01-30-2014 |
20140039002 | SOLID FORMS OF A PHARMACEUTICALLY ACTIVE SUBSTANCE - The present invention provides solid forms of the compound of formula 1 and pharmaceutical uses thereof. (I) | 02-06-2014 |
20140039003 | TREATMENT OF GLAUCOMA - A method is provided for treating patients suffering from elevated intraocular pressure or fluctuation in intraocular pressure, including for example glaucoma patients. The method comprises administering to the patient an inhibitor of orexin activity in an amount sufficient to reduce intraocular pressure or intraocular pressure fluctuation in one or both eyes of the patient. | 02-06-2014 |
20140045883 | ACK1 KINASE INHIBITION TO TREAT TRIPLE NEGATIVE BREAST CANCER - Compositions and methods are disclosed for treating Triple Negative Breast Cancers (TNBCs). The methods involve administering to a subject with TNBC a composition containing an Ack1 kinase inhibitor. In some embodiments, the method involves first assaying a sample from the subject for Tyr176-phosphorylated-AKT and/or Tyr284-phosphorylated-Ack1. In these embodiments, detection of the phosphorylated AKT and/or Ack1 is an indication that the subject is a suitable candidate for treatment with the Ack1 kinase inhibitor. | 02-13-2014 |
20140051720 | N-Cyclobutyl - Imidazopyridine - Methylamine As TRPV1 Antagonists - A compound of formula (I) | 02-20-2014 |
20140073666 | COMPOSITIONS AND METHODS FOR TREATMENT - The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the treatment of LFA-1 mediated diseases. One aspect of the invention provides for diagnosis of an LFA-1 mediated disease and administration of a LFA-1 antagonist, after the patient is diagnosed with a LFA-1 mediated disease. In some embodiments, the LFA-1 mediated diseases treated are dry eye disorders. Also provided herein are methods for identifying compounds which are LFA-1 antagonists. | 03-13-2014 |
20140094488 | 2-AMINO-3-(IMIDAZOL-2-YL)-PYRIDIN-4-ONE DERIVATIVES AND THEIR USE AS VEGF RECEPTOR KINASE INHIBITORS - The invention relates to the compounds of general formula (I): Preparation process and therapeutic use. | 04-03-2014 |
20140100243 | SUBSTITUTED 4-ARYL-1,4-DIHYDRO-1,6-NAPHTHYRIDINE AMIDES AND THEIR USE - The present application relates to novel substituted 4-aryl-1,4-dihydro-1,6-naphthyridine-3-carboxamides, a process for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially cardiovascular disorders. | 04-10-2014 |
20140113931 | SUBSTITUTED PICOLINAMIDE KINASE INHIBITORS - Provided are picolinamide compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibiting Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity. | 04-24-2014 |
20140121235 | Method for Treating S6K-Overexpressing Cancers - Disclosed herein are methods for treating an S6K-overexpressing cancer, comprising administering a therapeutically effective amount of leflunomide to a subject in need thereof. | 05-01-2014 |
20140121236 | Compositions and Methods for Treating Myotonic Dystrophy Type 1 - Disclosed is a compound for treatment of Myotonic Dystrophy type 1 having the formula: | 05-01-2014 |
20140128424 | Hydroxy-substituted imidazo[1,2-a]-pyridinecarboxamides and their use - The present application relates to novel substituted imidazo[1,2-a]pyridine-3-carboxamides, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders. | 05-08-2014 |
20140128425 | Carboxy-substituted imidazo[1,2-a]pyridinecarboxamides and their use - The present application relates to novel substituted imidazo[1,2-a]pyridine-3-carboxamides, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders. | 05-08-2014 |
20140128426 | 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 | 05-08-2014 |
20140142135 | 4-DIMETHYLAMINO-PHENYL-SUBSTITUTED NAPHTHYRIDINES, AND USE THEREOF AS MEDICAMENTS - The invention relates to new substituted naphthyridines of formula 1, as well as pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates or solvates thereof, | 05-22-2014 |
20140163061 | Methods For Reducing Blood Pressure - The present invention provides methods and medicaments for reducing blood pressure. Methods and medicaments for treating or preventing hypertension are also provided. | 06-12-2014 |
20140171463 | 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). | 06-19-2014 |
20140179733 | DIAZOLE AMIDES - Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are diazole lactam derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated disease, and as controls in assays for the identification of competitive CCR1 antagonists. | 06-26-2014 |
20140187576 | SALT OF NAPHTHYRIDINE CARBOXYLIC ACID DERIVATIVE - 7-(3-Aminomethyl-4-methoxyiminopyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid methanesulfonate and hydrates thereof, processes for their preparation, pharmaceutical compositions comprising them, and their use in antibacterial therapy. | 07-03-2014 |
20140200239 | AGONISTS OF SRC HOMOLOGY-2 CONTAINING PROTEIN TYROSINE PHOSPHATASE-1 AND TREATMENT METHODS USING THE SAME - The present invention provides new compounds of formula I, II or III, which have Src homology-2 containing protein tyrosine phosphatase-1 (SHP-1) agonist activity. Also provided are treatment methods using the compounds of formula I, II or III. | 07-17-2014 |
20140206715 | PREPARATION AND USE OF COMPOUNDS AS PROTEASE INHIBITORS - Disclosed are compounds of the formula I | 07-24-2014 |
20140221420 | CCR5 ANTAGONISTS FOR TREATING HIV - Compounds that modulate the CCR5 chemokine receptor, pharmaceutical compositions containing them, and uses therefor in the treatment of HIV and related diseases are described. | 08-07-2014 |
20140221421 | THERAPEUTIC COMPOUNDS - Compounds of formula I: | 08-07-2014 |
20140235666 | IMIDAZOPYRIDINE DERIVATIVES WHICH INHIBIT THE SECRETION OF GASTRIC ACID - The present invention relates to substituted imidazo [1,2-a]pyridines of formula I where R is —CH | 08-21-2014 |
20140235667 | IMIDAZOPYRIDYL COMPOUNDS AS ALDOSTERONE SYNTHASE INHIBITORS - This invention relates to imidazopyridyl compounds of the structural formula: I or their pharmaceutically acceptable salts, wherein the variable are defined herein. The inventive compounds selectively inhibit aldosterone synthase. This invention also provides for pharmaceutical compositions comprising the compounds of Formula I or their salts as well as potentially to methods for the treatment, amelioration or prevention of conditions that could be treated by inhibiting aldosterone synthase. | 08-21-2014 |
20140243365 | 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. | 08-28-2014 |
20140249177 | SALT FORMS OF BICYCLIC HETEROCYCLIC DERIVATIVES - The present invention provides novel solid forms of pharmaceutically active agents and therapeutic uses thereof. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition. | 09-04-2014 |
20140249178 | COMPOSITIONS AND METHODS FOR TREATING VIRAL DISEASES - Substituted perhydro pyrrolopyridines and methods for their use in the treatment of HIV infections, AIDS, and AIDS-related diseases, and in the treatment of BVDV infections are described herein. Also, pharmaceutical compositions comprising the substituted perhydro pyrrolopyridines are useful for the treatment of HIV infections, AIDS, and AIDS-related diseases. The compositions include one or more carriers, diluents, or excipients, or a combination thereof. | 09-04-2014 |
20140256768 | HETEROCYCLIC MOLECULES AS APOPTOSIS INDUCERS - The present document describes novel compounds which may inhibit the activity of anti-apoptotic proteins such as Bcl-2 family protein members, compositions containing the compounds and methods of treating diseases involving a defect in apoptosis, such as, for example, in the treatment of cancer. | 09-11-2014 |
20140275152 | Compounds and uses thereof for the modulation of hemoglobin - Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation. | 09-18-2014 |
20140275153 | CDK9 KINASE INHIBITORS - Disclosed are compound of Formula (Ia), | 09-18-2014 |
20140288116 | Classification and Actionability Indices for Lung Cancer - The disclosure provides compositions, kits, and methods for detecting a plurality of genes and associated variants in a sample from a subject with lung cancer. The compositions, kits, and methods include a set of oligonucleotides, typically primers and/or probes that can hybridize to identify a gene variant. The methods disclosed herein provide for a mutation status of a tumor to be determined and subsequently associated with an actionable treatment recommendation. | 09-25-2014 |
20140296283 | Substituted 6,5-Fused Bicyclic Heteroaryl Compounds - The present invention relates to azole 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. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes. | 10-02-2014 |
20140309254 | PYRROLOPYRIDINE DERIVATIVES AND THEIR USE AS CRTH2 ANTAGONISTS - There are provided according to the invention compounds of formula (I) | 10-16-2014 |
20140315944 | SUBSTITUTED NAPHTHYRIDINE AND QUINOLINE COMPOUNDS AS MAO INHIBITORS - The invention provides a chemical entity of Formula (I) | 10-23-2014 |
20140315945 | Substituted Benzene Compounds - The present invention relates to azole 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. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes. | 10-23-2014 |
20140329850 | APOPTOSIS SIGNAL-REGULATING KINASE 1 INHIBITORS - The present invention relates to apoptosis signal-regulating kinase 1 (“ASK1”) inhibiting compounds of the formula | 11-06-2014 |
20140371261 | INDOMETHACIN ANALOGS FOR THE TREATMENT OF CASTRATE-RESISTANT PROSTATE CANCER - Provided are compositions for inhibiting a biological activity of an aldoketo reductase family 1, member C3 (AKR1 C3) polypeptide. In some embodiments, the compositions are indomethacin derivatives that are AKR1 C3-specific inhibitors. Also provided are methods for producing disclosed indomethacin derivatives that substantially lack cyclooxygenase inhibitory activity but that have AKR1C3 inhibitory activity, methods for inhibiting AKR1C3 polypeptide biological activities, and methods for treating prostate tumors in subjects. | 12-18-2014 |
20140378505 | SNS-595 AND METHODS OF USING THE SAME - The present invention relates to SNS-595 and of treating cancer using the same. | 12-25-2014 |
20150011580 | 1H-Pyrrolo [2, 3 -B] Pyridine Derivatives and Their Use as Radical Quenchers - The present disclosure provides biologically active compounds of formula (I): and pharmaceutically acceptable salts thereof, compositions comprising these compounds, and methods of using these compounds in a variety of applications, such as treatment or suppression of diseases associated with decreased mitochondrial function resulting in diminished ATP production and/or oxidative stress and/or lipid peroxidation. | 01-08-2015 |
20150011581 | 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). | 01-08-2015 |
20150011582 | Carboxamide Compounds and Methods for Using the Same - Disclosed are carboxamide compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure | 01-08-2015 |
20150018384 | TREATMENT FOR HIGH CHOLESTEROL - The present invention provides a method for treatment of high cholesterol by reducing low density lipoprotein cholesterol (LDL-C) and/or very low density Opoproiein cholesterol (VLDL-C) in subjects In need thereof by administering a compound that inhibits HIF hydroxylase activity. The method is useful, for reducing LDL cholesterol levels and total cholesterol levels even In subjects already undergoing treatment with other cholesterol-lowering medications, for example statins, fibrates, nicotinic acids and bile acid-binding resins, and in patients having chronic kidney disease or end stage renal disease, inter alia. | 01-15-2015 |
20150045385 | BRAIN FUNCTION IMPROVING AGENT - The present invention provides a pharmaceutical composition used in improving brain function including a compound of formula (I). | 02-12-2015 |
20150057307 | NOVEL MODULATORS OF SPHINGOSINE PHOSPHATE RECEPTORS - Compounds that activate a sphingosine-1-phosphate receptor of the subtype 1 are provided. Certain compounds selectively activate the receptor subtype 1 in relation to the sphinogosine-1-phosphate receptor subtype 3. Uses and methods of inventive compounds for treatment of malconditions wherein activation, agonism, inhibition or antagonism of the S1P1 is medically indicated are provided. | 02-26-2015 |
20150057308 | Fluorinated 3-(2-Oxo-3-(3-Arylpropyl)Imidazolidin-1-yl)-3-Arylpropanoic Acid Derivatives - The invention relates to fluorinated compounds and their use as integrin receptor antagonists. Novel fluorinated 3-(2-oxo-3-(3 -arylpropyl)imidazolidin-1-yl)-3 -arylpropanoic acid derivatives and pharmaceutically acceptable salts or solvates thereof and their use are described. | 02-26-2015 |
20150073011 | Beta-Lactamase Inhibitor Compounds - The present invention is directed to compounds which are beta-lacatamase inhibitors. The compounds and their pharmaceutically acceptable salts, are useful in combination with beta-lactam antibiotics, or alone, for the treatment of bacterial infections, including infections caused by drug resistant organisms, including multi-drug resistant organisms. The present invention includes compounds according to formula (Ia): | 03-12-2015 |
20150094327 | COMPOSITIONS AND METHODS FOR INHIBITING RESOLVASES - The invention provides a fluorescence polarization (FP)-based assay to identify inhibitors of resolvase's DNA cleavage activity. The invention also provides resolvase inhibitors identified by the assay, as well as derivatives and analogs thereof. In certain embodiments, the compounds of the invention are useful to treat a poxvirus infection in an infected subject. | 04-02-2015 |
20150094328 | 4-Azaindole Derivatives - 4-Azaindole derivatives which are modulators of muscarinic acetylcholine receptor (mAChR) M1 and which may be effective for the prevention or disease modifying or symptomatic treatment of cognitive deficits associated with neurological disorders such as Alzheimer-type dementia (AD) or dementia with Lewy bodies (DLB), and a pharmaceutical composition comprising a 4-azaindole derivative as an active ingredient. | 04-02-2015 |
20150099777 | HETEROCYCLIC COMPOUND - A compound having an SSTR5 antagonist action and use of the compound as a medicament are provided. Specifically, a compound represented by the following formula: | 04-09-2015 |
20150105418 | SUBSTITUTED HYDROXAMIC ACIDS AND USES THEREOF - This invention provides compounds of formula (I): | 04-16-2015 |
20150133489 | COMPACTED MOXIFLOXACIN - The invention relates to a process for the preparation of tablets containing moxifloxacin, comprising the steps of (i) providing moxifloxacin, pharmaceutically acceptable salts, solvates or hydrates thereof, optionally mixed with one or more pharmaceutical excipients; (ii) compacting it into a slug; (iii) granulating the slug; and (iv) compressing the resulting granules into tablets; and also tablets, granules and compacted material containing compacted moxifloxacin. | 05-14-2015 |
20150148372 | 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 |
20150290177 | COMPOSITIONS FOR DELIVERING HYPNOTIC AGENTS ACROSS THE ORAL MUCOSA AND METHODS OF USE THEREOF - The present invention provides novel compositions for the delivery of a hypnotic agent across the oral mucosa. In particular, the buffer system in the compositions of the present invention raises the pH of saliva to a pH greater than about 7.8, thereby facilitating the substantially complete conversion of the hypnotic agent from its ionized to its un-ionized form. As a result, the dose of hypnotic agent is rapidly and efficiently absorbed by the oral mucosa with surprisingly low inter-subject variability. Furthermore, delivery of the hypnotic agent across the oral mucosa advantageously bypasses hepatic first pass metabolism of the drug and avoids enzymatic degradation of the drug within the gastrointestinal tract. Methods for using the compositions of the present invention for treating sleep disorders such as insomnia are also provided. | 10-15-2015 |
20150291585 | SALT OF NAPHTHYRIDINE CARBOXYLIC ACID DERIVATIVE - 7-(3-Aminomethyl-4-methoxyiminopyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid methanesulfonate and hydrates thereof, processes for their preparation, pharmaceutical compositions comprising them, and their use in antibacterial therapy. | 10-15-2015 |
20150297577 | METHODS AND COMPOSITIONS FOR TARGETING CANCER STEM CELLS - The present invention relates to chemical compounds, methods for their discovery, and their therapeutic and research use. In particular, the present invention provides compounds as therapeutic agents against cancer stem cells. | 10-22-2015 |
20150299152 | GLUTAMASE INHIBITORS AND METHOD OF USE - Compounds and compositions comprising compounds that inhibit glutaminase are described herein. Also described herein are methods of using the compounds that inhibit glutaminase in the treatment of cancer. | 10-22-2015 |
20150306070 | USE OF MALEIMIDE DERIVATIVES FOR PREVENTING AND TREATING LEUKEMIA - The present invention is related to a compound of formula (I): a pharmaceutically acceptable salt thereof, a hydrate thereof, a solvate thereof, a metabolite thereof or a prodrug thereof; for use in a method for the treatment and/or prevention of leukemia, wherein X is selected from the group consisting of N—R | 10-29-2015 |
20150306077 | Novel Compositions and Methods for Treating Cancer - Provided herein are methods and compositions inter alia for treating diseases, including hyperproliferative diseases, migraine headaches, and depression. | 10-29-2015 |
20150306080 | METHODS FOR TREATMENT OF MELANOMA - Embodiments of the present invention are directed to methods for treatment of melanoma using an inhibitor of dihydroorotate dehydrogenase (DHODH) and to combination therapies that involve administering to a subject an inhibitor of oncogenic BRAF (e.g. BRAF(V600E)), as well as an inhibitor of dihydroorotate dehydrogenase (DHODH). Assays for identifying compounds useful for the treatment of melanoma are also provided. The methods comprise screening for compounds or agents that inhibit neural crest progenitor formation in a zebra fish model of melanoma. | 10-29-2015 |
20150306219 | SMALL MOLECULE INHIBITORS OF POLYNUCLEOTIDE KINASE/PHOSPHATASE, POLY(ADP-RIBOSE) POLYMERASE AND USES THEREOF - The present invention generally relates to use of compounds and compositions as a chemosensitizers and/or radiosensitizers and/or inhibitors of PNKP phosphatase activity. The present invention provides pharmaceutical combinations and/or a pharmaceutically acceptable salt thereof, kits containing such compounds and/composition and methods of using such compounds and/or compositions. | 10-29-2015 |
20150307485 | 3 -AMINO- PYRAZOLE DERIVATIVES USEFUL AGAINST TUBERCULOSIS - A compound of Formula (I) or a pharmaceutically acceptable salt thereof: | 10-29-2015 |
20150307492 | 3,5-Diarylazaindoles as DYRK1A Protein Inhibitors for the Treatment of Cognitive Deficiencies Associated with Down's Syndrome and with Alzheimer's Disease - The present invention relates to a compound of formula (I′) or a pharmaceutically acceptable salt, solvate or hydrate thereof, in which: X | 10-29-2015 |
20150320729 | PHARMACEUTICAL COMPOSITION COMPRISING BICYCLIC PYRIDINOL DERIVATIVES FOR PREVENTING OR TREATING DISEASES CAUSED BY ANGIOGENESIS - Disclosed is a pharmaceutical composition including a bicyclic pyridinol derivative as an active ingredient for preventing or treating diseases caused by angiogenesis. The bicyclic pyridinol derivative expressed by Chemical Formula 1 can be effectively used as a drug for preventing and treating diseases caused by angiogenesis since it inhibits neovascularization in a chorioallantoic membrane model. | 11-12-2015 |
20150328205 | 2-AMINO-3-(IMIDAZOL-2-YL)-PYRIDIN-4-ONE DERIVATIVES AND THEIR USE AS VEGF RECEPTOR KINASE INHIBITORS - The invention relates to the compounds of general formula (I): Preparation process and therapeutic use. | 11-19-2015 |
20150336948 | Isotopically Labeled Biaryl Urea Compounds - The present invention is directed to isotopically labeled biaryl urea compounds which possess high affinity to neurofibrillary tangles (NFTs), and thus are useful to determine the amount and distribution of NFTs in brain. The isotopically labeled biaryl urea compounds may also be useful as PET tracers and in competition assays to identify other compounds that may serve as PET tracers. | 11-26-2015 |
20150336956 | AZAINDOLE DERIVATIVES AS CFTR MODULATORS - The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators. | 11-26-2015 |
20150344472 | SUBSTITUTED BENZALDEHYDE COMPOUNDS AND METHODS FOR THEIR USE IN INCREASING TISSUE OXYGENATION - Provided are substituted benzaldehydes and derivatives thereof that act as allosteric modulators of hemoglobin, methods and intermediates for their preparation, pharmaceutical compositions comprising the modulators, and methods for their use in treating disorders mediate by hemoglobin and disorders that would benefit from increased tissue oxygenation. | 12-03-2015 |
20150352084 | COMPOSITIONS AND METHODS FOR TREATING MIDDLE-OF-THE-NIGHT INSOMNIA - The present invention provides liquid dosage forms for treating narcolepsy. The liquid dosage form includes zolpidem or a pharmaceutically acceptable salt thereof, a carbonate salt, a metal oxide, and a borate salt. The present invention also provides methods for treating somnambulism. The methods include administering an emulsion that includes zolpidem, a bicarbonate salt, a citrate salt, and a phosphate salt. | 12-10-2015 |
20150352086 | HEAT SHOCK PROTEIN (HSP) INHIBITION AND MONITORING EFFECTIVENESS THEREOF - Provided herein are methods of treating a BRAF inhibitor resistant cancer in a subject. Also provided are methods of monitoring or evaluating the treatment of a cancer in a subject. Further provided are methods of diagnosing a cancer or disease associated with antibody production in a subject. | 12-10-2015 |
20150366847 | COMBINATION OF GERANYLGERANYLACETONE AND IBUDILAST AND METHODS OF USING SAME - The present invention relates generally to methods for treating progressive neurodegenerative diseases, including their progressive forms. In particular, the present invention pertains to methods of treating or preventing progressive neurodegenerative diseases and its associated symptoms by administration of a combination of geranylgeranylacetone (teprenone) and ibudilast (3-isobutyryl-2-isopropylpyrazolo[1,5-a]pyridine), or pharmaceutically acceptable salts thereof. | 12-24-2015 |
20150374674 | R-7-(3-AMINOMETHYL-4-METHOXYIMINO-3-METHYL-PYRROLIDIN-1-YL)-1-CYCLOPROPYL-- 6-FLUORO-4-OXO-1,4-DIHYDRO-[1,8]NAPHTHYRIDINE-3-CARBOXYLIC ACID AND L-ASPARTIC ACID SALT, PROCESS FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME FOR ANTIMICROBIAL - Disclosed herein are R-7-(3-aminomethyl-4-methoxyimino-3-methyl-pyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-[1,8]naphthyridine-3-carboxylic acid and L-aspartic acid salt, process for the preparation thereof and pharmaceutical composition comprising the same for antimicrobial. Because the R-7-(3-aminomethyl-4-methoxyimino-3-methyl-pyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-[1,8]naphthyridine-3-carboxylic acid and L-aspartic acid salt is more soluble and less toxic and has less side effects as an antimicrobial agent than hydrochloride and the other salts (D-aspartate and phosphate) conventionally used, the salt may be useful for oral and injectable administration. | 12-31-2015 |
20150376182 | Substituted Acetylene Derivatives and their Use as Positive Allosteric Modulators of mGluR4 - The present invention relates to novel acetylene derivatives as positive allosteric modulators for modulating metabotropic glutamate receptor subtype 4 (mGluR4) and/or altering glutamate level or glutamatergic signalling. | 12-31-2015 |
20150376183 | IP Receptor Agonist Heterocyclic Compounds - The present invention provides heterocyclic derivatives which activate the IP receptor. Activating the IP receptor signaling pathway is useful to treat many forms of PAH, pulmonary fibrosis and exert beneficial effects in fibrotic conditions of various organs in animal models and in patients. Pharmaceutical compositions comprising such derivatives are also encompassed. | 12-31-2015 |
20160000771 | Inhibitors of Human Immunodeficiency Virus Replication - The disclosure generally relates to compounds of formula (I), including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection. | 01-07-2016 |
20160002172 | PHENYLPYRAZOLE DERIVATIVES AS POTENT ROCK1 AND ROCK2 INHIBITORS - The present invention provides compounds of Formula (I): (I) or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same. | 01-07-2016 |
20160009716 | 2 - (AZAINDOL-2-YL) BENZ IMIDAZOLES AS PAD4 INHIBITORS | 01-14-2016 |
20160015688 | COMPOUNDS FOR TREATMENT OF CANCER - The present invention relates to pharmaceutical compositions for treating cancer comprising BRAF inhibitors, (e.g. vemurafenib) and/or MEK inhibitor, (e.g. trametinib, RO5068760), in combination with anti-tubulin compounds of the invention or other known tubulin inhibitors, and using such compositions for treating cancer such as melanoma, drug-resistant cancer, and cancer metastasis. | 01-21-2016 |
20160016895 | ANTIBACTERIAL AGENTS - Antibacterial compounds of formula (I) are provided: | 01-21-2016 |
20160016932 | 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. | 01-21-2016 |
20160016950 | SOLID STATE FORMS OF VEMURAFENIB HYDROCHLORIDE - Provided herein are solid state forms of Vemurafenib hydrochloride, processes for preparing the solid state forms, as well as pharmaceutical compositions and formulations comprising said solid state forms. | 01-21-2016 |
20160022666 | Systems and Methods for Treating Ear Disorders and Formulations Therefor - An apparatus for insertion in an ear is provided and includes a drug delivery device for insertion into an external auditory canal, wherein the drug delivery device contains one or more pharmaceutically active agents that can be released from the drug delivery device into the external auditory canal and onto the tympanic membrane to treat ear disorders. In more particular instances, the drug delivery device can conform to the profile of the external auditory canal. Formulations of agents for the drug delivery device are also provided. | 01-28-2016 |
20160024081 | Substituted 6,5-Fused Bicyclic Heteroaryl Compounds - The present invention relates to azole 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. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes. | 01-28-2016 |
20160024589 | METHODS OF IDENTIFYING RESPONSES TO MAP KINASE INHIBITION THERAPY - The invention provides methods and devices for determining molecular signatures in a cancer that predict response to a MARPK pathway inhibitor and methods of use of such signatures. | 01-28-2016 |
20160030404 | Therapeutic Agents and Methods for the Treatment of DNA Repair Deficiency Disorders - The present invention provides compounds, compositions, its, and methods which are effective for mitigating, treating, or ameliorating a DNA repair-deficiency disorder or a symptom of a DNA repair-deficiency disorder. The compounds, compositions, kits, and methods are also effective for modulating a level or activity of a DNA repair enzyme or a level or activity of gene encoding a DNA repair enzyme. | 02-04-2016 |
20160031882 | IMIDAZOPYRIDYL COMPOUNDS AS ALDOSTERONE SYNTHASE INHIBITORS - This invention relates to imidazopyridyl compounds of the structural formula: | 02-04-2016 |
20160031907 | Substituted Benzene Compounds - The present invention relates to compounds of Formula (I), wherein the variables are as defined herein. Pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof are disclosed. | 02-04-2016 |
20160067224 | THERAPEUTIC COMPOUNDS - Compounds of formula I: | 03-10-2016 |
20160068530 | SOLID STATE FORMS OF VEMURAFENIB AND VEMURAFENIB SALTS - The present invention provides Vemurafenib salts, particularly Vemurafenib esylate and Vemurafenib choline, and solid state forms thereof and processes for preparing these compounds. The present invention also provides the use of the solid state forms of Vemurafenib and of the Vemurafenib salts for preparing Vemurafenib or other Vemurafenib salts, and solid state forms thereof. | 03-10-2016 |
20160074377 | SUBSTITUTED NAPHTHYRIDINE AND QUINOLINE COMPOUNDS AS MAO INHIBITORS - The invention provides a chemical entity of Formula (I) | 03-17-2016 |
20160108033 | HISTONE DEMETHYLASE INHIBITORS - The present invention relates generally to compositions and methods for treating cancer and neoplastic diseases. Provided herein are substituted imidazole-pyridine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of histone demethylase enzymes. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as pancreatic cancer, prostate cancer, breast cancer, bladder cancer, lung cancer, gastric cancer, leukemia and/or melanoma and the like. | 04-21-2016 |
20160108041 | SUBSTITUTED PYRIDINONE COMPOUNDS AS MEK INHIBITORS - The invention provides novel substituted heterocyclic compounds represented by Formula I and Formula II, or a pharmaceutically acceptable salt, solvate, polymorph, ester, tautomer or prodrug thereof, and a composition comprising these compounds. The compounds provided can be used as inhibitors of MEK and are useful in the treatment of inflammatory diseases, cancer and other hyperproliferative diseases. The invention further provides a method of treatment for inflammatory diseases, cancer and other hyperproliferative diseases in mammals, especially humans. | 04-21-2016 |
20160122345 | DIHYDROPYRROLOPYRIDINE INHIBITORS OF ROR-GAMMA - Provided are novel compounds of Formula (I): | 05-05-2016 |
20160130269 | 7-AZAINDOLE DERIVATIVES - Compounds of the formula (I) in which R, R | 05-12-2016 |
20160152613 | SUBSTITUTED OXOPYRIDINE DERIVATIVES AND USE THEREOF AS FACTOR XIA/PLASMA | 06-02-2016 |
20160176824 | 1,3-DISUBSTITUTED CYCLOPENTANE DERIVATIVES | 06-23-2016 |
20160176869 | Solid State Forms of Fused Heteroaromatic Pyrrolidinones | 06-23-2016 |
20160176872 | HETEROCYCLIC COMPOUND | 06-23-2016 |
20160176873 | HETEROCYCLIC COMPOUND | 06-23-2016 |
20160185773 | BICYCLIC INHIBITORS - The present invention provides compounds of formula (I): compositions comprising such compounds; the use of such compounds in therapy (for example in the treatment or prevention of a disease or condition in which plasma kallikrein activity is implicated); and methods of treating patients with such compounds; wherein A, B, W, X and Y are as defined herein. | 06-30-2016 |
20160193185 | DIAZOLE AMIDES | 07-07-2016 |
20160194315 | HISTONE DEMETHYLASE INHIBITORS | 07-07-2016 |
20160194320 | HETEROCYCLIC COMPOUNDS AND THEIR USE AS GLYCOGEN SYNTHASE KINASE-3 INHIBITORS | 07-07-2016 |
20160194321 | PYRROLOPYRIDINE OR PYRAZOLOPYRIDINE DERIVATIVES | 07-07-2016 |
20170233390 | Methyl- and Trifluoromethyl-Substituted Pyrrolopyridine Modulators of RORC2 and Methods of Use Thereof | 08-17-2017 |
20180022699 | ARYL SUBSTITUTED INDOLES AND THE USE THEREOF | 01-25-2018 |
20190144387 | SELECTIVE ANDROGEN RECEPTOR DEGRADER (SARD) LIGANDS AND METHODS OF USE THEREOF | 05-16-2019 |
20220133701 | METHODS OF TREATING PAIN - Methods of treating pain are provided. Accordingly, there is provided a method of treating nociceptive or neuropathic pain in a subject in need thereof, the method comprising administering to the subject a therapeutically effective amount of an agent which binds importin alpha3 or a polynucleotide encoding same and inhibits expression and/or activity of said importin α3. | 05-05-2022 |
20220136057 | METHODS OF IDENTIFYING RESPONSES TO MAP KINASE INHIBITION THERAPY - The invention provides methods and devices for determining molecular signatures in a cancer that predict response to a MARPK pathway inhibitor and methods of use of such signatures. | 05-05-2022 |