Entries |
Document | Title | Date |
20080200455 | 1-Aryl- or 1-Alkylsulfonyl-Heterocyclylbenzazoles As 5-Hydroxytryptamine-6 Ligands - The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of disorders related to or affected by the 5-HT6 receptor. | 08-21-2008 |
20080200456 | Substituted 8-Heteroaryl Xanthines - The present invention provides compounds and pharmaceutical compositions that are selective antagonists of A | 08-21-2008 |
20080207597 | HOMOPIPERAZINE COMPOUNDS THAT INHIBIT RIBOSOMAL FRAMESHIFTING BY BINDING TO RNA PSEUDOKNOT STRUCTURE OF SARS CORONAVIRUS - Provided is a homopiperazine compound for inhibiting ribosomal frameshifting by binding to an RNA pseudoknot structure of SARS coronavirus. Particularly, the present invention provides a pharmaceutical composition for inhibiting synthesis of protein induced by −1 frameshifting by binding to an RNA pseudoknot structure specifically existing in SARS coronavirus. The composition includes a therapeutically effective amount of homopiperazine compound of following chemical formula 1 or a pharmaceutically accepted salt thereof, and a pharmaceutically accepted carrier or excipient. | 08-28-2008 |
20080207598 | INDOLE DERIVATIVES - The invention relates to indole derivative having the general Formula I | 08-28-2008 |
20080221085 | Nicotinic Receptor Agonists for the Treatment of Inflammatory Diseases - Nicotine receptor agonists or analogs or derivatives thereof for treating inflammatory pulmonary diseases, and pharmaceutical compositions including nicotine receptor agonists or analogs or derivatives thereof. Compounds of formula wherein R1, R2, Xa and Ya are as defined herein are also provided. | 09-11-2008 |
20080221086 | Novel Inhibitors of Glutaminyl Cyclase - The present invention relates to compounds of formula (I), combinations and uses thereof for disease therapy, | 09-11-2008 |
20080234253 | Methods and Compositons for Stimulating Neurogenesis and Inhibiting Neuronal Degeneration - The present invention provides methods and compositions comprising compounds useful for stimulating neurogenesis. The methods and compositions comprising compounds are also useful for inhibiting neuronal degeneration. Thus, the present invention can be used in the treatment of diseases and conditions characterized by neuronal loss and reduced neurogenesis including Alzheimer's disease, stroke, traumatic brain injury, and depression. This invention could also be used for research products including single agents or mixtures of agents to promote, proliferate, differentiate, or maintain neurons from stem or progenitor cells. | 09-25-2008 |
20080242660 | Therapeutic Agent for Vasospasm Accompanying Bypass Operation - An agent and composition for the prevention of and/or treatment for vasospasm accompanying a bypass operation, which contains as an active ingredient either a compound represented by the following general formula (I) or an acid addition salt or hydrate thereof. R | 10-02-2008 |
20080242661 | Novel compounds useful for the treatment of degenerative & inflammatory diseases - The present invention relates to compounds that are inhibitors of PDE1A, a phosphodiesterase that is involved in the modulation of the degradation of cartilage, joint degeneration and diseases involving such degradation and/or inflammation. | 10-02-2008 |
20080249081 | COMPOUNDS FOR THE TREATMENT OF PAIN AND SCREENING METHODS THEREFOR - Disclosed herein are benzoimidazole compounds; pharmaceutical compositions comprising a therapeutically effective amount of the same; methods of modulating the activity of an MrgX1 or an MrgX2 receptor using the same; and methods of alleviating acute, chronic and neuropathic pain in a subject using the same. Also disclosed are methods of identifying a benzoimidazole compound that modulates the activity of an MrgX1 or an MrgX2 receptor; methods of identifying a benzoimidazole compound effective for the treatment of pain. | 10-09-2008 |
20080261956 | Substituted Phenols as Active Agents Inhibiting Vegf Production - The present invention relates to methods, compounds, and compositions for inhibiting angiogenesis. More particularly, the present invention relates to methods, compounds, and compositions for inhibiting VEGF production. | 10-23-2008 |
20080275029 | Compounds for Treating Protein-Kinase Mediated Disorders - The invention provides a compound of the formula (I) or a salt, solvate, tautomer or N-oxide thereof for use in the treatment or prophylaxis of a disease state or condition mediated by protein kinase A and/or protein kinase B; | 11-06-2008 |
20080280883 | Muscarinic Receptor Antagonists - This present invention generally relates to muscarinic receptor antagonists which are useful, among other uses, for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. The invention also relates to the process for the preparation of disclosed compounds, pharmaceutical compositions containing the disclosed compounds, and the methods for treating diseases mediated through muscarinic receptors. | 11-13-2008 |
20080300237 | Pharmaceutically Active Diazepanes - Leukocyte Function-Associated Antigen One (LFA-1) is a cell adhesion molecule selectively expressed on leukocytes, and plays a major role in the activation and trafficking of T lymphocytes in the tissue at sites of inflammation. In the last decade a large body of preclinical data has accumulated to establish the importance of LFA-1 as a biological target, 10 particularly in chronic, T-cell driven inflammatory conditions. The present invention provides pharmaceutically active 1,4-diazepan-2-ones of formula I useful for the treatment of conditions related to LFA-1 activity. | 12-04-2008 |
20080306048 | THERAPEUTIC PYRAZOLOQUINOLINE UREA DERIVATIVES - The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABA | 12-11-2008 |
20080306049 | THERAPEUTIC PYRAZOLOQUINOLINE DERIVATIVES - The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABA | 12-11-2008 |
20080312215 | Substituted [1,4]-diazepanes as CXCR3 antagonists and their use in the treatment of inflammatory disorders - CXCR3 inhibitors of formula | 12-18-2008 |
20080312216 | PIPERAZINE AND [1,4]DIAZEPAN DERIVATIVES AS NK ANTAGONISTS - The present invention relates to a compound of formula I | 12-18-2008 |
20080312217 | Organic Compounds - A Compound of formula (I) | 12-18-2008 |
20090005365 | THERAPEUTIC PYRAZOLONAPHTHYRIDINE DERIVATIVES - The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABA | 01-01-2009 |
20090012060 | Antitumor Agent - The present invention provides an antitumor agent and the like, which comprises as an active ingredient, a pyrimidine derivative represented by Formula (I): | 01-08-2009 |
20090012061 | A Method of Treating Cancer - The present invention relates to a method of treating cellular proliferative diseases, in particular cancer, which comprises administering a modulator of the activity of the mitotic kinesin KSP, wherein the activity of the KSP modulator is dependent on the presence of microtubules. It is believed that the KSP modulators utilized in the instant method bind to the KSP protein in a previously unreported manner, since the compounds do not bind competitively with respect to either microtubules or ATP, the substrates of KSP. The modulators useful in the instant methods are furthermore not active against the non-microtubule stimulated activity of KSP. Cellular proliferative diseases that may be treated using the method disclosed herein are, for example cancer, hyperplasias, restenosis, cardiac hypertrophy, immune disorders and inflammation. | 01-08-2009 |
20090012062 | Novel Substituted Pyrazinone Derivatives for Use in Mch-1 Mediated Diseases - The present invention concerns aryl and heteroaryl substituted pyrazinone derivatives having antagonistic melanin-concentrating hormone (MCH) activity, in particular MCH-1 activity according to the general Formula (I) | 01-08-2009 |
20090012063 | Novel imidazole derivatives - The invention is concerned with novel imidazole derivatives of formula (I), | 01-08-2009 |
20090018117 | 2-CARBAMIDE-4-PHENYLTHIAZOLE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF - The disclosure relates to 2-carbamide-4-phenylthiazole derivatives having the following general formula (I): | 01-15-2009 |
20090018118 | HETEROCYCLIC COMPOUNDS - The invention is related to novel substituted diazaheterocycles useful as effective antihypercholesterolemic agents, methods of their preparation, and pharmaceutical compositions containing them. | 01-15-2009 |
20090023711 | Piperazines and Piperidines as Mglur5 Potentiators - Compounds of Formula I or pharmaceutically acceptable salts or solvates thereof: | 01-22-2009 |
20090029970 | PAIN REMEDY CONTAINING ROCK INHIBITOR - Since a ROCK inhibitor exerts a potent analgesic effect by a single dose after the onset of a cartilage-related disease such as osteoarthritis, and can regenerate or suppress destruction of cartilage tissue and alleviate pain associated with cartilage diseases by multiple doses, administration of an therapeutically effective amount of the ROCK inhibitor to a patient with cartilage-related disease such as osteoarthritis or rheumatoid arthritis can treat the patient with cartilage-related disease and the ROCK inhibitor is thus useful. | 01-29-2009 |
20090029971 | SULFONYL-SUBSTITUTED BICYCLIC COMPOUNDS AS MODULATORS OF PPAR - Compounds as modulators of peroxisome proliferator activated receptors, pharmaceutical compositions comprising the same, and methods of treating disease using the same are disclosed. | 01-29-2009 |
20090036430 | PYRIDO(3,2-D)PYRIMIDINES AND PHARMACEUTICAL COMPOSITIONS USEFUL FOR MEDICAL TREATMENT - This invention relates to substituted pyrido(3,2-d)pyrimidine derivatives, their pharmaceutically acceptable salts, N-oxides, solvates, pro-drugs and enantiomers, possessing unexpectedly desirable pharmaceutical properties, in particular which are highly active immunosuppressive agents, and as such are useful in the treatment in transplant rejection and/or in the treatment of certain inflammatory diseases. These derivatives are also useful in preventing or treating cardiovascular disorders, disorders of the central nervous system, TNF-α related disorders, viral diseases (including hepatitis C), erectile dysfunction and cell proliferative disorders. | 02-05-2009 |
20090042865 | DNA-PK INHIBITORS - A compound of formula I: | 02-12-2009 |
20090048237 | COMPOSITIONS AND METHODS FOR PROCEDURAL SEDATION AND ANALGESIA USING ORAL TRANSMUCOSAL DOSAGE FORMS - Dosage forms for procedural sedation and analgesia comprising the combination of an opioid such as sufentanil and a benzodiazepine such as triazolam for administration via the oral transmucosal route and methods for using the same are provided. | 02-19-2009 |
20090048238 | NOVEL BIARYL DERIVATIVES - The invention is concerned with novel biaryl derivatives of formula (I), | 02-19-2009 |
20090054408 | Monocyclic anilide spirolactam cgrp receptor antagonists - The present invention is directed to compounds of Formula I: I (where A | 02-26-2009 |
20090054409 | IMIDAZO [1,2-A] PYRIDINE HAVING ANTI-CELL-PROLIFERATION ACTIVITY - Compounds of formula (I): | 02-26-2009 |
20090054410 | THIADIAZOLE DERIVATIVES FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES - This invention provides specifically substituted 1,2,4-thiadiazole derivatives for use in the treatment of an α-synucleopathy such as Parkinson's disease, diffuse Lewy body disease, traumatic brain injury, amyotrophic lateral sclerosis, Niemann-Pick disease, Hallervorden-Spatz syndrome, Down syndrome, neuroaxonal dystrophy, multiple system atrophy and Alzheimer's disease. This invention also provides various methods for producing such substituted 1,2,4-thiadiazole derivatives. | 02-26-2009 |
20090054411 | 4-ANILINOQUINOLINE-3-CARBOXAMIDES AS CSF-1R KINASE INHIBITORS - The invention relates to chemical compounds of formula IA or IB: | 02-26-2009 |
20090062261 | NITROGEN-CONTAINING HETEROCYCLE DERIVATIVES SUBSTITUTED WITH CYCLIC GROUP - It was found out that the nitrogen-containing heterocyclic derivative represented by the formula (I) specifically binds to a receptor of NR1/NR2B, and is used as a NR2B receptor antagonist. | 03-05-2009 |
20090069301 | Acridine and Quinoline Derivatives as Sirtuin Modulators - Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, chemotherapeutic induced neuropathy, neuropathy associated with an ischemic event, polyglutamine diseases, ocular diseases and/or disorders, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent. | 03-12-2009 |
20090069302 | CHEMICAL COMPOUNDS - The present invention relates generally to novel therapeutic compounds and AXOR 109 agonists, and processes for the manufacture and use of the same. | 03-12-2009 |
20090069303 | PHTHALAZINONE DERIVATIVES - A compound of the formula (I): | 03-12-2009 |
20090069304 | MMP-13 SELECTIVE INHIBITOR - Since it is thought that if the activity of MMP-13 can be inhibited, this will largely contribute to improvement or prevention of progession of pathological states, particularly, osteoarthritis (OA), resulting from or associated with the MMP-13 activity, the development of MMP-13 inhibitors is anticipated. There are provided a compound represented by the general formula (I): | 03-12-2009 |
20090069305 | Substituted nitrogen-containing heteroaryl derivatives useful as modulators of the histamine H4 receptor - The present invention relates to substituted nitrogen-containing heteroaryl derivatives, pharmaceutical compositions containing them, and methods of using any of these derivatives and compositions for H | 03-12-2009 |
20090075981 | INHIBITORS OF p38 - The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders. | 03-19-2009 |
20090075982 | Piperazine compounds - A compound selected from those of formula (I): | 03-19-2009 |
20090082338 | PREVENTIVE OR REMEDY FOR GLAUCOMA - There is provided a preventive for glaucoma or a preventive or a remedy for ocular hypertension, with a potent ocular hypotensive effect and prolonged duration thereof. A preventive or a remedy for glaucoma comprising a Rho kinase inhibitor and an α | 03-26-2009 |
20090082339 | NOVEL AZACYCLYL-SUBSTITUTED ARYLTHIENOPYRIMIDINONES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS MEDICAMENTS - The invention relates to azacyclyl-substituted arylthienopyrimidinones and their derivatives, and their physiologically tolerated salts and physiologically functional derivatives, their preparation, medicaments comprising at least one azacyclyl-substituted arylthienopyrimidinone of the invention or its derivative, and the use of the azacyclyl-substituted arylthienopyrimidinones of the invention and their derivatives as MCH antagonists. | 03-26-2009 |
20090082340 | 3-SUBSTITUTED-5- AND 6-AMINOALKYL INDOLE-2-CARBOXYLIC ACID AMIDES AND RELATED ANALOGS AS INHIBITORS OF CASEIN KINASE I - The present invention discloses and claims methods for the treatment of a patient suffering from a disease or disorder ameliorated by inhibition of casein kinase Iε activity comprising the administration of a compounds of formula (I) and formula (II) | 03-26-2009 |
20090093463 | NOVEL COMPOUNDS OF SUBSTITUTED AND UNSUBTITUTED ADAMANTYL AMIDES - The present invention relates to compounds with the formula (I) or a pharmaceutically acceptable salt thereof: The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and methods of treating a condition that is mediated by the modulation of 11-β-hsd-1, the method comprising administering to a mammal an effective amount of a compound of formula (I). | 04-09-2009 |
20090093464 | Naphthalene Derivatives as Modulators of the Glucocorticoid Receptor - The present invention relates to naphthalene derivatives of formula (I) that are modulators of the glucocorticoid receptor, and to processes for the preparation and use of the same. | 04-09-2009 |
20090093465 | THERAPEUTIC KINASE MODULATORS - The invention relates in part to molecules having certain biological activities that include, but are not limited to, inhibiting cell proliferation, and modulating protein kinase activity. Molecules of the invention can modulate casein kinase (CK) activity. The invention also relates in part to methods for using such molecules. | 04-09-2009 |
20090099156 | Heterocyclic Compounds as Ccr2b antagonists - Compounds of formula (I) Q-L-W—C(═X)-Z-P wherein Q is an amine of the formula —N(R | 04-16-2009 |
20090099157 | TETRAHYDRO-PYRAZOLO-PYRIDINE THIOETHER MODULATORS OF CATHEPSIN S - Tetrahydro-pyrazolo-pyridine thioether compounds are described, which are useful as cathepsin S modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by cathepsin S activity, such as psoriasis, pain, multiple sclerosis, atherosclerosis, and rheumatoid arthritis. | 04-16-2009 |
20090099158 | TETRAHYDROISOQUINOLINE COMPOUNDS AS MODULATORS OF THE HISTAMINE H3 RECEPTOR - Certain substituted tetrahydroisoquinoline compounds are histamine H | 04-16-2009 |
20090111795 | Multimers of Heterocyclic Compounds and Their Use - A compound of formula (I): M-L-M, wherein L is a linker and each M is independently a group of formula (II): is useful in therapy, e.g. of respiratory diseases. | 04-30-2009 |
20090118263 | Novel Adenine Compound - An adenine compound represented by the formula (1): (1) [wherein A | 05-07-2009 |
20090118264 | Medicament having neovascularization promoting action - Methods of use of medicaments having neovascularization promoting action, which medicaments comprise a retinoid antagonist such as 4-(5H-7,8,9,10-tetrahydro-5,7,7,10,10-pentamethylbenzo[e]naphtho[2,3-b][1-,4]diazepin-13-yl)benzoic acid as an active ingredient. | 05-07-2009 |
20090124601 | Tartaric Acid Salts of a Dipeptidyl Peptidase-IV Inhibitor - Tartaric acid salts of (3R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl) butanoyl]hexahydro-3-(2,2,2-trifluoroethyl)-2H-1,4-diazepin-2-one are potent inhibitors of dipeptidyl peptidase-IV and are useful for the prevention and/or treatment of non-insulin dependent diabetes mellitus, also referred to as Type 2 diabetes. The invention also relates to crystalline anhydrate forms of the tartaric acid salts as well as a process for their preparation, pharmaceutical compositions containing these novel forms and methods of use for the treatment of Type 2 diabetes. | 05-14-2009 |
20090124602 | KINASE INHIBITORS - The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions. | 05-14-2009 |
20090124603 | Diazepan Orexin Receptor Antagonists - The present invention is directed to diazepan compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors 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 orexin receptors are involved. | 05-14-2009 |
20090131413 | Thienopyrazole Derivative Having PDE7 Inhibitory Activity - To provide thienopyrazole derivatives inhibiting PDE 7 selectively, and therefore, enhance cellular cAMP level. Consequently, the compound is useful for treating various kinds of disease such as allergic diseases, inflammatory diseases or immunologic diseases. The compound is thienopyrazole compound represented by the following formula (I): | 05-21-2009 |
20090131414 | PYRIDO(3,2-D)PYRIMIDINES AND PHARMACEUTICAL COMPOSITIONS USEFUL FOR TREATING HEPATITIS C - Specifically substituted pyrido(3,2-d)pyrimidine derivatives having the structural formula (I) are useful for the treatment of hepatitis C. | 05-21-2009 |
20090131415 | CYCLOALKYLOXY-AND HETEROCYCLOALKYLOXYPYRIDINE COMPOUNDS AS MODULATORS OF THE HISTAMINE H3 RECEPTOR - Certain cycloalkyloxy- and heterocycloalkyloxypyridine compounds are histamine H | 05-21-2009 |
20090131416 | SUBSTITUTED PYRAZINYL AMIDE COMPOUNDS AS MODULATORS OF THE HISTAMINE H3 RECEPTOR - Certain substituted pyrazinyl amide compounds are histamine H | 05-21-2009 |
20090131417 | SUBSTITUTED PYRIDYL AMIDE COMPOUNDS AS MODULATORS OF THE HISTAMINE H3 RECEPTOR - Certain substituted pyridyl amide compounds are histamine H | 05-21-2009 |
20090137562 | SUBSTITUTED BENZYL AMINE COMPOUNDS - Certain substituted benzyl amine compounds are histamine H | 05-28-2009 |
20090143365 | DERIVATIVES OF ALKYLPIPERAZINE- AND ALKYLHOMOPIPERAZINE-CARBOXYLATES, PREPARATION METHOD THEREOF AND USE OF SAME AS FATTY ACID AMIDO HYDROLASE ENZYME INHIBITORS - The present invention comprises alkylpiperazine- and alkylhomopiperazine carboxylates and their derivatives, methods for their preparation and the therapeutic use thereof as fatty acid amido hydrolase (FAAH) enzyme inhibitors. These derivatives exert various pharmacological activities by interacting, inter alia, with cannabinoid and vanilloid receptors. By inhibiting the metabolic activity of the FAAH enzyme, compounds often responsible for the onset of disease and other pathological conditions are not generated and the incidence of the disease is greatly reduced. | 06-04-2009 |
20090149447 | Novel M3 Muscarinic Acetylcholine Receptor Antagonists - Muscarinic Acetylcholine receptor antagonists and methods of using them are provided. | 06-11-2009 |
20090149448 | Phenoxyacetic Acid Derivatives Useful for Treating Respiratory Diseases - The invention relates to substituted phenoxyacetic acids as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation. | 06-11-2009 |
20090163476 | N-Phenyl Benzamide Derivatives as Sirtuin Modulators - Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent. | 06-25-2009 |
20090163477 | PHTHALAZINONE DERIVATIVES - A compound of formula (I): | 06-25-2009 |
20090170834 | Fused Pyrimidones and Thiopyrimidones, and Uses Thereof - Compounds represented by Structural Formula (I): | 07-02-2009 |
20090170835 | ISOINDOLINE DERIVATIVES - Provided is a novel isoindoline compound of the formula (I): | 07-02-2009 |
20090170836 | NEW INHIBITORS OF HISTONE DEACETYLASE - This invention comprises the novel compounds of formula (I) | 07-02-2009 |
20090176765 | Pyridinone and Pyridazinone Derivatives as Inhibitors of Poly (Adp-Ribose) Polymerase (Parp) - The present invention relates to compounds of formula I: | 07-09-2009 |
20090176766 | IMIDAZOLIDINONE AND IMIDAZOLIDINETHIONE DERIVATIVES - Imidazolidinone and imidazolinethione compounds of formula (I): | 07-09-2009 |
20090176767 | BIPHENYL COMPOUNDS USEFUL AS MUSCARINIC RECEPTOR ANTAGONISTS - This invention provides compounds of formula I: | 07-09-2009 |
20090176768 | DIAZA HETEROCYCLIC AMIDE COMPOUNDS AND THEIR USES - Diaza heterocyclic amide derivatives according to Formula (I) have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders: | 07-09-2009 |
20090181952 | COMPOUNDS USEFUL AS ALPHA7 NICOTINIC ACETYLCHOLINE RECEPTOR AGONISTS - The present invention provides compounds and compositions, and methods of using them to modulate α7 nicotinic acetylcholine receptors and/or to treat any of a variety of disorders, diseases, and conditions. Provided compounds can affect, among other things, neurological, psychiatric and/or inflammatory systems. | 07-16-2009 |
20090186876 | Pyridine Analogues II - The present invention relates to certain new pyridin analogues of Formula (I) [Chemical formula should be inserted here. Please see paper copy] Formula (I) to processes for preparing such compounds, to their utility in medicine in general and especially as P2Y | 07-23-2009 |
20090186877 | SUBSTITUTED 1H-BENZIMIDAZOLE-4-CARBOXAMIDES ARE POTENT PARP INHIBITORS - The present invention relates to 1H-benzimidazole-4-carboxamides of formula (I), | 07-23-2009 |
20090197871 | Dual Pharmacophores - PDE4-Muscarinic Antagonistics - The present invention is directed to novel compounds of Formula (I), pharmaceutical compositions and their use in therapy, for example as inhibitors of phosphodiesterase type IV (PDE4) and as antagonists of muscarinic acetylcholine receptors (mAChRs), in the treatment of/and or prophylaxis of respiratory diseases, including antiinflammatory and/or allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rhinitis (e.g. allergic rhinitis), atopic dermatitis or psoriasis. | 08-06-2009 |
20090203676 | G-protein Coupled Receptor Agonists - Compounds of formula (I): or pharmaceutically acceptable salts thereof, are GPCR agonists and are useful as for the treatment of obesity and diabetes. | 08-13-2009 |
20090203677 | Dual Pharmacophores - PDE4-Muscarinic Antagonistics - The present invention relates to novel compounds of Formula (I) | 08-13-2009 |
20090203678 | PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT OF PROTOZOAN PARASITIC DISEASES - The present invention relates to the use of a Rho/ROCK/PI3K/Akt pathway modulator for the manufacture of a medicament intended for the prevention or the treatment of pathologies associated with an infection by a protozoan parasite. | 08-13-2009 |
20090209521 | Inhibition of VEGF Translation - In accordance with the present invention, methods for inhibiting the translation of VEGF and methods for decreasing VEGF level by inhibiting VEGF translation are provided. In another aspect of the invention, compounds that inhibit the 5′-UTR-dependent translation of VEGF and methods for identifying such compounds are provided. | 08-20-2009 |
20090209522 | Heterocyclic Non-Peptide GNRH Antagonists - A compound of formula (I): wherein either B is absent and A and Z are the same or different and are each hydrogen, halogen, alkyl, hydroxy, alkoxy, —CN, —C(R | 08-20-2009 |
20090209523 | Pyrrolo[1,2-A] Pyrazin-1(2H)-One and Pyrrolo[1,2-D][1,2,4]Triazin-1(2H)-One Derivatives as Inhibitors of Poly(Adp-Ribose)Polymerase (Parp) - The present invention relates to compounds of formula I: and pharmaceutically acceptable salts or tautomers thereof which are inhibitors of poly(ADP-ribose)polymerase (PARP) and thus useful for the treatment of cancer, inflammatory diseases, reperfusion injuries, ischaemic conditions, stroke, renal failure, cardiovascular diseases, vascular diseases other than cardiovascular diseases, diabetes mellitus, neurodegenerative diseases, retroviral infections, retinal damage, skin senescence and UV-induced skin damage, and as chemo- or radiosensitizers for cancer treatment. | 08-20-2009 |
20090209524 | Novel Compounds - The present invention provides compounds of formula (1) | 08-20-2009 |
20090221556 | HYDROXY AND ALKOXY SUBSTITUTED 1H-IMIDAZOQUINOLINES AND METHODS - 1H-Imidazo[4,5-c]quinolin-4-amines with a hydroxy, alkoxy, hydroxyalkoxy, or alkoxyalkoxy substituent at the 2-position, pharmaceutical compositions containing these compounds, methods of making the compounds, intermediates, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed. | 09-03-2009 |
20090221557 | 3-AMINOALKYL-1,4-DIAZEPAN-2-ONE MELANOCORTIN-5 RECEPTOR ANTAGONISTS - The present invention provides compounds of Formula (I) that are useful for modulating the biological activity of the melanocortin-5 receptor (MC5R). Compounds of this invention can be used to treat diseases and/or conditions in which downregulation of MC5R is beneficial. Such diseases and/or conditions include, but are not limited to, acne, seborrhea, seborrheic dermatitis, cancer, and inflammatory diseases. | 09-03-2009 |
20090221558 | METHODS OF MODULATING THE ACTIVITY OF THE MC5 RECEPTOR AND TREATMENT OF CONDITIONS RELATED TO THIS RECEPTOR - The present invention provides compounds of Formula (I) that are useful for modulating the biological activity of the melanocortin-5 receptor (MC5R). Compounds of this invention can be used to treat diseases and/or conditions in which downregulation of MC5R is beneficial. Such diseases and/or conditions include, but are not limited to, acne, seborrhea, seborrheic dermatitis, cancer, and inflammatory diseases. | 09-03-2009 |
20090239846 | Novel Compounds - Novel substituted 1,5,7-trisubstituted-3,4-dihydro-pyrimido[4,5-d]pyrimidin-2-(1H)-one compounds and compositions, and their use in therapy as CSBP/RK/p38 kinase inhibitors. | 09-24-2009 |
20090239847 | Organic compounds - The present invention concerns a compound of formula (I) | 09-24-2009 |
20090239848 | NOVEL PIPERAZINE DERIVATIVES AS INHIBITORS OF STEAROYL-CoA DESATURASE - The present invention relates to piperazine derivatives that act as inhibitors of stearoyl-CoA desaturase. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds. | 09-24-2009 |
20090247507 | Enzyme Inhibitors - Compounds of formula (I), are aurora kinase inhibitors: wherein X is —N—, —CH2—N—, —CH2—CH—, or —CH—; R1 is a radical of formula (IA) wherein Z is —CH2—, —NH—, -0-, —S(O)— —S—, —S(O)2 or a divalent monocyclic carbocyclic or heterocyclic radical having 3-7 ring atoms; Alk is an optionally substituted divalent C1-C6 alkylene radical; A is hydrogen or an optionally substituted monocyclic carbocyclic or heterocyclic ring having 5-7 ring atoms; r, s and t are independently 0 or 1, provided that when A is hydrogen then at least one of r and s is 1; R2 is halogen, —CN, —CF3, —OCH3, or cyclopropyl; and R3 is a radical of formula (IB) wherein Q is hydrogen or an optionally substituted phenyl or monocyclic heterocyclic ring with 5 or 6 ring atoms; Z&It;1> is —S—, —S(O)—, —S(O)2—, —O—, —SO2NH—, —NHSO2—, NHC(═O)NH, —NH(C═S)NH—, Or —N(R4)—wherein R4 is hydrogen, C1-C3 alkyl, cycloalkyl, or benzyl; and Alk&It;1> and Alk&It;2> are, independently, optionally substituted divalent C1-C3 alkylene radicals; and m, n and p are independently 0 or 1. Data supplied from the esp@cenet datatbase—Worldwide d77 | 10-01-2009 |
20090247508 | Benzoimidazole Compounds - Benzoimidazole compounds, compositions, and methods of using them in leukocyte recruitment inhibition, in modulating H | 10-01-2009 |
20090247509 | Novel Heterocyclic Substituted Carbonyl Derivatives and Their Use as Dopamine D3 Receptor Ligands - The invention relates to heterocyclic substituted carbonyl derivatives that display selective binding to dopamine D | 10-01-2009 |
20090253683 | 7-MEMBERED RING COMPOUND AND METHOD OF PRODUCTION AND PHARMACEUTICAL APPLICATION THEREOF - A 7-membered heterocyclic compound having the formula (I), or its salt, or a solvate thereof with a chymase inhibitory action and useful for the prevention or treatment of various diseases, in which chymase is involved: | 10-08-2009 |
20090253684 | LEUKOTRIENE B4 INHIBITORS - Provided herein are compounds of the formula (I): | 10-08-2009 |
20090264415 | PYRIDO(3,2-D)PYRIMIDINES AND PHARMACEUTICAL COMPOSITIONS USEFUL FOR MEDICAL TREATMENT - This invention relates to substituted pyrido(3,2-d)pyrimidine derivatives, their pharmaceutically acceptable salts, N-oxides, solvates, pro-drugs and enantiomers, possessing unexpectedly desirable pharmaceutical properties, in particular which are highly active immunosuppressive agents, and as such are useful in the treatment in transplant rejection and/or in the treatment of certain inflammatory diseases. These derivatives are also useful in preventing or treating cardiovascular disorders, disorders of the central nervous system, TNF-α related disorders, viral diseases (including hepatitis C), erectile dysfunction and cell proliferative disorders. | 10-22-2009 |
20090264416 | N-BENZYL,N'-ARYLCARBONYLPIPERAZINE DERIVATIVES - The present invention relates to N-benzyl,N′-arylcarbonylpiperazine derivatives having the general formula I | 10-22-2009 |
20090264417 | SULFONYL-SUBSTITUTED BICYCLIC COMPOUNDS AS MODULATORS OF PPAR - Compounds as modulators of peroxisome proliferator activated receptors, pharmaceutical compositions comprising the same, and methods of treating disease using the same are disclosed. | 10-22-2009 |
20090264418 | 5-AMIDO-INDOLE-2-CARBOXAMIDE DERIVATIVES - The present invention relates to compounds of formula I | 10-22-2009 |
20090275564 | HALOARYL SUBSTITUTED AMINOPURINES, COMPOSITIONS THEREOF, AND METHODS OF TREATMENT THEREWITH - Provided herein are Aminopurine Compounds having the following structure: | 11-05-2009 |
20090281086 | 2 -OXYHETEROARYLAMIDE DERIVATIVES AS PARP INHIBITORS - A compound of the formula (I): and pharmaceutically acceptable salts thereof, wherein: HetA is a C | 11-12-2009 |
20090281087 | Compounds II - The present application relates to new compounds of formula (I), | 11-12-2009 |
20090281088 | BICYCLIC NITROIMIDAZOLE-SUBSTITUTED PHENYL OXAZOLIDINONES - The current invention provides a series of bicyclic nitroimidazole-substituted phenyl oxazolidinones in which a bicyclic nitroimidazole pharmacophore is covalently bonded to a phenyl oxazolidinone, their pharmaceutical compositions, and the method of use of the compositions for prevention and treatment of bacterial infections. The bicyclic nitroimidazole-substituted phenyl oxazolidinones possess surprising antibacterial activity against wild-type and resistant strains of pathogens, and are therefore useful for the prevention, control and treatment of a number of human and veterinary bacterial infections caused by these pathogens, such as | 11-12-2009 |
20090281089 | PYRIDYL INHIBITORS OF HEDGEHOG SIGNALLING - The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: | 11-12-2009 |
20090306053 | Highly selective rho-kinase inhibitor - The present invention relates to a compound having a highly selective Rho-kinase inhibiting activity and being useful as a therapeutic agent for a disease such as hypertension, pulmonary hypertension, cerebral vasospasm, cardiac angina, cardiac failure, arteriosclerosis, glaucoma, dysuria, asthma, or erectile dysfunction, and a drug containing the compound. | 12-10-2009 |
20090306054 | INTEGRASE INHIBITORS - Tricyclic compounds of formulae I-III, protected intermediates thereof, and methods for inhibition of HIV-integrase are disclosed. | 12-10-2009 |
20090306055 | PHENYLAZOLE COMPOUNDS, PRODUCTION PROCESS AND ANTIOXIDANTS - The present invention is directed to compounds represented by the formula (1): | 12-10-2009 |
20090306056 | PYRROLO-PYRIDINE KINASE MODULATORS - The present invention provides novel pyrrolo-pyridine kinase modulators and methods of using the novel pyrrolo-pyridine kinase modulators to treat diseases mediated by kinase activity. | 12-10-2009 |
20090312309 | Novel Medicaments - Novel compounds which interact with the histamine H3 receptor are defined. These compounds are particularly useful in the treatment of a variety of diseases or conditions in which histamine H3 interactions are beneficial. Thus, the compounds may find use, e.g., in the treatment of diseases of the central nervous system, the peripheral nervous system, the cardiovascular system, the pulmonary system, the gastrointestinal system and the endocrinological system. The novel compounds have a core consisting of a 6 membered aromatic ring containing at least one nitrogen atom and two carbon atoms in the ring and, at the remaining positions in the ring, there is either a carbon or a nitrogen atom. | 12-17-2009 |
20090312310 | Imidazothiazole derivatives - There is provided a novel compound that inhibits interaction between murine double minute 2 (Mdm2) protein and p53 protein and exhibits anti-tumor activity. The present invention provides an imidazothiazole derivative represented by the following formula (1) having various substituents that inhibits interaction between Mdm2 protein and p53 protein and exhibits anti-tumor activity: | 12-17-2009 |
20090318425 | APOPTOSIS SIGNAL-REGULATING KINASE 1 INHIBITORS - The present invention relates to apoptosis signal-regulating kinase 1 (“ASK1”) inhibiting compounds of the formula | 12-24-2009 |
20090325935 | GYRASE INHIBITORS AND USES THEREOF - The present invention relates to compounds that inhibit bacterial gyrase and/or Topo IV and pharmaceutically acceptable compositions comprising said compounds. These compounds, and compositions thereof, are useful in treating bacterial infection. Accordingly, the present invention also relates to methods for treating bacterial infections in mammals. | 12-31-2009 |
20090325936 | IMIDAZOPYRIDINE ANALOGS AS CB2 RECEPTOR MODULATORS, USEFUL IN THE TREATMENT OF PAIN, RESPIRATORY AND NON-RESPIRATORY DISEASES - The present invention relates to compounds represented by Formula (I) and Formula (II): (I) (II) or pharmaceutically acceptable salts thereof. The present invention also provides pharmaceutical compositions comprising the instant compounds. This invention further provides methods to treat and prevent pain, respiratory and non-respiratory diseases. | 12-31-2009 |
20100009970 | COMPOSITIONS AND METHODS FOR TREATMENT OF VIRAL DISEASES - The present invention features compositions, methods, and kits useful in the treatment of viral diseases. In certain embodiments, the viral disease is caused by a single stranded RNA virus, a flaviviridae virus, or a hepatic virus. In particular embodiments, the viral disease is viral hepatitis (e.g., hepatitis A, hepatitis B, hepatitis C, hepatitis D, hepatitis E) and the agent or combination of agents includes sertraline, a sertraline analog, UK-416244, or a UK-416244 analog. Also featured are screening methods for identification of novel compounds that may be used to treat a viral disease. | 01-14-2010 |
20100009971 | Pyridyl Non-Aromatic Nitrogen-Containing Heterocyclic-1-Carboxylate Compound - A novel pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate compound or its pharmaceutically acceptable salt has a potent FAAH-inhibitory activity. Further, the pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate compound of the present disclosure is also useful in the treatment of urinary frequency and urinary incontinence, overactive bladder and/or pain. | 01-14-2010 |
20100009972 | Pyridyl Non-Aromatic Nitrogen-Containing Heterocyclic-1-Carboxylate Compound - A novel pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate compound and its pharmaceutically acceptable salt has a potent FAAH-inhibitory activity. Further, the pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate compound of the present disclosure is also useful in the treatment of urinary frequency and urinary incontinence, overactive bladder and/or pain. | 01-14-2010 |
20100016292 | INHIBITORS OF LETHAL FACTOR PROTEASE - The invention provides compounds that can efficiently and specifically inhibit bacterial toxins, such as inhibit the lethal factor (LF) protease activity of anthrax toxin and/or botulinum neurotoxin type A. The invention also provides methods for inhibiting proteases, such as lethal factor protease, as well as methods for treating bacterial infections, such as anthrax and botulinum. | 01-21-2010 |
20100016293 | Quinazolines and Related Heterocyclic Compounds, and Their Therapeutic Use - Compounds that interact with the histamine H4 receptor, and which may be useful for treating or preventing disorders and conditions mediated by the histamine H4 receptor, e.g. inflammation, are of formula (I) wherein Q is CR | 01-21-2010 |
20100022518 | NOVEL HETEROCYCLYL COMPOUNDS - The invention is concerned with novel heterocyclyl compounds of formula (I): | 01-28-2010 |
20100029620 | SUBSTITUTED TRIAZOLINE, TETRAZOLONE AND IMIDAZOLONE DERIVATIVES FOR USE AS A MEDICINE - The present invention concerns substituted triazolone, tetrazolone and imidazolone derivatives according to the general Formula (I) | 02-04-2010 |
20100029621 | HEXAFLUOROISOPROPANOL DERIVATIVES - The present invention relates to hexafluoroisopropanol derivatives having the general formula I | 02-04-2010 |
20100035863 | 2 Amino-Pyrimidine Derivatives As H4 Receptor Antagonists, Processes For Preparing Them And Their Use In Pharmaceutical Compositions - The present invention concerns novel 2 amino pyrimidine derivatives of formula (I), processes for preparing them, pharmaceutical compositions containing them and their use as harmaceuticals. | 02-11-2010 |
20100035864 | Diacylglycerol Acyltransferase Inhibitors - Provided herein are compounds of the formula (1): | 02-11-2010 |
20100041642 | UREA INHIBITORS OF MAP KINASES - Urea containing compounds that inhibit MAP kinases, pharmaceutical compositions including such compounds and methods for using these compounds to treat inflammatory diseases and cancer are described herein. | 02-18-2010 |
20100048540 | Heterocyclic N-Oxides as Hypoxic Selective Protein Kinase Inhibitors - The invention relates to novel heterocyclic N-oxides which are useful as hypoxic selective cytotoxic agents that mediate and/or inhibit cell proliferation, for example, through the activity of protein kinases. The invention is further related to pharmaceutical compositions containing such compounds and compositions, and to methods of treating cancer as well as other disease states associated with unwanted ahgiogenesis and/or cellular proliferation by administering effective amounts of such compounds. | 02-25-2010 |
20100056498 | SUBSTITUTED MONOCYCLIC CGRP RECEPTOR ANTAGONISTS - Compounds of formula I: | 03-04-2010 |
20100063031 | KINASE INHIBITOR COMPOUNDS - Pyridine and pyridazine derivatives have unexpected drug properties as inhibitors of protein kinases and are useful in treating disorders related to abnormal protein kinase activities such as cancer. | 03-11-2010 |
20100063032 | SUBSTITUTED PYRIDO[2,3-D]PYRIMIDINE DERIVATIVES AS CANNABINOID-1 RECEPTOR MODULATORS - Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, Alzheimer s disease, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson s disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, cirrhosis of the liver, non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and the promotion of wakefulness. | 03-11-2010 |
20100069365 | Diazepane-acetamide derivatives as selective 11B-HSD1 inhibitors - The present invention relates to diazepane-acetamide 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. | 03-18-2010 |
20100069366 | ANTIBACTERIAL QUINOLINE DERIVATIVES - The present invention relates to novel substituted quinoline derivatives according to the general Formula (Ia) or Formula (Ib): | 03-18-2010 |
20100069367 | LXR and FXR Modulators - Compounds of the invention are disclosed, such as compounds of formulae LX-LXIV, and pharmaceutically acceptable salts, isomers, or prodrugs thereof, which are useful as modulators of the activity of liver X receptors (LXR) and Farnesoid X receptors (FXR), where R | 03-18-2010 |
20100069368 | Organic Compounds and Their Uses - The present disclosure relates to compounds relating to the diagnosis and treatment of pathologies relating to the Hedgehog pathway, including but not limited to tumor formation, cancer, neoplasia, and non-malignant hyperproliferative disorders; specifically relating to compounds of formula I: | 03-18-2010 |
20100069369 | Kinase Inhibitors And Their Uses - The present disclosure provides compounds that inhibit protein kinases, such as JAK, Axl, or Syk kinases, compositions comprising the compounds and methods of using the compounds to inhibit protein kinase and treat and/or prevent diseases associated with inappropriate kinase activity. The compounds of the present invention are according to structural formula (I): | 03-18-2010 |
20100069370 | COMPOUNDS, COMPOSITIONS AND METHODS - Certain substituted sulfonamide derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure. | 03-18-2010 |
20100069371 | THIENOPYRIDINE AND FUROPYRIDINE KINASE INHIBITORS - Compounds having the formula | 03-18-2010 |
20100087423 | NEW BENZAMIDE DERIVATIVES AS BRADYKININ ANTAGONISTS - The present invention relates to new phenylsulfamoyl benzamide derivatives of formula (I) | 04-08-2010 |
20100093703 | SUBSTITUTED ARYLSULPHONYLGLYCINES, THE PREPARATION THEREOF AND THE USE THEREOF AS PHARMACEUTICAL COMPOSITIONS - The present invention relates to substituted arylsulphonylglycines of general formula wherein R, R | 04-15-2010 |
20100099665 | ISOQUINOLINONE DERIVATIVES - The present invention relates to isoquinolinone derivatives of formula (I): | 04-22-2010 |
20100105664 | ORGANIC COMPOUNDS - A compound of formula (I) or a pharmaceutically acceptable salt or prodrug ester thereof: | 04-29-2010 |
20100105665 | RENIN INHIBITORS - Compounds, pharmaceutical compositions, kits, article of manufacture, methods of using, and method of preparing of compounds having the formula of: | 04-29-2010 |
20100113424 | N-BENZYL PYRROLIDINE DERIVATIVES - The present invention relates to a compound of formula I | 05-06-2010 |
20100120750 | METHODS FOR INDUCING POLYPLOIDIZATION OF MEGAKARYOCYTES AND FOR TREATING BLOOD AND BONE MARROW DISEASES AND DISORDERS - Disclosed are methods for inducing polyploidization of megakaryocyte cells and for promoting differentiation of megakaryocyte cells into platelet-producing cells. The methods may be utilized for treating blood and bone marrow diseases and disorders in a subject in need thereof and for identifying agents for treating blood and bone marrow diseases and disorders. | 05-13-2010 |
20100125065 | CARBOLINE DERIVATIVES USEFUL IN THE INHIBITION OF ANGIOGENESIS - In accordance with the present invention, compounds that inhibit the expression of VEGF post-transcriptionally have been identified, and methods for their use provided. In one aspect of the invention, compounds useful in the inhibition of VEGF production, in the inhibition of angiogenesis, and/or in the treatment of cancer, diabetic retinopathy or exudative macular degeneration are provided. In another aspect of the invention, methods are provided for the inhibition of VEGF production, the inhibition of angiogenesis, and/or the treatment of cancer, diabetic retinopathy or exudative macular degeneration using the compounds of the invention. | 05-20-2010 |
20100130476 | COMPOUNDS THAT INDUCE PANCREATIC BETA-CELL EXPANSION - The present invention relates to compounds and compositions for inducing the expansion of pancreatic β-cells. The invention further relates to a use of these expanded pancreatic β-cells to reversibly expand pancreatic β-cells and other quiescent cells to overcome deficits associated with degenerative and/or autoimmune diseases. | 05-27-2010 |
20100130477 | Spirocyclobutyl Piperidine Derivatives - Disclosed herein is at least one spirocyclobutyl piperidine derivative, at least one pharmaceutical composition comprising at least one spirocyclobutyl piperidine derivative disclosed herein, and at least one method of using at least one spirocyclobutyl piperidine derivative disclosed herein for treating at least one histamine H3 receptor associated condition therewith. | 05-27-2010 |
20100144707 | Pharmacokinetically improved compounds - The present invention relates to inhibitors of ROCK1 and ROCK2 and methods of modulating the pharmacokinetic and/or pharmacodynamic properties of such compounds. Also provided are methods of inhibiting ROCK1 and or ROCK2 that are useful for the treatment of disease. | 06-10-2010 |
20100144708 | HETEROCYCLIC COMPOUNDS CONTAINING NITROGEN ATOMS OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF, PROCESS FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME FOR TREATMENT OF CANCER - The present invention relates to new heterocyclic compounds containing nitrogen atoms or pharmaceutically acceptable salts thereof, a process for the preparation thereof, and a pharmaceutical composition comprising the same for treatment of cancer. The compounds according to the present invention induce DNA damage due to reactive oxygen species to activate c-abl and p53, induce RhoB to generate apoptosis, and induce cell death by down-regulating Bcl2 involved in cell survival, which is generated by dysregulated signals via the mitochondria pathway, thereby inhibiting tumor cell growth and inducing apoptosis. Accordingly, the composition according to the present invention can be used to treat cancer. | 06-10-2010 |
20100144709 | THIADIAZOLE DERIVATIVES FOR THE TREATMENT OF NEURO-DEGENERATIVE DISEASES - The invention provides novel 1,2,4-thiadiazole derivatives useful for preventing or treating an α-synucleopathy such as Parkinson's disease, as well as pharmaceutical compositions including them as biologically active ingredients, and methods for manufacturing them. | 06-10-2010 |
20100144710 | Piperazine and Piperidine MGLUR5 Potentiators - Compounds of Formula I or pharmaceutically acceptable salts or solvates thereof, wherein A, B, D, Ar1, Ar2, R2, R3, R4, a, m and n are defined in the specification, methods for the use thereof, processes for making and pharmaceutical compositions containing the same. | 06-10-2010 |
20100144711 | PHARMACEUTICAL COMPOSITION FOR ORAL ADMINISTRATION - A pharmaceutical composition for oral administration, comprising 3-hydroxy-N | 06-10-2010 |
20100144712 | TRIAZOLE DERIVATIVES HAVING ANTIFUNGAL ACTIVITY, METHOD FOR THE PREPARATION THEREOF, AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME - A triazole derivative of formula 1 or a pharmaceutically acceptable salt, hydrate, solvate or isomer thereof is superior to the conventional antifungal drugs in antifungal activity against a wide spectrum of pathogenic fungi, and has advantageously low toxicity. | 06-10-2010 |
20100144713 | 6-AND 7-AMINO ISOQUINOLINE COMPOUNDS AND METHODS FOR MAKING AND USING THE SAME - 6- and 7-amino isoquinoline compounds are provided that influence, inhibit or reduce the action of a kinase. Pharmaceutical compositions including therapeutically effective amounts of the 6- and 7-aminoisoquinoline compounds and pharmaceutically acceptable carriers are also provided. Various methods using the compounds and/or compositions to affect disease states or conditions such as cancer, obesity and glaucoma are also provided. | 06-10-2010 |
20100152168 | SUBSTITUTED BENZIMIDAZOLONE DERIVATIVES, MEDICAMENTS COMPRISING THEM AND THEIR USE - The present invention relates to novel benzimidazolone derivatives of the general formula (I) in which the substituents R | 06-17-2010 |
20100152169 | 4-OXOQUINAZOLIN-3-YL BENZAMIDE DERIVATIVES FOR THE TREATMENT OF CYTOKINE DISEASES - The invention concerns a compound of the Formula (I) wherein m is 1-2 and each R | 06-17-2010 |
20100160297 | COMPOUNDS FOR PIM KINASE INHIBITION AND FOR TREATING MALIGNANCY - The present invention relates to the compounds of formula I as well as to their use as PIM kinase inhibitors and, thereby, their use for treating oncological diseases, particularly of the hematopoietic system, the liver and the prostate gland. | 06-24-2010 |
20100160298 | METHOD OF TREATING OCULAR ALLERGY - The topical use of 5,6,7-trihydroxyheptanoic acid and analogs alone or in combination with histamine antagonists and/or mast cell stabilizers is disclosed for the treatment of ocular allergy. | 06-24-2010 |
20100168084 | Therapeutic compounds and related methods of use - Methods of using compounds that are HAT inhibitors are described herein. | 07-01-2010 |
20100173895 | IMIDAZOLOPYRIMIDINES AND IMIDAZOLOTRIAZINE DERIVATIVES AS INHIBITORS OF POLY(ADP-RIBOSE)POLYMERASE(PARP) - The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts or tautomers thereof which are inhibitors of poly(ADP-ribose)polymerase (PARP) and thus useful for the treatment of cancer, inflammatory diseases, reperfusion injuries, ischaemic conditions, stroke, renal failure, cardiovascular diseases, vascular diseases other than cardiovascular diseases, diabetes mellitus, neurodegenerative diseases, retroviral infections, retinal damage, skin senescence and UV-induced skin damage, and as chemo-or radiosensitizers for cancer treatment. | 07-08-2010 |
20100179132 | CARBOLINE DERIVATIVES USEFUL IN THE INHIBITION OF ANGIOGENESIS - In accordance with the present invention, compounds that inhibit the expression of VEGF post-transcriptionally have been identified, and methods for their use provided. In one aspect of the invention, compounds useful in the inhibition of VEGF production, in the treatment of solid tumor cancer, and in reducing plasma and/or tumor VEGF levels, are provided. In another aspect of the invention, methods are provided for the inhibition of VEGF production, the treatment of cancer, and the reduction of plasma and/or tumor VEGF levels, using the compounds of the invention. | 07-15-2010 |
20100184747 | INDOLINE DERIVATIVES AND THEIR USE IN TREATING DISEASE-STATES SUCH AS CANCER - The present invention encompasses compounds of general formula (1) wherein R | 07-22-2010 |
20100184748 | COMPOUNDS AND COMPOSITIONS AS ITPKB INHIBITORS - The invention provides a novel class of compounds of formula (I), pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or dysregulated B cell activities, particularly diseases or disorders that involve aberrant activation of inositol 1,4,5-trisphosphate 3-kinase B (ITPKb). | 07-22-2010 |
20100197665 | INDAZOLE DERIVATIVES AS KINASE INHIBITORS FOR THE TREATMENT OF CANCER - Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a dysregulated protein kinase activity, like cancer formula (I). | 08-05-2010 |
20100197666 | (THIO) -CARBAMOYL-CYCLOHEXANE DERIVATIVES AND METHOD FOR TREATING SCHIZOPHRENIA - The present invention relates to use of (thio)-carbamoyl-cyclohexane derivatives, particularly trans-4-{2-[4-(2,3-dichlorophenyl)-piperazin-1-yl]-ethyl}-N,N-dimethylcarbamoyl-cyclohexylamine and pharmaceutically acceptable salts thereof in the manufacture of a medicament for the treatment of schizophrenia. Furthermore, the present invention relates to the treatment of schizophrenia through the administration of (thio)-carbamoyl cyclohexane derivatives, particularly trans-4-{2-[4-(2,3-dichlorophenyl)-piperazin-1-yl]-ethyl}-N,N-dimethylcarbamoyl-cyclohexylamine and pharmaceutically acceptable salts thereof. | 08-05-2010 |
20100197667 | BIPHENYL COMPOUNDS USEFUL AS MUSCARINIC RECEPTOR ANTAGONISTS - The invention provides compounds of formula I: | 08-05-2010 |
20100204211 | MEDICAMENTS FOR THE TREATMENT OR PREVENTION OF FIBROTIC DISEASES - The present invention relates to the use of indolinones of general formula | 08-12-2010 |
20100204212 | FUSED HETEROCYCLIC COMPOUNDS USEFUL AS KINASE MODULATORS - Compounds having the formula (I), and enantiomers, and diastereomers, pharmaceutically-acceptable salts, thereof, | 08-12-2010 |
20100204213 | ARYLSULFONAMIDE DERIVATIVES FOR USE AS CCR3 ANTAGONISTS IN THE TREATMENT OF INFLAMMATORY AND IMMUNOLOGICAL DISORDERS - The present invention relates to a sulfonamide derivative which is useful as an active ingredient of pharmaceutical preparations. The sulfonamide derivatives of the present invention have CCR3 (CC type chemokine receptor) antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with CCR3 activity, in particular for the treatment of asthma, atopic dermatitis, allergic rhinitis and other inflammatory/immunological disorders. | 08-12-2010 |
20100210629 | 1,6-DIHYDRO-1,3,5,6-TETRAAZA-AS-INDACENE BASED TRICYCLIC COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS COMPRISING SAME - The present invention provides for tricyclic compounds having the formula (I), | 08-19-2010 |
20100210630 | Diamine Derivatives as Inhibitors of Leukotriene A4 Hydrolase - This invention is directed to compounds of formula (I): | 08-19-2010 |
20100216779 | Imidazopyridine Kinase Inhibitors - The present invention provides imidazopyridine compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents. | 08-26-2010 |
20100222330 | New Compounds - The present invention relates to substituted sulfonamide compounds of the general formula (I), wherein P is sulfonamide or amide-substituted sulfonic acid, which compounds are potentially useful for the prophylaxis and treatment of medical conditions relating to obesity, type II diabetes and/or disorders of the central nervous system. | 09-02-2010 |
20100234356 | COMPOUNDS USEFUL AS CHEMOKINE RECEPTOR ANTAGONISTS - The present invention relates to compounds useful as Chemokine Receptor antagonists. Compounds of general formula I are provided: | 09-16-2010 |
20100234357 | Benzofuran derivatives - The present invention provides a compound represented by the following formula (I): | 09-16-2010 |
20100240638 | Organic Compounds and their uses - The present application describes macrocyclic compounds of formula (I) with NS3 protease inhibitory activity for treating hepatitis C virus infection. | 09-23-2010 |
20100240639 | Sulfonyl-Derivatives as Novel or Histone Deacetylase - This invention comprises the novel compounds of formula (I) | 09-23-2010 |
20100240640 | (THIO) Carbamoyl-Cyclohexane Derivatives as D3/D2 Receptor Antagonists - The present invention relates to new D3 and D2 dopamine receptor subtype preferring ligands of formula (I): | 09-23-2010 |
20100249112 | COMBINATION OF CHK AND PARP INHIBITORS FOR THE TREATMENT OF CANCERS - A combination, comprising a checkpoint kinase (CHK) inhibitor, or a pharmaceutically acceptable salt thereof, and a poly (ADP-ribose)polymerase (PARP) inhibitor, or a pharmaceutically acceptable salt thereof is described. | 09-30-2010 |
20100249113 | MODULATORS OF ATP BINDING CASSETTE TRANSPORTERS - Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention. | 09-30-2010 |
20100261707 | THIADIAZOLE DERIVATIVES FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES - This invention provides specifically substituted 1,2,4-thiadiazole derivatives for use in the treatment of an α-synucleopathy such as Parkinson's disease, diffuse Lewy body disease, traumatic brain injury, amyotrophic lateral sclerosis, Niemann-Pick disease, Hallervorden-Spatz syndrome, Down syndrome, neuroaxonal dystrophy, multiple system atrophy and Alzheimer's disease. This invention also provides various methods for producing such substituted 1,2,4-thiadiazole derivatives. | 10-14-2010 |
20100261708 | Diazepane Compounds Which Modulate The CB2 Receptor - Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain. | 10-14-2010 |
20100261709 | PYRIDAZINONE DERIVATIVES AS PARP INHIBITORS - The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts or tautomers thereof which are inhibitors of poly(ADP-ribose)polymerase (PARP) and thus useful for the treatment of cancer, inflammatory diseases, reperfusion injuries, ischaemic conditions, stroke, renal failure, cardiovascular diseases, vascular diseases other than cardiovascular diseases, diabetes mellitus, neurodegenerative diseases, retroviral infections, retinaldamage, skin senescence and UV-induced skin damage, and as chemo- or radiosensitizers for cancer treatment. | 10-14-2010 |
20100267699 | CHEMICAL COMPOUNDS - 643 - The invention concerns bicyclic compounds of Formula I | 10-21-2010 |
20100267700 | IMMUNOSUPPRESSIVE AGENT AND ANTI-TUMOR AGENT COMPRISING HETEROCYCLIC COMPOUND AS ACTIVE INGREDIENT - A novel method for immunosuppressive in a mammal suffering from an immune disease, including administering to the mammal a therapeutically effective amount of a heterocyclic compound represented by the general formula (I) (wherein X or other variables are as defined in the specification) or a pharmaceutically acceptable salt thereof is disclosed. A novel heterocyclic compound represented by the general formula (II) (wherein X or other variables are as defined in the specification) or a pharmaceutically acceptable salt thereof is also disclosed. | 10-21-2010 |
20100267701 | SUBSTITUTED PYRIDYL AMIDE COMPOUNDS AS MODULATORS OF THE HISTAMINE H3 RECEPTOR - Certain substituted pyridyl amide compounds are histamine H | 10-21-2010 |
20100267702 | Bisbenzamidines and bisbenzamidoximes for the treatment of human African trypanosomiasis - Disclosed are bisbenzamidine and bisbenzamidoxime compounds useful for treatment of trypanosomiasis. The compounds disclosed are useful for treating mammals infected with parasitic hemoflagellates, in particular | 10-21-2010 |
20100273780 | SUBSTITUTED 8-HETEROARYL XANTHINES - The present invention provides compounds and pharmaceutical compositions that are selective antagonists of A | 10-28-2010 |
20100273781 | CXCR3 RECEPTOR ANTAGONISTS - The present invention relates to compounds of formula (I): | 10-28-2010 |
20100273782 | 2,5-DISUBSTITUTED ARYLSULFONAMIDE CCR3 ANTAGONISTS - Provided herein are 2,5-disubstituted arylsulfonamides that are useful for modulating CCR3 activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition. | 10-28-2010 |
20100280010 | CHEMICAL COMPOUNDS - The present invention provides compounds that demonstrate protective effects on target cells from HIV infection in a manner as to bind to chemokine receptor, and which affect the binding of the natural ligand or chemokine to a receptor such as CXCR4 of a target cell. | 11-04-2010 |
20100280011 | DUAL MECHANISM INHIBITORS FOR THE TREATMENT OF DISEASE - Provided are compounds that are inhibitors of both rho kinase and of a monoamine transporter (MAT) act to improve the disease state or condition. Further provided are compositions comprising the compounds. Further provided are methods for treating diseases or conditions, the methods comprising administering compounds according to the invention. One such disease may be glaucoma for which, among other beneficial effects, a marked reduction in intraocular pressure (IOP) may be achieved. | 11-04-2010 |
20100280012 | AZAAZULENE COMPOUNDS - An azaazulene compound is provided. The azaazulene compound has formula (I) shown below. Each variable in formula (I) is defined in the specification. The compound can be used to treat cancer. The invention also provides a method for treating cancer. The method includes administering to a subject in need thereof an effective amount of one or more azaazulene compounds of formula (I). | 11-04-2010 |
20100280013 | CARBINOL DERIVATIVES HAVING HETEROCYCLIC LINKER - [Object] It is to provide a novel LXRβ agonist useful as a preventative and/or therapeutic agent for atherosclerosis; arteriosclerosis such as those resulting from diabetes; dyslipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases that are caused by inflammatory cytokines; skin diseases such as allergic skin diseases; diabetes; or Alzheimer's disease. | 11-04-2010 |
20100280014 | N-PHENYL- (PIPERAZINYL OR HOMOPIPERAZINYL)-BENZENESULFONAMIDE OR BENZENESULFONYL-PHENL-(PIPERAZINE OR HOMOPIPERAZINE) COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE SEROTONIN 5-HT6 RECEPTOR - The present invention relates to N-phenyl-(piperazinyl or homopiperazinyl)-benzenesulfonamide or benzenesulfonyl-phenyl-(piperazine or homopiperazine) compounds, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating diseases that respond to modulation of the serotonin 5-HT | 11-04-2010 |
20100286126 | Organic Compounds - A compound of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof, and their preparation and use as pharmaceuticals | 11-11-2010 |
20100292220 | BENZENESULFONANILIDE COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE SEROTONIN 5-HT6 RECEPTOR - The present invention relates to novel benzenesulfonanilide compounds of the formulae I and I′ and physiologically tolerated acid addition salts and the N-oxides thereof. The compounds possess valuable therapeutic properties and are particularly suitable, for treating diseases that respond to modulation of the serotonin 5-HT | 11-18-2010 |
20100292221 | BENZENESULFONANILIDE COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE SEROTONIN 5-HT6 RECEPTOR - The present invention relates to novel benzenesulfonanilide compounds of the formulae I and I′ and physiologically tolerated acid addition salts and the N-oxides thereof. The compounds possess valuable therapeutic properties and are particularly suitable, for treating diseases that respond to modulation of the serotonin 5-HT | 11-18-2010 |
20100292222 | CHEMICAL COMPOUNDS 751 - The invention concerns bicyclic compounds of Formula (I) | 11-18-2010 |
20100292223 | INDAZOLE-CARBOXAMIDE COMPOUNDS - The invention provides novel indazole-carboxamide 5-HT | 11-18-2010 |
20100298300 | TRIAZOLOPYRAZINE COMPOUNDS USEFUL FOR THE TREATMENT OF DEGENERATIVE & INFLAMMATORY DISEASES - Novel [1.2.4]triazolo[1,5-a]pyrazine compounds are disclosed that have a formula represented by the following: | 11-25-2010 |
20100298301 | OXAZOLE TYROSINE KINASE INHIBITORS - The invention provides a compound which is an amide of the formula (1), or a salt, solvate, N-oxide or tautomer thereof; wherein: a is 0 or 1; b is 0 or 1: provided that the sum of a and b is 0 or 1; T is O or NH Ar | 11-25-2010 |
20100298302 | NOVEL PROTEIN KINASE MODULATORS - The invention provides compounds that inhibit selected kinases (Pim, Flt and/or CK2 kinases) and compositions containing such compounds. These compounds and compositions are useful for treating proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation, pain, and certain infections and immunological disorders. | 11-25-2010 |
20100298303 | CGRP RECEPTOR ANTAGONISTS - The present invention is directed to compounds of Formula I: | 11-25-2010 |
20100305106 | INHIBITORS OF FATTY ACID UPTAKE AND METHODS OF USE - The present disclosure describes inhibitors of fatty acid uptake and methods of using such inhibitors. Specifically, the present disclosure describes inhibitors with specificity for FATP2. | 12-02-2010 |
20100305107 | QUINOLINE DERIVATIVES AND THEIR USE AS 5-HT6 LIGANDS - Disclosed are quinoline compounds having affinity for the 5-HT | 12-02-2010 |
20100317652 | Compounds Useful In Therapy - The present invention provides compounds of formula (I), | 12-16-2010 |
20100317653 | OXADIAZOLE DERIVATIVES AS DGAT INHIBITORS - Compounds of formula (I), and salts and pro-drugs thereof: | 12-16-2010 |
20100324026 | FUSED TRICYCLIC COMPOUNDS AS INHIBITORS OF TUMOR NECROSIS FACTOR-ALPHA - Compounds of formula 1: | 12-23-2010 |
20100331313 | Thiazole Derivatives as Protein Kinase Inhibitors - The present invention relates to novel Thiazole Derivatives, compositions comprising the Thiazole Derivatives, and methods for using the Thiazole Derivatives for treating or preventing a proliferative disorder, an anti-proliferative disorder, inflammation, arthritis, a central nervous system disorder, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral infection, a fungal infection, or a disorder related to the activity of a protein kinase. | 12-30-2010 |
20100331314 | PYRAZOLOPYRIMIDINES AND RELATED HETEROCYCLES AS KINASE INHIBITORS - The invention provides compounds of general formula (I) that inhibit selected kinases (Pim and/or CK2 kinases) and compositions containing such compounds. These compounds and compositions are useful for treating proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation, pain, and certain infections and immunological disorders. | 12-30-2010 |
20100331315 | RHODANINES AND RELATED HETEROCYCLES AS KINASE INHIBITORS - The invention provides compounds that inhibit PIM kinases and/or CK2, and compositions containing such compounds. These compounds and compositions are useful for treating proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation, pain, vascular disorders, pathogenic infections and certain immunological disorders. | 12-30-2010 |
20110009390 | 2-OXO-2- (2-PHENYL-5,6,7,8-TETRAHYDRO-INDOLIZIN-3-YL) -ACETAMIDE DERIVATIVES AND RELATED COMPOUNDS AS ANTIFUNGAL AGENTS - The invention provides compounds of formula (I), and pharmaceutically and agriculturally acceptable salts thereof: wherein: R1, R2, R3, R4, R5, R6, R7, R8, A1, L1 and n are as defined herein. These compounds and their pharmaceutically acceptable salts are useful in the manufacture of medicaments for use in the prevention or treatment of a fungal disease. Compounds of formula (I), and agriculturally acceptable salts thereof, may also be used as agricultural fungicides. | 01-13-2011 |
20110009391 | TETRAHYDROQUINOXALINE UREA DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION - The present invention relates to tetrahydroquinoxaline urea derivatives, to their preparation and to their therapeutic application. | 01-13-2011 |
20110015185 | Benzofuran Compounds - The present invention relates to compounds of formula (I): | 01-20-2011 |
20110021506 | ANTHELMINTIC AGENTS AND THEIR USE - This invention is directed to compounds and salts that are generally useful as anthelmintic agents or as intermediates in processes for making anthelmintic agents. This invention also is directed to processes for making the compounds and salts, pharmaceutical compositions and kits comprising the compounds and salts, uses of the compounds and salts to make medicaments, and treatments comprising the administration of the compounds and salts to animals in need of the treatments. | 01-27-2011 |
20110028455 | Indole-substituted 3-cyanopyridines As Kinase Inhibitors - Disclosed are compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein X is —O—, —N(R | 02-03-2011 |
20110034441 | INDAZOLES AS WNT/B-CATENIN SIGNALING PATHWAY INHIBITORS AND THERAPEUTIC USES THEREOF - Described herein are methods of treating a disorder or disease in which aberrant Wnt signaling is implicated, with a variety of compounds, including Wnt inhibitor compounds. More particularly, it concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases due to mutations in Wnt signaling components. | 02-10-2011 |
20110039829 | PYRAZOLE-CARBOXAMIDE DERIVATIVES AS P2Y12 ANTAGONISTS - The present invention relates to compounds of the formula I, | 02-17-2011 |
20110039830 | CYCLIC INDOLE-3-CARBOXAMIDES, THEIR PREPARATION AND THEIR USE AS PHARMACEUTICALS - The present invention relates to cyclic indole-3-carboxamides of the formula I, | 02-17-2011 |
20110039831 | 3-HETEROARYLMETHYL-IMIDAZO[1,2-B]PYRIDAZIN-6-YL DERIVATIVES - The invention relates to compounds of formula (I) and salts thereof | 02-17-2011 |
20110039832 | DIHYDRO)PYRROLO[2,1-A]ISOQUINOLINES - The invention relates to 5,6-dihydropyrrolo[2,1-a]isoquinoline and pyrrolo[2,1-a]isoquinoline derivatives according to general formula (I) or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility. | 02-17-2011 |
20110039833 | 1-BENZOYL SUBSTITUTED DIAZEPINE DERIVATIVES AS SELECTIVE HISTAMINE H3 RECEPTOR AGONISTS - The present invention relates to novel diazepanyl derivatives having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of neurological and psychiatric disorders. | 02-17-2011 |
20110053916 | PYRIMIDINE COMPOUNDS AS TUBERCULOSIS INHIBITORS - The present invention relates to compounds useful as inhibitors of treating tuberculosis. The invention also provides processes for preparing compounds of the inventions and | 03-03-2011 |
20110053917 | Allosteric Modulators of the A1 Adenosine Receptor - The present invention provides compounds of formula (I) | 03-03-2011 |
20110059951 | HETEROCYCLIC DERIVATIVES OF PYRAZOL-4-YL-PYRROLO[2,3-d]PYRIMIDINES AS JANUS KINASE INHIBITORS - The present invention provides heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines, as well as their compositions and methods of use, that modulate the activity of Janus kinases (JAKs) and are useful in the treatment of diseases related to the activity of JAKs including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases. | 03-10-2011 |
20110059952 | 3-SUBSTITUTED-1,4-DIAZEPAN-2-ONE MELANOCORTIN-5 RECEPTOR ANTAGONISTS - The present invention provides compounds of Formula (I) that are useful for modulating the biological activity of the melanocortin-5 receptor (MC5R). Compounds of this invention can be used to treat diseases and/or conditions in which downregulation of MC5R is beneficial. Such diseases and/or conditions include, but are not limited to, acne, seborrhea, seborrheic dermatitis, cancer, and inflammatory diseases. | 03-10-2011 |
20110059953 | COMPOUNDS FOR USE IN STABILIZING P53 MUTANTS - Compounds of formula (I): wherein X is selected from CR | 03-10-2011 |
20110065687 | HYDRAZIDE COMPOUNDS AND USES THEREOF - This application relates to certain novel polycyclic compounds that interact with quadruplex-forming regions of polynucleotides and thereby inhibit translation of genetic information into polypeptides. These compounds can thus provide anticancer and antibacterial and antiviral effects. The invention includes novel compounds and pharmaceutical compositions, and methods of using them to treat cancer and other conditions. | 03-17-2011 |
20110065688 | THERAPEUTIC PIPERAZINES - The invention includes a compound of formula I: | 03-17-2011 |
20110065689 | THERAPEUTIC PIPERAZINES - The invention includes a compound of formula I: | 03-17-2011 |
20110065690 | COMPOSITIONS AND METHODS FOR TREATMENT OF LEUKEMIA - The invention relates generally to effective treatment leukemia. In particular, the present invention provides compositions and methods to inhibit the interaction of menin with MLL and MLL-fusion oncoproteins, and well as systems and methods to screen for such compositions. | 03-17-2011 |
20110065691 | THERAPEUTIC PIPERAZINES - The invention includes a compound of formula I: | 03-17-2011 |
20110065692 | THERAPEUTIC PYRAZOLONAPHTHYRIDINE DERIVATIVES - The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABA | 03-17-2011 |
20110065693 | THERAPEUTIC PYRAZOLOQUINOLINE DERIVATIVES - The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABA | 03-17-2011 |
20110071139 | Cycloalkyl Lactame Derivatives As Inhibitors Of 11-Beta-Hydroxysteroid Dehydrogenase 1 - This invention relates to novel compounds of the Formula (I), any of the formulas I | 03-24-2011 |
20110071140 | THERAPEUTIC PYRAZOLOQUINOLINE UREA DERIVATIVES - The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABA | 03-24-2011 |
20110077237 | KINASE INHIBITORS - The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions. | 03-31-2011 |
20110092489 | 3-Aryl-Substituted Quinazolones, and Uses Thereof - Compounds represented by Structural Formula (I): | 04-21-2011 |
20110092490 | PYRIMIDINES, TRIAZINES AND THEIR USE AS PHARMACEUTICAL AGENTS - A compound of formula (I) and its pharmaceutically acceptable salts or solvates and physiologically hydrolysable, solubilising or immobilisable derivatives wherein: Ar is a 5-membered heteroaryl ring wherein X | 04-21-2011 |
20110092491 | Compounds and Compositions as Inhibitors of Receptor Tyrosine Kinase Activity - The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with cSRC, Lck, FGFR3, Flt3, TrkB, Bmx, and/or PFGFRα kinase activity. | 04-21-2011 |
20110098282 | NEW COMPOUNDS - Novel compounds of which the following is exemplary: | 04-28-2011 |
20110098283 | 3-CINNOLINECARBOXAMIDE DERIVATIVES AND THEIR USE FOR TREATING CANCER - The invention relates to chemical compounds of formula (I): | 04-28-2011 |
20110105475 | BENZOFURANE, BENZOTHIOPHENE, BENZOTHIAZOL DERIVATIVES AS FXR MODULATORS - The present invention relates to compounds of formula (I) wherein the substituents are as defined in the claims, including pharmaceutical compositions thereof and for their use in the treatment and/or prevention and/or amelioration of one or more symptoms of disease or disorders related to the activity of FXR. The invention is also directed to intermediates and to a method of preparation of compounds of formula (I). | 05-05-2011 |
20110112077 | Quinolizidinone m1 Receptor Positive Allosteric Modulators - The present invention is directed to compounds of formula (I) 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. | 05-12-2011 |
20110130387 | SIRTUIN MODULATING COMPOUNDS - Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent. | 06-02-2011 |
20110130388 | PROPHYLACTIC OR THERAPEUTIC AGENT FOR AXIAL MYOPIA - Since high myopia increases the risks of retinal detachment, myopic chorioretinal atrophy, myopic choroidal neovascularization, glaucoma, and cataract, establishment of prophylaxis against the progress of myopia is desired. However, at present, there is no effective prophylaxis or therapy for axial myopia, which is considered to cause high myopia. The present invention, which was completed based on the finding that Rho kinase inhibitors have an inhibitory action on axial length extension, provides a prominently effective prophylactic or therapeutic agent comprising a Rho kinase inhibitor as an active ingredient for axial myopia. | 06-02-2011 |
20110160189 | COMPOUND THAT CAN INHIBIT UBC13-UEV INTERACTIONS, PHARMACEUTICAL COMPOSITIONS AND THERAPEUTIC USES - The invention relates to a compound (I) wherein R is a heterocyclyl radical; R | 06-30-2011 |
20110160190 | CARBOLINE DERIVATIVES USEFUL IN THE INHIBITION OF ANGIOGENESIS - In accordance with the present invention, compounds that inhibit the expression of VEGF post-transcriptionally have been identified, and methods for their use provided. In one aspect of the invention, compounds useful in the inhibition of VEGF production, in the treatment of solid tumor cancer, and in reducing plasma and/or tumor VEGF levels, are provided. In another aspect of the invention, methods are provided for the inhibition of VEGF production, the treatment of cancer, and the reduction of plasma and/or tumor VEGF levels, using the compounds of the invention. | 06-30-2011 |
20110178067 | TRIAZOLOPYRAZINE COMPOUNDS USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES - Novel [1.2.4]triazolo[1,5-a]pyrazine compounds are disclosed that have a formula represented by the following: | 07-21-2011 |
20110183965 | 6-AMINOISOQUINOLINE COMPOUNDS - 6-Amino isoquinoline compounds are provided that influence, inhibit or reduce the action of a kinase. Pharmaceutical compositions including therapeutically effective amounts of the 6-aminoisoquinoline compounds and pharmaceutically acceptable carriers are also provided. Various methods using the compounds and/or compositions to affect disease states or conditions such as cancer, obesity and glaucoma are also provided. | 07-28-2011 |
20110183966 | AMINOPYRIDINE KINASE INHIBITORS - The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions. | 07-28-2011 |
20110183967 | BENZOXAZOLE COMPOUNDS AND METHODS OF USE - The present invention provides benzoxazole compounds and pharmaceutically acceptable salts thereof and pharmaceutical compositions including the same. The present invention further provides methods of use as described herein. | 07-28-2011 |
20110190270 | METHODS OF TREATING THROMBOEMBOLIC DISORDERS - The field of the invention relates to methods for dissolving a thrombus using inhibitors of platelet contractility. More particularly, the present invention relates to the use of an inhibitor of platelet contractility in combination with one or more thrombolytic agents and optionally one or more anticoagulants for inhibiting platelet contraction and consolidation in the developing thrombus. | 08-04-2011 |
20110190271 | 2,4-Pyrimidinediamine Compounds and Uses as Anti-Proliferative Agents - The present invention provides 2,4-pyrimidinediamine compounds having antiproliferative activity, compositions comprising the compounds and methods of using the compounds to inhibit cellular proliferation and to treat proliferative diseases such as tumorigenic cancers. | 08-04-2011 |
20110190272 | CHEMICAL COMPOUNDS - The invention relates to chemical compounds of formula (I): or pharmaceutically acceptable salts thereof which possess CSF-IR kinase inhibitory activity and are accordingly useful for their anti-cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm-blooded animal such as man. | 08-04-2011 |
20110190273 | METHODS AND COMPOSITIONS IN THE TREATMENT OF CORONAVIRUSES - The invention relates generally to the field of virology, and relates to the identification and characterization of the targets involved in the evasion strategy of viruses and to the use thereof in methods to identify anti-viral compounds. More in particular to identify compounds which are modulators of myosin light chain kinase (MLCK), a target within said entry and immune-evasion strategy. Other aspects of the invention are directed to anti-viral compounds identified using the models and methods of the present invention, as well as to the use thereof in treating viral infections, such as for example caused by the feline infectious peritonitis virus (FIPV), a coronavirus which belongs to an antigenic group which comprises in particular feline enteric coronavirus (FECV), canine coronavirus (CCV), swine transmissible gastroenteritis coronavirus (TGEV), porcine respiratory coronavirus (PRCV) and human coronavirus (HCV), and which induces, in a host-dependent manner, a range of symptoms which range from mild enteritis to the severe debilitating disease, and, in some cases, up to death. In a particular aspect the present invention provides the use of MLCK inhibitors for the treatment of feline infectious peritonitis (FIP). | 08-04-2011 |
20110190274 | SALT OF, AND PROCESSES FOR THE PREPARATION OF, 1-ISOPROPYL-4-HEXAHYDRO-1H-1,4-DIAZEPINE - The invention relates to 1-isopropyl-4-{[4-(tetrahydro-2H-pyran-4-yloxy)phenyl]carbonyl}hexahydro-1H-1,4-diazepine mono-maleate, and crystalline Form 1 thereof. | 08-04-2011 |
20110195957 | SUBSTITUTED DIAZEPAN OREXIN RECEPTOR ANTAGONISTS - The present invention is directed to substituted diazepan compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors 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 orexin receptors are involved. | 08-11-2011 |
20110195958 | ACTIVATORS OF HUMAN PYRUVATE KINASE - Disclosed are pyruvate kinase M2 activators, which are bis sulfonamide piperazinyl and piperidinyl compounds of Formula (I), 2,4-disubstituted 4H-thieno[3,2-c]pyrrole-2-(substituted benzyl)pyridazin-3(2H)-ones of Formula (II) and 6-(3,4-dimethylphenylaminosulfonyl)-3,4-dihydro-1H-quinolin-2-one of formula (III), wherein L, R | 08-11-2011 |
20110207720 | QUINOLIN-4-ONE AND 4-OXODIHYRDOCINNOLINE DERIVATIVES AS INHIBITORS OF POLY(ADP-RIBOSE) POLYMERASE (PARP) - The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts or tautomers thereof which are inhibitors of poly(ADP-ribose)polymerase (PARP) and thus useful for the treatment of cancer, inflammatory diseases, reperfusion injuries, ischaemic conditions, stroke, renal failure, cardiovascular diseases, vascular diseases other than cardiovascular diseases, diabetes mellitus, neurodegenerative diseases, retroviral infections, retinal damage, skin senescence and UV-induced skin damage, and as chemo-or radiosensitizers for cancer treatment. | 08-25-2011 |
20110224193 | INHIBITORS OF DIACYLGLYCEROL ACYLTRANSFERASE - The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase (“DGAT”) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the invention is shown with this abstract. | 09-15-2011 |
20110230470 | SUBSTITUTED PYRAZOLO[4,3-C]PYRIDINE DERIVATIVES ACTIVE AS KINASE INHIBITORS - Substituted pyrazolo[4,3-c]pyridine derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a dysregulated protein kinase activity, like cancer. | 09-22-2011 |
20110230471 | BENZONAPHTYRIDINE COMPOUNDS AS INHIBITORS OF AUTOTAXIN - Compounds of the formula (I), in which R | 09-22-2011 |
20110237571 | PHTHALAZINE DERIVATIVES - The present invention relates to novel phthalazine derivatives and, more particularly, to phthalazine derivatives that are useful as protein kinase inhibitors. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and methods of treatment using the compounds. | 09-29-2011 |
20110237572 | Treating diseases mediated by blockade of the epithelial sodium channel with pyrazine-2-carboxamide derivatives - A compound of Formula I | 09-29-2011 |
20110251181 | 5H-CYCLOPENTA[D]PYRIMIDINES AS AKT PROTEIN KINASE INHIBITORS - Compounds of Formula I are useful for inhibiting AKT protein kinases. Methods using compounds of Formula I and stereoisomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed. Formula (I). | 10-13-2011 |
20110251182 | AGENTS AND METHODS FOR TREATING ISCHEMIC AND OTHER DISEASES - This invention relates to methods of screening for modulators of mammalian cell injury cause by TRPM7 gene and protein activity, compounds that modulate TRPM7 gene and protein activity and methods of treatment of mammalian cell injury using modulators of TRPM7 gene and protein activity. | 10-13-2011 |
20110263571 | NOVEL AMIDE DERIVATIVE AND USE THEREOF AS MEDICINE - Provided are a novel low-molecular-weight compound that suppresses production of induction type MMPs, particularly MMP-9, rather than production of hemostatic type MMP-2, as well as a prophylactic/therapeutic drug for autoimmune diseases or osteoarthritis. An amide derivative represented by the following formula (I) | 10-27-2011 |
20110263572 | 3-AMINOALKYL-1,4-DIAZEPAN-2-ONE MELANOCORTIN-5-RECEPTOR ANTAGONISTS - The present invention provides compounds of Formula (I) that are useful for modulating the biological activity of the melanocortin-5 receptor (MC5R). Compounds of this invention can be used to treat diseases and/or conditions in which downregulation of MC5R is beneficial. Such diseases and/or conditions include, but are not limited to, acne, seborrhea, seborrheic dermatitis, cancer, and inflammatory diseases. | 10-27-2011 |
20110269747 | POLYARYLCARBOXAMIDES USEFUL AS LIPID LOWERING AGENTS - Polyarylcarboxamide compounds of formula (I) | 11-03-2011 |
20110281849 | Aryl Indolyl Sulfonamide Compounds and Their Use as 5-HT6 Ligands - The present invention relates to novel aryl indolyl sulfonamide compounds of the formula (I), their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates described herein and pharmaceutically acceptable compositions containing them. | 11-17-2011 |
20110281850 | INTRACELLULAR KINASE INHIBITORS - Intracellular kinase inhibitors and their therapeutic uses for patients with T cell malignancies, B cell malignancies, autoimmune disorders, and transplanted organs. | 11-17-2011 |
20110281851 | BIPHENYL COMPOUNDS USEFUL AS MUSCARINIC RECEPTOR ANTAGONISTS - The invention provides compounds of formula I: | 11-17-2011 |
20110288077 | COMPOUNDS FOR THE TREATMENT OF INFLAMMATORY DISEASES - This invention relates to compounds of the Formula (I)-(IX):, as defined herein, or a pharmaceutically acceptable salt, solvate or ester thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF-α combinations thereof. | 11-24-2011 |
20110294789 | COMPOUNDS FOR RHO KINASE INHIBITION AND FOR IMPROVING LEARNING AND MEMORY - The present invention provides a compound of Formula (I) and methods for improving memory, inhibiting rho kinase 1 or 2, inhibiting PIM kinase, or inhibiting IRAK1 kinase in a subject by administering a therapeutically effective amount of the compound. | 12-01-2011 |
20110294790 | BICYCLIC PYRAZOLE AND ISOXAZOLE DERIVATIVES AS ANTITUMOR AND ANTINEURODEGENERATIVE AGENTS - Bicyclic pyrazole and isoxazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases mediated by HSP90 protein, like cancer and neurodegenerative disorders. | 12-01-2011 |
20110301150 | SUBSTITUTED AZOLE DERIVATIVES, PHARMACEUTICAL COMPOSITION CONTAINING THE DERIVATIVES, AND METHOD FOR TREATING PARKINSON'S DISEASE USING THE SAME - Provided are a substituted azole derivative and pharmaceutically acceptable salts thereof, a pharmaceutical composition including an effective amount of the derivative, and a method for treating Parkinson's disease in a mammal including administering an effective amount of the compound to the mammal. The azole derivative of the following Formula (I) and pharmaceutically useful salts thereof have an efficacy against Parkinson's disease from inhibitory effects of the activity of MAO-B. | 12-08-2011 |
20110319390 | 6-Aminoisoquinoline Compounds - 6-Amino isoquinoline compounds are provided that influence, inhibit or reduce the action of a kinase. Pharmaceutical compositions including therapeutically effective amounts of the 6-aminoisoquinoline compounds and pharmaceutically acceptable carriers are also provided. Various methods using the compounds and/or compositions to affect disease states or conditions such as cancer, obesity and glaucoma are also provided. | 12-29-2011 |
20110319391 | METHODS AND COMPOSITIONS FOR STIMULATING NEUROGENESIS AND INHIBITING NEURONAL DEGENERATION - The present invention provides methods and compositions comprising compounds useful for stimulating neurogenesis. The methods and compositions comprising compounds are also useful for inhibiting neuronal degeneration. Thus, the present invention can be used in the treatment of diseases and conditions characterized by neuronal loss and reduced neurogenesis including Alzheimer's disease, stroke, traumatic brain injury, and depression. This invention could also be used for research products including single agents or mixtures of agents to promote, proliferate, differentiate, or maintain neurons from stem or progenitor cells. | 12-29-2011 |
20110319392 | Thiazole Sulfonamide And Oxazole Sulfonamide Kinase Inhibitors - The present invention provides thiazole sulfonamide and oxazole sulfonamide compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents. | 12-29-2011 |
20110319393 | ANTHELMINTIC AGENTS AND THEIR USE - This invention is directed to compounds and salts that are generally useful as anthelmintic agents or as intermediates in processes for making anthelmintic agents. This invention also is directed to processes for making the compounds and salts, pharmaceutical compositions and kits comprising the compounds and salts, uses of the compounds and salts to make medicaments, and treatments comprising the administration of the compounds and salts to animals in need of the treatments. | 12-29-2011 |
20120004212 | ORGANIC COMPOUNDS - A compound of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof, and their preparation and use as pharmaceuticals | 01-05-2012 |
20120004213 | NOVEL PIPERAZINE DERIVATIVES AS INHIBITORS OF STEAROYL-CoA DESATURASE - The present invention relates to piperazine derivatives that act as inhibitors of stearoyl-CoA desaturase. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds. | 01-05-2012 |
20120010196 | METHODS OF TREATING NEURODEGENERATIVE DISORDERS AND DISEASES - This invention is directed to a novel method of treating neurodegenerative disorders and diseases. Another, related aspect of this invention is directed to a screening method of identifying compounds that can be used to treat neurodegenerative disorders and diseases. The foregoing aspects of the invention particularly relate to neurodegenerative disorders and diseases have degeneration of neuronal axons as part of their pathologies. The method of treatment involves administering a pharmaceutical formulation that comprises a compound or mixture of compounds that inhibits one or more intracellular signaling mechanism that regulate axon degeneration or growth cone collapse. The screening method aspect of the invention identifies test compounds that can be used for the treatment or prevention of neurodegenerative disorders based on the test compound's ability to inhibit axon degeneration or growth cone collapse. | 01-12-2012 |
20120015937 | Kinase Inhibitors And Their Uses - The present disclosure provides compounds that inhibit protein kinases, such as JAK, Axl, or Syk kinases, compositions comprising the compounds and methods of using the compounds to inhibit protein kinase and treat and/or prevent diseases associated with inappropriate kinase activity. | 01-19-2012 |
20120022049 | NICOTINIC RECEPTOR AGONISTS FOR THE TREATMENT OF INFLAMMATORY DISEASES - Nicotine receptor agonists or analogs or derivatives thereof for treating inflammatory pulmonary diseases, and pharmaceutical compositions including nicotine receptor agonists or analogs or derivatives thereof. Compounds of formula wherein R1, R2, Xa and Ya are as defined herein are also provided. | 01-26-2012 |
20120028963 | NOVEL HYDROXAMATE DERIVATIVE, A PRODUCTION METHOD FOR THE SAME, AND A PHARMACEUTICAL COMPOSITION COMPRISING THE SAME - The present invention relates to hydroxamate derivatives, isomers thereof, pharmaceutically acceptable salts thereof, hydrates thereof, or solvates thereof, the use thereof for preparing pharmaceutical compositions, pharmaceutical compositions containing the same, a method of treating disease using the compositions, and a method for preparing the hydroxamate derivatives. | 02-02-2012 |
20120035159 | SUBSTITUTED ISOQUINOLINE DERIVATIVE - The present invention provides an isoquinoline-6-sulfonamide derivative that is useful as a novel pharmaceutical agent. The present invention provides an isoquinoline-6-sulfonamide derivative represented by Formula (1), a salt thereof, or a solvate of the derivative or the salt: wherein X and Y each independently represent a direct bond, NH, CH═CH, O, or S; R | 02-09-2012 |
20120040969 | N-PHENYL-(PIPERAZINYL OR HOMOPIPERAZINYL)-BENZENESULFONAMIDE OR BENZENESULFONYL-PHENYL-(PIPERAZINE OR HOMOPIPERAZINE) COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE SEROTONIN 5-HT6 RECEPTOR - The present invention relates to N-phenyl-(piperazinyl or homopiperazinyl)-benzenesulfonamide or benzenesulfonyl-phenyl-(piperazine or homopiperazine) compounds, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating diseases that respond to modulation of the serotonin 5-HT | 02-16-2012 |
20120046277 | BENZOFURAN DERIVATIVES - The present invention provides a compound represented by the following formula (I): wherein: Ring A represents an optionally substituted piperazine ring, an optionally substituted morpholine ring, or an optionally substituted bromopiperazine ring; R | 02-23-2012 |
20120046278 | THIAZOLOPYRIMIDINE MODULATORS AS IMMUNOSUPPRESSIVE AGENTS - The present invention relates to compound of formula I, II, III, or IV, and/or a pharmaceutical acceptable addition salt thereof and/or a stereoisomer thereof and/or a solvate thereof, wherein R | 02-23-2012 |
20120065192 | N-ARYL-2-(2-ARYLAMINOPYRIMIDIN-4-YL)PYRROL-4-CARBOXAMIDE DERIVATIVES AS MPS1 KINASE INHIBITORS - The present invention relates to substituted pyrrolyl-pyrimidines which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular MPS1. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such these compounds or the pharmaceutical compositions containing them. | 03-15-2012 |
20120065193 | Cyclopropyl Amide Derivatives '978 - Disclosed herein is at least one cyclopropyl amide derivative, at least one pharmaceutical composition comprising at least one cyclopropyl amide derivative disclosed herein, and at least one method of using at least one cyclopropyl amide derivative disclosed herein for treating at least one histamine H3 receptor associated condition therewith. | 03-15-2012 |
20120071467 | AMIDE DERIVATIVE - Compounds or pharmacologically acceptable salts thereof are provided. In various embodiments the compounds have an antagonistic effect on a neurokinin NK | 03-22-2012 |
20120088753 | PYRROLOPYRIMIDINES AND USED AS KINASE INHIBITORS - The invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or ester thereof, wherein: R | 04-12-2012 |
20120088754 | SULFONYL-DERIVATIVES AS NOVEL INHIBITORS OF HISTONE DEACETYLASE - This invention comprises the novel compounds of formula (I) | 04-12-2012 |
20120094980 | PYRIDYL INHIBITORS OF HEDGEHOG SIGNALLING - The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: | 04-19-2012 |
20120094981 | ANTHELMINTIC AGENTS AND THEIR USE - This invention is directed to compounds of the formula (I) and salts therefore that are generally useful as anthelmintic agents or as intermediates in processes for making anthelmintic agents. This invention also is directed to processes for making the compounds of this invention, pharmaceutical compositions and kits comprising the compounds of this invention, uses of the compounds of this invention to make medicaments, and treatments comprising the administration of the compounds of this invention to animals in need of the treatments. | 04-19-2012 |
20120101087 | Generation of Combinatorial Synthetic Libraries and Screening for Novel Proadhesins and Nonadhesins - The present invention relates to, in part, novel bisphenol compounds useful for the recognition, attachment and growth of unwanted biologics on natural and manmade surfaces. Another aspect of the invention relates to combinatorial libraries for producing the same. Another aspect of the invention relates to pharmaceutical formulations comprising the same. | 04-26-2012 |
20120108573 | SULFUR SUBSTITUTED SULFONYLAMINOCARBOXYLIC ACID N-ARYLAMIDES, THEIR PREPARATION, THEIR USE AND PHARMACEUTICAL PREPARATIONS COMPRISING THEM - The present invention relates to compounds of the formula I | 05-03-2012 |
20120115850 | SUBSTITUTED ARYLAMINE COMPOUNDS AND METHODS OF TREATMENT - The invention relates to 5-HT | 05-10-2012 |
20120115851 | COMPOUND INHIBITING IN VIVO PHOSPHORUS TRANSPORT AND MEDICINE CONTAINING THE SAME - An objective of the present invention is to provide compounds that can effectively suppress the concentration of phosphorus in serum to effectively prevent or treat diseases induced by an increase in concentration of phosphate in serum. The compounds according to the present invention are compounds represented by formula (I) and pharmaceutically acceptable salts and solvates thereof: | 05-10-2012 |
20120122849 | PKM2 MODULATORS FOR USE IN THE TREATMENT OF CANCER - Compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are pharmaceutical compositions comprising the compounds, and methods of using the compounds in the treatment of cancer. | 05-17-2012 |
20120122850 | BIPHENYL COMPOUNDS USEFUL AS MUSCARINIC RECEPTOR ANTAGONISTS - The invention provides compounds of formula I: | 05-17-2012 |
20120129841 | CARBOLINE DERIVATIVES USEFUL IN THE TREATMENT OF CANCER AND OTHER DISEASES - In accordance with the present invention, compounds that inhibit the expression of VEGF post-transcriptionally have been identified, and compositions, and methods for the administration and use of those compounds. provided. In one aspect of the invention, compounds useful in the inhibition of VEGF production, in the treatment of solid tumor cancer, and in reducing serum, plasma, and/or tumor VEGF levels, are provided. In another aspect of the invention, methods are provided for the inhibition of VEGF production, the treatment of cancer, and the reduction of plasma and/or tumor VEGF levels, using the compounds of the invention. | 05-24-2012 |
20120129842 | BISTHIAZOLE INHIBITORS OF PRO-MATRIX METALLOPROTEINASE ACTIVATION - This invention relates to bisthiazole I and its therapeutic and prophylactic uses, wherein the variables A, R | 05-24-2012 |
20120129843 | PYRIDYL-THIAZOLYL INHIBITORS OF PRO-MATRIX METALLOPROTEINASE ACTIVATION - This invention relates to thiazole I and its therapeutic and prophylactic uses, wherein the variables R | 05-24-2012 |
20120129844 | N-[5-[2-(3,5-DIMETHOXYPHENYL)ETHYL]-1H-PYRAZOL-3-YL]-4-(3,4-DIMETHYLPIPERA- ZIN-1-YL)BENZAMIDE AND SALTS THEREOF - There is provided a compound of formula (I): | 05-24-2012 |
20120135983 | DNA Damage Repair Inhibitors for the Treatment of Cancer - The present invention relates to the recognition that inhibition of the base excision repair pathway is selectively lethal in cells which are deficient in HR dependent DNA DSB repair. Methods and means relating to the treatment of cancers which are deficient in HR dependent DNA DSB repair using inhibitors which target base excision repair components, such as PARP, is provided herein. | 05-31-2012 |
20120135984 | DUAL-ACTION INHBITORS AND METHODS OF USING SAME - Provided are compounds, compositions, and methods for treating diseases and conditions wherein an inhibitor of a kinase, such as rho kinase (ROCK), and an inhibitor of one or more of the monoamine transporters, such as NET or SERT, act in concert to improve the condition. | 05-31-2012 |
20120142674 | N-PHENYL-(HOMO)PIPERAZINYL-BENZENESULFONYL OR BENZENESULFONAMIDE COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO THE MODULATION OF THE SEROTONIN 5-HT6 RECEPTOR - The present invention relates to N-Phenyl-(homo)piperazinyl-benzenesulfonyl or benzenesulfonamide compounds of formula I | 06-07-2012 |
20120184534 | TRI-CYCLIC PYRAZOLOPYRIDINE KINASE INHIBITORS - The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions. | 07-19-2012 |
20120184535 | COMPOUND, A PROCESS FOR ITS PREPARATION, A PHARMACEUTICAL COMPOSITION, USE OF A COMPOUND, A METHOD FOR MODULATING OR REGULATING SERINE/THREONINE KINASES AND A SERINE/THREONINE KINASES MODULATING AGENT - A compound, a process for its preparation, a pharmaceutical composition, use of a compound, a method for modulating or regulating serine/threonine and tyrosine kinases and a serine/threonine and tyrosine kinases modulating agent. Novel small-molecule compounds with kinase inhibitory activity, having superior properties as pharmaceutical agents, production method thereof and uses thereof. In particular, new derivatives of tetrahalogenated benzimidazole with serine/threonine and tyrosine kinases inhibitory properties, preferably selected from the group of PIM, HIPK, DYRK, CLK, CDK, FLT, PKG, Haspin, MER, TAO, MNK, TRK kinases which exhibit superior pharmacological actions, and can be useful for the treatment of disease conditions, especially cancers depending on serine/threonine and tyrosine kinases, such as but not limited to leukemias and solid tumors. | 07-19-2012 |
20120190669 | OXINDOLE COMPOUNDS - The invention provides compounds that inhibit PIM kinases and Flt3 kinase, and compositions containing such compounds. These compounds and compositions are useful for treating proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation. | 07-26-2012 |
20120202793 | RHO KINASE INHIBITORS - The present invention relates to inhibitors of ROCK1 and ROCK2, which may be selective for ROCK2, and methods of modulating the pharmacokinetic and/or pharmacodynamic properties of such compounds. Also provided are methods of inhibiting ROCK1 and/or ROCK2. Also provided are treatments combining inhibitors of ROCK1 and/or ROCK2 with statins. | 08-09-2012 |
20120202794 | COMPOUNDS - Disclosed herein are compounds useful for treating a viral infection, such as HCV. | 08-09-2012 |
20120202795 | SUBSTITUTED PYRIDONES AS INHIBITORS OF POLY(ADP-RIBOSE) POLYMERASE (PARP) - The present invention relates to a series of 2,3,5-substituted pyridone derivatives of formula I: | 08-09-2012 |
20120208798 | Tetrahydroquinoline Derivatives And Their Pharmaceutical Use - Tetrahydroquinoline compounds of formula (I) | 08-16-2012 |
20120208799 | COMPOUNDS - The present invention relates to compounds of formula (I) | 08-16-2012 |
20120214798 | Novel Ethanediamone Hepcidine Antagonists - The present invention relates to novel hepcidin antagonists of formula (I), pharmaceutical compositions comprising them and the use thereof as medicaments, in particular for treatment of disorders in iron metabolism, such as, in particular, iron deficiency diseases and anaemias, in particular anaemias in connection with chronic inflammatory diseases (ACD: anaemia of chronic disease and AI: anaemia of inflammation). | 08-23-2012 |
20120214799 | KINASE INHIBITORS - The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions. | 08-23-2012 |
20120214800 | Organic Compounds - The present invention concerns a compound of formula (I) | 08-23-2012 |
20120225864 | Methods and Compositions for Modulating Tau Levels - Methods and agents for reducing a level of an acetylated Tau polypeptide in a cell are provided. Methods for treating a tauopathy in an individual are also provided. Also provided is a method for diagnosing a cognitive impairment disorder in an individual. Methods for identifying an agent suitable for treating a tauopathy are also provided. | 09-06-2012 |
20120232064 | ASPARTYL PROTEASE INHIBITORS - Disclosed are compounds of formula I | 09-13-2012 |
20120245148 | TETRAHYDROQUINOXALINE UERA DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION - The present invention relates to tetrahydroquinoxaline urea derivatives, to their preparation and to their therapeutic application. | 09-27-2012 |
20120245149 | NOVEL (HETEROCYCLE/CONDENSED PIPERIDINE)-(PIPERAZINYL)-1-ALKANONE OR (HETEROCYCLE/CONDENSED PYRROLIDINE)-(PIPERAZINYL)-1-ALKANONE DERIVATIVES AND USE THEREOF AS p75 INHIBITORS - The disclosure relates to (heterocycle-fused piperidine)-(piperazinyl)-1-alkanone derivatives and (heterocycle-fused pyrrolidine)-(piperazinyI)-1-alkanone derivatives of formula (I): | 09-27-2012 |
20120245150 | NOVEL (HETEROCYCLE/TETRAHYDROPYRIDINE)-(PIPERAZINYL)-1-ALCANONE AND (HETEROCYCLE/DIHYDROPYRROLIDINE)-(PIPERAZINYL)-1-ALCANONE DERIVATIVES, AND USE THEREOF AS p75 INHIBITORS - The disclosure relates to (heterocycle-tetrahydropyridine)(piperazinyl)-1-alkanone and (heterocycle-dihydropyrrolidine)(piperazinyl)-1-alkanone derivatives of formula (I): | 09-27-2012 |
20120252792 | METHODS AND COMPOSITIONS FOR MODULATING RHO-MEDIATED GENE TRANSCRIPTION - The invention provides methods, compositions, and kits for the inhibition of members of the Rho GTPase family. Specifically, the invention provides methods, compositions and kits for the inhibition of RhoA and/or RhoC transcriptional signalling. The invention finds use in treatment of Rho-mediated disease states (e.g., tumor metastasis, inflammation, inflammatory disease), Rho-mediated biological conditions, and in cell signaling research. | 10-04-2012 |
20120258960 | NOVEL MULTIFUNCTIONAL PEPTIDASE INHIBITORS, ESPECIALLY FOR MEDICAL USE - The invention relates to compounds of the general formula (1) or the acid addition salts thereof with organic and/or inorganic acids; as well as to the use of the compounds of the general formula (1) in medicine. | 10-11-2012 |
20120270859 | INDOLINE DERIVATIVES AND THEIR USE IN TREATING DISEASE-STATES SUCH AS CANCER - The present invention encompasses compounds of general formula (1) | 10-25-2012 |
20120277218 | METHODS AND PHARMACEUTICAL COMPOSITIONS FOR TREATING DOWN SYNDROME - The compounds and pharmaceutical compositions of the present invention are believed to significantly inhibit Dyrk 1a activity which suggests that the agents could provide therapeutic benefit for Down syndrome, since Dyrk 1a overproduction in Down syndrome appears to account for the developmental cognitive impairment and reduction in neurogenesis. The compounds and pharmaceutical compositions, administered during early post-natal development, may increase neurogenesis and thereby reduce cognitive impairment which may ultimately allow individuals with Down syndrome to live a more independent life. | 11-01-2012 |
20120277219 | NOVEL PYRIDOPYRAZINE DERIVATIVES, PROCESS OF MANUFACTURING AND USES THEREOF - The invention relates to pyrido[2,3-b]pyrazine compounds of general formulae (Ia) and (Ib), to their preparation and use, for example, for the treatment of malignant disorders and other disorders based on pathological cell proliferations. | 11-01-2012 |
20120277220 | 5 OXO-5,8-DIHYDROPYRIDO[2,3-d]PYRIMIDINE DERIVATIVES AS CAMKII KINASE INHIBITORS FOR TREATING CARDIOVASCULAR DISEASES - The present invention relates to 5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine derivatives, to their preparation and to their therapeutic use. | 11-01-2012 |
20120283247 | DIAZEPANE ACETAMIDE DERIVATIVES AS SELECTIVE 11B-HSD1 INHIBITORS - The present invention relates to diazepane-acetamide 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. | 11-08-2012 |
20120295891 | NOVEL SUBSTITUTED TRIAZOLE DERIVATIVES AS GAMMA SECRETASE MODULATORS - The present invention is concerned with novel substituted triazole derivatives of Formula (I) | 11-22-2012 |
20120302553 | PHENYL-PIPERAZINE DERIVATIVES AS SEROTONIN REUPTAKE INHIBITORS - The invention provides compounds represented by the general formula I | 11-29-2012 |
20120309746 | TRIAZOLOPYRIDINE COMPOUNDS - The present invention relates to the use of novel triazolopyridine derivatives of formula I: | 12-06-2012 |
20120316155 | Imidazole-2,4-Dione Inhibitors of Casein Kinase 1 - Disclosed are compounds, pharmaceutical compositions containing those compounds, and uses of the compounds and compositions as modulators of casein kinase 1 (e.g., CK1γ), the TGFβ pathway and/or the Wnt pathway. Uses are also disclosed for the treatment or prevention of a range of therapeutic indications due at least in part to aberrant physiological activity of casein kinase 1 (e.g., CK1γ), the TGFβ pathway and/or the Wnt pathway. | 12-13-2012 |
20120329784 | COMPOUNDS AND METHODS - Disclosed are compounds having the formula: | 12-27-2012 |
20130005710 | AMINOPYRIDINE DERIVATIVE - The present invention provides a novel aminopyridine derivative that is excellent in pharmaceutical effects such as a neuroprotective effect, a neurogenesis or nerve regeneration promoting effect, and a cognitive function improving effect and, preferably, is low toxic and delivered at a high rate to the central nervous system. Specifically, the present invention provides a compound represented by the formula (I), wherein ring A represents a monocyclic aromatic hydrocarbon ring or the like; ring B may further have a substituent(s); ring D represents a monocyclic aromatic hydrocarbon ring or the like; L represents a bond, or a methylene group or the like; X represents —NRa- or the like, wherein Ra represents a hydrogen atom or the like; n represents 1 or 2; and R | 01-03-2013 |
20130005711 | FASUDIL IN COMBINATION THERAPIES FOR THE TREATMENT OF PULMONARY ARTERIAL HYPERTENSION - Preferred embodiments of the present invention are related to novel therapeutic drug combinations and methods for treating and/or preventing pulmonary arterial hypertension and/or stable angina. More particularly, aspects of the present invention are related to therapeutic combinations comprising a Rho-kinase inhibitor, such as fasudil, and one or more additional compounds selected from the group consisting of prostacyclins, such as iloprost, endothelin receptor antagonists, PDE inhibitors, calcium channel blockers, 5-HT | 01-03-2013 |
20130012500 | ORGANIC COMPOUNDS - A compound of Formula I | 01-10-2013 |
20130018045 | New Chemical Entities To Be Used For Wee1 Inhibition For The Treatment Of Cancer - The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, | 01-17-2013 |
20130018046 | Acetylenic Heteroaryl Compounds - This invention relates to compounds of the general formula: | 01-17-2013 |
20130018047 | N-PHENYL-(PIPERAZINYL OR HOMOPIPERAZINYL)-BENZENESULFONAMIDE OR BENZENESULFONYL-PHENYL-(PIPERAZINE OR HOMOPIPERAZINE) COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE SEROTONIN 5-HT6 RECEPTOR - The present invention relates to N-phenyl-(piperazinyl or homopiperazinyl)-benzenesulfonamide or benzenesulfonyl-phenyl-(piperazine or homopiperazine) compounds, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating diseases that respond to modulation of the serotonin 5-HT | 01-17-2013 |
20130023522 | BENZAMIDES - Novel benzamide derivatives of formula (I) | 01-24-2013 |
20130023523 | PYRIDAZINO[4,5-D]PYRIMIDIN-5(6H)-ONE INHIBITORS OF KINASES - The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, | 01-24-2013 |
20130035329 | THERAPEUTICALLY ACTIVE COMPOSITIONS AND THEIR METHODS OF USE - Compounds and compositions comprising compounds useful in the treatment of cancer are described herein. | 02-07-2013 |
20130053370 | THIENO[3,2-d]PYRIMIDINE DERIVATIVES HAVING INHIBITORY ACTIVITY ON PROTEIN KINASES - The present invention relates to a thieno[3,2-d]pyrimidine derivative of formula (I), or a pharmaceutically acceptable salt, hydrate or solvate thereof, which has an excellent inhibitory activity on protein kinases, and a pharmaceutical composition comprising the same is effective in preventing or treating abnormal cell growth diseases. | 02-28-2013 |
20130053371 | INHIBITORS OF PI3 KINASE - There is provided compounds of formula (I), wherein A | 02-28-2013 |
20130053372 | 5-HT RECEPTOR MODULATORS - The invention relates to compounds of formula (I), useful for treating disorders mediated by the 5-hydroxytryptamine (serotonin) receptor IB (5-HT1B), e.g. vascular disorders, cancer and CNS disorders. The invention also provides methods of treating such disorders, and compounds and compositions etc. for their treatment. | 02-28-2013 |
20130059839 | PYRIDYLTHIAZOLE-BASED UREAS AS INHIBITORS OF RHO ASSOCIATED PROTEIN KINASE (ROCK) AND METHODS OF USE - Compounds and compositions having activity as inhibitors of Rho-associated proteinkinases (ROCKs), and methods of making and using the subject compounds are disclosed. | 03-07-2013 |
20130085135 | 5H-CYCLOPENTA[D]PYRIMIDINES AS AKT PROTEIN KINASE INHIBITORS - Compounds of Formula I are useful for inhibiting AKT protein kinases. Methods of using compounds of Formula I and stereoisomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed. | 04-04-2013 |
20130102592 | OXAZOLE TYROSINE KINASE INHIBITORS - The invention provides a compound which is an amide of the formula (1), or a salt, solvate, N-oxide or tautomer thereof; wherein: a is 0 or 1; b is 0 or 1: provided that the sum of a and b is 0 or 1; T is O or NH Ar | 04-25-2013 |
20130109678 | RADIOPROTECTOR COMPOUNDS AND METHODS | 05-02-2013 |
20130123243 | DIAMINE DERIVATIVES AS INHIBITORS OF LEUKOTRIENE A4 HYDROLASE - This invention is directed to compounds of formula (I): | 05-16-2013 |
20130131047 | PHARMACOKINETICALLY IMPROVED COMPOUNDS - The present invention relates to inhibitors of ROCK1 and ROCK2 and methods of modulating the pharmacokinetic and/or pharmacodynamic properties of such compounds. Also provided are methods of inhibiting ROCK1 and or ROCK2 that are useful for the treatment of disease. | 05-23-2013 |
20130137679 | Novel Functionally Selective Ligands of Dopamine D2 Receptors - The present invention relates to novel functionally selective ligands of dopamine D2 receptors, FIG. | 05-30-2013 |
20130150349 | 2,4-PYRIMIDINEDIAMINE COMPOUNDS AND THEIR USES - The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades. | 06-13-2013 |
20130158015 | DUAL MECHANISM INHIBITORS FOR THE TREATMENT OF DISEASE - Provided are compounds that are inhibitors of both rho kinase and of a monoamine transporter (MAT) act to improve the disease state or condition. Further provided are compositions comprising the compounds. Further provided are methods for treating diseases or conditions, the methods comprising administering compounds according to the invention. One such disease may be glaucoma for which, among other beneficial effects, a marked reduction in intraocular pressure (IOP) may be achieved. | 06-20-2013 |
20130172325 | NOVEL HOMOPIPERAZINE DERIVATIVES AS PROTEIN TYROSINE KINASE INHIBITORS AND PHARMACEUTICAL USE THEREOF - The invention relates to compounds of general formula (I) wherein R | 07-04-2013 |
20130172326 | DERIVATIVES OF HETEROARYLSULFONAMIDES, THEIR PREPARATION AND THEIR APPLICATION IN HUMAN THERAPY - The present invention concerns derivatives of heteroarylsulfonamides, notably as blockers of Kv potassium channels, and more particularly of channels Kv1.5, Kv4.3 or Kv11.1, their application in clinical therapy and their preparation methods. These compounds correspond to the following general formula (I): where R1 represents one or more substituents of the phenyl core X such as: hydrogen, halogen, trifluoromethyl, trifluoromethoxy, linear or branched C | 07-04-2013 |
20130184263 | Derivatives of Betulin - The present invention relates to compounds characterized by having a structure according to the following Formula I: | 07-18-2013 |
20130190297 | Antiviral Activity of Novel Bicyclic Heterocycles - The present invention relates to compound of Formula I, II, III, or IV, and/or a pharmaceutical acceptable addition salt thereof and/or a stereoisomer thereof and/or a solvate thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R11, and R12 are as defined in the claim | 07-25-2013 |
20130190298 | SUBSTITUTED PYRIDAZINE CARBOXAMIDE COMPOUNDS - The new pyridazine derivatives have unexpected drug properties as inhibitors of protein kinases especially against ALK and are useful in treating disorders related to abnormal protein kinase activities such as cancer, neurological and psychiatric diseases. | 07-25-2013 |
20130196979 | Bicyclic Heteroaryl Compounds - This invention relates to compounds of the general formula: | 08-01-2013 |
20130210811 | PICOLINAMIDE AND PYRIMIDINE-4-CARBOXAMIDE COMPOUNDS, PROCESS FOR PREPARING AND PHAMACEUTICAL COMPOSITION COMPRISING THE SAME - Provided are picolinamide and pyrimidine-4-carboxamide compounds, a method for preparing the same, a pharmaceutical composition containing the same, and a medical use using the compound as an agent for preventing, regulating, and treating diseases related to regulation of glucocorticoids by using selective inhibitory activity of the compound for an 11β-HSD1 enzyme. The picolinamide and pyrimidine-4-carboxamide compounds of the present invention are selective inhibitors of human-derived 11β-HSD1 enzymes, and are useful in an agent for preventing, regulating, and treating diseases related to glucocorticoid regulation in which human-derived 11β-HSD1 enzymes are involved, for example, metabolic syndromes such as, type 1 and type 2 diabetes, diabetes later complications, latent autoimmune diabetes adult (LADA), insulin tolerance syndromes, obesity, impaired glucose tolerance (IGT), impaired fasting glucose (IFG), damaged glucose tolerance, dyslipidemia, atherosclerosis, hypertension, etc. | 08-15-2013 |
20130210812 | Aqueous Pharmaceutical Composition With Enhanced Stability - The present invention is an aqueous pharmaceutical composition that includes an ionized therapeutic agent, an ionic component and guar gum. The guar gum is present in the composition a concentration sufficient to limit interactions between the ionized therapeutic agent and the ionic component thereby imparting stability to the composition. The composition is preferably at or near physiologic pH. The aqueous pharmaceutical composition has been found particularly useful as an aqueous ophthalmic, otic or nasal composition. The pharmaceutical composition, due to its characteristics, is particularly suitable as an ophthalmic composition. | 08-15-2013 |
20130217680 | Inhibitors of the Renal Outer Medullary Potassium Channel - This invention relates to compounds having structural Formula (I); and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir 1.1). The compounds of Formula I are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure. | 08-22-2013 |
20130225562 | PYRIDYLTRIAZOLES - The present invention encompasses compounds of general formula (1) wherein the groups R | 08-29-2013 |
20130225563 | METHODS OF MODULATING THE ACTIVITY OF THE MC5 RECEPTOR AND TREATMENT OF CONDITIONS RELATED TO THIS RECEPTOR - The present invention provides compounds of Formula (I) that are useful for modulating the biological activity of the melanocortin-5 receptor (MC5R). Compounds of this invention can be used to treat diseases and/or conditions in which downregulation of MC5R is beneficial. Such diseases and/or conditions include, but are not limited to, acne, seborrhea, seborrheic dermatitis, cancer, and inflammatory diseases. | 08-29-2013 |
20130225564 | HALOARYL SUBSTITUTED AMINOPURINES, COMPOSITIONS THEREOF,AND METHODS OF TREATMENT THEREWITH - Provided herein are Aminopurine Compounds having the following structure: | 08-29-2013 |
20130225565 | 2,5-DISUBSTITUTED ARYLSULFONAMIDE CCR3 ANTAGONISTS - Provided herein are 2,5-disubstituted arylsulfonamides that are useful for modulating CCR3 activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition. | 08-29-2013 |
20130231332 | SMALL MOLECULE INHIBITORS OF EBOLA AND LASSA FEVER VIRUSES AND METHODS OF USE - The present invention relates to compositions and methods for the treatment of infection by enveloped viruses, such as Ebola and Lassa fever viruses. | 09-05-2013 |
20130237529 | COMPOUND THAT CAN INHIBIT UBC13-UEV INTERACTIONS, PHARMACEUTICAL COMPOSITIONS AND THERAPEUTIC USES - The invention relates to a compound (I) wherein R is a heterocyclyl radical; R | 09-12-2013 |
20130245006 | NOVEL INDOLIZINE DERIVATIVES, AND PREPARATION AND THERAPEUTIC USE THEREOF - The invention relates to indolizine derivatives of general formula (I), where A, B, m, W, n and R2 are as defined in claim | 09-19-2013 |
20130267502 | Treatment of Addiction and Impulse-Control Disorders Using PDE7 Inhibitors - This disclosure is directed to treatment of addictions and primary impulse-control disorders using phosphodiesterase 7 (PDE7) inhibitors, alone or in combination with other therapeutic agents. | 10-10-2013 |
20130296306 | Modulators of ATP-Binding Cassette Transporters - Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention. | 11-07-2013 |
20130296307 | 1H-PYRAZOLO[3,4-B]PYRIDINES AND THERAPEUTIC USES THEREOF - Provided herein are compounds according to Formula I and pharmaceutically acceptable salts thereof, and compositions comprising the same, for use in various methods, including treating cancers such as colon, ovarian, pancreatic, breast, liver, prostate and hematologic cancers: | 11-07-2013 |
20130310370 | DRUG THERAPY FOR PREVENTING OR TREATING GLAUCOMA - There is provided a drug therapy for prevention of glaucoma or prevention or treatment of ocular hypertension, with a potent ocular hypotensive effect and prolonged duration thereof. Disclosed is a combination of (S)-(−)-1-(4-fluoro-5-isoquinolinesulfonyl)-2-methyl-1,4-homopiperazine or a salt thereof, or a solvate thereof, and a prostaglandin for prevention or treatment of glaucoma. | 11-21-2013 |
20130331379 | PROCESS FOR THE PREPARATION OF AN OREXIN RECEPTOR ANTAGONIST - The present invention is directed to processes for preparing a diazepane compound which is an antagonist of orexin receptors, and which is useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is further directed to crystalline forms of this diazepane compound and pharmaceutical compositions thereof. | 12-12-2013 |
20130345200 | INDOLES - Herein are disclosed indoles of formula (I) | 12-26-2013 |
20140018350 | COMBINATION OF SULFONAMIDE COMPOUND AND TAFLUPROST - The object of the present invention is to discover a combination of preventive or therapeutic drugs for glaucoma or ocular hypertension, which is useful as a preventive or therapeutic agent for glaucoma or ocular hypertension. By combining isopropyl(6-{[4-(pyrazol-1-yl)benzyl](pyridin-3-ylsulfonyl)aminomethyl}pyridin-2-ylamino)acetate with tafluprost, their intraocular pressure lowering effects are complemented and/or enhanced each other. As for the administration form, these drugs may be administered concomitantly or may be administered as a combination drug. | 01-16-2014 |
20140038945 | PIPERAZINE PDE4 INHIBITORS AND USES THEREOF - The invention includes a compound of formula I: | 02-06-2014 |
20140038946 | NOVEL (HETEROCYCLE/CONDENSED PIPERIDINE)-(PIPERAZINYL)-1-ALKANONE OR (HETEROCYCLE/CONDENSED PYRROLIDINE)-(PIPERAZINYL)-1-ALKANONE DERIVATIVES AND USE THEREOF AS p75 INHIBITORS - The disclosure relates to (heterocycle-fused piperidine)-(piperazinyl)-1-alkanone derivatives and (heterocycle-fused pyrrolidine)-(piperazinyl)-1-alkanone derivatives of formula (I): | 02-06-2014 |
20140045825 | Inhibitors of PI3K-Delta and Methods of Their Use and Manufacture - The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds. | 02-13-2014 |
20140045826 | METHODS AND COMPOSITIONS FOR TREATING NEURODEGENERATIVE DISEASES - The invention discloses methods and compositions for treating or preventing neurodegenerative disease by administering a compound of Formula I: or a pharmaceutically acceptable salt, solvate or hydrate thereof, wherein the variables are defined as herein. | 02-13-2014 |
20140066434 | Methods and Compositions for Treating Parkinson's Disease - The invention discloses methods and compositions for treating or preventing Parkinson's disease by administering a compound of Formula (I): or a pharmaceutically acceptable salt, solvate or hydrate thereof, wherein the variables are defined as herein. | 03-06-2014 |
20140088088 | ANTI-CANCER ACTIVITY OF NOVEL BICYCLIC HETEROCYCLES - The present invention relates to compound of formula I, II, III, or IV, and/or a pharmaceutical acceptable addition salt thereof and/or a stereoisomer thereof and/or a solvate thereof, Formulas (I), (II), (III) and (IV) wherein R | 03-27-2014 |
20140094451 | PREVENTIVE OR REMEDY FOR GLAUCOMA - There is provided a preventive for glaucoma or a preventive or a remedy for ocular hypertension, with a potent ocular hypotensive effect and prolonged duration thereof. A preventive or a remedy for glaucoma comprising a Rho kinase inhibitor and an α | 04-03-2014 |
20140107105 | SUBSTITUTED PYRIDYL AMIDE COMPOUNDS AS MODULATORS OF THE HISTAMINE H3 RECEPTOR - Certain substituted pyridyl amide compounds are histamine H | 04-17-2014 |
20140148443 | Novel Imidazolines as dual inhibitors of MDM2 and MDMX - Disclosed are compounds of Formula I | 05-29-2014 |
20140148444 | METHODS OF USING PYRUVATE KINASE ACTIVATORS - Described herein are compounds that activate pyruvate kinase, for use in a method for increasing lifetime of the red blood cells, for regulating 2,3-diphosphoglycerate levels in blood and for treating sickle cell anemia. | 05-29-2014 |
20140171421 | TREATING DISEASES MEDIATED BY BLOCKADE OF THE EPITHELIAL SODIUM CHANNEL WITH PYRAZINE-2-CARBOXAMIDE DERIVATIVES - A compound of Formula I | 06-19-2014 |
20140179688 | PLOD-2 Modulators and Their Use in the Treatment of Skin - Methods for preventing, ameliorating, or reducing dermatological signs of aging are provided which employ active agents that modulate the PLOD-2 enzyme in the skin. Also provided are methods for screening for substances which modulate PLOD-2 enzyme levels and the methods of using active agents identified by the screening protocol in the treatment of skin. | 06-26-2014 |
20140179689 | NOVEL RHO KINASE INHIBITORS AND METHODS OF USE - The subject invention concerns materials and methods for treating diseases and disorders associated with expression of Rho associated kinases (ROCKs). Examples of diseases and disorders contemplated within the scope of the invention include, but are not limited to, oncological disorders, cardiovascular diseases, CNS disorders, and inflammatory disorders. In one embodiment, a method of the invention comprises administering a therapeutically effective amount of one or more compounds of the present invention, or a composition comprising the compounds, to a person or animal in need of treatment. The subject invention also concerns compounds that inhibit ROCKs, and compositions that comprise the inhibitor compounds of the invention. Compounds contemplated within the scope of the invention include, but are not limited to, those compounds shown in Table 5. | 06-26-2014 |
20140187540 | COMPOUNDS AND METHODS OF USE THEREOF FOR TREATING NEURODEGENERATIVE DISORDERS - Compounds, compositions, kits and methods for treating conditions related to neurodegeneration or ocular disease, are disclosed. | 07-03-2014 |
20140206673 | THERAPEUTICALLY ACTIVE COMPOSITIONS AND THEIR METHODS OF USE - Provided are compounds of formula (I), wherein X, Y, Z, W, V, R | 07-24-2014 |
20140213580 | THERAPEUTICALLY ACTIVE COMPOSITIONS AND THEIR METHODS OF USE - Provided are compounds with the following structure, formula (I) pharmaceutically acceptable salts thereof, use of those compounds for treating cancer and pharmaceutical compositions comprising those compounds. | 07-31-2014 |
20140221354 | IMIDAZO [1,2-a]PYRIDINE COMPOUNDS FOR USE IN THERAPY - The present invention provides novel imidazo[1,2-a]pyridine compounds that are useful in therapy of diseases and disorders. The novel compounds inhibit the activation of Hypoxia Inducible Factor (HIF)-mediated transcription and signaling under hypoxic conditions. In one aspect, the compounds of the present invention are useful for the preparation of a medicament for the treatment or prevention of a disease or disorder selected from the group consisting of an inflammatory disease, a hyperproliferative disease or disorder, a hypoxia-related pathology and a disease characterized by excessive vascularization. Also provided is a pharmaceutical composition, comprising a compound of the invention and a second therapeutic agent or radiation, useful for the treatment or prevention of the mentioned diseases or disorders, wherein X is CH | 08-07-2014 |
20140235619 | AGENTS AND METHODS FOR TREATING ISCHEMIC AND OTHER DISEASES - This invention relates to methods of screening for modulators of mammalian cell injury cause by TRPM7 gene and protein activity, compounds that modulate TRPM7 gene and protein activity and methods of treatment of mammalian cell injury using modulators of TRPM7 gene and protein activity. | 08-21-2014 |
20140235620 | 3-PYRIMIDIN-4-YL-OXAZOLIDIN-2-ONES AS INHIBITORS OF MUTANT IDH - The invention is directed to a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R | 08-21-2014 |
20140243320 | NOVEL COMPOUND HAVING PARP INHIBITORY ACTIVITY - A compound represented by the following general formula (1) or a salt thereof. R | 08-28-2014 |
20140249137 | PYRIMIDINE COMPOUNDS AS TUBERCULOSIS INHIBITORS - The present invention relates to compounds useful as inhibitors of treating tuberculosis. The invention also provides processes for preparing compounds of the inventions and | 09-04-2014 |
20140249138 | AZAINDOLES USEFUL AS INHIBITORS OF JAK AND OTHER PROTEIN KINASES - The present invention relates to inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders. | 09-04-2014 |
20140249139 | Quinazoline Derivatives - The invention relates to substituted quinazoline derivative of the formula (I), wherein A, X | 09-04-2014 |
20140275040 | NEW COMPOUNDS - The present invention relates to compounds which are inhibitors of SSAO activity. The invention also relates to pharmaceutical compositions comprising these compounds and to the use of these compounds in the treatment or prevention of medical conditions wherein inhibition of SSAO activity is beneficial, such as inflammatory diseases, immune disorders and the inhibition of tumor growth. | 09-18-2014 |
20140275041 | OXAZOLE TYROSINE KINASE INHIBITORS - The invention provides a compound which is an amide of the formula (1), or a salt, solvate, N-oxide or tautomer thereof; wherein: a is 0 or 1; b is 0 or 1: provided that the sum of a and b is 0 or 1; T is O or NH Ar | 09-18-2014 |
20140296214 | SUBSTITUTED TETRAHYDROISOQUINOLINE COMPOUNDS AS FACTOR XIA INHIBITORS - The present invention provides compounds of Formula (I): or stereoisomers, pharmaceutically acceptable salts thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of factor XIa and/or plasma kallikrein which may be used as medicaments. | 10-02-2014 |
20140296215 | Cyanoquinoline Compounds Having Activity in Correcting Mutant-Cftr Processing and Increasing Ion Transport and Uses Thereof - The present disclosure provides pharmaceutical compositions, pharmaceutical preparations and methods for increasing activity of a mutant cystic fibrosis transmembrane conductance regulator protein (mutant-CFTR). The pharmaceutical compositions, pharmaceutical preparations and methods are useful for the study and treatment of disorders associated with mutant-CFTR, such as cystic fibrosis. The pharmaceutical compositions and pharmaceutical preparations may include one or more cyanoquinoline-containing compounds of the embodiments, or an analog or derivative thereof. | 10-02-2014 |
20140296216 | PYRIMIDO[4,5-D]PYRIMIDINYL COMPOUNDS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF - A compound of formula (I) or (II) and use of the compound in the preparation of drugs for treating cancer are disclosed. The study shows that the compounds can inhibit the growth of many kinds of tumor cells, can be used for targeting epidermal growth factor receptor (EGFR), and particularly can inhibit tumor cells with single or multiple mutations of EGFR (T790M). Therefore, the compound can be used as EGFR inhibitor to treat cancer and has a relatively large application value. | 10-02-2014 |
20140296217 | MEDICAMENTS FOR THE TREATMENT OR PREVENTION OF FIBROTIC DISEASES - The present invention relates to the use of indolinones of general formula | 10-02-2014 |
20140303151 | Inhibitors of PI3K-Delta and Methods of Their Use and Manufacture - The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds. | 10-09-2014 |
20140309216 | PHARMACEUTICAL COMPOUNDS - Compounds of Formulae Ia, and stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. | 10-16-2014 |
20140357623 | NEW ENZYME INHIBITOR COMPOUNDS - 2-{4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}ethan-1-amine; 3-aminopropyl 4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidine-1-carboxylate; 1-{4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}-4-(dimethylamino)butan-1-one; 5-amino-1-{4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}pentan-1-one; N-(2-aminoethyl)-4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidine-1-carboxamide; N-(3-aminopropyl)-4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidine-1-carboxamide; 4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]-N-[3-(dimethylamino)propyl]piperidine-1-carboxamide; 1-({4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}carbonyl)piperazine; 4-({4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}carbonyl)morpholine; 1-({4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}carbonyl)-1,4-diazepane; ethyl 1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-4-carboxylate; ethyl 1-[1-(4-methylphenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-4-carboxylate; 1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-4-carboxylic acid; N-(2-aminoethyl)-1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-4-carboxamide; 4-({1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidin-4 yl}carbonyl)morpholine; 1-({1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidin-4-yl}carbonyl)piperazine; {4-[1-(4-methylphenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholin-3-yl}methanol; {4-[1-(4-methyl-phenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholin-2-yl}methanol; [(3R)-4-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholin-3-yl]methanol; methyl 4-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholine-3-carboxylate; N-(2-aminoethyl)-4-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholine-3-carboxamide; 2-{4-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholin-3-yl}ethan-1-ol; methyl 1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-2-carboxylate; N-(2-aminoethyl)-1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-2-carboxamide; 1-({1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidin-2-yl}carbonyl)piperazine; 4-[1-(4-methylphenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]morpholine; 1-(4-chlorophenyl)-3-(piperidin-4-yl)-1H-pyrrolo[2,3-c]pyridin-4-ol; N-butyl-1-(4-chlorophenyl)-N-methyl-1H-pyrazolo[3,4-c]pyridin-3-amine; 1-[4-(fluoromethyl)phenyl]-3-(oxan-4-yl)-1H-pyrazolo[3,4-c]pyridine; and 3-({4-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidin-1-yl}methyl)pyridine are useful for the inhibition of SSAO activity. | 12-04-2014 |
20140357624 | DERIVATIVES OF HETEROARYLSULFONAMIDES, THEIR PREPARATION AND THEIR APPLICATION IN HUMAN THERAPY - The present invention concerns derivatives of heteroarylsulfonamides, notably as blockers of Kv potassium channels, and more particularly of channels Kv1.5, Kv4.3 or Kv11.1, their application in clinical therapy and their preparation methods. These compounds correspond to the following general formula (I): where R1 represents one or more substituents of the phenyl core X such as: hydrogen, halogen, trifluoromethyl, trifluoromethoxy, linear or branched C | 12-04-2014 |
20140364420 | SUBSTITUTED PIPERAZINYL-PYRROLIDINE COMPOUNDS USEFUL AS CHEMOKINE RECEPTOR ANTAGONISTS - The present invention relates to compounds useful as Chemokine Receptor antagonists. Compounds of general formula I are provided: | 12-11-2014 |
20140364421 | BENZOTHIOPHENE COMPOUND - [Problem] A compound which is useful as an IK1 channel activator is provided. | 12-11-2014 |
20140364422 | Aqueous Pharmaceutical Composition With Enhanced Stability - The present invention is an aqueous pharmaceutical composition that includes an ionized therapeutic agent, an ionic component and guar gum. The guar gum is present in the composition a concentration sufficient to limit interactions between the ionized therapeutic agent and the ionic component thereby imparting stability to the composition. The composition is preferably at or near physiologic pH. The aqueous pharmaceutical composition has been found particularly useful as an aqueous ophthalmic, otic or nasal composition. The pharmaceutical composition, due to its characteristics, is particularly suitable as an ophthalmic composition. | 12-11-2014 |
20140378441 | THERAPEUTIC AGENT FOR OCULAR FUNDUS DISEASE - Disclosed herein is a prophylactic or therapeutic agent for ocular fundus disease, especially diabetic retinopathy or age-related macular degeneration. The prophylactic or therapeutic agent for ocular fundus disease comprising: (S)-(−)-1-(4-fluoro-5-isoquinolinesulfonyl)-2-methyl-1,4-homopiperazine, a salt thereof, or a solvate thereof, as an active ingredient. | 12-25-2014 |
20140378442 | PHTHALAZINONE DERIVATIVES - Compounds of the formula (I): | 12-25-2014 |
20150011535 | HETEROCYCLIC COMPOUNDS, MEDICAMENTS CONTAINING THEM, USE AND PROCESSES FOR THE PREPARATION THEREOF - The present invention relates to compounds of general formula (I) | 01-08-2015 |
20150018343 | Tetraaza-cyclopenta[a]indenyl and their use as Positive Allosteric Modulators - The present invention provides compounds of Formula (I) as M1 receptor positive allosteric modulators for the treatment of diseases mediated by the muscarinic M1 mediator. | 01-15-2015 |
20150018344 | THIAZOLYL- OR THIADIAZOLYL-SUBSTITUTED PYRIDYL COMPOUNDS USEFUL AS KINASE INHIBITORS - Compounds having the following formula (I) or an enantiomer, diastereomer or a pharmaceutically-acceptable salt thereof, wherein X is N or C—R | 01-15-2015 |
20150031682 | ANTI-MALARIAL AGENTS - The present invention is related to a use of aminopyrazine derivatives in the manufacture of a medicament for preventing or treating malaria. Specifically, the present invention is related to aminopyrazine derivatives useful for the preparation of a pharmaceutical formulation for the inhibition of malaria parasite proliferation. | 01-29-2015 |
20150031683 | RHO KINASE INHIBITORS FOR USE IN TREATING AMYOTROPHIC LATERAL SCLEROSIS - The invention relates to a new use of a known Rho kinase inhibitor, fasudil or a fasudil derivative selected from hydroy-fasudil or dimethylfasudil, in the treatment of amyotrophic lateral sclerosis (ALS). | 01-29-2015 |
20150038494 | Thiazolopyrimidine Modulators as Immunosuppressive Agents - The present invention relates to compound of formula I, II, III, or IV, and/or a pharmaceutical acceptable addition salt thereof and/or a stereoisomer thereof and/or a solvate thereof, wherein R | 02-05-2015 |
20150080382 | DIAMINE DERIVATIVES AS INHIBITORS OF LEUKOTRIENE A4 HYDROLASE - This invention is directed to compounds of formula (I): | 03-19-2015 |
20150080383 | COMPOUNDS FOR TREATING SPINAL MUSCULAR ATROPHY - Provided herein are compounds, compositions thereof and uses therewith for treating spinal muscular atrophy. | 03-19-2015 |
20150087635 | SUBSTITUTED PYRIDYL AMIDE COMPOUNDS AS MODULATORS OF THE HISTAMINE H3 RECEPTOR - Certain substituted pyridyl amide compounds are histamine H | 03-26-2015 |
20150105377 | Methods and Compositions for RAF Kinase Mediated Diseases - The invention discloses methods and compositions for treating or preventing RAF kinase mediated diseases or conditions by administering a compound of Formula 1: or a pharmaceutically acceptable salt, solvate or hydrate thereof, wherein the variables are defined as herein. | 04-16-2015 |
20150111879 | PYRIDYL INHIBITORS OF HEDGEHOG SIGNALLING - The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: | 04-23-2015 |
20150126494 | NON-RETINOID ANTAGONISTS FOR TREATMENT OF AGE-RELATED MACULAR DEGENERATION AND STARGARDT DISEASE - A method for treating a disease characterized by excessive lipofuscin accumulation in the retina in mammals afflicted therewith, comprising administering to the mammal an effective amount of a non-retinoid antagonist compound or a pharmaceutically acceptable salt thereof. | 05-07-2015 |
20150133432 | SUBSTITUTED 6-(4-HYDROXY-PHENYL)-1H-PYRAZOLO[3,4-B]PYRIDINE DERIVATIVES AS KINASE INHIBITORS - The present invention relates to pyrazolo[3,4-b]pyridine compounds of the formula I, | 05-14-2015 |
20150133433 | BENZOTHIOPHENE COMPOUND - A method for preventing or treating a disease selected from the group consisting of visceral pain, inflammatory pain, osteoarthritis pain, neuropathic pain, and fibromyalgia in a subject in need thereof, comprising administering to said subject an effective amount of the compound of the following formula (I) or a salt thereof: | 05-14-2015 |
20150291605 | MERTK-SPECIFIC PYRAZOLOPYRIMIDINE COMPOUNDS - The present invention includes pyrazolopyrimidine compounds of Formula I that selectively inhibit Mer tyrosine kinase (MerTK) activity and/or Tyro3 tyrosine kinase activity, and use of these pyrazolopyrimidine compounds as anti-cancer agents, immunostimulatory and immunomodulatory agents, anti-platelet agents, anti-infective agents, and as adjunctive agents in combination with chemotherapeutic, radiation or other standard of care for neoplasms. | 10-15-2015 |
20150291609 | MERTK-SPECIFIC PYRIMIDINE COMPOUNDS - The present invention includes pyrimidine compounds that selectively inhibit Mer tyrosine kinase (MerTK) activity and/or Tyro3 tyrosine kinase activity, and use of these pyrimidine compounds as anti-cancer agents, immunostimulatory and immunomodulatory agents, anti-platelet agents, anti-infective agents, and as adjunctive agents in combination with chemotherapeutic, radiation or other standard of care for neoplasms. | 10-15-2015 |
20150297611 | Inhibition of Histone Methyltransferase for Cardiac Reprogramming - A method for promoting the reprogramming of a non-cardiomyocytic cell or tissue into cardiomyocytic cell or tissue comprising is carried out by contacting a non-cardiomyocytic cell or tissue with a modulator of histone methyltransferase activity or expression. | 10-22-2015 |
20150299134 | NOVEL COMPOUNDS - There is provided a compound of formula (I): | 10-22-2015 |
20150299246 | N-SUBSTITUTED INDENOISOQUINOLINES AND SYNTHESES THEREOF - N-Substituted indenoisoquinoline compounds, and pharmaceutical formulations of N-substituted indenoisoquinoline compounds are described. Also described are processes for preparing N-substituted indenoisoquinoline compounds. Also described are methods for treating cancer in mammals using the described N-substituted indenoisoquinoline compounds or pharmaceutical formulations thereof. | 10-22-2015 |
20150313887 | INDOLES - Herein are disclosed indoles of formula (I) | 11-05-2015 |
20150336949 | 3-(Pyrazolyl)-1H-Pyrrolo[2,3-b]Pyridine Derivatives as Kinase Inhibitors - The present application relates to novel 3-(pyrazolyl)-1H-pyrrolo[2,3-b]pyridine derivatives of formula (I), as protein kinase inhibitors. | 11-26-2015 |
20150336976 | DIPICOLYLAMINE DERIVATIVES AND THEIR PHARMACEUTICAL USES - Dipicolylamine compounds of Formula (I) set forth herein. Also disclosed are pharmaceutical compositions containing metal ions and these compounds. Further disclosed is a method for treating a condition associated with cells containing inside-out phosphatidylserine, with these compounds. | 11-26-2015 |
20160000781 | PHTHALAZINONE DERIVATIVES - Compounds of the formula (I): | 01-07-2016 |
20160015715 | USE OF PDE7 INHIBITORS FOR THE TREATMENT OF MOVEMENT DISORDERS - A method of treating a movement abnormality associated with the pathology of a neurological movement disorder, such as Parkinson's disease or Restless Leg(s) Syndrome by administering a therapeutically effective amount of a PDE7 inhibitory agent. An aspect of the invention provides for the administration of a PDE& inhibitory agent in conjunction with a dopamine agonist or precursor, such as levodopa. In another aspect of the invention, the PDE7 inhibitory agent may be selective for PDE7 relative to other molecular targets (i) known to be involved with the pathology of Parkinson's disease or (ii) at which other drug(s) that are therapeutically effective to treat Parkinson's disease act. | 01-21-2016 |
20160024066 | Small Molecule Inhibitors of Ebola and Lassa Fever Viruses and Methods of Use - The present invention relates to compositions and methods for the treatment of infection by enveloped viruses, such as Ebola and Lassa fever viruses. | 01-28-2016 |
20160024093 | IMIDAZO[1,2-b]PYRIDAZINE-BASED COMPOUNDS, COMPOSITIONS COMPRISING THEM, AND METHODS OF THEIR USE - Imidazo[1,2-b]pyridazine-based compounds of the formula: | 01-28-2016 |
20160030447 | Antiviral Activity of Novel Bicyclic Heterocycles - The present invention relates to compound of Formula I, II, III, or IV, and/or a pharmaceutical acceptable addition salt thereof and/or a stereoisomer thereof and/or a solvate thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R11, and R12 are as defined in the claim | 02-04-2016 |
20160052923 | PIPERAZINE AND HOMOPIPERAZINE DERIVATIVES AS HIV ATTACHMENT INHIBITORS - Compounds of Formula I, including pharmaceutically acceptable salts thereof, are useful as HIV attachment inhibitors. | 02-25-2016 |
20160060265 | PYRAZOLONAPHTHYRIDINONE DERIVATIVES AS METAP2 INHIBITORS (METHIONINE AMINOPEPTIDASE TYPE-2) - The invention related to pyrazolonaphthyridinone derivatives of formula (I) to their preparation and to their therapeutic use as selective inhibitors of type 2 methionine aminopeptidase (hMETAP2). | 03-03-2016 |
20160068493 | SUBSTITUTED PYRIDAZINE CARBOXIMIDE COMPOUNDS - The new pyridazine derivatives have unexpected drug properties as inhibitors of protein kinases especially against ALK and are useful in treating disorders related to abnormal protein kinase activities such as cancer, neurological and psychiatric diseases. | 03-10-2016 |
20160083379 | HISTONE DEMETHYLASE INHIBITORS - The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted pyrido[3,4-d]pyrimidin-4-one derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like. | 03-24-2016 |
20160090369 | RADIOMITIGATING PHARMACEUTICAL FORMULATIONS - The present disclosure relates to compounds of Formula (I) and (II), compositions containing the compounds (alone or in combination with other agents), and their use to prevent, mitigate or treat a) damage induced by ionizing radiation, b) inflammation or c) cancer. | 03-31-2016 |
20160095864 | COMPOSITION FOR REDUCING CELL SENESCENCE COMPRISING RHO-KINASE INHIBITOR AND USE THEREOF - A composition for reducing cell senescence including a Rho-kinase inhibitor and method of treating a cell senescence-related symptom in mammals. | 04-07-2016 |
20160101113 | AGENT FOR PROMOTING CORNEAL ENDOTHELIAL CELL ADHESION - The invention provides an agent for promoting adhesion of a corneal endothelial cell, containing a Rho kinase inhibitor, as well as a culture medium for a corneal endothelial cell, a solution for preservation of cornea, and a method of producing a corneal endothelial preparation, which includes culturing the corneal endothelial cell using the aforementioned culture medium. | 04-14-2016 |
20160108048 | IMIDAZOLE DERIVATIVES AND METHODS OF USE THEREOF FOR IMPROVING THE PHARMACOKINETICS OF A DRUG - The present invention relates to Imidazole Derivatives of Formula (I), and pharmaceutically acceptable salts thereof, wherein A, B, Y, R | 04-21-2016 |
20160136133 | MEDICAMENTS FOR THE TREATMENT OR PREVENTION OF FIBROTIC DISEASES - The present invention relates to the use of indolinones of general formula | 05-19-2016 |
20160152569 | PYRIDYL INHIBITORS OF HEDGEHOG SIGNALLING | 06-02-2016 |
20160152632 | PHARMACEUTICAL COMPOUNDS | 06-02-2016 |
20160159752 | PIPERAZINE DERIVATIVES AS HIV PROTEASE INHIBITORS - The present invention is directed to piperazine derivatives, pharmaceutical compositions comprising the same, and their use in the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS. | 06-09-2016 |
20160194299 | COMPOUNDS FOR TREATMENT OF DRUG RESISTANT AND PERSISTENT TUBERCULOSIS | 07-07-2016 |
20160194323 | HISTONE DEMETHYLASE INHIBITORS | 07-07-2016 |
20160250224 | OREXIN-CONTROL OF BONE FORMATION AND LOSS | 09-01-2016 |
20170233381 | DUAL MECHANISM INHIBITORS FOR THE TREATMENT OF DISEASE | 08-17-2017 |
20190144455 | TETRAHYDROPYRIMIDODIAZEPINE AND DIHYDROPYRIDODIAZEPINE COMPOUNDS FOR TREATING PAIN AND PAIN RELATED CONDITIONS | 05-16-2019 |
20220135583 | BICYCLIC PYRIDINE COMPOSITIONS AND METHODS OF USING THE SAME FOR CANCER THERAPY - Disclosed herein are bicyclic pyridines, such as thienopyridine, pyrrolopyridine, furopyridine compounds, and methods for treating cancers. | 05-05-2022 |