Chalcogen Bonded Directly To The Triazole Ring Patents (Class 514/384)
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Publication number: 20130156755Abstract: A pharmaceutical combination comprising a VEGF inhibitor, and an Hsp90 inhibitor according to the following formulae (I) or (Ia) a tautomer, or a pharmaceutically acceptable salt thereof, wherein the variables in the structural formulae are defined herein. Also provided are methods for treating a proliferative disorder in a subject in need thereof, using pharmaceutical combinations described herein.Type: ApplicationFiled: April 19, 2011Publication date: June 20, 2013Applicant: Synta Pharmaceuticals Corp.Inventors: Ronald K. Blackman, Kevin Paul Foley, David Proia
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Patent number: 8455481Abstract: Process for the protection of fish and invertebrates and all their stages of development against or for the treatment of mycoses caused by fungi of the genera Saprolegnia, Aphanomyces, Achlyaflagellata and other species important in aquacultures by use of 2-[[[[1-[3-(1-fluoro-2-phenylethyl)oxy]phenyl]ethylidene]amino]oxy]methyl]alpha-(methoxyimino)-N-methyl-alphaE-benzeneacetamide, amisulbrom, cyazofamid, enestrobin, famoxadone, fenamidone, fluoxastrobin, orysastrobin, picoxystrobin and pyribencarb. This use leads to an inhibition or destruction of pathogenic fungi. The composition, comprising at least one fungicide selected from the abovementioned group for use in fish fanning and keeping is suitable for the prophylaxis and therapy of diseases of fish in aquaculture, in breeding ponds, breeding tanks, aquariums, natural stretches of game fish waters, ponds, and marine fish farms. Addition to the water and feed and direct application are the associated use forms.Type: GrantFiled: September 14, 2012Date of Patent: June 4, 2013Assignee: Bayer CropScience AGInventors: Isolde Häuser-Hahn, Klaus Stenzel, Ulrike Wachendorff-Neumann
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Publication number: 20130137739Abstract: A solid dispersion comprising a poorly soluble pharmaceutical compound, such as 3-methoxy-1,5-bis(4-methoxyphenyl)-1H-1,2,4-triazole, which has excellent ease of handling and stability is provided. The solid dispersion comprises a polymeric carrier (for example, a polymer selected from a group consisting of polyvinylpyrrolidone and copolyvidone) and further comprising hydroxypropyl methylcellulose as desired.Type: ApplicationFiled: May 27, 2011Publication date: May 30, 2013Inventors: Atsushi Sakurai, Kazuhiro Sako, Toshiro Sakai
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Publication number: 20130123263Abstract: Benzopyran and benzoxepin compounds of Formulas I and II, and including stereoisomers, geometric isomers, tautomer solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formulas I and II for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: January 10, 2013Publication date: May 16, 2013Applicants: F. HOFFMANN - LA ROCHE AG, GENENTECH, INC.Inventors: GENENTECH, INC., F. HOFFMANN - LA ROCHE AG
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Publication number: 20130116253Abstract: Disclosed is a triazole derivative(s) represented by the general formula (1) below or a pharmacologically acceptable salt(s) thereof. Also disclosed are a prodrug(s) of such a triazole derivative(s) and an HSP90 inhibitor(s) containing any one of them as an active constituent. (1) (In the formula, X represents a halogen atom, an optionally substituted alkyl group, an optionally substituted alkynyl group or the like; Y represents a mercapto group, a hydroxyl group, an optionally substituted sulfonyl group, an optionally substituted amino group or the like; and R represents an optionally substituted aryl or alkyl group or the like.Type: ApplicationFiled: November 7, 2012Publication date: May 9, 2013Applicant: NIPPON KAYAKU KABUSHIKI KAISHAInventor: Nippon Kayaku Kabushiki Kaisha
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Publication number: 20130116251Abstract: Disclosed is a triazole derivative(s) represented by the general formula (1) below or a pharmacologically acceptable salt(s) thereof. Also disclosed are a prodrug(s) of such a triazole derivative(s) and an HSP90 inhibitor(s) containing any one of them as an active constituent. (1) (In the formula, X represents a halogen atom, an optionally substituted alkyl group, an optionally substituted alkynyl group or the like; Y represents a mercapto group, a hydroxyl group, an optionally substituted sulfonyl group, an optionally substituted amino group or the like; and R represents an optionally substituted aryl or alkyl group or the like.Type: ApplicationFiled: November 5, 2012Publication date: May 9, 2013Applicant: Nippon Kayaku Kabushiki KaishaInventor: Nippon Kayaku Kabushiki Kaisha
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Publication number: 20130116252Abstract: Disclosed is a triazole derivative(s) represented by the general formula (1) below or a pharmacologically acceptable salt(s) thereof. Also disclosed are a prodrug(s) of such a triazole derivative(s) and an HSP90 inhibitor(s) containing any one of them as an active constituent. (1) (In the formula, X represents a halogen atom, an optionally substituted alkyl group, an optionally substituted alkynyl group or the like; Y represents a mercapto group, a hydroxyl group, an optionally substituted sulfonyl group, an optionally substituted amino group or the like; and R represents an optionally substituted aryl or alkyl group or the like.Type: ApplicationFiled: November 7, 2012Publication date: May 9, 2013Applicant: NIPPON KAYAKU KABUSHIKI KAISHAInventor: NIPPON KAYAKU KABUSHIKI KAISHA
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Publication number: 20130116269Abstract: The present invention relates to novel cyclic N,N?-diarylureas and N,N?-diarylthioureas—androgen receptor antagonists, anti-cancer agent, pharmaceutical composition, medicament, and method for treatment of cancerous diseases, among them prostate cancer.Type: ApplicationFiled: July 1, 2011Publication date: May 9, 2013Inventors: Alexandre Vasilievich Ivachtchenko, Oleg Dmitrievich Mitkin
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Publication number: 20130085147Abstract: The present disclosure is generally directed to antiviral compounds, and more specifically directed to compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such compounds, and methods for inhibiting the function of the NS5A protein.Type: ApplicationFiled: November 7, 2012Publication date: April 4, 2013Applicant: Bristol-Myers Squibb CompanyInventor: Bristol-Myers Squibb Company
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Publication number: 20130079378Abstract: An ester compound represented by formula (1): wherein R3 represents hydrogen or methyl, R4 represents hydrogen or C1-C4 alkyl, and R5 represents hydrogen or C1-C4 alkyl; has an excellent pest control effect and is therefore useful as an active ingredient of a pest control agent.Type: ApplicationFiled: March 18, 2011Publication date: March 28, 2013Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventor: Noritada Matsuo
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Publication number: 20130072461Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.Type: ApplicationFiled: November 13, 2012Publication date: March 21, 2013Applicant: SYNTA PHARMACEUTICALS CORP.Inventor: Synta Pharmaceuticals Corp.
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Patent number: 8399464Abstract: Disclosed is a triazole derivative(s) represented by the general formula (1) below or a pharmacologically acceptable salt(s) thereof. Also disclosed are a prodrug(s) of such a triazole derivative(s) and an HSP90 inhibitor(s) containing any one of them as an active constituent. (1) (In the formula, X represents a halogen atom, an optionally substituted alkyl group, an optionally substituted alkynyl group or the like; Y represents a mercapto group, a hydroxyl group, an optionally substituted sulfonyl group, an optionally substituted amino group or the like; and R represents an optionally substituted aryl or alkyl group or the like.Type: GrantFiled: March 8, 2006Date of Patent: March 19, 2013Assignee: Nippon Kayaku Kabushiki KaishaInventors: Hiroshi Kuramochi, Setsuko Niitsuma, Masaharu Nakamura, Yoshitaka Sato, Seiichi Saito, Arihiro Tomura, Yuh-ichiro Ichikawa, Yousuke Kasuga
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Publication number: 20130065850Abstract: Alterations of certain metabolite concentrations and fluxes that occur in response to viral infection are described. Host cell enzymes in the involved metabolic pathways are selected as targets for intervention; i.e., to restore metabolic flux to disadvantage viral replication, or to further derange metabolic flux resulting in “suicide” of viral-infected cells (but not uninfected cells) in order to limit viral propagation. While any of the enzymes in the relevant metabolic pathway can be selected, pivotal enzymes at key control points in these metabolic pathways are preferred as candidate antiviral drug targets. Inhibitors of these enzymes are used to reverse, or redirect, the effects of the viral infection. Drug candidates are tested for antiviral activity using screening assays in vitro and host cells, as well as in animal models. Animal models are then used to test efficacy of candidate compounds in preventing and treating viral infections. The antiviral activity of enzyme inhibitors is demonstrated.Type: ApplicationFiled: April 3, 2012Publication date: March 14, 2013Applicant: THE TRUSTEES OF PRINCETON UNIVERSITYInventors: Josh MUNGER, Bryson BENNETT, Thomas SHENK, Joshua RABINOWITZ
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Publication number: 20130065854Abstract: A composition comprising a carboxamide compound represented by following formula (I), wherein R1 represents a hydrogen atom or a methyl group, and R2 represents a methyl group, a difluoromethyl group or a trifluoromethyl group, and one or more azole compounds selected from group (A) consisting of propiconazole, prothioconazole, triadimenol, prochloraz, penconazole, tebuconazole, flusilazole, diniconazole, bromuconazole, epoxiconazole, difenoconazole, cyproconazole, metconazole, triflumizole, tetraconazole, myclobutanil, fenbuconazole, hexaconazole, fluquinconazole, triticonazole, bitertanol, imazalil, ipconazole, simeconazole, hymexazol, etridiazole and flutriafol.Type: ApplicationFiled: April 25, 2011Publication date: March 14, 2013Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventor: Yuichi Matsuzaki
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Publication number: 20130059868Abstract: Sodium 2-(5-bromo-4-(4-cyclopropyl-naphthalen-1-yl)-4H-1,2,4-triazol-3-ylthio)acetate is described. In addition, pharmaceutical compositions and uses such compositions for the treatment of a variety of diseases and conditions.Type: ApplicationFiled: March 29, 2011Publication date: March 7, 2013Applicant: Ardea Biociences, Inc.Inventors: Jeffrey Miner, Jean-Luc Girardet, Barry D. Quart
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Publication number: 20130059852Abstract: Some embodiments of this invention include methods for treating disease and methods for administering a compound of Formula (I). In some aspects of the invention, diseases can be treated by administration of compositions comprising a compound of Formula (I). Pharmaceutical compositions of some embodiments of the present invention comprise a compound of Formula (I).Type: ApplicationFiled: April 8, 2011Publication date: March 7, 2013Applicant: UNIVERSITY OF LOUISVILLE RESEARCH FOUNDATION, INC.Inventors: John O. Trent, Jason B. Meier, Kelby B. Napier
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Publication number: 20130040907Abstract: Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of making and using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.Type: ApplicationFiled: May 4, 2012Publication date: February 14, 2013Applicant: Ardea Biosciences Inc.Inventors: Esmir GUNIC, Jean-Luc GIRARDET, Jean-Michel VERNIER, Martina E. TEDDER, David A. PAISNER
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Patent number: 8361927Abstract: Combination comprising Prothioconazol and Metominostrobin preferably as a mixture, agrochemical formulation or composition for curatively and/or preventively controlling phytopathogenic fungi and/or microorganisms of plants and crops.Type: GrantFiled: December 21, 2010Date of Patent: January 29, 2013Assignee: Bayer CropScience AGInventors: Ulrike Wachendorff-Neumann, Anton Kraus, Ingo Wetcholowsky, Peter Dahmen, Hiroyuki Hadano
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Patent number: 8357713Abstract: Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.Type: GrantFiled: June 30, 2011Date of Patent: January 22, 2013Assignee: Ardea Biosciences Inc.Inventors: Barry D. Quart, Jean-Luc Girardet, Esmir Gunic, Li-Tain Yeh
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Publication number: 20130011361Abstract: The present invention provides heterocyclic derivatives of formula (I) that modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.Type: ApplicationFiled: October 1, 2010Publication date: January 10, 2013Applicants: XENON PHARMACEUTICALS INC., NOVARTIS AGInventors: Natalie Dales, Jianmin Fu, Qi Jia, Natalia Pokrovskaia, Shaoyi Sun, Zaihui Zhang
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Publication number: 20130012557Abstract: Small molecule choline kinase inhibitors, pharmaceutical compositions thereof, and screening methods for identifying and evaluating choline kinase inhibitors are provided. Safe and effective methods for treating subjects suffering from a disorder or disease characterized by neoplastic cell proliferation employing the choline kinase inhibitors are also provided.Type: ApplicationFiled: May 12, 2012Publication date: January 10, 2013Applicant: UNIVERSITY OF LOUISVILLE RESEARCH FOUNDATION, INC.Inventors: Brian Clem, Sucheta Telang, John Trent, Jason Chesney, Pooran Chand, Gilles Tapolsky
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Publication number: 20130005704Abstract: The present application relates to novel, substituted 4-arylimidazol-2-ones and 5-aryl-1,2,4-triazolones, processes for the production thereof, the use thereof alone or in combinations for the treatment and/or prevention of diseases and the use thereof for the production of medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular diseases.Type: ApplicationFiled: December 26, 2011Publication date: January 3, 2013Applicant: BAYER PHARMA AKTIENGESELLSHAFTInventors: Heinrich Meier, Eckhard Bender, Ulf Brüggemeier, Ingo Flamme, Dagmar Karthaus, Peter Kolkhof, Daniel Meibom, Dirk Schneider, Verena Voehringer, Chantal Fürstner, Jörg Keldenich, Dieter Lang, Elisabeth Pook, Carsten Schmeck
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Publication number: 20120316151Abstract: This invention relates to the use of triazolone derivatives of Formula (I) for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of triazolones in the treatment of cancer.Type: ApplicationFiled: February 22, 2011Publication date: December 13, 2012Inventors: Nicholas D. Adams, Christopher Joseph Aquino, Amita M. Chaudhari, Jonathan M. Ghergurovich, Terence John Kiesow, Cynthia A. Parrish, Alexander Joseph Reif, Kenneth Wiggall
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Publication number: 20120316157Abstract: The present invention provides a composition having an excellent controlling activity on plant disease. The composition comprising the compound represented by the formula (1) and one or more heterocyclic fungicidal compound selected from the group (A) shows an excellent controlling activity on a plant disease.Type: ApplicationFiled: March 2, 2011Publication date: December 13, 2012Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: So Kiguchi, Soichi Tanaka, Mayuko Ozawa, Atsushi Iwata
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Patent number: 8329736Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.Type: GrantFiled: April 20, 2012Date of Patent: December 11, 2012Assignee: Synta Pharmaceuticals, Corp.Inventors: Dinesh U. Chimmanamada, Weiwen Ying, Teresa Kowalczyk Przewloka, Shijie Zhang, Kevin Foley, Zhenjian Du, Dan Zhou, Shuzhen Qin
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Publication number: 20120309802Abstract: An ester compound represented by formula (1): wherein R1 represents C1-C4 alkyl, has an excellent pest control effect and is therefore useful as an active ingredient of a pest control agent.Type: ApplicationFiled: February 18, 2011Publication date: December 6, 2012Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventor: Noritada Matsuo
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Patent number: 8318790Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.Type: GrantFiled: May 25, 2007Date of Patent: November 27, 2012Assignee: Synta Pharmaceuticals Corp.Inventors: Weiwen Ying, David James, Shijie Zhang, Junghyun Chae, Teresa Przewloka, Howard P. Ng, Hao Li, Zachary Demko, Dinesh U. Chimmanamada, Chi-wan Lee, Zhenjian Du, Kevin Foley, Minghu Song, Lijun Sun, Keizo Koya, Dan Zhou, Shuzhen Qin
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Patent number: 8318184Abstract: The present invention provides novel mGlu2 agonists useful in the treatment of bipolar disorder, schizophrenia, depression, and generalized anxiety disorder.Type: GrantFiled: December 15, 2010Date of Patent: November 27, 2012Assignee: Eli Lilly and CompanyInventors: James Allen Monn, Lourdes Prieto, Lorena Taboada Martinez, Carlos Montero Salgado, Bruce William Shaw
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Patent number: 8314133Abstract: The present invention relates to a catalytic process for preparing 3-triazolyl sulphoxide derivatives in enantiomerically pure or enantiomerically enriched form.Type: GrantFiled: July 16, 2010Date of Patent: November 20, 2012Assignee: Bayer Cropscience AGInventors: Stefan Antons, Norbert Lui, Wahed Ahmed Moradi
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Publication number: 20120283301Abstract: A series of S-triazolyl ?-mercaptoacetanilides having general structure (1) are provided, where Q is CO2H, CONR2, SO3H, or SO2NR2. The compounds inhibit several variants of the reverse transcriptase of HIV, and are useful in the treatment of HIV infections.Type: ApplicationFiled: July 18, 2012Publication date: November 8, 2012Applicant: Ardea Biosciences Inc.Inventors: Jean-Luc Girardet, Yung-Hyo Koh, Martha De La Rosa, Esmir Gunic, Zhi Hong, Stanley Lang, Woo-Hong Kim
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Patent number: 8293778Abstract: The present invention relates to a method of treating an HIV-I infection with a compound according to formula I where R1, R2, R3, R4, R5, are as defined herein.Type: GrantFiled: February 20, 2010Date of Patent: October 23, 2012Assignee: Roche Palo Alto LLCInventors: James Patrick Dunn, Todd Richard Elworthy, Dimitrios Stefanidis, Zachary Kevin Sweeney
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Patent number: 8293723Abstract: Inclusion compounds consisting of certain Angiotensin II AT1 receptors antagonist and cyclodextrins are described. These inclusion compounds are useful in the treatment of hypertension.Type: GrantFiled: December 23, 2010Date of Patent: October 23, 2012Assignee: Universidade Federal de Minas GeraisInventors: Ruben Dario Sinisterra Millan, Robson Augusto Souza Dos Santos, Frederic Jean Georges Frezard, Washington Xavier De Paula
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Patent number: 8293776Abstract: The present invention provides compositions and methods for treating inflammatory conditions (e.g., of the bowel). In particular, the present invention provides methods of treating (e.g., therapeutically and/or prophylactically treating) inflammatory conditions (e.g., of the bowel), compositions useful for such methods (e.g., antagonists and/or inhibitors of angiotensin II (AngII) receptor Type 1a (AT1a)), and methods of identifying, characterizing and/or optimizing such compositions. Compositions and methods of the present invention find use in, among other things, clinical (e.g. therapeutic and preventative medicine) and research applications.Type: GrantFiled: August 5, 2009Date of Patent: October 23, 2012Assignee: The Regents of the University of MichiganInventors: Daniel H. Teitelbaum, Hollis Showalter, Scott Larsen, Peter Lucas, Hiroyuki Koga
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Patent number: 8288426Abstract: A composition comprising fenamidone (a) and an insecticide compound (b) in a (a)/(b) weight ratio of from 1/1000 to 1000/1. A composition further comprising an additional fungicidal compound. A method for preventively or curatively combating the pests and diseases of crops by using this composition.Type: GrantFiled: December 21, 2007Date of Patent: October 16, 2012Assignee: Bayer CropScience AGInventors: Heike Hungenberg, Wolfgang Thielert, Koen Van Den Eynde
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Patent number: 8283369Abstract: Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.Type: GrantFiled: June 30, 2011Date of Patent: October 9, 2012Assignee: Ardea Biosciences. Inc.Inventors: Barry D. Quart, Jean-Luc Girardet, Esmir Gunic, Li-Tain Yeh
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Publication number: 20120245186Abstract: Disclosed is a method for treating a subject with cancer, comprising administering to the subject an effective amount of paclitaxel or a paclitaxel analogue and an effective amount of a compound represented by the following structural formula: a tautomer, or a pharmaceutically acceptable salt thereof. The variables depicted in the structural formula are defined herein.Type: ApplicationFiled: October 19, 2010Publication date: September 27, 2012Applicant: SYNTA PHARMACEUTICALS CORP.Inventors: Ronald K. Blackman, Kevin Paul Foley, David Proia
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Publication number: 20120238607Abstract: The present application relates to new, substituted 2-acetamido-5-aryl-1,2,4-triazolones, to processes for preparing them, to their use alone or in combinations for the treatment and/or prevention of diseases and also to their use for the production of medicaments for the treatment and/or prevention of diseases, more particularly for the treatment and/or prevention of cardiovascular disorders.Type: ApplicationFiled: March 21, 2012Publication date: September 20, 2012Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Ulf BRÜGGEMEIER, Chantal FÜRSTNER, Volker GEISS, Joerg KELDENICH, Armin KERN, Martina DELBECK, Peter KOLKHOF, Axel KRETSCHMER, Elisabeth POOK, Carsten SCHMECK, Hubert TRÜBEL
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Patent number: 8263600Abstract: A liquid suspension comprising an antifungally effective amount of the micronized compound represented by the chemical structural formula I: at least one thickening agent, a non-ionic surfactant, and a pharmaceutically acceptable liquid carrier is disclosed.Type: GrantFiled: June 15, 2011Date of Patent: September 11, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Stefan Sharpe, Joel Sequeira, David Harris, Shashank Mahashabde
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Patent number: 8258132Abstract: The present invention is directed to novel pharmaceutical compositions of the compound 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(S)-(4-fluoro)phenyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine. The pharmaceutical compositions of this invention useful in the treatment or prevention of disorders such as psychiatric disorders including depression and anxiety, inflammatory diseases and emesis.Type: GrantFiled: December 9, 2002Date of Patent: September 4, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: H. William Bosch, Elaine Liversidge, Suhas D. Shelukar, Karen C. Thompson
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Publication number: 20120220610Abstract: The present invention relates to a method of reducing the production of glutamate from glutamine by glutaminase C in a cell or tissue. The method involves inhibiting glutaminase C activity in the cell or tissue under conditions effective to reduce production of glutamate from glutamine. Compounds for carrying out this method are also disclosed.Type: ApplicationFiled: March 25, 2010Publication date: August 30, 2012Applicant: CORNELL UNIVERSITYInventors: Richard A. Cerione, Jon W. Erickson, Kristin Wilson Cerione, Jianbin Wang
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Patent number: 8252828Abstract: A series of S-triazolyl ?-mercaptoacetanilides having general structure (1) are provided, where Q is CO2H, CONR2, SO3H, or SO2NR2. The compounds inhibit several variants of the reverse transcriptase of HIV, and are useful in the treatment of HIV infections.Type: GrantFiled: June 30, 2011Date of Patent: August 28, 2012Assignee: Ardea Biosciences, Inc.Inventors: Jean-Luc Girardet, Yung Hyo Koh, Martha De La Rosa, Esmir Gunic, Zhi Hong, Stanley Lang, Hong Woo Kim
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Publication number: 20120213806Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, Z, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.Type: ApplicationFiled: February 16, 2012Publication date: August 23, 2012Applicant: THERAVANCE, INC.Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes
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Publication number: 20120208852Abstract: The present application relates to new, heterocyclyl-substituted 2-acetamido-5-aryl-1,2,4-triazolones, to processes for preparing them, to their use alone or in combinations for the treatment and/or prevention of diseases and also to their use for the production of medicaments for the treatment and/or prevention of diseases, more particularly for the treatment and/or prevention of cardiovascular disorders.Type: ApplicationFiled: August 24, 2010Publication date: August 16, 2012Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Chantal Fürstner, Joerg Keldenich, Armin Kern, Martina Delbeck, Peter Kolkhof, Axel Kretschmer, Elisabeth Pook, Carsten Schmeck, Hubert Trübel
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Patent number: 8242154Abstract: Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of making and using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.Type: GrantFiled: September 4, 2009Date of Patent: August 14, 2012Assignee: Ardea Biosciences, Inc.Inventors: Esmir Gunic, Jean-Luc Girardet, Jean-Michel Vernier, Martina E. Tedder, David A. Paisner
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Publication number: 20120202813Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.Type: ApplicationFiled: April 20, 2012Publication date: August 9, 2012Applicant: Synta Pharmaceuticals Corp.Inventors: Dinesh U. Chimmanamada, Weiwen Ying, Teresa Kowalczyk Przewloka, Shijie Zhang, Kevin Foley, Zhenjian Du, Dan Zhou, Shuzhen Qin
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Publication number: 20120196910Abstract: The present invention provides a new use of a compound of formula (I) or a pharmaceutically acceptable salt or solvate salt thereof: for the treatment of a somatoform disorder such as body dysmorphic disorder or hyperchondriasis, bulimia nervosa, anorexia nervosa, binge eating, paraphilia and nonparaphilic sexual addictions, Sydeham's chorea, torticollis, autism, a movement disorder including Tourette's syndrome.Type: ApplicationFiled: March 28, 2012Publication date: August 2, 2012Inventors: Dieter HAMPRECHT, Christian Heidbreder, Sergio Melotto, Fabrizio Micheli, Tadataka Yamada
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Publication number: 20120189614Abstract: Organic compounds showing the ability to inhibit viral glycoprotein (GP)-mediated entry of a filovirus into a host cell are disclosed. The disclosed filovirus entry inhibitor compounds are useful for treating, preventing, or reducing the spread of infections by filovirus including the type species Marburg virus (MARV) and Ebola virus (EBOV). Preferred inhibitors of the invention provide therapeutic agents for combating the Ivory Coast, Sudan, Zaire, Bundibugyo, and Reston Ebola virus strains.Type: ApplicationFiled: July 10, 2010Publication date: July 26, 2012Applicant: Crobiotix, Inc.Inventors: Arnab Basu, Debra M. Mills, Norton P. Peet, John D. Williams
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Patent number: 8216971Abstract: The present invention relates to a pesticide composition intended for protecting plants, crops or seeds against phyto-pathogenic fungi or damaging insects, and the corresponding methods of treatment using the said composition. More precisely, the subject of the present invention is a pesticide composition based on propamocarb-HCl, an insecticide active substance and optionally a further fungicide active substance.Type: GrantFiled: December 21, 2007Date of Patent: July 10, 2012Assignee: Bayer Intellectual Property GmbHInventors: Koen van Den Eynde, Wolfgang Thielert, Heike Hungenberg
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Publication number: 20120172405Abstract: Crystalline polymorph forms of 2-(5-bromo-4-(4-cyclopropyl naphthalen-1-yl)-4H-1,2,4-triazol-3-ylthio)acetic acid are described. Pharmaceutical compositions and the uses of such compounds, compound forms, and compositions for the treatment of a variety of diseases and conditions are also presented.Type: ApplicationFiled: December 28, 2011Publication date: July 5, 2012Applicant: Ardea Biosciences Inc.Inventors: Gabriel Galvin, Laszlo R. Treiber, Irina Zamansky, Jean-Luc Girardet
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Publication number: 20120164222Abstract: Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.Type: ApplicationFiled: June 30, 2011Publication date: June 28, 2012Applicant: Ardea Biosciences, Inc.Inventors: Barry D. Quart, Jean-Luc Girardet, Esmir Gunic, Li-Tain Yeh