Benzene Ring Bonded Directly To The Triazole Ring Patents (Class 548/269.4)
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Publication number: 20120202834Abstract: The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, A1, A2, A3, A4, L, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.Type: ApplicationFiled: February 7, 2012Publication date: August 9, 2012Applicant: PFIZER INC.Inventors: Gary Erik Aspnes, Mary Theresa Didiuk, Kevin James Filipski, Angel Guzman-Perez, Esther Cheng Yin Lee, Jeffrey Allen Pfefferkorn, Benjamin Dawson Stevens, Meihua Mike Tu
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Publication number: 20120202688Abstract: This document discloses pesticidal compostions comprising molecules having the following formulas: and processes related thereto.Type: ApplicationFiled: February 8, 2012Publication date: August 9, 2012Applicant: DOW AGROSCIENCES LLCInventors: Gary D. Crouse, William T. Lambert, Thomas C. Sparks, Vidyadhar B. Hegde
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Publication number: 20120190543Abstract: The present invention concerns novel heteroaryl-N-aryl carbamates and their use in pest control, as insecticides and acaricides This invention also includes preparation of the pesticide compositions containing the compounds, and methods of controlling insects using the compounds.Type: ApplicationFiled: August 5, 2010Publication date: July 26, 2012Applicant: DOW AGROSCIENCES LLCInventors: William T. Lambert, Gary D. Crouse, Thomas C. Sparks, Denise P. Cudworth
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Publication number: 20120165303Abstract: Compounds are provided that act as potent antagonists of the CCR2 or CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2 and CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, CCR9-mediated diseases, as controls in assays for the identification of CCR2 antagonists and as controls in assays for the identification of CCR9 antagonists.Type: ApplicationFiled: March 2, 2012Publication date: June 28, 2012Applicant: ChemoCentryx, Inc.Inventors: Trevor T. Charvat, Cheng Hu, Anita Melikian, Aaron Novack, Andrew M.K. Pennell, Sreenivas Punna, Edward J. Sullivan, Xuefei Tan, William D. Thomas, Solomon Ungashe, Yibin Zeng
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Patent number: 8188128Abstract: Opioid receptor compounds and pharmaceutical compositions thereof are presented. Also presented are methods for treating a condition mediated by an opioid receptor by administering an effective amount of the opioid receptor compound to a patient in need thereof.Type: GrantFiled: May 12, 2006Date of Patent: May 29, 2012Assignee: The University of Medicine and Dentistry of New JerseyInventors: William J. Welsh, Youyi Peng, Qiang Zhang, Susan M. Keenan, Sonia Arora
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Patent number: 8153672Abstract: The invention relates to crystalline forms of 4-[3,5-bis(2-hydroxyphenyl)-[1,2,4]triazol-1-yl]benzoic acid and to its amorphous form, to processes for the preparation thereof, to compositions containing the same and their uses for the manufacture of a medicament for the treatment of the human body.Type: GrantFiled: November 27, 2007Date of Patent: April 10, 2012Assignee: Novartis AGInventor: Michael Mutz
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Patent number: 8129372Abstract: This invention provides a compound of the formula (I): a pharmaceutically acceptable salt or solvate thereof, wherein R1 is substituted or unsubstituted alkyl or the like, R2 is hydrogen or substituted or unsubstituted alkyl, Ring A is monocyclic or bicyclic aromatic heterocycle, R3 is substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl or substituted or unsubstituted heterocycle, R4 is halogen, cyano, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl or the like, m is an integer between 0 and 2, n is an integer between 0 and 5, R is halogen, oxo, cyano, nitro, substituted or unsubstituted alkyl or the like, and p is an integer between 0 and 2 as novel compounds having NPY Y5 antagonistic activity.Type: GrantFiled: April 20, 2009Date of Patent: March 6, 2012Assignee: Shionogi & Co., Ltd.Inventor: Masahiro Sakagami
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Publication number: 20120053165Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.Type: ApplicationFiled: March 2, 2010Publication date: March 1, 2012Applicant: Pfizer Inc.Inventors: Martin Patrick Allen, Christopher William Am Ende, Michael Aaron Brodney, Amy Beth Dounay, Douglas Scott Johnson, Martin Youngjin Pettersson, Jacob Bradley Schwartz, Tuan Phong Tran
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Publication number: 20120022083Abstract: Compounds, particularly compounds having activity as modulators of cadherin-mediated cell adhesion having the following structure: or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein R1, R2, R3, R4, R5, R6, A, X, Y, Z, m and n are as defined herein. Methods associated with preparation and use of the same, as well as pharmaceutical compositions containing the same, are also disclosed.Type: ApplicationFiled: February 9, 2011Publication date: January 26, 2012Applicant: ADHEREX TECHNOLOGIES, INC.Inventors: Mukur Gupta, Brian Huber, Orest W. Blaschuk
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Publication number: 20110313171Abstract: The present invention relates to the preparation of aryl hydrazines and their salts by treating aryl diazonium salts with triphenyl phosphine followed by hydrolysis of the resulting triphenyl-aryl hydrazyl phosphonium salt to get aryl hydrazine or its salt.Type: ApplicationFiled: January 12, 2007Publication date: December 22, 2011Inventors: Chandra Purna Ray, Sreekanth Medikonduri, Gorantla Seeta Ramanjaneyulu
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Patent number: 8076324Abstract: The present invention relates to di(hetero)arylcyclohexane derivatives of the formula I, in which Ar1, Ar2, R1 and R2 have the meanings indicated in the claims. The compounds of the formula I are valuable pharmaceutical active compounds which inhibit ATP-sensitive potassium channels in the heart muscle and are suitable, for example, for the treatment of disorders of the cardiovascular system such as arrhythmias or a decreased contractility of the heart, such as can occur, for example, in coronary heart disease, cardiac insufficiency or cardiomyopathies. In particular, they are suitable for the prevention of sudden cardiac death. The invention furthermore relates to processes and intermediates for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.Type: GrantFiled: December 3, 2009Date of Patent: December 13, 2011Assignee: Sanofi-AventisInventors: Thomas Bohme, Uwe Gerlach, Dirk Gretzke, Heinz-Werner Kleemann, Stefania Pfeiffer-Marek, Henning Vollert, Jean-Michel Altenburger, Sergio Mallart
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Publication number: 20110190330Abstract: The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula IA, IB, I?A or I?B: where the definitions of the variables are provided herein. The present invention also provides compositions that include, and methods for using, the compounds in preparing medicaments and for treating metabolic disorders such as, for example, type II diabetes.Type: ApplicationFiled: October 13, 2009Publication date: August 4, 2011Applicant: AMGEN INC.Inventors: Sean P. Brown, Paul Dransfield, Xiaohui Du, Zice Fu, Jonathan Houze, XianYun Jiao, Sujen Lai, An-Rong Li, Jiwen Liu, Zhihua Ma, Julio C. Medina, Vatee Pattaropong, Wang Shen, Marc Vimolratana, Yingcai Wang, Zhongyu Wang, Ming Yu, Liusheng Zhu
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Publication number: 20110171138Abstract: Provided herein is a highly pure deferasirox or a pharmaceutically acceptable salt thereof substantially free of hydrazine impurity, 4-hydrazinobenzoic acid, processes for the preparation thereof, and pharmaceutical compositions comprising highly pure deferasirox or a pharmaceutically acceptable salt thereof substantially free of hydrazine impurity.Type: ApplicationFiled: June 2, 2009Publication date: July 14, 2011Applicant: ACTAVIS GROUP PTC EHFInventors: Rajendra Suryabhan Patil, Kishore Charugundla, Praveen Kumar Neela, Nitin Sharadchandra Pradhan, Jon Valgeirsson
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Publication number: 20110124559Abstract: Novel compounds which are antagonists or inverse agonists at one or more of the opioid receptors, pharmaceutical compositions containing them, to processes for their preparation.Type: ApplicationFiled: August 8, 2007Publication date: May 26, 2011Applicant: Smithkline Beecham CorporationInventors: David John Cowan, Andrew Lamont Larkin, Cunyu Zhang, David Lee Musso, Gary Martin Green, Rodolfo Cadilla, Paul Kenneth Spearing, Michael Joseph Bishop, Jason Daniel Speake
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Publication number: 20110105532Abstract: The present invention relates to halogen-substituted amide derivatives of the general formula (I) in which R1 to R6, Q1 to Q8, A, V, W, X, Y, n and m are each defined as described in the description—and to a process for preparation thereof and to the use thereof as insecticides and acaricides.Type: ApplicationFiled: October 27, 2010Publication date: May 5, 2011Applicant: Bayer CropScience AGInventors: Markus HEIL, Eike Kevin Heilmann, Alexander Sudau, Tobias Kapferer, Friedrich August Mühlthau, Peter Jeschke, Arnd Voerste, Ulrich Görgens, Klaus Raming, Ulrich Ebbinghaus-Kintscher, Mark Drewes, Martin Adamczewski, Angela Becker
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Patent number: 7906503Abstract: 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, 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, and cirrhosis of the liver.Type: GrantFiled: October 21, 2008Date of Patent: March 15, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Robert K. Baker, Jianming Bao, Shouwu Miao, Kathleen M. Rupprecht
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Publication number: 20110059940Abstract: The disclosure provides compounds of Formula I, including pharmaceutically acceptable salts, their pharmaceutical compositions, and their uses in inhibiting ?-amyloid peptide (?-AP) production.Type: ApplicationFiled: May 7, 2009Publication date: March 10, 2011Inventors: Paul J. Gilligan, Michael G. Yang, Jianliang Shi
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Publication number: 20110046194Abstract: The present invention constitutes new 3-triazolylphenyl-substituted sulphide derivatives of the formula (I) in which A1, A2, B0, B1, B2, B3, X, R1, R2 and n are as defined in the description, to their use as acaricides and insecticides for controlling animal pests, and to processes for preparing them.Type: ApplicationFiled: August 19, 2010Publication date: February 24, 2011Applicant: Bayer CropScience AGInventors: Bernd Alig, Stefan Antons, Reiner Fischer, Norbert Lui, Adeline Köhler, Arnd Voerste, Ulrich Görgens
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Publication number: 20110028468Abstract: This invention provides a compound of the formula (I): a pharmaceutically acceptable salt or solvate thereof, wherein R1 is substituted or unsubstituted alkyl or the like, R2 is hydrogen or substituted or unsubstituted alkyl, Ring A is monocyclic or bicyclic aromatic heterocycle, R3 is substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl or substituted or unsubstituted heterocycle, R4 is halogen, cyano, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl or the like, m is an integer between 0 and 2, n is an integer between 0 and 5, R is halogen, oxo, cyano, nitro, substituted or unsubstituted alkyl or the like, and p is an integer between 0 and 2 as novel compounds having NPY Y5 antagonistic activity.Type: ApplicationFiled: April 20, 2009Publication date: February 3, 2011Applicant: Shinonogi & Co., LtdInventors: Masahiro Sakagami, Hiroshi Hashizume, Satoru Tanaka, Takayuki Okuno, Hiroshi Yari, Keisuke Tonogaki, Naoki Kouyama
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Publication number: 20110015405Abstract: The present invention relates to a catalytic process for preparing 3-triazolyl sulphoxide derivatives in enantiomerically pure or enantiomerically enriched form.Type: ApplicationFiled: July 16, 2010Publication date: January 20, 2011Applicant: Bayer CropScience AGInventors: Stefan Antons, Norbert Lui, Wahed Ahmed Moradi
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Publication number: 20100256387Abstract: 2,5-Diaryl-1,2,4-triazole derivatives of structural formula I are selective inhibitors of the 11?-hydroxysteroid dehydrogenase Type 1 enzyme (11?-HSD-1). The compounds are useful for the treatment of diabetes, hyperglycemia, obesity, insulin resistance, atherosclerosis, dyslipidemia, hyperlipidemia, hypertension, and Metabolic Syndrome. Also disclosed are novel compounds of structural formula II which are inhibitors of 11?-HSD-1.Type: ApplicationFiled: April 14, 2010Publication date: October 7, 2010Applicant: MERCK SHARP & DOHMEInventors: Susan D. Aster, James M. Balkovec, Donald W. Graham, Xin Gu, Nancy J. Kevin, Gool F. Patel, Mitree Ponpipom
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Publication number: 20100249424Abstract: Disclosed is a method for preparing a compound of Formula 1 wherein R1 is CHX2, CX3, CX2CHX2 or CX2CX3; each X is independently Cl or F; Z is optionally substituted phenyl; and Q is phenyl or 1-naphthalenyl, each optionally substituted as defined in the disclosure; comprising contacting a compound of Formula 2 with hydroxylamine in the presence of a base. The present invention also relates to novel compounds of Formula 2, useful as starting materials for the aforedescribed method.Type: ApplicationFiled: August 4, 2008Publication date: September 30, 2010Applicant: E.I.DuPont De Nemours and CompanyInventors: Gary David Annis, Brenton Todd Smith
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Publication number: 20100204206Abstract: Di(hetero)arylcyclohexane derivatives, their preparation, their use and pharmaceutical compositions comprising them The present invention relates to di(hetero)arylcyclohexane derivatives of the formula I, in which Ar1, Ar2, R1 and R2 have the meanings indicated in the claims. The compounds of the formula I are valuable pharmaceutical active compounds which inhibit ATP-sensitive potassium channels in the heart muscle and are suitable, for example, for the treatment of disorders of the cardiovascular system such as arrhythmias or a decreased contractility of the heart, such as can occur, for example, in coronary heart disease, cardiac insufficiency or cardiomyopathies. In particular, they are suitable for the prevention of sudden cardiac death. The invention furthermore relates to processes and intermediates for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.Type: ApplicationFiled: December 3, 2009Publication date: August 12, 2010Applicant: SANOFI-AVENTISInventors: Thomas BOHME, Uwe GERLACH, Dirk GRETZKE, Heinz-Werner KLEEMANN, Stefania PFEIFFER-MAREK, Henning VOLLERT, Jean-Michel ALTENBURGER, Sergio MALLART
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Publication number: 20100190997Abstract: The present invention relates to the process for the preparation of Letrozole free from its regioisomer (7) and other impurities by selective extraction of desired intermediate (3) using suitable solvent and mixture of solvents.Type: ApplicationFiled: September 4, 2006Publication date: July 29, 2010Inventors: Hussain Haider, Kirtipalsinh Saijansinh Solanki, Gautam Pal, Manoj Kumar Singh, Jay Shantilal Kothari, Virendra Kumar Agarwal
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Publication number: 20100190762Abstract: Compounds are provided that act as potent antagonists of the CCR2 or CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2 and CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, CCR9-mediated diseases, as controls in assays for the identification of CCR2 antagonists and as controls in assays for the identification of CCR9 antagonists.Type: ApplicationFiled: April 2, 2010Publication date: July 29, 2010Applicant: CHEMOCENTRYX, INC.Inventors: Trevor T. Charvat, Cheng Hu, Anita Melikian, Aaron Novack, Andrew M.K. Pennell, Sreenivas Punna, Edward J. Sullivan, Xuefei Tan, William D. Thomas, Solomon Ungashe, Yibin Zeng
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Patent number: 7754749Abstract: Compounds of formula (I) wherein X is chloro or bromo; Y is chloro or trifluoromethyl; and A and B are hydrogen or methyl with the proviso that one of A or B must be methyl; or the enantiomers or salts thereof, use of compounds of formula I for combating insects or acarids and for treating, controlling, preventing or protecting animals against infestation or infection by parasites, and compositions comprising compounds of formula I.Type: GrantFiled: May 30, 2006Date of Patent: July 13, 2010Assignee: BASF AktiengesellschaftInventors: Christopher Koradin, Wolfgang Von Deyn, Michael Rack, Thomas Zierke, David G. Kuhn, Deborah L. Culbertson, Douglas D. Anspaugh, Hassan Oloumi-Sadeghi
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Publication number: 20100160327Abstract: The present invention relates to a novel class of modified malonate derivatives. The modified malonate compounds can be used to treat cancer. The modified malonate compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.Type: ApplicationFiled: June 21, 2006Publication date: June 24, 2010Inventors: Jonathan Grimm, Paul Harrington, Richard Heidebrecht, JR., Thomas Miller, Karin Otte, Phieng Siliphaivanh, David Sloman, Matthew Stanton, Kevin Wilson, David Witter, Solomon Kattar, Paul Tempest
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Patent number: 7741347Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of Hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: GrantFiled: May 14, 2008Date of Patent: June 22, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Carol Bachand, Makonen Belema, Daniel H. Deon, Andrew C. Good, Jason Goodrich, Lawrence G. Hamann, Clint A. James, David R. Langley, Rico Lavoie, Omar D. Lopez, Alain Martel, Nicholas A. Meanwell, Van N. Nguyen, Jeffrey Lee Romine, Edward H. Ruediger, Lawrence B. Snyder, Denis R. St. Laurent, Gan Wang, Fukang Yang
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NOVEL ORGANOMETALLIC COMPLEXES WHICH EMIT IN THE RED TO GREEN SPECTRAL REGION AND THEIR USE IN OLEDS
Publication number: 20100127215Abstract: Organometallic complexes which bear at least one ligand which has a unit having a triplet energy of at least 22 000 cm?1, a process for preparing the organometallic complexes, a mixture comprising at least one inventive organometallic complex, the use of the organometallic complexes or of the mixture in organic light-emitting diodes, the organometallic complexes preferably being used as emitter materials, and specific nitrogen- or phosphorus-substituted triphenylene derivatives and a process for their preparation.Type: ApplicationFiled: April 4, 2008Publication date: May 27, 2010Applicant: BASF SEInventors: Herbert Friedrich Boerner, Hans-Peter Loebl, Josef Salbeck, Elena Popova -
Publication number: 20100120714Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein W is O or S; V is a direct bond or NR3; Q is or CR6aR6b, O, NR7, C?N—O—R7 or C(?O); Y is —C(R5)?N—O—(CR8aR8b)p—X—(CR9aR9b)q—SiR10aR10bR10c; or a phenyl ring substituted as defined in the disclosure; or Z; and R1, R2, R3, R4, R5, R6a, R7, R8a, R8b, R9b, R10a, R10b, R10c, Z, p and q are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.Type: ApplicationFiled: April 4, 2008Publication date: May 13, 2010Applicant: E.I. DU PONT DE NEMOURS AND COMPANYInventors: Bruce Lawrence Finkelstein, Andrew Edmund Taggi, Jefrey Keith Long, Paula Louise Sharpe, Chi-ping Tseng, Stephen Frederick Mccann, Amy X. Ding, Steven Lewis Swann, JR.
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Patent number: 7714319Abstract: A thin film transistor comprising at least three terminals consisting of a gate electrode, a source electrode and a drain electrode; an insulating layer and an organic semiconductor layer on a substrate, which controls its electric current flowing between the source and the drain by applying a electric voltage across the gate electrode, wherein the organic semiconductor layer comprises a heterocyclic compound containing a nitrogen atom formed by condensation between five member rings each having a nitrogen atom at their condensation sites or between a five member ring and a six member ring each having a nitrogen atom at their condensation sites. The transistor became to have a fast response speed (driving speed), and further, achieved a large on/off ratio getting an enhanced performance as a transistor.Type: GrantFiled: October 27, 2004Date of Patent: May 11, 2010Assignee: Idemitsu Kosan Co., Ltd.Inventors: Hiroaki Nakamura, Hiroshi Yamamoto
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Publication number: 20100113542Abstract: 5-[4-(2-Methylphenyl)-3-hydroxy-4H-1,2,4-triazol-5-yl]-2,4-dihydroxy-N-methyl-N-butylbenzamide is an HSP90 inhibitor and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.Type: ApplicationFiled: December 11, 2007Publication date: May 6, 2010Applicant: Merck Patent GesellschaftInventors: Hans-Michael Eggenweiler, Michael Wolf, Hans Peter Buchstaller, Christian Sirrenberg
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Publication number: 20100056426Abstract: The present invention relates to a method of treating and/or preventing myocardial infarction comprising administering an iron chelator to a warm-blooded animal. The iron chelator is preferably 4-[3,5-bis(2-hydroxyphenyl)-[1,2,4]triazol-1-yl]benzoic.Type: ApplicationFiled: May 12, 2008Publication date: March 4, 2010Applicant: NOVARTIS AGInventor: John Glasspool
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Publication number: 20100056590Abstract: The invention relates to crystalline forms of -[3,5-bis(2-hydroxyphenyl)-[1,2,4]triazol-1-yl]benzoic acid and to its amorphous form, to processes for the preparation thereof, to compositions containing the same and their uses for the manufacture of a medicament for the treatment of the human body.Type: ApplicationFiled: November 27, 2007Publication date: March 4, 2010Applicant: NOVARTIC AGInventor: Michael Mutz
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Patent number: 7642273Abstract: A class of novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including obesity, diabetes, inflammatory and immune diseases, and have the structure of formula (I) or (II): including a stereoisomer thereof, a tautomer thereof, a prodrug thereof, or a pharmaceutically acceptable salt thereof, where Q is selected from N, O, and S; Y is aryl or heteroaryl; Z is H, C2-6alkyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, halo, or alkoxy; and A, B, R, Ra, Rb, Rc and Rd are defined herein. Also provided are pharmaceutical compositions and methods of treating obesity, diabetes and inflammatory or immune associated diseases comprising said compounds.Type: GrantFiled: January 12, 2006Date of Patent: January 5, 2010Assignee: Bristol-Myers Squibb CompanyInventors: T. G. Murali Dhar, Hai-Yun Xiao, Bingwei Yang
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Publication number: 20090317440Abstract: Substituted triazole compounds and pharmaceutical compositions thereof are presented. Also presented are methods for treating a pathology linked to a hyperproliferative disorder by administering the substituted triazole compounds to a patient in need thereof.Type: ApplicationFiled: October 25, 2005Publication date: December 24, 2009Applicant: UNIVERSITY OF MEDICINE AND DENTISTRY OF NEW JERSEYInventors: William J. Welsh, Youyi Peng, Xin Wang, Susan M. Keenan, Qiang Zhang, Sonia Arora
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Publication number: 20090306112Abstract: The invention is related to compounds of Formula I or a pharmaceutically acceptable salt, solvate, ester, and/or phosphonate thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.Type: ApplicationFiled: July 19, 2007Publication date: December 10, 2009Applicant: Gilead Sciences, Inc.Inventors: Carina E. Cannizzaro, James M. Chen, Manoj C. Desai, Michael L. Mitchell, Sundaramoorthi Swaminathan, Lianhong Xu, Zheng-Yu Yang
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Publication number: 20090286776Abstract: Compounds of the formula (I): in which R, R1, R2 and R3 are as defined in the description, the use thereof for the treatment of dyslipidaemia, atherosclerosis and diabetes, pharmaceutical compositions comprising them, and processes for the preparation of these compounds.Type: ApplicationFiled: July 23, 2009Publication date: November 19, 2009Inventors: Jean Jacques ZEILLER, Hervè Dumas, Valérie Guyard-Dangremont, Isabelle Berard, Francis Contard, Daniel Guerrier, Gérard Ferrand, Yves Bonhomme
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Publication number: 20090181998Abstract: Opioid receptor compounds and pharmaceutical compositions thereof are presented. Also presented are methods for treating a condition mediated by an opioid receptor by administering an effective amount of the opioid receptor compound to a patient in need thereof.Type: ApplicationFiled: May 12, 2006Publication date: July 16, 2009Applicant: UNIVERSITY OF MEDICINE AND DENTISTRY OF NEW JERSEYInventors: William J. Welsh, Youyi Peng, Qiang Zhang, Susan M. Keenan, Sonia Arora
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Publication number: 20090181994Abstract: Triazole derivatives of structural formula I are selective inhibitors of the 11?-hydroxysteroid dehydrogenase-1. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Metabolic Syndrome, and other symptoms associated with NIDDM.Type: ApplicationFiled: February 3, 2009Publication date: July 16, 2009Applicant: Merck & Co., Inc.Inventors: Sherman T. Waddell, Gina M. Santorelli, Milana M. Maletic, Aaron H. Leeman, Xin Gu, Donald W. Graham, James M. Balkovec, Susan D. Aster
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Patent number: 7544738Abstract: The invention provides a method for preparing a 1-benzotriazolylcarbonate ester of a water-soluble and non-peptidic polymer by reacting a terminal hydroxyl group of a water-soluble and non-peptidic polymer with di(1-benzotriazolyl)carbonate in the presence of an amine base and an organic solvent. The polymer backbone can be poly(ethylene glycol). The 1-benzotriazolylcarbonate ester can then be reacted directly with a biologically active agent to form a biologically active polymer conjugate or reacted with an amino acid, such as lysine, to form an amino acid derivative.Type: GrantFiled: April 25, 2008Date of Patent: June 9, 2009Assignee: Nektar Therapeutics AL, CorporationInventor: Antoni Kozlowski
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Compounds, Compositions and Methods for the Treatment of Beta-Amyloid Diseases and Synucleinopathies
Publication number: 20090111863Abstract: Dihydroxyaryl compounds and pharmaceutically acceptable esters, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of ?-amyloid diseases, such as observed in Alzheimer's disease, and synucleinopathies, such as observed in Parkinson's disease, and the manufacture of medicaments for such treatment.Type: ApplicationFiled: October 3, 2008Publication date: April 30, 2009Inventors: Luke A. Esposito, F. Michael Hudson, Thomas Lake, Joel Cummings, Manfred Weigele, Alan Snow, Lesley Larsen -
Publication number: 20090106915Abstract: The present invention concerns coloring keratin fibers, especially human hair, with colored metal complexes.Type: ApplicationFiled: May 3, 2006Publication date: April 30, 2009Inventors: Nicole End, Kai-Uwe Schoning, Beate Frohling
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Publication number: 20090076282Abstract: To provide novel 3-triazolylphenyl sulfide derivatives having excellent soil treatment activity as insecticides, miticides or nematicides for agricultural and horticultural plants. 3-Triazolylphenyl sulfide derivatives represented by the formula [1]: wherein R is a cyclopropylmethyl group or a trifluoroethyl group, B2 is a hydrogen atom, a halogen atom or a methyl group, B4 is a halogen atom, a cyano group, a nitro group or a C1-C6 alkyl group, and each of A1 and A3 is a hydrogen atom, a halogen atom, a C1-C6 alkyl group which may be substituted or an amino group which may be substituted.Type: ApplicationFiled: October 20, 2005Publication date: March 19, 2009Applicants: KUMIAI CHEMICAL INDUSTRY CO., LTD, IHARA CHEMICAL INDUSTRY CO., LTDInventors: Keiji Toriyabe, Mikio Yamaguchi, Yoshihiro Ito, Shiori Kinpara, Hiroyuki Yano, Satoru Takahashi, Norihisa Yonekura, Ryuji Hamaguchi
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Publication number: 20090069284Abstract: 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, 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, and cirrhosis of the liver.Type: ApplicationFiled: October 21, 2008Publication date: March 12, 2009Inventors: Robert K. Baker, Jianming Bao, Shouwu Miao, Kathleen M. Rupprecht
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Publication number: 20080280869Abstract: The present invention relates to methods, compounds, and compositions for treating or preventing diseases associated with nonsense mutations in an mRNA by administering the compounds or compositions of the present invention. More particularly, the present invention relates to methods, compounds, and compositions for suppressing premature translation termination associated with a nonsense mutation in an mRNA.Type: ApplicationFiled: October 13, 2005Publication date: November 13, 2008Inventors: Neil Almstead, Gary M. Karp, Richard Wilde, Ellen Welch, Jeffrey A. Campbell, Hongyu Ren, Guangming Chen
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Patent number: 7442760Abstract: Electroactive polymeric arylenes and intermediates useful for making such polymers are disclosed. The present invention also provides electroactive compositions comprising the electroactive polymeric arylenes, organic electronic devices which comprise these polymers and compositions, and methods of fabricating these devices.Type: GrantFiled: March 17, 2006Date of Patent: October 28, 2008Assignee: 3M Innovative Properties CompanyInventors: Ralph R. Roberts, James G. Bentsen, Yingbo Li
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Publication number: 20080262060Abstract: The present invention provides novel crystalline forms of deferasirox, methods for their production, and methods for conversion of the novel forms to the known crystalline form I.Type: ApplicationFiled: January 29, 2008Publication date: October 23, 2008Inventors: Zoltan G. Toth, Tivadar Tamas, Csilla Nemethne Racz
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Publication number: 20080200528Abstract: Compounds of formula (I) wherein X is chloro or bromo; Y is chloro or trifluoromethyl; and A and B are hydrogen or methyl with the proviso that one of A or B must be methyl; or the enantiomers or sats thereof, use of compounds of formula I for combating insects or acarids and for treating, controlling, preventing or protecting animals against infestation or infection by parasites, and compositions comprising compounds of formula I.Type: ApplicationFiled: May 30, 2006Publication date: August 21, 2008Applicant: BASF AktiengesellschaftInventors: Christopher Koradin, Wolfgang Von Deyn, Michael Rack, Thomas Zierke, David G. Kuhn, Deborah L. Culbertson, Douglas D. Anspaugh, Hassan Oloumi-Sadeghi
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Patent number: 7407974Abstract: The present invention provides compounds of Formula (I): wherein A, B, C, G, and W1 have any of the values defined in the specification, and pharmaceutically acceptable salt thereof, that are useful to treat thrombotic disorders. Also disclosed are pharmaceutical compositions comprising one or more compounds of Formula I, processes for preparing compounds of Formula I, and intermediates useful for preparing compounds of Formula I.Type: GrantFiled: April 18, 2005Date of Patent: August 5, 2008Assignee: Pfizer Inc.Inventors: Christopher Franklin Bigge, Agustin Casimiro-Garcia, Danette Andrea Dudley, Jeremy John Edmunds, Kevin James Filipski, Jeffrey Thomas Kohrt, Chad Alan Van Huis