Benzene Ring Bonded Directly To The Diazole Ring Patents (Class 548/377.1)
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Publication number: 20090270359Abstract: The present invention provides a novel pyrazole derivative and an androgen receptor antagonist containing the derivative. The present invention provides a compound represented by the formula (I?) wherein R1 is a hydrogen atom, a group via a carbon atom, a group via a nitrogen atom, a group via an oxygen atom, or a group via a sulfur atom; R2 is a phenyl group having cyano (the phenyl group may further have substituent(s) other than cyano); R3 is a hydrogen atom, a group via a carbon atom, a group via a nitrogen atom, a group via an oxygen atom, or a group via a sulfur atom; R4 is a cyclic group optionally having substituent(s); and X is methylene optionally having substituent(s), or CO, or a salt thereof.Type: ApplicationFiled: August 27, 2008Publication date: October 29, 2009Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Mitsuhiro ITO, Tomohiko SUZAKI, Satoshi YAMAMOTO
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Patent number: 7608635Abstract: Compounds of formula (I), pharmaceutical compositions comprising compounds of formula (I) and methods of inhibiting Hsp90 in a cell, treating or preventing a proliferation disorder in a mammal and treating cancer in a mammal comprising administering a compound of formula (I) to a patient or a cell. Variable R5 is an optionally substituted heteroaryl; an optionally substituted 6 to 14-membered aryl; a bicyclic 9-member heterocycle optionally substituted at any substitutable nitrogen or carbon atoms; or a substituent R18, defined herein. Ring A is an aryl or a heteroaryl optionally further substituted with one or more substituents in addition to R3. Substituent R3 is defined herein.Type: GrantFiled: August 10, 2006Date of Patent: October 27, 2009Assignee: Synta Pharmaceuticals Corp.Inventors: Weiwen Ying, Shijie Zhang, Zhenjian Du, Kevin Foley
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Publication number: 20090253699Abstract: 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: October 8, 2009Applicant: PCT Therapeutics, Inc.Inventors: Neil G. Almstead, Guangming Chen, Gary M. Karp, Ellen Welch, Richard Wilde, Jeffrey A. Campbell
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Patent number: 7598285Abstract: Pyrazoles having a naphthyl group attached are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.Type: GrantFiled: June 3, 2005Date of Patent: October 6, 2009Assignee: Merck & Co., IncInventors: Emma R. Parmee, Yusheng Xiong, Jian Guo, Rui Liang, Linda Brockunier
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Publication number: 20090240061Abstract: The invention relates to a method for forming a carbon-carbon or carbon-heteroatom bond by reacting an unsaturated compound carrying a leaving group and a nucleophilic compound, in the absence of a ligand. The aim of the invention is especially to form carbon-nitrogen bonds according to a method for the arylation of nitrogenated organic derivatives. According to the inventive method, a carbon-carbon or carbon-heteroatom bond is formed by reacting an unsaturated compound carrying a leaving group with a nucleophilic compound donating a carbon atom or a heteroatom (HE) that can substitute the leaving group, thus forming a C—C or C—HE bond, in the presence of a copper-based catalyst and a base. Said metal is characterised in that the reaction takes place in the absence of a ligand and in a nitrile-type solvent.Type: ApplicationFiled: July 28, 2004Publication date: September 24, 2009Applicant: Shasun Pharma Solutions, Inc.Inventors: Jean-Francis Spindler, Marc Taillefer, Henri-Jean Cristau, Pascal Philippe Cellier, Armelle Ouali
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Publication number: 20090240058Abstract: A compound or its salt having the following formula (II) is used as an activator for PPAR ?: in which each of R11 and R13 is a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, an alkoxy group having 1 to 8 carbon atoms, an alkyl group having 1 to 8 carbon atoms and a halogen atom substituent, etc.; R12 is a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, an alkoxy group having 1 to 8 carbon atoms, an alkyl group having 1 to 8 carbon atoms and a halogen atom substituent, etc.; each of R14 and R15 is a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, or an alkyl group having 1 to 8 carbon atoms and a halogen atom substituent; X1 is CH or N; Z1 is an oxygen atom or a sulfur atom; W1 is an oxygen atom or CH2; and q is an integer of 2 to 4.Type: ApplicationFiled: February 28, 2006Publication date: September 24, 2009Inventors: Shogo Sakuma, Tomio Yamakawa, Nobutaka Mochiduki, Seiichiro Masui, Rie Takahashi, Toshitake Hirai
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Patent number: 7572922Abstract: The present invention relates to substituted pyrazoles, compositions containing such compounds and methods of treatment The compounds are glucagon receptor antagonists and thus are useful for treating, preventing or delaying the onset of type 2 diabetes mellitus.Type: GrantFiled: January 23, 2004Date of Patent: August 11, 2009Assignee: Merck & Co., Inc.Inventors: Emma Parmee, Subharekha Raghavan, Teresa Beeson, Dong-Ming Shen
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Patent number: 7566709Abstract: Compounds of the formula (I) and salts and solvates thereof, in which X, R1, R2, R5 and Q have the meanings indicated in Claim 1, are suitable as ligands of 5 HT receptors; as well as intermediate compounds of the formula (IA).Type: GrantFiled: March 8, 2004Date of Patent: July 28, 2009Assignee: Merck Patent GmbHInventors: Kai Schiemann, Oliver Schadt, Christoph Van Amsterdam, Gerd Bartoszyk, Christoph Seyfried
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Publication number: 20090186895Abstract: The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggreagation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like.Type: ApplicationFiled: May 17, 2007Publication date: July 23, 2009Applicant: ARENA PHARMACEUTICALS, INC.Inventors: Bradley Teegarden, Dennis Chapman, Marc Decaire, Peter I. Dosa, Konrad Feichtinger, Honnappa Jayakumar, Thuy-Anh Tran, Sonja Strah-Pleynet, Jingdong Xu
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Patent number: 7538134Abstract: This invention relates to a range of 1-aryl-4-cyclopropylpyrazoles in which the cyclopropyl ring is substituted at the angular position, and pharmaceutically acceptable salts and solvates thereof, to compositions comprising such compounds, processes to their synthesis and their use as parasiticides.Type: GrantFiled: June 14, 2006Date of Patent: May 26, 2009Assignees: Pfizer Inc., Pfizer Products Inc.Inventors: Denis Billen, Jessica Boyle, Douglas James Critcher, David Morris Gethin, Kim Thomas Hall, Graham Michael Kyne
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Patent number: 7531669Abstract: In accordance with the present invention, there are provided novel compounds that protect neurons and/or promote neuroregeneration and/or promote memory formation. Such compounds are useful for treatment of a variety of neural disorders and conditions. In another aspect of the present invention, there are also provided formulations containing one or more of the above-described compounds, optionally further containing additional neurologically active compound(s) and/or adjuvants to facilitate delivery thereof across the blood/brain barrier. In still another aspect of the present invention, there are further provided methods for treating a wide variety of neurological indications, e.g., acute neural injuries, chronic injuries, promoting memory formation, and the like.Type: GrantFiled: December 30, 2005Date of Patent: May 12, 2009Assignee: The Salk Institute for Biological StudiesInventors: David R. Schubert, Yuanbin Liu, Thomas Baiga
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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: 20090093637Abstract: This invention concerns the synthesis of highly substituted pyrazoles, which are structural components of pharmacological compounds, through reaction of hydrazones with nitroolefins.Type: ApplicationFiled: October 2, 2008Publication date: April 9, 2009Inventors: Xiaohu Deng, Neelakandha S. Mani
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Publication number: 20090093444Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.Type: ApplicationFiled: July 5, 2006Publication date: April 9, 2009Applicant: MERCK FROSST CANADA LTD.Inventors: Cameron Black, Sheldon Crane, Renata Oballa, Joel Robichaud
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Patent number: 7514464Abstract: This invention relates to a combination product comprising a compound of formula I wherein X, R1, R2, R3, R4, R5, R6, R7 and R9 are as described herein, and one or more further biologically active compounds as described herein, particularly anti-parasitic agents.Type: GrantFiled: June 15, 2005Date of Patent: April 7, 2009Assignee: Pfizer LimitedInventors: Denis Billen, Nathan Anthony Logan Chubb, David Morris Gethin, Kim Thomas Hall, Lee Richard Roberts, Nigel Derek Arthur Walshe
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Publication number: 20090062540Abstract: Methods useful for preparing compounds of formula I: and salts thereof are disclosed. Also disclosed are intermediates useful in the preparation of such compounds.Type: ApplicationFiled: August 22, 2008Publication date: March 5, 2009Inventors: Mark S. Bednarz, Hugh Alfred Burgoon, JR., Shinya Iimura, Ramanaiah C. Kanamarlapudi, Qiuling Song, Wenxue Wu, Jie Yan, Haiming Zhang
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Publication number: 20090062364Abstract: The present application describes deuterium-enriched celecoxib, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: August 21, 2008Publication date: March 5, 2009Applicant: PROTIA, LLCInventor: Anthony W. Czarnik
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Publication number: 20090054662Abstract: The present invention relates to substituted pyrazoles, compositions containing such compounds and methods of treatment. The compounds are glucagon receptor antagonists and thus are useful for treating, preventing or delaying the onset of type 2 diabetes mellitus.Type: ApplicationFiled: July 21, 2006Publication date: February 26, 2009Inventors: Lushi Tan, James Christopher McWilliams, Frederick W. Hartner, Naoki Yoshikawa, Wenji Li
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Publication number: 20090043096Abstract: A method of producing an aromatic compound of the following formula (3) comprising reacting a compound of the following formula (1) with an olefin compound of the following formula (2) in the presence of a transition metal complex: (wherein, an Ar1 ring represents an aromatic hydrocarbon ring or aromatic heterocyclic ring, an Ar2 ring represents a heterocyclic ring containing X1 and N*, and the X1 represents a nitrogen atom or carbon atom and the N represents a nitrogen atom connecting via a double bond to either one of two adjacent atoms in the Ar2 ring.) (wherein, R1, R2, R3 and R4 represent each independently a hydrogen atom, an alkyl group having 1 to 10 carbon atoms or an aryl group having 6 to 18 carbon atoms.) (wherein, Ar1, Ar2, X1, N*, R1, R2 and R3 represent the same meanings as described above.).Type: ApplicationFiled: February 2, 2007Publication date: February 12, 2009Applicants: SUMITOMO CHEMICAL COMPANY, LIMITED, OSAKA UNIVERSITYInventors: Fumitoshi Kakiuchi, Yusuke Matsuura, Masato Ueda
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Publication number: 20090005410Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.Type: ApplicationFiled: June 17, 2008Publication date: January 1, 2009Applicant: CHEMOCENTRYX, INC.Inventors: Trevor T. Charvat, Cheng Hu, Anita Melikian, Aaron Novack, Andrew M.K. Pennell, Edward J. Sullivan, William D. Thomas, Solomon Ungashe, Penglie Zhang, Jay Powers, Sreenivas Punna
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Publication number: 20090005350Abstract: The invention describes novel cyclooxygenase 2 (COX-2) selective inhibitors and novel compositions comprising at least one cyclooxygenase 2 (COX-2) selective inhibitor, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one COX-2 selective inhibitor, optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor, and/or, optionally, at least one therapeutic agent. The novel cyclooxygenase 2 selective inhibitors of the invention can be optionally nitrosated and/or nitrosylated.Type: ApplicationFiled: September 15, 2008Publication date: January 1, 2009Applicant: NitroMed, Inc.Inventors: Upul K. Bandarage, Richard A. Earl, Maiko Ezawa, Xinqin Fang, David S. Garvey, Subhash P. Khanapure, Ramani R. Ranatunge, Stewart K. Richardson, Joseph D. Schroeder, Cheri A. Stevenson, Shiow-Jyi Wey
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Publication number: 20080312452Abstract: A metal extractant comprising Formula (1) wherein R5, R6, R7 and R8 each independently are hydrogen, an optionally substituted hydrocarbyl group, an electron withdrawing group, an electron donating group, or one or more of R5 & R6, R6 & R7, R7 & R8 are linked in such way as to form an optionally substituted ring; Y is N or CR9 wherein R9 is hydrogen, an optionally substituted hydrocarbyl, optionally substituted hydrocarbyloxy, optionally substituted hydrocarbyloxycarbonyl, optionally substituted hydrocarbylcarbonyloxy group, optionally substituted optionally substituted mono or dihydrocarbylaminocarbonyl group; Z is N or CR10 wherein R10 is hydrogen, an optionally substituted hydrocarbyl, optionally substituted hydrocarbyloxy, optionally substituted hydrocarbyloxycarbonyl, optionally substituted hydrocarbylcarbonyloxy group, optionally substituted optionally substituted mono or dihydrocarbylaminocarbonyl group; and tautomers or salts thereof, with the proviso that both Y and Z could be N providedType: ApplicationFiled: August 7, 2006Publication date: December 18, 2008Inventors: John Campbell, Ronald Matthys Swart, Lucy Emeleus, Susan Owens
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Patent number: 7465808Abstract: There are provided by the present invention certain pyrazole based CCK-1 receptor modulators.Type: GrantFiled: September 19, 2005Date of Patent: December 16, 2008Assignee: Janssen Pharmaceutica, N.V.Inventors: Terrance D. Barrett, J. Guy Breitenbucher, Laurent Gomez, Michael D. Hack, Liming Huang, Kelly J. McClure, Magda F. Morton, Clark A. Sehon, Nigel P. Shankley
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Publication number: 20080293573Abstract: The present invention relates to novel pyrazolyl-substituted heterocycles of the formula (I) in which X, Y, Z and Het are as defined in the disclosure, to processes for their preparation, and to their use as pesticides, microbicides and herbicides.Type: ApplicationFiled: July 21, 2008Publication date: November 27, 2008Inventors: Reiner Fischer, Astrid Ullmann, Thomas Bretschneider, Axel Trautwein, Ralf Wischnat, Christoph Erdelen, Angelika Lubos-Erdelen, Dieter Feucht, Mark Wilhelm Drewes
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Patent number: 7452899Abstract: Compounds of Formula (I): inhibit the processing of APP by gamma-secretase, and hence are useful for treatment or prevention of Alzheimer's disease.Type: GrantFiled: July 29, 2004Date of Patent: November 18, 2008Assignee: Merck Sharp & Dohme LimitedInventors: Michela Bettati, Amanda Louise Boase, Ian Churcher, Tamara Ladduwahetty, Kevin John Merchant, Abdul Quddus
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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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Publication number: 20080275053Abstract: Compounds of formula (I) or a pharmaceutically acceptable derivative thereof: wherein A, B, D, Z, R1, R2a, R2b, and Rx are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.Type: ApplicationFiled: October 6, 2004Publication date: November 6, 2008Inventors: Gerard Martin Paul Giblin, Adrian Hall, Ian Reginald Kilford, Xiao Qing Lewell, Neil Derek Miller, Alan Naylor
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Publication number: 20080261952Abstract: A method of treating a condition associated with the CB-1 receptor, in particular obesity, by administering an effective amount of an aryl urea CB-1 receptor modulating compound to a subject in need of such treatment.Type: ApplicationFiled: August 16, 2005Publication date: October 23, 2008Inventors: Jason Bloxham, Matthew Colin Thor Fyfe, James Horswill, Revathy Perpetua Jeevaratnam, John Keily, Martin James Procter, Karen Lesley Schofield, Salam Shaaban, Andrew Simon Swain, Phillppe Wong-Kai-In
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Patent number: 7435753Abstract: This invention relates to a range of 1-aryl-4-cyclopropylpyrazoles in which there is at least one fluorine attached to the cyclopropyl ring, to compositions comprising such compounds, processes to their synthesis and their use as parasiticides.Type: GrantFiled: December 15, 2004Date of Patent: October 14, 2008Assignee: Pfizer LimitedInventors: Denis Billen, Nathan Anthony Logan Chubb, David Morris Gethin, Kim Thomas Hall, Lee Richard Roberts, Nigel Derek Arthur Walshe
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Publication number: 20080167360Abstract: The present invention relates to compounds of formula (I) with a variety of therapeutic uses, more particularly the substituted cyclic alkylidene compounds are useful for selective estrogen receptor modulation.Type: ApplicationFiled: May 24, 2006Publication date: July 10, 2008Inventors: Jing Fang, Dennis Heyer, Subba Reddy Katamreddy, Kenneth William Batchelor, Richard Dana Caldwell
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Publication number: 20080161347Abstract: Substituted aryl and heteroaryl derivatives are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.Type: ApplicationFiled: March 17, 2006Publication date: July 3, 2008Applicant: MERCK & CO., INC.Inventors: John E. Stelmach, Keith G. Rosauer, Emma R. Parmee, James R. Tata
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Publication number: 20080152950Abstract: An anthracene derivative and an organic electroluminescent device using the same are provided. More specifically, provided are an anthracene derivative represented by Formula 1: wherein each R1 is aryl; and each R2 is independently C6-C20 aryl or C3-C19 heteroaryl, which are unsubstituted or substituted with one or more substituents selected from the group consisting of C1-C10 alkyl, C1-C10 alkoxy, cyano, C1-C10 alkylamino, C1-C10 alkylsilyl, halogen, C6-C10 aryl, C6-C10 aryloxy, C6-C10 arylamino, C6-C10 arylsilyl, C3-C19 heteroaryl and hydrogen; and an organic electroluminescent device using the same. The present invention can provide an organic electroluminescent device having excellent power and luminance efficiencies in conjunction with a long service life.Type: ApplicationFiled: November 30, 2007Publication date: June 26, 2008Applicant: SFC CO., LTD.Inventors: Jong-Tae JE, Sug-Kwang Hwang, Sung-Hoon Kim, Seung-Hyuck Choi, Seon-Keun Yoo
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Publication number: 20080146614Abstract: The present invention relates to 1,5-diphenylpyrazole compounds of formula I (A chemical formula should be inserted here—please see paper copy enclosed herewith) and processes for preparing such compounds, their use in the treatment of obesity, psychiatric and neurological disorders, to methods for their therapeutic use and to pharmaceutical compositions containing them.Type: ApplicationFiled: December 21, 2005Publication date: June 19, 2008Inventor: Leifeng Cheng
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Patent number: 7361679Abstract: The present invention relates to a 2-phenyl-3-heteroarylpropionic acid derivative or a salt thereof, and also relates to a pharmaceutical agent and a VLA-4 and/or LPAM-1 antagonist each of which contains the same as an active ingredient.Type: GrantFiled: September 3, 2002Date of Patent: April 22, 2008Assignee: Kaken Pharmaceutical Co., Ltd.Inventors: Satoru Ikegami, Yoichiro Hoshina
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Patent number: 7348342Abstract: We describe substituted benzenesulfoximine compounds having anti-inflammatory activity, processes for their preparation, pharmaceutical compositions containing them, and their use in the treatment of inflammatory diseases.Type: GrantFiled: April 1, 2003Date of Patent: March 25, 2008Assignee: Cadila Healthcare LimitedInventors: Braj B. Lohray, Vidya B. Lohray, Mukul R. Jain, Gautam D. Patel, Harikishore Pingali
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Publication number: 20070244177Abstract: There is dislosed herein compounds of formula (I), wherein: R1, R2, R3, R4 and R5 are defined throughout the description and the claims. The compounds of formula (I) are useful for the treatment of neurological diseases and neurodegenerative diseases, e.g. anxiety, depression, Alzheimer's disease etc.Type: ApplicationFiled: April 12, 2007Publication date: October 18, 2007Applicant: PROBIODRUG AGInventors: Michael Thormann, Michael Almstetter, Andreas Treml
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Patent number: 7282516Abstract: The invention relates to 4-cyanopyrazole-3-carboxamide derivatives of formula (I): in which R1, R2, R3, R4, R5, R6, R7, R8 are as described herein. Also disclosed and claimed are the method of preparation and therapeutic application of compound of formula (I).Type: GrantFiled: December 22, 2005Date of Patent: October 16, 2007Assignee: Sanofi-AventisInventors: Francis Barth, Christian Congy, Serge Martinez, Murielle Rinaldi-Carmona
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Publication number: 20070232810Abstract: The application claims a process for the preparation of a RAR modulator according to formula Ia or Ib comprising to sequential Heck couplings steps to elaborated the disubstituted olefin.Type: ApplicationFiled: March 30, 2007Publication date: October 4, 2007Inventor: Michael Martin
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Publication number: 20070185058Abstract: Compounds of formula I wherein R1, R2, R4, R5, A, B, D and n are as defined, and pharmaceutically acceptable salts thereof, processes for their preparation, their use as pharmaceuticals and pharmaceutical compositions comprising them.Type: ApplicationFiled: January 25, 2007Publication date: August 9, 2007Inventors: Aurelia Conte, Holger Kuehne, Thomas Luebbers, Patrizio Mattei, Cyrille Maugeais, Werner Mueller, Philippe Pflieger
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Patent number: 7247734Abstract: The present invention pertains to the use of certain 3,4-diarylpyazoles of formula (I), both in vitro and in vivo, to inhibit heat shock protein 90 (HSP90), and in the treatment of conditions mediated by HSP90, including, for example, cancer; wherein: Ar3 is independently: a C5-20aryl group, and is optionally substituted; Ar4 is independently: a C5-20aryl group, and is optionally substituted; R5 is independently: hydrogen; halo; hydroxyl; ether; formyl; acyl; carboxy; ester; acyloxy; oxycarbonyloxy; amido; acylamido; aminocarbonyloxy; tetrazolyl; amino; nitro; cyano; azido; sulfhydryl; thioether; sulfonamide; C1-7alkyl; C3-20heterocycyl; or C5-20aryl; R<SP>N</SP> is independently: —H; C1-7alkyl; C3-20heterocycyl; or, C5-20aryl; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, and prodrugs thereof.Type: GrantFiled: December 19, 2002Date of Patent: July 24, 2007Assignees: Vernalis (Cambridge) Limited, Cancer Research Technology Ltd., Institute of Cancer Research of Royal Cancer HospitalInventors: Martin James Drysdale, Brian William Dymock, Xavier Barril-Alonso, Paul Workman, Laurence Harris Pearl, Chrisostomos Prodromou, Edward McDonald
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Patent number: 7244753Abstract: The invention describes novel cyclooxygenase 2 (COX-2) selective inhibitors and novel compositions comprising at least one cyclooxygenase 2 (COX-2) selective inhibitor, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one COX-2 selective inhibitor, optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor, and/or, optionally, at least one therapeutic agent. The novel cyclooxygenase 2 selective inhibitors of the invention can be optionally nitrosated and/or nitrosylated.Type: GrantFiled: July 29, 2003Date of Patent: July 17, 2007Assignee: NitroMed, Inc.Inventors: David S. Garvey, Subhash P. Khanapure, Ramani R. Ranatunge, Stewart K. Richardson, Joseph D. Schroeder
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Patent number: 7202232Abstract: What is claimed is a compound represented by the following structural formula: or a pharmaceutically acceptable salt, solvate or clathrate thereof. The variables for Structural Formula (I) are as described herein.Type: GrantFiled: March 24, 2005Date of Patent: April 10, 2007Assignee: Synta Pharmaceuticals Corp.Inventors: Shoujun Chen, Weiwen Ying, Jun Jiang, Mitsunori Ono, Lijun Sun
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Patent number: 7183306Abstract: A compound of the formula (I): wherein R1 is hydrogen or lower alkyl; R2 is lower alkyl, etc.; R3 is lower alkoxy, etc.; R4 is hydroxy, etc.; X is O, S, etc.; Y is CH or N; Z is lower alkylene or lower alkenylene; and m is 0 or 1; or salts thereof, which are useful as a medicament.Type: GrantFiled: November 14, 2003Date of Patent: February 27, 2007Assignee: Astellas Pharma Inc.Inventors: Fumiyuki Shirai, Hidenori Azami, Natsuko Kayakiri, Kazuo Okumura, Katsuya Nakamura
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Patent number: 7144910Abstract: Compounds of formula I: inhibit the processing of APP by gamma-secretase, and hence are useful in treating or preventing Alzheimer's disease.Type: GrantFiled: October 29, 2003Date of Patent: December 5, 2006Assignee: Merck Sharp & Dohme LimitedInventors: Andrew Madin, Mark Peter Ridgill
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Patent number: 7141678Abstract: A process for the qualitative preparation of 3-haloalkyl-1H-pyrazoles suitable for efficient, high payload commercial application.Type: GrantFiled: May 23, 2003Date of Patent: November 28, 2006Assignee: Pharmacia CorporationInventors: Leo J. Letendre, William D. McGhee, Cynthia Snoddy, George Klemm, Henry T. Gaud
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Patent number: 7132544Abstract: The present invention relates to a process for preparing tetrasubstituted imidazole derivatives of the general formula (I) wherein R1, R2, R3 and R4 are as defined in the specification below. The present invention further relates to a process for preparing the compound of formula (II) and novel crystalline structures of the compound of formula (II).Type: GrantFiled: October 4, 2005Date of Patent: November 7, 2006Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Hua Zhong, Silke Dubberke, Stefan Müller, Armin Rossler, Thomas W. Schultz, Daniel J. Korey, Thomas Otten, Donald G. Walker, Ahmed Abdel-Magid
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Patent number: 7112601Abstract: Compounds of Formula I are disclosed which inhibit hepatitis C NS5B RNA-dependent RNA polymerase and are useful for treating hepatitis C.Type: GrantFiled: August 19, 2004Date of Patent: September 26, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Peter W. Glunz, Brent D. Douty, Scott W. Martin, Jeffrey Romine
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Patent number: 7094906Abstract: The present invention relates to processes for the preparation of a compound of the formula wherein W is nitrogen or —CR3; R1 is halogen, haloalkyl, haloalkoxy, R4S(O)n— or —SF5; R2 is hydrogen or halogen; R3 is halogen; R4 is alkyl or haloalkyl; and n is 0, 1 or 2; and processes for using a compound of the formula (I) in the synthesis of compounds of the formulaType: GrantFiled: November 10, 2003Date of Patent: August 22, 2006Assignee: Basf Agro B.V. Arnthem (NL) Wädenswil-BranchInventor: Jean-Erick Ancel
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Patent number: 6960609Abstract: This invention relates to 1-diphenylmethyl-pyrazole derivatives of formula (I): and pharmaceutically acceptable salts thereof; wherein R1, R2, R3, R4 and R5 are defined herein, as ligands for opioid receptors, particularly the delta opioid receptor. The compounds of the invention have a broad range of therapeutic uses in the area of addictions, analgesia, immunotherapy, shock and brain injuries, neurological dysfunction, gastrointestinal dysfunction, among others.Type: GrantFiled: July 23, 2002Date of Patent: November 1, 2005Assignees: Pfizer, Inc., Pfizer Products, Inc.Inventors: Stanton F. McHardy, Michael G. Vetelino
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Patent number: RE39708Abstract: Estrogen receptor-modulating pyrazole compounds are described in addition to methods and compositions for treating or preventing estrogen receptor-mediated disorders. The compounds described have been found to have unexpected and surprising activity in modulating estrogen receptor activity. Thus, the compounds of the present invention have utility in preventing or treating estrogen receptor-mediated disorders such as osteoporosis, breast and endometrial cancers, atherosclerosis, and Alzheimer's disease.Type: GrantFiled: January 13, 2004Date of Patent: June 26, 2007Assignee: Chiron CorporationInventors: Verena D. Huebner, Xiaodong Lin, Ian James, Liya Chen, Manoj C. Desai, Beata Krywult, Rajinder Singh, Liang Wang