Nitrogen Attached Directly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 546/289)
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Patent number: 9075014Abstract: This invention relates to compounds having the following structure: wherein Y is O, X is O, bond ? is absent and bond ? is present, or Y is H, X is CH, bond ? is present, and bond ? is absent; atom Z is a carbon and bonds ?, ? and ? are present, or atom Z is a nitrogen and bonds ?, ? and ? are absent, or atom Z is a nitrogen and bonds ? and ? are present and ? is absent. R1, R2, R3, R4, R5, and R6 are various substituents as described in the specification.Type: GrantFiled: January 28, 2011Date of Patent: July 7, 2015Assignee: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORKInventors: Dalibor Sames, David Sulzer, Minhee Lee, Niko Gubernator
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Patent number: 9073873Abstract: Methods of treating or suppressing oxidative stress disorders including mitochondrial diseases, impaired energy processing disorders, neurodegenerative diseases and diseases of aging are disclosed, as well as compounds useful in the methods of the invention, such as 2-heterocyclylaminoalkyl-(p-quinone) derivatives.Type: GrantFiled: March 24, 2014Date of Patent: July 7, 2015Assignee: Edison Pharmaceuticals, Inc.Inventors: Andrew W. Hinman, Orion D. Jankowski, Kieron E. Wesson
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Publication number: 20150057279Abstract: This invention relates to certain heteroaryl compounds which may be used as medicaments, more specifically as medicaments for treating animals. The medicament can be used for the treatment of parasitic infections such as helminth infections and the treatment of parasitosis caused by such infections. This invention also relates to uses of the compounds to make medicaments and treatments comprising the administration of the compounds to animals in need of the treatments. This invention also relates to pharmaceutical compositions and kits comprising the compounds.Type: ApplicationFiled: March 27, 2013Publication date: February 26, 2015Inventors: Michael Berger, Marko Eck, Christopher Kern
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Publication number: 20150005167Abstract: The present invention relates to novel non-steroidal brassinosteroid mimetic derivatives, to processes and intermediates for preparing them, to plant growth regulator compositions comprising them and to methods of using them for controlling the growth of plants and/or promoting the germination of seeds.Type: ApplicationFiled: September 11, 2012Publication date: January 1, 2015Applicants: Syngenta Limited, Syngenta Participations AGInventors: Pierre Joseph Marcel Jung, Joerg Leipner, Mathilde Denise Lachia, Alain De Mesmaeker, Matthew Murdoch Woodhead McLachlan
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Publication number: 20140142317Abstract: 4-Amino-3-chloro-5-fluoro-6-(substituted)picolinates are conveniently prepared from 3,4,5,6-tetrachloropicolinonitrile by a series of steps involving fluorine exchange, amination, halogen exchange and hydrolysis, esterification and transition metal assisted coupling.Type: ApplicationFiled: February 4, 2014Publication date: May 22, 2014Applicant: DOW AGROSCIENCES LLCInventors: James M. Renga, Yuanming Zhu, Gregory T. Whiteker, Christian T. Lowe
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Patent number: 8716486Abstract: Methods of treating or suppressing oxidative stress disorders including mitochondrial diseases, impaired energy processing disorders, neurodegenerative diseases and diseases of aging are disclosed, as well as compounds useful in the methods of the invention, such as 2-heterocyclylaminoalkyl-(p-quinone) derivatives.Type: GrantFiled: June 23, 2009Date of Patent: May 6, 2014Assignee: Edison Pharmaceuticals, Inc.Inventors: Andrew W. Hinman, Orion D. Jankowski, Kieron E. Wesson
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Patent number: 8609853Abstract: 4-Amino-3-chloro-5-fluoro-6-(substituted)picolinates are conveniently prepared from 3,4,5,6-tetrachloropicolinonitrile by a series of steps involving fluorine exchange, amination, reaction with hydrazine, halogenation, hydrolysis and esterification, and transition metal assisted coupling.Type: GrantFiled: January 24, 2012Date of Patent: December 17, 2013Assignee: Dow AgroSciences, LLC.Inventors: Yuanming Zhu, Gregory T. Whiteker, James M. Renga, Robert D. Froese, Cynthia Arndt
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Publication number: 20130172564Abstract: The use of compounds in the treatment of skin disorders is described. In particular, use of a compound of formula (I): or one of its pharmaceutically acceptable salts, solvates or hydrates in the preparation of a medicament to treat skin pathologies is described.Type: ApplicationFiled: December 22, 2010Publication date: July 4, 2013Applicant: GALDERMA RESEARCH & DEVELOPMENTInventors: Cédric Poinsard, Jean-Michel Rethore, Patrice Lucien Maurice Collette, Isabelle Marie Joëlle Collette
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Patent number: 8461343Abstract: A novel synthesis of the anti-androgen, A52, which has been found to be useful in the treatment of prostate cancer, is provided. A52 as well as structurally related analogs may be prepared via the inventive route. This new synthetic scheme may be used to prepare kilogram scale quantities of pure A52.Type: GrantFiled: March 27, 2008Date of Patent: June 11, 2013Assignee: Sloan-Kettering Institute for Cancer ResearchInventors: Ouathek Ouerfelli, Anna Dilhas, Guangbin Yang, Hong Zhao
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Patent number: 8383827Abstract: The present invention provides a compound of formula I; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: GrantFiled: May 14, 2010Date of Patent: February 26, 2013Assignee: Novartis AGInventors: Sylvie Chamoin, Qi-Ying Hu, Julien Papillon
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Publication number: 20120190857Abstract: 4-Amino-3-chloro-5-fluoro-6-(substituted)picolinates are conveniently prepared from 3,4,5,6-tetrachloropicolinonitrile by a series of steps involving fluorine exchange, amination, halogen exchange and hydrolysis, esterification and transition metal assisted coupling.Type: ApplicationFiled: January 24, 2012Publication date: July 26, 2012Applicant: DOW AGROSCIENCES LLCInventors: Kim E. Arndt, James M. Renga, Yuanming Zhu, Gregory T. Whiteker, Christian T. Lowe, Cynthia Arndt
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Publication number: 20120190859Abstract: 4-Amino-5-fluoro-3-halo-6-(substituted)picolinates are conveniently prepared from 4,5,6-trichloropicolinonitrile by a series of steps involving fluorine exchange, amination, halogen exchange, halogenation, nitrile hydrolysis, esterification, and transition metal assisted coupling.Type: ApplicationFiled: January 24, 2012Publication date: July 26, 2012Applicant: Dow AgroSciences LLCInventors: Yuanming Zhu, Gregory T. Whiteker, James M. Renga, Kim E. Arndt, Gary A. Roth, David E. Podhorez, Scott P. West, Cynthia Arndt
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Publication number: 20120190858Abstract: 4-Amino-3-chloro-5-fluoro-6-(substituted)picolinates are conveniently prepared from 3,4,5,6-tetrachloropicolinonitrile by a series of steps involving fluorine exchange, amination, reaction with hydrazine, halogenation, hydrolysis and esterification, and transition metal assisted coupling.Type: ApplicationFiled: January 24, 2012Publication date: July 26, 2012Applicant: DOW AGROSCIENCES LLCInventors: Yuanming Zhu, Gregory T. Whiteker, Kim E. Arndt, Cynthia Arndt, James M. Renga, Robert D. Froese
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Publication number: 20120088800Abstract: The invention provides compounds represented by the formula (I), each of which compounds may have sphingosine-1-phosphate receptor agonist and or antagonist biological activity: wherein: A, m, n, p, a, X, Y and Z are defined in the specification. These compounds are useful for treating a disease or condition selected from the group consisting of glaucoma, dry eye, angiogenesis and pulmonary edema.Type: ApplicationFiled: June 25, 2010Publication date: April 12, 2012Applicant: ALLERGAN, INC.Inventors: Wenkui K. Fang, Ken Chow
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Patent number: 7939548Abstract: Chemical entities that modulate smooth muscle myosin and/or non-muscle myosin, and chemical entities, pharmaceutical compositions and methods of treatment of diseases and conditions associated with smooth muscle myosin and/or non-muscle myosin are described.Type: GrantFiled: July 31, 2007Date of Patent: May 10, 2011Assignee: Cytokinetics, Inc.Inventors: Pu-Ping Lu, Xiangping Qian, Chihyuan (Grace) Chuang, Bradley P. Morgan, David J. Morgans, Jr.
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Patent number: 7935715Abstract: Compound of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: GrantFiled: July 23, 2007Date of Patent: May 3, 2011Assignee: Boehringer Ingelheim International GmbHInventors: Angela Berry, Pier Francesco Cirillo, Eugene Richard Hickey, Doris Riether, David S. Thomson, Monika Ermann, James Edward Jenkins, Innocent Mushi, Malcolm Taylor, Christopher Francis Palmer, Nigel Blumire
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Patent number: 7868026Abstract: The present invention provides compounds of formula (I), or pharmaceutically acceptable salts or solvates thereof, methods for their preparation, methods for their use, and pharmaceutical formulations comprising them.Type: GrantFiled: January 9, 2007Date of Patent: January 11, 2011Assignee: Pfizer Inc.Inventors: Mitchell David Nambu, Leena Bharat Kumar Patel, Brian Douglas Patterson, Sylvie Kim Sakata, John Howard Tatlock
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Publication number: 20100256149Abstract: The invention provides novel arylamino N-heteroaryl MEK inhibitors of Formula (I): Such compounds are MEK inhibitors that are useful in the treatment of hyperproliferative diseases, such as cancer and inflammation. Also disclosed is the treatment of a hyperproliferative disease in mammals, and pharmaceutical compositions containing such compounds.Type: ApplicationFiled: June 14, 2010Publication date: October 7, 2010Applicant: MERCK SERONO S.A.Inventors: Andreas Goutopoulos, Benny C. Askew, JR., Nhut Kiet Diep, Srinivasa Karra, Matthias Schwarz, Henry Yu
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Publication number: 20100204472Abstract: This invention relates to novel indane acetic acid derivatives which are useful in the treatment of diseases such as diabetes, obesity, hyperlipidemia, and atherosclerotic diseases. The invention also relates to intermediates useful in preparation of indane acetic derivatives and to methods of preparation.Type: ApplicationFiled: April 13, 2010Publication date: August 12, 2010Inventors: Louis-David Cantin, Soongyu Choi, Roger B. Clark, Martin F. Hentemann, Xin Ma, Joachim Rudolph, Sidney X. Liang, Christiana Akuche, Rico C. Lavoie, Libing Chen, Dyuti Majumdar, Philip L. Wickens
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Publication number: 20100190991Abstract: A novel synthesis of the anti-androgen, A52, which has been found to be useful in the treatment of prostate cancer, is provided. A52 as well as structurally related analogs may be prepared via the inventive route. This new synthetic scheme may be used to prepare kilogram scale quantities of pure A52.Type: ApplicationFiled: March 27, 2008Publication date: July 29, 2010Inventors: Ouathek Ouerfelli, Anna Dilhas, Guangbin Yang, Hong Zhao
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Patent number: 7700632Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3, R4, m, n, p and s are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases that are associated with the activation of the glycogen synthase enzyme, such as diabetes.Type: GrantFiled: January 8, 2008Date of Patent: April 20, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Chang An Chu, Paul Gillespie, Jefferson Wright Tilley
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Patent number: 7691854Abstract: The invention relates to novel dihydropyridine derivatives, of Formula (I) processes for their preparation, and their use in medicaments, especially for the treatment of chronic obstructive pulmonary diseases, acute coronary syndrome, acute myocardial infarction and heart failure development.Type: GrantFiled: August 18, 2003Date of Patent: April 6, 2010Assignee: Bayer Schering Pharma AktiengesellschaftInventors: Heike Gielen-Haertwig, Volkhart Min-Jian Li, Ulrich Rosentreter, Karl-Heinz Schlemmer, Swen Allerheiligen, Leila Telan, Lars Bärfacker, Jörg Keldenich, Mary F. Fitzgerald, Kevin Nash, Barbara Albrecht, Dirk Meurer
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Publication number: 20090253912Abstract: The invention relates to a method for producing onium salts with tetrafluoroborate anion by reacting an onium halide with an oxonium tetrafluoroborate, sulfonium tetrafluoroborate, or triphenylcarbonium tetrafluoroborate.Type: ApplicationFiled: November 18, 2005Publication date: October 8, 2009Inventors: Nikolai (Mykola) Ignatyev, Urs Welz-Biermann, Andriy Kucheryna, Helge Willner
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Publication number: 20090156646Abstract: The present invention provides a compound which has metastin receptor antagonist activity and is useful for preventing and treating hormone-dependent cancer, benign prostatomegaly, endometriosis, precocious puberty, uterine myoma or the like. More specifically, the present invention provides a compound, represented by the formula: or a salt thereof, a prodrug thereof, and a pharmaceutical agent containing the same; wherein Ring A represents a 5- to 8-membered homocyclic or heterocyclic group optionally having a substituent other than formula —X-R1 wherein X represents a bond or a spacer, and R1 represents optionally substituted amino or an optionally substituted nitrogen-containing heterocyclic group; Ring B represents an optionally substituted benzene ring; R2 represents an optionally substituted homocyclic or heterocyclic group; and R3 and R4 independently represent a hydrogen atom, cyano, acyl or an optionally substituted hydrocarbon group.Type: ApplicationFiled: August 10, 2006Publication date: June 18, 2009Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Satoshi Sasaki, Atsuo Baba
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Publication number: 20090142554Abstract: A process for printing an image on a substrate by means of an ink-jet printer which comprises applying thereto a composition comprising a liquid medium and a mono-azo compound of Formula (1) and salts thereof: wherein: D is an optionally substituted aryl group carrying at least one direct substituent selected from the group consisting of —SO3H, —CO2H, —PO3H2 or an optionally substituted nitrogen heteroaryl group carrying at least one direct substituent selected from the group consisting of —SO3H, —CO2H, —PO3H2; R1 is H: optionally substituted alkyl: amino: —NR4R5; wherein R4 is H, optionally substituted alkyl, optionally substituted alkoxy, optionally substituted acyl, optionally substituted aryl, optionally substituted heterocyclyl; and R5 is optionally substituted alkyl, optionally substituted alkoxy, optionally substituted acyl, optionally substituted aryl, optionally substituted heterocyclyl: —OR6; wherein R6 is H or optionally substituted alkyl: or —SR7; wherein R7 is optionally substituted alkyl; RType: ApplicationFiled: October 13, 2006Publication date: June 4, 2009Inventors: Gavin Wright, Rachel Anne James, Roy Bradbury, Lynn Bradbury
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Publication number: 20090036628Abstract: The present invention relates to oxonium salts having [(Ro)3O]+ cations and sulfonium salts having [(Ro)3S]+ cations, where Ro denotes straight-chain or branched alkyl groups having 1-8 C atoms or phenyl which is unsubstituted or substituted by Ro, ORo, N(Ro)2, CN or halogen, and anions selected from the group of [PFx(CyF2y+1?zHz)6?x]? anions, where 2?x?5, 1?y?8 and 0?z?2y+1, or anions selected from the group of [BFn(CN)4?n]? anions, where n=0, 1 , 2 or 3, or anions selected from the group of [(Rf1SO2)2N]? anions or anions selected from the group of [BFwRf24?w]? anions, to processes for the preparation thereof, and to the use thereof, in particular for the preparation of ionic liquids.Type: ApplicationFiled: January 5, 2007Publication date: February 5, 2009Inventors: Nikolai (Mykola) Ignatyev, German Bissky, Helge Willner
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Patent number: 7446117Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof are potent and selective inhibitors of COX-2 and are of use in the treatment of the pain, fever and inflammation of a variety of conditions and diseases.Type: GrantFiled: September 12, 2003Date of Patent: November 4, 2008Assignee: Glaxo Group LimitedInventors: Paul Beswick, Neil Pegg, Martin Swarbrick, John Skidmore, Sandeep Modi
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Patent number: 7435743Abstract: Pyrimidine compounds of general formula: wherein —R1 represents in which R11 is hydrogen, C1-6 alkyl, halogen, hydroxy, C1-12 alkoxy, nitro, amino, C1-6 alkylsulfonylamino, C1-6 alkoxycarbonyl, C1-6 alkylamino, di (C1-6 alkyl)amino, C1-6 alkanoylamino, phenyl C1-6 alkylamino, phenylsulfonylamino, or —O—(CH2)n—R111; R2 represents hydrogen or halogen; R3 represents hydrogen, —CR31R32R33; R4 is hydrogen, carbamoyl, CN, carboxyl, etc.; R5 is amino, C1-6 alkylamino, di C1-6 alkylamino, etc. or salt thereof. The compound has an excellent anti-inflammatory activity, and other biological activity.Type: GrantFiled: September 30, 2005Date of Patent: October 14, 2008Assignee: Bayer AktiengesellschaftInventors: Toshiki Murata, Masaomi Umeda, Sachiko Sakakibara, Takashi Yoshiro, Hiroki Sato, Tsutomu Masuda, Yuji Koriyama, Mitsuiyuki Shimada, Takuya Shintani, Hiroshi Kadono, Timothy B. Lowinger, Karl B. Ziegelbauer, Kinji Fuchikami, Hiroshi Komura
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Publication number: 20080132545Abstract: Chemical entities that modulate smooth muscle myosin and/or non-muscle myosin, and chemical entities, pharmaceutical compositions and methods of treatment of diseases and conditions associated with smooth muscle myosin and/or non-muscle myosin are described.Type: ApplicationFiled: July 31, 2007Publication date: June 5, 2008Inventors: Pu-Ping Lu, Xiangping Qian, Chihyuan (Grace) Chuang, Bradley P. Morgan, David J. Morgans
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Patent number: 7342115Abstract: 3-substituted-6-aryl pyridines of Formula I are provided: wherein R1, R2, R3, R8, R9, A and Ar are defined herein. Such compounds are ligands of C5a receptor. Preferred compounds of Formula I bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled 3-substituted-6-aryl pyridines, which are useful as probes for the localization of C5a receptors.Type: GrantFiled: November 7, 2003Date of Patent: March 11, 2008Assignee: Neurogen CorporationInventors: Alan J. Hutchison, Jun Yuan, Kyungae Lee, George D. Maynard, Bertrand L. Chenard, Nian Liu, Qin Guo, Zihong Guo, Peter Hrnciar
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Patent number: 7332498Abstract: A method of modulating KSP kinesin activity in vitro comprising contacting KSP kinesin with at least one chemical entity chosen from compounds represented by Formula I: and pharmaceutically acceptable salts thereof, where the variables are as defined further herein.Type: GrantFiled: November 23, 2005Date of Patent: February 19, 2008Assignees: Cytokinetics, Inc., SmithKline Beecham CorporationInventors: Pu-Ping Lu, David J. Morgans, Jr., Bing Yao, Dashyant Dhanak, Steven David Knight
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Patent number: 7320993Abstract: The invention relates to new pyridylalkane, alkene, and alkine acid amides substituted with an aryl and/or heteroaryl residue according to the general formula (I), with a saturated or one or several-fold unsaturated hydrocarbon residue in the carboxylic acid group, methods for the synthesis of these compounds, medicaments containing these and their production as well as their therapeutic use, especially as cytostatic agents and immunosuppressive agents, for example in the treatment or prevention of various types of tumors and control of immune reactions such as autoimmune diseases.Type: GrantFiled: June 16, 2000Date of Patent: January 22, 2008Assignee: Astellas Deutschland GmbHInventors: Elfi Biedermann, Max Hasmann, Roland Löser, Benno Rattel, Friedemann Reiter, Barbara Schein, Klaus Seibel, Klaus Vogt, Katja Wosikowski, Isabel Schemainda
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Patent number: 7262252Abstract: There is provided a fluorine-containing resin composition which is used for nonlinear optical material and comprises (I) a fluorine-containing prepolymer and (II) an organic compound exhibiting a second- or higher-order nonlinear optical effect, in which the fluorine-containing prepolymer (I): (1) is a non-crystalline polymer having a fluorine content of not less than 25% and (2) has a carbon-carbon double bond in a polymer side chain or at an end of a polymer trunk chain and also there is provided a nonlinear optical waveguide device produced from the fluorine-containing resin composition. A suitable nonlinear optical material having a stable structure with a nonlinear substance is produced, and an excellent nonlinear optical waveguide device is produced by relatively simple steps while maintaining transparency in a near infrared region.Type: GrantFiled: November 12, 2003Date of Patent: August 28, 2007Assignee: Daikin Industries, Ltd.Inventors: Takayuki Araki, Yoshito Tanaka, Mihoko Ohashi, Yuzo Komatsu
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Patent number: 7223868Abstract: 2,3-Di-substituted N-heteroaromatic propionamides with said substitution at the 3-position being a substituted phenyl group and at the 2-position being a methyl cycloalkyl ring, said propionamides being glucokinase activators which increase insulin secretion in the treatment of type II diabetes.Type: GrantFiled: April 4, 2005Date of Patent: May 29, 2007Assignee: Hoffmann-La Roche Inc.Inventors: Fred Thomas Bizzarro, Wendy Lea Corbett, Joseph Francis Grippo, Nancy-Ellen Haynes, George William Holland, Robert Francis Kester, Paige Erin Mahaney, Ramakanth Sarabu
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Patent number: 7151182Abstract: N-substituted carbamoyloxyalkyl-azolium derivatives which have antifungal activity and are useful for the treatment of fungal diseases.Type: GrantFiled: September 3, 2004Date of Patent: December 19, 2006Assignee: Basilea Pharmaceutica AGInventors: Hiroshi Fukuda, Tadakatsu Hayase, Eisaku Mizuguchi, Nobuo Shimma, Jun Ohwada, Nobuhiro Oikawa, Masahiro Sakaitani, Masao Tsukazaki, Isao Umeda
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Patent number: 7115637Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.Type: GrantFiled: August 8, 2003Date of Patent: October 3, 2006Assignee: Vertex Pharmaceuticals IncorporatedInventors: Francesco Salituro, Vincent Galullo, Steven Bellon, Guy Bemis, John Cochran
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Preparation and use of 1,5,6,7-tetrahydropyrrolo[3,2-c]pyridine derivatives for treatment of obesity
Patent number: 7071207Abstract: This invention relates to 1,5,6,7-tetrahydropyrrolo[3,2-c]pyridine derivatives which have been found to suppress appetite and induce weight loss. The invention also provides methods for synthesis of the compounds, pharmaceutical compositions comprising the compounds, and methods of using such compositions for inducing weight loss and treating obesity and obesity-related disorders.Type: GrantFiled: September 24, 2002Date of Patent: July 4, 2006Assignee: Bayer Pharmaceuticals CorporationInventors: Roger A. Smith, Stephen J. O'Connor, Wai C. Wong, Soongyu Choi, Harold C. Kluender, Jianmei Fan, Zhonghua Zhang, Rico C. Lavoie, Brent L. Podlogar -
Patent number: 7064124Abstract: A NF-?B inhibitor represented by the following formula (I) is provided: ?Type: GrantFiled: March 27, 2002Date of Patent: June 20, 2006Assignees: Daiichi Suntory Pharma Co., Ltd., Daiichi Suntory Biomedical Research Co., Ltd.Inventors: Kenji Suzuki, Yoichi Nunokawa, Naohisa Ogou
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Patent number: 7056925Abstract: Compounds having the formula are useful for inhibiting protein kinases. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.Type: GrantFiled: August 13, 2003Date of Patent: June 6, 2006Assignee: Abbott LaboratoriesInventors: Gaoquan Li, Qun Li, Tongmei Li, Nan-Horng Lin, Robert A. Mantei, Hing L. Sham, Gary T. Wang
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Patent number: 7015237Abstract: Selective MMP-13 inhibitors are pyridine derivatives of the formula or a pharmaceutically acceptable salt thereof, wherein: R1 and R2 independently are hydrogen, halo, hydroxy, C1–C6 alkyl, C1–C6 alkoxy, C2–C6 alkenyl, C2–C6 alkynyl, NO2, NR4R5, CN, or CF3; E is independently O or S; A and B independently are OR4 or NR4R5; R4 and R5 independently are H, C1–C6 alkyl, C2–C6 alkenyl, C2–C6 alkynyl, (CH2)n aryl, (CH2)n cycloalkyl, (CH2)n heteroaryl, or R4 and R5 when taken together with the nitrogen to which they are attached complete a 3- to 8-membered ring containing carbon atoms and optionally containing a heteroatom selected from O, S, or NH, and optionally substituted or unsubstituted; n is an integer of from 0 to 6.Type: GrantFiled: May 10, 2004Date of Patent: March 21, 2006Assignee: Warner-Lambert CompanyInventors: Nicole Chantel Barvian, David Thomas Connor, Patrick Michael O'Brien, Daniel Fred Ortwine, William Chester Patt, Michael William Wilson
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Patent number: 6984649Abstract: Pyridine compounds of general formula: wherein —R1 represents in which R11 is hydrogen, C1-6 alkyl, halogen, hydroxy, C1-12 alkoxy, nitro, amino, C1-6 alkylsulfonylamino, C1-6 alkoxycarbonyl, C1-6 alkylamino, di (C1-6 alkyl)amino, C1-6 alkanoylamino, phenyl C1-6 alkylamino, phenylsulfonylamino, or —O—(CH2)n—R111; R2 represents hydrogen or halogen; R3 represents 1.2.3.6-tetrahydro-pyridine, or —CR31R32R33 wherein R31 represents H or C1-6 alkyl and R32 and R33 are joined to form a 5-8 membered saturated ring optionally containing up to three heteroatoms; R4 is carbamoyl, CN, carboxyl, etc.; R5 is amino, C1-6 alkylamino, di C1-6 alkylamino, etc. or salt thereof. The compound has an excellent anti-inflammatory activity, and other biological activity.Type: GrantFiled: March 28, 2003Date of Patent: January 10, 2006Assignee: Bayer AktiengesellschaftInventors: Toshiki Murata, Masaomi Umeda, Sachiko Sakakibara, Takashi Yoshino, Hiroki Sato, Tsutomu Masuda, Yuji Koriyama, Mitsuyuki Shimada, Takuya Shintani, Hiroshi Kadono, Timothy B. Lowinger, Karl B. Ziegelbauer, Kinji Fuchikami, Hiroshi Komura
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Patent number: 6881845Abstract: The present invention relates to a process for preparing (±)-trans-4-p-fluorophenyl-3-hyroxymethyl-1-methylpiperdine of formula (I). The present invention also relates to novel intermediates of the formula (IX) and (IX?) methods for preparing said intermediates and the use of said compounds for preparing Paroxetine and Omiloxetine.Type: GrantFiled: January 4, 2001Date of Patent: April 19, 2005Assignee: Ferrer Internacional, S.A.Inventors: Rafael Foguet, Jorge Ramentol, Diego Fernandez-Cano, Miguel P. Armengol, Inés Petschen, Juan Sallares, Francesc X. Camps, Manuel M. Raga, Josep M. Castello
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Patent number: 6809109Abstract: The present invention relates to 2,4-disubstituted pyridine-N-oxide compounds of formula (I): or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, and to pharmaceutical compositions and diagnostic kits comprising the same, and methods of using the same for treating viral infection or as an assay standard or reagent.Type: GrantFiled: June 25, 2003Date of Patent: October 26, 2004Assignee: Bristol-Myers Squibb CompanyInventors: James D. Rodgers, Haisheng Wang
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Patent number: 6794377Abstract: Ortho, ortho-substituted nitrogen-containing bisaryl compounds, processes for their preparation, their use as medicaments, and pharmaceutical preparations including their use as antiarrhythmic active compounds, for example, for the treatment and prophylaxis of atrial arrhythmias, e.g. atrial fibrillation (AF) or atrial flutters.Type: GrantFiled: December 5, 2001Date of Patent: September 21, 2004Assignee: Aventis Pharma Deutschland GmbHInventors: Stefan Peukert, Joachim Brendel, Horst Hemmerle, Heinz-Werner Kleemann
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Publication number: 20040147598Abstract: The present invention provides a compound containing at least one sulfhydryl group and at least one NO donor group, wherein said compound contains one or more protected sulfhydryl groups linked to at least one aromatic ring or a heteroaromatic ring with a nitrogen in the ring structure, which ring is substituted by one or more substituents bearing at least one terminal —ONO2 group. The present invention further provides pharmaceutical compositions comprising one or more of said compounds as an active ingredient.Type: ApplicationFiled: November 3, 2003Publication date: July 29, 2004Inventor: Abdullah Haj-Yehia
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Publication number: 20040142978Abstract: Aminocyanopyridine compounds are described which can inhibit mitogen activated protein kinase-activated protein kinase-2. Pharmaceutical compositions and kits that contain these compounds are also described.Type: ApplicationFiled: December 5, 2003Publication date: July 22, 2004Applicant: Pharmacia CorporationInventors: David R. Anderson, Nathan W. Stehle, Stephen A. Kolodziej, Emily J. Reinhard, Len F. Lee
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Patent number: 6750211Abstract: Compositions, methods of use, isolation and biosynthesis of diimino-piperazine derivatives useful for the modification of sphingolipid metabolism and other biological functions are described. The preferred derivative is 2,6-bis-(&ohgr;-aminobutyl)-3,5-diimino-piperazine. This is a naturally occurring biochemical compound isolated from cells. The diimino-piperazine derivatives are useful as therapeutic agents when administered to patients to treat diseases and disorders involving cell regulation.Type: GrantFiled: February 3, 2003Date of Patent: June 15, 2004Assignee: Emory UniversityInventors: Alfred H. Merrill, Jr., Lisa Warden, Dennis C. Liotta
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Patent number: 6750232Abstract: A class of substituted compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by formula (II), wherein R1 is selected from hydrido, halo, alkoxy, aryl, alkylthio, alkylamino, aralkoxy, azido and alkenyloxy; wherein R2 is selected from hydrido, cyano, hydroxyalkyl, haloalkyl, aminoalkyl, alkylaminoalkyl, alkylcarbonyloxyalkyl, aminocarbonyl and alkylcarbonylaminoalkyl; and wherein R5 and R6 are one more radicals independently selected from halo, alkylsulfonyl, aminosulfonyl, alkoxy and alkylthio; provided one of R5 and R6 is substituted with alkysulfonyl, aminosulfonyl, or haloalkylsulfonyl; or a pharmaceutically-acceptable salt thereof.Type: GrantFiled: January 23, 2003Date of Patent: June 15, 2004Assignee: Eisai Co., Ltd.Inventors: Hitoshi Harada, Osamu Asano, Shuhei Miyazawa, Masato Ueda, Masahiro Yasuda, Nobuyuki Yasuda
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Publication number: 20040002521Abstract: The present invention provides an NF-kappa B activation inhibitor, an inflammatory cytokine production inhibitor, a matrix metalloprotease production inhibitor, an inflammatory cell adhesion factor expression inhibitor, and an anti-inflammatory agent, an antirheumatic agent, an immuno-suppressive agent, an antiallergic agent, an antiviral agent, or a therapeutic agent for arteriosclerosis, which comprise, as the active ingredient, a cyclopropanecarboxylic acid amide compound or a pharmaceutically acceptable salt thereof effective for the treatment of inflammatory diseases.Type: ApplicationFiled: April 30, 2003Publication date: January 1, 2004Applicant: AJINOMOTO CO. INCInventors: Yukio Iino, Takashi Yamamoto, Tsuyoshi Kobayashi
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Publication number: 20030216427Abstract: The present invention is related to substituted amine derivatives notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such amine derivatives of formula (I). Said substituted amine derivatives are efficient modulators, in particular inhibitors, of the Bax function and/or activation. The present invention is furthermore related to novel substituted amine derivatives as well as methods of their preparation.Type: ApplicationFiled: December 26, 2002Publication date: November 20, 2003Inventors: Serge Halazy, Matthias Schwarz, Bruno Antonsson, Agnes Bombrun, Jean-Claude Martinou, Dennis Church