Plural Double Bonds Between Ring Members Of The Oxazole Ring Patents (Class 548/247)
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Patent number: 7030239Abstract: The present invention is directed toward substituted hydroxyethylene compounds of formula (XII) useful in treating Alzheimer's disease and other similar diseases.Type: GrantFiled: May 18, 2004Date of Patent: April 18, 2006Assignee: Elan Pharmaceuticals, Inc.Inventors: Roy Hom, Shumeye S. Mamo, Jay Tung, Andrea Gailunas, Varghese John, Lawrence Y. Fang
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Patent number: 6982336Abstract: A 1,2-dioxetane derivative of the formula (I): wherein R1–R3 and Ar are defined in the claims is provided.Type: GrantFiled: March 7, 2002Date of Patent: January 3, 2006Assignee: Tosoh CorporationInventors: Masakatsu Matsumoto, Nobuko Watanabe, Masashi Yamada
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Patent number: 6972292Abstract: The present invention relates to certain substituted polyketides of formula I, wherein A, B, C, D, E, F and m are as defined herein, pharmaceutical compositions containing said compounds, and the use of said compounds in treating tumors.Type: GrantFiled: August 5, 2002Date of Patent: December 6, 2005Assignee: Novartis AGInventors: Frederick Ray Kinder, Jr., Kenneth W. Bair, Timothy M. Ramsey, Michael L. Sabio
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Patent number: 6930208Abstract: What is described are derivatives of benzoylcyclohexanediones of the formula (I) and their use as herbicides. In this formula (I), R1a, R1b, R1c, R2, R3, R4 and R5 denote various radicals, X1 is a bridging atom, X2 is a carbon chain and X3 is a chalcogen atom or an oximino radical.Type: GrantFiled: April 8, 2003Date of Patent: August 16, 2005Assignee: Bayer CropScience GmbHInventors: Thomas Seitz, Andreas van Almsick, Lothar Willms, Monika H. Schmitt, Thomas Auler, Hermann Bieringer, Hubert Menne
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Patent number: 6924297Abstract: Compounds of formula (I) and pharmaceutically acceptable derivatives thereof bind with high affinity to the EP4 receptor and are of use in the treatment or prevention of conditions such as a pain, inflammatory, immunological, bone, neurodegenerative or renal disorder.Type: GrantFiled: December 20, 2001Date of Patent: August 2, 2005Assignee: SmithKline Beecham CorporationInventors: Gerard Martin Paul Giblin, Haydn Terence Jones, Andrew McMurtrie Mason, Neil Derek Miller, Susan Roomans, Stephen Edward Shanahan, Ann Louise Walker
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Patent number: 6919343Abstract: N-Biphenyl(substituted methyl)aminocycloalkanecarboxamide derivatives are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.Type: GrantFiled: January 30, 2003Date of Patent: July 19, 2005Assignee: Merck & Co., Inc.Inventors: Michael R. Wood, Neville J. Anthony, Mark G. Bock, Dong-Mei Feng, Scott D. Kuduk, Dai-Shi Su, Jenny Miu-chun Wai
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Patent number: 6916819Abstract: This invention relates to benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds, all of which may be described by of Formula I The invention is particularly related to such compounds that bind with high selectivity and high affinity to the benzodiazepine site of GABAA receptors. This invention also relates to pharmaceutical compositions comprising such compounds and to the use of such compounds in treatment of certain central nervous system (CNS) diseases. Novel processes for preparing compounds of Formula I are disclosed. This invention also relates to the use of benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds of Formula I in combination with one or more other CNS agents to potentiate the effects of the other CNS agents. Additionally this invention relates to the use such compounds as probes for the localization of GABAA receptors in tissue sections.Type: GrantFiled: December 21, 2001Date of Patent: July 12, 2005Assignee: Neurogen CorporationInventors: Guiying Li, John M. Peterson, Pamela Albaugh, Kevin S. Currie, Guolin Cai, Linda M. Gustavson, Kyungae Lee, Alan Hutchison, Vinod Singh, George D. Maynard, Jun Yuan, Ling Hong Xie, Manuka Ghosh, Nian Liu
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Patent number: 6906046Abstract: Benzobicyclooctane compounds, their use in inhibiting cellular events involving TNF-? and IL-8, and in the treatment of inflammation events in general; a combinatorial library of diverse bicyclooctanes and process for their synthesis as a library and as individual compounds.Type: GrantFiled: December 11, 2001Date of Patent: June 14, 2005Assignee: Celltech R & D Inc.Inventors: Randy W. Jackson, Ihab Darwish, Ted A. Baughman, J. Jeffry Howbert
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Patent number: 6887877Abstract: The present invention provides novel compounds represented by formula I: or pharmaceutically acceptable salts thereof useful for treating Flaviviridae viral infection.Type: GrantFiled: June 11, 2002Date of Patent: May 3, 2005Assignee: ViroChem Pharma Inc.Inventors: Laval Chan Chun Kong, Jean Bedard, Sanjoy Kumar Das, Nghe Nguyen Ba, Oswy Z. Pereira, Stephen Joseph Shuttleworth, Mohammad Arshad Siddiqui, Wuyi Wang
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Patent number: 6887871Abstract: There is disclosed the use of a compound of formula (I) wherein R1, R2, X, Y, V, W and Z are as defined in the specification, and pharmaceutically acceptable salts, enantiomers or racemates thereof, in the manufacture of a medicament, for the treatment or prophylaxis of diseases or conditions in which inhibition of nitric oxide synthase activity is beneficial. Certain novel compounds of formula (Ia) and pharmaceutically acceptable salts thereof, and enantiomers and racemates thereof are disclosed; together with processes for their preparation, compositions containing them and their use in therapy. The compounds of formulae (I) and (Ia) are inhibitors of the enzyme nitric oxide synthase and are thereby particularly useful in the treatment or prophylaxis of inflammatory disease.Type: GrantFiled: February 20, 2001Date of Patent: May 3, 2005Assignee: AstraZeneca ABInventors: David Cheshire, Stephen Connolly, David Cox, Peter Hamley, Antonio Mete, Austen Pimm
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Patent number: 6878728Abstract: The invention provides novel compounds of formula (I) wherein all variables are as defined in the specification, that are useful as inhibitors of aspartyl proteases.Type: GrantFiled: June 9, 2000Date of Patent: April 12, 2005Assignee: Vertex Pharmaceutical IncorporatedInventors: Michael R. Hale, Roger Tung, Stephen Price, Robin David Wilkes, Wayne Carl Schairer, Ashley Nicholas Jarvis, Andrew Spaltenstein, Eric Steven Furfine, Vicente Samano, Istvan Kaldor, John Franklin Miller, Michael Stephen Brieger
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Patent number: 6869969Abstract: Isoxazole estrogen receptor agonist and antagonist compounds having unexpected and surprising activity in modulating estrogen receptor activity are described. In addition, methods and compositions for treating or preventing estrogen receptor-mediated disorders are disclosed. The compounds, methods, and compositions of the 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: November 13, 2003Date of Patent: March 22, 2005Assignee: Chiron CorporationInventors: Verena D. Huebner, Xiaodong Lin, Ian James, Liya Chen, Manoj Desai, Jennifer C. Moore, Beata Krywult, Thayalan Navaratnam, Rajinder Singh, Rob Trainor, Liang Wang
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Patent number: 6861561Abstract: The invention relates to substituted aromatic polycyclic tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases.Type: GrantFiled: September 26, 2002Date of Patent: March 1, 2005Assignee: G. D. Searle & Co.Inventors: James A. Sikorski, Richard C. Durley, Mark A. Massa, Jane L. Wang, Deborah A. Mischke, Barry L. Parnas, Melvin L. Rueppel
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Patent number: 6858635Abstract: Disclosed are novel compounds that are useful and effective as photoaffinity probes and methods of using oxazolidinone photoaffinity probes.Type: GrantFiled: February 6, 2003Date of Patent: February 22, 2005Assignee: Pharmacia & Upjohn CompanyInventors: Lisa Marie Thomasco, Robert C. Gadwood
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Patent number: 6846934Abstract: Novel photochromic diarylethenes substituted with an isoxazole group and the method of preparation are disclosed. Also disclosed are compositions made with the photochromic diarylethenes. The preparation of thin films with the photochromic diarylethenes or compositions thereof are disclosed. The photochromic diarylethenes or compositions thereof may be used, for example in recording materials, photochromic windows, indicating elements, plastic mirrors, photochromic filters, photo switches, photosensitive drums, recording elements, solar cells, lens, fibers and optical elements.Type: GrantFiled: June 28, 2001Date of Patent: January 25, 2005Assignee: Korea Research Institute of Chemical TechnologyInventors: Eun Kyoung Kim, Song Yun Cho, Dong Ju Jeon, Young Mi Kim
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Patent number: 6838472Abstract: The current invention provide novel compounds, methods of treating or preventing emphysema, cancer and dermatological disorders, pharmaceutical compositions suitable for the treatment or prevention of emphysema, cancer and dermatological disorders and methods for delivering formulations into the lung of a mammal suffering from emphysema, cancer and dermatological disorders.Type: GrantFiled: September 17, 2002Date of Patent: January 4, 2005Assignee: Syntex (U.S.A.) LLCInventors: Michael Klaus, Jean-Marc Lapierre
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Patent number: 6833367Abstract: The present invention relates to certain substituted polyketides of formula I, wherein A, B and C are as defined herein, pharmaceutical compositions containing said compounds, and the use of said compounds in treating tumors.Type: GrantFiled: November 12, 2002Date of Patent: December 21, 2004Assignee: Novartis ACInventors: Frederick R. Kinder, Jr., Kenneth W. Bair, Timothy M. Ramsey, Michael L. Sabio
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Publication number: 20040248943Abstract: This invention is in the field of antiinflammatory pharmaceutical agents and specifically relates to compounds, compositions and methods for treating disorders mediated by cyclooxygenase-2 or 5-lipoxygenase, such as inflammation.Type: ApplicationFiled: July 8, 2002Publication date: December 9, 2004Applicant: Pharmacia CorporationInventors: John J. Talley, James A. Sikorski, Matthew J. Graneto, Bryan H. Norman, Balekudru Devadas, Hwang-Fun Lu
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Patent number: 6815460Abstract: Prodrugs of COX-2 inhibitors and methods of their preparation are described. The prodrugs of COX-2 inhibitors are described as being useful in treating inflammation and inflammation-related disorders.Type: GrantFiled: June 24, 2002Date of Patent: November 9, 2004Assignee: Pharmacia CorporationInventors: John J Talley, James W Malecha, Stephen Bertenshaw, Matthew J Graneto, Jeffery Carter, Jinglin Li, Srinivasan Nagarajan, David L Brown, Donald J Rogier, Jr., Thomas D Penning, Ish K Khanna, Xiangdong Xu, Richard M Weier
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Patent number: 6809111Abstract: A compound of Formula (I), or a pharmaceutically-acceptable salt thereof, suitable for use in the treatment of a cyclooxygenase-2 mediated disease is provided. Also provided is a pharmaceutical composition comprising a compound of Formula (I), or a pharmaceutically-acceptable salt thereof, and a method for treatment of a cyclooxygenase-2 mediated disease by administering to a subject in need thereof a therapeutically-effective amount of the pharmaceutical composition.Type: GrantFiled: May 15, 2003Date of Patent: October 26, 2004Assignee: Pharmacia CorporationInventor: Jeffery S. Carter
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Patent number: 6797723Abstract: The invention relates to novel heterocycle substituted diphenyl leukotriene B4 (LTB4) antagonists, to compositions containing such compounds, and to methods of using such compounds for treatment of inflammatory diseases.Type: GrantFiled: April 24, 2002Date of Patent: September 28, 2004Assignee: Eli Lilly and CompanyInventors: Jason Scott Sawyer, Douglas Wade Beight, Edward C R Smith, William Thomas McMillen
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Patent number: 6794404Abstract: A compound of the formula I: wherein: X is CH or N; Y is O or S; Z is OH, NH2, NMeR3, NHR3; OR3 or 5- or 6-membered heterocycle, having 1 to 4 heteroatoms selected from O, N and S, said heterocycle being optionally substituted with from 1 to 4 substituents; A is N, COR7 or CR5, wherein R5 is H, halogen, or (C1-6) alkyl and R7 is H or (C1-6 alkyl), with the proviso that X and A are not both N; R6 is H, halogen, (C1-6 alkyl) or OR7, wherein R7 is H or (C1-6 alkyl); R1 is selected from the group consisting of 5- or 6-membered heterocycle having 1 to 4 heteroatoms selected from O, N, and S, phenyl, phenyl(C1-3)alkyl, (C2-6)alkenyl, phenyl(C2-6)alkenyl, (C3-6)cycloalkyl, (C1-6)alkyl, CF3, 9- or 10-membered heterobicycle having 1 to 4 heteroatoms selected from O, N and S, wherein said heterocycle, phenyl, phenyl(C2-6)alkenyl and phenyl(C1-3)alkyl), alkenyl, cycloalkyl, (C1-6)alkyl, and heterobicycle are all optionally substituted with from 1 to 4 substituents; R2 is selected from (C1-6)alkyl, (CType: GrantFiled: September 10, 2002Date of Patent: September 21, 2004Assignee: Boehringer Ingelheim (Canada) Ltd.Inventors: Pierre Louis Beaulieu, Gulrez Fazal, James Gillard, George Kukolj, Volkhard Austel
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Publication number: 20040171616Abstract: The invention relates to polycyclic aryl and heteroaryl substituted 1,4-quinone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.Type: ApplicationFiled: February 19, 2003Publication date: September 2, 2004Inventors: Michael S. South, John J. Parlow
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Patent number: 6767918Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: GrantFiled: December 9, 2002Date of Patent: July 27, 2004Assignees: Athena Neurosciences, Inc., Eli Lilly & CompanyInventors: Jing Wu, Eugene D. Thorsett, Jeffrey S. Nissen, Thomas E. Mabry, Lee H. Latimer, Varghese John, Lawrence Y. Fang, James E. Audia
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Patent number: 6759419Abstract: The present invention relates to substituted pyrrolidinone compounds of formula 1, wherein n is 0 or 1; Aza is a heterocycle optionally substituted with C1-4 alkyl, or C1-4 alkyl substituted with a heterocycle, which represents a saturated or unsaturated five- or six-membered ring having nitrogen(s) as a heteroatom, which are muscarinic acetylcholine receptor agonists and useful as nootropics and therapeutic agents for cerebral neural diseases such as Alzheimer's disease; and pharmaceutically acceptable salts thereof; processes for the preparation thereof; and pharmaceutical compositions comprising these compounds or salts.Type: GrantFiled: October 18, 2002Date of Patent: July 6, 2004Assignee: Korea Institute of Science and TechnologyInventors: Youseung Kim, Soon Bang Kang, Gyochang Keum, Min Seok Jang, Jae Yang Kong, Dae Young Jeong, Taeg-Su Jang
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Patent number: 6756497Abstract: Benzoic acid derivatives useful as intermediates for the preparation of drugs and agricultural chemicals, particularly compounds having herbicidal activity; and easy and economical processes for the preparation of the same. The processes are specifically those represented by reaction formula for the preparation of compounds represented by general formulae (1) and (6).Type: GrantFiled: January 12, 2001Date of Patent: June 29, 2004Assignee: Nippon Soda Co., Ltd.Inventors: Yuuki Nakagawa, Masao Yamaguchi, Hiroyuki Adachi, Hiroyuki Yamanaka, Tomio Yagihara, Masami Hatano
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Patent number: 6727360Abstract: The present invention relates to processes for the production of &agr;-aryl-&bgr;-ketonitriles, which serve as synthetic intermediates in the preparation of a series of biologically important molecules such as corticotropin releasing factor (CRF) receptor antagonists.Type: GrantFiled: March 13, 2003Date of Patent: April 27, 2004Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Jiacheng Zhou, Lynette May Oh, Philip Ma
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Patent number: 6713436Abstract: The present invention relates to 1-cycloalkylpyrazolylbenzoyl derivatives of the formula I wherein all variables are as defined in the specification, their agriculturally useful salts, processes for their preparation, and for the use of these compounds or compositions comprising them, for controlling undesirable plants.Type: GrantFiled: February 6, 2002Date of Patent: March 30, 2004Assignee: BASF AktiengesellschaftInventors: Ulf Neidlein, Norbert Götz, Ulf Misslitz, Roland Götz, Ernst Baumann, Wolfgang von Deyn, Steffen Kudis, Klaus Langemann, Guido Mayer, Matthias Witschel, Martina Otten, Karl-Otto Westphalen, Helmut Walter
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Patent number: 6706743Abstract: The instant invention provides &bgr;3 adrenergic receptor agonists of structural Formula (I), the stereoisomers and prodrugs thereof, and the pharmaceutically acceptable salts of the compounds, stereoisomers and prodrugs, wherein Ar, R, R1, R2, R3, R4, R5, R6, R7, R8, X, and Y, are as defined herein.Type: GrantFiled: March 5, 2003Date of Patent: March 16, 2004Assignee: Pfizer IncInventors: Robert F. Day, Jennifer A. Lafontaine
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Publication number: 20040034229Abstract: Disclosed are compounds of the formula (I) 1Type: ApplicationFiled: October 11, 2002Publication date: February 19, 2004Applicant: Schering CorporationInventors: Arthur G. Taveras, Michael Dwyer, Johan A. Ferreira, Viyyoor M. Girijavallabhan, Jianping Chao, John J. Baldwin, J. Robert Merritt, Ge Li
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Publication number: 20040030132Abstract: The present invention relates to biphenyl and biphenyl-analogous compounds, their preparation and use as pharmaceutical compositions, as integrin antagonists and in particular for the production of pharmaceutical compositions for the treatment and prophylaxis of cancer, arteriosclerosis, restenosis, osteolytic disorders such as osteoporosis and ophthalmic diseases.Type: ApplicationFiled: October 31, 2002Publication date: February 12, 2004Inventors: Markus Albers, Klaus Urbahns, Andrea Vaupel, Michael Harter, Delf Schmidt, Beatrix Stelte-Ludwig, Christoph Gerdes, Elke Stahl, Jorg Keldenich, Ulf Brueggemeier, Klemens Lustig
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Patent number: 6683103Abstract: Thienylsulfonamides and their pharmaceutically acceptable derivatives, pharmaceutical compositions, articles of manufacture, combinations, lyophilized powders and methods for the treatment of endothelin diseases using these formulations and sulfonamides are provided. A process of preparing an alkali metal salt of a hydrophobic sulfonamide is provided. The process includes the step of dissolving a free sulfonamide in an organic solvent in the presence of a saturated alkali metal salt solution and recovering the formed sulfonamide salt from the organic phase.Type: GrantFiled: December 20, 2001Date of Patent: January 27, 2004Assignee: Texas Biotechnology CorporationInventors: Chengde Wu, Natalie Blok, Timothy Kogan, Karin Keller
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Patent number: 6677341Abstract: The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described. Preferred (R)-Chiral 1-Substitutedamino-(n+1)-Alkanol compounds are substituted (R)-Chiral heteroaryl aminoalcohols.Type: GrantFiled: December 12, 2001Date of Patent: January 13, 2004Assignee: Pharmacia CorporationInventors: James A. Sikorski, Richard C. Durley, Margaret L. Grapperhaus, Mark A. Massa, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Brian S. Hickory, Monica B. Norton, William F. Vernier, Deborah A. Mischke, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Patent number: 6673780Abstract: The present invention relates to novel sulfoxide and bis-sulfoxide compounds, compositions comprising sulfoxide and bis-sulfoxide compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising an ether compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer, inflammation, and impotence. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.Type: GrantFiled: October 11, 2001Date of Patent: January 6, 2004Assignee: Esperion Therapeutics, Inc.Inventors: Jean-Louis Henri Dasseux, Carmen Daniela Oniciu
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Patent number: 6673818Abstract: Methods of treating cyclooxygenase-2 mediated disorders comprising administering to a subject a therapeutically effective amount of one or more fluoro-substituted benzenesulfonyl compounds corresponding to Formula I: wherein A, X, n, R1, R2, and R3 are as described in the specification, and novel fluoro-substituted benzenesulfonyl compounds within Formula I.Type: GrantFiled: April 16, 2002Date of Patent: January 6, 2004Assignee: Pharmacia CorporationInventors: David L. Brown, Matthew J. Graneto, Cindy L. Ludwig, John M. Molyneaux, John J. Talley
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Publication number: 20030236274Abstract: A composition containing a compound of the formula: 1Type: ApplicationFiled: May 22, 2003Publication date: December 25, 2003Inventors: Akihiro Tasaka, Akio Ojida, Tomohiro Kaku, Masami Kusaka, Masuo Yamaoka
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Patent number: 6664395Abstract: The present invention relates to novel benzotriazoles of the formula I wherein Het is an optionally substituted 5-membered heterocycle containing one to two heteroatoms selected from nitrogen, sulfur and oxygen wherein at least one of said heteroatoms atoms must be nitrogen; R2 is selected from the group consisting of hydrogen, (C1-C6)alkyl or other suitable substituents; R3 is selected from the group consisting of hydrogen, (C1-C6)alkyl or other suitable substituents; s is an integer from 0-5; to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the present invention are potent inhibitors of MAP kinases, preferably p38 kinase. They are useful in the treatment of inflammation, osteoarthritis, rheumatoid arthritis, cancer, repurfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.Type: GrantFiled: April 4, 2002Date of Patent: December 16, 2003Assignee: Pfizer IncInventors: Michael A. Letavic, Mark A. Dombroski, Kim F. McClure, Ellen R. Laird
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Patent number: 6664277Abstract: The present invention is directed to compounds useful in the treatment of diseases associated with prenylation of proteins and pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising same, and to methods for inhibiting protein prenylation in an organism using the same.Type: GrantFiled: January 3, 2003Date of Patent: December 16, 2003Assignee: PPD Discovery, Inc.Inventors: Bradley B. Brown, Kenneth S. Rehder, Jon-Paul Strachan, Jeron H. Eaves, Christopher T. Lowden
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Patent number: 6660736Abstract: This invention relates to phthalimido derivatives of the formula wherein X is —N═ or —CH═, and R1 to R4 and m are as defined in the specification, as well as their pharmaceutically acceptable salts. The invention further relates to pharmaceutical compositions containing these compounds, a method of treating a disease by administering a therapeutically effective amount of at least one of these compounds, and a process for their preparation for the treatment or prevention of diseases in which MAO-B inhibitors might be beneficial.Type: GrantFiled: March 13, 2003Date of Patent: December 9, 2003Assignee: Hoffmann-La Roche Inc.Inventors: Andrea Cesura, Rosa Maria Rodriguez Sarmiento, Andrew William Thomas, Rene Wyler
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Publication number: 20030225086Abstract: The invention relates to polycyclic aryl and heteroaryl substituted 1,4-quinone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.Type: ApplicationFiled: February 19, 2003Publication date: December 4, 2003Inventors: Michael S. South, John J. Parlow
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Patent number: 6649640Abstract: Described herein are compounds that are useful as protein kinase inhibitors, especially inhibitors of ERK, having the formula: where A, B, R1, R2, T and Ht are described in the specification. The compounds are useful for treating diseases in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, and cardiovascular disease.Type: GrantFiled: October 15, 2002Date of Patent: November 18, 2003Assignee: Vertex Pharmaceuticals IncorporatedInventors: Michael Hale, James Janetka, Francois Maltais, Jingrong Cao
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Patent number: 6649629Abstract: The present invention describes novel nitrosated and/or nitrosylated cyclooxygenase 2 (COX-2) inhibitors and novel compositions comprising at least one nitrosated and/or nitrosylated cyclooxygenase 2 (COX-2) 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 optionally, at least one therapeutic agent, such as, steroids, nonsteroidal antiinflammatory compounds (NSAID), 5-lipoxygenase (5-LO) inhibitors, leukotriene B4 (LTB4) receptor antagonists, leukotriene A4 (LTA4) hydrolase inhibitors, 5-HT agonists, 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) inhibitors, H2 antagonists, antineoplastic agents, antiplatelet agents, decongestants, diuretics, sedating or non-sedating anti-histamines, inducible nitric oxide synthase inhibitors, opioids, analgesics, Helicobacter pylori inhibitors, proton pump inhType: GrantFiled: December 22, 2000Date of Patent: November 18, 2003Assignee: Nitromed, Inc.Inventors: Upul K. Bandarage, Xinqin Fang, David S. Garvey, L. Gordon Letts, Joseph D. Schroeder, Sang William Tam
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Publication number: 20030208067Abstract: The present invention is directed in part towards methods of modulating the function of protein kinases with phenol- and hydroxynaphthalene-based compounds. The methods incorporate cells that express a protein kinase. In addition, the invention describes methods of preventing and treating protein kinase-related abnormal conditions in organisms with a compound identified by the invention. Furthermore, the invention pertains to phenol- and hydroxynaphthalene-based compounds and pharmaceutical compositions comprising these compounds.Type: ApplicationFiled: May 28, 2002Publication date: November 6, 2003Inventors: Sheldon Xiaodong Cao, David Paul Dumas, Xiaohua Chen, Jae Young Yang
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Publication number: 20030208073Abstract: The invention relates to novel substituted N-aryl nitrogen-containing heterocyclic compounds of the general formula (I) 1Type: ApplicationFiled: January 29, 2003Publication date: November 6, 2003Inventors: Karl-Heinz Linker, Kurt Findeisen, Otto Schallner, Andreas Lender, Hans-Joachim Santel, Markus Dollinger, Akihiko Yanagi, Toshio Goto
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Patent number: 6639078Abstract: The present invention includes nuclear receptor heterodimer and nuclear receptor-coactivator pepetide assays for identifying ligands for nuclear receptors, utilizing scintillation proximity and fluorescence resonance energy transfer (FRET), and methods of using identified ligands.Type: GrantFiled: June 18, 2001Date of Patent: October 28, 2003Assignee: SmithKline Beecham CorporationInventors: Curt Dare Haffner, Patrick Reed Maloney, Timothy Mark Wilson
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Publication number: 20030195208Abstract: This invention relates to phthalimido derivatives of the formula 1Type: ApplicationFiled: March 13, 2003Publication date: October 16, 2003Inventors: Andrea Cesura, Rosa Maria Rodriguez Sarmiento, Andrew William Thomas, Rene Wyler
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Publication number: 20030195241Abstract: Described herein are compounds that are useful as protein kinase inhibitors, especially inhibitors of ERK, having the formula: 1Type: ApplicationFiled: October 15, 2002Publication date: October 16, 2003Inventors: Michael Hale, James Janetka, Francois Maltais, Jingrong Cao, Robert Mashal
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Patent number: 6630506Abstract: Acyl guanidines are provided which are sodium/proton exchange (NHE) inhibitors which have the structure wherein n is 0 to 4; X is a bond, O, S, SO, SO2, CO, or NR7; Y is a bond, O, S, SO, SO2, CO, or NR7′ wherein at least one of X and Y is other than a bond; and R1, R2, R3, R4, R5, R6, R7 and Ra, Rb, Rc, Rd are as defined herein, and are useful as antianginal, cardioprotective agents, antiischemic agents, and agents for peripheral vascular disease including intermittent claudication. In addition, a method is provided for preventing or treating angina pectoris, cardiac dysfunction, myocardial necrosis, arrhythmia, peripheral vascular diseases (PVD), including peripheral atherosclerotic disease (PAD), including intermittent claudication, Raynaud's diseases, and LeRiches Syndrome, pain, parethesia or discomfort in the lower limb and gluteal regions produced by vascular (e.g.Type: GrantFiled: April 21, 2000Date of Patent: October 7, 2003Assignee: Bristol-Myers Squibb Co.Inventors: Sundeep Dugar, Steven V. O'Neil
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Publication number: 20030187042Abstract: The present invention relates to compounds according to the general formula (I) which bind to the nuclear receptor, NR1H4, and act as agonists and antagonists of the NR1H4 receptor. The invention further relates to the treatment of diseases and/or conditions through binding of the nuclear receptor by the compounds.Type: ApplicationFiled: July 1, 2002Publication date: October 2, 2003Inventors: Ulrike Bauer, Zach Cheruvallath, Ulrich Deuschle, Elena Dneprovskaia, Tim Gahman, Kristina Giegrich, Ronnie Hanecak, Normand Hebert, John Kiely, Ingo Kober, Manfred Kogl, Harald Kranz, Claus Kremoser, Matthew Lee, Kerstin Otte, Carlton Sage, Manish Sud
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Patent number: 6624309Abstract: Benzoic acid derivatives of the formula where X is oxygen, sulfur, —NH, —NR1, —N—CN, —N—OR1 or —N—NO2; Y is a single bond, —C═C—, or —NH; R1 is alkyl, alkenyl, alkynyl, aryl, cycloalkyl, heterocyclo, or (heterocyclo)alkyl; and R2 is aryl or heterocyclo. The compounds of formula I are useful in the treatment of arrhythmia.Type: GrantFiled: September 25, 2002Date of Patent: September 23, 2003Assignee: Bristol-Myers Squibb CompanyInventors: John Lloyd, George C. Rovnyak, Philip D. Stein, Saleem Ahmad, Karnail S. Atwal, Thomas J. Caulfield, Michael A. Poss