Acyclic Nitrogen Bonded Directly To A -c(=x)- Group, Wherein X Is Chalcogen Patents (Class 544/393)
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Patent number: 7407959Abstract: 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: GrantFiled: November 18, 2005Date of Patent: August 5, 2008Assignee: Merck Frosst Canada & Co.Inventors: Jacques Yves Gauthier, Chun Sing Li, Christophe Mellon
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Patent number: 7375134Abstract: 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: GrantFiled: February 28, 2003Date of Patent: May 20, 2008Assignees: Axys Pharmaceuticals, Inc., Merck Frosst Canada & Co.Inventors: Christopher I. Bayly, Cameron Black, Serge Leger, Chun Sing Li, Dan McKay, Christophe Mellon, Jacques Yves Gauthier, Vouy-Linh Truong, Cheuk Lau, Michel Therien
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Patent number: 7371747Abstract: The present invention is directed to novel cyanoalkylamino derivatives that are inhibitors of cysteine protease such as cathepsins K, S, B and L, in particular cathepsin K Pharmaceutical composition comprising these compounds, method of treating diseases mediated by unregulated cysteine protease activity, in particular cathepsin K utilizing these compounds and methods of preparing these compounds are also disclosed.Type: GrantFiled: November 13, 2002Date of Patent: May 13, 2008Assignee: Merck Frosst Canada & Co.Inventors: Cameron Black, Sheldon N. Crane, Dana Davis, Eduardo L. Setti
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Publication number: 20080081813Abstract: Biphenylcarboxamide compounds of formula (I) methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of hyperlipidemia, obesity and type II diabetes.Type: ApplicationFiled: March 27, 2002Publication date: April 3, 2008Inventors: Lieven Meerpoel, Marcel Viellevoye
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Patent number: 7300936Abstract: There is provided a series of novel ?-(N-sulfonamido)acetamide compounds of the Formula (I) wherein R, R1, R2 and R3 are defined herein, which are inhibitors of ?-amyloid peptide (?-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by anti-amyloid activity.Type: GrantFiled: December 20, 2002Date of Patent: November 27, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Michael F. Parker, Katharin E. McElhone, Robert A. Mate, Joanne J. Bronson, Yonghua Gai, Carl P. Bergstrom, Lawrence R. Marcin, John E. Macor
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Patent number: 7291621Abstract: Substituted biaryl amides of Formula I are provided. Such compounds are ligands that may be used to modulate C5a receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological C5a receptor activation in humans, domesticated companion animals and livestock animals.Type: GrantFiled: January 3, 2006Date of Patent: November 6, 2007Assignee: Neurogen CorporationInventors: Yang Gao, Andrew Thrukauf, He Zhao
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Patent number: 7271289Abstract: Compounds of formula (I): or pharmaceutically acceptable derivatives thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors.Type: GrantFiled: April 7, 2004Date of Patent: September 18, 2007Assignee: SmithKline Beecham CorporationInventor: Nicola Mary Aston
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Patent number: 7238693Abstract: The present invention relates to novel compounds, the preparation and use, particularly therapeutic, thereof. More specifically, it relates to compounds derived from aryl carbamates, the preparation and use thereof, particularly in the field of human and animal health. The compounds according to the invention are preferably 5-HT4 serotoninergic receptor ligands and can therefore be used in the therapeutic or prophylactic treatment of any disorder involving a 5-HT4 receptor. The invention also relates to pharmaceutical compositions comprising such compounds, the preparation and use thereof and treatment methods using said compounds.Type: GrantFiled: February 22, 2002Date of Patent: July 3, 2007Assignees: Cerep, Centre National de la Recherche Scientifique, Institut National de la Santa et de la Recherche Medicale (inserm)Inventors: Eric Nicolai, Sophie Curtet, James Sicsic, Frank Lezoualc'h, Rodolphe Fischmeister, Michel Langlois, Magali Maillet, Michèle Launay
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Patent number: 7214680Abstract: The present invention relates to piperazine of formula (I) wherein R represents halogen, C1-4 alkyl, trifluoromethoxy or trifluoromethyl; R1 is trifluoromethyl, C1-4 alkyl, C1-4 alkoxy, halogen or trifluoromethoxy; R2 is hydrogen, C1-4 alkyl or C2-6 alkenyl; R3 represents hydrogen or C1-4 alkyl; n and m are independently 0 or an integer from 1 to 3; and pharmaceutically acceptable salts and solvates thereof, process for their preparation and their use in the treatment of condition mediated by tachykinins and/or by selective inhibition of the serotonin reuptake transporter protein.Type: GrantFiled: August 13, 2002Date of Patent: May 8, 2007Assignee: Glaxo Group LimitedInventors: Giuseppe Alvaro, Torquil I. M. Jack, Maria Elvira Tranquillini
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Patent number: 7208629Abstract: Compounds of formula (I): wherein when m is 0 to 4 R1 is selected from C1–6alkyl, C3–7cycloalkyl, C2–6alkenyl, —SO2NR4R5, —CONR4R5 and —COOR4; and when m is 2 to 4 R1 is additionally selected from C1–6alkoxy, hydroxy, NR4R5, —NR4SO2R5, —NR4SOR5, —NR4COR5, and —NR4CONR4R5; R2 is selected from hydrogen, C1–6alkyl and —(CH2)n-C3–7cycloalkyl; R3 is the group —CO—NH—(CH2)p-R6; U is selected from methyl and halogen; W is selected from methyl and chlorine; V and Y are each selected independently from hydrogen, methyl and halogen; m is selected from 0, 1, 2, 3 and 4 wherein each carbon atom of the resulting carbon chain may be optionally substituted with one or two groups selected independently from C1–6alkyl; n is selected from 0, 1, 2 and 3; p and r are independently selected from 0, 1 and 2; s is selected from 0, 1 and 2; or pharmaceutically acceptable salts or solvates thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitorsType: GrantFiled: October 16, 2002Date of Patent: April 24, 2007Assignee: Glaxo Group LimitedInventors: Richard Martyn Angell, Nicola Mary Aston, Paul Bamborough, George Stuart Cockerill, Suzanne Joy Merrick, Kathryn Jane Smith, Ann Louise Walker
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Patent number: 7153858Abstract: The invention relates to 5-HT receptor agonists or antagonists. Novel arylpiperazinyl sulfonamide compounds represented by Formulae I: and II, and synthesis and uses of those compounds for treating diseases including those mediated directly or indirectly by 5-HT receptors, are disclosed. Such conditions include central nervous system disorders such as generalized anxiety disorder, ADD/ADHD, neural injury, stroke, and migraine. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also included.Type: GrantFiled: January 30, 2004Date of Patent: December 26, 2006Assignee: Epix Delaware, Inc.Inventors: Dale S. Dhanoa, Dongli Chen, Oren Becker, Silvia Noiman, Srinivasa Rao Cheruku, Yael Marantz, Anurag Sharadendu, Sharon Shachem, Alexander Heifetz, Pradyumna Mohanty, Boaz Inbal, Merav Fichman, Raphael Nudelman, Shay Bar-Haim
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Patent number: 7148225Abstract: Substituted biaryl amides of Formula I are provided. Such compounds are ligands that may be used to modulate C5a receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological C5a receptor activation in humans, domesticated companion animals and livestock animals.Type: GrantFiled: November 19, 2004Date of Patent: December 12, 2006Assignee: Neurogen CorporationInventors: Yang Gao, Alan J. Hutchinson, Wallace C. Pringle, Taeyoung Yoon, He Zhao
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Patent number: 7125997Abstract: The invention is directed to novel biaryl derivatives, to the uses of these compounds in various medicinal applications, including the treatment, prevention and control of proliferative diseases such as tumors, and to pharmaceutical compositions comprising these compounds. Compounds of the invention can be used to treat or prevent diseases or disorders that involve the activity of MIF-1 and/or adenosine kinase.Type: GrantFiled: December 18, 2003Date of Patent: October 24, 2006Assignee: IRM LLCInventors: Jason Chyba, Quinn Devereax, Garret Hampton, Fred King
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Patent number: 7078404Abstract: The invention relates to acyl-3-carboxyphenylurea derivatives and to their physiologically tolerated salts and physiologically functional derivatives. The invention relates to compounds of formula I, in which the radicals have the given meanings, and to their physiologically tolerated salts and processes for preparing them. The compounds are, for example, suitable for use as antidiabetics.Type: GrantFiled: April 10, 2003Date of Patent: July 18, 2006Assignee: Sanofi-Aventis Deutschland GmbHInventors: Elisabeth Defossa, Dieter Kadereit, Karl Schoenafinger, Thomas Klabunde, Hans-Joerg Burger, Andreas Herling, Karl-Ulrich Wendt, Erich Von Roedern, Alfons Enhsen
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Patent number: 7056922Abstract: A compound of the formula wherein D, E, F, G, L, T, W, X, Y, Z, U, A, R1, R2, R3, R4, R5, R6 R7 are as defined in the specification, pharmaceutical compositions thereof, and methods of use to treat diseases and as D3 receptor modulators.Type: GrantFiled: July 29, 2003Date of Patent: June 6, 2006Assignee: Pfizer IncInventors: Anton F. J. Fliri, Anthony R. Reinhold
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Patent number: 7026323Abstract: Compounds of the following formula (I): where a, b, R1, R2, R3, R4 and R6 are described herein, are useful as inhibitors of platelet adenosine diphosphate. Pharmaceutical compositions containing these compounds, methods of using these compounds as antithrombotic agents and processes for synthesizing these compounds are also described herein.Type: GrantFiled: September 22, 2004Date of Patent: April 11, 2006Assignee: Schering AktiengesellschaftInventors: Judi A. Bryant, Brad O. Buckman, Imadul Islam, Raju Mohan, Michael M. Morrissey, Guo Ping Wei, Wei Xu, Shendong Yuan
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Patent number: 6969713Abstract: The invention provides piperidine and piperazine derivatives of general formula (I), processes for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapyType: GrantFiled: December 18, 2000Date of Patent: November 29, 2005Assignee: AstraZeneca ABInventors: Premji Meghani, Colin Bennion
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Patent number: 6906073Abstract: The invention provides compounds of Formula (I): wherein: R1-R4, A, L, and X have any of the values defined in the specification that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use, and methods and intermediates useful for preparing them.Type: GrantFiled: November 29, 2002Date of Patent: June 14, 2005Assignee: Roche Palo Alto LLCInventors: Daisy Joe Du Bois, Denis John Kertesz, Eric Brian Sjogren, David Bernard Smith, Beihan Wang
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Patent number: 6903120Abstract: New 3-substituted 4-(phenyl-N-alkyl)-piperazine and 4-(phenyl-N-alkyl)-piperidine compounds of Formula (1), wherein X N, CH, or C, however X may only be C when the compound comprises a double bond at the dotted line; R1 is OSO2CF3, OSO2CH3, SOR3, SO2R3, COR3, NO2, or CONHR3 and when X is CH or C R1 may also be CF3, CN, F, Cl, Br, or I; R2 is a C1-C4 alkyl, an allyl, CH2SCH3, CH2CH2OCH3, CH2CH2CH2F, CH2CF3, 3,3,3-trifluoropropyl, 4,4,4,-trifluorobutyl, or —(CH2)—R4; R3 is a C1-C3 alkyl CF3, or N(R2)2; R4 is a C3-C6 cycloalkyl, 2-tetrahydrofurane or 3-tetra-hydrofurane, as well as pharmaceutically acceptable salts thereof are disclosed.Type: GrantFiled: December 22, 2000Date of Patent: June 7, 2005Assignee: A. Carlsson Research ABInventors: Clas Sonesson, Ingela Marianne Svan, Anders Kristoffer Lilja, Liselott Lilja Rönnqvist, Jenny Maria Carlberg, Susanna Waters, Nicholas Waters, Joakim Tedroff, Bengt Andersson
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Patent number: 6894053Abstract: Compounds of the formula have a long duration of action and are useful for the treatment of chronic diseases resulting from the dysfunction of the serotonergic 5-HT1A system, such as schizophrenia and other psychotic disorders such as paranoia and mano-depressive illness.Type: GrantFiled: December 12, 2003Date of Patent: May 17, 2005Assignee: WyethInventors: Wayne E. Childers, Michael G. Kelly, Lee E. Schechter, Sharon J. Rosenzweig-Lipson
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Patent number: 6894052Abstract: Disclosed herein are novel compounds and methods for the treatment of disorders of the lower urinary tract. The novel compounds are diarylalkylpiperazine derivatives. The methods comprise the administration of the novel compounds of the invention, and other compounds that bind to 5HT1A receptors, for treating disorders of the lower urinary tract.Type: GrantFiled: July 31, 1998Date of Patent: May 17, 2005Assignee: Recordati S.A. Chemical and Pharmaceutical CompanyInventors: Amedeo Leonardi, Gianni Motta, Carlo Riva, Rodolfo Testa
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Patent number: 6887876Abstract: Benzamidine derivatives are useful delta-opioid receptor modulators, agonists useful as analgesics and antagonists useful as immunosuppressants, antiinflammatory agents, agents for the treatment of neurological and psychiatric conditions, medicaments for drug and alcohol abuse, agents for treating gastritis and diarrhea, cardiovascular agents and agents for the treatment of respiratory diseases.Type: GrantFiled: December 11, 2001Date of Patent: May 3, 2005Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Ellen W. Baxter, Samuel O. Nortey, Allen B. Reitz
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Patent number: 6831080Abstract: There is provided novel cinnamide derivatives of Formula I: wherein R is C1-4 alkyl or trifluoromethyl; R1 is selected from the group consisting of pyridinyl, quinolinyl, thienyl, furanyl, 1,4-benzodioxanyl, 1,3-benzodioxolyl, chromanyl, indanyl, biphenylyl, phenyl and substituted phenyl in which said substituted phenyl is substituted with one or two substituents each independently selected-from the group consisting of halogen, C1-4 alkyl, C1-4 alkoxy, trifluoromethyl, trifluoromethoxy and nitro; R2 and R3 are each independently selected from the group consisting of hydrogen, C1-4 alkyl, and halogen; R4 is selected from the group consisting of di(C1-4 alkyl)amino, trifluoromethoxy and optionally substituted morpholin-4-yl, pyridinyl, pyrimidinyl, piperazinyl, and pyrazinyl with one or two substituents in which said substituent is independently selected from the group consisting of C1-4 alkyl, aminomethyl, hydroxymethyl, chloro or fluoro; R5 is hydrogen, chloro or fluoro; or R4 and R5 taken tType: GrantFiled: May 31, 2002Date of Patent: December 14, 2004Assignee: Bristol-Myers Squibb CompanyInventors: Yong-Jin Wu, Li-Quang Sun, Jie Chen, Huan He, Alexandre L'Heureux, Pierre Dextraze, Jean-Paul Daris, Gene G. Kinney, Steven I. Dworetzky, Piyasena Hewawasam
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Patent number: 6784183Abstract: Compounds of formula (I): and medicinal products containing the same which are useful as dual &agr;2/5-HT2c antagonists.Type: GrantFiled: June 29, 2001Date of Patent: August 31, 2004Assignee: Les Laboratoires ServierInventors: Gilbert Lavielle, Olivier Muller, Mark Millan, Anne Dekeyne, Mauricette Brocco
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Patent number: 6777414Abstract: Disclosed are compounds represented by formula (I) which have triglyceride biosynthesis inhibitory activity in the liver and inhibitory activity against the secretion of apolipoprotein B-containing lipoprotein from the liver and particularly have excellent inhibitory activity against the secretion of apolipoprotein B-containing lipoprotein, are free from side effect of accumulation of lipids in the liver, and are useful for the treatment and prevention of hyperlipidemia and arteriosclerotic diseases.Type: GrantFiled: October 5, 2001Date of Patent: August 17, 2004Assignee: Meiji Seika Kaisha, Ltd.Inventors: Naoto Ohkura, Yukiko Hiraiwa, Tetsuya Matsushima, Kazue Sasaki, Takehiro Yamamoto, Masaharu Shiotani, Shigeki Suzuki, Yuuko Nakatani, Chizuko Kuroda, Mieko Nagasawa, Kiyoaki Katano
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Patent number: 6770644Abstract: Hydroxamic acid derivatives of the formula (I) (wherein all the symbols have the same meaning as defined in the specification.), non-toxic salt thereof or prodrugs thereof. The compounds of the formula (I) inhibit producing IL-6, so it may be used for the prevention and/or treatment of various inflammatory diseases, sepsis, multiple myeloma, plasma cell leukemia, osteoporosis, cachexia, psoriasis, nephritis, renal cell carcinoma, Kaposi's sarcoma, rheumatoid arthritis, hypergammaglobulinemia, Castleman's disease, atrial myxoma, diabetes mellitus, autoimmune diseases, hepatitis, colitis, graft versus host disease, infectious diseases and endometriosis.Type: GrantFiled: March 22, 2002Date of Patent: August 3, 2004Assignee: Ono Pharmaceuticals Co., Ltd.Inventors: Mitoshi Konno, Katsuhito Sakaki, Masao Naka, Mikio Konishi, Tadamitsu Kishimoto
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Patent number: 6696450Abstract: Compounds of the formula have a long duration of action and are useful for the treatment of chronic diseases resulting from the dysfunction of the serotonergic 5-HT1A system, such as schizophrenia and other psychotic disorders such as paranoia and mano-depressive illness.Type: GrantFiled: April 2, 2002Date of Patent: February 24, 2004Assignee: WyethInventors: Wayne E. Childers, Michael G. Kelly, Lee E. Schechter, Sharon J. Rosenzweig-Lipson
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Patent number: 6686360Abstract: The present invention relates to a compound selected from those of formula (I): wherein: R1 represents alkyl, R2 represents hydroxy, alkoxy, or amino, n represents an integer from 1 to 12 inclusive, R3 represents: hydrogen, optionally substituted alkyl, cycloalkyl, pyrimidinyl or optionally substituted phenyl, its isomers, and addition salts thereof with a pharmaceutically acceptable acid or base, medicinal products containing the same are useful in the prevention or treatment of acute and chronic cell ischaemia.Type: GrantFiled: July 16, 2002Date of Patent: February 3, 2004Assignee: Les Laboratoires ServierInventors: Serge Labidalle, Jean-Paul Tillement, Bernard Testa, Roméo Cecchelli, Alain Le Ridant, Catherine Harpey, Michael Spedding, Esther Schenker
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Patent number: 6680321Abstract: Compounds of the formula (I) as well as their pharmaceutically acceptable salts, and pharmaceutical compositions comprising the novel compounds. The novel compounds of the formula (I) are useful in the management of pain.Type: GrantFiled: August 2, 2000Date of Patent: January 20, 2004Assignee: AstraZeneca Canada, Inc.Inventors: Edward Roberts, Niklas Plobeck, Claes Wahlestedt
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Patent number: 6642239Abstract: Dipeptide nitrile Cathepsin K inhibitors of formula I, and pharmaceutically acceptable salts or esters thereof: In which R1 and R2 are independently H or C1-C7lower alkyl, or R1 and R2 together with the carbon atom to which they are attached form a C3-C8cycloalkyl ring, and Het is an optionally substituted nitrogen-containing heterocyclic substituent, are provided, useful e.g. for therapeutic or prophylactic treatment of a disease or medical condition in which cathepsin K is implicated.Type: GrantFiled: February 7, 2001Date of Patent: November 4, 2003Assignee: Novartis AGInventor: Martin Missbach
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Patent number: 6596866Abstract: A process for the preparation of Nefazodone hydrochloride comprising direct conversion of semicarbazide dihydrochloride 3 into Nefazodone hydrochloride which process involves a reaction of triethyl orthopropionate in the presence of trimethylsilylchloride and hydrochloric acid.Type: GrantFiled: September 17, 2001Date of Patent: July 22, 2003Assignee: Brantford Chemicals Inc.Inventors: K. S. Keshava Murthy, Bhaskar Reddy Guntoori, Daqing Che
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Patent number: 6593474Abstract: This invention relates to a series of arylsubstituted piperazines, of Formula I pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention selectively inhibit binding to the &agr;-1a adrenergic receptor, a receptor which has been implicated in benign prostatic hyperplasia. As such the compounds are potentially useful in the treatment of this and other disease.Type: GrantFiled: June 12, 2000Date of Patent: July 15, 2003Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Linda Jolliffe, William Murray, Virginia Pulito, Linda Mulcahy, Xiaobing Li, Allen Reitz, Cynthia Maryanoff, Frank Villani
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Patent number: 6579870Abstract: The present invention provides pharmaceutically active compounds useful for the treatment of diseases or disorders of the central nervous system.Type: GrantFiled: June 8, 2001Date of Patent: June 17, 2003Assignee: Pharmacia & Upjohn CompanyInventors: Eric Jon Jacobsen, Stephen J. King
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Patent number: 6569861Abstract: Disclosed are compounds of the formula: and the pharmaceutically acceptable salts thereof wherein Q, X, Y, Z, and R1 R9, and R12-R19 are defined herein. These compounds are selective modulators of MCH 1 receptors that are, therefore, useful in the treatment of a variety of metabolic, feeding, and sexual disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also disclosed.Type: GrantFiled: July 6, 2001Date of Patent: May 27, 2003Assignee: Neurogen CorporationInventors: Rajagopal Bakthavatchalam, Andrew Thurkauf, Alan Hutchison
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Patent number: 6555541Abstract: The invention provides substituted phenyl compounds of general formula wherein R1, T, U and Ar are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy.Type: GrantFiled: July 10, 2000Date of Patent: April 29, 2003Assignee: Astrazeneca UK LimitedInventors: Mark Furber, Timothy J Luker, Michael P Mortimore, Philip Thorne, Premji Meghani
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Publication number: 20030078423Abstract: A process for the preparation of Nefazodone hydrochloride comprising direct conversion of semicarbazide dihydrochloride 3 into Nefazodone hydrochloride which process involves a reaction of triethyl orthopropionate in the presence of trimethylsilylchloride and hydrochloric acid.Type: ApplicationFiled: September 17, 2001Publication date: April 24, 2003Applicant: Brantford Chemicals Inc.Inventors: K. S. Keshava Murthy, Bhaskar Reddy Guntoori, Daqing Che
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Patent number: 6552022Abstract: The invention relates to therapeutic benzamide compounds of formula (I) wherein A, X, Z, R1, Y, R2, R3, are as defined herein, and physiologically acceptable salts, solvates or derivatives thereof. The present invention also provides pharmaceutical compositions, processes for the preparation of compounds of formula (I) and their use in the treatment of conditions mediated by ApoB-100 regulation.Type: GrantFiled: May 15, 2001Date of Patent: April 22, 2003Assignee: SmithKline Beecham CorporationInventor: Alain Claude-Marie Daugan
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Publication number: 20030073833Abstract: Phenyl acetamide compounds are described, including compounds of Formula I: 1Type: ApplicationFiled: October 3, 2002Publication date: April 17, 2003Applicant: 3-Dimensional Pharmaceuticals, Inc.Inventors: Wenxi Pan, Tianbao Lu, Thomas P. Markotan, Bruce E. Tomczuk
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Patent number: 6525036Abstract: The present invention relates to novel cysteine protease inhibitors of Formula I: the pharmaceutically acceptable salts and N-oxide derivatives thereof, their use as therapeutic agents and methods of making them.Type: GrantFiled: January 5, 2001Date of Patent: February 25, 2003Assignee: Merck & Co., Inc.Inventors: Renata Marcella Oballa, Petpiboon Prasit, Joel Stephane Robichaud, Elise Isabel, Eduardo Setti, Dan-Xiong Wang, Rohan V. Mendonca, Shankar Venkatraman
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Publication number: 20020198200Abstract: Substituted benzene acetamide compounds and pharmaceutically acceptable salts thereof are useful as glucokinase activators.Type: ApplicationFiled: June 25, 2002Publication date: December 26, 2002Inventors: Robert F. Kester, Ramakanth Sarabu
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Patent number: 6455528Abstract: The present invention relates to a piperazine compound of the formula wherein R1 and R2 are each hydrogen, halogen, lower alkyl, lower alkoxy, amino, substituted amino, nitro, hydroxy or cyano, R3, R4 and R5 are each hydrogen, halogen, lower alkyl, lower alkoxy, nitro, amino, substituted amino or hydroxy, R6 and R7 are each hydrogen, lower alkyl, lower alkyl substituted by halogen, aralkyl, acyl or lower acyl substituted by halogen, R8 and R9 are each hydrogen or lower alkyl, Y is lower alkylene and the like, and ring A is phenyl, pyrimidyl, thiazolyl, pyridyl, pyrazyl or imidazolyl, a pharmaceutically acceptable salt thereof and pharmaceutical agents containing these compounds.Type: GrantFiled: April 14, 2000Date of Patent: September 24, 2002Assignee: Mitsubishi Pharma CorporationInventors: Kunitomo Adachi, Yoshiyuki Aoki, Tokushi Hanano, Hiroshi Morimoto, Masao Hisadome
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Patent number: 6451800Abstract: An objective of the present invention is to provide compounds having integrin &agr;v&bgr;3 antagonistic activity, GP IIb/IIIa antagonistic activity, and/or human platelet aggregation inhibitory activity, and therapeutic agents for treating integrin &agr;v&bgr;3-mediated diseases and for inhibiting platelet aggregation. The derivatives according to the present invention are compounds represented by formula (I) or pharmaceutically acceptable salts or solvates thereof: wherein A represents a five- to seven-membered heterocyclic ring containing two nitrogen atoms or the like; X and Z represent CH or a nitrogen atom; R4 and R5 represent alkyl, halogen or the like; Q represents >C=O, >CH2 or the like; R6 represents H, alkyl, aralkyl or the like; R7 represents H, alkynyl or the like; R8 represents H, substituted amino or the like; R9 represents H or alkyl; m is 0 to 5; n is 0 to 4; p is 2 or 3; and q is 0 or 1.Type: GrantFiled: July 28, 2000Date of Patent: September 17, 2002Assignee: Meiji Seika Kaisha, Ltd.Inventors: Keiichi Ajito, Shoichi Murakami, Minoru Ishikawa, Mikio Yamamoto, Dai Kubota, Shuichi Gomi, Mitsugu Hachisu, Kiyoaki Katano
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Publication number: 20020103234Abstract: Described is a heterocycle-containing carboxylic acid derivative represented by the following formula (I): 1Type: ApplicationFiled: July 23, 2001Publication date: August 1, 2002Applicant: Eisai Co. Ltd.Inventors: Kouichi Kikuchi, Katsuya Tagami, Hiroyuki Yoshimura, Shigeki Hibi, Mitsuo Nagai, Shinya Abe, Makoto Okita, Takayuki Hida, Seiko Higashi, Naoki Tokuhara, Seiichi Kobayashi
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Patent number: 6413947Abstract: This invention is to provide a compound of the formula: wherein R1 is an optionally substituted 5- to 6-membered ring; W is a divalent group of the formula: wherein the ring A is an optionally substituted 5- to 6-membered aromatic ring, X is an optionally substituted C, N or O atom, and the ring B is an optionally substituted 5- to 7-membered ring; Z is a chemical bond or a divalent group; R2 is (1) an, optionally substituted amino group in which a nitrogen atom may form a quaternary ammonium, etc., or a salt thereof, which is useful for antagonizing MCP-1 receptor.Type: GrantFiled: September 13, 2000Date of Patent: July 2, 2002Assignee: Takeda Chemical Industries, Ltd.Inventors: Mitsuru Shiraishi, Takahito Kitayoshi, Yoshio Aramaki, Susumu Honda, Tsuneo Oda
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Patent number: 6376494Abstract: This invention relates to compounds which have activity as 5-HT1A agonists and antagonists which may be useful for the treatment of anxiety, depression, cognitive deficits, and prostate cancer, having the formula wherein: X is a moiety selected from the group of: n is selected from the integers 1 through 5; R1 is optionally substituted aryl or mono or bicyclic heteroaryl, with a proviso that heteroaryl is not thiadiazole; R2 is H or alkyl; R3 is H, COR5, COOR5, and CONR5R6; R4 is H, alkyl, alkenyl, alkynyl, aryl, mono or bicyclic heteroaryl, aralkyl, and mono or bicyclic heteroaralkyl, wherein the aryl or heteroaryl groups are optionally substituted; R5 and R6 are H, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, adamantyl, and noradamantyl or R5 and R6 taken together may form a 5-7 membered azacyclic ring, optionally containing an additional heteroatom selected from O, S, or NR4; when R5 or R6 are chosen from cycloalkyl or cycloalkenyl, the cyclic group may optionallyType: GrantFiled: November 28, 2000Date of Patent: April 23, 2002Assignee: American Home Products CorporationInventors: Wayne E. Childers, Michael G. Kelly, Yvette L. Palmer, Edward J. Podlesny
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Patent number: 6369226Abstract: Nonpeptide benzamide-containing inhibitors of human rhinovirus (HRV) 3C protease are described.Type: GrantFiled: June 20, 2000Date of Patent: April 9, 2002Assignee: Agouron Pharmaceuticals, Inc.Inventors: Siegfried Heinz Reich, Susan Elizabeth Kephart, Michael Brennan Wallace, Theodore Otto Johnson, Jr.
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Patent number: 6344458Abstract: Compounds of the formula are useful for the treatment of disorder of the central nervous system including anxiety, depression, panic, alcohol and drug addiction, sexual dysfunction, sleep disorders, migraine, obesity, cognitive disorders, and neurodegenerative diseases.Type: GrantFiled: December 13, 1999Date of Patent: February 5, 2002Assignee: American Home Products CorporationInventors: Michael G. Kelly, Yvette L. Palmer
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Patent number: 6344456Abstract: The invention concerns compounds of formula (I) wherein R1, R2, R3, R4 and R5 are as defined herein. Said compounds are useful in therapy as antithrombotic agents.Type: GrantFiled: January 10, 2001Date of Patent: February 5, 2002Assignee: Laboratoire L. LafonInventors: Christophe Yue, Marguerite Henry, Thierry Giboulot, Brigitte Lesur
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Patent number: 6335337Abstract: Novel compounds which are inhibitors of the binding of fibrinogen to the Gp iib/iiia platelet receptors, and which can be used therapeutically as antithrombotic agents.Type: GrantFiled: January 9, 2001Date of Patent: January 1, 2002Assignee: Laboratoire L. LafonInventors: Christophe Yue, Marguerite Henry, Thierry Giboulot, Brigitte Lesur
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Patent number: 6323229Abstract: A compound of the formula wherein m, R1, R2, R3, R4, R5 and X are as defined, useful in treating or preventing migraine, depression and other disorders for which a 5-HT1 agonist or antagonist is indicated.Type: GrantFiled: April 14, 1999Date of Patent: November 27, 2001Assignee: Pfizer INCInventor: Harry R. Howard
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Patent number: 5125102Abstract: A digitally trunked radio repeater system provides substantial improvements in timeliness of channel acquisition and channel drop, and in reliability of critical control signalling. The system uses a much higher digital signalling rate than is typically found in prior art systems, and uses a control channel to convey digital channel request and assignment messages between the central site and mobile transceivers. The mobile radio transceivers transmit channel requests on the control channel (if no response is received, the mobile retries during a retry time window which increases in duration in dependence on the number of retries). The mobile transceiver switches to a working channel in response to an assignement message received on the control channel. Subaudible digital signals transmitted on the control channel and on active working channels allow late entry, shifting to higher priority calls, and other advanced functions.Type: GrantFiled: January 3, 1990Date of Patent: June 23, 1992Assignee: Ericsson GE Mobile Communications Inc.Inventors: Jeffrey S. Childress, Marc A. Dissosway, Gerald M. Cooper, Houston H. Hughes, III