Cyano Attached Indirectly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 546/330)
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Publication number: 20030032657Abstract: 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: 1Type: ApplicationFiled: April 16, 2002Publication date: February 13, 2003Applicant: Pharmacia CorporationInventors: David L. Brown, Matthew J. Graneto, Cindy L. Ludwig, John M. Molyneaux, John J. Talley
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Patent number: 6503933Abstract: Compounds of formula (I) and salts thereof as phytopathogenic fungicides wherein A1 is substituted 2-pyridyl; A2 is optionally substituted phenyl; L is —(C═O)—, —SO2— or —(C═S)—; R1 is hydrogen, optionally substituted alkyl or acyl; and R2 is hydrogen or optionally substituted alkyl are useful phytopathogenic fungicides.Type: GrantFiled: September 21, 2000Date of Patent: January 7, 2003Assignee: Aventis CropScience UK LimitedInventors: Brian Anthony Moloney, David Hardy, Elizabeth Anne Saville-Stones
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Publication number: 20020151571Abstract: The invention relates to novel cyclic imines of the formula (I) 1Type: ApplicationFiled: December 19, 2001Publication date: October 17, 2002Inventors: Andrew Plant, Gerd Kleefeld, Thorsten Potter, Christoph Erdelen, Norbert Mencke, Andreas Turberg, Ulrike Wachendorff-Neumann
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Publication number: 20020143188Abstract: The present invention describes novel nitrosated and/or nitrosylated potassium channel activators, and novel compositions comprising at least one nitrosated and/or nitrosylated potassium channel activator, and, optionally, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one vasoactive agent. The present invention also provides novel compositions comprising at least one potassium channel activator, and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one vasoactive agent.Type: ApplicationFiled: May 28, 2002Publication date: October 3, 2002Inventors: David S. Garvey, Inigo Saenz de Tejada
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Patent number: 6437122Abstract: A method for producing a heterocyclic nitrile in high yield by a gas-phase catalytic reaction of a heterocyclic carboxylic acid or an ester thereof with ammonia in the presence of a catalyst comprising an oxide of at least one element selected from copper and zinc, and an effective method for producing a heterocyclic aldehyde, using the heterocyclic nitrile thus obtained as a starting material, are provided.Type: GrantFiled: December 14, 2000Date of Patent: August 20, 2002Assignee: Koei Chemical Company, LimitedInventors: Takayuki Shoji, Mitsuhide Matsubara, Manabu Kimura, Yasuhiro Shiomi
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Patent number: 6417207Abstract: The present invention describes novel nitrosated and/or nitrosylated potassium channel activators, and novel compositions comprising at least one nitrosated and/or nitrosylated potassium channel activator, and, optionally, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one vasoactive agent. The present invention also provides novel compositions comprising at least one potassium channel activator, and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one vasoactive agent.Type: GrantFiled: May 12, 2000Date of Patent: July 9, 2002Assignee: NitroMed, Inc.Inventors: David S. Garvey, Inigo Saenz de Tejada
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Publication number: 20020087030Abstract: A process for preparing polymerizable biaryl derivatives comprises reacting an aromatic comprising a 6-membered ring which bears ester or benzylic OH groups in the 1,4 position with a second aromatic in a palladium-catalyzed cross-coupling reaction to give a biaryl and converting the ester or benzylic OH groups into polymerizable groups in one or more steps. The biaryls obtained are suitable for preparing polymers which are used as electroluminescence materials.Type: ApplicationFiled: October 16, 2001Publication date: July 4, 2002Inventors: Hubert Spreitzer, Willi Kreuder, Heinrich Becker, Jochen Krause
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Patent number: 6392050Abstract: The invention relates to a process for preparing substituted pyridines in a simple and cost-effective manner in good yields by reacting substituted 1,4-dihydropyridines with methyl nitrite in the presence of an acid that contains less than 20% by weight of oxidizing components.Type: GrantFiled: June 4, 2001Date of Patent: May 21, 2002Assignee: Bayer AktiengesellschaftInventors: Norbert Lui, Hans Panskus, Albert Schnatterer
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Publication number: 20020058804Abstract: The present invention provides a compound that includes an active therapeutic agent attached to a blocking moiety that is sensitive to the catalytic action of molecules having retro-aldol and retro-Michael catalytic activity, methods for making such compounds and methods of converting such compounds to active therapeutic agents using molecules having aldolase activity.Type: ApplicationFiled: June 18, 2001Publication date: May 16, 2002Applicant: The Scripps Research InstituteInventors: Carlos F. Barbas, Doron Shabat, Christoph Rader, Benjamin List, Richard A. Lerner
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Patent number: 6387934Abstract: 2-Cyano-3,5-dihydroxyhex-2-enecarboxamide derivatives are suitable for the production of pharmaceuticals for the prophylaxis and therapy of diseases or disorders whose course involves increased connective tissue or cartilage degradation.Type: GrantFiled: October 23, 2000Date of Patent: May 14, 2002Assignee: Aventis Pharma Deutschland GmbHInventors: Wilfried Schwab, Ruth Raiss
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Patent number: 6376671Abstract: 2-Sulfamoylbenzoic acid derivatives of general formula (I): which have both an antagonistic effect on the leukotriene D4 receptor and an antagonistic effect on the thromboxane A2 receptor and salts thereof, pharmaceuticals, anti-allergic agents and leukotriene-thromboxane A2 antagonistic agents containing them as an active ingredient.Type: GrantFiled: April 27, 2001Date of Patent: April 23, 2002Assignee: Kaken Pharmaceutical Co., Ltd.Inventors: Yoshihiro Ichikawa, Tokiko Nishida, Jun Nakano, Mitsuru Watanuki, Masahiro Suda, Tsutomu Nakamura
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Publication number: 20020019422Abstract: The present invention relates to novel cycloalkylalkanecarboxamides of the formula I 1Type: ApplicationFiled: May 31, 2001Publication date: February 14, 2002Inventors: Frank Wetterich, Karl Eicken, Gisela Lorenz, Eberhard Ammermann, Siegfried Strathmann, Ingo Rose
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Publication number: 20020016347Abstract: Heteroaryl aminobenzophenones of general formula I inhibit interleukin-1&bgr; and TNF-&agr; and may therefore be useful in the therapy of inflammatory diseases and conditions.Type: ApplicationFiled: May 21, 2001Publication date: February 7, 2002Inventor: Anne Marie Horneman
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Patent number: 6335446Abstract: The present invention relates to quinolinium- and pyridinium-based fluorescent dyes. The dyes are useful for staining proteins in solution, in gels and on solid supports. The dyes of the invention exhibit higher fluorescence emission than known compounds when bound to proteins and also exhibit improved contrast of fluorescence intensity between their protein-bound and unbound states.Type: GrantFiled: October 5, 1999Date of Patent: January 1, 2002Assignee: Oxford Glycosciences (UK) Ltd.Inventors: Mark William Pennington, David Ian Scopes, Michael Glen Orchard
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Patent number: 6335352Abstract: Novel compounds useful in the treatment of Interleukin-8 mediated diseases, and methods of using them are disclosed.Type: GrantFiled: February 4, 1999Date of Patent: January 1, 2002Assignee: SmithKline Beecham CorporationInventors: Deborah Lynn Bryan, John Gerald Gleason, Katherine L. Widdowson
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Publication number: 20010056107Abstract: Cyano and carboxy derivatives of substituted styrenes are inhibitors of tumor necrosis factor &agr;, nuclear factor &kgr;B, and phosphodiesterase and can be used to combat cachexia, endotoxic shock, retrovirus replication, asthma, and inflammatory conditions. A typical embodiment is 3,3-bis-(3,4-dimethoxyphenyl)acrylonitrile.Type: ApplicationFiled: July 16, 2001Publication date: December 27, 2001Inventors: George W. Muller, Mary Shire
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Patent number: 6303782Abstract: A process is described for preparing an aromatic compound substituted by a tertiary nitrile of Formula (1.0.0): comprising treating a substituted aromatic compound of Formula (2.0.0): with a secondary nitrile of Formula (3.0.0): in the presence of a base having a pKa numerical value in the range of from about 17 to about 30, provided that the difference in pKa numerical values between said base and the corresponding tertiary nitrile of Formula (3.0.0) is no more than about 6; in an aprotic solvent having a dielectric constant (∈) of less than about 20; and at a reaction temperature in the range of from about 0° C. to about 120° C.; whereby there is formed said tertiary-nitrile-substituted aromatic compound final product of Formula (1.0.0); wherein the constituent parts W1, W2, W3, W4, and W5; and the substituent moieties R1, R2, R3, R4, R5, R6, and R7 in the compounds of Formulas (1.0.0), (2.0.0) and (3.0.Type: GrantFiled: March 1, 2000Date of Patent: October 16, 2001Assignee: Pfizer IncInventor: Stéphane Caron
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Patent number: 6303641Abstract: Compounds of the following formula are used for inhibiting cell proliferation: wherein R, R1, Q, X are as defined in the specification.Type: GrantFiled: November 26, 1999Date of Patent: October 16, 2001Assignee: Leo Pharmaceuticals Products Ltd.Inventor: Erik Rytter Ottosen
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Patent number: 6291476Abstract: Pyrazole carboxamide derivatives of the formula: which are ligands for the neuropeptide Y, subtype 5 receptor, and pharmaceutical compositions containing a pyrazole carboxamide derivative as the active ingredient are described. The pyrazole carboxamides are useful in the treatment of disorders and diseases associated with the NPY receptor subtype Y5.Type: GrantFiled: May 2, 2000Date of Patent: September 18, 2001Assignee: Ortho-Mcneil Pharmaceutical, Inc.Inventors: Cheryl P. Kordik, Timothy W. Lovenberg, Allen B. Reitz
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Patent number: 6288071Abstract: Pesticidally active cyclohexadienyl derivative compounds of the formula I that are esters, oximes or amides are claimed. These compounds may be used as fungicides, acaricides and insecticides in plant protection.Type: GrantFiled: December 10, 1998Date of Patent: September 11, 2001Assignee: Bayer AktiengesellschaftInventors: Henry Szczepanski, Martin Zeller, Ottmar Franz Hüter
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Patent number: 6262263Abstract: The present invention relates to quinolinium- and pyridinium-based fluorescent dyes. The dyes are useful for staining proteins in solution, in gels and on solid supports. The dyes of the invention exhibit higher fluorescence emission than known compounds when bound to proteins and also exhibit improved contrast of fluorescence intensity between their protein-bound and unbound states.Type: GrantFiled: October 5, 1999Date of Patent: July 17, 2001Assignee: Oxford Glycosciences (UK) Ltd.Inventors: Mark William Pennington, David Ian Scopes, Michael Glen Orchard
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Patent number: 6242607Abstract: The invention relates to glutarimides of formula (I): in which Ar represents a phenyl non substituted or substituted one or more times with one of the substituents selected from a halogen atom, a hydroxyl, a (C1-C4)alkoxy, a trifluoromethyl, a (C1-C4)alkyl, said substituents being identical or different; a pyridyl group; a thienyl group and X is methylene or ethylene, their salts and their enantiomers, as well as their method of preparation and their use for the preparation of the corresponding 3,3-disubstituted piperidines.Type: GrantFiled: November 10, 1999Date of Patent: June 5, 2001Assignee: Sanofi-SynthelaboInventors: Philippe Camus, Marcel Descamps, Joël Radisson
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Patent number: 6187944Abstract: Acrylonitrile compounds having pesticidal activity of formula (I) and salts thereof. wherein Q is Y is ═C(R4)— or ═N—, R1 is alkyl, haloalkyl, etc., each of R2 and R3 is halogen, alkyl which may be substituted, alkenyl which may be substituted, etc., R4 is hydrogen, halogen, alkyl or haloalkyl, 1 is from 1 to 4, m is from 0 to 5, n is from 0 to 3, q is from 0 to 4, when 1 is 2 or more, a plurality of R2 may be the same or different, when each of m, n and q is 2 or more, a plurality of R3 may be the same or different.Type: GrantFiled: August 16, 1999Date of Patent: February 13, 2001Assignee: Ishihara Sangyo Kaisha Ltd.Inventors: Toru Koyanagi, Yuji Nakamura, Masayuki Morita, Koji Sugimoto, Tsuyoshi Ikeda, Munekazu Ogawa
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Patent number: 6147098Abstract: Guanidine and diaminonitroethene derivatives represented by the formula ##STR1## wherein X, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are defined in the description, compositions thereof and methods for preparing the compounds are described. The se compounds are useful in the treatment of diseases of the central nervous system, cardiovascular system, pulmonary system, gastrointestinal system and endocrinologic system.Type: GrantFiled: May 6, 1999Date of Patent: November 14, 2000Assignee: Novo Nordisk A/SInventors: John Patrick Mogensen, John Bondo Hansen, Tina Moller Tagmose
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Patent number: 6140353Abstract: N-(4-carbamimidophenylamino) phenylglycineamide derivative compounds having the formula: ##STR1## in which E, g.sup.1, g.sup.2, Q, R and X.sup.1 to X.sup.4 are each as defined in the description, and hydrates or solvates and physiologically acceptable salts thereof can be used as inhibitors of the formation of the coagulation factors Xa, IXa and thrombin induced by the factor VIIa and by the tissue factor. These compounds can be used as medicaments for the treatment and/or prevention of thromboses, apoplexy, cardiac infarction, inflammation and arteriosclerosis or as antitumor agents.Type: GrantFiled: December 2, 1998Date of Patent: October 31, 2000Assignee: Hoffmann-La Roche Inc.Inventors: Jean Ackermann, Katrin Grobke, Yu-Hua Ji, Sabine Wallbaum, Lutz Weber
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Patent number: 6140504Abstract: Compounds of the formula: ##STR1##Type: GrantFiled: February 4, 2000Date of Patent: October 31, 2000Assignee: Aventis Pharmaceuticals Products Inc.Inventors: Scott I. Klein, Kevin R. Guertin, Alfred P. Spada
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Patent number: 6066641Abstract: The present invention relates to novel compounds of the formula (I): ##STR1## wherein Q.sub.3 R.sub.3 and Q.sub.8 R.sub.8 are described herein. The compounds possess PDE-IV inhibitory activity and improved selectivity with regard to PDE-III inhibition. Also disclosed are pharmaceutical compositions and methods of treatment utilizing the disclosed compounds.Type: GrantFiled: June 11, 1997Date of Patent: May 23, 2000Assignee: Euro-Celtique S.A.Inventors: David Cavalla, Peter Hofer, Mark Chasin
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Patent number: 6034106Abstract: Oxadiazole substituted benzenesulfonamides are selective .beta..sub.3 adrenergic receptor agonists with very little .beta..sub.1 and .beta..sub.2 adrenergic receptor activity and as such the compounds are capable of increasing lipolysis and energy expenditure in cells. The compounds thus have potent activity in the treatment of Type II diabetes and obesity. The compounds can also be used to lower triglyceride levels and cholesterol levels or raise high density lipoprotein levels or to decrease gut motility. In addition, the compounds can be used to reduced neurogenic inflammation or as antidepressant agents. The compounds are prepared by coupling an aminoalkylphenyl-sulfonamide with an appropriately substituted epoxide. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for increasing gut motility are also disclosed.Type: GrantFiled: June 4, 1997Date of Patent: March 7, 2000Assignee: Merck & Co., Inc.Inventors: Tesfaye Biftu, Michael H. Fisher, Danqing Dennis Feng, Chan-Hwa Kuo, Gui-Bai Liang, Elizabeth M. Naylor, Ann E. Weber
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Patent number: 6028199Abstract: Hardeners for photographic materials, the binders of which substantially consist of gelatine, wherein the hardeners are carbamoylpyridinium salts, the amine components of which are derived from secondary amines, which amines are converted into photographically inert products by an intramolecular cyclisation reaction, improve photographic properties, even when the material is stored under extreme conditions.Type: GrantFiled: May 1, 1998Date of Patent: February 22, 2000Assignee: Agfa-Gevaert NVInventors: Erich Wolff, Peter Bergthaller
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Patent number: 6010980Abstract: Substituted 2-phenylpyridines I and their salts ##STR1## where n=0, 1;R.sup.1 =halogen, C.sub.1 -C.sub.4 -haloalkyl;R.sup.2 and R.sup.3 =H, halogen;R.sup.4 =CN, halogen;R.sup.5 =--CO--O-(C.sub.1 -C.sub.4 -alkylene)-CO--OR.sup.6, --CO--O-(C.sub.1 -C.sub.4 -alkylene)-CO--N(R.sup.7)R.sup.8, --O-(C.sub.1 -C.sub.4 -alkylene)-CO--O-(C.sub.1 -C.sub.4 -alkylene)-CO--OR.sup.6, --O-(C.sub.1 -C.sub.4 -alkylene)-CO--O-(C.sub.1 -C.sub.4 -alkylene)-CO--N(R.sup.7) R.sup.8, --S-(C.sub.1 -C.sub.4 -alkylene)-CO--O-(C.sub.1 -C.sub.4 -alkylene)-CO--OR.sup.6 or --S-(C.sub.1 -C.sub.4 -alkylene)-CO--O-(C.sub.1 -C.sub.4 -alkylene)-CO--N(R.sup.7)R.sup.8 ;R.sup.6 =H, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy-C.sub.1 -C.sub.4 -alkyl, C.sub.2 -C.sub.4 -alkenyl, C.sub.3 -C.sub.4 -alkynyl;R.sup.7 =H, C.sub.1 -C.sub.4 -alkyl, carboxy-C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxycarbonyl-C.sub.1 -C.sub.4 -alkyl;R.sup.8 =H or C.sub.1 -C.sub.4 -alkyl,are used as herbicides and for the desiccation/defoliation of plants.Type: GrantFiled: March 13, 1998Date of Patent: January 4, 2000Assignee: BASF AktiengesellschaftInventors: Peter Schafer, Gerhard Hamprecht, Elisabeth Heistracher, Olaf Menke, Cyrill Zagar, Michael Rack, Norbert Gotz, Albrecht Harreus, Karl-Otto Westphalen, Helmut Walter, Ulf Misslitz
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Patent number: 6008219Abstract: This invention relates to compounds of formula (I) ##STR1## which are useful as modulators of D.sub.3 receptors, in particular as antipsychotic agents.Type: GrantFiled: October 29, 1997Date of Patent: December 28, 1999Assignee: SmithKline Beech p.l.c.Inventors: Geoffrey Stemp, Christopher Norbert Johnson
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Patent number: 5994359Abstract: 2-Iminooxyphenylacetic acid derivatives ##STR1## where the substituents and the index have the following meanings: R.sup.1 is C(CO.sub.2 CH.sub.3).dbd.NOCH.sub.3 (Ia), C(CONHCH.sub.3).dbd.NOCH.sub.3 (Ib), C(CONH.sub.2).dbd.NOCH.sub.3 (Ic), C(CO.sub.2 CH.sub.3).dbd.CHOCH.sub.3 (Id) or C(CO.sub.2 CH.sub.3).dbd.CHCH.sub.3 (Ie);R.sup.2 is cyano, nitro, halogen, alkyl, haloalkyl or alkoxy;m is 0, 1 or 2;R.sup.3 is hydrogen, cyano, hydroxyl, halogen,alkyl, haloalkyl, alkoxyalkyl, alkoxy, haloalkoxy, alkylthio, cyclopropyl, alkenyl,unsubstituted or substituted aryloxyalkyl, benzyl or benzyloxy,R.sup.4 is hydrogen, cyano,unsubstituted or substituted alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl and hetaryl;unsubstituted or substituted alkoxy, alkenyloxy, alkynyloxy, cycloalkoxy, heterocyclyloxy, aryloxy and hetaryloxy;unsubstituted or substituted arylthio and hetarylthio;--Q--C(R.sup.5).dbd.N--Y.sup.1 --R.sup.6 or --Q--O--N.dbd.CR.sup.7 R.sup.8,R.sup.3 and R.sup.Type: GrantFiled: June 25, 1998Date of Patent: November 30, 1999Assignee: BASF AktiengesellschaftInventors: Thomas Grote, Hubert Sauter, Reinhard Kirstgen, Herbert Bayer, Ruth Muller, Bernd Muller, Klaus Oberdorf, Wassilios Grammenos, Norbert Gotz, Michael Rack, Albrecht Harreus, Franz Rohl, Eberhard Ammermann, Volker Harries, Gisela Lorenz, Siegfried Strathmann
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Patent number: 5968874Abstract: Substituted 2-phenylpyridines I ##STR1## where n is 0, 1;R.sup.1 is halogen, C.sub.1 -C.sub.6 -haloalkyl;R.sup.2 and R.sup.3 are H, halogen;R.sup.4 is cyano, halogen;X and Y are --O--, --S--;R.sup.5 and R.sup.6 are H, C.sub.1 -C.sub.4 -alkyl or together are a 1,2-ethylene, 1,3-propylene, 1,4-tetramethylene or 1,5-pentamethylene chain;R.sup.7 is C.sub.1 -C.sub.6 -haloalkyl, C.sub.3 -C.sub.6 -haloalkenyl, C.sub.2 -C.sub.6 -alkenyloxy-C.sub.1 -C.sub.4 -alkyl, C.sub.2 -C.sub.6 -alkenyloxy-C.sub.1 -C.sub.4 -alkoxy-C.sub.1 -C.sub.4 -alkyl, C.sub.3 -C.sub.6 -alkenyl, C.sub.3 -C.sub.6 -alkadienyl, C.sub.3 -C.sub.6 -alkynyl, C.sub.3 -C.sub.6 -cycloalkyl, C.sub.5 -C.sub.6 -cycloalkenyl, 3-oxetanyl, 3-thietanyl, phenyl, phenyl-C.sub.1 -C.sub.4 -alkyl or 5/6-membered heteroaryl having 1 to 3 hetero atoms selected from the group consisting of two oxygen atoms, two sulfur atoms and 3 nitrogen atoms, orR.sup.6 and R.sup.7 together are a 1,2-ethylene or 1,3-propylene chain which can have attached to it one or two C.sub.1 -C.Type: GrantFiled: January 20, 1998Date of Patent: October 19, 1999Assignee: BASF AktiengesellschaftInventors: Peter Schafer, Gerhard Hamprecht, Elisabeth Heistracher, Olaf Menke, Cyrill Zagar, Michael Rack, Norbert Gotz, Albrecht Harreus, Karl-Otto Westphalen, Helmut Walter, Ulf Misslitz
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Patent number: 5945436Abstract: Compounds of of the formula ##STR1## wherein R is a C.sub.6 -C.sub.10 aryl group, optionally substituted with one or more halogen atoms, phenoxy, or, linear or branched, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 haloalkoxy, or C.sub.1 -C.sub.6 haloalkyl; R.sup.1 is C.sub.3 -C.sub.6 cycloalkyl or, linear or branched, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.3 -C.sub.6 haloalkenyl, C.sub.2 -C.sub.8 alkoxyalkyl or C.sub.1 -C.sub.6 haloalkyl; n is 1, 2 or 3; and R.sup.2 is CN, C(O)NH.sub.2 or C(S)NH.sub.2, or the physiologically acceptable salts thereof with organic and inorganic acids. These compounds are useful as fungicides.Type: GrantFiled: September 26, 1997Date of Patent: August 31, 1999Assignees: Uniroyal Chemical Company, Inc., Uniroyal Chemical Co./Cie.Inventors: Hoi Kiong Lai, Douglas Irving Relyea, Robert Allan Davis
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Patent number: 5932736Abstract: Described are preferred processes for preparing heterocycles having one or more nitrogen and/or oxygen heteroatoms, utilizing a 1,3-dihalopropene as an effective 3-carbon fragment. Preferred processes yield pyridines, quinolines, oxazoles, pyrimidines and pyrazoles, depending upon the other reactant or reactants utilized with the 1,3-dihalopropene.Type: GrantFiled: April 7, 1998Date of Patent: August 3, 1999Assignee: Reilly Industries, Inc.Inventors: Ramiah Murugan, Eric F. V. Scriven
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Patent number: 5886186Abstract: The subject invention features substituted N-heteroaromatic compounds, libraries of substituted N-heteroaromatic compounds, and methods of synthesis thereof. For example, the present invention provides methods for synthesizing substituted N-heteroaromatic compounds, and is particularly amenable to the generation of libraries of substituted N- heteroaromatic compounds by combinatorial chemistry. The methods of the invention generally feature the reaction of O-linked heteroaromatic N-oxides with nucleophiles to produce substituted N-heteroaromatic compounds.Type: GrantFiled: October 25, 1995Date of Patent: March 23, 1999Assignee: Versicor, Inc.Inventors: Robert L. Smith, Gnanasambandam Kumaravel, Donald E. Kuhla
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Patent number: 5859034Abstract: Tri-substituted phenyl derivatives having the general formula (I): ##STR1## In a preferred embodiment, Y is preferably an --XR.sup.a group, X is preferably --O--, Z is preferably an --XR.sup.5 group, R.sup.a is preferably hydrogen or an optionally substituted alkyl group, R.sup.1 is preferably an --NHC(--NCN)NHR.sup.13 or --NHC(.dbd.CHNO.sub.2)NHR.sup.13 group, R.sup.2, R.sup.3 and R.sup.4 are preferably hydrogen, R.sup.5 is preferably an optionally substituted alkyl, alkenyl, cycloalkyl, cycloalkenyl or heterocycloalkyl group, R.sup.12 is preferably hydrogen or a C.sub.1-3 alkyl group, R.sup.13 is preferably hydrogen, a C.sub.1-3 alkyl group, an optionally substituted phenyl group or an optionally substituted phenylC.sub.1-3 alkyl group, Ar.sup.1 is preferably an optionally substituted nitrogen containing heteroaryl group, and Ar is preferably a phenyl group.Type: GrantFiled: December 3, 1997Date of Patent: January 12, 1999Assignee: Celltech Therapeutics, LimitedInventors: Graham John Warrellow, Julien Alistair Brown
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Patent number: 5849768Abstract: .alpha.-Unsaturated amines of the formula: ##STR1## wherein X.sup.1 and X.sup.2 are such that one is an electron-attracting group with the other being a hydrogen atom or an electron-attracting group; R.sup.1 is a group attached through a nitrogen atom; R.sup.2 is a hydrogen atom or a group attached through a carbon, nitrogen or oxygen atom; n is an integer equal to 0, 1 or 2; A is a heterocyclic group or a cyclic hydrocarbon group, and salts thereof and their agrochemical use as insecticidal and/or miticidal agents are described.Type: GrantFiled: July 28, 1988Date of Patent: December 15, 1998Assignee: Takeda Chemical Industries, Ltd.Inventors: Isao Minamida, Koichi Iwanaga, Tetsuo Okauchi
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Patent number: 5849771Abstract: Compounds of formula (I), wherein Ar, R.sub.1, R.sub.2, Y and R are as defined in claim 1, are effective as traps for free radicals.Type: GrantFiled: January 26, 1998Date of Patent: December 15, 1998Assignee: Centre National de la Recherche Scientifique (C.N.R.S.)Inventors: Abdelhamid Zeghdaoui, Jean-Pierre Finet, Beatrice Tuccio, Viviane Cerri, Paul Tordo
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Patent number: 5846907Abstract: Pyrazol-4-ylbenzoyl compounds of the formula I ##STR1## where Z is a 5- or 6-membered heterocyclic saturated or unsaturated radical, Q is a pyrazole ring and L and M are as defined in the specification, their use as herbicidal compounds and to processes for preparing the compounds.Type: GrantFiled: July 30, 1997Date of Patent: December 8, 1998Assignee: BASF AktiengesellschaftInventors: Wolfgang von Deyn, Regina Luise Hill, Uwe Kardorff, Stefan Engel, Martina Otten, Marcus Vossen, Peter Plath, Harald Rang, Albrecht Harreus, Hartmann Konig, Helmut Walter, Karl-Otto Westphalen, Ulf Misslizt
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Patent number: 5846906Abstract: Herbicidally active phenyldiketone compounds of the formula I ##STR1## in which the substituents have the following meanings: L and M are hydrogen, C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl, C.sub.2 -C.sub.6 -alkynyl, C.sub.1 -C.sub.4 -alkoxy, it being possible for these groups to be unsubstituted or substituted by one to five halogen atoms or C.sub.1 -C.sub.4 -alkoxy, or halogen, cyano, nitro, a group --(Y).sub.n --S(O).sub.m R.sup.7 or a group --(Y).sub.n --CO--R.sup.8,Z is a 5- or 6-membered heterocyclic saturated or unsaturated radical which has one to three hetero atoms selected from the group consisting of oxygen, sulfur or nitrogen and which is unsubstituted or substituted by halogen, cyano, nitro, a group --CO--R.sup.8, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl, C.sub.3 -C.sub.8 -cycloalkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -haloalkoxy, C.sub.1 -C.sub.4 -alkylthio, C.sub.1 -C.sub.4 -haloalkylthio, di-C.sub.1 -C.sub.Type: GrantFiled: July 30, 1997Date of Patent: December 8, 1998Assignee: BASF AktiengesellschaftInventors: Wolfgang von Deyn, Regina Luise Hill, Uwe Kardorff, Stefan Engel, Martina Otten, Marcus Vossen, Peter Plath, Harald Rang, Albrecht Harreus, Hartmann Konig, Helmut Walter, Karl-Otto Westphalen, Ulf Misslitz
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Patent number: 5840902Abstract: .beta.-Hydroxyalkylpicolinium salts of the formula (I) ##STR1## wherein A, R.sup.1 to R.sup.3 and X have the meanings given in the description, which are obtained by reaction of picolines of the formula (II) ##STR2## with alkylene oxides of the formula (III) in the presence of a 1- to 3-basic acid and in water or an organic solvent as the reaction medium and are used as intermediate products for the preparation of cationic dyestuffs, and dyestuff preparations comprising such cationic dyestuffs.Type: GrantFiled: November 20, 1996Date of Patent: November 24, 1998Assignee: Bayer AktiengesellschaftInventors: Karlheinrich Meisel, Klaus Walz, Gerd-Friedrich Renner, Hans Schulze, Carsten Gerdes, Karl-Rudolf Gassen, Reiner Ditzer, Lothar Klein
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Patent number: 5808082Abstract: A process for the preparation of Phosphodiesterase IV inhibitors is described. The process consists of eight chemical steps involving five isolations to prepare the title compound from readily available isovanillin in 35% overall yield (Scheme 1). The process is highlighted by: a) a highly diastereoselective Michael addition of phenyllithium using (1R, 2S) cis-aminoindanol as a chiral auxiliary, b) highly crystalline intermediates providing for efficient purifications, c) crystallization of the final compound as its CSA salt for excellent enantiomeric purity.Type: GrantFiled: April 22, 1997Date of Patent: September 15, 1998Assignee: Merck & Co., Inc.Inventors: Woo-Baeg Choi, Hywyn R. D. Churchill, Joseph E. Lynch, Paul J. Reider, Ralph P. Volante
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Patent number: 5789427Abstract: The present invention concerns compounds and their use to inhibit the activity of a receptor tyrosine kinase. The invention is preferably used to treat cell proliferative disorders such as cancers characterized by over-activity or inappropriate activity HER2 or EGFR.Type: GrantFiled: March 7, 1995Date of Patent: August 4, 1998Assignees: Sugen, Inc., Yissum Research & Development Company of the Hebrew University of JerusalemInventors: Hui Chen, Aviv Gazit, Klaus Peter Hirth, Elaina Mann, Laura K. Shawver, Jianming Tsai, Peng Cho Tang
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Patent number: 5783522Abstract: Substituted 2-phenylpyridines I ##STR1## R.sup.1,R.sup.3 =H, halogen, alkyl, haloalkyl, alkoxyalkyl, alkoxy, alkoxyalkoxy, OH, haloalkoxy, alkylcarbonyloxy, haloalkylcarbonyloxy, SH, alkylthio, alkylsulfinyl, alkylsulfonyl, haloalkylthio, haloalkylsulfinyl, haloalkylsulfonyl, CHO, CN, CO.sub.2 H, alkoxycarbonyl, alkoxyalkoxycarbonyl, haloalkoxycarbonyl, alkylcarbonyl, haloalkylcarbonyl, alkoxyalkylcarbonyl, CONH.sub.2, alkyl-aminocarbonyl, dialkylaminocarbonyl, pyrrolidinyl-carbonyl piperidylcarbonyl, morpholinylcarbonyl, NO.sub.2, NH.sub.2, alkylamino, dialkylamino, pyrrolidinyl, piperidinyl, morpholinyl, alkylcarbonylamino, haloalkylcarbonylamino, alkylsulfonylamino;R.sup.2 =halogen, CN, NO.sub.2, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio, haloalkylthio; orR.sup.1 +R.sup.2 or R.sup.2 +R.sup.3 =trimethylene or tetramethylene chain;R.sup.Type: GrantFiled: January 11, 1996Date of Patent: July 21, 1998Assignee: BASF AktiengesellschaftInventors: Peter Schaefer, Gerhard Hamprecht, Elisabeth Heistracher, Hartmann Koenig, Ralf Klintz, Peter Muenster, Harald Rang, Karl-Otto Westphalen, Matthias Gerber, Helmut Walter
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Patent number: 5767151Abstract: The present invention relates to novel 3,3-(disubstituted)-cyclohexan-1-ylidene acetate dimers of Formula (I): ##STR1## and related compounds, pharmaceutical compositions containing these compounds, and their use in treating allergic and inflammateory diseases and for inhibiting the production of Tumor Necrosis Factor (TNF).Type: GrantFiled: June 23, 1997Date of Patent: June 16, 1998Assignee: SmithKline Beecham CorporationInventors: Siegfried B. Christensen, IV, Joseph M. Karpinski
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Patent number: 5760063Abstract: The subject invention, provides arylhydrazone compounds having the Formula 1: ##STR1## wherein A and B are independently aryl or heteroaryl and A and B independently are substituted with at least one group selected from alkyl, halogen, CN, COOR.sup.7, NR.sup.7 R.sup.8, CONR.sup.7 R.sup.8, NO.sub.2, SR.sup.7, SOR.sup.7, SO.sub.2 R.sup.7, NHCOR.sup.7, NHSO.sub.2 R.sup.7, OR.sup.7, hydroxyalkyl, and aminoalkyl. The compounds of this invention are useful for treating a wide variety of bacterial infections, including diseases of the skin, e.g., acne and skin ulcers, gastroenteritis, colitis, meningitis, keratinitis, conjunctivitis, diseases of the urinary and genital tracts, etc.Type: GrantFiled: September 13, 1996Date of Patent: June 2, 1998Assignee: Scriptgen Pharmaceuticals, Inc.Inventors: Kelvin T. Lam, David G. Powers
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Patent number: 5728838Abstract: A process for the preparation of a compound of structural formula I ##STR1## wherein R.sup.1 is alkyl, alkenyl, phenyl or substituted phenyl, which comprises the addition of R.sup.1 to an intermediate 2: ##STR2## by treatment of 2 with (R.sup.1).sub.3 M followed by reductive removal of the sulfinyl group.Type: GrantFiled: April 2, 1997Date of Patent: March 17, 1998Assignee: Merck & Co., Inc.Inventors: Ioannis Houpis, Audrey Molina, Ralph P. Volante
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Patent number: 5726314Abstract: Novel quaternary pyridinium compounds useful in inhibiting acetylcholinesterase in mammals of the general structure: ##STR1## or pharmaceutically acceptable salts thereof, where R.sub.5 is pentafluorophenyl, phenyl monosubstituted with K, phenyl disubstituted with K, phenyl trisubstituted with K, or naphthyl; R.sub.6 is H, C.sub.1-6 alkyl, phenyl, pentafluorophenyl, phenyl mono, di, or trisubstituted with K, C.sub.1-6 alkyl with an attached phenyl group, C.sub.1-6 alkyl with an attached phenyl group mono, di, or trisubstituted with K; K is halogen, COOH, OH, CN, NO.sub.2, NH.sub.2, C.sub.1-6 alkyl, C.sub.1-6 fluorinated alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylamine, C.sub.1-6 alkyl--O--CO--, C.sub.1-6 alkyl--CO--NH--, C.sub.1-6 alkyl--NH--CO--NH--, C.sub.1-6 alkyl--NH--CO--O--, C.sub.1-6 alkyl--NH--CO--, or (C.sub.1-6 alkyl).sub.2 N--CO--; X is OH, C.sub.1-6 alkyl--NH--CO--O--, (C.sub.1-6 alkyl).sub.2 --N--CO--O--, C.sub.1-6 fluoroalkyl--NH--CO--, or (C.sub.1-6 fluoroalkyl).sub.Type: GrantFiled: September 30, 1996Date of Patent: March 10, 1998Assignee: Georgia Tech Research Corp.Inventors: James C. Powers, Jerry J. Buccafusco, Kenneth M. Starks
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Patent number: 5716971Abstract: Pyridine derivatives of the formula ##STR1## wherein the ring A stands for an optionally further substituted benzene ring; the ring B stands for an optionally substituted pyridine ring; Q stands for hydroxyl group, or OQ.sup.1 or Q.sup.1 wherein Q.sup.1 stands for an optionally substituted aliphatic hydrocarbon group; and n denotes 0 or 1, or their salts, which have potassium.channel opening activity and are useful as therapeutic agents of circulatory diseases such as angina pectoris, hypertension, etc.Type: GrantFiled: August 9, 1996Date of Patent: February 10, 1998Assignee: Takeda Chemical Industries, Ltd.Inventors: Mitsuru Shiraishi, Toshifumi Watanabe