Cyano Attached Indirectly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 546/330)
  • Publication number: 20030032657
    Abstract: 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: 1
    Type: Application
    Filed: April 16, 2002
    Publication date: February 13, 2003
    Applicant: Pharmacia Corporation
    Inventors: David L. Brown, Matthew J. Graneto, Cindy L. Ludwig, John M. Molyneaux, John J. Talley
  • Patent number: 6503933
    Abstract: 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: Grant
    Filed: September 21, 2000
    Date of Patent: January 7, 2003
    Assignee: Aventis CropScience UK Limited
    Inventors: Brian Anthony Moloney, David Hardy, Elizabeth Anne Saville-Stones
  • Publication number: 20020151571
    Abstract: The invention relates to novel cyclic imines of the formula (I) 1
    Type: Application
    Filed: December 19, 2001
    Publication date: October 17, 2002
    Inventors: Andrew Plant, Gerd Kleefeld, Thorsten Potter, Christoph Erdelen, Norbert Mencke, Andreas Turberg, Ulrike Wachendorff-Neumann
  • Publication number: 20020143188
    Abstract: 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: Application
    Filed: May 28, 2002
    Publication date: October 3, 2002
    Inventors: David S. Garvey, Inigo Saenz de Tejada
  • Patent number: 6437122
    Abstract: 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: Grant
    Filed: December 14, 2000
    Date of Patent: August 20, 2002
    Assignee: Koei Chemical Company, Limited
    Inventors: Takayuki Shoji, Mitsuhide Matsubara, Manabu Kimura, Yasuhiro Shiomi
  • Patent number: 6417207
    Abstract: 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: Grant
    Filed: May 12, 2000
    Date of Patent: July 9, 2002
    Assignee: NitroMed, Inc.
    Inventors: David S. Garvey, Inigo Saenz de Tejada
  • Publication number: 20020087030
    Abstract: 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: Application
    Filed: October 16, 2001
    Publication date: July 4, 2002
    Inventors: Hubert Spreitzer, Willi Kreuder, Heinrich Becker, Jochen Krause
  • Patent number: 6392050
    Abstract: 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: Grant
    Filed: June 4, 2001
    Date of Patent: May 21, 2002
    Assignee: Bayer Aktiengesellschaft
    Inventors: Norbert Lui, Hans Panskus, Albert Schnatterer
  • Publication number: 20020058804
    Abstract: 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: Application
    Filed: June 18, 2001
    Publication date: May 16, 2002
    Applicant: The Scripps Research Institute
    Inventors: Carlos F. Barbas, Doron Shabat, Christoph Rader, Benjamin List, Richard A. Lerner
  • Patent number: 6387934
    Abstract: 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: Grant
    Filed: October 23, 2000
    Date of Patent: May 14, 2002
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Wilfried Schwab, Ruth Raiss
  • Patent number: 6376671
    Abstract: 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: Grant
    Filed: April 27, 2001
    Date of Patent: April 23, 2002
    Assignee: Kaken Pharmaceutical Co., Ltd.
    Inventors: Yoshihiro Ichikawa, Tokiko Nishida, Jun Nakano, Mitsuru Watanuki, Masahiro Suda, Tsutomu Nakamura
  • Publication number: 20020019422
    Abstract: The present invention relates to novel cycloalkylalkanecarboxamides of the formula I 1
    Type: Application
    Filed: May 31, 2001
    Publication date: February 14, 2002
    Inventors: Frank Wetterich, Karl Eicken, Gisela Lorenz, Eberhard Ammermann, Siegfried Strathmann, Ingo Rose
  • Publication number: 20020016347
    Abstract: 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: Application
    Filed: May 21, 2001
    Publication date: February 7, 2002
    Inventor: Anne Marie Horneman
  • Patent number: 6335446
    Abstract: 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: Grant
    Filed: October 5, 1999
    Date of Patent: January 1, 2002
    Assignee: Oxford Glycosciences (UK) Ltd.
    Inventors: Mark William Pennington, David Ian Scopes, Michael Glen Orchard
  • Patent number: 6335352
    Abstract: Novel compounds useful in the treatment of Interleukin-8 mediated diseases, and methods of using them are disclosed.
    Type: Grant
    Filed: February 4, 1999
    Date of Patent: January 1, 2002
    Assignee: SmithKline Beecham Corporation
    Inventors: Deborah Lynn Bryan, John Gerald Gleason, Katherine L. Widdowson
  • Publication number: 20010056107
    Abstract: 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: Application
    Filed: July 16, 2001
    Publication date: December 27, 2001
    Inventors: George W. Muller, Mary Shire
  • Patent number: 6303782
    Abstract: 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: Grant
    Filed: March 1, 2000
    Date of Patent: October 16, 2001
    Assignee: Pfizer Inc
    Inventor: Stéphane Caron
  • Patent number: 6303641
    Abstract: Compounds of the following formula are used for inhibiting cell proliferation: wherein R, R1, Q, X are as defined in the specification.
    Type: Grant
    Filed: November 26, 1999
    Date of Patent: October 16, 2001
    Assignee: Leo Pharmaceuticals Products Ltd.
    Inventor: Erik Rytter Ottosen
  • Patent number: 6291476
    Abstract: 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: Grant
    Filed: May 2, 2000
    Date of Patent: September 18, 2001
    Assignee: Ortho-Mcneil Pharmaceutical, Inc.
    Inventors: Cheryl P. Kordik, Timothy W. Lovenberg, Allen B. Reitz
  • Patent number: 6288071
    Abstract: 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: Grant
    Filed: December 10, 1998
    Date of Patent: September 11, 2001
    Assignee: Bayer Aktiengesellschaft
    Inventors: Henry Szczepanski, Martin Zeller, Ottmar Franz Hüter
  • Patent number: 6262263
    Abstract: 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: Grant
    Filed: October 5, 1999
    Date of Patent: July 17, 2001
    Assignee: Oxford Glycosciences (UK) Ltd.
    Inventors: Mark William Pennington, David Ian Scopes, Michael Glen Orchard
  • Patent number: 6242607
    Abstract: 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: Grant
    Filed: November 10, 1999
    Date of Patent: June 5, 2001
    Assignee: Sanofi-Synthelabo
    Inventors: Philippe Camus, Marcel Descamps, Joël Radisson
  • Patent number: 6187944
    Abstract: 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: Grant
    Filed: August 16, 1999
    Date of Patent: February 13, 2001
    Assignee: Ishihara Sangyo Kaisha Ltd.
    Inventors: Toru Koyanagi, Yuji Nakamura, Masayuki Morita, Koji Sugimoto, Tsuyoshi Ikeda, Munekazu Ogawa
  • Patent number: 6147098
    Abstract: 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: Grant
    Filed: May 6, 1999
    Date of Patent: November 14, 2000
    Assignee: Novo Nordisk A/S
    Inventors: John Patrick Mogensen, John Bondo Hansen, Tina Moller Tagmose
  • Patent number: 6140353
    Abstract: 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: Grant
    Filed: December 2, 1998
    Date of Patent: October 31, 2000
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jean Ackermann, Katrin Grobke, Yu-Hua Ji, Sabine Wallbaum, Lutz Weber
  • Patent number: 6140504
    Abstract: Compounds of the formula: ##STR1##
    Type: Grant
    Filed: February 4, 2000
    Date of Patent: October 31, 2000
    Assignee: Aventis Pharmaceuticals Products Inc.
    Inventors: Scott I. Klein, Kevin R. Guertin, Alfred P. Spada
  • Patent number: 6066641
    Abstract: 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: Grant
    Filed: June 11, 1997
    Date of Patent: May 23, 2000
    Assignee: Euro-Celtique S.A.
    Inventors: David Cavalla, Peter Hofer, Mark Chasin
  • Patent number: 6034106
    Abstract: 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: Grant
    Filed: June 4, 1997
    Date of Patent: March 7, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Tesfaye Biftu, Michael H. Fisher, Danqing Dennis Feng, Chan-Hwa Kuo, Gui-Bai Liang, Elizabeth M. Naylor, Ann E. Weber
  • Patent number: 6028199
    Abstract: 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: Grant
    Filed: May 1, 1998
    Date of Patent: February 22, 2000
    Assignee: Agfa-Gevaert NV
    Inventors: Erich Wolff, Peter Bergthaller
  • Patent number: 6010980
    Abstract: 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: Grant
    Filed: March 13, 1998
    Date of Patent: January 4, 2000
    Assignee: BASF Aktiengesellschaft
    Inventors: Peter Schafer, Gerhard Hamprecht, Elisabeth Heistracher, Olaf Menke, Cyrill Zagar, Michael Rack, Norbert Gotz, Albrecht Harreus, Karl-Otto Westphalen, Helmut Walter, Ulf Misslitz
  • Patent number: 6008219
    Abstract: 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: Grant
    Filed: October 29, 1997
    Date of Patent: December 28, 1999
    Assignee: SmithKline Beech p.l.c.
    Inventors: Geoffrey Stemp, Christopher Norbert Johnson
  • Patent number: 5994359
    Abstract: 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: Grant
    Filed: June 25, 1998
    Date of Patent: November 30, 1999
    Assignee: BASF Aktiengesellschaft
    Inventors: 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
  • Patent number: 5968874
    Abstract: 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: Grant
    Filed: January 20, 1998
    Date of Patent: October 19, 1999
    Assignee: BASF Aktiengesellschaft
    Inventors: Peter Schafer, Gerhard Hamprecht, Elisabeth Heistracher, Olaf Menke, Cyrill Zagar, Michael Rack, Norbert Gotz, Albrecht Harreus, Karl-Otto Westphalen, Helmut Walter, Ulf Misslitz
  • Patent number: 5945436
    Abstract: 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: Grant
    Filed: September 26, 1997
    Date of Patent: August 31, 1999
    Assignees: Uniroyal Chemical Company, Inc., Uniroyal Chemical Co./Cie.
    Inventors: Hoi Kiong Lai, Douglas Irving Relyea, Robert Allan Davis
  • Patent number: 5932736
    Abstract: 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: Grant
    Filed: April 7, 1998
    Date of Patent: August 3, 1999
    Assignee: Reilly Industries, Inc.
    Inventors: Ramiah Murugan, Eric F. V. Scriven
  • Patent number: 5886186
    Abstract: 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: Grant
    Filed: October 25, 1995
    Date of Patent: March 23, 1999
    Assignee: Versicor, Inc.
    Inventors: Robert L. Smith, Gnanasambandam Kumaravel, Donald E. Kuhla
  • Patent number: 5859034
    Abstract: 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: Grant
    Filed: December 3, 1997
    Date of Patent: January 12, 1999
    Assignee: Celltech Therapeutics, Limited
    Inventors: Graham John Warrellow, Julien Alistair Brown
  • Patent number: 5849768
    Abstract: .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: Grant
    Filed: July 28, 1988
    Date of Patent: December 15, 1998
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Isao Minamida, Koichi Iwanaga, Tetsuo Okauchi
  • Patent number: 5849771
    Abstract: 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: Grant
    Filed: January 26, 1998
    Date of Patent: December 15, 1998
    Assignee: Centre National de la Recherche Scientifique (C.N.R.S.)
    Inventors: Abdelhamid Zeghdaoui, Jean-Pierre Finet, Beatrice Tuccio, Viviane Cerri, Paul Tordo
  • Patent number: 5846907
    Abstract: 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: Grant
    Filed: July 30, 1997
    Date of Patent: December 8, 1998
    Assignee: BASF Aktiengesellschaft
    Inventors: 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
  • Patent number: 5846906
    Abstract: 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: Grant
    Filed: July 30, 1997
    Date of Patent: December 8, 1998
    Assignee: BASF Aktiengesellschaft
    Inventors: 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
  • Patent number: 5840902
    Abstract: .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: Grant
    Filed: November 20, 1996
    Date of Patent: November 24, 1998
    Assignee: Bayer Aktiengesellschaft
    Inventors: Karlheinrich Meisel, Klaus Walz, Gerd-Friedrich Renner, Hans Schulze, Carsten Gerdes, Karl-Rudolf Gassen, Reiner Ditzer, Lothar Klein
  • Patent number: 5808082
    Abstract: 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: Grant
    Filed: April 22, 1997
    Date of Patent: September 15, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Woo-Baeg Choi, Hywyn R. D. Churchill, Joseph E. Lynch, Paul J. Reider, Ralph P. Volante
  • Patent number: 5789427
    Abstract: 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: Grant
    Filed: March 7, 1995
    Date of Patent: August 4, 1998
    Assignees: Sugen, Inc., Yissum Research & Development Company of the Hebrew University of Jerusalem
    Inventors: Hui Chen, Aviv Gazit, Klaus Peter Hirth, Elaina Mann, Laura K. Shawver, Jianming Tsai, Peng Cho Tang
  • Patent number: 5783522
    Abstract: 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: Grant
    Filed: January 11, 1996
    Date of Patent: July 21, 1998
    Assignee: BASF Aktiengesellschaft
    Inventors: Peter Schaefer, Gerhard Hamprecht, Elisabeth Heistracher, Hartmann Koenig, Ralf Klintz, Peter Muenster, Harald Rang, Karl-Otto Westphalen, Matthias Gerber, Helmut Walter
  • Patent number: 5767151
    Abstract: 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: Grant
    Filed: June 23, 1997
    Date of Patent: June 16, 1998
    Assignee: SmithKline Beecham Corporation
    Inventors: Siegfried B. Christensen, IV, Joseph M. Karpinski
  • Patent number: 5760063
    Abstract: 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: Grant
    Filed: September 13, 1996
    Date of Patent: June 2, 1998
    Assignee: Scriptgen Pharmaceuticals, Inc.
    Inventors: Kelvin T. Lam, David G. Powers
  • Patent number: 5728838
    Abstract: 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: Grant
    Filed: April 2, 1997
    Date of Patent: March 17, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Ioannis Houpis, Audrey Molina, Ralph P. Volante
  • Patent number: 5726314
    Abstract: 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: Grant
    Filed: September 30, 1996
    Date of Patent: March 10, 1998
    Assignee: Georgia Tech Research Corp.
    Inventors: James C. Powers, Jerry J. Buccafusco, Kenneth M. Starks
  • Patent number: 5716971
    Abstract: 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: Grant
    Filed: August 9, 1996
    Date of Patent: February 10, 1998
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Mitsuru Shiraishi, Toshifumi Watanabe