Plural Chalcogens Attached Directly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 546/155)
-
Patent number: 5399698Abstract: The novel quinolin-2-yl-methoxybenzylhydroxyureas can be prepared by reaction of appropriate ketones with hydroxylamine and reduction of the ketoximes and subsequent reaction with isocyanates. The new substances can be employed as active substances in medicaments.Type: GrantFiled: February 17, 1993Date of Patent: March 21, 1995Assignee: Bayer AktiengesellschaftInventors: Michael Matzke, Klaus-Helmut Mohrs, Siegfried Raddatz, Romanis Fruchtmann, Armin Hatzelmann, Christian Kohlsdorfer, Reiner Muller-Peddinghaus, Pia Theisen-Popp
-
Patent number: 5395937Abstract: A process that involves reacting a 3-nitroquinoline-2,4-disulfonate with an amine or a substituted amine to selectively aminate at the 4-position to yield 1H-imidazo[4,5-c]quinolin-4-amines is disclosed.Type: GrantFiled: January 29, 1993Date of Patent: March 7, 1995Assignee: Minnesota Mining and Manufacturing CompanyInventors: Nick Nikolaides, Kyle J. Lindstrom
-
Patent number: 5391747Abstract: A (quinolin-2-yl-methoxy) phenylacyl-sulphonamide or -cyanamide of the formula ##STR1## and physiologically acceptable salts thereof. The (quinolin-2-yl-methoxy)phenylacylsulphonamide or -cyanamide is useful as an active compound in medicaments, particularly as a lipoxygenase inhibitor.Type: GrantFiled: September 23, 1991Date of Patent: February 21, 1995Assignee: Bayer AktiengesellschaftInventors: Siegfried Raddatz, Klaus-Helmut Mohrs, Romanis Fruchtmann, Christian Kohlsdorfer, Pia Theisen-Popp, Reiner Muller-Peddinghaus
-
Patent number: 5391705Abstract: This invention relates to novel polyfluorinated alkyl derivatives of certain tripeptides, to the methods for their preparation, the intermediates therefore, to their use in inhibiting thrombin and lung tryptase and in their end-use application as anti-coagulants useful in treating thrombophlebitis and coronary thrombosis and in the treatment of asthma.Type: GrantFiled: February 18, 1994Date of Patent: February 21, 1995Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Bernhard Neises, Axel Ganzhorn, Celine Tarnus, Robert J. Broersma, Jr.
-
Patent number: 5387592Abstract: The invention concerns pharmaceutically useful compounds of the formula I, in which Q, X, Z and Ra have the various meanings defined herein, and their non-toxic salts, and pharmaceutical compositions containing them for treating conditions as hypertension and congestive heart failure.Type: GrantFiled: June 25, 1992Date of Patent: February 7, 1995Assignee: Imperial Chemical Industries PLCInventors: Robert H. Bradbury, Andrew P. Thomas
-
Patent number: 5384318Abstract: Compounds of the formula ##STR1## and pharmaceutical compositions comprising them, wherein R.sup.1, R.sup.2, R.sup.3, W, X and Z are as defined below. The compounds are inhibitors of 5-lipoxygenase enzyme and antagonists of leukotriene B4, leukotriene C4, leukotriene D4 and leukotriene E4.Type: GrantFiled: February 21, 1992Date of Patent: January 24, 1995Assignee: Pfizer Inc.Inventors: James F. Eggler, Anthony Marfat, Lawrence S. Melvin, Jr., Hiroko Masamune
-
Patent number: 5382572Abstract: Compounds useful as antiviral agents against DNA-containing viruses, such as herpes group viruses, are disclosed. The compounds are represented by Formula 1.0: ##STR1## and their pharmaceutically acceptable salts and solvates; wherein:(A) X is selected from the group consisting of N--R.sup.3, O, S, and C(R.sup.3).sub.2 ;(B) R.sup.3 is selected from H and a range of substituents;(C) R.sup.1 is an etherifying or esterifying group;(D) R.sup.2 is selected from a range of substituents;(E) m is 0 or an integer from 1 to 4; and(F) R.sup.4 and R.sup.5 are the same and are selected from alkyl and acyl groups;together with the pharmaceutically acceptable salts of the compounds of Formula 1.0 that are acidic or basic.Pharmaceutical compositions containing compounds represented by Formula 1.0 are disclosed. Also disclosed are methods of treating a viral infection using compounds represented by Formula 1.0.Type: GrantFiled: March 1, 1993Date of Patent: January 17, 1995Assignee: Schering CorporationInventors: Adriano Afonso, Jay Weinstein, Margaret J. Gentles
-
Patent number: 5380850Abstract: Compounds having the formula I: ##STR1## are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating diarrhea, hypertension, angina, platelet aggregation, cerebral spasm, premature labor, spontaneous abortion, dysmenorrhea, and migraine.Type: GrantFiled: December 16, 1993Date of Patent: January 10, 1995Assignee: Merck Frosst Canada, Inc.Inventors: Petpiboon Prasit, Rejean Fortin, John H. Hutchinson, Michel L. Belley, Serge Leger, Richard Frenette, John Gillard
-
Patent number: 5378699Abstract: Methods of treating an immune disease, cell proliferation, restenosis and vascular smooth muscle cells using the pharmaceutical compounds of the formula ##STR1## in which R.sup.2 is phenyl, naphthyl or heteroaryl selected from thienyl, pyridyl, benzothienyl, quinolinyl, benzofuranyl or benzimidazolyl, said phenyl, naphthyl and heteroaryl groups being optionally substituted, or R.sup.2 is furanyl optionally substituted with C.sub.1-4 alkyl; and salts thereof.Type: GrantFiled: February 5, 1993Date of Patent: January 3, 1995Assignees: Lilly Industries Limited, Eli Lilly and CompanyInventors: Michael Brunavs, Colin P. Dell, Peter T. Gallagher, William M. Owton, Jai P. Singh, Colin W. Smith
-
Patent number: 5378694Abstract: Compounds useful as antiviral agents against DNA-containing viruses, such as herpes group viruses, are disclosed. The compounds are are represented by compounds of Formula 1.0: ##STR1## and their pharmaceutically acceptable salts and solvates. Pharmaceutical compositions containing compounds represented by Formula 1.0 and methods of treating a viral infection using compounds represented by Formula 1.0 are disclosed.Also disclosed are compounds useful as antihypertensive agents and methods of treating hypertension using such compounds. The antihypertensive agents are compounds represented by Formula 1.0 wherein R.sup.4 is selected from the group consisting of alkyl and aminoalkyl. Preferably R.sup.1 is H.Type: GrantFiled: March 1, 1993Date of Patent: January 3, 1995Assignee: Schering CorporationInventors: Adriano Afonso, Jay Weinstein, Margaret J. Gentles, Stuart B. Rosenblum
-
Patent number: 5376748Abstract: A class of optionally 4-substituted 3-nitro-2-oxo-1,2,3,4-tetrahydroquinoline derivatives are selective non-competitive antagonists of NMDA receptors and/or are antagonists of AMPA receptors, and are therefore of utility in the treatment of conditions, such as neurodegenerative disorders, convulsions or schizophrenia, which require the administration of an NMDA and/or AMPA receptor antagonist.Type: GrantFiled: January 7, 1993Date of Patent: December 27, 1994Assignee: Merck Sharp & Dohme LimitedInventors: William R. Carling, Julian D. Smith, Paul D. Leeson
-
Patent number: 5374721Abstract: There are disclosed certain novel compounds identified as benzo-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. Growth promoting compositions containing such benzo-fused lactams as the active ingredient thereof are also disclosed.Type: GrantFiled: October 14, 1992Date of Patent: December 20, 1994Assignee: Merck & Co., Inc.Inventors: William R. Schoen, Matthew J. Wyvratt
-
Patent number: 5352687Abstract: Substituted phenylacetamides can be prepared by reaction of appropriately substituted phenylacetic acids with imidazoles and subsequent amidation. The substituted phenylacetic acid derivatives can be employed in medicaments for the treatment of high blood pressure and atherosclerosis.Type: GrantFiled: March 3, 1993Date of Patent: October 4, 1994Assignee: Bayer AktiengesellschaftInventors: Ulrich E. Muller, Matthias Muller-Gliemann, Jurgen Dressel, Peter Fey, Rudolf Hanko, Walter Hubsch, Thomas Kramer, Martin Beuck, Stanislav Kazda, Stefan Wohlfeil, Ozkan Yalkinoglu, Andreas Knorr, Johannes-Peter Stasch
-
Patent number: 5348962Abstract: This present invention relates to a class of 4-hydroxy-2-(1H)-quinolones which are substituted in the 3-position by an optionally substituted aryl substituent. These compounds are selective non-competitive antagonists of N-methyl-D-aspartate (NMDA) receptors.Type: GrantFiled: November 18, 1993Date of Patent: September 20, 1994Assignee: Merck Sharpe & Dohme Ltd.Inventors: Janusz J. Kulagowski, Ian M. Mawer, Paul D. Leeson, Michael Rowley
-
Patent number: 5326770Abstract: This invention relates to monoamine oxidase-B (MAO-B) inhibitory 5-substituted 2,4-thiazolidinediones, such as Formula I, to pharmaceutical compositions thereof, process of preparation, and methods of use in mammals to treat cognitive disorders, neurological dysfunction, and/or mood disturbances such as, but not limited to degenerative nervous system diseases.Type: GrantFiled: July 17, 1992Date of Patent: July 5, 1994Assignee: The Du Pont Merck Pharmaceutical CompanyInventor: Wendell W. Wilkerson
-
Patent number: 5326766Abstract: Compounds of the formula (I): ##STR1## wherein: Het is pyridyl, pyrazinyl, pyrimidinyl, or pyridizinyl, optionally substituted with one or more groups selected from halo, lower alkyl, lower alkoxy, haloalkyl, haloalkoxy, NO.sub.2, CN, and lower alkoxy-carbonyl;Z is a C--C single bond, CH.sub.2, NH, O, S, --CH.sub.2 O--, or --OCH.sub.2 --; andthe remaining groups are as defined in the specification are useful as pesticides.Type: GrantFiled: August 19, 1992Date of Patent: July 5, 1994Inventors: Barry A. Dreikorn, Sylvester V. Kaster, Neil V. Kirby, Robert G. Suhr, Brian R. Thoreen
-
Patent number: 5318971Abstract: Novel 3-substituted-1-aryl-2(1H)-quinolones useful as anti-allergy, anti-inflammatory, anti-hyperproliferative skin disease agents are disclosed. The quinolones are represented by Formula 1: ##STR1## Pharmaceutical compositions and methods of treatment employing such compounds are also disclosed.Type: GrantFiled: July 19, 1991Date of Patent: June 7, 1994Assignee: Schering CorporationInventor: Stuart W. McCombie
-
Patent number: 5312922Abstract: Fluorogenic chelators for Eu.sup.3+ and Tb.sup.3+ are provided, they form highly fluorescent complexes with Eu.sup.3+ and Tb.sup.3+. In all cases, the fluorescence observed was lanthanide-specific, long-lived and it was monitored by microsecond time-resolved fluorometry. The fluorogenic chelators could be quantified, in the presence of excess lanthanide, at levels <10.sup.-8 mol/L. Two new fluorogenic chelators can form ternary complexes with Eu.sup.3+ and Tb.sup.3+, in the presence of EDTA. The structures of the identified chelators is such that enzyme substrates can be used for enzyme-labelled time-resolved fluorometric immunoassays. The chelator 4-methylumbelliferyl phosphate which forms fluorescent, long-lived complexes with Eu.sup.3+, can be split by alkaline phosphatase to phosphate and 4-methylumbelli-ferone which does not form fluorescent complexes with Eu.sup.3+. Highly sensitive immunoassays for thyrotropin and thyroxine in human serum are demonstrated.Type: GrantFiled: April 6, 1992Date of Patent: May 17, 1994Assignee: Nordion International Inc.Inventor: Eleftherios P. Diamandis
-
Patent number: 5310744Abstract: Quinolylmethoxyphenyl-acetamides of the formula: ##STR1## in which A, B, D, E, G, L and M are hydrogen, hydroxyl, halogen, cyano, carboxyl, nitro, trifluoromethyl, trifluoromethoxy, alkyl, alkoxy or optionally substituted aryl;R.sub.1 represents optionally substituted cycloalkyl; andR.sub.2 and R.sub.3 independently represent hydrogen, alkyl, benzyl, or optionally substituted cycloalkyl; or together represent piperidinyl, morpholino, or piperazinyl;show a high in vitro activity as leukotriene synthesis inhibitors and, therefore, are suitable for the treatment and prevention of inflammations.Type: GrantFiled: November 23, 1992Date of Patent: May 10, 1994Assignee: Bayer AktiengesellschaftInventors: Siegfried Raddatz, Klaus-Helmut Mohrs, Michael Matzke, Romanis Fruchtmann, Armin Hatzelmann, Reiner Muller-Peddinghaus
-
Patent number: 5310743Abstract: 1-Acylpiperidine compound of the formula I ##STR1## in which R.sub.1 is an optionally substituted aralkyl, aryloxyalkyl, heteroaralkyl, aroyl, heteroaroyl, cycloalkylcarbonyl, aralkanoyl, heteroarylalkanoyl, aralkoxycarbonyl or arylcarbamoyl radical or the acyl radical of an .alpha.-amino acid which is optionally N-substituted by lower alkanoyl or carbamoyl-lower-alkanoyl, R.sub.2 is cycloalkyl or an optionally substituted aryl or heteroaryl radical, R.sub.3 is hydrogen, alkyl, carbamoyl or an alkanoyl or alkenoyl radical which is optionally substituted by carboxyl or esterified or amidated carboxyl, R.sub.4 is an optionally substituted aryl or optionally partially hydrogenated heteroaryl radical, X.sub.1 is methylene, ethylene, a direct linkage, an optionally ketalised carbonyl group or an optionally etherified hydroxymethylene group, X.sub.2 is alkylene, carbonyl or a direct linkage, and X.sub.Type: GrantFiled: August 11, 1992Date of Patent: May 10, 1994Assignee: Ciba-Geigy Corp.Inventors: Walter Schilling, Silvio Ofner, Siem J. Veenstra
-
Patent number: 5310913Abstract: Compounds having formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 are selected from the group consisting of hydrogen, hydroxy and methoxy. At most one of R.sup.1, R.sup.2 and R.sup.3 and at most one of R.sup.4, R.sup.5, R.sup.6 and R.sup.7 is selected from the group consisting of hydroxy and methoxy. M is selected from the group consisting of hydrogen and pharmaceutically acceptable inorganic or organic cations or tautomeric forms thereof. The compounds have immunomodulating activity.Type: GrantFiled: August 5, 1993Date of Patent: May 10, 1994Assignee: Kabi Pharmacia AktiebolagInventors: Per O. Gunnarsson, Torbjorn Stalhandske, Kerstin Strandgarden, Karl-Erik Lundvall, Kaj Johansson
-
Patent number: 5306820Abstract: (Quinolin-2-yl-methoxy)phenylacetic acids are known as inhibitors of enzymatic reactions in the context of arachidonic acid metabolism.Enantiomerically pure (quinolin-2-yl-methoxy)phenylacetic acids can be prepared in a simple manner and in high purity and yield by diastereoselective alkylation of corresponding (quinolin-2-yl-methoxy)phenylacetic acid menthyl esters and subsequent specific removal of the ester radical with acids.Type: GrantFiled: April 10, 1992Date of Patent: April 26, 1994Assignee: Bayer AktiengesellschaftInventors: Matthias Decker, Klaus-Helmut Mohrs, Siegfried Raddatz
-
Patent number: 5298511Abstract: The invention concerns alkanoic acid derivatives of the formula I ##STR1## wherein Ar.sup.1 is optionally-substituted phenyl or naphthyl, or a 10-membered bicyclic heterocyclic moiety containing one or two nitrogen heteroatoms and optionally containing a further heteroatom selected from nitrogen, oxygen and sulphur;A.sup.1 is a direct link to X.sup.1 or is (1-3 C)alkylene;X.sup.1 is oxy, thio, sulphinyl or sulphonyl;n is 0, 1 or 2 and R.sup.1 is halogeno, (1-4 C)alkyl, (1-4 C)alkoxy or fluoro-(1-4 C)alkyl;each of R.sup.2 and R.sup.3 is (1-4 C)alkyl, (2-4 C)alkenyl or (2-4 C)alkynyl; andR.sup.4 is hydrogen or (1-4 C)alkyl;or a pharmaceutically-acceptable salt thereof;processes for their manufacture; pharmaceutical compositions containing them and their use as 5-lipoxygenase inhibitors.Type: GrantFiled: September 23, 1992Date of Patent: March 29, 1994Assignees: Imperial Chemical Industries PLC, I.C.I. PharmaInventor: David Waterson
-
Patent number: 5288811Abstract: Accordingly, novel carbonyl containing compositions are prepared by contacting, in the presence of a free radical initiator, a compound selected from the group consisting of saturated hydrocarbons, substituted saturated hydrocarbons, polymers and mixtures thereof with a carbonyl containing compound or mixtures thereof having the structures: ##STR1## wherein Q.dbd.HOH, MeOH, EtOH, or n-BuOH; n.dbd.0,1,>; and X and Y are independently selected from the group consisting of CH.sub.2, C.dbd.O; W is independently selected from the group consisting of CH.sub.2, C.dbd.O, O, NH, CMe.sub.2, C.dbd.N-alkyl and N-alkyl, wherein alkyl is 1 to 18 carbons; U and V are independently selected from the same groups as W and dependently selected so that U and V taken together are one of 1,2-phenylene, 1,8-naphthalene-diyl, and 1,2-naphthalene-diyl.Type: GrantFiled: November 5, 1992Date of Patent: February 22, 1994Assignee: Exxon Research and Engineering CompanyInventor: Stanley J. Brois
-
Patent number: 5283245Abstract: The invention concerns a thiazole of the formula I, ##STR1## wherein Q.sup.1 is an optionally substituted 6-membered monocyclic or 10-membered bicyclic heterocyclic moiety containing one or two nitrogen atoms;X is oxy, thio, sulphinyl, sulphonyl or imino;Ar is phenylene which may optionally bear one or two substituents, or Ar is an optionally substituted 6-membered heterocyclene moiety contining up to three nitrogen atoms;R.sup.1 is hydrogen, (1-6C)alkyl, (2-6C)alkenyl, (2-6C)alkynyl or substituted (1-4C)alkyl;R.sup.2 is hydrogen, (1-6C)alkyl, (3-6C)alkenyl, (3-6C)alkynyl or substituted (1-4C)alkyl or R.sup.2 is optionally substituted benzoyl; andQ.sup.2 is optionally substituted thiazolyl;or a pharmaceutically-acceptable salt thereof.The invention also concerns processes for the manufacture of a thiazole of the formula I and pharmaceutical compositions containing said thiazole.Type: GrantFiled: November 18, 1991Date of Patent: February 1, 1994Assignees: Imperial Chemical Industries PLC, ICI PharmaInventors: Graham C. Crawley, Martin P. Edwards
-
Patent number: 5268380Abstract: (1H-azol-1-ylmethyl)substituted quinoline derivatives, compositions containing the same, and methods of treating mammals suffering from disorders which are characterized by an increased proliferation and/or abnormal differentiation of epithelial tissues.Type: GrantFiled: November 10, 1992Date of Patent: December 7, 1993Assignee: Janssen Pharmaceutica N.V.Inventors: Gerard C. Sanz, Marc G. Venet, Eddy J. E. Freyne, Alfons H. M. Raeymakers
-
Patent number: 5268378Abstract: A class of 2,4-dioxo-1,2,3,4-tetrahydroquinoline derivatives, substituted at the 3-position by a range of carbonyl-containing substituents or by a five- or six-membered heteroaromatic moiety, are selective non-competitive antagonists of NMDA receptors and/or are antagonists of AMPA receptors, and are therefore of utility in the treatment of conditions, such as neurodegenerative disorders, convulsions or schizophrenia, which require the administration of an NMDA and/or AMPA antagonist.Type: GrantFiled: January 22, 1992Date of Patent: December 7, 1993Assignee: Merck Sharp & Dohme, LimitedInventors: Raymond Baker, Paul D. Leeson, Michael Rowley, Graeme I. Sevenson
-
Patent number: 5266578Abstract: Heterocyclically substituted quinolylmethoxyphenylacetamides are prepared by amidation of corresponding carboxylic acids. The compounds can be used in medicaments, in particular those having lipoxygenase-inhibiting action.Type: GrantFiled: August 26, 1992Date of Patent: November 30, 1993Assignee: Bayer AktiengesellschaftInventors: Siegfried Raddatz, Klaus-Helmut Mohrs, Michael Matzke, Romanis Fruchtmann, Armin Hatzelmann, Christian Kohlsdorfer, Reiner Muller-Peddinghaus, Pia Theisen-Popp
-
Patent number: 5252584Abstract: A class of 4-hydroxy-2(1H)-quinolone derivatives, substituted at the 3-position by an N-linked heteroaromatic ring system, are selective non-competitive antagonists of NMDA receptors and/or are antagonists of AMPA receptors, and are therefore of utility in the treatment of conditions, such as neurodegenerative disorders, convulsions or schizophrenia, which require the administration of an NMDA and or AMPA receptor antagonist.Type: GrantFiled: December 3, 1991Date of Patent: October 12, 1993Assignee: Merck Sharp & Dohme LimitedInventors: William R. Carling, Paul D. Leeson, Kevin W. Moore
-
Patent number: 5242931Abstract: Novel Tricyclic compound represented by formula ##STR1## possess a TXA.sub.2 biosynthesis inhibiting act and/or a TXA.sub.2 receptor antagonizing activity, and are expected to have preventive and therapeutic effects on ischemic diseases, cerebro-vascular diseases, etc.Type: GrantFiled: March 23, 1992Date of Patent: September 7, 1993Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Etsuo Oshima, Hiroyuki Obase, Akira Karasawa, Kazuhiro Kubo, Ichiro Miki, Akio Ishii
-
Patent number: 5240941Abstract: The invention concerns a thioxo heterocycle of the formula I ##STR1## wherein Q is a 10-membered bicyclic heterocyclic moiety containing 1 or 2 N's which bears 1 or 2 thioxo substituents and which is optionally further substituted;A.sup.1 is a direct link to X.sup.1 or (1-3C)alkylene;X.sup.1 is oxy, thio, sulphinyl, sulphonyl or imino;Ar is optionally substituted phenylene or pyridylene;R.sup.1 is (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl; andR.sup.2 and R.sup.3 together form a group of the formula --A.sup.2 --X.sup.2 --A.sup.3 -- which, together with the carbon atom to which A.sup.2 and A.sup.3 are attached, defines a ring having 5 to 7 ring atoms, wherein each of A.sup.2 and A.sup.3 is (1-3C)alkylene and X.sup.2 is oxy, thio, sulphinyl or sulphonyl;or a pharmaceutically-acceptable salt thereof.The compounds of the invention are inhibitors of the enzyme 5-lipoxygenase.Type: GrantFiled: July 11, 1991Date of Patent: August 31, 1993Assignees: ICI Pharma, Imperial Chemical Industries PLCInventor: Pierre A. R. Bruneau
-
Patent number: 5231103Abstract: The novel quinolin-2-yl-methoxybenzylhydroxyureas can be prepared by reaction of appropriate ketones with hydroxylamine and reduction of the ketoximes and subsequent reaction with isocyanates. The new substances can be employed as active substances in medicaments.Type: GrantFiled: July 21, 1992Date of Patent: July 27, 1993Assignee: Bayer AktiengesellschaftInventors: Michael Matzke, Klaus-Helmut Mohrs, Siegfried Raddatz, Romanis Fruchtmann, Armin Hatzelmann, Christian Kohlsdorfer, Reiner Muller-Peddinghaus, Pia Theisen-Popp
-
Patent number: 5221678Abstract: Compounds having the Formula I: ##STR1## are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating diarrhea, hypertension, angina, platelet aggregation, cerebral spasm, premature labor, spontaneous abortion, dysmenorrhea, and migraine.Type: GrantFiled: July 12, 1991Date of Patent: June 22, 1993Assignee: Merck Frosst Canada, Inc.Inventors: Joseph G. Atkinson, John W. Gillard, Erich L. Grimm
-
Patent number: 5221677Abstract: The invention concerns a heterocyclic derivative of the formula I ##STR1## wherein Q is an optionally substituted 6-membered monocyclic or 10-membered bicyclic heterocyclic moiety containing one or two nitrogen atoms;X.sup.1 is oxy, thio, sulphinyl, sulphonyl or imino;Ar is phenylene which may optionally bear one or two substituents or Ar is an optionally substituted 6-membered heterocyclene moiety containing up to three nitrogen atoms;R.sup.1 is (1-6C)alkyl, (3-6C)alkenyl or (3-6C)alkynyl; andR.sup.2 and R.sup.3 together form a group of the formula --A.sup.2 --X.sup.2 --A.sup.3 -- which, together with the carbon atom to which A.sup.2 and A.sup.3 are attached, defines a ring having 4 to 7 ring atoms, wherein A.sup.2 and A.sup.3, which may be the same or different, each is (1-4C)alkylene and X.sup.2 is oxy, thio, sulphinyl, sulphonyl or imino;or a pharmaceutically-acceptable salt thereof.The compounds of the invention are inhibitors of the enzyme 5-lipoxygenase.Type: GrantFiled: September 21, 1990Date of Patent: June 22, 1993Assignees: Imperial Chemical Industries PLC, ICI PharmaInventors: Graham C. Crawley, Philip N. Edwards
-
Patent number: 5220000Abstract: Novel bifunctional bis-quinolinols are provided as well as their chelates and processes for their production. The quinolinols can be attached to organic substrates before or after chelation and are useful for diagnostic and therapeutic purposes.Type: GrantFiled: January 23, 1992Date of Patent: June 15, 1993Inventor: Spyros Theodoropulos
-
Patent number: 5217982Abstract: This invention relates to compounds which are derivatives of cyclopentane which are useful as antihypertensive agents, to pharmaceutical compositions including such compounds, and to their use in treating hypertension.Type: GrantFiled: November 15, 1990Date of Patent: June 8, 1993Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.Inventors: Cynthia A. Fink, Alfred P. Spada
-
Patent number: 5215998Abstract: Compounds and compositions containing alkylphosphonothioates, for insecticidal control, particularly for use as soil and/or foliar insecticides, having the formula. ##STR1## in which R is C.sub.1 -C.sub.3 alkyl;R.sub.1 is C.sub.4 -C.sub.6 branched alkyl;R.sub.2 is hydrogen, methyl, ethyl, cyano or C.sub.2 -C.sub.4 alkynyl; ##STR2## R.sub.4 is halo, C.sub.1 -C.sub.2 haloalkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 thioalkyl or mono-or di-C.sub.1 -C.sub.2 alkylamino;n is 1-3; andX is O or S.Type: GrantFiled: December 18, 1990Date of Patent: June 1, 1993Assignee: Imperial Chemical Industries PLCInventors: David B. Kanne, Charles G. Chavdarian
-
Patent number: 5204344Abstract: Compounds having the formula I: ##STR1## are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating diarrhea, hypertension, angina, platelet aggregation, cerebral spasm, premature labor, spontaneous abortion, dysmenorrhea, and migraine.Type: GrantFiled: February 5, 1991Date of Patent: April 20, 1993Assignee: Merck Frosst Canada, Inc.Inventors: Petpiboon Prasit, Rejean Fortin, John H. Hutchinson, Michel L. Belley, Serge Leger, John Gillard, Richard Frenette
-
Patent number: 5204374Abstract: New cycloalkano[b]dihydroindoles and -indolesulphonamides, substituted by heterocycles, of the formula (I) ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are identical or different andrepresent hydrogen, nitro, cyano, halogen, trifluoromethyl, carboxyl, hydroxyl or trifluoromethoxy, orrepresent a group of the formula --S(O).sub.w R.sup.5, in whichR.sup.5 denotes alkyl or optionally substituted aryl,w denotes the number 0, 1 or 2, orrepresents alkoxy or alkoxycarbonyl, or benzyloxy, orrepresents a group of the formula --NR.sup.6 R.sup.7, in whichR.sup.6 and R.sup.7 are identical or different anddenote hydrogen, alkyl or acyl ordenote aryl, ordenote a group of the formula --S(O).sub.w R.sup.5, in which R.sup.Type: GrantFiled: April 3, 1991Date of Patent: April 20, 1993Assignee: Bayer AktiengesellschaftInventors: Ulrich E. Muller, Ulrich Rosentreter, Ulrich Niewohner, Elisabeth Perzborn, Erwin Bischoff, Hans-Georg Dellweg, Peter Norman, Nigel J. Cuthbert, Hilary P. Francis
-
Patent number: 5194439Abstract: Pyridine derivatives of formula ##STR1## their heteroaromatic N-oxides and their pharmaceutically acceptable acid addition salts are disclosed. In the formula z is 0, 1 and 2; R is hydrogen, hydroxy, lower alkyl, lower alkoxy, halogen, trifluoromethyl, nitro, amino, (lower)alkylamino or di(lower)alkylamino; R.sup.1 is hydrogen or lower alkyl; R.sup.2 is --(CH.sub.2).sub.n --R.sup.3 or --CH.sub.2 --CH.dbd.CH--(CH.sub.2).sub.m --R.sup.3 or --CH.sub.2.C.tbd.C.(CH.sub.2).sub.m --R.sup.3 where n is 1 to 6, and m is 0 to 3; and R.sup.3 is a ring of formula ##STR2## The compounds exhibit activity as 5-HT.sub.1A agonists, antagonists or partial agonists and are used for the treatment of CNS disorders, e.g. anxiety, as antihypertensives and in treating anorexia.Type: GrantFiled: September 25, 1991Date of Patent: March 16, 1993Assignee: John Wyeth & Brother LimitedInventors: Ian A. Cliffe, Howard L. Mansell, Richard S. Todd, Alan C. White
-
Patent number: 5194446Abstract: Methods of treating chronic arthritis and osteoporosis which utilize both known and novel compounds which would fall under the general formula:(HO)p--A--[--OS(O).sub.2 NR.sup.1 R.sup.2 ].sub.zwherein A encompasses a wide range of values including but not limited to aryl, loweralkyl, cycloalkyl, and carbohydrates including sucrose and fructose; p is equal to the number of unreacted hydroxy groups contained on the molecule and may be zero; z is the number of --OS(O).sub.2 NR.sup.1 R.sup.2 groups and is always at least one; R.sup.1 and R.sup.2 are selected from hydrogen, loweralkyl, carboxy and the like; a novel process for preparing the compounds is provided wherein an appropriate sulfamic acid aryl ester is reacted with a hydroxy substituted A radical which may or may not contain thereon protected carboxyl, amino or hydroxy substituents, in an aprotic solvent containing a tertiary amine base. Pharmaceutical compositions for the treatment of chronic arthritis and osteoporosis are also provided.Type: GrantFiled: July 24, 1991Date of Patent: March 16, 1993Assignee: A. H. Robins Company, IncorporatedInventors: Young S. Lo, Joseph C. Nolan, William J. Welstead, Jr., David A. Walsh, Dwight A. Shamblee, Ibrahim M. Uwaydah
-
Patent number: 5192771Abstract: For inhibiting lipoxygenzce, (quinolin-2-yl-methoxy) phenylacetic acid derivatives containing cyclic substituents of the formula ##STR1## in which A, Q, D, E, G, T and M are hydrogen or various radicals,R.sup.3 is halogen or an alkyl or phenyl radical, andR.sup.1 and R.sup.2 complete a carbocyclic ring which may be substituted and/or fused to another ring,and salts thereof.Type: GrantFiled: August 1, 1990Date of Patent: March 9, 1993Assignee: Bayer AktiengesellschaftInventors: Klaus Mohrs, Siegfried Raddatz, Romanis Fruchtmann, Christian Kohlsdorfer, Reiner Muller-Peddinghaus, Pia Theisen-Popp
-
Patent number: 5190956Abstract: Compounds useful as antiviral agents against DNA containing viruses, such as herpes group viruses, are disclosed. The compounds are selected from the group consisting of: ##STR1## and their pharmaceutically acceptable salts and solvates. Pharmaceutical compositions containing compounds represented by Formula 1.00 are disclosed. Also disclosed are methods of treating a viral infection using compounds represented by Formula 1.00The compounds of Formula 1.00 are also useful as intermediates to compounds of: ##STR2## Compounds of Formula 1.0 are useful as antiviral agents against the same viruses that the compounds of Formula 1.00 are useful against.Type: GrantFiled: September 7, 1990Date of Patent: March 2, 1993Assignee: Schering CorporationInventors: Adriano Afonso, Jay Weinstein, Margaret J. Gentles
-
Patent number: 5187180Abstract: (Quinolin-2-ylmethoxy)Heterotetrahydrocarbazoles as inhibitors of the biosynthesis of leukotrienes useful in the treatment of asthma and eye inflamation.Type: GrantFiled: July 12, 1991Date of Patent: February 16, 1993Assignee: Merck Frosst Canada, Inc.Inventor: John W. Gillard
-
Patent number: 5180823Abstract: The present invention relates to a process for preparing bicyclic compounds and intermediates thereof. The compounds are useful as anti-allergic, anti-inflammatory and/or cytoprotective agents.Type: GrantFiled: October 8, 1991Date of Patent: January 19, 1993Assignee: Schering CorporationInventors: Dinesh Gala, Martin Steinman, Ashit Ganguly
-
Patent number: 5179107Abstract: Compounds useful as antiviral agents against DNA containing viruses, such as herpes group viruses, are disclosed. The compounds are selected from the group consisting of: ##STR1## and their pharmaceutically acceptable salts and solvates. Pharmaceutical compositions containing compounds represented by Formula 1.0 are disclosed. Also disclosed are methods of treating a viral infection using compounds represented by Formula 1.0.A process for making compounds of Formula 1.0 from the appropriate 3-oximino-quinolin-2,4(1H)-dione (Formula 2.5) is also disclosed. The process comprises reductively hydrolyzing an appropriate 3-oximino-quinolin-2,4(1H)-dione (Formula 2.5) in a mixture with a hydrogenation catalyst and an acidic solvent mixture.Type: GrantFiled: December 19, 1991Date of Patent: January 12, 1993Assignee: Schering CorporationInventors: Adriano Afonso, Jay Weinstein, Margaret J. Gentles
-
Patent number: 5179093Abstract: Compounds of the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein, R is H, halogen, (C.sub.1 -C.sub.6) alkyl, N(C.sub.1 -C.sub.6 alkyl/aryl).sub.2, OH, O--(C.sub.1 -C.sub.6) alkyl/aryl, CH.sub.2 OH, COOH, COO-alkyl/aryl, SO.sub.2 NH.sub.2, or SO.sub.2 NH (C.sub.1 -C.sub.6 alkyl/aryl);R.sub.1 is C.sub.1 -C.sub.6 alkyl, cycloalkyl, C.sub.2 -C.sub.6 alkenyl, heteroaryl, substituted heteroaryl, heterocycloalkyl, --CH.sub.2 -aryl, --CH.sub.2 -substituted aryl, --CH.sub.2 -heteroaryl, or --CH.sub.2 -substituted heteroaryl;R.sub.2 is H, C.sub.1 -C.sub.6 alkyl or aryl; ##STR2## is an aromatic ring or a heteroaromatic ring; and X is O or N-(alkyl/aryl/alkyl-aryl/alkoxylalkoxyaryl)are described. These compounds are useful as agents for treating viruses.Type: GrantFiled: May 10, 1991Date of Patent: January 12, 1993Assignee: Schering CorporationInventors: Adriano Afonso, Stuart W. McCombie, Jay Weinstein
-
Patent number: 5175151Abstract: Compounds useful as antihypertensive agents, or antiviral agents against DNA containing viruses, such as herpes group viruses, are disclosed. The compounds are represented by Formula 1.0: ##STR1## and their pharmaceutically acceptable salts and solvates. Pharmaceutical compositions containing compounds represented by Formula 1.0 are disclosed. Also disclosed are methods of treating hypertension or a viral infection using compounds represented by Formulas 1.0.Also disclosed is a compound of Structure B ##STR2## useful as an intermediate in producing compounds of Formula 1.0. A process for preparing the compounds of Formula 1.0 is also disclosed. In the process a compound of Structure B ##STR3## is reacted with an alkoxide R.sub.1 O.sup.- M.sup.+ in a solvent comprising the corresponding alcohol R.sub.1 OH of the alkoxide. Optionally, an organic cosolvent may be used with the solvent.Type: GrantFiled: February 5, 1992Date of Patent: December 29, 1992Assignee: Schering CorporationInventors: Adriano Afonso, Jay Weinstein, Margaret J. Gentles
-
Patent number: 5158954Abstract: Fungicidal compounds of the formula (I): ##STR1## and stereoisomers thereof, wherein K is oxygen or sulphur; Z is optionally substituted aryl or optionally substituted heteroaryl; X is O, S(O).sub.n, NR.sup.4, CR.sup.1 R.sup.2, CHR.sup.5, CO, CR.sup.1 (OR.sup.2), C.dbd.CR.sup.1 R.sup.2, CHR.sup.1 CHR.sup.2, CR.sup.1 .dbd.CR.sup.2, CHR.sup.1 CR.sup.2 .dbd.CH, C.dbd.C, OCHR.sup.1, CHR.sup.1 O, OCHR.sup.1 O, S(O).sub.n CHR.sup.1, S(O).sub.n CHR.sup.1 O, CHR.sup.1 S(O).sub.n, CHR.sup.1 OSO.sub.2, NR.sup.4 CHR.sup.1, CHR.sup.1 NR.sup.4, CO.sub.2, O.sub.2 C, SO.sub.2 O, OSO.sub.2, CO.CO, COCHR.sup.1, COCHR.sup.1 O, CHR.sup.1 CO, CHOH.CHR.sup.1, CHR.sup.1.CHOH, ##STR2## CONR.sup.4, OCONR.sup.4, NR.sup.4 CO, CSNR.sup.4, OCS.NR.sup.4, SCO.NR.sup.4, NR.sup.4 CO.sub.2, NR.sup.4 CS, NR.sup.4 CSO, NR.sup.4 COS, NR.sup.4 CONR.sup.4, S(O).sub.n NR.sup.4, NR.sup.4 S(O).sub.n, CS.sub.2, S.sub.2 C, CO.S, SCO, N.dbd.N, N.dbd.CR.sup.1, CR.sup.1 .dbd.N, CHR.sup.1 CHR.sup.2 CH(OH), CHR.sup.1 OCO, CHR.sup.1 SCO, CHR.sup.1 NR.sup.Type: GrantFiled: October 15, 1990Date of Patent: October 27, 1992Assignee: Imperial Chemical Industries PLCInventors: John M. Clough, Christopher R. A. Godfrey, Stephen P. Heaney, Kenneth Anderton
-
Patent number: 5157040Abstract: Substituted quinolines of the formula (I), are angiotensin II antagonists, ##STR1## and useful in the treatment of hypertension, ocular hypertension and certain CNS disorders.Type: GrantFiled: April 5, 1991Date of Patent: October 20, 1992Assignee: Merck & Co., Inc.Inventors: William J. Greenlee, David B. R. Johnston, Malcolm MacCoss