Bicyclo Ring System Which Contains The Hetero Ring As One Of The Cyclos Patents (Class 540/593)
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Patent number: 5274097Abstract: Novel 1,3-disubstituted pyrrolidines active on the central nervous system of the formula ##STR1## wherein A--denotes phenyl or hetaryl, which is optionally fused with aromatic, saturated or unsaturated cyclic or heterocyclic hydrocarbons, where this radical can optionally be substituted,X--denotes --O--CH.sub.2 --, --CH.sub.2 --O-- or --O--,n--denotes a number from 1 to 19, andB--denotes cyano or a group of the formula --COOR.sup.1, --CONR.sup.2 R.sup.3, --SO.sub.2 NR.sup.2 R.sup.3, --SO.sub.m R.sup.4, --NR.sup.5 R.sup.6, or --C.tbd.C--CH.sub.2 --NR.sup.5 R.sup.6,and salts thereof.Type: GrantFiled: April 9, 1991Date of Patent: December 28, 1993Assignee: Bayer AktiengesellschaftInventors: Rudolf Schohe, Peter-Rudolf Seidel, Jorg Traber, Thomas Glaser
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Patent number: 5244898Abstract: Novel benzoheterocyclic compounds of the formula: ##STR1## wherein R.sup.1 is H, halogen, OH, etc,; R.sup.2 is H, alkyl, halogen or alkoxy; R.sup.3 is phenyl-alkanoylamino, or ##STR2## R.sup.4 is H, --NR.sup.6 R.sup.7, alkenyloxy, HO-alkyl, --O--CO--A--NR.sup.8 R.sup.9, etc.; R.sup.5 is H, OH, etc., or a salt thereof, which have excellent vasopressin antagonistic activities and useful as vasodilator, hypotensive agent, water diuretics, platelet agglutination inhibitor, and a vasopressin antagonistic composition containing the compound as the active ingredient.Type: GrantFiled: April 17, 1992Date of Patent: September 14, 1993Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Hidenori Ogawa, Kazumi Kondo, Hiroshi Yamashita, Kenji Nakaya, Hajime Komatsu, Michinori Tanaka, Kazuyoshi Kitano, Michiaki Tominaga, Yoichi Yabuuchi
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Patent number: 5242912Abstract: The following cyclic anthranilic acid derivative, their acid addition salts or alkali salts thereof represented by a general formula [I] are useful for antirheumatic drug, autoimmune disease curing drug and metabolic bone disease curing drug. ##STR1## wherein R.sup.1 to R.sup.6 and X are as defined in claim 1.Type: GrantFiled: April 25, 1991Date of Patent: September 7, 1993Assignee: Kyorin Pharmaceutical Co., Ltd.Inventors: Mitsutomo Miyashita, Yasushi Kohno, Eisuke Kojima, Koji Saito
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Patent number: 5223505Abstract: This invention concerns novel aminopyrimidinium salts of the formula I: ##STR1## in which R.sup.1 is alkyl, alkenyl, cycloalkyl, phenyl, phenylalkyl or cycloalkyl-alkyl; one of R.sup.2 and R.sup.6 is a basic group selected from amino, alkylamino, dialkylamino of up to eight carbon atoms, pyrrolidino, piperidino and morpholino; and the other of R.sup.2 and R.sup.6 is hydrogen, alkyl, alkenyl, alkoxyalkyl, phenyl, phenylalkyl, cycloalkyl or cycloalkyl-alkyl; or both of R.sup.2 and R.sup.6 are basic groups as mentioned above; and R.sup.5 is hydrogen, (1-4C)alkyl or (3-6C)alkenyl; or R.sup.2 is a basic group as mentioned above, and R.sup.5 and R.sup.6 together form alkylene or, together with the appendant carbon atoms of the pyrimidine ring, complete a benzene ring; R.sup.4 is hydrogen, alkyl, cycloalkyl-alkyl, alkenyl, alkynyl or phenylalkyl; or R.sup.4 is an optionally substitutued alkylene or alkenylene linked to the nitrogen atom of the group Q.A.Type: GrantFiled: April 20, 1990Date of Patent: June 29, 1993Assignee: Imperial Chemical Industries PlcInventors: Rodney B. Hargreaves, Paul W. Marshall, Bernard J. McLoughlin, Stuart D. Mills
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Patent number: 5212301Abstract: Introduction of a fluoro substituent into an aromatic ring adjacent an electron donating group is difficult producing mixed isomers and low yields of desired products.A process for the introduction of a fluoro substituent into a substantially adjacent position to an electron-donating group into an aromatic compound in high yield is disclosed.The fluoroaromatic compounds are useful as synthetic intermediates for example in the manufacture of agrochemicals, pharmaceuticals and dyestuffs.Type: GrantFiled: May 8, 1992Date of Patent: May 18, 1993Assignee: Imperial Chemical Industries PLCInventors: John S. Moilliet, Richard D. Chambers, Michael H. Rock
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Patent number: 5206363Abstract: The invention relates to a process for the resolution of enantiomers of 5-heteroaryl-1,3,4-thiadiazinones of formula I by the kinetic resolution of racemates, characterized in that racemic I is dissolved in an inert solvent or solvent mixture and acylated with a chiral acid chloride. The resulting mixture of diastereoisomers is reacted with an amine or alcohol, thereby achieving a complete resolution of one of the diastereoisomers and a very slight or partial resolution of the other diastereoisomer into the enantiomers on which they are based, the resolution products are then separated off and the remaining pure diastereoisomer is converted to the corresponding pure enantiomer by reaction with an amine or an alcohol.Type: GrantFiled: September 2, 1992Date of Patent: April 27, 1993Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Rochus Jonas, Peter Ersing
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Patent number: 5204470Abstract: Azabicyclic compounds of formula ##STR1## and their pharmaceutically acceptable acid addition salts are disclosed. In the formula, ##STR2## is an optionally substituted heteroaryl group containing at least one hetero atom X; n is 2, 3 or 4; m is 1 or 2; R.sup.1 is hydrogen, C.sub.1-6 alkyl, C.sub.3-5 -alkenyl, C.sub.3-6 cycloalkyl, C.sub.3-6 cycloalkyl-C.sub.1-2 alkyl or aryl- or heteroaryl-C.sub.1-2 -alkyl; and the --(CH.sub.2).sub.m ##STR3## moiety is ortho to the hetero atom X. The compounds exhibit activity as 5-HT.sub.3 -antagonists and can be used, inter alia, for the treatment of neuropsychiatric disorders.Type: GrantFiled: September 9, 1991Date of Patent: April 20, 1993Assignee: John Wyeth & Brother, LimitedInventor: Ian A. Cliffe
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Patent number: 5190938Abstract: The invention relates to compounds of formula ##STR1## in which R.sub.1 is selected from the groups R.sub.3 and OR.sub.3, R is selected from H and a group CHR.sub.2 R', in which R.sub.2 is selected from H, alkyl, carboxy and carboxamido and R', is H, alkyl or phenyl, Z represents S or O; and m and n, which may be identical or different, equal 1 or 2, and their N-oxides, salts and quaternary ammonium derivatives.The invention also relates to the process for preparing these compounds, as well as to pharmaceutical compositions containing them.Type: GrantFiled: October 2, 1990Date of Patent: March 2, 1993Assignee: SanofiInventors: Alain Badorc, Marie-Francoise Bordes, Daniel Frehel, Jean-Marc Herbert
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Patent number: 5185452Abstract: The invention concerns novel, pharmaceutically useful, benzheterocyclyl sulphones of the formula I: ##STR1## in which ring A may bear optional halogeno, (1-4C)alkyl or fluoro(1-4C)alkyl substituents; X is oxygen, or a group of the formula --S(O).sub.n -- or --NR.sup.1 -- in which n is zero, 1 or 2 and R.sup.1 is hydrogen, (1-4C)alkyl, (1-6C)alkanoyl, benzoyl or phenyl(1-4C)alkyl, the last two optionally substituted; Y is various linking groups defined hereinafter, such as ethylene or trimethylene; and in which the group --SO.sub.2 CH.sub.2 NO.sub.2 is located at position a, b or c in ring A; together with the non-toxic thereof. Other aspects of the invention include the production of the novel compounds by analogy processes and pharmaceutical compositions of the novel compounds for use in the treatment of diabetic complications.Type: GrantFiled: February 5, 1990Date of Patent: February 9, 1993Assignee: Imperial Chemical Industries PLCInventors: David R. Brittain, Michael T. Cox
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Patent number: 5175157Abstract: Disclosed are new cyclic amine derivatives of the formula I ##STR1## wherein the substituents are defined in the specification. These compounds are useful as for treating sinus tachycardia.Type: GrantFiled: July 3, 1991Date of Patent: December 29, 1992Assignee: Boehringer Ingelheim GmbHInventors: Manfred Psiorz, Joachim Heider, Andreas Bomhard, Manfred Reiffen, Norbert Hauel, Klaus Noll, Berthold Narr, Christian Lillie, Walter Kobinger, Jurgen Dammgen
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Patent number: 5166161Abstract: 3-Oxo-4-acyl or carbamyl-bicyclic aromatic and heterocyclic compounds as inhibitors of cyclooxygenase and lipoxygenase and useful as antiallergy and antiinflammatory agents.Type: GrantFiled: January 22, 1991Date of Patent: November 24, 1992Assignee: Pfizer Inc.Inventors: Toshihide Kokura, Kazunari Nakao, Fumitaka Ito, Masami Nakane
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Patent number: 5114934Abstract: The compounds of the formula ##STR1## wherein R.sub.a, R.sub.b, R.sub.c, R.sub.d are defined in the specification and pharmaceutically acceptable addition salts are disclosed. The compounds of formula I have valuable pharmacological properties and can be used for the control of prevention of illnesses. In particular, they have muscle relaxant, seditive-hypnotic, anxiolytic and/or anticonvulsive activity and can accordingly be used in the control or prevention of muscle tensions, stress conditions, isomnia, anxiety states and/or convulsions.Type: GrantFiled: June 1, 1989Date of Patent: May 19, 1992Assignee: Hoffman-La Roche, Inc.Inventors: Ulf Fischer, Fernand Schneider, Ulrich Widmer
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Patent number: 5104868Abstract: This invention relates to novel tricyclic derivatives of 7-substituted-6-fluoro-1,4-dihydroquinol-4-one-3-carboxylic acids and certain esters and cation salts thereof. The compounds of this invention are substituted at the 7-position by vinyl, W--CH.dbd.CH--, CH.sub.3 C.tbd.C--, W--CH.sub.2 C.tbd.C-- or ##STR1## where W is selected from certain substituted alkyl groups. This invention also relates to antibacterial compositions containing the compounds and methods of using the compounds to treat bacterial disease.Type: GrantFiled: August 29, 1990Date of Patent: April 14, 1992Assignee: Pfizer Inc.Inventor: Paul R. McGuirk
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Patent number: 5096900Abstract: A benzazepine derivative which is a compound of formula (I): ##STR1## in which: each of m and n denotes the number 1, oreach of m and n denoted the number 2, orm denotes the number 3 and n denoted the number 1; andR denotes hydrogen or a group of formula --Z--R' in which Z denotes a --CO-- or --CH.sub.2 -- group and R' denotes a phenyl group which is unsubstituted or substituted with from one to three substituents selected from halogen atoms, linear or branch (C.sub.1 -C.sub.3) groups and linear or branched (C.sub.1 -C.sub.3) alkoxy groups,or a pharmacologically acceptable acid addition salt.Type: GrantFiled: February 8, 1990Date of Patent: March 17, 1992Assignee: SynthelaboInventors: Pascal George, Mireille Sevrin, Michel Mangane
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Patent number: 5096918Abstract: The invention concerns pharmaceutially useful heterocyclic nitromethane compounds of the formula I: ##STR1## in which ring Q is a heterocycle of 4 to 7 ring atoms, the fragment completing the ring Q having 2 to 5 atoms, one of which is carbon, oxygen, sulphur or a group of the formula --NRa--, and the remainder are carbon; Ra is hydrogen, (1-6C)alkyl, (2-6C)alkanoyl, trifluoroacetyl, phenyl, benzoyl, or phenyl(1-4C)alkyl, the latter three optionally substituted; and R.sup.1 R.sup.2 and R.sup.3 are independently hydrogen, hydroxy, (1-6C)alkyl, (1-6C)alkoxy, phenyl, phenoxy or phenyl(1-4C)alkyl, the last three optionally substituted, or two of R.sup.1, R.sup.2 and R.sup.3 situated on adjacent ring carbon atoms and together with said carbon atoms form a benzene ring fused to ring Q, the benzene ring itself optionally substituted, provided that when the fragment completion ring Q is of 3 atoms then at least one of R.sup.1, R.sup.2 and R.sup.3 is hydrogen; and salts thereof.Type: GrantFiled: February 5, 1990Date of Patent: March 17, 1992Assignee: Imperial Chemical Industries PLCInventor: Keith B. Mallion
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Patent number: 5063208Abstract: A renin inhibiting compound having an aminodiol functional group is useful for treating hypertension, congestive heart failure and glaucoma and inhibits retroviral protease.Type: GrantFiled: June 29, 1990Date of Patent: November 5, 1991Assignee: Abbott LaboratoriesInventors: Saul H. Rosenberg, Kenneth P. Spina, Steven R. Crowley
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Patent number: 5059608Abstract: The invention relates to a compound useful as an anticonvulsant, and for treatment of delayed neuronal death, the compound being a bicyclic amine of the formula: ##STR1## wherein R.sup.1 is lower alkyl,R.sup.2 is aryl which may have one or more suitable substituent(s), cyclo(lower)alkyl or heterocyclic group,R.sup.3 is hydrogen, lower alkyl which may have one or more suitable substituent(s), lower alkenyl, or acyl which may have one or more suitable substituent(s),R.sup.4 is hydrogen, lower alkyl, or hydroxy(lower)alkyl,R.sup.5 is hydrogen, lower alkyl, halogen, or protected amino, andn is an integer of 1 or 2, with the proviso that when R.sup.3 is lower alkyl which may have one or more suitable substituent(s), R.sup.2 is cyclo(lower)alkyl or heterocyclic group,or a pharmaceutically acceptable salt thereof.Type: GrantFiled: March 23, 1989Date of Patent: October 22, 1991Assignee: Fujisawa Pharmaceutical Company, Ltd.Inventors: Hisashi Takasugi, Atsushi Kuno, Mitsuru Ohkubo
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Patent number: 5036092Abstract: Aminomethyl oxooxazolidinyl aza cycloalkylbenzene derivatives, such as l-N-[3-(2,3-dihydro-3-aza-1H-inden-5-yl)-2-oxooxazolidin-5-ylmethyl]acetam ide, possess useful antibacterial activity.Type: GrantFiled: March 15, 1990Date of Patent: July 30, 1991Assignee: Du Pont Merck PharmaceuticalInventors: Chia-Lin J. Wang, Mark A. Wuonola
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Patent number: 5036093Abstract: Aminomethyl oxooxazolidinyl azacycloalkylbenzene derivatives, such as l-N-[3-(2,3-dihydro-3-aza-1H-inden-5-yl)-2-oxooxazolidin-5-ylmethyl]acetam ide, possess useful antibacterial activity.Type: GrantFiled: March 15, 1990Date of Patent: July 30, 1991Assignee: Du Pont Merck PharmaceuticalInventors: Chia-Lin J. Wang, Mark A. Wuonola
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Patent number: 5028602Abstract: Pharmaceutical compounds having the formula ##STR1## in which R.sup.1 is hydrogen, hydroxy, nitro, cyano, halo, amino, acetamido, hydroxy-C.sub.1-4 alkyl, carboxaldehydo, C.sub.1-4 alkyl-carbonyl, carboxy, C.sub.1-4 alkoxy-carbonyl, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, C.sub.1-4 alkylsulphonyl or C.sub.1-4 alkoxy-C.sub.1-4 alkyl, R.sup.2 is hydrogen or halo, R.sup.3 is optionally substituted phenyl or optionally substituted phenyl ortho condensed with an optionally substituted ring selected from benzene, cyclohexane, cyclohexene, cyclopentane or cyclopentene, in which ring one of the carbon atoms may be replaced by oxygen, sulphur or nitrogen, and R.sup.4 is hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl or optionally substituted benzyl; and salts thereof.Type: GrantFiled: April 12, 1990Date of Patent: July 2, 1991Assignee: Lilly Industries LimitedInventors: Barry P. Clark, David E. Tupper
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Patent number: 5017708Abstract: A compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 each is hydrogen, hydroxy, oxo, halogen, azido, amino, C.sub.1 -C.sub.3 alkylamino, or aminomethyl, in which said amino, C.sub.1 -C.sub.3 alkylamino and aminomethyl each is optionally substituted by one or two members selected from the group consisting of C.sub.1 -C.sub.3 alkyl and amino-protecting group; n is an integer of 1 to 3; p and q each is an integer of 0 to 3 with proviso that p+q=1 to 4 or acid-addition salts thereof, being useful materials for preparing side chains of antibacterial quinolonecarboxylic acids, cephalosporines, or other antibiotics.Type: GrantFiled: September 8, 1989Date of Patent: May 21, 1991Assignee: Shionogi & Co., Ltd.Inventors: Masaru Ogata, Hiroshi Matsumoto, Sumio Shimizu, Shiro Kida
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Patent number: 5001129Abstract: The present invention relates to tricyclic carbamates coplying with the formula ##STR1## in which n=0, 1 or 2,p=0 or 1,R.sub.1 represents a hydrogen atom; a group which is alkyl in C.sub.1 -C.sub.4 ; a phenyl group; a group which is alkenyl in C.sub.2 -C.sub.3 ; or a methyl group substituted by a hydroxy group, a group which is alkoxy in C.sub.1 -C.sub.4, an amino group or an N-alkylamino or N,N-dialkylamino group where the alkyl radical is in C.sub.1 -C.sub.4, andR.sub.2 represents a hydrogen atom; a halogen atom; a group which is alkyl in C.sub.1 -C.sub.4, or a group which is alkoxy in C.sub.1 -C.sub.4, and their salts of addition of acid.These compounds are therapeutically useful, notably as antidepressant agents.Type: GrantFiled: December 13, 1988Date of Patent: March 19, 1991Assignee: Delalande S.A.Inventors: Alain J. L. Renaud, Alain R. Schoofs, Jean-Marc M. Guiraudie, Denis M. Brochet
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Patent number: 4999359Abstract: A compound, or a solvate or salt thereof, of formula I: ##STR1## in which: R.CO-- is an acyl group containing a substituted or unsubstituted carbocyclic aromatic or heterocyclic aromatic group;R.sub.1 and R.sub.2 are independently hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.3-6 cycloalkyl or C.sub.4-12 cycloalkylalkyl groups or together form a C.sub.2-8 branched or linear polymethylene or C.sub.2-6 alkenylene group, optionally substituted with a hetero-atom;R.sub.3 is hydrogen, C.sub.1-6 alkyl, or phenyl or R.sub.3 together with R.sub.1 form a --(CH.sub.2).sub.3 -- or --(CH.sub.2).sub.4 -- group;R.sub.4 is C.sub.1-6 alkyl, or phenyl;R.sub.5 is hydrogen or together with R.sub.4 forms a --(CH.sub.2).sub.n -- group in which n=1, 2 or 3; and `Het` is an optionally substituted single or fused ring heterocyclic group, containing from 5 to 12 ring atoms and comprising up to four hetero-atoms in the or each ring selected from oxygen, nitrogen and sulphur, with the proviso that when, simultaneously, R.sub.Type: GrantFiled: March 14, 1989Date of Patent: March 12, 1991Assignee: Dr. Lo Zambeletti S.p.A.Inventors: Vittorio Vecchietti, Giuseppe Giardina
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Patent number: 4996202Abstract: Substituted 8-amino-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines useful in treating mental disorders and which have activities of prolonged duration are disclosed. Methods for preparing these compounds and methods for their use are also described.Type: GrantFiled: October 17, 1985Date of Patent: February 26, 1991Assignee: Schering CorporationInventors: Joel G. Berger, Wei K. Chang, Elijah H. Gold, Arthur J. Elliott
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Patent number: 4992448Abstract: There are described compounds of the formula, ##STR1## where R is hydrogen, loweralkyl, arylloweralkyl or loweralkylcarbonyl;k is 0 or 1;m is 1,2 or 3;k+m is 2 or 3; andn is 0 or 1;which compounds are useful as topical antiinflammatory agents for the treatment of various dermatoses.Type: GrantFiled: October 24, 1989Date of Patent: February 12, 1991Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Richard C. Effland, Joseph T. Klein, Gordon E. Olsen, Larry Davis
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Patent number: 4988690Abstract: The invention relates to 1-aryloxy-2,3,4,5-tetrahydro-3-benzazepines of the formula ##STR1## wherein Y is the same or different and is hydrogen and lower alkoxy; X is hydrogen, halogen, lower alkyl, lower alkoxy, CF.sub.3, NO.sub.2, CN and NH.sub.2 ; R is hydrogen, lower alkyl, cycloalkyllower alkyl, ##STR2## Ar lower alkyl of the formula -alkylene ##STR3## where Z is hydrogen, lower alkyl, lower alkoxy, halogen, CF.sub.3, NO.sub.2 and NH.sub.2 ; and an alkylene amine of the formula ##STR4## where R.sub.1 and R.sub.2 are the same of different and are hydrogen and lower alkyl, and the pharmaceutically acceptable acid addition salts thereof.Type: GrantFiled: June 14, 1982Date of Patent: January 29, 1991Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Richard C. Effland, Joseph T. Klein, Larry Davis
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Patent number: 4985063Abstract: A 3-aryl-pyrrolidine-2,4-dione (e) derivative of the formula (I) ##STR1## in which X represents alkyl, halogen and alkoxy,Y represents hydrogen, alkyl, halogen, alkoxy and halogenoalkyl,Z represents alkyl, halogen and alkoxy,m represents a number from 1-4,n represents a number from 0-3, R represents hydrogen, ##STR2## or A where A represents a metal cation equivalent or represents an ammonium ion,R.sup.1 represents optionally halogen-substituted alkyl, alkenyl, alkoxyalkyl, alkylthioalkyl, polyalkoxyalkyl and optionally substituted cycloalkyl which can be interrupted by hetero atoms, or represents optionally substituted phenyl, optionally substituted phenylalkyl, substituted hetaryl, substituted phenoxyalkyl and substituted hetaryloxyalkyl andR.sup.2 represents optionally halogen-substituted alkyl, cycloalkyl, alkenyl, alkoxyalkyl, polyalkoxyalkyl and optionally substituted phenyl,as well as the pure enantiomeric forms of compounds of the formula (I).Type: GrantFiled: August 8, 1989Date of Patent: January 15, 1991Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Hermann Hagemann, Andreas Krebs, Albrecht Marhold, Klaus Lurssen, Robert R. Schmidt, Hans-Joachim Santel, Benedikt Becker, Klaus Schaller, Wilhelm Stendel
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Patent number: 4965268Abstract: Aminomethyl oxooxazolidinyl cycloalkylbenzene derivatives, such as l-N-[3-(2,3-dihydro-1-oxo-1H-inden-5-yl)-2-oxooxazolidin-5-ylmethyl]acetam ide, possess useful antibacterial activity.Type: GrantFiled: March 15, 1990Date of Patent: October 23, 1990Assignee: E. I. Du Pont de Nemours and CompanyInventors: Chia-Lin J. Wang, Mark A. Wuonola
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Patent number: 4962108Abstract: Novel quinoline-, naphthyridine-, and benzoxazine-carboxylic acid derivatives with bridged sidechains useful as antibacterial agents are described. Methods for their preparation, formulation, and use in treatment of bacterial infections is also described.Type: GrantFiled: December 9, 1988Date of Patent: October 9, 1990Assignee: Warner-Lambert CompanyInventors: Marland P. Hutt, Jr., John S. Kiely
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Patent number: 4959374Abstract: A compound of formula (I): ##STR1## or a pharmaceutically acceptable salt, ester or amide thereif, wherein: Z represents a residue of a substituted or unsubstituted aryl group,X represents o or NR.sup.o wherein R.sup.0 represents a hydrogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted aryl group, an alkanoyl group substituted or unsubstituted in the alkyl moiety, or an arylalkyl moiety substituted or unsubstituted in the aryl moiety,n represents an integer 1 or 2,m represents an integer 1 or 2,p represents an integer 2 or 3,andq represents an integer in the range of from 1 to 12; pharmaceutical compositions containing such compounds and the use of such compounds and compositions in medicine.Type: GrantFiled: July 6, 1989Date of Patent: September 25, 1990Assignee: Beecham Group P.L.C.Inventor: John M. Berge
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Patent number: 4936121Abstract: A compound of the formula (I) ##STR1## where A is an alkylene or alkenylene group, R.sub.1 is an aryl group which may be substituted, R.sub.2 is a hydrogen atom, a lower alkyl group, a lower alkenyl group, a lower alkynyl group, a halogenated lower alkyl group, a cycloalkyl group, a lower alkoxyalkyl group, a lower alkylthioalkyl group, a phenyl group which may be substituted or an aralkyl group which may be substituted, R.sub.3 is a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkenyl group, a lower alkynyl group or a halogenated lower alkyl group, or R.sub.2 and R.sub.3 may be combined to form a group of --(CH.sub.2).sub.n --(n is 3 or 4), or salt thereof, which is useful as a herbicide.Type: GrantFiled: October 12, 1988Date of Patent: June 26, 1990Assignee: Daicel Chemical Industries Ltd.Inventors: Yukihisa Goto, Hiroshi Yagihara, Kazuhisa Masamoto, Yasuo Morishima, Yukihiro Sagawa, Hirokazu Osabe
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Patent number: 4916128Abstract: Thiadiazinones of the formula I ##STR1## wherein A is --CHR.sup.4 --CHR.sup.5 --, --CH.sub.2 --CR.sup.4 R.sup.5 --, --CR.sup.4 R.sup.5 --CH.sub.2 --, --CHR.sup.4 --CHR.sup.5 --CH.sub.2 --, --CHR.sup.4 --CH.sub.2 --CHR.sup.5 --, --CH.sub.2 --CHR.sup.4 --CHR.sup.5 --, --CR.sup.4 R.sup.5 --CH.sub.2 CH.sub.2 --, --CH.sub.2 --CR.sup.4 R.sup.5 --CH.sub.2 -- or --CH.sub.2 CH.sub.2 --CR.sup.4 R.sup.5 --,R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are each independently H, C.sub.1-5 -alkyl, C.sub.2-5 -alkenyl or C.sub.2-5 -alkinyl,R.sup.3 is also C.sub.1-15 -acyl,R.sup.6 is H, alkyl, alkoxyl, OH, F, Cl, Br or I andZ is (H, H), (H, alkyl), (alkyl, alkyl) or O,the alkyl, alkenyl, alkinyl and/or alkoxy groups in each case containing up to 5 C atoms, but wherein, if A is --CH.sub.2 CH.sub.2 -- and Z is O, one of the radicals R.sup.1, R.sup.2, R.sup.3 and R.sup.6 must be other than H,and salts thereof demonstrate positive inotropic action and are suitable for combating cardiovascular diseases.Type: GrantFiled: June 6, 1988Date of Patent: April 10, 1990Assignee: Merck Patent Gesellschaft mit Beschrankter HaftungInventors: Rochus Jonas, Jaime Piulats, Michael Klockow, Ingeborg Lues, Hans-Jochen Schliep
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Patent number: 4912258Abstract: Fluorinated aniline derivatives of the general formula I are described ##STR1## in which R.sup.1 represents H or (CH.sub.2).sub.n -X, n is a whole number from 1 to 3, X is H, OH, NH.sub.2, CH.sub.3 CONH, CH.sub.3 SO.sub.2 NH, SO.sub.3 H or ArSO.sub.3 H, Ar is optionally substituted arylene radical, R.sup.1 is alternatively also a --(CH.sub.2).sub.3 -- group, which is bonded to the free o-position next to the N-atom, Y is H, --O--, --NH--, --S-- or a C--C single bond, R.sup.2, in the event that Y=H, is the same as or different from R.sup.1 and means one of the radicals shown for R.sup.1, and in the event that Y is a C--C single bond or --O--, --NH-- or --S--, is an alkylene group having 1 to 3 carbon atoms linked with Y, and R.sup.3 =H, alkyl having 1 to 3 carbon atoms, OCH.sub.3, CH.sub.3 CONH, CO.sub.2 H or SO.sub.3 H.Type: GrantFiled: February 5, 1988Date of Patent: March 27, 1990Assignee: Boehringer Mannheim GmbHInventors: Hans-Georg Batz, Rupert Herrmann
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Patent number: 4863946Abstract: A compound of formula (I): ##STR1## or a pharmaceutically acceptable salt, ester or amide thereof, wherein: Z represents a residue of a substituted or unsubstituted aryl group,X represents O or NR.sup.o wherein R.sup.o represents a hydrogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted aryl group, an alkanoyl group substituted or unsubstituted in the alkyl moiety, or an arylalkyl moiety substituted or unsubstituted in the aryl moiety.n represents an integer 1 or 2,m represents an integer 1 or 2,p represents an integer 2 or 3, andq represents an integer in the range of from 1 to 12; pharmaceutical compositions containing such compounds and the use of such compounds and compositions in medicine.Type: GrantFiled: December 1, 1986Date of Patent: September 5, 1989Assignee: Beecham Group plcInventor: John M. Berge
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Patent number: 4845079Abstract: A renin inhibiting compound of the formula: ##STR1## wherein A is a substituent; W is C.dbd.O or CHOH; U is CH.sub.2 or NR.sub.2, provided that when W is CHOH then U is CH.sub.2 ; R.sub.1 is loweralkyl, cycloalkylmethyl, benzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)methyl, (2-napththyl)methyl, (4-imidazoyl)methyl, .alpha.,.alpha.-dimethylbenzyl, 1-benzyloxyethyl, phenethyl, phenoxy, thiophenoxy or anilino; R.sub.2 is hydrogen or loweralkyl; R.sub.3 is loweralkyl, [(alkoxy)alkoxy]alkyl, (thioalkoxy)alkyl, loweralkenyl, benzyl or heterocyclic ring substituted methyl; R.sub.4 is loweralkyl, cycloalkylmethyl or benzyl; R.sub.5 is vinyl, formyl, hydroxymethyl or hydrogen; R.sub.7 is hydrogen or loweralkyl; R.sub.8 and R.sub.9 are independently selected from OH and NH.sub.2 ; and R.sub.6 is hydrogen, loweralkyl, vinyl or arylalkyl; provided that when R.sub.5 and R.sub.7 are both hydrogen and R.sub.8 and R.sub.9 are OH, the carbon bearing R.sub.5 is of the "R" configuration and the carbon bearing R.sub.Type: GrantFiled: July 11, 1988Date of Patent: July 4, 1989Inventors: Jay R. Luly, Jacob J. Plattner, Dale J. Kempf
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Patent number: 4831132Abstract: Novel ortho-(mono-substituted amino)phenylimines being intermediates to psychotropic drugs and other drugs are economically and industrially prepared by reacting anilines with nitriles in the presence of a boron trifluoride ether adduct and a halide-type Lewis acid, if necessary together with an organic base. Furthermore, the imines can be hydrolyzed with an acid to afford the corresponding ketones.Type: GrantFiled: December 30, 1986Date of Patent: May 16, 1989Assignee: Shionogi & Co., Ltd.Inventors: Tsutomu Sugasawa, Kazuyuki Sasakura
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Patent number: 4826974Abstract: Pyrrolo[1,2-a]azepinone derivatives of formula: ##STR1## in which R.sub.3 is H or halogen and either (A) R is benzyl or phenylthio in which the phenyls are optionally substituted by one or more halogens or hydroxy, alkyl, alkyloxy or alkylthio radicals, R.sub.1 and R.sub.2, which may be identical or different, denote alkyl optionally substituted by dialkylamino in which the alkyls are optionally joined to form a 1-pyrrolidinyl, piperidino, morpholino or 1-piperazinyl ring substituted by alkyl, or alternatively R.sub.1 and R.sub.2 form a heterocyclic ring chosen from pyrrolidine, piperidine, morpholine and piperazine, substituted by alkyl, alkenyl (2 to 4 C), benzyl or phenethyl optionally substituted by halogen, alkyl, alkyloxy, alkylthio, CF.sub.Type: GrantFiled: November 4, 1987Date of Patent: May 2, 1989Assignee: Rhone-Poulenc SanteInventors: Michel Barreau, Marie-Therese Comte, Daniel Farge, Jean-Luc Malleron, Gerard Ponsinet, Gerard Roussel
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Patent number: 4824831Abstract: Compound of the formula ##STR1## wherein R.sub.3 is aryl and R.sub.1 is hydrogen or ##STR2## are disclosed. These compounds are useful as cardiovascular agents, and especially as anti-hypertensive agents.Type: GrantFiled: December 21, 1987Date of Patent: April 25, 1989Assignee: E. R. Squibb & Sons, Inc.Inventor: Karnail Atwal
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Patent number: 4824472Abstract: Novel herbicidal 1-cyclyl or polycyclyl substituted 1H-imidazole-5-carboxylic acid derivatives, compositions containing these compounds as active ingredients, and a method for controlling weeds, preferably selectively in crops of useful plants. Processes for making these novel compounds.Type: GrantFiled: December 23, 1987Date of Patent: April 25, 1989Assignee: Janssen Pharmaceutica N.V.Inventors: Guy R. E. Van Lommen, Victor Sipido, Wim G. Verschueren, William R. Lutz
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Patent number: 4813998Abstract: Novel herbicidal 1-heterocyclyl-1H-imidazole-5-carboxylic acid derivatives, compositions containing these compounds as active ingredients, and a method for controlling weeds, preferably selectively in crops of useful plants. Further the invention also relates to a process for making these novel compounds.Type: GrantFiled: August 24, 1987Date of Patent: March 21, 1989Assignee: Janssen Pharmaceutica N.V.Inventors: Guy R. E. Van Lommen, William R. Lutz, Jozef F. E. Van Gestel
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Patent number: 4769366Abstract: Pyrrolo[1,2-a]azepinone derivatives of formula: ##STR1## in which R.sub.3 is H or halogen and either (A) R is benzyl or phenylthio in which the phenyls are optionally substituted by one or more halogens or hydroxy, alkyl, alkyloxy or alkylthio radicals, R.sub.1 and R.sub.2, which may be identical or different, denote alkyl optionally substituted by dialkylamino in which the alkyls are optionally joined to form a 1-pyrrolidinyl, piperidino, morpholino or 1-piperazinyl ring substituted by alkyl, or alternatively R.sub.1 and R.sub.2 form a heterocyclic ring chosen from pyrrolidine, piperidine, morpholine and piperazine, substituted by alkyl, alkenyl (2 to 4 C), benzyl or phenethyl optionally substituted by halogen, alkyl, alkyloxy, alkylthio, CF.sub.Type: GrantFiled: March 13, 1986Date of Patent: September 6, 1988Assignee: Rhone-Poulenc SanteInventors: Michel Barreau, Marie-Therese Comte, Daniel Farge, Jean-Luc Malleron, Gerard Ponsinet, Gerard Roussel
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Patent number: 4721708Abstract: Novel N-substituted tetrahydropyridine compounds are disclosed. The compounds have the property of inhibiting calcium induced contraction of smooth muscle and are adaptable to being employed in the chemotherapeutic treatment of cardiovascular diseases.Type: GrantFiled: November 26, 1985Date of Patent: January 26, 1988Assignee: Merck & Co., Inc.Inventors: George D. Hartman, Brian T. Phillips
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Patent number: 4680284Abstract: The invention relates to renin inhibiting compounds of the formula: ##STR1## wherein R.sub.2 is loweralkyl or arylalkyl; R.sub.3 is loweralkyl; X is ##STR2## wherein A is hydrogen or an N-protecting group, R.sub.1 is loweralkyl or arylalkyl, m is 1-3, n is 1-3, p is 1-3, q is 1-3, s is 1-3, and t is 0-2.Type: GrantFiled: January 16, 1986Date of Patent: July 14, 1987Assignee: Abbott LaboratoriesInventors: Jay R. Luly, Jacob J. Plattner, Anthony K. Fung
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Patent number: 4677101Abstract: Substituted dihydroazepines, their preparation, and the use thereof as calcium channel blockers are disclosed.Type: GrantFiled: September 26, 1983Date of Patent: June 30, 1987Assignee: Merck & Co., Inc.Inventors: David A. Claremon, David E. McClure
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Patent number: 4619784Abstract: There are disclosed diffusion transfer color processes and products which employ novel image dye-providing materials which provide image dyes having the chromophoric system represented by the formula ##STR1## X is H, alkyl, aryl or substituted aryl; W is H or alkyl, R is H or alkyl; m and n are each integers of from 2 to 6.The image dye-providing material includes a diffusion control moiety such as a hydroquinonyl group and may be diffusible or nondiffusible as a function of the diffusion control moiety.Type: GrantFiled: October 27, 1980Date of Patent: October 28, 1986Assignee: Polaroid Corporation, Patent Dept.Inventors: Louis Locatell, Jr., Charles M. Zepp, Ronald F. Cieciuch
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Patent number: 4616014Abstract: New triazine derivatives represented by the formula: ##STR1## wherein R.sup.1 is aryl, pyridyl, thienyl, 1,2,3,4-tetrahydroquinolyl or 1,3,4,5-tetrahydro-2H-1-benzazepinyl, optionally substituted with lower alkyl, lower alkoxy, halogen, nitro or oxo, R.sup.2 is hydrogen, lower alkyl or carbamoyl substituted with lower alkyl or ar(lower)alkyl, and Z is a group selected from ##STR2## and pharmaceutically acceptable salt thereof, processes for preparation thereof and pharmaceutical compositions comprising the same of antihypertensive and antithrombotic activity.Type: GrantFiled: October 8, 1982Date of Patent: October 7, 1986Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Tsutomu Teraji, Youichi Shiokawa, Kazuo Okumura, Yoshinari Sato