Nitrogen Attached Indirectly To The Six-membered Hetero Ring Through The Directly Attached Nitrogen By Nonionic Bonding Patents (Class 546/162)
-
Patent number: 5089504Abstract: Substituted 4-aminoquinazoline derivatives of the formula: ##STR1## in which R.sup.1 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkoxyC.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, C.sub.3-6 cycloalkylC.sub.1-6 alkyl, phenylC.sub.1-6 alkyl, the phenyl group being optionally substituted;R.sup.2 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, amino, C.sub.1-6 alkylthio, halogen, cyano, hydroxy, carbamoyl, carboxy, C.sub.1-6 alkanoyl or trifluoromethyl;m is 1 to 3;p is 0 to 4;R.sup.3 is COR.sup.4 ;R.sup.4 is hydroxy, C.sub.1-6 alkoxy, or NR.sup.5 R.sup.6 ;R.sup.5 and R.sup.6 are each hydrogen or C.sub.1-6 alkyl or together with the nitrogen atom to which they are attached form a heterocyclic ring; andR.sup.7 is hydrogen, C.sub.1-6 alkoxy or C.sub.1-6 alkyl;or a salt thereof.Type: GrantFiled: February 23, 1989Date of Patent: February 18, 1992Assignee: SmithKline Beckman Intercredit B.V.Inventors: Robert J. Ife, Thomas H. Brown, Colin A. Leach
-
Patent number: 5089498Abstract: Substituted 4-aminiquinazoline derivatives of the formula: ##STR1## in which R.sup.1 hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkoxyC.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, C.sub.3-6 cycloalkylC.sub.1-6 alkyl, phenylC.sub.1-6 alkyl, the phenyl group being optionally substituted;R.sup.2 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, amino, C.sub.1-6 alkylthio, halogen, cyano, hydroxy, carbamoyl, carboxy, C.sub.1-6 alkanoyl or trifluromethyl;m is 1 to 3;p is 0 to 4;R.sup.3 is COR.sup.4 ;R.sup.4 is hydroxy, C.sub.1-6 alkoxy, or NR.sup.5 R.sup.6 ;R.sup.5 and R.sup.6 are each hydrogen or C.sub.1-6 alkyl or together with the nitrogen atom to which they are attached form a heterocyclic ring; andR.sup.7 is hydrogen, C.sub.1-6 alkoxy or C.sub.1-6 alkyl;or a salt thereof.Type: GrantFiled: February 23, 1989Date of Patent: February 18, 1992Assignee: SmithKline Beckman Intercredit B.V.Inventors: Robert J. Ife, Thomas H. Brown, Colin A. Leach
-
Patent number: 5082841Abstract: Aminoquinoline derivatives are described as inhibitors of the H.sup.+ K.sup.+ ATPase enzyme useful in the treatment of gastric acidity. A compound of the invention is 3-butyryl-4-(2-methylphenylamino)-8-(3-dimethylaminopropoxy)quinoline.Type: GrantFiled: August 7, 1990Date of Patent: January 21, 1992Assignee: SmithKline Beecham Intercredit B.V.Inventors: Thomas H. Brown, Robert J. Ife, Colin A. Leach
-
Patent number: 5082848Abstract: Substituted 4-aminoquinoline derivatives of the formula: ##STR1## wherein R.sup.1 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxyC.sub.1-6 alkyl; C.sub.3-6 cycloalkyl, C.sub.3-6 cycloalkyl-C.sub.1-6 alkyl, phenyl C.sub.1-6 alkyl, the phenyl groups being optionally substituted;R.sup.2 is hydroxy C.sub.1-6 alkyl, C.sub.1-6 alkoxyC.sub.1-6 alkyl or two adjacent groups R.sup.2 together form a C.sub.1-4 alkylenedioxy group;R.sup.3 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, amino, C.sub.1-6 alkylthio, halogen, cyano, hydroxy, C1-6alkanoyl, or trifluromethyl;R.sup.4 is hydrogen, C.sub.1-6 alkyl, phenyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, C.sub.1-6 alkanoyl, amino, C.sub.1-6 alkylamino, di- C.sub.1-6 alkyl amino, halogen, or trifluromethyl;n is 1 or 2;q is 0 to 4;m is 1, 2, or 3; andp is 1, 2, 3, or 4 provided that m+p is not greater than 5;or a salt thereof are useful as inhibitors of gastric acid secretion.Type: GrantFiled: February 23, 1989Date of Patent: January 21, 1992Assignee: Smith Kline & French Laboratories, Ltd.Inventors: Robert J. Ife, Thomas H. Brown, Colin A. Leach
-
Patent number: 5049567Abstract: Substituted 4-aminoquinazoline derivatives which are inhibitors of gastric acid secretion. A compound of the invention is ethyl 8-methoxy-4-(4-methyl-3-thinenylamino)quinoline-3-carboxylate.Type: GrantFiled: January 9, 1991Date of Patent: September 17, 1991Assignee: SmithKline Beckman Intercredit B.V.Inventors: Robert J. Ife, Thomas H. Brown, Colin A. Leach
-
Patent number: 5026711Abstract: Compounds represented by the general formula: ##STR1## in which R.sub.1 and R.sub.2 are selected from hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.2 -C.sub.6 alkenyl , phenyl or benzyl or R.sub.1 and R.sub.2 form together with the nitrogen atom to which they are attached a C.sub.4 -C.sub.8 saturated heterocycle, R.sub.3 is selected from hydrogen, C.sub.1 -C.sub.6 alkyl, phenyl or C.sub.7 -C.sub.9 phenyl-alkyl, R.sub.4 is selected from hydrogen or C.sub.1 -C.sub.4 alkyl, R.sub.5 and R.sub.6 are selected from hydrogen or halogen, C.sub.1 -C.sub.3 or alkoxy, nitro or trifluoromethyl; Z is selected from OH, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.4 alkyl, benzyl, C.sub.4 -C.sub.6 aryl with or without a heteroatom, or NR.sub.8 R.sub.9, R.sub.8 and R.sub.9 being selected from hydrogen, C.sub.1 -C.sub.4 alkyl, phenyl or benzyl; R.sub.10 is selected from hydrogen, C.sub.1 -C.sub.Type: GrantFiled: June 6, 1989Date of Patent: June 25, 1991Assignee: SanofiInventors: Etienne Mendes, Jean-Claude Vernieres, Peter E. Keane, Andre Bachy
-
Patent number: 5026700Abstract: The present invention is directed to a new class of excitatory amino acid antagonists. The compounds contain quinoline or thieno pyridine moieties.Type: GrantFiled: March 21, 1990Date of Patent: June 25, 1991Assignee: Merrell Dow PharmaceuticalsInventors: Boyd L. Harrison, Bruce M. Baron
-
Patent number: 5017583Abstract: Compounds of the Formula I: ##STR1## and pharmaceutically acceptable salts thereof are leukotriene antagonists. These compounds inhibit SRS-A and leukotriene synthesis and are antagonists of SRS-A and are thus useful in the treatment of asthma, allergic disorders, inflammation, skin diseases and certain cardiovascular disorders.Type: GrantFiled: February 23, 1988Date of Patent: May 21, 1991Assignee: Merck Frosst Canada, Inc.Inventors: Robert N. Young, Joshua Rokach, Haydn R. Williams, Masatoshi Kakushima, Yvan Guindon
-
Patent number: 5010087Abstract: Novel tricyclic compounds having a TXA.sub.2 -antagonizing activity represented by formula (I): ##STR1## which strongly antagonize an action of thromboxane A.sub.2 and are expected to have preventive and therapeutic effects on ischemica diseases, cerebro-vascular diseases, etc.Type: GrantFiled: July 18, 1989Date of Patent: April 23, 1991Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Etsuo Oshima, Hiroyuki Obase, Akira Karasawa, Kazuhiro Kubo, Ichiro Miki, Akio Ishii
-
Patent number: 5010198Abstract: Benzoxazol- and benzothiazolamine derivatives having anti-anoxic properties which compounds are useful in the treatment of anoxia. These compounds are produced from certain benzoxazol- and benzothizolamine intermediates.Type: GrantFiled: August 24, 1989Date of Patent: April 23, 1991Assignee: Janssen Pharmaceutica N.V.Inventors: Raymond A. Stokbroekx, Marcel G. M. Luyckx, Frans E. Janssens
-
Patent number: 5008276Abstract: 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 17, 1988Date of Patent: April 16, 1991Assignee: Imperial Chemical Industries PLCInventors: John M. Clough, Christopher R. A. Godfrey, Stephen P. Heaney, Kenneth Anderton
-
Patent number: 4977160Abstract: 7- or 8-Substituted, partially hydrogenated pyrazolo[3,4-g]quinoline, thiazolo[4,5-g]quinoline, oxazolo[4,5-g]quinoline, and pyrrolo[3,4-g]quinoline derivatives, and 8- or 9-substituted, partially hydrogenated pyrido[2,3-g]quinazoline derivatives are D-2 dopamine agonists. 6-Oxo-1-substituted-octahydroquinolines and 6-oxo-1-substituted-decahydroquinolines which are additionally substituted in the 3- or 4-position are intermediates useful in preparation of the dopamine agonists. Acetals of 4,6-dioxo-1-substituted-decahydroquinoline 3-carboxylic acid esters enable synthesis of the foregoing compounds.Type: GrantFiled: February 16, 1989Date of Patent: December 11, 1990Assignee: Eli Lilly and CompanyInventors: Diane L. Huser, John M. Schaus
-
Patent number: 4968702Abstract: Substituted quinolinecarboxylic acids useful in the treatment of arthritis by inhibiting the progressive joint deterioration characteristic of arthritic disease and for inducing immunosuppression are disclosed. Methods of synthesis and use of the novel compounds are also disclosed.Type: GrantFiled: January 17, 1989Date of Patent: November 6, 1990Assignee: American Cyanamid CompanyInventors: John F. Poletto, Dennis W. Powell, Diane H. Boschelli
-
Patent number: 4960779Abstract: Pyrrole derivatives of formula (I): ##STR1## in which A forms with the pyrrole ring an isoindoline, 6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine, 2,3,6,7-tetrahydro-5H-[1,4]oxathiino[2,3-c]pyrrole or 2,3,6,7-tetrahydro-5H-[1,4]dithiino[2,3-c]pyrrole ring-system, Het.dbd.naphthyridinyl, pyridyl or quinolyl which are unsubstituted or substituted with halogen, (1 to 4 C) alkyl, (1 to 4 C) alkyloxy, (1 to 4 C) alkylthio or CF.sub.3, Y.dbd.CO, C.dbd.NOH or CHOH and R.dbd.(3 to 10 C) alkenyl, alkyl which is unsubstituted or substituted with OH, alkyloxy, alkylthio, (3 to 6 C) cycloalkyl, NH.sub.2, alkylamino, dialkylamino, alkylcarbonylamino, piperazinyl, piperidyl, 1-azetidinyl, morpholino, pyrrolidinyl, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, (1-piperazinyl)carbonyl, piperidinocarbonyl, pyrrolidinocarbonyl, phenyl, pyridyl, 1-imidazolyl or alternatively R.dbd.Type: GrantFiled: June 1, 1989Date of Patent: October 2, 1990Assignee: Rhone-Poulenc SanteInventors: Jean-Dominique Bourzat, Marc Capet, Claude Cotrel, Richard Labaudiniere, Philippe Pitchen, Gerard Roussel
-
Patent number: 4952589Abstract: This invention relates to aminoalkylphenoxyalkyl substituted heterocycles. These compounds antagonize the action of histamine on histamine H.sub.2 -receptors in the brain. A compound of the invention is 2-[3-[3-(piperidinomethyl)phenoxy]propylamino]benzthiazole.Type: GrantFiled: June 3, 1987Date of Patent: August 28, 1990Assignee: Smith Kline & French Laboratories LimitedInventors: Thomas H. Brown, Robert C. Mitchell, Ian R. Smith, Rodney C. Young
-
Patent number: 4916135Abstract: There are described compounds of the formula ##STR1## where --R is ##STR2## --R.sub.3 and R.sub.3 being independently --H, loweralkyl, --CHO, --CH.dbd.CH.sub.2, --CH.dbd.CH--loweralkyl, --CH.dbd.CHCO.sub.2 C.sub.2 H.sub.5, --CH.sub.2 N(C.sub.2 H.sub.5).sub.2 or ##STR3## --R.sub.1 when existent is --H, loweralkyl, --CH.sub.2 C.tbd.CH, ##STR4## R.sub.5 being methyl or phenyl optionally mono-substituted with loweralkyl or loweralkoxy;--R.sub.2 when existent is loweralkyl or --CH.sub.2 C.tbd.CH;--X is --H, loweralkyl, loweralkoxy, halogen or trifluoromethyl; and the two --Y groups when existent are both --H, or combine to constitute --(CH.sub.2).sub.4 --;which compounds are useful as analgesic agents, and for treating various memory dysfunctions characterized by decreased cholinergic function such as Alzheimer's disease.Type: GrantFiled: May 8, 1989Date of Patent: April 10, 1990Assignee: Hoechst Roussel Pharmaceuticals Inc.Inventors: Richard C. Effland, Joseph T. Klein, Larry Davis, Gordon E. Olsen
-
Patent number: 4908056Abstract: This invention relates to novel heterocyclic carbonyl sulfonamides which are particularly useful as agricultural chemicals.Type: GrantFiled: February 17, 1989Date of Patent: March 13, 1990Assignee: E. I. Du Pont De Nemours and CompanyInventor: Chi-Ping Tseng
-
Patent number: 4906643Abstract: N-(3-hydroxy-4-piperidinyl)substituted benzamides, their N-oxide forms and pharmaceutically acceptable acid-addition salts having gastrointestinal motility stimulating properties, compositions containing the same, and methods of treating warm blooded animals suffering from a decreased peristalsis of the gastrointestinal system.Type: GrantFiled: June 10, 1988Date of Patent: March 6, 1990Assignee: Janssen Pharmaceutica N.V.Inventors: Georges H. P. Van Daele, Freddy F. Vlaeminck, Karel J. Van Loon
-
Patent number: 4889953Abstract: Compounds of the formula: ##STR1## wherein R.sup.1 is a higher alkyl group which may be substituted; R.sup.2 is a hydrogen, a lower alkyl group which may be substituted, a lower alkanoyl group which may be substituted or a lower alkylthiocarbamoyl group; R.sup.3 is a primary to tertiary amino group or a quaternary ammonium group; and n is 2 or 3, and salts thereof, have antitumor activity and platelet activating factor inhibitory activity.Type: GrantFiled: July 22, 1987Date of Patent: December 26, 1989Assignee: Takeda Chemical Industries, Ltd.Inventors: Keizo Inoue, Hiroaki Nomura, Tetsuya Okutani
-
Patent number: 4886803Abstract: Compounds are described of formula (I) ##STR1## wherein R.sup.1 is a hydrogen atom, an alkyl group, an alkoxy group, a dialkylamino group or a halogen atom; n is 1 to 4; R.sup.2 is a hydrogen atom, an alkyl group, an unsubstituted or substituted aminoalkyl group, an acyl group, an unsubstituted or substituted aralkyl group, a carboxyalkyl group, an alkoxycarbonyalkyl group or ##STR2## wherein X is an unsubstituted or substituted-phenyl, -benzyl, -benzoyl or -furoyl group; A is -NR.sup.3 - where R.sup.3 is hydrogen or alkyl, an alkylene or an alkylidene; and B is a heterocyclic group selected from triazolyl, pyridyl, pyridazinyl, pyrimidinyl, pyrazinyl, benzimidazolyl, benzothiazolyl, quinolyl and isoquinolyl, said heterocyclic group being optionally substituted by one or more alkyl, alkoxy, nitro or phenyl group, and the physiologically acceptable acid addition salts thereof. The compound of formula (I) are or cardiotonic activity and thus may be useful for the treatment of circulatory diseases.Type: GrantFiled: July 15, 1987Date of Patent: December 12, 1989Assignee: Nisshin Flour Milling Co., Ltd.Inventors: Noriyoshi Sueda, Yoshikuni Suzuki, Toshiji Sugai, Hiroaki Yamada, Makoto Yanai
-
Patent number: 4880818Abstract: There are disclosed compounds of the formula ##STR1## where X,Y are each independently hydrogen, loweralkyl, loweralkoxy, hydroxy, halogen, trifluoromethyl or nitro; R.sub.1 is hydrogen or loweralkyl; R.sub.2 ' is hydrogen or loweralkyl and R.sub.4 is hydrogen, loweralkyl or aryl, which are useful as hypotensive agents and as intermediates.Type: GrantFiled: July 12, 1988Date of Patent: November 14, 1989Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Karl Schonafinger, Helen Hu Ong
-
Patent number: 4874864Abstract: Compounds of the formula ##STR1## where HET is a heterocyclic group, n is an integer of 0 to 2 and R.sup.1 is hydrogen or lower alkyl are protease inhibitors use as anti-plasmin and anti-thrombin agents.Type: GrantFiled: May 24, 1988Date of Patent: October 17, 1989Assignee: Pfizer Inc.Inventors: Rodney C. Schnur, Anton F. J. Fliri
-
Patent number: 4874759Abstract: Hydroxyindole-3-carboxylic acid amide compounds of the general formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are, the same or different, respectively a hydrogen atom, an alkyl group, an aryl group, an aralkyl group or a heteroaryl group, or R.sup.1 and R.sup.2 and/or R.sup.3 and R.sup.4 are respectively groups which are combined to each other taken together with the adjacent nitrogen atom to form a heterocyclic group, R.sup.5 is an alkyl group, R.sup.6 is a hydrogen atom, an alkyl group, a cycloalkyl group, an aryl group or an aralkyl group and X is a hydrogen atom, a halogen atom or a lower alkanoyl group, or their acid addition salts.These compounds are of use as diuretics or a therapeutic medicine for circulation system diseases.Type: GrantFiled: September 23, 1988Date of Patent: October 17, 1989Assignee: Yoshitomi Pharmaceutical Industries, Ltd.Inventors: Tetsuya Tahara, Tsuguo Ikebe, Ichiro Hakamada, Osamu Yaoka
-
Patent number: 4866075Abstract: The invention concerns compounds of formula: ##STR1## wherein R.sub.1 is hydrogen, lower alkyl, halogen, lower alkoxy or hydroxy; R.sub.2 represents hydrogen or lower alkyl; A represents an alkylene, oxoalkylene or hydoxyalkylene chain each having 2 to 6 carbon atoms, R.sub.3 and R.sub.4 may be in the same or different rings and independently represent hydrogen, lower alkyl, lower alkoxy, amino or halogen and one of X and Y represents nitrogen the other represents CR.sub.5 wherein R.sub.5 is one of the values for R.sub.3 or R.sub.5 is the bond to the NHCO group; or a pharmaceutically acceptable salt thereof, which compounds possess antihypertensive activity whilst exhibiting reduced CNS depressant properties. Also disclosed are processes for preparing the compounds and pharmaceutical compositions containing them.Type: GrantFiled: August 12, 1988Date of Patent: September 12, 1989Assignee: John Wyeth and Brother LimitedInventors: John L. Archibald, Terence J. Ward, Janet C. White
-
Patent number: 4861785Abstract: Benzoxazol-and benzothiazolamine derivatives having anti-anoxic properties which compounds are useful in the treatment of anoxia.Type: GrantFiled: October 11, 1985Date of Patent: August 29, 1989Assignee: Janssen Pharmaceutica N.V.Inventors: Raymond A. Stokbroekx, Marcel G. M. Luyckx, Frans E. Janssens
-
Patent number: 4853400Abstract: Compounds of any one of formulae I-VII ##STR1## where is a single or double bond;A is oxygen or sulphurR.sup.1 is aryl;R.sup.2 is 1-imidazolyl or 1,2,4-triazol-1-yl andR.sup.3, R.sup.4, R.sup.5 and R.sup.6, which may be the same or different, are each hydrogen, halo, alkyl or alkoxy, have fungicidal activity.Type: GrantFiled: May 16, 1988Date of Patent: August 1, 1989Assignee: Schering Agrochemicals LimitedInventors: John H. Parsons, Russell G. Hunt, Susan E. Leach, Anthony D. Buss, David E. Green, Michael Mellor, Albert Percival
-
Patent number: 4851409Abstract: Compounds having the formula: ##STR1## are antagonists of leukotrienes and inhibitors of their biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents.Type: GrantFiled: February 5, 1987Date of Patent: July 25, 1989Assignee: Merck Frosst Canada Inc.Inventors: Robert N. Young, Robert Zamboni, Serge Leger
-
Patent number: 4839367Abstract: Provided are antihypertensive compounds of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, and R.sub.6 are hydrogen, alkyl, alkenyl, alkynyl, phenyl-alkyl, or cycloalkyl, and may be the same or different,m is an integer from 0 to 2 inclusive,n is an integer from 0 to 4 inclusive,M is alkyl, alkynyl, cycloalkyl, cycloalkyl-alkyl, polycycloalkyl, polycycloalkyl-alkyl, aryl, aralkyl, heteroaryl, heteroaryl-alkyl, hetero-cycloalkyl, hetero-cycloalkyl-alkyl, fused aryl-cycloalkyl, fused aryl-cycloalkyl-alkyl, fused heteroaryl-cycloalkyl, fused heteroaryl-cycloalkyl-alkyl, alkoxyalkyl, alkylthioalkyl, alkylamino-alkyl, or dialkylaminoalkyl,Y is hydroxy, alkoxy, amino, or substituted amino, aminoalkanoyl, aryloxy, aminoalkoxy, or hydroxyalkoxy, andR.sub.7 is alkyl, aryl, aralkyl, cycloalkyl, cycloalkyl-alkyl, heterocyclic, --CO--SR, --CS--SR, ##STR2## CH.sub.2 CO.sub.R, --CHM--CO.sub.2 R, --CH.sub.2 --CO--SR, --CN, ##STR3## --CO--NH--CH.sub.2 CO.sub.2 R, ##STR4## or --CO--CO.sub.2 CO.sub.Type: GrantFiled: August 11, 1986Date of Patent: June 13, 1989Assignee: Rorer Pharmaceutical CorporationInventors: Raymond D. Youssefyeh, Howard Jones
-
Patent number: 4826986Abstract: 7- or 8-Substituted, partially hydrogenated pyrazolo[3,4-g]quinoline, thiazolo[4,5-g]quinoline, oxazolo[4,5-g]quinoline, and pyrrolo[3,4-g]quinoline derivatives, and 8- or 9-substituted, partially hydrogenated pyrido[2,3-g]quinazoline derivatives are D-2 dopamine agonists. 6-Oxo-1-substituted-octahydroquinolines and 6-oxo-1-substituted-decahydroquinolines which are additionally substituted in the 3- or 4-position are intermediates useful in preparation of the dopamine agonists. Acetals of 4,6-dioxo-1-substituted-decahydroquinoline 3-carboxylic acid esters enable synthesis of the foregoing compounds.Type: GrantFiled: June 16, 1986Date of Patent: May 2, 1989Assignee: Eli Lilly and CompanyInventors: Diane L. Huser, John M. Schaus
-
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
-
Patent number: 4806549Abstract: This invention relates to novel substituted 4-aminoquinoline derivatives which are inhibitors of gastric acid secretion in mammals. A compound of the invention is 3-butyryl-4-(2-methylphenylamino)-8-methoxyquinoline.Type: GrantFiled: September 3, 1987Date of Patent: February 21, 1989Assignee: Smith Kline & French Laboratories LimitedInventors: Robert J. Ife, Thomas H. Brown, Colin A. Leach
-
Patent number: 4806540Abstract: Novel microbicidally active 1-heteroaryl-4-arylpyrazole derivatives of the formulae (I) and/or (1A) ##STR1## in which R represents hydrogen or alkyl,R.sup.1 represents halogen, hydroxyl, optionally substituted alkyl, optionally substituted alkoxy, a radical --S(O).sub.p -alkyl which is optionally substituted in the alkyl part, nitro or optionally substituted amino, or represents a fused-on carbocyclic or heterocyclic radicalp represents the integer 0, 1 or 2,n represents an integer from 0 to 5,X represents .dbd.CH--, or represents a nitrogen atom,Y represents CO or SO.sub.2 andR.sup.2 represents hydrogen, in each case optionaly substituted alkyl, cycloalkyl or aryl or a heterocyclic radical, or represents OR.sup.3, or also represents SR.sup.3, if Y is CO,whereinR.sup.3 represents optionally substituted alkyl or aryl, orR.sup.2 represents a radical ##STR2## wherein R.sup.Type: GrantFiled: September 23, 1987Date of Patent: February 21, 1989Assignee: Bayer AktiengesellschaftInventors: Klaus Sasse, Gerd Hanssler, Hans-Georg Schmitt, Wilfried Paulus
-
Patent number: 4806550Abstract: This invention relates to novel substituted 4-aminoquinoline derivatives which are inhibitors of gastric acid secretion in mammals. A compound of the invention is 3-butyryl-4-(2-methylphenylamino)-8-methoxyquinoline.Type: GrantFiled: May 12, 1988Date of Patent: February 21, 1989Assignee: SmithKline & French Laboratories LimitedInventors: Robert J. Ife, Thomas H. Brown, Colin A. Leach
-
Patent number: 4803225Abstract: There are provided compounds of formula I, ##STR1## and pharmaceutically acceptable derivatives thereof. There are also described the use of the compounds of formula I as pharmaceuticals, methods for making the compounds and pharmaceutical, e.g. cardiac, compositions containing the compounds.Type: GrantFiled: December 2, 1987Date of Patent: February 7, 1989Assignee: Fisons, plcInventors: John Dixon, Francis Ince
-
Patent number: 4788188Abstract: The present invention relates to new quinolylglycinamide derivatives corresponding to the following general formula: ##STR1## The invention also relates to a process for preparing these compounds and their therapeutic application as a psychotropic agent.Type: GrantFiled: May 6, 1986Date of Patent: November 29, 1988Assignee: Sanofi (S.A.)Inventors: Jean-Claude Vernieres, Etienne Mendes, Michel Morre, Peter Keane, Jacques Simiand
-
Patent number: 4786646Abstract: The invention relates to compounds of the formula ##STR1## Y is O or S, *A is paraphenylene or *--(CH.sub.2).sub.n --(X).sub.m --(CH.sub.2).sub.r --, X is O, S or --CH.dbd.CH--, n or r, independently, are integers from 0 to 3, s is an integer from 0 to 1, m is an integer from 0 to 1, provided that when m is 1, n+s must be at least 2, R.sub.1 and R.sub.2, independently, are hydrogen, lower alkyl, cycloalkyl, lower alkenyl, Het or aryl, *E is ##STR2## or --(CH.sub.2).sub.k -- wherein k is an integer from 0 to 4, R.sub.3, R.sub.4 and R.sub.8 are independently hydrogen or lower alkyl, R.sub.5 and R.sub.6, independently are hydrogen or lower alkyl, R.sub.Type: GrantFiled: July 10, 1987Date of Patent: November 22, 1988Assignee: Hoffmann-La Roche Inc.Inventors: Robert W. Guthrie, Richard W. Kierstead, Jefferson W. Tilley
-
Patent number: 4772613Abstract: Compounds of any of one of formulae I-VII ##STR1## where is a single or double bond;A is oxygen or sulphur;R.sup.1 is aryl;R.sup.2 is 1-imidazolyl or 1,2,4-triazol-1-yl; andR.sup.3, R.sup.4, R.sup.5 and R.sup.6, which may be the same or different, are each hydrogen, halo, alkyl or alkoxy, have fungicidal activity.Type: GrantFiled: May 26, 1987Date of Patent: September 20, 1988Assignee: Schering Agrochemicals Ltd.Inventors: John H. Parsons, Russell G. Hunt, Susan E. Leach, Anthony D. Buss, David E. Green, Michael Mellor, Albert Percival
-
Patent number: 4771052Abstract: There are disclosed compounds of the formula ##STR1## where X and Y are independently hydrogen, loweralkyl, loweralkoxy, hydroxy, halogen, trifluoromethyl or nitro; R.sub.1 is hydrogen or loweralkyl; R.sub.2 is hydrogen, loweralkyl, loweralkylcarbonyl or arylcarbonyl; and R.sub.3 is hydrogen, loweralkyl, arylloweralkyl, ##STR2## loweralkylcarbonyl or arylcarbonyl, n being an interger of 1 to 6 inclusive and Z being hydrogen, loweralkyl, loweralkoxy, hydroxy or halogen; which are useful as hypotensive agents.Type: GrantFiled: February 5, 1987Date of Patent: September 13, 1988Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Karl Schonafinger, Helen H. Ong
-
Patent number: 4749698Abstract: Compounds having the general structure ##STR1## and their pharmaceutically acceptable salts, wherein the substituents are defined herein, which exhibit antihypertensive activity.Type: GrantFiled: July 8, 1985Date of Patent: June 7, 1988Assignee: Rorer Pharmaceutical CorporationInventors: Edward S. Neiss, John T. Suh, John R. Regan, Jerry W. Skiles, Jeffrey N. Barton, James J. Mencel, Paul Menard
-
Patent number: 4720586Abstract: There are provided compounds of formula I, ##STR1## in which R.sub.1 represents OH,R.sub.2 and R.sub.3, which may be the same or different, each independently represent hydrogen, fluorine, chlorine, bromine, alkyl C1 to 6, nitro, nitrile, (CH.sub.2).sub.p R.sub.9 or SR.sub.9,W represents a single bond, a 1,2; 1,3; or 1,4-disubstituted benzene ring; a --CH.dbd.CH--group or a 1,4-cyclohexanediyl group;X respresents NH, O, S, SO.sub.2, CO, CH.sub.2, CONH or --COO;Y represents (CH.sub.2)q, CO, CS, SO.sub.2 and R.sub.20 represents hydrogen,or Y represents CR.sub.15 R.sub.16 CR.sub.17 R.sub.18,wherein the carbon atom bearing R.sub.15 and R.sub.16 is adjacent to X and in whichR.sub.15 and R.sub.18, together with the carbon atom to which they are attached form a carbonyl group, and R.sub.15, R.sub.16 and R.sub.20 each represent hydrogen, orR.sub.15 and R.sub.20 together form a chain --CH.sub.2 --, and R.sub.16, R.sub.17 and R.sub.18 each represent hydrogen, orR.sub.15, R.sub.16, R.sub.17 and R.sub.Type: GrantFiled: October 18, 1984Date of Patent: January 19, 1988Assignee: Fisons, plcInventors: John Dixon, Francis Ince
-
Patent number: 4696939Abstract: Compounds of the formula ##STR1## and their pharmaceutically acceptable salts, wherein the substituents are as defined herein, having antihypertensive activity.Type: GrantFiled: November 29, 1985Date of Patent: September 29, 1987Assignee: USV Pharmaceutical CorporationInventors: John T. Suh, John J. Piwinski, Howard Jones, Edward S. Neiss
-
Patent number: 4677210Abstract: Z is a chemical bond or an alkylene chain containing up to 5 carbons in the principal chain and up to a total of 7 carbons;X is O or S;R and R.sub.1 are independently hydrogen, hydroxy, lower alkoxy, lower alkanoyloxy, halo, cyano, carboloweralkoxy, carboxyloweralkyl, aryloxy or benzyloxy;R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are independently hydrogen, lower alkyl, lower aralkyl, lower alkenyl, lower alkynyl, aryl or carboxyloweralkyl;and pharmaceutically acceptable salts thereof have pharmaceutical activity, particularly as lipoxygenase inhibitors possessing anti-inflammatory and anti-allergic properties.Type: GrantFiled: June 19, 1985Date of Patent: June 30, 1987Assignee: Rorer Pharmaceutical CorporationInventor: Fu-chih Huang
-
Patent number: 4675405Abstract: There are disclosed compounds of the formula ##STR1## wherein X is ##STR2## W is --O--, --S--, ##STR3## when n=0, or W is ##STR4## when n=1, and the dotted line represents an optional double bond; Y is --CH.sub.2 O--, --OCH.sub.2 --, --CH.sub.2 S--, --SCH.sub.2 --, ##STR5## n is 0-1; R.sup.1 is hydrogen, loweralkyl, loweralkoxy, lower alkanoyl, halo, trifluoromethyl, cyano or nitro;R.sup.2 is hydrogen or loweralkyl;R.sup.3 is loweralkyl, perfluoroloweralkyl or perfluorophenyl, with the proviso that when X=N, W=O or S and n=0, R.sup.3 is other than loweralkyl;and the pharmaceutically acceptable salts thereof, and their use in the treatment of leukotriene-mediated naso-bronchial obstructive airpassageway conditions, such as allergic rhinitis, allergic bronchial asthma and the like, and in antithrombotic therapy.Type: GrantFiled: January 27, 1986Date of Patent: June 23, 1987Assignee: American Home Products CorporationInventors: John H. Musser, Dennis M. Kubrak, Anthony F. Kreft, III
-
Patent number: 4663334Abstract: Heterocyclic acetylenes of the formula (I): ##STR1## wherein Y is alkyl, alkoxy, alkoxyalkyl, chloro, fluoro, bromo or carboxamidoalkyl and R.sup.1 is hydrogen, alkyl, alkoxy, alkylthio, alkoxycarbonyl, chloro, fluoro or dialkylamino, m is 0-2, R.sup.2 is branched alkyl and Het is an aromatic heterocycle. The acetylenes are useful in treating hypertension and/or angina.Type: GrantFiled: December 11, 1985Date of Patent: May 5, 1987Assignee: McNeilab, Inc.Inventor: John R. Carson
-
Patent number: 4659720Abstract: 5-Amino or substituted amino imidazoles are disclosed as having anticoccidial activity. The compounds are useful for controlling cecal and or intestinal coccidiosis when administered in minor quantitites to animals, in particular to poultry, usually in admixture with animal sustenance.Type: GrantFiled: November 16, 1983Date of Patent: April 21, 1987Assignee: Merck & Co., Inc.Inventors: John C. Chabala, Michael H. Fisher, Arthur A. Patchett
-
Patent number: 4647565Abstract: Dihydropyridines of the formulae ##STR1## wherein R is chlorothienyl or mono- or disubstituted phenyl where said substituent is fluoro, chloro, bromo or trifluoromethyl; R.sup.1 and R.sup.2 are each alykl; R.sup.3 and R.sup.4 when taken separately are each hydrogen or alkyl; R.sup.3 and R.sup.4 when taken together with the nitrogen to which they are attached are piperidine or pyrrolidine; R.sup.5 is alkyl or 2-hydroxyethyl; R.sup.6 is hydrogen or methoxy; X and Z are each hydrogen or methoxy; Y is alkylene; R.sup.7 is chlorophenyl or trifluoromethyl-chlorophenyl; p is 0 or 1; and Q is CH or N are useful in the treatment of hypertension, heart failure and angina.Type: GrantFiled: June 5, 1985Date of Patent: March 3, 1987Assignee: Pfizer Inc.Inventors: John E. Arrowsmith, Simon F. Campbell, Peter E. Cross, Roger P. Dickinson
-
Patent number: 4642308Abstract: The invention provides novel substituted amides of formula:R--CONH--Hetin which R is cycloalkyl, cyclohexadienyl, phenyl optionally substituted with one or 2 fluorine atoms or with a hydroxy radical, or substituted at position 3- or 4- with an alkyl or alkyloxy radical, or with a methylenedioxy radical at positions 3- and 4-, or at position 2- or 3- with a dialkylamino radical, or is 3-pyridyl, alkyloxy-3-pyridyl, thienyl, alkylthienyl, furyl, tetrahydropyridyl, pyridazinyl and alkylpyridazinyl, and Het is 2-quinolyl or 1,8-naphthyridin-2-yl, both optionally substituted at position 7- with a halogen atom or a hydroxymethyl, alkyl, alkyloxy, alkyloxyalkyloxy, alkenyloxy or alkynyloxy radical (of 3 or 4 carbon atoms), an alkylthio or benzylthio radical, a phenoxy radical which is optionally substituted (with fluorine, with chlorine or bromine at position 2-, or with an alkyloxy radical or 1 or 2 alkyl radicals) or with pyridyloxy or alkylpiperidyloxy, provided that, when Het is 2-quinolyl, R is other than phenyType: GrantFiled: July 17, 1985Date of Patent: February 10, 1987Assignee: Rhone-Poulenc SanteInventors: Claude Cotrel, Claude Guyon, Gerard Roussel, Gerard Taurand
-
Patent number: 4631343Abstract: 5-Cyano-1-substituted-1H-pyrazole-4-carboxylic acids and esters useful as intermediates to the corresponding 4-carboxyamide derivatives having herbicidal and algicidal activity.Type: GrantFiled: September 13, 1984Date of Patent: December 23, 1986Assignee: Eli Lilly and CompanyInventor: James R. Beck
-
Patent number: 4622330Abstract: Novel 3-amino or substituted amino pyrazoles are disclosed as having antiprotozoal and antiparasitic activity in particular anticoccidial activity and are useful for controlling cecal and or intestinal coccidiosis when administered in minor quantities to animals, in particular to poultry usually in admixture with animal sustenance.Type: GrantFiled: June 19, 1984Date of Patent: November 11, 1986Assignee: Merck & Co., Inc.Inventors: Richard J. Bochis, Richard A. Dybas, Edward F. Rogers
-
Patent number: 4620865Abstract: 1,5-Disubstituted-1H-pyrazole-4-carboxamide derivatives, useful as herbicides and aquatic algicides.Type: GrantFiled: February 24, 1986Date of Patent: November 4, 1986Assignee: Eli Lilly and CompanyInventors: James R. Beck, Michael P. Lynch