Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Carbocyclic Ring Patents (Class 546/161)
  • Patent number: 5091392
    Abstract: A quinolin-2-yl-methoxy)phenylacyl-sulphonamide or -cyanamide of the formula ##STR1## in which A, B, D, E, F and G are identical or different andrepresent hydrogen, hydroxyl, halogen, carboxyl, nitro, trifluoromethyl, trifluoromethoxy or a group of the formula --NH.sup.3 R.sup.4, in whichR.sup.3 and R.sup.4 are identical or different and denote hydrogen, straight-chain or branched alkyl having up to 8 carbon atoms or aryl having 6 to 10 carbon atoms,represent straight-chain or branched alkyl, alkoxy or alkoxycarbonyl in each case having up to 12 carbon atoms,represent aryl having 6 to 10 carbon atoms,R.sup.1 represents cycloalkyl having 3 to 8 carbon atoms,R.sup.2 represents hydrogen orstraight-chain or branched alkyl having up to 10 carbon atoms,represents an alkali metal,represents cycloalkyl having 3 to 8 carbon atoms,X represents a group of the formula --SO.sub.2 --R.sup.5, in whichR.sup.
    Type: Grant
    Filed: May 1, 1990
    Date of Patent: February 25, 1992
    Assignee: Bayer Aktiengesellschaft
    Inventors: Siegfried Raddatz, Klaus-Helmut Mohrs, Romanis Fruchtmann, Christian Kohlsdorfer, Pia Theisen-Popp, Reiner Muller-Peddinghaus
  • Patent number: 5089504
    Abstract: 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: Grant
    Filed: February 23, 1989
    Date of Patent: February 18, 1992
    Assignee: SmithKline Beckman Intercredit B.V.
    Inventors: Robert J. Ife, Thomas H. Brown, Colin A. Leach
  • Patent number: 5089498
    Abstract: 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: Grant
    Filed: February 23, 1989
    Date of Patent: February 18, 1992
    Assignee: SmithKline Beckman Intercredit B.V.
    Inventors: Robert J. Ife, Thomas H. Brown, Colin A. Leach
  • Patent number: 5082848
    Abstract: 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: Grant
    Filed: February 23, 1989
    Date of Patent: January 21, 1992
    Assignee: Smith Kline & French Laboratories, Ltd.
    Inventors: Robert J. Ife, Thomas H. Brown, Colin A. Leach
  • Patent number: 5082841
    Abstract: 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: Grant
    Filed: August 7, 1990
    Date of Patent: January 21, 1992
    Assignee: SmithKline Beecham Intercredit B.V.
    Inventors: Thomas H. Brown, Robert J. Ife, Colin A. Leach
  • Patent number: 5008276
    Abstract: 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: Grant
    Filed: October 17, 1988
    Date of Patent: April 16, 1991
    Assignee: Imperial Chemical Industries PLC
    Inventors: John M. Clough, Christopher R. A. Godfrey, Stephen P. Heaney, Kenneth Anderton
  • Patent number: 4806550
    Abstract: 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: Grant
    Filed: May 12, 1988
    Date of Patent: February 21, 1989
    Assignee: SmithKline & French Laboratories Limited
    Inventors: Robert J. Ife, Thomas H. Brown, Colin A. Leach
  • Patent number: 4806549
    Abstract: 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: Grant
    Filed: September 3, 1987
    Date of Patent: February 21, 1989
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Robert J. Ife, Thomas H. Brown, Colin A. Leach
  • Patent number: 4789677
    Abstract: New compounds having the formula I ##STR1## where one of A and B is CH or N, the other of A and B is CH, Q is lower alkylene, R is lower alkyl, X.sub.1 is halogen or trifluoromethyl and X.sub.2 and X.sub.3 are independently selected from hydrogen, halogen, trifluoromethyl, lower alkoxy and lower alkyl and the pharmaceutically acceptable acid additions are disclosed as anti-hypertensive agents. New compounds having the formula II ##STR2## where Q, R, X.sub.2 and X.sub.3 are as explained above and n is 0 or 1 and their acid addition salts are useful as intermediates.
    Type: Grant
    Filed: September 2, 1987
    Date of Patent: December 6, 1988
    Assignee: John Wyeth and Brothers Limited
    Inventors: John T. A. Boyle, Richard S. Todd
  • Patent number: 4769461
    Abstract: There are disclosed compounds of the formula ##STR1## wherein W represents a covalent bond or ##STR2## X is N or CR.sup.2 ; Y is O, S, NR.sup.2 or C(R.sup.2).sub.2 when n=0, or N or CR.sup.2 when n=1Z is ##STR3## R.sup.1 is hydrogen, lower alkyl, trifluoromethyl, nitro, hydroxy, lower alkoxy, mercapto, loweralkylthio or halo;R.sup.2 is hydrogen or lower alkyl;n is 0-1;m is 1-6 with the proviso that m is 0-5 when W represents a covalent bond;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, in psoriasis, ulcerative colitis, rheumatoid arthritis as well as in other immediate hypersensitivity reactions.
    Type: Grant
    Filed: September 16, 1986
    Date of Patent: September 6, 1988
    Assignee: American Home Products Corporation
    Inventors: John H. Musser, Dennis M. Kubrak
  • Patent number: 4767767
    Abstract: 2-amino-benzoic acid derivatives, method for making the same as well as its use for therapeutical purposes are proposed. The general formula of 2-amino-benzoic acid derivatives is ##STR1## wherein R represents chlorine or trifluoromethyl,R' is of general formula ##STR2## wherein n=0 or 1, m=4, 5, 6, 2-tetrahydropyranyl-methyl, benzyloxymethyl, benzoyloxymethyl of 1(3H)-isobenzofuranone-3-yl.The compounds show an outstanding analgesic and anti-inflammatory activity and a low toxicity.
    Type: Grant
    Filed: July 17, 1987
    Date of Patent: August 30, 1988
    Assignee: Ferrer Internacional S.A.
    Inventors: Rafael Foguet, Ernesto Forne, Jose Ortiz, Aurelio Sacristan
  • Patent number: 4735952
    Abstract: This invention provides a piperidine compound of the formula: ##STR1## wherein R.sup.1 is hydrogen or trihalomethyl,R.sup.2 is hydrogen or protected carboxy,R.sup.3 is heterocyclic group or aryl which may be halogen substituted, andX is --S--, ##STR2## --O--, --NH-- or lower alkylene which may be hydroxy substituted, and pharmaceutically acceptable salt thereof, These compounds possess hypotensive activity and are useful as anti-hypertensive agents. The invention further relates to processes for the preparation of these compounds and pharmaceutical compositions comprising compounds of the above formula.
    Type: Grant
    Filed: January 24, 1986
    Date of Patent: April 5, 1988
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Ikuo Ueda, Masaaki Matsuo, Kiyoshi Taniguchi, Takatomo Ogahara
  • Patent number: 4686220
    Abstract: This disclosure describes certain substituted piperazine-1,4-naphthalenediones useful as anti-asthmatic agents.
    Type: Grant
    Filed: December 19, 1985
    Date of Patent: August 11, 1987
    Assignee: American Cyanamid Company
    Inventors: Jeffrey B. Medwid, Lawrence W. Torley, Andrew S. Tomcufcik
  • Patent number: 4617389
    Abstract: Antineoplastic compounds of the formula, IIa, ##STR1## wherein: Y is hydrogen or lower alkyl; and Z is a lower alkoxy substituted quinolinylamino radical, a cyano substituted pyrazolylamino radical or a mono- or di-lower alkyl substituted thiazolamino radical, ora nitrogen-containing heterocyclic radical, ora cyano, phenyl, carboxamido or lower alkoxycarbonyl substituted 1-aziridinyl radical ora lower alkyl, formyl or acetylphenyl substituted 1-piperazinyl radical, oran hydroxy or piperidyl substituted 1-piperidyl radical, ora lower alkoxy, amino or halo substituted pyridylamino radical, ora carboxamido, mercapto or methylenedioxy substituted anilino radical, ora radical of the formula, ##STR2## wherein R is hydrogen or lower alkyl and R" is a nitrogen-containing heterocyclic radical, ora butyrolactonyl radical, oran adamantyl radical, ora mono- lower alkoxy substituted phenyl radical, ora substituted lower alkyl radical selected from the group consisting of mercapto lower alkyl, carboxy lower alkyl, mono-, d
    Type: Grant
    Filed: December 15, 1983
    Date of Patent: October 14, 1986
    Assignee: University Patents, Inc.
    Inventor: William A. Remers
  • Patent number: 4552966
    Abstract: 2-Nitro-4-(4-pyridinyl)benzoic acids, such as 2-nitro-4-(4-pyridinyl)benzoic acid, are prepared by oxidizing the appropriate 4-(4-alkyl-3-nitrophenyl)pyridine with, e.g., potassium permanganate or nitric acid. The products are particularly useful in the preparation of antibacterial 1-alkyl-1,4-dihydro-4-oxo-7-pyridinyl-3-quinolinecarboxylic acids.
    Type: Grant
    Filed: July 8, 1983
    Date of Patent: November 12, 1985
    Assignee: Ethyl Corporation
    Inventors: Paul F. Ranken, Thomas J. Walter
  • Patent number: 4524203
    Abstract: 4-(4-Pyridinyl)isatoic anhydrides are prepared by reacting a 2-amino-4-(4-pyridinyl)benzoic acid, i.e., an acid, ester, or salt, with phosgene, preferably gaseous phosgene. The products are particularly useful in the preparation of antibacterial 1-alkyl-1,4-dihydro-4-oxo-7-pyridinyl-3-quinolinecarboxylic acids.
    Type: Grant
    Filed: August 15, 1983
    Date of Patent: June 18, 1985
    Assignee: Ethyl Corporation
    Inventors: Thomas J. Walter, Paul F. Ranken
  • Patent number: 4507308
    Abstract: The novel anthranilic acid derivatives having the structural formula (I): ##STR1## wherein n is 0, 1 or 2, one of R.sub.1 and R.sub.2 is chloro or trifluoromethyl and the other is hydrogen, and R is 2-oxo-3-oxolanyl or 2-oxo-3-oxazolidinyl, are effective analgesics and anti-inflammatories.
    Type: Grant
    Filed: September 28, 1982
    Date of Patent: March 26, 1985
    Assignee: Recordati S.A.
    Inventors: Dante Nardi, Gianni Motta, Rodolfo Testa, Gabriele Graziani, Silvano Casadio
  • Patent number: 4482561
    Abstract: The N-substituted-4-(optionally substituted)-2-, 3- or 4-piperidyl N-(7- or 8-substituted-4-quinolyl)-anthraniloyloxyalkanoates having the structural formula (I): ##STR1## in which R is a straight or branched chain alkyl radical having from 1 to 4 carbon atoms; an alkenyl or alkynyl radical having from 2 to 6 carbon atoms; a benzyl, phenethyl, 4-nitrophenethyl or 4-aminophenethyl radical; or a phenacyl, benzoylethyl, .beta.-hydroxyphenethyl or .alpha.-hydroxyphenylpropyl radical, optionally substituted on the phenyl ring by one or more halogen atom, trifluoromethyl, nitro or amino substituents, or an alkyl substituent having from 1 to 4 carbon atoms or an alkoxy substituent having from 1 to 4 carbon atoms; R.sub.1 is a hydrogen atom or a phenyl radical; each of R.sub.2 and R.sub.3 is independently a hydrogen atom or an alkyl radical having from 1 to 4 carbon atoms; one of R.sub.4 and R.sub.5 is a chlorine atom or a trifluoromethyl radical and the other of R.sub.4 and R.sub.
    Type: Grant
    Filed: November 12, 1982
    Date of Patent: November 13, 1984
    Assignee: Recordati, S. A., Chemical & Pharmaceutical Co.
    Inventors: Dante Nardi, Gianni Motta, Rodolfo Testa, Gabriele Graziani
  • Patent number: 4421920
    Abstract: 4-Amino-chloroquinolines of the formula: ##STR1## in which R.sub.1 represents a hydrogen atom or an alkyl radical (1 to 5 carbon atoms), and R.sub.2 represents an alkyl radical (1 to 5 carbon atoms) optionally substituted by a dialkylamino group, or a phenyl radical optionally substituted by one or more carboxy and hydroxy radicals and alkyl radicals (1 to 4 carbon atoms) optionally substituted by a dialkylamino group, are prepared by the condensation of an amine of the formula: ##STR2## with a chloro-1,2,3,4-tetrahydroquinolin-4-one of the formula: ##STR3## with aromatization of the tetrahydroquinoline, the reaction being carried out in the presence of a ruthenium based catalyst on a support.The 4-amino-chloroquinoline products are useful as pharmaceuticals.
    Type: Grant
    Filed: January 15, 1982
    Date of Patent: December 20, 1983
    Assignee: Rhone-Poulenc Sante
    Inventors: Michel Baudouin, Daniel Michelet
  • Patent number: 4357333
    Abstract: The disclosure describes new 4-aminoquinoline derivatives of general formula ##STR1## and their pharmaceutically acceptable acid addition salts, where X is trifluoromethyl or halogen, Z is hydrogen or a defined substituent and R is a group having one of the formulae ##STR2## where R.sup.1 is hydrogen or lower alkyl, R.sup.2 is lower alkyl, R.sup.3 is lower alkyl and A is lower alkylene. The new 4-aminoquinoline derivatives show analgesic activity and, in some cases, anti-inflammatory activity.
    Type: Grant
    Filed: August 11, 1980
    Date of Patent: November 2, 1982
    Assignee: John Wyeth & Brother Limited
    Inventors: John L. Archibald, John T. A. Boyle
  • Patent number: 4343804
    Abstract: A method of reducing gastric acidity and treating peptic ulcers and pharmaceutical compositions therefor with certain 4-amino-3-quinolinecarboxylic acids and esters are disclosed.
    Type: Grant
    Filed: March 4, 1980
    Date of Patent: August 10, 1982
    Assignee: A. H. Robins Company, Inc.
    Inventors: Harry R. Munson, Jr., Reevis S. Alphin
  • Patent number: 4259335
    Abstract: 1-methyl-4-piperidinol esters of the formula: ##STR1## in which R is 7-chloro-4-quinolyl, 7-trifluoromethyl-4-quinolyl or 8-trifluoromethyl-4-quinolyl.These compounds and physiologically tolerable acid addition salts thereof may be used as medicines especially in the treatment of inflammatory processes and painful syndroms.
    Type: Grant
    Filed: August 6, 1979
    Date of Patent: March 31, 1981
    Assignee: Science Union et Cie, Societe Francaise de Recherche Medicale
    Inventors: Laszlo Beregi, Pierre Hugon, Jacques Bure, Francoise Degrand
  • Patent number: 4241068
    Abstract: Compounds of the formula ##STR1## wherein A is .dbd.CH-- or .dbd.N--;R.sub.1 is (a) hydrogen, lower alkyl, lower alkoxy or a fused benzene ring, or (b) --CO--R.sub.4, tetrazol-5-yl or cyano in the 4- or 5-position;R.sub.2 is --CO--R.sub.4, tetrazol-5-yl, cyano or, when R.sub.1 has one of the meanings included in (b), also hydrogen, lower alkyl, lower alkoxy or a fused benzene ring;R.sub.3 is hydrogen or lower alkanoyl; andR.sub.4 is hydroxyl, amino, hydroxy-amino, tetrazol-5-yl-amino or lower alkoxy;internal salts thereof, and non-toxic salts thereof formed with a basic substance. The compounds as well as their salts are useful as antiallergics.
    Type: Grant
    Filed: August 7, 1979
    Date of Patent: December 23, 1980
    Assignee: Boehringer Ingelheim GmbH
    Inventors: Kurt Schromm, Anton Mentrup, Ernst-Otto Renth, Armin Fugner, Volker Jacobi
  • Patent number: 4235908
    Abstract: New 4-aminoquinoline derivatives having the formula ##STR1## wherein X is halogen or trifluoromethyl at the designated 7- or 8-position; Z is hydrogen, halogen, lower alkyl, lower alkoxy, nitro, di(lower alkyl)amino or trifluoromethyl, n is from 1 to 4, R.sup.1 is hydrogen or lower alkyl, R.sup.2 is lower alkyl, R.sup.3 is lower alkyl and A is lower alkylene, and their pharmaceutically acceptable acid addition salts show anti-inflammatory activity.
    Type: Grant
    Filed: April 9, 1979
    Date of Patent: November 25, 1980
    Assignee: John Wyeth & Brother Limited
    Inventor: John T. A. Boyle
  • Patent number: 4233305
    Abstract: Derivatives of 2-(4-quinolinylamino)-5-fluorobenzoic acid compounds of the formula ##STR1## wherein X is selected from the group consisting of chlorine and --CF.sub.3 in the 7- or 8-position and R is selected from the group consisting of hydrogen, an esterifying group, alkali metals, alkaline earth metals, ammonium and non-toxic, pharmaceutically acceptable organic amines and their non-toxic, pharmaceutically acceptable acid addition salts having remarkable analgesic properties and their preparation.
    Type: Grant
    Filed: December 6, 1978
    Date of Patent: November 11, 1980
    Assignee: Roussel Uclaf
    Inventors: Andre Allais, Jean Meier, Roger Deraedt
  • Patent number: 4173636
    Abstract: The invention relates to decahydroquinoline derivatives represented by the general formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein R.sup.1 represents an alkyl or alkoxy group, a lower dialkylamino group, an optionally substituted phenyl group, a heterocyclic group; R.sup.2 represents an alkyl group, an optionally substituted phenyl group, a naphthyl group, an unsaturated heterocyclic group, an aralkyl group or an alicyclic group; and R.sup.3 represents a substituted furyl group, an aralkyl group or a group represented by the general formula: ##STR2## wherein A represents an alkylene group; Y represents an oxygen or sulphur atom, a carbonyl, carbonyl-hydroxyimino, carbonyl-hydrazono or sulphoxide group, or a group; ##STR3## n is O or an integer of from 1 to 4, with the proviso that when n is O, Y represents a carbonyl group; and R.sup.4 and R.sup.5, which are identical or different, each represent hydrogen, a halogen atom or a methyl, methoxy or acetyl group.
    Type: Grant
    Filed: March 8, 1978
    Date of Patent: November 6, 1979
    Assignee: Labaz
    Inventor: Maurice Prost
  • Patent number: 4166853
    Abstract: Antihypertensive compounds of the formula II ##STR1## wherein D is a piperidino or 1,2,5,6-tetrahydropyridino ring; wherein X is chloro or trifluoromethyl; wherein R.sub.1 is hydrogen or hydroxy when the D ring is piperidino, or nothing when the D ring is 1,2,5,6-tetrahydropyridino; and, wherein the moiety Ar is 2-oxo-1-benzimidazolinyl, phenyl, or phenyl substituted by one or two halo, trifluoromethyl, or alkyl, alkoxy, in which the carbon moieties are of 1 to 3 carbon atoms, inclusive, and halo is chloro, bromo, or fluoro, are produced by reacting 4-[[7-(chloro) or (trifluoromethyl)-4-quinolinyl]-amino]benzoic acid with thionyl chloride or a carbonyl diimidazole and subsequent reaction with the selected substituted piperidine or 1,2,5,6-tetrahydropyridine.The pharmacologically acceptable acid addition salts of II can also be used as antihypertensives.
    Type: Grant
    Filed: May 5, 1978
    Date of Patent: September 4, 1979
    Assignee: The Upjohn Company
    Inventor: John M. McCall