The -c(=x)- Is Part Of A -c(=x)x- Group, Wherein The X's Are The Same Or Diverse Chalcogens Patents (Class 546/170)
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Patent number: 5206367Abstract: This invention relates to the preparation of preparing optically-active asymmetric spiro-hydantoin compounds, which are known to be of value in the medical control of certain chronic diabetic complications arising from diabetes mellitus. This invention also includes within its scope certain corresponding novel amino and hydantoic acid compounds and the cinchonine salt of optically active hydantoic acid, which are used as intermediates in the aforesaid process.Type: GrantFiled: February 18, 1992Date of Patent: April 27, 1993Assignee: Pfizer Inc.Inventor: Frank J. Urban
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Patent number: 5204344Abstract: Compounds having the formula I: ##STR1## are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating diarrhea, hypertension, angina, platelet aggregation, cerebral spasm, premature labor, spontaneous abortion, dysmenorrhea, and migraine.Type: GrantFiled: February 5, 1991Date of Patent: April 20, 1993Assignee: Merck Frosst Canada, Inc.Inventors: Petpiboon Prasit, Rejean Fortin, John H. Hutchinson, Michel L. Belley, Serge Leger, John Gillard, Richard Frenette
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Patent number: 5192771Abstract: For inhibiting lipoxygenzce, (quinolin-2-yl-methoxy) phenylacetic acid derivatives containing cyclic substituents of the formula ##STR1## in which A, Q, D, E, G, T and M are hydrogen or various radicals,R.sup.3 is halogen or an alkyl or phenyl radical, andR.sup.1 and R.sup.2 complete a carbocyclic ring which may be substituted and/or fused to another ring,and salts thereof.Type: GrantFiled: August 1, 1990Date of Patent: March 9, 1993Assignee: Bayer AktiengesellschaftInventors: Klaus Mohrs, Siegfried Raddatz, Romanis Fruchtmann, Christian Kohlsdorfer, Reiner Muller-Peddinghaus, Pia Theisen-Popp
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Patent number: 5187180Abstract: (Quinolin-2-ylmethoxy)Heterotetrahydrocarbazoles as inhibitors of the biosynthesis of leukotrienes useful in the treatment of asthma and eye inflamation.Type: GrantFiled: July 12, 1991Date of Patent: February 16, 1993Assignee: Merck Frosst Canada, Inc.Inventor: John W. Gillard
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Patent number: 5155227Abstract: A dihydropyridine.revreaction.pyridinium salt type of redox, or chemical, delivery system for the site-specific and/or site-enhanced delivery of a radionuclide to the brain. A chelating agent capable of chelating with a radionuclide and having a reactive hydroxyl, carboxyl, amino, amide or imide group is coupled to a carrier moiety comprising a dihydropyridinie.revreaction.pyridinium salt nucleus and then complexed with a radionuclide to provide a new radionuclide pharmaceutial that, in its lipoidal dihydropyridine form, penetrates the blood-brain barrier (`BBB`) and allows increased levels of radionuclide concentration in the brain, particularly since oxidation of the dihydropyridine carrier moiety in vivo to the ionic pyridinium salt retards elimination from the brain while elimination from the general circulation is accelerated. This radionuclide delivery system is well suited for use in scintigraphy and similar radiographic techniques.Type: GrantFiled: August 2, 1990Date of Patent: October 13, 1992Assignee: University of FloridaInventor: Nicholas S. Bodor
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Patent number: 5142057Abstract: A process for producing a carboxylic acid amide or ester, which comprises reacting an organic chloride having at least one chlorine atom on its ring of a substituted or unsubstituted, aromatic or heterocyclic hydrocarbon with carbon monoxide and an amine or an alcohol in the presence of a base by using as catalysts a palladium compound and a phosphine compound represented by the general formula (V):(R).sub.2 P--X--P(R).sub.2 (V)wherein R is an alkyl group or a substituted or unsubstituted phenyl group, and X is an alkylene group having 1 to 6 carbon atoms ##STR1## or a binaphthyl group.Type: GrantFiled: May 29, 1990Date of Patent: August 25, 1992Assignee: Nihon Nohyaku Co., Ltd.Inventors: Keiji Suto, Masaaki Kudo, Moriharu Yamamoto
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Patent number: 5137892Abstract: Novel antibacterial compounds are disclosed having the formula ##STR1## as well as pharmaceutically acceptable salts, esters, amide and prodrugs thereof,wherein R.sup.1 is selected from the group consisting of (a) lower alkyl, (b) halo(lower alkyl), (c) lower alkyl(alkynyl), (d) lower cycloalkyl, (e) lower alkylamino, (f) nitrogen-containing aromatic heterocycle, (g) bicyclic alkyl and (h) phenyl;R.sup.2 is selected from the group consisting of hydrogen, lower alkyl, a pharmaceutically acceptable cation, and a prodrug ester group;R.sup.3 and R.sup.4 are independently selected from the group consisting of hydrogen, halogen, amino, and lower alkyl;R.sup.5 is either a nitrogen-containing heterocycle or a nitrogen-containing spiro-bicyclic-heterocycle; andA is N or C--R.sup.6, wherein R.sup.6 is selected from the group consisting of hydrogen, halogen, lower alkyl, and lower alkoxy, or R.sup.1 and R.sup.Type: GrantFiled: December 12, 1990Date of Patent: August 11, 1992Assignee: Abbott LaboratoriesInventors: Daniel T. Chu, Curt S. Cooper
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Patent number: 5136034Abstract: Thioacids, thiols, an acid, and an aldehyde are used to produce chiral thioacetals of the general formula. ##STR1## The compounds are leukotriene antagonists.Type: GrantFiled: October 5, 1990Date of Patent: August 4, 1992Assignee: Merck Frosst Canada, Inc.Inventors: Robert N. Young, Michel Therien, Jacques-Yves Gauthier, Robert Zamboni, Michel L. Belley
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Patent number: 5134143Abstract: 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: October 5, 1990Date of Patent: July 28, 1992Assignee: Eli Lilly and CompanyInventors: Diane L. Huser, John M. Schaus
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Patent number: 5130434Abstract: 3-Methylquinoline-8-carboxylic acid I ##STR1## and derivatives thereof are prepared by reacting o-toluidine II or a derivative thereof ##STR2## with methacrolein II ##STR3## in 70-90% strength by weight sulfuric acid in the presence of iodine or of an iodine compound, and oxidizing the resulting 3,8-dimethylquinoline IV or a derivative thereof ##STR4## with nitric acid in a solution containing sulfuric acid, in the presence of vanadium ions, by a process in which, in the sulfuric acid-containing reaction solution of the 3,8-dimethylquinoline IV, the byproducts of the reaction are first decomposed by oxidation, the resulting 3,8-dimethylquinoline solution is concentrated by distillation and the 3,8-dimethylquinoline is then oxidized in situ with nitric acid to give the 3-methylquinoline-carboxylic acid.Type: GrantFiled: August 23, 1990Date of Patent: July 14, 1992Assignee: BASF AktiengesellschaftInventors: Helmut Hagen, Jacques Dupuis, Karlheinz Arbogast
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Leukotriene synthesis-inhibiting disubstituted (quinolin-2-yl-methoxy) phenylacetic acid derivatives
Patent number: 5126354Abstract: Inhibiting leucotriene synthesis in patients with novel disubstituted (quinolin-3-yl-methoxy)phenylacetic acid derivatives of the formula ##STR1## in which A, B, D, E, G, K and M each independently is H, OH, halogen, CF.sub.3, OCF.sub.3, COOH, alkyl, alkoxycarbonyl or aryl,R.sup.1 is alkyl or cycloalkyl,R.sup.2 and R.sup.3 each independently is H, alkyl or aryl, andX is O or S,and salts thereof.Type: GrantFiled: August 1, 1990Date of Patent: June 30, 1992Assignee: Bayer AktiengesellschaftInventors: Klaus Mohrs, Siegfried Raddatz, Romanis Fruchtmann, Christian Kohlsdorfer, Reiner Muller-Peddinghaus, Pia Theisen-Popp -
Patent number: 5122608Abstract: There is provided a process for the preparation of a substituted or unsubstituted 2,3-pyridine or quinolinedicarboxylic acid by hydrolysis of a substituted or unsubstituted 2,3-pyridine or quinolinedicarboxylic acid diester with an acid having an ionization constant pK.sub.a of less than 3.0 followed by isolation of the product as the free acid or an acid salt.Type: GrantFiled: December 19, 1990Date of Patent: June 16, 1992Assignee: American Cyanamid CompanyInventor: Henry L. Strong
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Patent number: 5120745Abstract: This invention relates to 1-dimethylcarbamoyl-3-substituted-5-substituted-1H-1,2,4-triazoles of the formula ##STR1## wherein the substituents are as defined herein, compositions containing those compounds and methods of use.Type: GrantFiled: September 27, 1990Date of Patent: June 9, 1992Assignee: Shell Internationale Research Maatschappij B.V.Inventors: Richard M. Jacobson, Luong T. Nguyen, Muthuvelu Thirugnanam
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Patent number: 5112832Abstract: The invention concerns compounds of formula I ##STR1## or a salt thereof, wherein R.sup.1 and R.sup.2 each independently represent hydrogen, lower alkyl, lower alkoxy, carboxyloweralkyl, carboxy, hydroxyloweralkyl, halogen, haloloweralkyl, lower alkoxycarbonyl, optionally substituted aryl or optionally substituted aralkyl, n represents an integer from 3 to 6; R.sup.3 represents hydrogen or single or multiple substitution on one or more of the aliphatic carbons by one or more substituents selected from lower alkyl, optionally substituted aryl and optionally substituted aralkyl; A represents a group of formula (i) or (ii) below:--CR.sup.4 R.sup.5 --(CR.sup.6 R.sup.7).sub.m -- (i)--CX--(CR.sup.6 R.sup.7).sub.m -- (ii)in which R.sup.4, R.sup.6 and R.sup.7 each independently represent hydrogen or lower alkyl (providing that when R.sup.5 is NH.sub.2, R.sup.0 is hydrogen); m is 0 or 1; R.sup.5 represents hydrogen, NH.sub.2, OH or loweralkoxy, and X is .dbd.O, .dbd.NH or .dbd.Type: GrantFiled: August 8, 1990Date of Patent: May 12, 1992Assignee: John Wyeth & Brother LimitedInventors: Roger Crossley, Albert Opalko, Robin G. Shepherd
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Patent number: 5104882Abstract: Compounds having the formula: ##STR1## are leukotriene antagonists and inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents.Type: GrantFiled: May 22, 1990Date of Patent: April 14, 1992Assignee: Merck Frosst Canada, Inc.Inventors: Robert N. Young, Robert Zamboni, Jacques-Yves Gauthier, Michel L. Belley
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Patent number: 5102881Abstract: Compounds having the formula: ##STR1## are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating diarrhea, hypertension, angina, platelet aggregation, cerebral spasm, premature labor, spontaneous abortion, dysmenorrhea, and migraine.Type: GrantFiled: December 20, 1989Date of Patent: April 7, 1992Assignee: Merck Frosst Canada, Inc.Inventors: Robert Zamboni, Petpiboon Prasit, Robert N. Young
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Patent number: 5102892Abstract: 2-alkyl-4-arylmethylaminoquinolines of the general formula I ##STR1## where R.sup.1, R.sup.2, R.sup.5 and R.sup.6 have the meanings specified in the claims, and the physiologically tolerated salts thereof, the use thereof for the preparation of drugs and the drugs thus obtained as described for the inhibition of gastric acid secretion.Type: GrantFiled: March 1, 1990Date of Patent: April 7, 1992Assignee: BASF AktiengesellschaftInventors: Karl-Heinz Geiss, Klaus Ruebsamen, Martin Traut
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Patent number: 5091533Abstract: Compounds of the formula: ##STR1## where R.sup.2 contains certain aryls or heteroaryls are effective leukotriene inhibitors.Type: GrantFiled: March 12, 1990Date of Patent: February 25, 1992Assignee: Merck Frosst Canada, Inc.Inventors: Patrice C. Belanger, Claude Dufresne, Brian Fitzsimmons, deceased, Maryann Fitzsimmons, Heir, Yvan Guindon, Cheuk K. Lau, Joshua Rokach, John Schiegetz, Michel Therien, Robert N. Young
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Patent number: 5091392Abstract: 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: GrantFiled: May 1, 1990Date of Patent: February 25, 1992Assignee: Bayer AktiengesellschaftInventors: Siegfried Raddatz, Klaus-Helmut Mohrs, Romanis Fruchtmann, Christian Kohlsdorfer, Pia Theisen-Popp, Reiner Muller-Peddinghaus
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Patent number: 5081252Abstract: A process for the preparation of aromatic carboxylic acids or their salts comprises heating carboxyl-free aromatic compounds and aromatic carboxylic acid salts whose basic structures differ from those of the aromatic compounds, or heating polycyclic aromatic compounds with three or more rings and monocyclic or bicyclic aromatic carboxylic acid salts, under carbon dioxide pressure in the presence of one or more metal compounds selected from group (a) of compounds of zinc, cadmium, and thallium and one or more compounds selected from group (b) of compounds of cesium, Group II metals, And Group IIIa metals to effect the intermolecular transfer of the carboxyl groups.Type: GrantFiled: June 5, 1989Date of Patent: January 14, 1992Assignees: Nippon Steel Corporation, Nippon Steel Chemical Co., Ltd.Inventors: Shuichi Mitamura, Yoshimi Kata, Koichi Fujishiro, Yasuhisa Tsutsumi
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Patent number: 5047540Abstract: Lipid derivatives represented by the formula: ##STR1## wherein R.sub.1 is alkyl or alkylcarbamoyl; R.sub.2 is lower alkyloxy, lower alkylcarbamoyloxy, lower alkylcarbonylamino, lower alkyloxycarbonylamino, lower alkylureido, lower alkyloxymethyl, lower alkylcarbonylmethyl, cyanomethyl, heterocyclic group, or he0 terocyclyloxy; R.sub.2 ' is hydrogen or R.sub.2 and R.sub.2 ' taken together form --O(CH.sub.2).sub.m -- wherein m is an integer of 1 to 5; R.sub.3, R.sub.4, and R.sub.5 each is hydrogen or lower alkyl or two or three of R.sub.3, R.sub.4, and R.sub.5 taken together with the adjacent nitrogen atom form cyclic ammonio; R.sub.6 is hydrogen or lower alkylcarbonyl; X.sup.- is a counter anion; Y is oxygen or sulfur; and n is an integer of 1 to 10, being useful as PAF antagonists, e.g., as antithrombotic, antivasoconstricting, antibronchoconstricting agent or antitumor agent.Type: GrantFiled: November 29, 1988Date of Patent: September 10, 1991Assignee: Shionogi & Co., Ltd.Inventors: Susumu Kamata, Tatsuo Tsuri, Nobuhiro Haga, Takeaki Matsui, Morio Kishi, Kimio Takahashi, Sanji Hagashita, Kaoru Seno
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Patent number: 5047410Abstract: New pharmacologically active amidino and guanidino derivatives which are 5-HT.sub.3 receptor antagonists useful as antiemetic, gastric prokinetic and antimigrainic agents of the following general formula (I) ##STR1## , wherein the substituents are defined hereinbelow, which compounds are 5-HT.sub.3 receptor antagonists useful as antiemetic gastric prokinetic and antimigraine agents, inter alia.Type: GrantFiled: July 12, 1989Date of Patent: September 10, 1991Assignee: Istituto de Angeli S.p.A.Inventors: Arturo Donetti, Marco Turconi, Massimo Nicola, Rosamaria Micheletti
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Patent number: 5041452Abstract: Novel diamides having a nitrogen-containing heterocyclic moiety such as pyridyl are disclosed that are useful for improving feed utilization efficiency of ruminants and for improving lactation of lactating ruminants.Type: GrantFiled: September 28, 1989Date of Patent: August 20, 1991Assignee: Eastman Kodak CompanyInventor: Alan W. White
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Patent number: 5039683Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, alkyl of 1 to 6 carbon atoms, or NR.sup.4 R.sup.5, wherein R.sup.4 and R.sup.5 are independently selected from hydrogen and alkyl of 1 to 6 carbon atoms or a pharmaceutically acceptable cation;R.sup.2 is hydrogen, hydroxy, alkanoylamino of 1 to 6 carbon atoms, morpholino, halogen, hydroxyalkyl of 1 to 6 carbon atoms, COOR.sup.6 wherein R.sup.6 is alkyl of 1 to 6 carbon atoms or a pharmaceutically acceptable cation, alkoxy of 1 to 6 carbon atoms, NR.sup.7 R.sup.8 wherein R.sup.7 and R.sup.8 are independently selected from alkyl of 1 to 6 carbon atoms, alkanoyl of 1 to 6 carbon atoms, hydrogen, alkoxy of 1 to 6 carbon atoms, aminoalkyl of 2 to 6 carbon atoms, alkylaminoalkyl wherein each alkyl group is independently selected from alkyl groups having 2 to 6 carbon atoms, and dialkylaminoalkyl wherein each alkyl group is independently selected from alkyl groups having one to six carbon atoms, with the proviso that only one of R.sup.7 and R.sup.Type: GrantFiled: May 31, 1989Date of Patent: August 13, 1991Assignee: Pfizer Inc.Inventor: Susumu Nakanishi
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Patent number: 5032590Abstract: Substituted hydroxylamines of the formula ##STR1## in which R.sup.1 stands for an aromatic or heterocyclic radical,are especially useful in the treatment of hyperlipoproteinaemia, lipoproteinaemia and atherosclerosis.Type: GrantFiled: March 8, 1990Date of Patent: July 16, 1991Assignee: Bayer AktiengesellschaftInventors: Walter Hubsch, Rolf Angerbauer, Peter Fey, Hilmar Bischoff, Dieter Petzinna, Delf Schmidt
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Patent number: 5028708Abstract: This invention provides azamethine compounds represented by the formula (I): ##STR1## (wherein X represents ##STR2## Y represents C.dbd.O, C.dbd.C(CN).sub.2 or SO.sub.2 ; R.sub.1 to R.sub.4 represent independently a hydrogen atom, an alkyl group which may be substituted, an alkoxyl group which may be substituted, a halogen atom, a nitro group, a cyano group, a hydroxyl group, an amino group which may be substituted, --A--R or ##STR3## R.sub.5 and R.sub.6 represent independently a hydrogen atom, an alkyl group which may be substituted, an aryl group which may be substituted or a cyclohexyl group; R.sub.5 and R.sub.6 may be combined to form a ring or may form a ring with a hetero atom; R.sub.7 and R.sub.Type: GrantFiled: April 8, 1988Date of Patent: July 2, 1991Assignee: Sumitomo Chemical Company, LimitedInventors: Takeshi Hioki, Kiyoteru Kojima, Jun Tomioka
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Patent number: 5026854Abstract: The invention concerns compounds of formula I ##STR1## or a salt thereof, wherein R.sup.1 and R.sup.2 each independently represent hydrogen, lower alkyl, lower alkoxy, carboxyloweralkyl, carboxy, hydroxyloweralkyl, halogen, haloloweralkyl, lower alkoxycarbonyl, optionally substituted aryl or optionally substituted aralkyl, n represents an integer from 3 to 6; R.sup.3 which is optionally present represents single or multiple substitution on one or more of the aliphatic carbons by one or more substituents selected from lower alkyl, optionally substituted aryl and optionally substituted aralkyl; A represents a group of formula (i) or (ii) below:--CR.sup.4 R.sup.5 --(CR.sup.6 R.sup.7).sub.m -- (i)--CX--(CR.sup.6 R.sup.7).sub.m -- (ii)in which R.sup.4, R.sup.6 and R.sup.7 each independently represent hydrogen or lower alkyl (providing that when R.sup.5 is NH.sub.2, R.sup.4 is hydrogen); m is 0 or 1; R.sup.5 represents hydrogen, NH.sub.2, OH or loweralkoxy, and X is .dbd.O, .dbd.NH or .dbd.Type: GrantFiled: August 8, 1990Date of Patent: June 25, 1991Assignee: John Wyeth & Brother LimitedInventor: Robin G. Shepherd
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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
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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
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Patent number: 5006659Abstract: 7-Chloroquinoline-8-carboxylic acids of the formula (I) ##STR1## where R is hydrogen, chlorine or methyl, are prepared by direct oxidation of the corresponding 8-methylqunoline compound with nitric acid or nitrogen oxide in the presence of sulfuric acid and a heavy metal catalyst.Type: GrantFiled: January 16, 1990Date of Patent: April 9, 1991Assignee: BASF AktiengesellschaftInventors: Helmut Hagen, Jacques Dupuis, Heinz Eilingsfeld
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Patent number: 5001254Abstract: The present invention relates to novel methods for the preparation of quinoline-2,3-dicarboxylic acid, useful for the preparation of the highly effective 2-(2-imidazolin-2-yl)quinoline-3-carboxylic acid herbicidal agents.Type: GrantFiled: May 19, 1988Date of Patent: March 19, 1991Inventor: Donald R. Maulding
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Patent number: 4996320Abstract: A pyridine-compound is reacted with fluorine together with a Bronsted acid-compound or Lewis acid to form a N-fluoropyridinium salt which is very active to other compounds but is very selective for the preparation of a desired product and this product is very useful for a fluorine-introducing agent which makes it useful for the preparation of fluoro-compounds such as thyroid inhibitor.Type: GrantFiled: January 9, 1989Date of Patent: February 26, 1991Assignee: Sagami Chemical Research CenterInventors: Teruo Umemoto, Kyoichi Tomita, Kosuke Kawada, Ginjiro Tomizawa
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Patent number: 4996350Abstract: The present invention relates to an improved method for the preparation of dialkyl dichlorosuccinates by chlorination of a dialkyl maleate in the presence of a catalytic amount of a C.sub.1 -C.sub.4 alkyl alcohol in the absence of a solvent which are useful intermediates in the preparation of anilinofumarates. Anilinofumarates are, in turn, used in the preparation of 2-(2-imidazolin-2-yl)quinoline-3-carboxylic acid herbicidal agents.Type: GrantFiled: November 17, 1989Date of Patent: February 26, 1991Assignee: American Cyanamid CompanyInventor: Albert A. Cevasco
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Patent number: 4980351Abstract: The present invention are novel 3-aminopropoxyaryl derivatives, compositions and methods of use thereof for treating congestive heart failure, coronary heart disease, or myocardial ischemia.Type: GrantFiled: November 4, 1987Date of Patent: December 25, 1990Assignee: Warner-Lambert CompanyInventors: Hubert G. K. Barth, Ila Sircar
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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
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Patent number: 4968681Abstract: Substituted hydroxylamines of the formula ##STR1## in which R.sup.1 stands for an aromatic or heterocyclic radical, are especially useful in the treatment of hyperlipoproteinaemia, lipoproteinaemia and atherosclerosis.Type: GrantFiled: November 15, 1988Date of Patent: November 6, 1990Assignee: Bayer AktiengesellschaftInventors: Walter Hubsch, Rolf Angerbauer, Peter Fey, Hilmar Bischoff, Dieter Petzinna, Delf Schmidt
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Patent number: 4968803Abstract: The present invention relates to a process for the preparation of hydroxypyridine based compounds. The process comprises the step of: in water, reacting a pyridine based compound with the proviso that the second position on the nitrogen ring is unsubstituted and the fourth position in the nitrogen ring is not substituted with halogen, with elemental fluorine at a temperature of about -25.degree. to about +30.degree. C. for a time sufficient to form a 2-hydroxypyridine based compound.The resulting 2-hydroxypyridine or quinoline carboxylic acids and esters are useful as herbicide and pharmaceutical intermediates.Type: GrantFiled: April 10, 1989Date of Patent: November 6, 1990Assignee: Allied-Signal Inc.Inventors: Michael Van Der Puy, David Nalewajek, Gene Wicks
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Patent number: 4950613Abstract: A method of preparing a labelled specific binding partner, such as a biological probe in the form of an antibody or oligonucleotide probe, using a protected label (the corresponding unprotected label being susceptible to inactivation, such as by hydrolysis to yield a non-chemiluminescent form of the label). The specific binding partner is linked to the label, and an adduct of the label is prepared using a protective adduct former which produces a protected label which is less susceptible to inactivation. Particularly preferred labels are the acridiniums and acridans, most preferably the former having the general structure: ##STR1## wherein the phenyl rings are optionally additionally substituted, R.sub.1 is preferably an alkyl, and R.sub.5 is an optionally substituted hydrocarbon, most preferably a phenyl moiety which is either linked to the specific binding partner, or capable of being linked thereto.Type: GrantFiled: February 26, 1988Date of Patent: August 21, 1990Assignee: Gen-Probe IncorporatedInventors: Lyle J. Arnold, Jr., Alexander A. Waldrop, III, Philip W. Hammond
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Patent number: 4937255Abstract: For inhibiting 3-hydroxy-3-methylglutaryl coenzyme A and cholesterol biosynthesis, the novel disubstituted pyrroles of the formula ##STR1## in which R.sup.1 is aryl or heteroaryl,R.sup.2 is cycloalkyl or optionally substituted alkyl,R.sup.3 is hydrogen or cycloalkyl, or optionally substituted alkyl, aryl or heteroaryl,X is --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--,A is ##STR2## R.sup.6 is hydrogen or alkyl, and R.sup.7 is hydrogen, a cation or alkyl, aryl or aralkyl.Type: GrantFiled: March 16, 1989Date of Patent: June 26, 1990Assignee: Bayer AktiengesellschaftInventors: Walter Hubsch, Rolf Angerbauer, Peter Fey, Hilmar Bischoff, Dieter Petzinna, Delf Schmidt, Gunter Thomas
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Patent number: 4933447Abstract: A quinoline derivative represented by the following formula is disclosed. ##STR1## wherein R.sub.1 represents a hydrogen atom or an alkyl group which may contain a substituent and R.sub.2 represents an alkyl group which may contain a substituent, or R.sub.1 and R.sub.2 in combination with each other and with the adjacent nitrogen atom from a ring which may contain a nitrogen atom other than said adjacent nitrogen atom, an oxygen atom, or a substituent, and R.sub.3 represents a cyano group, a carbamoyl group, or a lower alkoxycarbonyl group. The compound exhibits superior cardiotonic activity and vasodilative activity, and thus is effective as a medicine.Type: GrantFiled: September 16, 1988Date of Patent: June 12, 1990Assignee: SS Pharmaceutical Co., Ltd.Inventors: Fujiko Koono, Norimitsu Umehara, Hideaki Matsuda, Tatsuhiko Katori
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Patent number: 4927935Abstract: A compound of the formula I ##STR1## where A is nitro, amino, halocarbonyl or halosulfonyl, R is hydrogen, halogen, nitro, cyano, C.sub.1 -C.sub.4 -alkanoylamino, hydroxyl, C.sub.1 -C.sub.4 -alkoxy phenoxy which is unsubstituted by methyl or chloro, mercapto, C.sub.1 -C.sub.4 -alkylthio, phenylthio which is unsubstituted or substituted by ethyl, fluoro, or methoxy, carboxyl, C.sub.1 -C.sub.4 -alkoxycarbonyl, phenoxycarbonyl which is unsubstituted or substituted by isopropyl, bromo, or methoxy, carbamoyl, hydroxysulfonyl, C.sub.1 -C.sub.4 -alkylsulfonyl, phenylsulfonyl which is unsubstituted or substituted by ethyl, chloro, or isopropoxy, sulfamoyl or trifluoromethyl or is C.sub.1 -C.sub.4 -alkyl which may be substituted by hydroxyl, C.sub.1 -C.sub.4 -alkoxy or halogen, and X and Y are each, independently of one another, halogen, hydroxysulfonyl, C.sub.1 -C.sub.Type: GrantFiled: November 7, 1988Date of Patent: May 22, 1990Assignee: BASF AktiengesellschaftInventors: Alfred Hackenberger, Manfred Patsch
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Patent number: 4925861Abstract: According to the present invention, there are provided novel carboxystyrene derivatives of the general formula (I): wherein the symbols are as defined hereinabove. Also provided herein are leukotriene antagonists and phospholipase inhibitors containing the carboxystyrene derivative or pharmaceutically acceptable salt thereof as an effective ingredient.Type: GrantFiled: April 13, 1988Date of Patent: May 15, 1990Assignee: Mitsubishi Kasei CorporationInventors: Yoshio Hayashi, Oguri Tomei, Masaki Shinoda, Kazuo Takahashi, Munehiro Hashimoto
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Patent number: 4921961Abstract: The invention is novel 2-carbamoylnicotinic and 3-quinolinecarboxylic acids and esters which are intermediate compounds for the preparation of 2-(2-imidazolin-2-yl)pyridine and quinoline herbicides.Type: GrantFiled: July 18, 1988Date of Patent: May 1, 1990Assignee: American Cyanamid CompanyInventor: Marinus Los
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Patent number: 4904651Abstract: The present invention comprises certain amide derivatives of 4,8-disubstituted quinoline-3-carboxylic acids of formula I; pharmaceutically acceptable salts of the compounds of formula I; pharmaceutical compositions containing a compound of formula I, or a pharmaceutically acceptable salt thereof, for use in the treatment of anxiety; and processes for the manufacture of the compounds of formula I, as well as intermediates for use in such manufacture.Type: GrantFiled: August 3, 1988Date of Patent: February 27, 1990Assignee: ICI Americas Inc.Inventor: Edward J. Warawa
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Patent number: 4904816Abstract: There is provided a novel process for the manufacture of anilinofumarate via chloromaleate or chlorofumarate or mixtures thereof.Type: GrantFiled: June 15, 1989Date of Patent: February 27, 1990Assignee: American Cyanamid CompanyInventors: Albert A. Cevasco, Donald Roy
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Patent number: 4902803Abstract: Nitrogen-containing aromatic heterocyclic (poly)peroxycarbonxylic acids having the formula: ##STR1## wherein R represents a hydrogen atom or a straight or branched alkyl, (hetero)cycloalkyl, (hetero)aryl, alkylaryl or arylalkyl group, wherein said groups are optionally substituted, or a carboxylic group or any other substituents non-reactive in the presence of the active oxygen of the peroxycarboxylic group;n is a number selected from 0 and 1;m is a number selected from 1, 2 and 3, andX represents an acidic anion selected from HSO.sub.4.sup.- and CH.sub.3 SO.sub.3.sup.-, and wherein the pyridinic ring may in its turn be condensed with at least one further (hetero) aromatic or (hetero)cycloalkylic ring;to their preparation process and to their use as bleaching agents.Type: GrantFiled: July 15, 1988Date of Patent: February 20, 1990Assignee: Ausimont S.p.A.Inventors: Carlo Venturello, Claudio Cavallotti
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Patent number: 4895951Abstract: Novel diamides having a nitrogen-containing heterocyclic moiety such as pyridyl are disclosed that are useful for improving feed utilization efficiency of ruminants and for improving lactation of lactating ruminants.Type: GrantFiled: January 17, 1989Date of Patent: January 23, 1990Assignee: Eastman Kodak CompanyInventor: Alan W. White
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Patent number: 4888427Abstract: The invention provides novel amino acids and peptides containing them which comprise a dihydropyridine.revreaction.pyridinium salt-type redox system and which provide site-specific and sustained delivery of pharmacologically active peptides to the brain. These new amino acids contain a redox system appended directly or via an alkylene bridge to the carbon atom adjacent to the carboxyl carbon and may be incorporated into a peptide chain at a variety of positions, including non-terminal positions.Type: GrantFiled: April 7, 1987Date of Patent: December 19, 1989Assignee: University of FloridaInventor: Nicholas S. Bodor
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Patent number: 4877797Abstract: Compounds are described of the formula ##STR1## wherein R.sub.1 is a nitro or trifluoromethyl group; R.sub.2 is a C.sub.1 -C.sub.6 alkyl group; R.sub.3 is a pyridyl or pyridyl N-oxide group which may be substituted with halogen, hydroxyl, haloalkyl, C.sub.1 -C.sub.6 alkoxy or C.sub.1 -C.sub.6 alkyl and further may be fused with a benzene or naphthalene ring, said ring being optionally substituted with C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, halogen or haloalkyl, and a pharmaceutically acceptable acid addition salt thereof. The compounds of the formula (I) are of vasodilating and blood pressure lowering activities and thus may be useful for the treatment of cardiac diseases, cerebrovascular diseases and hypertension.Type: GrantFiled: June 15, 1987Date of Patent: October 31, 1989Assignee: Nisshin Flour Milling Co., Ltd.Inventors: Hiroaki Satoh, Hiroyasu Koyama, Yoshikuni Suzuki, Toshiji Sugai, Koichi Watanabe
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Patent number: 4871842Abstract: Novel compounds of the formula: ##STR1## [wherein A is an .alpha.-amino acid residue; B is a group represented by the formula: ##STR2## (wherein R.sup.4 is hydrogen, lower alkyl, aralkyl or amino-lower alkyl), whereby the linkage between the symbols A and B designates a peptide bond and the group R.sup.4 in B may be linked with A; R.sup.1 is hydrogen, lower alkyl or aralkyl; R.sup.2 is hydrogen, lower alkyl, aralkyl or acyl; X is alkylene] and salts thereof possess, for example, inhibitory activity on angiotensin converting enzyme, and are useful as an agent for diagnosis, prevention or treatment of hypertension as well as circulatory diseases such as cardiopathy and cerebral apoplexy.Type: GrantFiled: July 14, 1988Date of Patent: October 3, 1989Assignee: Takeda Chemical Industries, Ltd.Inventors: Hirosada Sugihara, Kohei Nishikawa, Katsumi Ito