Plural Chalcogens Attached Directly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 546/155)
-
Patent number: 5145843Abstract: Compounds of the formula (1) ##STR1## the substituents are described in the specification. The compouns of formula (I) are plant fungicides.Type: GrantFiled: April 7, 1989Date of Patent: September 8, 1992Assignee: DowElancoInventors: Wendell R. Arnold, Michael J. Coghlan, Glen P. Jourdan, Eriks V. Krumkalns, Robert G. Suhr
-
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
-
Patent number: 5136039Abstract: A compound of the formula: ##STR1## in which X, Y and Z are, independently, hydrogen, halogen, hydroxy, nitro, cyano, carboxyl, trifluoromethyl, phenyl, amino, alkylamino, dialkylamino, alkyl or alkoxy; R.sub.1 is alkyl, alkenyl, cycloalkyl, phenyl, benzyl or substituted phenyl or benzyl or alkoxy; R.sub.2 is: ##STR2## or a pharmaceutically acceptable salt thereof, are ACAT inhibitors.Type: GrantFiled: September 6, 1991Date of Patent: August 4, 1992Assignee: American Home Products CorporationInventors: William F. Fobare, Donald P. Strike
-
Patent number: 5134148Abstract: The invention concerns a heterocycle of the formula I ##STR1## wherein Q is an optionally substituted 6-membered monocyclic or 10-membered bicyclic heterocyclic moiety containing one or two nitrogen atoms;A is (1-6C)alkylene, (3-6C)alkenylene, (3-6C)alkynylene or cyclo(3-6C)alkylene;X is oxy, thio, sulphinyl, sulphonyl or imino;Ar is phenylene which may optionally bear one or two substituents or Ar is an optionally substituted 6-membered heterocyclene moiety containing up to three nitrogen atoms;R.sup.1 is hydrogen, (1-6C)alkyl, (3-6C)alkenyl, (3-6C)alkynyl, cyano-(1-4C)alkyl or (2-4C)alkanoyl, or optionally substituted benzoyl;and R.sup.2 and R.sup.3 together form a group of the formula --A.sup.2 --X.sup.2 --A.sup.3 -- which, together with the carbon atom to which A.sup.2 and A.sup.3 are attached, defines a ring having 4 to 7 ring atoms, wherein A.sup.2 and A.sup.3, which may be the same or different, each is (1-4C)alkylene and X.sup.Type: GrantFiled: September 5, 1991Date of Patent: July 28, 1992Assignees: Imperial Chemical Industries PLC, ICI PharmaInventors: Graham C. Crawley, Philip N. Edwards, Jean-Marc M. M. Girodeau
-
Patent number: 5132312Abstract: Disclosed are novel 3-hydroxy-3-methylglutarylcoenzyme A reductase inhibitors useful as antihypercholesterolemic agents represented by the formula ##STR1## and the corresponding ring-opened hydroxy acids derived therefrom and pharmaceutically acceptable salts thereof.Pharmaceutical compositions containing said compounds and method of inhibiting the biosynthesis of cholesterol therewith are also disclosed.Type: GrantFiled: November 27, 1990Date of Patent: July 21, 1992Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.Inventors: John R. Regan, Kent E. Neuenschwander
-
Patent number: 5125954Abstract: The present invention relates to novel bicyclo ether derivatives, to compositions containing them, and to their method of use especially to control the growth of undesired vegetation in rice.Type: GrantFiled: November 2, 1990Date of Patent: June 30, 1992Assignee: E.I. Du Pont de Nemours and CompanyInventors: James E. Powell, Richard B. Phillips
-
Patent number: 5122537Abstract: The invention relates to new arylvinylamide derivatives of formula ##STR1## wherein Y is a bicyclic ring system chosen from (A), (B), (C), (D), and (E); ##STR2## in which m is zero, 1 or 2; R is hydrogen, a C.sub.1 -C.sub.6 alkyl or C.sub.1 -C.sub.6 alkanoyl group;R.sub.1 is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.2 is hydrogen, halogen, cyano or C.sub.1 -C.sub.6 alkyl; andn is an integer of 1 to 3; and wherein each of the substituents --CH.dbd.CHNHCOR.sub.1, OR and R.sub.2 may be independently on either of the aryl and heteroaryl moieties of the bicyclic ring system (A), (C), (D) and (E); whereas only the benzene ring may be substituted in the bicyclic ring system (B),which are useful as tyrosine kinase inhibitors.Type: GrantFiled: November 2, 1990Date of Patent: June 16, 1992Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Franco Buzzetti, Angelo Crugnola
-
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
-
Patent number: 5114939Abstract: A fungicidal method which comprises applying to the locus of a plant pathogen a fungicidally effective but non-phytotoxic amount of a compound of the formula (1) ##STR1## wherein: R.sup.1 to R.sup.4 are independentlyH, halo, (C.sub.1 -C.sub.4) alkyl, branched (C.sub.3 -C.sub.4) alkyl, halo (C.sub.1 -C.sub.4) alkyl, (C.sub.1 -C.sub.4) alkoxy, NO.sub.2, or HN.sub.2, at least two of R.sup.1 to R.sup.4 being H,or one of R.sup.2 to R.sup.4 is --NR.sup.7 --Y--Ar or O--Y--Ar and the rest of R.sup.1 to R.sup.4 are H;W is N, or CR.sup.5 ;R.sup.5 is H, CH.sub.3, Cl, O--Y--Ar, or --NR.sup.7 --Y--Ar;R.sup.6 is H, CH.sub.3, Cl, or Br;A is --O--Alk or --X--Y--Ar;Alk is a C.sub.2 -C.sub.18 saturated or unsaturated hydrocarbon chain, straight chain or branched, optionally substituted with halo, halo (C.sub.1 -C.sub.4) alkoxy, (C.sub.3 -C.sub.8) cycloalkyl, hydroxy, or acetyl;X is O, NR.sup.7, or CR.sup.8 R.sup.9, provided that if one of R.sup.2 to R.sup.5 is NR.sup.Type: GrantFiled: March 16, 1989Date of Patent: May 19, 1992Assignee: DowElancoInventors: Barry A. Dreikorn, Glen P. Jourdan, Robert G. Suhr
-
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
-
Patent number: 5112837Abstract: The invention relates to a quinoline of the formula: ##STR1## wherein each of R.sup.1 and R.sup.2, which may be the same or different, is hydrogen, halogeno, hydroxy, cyano, carbamoyl, nitro or amino, alkyl, alkoxy, alkylthio, alkylamino, dialkylamino or alkanoylamino each of up to 4 carbon atoms, or substituted alkyl or alkoxy each of up to 3 carbon atoms, provided that both R.sup.1 and R.sup.2 are not hydrogen; the quinoline ring may bear further substituents; R.sup.3 is hydrogen or alkyl of up to 4 carbon atoms; R.sup.4 is hydrogen, alkyl, alkenyl or alkynyl each of up to 4 carbon atoms or substituted alkyl of up to 3 carbon atoms; Ar is phenylene, naphthylene or heterocyclene which is unsubstituted or which bears one or more substituents; R.sup.5 is such that R.sup.5 --NH.sub.2 is an amino acid; or a pharmaceutically-acceptable salt or ester thereof. The compounds possess anti-tumor activity.Type: GrantFiled: September 17, 1990Date of Patent: May 12, 1992Assignee: Imperial Chemical Industries PLCInventors: Kenneth D. Burrows, Leslie R. Hughes, Peter Warner
-
Patent number: 5106407Abstract: The present invention discloses the antimicrobial utility of certain iodonium ylide compounds. The particular iodonium ylide compounds are phenyl iodonium ylides having an ortho substituent that stabilizes the positive charge on the polyvalent iodine by a nonbonded electrostatic interaction. The polyvalent iodine is further stabilized by a cyclic 1,3-dicarbonyl anion.Type: GrantFiled: December 4, 1989Date of Patent: April 21, 1992Assignee: The Dow Chemical CompanyInventors: Attila G. Relenyi, Gerald F. Koser, Richard W. Walter, Jr., William J. Kruper, Jr., Ravi B. Shankar, Anthony P. Zelinko
-
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
-
Patent number: 5097034Abstract: Color formers of the formula ##STR1## in which X.sup.1 denotes hydroxyl, alkoxy, alkenyloxy, aralkoxy, cycloalkoxy, aryloxy or acyloxy,R.sup.1 denotes hydrogen, halogen, alkyl or alkoxy,R.sup.2 denotes hydrogen, alkoxy, aralkoxy, aryloxy or a radical of the formula ##STR2## Y.sup.1 and Y.sup.2, independently of one another, denote alkyl, cycloalkyl or aralkyl,R.sup.2 can form a heterocyclic ring with A in the o-position, in which a benzene ring can be additionally fused onto ring A in the o-/m-position with respect to R.sup.2,R.sup.3 denotes hydrogen, alkyl, alkenyl, aralkyl, cycloalkyl or aryl, or R.sup.3 is linked to ring B in the o-position with respect to the nitrogen,Z.sup.1 stands for the remaining members of a partially hydrogenated or completely hydrogenated ring, with the proviso that Z.sup.Type: GrantFiled: May 14, 1991Date of Patent: March 17, 1992Assignee: Bayer AktiengesellschaftInventor: Udo Eckstein
-
Patent number: 5094683Abstract: Herbicidal sulphonylaminocarbonyltriazolinones of the formula ##STR1## in which R.sup.1 represents hydrogen, hydroxyl or amino, or represents an optionally substituted radical from the series comprising alkyl, alkenyl, akinyl, cycloalkyl, aralkyl, aryl, alkoxy, alkenyloxy, alkylamino and dialkylamino,R.sup.2 represents hydrogen hydroxyl, mercapto or amino, or represents an optionally substituted radical from the series comprising alkyl, cycloalkyl, cycloalkenyl, aralkyl, aryl, alkoxy, alkylamino and dialkylamino, andR.sup.3 represents an optionally substituted radical from the series comprising alkyl, aralkyl, aryl and heteroaryl, and salts thereof. Intermediates of the formula ##STR2## in which A.sup.1 represents in each case optionally substituted alkyl, alkenyl, cycloalkyl, alkoxy or dialkylamino andA.sup.2 represents hydrogen, or represents in each case optionally substituted alkyl, cycloalkyl, aralkyl, aryl or alkoxy,provided that both A.sup.1 and A.sup.Type: GrantFiled: April 29, 1991Date of Patent: March 10, 1992Assignee: Bayer AktiengesellschaftInventors: Werner Daum, Klaus-Helmut Muller, Michael Schwamborn, Peter Babczinski, Hans-Joachim Santel, Robert R. Schmidt, Harry Strang
-
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
-
Patent number: 5082853Abstract: The subject compounds, which are adapted for the site-specific/sustained delivery of centrally acting drug species to the brain, are compounds of the formula ##STR1## and the non-toxic pharmaceutically acceptable salts thereof, wherein D is the residue of a centrally acting primary, secondary or tertiary amine and ##STR2## is an unsubstituted or substituted dihydropyridyl, dihydroquinolyl or dihydroisoquinolyl radical. The corresponding ionic pyridinium, quinolinium and isoquinolinium salts ##STR3## wherein X.sup.- is the anion of a non-toxic pharmaceutically acceptable acid, are also disclosed.Type: GrantFiled: April 4, 1990Date of Patent: January 21, 1992Inventor: Nicholas S. Bodor
-
Patent number: 5081126Abstract: The invention relates to dithioacetal compounds having 5-lipoxygenase-inhibiting activity, of the formula: ##STR1## wherein R.sup.1 is lower alkyl, di-(lower)alkylamino, aryl, or heterocyclic group which may have one or more substitutents selected from halogen, lower alkyl, lower alkoxy and phenyl,R.sup.2 and R.sup.3 are each lower alkyl, aryl or ar-(lower)alkyl, or R.sup.2 and R.sup.3 are together to form 1,3-dithian ring,R.sup.4 is hydrogen or lower alkoxy, andn is 0 or an integer 1 to 4 and pharmaceutically acceptable salts thereof.Type: GrantFiled: June 15, 1990Date of Patent: January 14, 1992Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Teruo Oku, Yoshio Kawai, Hiroshi Kayakiri, Kazuyoshi Kuratani, Masashi Hashimoto
-
Patent number: 5079360Abstract: The process for making certain bicyclic compounds and intermediates which are useful as anti-allergic, anti-inflammatory and cytoprotective agents.Type: GrantFiled: November 13, 1989Date of Patent: January 7, 1992Assignee: Schering CorporationInventors: Dinesh Gala, Martin Steinman, Ashit Ganguly
-
Patent number: 5079264Abstract: A process to prepare compounds of formula I ##STR1## in which n=0, 1 or 2 comprising the cyclization of compounds of formula II ##STR2## in which n=0, 1 or 2. The cyclization may be effected in the presence of an organic or inorganic base or thermally at a temperature in the range 40.degree.-160.degree. C.Compounds of formula II and certain analogues thereof are disclosed as cardiovascular agents.Type: GrantFiled: March 1, 1991Date of Patent: January 7, 1992Assignee: The Boots Co. PLCInventors: Lachlan MaClean, David L. Roberts, Kenneth Barron, Kenneth J. Nichol, Albert E. Harrison
-
Patent number: 5075303Abstract: Pyridine derivatives of formula ##STR1## their heteroaromatic N-oxides and their pharmaceutically acceptable acid addition salts are disclosed. In the formula z is 0, 1 and 2 and R, R.sup.1, R.sup.2 and R.sup.2 have specified meanings. The compounds exhibit activity as 5-HT.sub.1A agonists, antagonists or partial agonists and are useful for the treatment of CNS disorders e.g. anxiety, as antihypertensives and in treating anorexia.Type: GrantFiled: April 6, 1990Date of Patent: December 24, 1991Assignee: John Wyeth & Brother LimitedInventors: Ian A. Cliffe, Howard L. Mansell, Richard S. Todd, Alan C. White
-
Patent number: 5071860Abstract: Insecticidally active substituted heteroaryl phenyl ethers of the formula ##STR1## in which Het represents an optionally substituted heteroaromatic radical,X represents O, S, --CH.sub.2 --, --O--CH.sub.2 --, --S--CH.sub.2 --, --CH.sub.2 --O--, ##STR2## Y represents O, --O--CH.sub.2 -- or S, Z represents an optionally substituted aromatic or heteroaromatic radical;m represents integers from 1-4n represents 0, 1, 2, 3, 4O represents 0, 1, 2, 3, 4, provided than n and o do not simultaneously represent 0p represents integers from 1-4,R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 independently of one another represent hydrogen, C.sub.1 -C.sub.6 -alkyl which is optionally substituted; two radicals adjacent to one another can also, together with the C atoms to which they are bonded, form a saturated carbocyclic 5- or 6-ring,R.sup.1 represents identical or different radicals hydrogen, halogen, CN, C.sub.1-4 -alkyl, 1-5-halogeno-C.sub.1-4 -alkyl, C.sub.1-4 -alkoxy, C.sub.1-4 -alkylthio, 1-5-halogeno-C.sub.Type: GrantFiled: March 7, 1990Date of Patent: December 10, 1991Assignee: Bayer AktiengesellschaftInventors: Bernd Alig, Wilhelm Stendel, Michael Londershausen
-
Patent number: 5061712Abstract: Process for the preparation of antibacterial compounds of the formula ##STR1## comprises condensing an oxo compound of the formula ##STR2## with an amino compound of the formula ##STR3## to produce a compound of the formula ##STR4## reacting the compound of the formula (III) with a compound of the formula ##STR5## to give a compound of the formula ##STR6## and then eliminating the amino-protective group ##STR7##Type: GrantFiled: May 25, 1990Date of Patent: October 29, 1991Assignee: Bayer AktiengesellschaftInventors: Uwe Petersen, Andreas Krebs, Thomas Schenke, Klaus Grohe, Michael Schriewer, Ingo Haller, Karl G. Metzger, Rainer Endermann, Hans-Joachim Zeiler
-
Patent number: 5047412Abstract: The invention describes novel (2-styryl-, 2-naphthyl- and 2-phenethyl-4-o-hydroxyphenyl-1,3-dioxan-5-yl)alkenoic acids and related tetrazoles and sulphonamides, of the formula I wherein Q completes a benzene or pyridine ring, Y is vinylene, Z is carboxy, 1(H)-tetrazol-5-yl or a group of the formula --CO.NHSO.sub.2 R.sup.6, and R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, A.sup.1, A.sup.2, n and m have the meanings defined in the specification, and pharmaceutically acceptable salts thereof, for use in conjunction with their pharmaceutical compositions in treating certain pulmonary and/or vascular disorders. The invention also describes various processes and intermediates for the manufacture of the novel compounds.Type: GrantFiled: February 1, 1989Date of Patent: September 10, 1991Assignee: Imperial Chemical Industries PLCInventors: George R. Brown, Michael J. Smithers
-
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
-
Patent number: 5021438Abstract: Novel compounds having an affinity for 5-hydroxytryptamine receptors of the formula ##STR1## in which R.sup.1 stands for H, alkyl, aralkyl or heteroarylalkyl,X stands for H, OCH.sub.3, OH, SCH.sub.3, halogen, CN or CONH.sub.2,Y stands for a straight-chain or branched, saturated or unsaturated alkylene chain having up to 6 carbon atomsandZ stands for a group of the formula ##STR2## --OR.sup.4, --SO.sub.m R.sup.5, --COOR.sup.6 or CONR.sup.7 R.sup.8 or salts thereof.Type: GrantFiled: March 15, 1989Date of Patent: June 4, 1991Assignee: Bayer AktiengesellschaftInventors: Bodo Junge, Bernd Richter, Thomas Glaser, Jorg Traber
-
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: 5017708Abstract: A compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 each is hydrogen, hydroxy, oxo, halogen, azido, amino, C.sub.1 -C.sub.3 alkylamino, or aminomethyl, in which said amino, C.sub.1 -C.sub.3 alkylamino and aminomethyl each is optionally substituted by one or two members selected from the group consisting of C.sub.1 -C.sub.3 alkyl and amino-protecting group; n is an integer of 1 to 3; p and q each is an integer of 0 to 3 with proviso that p+q=1 to 4 or acid-addition salts thereof, being useful materials for preparing side chains of antibacterial quinolonecarboxylic acids, cephalosporines, or other antibiotics.Type: GrantFiled: September 8, 1989Date of Patent: May 21, 1991Assignee: Shionogi & Co., Ltd.Inventors: Masaru Ogata, Hiroshi Matsumoto, Sumio Shimizu, Shiro Kida
-
Patent number: 5011931Abstract: A process to prepare compounds of formula I ##STR1## in which n=0, 1 or 2 comprising the cyclisation of compounds of formula II ##STR2## in which n=0, 1 or 2. The cyclisation may be effected in the presence of an organic or inorganic base or thermally at a temperature in the range 40.degree.-160.degree. C.Compounds of formula II and certain analogues thereof are disclosed as cardiovascular agents.Type: GrantFiled: June 23, 1989Date of Patent: April 30, 1991Assignee: The Boots Company PLCInventors: Lachlan MacLean, David L. Roberts, Kenneth Barron, Kenneth J. Nichol, Albert E. Harrison
-
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: 5006534Abstract: Substituted benzyl ethers, benzyl thioethers, and benzylamines of the formula ##STR1## in which R.sup.1 and R.sup.2 are identical or different and represent hydrogen, alkyl, alkenyl, cycloalkyl, alkoxy, alkylthio, halogenoalkyl, sulphonylalkyl, halogenoalkoxy, halogenoalkylthio, aralkoxy, aralkylthio, halogen, nitro, cyano or hydroxyl, or represent a group of the formula ##STR2## wherein R.sup.4 and R.sup.5 are identical or different and represent hydrogen, alkyl, alkenyl, cycloalkyl, aralkyl, aryl or acyl,R.sup.3 represents a group of the formula ##STR3## in which R.sup.6 represents hydrogen, alkyl or acyl,R.sup.7 represents hydrogen or alkyl andn represents a number from 3 to 10,B represents --CH.sub.2 --X-- or --X--CH.sub.2 --,wherein X represents O, S or NR.sup.7,and wherein R.sup.7 has the abovementioned meaning and the group ##STR4## represents a benzo-fused heterocyclic system, A in the heterocyclic radical being 3-, 4- or 5-membered and containing nitrogen, oxygen and/or sulphur as hetero-atoms.Type: GrantFiled: January 30, 1989Date of Patent: April 9, 1991Assignee: Bayer AktiengesellschaftInventors: Klaus-Helmut Mohrs, Romanis Fruchtmann, Christian Kohlsdorfer
-
Patent number: 5002957Abstract: Azaneophyl and silazaneophyl sulfides, processes for their preparation, agents containing them, and their use as pesticides.Compounds of the formula I, their optical isomers and mixtures thereof ##STR1## where M denotes C or Si,R.sup.1 denotes unsubstituted or substituted pyridyl, unsubstituted or substituted pyrimidyl, andwhen M=C- denotes unsubstituted or substituted pyridazinyl, unsubstituted or substituted pyrazinyl, unsubstituted or substituted 1,2,4-triazinyl, unsubstituted or substituted 1,2,4,5-tetrazinyl,R.sup.2, R.sup.3 independently or one another denote alkyl, alkenyl, haloalkyl, phenyl, or R.sup.2 and R.sup.3 denote an alkylene chain which - together with the quaternary central atom (M) - form an unsubstituted or fluorine-substituted ring having four to six ring members (when M=Si) or having three to six ring members (when M=C),R.sup.4 denotes H, F, --CN, --CCl.sub.3, --C.dbd.CH, (C.sub.1 -C.sub.4)alkyl, ##STR2## R.sup.Type: GrantFiled: March 23, 1989Date of Patent: March 26, 1991Assignee: Hoechst AktiengesellschaftInventors: Hans H. Schubert, Gerhard Salbeck, Hans-Peter Krause, Werner Knauf, Anna Waltersdorfer, Manfred Kern
-
Patent number: 4997840Abstract: Quinolone sulphonates of formula I ##STR1## in which R.sub.1 is lower alkyl; R.sub.2 is lower alkyl; and R.sub.3, R.sub.4 and R.sub.5, which may be the same or different, are hydrogen, lower alkyl, lower alkoxy, lower alkylthio, lower alkylsulphinyl, lower alkylsulphonyl, halo, halogenated lower alkyl, halogenated lower alkoxy, cyano, phenyl or phenyl substituted by 1 or 2 groups independently selected from lower alkyl, lower alkoxy and halo, have antihypertensive activity.Processes for preparing compounds of formula I and pharmaceutical compositions containing them are described.Compounds of formula I are also indicated for use in the treatment of heart failure and ischaemic heart disease.Type: GrantFiled: September 1, 1989Date of Patent: March 5, 1991Assignee: The Boots Company, PLCInventors: Roy V. Davies, Michael D. Brown, Nicholas J. Holman
-
Patent number: 4996218Abstract: Compounds of the general formula (I) ##STR1## and physiologically acceptable salts and solvates thereof, which have .beta..sub.2 -adrenoreceptor stimulant activity. They may be used in the treatment of diseases associated with reversible airways obstruction, such as asthma and chronic bronchitis.In preferred embodiments, Q represents a chlorine atom or a trifluoromethyl group, X represents a C.sub.3-4 alkylene chain, Y a C.sub.1-5 alkylene chain, R, R.sup.1 and R.sup.2 are each preferably a hydrogen atom or a methyl group and Het represents a pyrimidinyl pyrazinyl, triazinyl, thiazolyl, quinolinyl, benzimidazolyl, benzothiazolyl, benzoxazolyl or pyridyl group.Type: GrantFiled: August 10, 1988Date of Patent: February 26, 1991Assignee: Glaxo Group LimitedInventor: Lawrence H. C. Lunts
-
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
-
Patent number: 4985438Abstract: The invention concerns the preparation of compounds of formula ##STR1## and acid addition and quaternary ammonium salts thereof, wherein the dotted line represents an optional bond, Ar represents a ring system of formula ##STR2## in which Q is O, S, --CR.sup.7 .dbd.CR.sup.8 --, --N.dbd.CR.sup.8 -- and --N.dbd.N--; R.sup.4, R.sup.5 and R.sup.6 ; and R.sup.7 and R.sup.8 when present, each represent hydrogen or a substitutent selected from lower alkyl, lower alkenyl, lower alkoxy, NO.sub.2, NH.sub.2, haloloweralkyl, hydroxyloweralkyl, aminoloweralkyl, substituted amino, halogen, loweralkoxycarbonyl, cyano, CONH.sub.2 and hydroxy; and additionally either R.sup.4 and R.sup.5 when adjacent or R.sup.6 and R.sup.Type: GrantFiled: October 19, 1988Date of Patent: January 15, 1991Assignee: John Wyeth & Brother, LimitedInventors: John L. Archibald, Terence J. Ward
-
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
-
Patent number: 4960890Abstract: Methine dyes (I) which conform in one of their tautomeric forms to the general formula ##STR1## where Y.sup.1 is in both or either case an electron-attracting group and the other Y.sup.1 is hydrogen,Y.sup.2 is in each case, independently of the others, hydrogen, --CN, halogen, C.sub.1 -C.sub.6 -alkyl, C.sub.5 -C.sub.7 -cycloalkyl, phenyl, pyridyl or together with a further Y.sup.2 a five- or six-membered ring which may have a fused-on benzene ring,R is hydrogen, C.sub.1 -C.sub.20 -alkyl, C.sub.7 -C.sub.10 -aralkyl or .beta.Type: GrantFiled: October 5, 1989Date of Patent: October 2, 1990Assignee: BASF AktiengesellschaftInventors: Ewald Daltrozzo, Werner Sulger
-
Patent number: 4959363Abstract: Compounds of the formula ##STR1## where R is hydrogen, hydroxy, amino or lwer-alkyl; R.sup.1 is lower-alkyl, lower-alkenyl, cycloalkyl, pyridinyl, phenyl or substituted phenyl; R.sup.2 is hydrogen, amino or hydroxy; R.sup.6 is hydrogen or fluoro; and R.sup.7 is phenyl, pyridinyl or selected other heterocycles, have antiviral acitivity against herpes virus.The compounds are prepared from the corresponding carboxylic acids or ester, or by a tin-coupling reaction on the corresponding 7-halo compounds.Type: GrantFiled: June 23, 1989Date of Patent: September 25, 1990Assignee: Sterling Drug Inc.Inventor: Mark P. Wentland
-
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: 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
-
Patent number: 4933336Abstract: A compound of formula (I), or a pharmaceutically acceptable salt thereof, ##STR1## in which, R.sub.1 is hydrogen, lower alkyl or CH.sub.2 OR.sub.6 ;R.sub.2 is hydrogen or lower alkyl;R.sub.3 is hydrogen or lower alkyl;each of W and Z, which are different, represents --CR.sub.4 R.sub.5 -- or --(CR.sub.x R.sub.y).sub.n --, in which,R.sub.4 is hydrogen, C.sub.1-3 alkyl, C.sub.1-3 alkylthio or C.sub.1-3 alkoxy;R.sub.5 is C.sub.1-3 alkyl, C.sub.1-3 alkylthio or C.sub.1-3 alkoxy; or together R.sub.4 and R.sub.5 form a 3 to 6 membered carbocyclic ring, or a heterocyclic ring containing one or two ring oxygen, nitrogen or sulphur atoms;or R.sub.4 and R.sub.5 together form an oxo or methylene group;each of R.sub.x and R.sub.y is hydrogen or C.sub.1-3 alkyl; n is zero or 1;R.sub.6 is hydrogen, lower alkyl, lower alkylcarbonyl, arylcarbonyl, aralkylcarbonyl, heteroarylcarbonyl, optionally substituted aminocarbonyl, lower alkoxycarbonyl and aryloxycarbonyl;R.sub.Type: GrantFiled: August 9, 1988Date of Patent: June 12, 1990Assignee: Laboratoires Sobio S.A.Inventors: Michel Martin, Guy Nadler, Richard Zimmermann
-
Patent number: 4923991Abstract: The invention provides a compound of formula III ##STR1## or an acid addition salt thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 are the same or different and represent hydrogen or lower alkyl, cycloalkyl, lower aralkyl or phenyl radicals any of which radicals may be substituted by lower alkyl, lower alkoxy or trifluoromethyl or R.sup.2 and R.sup.3 taken together, form a 5, 6 or 7 membered saturated ring, R.sup.4 and R.sup.5 may also represent lower alkoxy or cycloalkoxy, n is 1, 2 or 3 and, if more than one R.sup.4 radical is present the R.sup.4 radicals may be the same or different and esters of carboxylic acids with the hydroxy group shown, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and n are as defined above, with the provisos that (1) R.sup.6 and R.sup.7 are other than hydrogen when R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are all hydrogen and (2) R.sup.6 and R.sup.7 are not both methyl when R.sup.4 is methyl.Type: GrantFiled: December 16, 1988Date of Patent: May 8, 1990Assignee: John Weyth & Brother LimitedInventors: Roger Crossley, Kenneth Heatherington
-
Patent number: 4921861Abstract: The 3-amino-4-ethylthio-quinoline of the Formula I ##STR1## and pharmaceutically acceptable acid addition salts thereof possess useful therapeutical properties. They exhibit a potent and highly selective anxiolytic and narcosis potentiating effect and are devoid of sedative and anti-convulsive effect. Consequently, the invention relates to pharmaceutical compositions comprising the compound of Formula I or a salt thereof as active agent.The invention also relates to a new and improved process for the preparation of the compound of Formula I.Type: GrantFiled: April 22, 1988Date of Patent: May 1, 1990Assignee: BASF AktiengesellschaftInventors: Jozsef Knoll, ne Simonyi Budai, Edit Berenyi ne Poldermann, Ildiko Miklya, Marton Fekete, Gabriella Zsilla, Berta Knoll, Attila Mandi, Lujza Petocz, Istvan Gyertyan, Istvan Gacsalyi
-
Patent number: 4921955Abstract: The invention relates to a process for the preparation of 1,5-disubstituted imidazoles of the formula ##STR1## by alkylation of an N-cyanoformamidine of the formula IIX--NH--CH.dbd.N--CH (II)to form an N,N-disubstituted N'-cyanoformamidine of the formula ##STR2## which is cyclised under the action of bases to form a 4-aminoimidazole of the formula ##STR3## and then reduced to form the product of the formula I. The invention relates also to a special process for the reduction of the aminoimidazole V to I, and to intermediate compounds for carrying out this process and to processes for the preparation of the intermediate compounds.The meaning of the substituents X and L is explained in detail in the text.Type: GrantFiled: December 18, 1987Date of Patent: May 1, 1990Assignee: Ciba-Geigy CorporationInventor: Werner Topfl
-
Patent number: 4920133Abstract: This invention relates to certain quinoline-diaryl compounds and their use as leukotriene D.sub.4 antagonists for the treatment of hypersensitive disorders.Type: GrantFiled: November 3, 1987Date of Patent: April 24, 1990Assignee: Rorer Pharmaceutical Corp.Inventors: Fu-chi Huang, Robert A. Galemmo, Jr., Henry F. Campbell
-
Patent number: 4920132Abstract: This invention relates to certain quinoline-diaryl compounds and their use as leukotriene D.sub.4 antagonists for the treatment of hypersensitive disorders.Type: GrantFiled: November 3, 1987Date of Patent: April 24, 1990Assignee: Rorer Pharmaceutical Corp.Inventors: Fu-chi Huang, Robert A. Galemmo, Jr., Henry F. Campbell
-
Patent number: 4920130Abstract: This invention relates to certain quinoline-diaryl compounds and their use as leukotriene D.sub.4 antagonists for the treatment of hypersensitive disorders.Type: GrantFiled: November 3, 1987Date of Patent: April 24, 1990Assignee: Rorer Pharamceutical Corp.Inventors: Fu-chi Huang, Robert A. Galemmo, Jr., Henry F. Campbell
-
Patent number: 4920225Abstract: Optically active compounds of formula 1 ##STR1## wherein R.sub.1 is H or lower alkyl;R.sub.2 and R.sub.6 are each independently lower alkyl, aryl, or arylalkyl;R.sub.3 is CN, NO.sub.2, CO.sub.2 R.sub.5, CONHR.sub.5, SO.sub.2 R.sub.5, or P(O)(OR.sub.5).sub.2, where R.sub.5 is lower alkyl, lower alkoxyalkyl, aryl, or arylalkyl;R.sub.4 is aryl, heterocyclyl, or fused-ring heterocyclyl, optionally substituted with one, two, or three halo, NO.sub.2, CN, lower alkyl, lower alkoxy, lower alkylamino, CF.sub.3, OCH.sub.2 F, or OCF.sub.3 ;are prepared by fractional crystallization from hot organic solvent and water in the presence of a suitable optically active amine base.Type: GrantFiled: December 22, 1986Date of Patent: April 24, 1990Assignee: Laboratoires Syntex S.A.Inventor: Gilles Genain
-
Patent number: 4918081Abstract: This invention relates to quinolinyl compounds of the general formula: ##STR1## and the use of these compounds as pharmacological agents which are lipoxygenase inhibitors and/or leukotriene antagonists possessing anti-inflammatory and anti-allergic properties and their pharmaceutical compositions and processes for this preparation.Type: GrantFiled: June 20, 1988Date of Patent: April 17, 1990Assignee: Rorer Pharmaceutical Corp.Inventors: Fu-Chi Huang, Robert A. Galemmo, Jr., Henry F. Campbell