Plural Chalcogens Attached Directly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 546/142)
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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: 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
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Patent number: 4983613Abstract: This invention relates to isoquinoline acetic acids and acetyl carbamates and their pharmaceutically acceptable salts thereof, to processes for their preparation, to methods for using the compounds, and to pharmaceutical preparations thereof. The compounds have pharmaceutical properties which render them beneficial for the treatment of diabetes mellitus and associated conditions.Type: GrantFiled: April 21, 1989Date of Patent: January 8, 1991Assignee: American Home Products CorporationInventor: Michael S. Malamas
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Patent number: 4975438Abstract: Compounds of the formula ##STR1## Y is O or S, *A is paraphenylene or *--(CH.sub.2).sub.n --(X).sub.m --(CH.sub.2).sub.r --, X is O, S or --CH.dbd.CH--, n or r, independently, are integers from 0 to 3, s is an integer from 0 to 1, m is an integer from 0 to 1, provided that when m is 1, n+s must be at least 2, R.sub.1 and R.sub.2, independently, are hydrogen, lower alkyl, cycloalkyl, lower alkenyl, Het, Aryl, R.sub.3, R.sub.4 and R.sub.8, independently, are hydrogen, lower alkyl, aryl, R.sub.5 and R.sub.6, independently, are hydrogen or lower alkyl, R.sub.7 is hydrogen, lower alkyl, cycloalkyl, Het-lower alkyl or aryl, Het is a monocyclic 5- or 6-membered hetero aromatic or a bicyclic heteroaromatic radical containing one or two hetero atoms selected from nitrogen, oxygen and sulfur, which radical may be substituted by lower alkyl, halogen or aryl, and the asterisk denotes the point of attachment,and when R.sub.6 and R.sub.7 are different, their enantiomers and racemic mixtures thereof, when R.sub.1 and R.sub.Type: GrantFiled: September 6, 1988Date of Patent: December 4, 1990Assignee: Hoffmann-La Roche Inc.Inventors: Robert W. Guthrie, Richard W. Kierstead, Jefferson W. Tilley
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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: 4966906Abstract: Novel 1-aryl-3-quinolinecarboxamides and 1-aryl-3-isoquinolinecarboxamides, processes for the preparation thereof, and methods for treating pain and inflammation utilizing compounds and compositions thereof are disclosed.Type: GrantFiled: July 14, 1988Date of Patent: October 30, 1990Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Edward J. Glamkowski, R. Richard L. Hamer
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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
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Patent number: 4952588Abstract: Novel 1-aryl-3-quinolinecarboxamides and 1-aryl-3-isoquinolinecarboxamides, processes for the preparation thereof, and methods for treating pain and inflammation utilizing compounds and compositions thereof are disclosed.Type: GrantFiled: August 31, 1989Date of Patent: August 28, 1990Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Edward J. Glamkowski, R. Richard L. Hamer
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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
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Patent number: 4948418Abstract: This invention pertains to novel heterocyclic 2,3-dihydrobenzofuran and chromane compounds, including stereoisomers, agriculturally suitable compositions containing them, and their use as broad spectrum herbicides.Type: GrantFiled: August 30, 1989Date of Patent: August 14, 1990Assignee: E. I. Du Pont de Nemours and CompanyInventor: Joseph E. Semple
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Patent number: 4942169Abstract: A novel piperidine derivative is defined by the formula (I), including a salt thereof, ##STR1## wherein R.sup.1 denotes a univalent group derived from one selected among substituted or unsubstituted benzene, pyridine, pyrazine, indole, anthraquinone, quinoline, substituted or unsubstituted phthalimide, homophthalimide, pyridinecarboxylic acid imide, pyridine N-oxide, pyrazinedicarboxylic acid imide, naphthalenedicarboxylic acid imide, substituted or unsubstituted quinazolinedione, 1,8-naphthalimide, bicyclo [2.2.2.] oct-5-ene-2,3-dicarboxylic acid imide and pyromerylimide,X denotes a group of the formula --(CH.sub.2).sub.n --, a group of the formula --O(CH.sub.2).sub.n --, a group of the formula --S(CH.sub.2).sub.n --, a group of the formula --NH(CH.sub.2).sub.n --, a group of the formula --SO.sub.2 NH(CH.sub.2).sub.n --, a group of the formula ##STR2## a group of the formula ##STR3## a group of the formula ##STR4## a group of the formula --CH.sub.2 NH(CH.sub.2).sub.Type: GrantFiled: March 10, 1989Date of Patent: July 17, 1990Assignee: Eisai Co., Ltd.Inventors: Hachiro Sugimoto, Takaharu Nakamura, Yutaka Tsuchiya, Hiroyuki Sugumi, Kunizou Higurashi, Norio Karibe, Yoshiharu Yamanishi, Hiroo Ogura, Shin Araki, Atsuhiko Kubota, Michiko Ohtake, Kiyomi Tamatsu
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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: 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
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Patent number: 4906643Abstract: N-(3-hydroxy-4-piperidinyl)substituted benzamides, their N-oxide forms and pharmaceutically acceptable acid-addition salts having gastrointestinal motility stimulating properties, compositions containing the same, and methods of treating warm blooded animals suffering from a decreased peristalsis of the gastrointestinal system.Type: GrantFiled: June 10, 1988Date of Patent: March 6, 1990Assignee: Janssen Pharmaceutica N.V.Inventors: Georges H. P. Van Daele, Freddy F. Vlaeminck, Karel J. Van Loon
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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: 4886803Abstract: Compounds are described of formula (I) ##STR1## wherein R.sup.1 is a hydrogen atom, an alkyl group, an alkoxy group, a dialkylamino group or a halogen atom; n is 1 to 4; R.sup.2 is a hydrogen atom, an alkyl group, an unsubstituted or substituted aminoalkyl group, an acyl group, an unsubstituted or substituted aralkyl group, a carboxyalkyl group, an alkoxycarbonyalkyl group or ##STR2## wherein X is an unsubstituted or substituted-phenyl, -benzyl, -benzoyl or -furoyl group; A is -NR.sup.3 - where R.sup.3 is hydrogen or alkyl, an alkylene or an alkylidene; and B is a heterocyclic group selected from triazolyl, pyridyl, pyridazinyl, pyrimidinyl, pyrazinyl, benzimidazolyl, benzothiazolyl, quinolyl and isoquinolyl, said heterocyclic group being optionally substituted by one or more alkyl, alkoxy, nitro or phenyl group, and the physiologically acceptable acid addition salts thereof. The compound of formula (I) are or cardiotonic activity and thus may be useful for the treatment of circulatory diseases.Type: GrantFiled: July 15, 1987Date of Patent: December 12, 1989Assignee: Nisshin Flour Milling Co., Ltd.Inventors: Noriyoshi Sueda, Yoshikuni Suzuki, Toshiji Sugai, Hiroaki Yamada, Makoto Yanai
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Patent number: 4881967Abstract: This invention pertains to novel heterocyclic 2,3-dihydrobenzofuran and chromane compounds, including stereoisomers, agriculturally suitable composition containing them, and their use as broad spectrum herbicides.Type: GrantFiled: June 2, 1988Date of Patent: November 21, 1989Assignee: E. I. Du Pont De Nemours and CompanyInventor: Joseph E. Semple
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Patent number: 4874803Abstract: The present invention comprises reaction products resulting from the reaction of hydrazido-substituted or certain amino-substituted polymer stabilizers and cyclic dianhydrides, as well as the use of such products. The polymer stabilizers of the invention are useful for protecting a large variety of synthetic polymeric organic materials from the degradative effects of heat, light and oxygen. Some of the modifiers are flame retardants and many are metal deactivators in addition to their primary activity.Type: GrantFiled: September 21, 1987Date of Patent: October 17, 1989Assignee: Pennwalt CorporationInventors: Arthur L. Baron, Terry N. Myers, Jerome Wicher
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Patent number: 4871387Abstract: New pyri(mi)dyl-oxy- or -thio-benzoic acid derivatives of the formula ##STR1## are taught which have herbicidal and plant growth regulating activity. In the formula Z can be Ch or N, X is oxygen or sulphur, A is oxygen, sulphur, a radical R.sup.5 --N.dbd.or a radical R.sup.6 O--N.dbd.and B is oxygen, sulphur, a radical ##STR2## with the proviso that at least one of the radicals R.sup.1, R.sup.2 or R.sup.3 represents alkyl or a part of a 3- to 6-membered fused carbocyclic ring.Type: GrantFiled: December 4, 1986Date of Patent: October 3, 1989Assignee: Bayer AktiengesellschaftInventors: Klaus Sasse, Reiner Fischer, Hermann Hagemann, Hans-Joachim Santel, Robert R. Schmidt, Kalus Lurssen
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Patent number: 4866075Abstract: The invention concerns compounds of formula: ##STR1## wherein R.sub.1 is hydrogen, lower alkyl, halogen, lower alkoxy or hydroxy; R.sub.2 represents hydrogen or lower alkyl; A represents an alkylene, oxoalkylene or hydoxyalkylene chain each having 2 to 6 carbon atoms, R.sub.3 and R.sub.4 may be in the same or different rings and independently represent hydrogen, lower alkyl, lower alkoxy, amino or halogen and one of X and Y represents nitrogen the other represents CR.sub.5 wherein R.sub.5 is one of the values for R.sub.3 or R.sub.5 is the bond to the NHCO group; or a pharmaceutically acceptable salt thereof, which compounds possess antihypertensive activity whilst exhibiting reduced CNS depressant properties. Also disclosed are processes for preparing the compounds and pharmaceutical compositions containing them.Type: GrantFiled: August 12, 1988Date of Patent: September 12, 1989Assignee: John Wyeth and Brother LimitedInventors: John L. Archibald, Terence J. Ward, Janet C. White
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Patent number: 4863945Abstract: Pyrrolobenzimidazoles of the formula: ##STR1## are useful for treatment of heart and circulatory diseases. R.sub.1 is substituted phenyl; or optionally substituted naphthyl or a five- or six-membered heterocyclic group which can be condensed with a phenyl ring to form a bicyclic radical. R.sub.2 is hydrogen, alkyl, alkenyl or cycloalkenyl; R.sub.3 is alkyl, alkenyl or hydroxyalkyl or with R.sub.2 together forms cycloakylene; or R.sub.2 and R.sub.3 together form alkylidene or cycloalkylidene. R.sub.4 is hydrogen or lower alkanoyl. X is a valency bond, alkylene, vinylene, imino or carbonylamino. T stands for two hydrogen atoms. When X is a valency bond, R.sub.1 can also be hydrogen, hydrocarbyl which may also contain oxygen, amino, sulfur, carbonyl and sulfonyl groups. When X is imino or carbonylamino or when R.sub.1 is a bicyclic radical, T can also be oxygen. The compounds also include the tautomers and physiologically acceptable salts with inorganic and organic acids.Type: GrantFiled: December 10, 1987Date of Patent: September 5, 1989Assignee: Boehringer Mannheim GmbHInventors: Walter-Gunar Friebe, Alfred Mertens, Klaus Strein, Erwin Boehm
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Patent number: 4849431Abstract: A novel piperidine derivative or a pharmacologically acceptable salt thereof is used in the treatment and prevention of dementias and sequelae of cerebrovascular diseases. These compounds also exhibit strong, highly selective anticholinesterase activity and may be orally or parenterally administered.Type: GrantFiled: December 24, 1986Date of Patent: July 18, 1989Assignee: Eisai Co., Ltd.Inventors: Hachiro Sugimoto, Takaharu Nakamura, Yutaka Tsuchiya, Hiroyuki Sugumi, Kunizou Higurashi, Norio Karibe, Yoshiharu Yamanishi, Hiroo Ogura, Shin Araki, Atsuhiko Kubota, Michiko Ohtake, Kiyomi Tamatsu
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Patent number: 4847202Abstract: Certain novel heterocyclic compounds, aromatic thioesters, their preparation, and their use in inhibiting serine proteases with chymotrypsin-like and elastase-like specificity and in the treatment of diseases such as emphysema which involve tissue proteolysis.Type: GrantFiled: March 26, 1986Date of Patent: July 11, 1989Assignee: Georgia Tech Research InstituteInventor: James C. Powers
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Patent number: 4826531Abstract: Acrylic acid derivatives having the formula (I): ##STR1## and stereoisomers thereof, wherein W is R.sup.1 O.sub.2 C--C.dbd.CH--ZR.sup.2, R.sup.1 and R.sup.2 are alkyl or fluoroalkyl groups, and Z is oxygen or sulphur; A, B, D and E are hydrogen, halogen, hydroxy or optionally substituted alkyl, alkoxy, aralkyl, arylalkoxy, alkenyl, alkynyl, aryl, aryloxy, arylthio, heteroaryloxy, heteroarylthio, acyloxy, amino, arylazo or acylamino, nitro, cyano, --CO.sub.2 R.sup.3, --CONR.sup.3 R.sup.4, --COR.sup.3, --CR.sup.3 .dbd.NR.sup.4, --N.dbd.CR.sup.3 R.sup.4 or --S(O).sub.n R.sup.3 groups; any two of the groups A, B, D and E, when they are in adjacent positions on the ring, optionally join to form a fused ring, n is 0, 1 or 2; and R.sup.3 and R.sup.4 are hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl or optionally substituted aryl or aralkyl; and metal complexes thereof. These compounds are useful as fungicides, insecticides, nematicides or plant growth regulators.Type: GrantFiled: April 17, 1987Date of Patent: May 2, 1989Assignee: Imperial Chemical Industries PLCInventors: Vivienne M. Anthony, John M. Clough, Paul DeFraine, Christopher R. A. Godfrey, Patrick J. Crowley, Kenneth Anderton
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Patent number: 4824835Abstract: The present invention provides isoquinolinedione derivatives of the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom or an alkyl, alkenyl or cycloalkyl radical which is optionally interrupted by a heteroatom or by a heteroatom substituted with an alkyl radical, R.sub.2 is a hydrogen atom or an alkyl or alkenyl radical, or together with R.sub.1, represents a cycloalkylene, alkylidene or cycloalkylidene radical which is optionally interrupted by a heteroatom or by a heteroatom substituted by an alkyl radical and R.sub.3 is a radical of the general formula: ##STR2## which can be in the 5- 6-, 7- or 8-position of the isoquinoline-1,3-dione and in which R.sub.4 and R.sub.5, which can be the same or different, are hydrogen atoms or alkyl, trihaloalkyl, cycloalkyl, cycloalkenyl, dealkylaminoalkyl, alkoxycarbonylalkyl, alkylcarbonyl, aryl or heterayl radicals and X is an oxygen or sulphur atom or a radical of the general formula .dbd.N--R.sub.6, in which R.sub.Type: GrantFiled: April 24, 1987Date of Patent: April 25, 1989Assignee: Boehringer Mannheim GmbHInventors: Alfred Mertens, Bernd Muller-Beckmann
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Patent number: 4822800Abstract: Substituted 3-isoquinolinol compounds of the general formula ##STR1## that exhibit cardiotonic, renal vasodilating and phosphodiesterase fraction III properties are pharmacologically active in the treatment of cardiac conditions. Methods for synthesizing and using those compounds are described.Type: GrantFiled: June 9, 1986Date of Patent: April 18, 1989Assignee: Ortho Pharmaceutical CorporationInventors: Robert Falotico, Ramesh M. Kanojia, Jeffery B. Press, Alfonso J. Tobia
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Patent number: 4794123Abstract: This invention relates to a method of treating ulcers or hypersecretion in a mammal which comprises administering a compound of formula ##STR1## or a pharmaceutically acceptable salt thereof wherein --B--B.sup.1 -- represents a chain of formula--CR.sup.5 .dbd.CR.sup.6 -- (Ib)or--(CHR.sup.5).sub.n --CR.sup.6 .dbd. (Ic);R represents an optionally substituted aryl or heteroaryl radical; R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represent hydrogen, or a defined substituent or any adjacent pair of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 together with the carbon atoms to which they are attached complete a five or six membered saturated or unsaturated carbocyclic or heterocyclic ring, said ring being optionally substituted by a defined substituent said heterocyclic ring having at least one heteroatom selected from oxygen, nitrogen and sulphur. Novel compositions and compounds of formula I are also disclosed.Type: GrantFiled: October 13, 1987Date of Patent: December 27, 1988Assignee: John Wyeth & Brother LimitedInventors: Roger Crossley, Peter J. Meade
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Patent number: 4771059Abstract: 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## X.sup.-, wherein X.sup.- is the anion of a non-toxic pharmaceutically acceptable acid, are also disclosed.Type: GrantFiled: August 29, 1985Date of Patent: September 13, 1988Assignee: University of FloridaInventor: Nicholas S. Bodor
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Patent number: 4761403Abstract: Hydroxy quinol-1-one and quinol-2-one based compounds found to be potent inhibitors of 5-, 12-, and 15-lipoxygenase enzymes.Type: GrantFiled: April 9, 1986Date of Patent: August 2, 1988Assignee: Abbott LaboratoriesInventors: Bruce P. Gunn, James B. Summers, Jr.
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Patent number: 4757078Abstract: Cyclic aryl hydroxamic acids and derivatives thereof are provided having the structure ##STR1## wherein R is H or arylalkyl, and including acid-addition salts thereof. These compounds are useful as inhibitors of leukotriene production and as such are useful as antiallergy, anti-inflammatory and anti-psoriatic agents.Type: GrantFiled: November 28, 1986Date of Patent: July 12, 1988Assignee: E. R. Squibb & Sons, Inc.Inventor: Raj N. Misra
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Patent number: 4751178Abstract: New substrates for .gamma.-glutamyltransferase (.gamma.-GT) are disclosed. These subtrates are useful in the colorimetric determination of .gamma.-GT since the cleavage of the .gamma.-glutamyl group produces a detectable species--an aminostyrylquinolinium dye. The substrates have the formula: ##STR1## wherein: R and R.sub.1 are independently selected from hydrogen, alkyl and alkoxy andQ is ##STR2## wherein: R.sub.2 is alkyl having from 1 to 4 carbon atoms;R.sub.3 and R.sub.4 are independently selected from hydrogen, alkyl, alkoxy, nitro, cyano and halogen; andX.sup..crclbar. is an anion.Type: GrantFiled: September 26, 1985Date of Patent: June 14, 1988Assignee: Eastman Kodak CompanyInventors: Bruce E. Babb, Roy E. Snoke
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Patent number: 4751309Abstract: 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: September 15, 1986Date of Patent: June 14, 1988Assignee: BASF AktiengesellschaftInventors: Ewald Daltrozzo, Werner Sulger
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Patent number: 4746669Abstract: Thiazole derivatives have been made, for example, by reacting a 2-aryl-2,2-dialkoxyethylamine with an appropriately substituted aryl acetyl halide followed by treating the resulting amide with diphosphoryl pentasulfide. The thiazole derivatives are found to be effective immunoregulants.Type: GrantFiled: March 26, 1987Date of Patent: May 24, 1988Assignee: Merck & Co., Inc.Inventors: Charles G. Caldwell, Ihor Kopka, Milton L. Hammond, Robert A. Zambias
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Patent number: 4725605Abstract: This invention relates to a method of treating ulcers or hypersecretion in a mammal which comprises administering a compound of formula ##STR1## or a pharmaceutically acceptable salt thereof wherein --B--B.sup.1 -- represents a chain of formula--CR.sup.5 .dbd.CR.sup.6 -- (Ib)or--(CHR.sup.5).sub.n --CR.sup.6 .dbd. (Ic);R represents an optionally substituted aryl or heteroaryl radical; R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represent hydrogen, or a defined substituent or any adjacent pair of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 together with the carbon atoms to which they are attached complete a five or six membered saturated or unsaturated carbocyclic or heterocyclic ring, said ring being optionally substituted by a defined substituent said heterocyclic ring having at least one heteroatom selected from oxygen, nitrogen and sulphur. Novel compositions and compounds of formula I are also disclosed.Type: GrantFiled: May 22, 1986Date of Patent: February 16, 1988Assignee: John Wyeth & Brother LimitedInventors: Roger Crossley, Peter J. Meade
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Patent number: 4721710Abstract: The present invention relates to derivatives of piperidinedione of formula: ##STR1## in which R is alkyl or forms with N a possibly substituted morpholino or piperidino group, n=2 or 3, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 represent H or lower alkyl; R.sub.3 and R.sub.4 taken together may represent (CH.sub.2).sub.m where m=4 or 5 and R.sub.2 and R.sub.3 taken together may represent (CH.sub.2).sub.p where p=3 or 4 and in this case R.sub.1 and R.sub.4 =H, R.sub.5 is H or alkyl. It also relates to a process for manufacturing the product of formula (I) and to the drugs containing a product of formula (I).Type: GrantFiled: March 10, 1986Date of Patent: January 26, 1988Assignee: SanofiInventors: Claude Bernhart, Werner Cautreels, Patrick Gautier
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Patent number: 4680400Abstract: The invention concerns novel compounds of the formula I ##STR1## wherein: A, B, D and E are selected from CH, N and N-Z wherein Z is selected from oxygen and the group YAn wherein Y is selected from alkyl and benzyl and An is an anion, and provided that no more than three of A, B, D and E are selected from N and N-Z and no more than one of A, B, D and E is selected from N-Z;W is a saturated or unsaturated C.sub.2 to C.sub.5 hydrocarbon chain;X and X.sup.1 are independently selected from halogen, nitro, cyano, alkyl, substituted alkyl, hydroxy, alkoxy, substituted alkoxy, alkenyl, alkenyloxy, alkynyl, alkynyloxy, acyloxy, alkoxycarbonyl, alkylthio, alkylsulfinyl, alkylsulfonyl, sulfamoyl, substituted sulfamoyl, alkanoyloxy, benzyloxy, substituted benzyloxy, amino, substituted amino and the groups formyl and alkanoyl and the oxime, imine and Schiff base derivatives thereof, or two of X.sup.1 on the same carbon atom may form an oxo group;R.sup.Type: GrantFiled: November 12, 1986Date of Patent: July 14, 1987Assignee: ICI Australia LimitedInventors: Graham J. Bird, Graeme J. Farquharson, Keith G. Watson
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Patent number: 4659833Abstract: Four different optical isomers of a new compound, 1-[2'-(o-methoxyphenoxy)-1'-methylethylamino]-3-(4"-isocarbostyriloxy)-2-p ropanol are now provided as new substances. These four optical isomers are now named as (2R, 1'S)-1-[2'-(o-methoxyphenoxy)-1'-methylethylamino]-3-(4"-isocarbostyriloxy )-2-propanol, (2S, 1'S)-1-[2'-(o-methoxyphenoxy)-1'-methylethylamino]-3-(4"-isocarbostyriloxy )-2-propanol, (2S, 1'R)-1-[2'-(o-methoxyphenoxy)-1'-methylethylamino]-3-(4"-isocarbostyriloxy )-2-propanol, and (2R, 1'R)-1-[2'-(o-methoxyphenoxy)-1'-methylethylamino]-3-(4"-isocarbostyriloxy )-2-propanol, respectively. These four optical isomers have different activities for their .beta.-adrenergic-blocking effect and .alpha.-adrenergic-blocking effect and are useful as valuable agents for therapeutic treatment of various cardiovascular diseases, as compared to an optically inactive racemic mixture of said isomer compounds.Type: GrantFiled: May 8, 1985Date of Patent: April 21, 1987Assignee: Nisshin Flour Milling Co., Ltd.Inventors: Toshihiro Takahashi, Noriyoshi Sueda, Masahiro Tsuji, Yoshiyuki Tahara, Hiroyasu Koyama, Yoshikuni Suzuki, Masao Nagase, Toshiji Sugai
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Patent number: 4657908Abstract: The invention relates to carbonyl derivatives which are histamine H-2 antagonists and which inhibit gastric acid secretion. According to the invention where is provided a guanidine derivative of the formula I: ##STR1## in which R.sup.1 and R.sup.2, same or different, are hydrogen or 1-10C alkyl, 3-8C cycloalkyl or 4-14C cycloalkylalkyl, each alkyl, cycloalkyl or cycloalkylalkyl optionally carrying one or more F, Cl or Br atoms, provided that one of R.sup.1 and R.sup.2 is halogen substituted, or R.sup.2 is hydrogen and R.sup.1 is R.sup.5 -E-W in which W is 2-6C alkylene optionally substituted by 1 or 2 1-4C alkyls, E is O, S, SO, SO.sub.2 or NR.sup.6 in which R.sup.6 is H or 1-6C alkyl, R.sup.5 is H or 1-6C alkyl optionally substituted by 1 or 2 1-4C alkyls, or R.sup.5 and R.sup.6 are joined to form a pyrrolidine, piperidine, morpholine, piperazine or N-methylpiperazine ring, or R.sup.2 is H and R.sup.Type: GrantFiled: February 12, 1985Date of Patent: April 14, 1987Assignees: ICI Americas, Inc., Imperial Chemical Industries PLCInventors: Tobias O. Yellin, David J. Gilman, Philip N. Edwards, Michael S. Large, Derrick F. Jones, Keith Oldham
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Patent number: 4634713Abstract: Certain 3-(ureidocyclohexyleneamino)propane-1,2-diol derivatives, such as the compounds of formula III below, represent novel and useful pharmaceutical agents, e.g. potent antihypertensive and cardioactive agents demonstrating both .alpha.- and .beta.-adrenergic blocking activity. ##STR1## R.sub.3 is hydrogen or lower alkyl; R.sub.7 is cyano, lower alkoxycarbonyl, pyrrolyl, morpholino, alkenyloxy of 3 to 6 carbon atoms, alkynyloxy of 3 to 6 carbon atoms, alkoxy of 1 to 3 carbon atoms substituted by cyclopropyl.Type: GrantFiled: August 19, 1985Date of Patent: January 6, 1987Assignee: Ciba-Geigy CorporationInventors: Lincoln H. Werner, Neville Ford
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Patent number: 4615726Abstract: Compounds of the formula ##STR1## wherein A denotes N or CR.sup.4, B denotes a carboxyl, carbo-(thio) ester, (substituted) carboxamide or carboxanilide, carbohydroxy(alkoxy)-amide, (substituted) carbohydrazide or (substituted) oxazoline group, X and Y denote, inter alia, alkyl or, together, spiroalkyl, Z denotes a carbo-(di)(thio) ester, carboxyl, (substituted) (thio)-carboxamide or -carboxanilide group or the radical of a ketone-acid or of a ketone-ester and R.sup.1, R.sup.2, R.sup.3 and R.sup.4 denote H or are identical or different and denote halogen, alkyl, alkoxy, alkoxycarbonyl, halogenoalkyl, NO.sub.2, CN, (substituted) phenyl or phenoxy, or two of these radicals can form a --CH.dbd.CH--CH.dbd.CH-- group, are useful total or selective herbicides for application by the pre-emergence and, in some cases, the post-emergence method.Type: GrantFiled: December 18, 1984Date of Patent: October 7, 1986Assignee: Hoechst AktiengesellschaftInventors: Roland Schmierer, Reinhard Handte, Hilmar Mildenberger, Klaus Bauer, Hermann Bieringer, Helmut Burstell
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Patent number: 4614535Abstract: Imidazolinones of the formula ##STR1## in which A denotes N or C--R.sup.4 ; B denotes halogenoalkyl, alkoxymethyl, cyanomethyl or thiocyanatomethyl; X denotes alkyl; and Y denotes alkyl, cycloalkyl, alkenyl, phenyl or benzyl; or X and Y, together with C, denote a spiro-cycloalkyl group; Z denotes H, (substituted) alkyl, alkenyl, propargyl or an alkyl, carboxylic acid ester or sulfonic acid ester group; and R.sup.1 -R.sup.4 denote H, halogen, alkyl, alkoxy, alkoxycarbonyl, halogenoalkyl, NO.sub.2, CN, (substituted) phenoxy or (substituted) phenyl, or in each case two adjacent radicals together denote the radical --CH.dbd.CH--CH--CH--, are active herbicides and growth regulators.Type: GrantFiled: November 8, 1984Date of Patent: September 30, 1986Assignee: Hoechst AktiengesellschaftInventors: Roland Schmierer, Reinhard Handte, Rainer Liebl, Hilmar Mildenberger, Klaus Bauer, Hermann Bieringer, Helmut Burstell
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2,4-diamino-(substituted-benzopyran(quinolyl,isoquinoly)methyl)pyrimidine s useful as antibacterials
Patent number: 4587342Abstract: Novel 2,4-diaminopyrimidines having substituted heterobicyclomethyl moieties in the 5-position have superior antibacterial properties.Type: GrantFiled: October 31, 1983Date of Patent: May 6, 1986Inventors: Susan M. Daluge, Paul M. Skonezny -
Patent number: 4576954Abstract: New derivatives of the general formula (I) in which:R=H or Cl and either R.sub.1 and R.sub.2 form a tetrahydroquinoxaline, tetrahydroquinoline, tetrahydroisoquinoline, dihydrobenzoxazine, tetrahydro-1H-benzazepine or isoindoline ring, it being possible for all these rings to be substituted by one or more halogen, carboxyl, alkoxycarbonyl, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, trifluoromethyl, cyano, nitro, alkoxy, alkylthio or alkyl, substituted by carboxyl, alkoxycarbonyl, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, hydroxyl, amino, alkylamino or dialkylamino, or R.sub.1 =alkyl and R.sub.2 =alkyl substituted by phenyl which is itself unsubstituted or substituted by one or more halogen, alkyl, alkoxy, alkylthio, hydroxy, amino, alkylamino, dialkylamino, carboxy, alkoxycarbonyl, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, trifluoromethyl, cyano or nitro, all the alkyls having 1 to 4 C in a straight or branched chain.These new products are used as antirheumatics.Type: GrantFiled: February 21, 1984Date of Patent: March 18, 1986Assignee: Phone-Poulenc SanteInventors: Jean-Dominique Bourzat, Claude Cotrel, Daniel Farge, Jean-Marc Paris, Gerard Taurand
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Patent number: 4535092Abstract: Acylanilides of the formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are substituents defined in claim 1; wherein R.sup.4 is hydrogen or alkyl of up to 4 carbon atoms, or is joined to R.sup.5 as stated below;wherein R.sup.5 is hydrogen, hydroxy, or alkoxy or acyloxy each of up to 15 carbon atoms, or is joined to R.sup.4 to form an oxycarbonyl group such that together with the --N--CO--C-- part of the molecule it forms an oxazolidinedione group;wherein R.sup.6 is alkyl or halogenoalkyl of up to 4 carbon atoms;and wherein R.sup.7 is 5- or 6- membered saturated or unsaturated heterocyclic which contains one, two or three hetero atoms selected from oxygen, nitrogen and sulphur, which heterocyclic may be a single ring or may be fused to a benzo-ring, and which heterocyclic is unsubstituted or bears one or two substituents defined in claim 1;processes for their manufacture and pharmaceutical compositions containing them. The compounds possess antiandrogenic activity.Type: GrantFiled: November 1, 1982Date of Patent: August 13, 1985Assignee: Imperial Chemical Industries PLCInventor: Leslie R. Hughes
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Patent number: 4520025Abstract: A class of bicyclic nitrogen heterocyclic ether and thioether compounds exhibiting pharmacological activity including anti-secretory and anti-ulcerogenic activity, pharmaceutical compositions comprising these compounds, and methods for the treatment of gastrointestinal hyperacidity and ulcerogenic disorders in mammals using said compositions are disclosed.Type: GrantFiled: July 21, 1982Date of Patent: May 28, 1985Assignee: William H. Rorer, Inc.Inventors: Henry F. Campbell, Donald E. Kuhla, William L. Studt, Stuart A. Dodson
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Patent number: 4517365Abstract: Isocarbostyrils of the formula ##STR1## wherein R is a branched alkyl of 3 to 4 carbon atoms, and the acid addition salts thereof, having .beta.-adrenergic blocking activity, are described.Type: GrantFiled: June 22, 1982Date of Patent: May 14, 1985Assignee: Nisshin Flour Milling Co., Ltd.Inventors: Hiroyasu Koyama, Masahiro Tsuji, Yoshikuni Suzuki
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Patent number: 4497813Abstract: Derivatives of 3-aminopropane-1,2-diol of the formula ##STR1## in which Ar represents optionally substituted aryl,n represents the number 0 or 1, andalk represents alkylene having 2 to 5 carbon atoms, the nitrogen atom and the oxygen atom, or, if n is zero, the phenyl radical, being separated from one another by at least two carbon atoms, andR.sub.1 and R.sub.2, independently of one another, each represents hydrogen or lower alkyl, or together they represent lower alkylene, oxa-lower alkylene, thia-lower alkylene, aza-lower alkylene or N-lower alkyl-aza-lower alkylene,and salts of such compounds, processes for their manufacture, medicaments containing the new compounds and their use for the treatment of Angina pectoris and cardiac arrhythmia, and as blood pressure-reducing agents, as well as for the treatment of reactive or endogenic states of depression.Type: GrantFiled: May 14, 1982Date of Patent: February 5, 1985Assignee: Ciba-Geigy CorporationInventors: Franz Ostermayer, Markus Zimmermann
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Patent number: 4491544Abstract: A compound having the formula (I): ##STR1## wherein D is a radical of a heterocyclic or aromatic component selected from the group of aniline, anthraquinone, phthalimide or aminobenzene radicals, wherein the radical is unsubstituted or is substituted by fluorine, chlorine, bromine, nitro, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, trifluoromethyl, cyano, C.sub.1 -C.sub.4 -alkylsulfonyl, carboxylic acid ester groups, carbamyl, sulfamyl, 1,3,4- or 1,2,4-oxadiazolyl or acylamino groups; X is CO-- or --SO.sub.2 --; and R is an aliphatic, aromatic or heterocyclic radical selected from the group of C.sub.1 -C.sub.Type: GrantFiled: August 18, 1982Date of Patent: January 1, 1985Assignee: BASF AktiengesellschaftInventors: Volker Radtke, Heinrich Kowarsch, Erwin Hahn, Peter Hauser
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Patent number: 4409017Abstract: The invention concerns novel compounds of the formula I ##STR1## The compounds are herbicides and in further embodiments the invention provides: processes for the preparation of compounds of formula I; intermediates useful in the preparation of compounds of formula I; compositions containing as active ingredient compounds of formula I; and processes for severely damaging or killing unwanted plants by applying to the plants or to the growth medium of the plants an effective amount of a compound of formula I.Type: GrantFiled: June 16, 1981Date of Patent: October 11, 1983Assignee: ICI Australia LimitedInventors: Alexander Serban, Graham J. Bird, Lindsay E. Cross
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Patent number: 4369322Abstract: The known synthesis for the production of aromatic substituted acetonitriles by reaction of aromatic substances with cyanogen chloride in the gas phase is improved by feeding the starting materials in gaseous form and separated from each other into the reactor. The process can be used to synthesize in general aromatic and especially hetero-aromatic substituted acetonitrile.Type: GrantFiled: March 9, 1981Date of Patent: January 18, 1983Assignee: Degussa AGInventors: Peter Schalke, Axel Kleemann