The Chalcogen, X, Is Part Of A -c(=x)x- Group, Wherein The X's Are The Same Or Diverse Chalcogens Patents (Class 549/79)
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Patent number: 4902709Abstract: Novel antihypercholesterolemic compounds of structure (I) or (II), ##STR1## pharmaceutically acceptable salts, thereof and a novel process for preparing compounds of structure I, are disclosed.Type: GrantFiled: August 12, 1988Date of Patent: February 20, 1990Assignee: Merck & Co., Inc.Inventor: Gerald E. Stokker
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Patent number: 4898868Abstract: 3-Demethyl-4-fluoromevalonic acid derivatives, a process for the preparation thereof, pharmaceutical products based on these compounds, the use thereof, and intermediates3-Demethyl-4-fluoromevalonic acid derivatives of the formula I, and the corresponding dihydroxy carboxylic acid derivatives of the formula II ##STR1## in which R, X and Y have the stated meanings, processes for the preparation of these compounds, the use thereof as medicaments, and pharmaceutical products are described. In addition, new intermediates for the preparation of the compounds of the formula I and formula II are described.Type: GrantFiled: July 8, 1988Date of Patent: February 6, 1990Assignee: Hoechst AktiengesellschaftInventors: Andreas Bergmann, Wilhelm Bartmann, Gerhard Beck, Hans-Hermann Lau
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Patent number: 4897397Abstract: Certain aryl-alkynoic, alkenoic and alkanoic acids and derivatives and their use in treating inflammation, allergy and hyperproliferative skin disease are disclosed.Type: GrantFiled: December 16, 1988Date of Patent: January 30, 1990Assignee: Schering CorporationInventors: Neng Y. Shih, David J. Blythin
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Patent number: 4895869Abstract: This invention related to leukotriene B.sub.4 antagonists having the structure ##STR1## and the pharmaceutically acceptable addition salts thereof; wherein R.sup.1 is lower alkyl having 1-10 carbon atoms; or lower alkenyl or alkynyl having 2-10 carbon atoms; or lower alkadienyl having 3-10 carbon atoms; or lower alkadienyl or alkenynyl having 4-10 carbon atoms;wherein R.sup.2 and R.sup.3 are the same or different and represent hydrogen or lower alkyl having 1-6 carbon atoms;wherein X is CH.dbd.CH, S, or O;wherein Y is CH.dbd.CH or C.tbd.C;wherein Z is OR.sup.4 or NR.sup.5 R.sup.6, and wherein R.sup.4 represents H, lower alkyl having 1-6 carbon atoms, or a pharmaceutically acceptable cation, and wherein R.sup.5 and R.sup.6 act independently and represent H or lower alkyl having 1-6 carbon atoms, or R.sup.5 and R.sup.Type: GrantFiled: June 3, 1988Date of Patent: January 23, 1990Assignee: C. D. Searle & Co.Inventors: Stevan W. Djuric, Richard A. Haack, Julie M. Miyashiro
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Patent number: 4889865Abstract: Mono, di and tri-esters of 1,8-dihydroxy-10-phenyl-9-anthrone or -9-anthranol have the formula ##STR1## wherein p is 0 or 1,(a) when p=0, t=1 and R.sub.2 represents hydrogen or --COR.sub.3,(b) when p=1, t=0 and R.sub.1 and R.sub.2 each independently represent hydrogen or --COR.sub.3,R.sub.3 represents linear or branched alkyl having 1-17 carbon atoms, cycloalkyl, phenyl or phenyl substituted by lower alkyl, lower alkoxy, halogen, a nitro function, --CF.sub.3 or a hydroxyl function, and mixtures of said esters. These esters are prepared by reacting 1,8-dihydroxy-10-phenyl-9-anthrone with an activated form of an acid. The esters are useful in human or veterinary medicine and in cosmetic compositions.Type: GrantFiled: February 21, 1989Date of Patent: December 26, 1989Assignee: Centre International de Recherches Dermatologiques C.I.R.D.Inventors: Braham Shroot, Gerard Lang, Jean Maignan, Serge Restle, Christopher Hensby, Michel Colin
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Patent number: 4886885Abstract: A pharmaceutical compound of the formula: ##STR1## in which R.sup.1 is C.sub.7-20 alkyl, C.sub.7-20 alkenyl or C.sub.7-20 alkynyl, the alkyl, alkenyl or alkynyl group being optionally substituted by phenyl or substituted phenyl and the alkenyl and alkynyl groups containing 1 to 3 unsaturated bonds, R.sup.2 is (i) optionally substituted phenyl, (ii) C.sub.1-10 alkyl optionally substituted by one or more substituents selected from optionally protected hydroxyl, optionally protected carboxyl, nitrile, optionally protected tetrazolyl, --COR.sup.4 where R.sup.4 is C.sub.1-14 alkyl, C.sub.1-4 alkoxy, an optionally protected amino acid residue or --NR.sub.2.sup.5 where each R.sup.5 is hydrogen or C.sub.1-4 alkyl, and --NHR.sup.6 where R.sup.6 is hydrogen, a protecting group, an optionally protected amino acid residue, C.sub.1-4 alkyl or --COR.sup.7 where R.sup.7 is C.sub.1-4 alkyl or C.sub.1-4 alkoxy, or (iii) C.sub.1-10 alkyl substituted with a group selected from ##STR2## where each R.sup.8 is hydrogen or C.sub.Type: GrantFiled: October 26, 1988Date of Patent: December 12, 1989Assignee: Lilly Industries LimitedInventors: Stephen R. Baker, Alec Todd
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Patent number: 4877811Abstract: Compounds of the formula: ##STR1## and stereoisomers thereof wherein X and Y, which are the same or different, are hydrogen, halogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted alkoxy, optionally substituted aryloxy, optionally substituted heteroaryloxy, optionally substituted arylalkoxy, optionally substituted heteroarylalkoxy, optionally substituted acyloxy, optionally substituted amino, acylamino, nitro, cyano, --CO.sub.2 R.sup.3, --CONR.sup.4 R.sup.5, or --COR.sup.6, except that X and Y are not both hydrogen; R.sup.1 and R.sup.2, which are the same or different, are alkyl or fluoroalkyl; and R.sup.3, R.sup.4, R.sup.5 and R.sup.6, which are the same or different, are hydrogen, alkyl, alkenyl, alkynyl, optionally substituted aryl, optionally substituted aralkyl, or cycloalkylalkyl.Type: GrantFiled: November 12, 1987Date of Patent: October 31, 1989Assignee: Imperial Chemical Industries PLCInventors: Vivienne M. Anthony, John M. Clough, Christopher A. Godfrey
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Patent number: 4866201Abstract: A new compound is provided by a cyclohexane derivative of the formula ##STR1## wherein R represents a hydrogen atom or an alkyl group, an alkylthioalkyl group or an unsubstituted or substituted phenyl group; and R.sup.1 represents an alkyl group, an unsubstituted or substituted benzyl group, a phenethyl group, a phenoxymethyl group, a 2-thienylmethyl group, an alkoxymethyl group or an alkylthiomethyl group, or a salt of said cyclohexane compound.This cyclohexane compound exhibits useful plant-growth regulating effects on crop-plants and also non-crop plants such as lawn and may be prepared by cyclization of an acetonylsuccinic acid dialkyl ester, followed by reaction with an organic acid chloride and by intermolecular rearrangement.Type: GrantFiled: July 7, 1987Date of Patent: September 12, 1989Assignee: Kumiai Chemical Industry Co., Ltd.Inventors: Kenji Motojima, Takeshige Miyazawa, Yasufumi Toyokawa, Masafumi Matsuzawa, Hiroshi Hokari, Shoji Kusano
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Patent number: 4863503Abstract: Compounds of formula (I): ##STR1## and stereoisomers thereof, wherein W is R.sup.1 O.sub.2 C--C.dbd.CH--ZR.sup.2, wherein R.sup.1 and R.sup.2, which are the same or different, are alkyl or fluoroalkyl groups, and Z is either an oxygen or sulphur atom; A is an oxygen or sulphur atom, --NR.sup.3 --, or --CR.sup.4 R.sup.5 --; X, Y and Z.sup.Type: GrantFiled: April 17, 1987Date of Patent: September 5, 1989Assignee: Imperial Chemical Industries PLCInventors: Vivienne M. Anthony, John M. Clough, Paul de Fraine, Christopher R. A. Godfrey, Kevin Beautement
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Patent number: 4833161Abstract: The present invention provides carboxylic acid derivatives of the general formula: ##STR1## wherein R.sub.1 and R.sub.2, which can be the same or different, are optionally substituted aryl radicals or optionally substituted heterocyclic radicals, A is a straight-chained or branched, saturated or unsaturated alkylene chain containing up to 10 carbon atoms which can contain an oxygen, sulphur or nitrogen atom and is optionally substituted by a hydroxyl group, Y is an S(O).sub.n group or an oxygen atom, n is 0, 1 or 2 and B is a valency bond or a saturated or unsaturated alkylene radical containing up to 5 carbon atoms; as well as the physiologically acceptable salts, esters and amides thereof, with the proviso that(a) R.sub.1 and R.sub.2 are not simultaneously aryl radicals and(b) when an unsaturated alkylene chain is present which contains a heteroatom, the heteroatom is not connected to an unsaturated aliphatic carbon atom.Type: GrantFiled: January 6, 1988Date of Patent: May 23, 1989Assignee: Boehringer Mannheim GmbHInventors: Hans P. Wolff, Hans-Frieder Kuhnle
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Patent number: 4829081Abstract: Compounds of the formula ##STR1## in which Y is ##STR2## X is O or S; Z is --CHOH--CH.sub.2 --CHOH--CH.sub.2 --COOH, an ester or salt thereof or the lactone thereof; andeach of R.sup.1, R.sup.2 and R.sup.3 can be alkyl, cycloalkyl; or substituted or unsubstituted phenyl; and additionally R.sup.3 can be hydrogen, are obtained by a multi-step process and are useful in the treatment of atherosclerosis, e.g. sodium(E)-7-(4-phenyl-2-isopropyl-5-phenylthien-3-yl)-3,5-dihydroxyhept-6- enoate.Type: GrantFiled: December 22, 1986Date of Patent: May 9, 1989Assignee: Sandoz Pharm. Corp.Inventors: Robert E. Damon, II, James R. Wareing
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Patent number: 4826829Abstract: Thiophene derivatives of the following formula are effective as acaricdies: ##STR1## wherein A is selected from -phenylthienyl and -phenyl optionally carrying one or more substitutents selected from -lower alkyl, -lower alkoxy, -phenoxy, -hydroxy, -halogen, -lower haloalkyl, -phenylcarbonyl, -lower alkyl carbonyloxy, -lower alkyl sulfonyl, -lower alkyl sulfonyloxy, -amino, -lowr alkyl carboxamido, and -lower haloalkyl carboxamido;R.sub.4 is selected from -hydrogen and -lower alkyl; andR.sub.5 is selected from -thienyl optionally carrying one or more substituents selected from -lower alkyl, -phenylethynyl, -lower alkylthio, -lower haloalkyl carbonyl, and lower alkyl sulfoxy; or -phenyl optionally carrying one or more substituents selected from -lower alkyl and -lower alkoxy.Type: GrantFiled: March 9, 1988Date of Patent: May 2, 1989Assignee: FMC CorporationInventors: Susan E. Eurkart, Richard B. Phillips, David M. Roush
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Patent number: 4827019Abstract: Photographic coupler solvents comprising aromatic carboxylic esters such as phthalates and isophthalates having bulky or branched ester substituents are described for incorporation in photographic emulsions and elements. The solvents are preferably employed in the cyan layer to protect the cyan dye against ferrous ion reduction. The solvents also provide improvements in yellow dye stability to light, cyan dye stability in the dark and magenta dye stability to heat and light.Type: GrantFiled: January 12, 1987Date of Patent: May 2, 1989Assignee: Eastman Kodak CompanyInventor: Sundaram Krishnamurthy
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Patent number: 4820823Abstract: In accordance with a process of the present invention, .alpha.-keto acids of the general formula RCOCOOH wherein R is aryl, alkenyl or heterocyclic group, can be obtained through one-step carbonylation reaction of an organic halogenide of the general formula RX wherein R is the same as above and X is a halogen atom, with carbon monoxide and water in the presence of a basic compound and a palladium containing catalyst.Type: GrantFiled: February 21, 1986Date of Patent: April 11, 1989Assignee: Director-General of Agency of Industrial Science and TechnologyInventors: Masato Tanaka, Toshiaki Kobayashi, Toshiyasu Sakakura
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Patent number: 4797456Abstract: Water-soluble sulfonium salts are converted, without the elimination of odorous volatile by-products, to water-insoluble products useful as binders in coating formulations by heating a water-soluble cyclic sulfonium salt in which the sulfonium sulfur is bonded only to aliphatic carbons.Type: GrantFiled: December 9, 1982Date of Patent: January 10, 1989Assignee: The Dow Chemical CompanyInventors: Ritchie A. Wessling, Donald L. Schmidt, Kiyoshi I. Aikawa
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Patent number: 4792567Abstract: Acaricidal aryl arylthien-2-yl ethenes of the formula ##STR1## in which R.sup.2 and R.sup.3 are each an optionally substituted phenyl or thienyl group are disclosed and claimed.Type: GrantFiled: June 9, 1987Date of Patent: December 20, 1988Assignee: FMC CorporationInventors: Susan E. Burkart, Cesar Rodriguez, David M. Roush, Richard B. Phillips
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Patent number: 4791133Abstract: This invention relates to leukotriene B.sub.4 antagonists having the structure ##STR1## and the pharmaceutically acceptable addition salts thereof; wherein R.sup.1 is lower alkyl having 1-10 carbon atoms; or lower alkenyl or alkynyl having 2-10 carbon atoms; or lower alkadienyl having 3-10 carbon atoms; or lower alkadiynyl or alkenynyl having 4-10 carbon atoms;wherein R.sup.2 and R.sup.3 are the same or different and represent hydrogen or lower alkyl having 1-6 carbon atoms;wherein X is CH.dbd.CH, S, or O;wherein Y is CH.dbd.CH or C.tbd.C;wherein Z is OR.sup.4 or NR.sup.5 R.sup.6, and wherein R.sup.4 represent H, lower alkyl having 1-6 carbon atoms, or a pharmaceutically acceptable cation, and wherein R.sup.5 and R.sup.6 act independently and represent H or lower alkyl having 1-6 carbon atoms, or R.sup.5 and R.sup.Type: GrantFiled: June 26, 1987Date of Patent: December 13, 1988Assignee: G. D. Searle & Co.Inventors: Stevan W. Djuric, Richard A. Haack, Julie M. Miyashiro
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Patent number: 4782079Abstract: Thiophene derivatives of the following formula are effective as acaricides: ##STR1## wherein R.sub.A is selected from -hydrogen, -halogen, -lower alkyl, hydroxy, -lower alkoxy, -lower alkylthio, -lower alkoxyalkoxy, -lower alkoxycarbonyl, -aryloxycarbonyl, -lower alkoxycarbonyloxy, -lower alkylsulfonyl, -lower alkylsulfonyloxy, -arylsulfonyloxy, and -lower alkyl phosphonyloxy;R.sub.B is -hydrogen, or R.sub.A and R.sub.B together are --C.sub.4 H.sub.4 --bridging 2'-3' or 3'-4';R.sub.3 and R.sub.4 are selected from -hydrogen, -lower alkyl, and -aryl;X is -halogen; andY is selected from -hydrogen and -halogen.Type: GrantFiled: January 26, 1988Date of Patent: November 1, 1988Assignee: FMC CorporationInventors: Susan E. Burkart, Richard B. Phillips, David M. Roush
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Patent number: 4772683Abstract: Disclosed herein is a novel process using novel silyl enol ether intermediates of the formula ##STR1## to generate novel azetidione thiolester intermediates of the formula ##STR2## which can be used to form 1-.beta.-alkyl carbapenem antibiotics. It has now been discovered that if the R.sup.4 group is selected from a small group of moieties having the formula: ##STR3## an increased .beta.-yield of up to approximately 100% can be obtained.Type: GrantFiled: February 24, 1986Date of Patent: September 20, 1988Assignee: Bristol-Myers CompanyInventors: Alain Martel, Jean-Paul Daris, Jacques Corbeil
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Patent number: 4766222Abstract: A novel class of acyl-derivatives of carnitine is disclosed wherein the acyl radical is either the radical of unsaturated organic acids (typically, acrylic acid) or the radical of saturated organic acids substituted with tert-alkyl, cycloalkyl, cycloalkenyl, alkoxyl, heterocyclic and carboalkoxylradicals, or with aldehyde or hydroxy groups. These acyl-derivatives of carnitine are useful therapeutical agents in the treatment of cardiac disorders, hyperlipidaemias and hyperlipoproteinaemias.Type: GrantFiled: June 30, 1987Date of Patent: August 23, 1988Assignee: Sigma-Tau Industrie Farmacuetiche Riunite S.p.A.Inventors: Claudio Cavazza, Paolo De Witt, Maria O. Tinti
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Cyclohexenone derivatives, the preparation and use thereof as herbicides and plant growth regulators
Patent number: 4761486Abstract: Cyclohexenone derivatives of the formula ##STR1## where R.sup.1, R.sup.2, A and X have the meanings given in the disclosure, a process for their manufacture, herbicidal and plant growth-regulating agents containing the novel active ingredients, and methods of combating unwanted plant growth and of regulating plant growth.Type: GrantFiled: January 14, 1987Date of Patent: August 2, 1988Assignee: BASF Aktiengesellschaft, PatentabteilungInventors: Bernd Zeeh, Dieter Jahn, Michael Keil, Dieter Kolassa, Bruno Wuerzer, Norbert Meyer, Wilhelm Rademacher, Johann Jung -
Patent number: 4757084Abstract: Analogs of 2,5-Diaryl tetrahydrothiophenes which were substituted or unsubstituted on 3,4-positions were prepared.These compounds are found to be leukotriene inhibitors and potent and specific PAF (Platelet Activating Factor) antagonists. They are therefore useful in the treatment of various diseases or disorders mediated by the leukotriene and/or PAF, for example, inflammation, cardiovascular disorder, asthma, lung edema, adult respiratory distress syndrome, pain, and aggregation of platelets.Type: GrantFiled: September 13, 1985Date of Patent: July 12, 1988Assignee: Merck & Co., Inc.Inventor: Tesfaye Biftu
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Patent number: 4748272Abstract: This invention relates to new lipoxygenase inhibitors possessing anti-inflammatory and anti-allergic properties. The present new compounds are of the formula: ##STR1## and salts thereof; whereinAr is phenyl, naphthyl or sulfur, oxygen or nitrogen heterocyclic;X is O, S, NR.sub.5, or a chemical bond;R is H, lower alkoxy, aryloxy, hydroxy, lower alkyl, aryl or lower aralkyl;R.sub.1 and R.sub.2 are independently hydrogen, hydroxy, lower alkoxy, lower alkyl, aryl, aryloxy, lower aralkyl, lower aralkoxy, formyl, lower alkanoyl, benzoyl, and lower aralkanoyl;R.sub.3 and R.sub.4 are independently hydrogen, halogen, hydroxy, lower alkoxy, aryloxy, lower aralkoxy, trifluoromethyl, lower carbalkoxy, carboxy, cyano, nitro, lower alkyl, lower alkenyl, lower alkynyl, aryl or lower aralkyl;R.sub.5 is H, lower alkyl, lower aralkyl or aryl;R.sub.6 is hydroxy or hydroxy-substituted lower alkyl;n and m are independently 0, 1, 2 or 3.Type: GrantFiled: August 1, 1986Date of Patent: May 31, 1988Assignee: Rorer Pharmaceutical Corp.Inventor: Raymond D. Youssefyeh
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Patent number: 4748253Abstract: Process for preparing esters of alkanoic acids via rearrangement of alpha-haloketals in the presence of a Lewis acid.The rection is preferably carried out in the presence of catalytic amounts of a Lewis acid and of a diluent at a temperature in the range from about 0.degree. to the reflux temperature of diluent.The esters thus obtained are useful as intermediate products for preparing drugs.The process involves the preparation of new alpha-haloketals.Type: GrantFiled: December 10, 1981Date of Patent: May 31, 1988Assignee: Blasinachim S.p.A.Inventors: Claudio Giordano, Aldo Belli, Fulvio Uggeri, Giovanni Villa
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Patent number: 4732901Abstract: Compounds of formula (I): ##STR1## in which R.sub.1 is hydrogen or C.sub.1-6 alkyl;R.sub.2 is hydrogen or a group --CO.sub.2 R.sub.3 where R.sub.3 is hydrogen or C.sub.1-6 alkyl;n is an integer of from 2 to 12;X represents a double or triple bond, and each of A and B represents hydrogen when X is a double bond, or both A and B are absent when X is a triple bond; and ##STR2## represents an aromatic heterocyclic ring, are disclosed as inhibitors of 5-lipoxygenase.Type: GrantFiled: February 27, 1986Date of Patent: March 22, 1988Assignee: Beecham Group p.l.c.Inventor: Derek R. Buckle
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Patent number: 4730005Abstract: The compounds represented by the following structural formula (I) ##STR1## wherein m is 1 or 2; n is 1, 2 or 3; R' is hydrogen or methyl; R is a radical selected from the group consisting of: ##STR2## wherein R.sub.1 is C.sub.8 to C.sub.13 alkyl, C.sub.7 to C.sub.12 alkoxy, C.sub.7 to C.sub.12 thioalkyl, C.sub.10 to C.sub.12 1-alkynyl, 11-dodecynyl, 1-trans-dodecenyl, 5-(4-acetyl-3-hydroxy-2-propylphenoxypentoxy, 2(Z), 5(Z)-undecadienyloxy, phenyl-C.sub.4 to C.sub.10 alkyl with the phenyl optionally mono substituted with bromo, chloro, trifluoromethyl, methoxy, methylthio or trifluoromethylthio, phenylthio-C.sub.3 to C.sub.9 alkyl with the phenyl optionally mono substituted with bromo, chloro, trifluoromethyl, methoxy, methylthio or trifluoromethylthio, phenyl-CH.dbd.CH--(CH.sub.2).sub.2-8, phenyl-C.sub.3 to C.sub.9 alkoxy, trifluoromethyl-C.sub.7 to C.sub.12 alkyl, cyclohexyl- C.sub.4 to C.sub.10 alkyl or ##STR3## wherein each q is 0, 1, 2 or 3 but the sum of both q's does not exceed 3, and R.sub.Type: GrantFiled: May 16, 1986Date of Patent: March 8, 1988Assignee: SmithKline Beckman CorporationInventors: John G. Gleason, Carl D. Perchonock
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Patent number: 4708963Abstract: Carbacyclin derivatives of Formula I ##STR1## wherein R.sub.1 is OR.sub.2, wherein R.sub.2 is hydrogen, alkyl, cycloalkyl, aryl, a heterocyclic residue, or NHR.sub.3, wherein R.sub.3 is an acid residue or hydrogen;X is oxygen;A is --CH.sub.2 --CH.sub.2 --, trans--CH.dbd.CH--, or --C.tbd.C--;W is free or functionally modified hydroxymethylene or free or functionally modified ##STR2## wherein the OH-group can be in the .alpha.- or .beta.-position; D is a straight-chain or branched, saturated or unsaturated aliphatic group of 1-10 carbon atoms, which can optionally be substituted by fluorine atoms, 1,2-methylene, 1,1-trimethylene;E is --C.tbd.C-- or --CR.sub.6 .dbd.CH.sub.7 -- wherein R.sub.6 and R.sub.7 are hydrogen or alkyl of 1-5 carbon atoms;R.sub.4 is an aliphatic group, cycloalkyl, optionally substituted aryl, or a heterocyclic group;R.sub.5 is free or functionally modified hydroxy and,when R.sub.Type: GrantFiled: May 28, 1985Date of Patent: November 24, 1987Assignee: Schering AktiengesellschaftInventors: Werner Skuballa, Bernd Raduchel, Norbert Schwarz, Helmut Vorbruggen, Jorge Casals-Stenzel, Ekkehard Schillinger, Michael H. Town
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Patent number: 4707549Abstract: Esters of optically active 2-arylalkanoic acids I ##STR1## where Ar is an isocyclic or heterocyclic aryl radical and R.sup.1 and R.sup.2 are each C.sub.1 -C.sub.4 -alkyl, are prepared by subjecting an optically active ester II ##STR2## where X is Cl, Br or --O--SO.sub.2 --Y and Y is Cl or a hydrocarbon radical, to a Friedel-Crafts reaction with an aromatic compound ArH (III).Type: GrantFiled: February 4, 1985Date of Patent: November 17, 1987Assignee: BASF AktiengesellschaftInventors: Gerhard Fritz, Manfred Eggersdorfer, Hardo Siegel
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Patent number: 4705802Abstract: The invention relates to new .omega.-aryl-alkylthienyl compounds having the Formula I ##STR1## i.e. omega-aryl-alkyl thienyl alkanoic acids and, respectively, omega-aryl-alkyl thienyl alkenoic acids, the alkali metal salts of such acids and certain esters thereof. The invention further relates to processes for the treatment of chronically inflammatory processes in humans.Type: GrantFiled: February 26, 1985Date of Patent: November 10, 1987Assignee: A. Nattermann & CIE GmbHInventors: Hans-Heiner Lautenschlager, Michael J. Parnham, Sigurd Leyck, Johannes Winkelmann, Axel Brekle
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Patent number: 4696941Abstract: Compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and represent a straight-chain or branched alkyl group of 1 to 15 carbon atoms, a cycloalkyl group of 3 to 6 carbon atoms, a 2-furyl, 3-furyl, 3-pyridyl, 4-pyridyl or 2-thienyl group or an aromatic group of the formula ##STR2## wherein X, Y and Z are the same or different and represent hydrogen, alkyl of 1 to 3 carbon atoms, trifluoromethyl, alkoxy with 1 to 4 carbon atoms, halogen, nitro or hydroxy groups are useful as pharmaceutical, veterinary and cosmetic agents.Type: GrantFiled: June 28, 1985Date of Patent: September 29, 1987Assignee: Groupement d'Interet Economique dit: Centre International 'de Recherches Dermatologiques C.I.R.D.Inventors: Braham Shroot, Gerard Lang, Jean Maignan
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Patent number: 4690945Abstract: The present invention relates to the preparation of compounds, useful in animals and in humans, as nonsteroid anti-inflammatory agents of the formula ##STR1## in which R.sub.1 is hydrogen, alkyl, alkanoyl, phenylalkyl or phenylalkanoyl, said alkyl and alkanoyl groups having 1 to 6 carbon atoms and said phenyl group having 1 to 3 halogen substituents or 1 to 3 alkyl or alkoxy substituents, said alkyl or alkoxy substituents having 1 to 4 carbon atoms, and their pharmaceutically acceptable salts.Type: GrantFiled: January 14, 1986Date of Patent: September 1, 1987Assignee: Laboratorios Madaus Cerafarm, S.A.Inventors: Sabastian J. Arechaga, Jose O. O. Granell, Carmen S. Linan, Alfonso P. Vallejo, Jose A. P. Gabarro
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Patent number: 4691029Abstract: A process for preparing 3-thienyl malonic acid, comprising treatment of a 3-thienyl cyanoacetate of formula (III): ##STR1## where R.sup.1 represents an aryl or alkyl group, with at least a molar excess of an alkali metal hydroxide.Type: GrantFiled: August 16, 1984Date of Patent: September 1, 1987Assignee: Beecham Group p.L.c.Inventors: Patrick C. Harris, John A. Wilcox
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Patent number: 4684743Abstract: .beta.-Dicarbonyl, .beta.-cyanocarbonyl and .beta.-dicyano compounds I ##STR1## where R.sup.1 is an organic radical, X and Y are COOR.sup.2, --CO--R.sup.2 or --CN and R.sup.2 is an organic radical, are prepared from R.sup.1 --CHO (II) and X--CH.sub.2 --Y (III) by reaction in the presence of a condensation catalyst, hydrogen and a hydrogenation catalyst, using an oxide or phosphate of Mg, Al, Ti, Zn or a rare earth metal as the condensation catalyst.Type: GrantFiled: October 1, 1985Date of Patent: August 4, 1987Assignee: BASF AktiengesellschaftInventors: Walter Gramlich, Klaus Halbritter, Gerd Heilen
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Patent number: 4683330Abstract: A compound of the formula ##STR1## and intermediates useful in preparing same.Type: GrantFiled: January 11, 1985Date of Patent: July 28, 1987Assignee: The Upjohn CompanyInventor: Paul A. Aristoff
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Patent number: 4681953Abstract: Novel syntheses of dihalovinylcyclopropanecarboxylates, including potent insecticides, are described. The processes begin with the reaction between an alkenol and an orthoester to produce a .gamma.-unsaturated carboxylate, followed by the catalyzed addition of a carbon tetrahalide to the double bond and dehydrohalogenation to produce a cyclopropane derivative.Type: GrantFiled: August 22, 1975Date of Patent: July 21, 1987Assignee: Sagami Chemical Research CenterInventors: Kiyoshi Kondo, Kiyohide Matsui, Akira Negishi, Yuriko Takahatake
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Patent number: 4680307Abstract: A compound of the formula: ##STR1## wherein X.sup.1 is a free or an esterified carboxyl group, or a group of the formula: ##STR2## (R.sup.a and R.sup.b are each independently a hydrogen atom, a C.sub.1 -C.sub.4 alkyl group, a C.sub.3 -C.sub.7 cycloalkyl group, a benzyl group, a phenyl group, a phenyl group substituted with a halogen atom or a C.sub.1 -C.sub.4 alkyl group, or, when taken together with the adjacent nitrogen atom to which they are attached, they represent a 5 to 7 membered saturated heterocyclic group, Y.sup.1 is a group of the formula: ##STR3## (R.sup.6 is a hydrogen atom or C.sub.1 -C.sub.4 alkyl group), ##STR4## (R.sup.6 is as defined above), ##STR5## R.sup.1 is a hydrogen atom, a hydroxyl group or a protected hydroxyl group, R.sup.2 is a hydrogen atom or R.sup.1 and R.sup.2, when taken together, mean a shingle linkage to from a double bond between the carbon atoms which they are linked, R.sup.3 is a hydroxyl group or a protected hydroxyl group, R.sup.4 is a hydrogen atom or a C.sub.1 -C.sub.Type: GrantFiled: January 26, 1984Date of Patent: July 14, 1987Assignee: Sumitomo Chemical Company, LimitedInventors: Masami Muraoka, Toshio Nakamura, Akihiko Sugie, Keiichi Ono, Michihiro Yamamoto
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Patent number: 4680288Abstract: Sulfur-containing 6-ketoprostaglandins of the formula I ##STR1## in which D is a bond, alkylene having 1-3 C atoms, cis-alkenylene having 2-5 C atoms or alkinylene having 2-5 C atoms,R.sup.1 is H, alkyl having 1-4 C atoms, aryl having 6-12 C atoms or --C.sub.6 H.sub.4 NHCOC.sub.6 H.sub.5,R.sup.2 is alkyl having 1-7 C atoms, alkyl having 1-7 C atoms which is substituted by halogen, cycloalkyl having 5-6 C atoms, cycloalkyl having 5-6 C atoms which is substituted by alkyl having 1-4 C atoms, phenyl, phenyl which is substituted by F, Cl, Br, alkyl having 1-4 C atoms, OH, OCH.sub.3 or CF.sub.3, pyridyl, naphthyl, thienyl or, if D is alkylene having 1-3 C atoms, also is alkoxy having 1-4 C atoms, alkylthio having 1-4 C atoms, phenoxy or phenoxy which is substituted by F, Cl, Br, alkyl having 1-4 C atoms, OH, OCH.sub.3 or CF.sub.3,R.sup.3 and R.sup.Type: GrantFiled: January 18, 1985Date of Patent: July 14, 1987Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Klaus Irmscher, Hans-Eckart Radunz, Ernst Schulze, Bernhard Riefling
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Patent number: 4678496Abstract: As new compound is provided a cyclohexane derivative of the formula ##STR1## wherein R represents a hydrogen atom or an alkyl group, an alkylthioalkyl group or an unsubstituted or substituted phenyl group; and R.sup.1 represents an alkyl group, an unsubstituted or substituted benzyl group, a phenethyl group, a phenoxymethyl group, a 2-thienylmethyl group, an alkoxymethyl group or an alkylthiomethyl group, or a salt of said cyclohexane compound.This cyclohexane compound exhibits useful plant-growth regulating effects on crop-plants and also non-crop plants such as lawn and may be prepared by cyclization of an acetonylsuccinic acid dialkyl ester, followed by reaction with an organic acid chloride and by intermolecular rearrangement.Type: GrantFiled: August 1, 1985Date of Patent: July 7, 1987Assignee: Kumiai Chemical Industry Co., Ltd.Inventors: Kenji Motojima, Takeshige Miyazawa, Yasufumi Toyokawa, Masafumi Matsuzawa, Hiroshi Hokari, Shoji Kusano
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Patent number: 4675418Abstract: Process for preparing alkanoic acid or their esters by rearrangement of alpha-halo-ketones in protic medium and in the presence of a non-noble metal salt.The protic medium is preferably an aliphatic alcohol having low molecular weight or water and the reaction is carried out at a temperature from 0.degree. C. to the boiling-point of the diluent or of the diluents mixture.Type: GrantFiled: July 15, 1982Date of Patent: June 23, 1987Assignee: Blaschim S.p.a.Inventors: Claudio Giordano, Giovanni Villa, Fulvio Uggeri, Graziano Castaldi
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Patent number: 4675419Abstract: The invention relates to a process for preparing .alpha.-hydroxy-acids of general formula: ##STR1## in which R represents hydrogen or a lower alkyl radical and Cy represents a phenyl, naphthyl or heterocyclic radical, these latter three radicals optionally comprising one or more substituents selected from the group consisting of lower alkyl, lower alkenyl, lower alkynyl, lower alkoxy radicals and halogen atoms, process which comprises the treatment of an .alpha.-monohalogenated ketone of general formula: ##STR2## in which R and Cy have the same meaning as above and X represents chlorine, bromine or iodine, in the presence of an aqueous solution of an alkali metal hydroxide, a non-polar organic solvent selected from an aromatic or alicyclic hydrocarbon and oxygen in excess optionally in the presence of an inert gas, the treatment being carried out at a temperature ranging from the boiling temperature of the reaction medium at atmospheric pressure and 240.degree. C.Type: GrantFiled: November 21, 1985Date of Patent: June 23, 1987Assignee: SanofiInventors: Jean-Daniel Andre, Pierre-Jean Grossi, Alain Heymes, Giovanni V. Manzaroli
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Patent number: 4668814Abstract: A compound of the formula ##STR1## and intermediates useful in preparing same.Type: GrantFiled: January 11, 1985Date of Patent: May 26, 1987Assignee: The Upjohn CompanyInventor: Paul A. Aristoff
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Patent number: 4663465Abstract: 2,2-Dimethyl-3-arylcyclopropanecarboxylic acids and esters, suitable as insecticide intermediates, of the formula ##STR1## in which Ar is naphthyl or substituted furyl, thienyl or phenyl, andR.sup.1 is hydrogen or alkyl, are produced by subjecting ##STR2## to radical polymerization to produce ##STR3## reacting that with chlorine or bromine to produce ##STR4## and reacting that with an alkali metal or alkaline earth metal hydroxide or carbonate. Various intermediates II and III are new.Type: GrantFiled: December 4, 1985Date of Patent: May 5, 1987Assignee: Bayer AktiengesellschaftInventors: Reinhard Lantzsch, Dieter Arlt, Manfred Jautelat
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Patent number: 4638011Abstract: Tetrahydrothienyl substituted prostaglandin analogs are provided having the structural formula ##STR1## and including all stereoisomers thereof. The compounds are cardiovascular agents useful, for example, in the treatment of thrombolytic disease.Type: GrantFiled: December 17, 1984Date of Patent: January 20, 1987Assignee: E. R. Squibb & Sons, Inc.Inventor: Jagabandhu Das
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Patent number: 4628110Abstract: Novel compounds of the following general formula: ##STR1##Type: GrantFiled: October 30, 1984Date of Patent: December 9, 1986Assignee: The Upjohn CompanyInventor: Paul A. Aristoff
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Patent number: 4620031Abstract: Alpha-alkyl-alkanoic acids are prepared by heating at boiling temperature a mixture of an alpha-halogen-alkyl-arylketone in a saturated aliphatic diol or in a mixture of saturated aliphatic diols in the presence of a Broensted's acid and by successively alkalifying the reaction mixture.Type: GrantFiled: February 1, 1985Date of Patent: October 28, 1986Assignee: Zambon S.p.A.Inventors: Fulvio Uggeri, Graziano Castaldi, Claudio Giordano
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Patent number: 4609744Abstract: 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: March 19, 1984Date of Patent: September 2, 1986Assignee: Merck Frosst Canada Inc.Inventors: Robert N. Young, Joshua Rokach, Haydn R. Williams, Masatoshi Kakushima, Yvan Guindon
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Patent number: 4608441Abstract: Process for preparing an arylalkanoic acid by adding iodine to a mixture of an arylalkanone and an excess of an orthoester, heating of the mixture thus obtained, adding an inorganic base and finally an acid.Type: GrantFiled: July 12, 1985Date of Patent: August 26, 1986Assignee: BLASCHIM S.p.A.Inventors: Attilio Citterio, Laura Tinucci, Aldo Belli, Lucio Filippini
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Patent number: 4602095Abstract: Novel 3-hydroxy-4-alkyloxphenyl heterocyclic aromatic carboxylate compounds particularly well suited as sweeteners in foodstuff.Type: GrantFiled: December 29, 1983Date of Patent: July 22, 1986Assignee: General Foods CorporationInventors: Paul R. Zanno, Ronald E. Barnett, Jed A. Riemer
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Patent number: 4596887Abstract: A cyclopropanecarboxylate of the formula ##STR1## is prepared by the reaction of a compound of the formula ##STR2## with an alkoxide in an ether type solvent. R.sup.1, R.sup.2, and R.sup.4 each independently is hydrogen or a hydrocarbon residue, R.sup.3 is an alcohol residue, X is halogen, and A is --CH.sub.2 --CX.sub.3 or --CH.dbd.CX.sub.2.Type: GrantFiled: January 29, 1985Date of Patent: June 24, 1986Assignee: Sagami Chemical Research CenterInventors: Kiyoshi Kondo, Kiyohide Matsui
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Patent number: 4588823Abstract: Novel compounds of the following general formula: ##STR1##Type: GrantFiled: September 27, 1984Date of Patent: May 13, 1986Assignee: The Upjohn CompanyInventor: Paul A. Aristoff