Patents Examined by Stephen Kapner
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Patent number: 4659726Abstract: Novel 4,5-bis(4-methoxyphenyl)-2-(pyrrol-2-yl)-thiazoles of the formula: ##STR1## wherein R.sup.1 is C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.2-4 alkynyl, 2,2,2-trifluoroethyl, a group of the formula: --CH.sub.2 COOR.sup.2 R.sup.2 is C.sub.1-8 alkyl, C.sub.2-4 alkenyl, C.sub.2-4 alkynyl, or phenyl-C.sub.1-2 alkyl), or a group of the formula: --(CH.sub.2).sub.n --A--R.sup.3 (A is oxygen or sulfur, R.sup.3 is C.sub.1-4 alkyl or C.sub.2-4 alkenyl, and n is 1, 2 or 3), a process for the preparation of the compounds, and a pharmaceutical composition useful as a platelet aggregation inhibitor which comprises as an active ingredient the above 4,5-bis(4-methoxyphenyl)-2-(pyrrol-2-yl)thiazole compound in admixture with a conventional pharmaceutically acceptable carrier or diluent.Type: GrantFiled: April 12, 1985Date of Patent: April 21, 1987Assignee: Kanebo, Ltd.Inventors: Koichiro Yoshino, Norihiko Seko, Koichi Yokota, Keizo Ito, Goro Tsukamoto
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Patent number: 4652665Abstract: The invention relates to new .alpha.-chlorinated carbonates characterized in that their formula is: ##STR1## in which X is a fluorine, chlorine or bromine atom and R.sup.1 is different from the ##STR2## group and represents; a substituted or non-substituted, saturated or unsaturated, aliphatic, araliphatic, primary, secondary, tertiary or cycloaliphatic radical.These .alpha.-chlorinated carbonates are prepared by the action of a compound of formula R.sup.1 OH on a chloroformate of formula: ##STR3## in a solvent medium in the presence of an acid scavenger which is added after the two preceding compounds.They are used to block the amine function of amino acids. The .alpha.-chlorinated carbonate and amino acid are reacted in a solvent medium at a temperature of -5.degree. to 100.degree. C. in the presence of an acid scavenger. Blocked amines are very useful in peptide synthesis.Type: GrantFiled: February 14, 1985Date of Patent: March 24, 1987Assignee: Societe Nationale des Poudres et ExplosifsInventors: Gerard Barcelo, Jean-Pierre Senet, Gerard Sennyey
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Patent number: 4631280Abstract: The invention relates to pyridazine derivatives substituted in the 4-position by a cyano group. It also relates to a process for the preparation of these products and their application as medicaments.Type: GrantFiled: May 20, 1985Date of Patent: December 23, 1986Assignee: SanofiInventors: Jean-Paul Kan, Kathleen Biziere, Camille-Georges Wermuth
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Patent number: 4544507Abstract: This invention provides a process for the production of a carbonate diester which involves heating an oxalate diester in a liquid medium containing an alcoholate catalyst to yield carbonate diester and carbon monoxide.Type: GrantFiled: February 6, 1984Date of Patent: October 1, 1985Assignee: Celanese CorporationInventor: Paul Foley
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Patent number: 4536574Abstract: A process for preparing 2-alkylthiomethyl-4-hydroxypyrimidines, known to be useful as intermediates in making insecticides, of the formula ##STR1## in which R.sup.1 is alkyl,R.sup.2 is hydrogen or alkyl, andR.sup.3 is hydrogen, alkyl or alkoxy, orR.sup.2 and R.sup.3 together represent a divalent alkylene radical,comprising reacting a sulphonyloxyacetonitrile of the formulaR--SO.sub.2 --O--CH.sub.2 --CN (II)in whichR is alkyl, halogenoalkyl or optionally substituted aryl,with methanol or ethanol, reacting the reaction mixture formed with ammonium chloride, reacting the reaction mixture formed with an alkali metal thiolate of the formulaR.sup.1 --S.sup..crclbar. Me.sup..sym. (III)in which Me.sup.+ is an alkali metal cation,and, in the presence of a base, with a .beta.-ketocarboxylic acid ester of the formula ##STR2## at a temperature between about -20.degree. and +100.degree. C.Type: GrantFiled: December 7, 1983Date of Patent: August 20, 1985Assignee: Bayer AktiengesellschaftInventor: Fritz Maurer
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Patent number: 4535083Abstract: The invention relates to compounds of the formula ##STR1## said compounds being obtainable by cleavage of compounds of formula ##STR2## The compounds of the invention as well as compositions and medicaments containing a compound of the invention are useful as antimicrobial agents.Type: GrantFiled: September 9, 1983Date of Patent: August 13, 1985Assignee: Bayer AktiengesellschaftInventors: Gunter Benz, Karl G. Metzger, Hans-Joachim Zeiler
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Patent number: 4532241Abstract: 10-Alkyl-8,10-dideazaminopterins of the formula ##STR1## where R is hydrogen or alkyl of 1 to about 8 carbon and their carboxylate and acid addition salts are described. These compounds exhibit antineoplastic activity that is similar to, but more effective than, methotrexate.Type: GrantFiled: January 17, 1984Date of Patent: July 30, 1985Assignee: SRI InternationalInventors: Joseph I. DeGraw, Lawrence F. Kelly, Francis M. Sirotnak
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Patent number: 4528372Abstract: The present invention relates to novel N-phthalidyl-5-fluorouracil derivatives represented by the general formula ##STR1## wherein one of R.sub.1 and R.sub.2 represents phthalidyl group ##STR2## (wherein R.sub.3 is a hydrogen atom, a halogen atom or a group selected from alkoxyl groups or alkyl groups) and the other represents a hydrogen atom, an acyl group or a cyclic ether group; ##STR3## (wherein n is 1 or 2) or R.sub.1 and R.sub.2 represent the same phthalidyl group; ##STR4## (wherein R.sub.3 has the same meaning as that defined above) and provides a compound which has antitumor activity and less toxicity and can be used as a cancerocidal agent.Type: GrantFiled: May 21, 1982Date of Patent: July 9, 1985Assignee: Grelan Pharmaceutical Co., Ltd.Inventors: Kazuo Kigasawa, Mineharu Hiiragi, Kikuo Wakisaka, Keiko Ichikawa, Kikuo Nakazato, Taiji Okada
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Patent number: 4522765Abstract: Described is di(7-octenyl) carbonate having the structure: ##STR1## and the use thereof as an intermediate in producing the compound having the structure: ##STR2## useful in perfumery.Type: GrantFiled: June 22, 1984Date of Patent: June 11, 1985Assignee: International Flavors & Fragrances Inc.Inventors: Wilhelmus J. Wiegers, Augustinus G. Van Loveren, Marie R. Hanna, Domenick Luccarelli, Jr., David R. Bowen, Manfred H. Vock