Nitrogen Or Halogen In Acid Moiety Patents (Class 560/153)
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Patent number: 4240823Abstract: Compounds of the formula: ##STR1## in which R.sub.1 is hydrogen, optionally halogenated alkyl, optionally halogenated cycloalkyl, optionally halogenated alkenyl, optionally halogenated aralkenyl or aryloxyalkenyl mono or bicyclic aryl (optionally substituted by halogen, alkyl, trifluoromethyl, nitro, cyano, amino, hydroxyl, alkoxy, aminosulphonyl or alkylcarbonyloxy), or monocyclic or bicyclic heterocyclic of 5-11 chain members and having one or two hetero-atoms (optionally substituted), and R.sub.2 is a carboxylic acid group or a salt or ester thereof, is found to have plant growth regulating activity.Type: GrantFiled: March 1, 1977Date of Patent: December 23, 1980Assignee: Philagro S.A.Inventors: Claude Clapot, Jean Vial, Jacqueline Mourier, Jean C. Boch
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Patent number: 4228184Abstract: New carboxyalkylacylamino acids which have the general formula ##STR1## are useful as angiotensin converting enzyme inhibitors.Type: GrantFiled: May 4, 1978Date of Patent: October 14, 1980Assignee: E. R. Squibb & Sons, Inc.Inventors: Miguel A. Ondetti, David W. Cushman
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Patent number: 4204064Abstract: A method, composition and compounds useful in said compositions for treating the skin and scalp characterized by an excessive secretion of sebum to improve the condition thereof by reducing said excessive secretion of sebum includes topically applying to a human having skin and/or a scalp so characterized a cosmetic composition containing as an active ingredient a derivative of cysteine or cysteamine. The composition contains about 0.1-5 weight percent of said derivative and also contains as a carrier for the active ingredient, water, a mixture of water and a lower alkanol, a lower alkanol, a mixture of a lower alkanol and a cosmetic resin, a reducing agent, a neutralizing agent or a vegetable oil.Type: GrantFiled: January 24, 1978Date of Patent: May 20, 1980Assignee: L'OrealInventor: Gregoire Kalopissis
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Patent number: 4200760Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is a straight or branched chain alkynyl group containing from 3 to 9 carbon atoms, inclusive; R.sup.2 is hydrogen, (lower)alkyl, halogen or hydroxymethyl; m is 1 or 2, and n is 2 or 3, provided that the sum of m and n is 3 or 4; X and Y each are independently hydrogen, nitro, cyano, --SO.sub.2 Ar or --COR.sup.3, provided that X and Y are not both hydrogen; R.sup.3 is (lower)alkyl, Ar, (lower)alkoxy, amino or (lower)-alkylamino; and Ar is an optionally substituted phenyl group; and nontoxic pharmaceutically acceptable acid addition salts thereof, are potent anti-ulcer agents. Processes for their preparation and novel intermediates are also disclosed.Type: GrantFiled: September 26, 1978Date of Patent: April 29, 1980Assignee: Bristol-Myers CompanyInventors: Aldo A. Algieri, Ronnie R. Crenshaw
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Patent number: 4196300Abstract: Glycidates and thioglycidates substituted in the .alpha.-position with a long chain alkyl of from 11 to 16 carbons having hypoglycemic activity.Type: GrantFiled: August 18, 1978Date of Patent: April 1, 1980Assignee: McNeilabs, Inc.Inventors: Richard J. Mohrbacher, Winston Ho, Gene Tutwiler
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Patent number: 4182891Abstract: Novel acetylenic derivatives of .alpha.-amino acids of the following general structure: ##STR1## wherein Z is .beta.-methylthioethyl, .beta.-benzylthioethyl, S-(5'-desoxyadenosin-5' -yl)-S-methylthioethyl, .gamma.-guanidinopropyl, or RHN(CH.sub.2).sub.n --; n is the integer 3 or 4; each R is hydrogen, alkylcarbonyl wherein the alkyl moiety has from 1 to 4 carbon atoms and is straight or branched, alkoxycarbonyl wherein the alkoxy moiety has from 1 to 4 carbon atoms and is straight or branched, or ##STR2## wherein R.sub.2 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; R.sub.1 is hydroxy, a straight or branched alkoxy group of from 1 to 8 carbon atoms, --NR.sub.4 R.sub.5 wherein each of R.sub.4 and R.sub.5 is hydrogen or a lower alkyl group of from 1 to 4 carbon atoms, or ##STR3## wherein R.sub.3 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; and the lactams thereof when Z is RHN(CH.sub.Type: GrantFiled: July 1, 1977Date of Patent: January 8, 1980Assignee: Merrell Toraude et CompagnieInventors: Brian W. Metcalf, Michel Jung
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Patent number: 4177277Abstract: A method for alleviating or reducing angiotensin related hypertension in hypertensive mammals comprises administering an effective amount of a compound having the general formula ##STR1## Intermediates for the preparation of such compounds are also included.Type: GrantFiled: September 15, 1978Date of Patent: December 4, 1979Assignee: E. R. Squibb & Sons, Inc.Inventors: Miguel A. Ondetti, Michael E. Condon
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Patent number: 4176235Abstract: New substituted acyl derivatives of amino acids which have the general formula ##STR1## are useful as angiotensin converting enzyme inhibitors.Type: GrantFiled: December 4, 1978Date of Patent: November 27, 1979Assignee: E. R. Squibb & Sons, Inc.Inventors: Miguel A. Ondetti, Frank L. Weisenborn
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Patent number: 4171282Abstract: The perfluoroalkylthio-substituted half esters and amides of succinic acid having the formula ##STR1## wherein R.sub.f is a perfluoroalkyl, R.sup.1 alkylene optionally interrupted with oxygen, sulfur or nitrogen atom, X is oxygen or NH, y is zero or 1, Q is a polyether or polyester diradical moiety having a molecular weight of 300 to 5000 or a polysiloxane having 5 to 80 repeating units and A is hydrogen, hydroxyl, amino, alkoxy of 1 to 21 carbons, phenoxy, alkylphenoxy of 7 to 20 carbons, dialkylamino where each alkyl has 1 to 18 carbons or the group ##STR2## said compounds being prepared by first reacting maleic anhydride with a polyether, polyester, diamine or a polysiloxane derivative of an alcohol or a primary amine and then reacting the product with a perfluoroalkyl alkylene thiol. The novel compounds are useful as surfactants with specific applications as wetting agents in coatings, waxes, emulsions, paints and resins.Type: GrantFiled: December 7, 1977Date of Patent: October 16, 1979Assignee: Ciba-Geigy CorporationInventor: Karl F. Mueller
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Patent number: 4169899Abstract: Penicillamine compounds of the formula: ##STR1## and of the formula: ##STR2## wherein R.sup.1, R.sup.2, R.sup.3, A and B are as defined hereinafter, and pharmaceutically acceptable acid addition salts thereof are disclosed. II are the products of hydrolysis or alcoholysis of I, and I are in turn the products of dehydration of II or alcohol removal form II. I and II are useful for the treatment of rheumatoid arthritis.Type: GrantFiled: January 6, 1978Date of Patent: October 2, 1979Assignee: Yoshitomi Pharmaceutical Industries, Ltd.Inventors: Masami Shiroki, Yutaka Maruyama, Kazuhiro Goto
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Patent number: 4154946Abstract: New substituted acyl derivatives of amino acids which have the general formula ##STR1## are useful as angiotensin converting enzyme inhibitors.Type: GrantFiled: June 28, 1978Date of Patent: May 15, 1979Assignee: E. R. Squibb & Sons, Inc.Inventors: Miguel A. Ondetti, Michael E. Condon
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Patent number: 4140681Abstract: N.sup.2 -arylsulfonyl-L-argininamides and the pharmaceutically acceptable salts thereof have been found to be effective as pharmaceutical agents for the inhibition and suppression of thrombosis in mammals.Type: GrantFiled: June 7, 1977Date of Patent: February 20, 1979Assignee: Mitsubishi Chemical Industries, LimitedInventors: Shosuke Okamoto, Akiko Hijikata, Ryoji Kikumoto, Yoshikuni Tamao, Kazuo Ohkubo, Tohru Tezuka, Shinji Tonomura
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Patent number: 4138423Abstract: Novel N-dithio carbamoyl oxime compounds have exceptional pesticidal activity.Type: GrantFiled: July 1, 1976Date of Patent: February 6, 1979Assignee: Union Carbide CorporationInventor: Themistocles D. J. D'Silva
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Patent number: 4130713Abstract: A novel procedure for the preparation of biotin employing cysteine as the starting material is disclosed. This synthesis involves the formation of the thiophane ring by a 1,3-dipolar addition. By virtue of this process pure d-biotin can be obtained, thus obviating the need for chemical resolution. Novel intermediates are also disclosed.Type: GrantFiled: August 5, 1977Date of Patent: December 19, 1978Assignee: Hoffmann-La Roche Inc.Inventors: Enrico G. Baggiolini, Hsi L. Lee, Milan R. Uskokovic
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Patent number: 4129571Abstract: New substituted acyl derivatives of amino acids which have the general formula ##STR1## are useful as angiotensin converting enzyme inhibitors.Type: GrantFiled: October 31, 1977Date of Patent: December 12, 1978Assignee: E. R. Squibb & Sons, Inc.Inventors: Miguel A. Ondetti, Michael E. Condon
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Patent number: 4129593Abstract: Very pure S-carboxymethyl-L-cysteine is prepared by reacting L-cystine in liquid ammonia with metallic sodium to form the disodium salt of L-cysteine, evaporating the ammonia, reacting the disodium salt of L-cysteine with an aqueous solution of chloroacetic acid and precipitating the S-carboxymethyl-L-cysteine formed by acidifying the reaction mixture. There is employed 0.1 to 10 weight percent of a reducing agent based on the chloroacetic acid.Type: GrantFiled: September 14, 1977Date of Patent: December 12, 1978Assignee: Deutsche Gold- und Silber-Scheideanstalt vormals RoesslerInventors: Alfred Maierhofer, Hans Wagner
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Patent number: 4125604Abstract: N.sup.2 -Arylsulfonyl-L-argininamides and the pharmaceutically acceptable salts thereof have been found to be effective as pharmaceutical agents for the inhibition and suppression of thrombosis in mammals.Type: GrantFiled: June 7, 1977Date of Patent: November 14, 1978Assignees: Mitsubishi Chemical Industries Limited, Shosuke OkamotoInventors: Shosuke Okamoto, Akiko Hijikata, Ryoji Kikumoto, Yoshikuni Tamao, Kazuo Ohkubo, Tohru Tezuka, Shinji Tonomura
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Patent number: 4116962Abstract: New substituted acyl derivatives of amino acids which have the general formula ##STR1## are useful as angiotensin converting enzyme inhibitors.Type: GrantFiled: December 3, 1976Date of Patent: September 26, 1978Assignee: E. R. Squibb & Sons, Inc.Inventors: Miguel Angel Ondetti, Frank Lee Weisenborn
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Patent number: 4107434Abstract: Novel process for the production of antibacterially active pleuromutilin derivatives.Type: GrantFiled: January 10, 1977Date of Patent: August 15, 1978Assignee: Sandoz Ltd.Inventor: Erwin Waldvogel
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Patent number: 4105789Abstract: New carboxyalkylacylamino acids which have the general formula ##STR1## are useful as angiotensin converting enzyme inhibitors.Type: GrantFiled: May 10, 1976Date of Patent: August 8, 1978Assignee: E. R. Squibb & Sons, Inc.Inventors: Miguel Angel Ondetti, David W. Cushman
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Patent number: 4096269Abstract: Novel N-haloalkanesulfenylcarbamoyloxime compounds have been found to have exceptional miticidal and insecticidal activity.Type: GrantFiled: May 20, 1976Date of Patent: June 20, 1978Assignee: Union Carbide CorporationInventor: Themistocles Damasceno Joaquim D'Silva
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Patent number: 4091024Abstract: New derivatives of amino acids which have the general formula ##STR1## are useful as angiotensin converting enzyme inhibitors.Type: GrantFiled: December 3, 1976Date of Patent: May 23, 1978Assignee: E. R. Squibb & Sons, Inc.Inventor: Miguel Angel Ondetti
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Patent number: 4086359Abstract: A new neutral fumarate salt of a derivative of the antibiotic pleuromutilin has been found whose physical properties made bulk manufacture more reproducible, simplify formulation and provide advantages in the administration of the substance.Type: GrantFiled: July 30, 1976Date of Patent: April 25, 1978Assignee: E. R. Squibb & Sons, Inc.Inventor: Friedrich Dursch
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Patent number: 4072718Abstract: Ditertiary organic disulfides are produced by contacting at least one ditertiary organic sulfide with at least one suitable hydrocarbyl sulfoxide and a catalyzing amount of a protonic acid.Type: GrantFiled: July 19, 1976Date of Patent: February 7, 1978Assignee: Phillips Petroleum CompanyInventor: William G. Billings
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Patent number: 4071531Abstract: New oxathiino- and dithiino-aminoacetic acids of the formula: ##STR1## in which A represents oxygen or sulphur, together with their racemic forms, their optically active forms and mixtures thereof, their reactive derivatives and their acid addition salts, are valuable intermediates for the preparation of therapeutically active derivatives, in particular cephalosporin derivatives of the formula: ##STR2## where R is hydrogen or acetoxy.Type: GrantFiled: September 26, 1975Date of Patent: January 31, 1978Assignee: Rhone-Poulenc IndustriesInventors: Christian Berger, Daniel Farge, Georges Gros, Mayer Naoum Messer, Claude Moutonnier
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Patent number: 4069243Abstract: A new method of preparing trifluoromethylthioacetic acid using a tertiary phosphine in a sulfur extrusion of lower alkyl trifluoromethyldithioacetate with optional is situ alkaline hydrolysis of said acetate using a biphasic hydrolysis system in the presence of a phase transfer catalyst.Type: GrantFiled: May 24, 1976Date of Patent: January 17, 1978Assignee: SmithKline CorporationInventor: Robert Michael DeMarinis
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Patent number: 4054740Abstract: This invention relates to a synthesis of biotin by the reduction of dehydrobiotin. The dehydrobiotin is prepared from 6-hydroxy-7-nitro-heptanoic acid methyl ester. Novel intermediates are also obtained by this synthesis.Type: GrantFiled: September 5, 1975Date of Patent: October 18, 1977Assignee: Hoffmann-La Roche Inc.Inventor: George Francis Field
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N.sup.2 -alkoxynaphthalenesulfonyl-L-argininamides and the pharmaceutically acceptable salts thereof
Patent number: 4046876Abstract: N.sup.2 -alkoxynaphthalenesulfonyl-L-argininamides and the pharmaceutically acceptable salts thereof have been found to be effective as pharmaceutical agents for the inhibition and suppression of thrombosis.Type: GrantFiled: February 10, 1976Date of Patent: September 6, 1977Assignee: Mitsubishi Chemical Industries LimitedInventors: Shosuke Okamoto, Ryoji Kikumoto, Kazuo Ohkubo, Tohru Tezuka, Shinji Tonomura, Yoshikuni Tamao, Akiko Hijikata