专利号:US-5202454-A 优先权日:1986-07-11 标 题 :Process for the manufacture of 1-bromoalkyl hydrocarbyl carbonates 发明人:WOODEN GARY; SENNYEY GERARD; SENET JEAN-PIERRE 权利人:POUDRES & EXPLOSIFS STE NALE 摘要:The invention relates to a new process for the preparation of 1-bromoalkyl hydrocarbyl carbonates. The carbonates according to the invention are prepared by reacting an alpha-chlorinated carbonate of formula with an anhydrous brominated compound of formula ZBr in which Z represents hydrogen, the group (CH3)3-Si-, the group or bromine if R2 is other than an aromatic radical, in the presence of a catalyst chosen from the group consisting of heteroaromatic amines, quaternary ammonium or phosphonium halides, hexasubstituted guanidinium halides, alkaline earth metal halides or alkali metal halides in combination with a complexing agent for their cation. The carbonates according to the invention find their preferential applications as blocking agents for some antibiotics or as agents for the synthesis of phosphorus-containing carbonates which can be used as insecticides.
专利号:US-8703747-B2 优先权日:2008-07-23 标题 :Aminophosphinic derivatives that can be used in the treatment of pain 发明人:ROQUES BERNARD; PORAS HERVÉ; FOURNIE-ZALUSKI MARIE-CLAUDE 权利人:ROQUES BERNARD; PORAS HERVÉ; FOURNIE-ZALUSKI MARIE-CLAUDE; PHARMALEADS 摘要:The present invention relates to a compound of the following general formula (I): R 1 —NH—CH(R 2 )—P(â•?O)(OR 3 )—CH 2 —C(R 4 )(R 5 )—CONH—CH(R 6 )—COOR 7 (I) or a pharmaceutically acceptable salt of the latter, an isomer or a mixture of isomers in any proportions, especially a mixture of enantiomers, and in particular a racemic mixture, for which R 1 represents a —C(â•?O)—O—C(R 8 )(R 9 )—OC(â•?O)—R 10 group; R 2 represents an optionally substituted hydrocarbon-based chain, an aryl or heteroaryl group or a methylene group substituted by a heterocycle; R 3 represents a hydrogen atom or a —C(R 12 )(R 13 )—OC(â•?O)—R 14 group; R 4 and R 5 form, together with the carbon that bears them, a saturated hydrocarbon-based ring or an optionally substituted piperidine ring or R 4 represents a hydrogen atom and R 5 represents a phenyl or a benzyl that is optionally substituted, a heteroaromatic ring or a methylene group substituted by a heterocycle; R 6 represents an optionally substituted hydrocarbon-based chain or a phenyl or a benzyl that is optionally substituted; and R 7 represents a hydrogen atom or a benzyl, alkyl, heteroaryl, alkylheteroaryl, —CHMe—COOR 18 , —CHR 19 —OC(â•?O)OR 20 and —CHR 19 —OC(â•?O)OR 20 group. The present invention also relates to the use of these compounds as a medicinal product, and in particular for the treatment of pain, more avantageously neuropathic and neuroinflammatory pain, to their method of synthesis and also to the compositions containing them.
专利号:US-4348264-A 优先权日:1980-05-14 标 题 :Photocatalyzed process for producing carbapenams and carbapen-2-ems 发明人:ROSATI ROBERT L 权利人:PFIZER 摘要:Carbapenam-3-carboxylic acids and carbapen-2-em-3-carboxylic acids substituted at the 1-position with an oxo, a hydroxy or an acetoxy group, variously substituted at the 2-position with such groups as methyl, acetoxymethyl, methanesulfonyloxy, alkoxy, alkylthio, aminoalkylthio or amidinoalkylthio and optionally substituted at the 6-position with a hydroxyalkyl group, an acetoxyalkyl group or a conventional penicillin side-chain, pharmaceutically-acceptable salts thereof and various esters thereof wherein the esterifying group is selectively removed in the laboratory, or hydrolyzed under physiological conditions. n These compounds are useful either systemically or topically in the treatment of diseases caused by susceptible microorganisms, as animal feed additives for promotion of growth, or in the preservation of biodegradable materials, or as intermediates to compounds having such antibacterial activity. n Key to the synthesis of these compounds is the light catalyzed rearrangement of 2-diazo-1-oxoceph-3-em-4-carboxylates to 1-oxocarbapen-2-em-3-carboxylates, a newly discovered reaction determined to be of general applicability.
专利号:US-4429128-A 优先权日:1981-02-09 标题 :Carbapenams and carbapen-2-ems and process therefor 发明人:ROSATI ROBERT L 权利人:PFIZER 摘要:Carbapenam-3-carboxylic acids and carbapen-2-em-3-carboxylic acids substituted at the 1-position with an oxo, a hydroxy or an acetoxy group, variously substituted at the 2-position with such groups as methyl, acetoxymethyl, methanesulfonyloxy, alkoxy, alkylthio, aminoalkylthio or amidinoalkylthio and optionally substituted at the 6-position with a hydroxyalkyl group, an acetoxyalkyl group or a conventional penicillin side-chain, pharmaceutically-acceptable salts thereof and various esters thereof wherein the esterifying group is selectively removed in the laboratory, or hydrolyzed under physiological conditions. n These compounds are useful either systemically or topically in the treatment of diseases caused by susceptible microorganisms, as animal feed additives for promotion of growth, or in the preservation of biodegradable materials, or as intermediates to compounds having such antibacterial activity. n Key to the synthesis of these compounds is the light catalyzed rearrangement of 2-diazo-1-oxoceph-3-em-4-carboxylates to 1-oxocarbapen-2-em-3-carboxylates, a newly discovered reaction determined to be of general applicability.
专利号:US-5827855-A 优先权日:1992-12-28 标题 :Hexahydronaphthalene ester derivatives their preparation and their therapeutic uses 发明人:KOGEN HIROSHI; ISHIHARA SADAO; KOGA TEIICHIRO; KITAZAWA EIICHI; SERIZAWA NOBUFUSA; HAMANO KIYOSHI 权利人:SANKYO CO 摘要:Compounds of formula (I): (I) wherein R1 represents a group of formula (II) or (III): (II) (III) R2 is alkyl, alkenyl or alkynyl; R3 and R4 are each hydrogen, alkyl, alkenyl or alkynyl; R5 is hydrogen or a carboxy-protecting group; Ra is a group of formula -OR6; R6 is hydrogen; R6a and R6b are each hydrogen, a hydroxy-protecting group, alkyl, alkanesulfonyl, halogenated alkanesulfonyl or arysulfonyl, and their salts and esters. Such compounds inhibit the synthesis of cholesterol, and can be used for the treatment and prophylaxis of hypercholesterolemia and of various cardiac disorders.
专利号:US-4939261-A 优先权日:1984-06-08 标 题:N-substituted butyramide derivatives useful for treatment of conditions responsive to inhibition of enkephalinase 发明人:KSANDER GARY M 权利人:CIBA GEIGY CORP 摘要:Disclosed are compounds of the formula (I) wherein X and Y independently represent hydroxymethyl; cyano; carboxy; functionally modified carboxy selected from esterified carboxy, carbamoyl, and N-substituted carbamoyl; 5-tetrazolyl; 2-oxazolyl, 4,5-dihydro-2-oxazolyl, 2-imidazolyl or 4,5-dihydro-2-imidazolyl or any said grouping substituted by lower alkyl; R and R0 independently represent hydrogen, lower alkyl, (C3-C7)-cycloalkyl-lower alkyl, or aryl-lower alkyl in which aryl represents phenyl, pyridyl, thienyl, furyl, biphenyl or naphthyl, each unsubstituted or mono- or di-substituted by halogen, lower alkyl, hydroxy, acyloxy, lower alkoxy, trifluoromethyl or cyano; A represents straight chain (C2-C5)-alkylene; or A represents straight chain (C2-C5)-alkylene substituted by lower alkyl, by lower alkylthio-lower alkyl, by hydroxy-lower alkyl, by acyloxy-lower alkyl, by lower alkoxy-lower alkyl, by amino or acyl-amino, by amino-lower alkyl, by acylamino-lower alkyl, by (C3-C7)-cycloalkyl, by (C3-C7)-cycloalkyl-lower alkyl, by aryl or aryl-lower alkyl in which aryl represents phenyl or phenyl mono- or disubstituted by halogen, lower alkyl, lower alkoxy, hydroxy, acyloxy, trifluoromethyl or cyano; or A represents phenylene or cyclohexylene; pharmaceutically acceptable prodrug derivatives of any said compounds having a free carboxy group; pharmaceutically acceptable salts of any said compounds with a salt-forming group; methods for synthesis; pharmaceutical compositions thereof; and use thereof as enkephalinase inhibitors.
参考标题:Alkyl 1-Chloroalkyl Carbonates: Reagents For The Synthesis Of Carbamates And Protection Of Amino Groups 作者:Gérard Barcelo,Jean-Pierre Senet,Gérard Sennyey,Jean Bensoam,Albert Loffet 摘要:The Synthesis Of 1-Chloroalkyl Carbonates And Their Reaction With Various Type Of Amines Are Described. This Reaction Is Useful For The Synthesis Of Carbamate Pesticides And For The Protection Of Various Amino Groups, Including Amino Acids.