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New oxime o - substituted by a radical comprising a quaternary ammonium and derived of the acid 7 - amino cephalosporanic, their process of preparation and their application as medicinal products

机译:新的肟o-被包含季铵盐的自由基取代并由酸7-氨基头孢菌素衍生而来,其制备方法及其作为医药产品的用途

摘要

Novel oximes of the syn isomers of 7-(2-amino-4-thiazolyl)-acetamido-cephalosporanic acid of the formula IMAGE I wherein R is selected from the group consisting of hydrogen, chlorine, methoxy, alkyl and alkylthio of 1 to 5 carbon atoms, cycloalkyl of 3 to 5 carbon atoms, acetoxymethyl, carbamoyloxymethyl, IMAGE A1K is 1 to 4 carbon atoms, azidomethyl and -CH2-S-R' and R' is selected from the group consisting of a nitrogen heterocycle optionally substituted, acyl of an alkanoic acid of 2 to 4 carbon atoms, 2-oxo-(3H)-thiazolin-4-yl-carbonyl and 3-methyl-1,2-oxazol-5-ylcarbonyl, n is an integer from 2 to 4, R1, R2 and R3 are individually alkyl of 1 to 4 carbon atoms or together taken with the nitrogen atom they are attached to form a group selected from the group consisting of 1,4-diazobicyclo (2,2,2)octan-1-ylium and 1,3,5,7-tetraazatricyclo(3,3,1,13,7) decan-1-ylium and their non-toxic, pharmaceutically acceptable acid addition salts having antibacterial properties and process for their preparation and novel intermediates.
机译: I的7-(2-氨基-4-噻唑基)-乙酰氨基-头孢菌烷酸的同分异构体的新型肟,其中R选自氢,氯,甲氧基,烷基和烷硫基1 1-5个碳原子,3-5个碳原子的环烷基,乙酰氧基甲基,氨基甲酰氧基甲基, A1K是1-4个碳原子,叠氮基甲基和-CH 2 -SR',R'选自任选被取代的氮杂环碳数为2至4的链烷酸的酰基,2-氧代-(3H)-噻唑啉-4-基-羰基和3-甲基-1,2-恶唑-5-基羰基,n为2至2的整数。在图4中,R 1,R 2和R 3分别是1-4个碳原子的烷基,或者与氮原子一起被连接形成选自1,4-重氮双环(2,2,2)辛基的基团。 1-ylium和1,3,5,7-四氮杂三环(3,3,1,13,7)decan-1-ylium及其无毒,可药用的酸加成盐,具有抗菌性能用于制备和新型中间体。

著录项

  • 公开/公告号FR2448543B1

    专利类型

  • 公开/公告日1982-02-12

    原文格式PDF

  • 申请/专利权人 ROUSSEL UCLAFF;

    申请/专利号FR19790003312

  • 发明设计人

    申请日1979-02-09

  • 分类号C07D501/20;A61K31/545;

  • 国家 FR

  • 入库时间 2022-08-22 12:30:35

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