首页> 外国专利> CEPHALOSPORINS WITH IMIDAZOLINONE SUBSTITUENTS IN THE 7-AND 1,2,4-THIADIAZOLYL-SUBSTITUENTS IN THE 3-POSITION,THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

CEPHALOSPORINS WITH IMIDAZOLINONE SUBSTITUENTS IN THE 7-AND 1,2,4-THIADIAZOLYL-SUBSTITUENTS IN THE 3-POSITION,THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

机译:头孢菌素在3位,7位和1,2,4-噻二唑取代基中带有咪唑啉酮取代基,其制备方法和组成它们的药物成分

摘要

Novel cephalosporins of the formula IMAGE in which R1 represents hydrogen, alkyl or acyl and R2 represents hydrogen, alkyl or aryl and which can be present with respect to the centre of chirality C* in the two possible configurations R and S and as mixtures of the diastereomers resulting therefrom, and their non-toxic, pharmaceutically tolerable salts are prepared. These compounds are obtained by reacting an appropriate cephalosporin, which has an acetoxymethyl group in the 3-position, with a 5-mercapto-1,2,4-thiadiazole substituted in the 3-position by R1 in the presence of a base. Resulting compounds can be converted into the free acid and pharmaceutically tolerable salts. The novel cephalosporins are used as medicaments, in particular as antibacterial agents in infectious diseases.
机译:的新型头孢菌素,其中R 1代表氢,烷基或酰基,并且R 2代表氢,烷基或芳基,并且相对于手性中心C *可以两种可能的构型R和S存在,并且作为混合物存在制备由此得到的非对映异构体及其无毒的药学上可接受的盐。这些化合物是通过在碱的存在下,使在3位具有乙酰氧基甲基的合适头孢菌素与在3位被R1取代的5-巯基1,2,4-噻二唑反应而获得的。所得化合物可以转化为游离酸和药学上可接受的盐。新型头孢菌素被用作药物,特别是在传染病中用作抗菌剂。

著录项

  • 公开/公告号IL50761A

    专利类型

  • 公开/公告日1979-11-30

    原文格式PDF

  • 申请/专利权人 BAYER AG;

    申请/专利号IL19760050761

  • 发明设计人

    申请日1976-10-25

  • 分类号A23K1/17;A61K31/545;C07D501/36;

  • 国家 IL

  • 入库时间 2022-08-22 18:31:20

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