首页> 外国专利> A method of preparing a medicament with an antibacterial action and a method of preparing the syn isomer of a 7- 2-substituted-2- (etherified oxyimino) acetamido -3- (substituted methyl) -3-cephem-4 -carboxylic acid derivative.

A method of preparing a medicament with an antibacterial action and a method of preparing the syn isomer of a 7- 2-substituted-2- (etherified oxyimino) acetamido -3- (substituted methyl) -3-cephem-4 -carboxylic acid derivative.

机译:具有抗菌作用的药物的制备方法和7- [2-取代的-2-(醚化的氧亚氨基)乙酰胺基] -3-(取代的甲基)-3-cephem-4-羧基的同分异构体的制备方法酸衍生物。

摘要

Novel syn-isomer of 3,7-disubstituted-3-cephem-4-carboxylic acid compounds are provided of the formula: IMG in which R1 is a group of the formula: IMG wherein R5 is hydrogen, halogen, nitro, hydroxy, lower alkoxy or acyloxy and R6 is hydroxy, lower alkoxy, acyloxy, acylamino or di(lower)alkylamino; a group of the formula: IMG wherein R7 is amino, protected amino, hydroxy or lower alkyl; or a group of the formula: IMG wherein R8 is lower alkyl and R9 is imino, protected imino or oxo; R2 is an aliphatic hydrocarbon group which may have suitable substituent (s); R3 is carboxy or protected carboxy; and R4 is acyloxymethyl, hydroxymethyl, formyl or a heterocyclicthiomethyl group which may have suitable substituent (s); or R3 and R4 are linked together to form -COOCH2-, and pharmaceutically acceptable salts and tautomers thereof; the novel compounds are highly active against a number of pathogenic bacteria.
机译:提供了具有以下化学式的3,7-二取代的3-cephem-4-羧酸化合物的新型同分异构体:其中R 1为具有化学式的基团:其中IM 5为氢,卤素,硝基,羟基,低级烷氧基或酰氧基,R 6是羟基,低级烷氧基,酰氧基,酰氨基或二(低级)烷基氨基;式:IMG,其中R7是氨基,被保护的氨基,羟基或低级烷基;或下式的基团:其中R 8为低级烷基且R 9为亚氨基,被保护的亚氨基或氧代;或R 2是可以具有合适的取代基的脂族烃基; R3是羧基或被保护的羧基; R4是可以具有合适的取代基的酰氧基甲基,羟甲基,甲酰基或杂环硫基甲基; R3和R4连接在一起形成-COOCH2-及其药学上可接受的盐和互变异构体;该新型化合物对许多病原菌具有高活性。

著录项

  • 公开/公告号NL191259B

    专利类型

  • 公开/公告日1994-11-16

    原文格式PDF

  • 申请/专利权人 FUJISAWA PHARMACEUTICAL CO. LTD.;

    申请/专利号NL19770003969

  • 发明设计人

    申请日1977-04-12

  • 分类号C07D501/36;A61K31/545;C07D501/34;C07D501/16;

  • 国家 NL

  • 入库时间 2022-08-22 04:19:03

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