申请人:Takeda Chemical Industries, Ltd.
公开号:EP0045198A2
公开(公告)日:1982-02-03
Novel carba-2-penem compounds having at the 1-position two substituents, at least one of which is other than an alkyl group, and represented by the formula
wherein R1 is an alkyl, aryl, alkylthio, arylthio or acyl-ami- noalkylthio group, R2 and R3 are each an alkoxycarbonyl or cyano group or a group of the formula COR1 (R1 being as above defined), R3 may further be an alkyl or aryl group, and R4 is a hydrogen atom, an alkyl, hydroxyalkyl or aryl group or an amino group which may optionally be protected, have excellent antibacterial and beta-lactamase inhibitory activities and are useful as drugs for use in humans and domestic animals.
在 1 位上有两个取代基(其中至少一个不是烷基)的新型卡巴-2-青霉烯化合物,其式为
其中 R1 是烷基、芳基、烷硫基、芳硫基或酰基-氨基-无烷基硫代基团,R2 和 R3 分别是烷氧羰基或氰基或式 COR1 的基团(R1 如上定义),R3 可进一步是烷基或芳基,R4 是氢原子、烷基、羟基烷基或芳基或氨基,这些基团可选择被保护,具有优异的抗菌和β-内酰胺酶抑制活性,可用作人类和家畜的药物。