申请人:Hoffmann-La Roche Inc.
公开号:US04512999A1
公开(公告)日:1985-04-23
There are presented .beta.-lactams of the formula ##STR1## wherein R.sup.1 is cyano or a group of the formula R.sup.4 --CO-- or R.sup.5 --A--CO--, R.sup.2 is hydrogen, lower alkyl or halogen, R.sup.3 is hydrogen or a group readily cleavable by hydrolysis, n is the number 0, 1 or 2, R.sup.4 is hydrogen, hydroxy, lower alkoxy, lower alkyl, aryl or a group of the formula ##STR2## R.sup.5 is halogen, lower alkoxy, lower alkylthio, lower alkylsulphinyl, lower alkylsulphonyl, aryl, aryloxy, arylthio, arylsulphinyl, arylsulphonyl or di-(loweralkoxy)phoshinyl, R.sup.6 and R.sup.7 are lower alkyl and A is lower alkylene, and pharmaceutically acceptable salts of carboxylic acids of formula I with bases. The compounds exhibit pronounced .beta.-lactamase-inhibiting properties.
提供了具有以下式子的β-内酰胺:##STR1## 其中R1是氰基或式子R4-CO-或R5-A-CO-的基团,R2是氢、低碳基或卤素,R3是氢或易于水解的基团,n为数字0、1或2,R4是氢、羟基、低烷氧基、低烷基、芳基或式子##STR2##的基团,R5是卤素、低烷氧基、低烷基硫、低烷基磺酰、芳基、芳氧基、芳基硫、芳基磺酰或二(低烷氧基)膦酰基,R6和R7是低烷基,A是低烷基烯烃,以及式子I的羧酸的药理学上可接受的盐。这些化合物表现出明显的β-内酰胺酶抑制作用。