申请人:Merck & Co., Inc.
公开号:US04298741A1
公开(公告)日:1981-11-03
Disclosed are 6-amido-3-substituted-1-azabicyclo[3.2.0]hept-2-en-7-one-2-carboxylic acids (I): ##STR1## wherein R.sup.1 is hydrogen or acyl; and X is halo, oxygen (the 2-3 bond is saturated and the species I exists as a carboxylate salt or ester), or --OR wherein R is, inter alia, acyl, alkyl, or aralkyl. Such compounds and their pharmaceutically acceptable salt, ester and amide derivatives are useful as antibiotics. Also disclosed are processes for the preparation of such compounds, pharmaceutical compositions comprising such compounds and methods of treatment comprising administering such compounds and compositions when an antibiotic effect is indicated.
本公开的是6-酰胺基-3-取代-1-氮杂双环[3.2.0]庚-2-烯-7-酮-2-羧酸(I):其中R.sup.1是氢或酰基;X是卤素、氧(2-3键饱和且物种I存在为羧酸盐或酯),或--OR其中R是酰基、烷基或芳基等。这些化合物及其药学上可接受的盐、酯和酰胺衍生物可用作抗生素。还公开了制备这些化合物的方法、包含这些化合物的药物组合物以及在需要抗生素作用时给予这些化合物和组合物的治疗方法。