Substituted N-methylene derivatives of thienamycin sulfoxide and sulfone and their preparation
申请人:Merck & Co., Inc.
公开号:EP0001264A1
公开(公告)日:1979-04-04
Disclosed are substituted N-methylene derivatives of thienamycin sulfoxide (1, n=1) and sulfone (I, n=2) which may be represented by the following structural formula:
wherein X and Y are selected from the group consisting of hydrogen, R, OR, SR, and NR' R2 wherein, inter alia, R is substituted or unsubstituted: alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, heteroaryl, heteroaralkyl, heterocyclyl, and heterocyclylalkyl; R1 and R2 are hydrogen or R. Such compounds and their pharmaceutically acceptable salt, ether, 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.
本发明公开了噻喃霉素亚砜(1,n=1)和砜(I,n=2)的取代 N-亚甲基衍生物,其结构式如下:
其中 X 和 Y 选自由氢、R、OR、SR 和 NR' R2 组成的组,其中除其他外,R 是取代或未取代的:烷基、烯基、炔基、环烷基、环烷基烷基、芳基、芳烷基、杂芳基、杂芳基烷基、杂环烷基和杂环烷基;R1 和 R2 是氢或 R。此类化合物及其药学上可接受的盐、醚、酯和酰胺衍生物可用作抗生素。此外,还公开了制备此类化合物的工艺;包含此类化合物的药物组合物;以及治疗方法,包括在需要抗生素效果时施用此类化合物和组合物。