申请人:Merck & Co., Inc.
公开号:US04232030A1
公开(公告)日:1980-11-04
Disclosed are substituted N-methylene derivatives of thienamycin sulfoxide (I, n=1) and sulfone (I, n=2) which may be represented by the following structural formula: ##STR1## wherein X and Y are selected from the group consisting of hydrogen, R, OR, SR, and NR.sup.1 R.sup.2 wherein, inter alia, R is substituted or unsubstituted: alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, heteroaryl, heteroaralkyl, heterocyclyl, and heterocyclylalkyl; R.sup.1 and R.sup.2 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.
本发明涉及替代的噻呋霉素亚砜(I,n=1)和砜(I,n=2)的N-亚甲基衍生物,其可以用以下结构式表示:##STR1##其中X和Y选自羟基,R,OR,SR和NR.sup.1R.sup.2的群,其中,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,芳基烷基,杂芳基,杂芳基烷基,杂环基和杂环基烷基;R.sup.1和R.sup.2是氢或R。这些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。本发明还涉及制备这些化合物的方法;包含这些化合物的制药组合物;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。