发明公开
EP0161541A1 6-[1-Hydroxyethyl]-2-SR8-1-methyl-1-carba-dethiapen-2-em-3-carboxylic acids
失效
6- [1-羟乙基] -2- SR8-1-甲基-1-碳代 - 去硫杂丙烯-2-烯-3-羧酸
- 专利标题: 6-[1-Hydroxyethyl]-2-SR8-1-methyl-1-carba-dethiapen-2-em-3-carboxylic acids
- 专利标题(中): 6- [1-羟乙基] -2- SR8-1-甲基-1-碳代 - 去硫杂丙烯-2-烯-3-羧酸
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申请号: EP85104844.7申请日: 1985-04-22
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公开(公告)号: EP0161541A1公开(公告)日: 1985-11-21
- 发明人: Christensen, Burton G. , Shih, David H.
- 申请人: Merck & Co., Inc.
- 申请人地址: 126, East Lincoln Avenue P.O. Box 2000 Rahway New Jersey 07065-0900 US
- 专利权人: Merck & Co., Inc.
- 当前专利权人: Merck & Co., Inc.
- 当前专利权人地址: 126, East Lincoln Avenue P.O. Box 2000 Rahway New Jersey 07065-0900 US
- 代理机构: Abitz, Walter, Dr.-Ing.
- 优先权: US603036 19840423
- 主分类号: C07D487/04
- IPC分类号: C07D487/04 ; A61K31/40
摘要:
Disclosed are antibiotic 6-[1-hydroxy-ethyl]-2-SR 8 -1-methyl-1-carbadethiapen-2-em-3-carboxylic acids and their pharmaceutically acceptable salts and esters (I):
wherein: R 8 is
;and wherein n and m are independently selected from 0, 1, 2, 3, 4; X is -NR; and Y is -R, or -NRR; and wherein R is independently selected from hydrogen, alkyl, alkenyl, alkynyl, (having 1-6 carbon atoms); cycloalkyl and cycloalkenyl (having 3-6 carbon atoms); and heterocyclyl, heteroary. (having 3-6 ring atoms, one or more of which is N, O or S).
Also disclosed are processes for the preparation of such compounds and pharmaceutical compositions comprising such compounds.
wherein: R 8 is
;and wherein n and m are independently selected from 0, 1, 2, 3, 4; X is -NR; and Y is -R, or -NRR; and wherein R is independently selected from hydrogen, alkyl, alkenyl, alkynyl, (having 1-6 carbon atoms); cycloalkyl and cycloalkenyl (having 3-6 carbon atoms); and heterocyclyl, heteroary. (having 3-6 ring atoms, one or more of which is N, O or S).
Also disclosed are processes for the preparation of such compounds and pharmaceutical compositions comprising such compounds.
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