6-, 1- and 2-substituted-1-carbapen-2-em-3-carboxylic acids, processes for the preparation of such compounds and pharmaceutical composition comprising such compounds
    2.
    发明公开
    6-, 1- and 2-substituted-1-carbapen-2-em-3-carboxylic acids, processes for the preparation of such compounds and pharmaceutical composition comprising such compounds 失效
    6-,1-和2-取代的-1-碳青霉素-2-青霉-2-烯-3-羧酸,给进程用于制备这样的化合物和含有这些化合物的药物组合物。

    公开(公告)号:EP0010317A1

    公开(公告)日:1980-04-30

    申请号:EP79104106.4

    申请日:1979-10-23

    申请人: Merck & Co., Inc.

    IPC分类号: C07D487/04 A61K31/40

    摘要: isclosed are 6-, 1- and 2-substituted-1 dethiapen-2-em-3 -carboxylic acids having the struc-
    in: R° is H or -SR 1 ; R', R 6 , R' and R 1 are, inter alia, endently selected from the group consisting of hyd- alkyl, alkenyl, aryl and aralkyl. Such compounds as is their pharmaceutically acceptable salt, ester and derivatives are useful as antibiotics. Also disclosed are ses for the preparation of such compounds and phar- tical compositions comprising such compounds.

    摘要翻译: 本发明公开了6-,1 - 和2- substituiertem-1 carbadethiapen-2-EM-3,其具有结构 - 羧酸: worin:R t <0>为H或-SR <8>; [R <1>,R <6> - [R <7>和R <8>是,除其他外,unabhängig选自氢,烷基,烯基,芳基和芳烷基。 搜索化合物以及药学上可接受的销售它们的酯和酰胺衍生物可用作抗生素。 所以圆盘游离缺失是用于包括测试的化合物检测的化合物和药物组合物的制备方法。

    1-Methylcarbapenems having a 2-position substituent joined through an alkylenethio bridge
    3.
    发明公开
    1-Methylcarbapenems having a 2-position substituent joined through an alkylenethio bridge 失效
    2-烷基硫代取代物1-甲基碳代青霉烯。

    公开(公告)号:EP0184844A1

    公开(公告)日:1986-06-18

    申请号:EP85115846.9

    申请日:1985-12-12

    申请人: Merck & Co., Inc.

    IPC分类号: C07D487/04 A61K31/40

    摘要: 1-Methylcarbapenems having the formula:

    wherein:

    R' and R 2 are independently H, CH 3 -, CH 3 CH 2 -, (CH 3 ) 2 CH-, HOCH 2 -, CH 3 CH(OH)-, (CH 3 ) 2 C(OH)-, FCH 2 , F 2 CH-, F 3 C-, CH 3 CH(F)-, CH 3 CF 2 - or (CH 3 ) 2 C(F)-;
    R 3 is CH 3 ;
    R 4 is a bridging group comprising substituted or unsubstituted C 1 -C 4 straight, C 2 -C 6 branched or C 3 -C 7 cycloalkyl groups wherein the substituents are selected from C 1 -C 6 alkyl, O-C 1 -C 6 alkyl, S-C 1 -C 6 alkyl, CF 3 , N(C 1 -C 6 alkyl) 2 ;
    X is -S-.
    -SO 2 -, -O- or -NH: and
    R 5 is, e. g., C 1 -C 10 straight or branched alkyl; their preparation and antibiotic use are disclosed.

    摘要翻译: 具有下式的1-甲基碳青霉烯类化合物其中:R 1和R 2独立地是H,CH 3 - ,CH 3 CH 2 - ,(CH 3)2 CH-,HOCH 2 - ,CH 3 CH(OH) - ,(CH 3) (OH) - ,FCH2,F2CH-,F3C-,CH3CH(F) - ,CH3CF2-或(CH3)2C(F) - ; R 3是CH 3; R 4是包含取代或未取代的C 1 -C 4直链,C 2 -C 6支链或C 3 -C 7环烷基的桥连基团,其中取代基选自C 1 -C 6烷基,O-C 1 -C 6烷基,S-C 1 -C 6 烷基,CF 3,N(C 1 -C 6烷基)2; X是-S - , - , - SO 2 - , - O-或-NH; 和R 5是例如C 1 -C 10直链或支链烷基; 公开了其制备和抗生素使用。

    6-[1-Hydroxyethyl]-2-SR8-1-methyl-1-carba-dethiapen-2-em-3-carboxylic acids
    8.
    发明公开
    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

    公开(公告)号:EP0161541A1

    公开(公告)日:1985-11-21

    申请号:EP85104844.7

    申请日:1985-04-22

    申请人: Merck & Co., Inc.

    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.

    摘要翻译: 公开了抗生素6- [1-羟基 - 乙基] -2-SR8-1-甲基-1-十八碳烯-2-烯-3-羧酸及其药学上可接受的盐和酯(I):其中:R8为;和 其中n和m独立地选自0,1,2,3,4; X是-NR; Y是-R或-NRR; 并且其中R独立地选自氢,烷基,烯基,炔基(具有1-6个碳原子); 环烷基和环烯基(具有3-6个碳原子); 和杂环基,杂芳基。 (具有3-6个环原子,其中一个或多个是N,O或S)。 还公开了用于制备这样的化合物的方法和包含这些化合物的药物组合物。