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    N-acyl derivatives of thienamycin
    1.
    发明授权
    N-acyl derivatives of thienamycin 失效
    噻吩霉素的N-酰基衍生物

    公开(公告)号：US4839352A

    公开(公告)日：1989-06-13

    申请号：US90400

    申请日：1987-08-27

    申请人： Louis Barash ,  Burton G. Christensen ,  John Hannah ,  William J. Leanza ,  David H. Shih

    发明人： Louis Barash ,  Burton G. Christensen ,  John Hannah ,  William J. Leanza ,  David H. Shih

    IPC分类号： C07D205/08 ,  C07D477/20 ,  C07D498/04

    CPC分类号： C07D477/20 ,  C07D205/08

    摘要： Disclosed are N-acyl derivatives of the antibiotic thienamycin having the following structural formula: ##STR1## wherein R.sup.1 and R.sup.2 are independently selected from the group consisting of hydrogen and acyl. Such derivatives and their pharmaceutically acceptable salts, are useful as antibiotics. Also disclosed are processes for the preparation of such derivatives, pharmaceutical compositions comprising such derivatives, and methods of treatment comprising administering such derivatives and compositions when an antibiotic effect is indicated.

    摘要翻译： 公开了具有以下结构式的抗生素硫霉素的N-酰基衍生物：其中R 1和R 2独立地选自氢和酰基。 这些衍生物及其药学上可接受的盐可用作抗生素。 还公开了制备这种衍生物的方法，包含这种衍生物的药物组合物，以及治疗方法，包括当指示抗生素效果时施用这样的衍生物和组合物。

    Substituted N-methylene derivatives of thienamycin
    4.
    发明授权
    Substituted N-methylene derivatives of thienamycin 失效
    噻吩霉素的取代的N-亚甲基衍生物

    公开(公告)号：US4311704A

    公开(公告)日：1982-01-19

    申请号：US159573

    申请日：1980-06-16

    申请人： Burton G. Christensen ,  William J. Leanza ,  David H. Shih ,  Kenneth J. Wildonger

    发明人： Burton G. Christensen ,  William J. Leanza ,  David H. Shih ,  Kenneth J. Wildonger

    IPC分类号： C07D477/20 ,  C07D487/04 ,  A61K31/40 ,  A61K31/425 ,  A61K31/44

    CPC分类号： C07D477/20

    摘要： Disclosed are substituted N-methylene derivatives of thienamycin having the formula: ##STR1## wherein: (1.) X.dbd.--NR.sup.1 R.sup.2, and Y.dbd.--R'--N.dbd.CRNR.sup.1 R.sup.2, and(2.) X.dbd.R, and Y.dbd.--NR.sup.1 R'N.dbd.CRNR.sup.1 R.sup.2 ; andwherein: R is, inter alia, hydrogen, NH.sub.2, --NHR.sup.1, --NR.sup.1 R.sup.2, R.sup.1 and R.sup.2 ; R.sup.1 and R.sup.2 are independently selected from: hydrogen, substituted, or unsubstituted: alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, heteroaryl, heteroaralkyl, heterocyclyl, and heterocyclylalkyl; R' is --(CH.sub.2).sub.n.sup.-, n is 1-6, or --(CH.sub.2).sub.m --Q--(CH.sub.2).sub.p.sup.-, m, n.dbd.1-3 and Q is O, S or R' is a carbocyclic or heterocyclic ring. 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.

    摘要翻译： 公开了具有下式的噻吩霉素的取代的N-亚甲基衍生物：其中：（1）X = -NR 1 R 2，Y = -R'-N = CRNR 1 R 2，和（2）X = R，Y = -NR1R'N = CRNR1R2; 并且其中：R特别是氢，NH 2，-NHR 1，-NR 1 R 2，R 1和R 2; R 1和R 2独立地选自：氢，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，杂芳烷基，杂环基和杂环基烷基; R'为 - （CH 2）n - ，n为1-6或 - （CH 2）m Q-（CH 2）p - ，m，n = 1-3，Q为O，S或R'为碳环或杂环 环。 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。 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; 和治疗方法，包括当指出抗生素效应时施用这些化合物和组合物。

    N-heterocyclic derivatives of thienamycin
    5.
    发明授权
    N-heterocyclic derivatives of thienamycin 失效
    噻吩霉素的N-杂环衍生物

    公开(公告)号：US4189493A

    公开(公告)日：1980-02-19

    申请号：US865283

    申请日：1977-12-28

    申请人： Burton G. Christensen ,  John Hannah ,  David H. Shih

    发明人： Burton G. Christensen ,  John Hannah ,  David H. Shih

    IPC分类号： C07D477/20 ,  C07D403/12

    CPC分类号： C07D477/20

    摘要： Disclosed are N-derivatives of thienamycin having structures I and II. ##STR1## wherein: the bifunctional radical may contain additional unsaturation in the ring; and wherein n is an integer selected from 1-6; p is 0, 1 or 2; R.sup.1 is selected from hydrogen, alkyl having 1-6 carbon atoms, and aryl having 6-10 carbon atoms; and Z is imino (.dbd.NH), oxo (.dbd.O), hydrogen, amino, or alkyl having 1-6 carbon atoms. Such compounds and their pharmaceutically acceptable salt and ester 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.

    摘要翻译： 公开了具有结构I和II的噻吩霉素的N-衍生物。 其中：双官能团可以在环中含有额外的不饱和键; 并且其中n是选自1-6的整数; p为0,1或2; R1选自氢，具有1-6个碳原子的烷基和具有6-10个碳原子的芳基; 和Z是亚氨基（= NH），氧代（= O），氢，氨基或具有1-6个碳原子的烷基。 这些化合物及其药学上可接受的盐和酯衍生物可用作抗生素。 还公开了制备这种化合物的方法，包含这些化合物的药物组合物和治疗方法，包括当指示抗生素效果时施用这些化合物和组合物。

    6-, 1- And 2-substituted-thio-1-carbadethiapen-2-em-3-carboxylic acid S-oxides
    7.
    发明授权
    6-, 1- And 2-substituted-thio-1-carbadethiapen-2-em-3-carboxylic acid S-oxides 失效
    6-，1-和2-取代 - 硫代-1-碳代萘二烯-2-酮-3-羧酸S-氧化物

    公开(公告)号：US4372965A

    公开(公告)日：1983-02-08

    申请号：US223505

    申请日：1981-01-08

    申请人： Burton G. Christensen ,  David H. Shih

    发明人： Burton G. Christensen ,  David H. Shih

    IPC分类号： C07D477/20

    CPC分类号： C07D477/20

    摘要： Disclosed are S-oxides of 6-, 1- and 2-substituted-1-carbadethiapen-2-em-3-carboxylic acids having the structure: ##STR1## wherein: n is 1 or 2; and R.sup.1, R.sup.6, R.sup.7 and R.sup.8 are, inter alia, independently selected from the group consisting of hydrogen, alkyl, alkenyl, aryl and aralkyl. Such compounds as well as 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.

    摘要翻译： 公开了具有以下结构的6-，1-和2-取代-1-碳代二烯-2-烯-3-羧酸的S-氧化物：其中：n为1或2; 并且R 1，R 6，R 7和R 8尤其独立地选自氢，烷基，烯基，芳基和芳烷基。 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和治疗方法，包括当指出抗生素作用时施用这些化合物和组合物。

    6- and 1-Substituted-1-carbadethiapen-2-em-3-carboxylic acid
    8.
    发明授权
    6- and 1-Substituted-1-carbadethiapen-2-em-3-carboxylic acid 失效
    6-和1-取代的1-碳代萘二烯-2-烯-3-羧酸

    公开(公告)号：US4206219A

    公开(公告)日：1980-06-03

    申请号：US954274

    申请日：1978-10-24

    申请人： Burton G. Christensen ,  David H. Shih

    发明人： Burton G. Christensen ,  David H. Shih

    IPC分类号： C07C205/42 ,  C07D205/08 ,  C07D477/20 ,  C07D477/26 ,  C07D498/04 ,  C07F7/18 ,  C07F9/568 ,  C07D487/04 ,  A61K31/40

    CPC分类号： C07D477/20 ,  C07C205/42 ,  C07D205/08 ,  C07D477/26 ,  C07F7/1804 ,  C07F9/5683

    摘要： Disclosed are 6- and 1-substituted-1-carbadethiapen-2-em-3-carboxylic acids of the following structure: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are, inter alia, independently selected from the group consisting of hydrogen, alkyl, aryl, and aralkyl. Such compounds as well as 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 antibiotics effect is indicated.

    摘要翻译： 公开了以下结构的6-和1-取代-1-碳氮杂萘-2-烯-3-羧酸：其中R 1，R 2和R 3特别地独立地选自氢，烷基 ，芳基和芳烷基。 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和治疗方法，包括当指出抗生素效应时施用这些化合物和组合物。