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    Novel antimicrobial fluoroquinolonyl cephems
    2.
    发明公开
    Novel antimicrobial fluoroquinolonyl cephems 失效
    新型抗微生物氟代喹啉CEPHEMS

    公开(公告)号：EP0366640A3

    公开(公告)日：1992-01-02

    申请号：EP89870151.1

    申请日：1989-10-20

    申请人： Norwich-Eaton Pharmaceuticals, Inc.

    发明人： Demuth, Thomas Prosser, Jr. ,  White, Ronald Eugene

    IPC分类号： C07D501/26 ,  A61K31/545

    CPC分类号： C07D501/34 ,  C07D501/26

    摘要： Antimicrobial fluoroquinolonyl cephems of the formula:
    wherein
    (1) R¹ and R² are groups among those known in the art for substitution at the 7-position of an antimicrobially-active cephem; (2) R³ is a substituted or unsubstituted, nitrogen-containing, heterocyclic moiety; and (3) R⁴ is hydrogen, halogen, lower alkoxy or cyclic alkoxy, amino, nitro or cyano. Preferably, R³ is substituted or unsubstituted piperazine, 3-aminopyrrolidine, or 3-aminomethylpyrrolidine. R⁴ is preferably hydrogen or halogen.

    Novel antimicrobial fluoroquinolonyl cephems
    7.
    发明公开
    Novel antimicrobial fluoroquinolonyl cephems 失效
    抗紫罗兰色素

    公开(公告)号：EP0366640A2

    公开(公告)日：1990-05-02

    申请号：EP89870151.1

    申请日：1989-10-20

    申请人： Norwich-Eaton Pharmaceuticals, Inc.

    发明人： Demuth, Thomas Prosser, Jr. ,  White, Ronald Eugene

    IPC分类号： C07D501/26 ,  A61K31/545

    CPC分类号： C07D501/34 ,  C07D501/26

    摘要： Antimicrobial fluoroquinolonyl cephems of the formula:
    wherein

    (1) R¹ and R² are groups among those known in the art for substitution at the 7-position of an antimicrobially-active cephem;
    (2) R³ is a substituted or unsubstituted, nitrogen-containing, heterocyclic moiety; and
    (3) R⁴ is hydrogen, halogen, lower alkoxy or cyclic alkoxy, amino, nitro or cyano.

    Preferably, R³ is substituted or unsubstituted piperazine, 3-aminopyrrolidine, or 3-aminomethylpyrrolidine. R⁴ is preferably hydrogen or halogen.

    摘要翻译： 其中（1）R 1和R 2是本领域已知的用于在抗微生物活性头孢烯的7位置换的基团，其具有下式的抗微生物氟喹诺酮基头孢烯： （2）R 3是取代或未取代的含氮杂环部分; 和（3）R 4是氢，卤素，低级烷氧基或环烷氧基，氨基，硝基或氰基。 优选地，R 3是取代或未取代的哌嗪，3-氨基吡咯烷或3-氨基甲基吡咯烷。 R 4优选为氢或卤素。

    Novel antimicrobial dithiocarbamoyl quinolones
    9.
    发明公开
    Novel antimicrobial dithiocarbamoyl quinolones 失效
    Antimikrobielle二硫代氨基甲酰喹诺酮。

    公开(公告)号：EP0366643A2

    公开(公告)日：1990-05-02

    申请号：EP89870161.0

    申请日：1989-10-24

    申请人： Norwich Eaton Pharmaceuticals, Inc.

    发明人： Demuth, Thomas Prosser, Jr. ,  White, Ronald Eugene

    IPC分类号： C07D215/56 ,  C07D471/04 ,  C07D498/06 ,  C07D513/04 ,  C07D519/00 ,  C07D487/08 ,  C07D401/04 ,  C07D498/04 ,  C07D471/06 ,  C07D513/06 ,  C07D413/04

    CPC分类号： C07D401/04 ,  C07D215/56 ,  C07D401/12 ,  C07D401/14 ,  C07D417/14 ,  C07D455/04 ,  C07D471/04 ,  C07D477/10 ,  C07D487/04 ,  C07D499/00 ,  C07D503/00 ,  C07D505/00 ,  C07D513/04

    摘要： Antimicrobial dithiocarbamoyl quinolone compounds of the general formula:
    wherein

    (1) A¹, A², A³, R¹, R³, R⁴, and R⁶ form any of a variety of quinolone and related heterocyclic structures similar to those known in the art to have antimicrobial activity; and
    (2)

    (1) R¹ is X, R³ is X, or both R¹ and R³ are X; and
    (2) X is -R¹⁵-N(R¹⁶)(R¹⁷) or -R¹⁵-R¹⁸-N(R¹⁹)(R¹⁷), where (a) (1) R¹⁵ is nil, alkyl, a carbocyclic ring, or a heterocyclic ring; and
    (2) R¹⁶ is hydrogen; alkyl; alkenyl; a carbocyclic ring; a heterocyclic ring; or
    (3) when X is R¹⁵-N(R¹⁶)(R¹⁷), R¹⁶ and R¹⁵ may together comprise a heterocyclic ring including the nitrogen atom to which R¹⁵ and R¹⁶ are bonded;
    (b) R¹⁷ is C(=S)-S-M, where M is a pharmaceutically-­acceptable salt or biohydrolyzable ester; and
    (c) (1) R¹⁸ is alkyl, a carbocyclic ring, or a heterocyclic ring; and
    (2) R¹⁹ is hydrogen; alkyl; alkenyl; a carbocyclic ring; a heterocyclic ring; or
    (3) R¹⁸ and R¹⁹ may together comprise a heterocyclic ring including the nitrogen atom to which R¹⁸ and R¹⁹ are bonded;


    and pharmaceutically-acceptable salts and biohydrolyzable esters thereof, and hydrates thereof.

    摘要翻译： 其中（1）A 1，A 2，A 3，R 1，R 3，R 4和R 6中的至少一个具有下列通式的抗微生物二硫代氨基甲酰喹诺酮化合物： 形成与本领域已知的具有抗微生物活性的各种喹诺酮和相关杂环结构中的任何一种; 和（2）（1）R 1是X，R 3是X，或者R 1和R 3都是X; 和（2）X是-R 1 - 5（R 1）6）（R 1）7或-R 1 - 5 -R 1 其中（a）（1）R 1为未取代的烷基，碳环或杂环; R 1，R 2， 和（2）R 1是氢; 烷基; 烯基; 碳环 杂环; 或（3）当X为R 1 -5（-N 1 R 6）（R 1）7），R 1和R 5为5时， 可以一起包含包含R 1和R 5之间的氮原子的杂环键合; （b）R 1是C（= S）-S-M，其中M是药学上可接受的盐或可生物水解的酯; 和（c）（1）R 1 8是烷基，碳环或杂环; 和（2）R 1 <9>是氢; 烷基; 烯基; 碳环 杂环; 或（3）R 1 8和R 9可以一起包含包含R 1和R 3的氮原子的杂环键合; 及其药学上可接受的盐和生物可水解的酯，及其水合物。