Derivatized 3-styryl-cephalosporins

    公开(公告)号:US09975905B2

    公开(公告)日:2018-05-22

    申请号:US14775528

    申请日:2014-03-12

    摘要: Broad spectrum beta-lactamase inhibitors. Certain inhibitors also exhibit potent antibiotic activity in addition to beta-lactamase inhibition. Compounds of the invention are designed such that on cleavage of the beta-lactam ring reactive moieties are generated which can inactivate beta-lactamase. Also provided are methods of making betalactamase inhibitors and beta-lactam antibiotics exhibiting such inhibition. Additionally provided are pharmaceutical compositions for treatment or prevention of bacterial infections and methods of treatment of such infections.

    Cephalosporin compounds
    3.
    发明授权
    Cephalosporin compounds 失效
    CEPHALOSPORIN化合物

    公开(公告)号:US5073551A

    公开(公告)日:1991-12-17

    申请号:US334206

    申请日:1989-03-24

    摘要: Cephalosporin compounds represented by the general formula ##STR1## in which R.sup.1 is a hydrogen atom or a protective group for the amino group,R.sup.2 is a hydrogen atom or a protective group for the hydroxyl group,R.sup.3 is a hydrogen atom, a salt-forming cation or a protective group for the carboxyl group, andR.sup.4 is a hydrogen atom, a halogen atom or a lower alkyl group,and their pharmacologically acceptable salts, process for their production and use of the same compounds as medicaments, particularly as antibiotic agents.

    Cephalosporin derivatives
    5.
    发明授权
    Cephalosporin derivatives 失效
    头孢菌素衍生物

    公开(公告)号:US4963542A

    公开(公告)日:1990-10-16

    申请号:US353216

    申请日:1989-05-17

    CPC分类号: C07D501/34 C07D501/24

    摘要: Disclosed 2-(syn)-hydroxyimino-acetamide derivatives of the formula: ##STR1## wherein Y is hydrogen, hydroxyl, an acyloxy, carbamoyloxy, a quaternary ammonium or a nitrogen-containing heterocyclic ring-substituted thio group; or pharmaceutically acceptable salts or esters thereof are useful as antibacterial agents. Also disclosed are processes for producing them.

    摘要翻译: 公开的下式的2-(顺式) - 羟基亚氨基 - 乙酰胺衍生物:其中Y是氢,羟基,酰氧基,氨基甲酰氧基,季铵或含氮杂环取代的硫基; 或其药学上可接受的盐或酯可用作抗菌剂。 还公开了用于生产它们的方法。

    Halovinyl cephem compounds
    9.
    发明授权
    Halovinyl cephem compounds 失效
    卤乙烯基头孢烯化合物

    公开(公告)号:US4631274A

    公开(公告)日:1986-12-23

    申请号:US704776

    申请日:1985-02-25

    CPC分类号: C07D501/24

    摘要: The invention relates to novel halovinyl cephem derivatives of high antimicrobial activity of the formula: ##STR1## wherein R.sup.1 is a group of the formula:R.sup.4 --A--CONH--in which R.sup.4 is cyano(lower)alkenylthio or a group of the formula: ##STR2## in which R.sup.6 is hydrogen, amino or a protected amino group, andA is carbonyl, lower alkylene, hydroxy(lower)alkylene or a group of the formula: ##STR3## in which R.sup.5 is hydrogen, carboxy(lower)alkyl or protected carboxy(lower)alkyl;R.sup.2 is carboxy or a protected carboxy group; andX is halogen, and pharmaceutically acceptable salts thereof.

    摘要翻译: 本发明涉及具有下式的高抗微生物活性的新的卤代乙烯基头孢烯衍生物:其中R 1是下式的基团:其中R 4是氰基(低级)烯硫基或下式的基团:R 4 -A-CONH- 其中R 6是氢,氨基或保护的氨基,A是羰基,低级亚烷基,羟基(低级)亚烷基或下式的基团:其中R 5是氢,羧基(低级)烷基 或保护的羧基(低级)烷基; R2是羧基或被保护的羧基; 和X是卤素,及其药学上可接受的盐。