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    Cephalosporin derivatives
    3.
    发明授权
    Cephalosporin derivatives 失效
    头孢菌素衍生物

    公开(公告)号：US5232918A

    公开(公告)日：1993-08-03

    申请号：US653149

    申请日：1991-02-11

    申请人： Jean C. Arnould ,  Dominique Boucherot ,  David H. Davies ,  Frederick H. Jung ,  Colin J. Strawson

    发明人： Jean C. Arnould ,  Dominique Boucherot ,  David H. Davies ,  Frederick H. Jung ,  Colin J. Strawson

    IPC分类号： A61K31/545 ,  C07D241/44 ,  C07D501/36 ,  C07D501/46

    CPC分类号： C07D501/46 ,  C07D501/40

    摘要： Cephalosporin derivatives having a 3-position substituent of formula I are described: ##STR1## wherein R.sup.1 is hydrogen, alkenyl or optionally substituted alkyl, Het is a 5- or 6-membered heterocyclic ring bonded via a carbon atom to the amide linkage, wherein Het is selected from a group of the formulae II-III: ##STR2## wherein A is CH or a nitrogen atom; B is oxygen, sulphur or a group NR.sup.4 ; one or two of D, E, F and G are nitrogen atoms and the remainder are CH groups: or Het is a pyrazinone, pyridinone, pyridazinone or pyrimidinone ring, or is a thione equivalent of such a ring, said rings having a substituent R.sup.4 on one nitrogen atom, or is pyranone, or pyranthione; the ring Het being fused by any two adjacent carbon atoms to the benzene ring; and Het being attached to the --CH.sub.2 NR.sup.1 CO-- group via a carbon atom;R.sup.2 is hydroxy or an in vivo hydrolysable ester thereof;R.sup.3 is ortho to R.sup.2 and is hydroxy or an in vivo hydrolysable ester thereof; and R.sup.4 has various values. The use of such compounds as antibacterial agents is described as are processes for their preparation and intermediates therefor.

    摘要翻译： 描述了具有式I的3位取代基的头孢菌素衍生物：其中R 1是氢，烯基或任选取代的烷基，Het是通过碳原子与酰胺键键合的5-或6-元杂环，其中 Het选自式II-III的基团：其中A是CH或氮原子; B是氧，硫或NR4基团; D，E，F和G中的一个或两个是氮原子，其余是CH基团：或Het是吡嗪酮，吡啶酮，哒嗪酮或嘧啶酮环，或者是这样的环的硫酮当量，所述环具有取代基R 4 在一个氮原子上，或是吡喃酮或吡喃硫酮; 环Het被任何两个相邻的碳原子融合到苯环上; Het通过碳原子连接到-CH 2 NR 1 CO-基团; R2为羟基或其体内可水解的酯; R3是R2的邻位，是羟基或其体内可水解的酯; R4具有各种价值。 这些化合物作为抗菌剂的使用被描述为它们的制备方法及其中间体。

    Cephalosporin compounds
    4.
    发明授权
    Cephalosporin compounds 失效
    头孢菌素化合物

    公开(公告)号：US5013731A

    公开(公告)日：1991-05-07

    申请号：US512069

    申请日：1990-04-19

    申请人： Jean C. Arnould ,  Jean J. Lohmann ,  Georges Pasquet

    发明人： Jean C. Arnould ,  Jean J. Lohmann ,  Georges Pasquet

    IPC分类号： C07D519/06 ,  A61K31/545 ,  A61P31/04 ,  C07D471/04 ,  C07D498/04 ,  C07D501/46 ,  C07D519/00

    CPC分类号： C07D501/46 ,  C07D519/00

    摘要： A cephalosporin derivative of the formula I: ##STR1## in which X is S, O, CH.sub.2 or SO, ##STR2## represents one of the C-7 acyl groups known in the cephalosporin art, R3 is hydrogen or methoxy, R4 is hydrogen, optionally substituted alkyl, allyl, furfuryl or benzyl, and R5 is an aromatic heterocyclic ring system which is linked via carbon, and which contains a quaternized nitrogen atom.

    摘要翻译： 式I的头孢菌素衍生物：其中X为S，O，CH 2或SO的化合物，其中X为S，O，CH 2或SO，IMAGE为头孢菌素领域已知的C 7酰基之一，R 3为氢或甲氧基， R 4是氢，任选取代的烷基，烯丙基，糠基或苄基，R 5是通过碳连接并含有季铵化氮原子的芳族杂环体系。

    Cephem derivatives
    5.
    发明授权
    Cephem derivatives 失效

    公开(公告)号：US5013730A

    公开(公告)日：1991-05-07

    申请号：US219779

    申请日：1988-07-18

    申请人： Jean C. Arnould ,  Thomas G. C. Bird

    发明人： Jean C. Arnould ,  Thomas G. C. Bird

    IPC分类号： A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D501/20 ,  C07D501/38 ,  C07D501/46 ,  C07D501/56

    CPC分类号： C07D501/46

    摘要： Cephalosporins having a 3-position substituent of the formula: ##STR1## are described, wherein R.sup.5 is hydrogen, alkenyl, alkyl or substituted alkyl, Q is a mono- or bicyclic heterocyclic ring, variously substituted, Y is variously substituted alkylene, Y' represents various linking groups, m and n are independently zero or one, and P is a benzene ring with two ortho groups, one of which is hydroxy or an in-vivo hydrolysable ester thereof and the other is hydroxy, an in vivo hydrolysable ester thereof, carboxy, sulpho, hydroxymethyl, --NHSO.sub.2 CH.sub.3 or --NHCONH.sub.2 ; or P is a particularly substituted pyridone or pyranone. The use of such compounds as antibacterial agents is described, as are processes for their preparation.