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    Cephalosporinderivatives, process for their preparation and pharmaceutical compositions
    3.
    发明公开
    Cephalosporinderivatives, process for their preparation and pharmaceutical compositions 失效
    Cephalosporinverbindungen，Verfahren zu ihrer Herstellung und pharmazeutischePräparate。

    公开(公告)号：EP0418020A2

    公开(公告)日：1991-03-20

    申请号：EP90309901.8

    申请日：1990-09-10

    申请人： BEECHAM GROUP PLC

    发明人： Gasson, Brian Charles ,  Hinks, Jeremy David

    IPC分类号： C07D501/36 ,  C07D501/46 ,  C07D501/59 ,  A61K31/545 ,  C07D463/00 ,  C07D498/053 ,  C07D501/18

    CPC分类号： C07D501/00 ,  Y02P20/55

    摘要： β-Lactam compounds of the formula (I) including pharmaceutically acceptable salts and in vivo hydrolysable esters, processes for their preparation and their use as antibiotics:
    wherein



    R 1 is hydrogen, methoxy or formamido;
    R 2 is an acyl group, in particular that of an antibacterially active cephalosporin;
    R 3 is hydrogen or a readily removable carboxy protecting group (such as a pharmaceutically acceptable in-vivo hydrolysable ester group);
    R 4 is a y- or δ-lactone,ring optionally containing one or (where applicable) two endocyclic double bonds, which ring is optionally substituted at any carbon atom by alkyl, dialkylamino, alkoxy, hydroxy, halogen or aryl, which in the case of more than one substituent may be the same or different, or is optionally di-substituted at two adjacent carbon atoms, which are available for substitution, to form an aromatic fused bicyclic system; x and y are independently 0 or 1; x is S, SO, S0 2 , 0 or CH 2 ; and Y is 0 or S.

    摘要翻译： 式（I）的β-内酰胺化合物包括药学上可接受的盐和体内可水解的酯，其制备方法及其作为抗生素的用途：其中R 1是氢，甲氧基或甲酰氨基; R 2是酰基，特别是抗菌活性头孢菌素的酰基; R 3是氢或易除去的羧基保护基（例如药学上可接受的体内可水解的酯基）; R 4是γ-或δ-内酯，任选地含有一个或（如适用的话）两个内环双键，所述环在任何碳原子上被烷基，二烷基氨基，烷氧基，羟基，卤素或芳基任选取代， 在多于一个取代基的情况下可以相同或不同，或者在可用于取代的两个相邻碳原子处任意地被二取代，以形成芳族稠合双环体系; x和y独立地为0或1; x是S，SO，SO 2，O或CH 2; 而Y是O或S.

    Cephalosporins and their homologues, process for their preparation and pharmaceutical compositions
    6.
    发明公开
    Cephalosporins and their homologues, process for their preparation and pharmaceutical compositions 失效
    头孢菌素及其同系物，其制备方法和药物制剂工艺。

    公开(公告)号：EP0395219A2

    公开(公告)日：1990-10-31

    申请号：EP90303177.1

    申请日：1990-03-26

    申请人： Beecham Group p.l.c.

    发明人： Bateson, John Hargreaves ,  Burton, George ,  Fell, Stephen Christopher Martin

    IPC分类号： C07D501/20 ,  C07D463/00 ,  C07D498/053 ,  C07D501/18 ,  A61K31/545

    CPC分类号： C07D505/00 ,  C07D463/20

    摘要： β-Lactam compounds of the formula (Ia) including pharmaceutically acceptable salts and in vivo hydrolysable esters, processes for their preparation and their use as antibiotics:

    wherein
    R¹ is hydrogen, methoxy or formamido;
    R² is an acyl group, in particular that of an antibacterially active cephalosporin;
    CO₂R⁶ is a carboxy group or a carboxylate anion;
    R³ is a γ-lactone ring optionally containing an endocyclic double bond, which ring is optionally substituted at any carbon atom by alkyl, dialkylamino, alkoxy, hydroxy, halogen or aryl, which in the case of more than one substituent may be the same or different, or is optionally di-substituted at two adjacent carbon atoms, which are available for substitution, to form an aromatic fused bicyclic system; and X is S, SO, SO₂, O or CH₂.

    摘要翻译： 在式（Ia）包括其药学上可接受的盐和体内可水解的酯的β-内酰胺化合物，其制备方法及其作为抗生素使用： worin - [R <1>是氢，甲氧基或甲酰胺基; [R <2>是酰基，特别是做了抗菌活性的头孢菌素; CO 2 <6>是羧基或羧酸盐阴离子; [R <3>是γ内酯环，其任选含有桥环双键，环，其任选在任何碳原子上被烷基，二烷基氨基，烷氧基，羟基，卤素或芳基，其在一个以上的取代基的情况下，可以是substituiertem 相同或不同，或为任选的二substituiertem在两个相邻的碳原子，它们是可用于取代，以形成芳族稠合的双环体系; 且X是S，SO，SO 2，O或CH 2。

    Piperaziniocephalosporins
    10.
    发明公开
    Piperaziniocephalosporins 失效

    公开(公告)号：EP0416410A1

    公开(公告)日：1991-03-13

    申请号：EP90116330.3

    申请日：1990-08-26

    申请人： SHIONOGI SEIYAKU KABUSHIKI KAISHA

    发明人： Onoue, Hiroshi ,  Konoike, Toshiro ,  Ishitobi, Hiroyuki

    IPC分类号： C07D501/46 ,  C07D501/40 ,  C07D501/42 ,  C07D498/053 ,  A61K31/54 ,  A61K31/535

    CPC分类号： C07D501/00 ,  C07D505/00

    摘要： Antibacterial hydroxyarylpiperaziniocephalosporins of the formula :
    [wherein, R 1 is amino or acylamino; R 2 is H or methoxy; R 3 is alkyl; R 4 is -(P-C-Q) n -(where, P, Q each is H, alkyl, OH, or P + Q show oxo, and n is 0 to 4); R 5 is optionally substituted hydroxyaryl; R 6 has a negative charge and shows COO-or an anion plus optionally protected carboxy ; and X is 0, S, or S→O], an antibacterial preparation containing the same; a method for killing bacteria and preventing or treating bacterial infection by using the same; and syntheses of the cephalosporins are provided.

    摘要翻译： 下式的抗菌羟基芳基哌嗪二头孢菌素：[其中，R1是氨基或酰氨基; R2是H或甲氧基; R3是烷基; R4是 - （P-C-Q）n - （其中，P，Q各自是H，烷基，OH或P + Q表示氧代，并且n是0至4）。 R5是任选取代的羟基芳基; R6具有负电荷并显示COO-或阴离子加任选保护的羧基; 并且X是O，S或S→O]，含有其的抗菌制剂; 使用该方法杀死细菌并预防或治疗细菌感染的方法; 并提供了头孢菌素的合成。