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    Cephalosporin antibiotics
    2.
    发明公开
    Cephalosporin antibiotics 失效
    头孢菌素抗生素

    公开(公告)号：EP0095329A2

    公开(公告)日：1983-11-30

    申请号：EP83302859.0

    申请日：1983-05-19

    申请人： GLAXO GROUP LIMITED

    发明人： Looker, Brian Edgar

    IPC分类号： C07D501/46 ,  A61K31/545

    CPC分类号： C07D277/587

    摘要： Cephalosporin antibiotics of general formula
    (wherein R 8 and R b , which may be the same or different, each represents a hydrogen atom or a methyl or ethyl group, and R represents a 3- or 4-carbamoyl group or a hydrogen atom) and non-toxic salts and non-toxic metabolically labile esters thereof. The compounds exhibit broad spectrum antibiotic activity both in vitro and in vivo, and may be used for treating a variety of diseases caused by pathogenic bacteria in human beings and animals. Pharmaceutical compositions containing the compounds and processes for the preparation of the compounds are also described.

    摘要翻译： 通式（其中R a和R b可以相同或不同，分别表示氢原子或甲基或乙基，R表示3-或4-氨基甲酰基 基团或氢原子）和其无毒盐和无毒的代谢不稳定的酯。 该化合物在体外和体内均表现出广谱抗生素活性，可用于治疗由人和动物引起的病原菌引起的各种疾病。 还描述了含有化合物的药物组合物和用于制备化合物的方法。

    Cephalosporins, process for their preparation and pharmaceutical compositions containing them
    3.
    发明公开
    Cephalosporins, process for their preparation and pharmaceutical compositions containing them 失效
    CEPHALOSPORINS，其制备方法和含有它们的药物组合物

    公开(公告)号：EP0266060A3

    公开(公告)日：1989-11-08

    申请号：EP87308525.2

    申请日：1987-09-25

    申请人： GLAXO GROUP LIMITED

    发明人： Newall, Christopher Earle ,  Looker, Brian Edgar

    IPC分类号： C07D501/34 ,  A61K31/545

    CPC分类号： C07D501/34 ,  Y02P20/55

    摘要： Compounds of formula (I)
    wherein
    R 1 represents a hydrogen atom or a C 1-4 alkyl group optionally substituted by one to three halogen atoms; R 2 and R 3 , which may be the same or different, each represents a hydrogen atom or a carboxyl blocking group; R 4 represents a hydrogen atom or an amino protecting group; R 5 and R 6 each represents a hydroxy or substituted hydroxy group or R 5 and R 6 together represent a cyclic protected diol group; Z is -S-or -SO-(α-or β-) and the dotted line bridging the 2-, 3-, and 4-positions indicate that the compound is a ceph-2-em or ceph-3-em compound; and salts and solvates thereof.

    Process for preparing cephalosporin compounds
    4.
    发明公开
    Process for preparing cephalosporin compounds 失效
    制备头孢菌素化合物的方法

    公开(公告)号：EP0160565A3

    公开(公告)日：1986-12-03

    申请号：EP85303032

    申请日：1985-04-29

    申请人： GLAXO GROUP LIMITED

    发明人： Looker, Brian Edgar

    IPC分类号： C07D501/46

    CPC分类号： C07D209/48

    摘要： There is described a process for the preparation of compounds of general formula (I)
    (wherein R 1 represents an amino or protected amino group, R 2 is hydrogen or a carboxyl blocking group, B is S or S → 0 and the dotted line indicates that the compound is a ceph-2-em or ceph-3-em compound) or a corresponding compound having a group -COOR 3 (wherein R 3 is a carboxyl blocking group) at the 4-position and an associated anion A G which comprises reacting a compound of formula (II)
    (wherein R 1 ,B and the dotted line are as defined above) or a corresponding compound having a group -COOR 3 at the 4-position (where R 3 is as described above) and an associated anion A with a hydroxylamine derivative of formula (III)
    (wherein R 2 is as defined above), or a salt or Zwitterion thereof. The process is of value as a means of preparing the antibiotic ceftazidime. Intermediates of value in the process and of methods of preparing them are also disclosed.

    摘要翻译： 描述了制备通式（I）化合物的方法（其中R 1代表氨基或被保护的氨基，R 2是氢或羧基封端基团，B是S或S→0，虚线表示 化合物是ceph-2-em或ceph-3-em化合物）或在4-位具有基团-COOR 3（其中R 3为羧基封闭基团）的相应化合物和相关的阴离子AG，该方法包括使化合物 式（II）（其中R 1，B和虚线如上所定义）或相应的在4-位具有基团-COOR 3的化合物（其中R 3如上所述）和相关的阴离子A与 式（III）（其中R 2如上定义）或其盐或两性离子。 该过程作为制备抗生素头孢他啶的手段是有价值的。 也披露了过程中的价值中间体及其制备方法。

    Process for preparing cephalosporin compounds
    5.
    发明公开
    Process for preparing cephalosporin compounds 失效
    Verfahren zur Herstellung von Cephalosporinen。

    公开(公告)号：EP0160565A2

    公开(公告)日：1985-11-06

    申请号：EP85303032.8

    申请日：1985-04-29

    申请人： GLAXO GROUP LIMITED

    发明人： Looker, Brian Edgar

    IPC分类号： C07D501/46

    CPC分类号： C07D209/48

    摘要： There is described a process for the preparation of compounds of general formula (I)
    (wherein R 1 represents an amino or protected amino group, R 2 is hydrogen or a carboxyl blocking group, B is S or S → 0 and the dotted line indicates that the compound is a ceph-2-em or ceph-3-em compound) or a corresponding compound having a group -COOR 3 (wherein R 3 is a carboxyl blocking group) at the 4-position and an associated anion A G which comprises reacting a compound of formula (II)
    (wherein R 1 ,B and the dotted line are as defined above) or a corresponding compound having a group -COOR 3 at the 4-position (where R 3 is as described above) and an associated anion A with a hydroxylamine derivative of formula (III)
    (wherein R 2 is as defined above), or a salt or Zwitterion thereof. The process is of value as a means of preparing the antibiotic ceftazidime. Intermediates of value in the process and of methods of preparing them are also disclosed.

    摘要翻译： 描述了制备通式（I）化合物的方法（其中R 1表示氨基或保护的氨基，R 2是氢或羧基封端基，B是S或S - > O，虚线表示该化合物是一种ceph-2-em或ceph-3-em化合物）或具有基团-COOR 3的相应化合物（其中R 3是羧基封端基团） 包括使式（II）化合物（其中R 1，B和虚线如上所定义）或相应的具有基团的化合物反应的相关阴离子A（ - ） -COOR 3在4-位（其中R 3如上所述）和相关阴离子A - 与式（III）的羟胺衍生物（其中R 2为 或其盐或两性离子。 该方法作为制备抗生素头孢他啶的手段是有价值的。 还公开了该方法中的价值中间体及其制备方法。

    Cephalosporin antibiotics
    10.
    发明公开
    Cephalosporin antibiotics 失效
    头孢菌素抗生素

    公开(公告)号：EP0181172A3

    公开(公告)日：1988-06-01

    申请号：EP85307950

    申请日：1985-11-01

    申请人： GLAXO GROUP LIMITED

    发明人： Bell, Richard ,  Foxton, Michael Walter ,  Looker, Brian Edgar

    IPC分类号： C07D501/24 ,  C07D277/20 ,  A61K31/545

    CPC分类号： C07D277/587 ,  Y02P20/55

    摘要： Compounds of general formula (I)

    (where R' is a carboxyl group, a group COO ⊖ or a blocked carboxyl group;
    R 2 is an amino or protected amino group; and R is hydrogen or a group of the formula CH 2 X, where X represents a halogen atom, a hydroxyl group, an acetoxy group; a group of the formula O.CO.NHR 3 , where R 3 is hydrogen, a C 1-4 alkyl group optionally substituted by 1 to 3 halogen atoms or an N-protecting group; a group of the formula OR 4 , where R" is a C 1-4 alkyl group optionally substituted by halogen or a C 1-4 alkoxy group; or a pyridinium, 3-carbamoylpyridinium or 4-carbamoyl-pyridinium group; B is -S- or -SO- (a- or β-); and the dotted line bridging the 2-, 3- and 4- positions indicates that the compound is a ceph-2-em or ceph-3-em compound) and salts thereof, the compounds of formula (I) being associated with an anion when X represents a pyridinium, 3-carbamoylpyridinium group or a 4-carbamoylpyridinium group and R' is other than COO ⊖ ) are disclosed. Processes for their preparation and pharmaceutical compositions containing them are also disclosed.

    摘要翻译： 通式（I）的化合物（其中R'为羧基，基团COO 8或封端的羧基; R 2为氨基或被保护的氨基;且R为氢或式CH 2 X的基团，其中X代表 卤素原子，羟基，乙酰氧基;式O.CO.NHR 3的基团，其中R 3是氢，任选被1至3个卤素原子取代的C 1-4烷基或N-保护基团; 其中R“为任选被卤素或C1-4烷氧基取代的C1-4烷基;或吡啶鎓，3-氨基甲酰基吡啶鎓或4-氨基甲酰基 - 吡啶鎓基团; B为-S-或 - SO-（α-或β-）;桥接2-，3-和4-位置的虚线表明化合物是ceph-2-em或ceph-3-em化合物）及其盐，化合物 当X代表吡啶鎓，3-氨基甲酰基吡啶鎓基团或4-氨基甲酰基吡啶鎓基团且R'不是COO时，式（I）的化合物与阴离子缔合） 还公开了含有它们的药物组合物和药物组合物。