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    Cephalosporin compounds
    5.
    发明授权
    Cephalosporin compounds 失效
    头孢菌素化合物

    公开(公告)号：US4474779A

    公开(公告)日：1984-10-02

    申请号：US433247

    申请日：1982-10-07

    申请人： Noriaki Nagano ,  Kohji Nakano ,  Tadao Shibanuma ,  Yukiyasu Murakami

    发明人： Noriaki Nagano ,  Kohji Nakano ,  Tadao Shibanuma ,  Yukiyasu Murakami

    IPC分类号： A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D277/20 ,  C07D501/20 ,  C07D501/24 ,  C07D501/36 ,  C07D501/56

    CPC分类号： C07D277/587 ,  Y02P20/55

    摘要： Cephalosporin compounds represented by the general formula ##STR1## wherein R represents a group shown by formula ##STR2## wherein R.sup.1 represents a hydrogen atom or a lower alkyl group of 1-3 carbon atoms and R.sup.2 represents a hydrogen atom, a lower alkyl group of 1-3 carbon atoms, a phenyl group which may be substituted by an amino or hydroxy group, a cyano group, a carboxy group, or a carboxymethyl group; said R.sup.1 and R.sup.2 may form a cycloalkylidene group of 4-6 carbon atoms together with the carbon atom to which they are bonded) or a group shown by formula --CH.sub.2 --R.sup.3 (wherein R.sup.3 represents a hydrogen atom, a halogenomethyl group, a carbamoyl group, a carboxymethyl group, .alpha.4-carboxy-3-hydroxyisothiazol-5-yl-thiomethyl group, or .alpha.2-carboxyphenylthiomethyl group); R' represents a group shown by formula ##STR3## (wherein R.sub.a represents a carboxy group, a cyano group, or a carbamoyl group which may be substituted by a lower alkyl group of 1-3 carbon atoms and R.sub.b represents a hydrogen atom or an amino group) or a group shown by formula ##STR4## (wherein R.sub.a and R.sub.b have the same significance as above); and the waveline .about. shows an anti-form or syn-form bond and the salts thereof. They possess excellent antibacterial activities against gram positive bacteria and gram negative bacteria, in particular, pseudomonas aeruginosa and are useful as anti-bacterial agents.

    摘要翻译： 由通式表示的头孢菌素化合物（其中R表示由式表示的基团，其中R1表示氢原子或1-3个碳原子的低级烷基，R2表示氢原子，低级烷基 1-3个碳原子的苯基，可以被氨基或羟基，氰基，羧基或羧甲基取代的苯基;所述R 1和R 2可以一起形成4-6个碳原子的亚环烷基 与其结合的碳原子）或式-CH 2 -R 3（其中R 3表示氢原子，卤代甲基，氨基甲酰基，羧甲基，α4-羧基-3-羟基异噻唑-5 - 基 - 硫代甲基或α2-羧基苯硫基甲基）; R'表示式IMA图示的基团（其中，Ra表示羧基，氰基或可被1-3个碳原子的低级烷基取代的氨基甲酰基，Rb表示氢原子或 氨基）或由式IMA IMA表示的基团（其中Ra和Rb具有与上述相同的含义）; 并且波纹差异显示出抗形式或顺式键及其盐。 它们对革兰氏阳性细菌和革兰氏阴性细菌，特别是铜绿假单胞菌具有优异的抗菌活性，可用作抗菌剂。