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    Cephalosporins
    5.
    发明授权
    Cephalosporins 失效
    头孢菌素

    公开(公告)号：US4489072A

    公开(公告)日：1984-12-18

    申请号：US304912

    申请日：1981-09-23

    申请人： Hiroshi Sadaki ,  Hirokazu Narita ,  Hiroyuki Imaizumi ,  Yoshinori Konishi ,  Takihiro Inaba ,  Tatsuo Hirakawa ,  Hideo Taki ,  Masaru Tai ,  Yasuo Watanabe ,  Isamu Saikawa

    发明人： Hiroshi Sadaki ,  Hirokazu Narita ,  Hiroyuki Imaizumi ,  Yoshinori Konishi ,  Takihiro Inaba ,  Tatsuo Hirakawa ,  Hideo Taki ,  Masaru Tai ,  Yasuo Watanabe ,  Isamu Saikawa

    IPC分类号： C07D501/24 ,  A61K31/545 ,  C07D20060101 ,  C07D501/04 ,  C07D501/18 ,  C07D501/20 ,  C07D501/38 ,  C07D501/40 ,  C07D501/46 ,  C07D501/56 ,  C07D501/57

    CPC分类号： C07D501/46 ,  A61K31/545 ,  C07D501/38 ,  C07D501/56 ,  C07D501/57

    摘要： Novel cephalosporins which has attached to the exomethylene group at the 3-position of the cephem ring a substituted or unsubstituted aryl, acylamino, aromatic heterocyclic, triazolyl or tetrazolyl group, said aromatic heterocyclic group being attached through a carbon-carbon bond and said triazolyl or tetrazolyl group being attached through a carbon-nitrogen bond, and has the following group attached to the amino group at the 7-position: ##STR1## wherein A represents a group of the formula, --CH.sub.2 -- or a group of the formula ##STR2## in which R.sup.5 represents a hydrogen atom or an alkyl group, and the bond represents syn or anti isomer or their mixture; R.sup.3 represents a hydrogen or halogen atom; and R.sup.4 represents a hydrogen atom or an amino group which may be protected or substituted. These cephalosporins have a broad antibacterial spectrum, are stable against .beta.-lactamase produced by bacteria, have a low toxicity, and are well absorbed when administered orally or parenterally.This invention relates to such novel cephalosporins, processes for producing said cephalosporins, intermediates for producing said cephalosporins, and a process for producing said intermediates.

    摘要翻译： 在头孢烯环的3位连接到外亚甲基的新型头孢菌素是取代或未取代的芳基，酰氨基，芳族杂环，三唑基或四唑基，所述芳族杂环基通过碳 - 碳键连接，所述三唑基或 四唑基通过碳 - 氮键连接，并且具有与7-位上的氨基连接的下列基团：其中A表示下式的基团：-CH 2 - 或式 其中R 5表示氢原子或烷基，并且该键表示顺式或反式异构体或其混合物; R3表示氢或卤素原子; R4表示氢原子或可被保护或取代的氨基。 这些头孢菌素具有广泛的抗菌谱，对细菌产生的β-内酰胺酶是稳定的，具有低毒性，并且当口服或肠胃外给药时被良好吸收。 本发明涉及这种新型头孢菌素，生产所述头孢菌素的方法，用于生产所述头孢菌素的中间体，以及生产所述中间体的方法。