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    Cephalosporin derivatives
    1.
    发明授权
    Cephalosporin derivatives 失效
    头孢菌素衍生物

    公开(公告)号：US4007177A

    公开(公告)日：1977-02-08

    申请号：US523819

    申请日：1974-11-14

    申请人： Hideo Nakao ,  Hiroaki Yanagisawa ,  Mitsuo Nagano ,  Bunji Shimizu ,  Masakatsu Kaneko ,  Shinichi Sugawara

    发明人： Hideo Nakao ,  Hiroaki Yanagisawa ,  Mitsuo Nagano ,  Bunji Shimizu ,  Masakatsu Kaneko ,  Shinichi Sugawara

    IPC分类号： C07C323/48 ,  C07D261/10 ,  C07D261/12 ,  C07D309/12 ,  C07D501/57 ,  C07D505/00 ,  C07D501/50 ,  C07D501/56

    CPC分类号： C07D309/12 ,  C07D261/10 ,  C07D261/12 ,  Y02P20/55

    摘要： A compound of the formula ##STR1## wherein A represents acetoxy group, carbamoyloxy group or (1-metyl-1H-tetrazol-5-yl)thio group and Y represents propargylthio group, azidomethylthio group, 2-hydroxyethylthio group, 3-isoxazolyloxy group, 3-isoxazolylthio group, methylsulfonyl group, ethylsulfonyl group, 2-cyanoethyl-sulfonyl group or sydnon-3-yl group and nontoxic pharmaceutically acceptable salts thereof are prepared by a process which comprises reacting a compound of the formula ##STR2## wherein R represents a protective group for a carboxyl group and A has the same meaning as defined above with a carboxylic acid of the formulaY - CH.sub.2 COOHwherein Y has the same meaning as defined above or a reactive derivative thereof to give a compound having the formula ##STR3## wherein A, R and Y have the same meanings as defined above and removing the protective group for the carboxyl group from said compound.The compounds are antibacterial agents.

    摘要翻译： 其中A表示乙酰氧基，氨基甲酰氧基或（1-甲基-1H-四唑-5-基）硫基，Y表示炔丙硫基，叠氮甲硫基，2-羟乙硫基，3-异恶唑基氧基 3-异恶唑基硫代基，甲基磺酰基，乙基磺酰基，2-氰基乙基磺酰基或者sydnon-3-基及其无毒的药学上可接受的盐通过以下方法制备，该方法包括使下式化合物 羧基的保护基和A具有如上所定义的与式Y-CH 2 COOH的羧酸的含义，其中Y具有与上述相同的含义或其反应性衍生物，得到具有下式的化合物： 其中A，R和Y具有与上述相同的含义，并从所述化合物中除去羧基的保护基。

    7-Methoxycephalosporin derivatives
    2.
    发明授权
    7-Methoxycephalosporin derivatives 失效
    7-甲氧基头孢菌素衍生物

    公开(公告)号：US4126745A

    公开(公告)日：1978-11-21

    申请号：US676488

    申请日：1976-04-13

    申请人： Hideo Nakao ,  Hiroaki Yanagisawa ,  Bunji Shimizu ,  Masakatsu Kaneko ,  Mitsuo Nagano ,  Shinichi Sugawara

    发明人： Hideo Nakao ,  Hiroaki Yanagisawa ,  Bunji Shimizu ,  Masakatsu Kaneko ,  Mitsuo Nagano ,  Shinichi Sugawara

    IPC分类号： A61K31/545 ,  C07D20060101 ,  C07D205/08 ,  C07D257/04 ,  C07D279/04 ,  C07D501/00 ,  C07D501/36 ,  C07D501/40 ,  C07D501/50 ,  C07D501/57 ,  C07D501/60

    CPC分类号： C07D501/57 ,  Y02P20/55

    摘要： A compound having the formula ##STR1## wherein Y represents a 2-carboxyethylthio group or a trifluoromethylthio group and a nontoxic pharmaceutically acceptable salt thereof are useful as antibacterial agents. They may be prepared by (a) reacting a compound having the formula ##STR2## wherein X.sub.1 represents a halogen atom with a compound having the formulaY -- Hwherein Y has the same meaning as defined above, or (b) reacting a compound having the formula ##STR3## wherein R represents a protective group for the carboxyl group with a compound having the formulaY -- CH.sub.2 COX.sub.2wherein X.sub.2 represents a halogen atom and Y has the same meaning as defined above and removing the protective group for the carboxyl group from the resulting product, or (c) reacting a compound having the formula ##STR4## wherein A represents an acetoxy group or a carbamoyloxy group and Y has the same meaning as defined above with 5-mercapto-1-methyl-1H-tetrazole or its alkali metal salt.

    摘要翻译： 具有式“IMAGE”的化合物，其中Y表示2-羧乙硫基或三氟甲硫基，其无毒的药学上可接受的盐可用作抗菌剂。 它们可以通过以下方法来制备：（a）使具有式“IMAGE”的化合物（其中X1表示卤素原子）与具有式Y-H的化合物反应，其中Y具有与上述相同的含义，或（b）使具有 其中R表示具有式Y-CH 2 COX 2的化合物的羧基保护基，其中X 2表示卤素原子，Y表示与上述相同的含义，并且从该基团除去羧基的保护基团 得到的产物，或（c）使具有式“IMAGE”的化合物，其中A表示乙酰氧基或氨基甲酰氧基，Y与上述定义同上，与5-巯基-1-甲基-1H-四唑或其碱 金属盐。