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    Penam derivatives and salts thereof, process for producing the same and antibacterial agent comprising the same
    1.
    发明授权
    Penam derivatives and salts thereof, process for producing the same and antibacterial agent comprising the same 失效
    Penam衍生物及其盐，其制备方法和含有它们的抗菌剂

    公开(公告)号：US5300497A

    公开(公告)日：1994-04-05

    申请号：US957372

    申请日：1992-10-07

    申请人： Hirokazu Ochiai ,  Yasuo Watanabe ,  Yoshiharu Murotani ,  Hirohiko Fukuda ,  Osamu Yoshino ,  Shinzaburo Minami ,  Toshio Hayashi ,  Kaishu Momonoi

    发明人： Hirokazu Ochiai ,  Yasuo Watanabe ,  Yoshiharu Murotani ,  Hirohiko Fukuda ,  Osamu Yoshino ,  Shinzaburo Minami ,  Toshio Hayashi ,  Kaishu Momonoi

    IPC分类号： C07D499/00 ,  C07D499/21 ,  C07D499/87 ,  C07D519/06 ,  A61K31/425

    CPC分类号： C07D499/00 ,  Y02P20/55

    摘要： A penam derivative represented by the following general formula or a salt thereof: ##STR1## wherein R.sup.1 represents a hydrogen atom, an amino-protecting group or an acyl group; R.sup.2 represents a hydrogen atom or a lower alkyl group; R.sup.3 represents a hydrogen atom, a lower alkoxy group, a lower alkylthio group or a formamido group; R.sup.4 represents an protected or unprotected carboxyl group or a carboxylato group; R represents a group of the formula, --NHR.sup.5 or --NR.sup.5 R.sup.6 (in which R.sup.5 and R.sup.6, which may be the same or different, represent protected or unprotected hydroxyl groups, cyano groups, sulfo groups, or unsubstituted or substituted lower alkyl, aryl, acyl, carbamoyl, sulfamoyl, lower alkylsulfonyl or heterocyclic groups) or a group of the formula, --N.dbd.CR.sup.7 R.sup.8 (in which R.sup.7 and R.sup.8, which may be the same or different, represent hydrogen atoms or protected or unprotected carboxyl groups, cyano groups or unsubstituted or substituted lower alkyl, lower alkenyl, lower alkynyl, aryl, amino, acyl, acyloxy, carbamoyl, carbamoyloxy, sulfamoyl, lower alkylthio, ureido or heterocyclic groups, or R.sup.7 and R.sup.8 may form a cycloalkene or a heterocyclic ring with the carbon atom to which R.sup.7 and R.sup.8 are attached); and n represents 1 or 2. The above penam derivative or its salt is very effective as antibacterial agents.

    摘要翻译： 由以下通式表示的penam衍生物或其盐：其中R 1表示氢原子，氨基保护基或酰基; R2表示氢原子或低级烷基; R3表示氢原子，低级烷氧基，低级烷硫基或甲酰氨基; R4代表受保护或未保护的羧基或羧基; R表示式-NHR 5或-NR 5 R 6基团（其中R 5和R 6可以相同或不同，表示保护或未被保护的羟基，氰基，磺基或未取代或取代的低级烷基，芳基， 酰基，氨基甲酰基，氨磺酰基，低级烷基磺酰基或杂环基）或下式基团-N = CR7R8（其中R7和R8可以相同或不同，表示氢原子或被保护或未被保护的羧基，氰基 或未取代或取代的低级烷基，低级烯基，低级炔基，芳基，氨基，酰基，酰氧基，氨基甲酰基，氨基甲酰氧基，氨磺酰基，低级烷硫基，脲基或杂环基，或者R7和R8可以与碳形成环烯或杂环 R7和R8所连接的原子）; 并且n表示1或2.上述阳am衍生物或其盐作为抗菌剂是非常有效的。

    Penam derivatives and salts thereof, and antibacterial agent comprising the same
    2.
    发明授权
    Penam derivatives and salts thereof, and antibacterial agent comprising the same 失效
    PENAM衍生物及其盐，以及包含其的抗菌剂

    公开(公告)号：US5185330A

    公开(公告)日：1993-02-09

    申请号：US540697

    申请日：1990-06-20

    申请人： Hirokazu Ochiai ,  Yasuo Watanabe ,  Yoshiharu Murotani ,  Hirohiko Fukuda ,  Osamu Yoshino ,  Shinzaburo Minami ,  Toshio Hayashi ,  Kaishu Momonoi

    发明人： Hirokazu Ochiai ,  Yasuo Watanabe ,  Yoshiharu Murotani ,  Hirohiko Fukuda ,  Osamu Yoshino ,  Shinzaburo Minami ,  Toshio Hayashi ,  Kaishu Momonoi

    IPC分类号： C07D499/00 ,  C07D499/21 ,  C07D499/87 ,  C07D519/06

    CPC分类号： C07D499/00 ,  Y02P20/55

    摘要： A penam derivative represented by the following general formula or a salt thereof: ##STR1## wherein R.sup.1 represents a hydrogen atom, an amino-protecting group or an acyl group; R.sup.2 represents a hydrogen atom or a lower alkyl group; R.sup.3 represents a hydrogen atom, a lower alkoxy group, a lower alkylthio group or a formamido group; R.sup.4 represents a protected or unprotected carboxy group or a craboxylato group; R represents a group of the formula, --NHR.sup.5 or --NR.sup.5 R.sup.6 (in which R.sup.5 and R.sup.6, which may be the same or different, represent protected or unprotected hydroxyl groups, cyano groups, sulfo groups, or unsubstituted or substituted lower alkyl, aryl, acyl, carbamoyl, sulfamoyl, lower alkylsulfonyl or heterocyclic groups) or a group of the formula, --N.dbd.CR.sup.7 R.sup.8 (in which R.sup.7 and R.sup.8, which may be the same or different, represent hydrogen atoms or protected or unprotected carboxyl groups, cyano groups or unsubstituted or substituted lower alkyl, lower alkenyl, lower alkynyl, aryl, amino, acyl, acyloxy, carbamoyl, carbamoyloxy, sulfamoyl, lower alkylthio, ureido or heterocyclic groups, or R.sup.7 and R.sup.8 may form a cycloalkene or a heterocyclic ring with the carbon atom to which R.sup.7 and R.sup.8 are attached); and n represents 1 or 2. The above penam derivative or its salt is very effective as antibacterial agents.

    摘要翻译： 由以下通式表示的penam衍生物或其盐：其中R 1表示氢原子，氨基保护基或酰基; R2表示氢原子或低级烷基; R3表示氢原子，低级烷氧基，低级烷硫基或甲酰氨基; R4表示保护或未保护的羧基或酰胺基; R表示式-NHR 5或-NR 5 R 6基团（其中R 5和R 6可以相同或不同，表示保护或未被保护的羟基，氰基，磺基或未取代或取代的低级烷基，芳基， 酰基，氨基甲酰基，氨磺酰基，低级烷基磺酰基或杂环基）或下式基团-N = CR7R8（其中R7和R8可以相同或不同，表示氢原子或被保护或未被保护的羧基，氰基 或未取代或取代的低级烷基，低级烯基，低级炔基，芳基，氨基，酰基，酰氧基，氨基甲酰基，氨基甲酰氧基，氨磺酰基，低级烷硫基，脲基或杂环基，或者R7和R8可以与碳形成环烯或杂环 R7和R8所连接的原子）; 并且n表示1或2.上述阳am衍生物或其盐作为抗菌剂是非常有效的。