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    CAPRAZENE AS NOVEL COMPOUND AND DERIVATIVES THEREOF, AND CAPRAZOL AS NOVEL COMPOUND AND DERIVATIVES THEREOF
    2.
    发明公开
    CAPRAZENE AS NOVEL COMPOUND AND DERIVATIVES THEREOF, AND CAPRAZOL AS NOVEL COMPOUND AND DERIVATIVES THEREOF 有权
    卡波拉DORIVAT ZUR SYNTHESE VON ANTIBIOTIKA

    公开(公告)号：EP1593684A1

    公开(公告)日：2005-11-09

    申请号：EP04706817.6

    申请日：2004-01-30

    申请人： ZAIDAN HOJIN BISEIBUTSU KAGAKU KENKYU KAI ,  Meiji Seika Kaisha, Ltd.

    发明人： MIYAKE, Toshiaki ,  IGARASHI, Masayuki ,  SHITARA, Tetsuo ,  TAKAHASHI, Yoshiaki ,  HAMADA, Masa

    IPC分类号： C07H19/06 ,  A61K31/7072 ,  A61P31/04 ,  A61P31/06

    CPC分类号： C07H19/067 ,  A61K31/7072 ,  C07D403/08 ,  C07D403/14 ,  C07D405/14 ,  C07H15/26 ,  C07H19/06 ,  Y02P20/55

    摘要： Caprazene and caprazol could be synthesized by hydrolysis of a caprazamycin. There could be synthesized a caprazene-1'''-amide derivative of the formula (II)
    and a caprazene-1'''-ester derivative of the formula (III)
    from caprazene. Further, there could be synthesized a caprazol-1'''-amide derivative of the formula (V)
    and a caprazol-1'''- amide-3'''-ester derivative and a caprazol-3'''-ester derivative, etc. from caprazol. Furthermore, an imidazolidinone derivative could be synthesized from the ring-opened product of the 1,4-diazepinone ring of caprazol.
    The novel caprazene derivative, novel caprazol derivative and novel imidazolidinone derivative now synthesized exhibit excellent antibacterial activities against a variety of bacteria, including acid-fast bacteria.

    摘要翻译： Caprazene和caprazol可以通过caprazamycin的水解合成。 可以从癸酰肼合成式（II）的二甲基-1“ - 酰胺衍生物＆lt; CHEM＆gt;和式（III）的癸酰-1” - 酯衍生物。 此外，可以合成式（V）的caprazol-1“ - 酰胺衍生物和caprazol-1”' - 酰胺-3' - 酯衍生物和caprazol-3“ 癸酯衍生物等。 此外，咪唑啉酮衍生物可以由四唑的1,4-二氮杂环酮环的开环产物合成。 现在合成的新型caprazene衍生物，新颖的吡唑衍生物和新的咪唑烷酮衍生物对各种细菌，包括耐酸细菌表现出优异的抗菌活性。