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    Taxoid derivative covalently linked to tumor-specific antibody and a method for preparing the same
    1.
    发明申请
    Taxoid derivative covalently linked to tumor-specific antibody and a method for preparing the same 审中-公开
    与肿瘤特异性抗体共价连接的紫杉烷衍生物及其制备方法

    公开(公告)号：US20070025995A1

    公开(公告)日：2007-02-01

    申请号：US11219686

    申请日：2005-09-07

    申请人： Hiroki Hamada ,  Katsuhiko Mikuni ,  Katsuyoshi Nakanishi ,  Tadakatsu Mandai

    发明人： Hiroki Hamada ,  Katsuhiko Mikuni ,  Katsuyoshi Nakanishi ,  Tadakatsu Mandai

    IPC分类号： A61K39/395 ,  C07K16/46

    CPC分类号： A61K47/6851 ,  A61K47/6809

    摘要： To provide a taxoid derivative that has improved solubility in water and acts specifically with respect to tumors, thereby mitigating side effects. The present invention provides an anticancer agent comprises covalent bond compound of an antibody that reacts specifically with respect to cancer cells with a taxoid derivative and a method for preparing the anticancer agent according to claim 1, characterized by reacting, in the presence of reduction agent, an antibody that reacts specifically with respect to cancer cells with a reaction product obtained by allowing periodic acid or periodate to act on a taxoid derivative.

    摘要翻译： 提供具有改善的在水中的溶解度并且特别针对肿瘤起作用的紫杉烷衍生物，从而减轻副作用。 本发明提供一种抗癌剂，其包含与癌细胞特异性反应的抗体的共价键化合物和紫杉烷衍生物，以及权利要求1所述的抗癌剂的制备方法，其特征在于，在还原剂存在下， 具有与癌细胞特异性反应的抗体与通过允许高碘酸或高碘酸盐作用于紫杉烷衍生物而获得的反应产物。

    Baccatin derivatives and a process for producing the same
    3.
    发明授权
    Baccatin derivatives and a process for producing the same 有权
    浆果赤霉素衍生物及其制备方法

    公开(公告)号：US06410757B1

    公开(公告)日：2002-06-25

    申请号：US09499393

    申请日：2000-02-07

    申请人： Tadakatsu Mandai ,  Hiroshi Okumoto ,  Katsuyoshi Nakanishi ,  Koji Hara ,  Katsuhiko Mikuni ,  Kozo Hara

    发明人： Tadakatsu Mandai ,  Hiroshi Okumoto ,  Katsuyoshi Nakanishi ,  Koji Hara ,  Katsuhiko Mikuni ,  Kozo Hara

    IPC分类号： C07D30514

    CPC分类号： C07D305/14 ,  Y02P20/55

    摘要： The object of the invention is to develop baccatin derivatives useful for preparing taxoid compounds such as paclitaxel and a process for the producing the same. The invention provides baccatin derivatives represented by the general formula (I) as well as a process for producing baccatin derivatives represented by the general formula (I) above, which comprises allowing a baccatin represented by the general formula (II) to react with a &bgr;-ketoester in the absence of a catalyst or in the presence of a tin compound or an amine base, preferably under reduced pressure.

    摘要翻译： 本发明的目的是开发可用于制备紫杉醇类紫杉醇类化合物的浆果赤霉素衍生物及其制备方法。 本发明提供由通式（I）表示的浆果赤霉素衍生物以及由上述通式（I）表示的浆果赤霉素衍生物的制备方法，其包括使由通式（II）表示的浆果赤霉素与β - 在不存在催化剂的情况下或在锡化合物或胺碱的存在下，优选在减压下进行。