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    Baccatin derivatives and a process for producing the same
    1.
    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。

    Taxoid derivative and method of producing thereof
    5.
    发明授权
    Taxoid derivative and method of producing thereof 失效
    紫杉烷衍生物及其制备方法

    公开(公告)号：US5767297A

    公开(公告)日：1998-06-16

    申请号：US868151

    申请日：1997-06-03

    申请人： Tadakatsu Mandai ,  Hiroshi Okumoto ,  Koji Hara ,  Katsuhiko Mikuni ,  Kozo Hara ,  Hiroki Hamada

    发明人： Tadakatsu Mandai ,  Hiroshi Okumoto ,  Koji Hara ,  Katsuhiko Mikuni ,  Kozo Hara ,  Hiroki Hamada

    IPC分类号： C07D305/14

    CPC分类号： C07D305/14

    摘要： A taxoid derivative wherein sugar is combined with any one of paclitaxel, docetaxel and 10-deacetyl-bacatin III via a spacer. A method of producing the taxoid derivative comprises protecting hydroxyl groups at specific position of paclitaxel or docetaxel by protective compound followed by reacting with tetrabenzyl acetyloxyglucoside, and then carrying out debenzyl and detriethylsilyl reactions. A method of producing the taxoid derivative comprises reacting paclitaxel or docetaxel with tetrabenzyl acetyloxyglucoside, and then carrying out debenzyl reaction.

    摘要翻译： 一种紫杉烷衍生物，其中糖通过间隔基与紫杉醇，多西他赛和10-脱乙酰基 - 条肽III中的任一种组合。 制备紫杉烷衍生物的方法包括用保护性化合物保护紫杉醇或多西他赛特定位置的羟基，然后与四苄基乙酰氧基葡糖苷反应，然后进行脱苄基和脱乙基甲硅烷基反应。 制备紫杉烷衍生物的方法包括使紫杉醇或多西紫杉醇与四苄基乙酰氧基葡糖苷反应，然后进行脱苄基反应。

    Taxoid derivatives and process for producing the same
    6.
    发明授权
    Taxoid derivatives and process for producing the same 有权
    紫杉烷衍生物及其生产方法

    公开(公告)号：US06306893B1

    公开(公告)日：2001-10-23

    申请号：US09529208

    申请日：2000-04-07

    申请人： Tadakatsu Mandai ,  Hiroshi Okumoto ,  Koji Hara ,  Katsuhiko Mikuni ,  Kozo Hara ,  Yoshinori Tsuchiya ,  Kosho Nakamura ,  Teruhiko Umetsu

    发明人： Tadakatsu Mandai ,  Hiroshi Okumoto ,  Koji Hara ,  Katsuhiko Mikuni ,  Kozo Hara ,  Yoshinori Tsuchiya ,  Kosho Nakamura ,  Teruhiko Umetsu

    IPC分类号： A61K3335

    CPC分类号： C07H15/04 ,  C07H15/26

    摘要： An object of the invention is to develop galactose or mannose derivatives of docetaxel, etc. having improved solubility and physiological activity, to alleviate burden imposed on patients and to provide effective therapeutic drug for tumors. The present invention provides taxoid derivatives comprising any of paclitaxel, docetaxel and 10-deacetyl-baccatin III to which galactose or mannose is linked through a spacer, and methods for producing taxoid derivatives comprising reacting paclitaxel, docetaxel or 10-deacetyl-baccatin III with tetrabenzyl acetyloxygalactoside or tetrabenzyl acetyloxymannoside, subjecting the product to debenzylation reaction, and optionally to detriethylsilylation reaction.

    摘要翻译： 本发明的目的是开发具有改善的溶解性和生理活性的多西紫杉醇等的半乳糖或甘露糖衍生物，以减轻施加于患者的负担并为肿瘤提供有效的治疗药物。本发明提供了包含紫杉醇， 多西紫杉醇和通过间隔基连接的10-脱乙酰基 - 浆果赤霉素III，以及用于制备紫杉醇，多西紫杉醇或10-脱乙酰基浆果赤霉素III与四苄基乙酰氧基半乳糖苷或四苄基乙酰氧基甘露糖苷的方法，所述方法包括使产物脱苄基反应 ，并任选地进行脱乙烯基硅烷化反应。

    Taxoid derivative covalently linked to tumor-specific antibody and a method for preparing the same
    7.
    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。

    Cyclodextrin inclusion complex of taxol, and method for its production and its use
    9.
    发明授权
    Cyclodextrin inclusion complex of taxol, and method for its production and its use 失效
    紫杉醇的环糊精包合物及其生产方法及其应用

    公开(公告)号：US5684169A

    公开(公告)日：1997-11-04

    申请号：US470018

    申请日：1995-06-06

    申请人： Hiroki Hamada ,  Kyoko Saito ,  Katsuhiko Mikuni ,  Nobuhiro Kuwahara ,  Hideki Takahashi

    发明人： Hiroki Hamada ,  Kyoko Saito ,  Katsuhiko Mikuni ,  Nobuhiro Kuwahara ,  Hideki Takahashi

    IPC分类号： A61K31/335 ,  A61K47/48 ,  C07D305/14

    CPC分类号： B82Y5/00 ,  A61K31/335 ,  A61K47/48969

    摘要： There is provided an unbranched cyclodextrin or a branched cyclodextrin inclusion complex of taxol. The complex is produced by adding an unbranched cyclodextrin of a branched cyclodextrin to taxol at a molar ratio of 1-20 times with respect to taxol. A method is provided for the improvement of the solubility of taxol in water by adding an unbranched cyclodextrin or a branched cyclodextrin thereto at a molar ratio of 1-20 times with respect to taxol. The solubility of taxol in water is improved by the present invention. A cyclodextrin inclusion complex of taxol according to the present invention serves to make taxol more easily absorbed when administered to a cancer patient, which is beneficial to cancer patients and the physiological effects of taxol may therefore be more effectively induced.

    摘要翻译： 提供紫杉醇的无支链环糊精或支链环糊精包合物。 通过将支链环糊精的无支链环糊精与紫杉醇以相对于紫杉醇为1-20倍的摩尔比添加到紫杉醇中而制备。 提供了一种通过以相对于紫杉醇为1-20倍的摩尔比添加无支链环糊精或支链环糊精来提高紫杉醇在水中的溶解度的方法。 本发明提高了紫杉醇在水中的溶解度。 根据本发明的紫杉醇的环糊精包合物用于在给予癌症患者时更容易地吸收紫杉醇，这有利于癌症患者，因此可以更有效地诱导紫杉醇的生理作用。