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    (-)-Epigallocatechin Gallate Derivatives For Inhibiting Proteasome
    2.
    发明申请
    (-)-Epigallocatechin Gallate Derivatives For Inhibiting Proteasome 有权
    （ - ） - 表没食子儿茶素镓酸盐衍生物抑制蛋白酶体

    公开(公告)号：US20080176931A1

    公开(公告)日：2008-07-24

    申请号：US11660513

    申请日：2005-08-15

    申请人： Tak-Hang Chan ,  Wai-Har Lam ,  Larry Ming-Cheung Chow ,  Qing Ping Dou ,  Deborah Joyce Kuhn ,  Aslamuzzaman Kazi ,  Sheng Biao Wan ,  Kristin R. Landis-Piwowar

    发明人： Tak-Hang Chan ,  Wai-Har Lam ,  Larry Ming-Cheung Chow ,  Qing Ping Dou ,  Deborah Joyce Kuhn ,  Aslamuzzaman Kazi ,  Sheng Biao Wan ,  Kristin R. Landis-Piwowar

    IPC分类号： A61K31/352 ,  A61P35/00 ,  C07D311/02

    CPC分类号： C07D311/62 ,  Y02P20/582

    摘要： (−)-EGCG, the most abundant catechin, was found to be chemopreventive and anticancer agent. However, (−)-EGCG has at least one limitation: it gives poor bioavailability. This invention provides compounds of generally formulae below, wherein R11, R12, R13, R21, R22, R2, R3, and R4 are each independently selected from the group consisting of —H, and C1 to C10 acyloxyl group; and R5 is selected from the group consisting of —H, C1-C10-alkyl, C2-C10-alkenyl, C2-C10-alkynyl, C3-C7-cycloalkyl, phenyl, benzyl and C3 -C7 -cycloalkenyl, whereas each of the last mentioned 7 groups can be substituted with any combination of one to six halogen atoms; at least one of R11, R12, R13, R21, R22, R2, R3 and R4 is —H, which were found to be more potent than their non-protected counterparts, which can be used as proteasome inhibitors to reduce tumor cell growth.

    摘要翻译： （ - ） - EGCG是最丰富的儿茶素，被发现是化学预防和抗癌剂。 然而，（ - ） - EGCG至少有一个限制：它具有差的生物利用度。 本发明提供下列通式的化合物，其中R 11，R 12，R 13，R 21， R 22，R 2，R 3和R 4各自独立地选自 - H和C 1至C 10酰氧基; 和R 5选自-H，C 1 -C 10 - 烷基，C 2 H 2 C 1 -C 10 - 烯基，C 2 -C 10 - 炔基，C 1 -C 3 - 7个 - 环烷基，苯基，苄基和C 3 -C 7 - 环烯基，而最后提到的7个基团中的每一个可以被一个 至六个卤素原子; R 11，R 12，R 13，R 21，R 22中的至少一个， R 2，R 3和R 4是-H，其被发现比它们的非保护对应物更有效 ，其可以用作蛋白酶体抑制剂以减少肿瘤细胞生长。

    (−)-epigallocatechin gallate derivatives for inhibiting proteasome
    5.
    发明授权
    (−)-epigallocatechin gallate derivatives for inhibiting proteasome 有权
    （ - ） - 表没食子儿茶素没食子酸酯衍生物用于抑制蛋白酶体

    公开(公告)号：US08193377B2

    公开(公告)日：2012-06-05

    申请号：US11660513

    申请日：2005-08-15

    申请人： Tak-Hang Chan ,  Wai-Har Lam ,  Larry Ming-Cheung Chow ,  Qing Ping Dou ,  Deborah Joyce Kuhn ,  Aslamuzzaman Kazi ,  Sheng Biao Wan ,  Kristin R. Landis-Piwowar

    发明人： Tak-Hang Chan ,  Wai-Har Lam ,  Larry Ming-Cheung Chow ,  Qing Ping Dou ,  Deborah Joyce Kuhn ,  Aslamuzzaman Kazi ,  Sheng Biao Wan ,  Kristin R. Landis-Piwowar

    IPC分类号： C07D311/00 ,  A01N43/16

    CPC分类号： C07D311/62 ,  Y02P20/582

    摘要： (−)-EGCG, the most abundant catechin, was found to be chemopreventive and anticancer agent. However, (−)-EGCG has at least one limitation: it gives poor bioavailability. This invention provides compounds of generally formulae below, wherein R11, R12, R13, R21, R22, R2, R3, and R4 are each independently selected from the group consisting of —H, and C1 to C10 acyloxyl group; and R5 is selected from the group consisting of —H, C1-C10-alkyl, C2-C10-alkenyl, C2-C10-alkynyl, C3-C7-cycloalkyl, phenyl, benzyl and C3-C7-cycloalkenyl, whereas each of the last mentioned 7 groups can be substituted with any combination of one to six halogen atoms; at least one of R11, R12, R13, R21, R22, R2, R3 and R4 is —H, which were found to be more potent than their non-protected counterparts, which can be used as proteasome inhibitors to reduce tumor cell growth.

    摘要翻译： （ - ） - EGCG是最丰富的儿茶素，被发现是化学预防和抗癌剂。 然而，（ - ） - EGCG至少有一个限制：它具有差的生物利用度。 本发明提供下列通式的化合物，其中R11，R12，R13，R21，R22，R2，R3和R4各自独立地选自-H和C1至C10酰氧基; 并且R 5选自-H，C 1 -C 10 - 烷基，C 2 -C 10 - 烯基，C 2 -C 10 - 炔基，C 3 -C 7 - 环烷基，苯基，苄基和C 3 -C 7 - 环烯基， 最后提到的7个基团可以被1-6个卤素原子的任意组合取代; R11，R12，R13，R21，R22，R2，R3和R4中的至少一个是-H，其被发现比其非保护对应物更有效，其可以用作蛋白酶体抑制剂以减少肿瘤细胞生长。