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    Flavonoid dimers and methods of making and using such
    3.
    发明授权
    Flavonoid dimers and methods of making and using such 有权
    黄酮类二聚体及其制备和使用方法

    公开(公告)号：US08710097B2

    公开(公告)日：2014-04-29

    申请号：US12301504

    申请日：2007-05-09

    申请人： Tak-Hang Chan ,  Larry Ming-Cheung Chow

    发明人： Tak-Hang Chan ,  Larry Ming-Cheung Chow

    IPC分类号： A61K31/353 ,  C07D405/12 ,  A61P43/00

    CPC分类号： C07D311/30 ,  C07D311/32 ,  C07D407/12

    摘要： Multidrug resistance (MDR) is a major problem in cancer chemotherapy. The best characterized resistance mechanism is the one mediated by the over-expression of drug efflux transporters, permeability-glycoprotein (P-gp), which pump a variety of anticancer drugs out of the cells, resulting in lowered intracellular drug accumulation. A series of flavonoid dimers are developed in this invention, which are linked together by linker groups of various lengths. These flavonoid dimers are found to be efficient P-gp modulators that increase cytotoxicity of anticancer drugs in vitro and dramatically enhance their intracellular drug accumulation. It is found that the flavonoid dimers of this invention is also useful in reducing drug resistance in treating parasitic diseases.

    摘要翻译： 多药耐药（MDR）是癌症化疗中的主要问题。 最好的抗性机制是由药物流出转运蛋白（P-gp）的过表达介导的，其将多种抗癌药物从细胞中泵出，导致细胞内药物积累降低。 在本发明中开发了一系列类黄酮二聚体，其通过各种长度的连接基团连接在一起。 发现这些类黄酮二聚体是有效的P-gp调节剂，其在体外增加抗癌药物的细胞毒性并显着增强细胞内药物的积累。 发现本发明的类黄酮二聚体也可用于降低治疗寄生虫病的耐药性。

    (-)-Epigallocatechin Gallate Derivatives For Inhibiting Proteasome
    5.
    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
    6.
    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。

    Flavonoid Dimers and Methods of Making and Using Such
    7.
    发明申请
    Flavonoid Dimers and Methods of Making and Using Such 有权
    黄酮类二聚体及其使用方法

    公开(公告)号：US20090197943A1

    公开(公告)日：2009-08-06

    申请号：US12301504

    申请日：2007-05-09

    申请人： Tak-Hang Chan ,  Larry Ming-Cheung Chow

    发明人： Tak-Hang Chan ,  Larry Ming-Cheung Chow

    IPC分类号： A61K31/353 ,  C07D405/12 ,  A61P43/00

    CPC分类号： C07D311/30 ,  C07D311/32 ,  C07D407/12

    摘要： Multidrug resistance (MDR) is a major problem in cancer chemotherapy. The best characterized resistance mechanism is the one mediated by the over-expression of drug efflux transporters, permeability-glycoprotein (P-gp), which pump a variety of anticancer drugs out of the cells, resulting in lowered intracellular drug accumulation. A series of flavonoid dimers are developed in this invention, which are linked together by linker groups of various lengths. These flavonoid dimers are found to be efficient P-gp modulators that increase cytotoxicity of anticancer drugs in vitro and dramatically enhance their intracellular drug accumulation. It is found that the flavonoid dimers of this invention is also useful in reducing drug resistance in treating parasitic diseases.

    摘要翻译： 多药耐药（MDR）是癌症化疗中的主要问题。 最好的抗性机制是由药物流出转运蛋白（P-gp）的过表达介导的，其将多种抗癌药物从细胞中泵出，导致细胞内药物积累降低。 在本发明中开发了一系列类黄酮二聚体，其通过各种长度的连接基团连接在一起。 发现这些类黄酮二聚体是有效的P-gp调节剂，其在体外增加抗癌药物的细胞毒性并显着增强细胞内药物的积累。 发现本发明的类黄酮二聚体也可用于降低治疗寄生虫病的耐药性。

    (−)-Epigallocatechin gallate derivatives for inhibiting proteasome
    8.
    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：US07544816B2

    公开(公告)日：2009-06-09

    申请号：US10921332

    申请日：2004-08-19

    申请人： Tak-Hang Chan ,  Wai-Har Lam ,  Larry Ming-Cheung Chow ,  Qing Ping Dou ,  Deborah Joyce Kuhn ,  Aslamuzzaman Kazi

    发明人： Tak-Hang Chan ,  Wai-Har Lam ,  Larry Ming-Cheung Chow ,  Qing Ping Dou ,  Deborah Joyce Kuhn ,  Aslamuzzaman Kazi

    IPC分类号： C07D311/82 ,  A61K31/35

    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 formula 10, wherein R1 is selected from the group of —H and C1 to C6 acyl group; R2, R3, and R4 are each independently selected from the group of —H, —OH, and C1 to C6 acyloxyl group; and at least one of R2, R3, or R4 is —H. The derivatives of (−)-EGCG that is at least as potent as (−)-EGCG. The carboxylate protected forms of (−)-EGCG and its derivatives are found to be more stable than the unprotected forms, which can be used as proteasome inhibitors to reduce tumor cell growth.

    摘要翻译： （ - ） - EGCG，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。 本发明提供通式为10的化合物，其中R 1选自-H和C 1至C 6酰基; R2，R3和R4各自独立地选自-H，-OH和C1至C6酰氧基; R2，R3或R4中的至少一个为-H。 （ - ） - EGCG的衍生物至少与（ - ） - EGCG一样有效。 发现羧酸酯保护形式的（ - ） - EGCG及其衍生物比未保护形式更稳定，可用作蛋白酶体抑制剂以减少肿瘤细胞生长。

    (-)-Epigallocatechin gallate derivatives for inhibiting proteasome
    10.
    发明申请
    (-)-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：US20060041010A1

    公开(公告)日：2006-02-23

    申请号：US10921332

    申请日：2004-08-19

    申请人： Tak-Hang Chan ,  Wai-Har Lam ,  Larry Chow ,  Qing Dou ,  Deborah Kuhn ,  Aslamuzzaman Kazi

    发明人： Tak-Hang Chan ,  Wai-Har Lam ,  Larry Chow ,  Qing Dou ,  Deborah Kuhn ,  Aslamuzzaman Kazi

    IPC分类号： A61K31/353 ,  C07D311/22

    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 formula 10, wherein R1 is selected from the group of —H and C1 to C6 acyl group; R2, R3, and R4 are each independently selected from the group of —H, —OH, and C1 to C6 acyloxyl group; and at least one of R2, R3, or R4 is —H. The derivatives of (−)-EGCG that is at least as potent as (−)-EGCG. The carboxylate protected forms of (−)-EGCG and its derivatives are found to be more stable than the unprotected forms, 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。 本发明提供通式为10的化合物，其中R 1选自-H和C 1至C 6酰基基团; R 2，R 3和R 4各自独立地选自-H，-OH和C 1的基团 C 6 -C 5酰氧基; 并且R 2，R 3或R 4中的至少一个为-H。 （ - ） - EGCG的衍生物至少与（ - ） - EGCG一样有效。 发现羧酸酯保护形式的（ - ） - EGCG及其衍生物比未保护形式更稳定，可用作蛋白酶体抑制剂以减少肿瘤细胞生长。