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    IONIC LIQUID SUPPORTED SYNTHESIS
    4.
    发明申请
    IONIC LIQUID SUPPORTED SYNTHESIS 有权
    离子液体支持合成

    公开(公告)号：US20100041869A1

    公开(公告)日：2010-02-18

    申请号：US11908487

    申请日：2006-03-15

    申请人： Tak-Hang Chan ,  Masad J. Damha ,  Weishi Miao ,  Robert Alexander Donga ,  Xun He

    发明人： Tak-Hang Chan ,  Masad J. Damha ,  Weishi Miao ,  Robert Alexander Donga ,  Xun He

    IPC分类号： C07K1/00 ,  C07H1/00

    CPC分类号： C07H21/00 ,  C07H3/06 ,  C07K1/023 ,  C07K1/04 ,  Y02P20/542

    摘要： The present invention relates to ionic liquids for use in chemical applications and capable of serving the dual function of solvent and liquid support. The ionic liquid lends itself to a method of synthesizing oligomers selected from the group consisting of oligopeptides, oligosaccharides and oligonucleotides, comprising contacting a first monomer unit with an ionic liquid at reaction conditions to provide an ionic liquid bound monomer unit; and contacting the ionic liquid bound monomer unit with at least one further monomer unit at reaction conditions to provide an ionic liquid bound oligomer comprising from 2 to 30 monomer units. The method lends itself to large scale manufacture of oligopeptides, oligosaccharides and oligonucleotides.

    摘要翻译： 本发明涉及用于化学应用并能够起到溶剂和液体载体的双重作用的离子液体。 离子液体本身适用于合成选自寡肽，寡糖和寡核苷酸的低聚物的方法，包括在反应条件下使第一单体单元与离子液体接触以提供离子液体结合的单体单元; 以及在反应条件下使离子液体结合的单体单元与至少一个其它单体单元接触，以提供包含2至30个单体单元的离子液体结合的低聚物。 该方法适合大规模生产寡肽，寡糖和寡核苷酸。

    Flavonoid dimers and methods of making and using such
    5.
    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
    7.
    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。

    IMIDAZOLIUM-TYPE IONIC OLIGOMERS
    10.
    发明申请
    IMIDAZOLIUM-TYPE IONIC OLIGOMERS 有权
    咪唑型离子低聚物

    公开(公告)号：US20100093975A1

    公开(公告)日：2010-04-15

    申请号：US12530890

    申请日：2008-03-12

    申请人： Tak-Hang Chan ,  Xun He

    发明人： Tak-Hang Chan ,  Xun He

    IPC分类号： C07K7/06 ,  C07D403/14

    CPC分类号： C07D233/61 ,  C07K1/042 ,  C08G73/0616

    摘要： The present disclosure relates to structurally defined imidazolium-type ionic oligomers of the formula: wherein n is an integer ranging from 1 to 20; A is N or m is an integer ranging from 1 to 5; X is selected from the group consisting of Br, OTf, CF3CO2, CH3CO2, BF4, PF6, NTf2, F, Cl and I; and R is selected from the group consisting of hydrogen and C1-10 alkyl. The imidazolium-type ionic oligomers lend themselves as soluble/solid supports for biopolymer synthesis.

    摘要翻译： 本公开涉及结构上定义的下式的咪唑鎓型离子低聚物：其中n是1至20的整数; A为N或m为1至5的整数; X选自Br，OTf，CF 3 CO 2，CH 3 CO 2，BF 4，PF 6，NTf 2，F，Cl和I; 并且R选自氢和C 1-10烷基。 咪唑型离子低聚物本身可用作生物聚合物合成的可溶/固体支持体。