TRIPTOLIDE DERIVATIVES AND THEIR USE
    9.
    发明申请
    TRIPTOLIDE DERIVATIVES AND THEIR USE 审中-公开
    三嵌段衍生物及其用途

    公开(公告)号:WO2004058770A8

    公开(公告)日:2005-07-14

    申请号:PCT/CN0300095

    申请日:2003-01-28

    CPC classification number: C07D493/22 A61K31/34

    Abstract: Triptolide derivatives of Formula (I), their pharmaceutically receptable salts and optical isomers, Formula (I), (wherein, C5 and C6 connect with each other by a C-C single bond or double bond; when C5 and C6 are connected with C-C single bond, X and Y represents independently hydrogen, oxygen, hydroxy, halogen, lower alkyloxy, lower alkylamino, mercapto, lower alkylthio, the group of formula -OCOR, -OSO2OR or -OPO(OH)2, each of which is attached to C5 and C6, R represents -(CH2)nCO2Na, -(CO2)nCO2K, or -(CH2)nCH3, wherein n = 1-6; Z represents hydrogen, oxygen, hydroxy, halogen, lower alkyloxy, lower alkylamino, mercapto, lower alkylthio, the group of formula -OCOR, -OSO2OR or -OPO(OH)2, each of which is linked at C14-position, R represents -(CH2)nCO2Na, -(CO2)nCO2K, or -(CH2)nCH3, wherein n = 1-6; wherein, the "__" linked with X, Y, and Z represents "(a) " or "(b)" , provided that X and Y cannot both be hydrogen atom at the same time), the methods for preparing them and their use as antiphlogistic agent, immunosuppressive agent or therapeutic agent for other related diseases.

    Abstract translation: 式(I)的雷公藤内酯衍生物,其药学上可接受的盐和旋光异构体式(I)(其中C5和C6通过CC单键或双键相互连接;当C5和C6与CC单键连接时) ,X和Y独立地表示氢,氧,羟基,卤素,低级烷氧基,低级烷基氨基,巯基,低级烷硫基,式-OCOR,-OSOOROR或-OPO(OH)2基团, C6,R表示 - (CH2)nCO2Na, - (CO2)nCO2K或 - (CH2)nCH3,其中n = 1-6; Z表示氢,氧,羟基,卤素,低级烷氧基,低级烷基氨基,巯基,低级烷硫基 ,式为-OCOR,-OSO 2 OR或-OPO(OH)2,其各自在C14位连接,R表示 - (CH 2)n CO 2 Na, - (CO 2)n CO 2 K或 - (CH 2)n CH 3,其中 n = 1-6;其中,与X,Y和Z连接的“_”表示“(a)”或“(b)”,条件是X和Y不能同时为氢原子) 制备它们的方法及其用途 神经毒素,免疫抑制剂或其他相关疾病的治疗剂。

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