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    • 57. 发明授权
    • Triptolide derivatives and their uses
    • 雷公藤内酯衍生物及其用途
    • US07626044B2
    • 2009-12-01
    • US10540908
    • 2003-01-28
    • Yuanchao LiJianping ZuoFan ZhangRu ZhouJian Ding
    • Yuanchao LiJianping ZuoFan ZhangRu ZhouJian Ding
    • C07D307/77C07F9/06
    • C07D493/22A61K31/34
    • Triptolide derivatives of Formula (I), their pharmaceutically acceptable salts and optical isomers, Formula (I): wherein, C5 and C6 are 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 represent independently hydrogen, oxygen, hydroxyl, halogen, lower alkyl-oxy, lower alkyl-amino, mercapto, lower alkyl-thio, 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, hydroxyl, halogen, lower alkyl-oxy, lower alkyl-amino, mercapto, lower alkyl-thio, 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)nCH2, wherein n=1-6; wherein, the“______” linked with X, Y, and Z represents the stereochemistry orientations “” or “” , but X and Y cannot both be hydrogen atom at the same time, methods for preparing the triptolides and their use as antiphiogistic agent, immunosuppressive agent or therapeutic agent for other related diseases.
    • 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C-C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,低级烷基氧基,低级烷基 - 氨基,巯基,低级烷基 - 硫基,式-OCOR,-OSO2OR 或-OPO(OH)2,其各自连接到C5和C6,R表示 - (CH2)nCO2Na, - (CO2)nCO2K或 - (CH2)nCH3,其中n = 1-6; Z代表氢,氧,羟基,卤素,低级烷基 - 氧基,低级烷基 - 氨基,巯基,低级烷基 - 硫基,式-OCOR,-OSO2OR或-OPO(OH)2基团, C14-位,R表示 - (CH2)nCO2Na, - (CO2)nCO2K或 - (CH2)nCH2,其中n = 1-6; 其中,与X,Y和Z相连的“______”表示立体化学取向“”或“”,但X和Y不能同时为氢原子, 制备雷公藤内酯的方法及其作为抗氧化剂,免疫抑制剂或其他相关疾病的治疗剂的用途。