申请人:Li Yuanchao
公开号:US20070197476A1
公开(公告)日:2007-08-23
The invention relates to triptolide derivatives of Formula (I), their pharmaceutically acceptable 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, hydroxyl, halogen, lower alkyl-oxy, lower alkyl-amino, mercapto, lower alkyl-thio, the group of formula —OCOR, —OSO
2
R or —OPO(OH)
2
, each of which is attached to C5 and C6, R represents —(CH
2
)nCO
2
Na, —(CO
2
)nCO
2
K, or —(CH
2
)nCH
3
, 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, —OSO
2
R or —OPO(OH)2, each of which is linked at C14-position, R represents —(CH2)nCO2Na, —(CO
2
)nCO
2
K, or —(CH
2
)nCH
2
, wherein n=1-6; wherein, the “_” linked with X, Y, and Z represents “
” or “
”, but 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.
本发明涉及式(I)的三酰甲基衍
生物、其药学上可接受的盐和光学异构体,式(I)如下:
其中,C5和C6通过C—C单键或双键连接;当C5和C6通过C—C单键连接时,X和Y分别表示氢、氧、羟基、卤素、较低的烷氧基、较低的烷基
氨基、巯基、较低的烷
硫基、式—OCOR、—OSO2R或—OPO(OH)2的基团,每个基团都连接在C5和C6上,其中R表示—(
CH2)n Na、—(
CO2)n K或—( )nCH3,其中n为1-6;Z表示氢、氧、羟基、卤素、较低的烷氧基、较低的烷基
氨基、巯基、较低的烷
硫基、式—OCOR、—OSO2R或—OPO(OH)2的基团,每个基团都连接在C14位点,其中R表示—( )n Na、—( )n K或—( )n ,其中n为1-6;其中,与X、Y和Z连接的“_”表示“”或“”,但X和Y不能同时为氢原子,本发明还涉及其制备方法以及作为抗炎剂、
免疫抑制剂或治疗其他相关疾病的治疗剂的用途。