申请人:Sankyo Company, Limited
公开号:EP1300405A1
公开(公告)日:2003-04-09
The present invention relates to compounds of formula (I) which exhibit excellent immune suppression activity, pharmacologically acceptable salts thereof, esters thereof or other derivatives:
wherein R1 and R2 are a hydrogen atom, an amino protecting group; R3 is a hydrogen atom, a hydroxy protecting group; R4 is a lower alkyl group; n is an integer from 1 to 6; X is an ethylene group; Y is a C1-C10 alkylene group, a C1-C10 alkylene group substituted with 1 to 3 substituents selected from substituent group a and b; R5 is an aryl group; R6 and R7 are a hydrogen atom, a group selected from substituent group a; with the proviso when R5 is a hydrogen atom, Y is not a single bond or a straight chain C1-C10 alkylene group.
本发明涉及具有优异免疫抑制活性的式(I)化合物、其药理学上可接受的盐、酯或其它衍生物:
其中,R1 和 R2 是氢原子、氨基保护基;R3 是氢原子、羟基保护基;R4 是低级烷基;n 是 1 至 6 的整数;X 是乙烯基;Y 是 C1-C10 亚烷基、被 1 至 3 个选自取代基 a 和 b 的取代基取代的 C1-C10 亚烷基;R5是芳基;R6和R7是氢原子、选自取代基a的基团;但当R5是氢原子时,Y不是单键或直链C1-C10亚烷基。