AMINO ALCOHOL DERIVATIVE OR PHOSPHONIC ACID DERIVATIVE AND MEDICINAL COMPOSITION CONTAINING THESE
申请人:Sankyo Company, Limited
公开号:EP1471054A1
公开(公告)日:2004-10-27
The present invention relates to amino alcohol derivatives or phosphonic acid derivatives having excellent immunosuppressive activity, pharmacologically acceptable salts thereof or pharmacologically acceptable esters thereof, and to pharmaceutical compositions comprising said compounds as an active ingredient:
[wherein,
R1 and R2 each represent a hydrogen atom, or a protecting group of the amino group;
R3 represents a hydrogen atom, or a protecting group of the hydroxyl group;
R4 represents a lower alkyl group;
n represents an integer of from 1 to 6;
X represents an oxygen atom or a nitrogen atom unsubstituted or substituted with a lower alkyl group or the like;
Y represents an ethylene group;
Z represents a C1-C10 alkylene group;
R5 represents an aryl group, or an aryl group substituted with substituents;
R6 and R7 each represents a hydrogen atom; provided that when R5 represents a hydrogen atom, then Z represents a group other than 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氨基醇衍生物或膦酸衍生物、其药理学上可接受的盐或其药理学上可接受的酯,以及包含上述化合物作为活性成分的药物组合物:
其中
R1 和 R2 分别代表氢原子或氨基的保护基团;
R3 代表氢原子或羟基的保护基团;
R4 代表低级烷基;
n 代表 1 至 6 的整数;
X 代表氧原子或氮原子,未被低级烷基或类似基团取代或取代;
Y 代表乙烯基
Z 代表 C1-C10 烯基;
R5 代表芳基或被取代基取代的芳基;
R6 和 R7 各代表一个氢原子;但当 R5 代表氢原子时,Z 代表除单键或直链 C1-C10 亚烷基以外的基团]。