申请人:——
公开号:US20030191307A1
公开(公告)日:2003-10-09
Novel compounds according to the formula
1
and pharmaceutically acceptable salts, solvates, or hydrates thereof; wherein
each occurrence of A is independently selected from CH or N;
X is selected from the group consisting of —CH
2
—, —O—, —NH—, (C
1
-C
6
)alkylamino-, (C
1
-C
6
)alkylaminocarbonylamino-, (C
1
-C
6
)alkylcarbonylamino-, (C
1
-C
6
)alkylsulfonylamino-, phenylsulfonylamino-, carbonyl, —NH—C(O)—, —N(C
1
-C
6
)alkyl-C(O)—, —S(O)
y
— where y is 0, 1 or 2, and;
n in —(CH
2
)
n
— is 1, 2 or 3; and
R
1
, R
2
, and R
3
are as described herein; pharmaceutical compositions that including these compounds, and methods for the treatment of autoimmune disease, inflammation, allergy, transplant rejection, and other circumstances where administration of an immunosuppressive agent is of therapeutic benefit.
根据公式1及其药学上可接受的盐、溶剂或水合物,制备了新的化合物;其中A的每次出现独立地选自CH或N;X选自以下群体:—CH2—、—O—、—NH—、(C1-C6)烷基氨基、(C1-C6)烷基氨基甲酰氨基、(C1-C6)烷基羧酰氨基、(C1-C6)烷基磺酰氨基、苯基磺酰氨基、羰基、—NH—C(O)—、—N(C1-C6)烷基-C(O)—、—S(O)y—,其中y为0、1或2,而—(CH2)n—中的n为1、2或3;R1、R2和R3如本文所述;包括这些化合物的药物组合物,以及用于治疗自身免疫性疾病、炎症、过敏、移植排斥以及其他需要免疫抑制剂治疗的情况的方法。