申请人:KOWA CO., LTD.
公开号:US20040002497A1
公开(公告)日:2004-01-01
Compounds having the formula (1):
1
wherein R
1
represents an alkyl or alkenyl group, R
2
and R
3
each independently represents a hydrogen atom or an alkyl, hydroxyalkyl, dihydroxyalkyl or alkynyl group, or R
2
and R
3
may be fused together with the adjacent nitrogen atom to form a substituted or unsubstituted, nitrogen-containing, saturated heterocyclic group, X, Y and Z each independently represents a hydrogen atom, an alkyl group, a halogen atom or the like, and n stands for an integer of from 1 to 5; and also to pharmaceutical compositions containing them. These compounds have inhibitory activity against IL-1&bgr; production, high water solubility and good oral absorbability.
化合物的分子式为(1):1,其中R1代表一个烷基或烯基基团,R2和R3分别独立地表示氢原子或烷基,羟基烷基,二羟基烷基或炔基基团,或者R2和R3可以与相邻的氮原子融合形成取代或未取代的含氮饱和杂环基团,X、Y和Z分别独立地表示氢原子,烷基,卤原子或类似物,n代表1到5之间的整数; 这些化合物具有抑制IL-1β产生的活性,高水溶性和良好的口服吸收性,还包括含有它们的制药组合物。