2-PHENYLMORPHOLIN-5-ONE DERIVATIVES AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
申请人:Nikken Chemicals Company, Limited
公开号:EP0924204A1
公开(公告)日:1999-06-23
A 2-phenylmorpholin-5-one derivative having the formula (I):
wherein R1 represents a C1 to C8 alkyl group, a C3 to C7 cycloalkyl group or an indanyl group, R2 represents a C1 to C4 alkyl group, R3 represents a hydrogen atom, a C1 to C5 alkyl group, etc., R4 represents a hydrogen atom, a C1 to C6 alkyl group, etc., R5, R6 represent a hydrogen atom, a C1 to C5 alkyl group, etc.,
an optical isomer thereof or a pharmacologically acceptable salt thereof, or a hydrate or solvate thereof and a pharmaceutical composition containing the same.
The above compound has a strong type IV phosphodiesterase (PDE) inhibitory activity and has bronchodilater and antiinflammatory effects.
具有式(I)的2-苯基吗啉-5-酮衍生物:
其中 R1 代表 C1 至 C8 烷基、C3 至 C7 环烷基或茚基,R2 代表 C1 至 C4 烷基,R3 代表氢原子、C1 至 C5 烷基等,R4 代表氢原子、C1 至 C6 烷基等,R5、R6 代表氢原子、C1 至 C5 烷基等、
其光学异构体或其药理学上可接受的盐,或其水合物或溶液,以及含有上述物质的药物组合物。
上述化合物具有很强的 IV 型磷酸二酯酶(PDE)抑制活性,并具有支气管扩张和抗炎作用。