申请人:Hashimoto Masaya
公开号:US20070078153A1
公开(公告)日:2007-04-05
The invention relates to 4-oxoimidazolidine-2-spiropiperidine derivatives represented by a general formula [I]
[in which A
1
, A
2
, A
3
, A
4
and A
5
stand for optionally halogen-substituted methine, or nitrogen atom; R
1
and R
2
stand for lower alkyl or the like; R
3
stands for hydrogen or lower alkyl; R
4
and R
5
stand for hydrogen, or lower alkyl which is optionally substituted with hydroxy, or the like]or salts thereof These compounds act as nociceptin receptor agonist, and are useful as analgesic, reliever from tolerance to narcotic analgesic, reliever from dependence on narcotic analgesic, analgesic enhancer, antiobestic, drug for ameliorating brain function, remedy for schizophrenia, drug for treating regressive neurodegenerative diseases, antianxiety agent or antidepressant and remedy for diabetes insipidus and polyuria; and the like.
本发明涉及一种由通式[I]表示的4-氧代咪唑啉-2-螺环吡啶衍生物[其中A1、A2、A3、A4和A5代表可选的卤代亚甲基或氮原子;R1和R2代表较低的烷基或类似物;R3代表氢或较低的烷基;R4和R5代表氢或较低的烷基,该烷基可选地被羟基等取代]或其盐。这些化合物作为伤害感受器激动剂,可用作镇痛剂、缓解对麻醉镇痛剂的耐受性、缓解对麻醉镇痛剂的依赖、镇痛增强剂、抗肥胖剂、改善脑功能的药物、治疗精神分裂症的药物、治疗退行性神经病的药物、抗焦虑剂或抗抑郁剂和治疗尿崩症和多尿症的药物等。