申请人:Japan Tobacco Inc.
公开号:US20030055087A1
公开(公告)日:2003-03-20
The present invention relates to a compound of the formula [1′]
1
wherein R
2
is lower alkyl optionally substituted by hydroxy, amino and the like, ring B is phenyl, thienyl and the like, E is a single bond, —O—, —S— and the like, ring G is aryl, heterocyclic group and the like, R
5
is halogen atom, hydroxy, lower alkyl optionally substituted by halogen atom etc., and the like, t is 0 or an integer of 1 to 5, when t is an integer of 2 to 5, each R
5
may be the same or different, m is 0 or an integer of 1 to 8, and n is 0 or an integer of 1 to 4, and a nociceptin antagonist containing compound [1′] as an active ingredient. The compound [1′] shows, due to nociceptin antagonistic action, analgesic effect against sharp pain such as postoperative pain and the like. The present invention also relates to the use of certain amide derivative inclusive of compound [1′] as a nociceptin antagonist or analgesic.
本发明涉及一种化合物,其化学式为[1′]1,其中R2是低碳基,可选择性地被羟基、氨基等取代,环B是苯基、噻吩基等,E是单键,-O-,-S-等,环G是芳基、杂环基等,R5是卤素原子、羟基、低碳基,可选择性地被卤素原子等取代,t为0或1至5的整数,当t为2至5的整数时,每个R5可能相同也可能不同,m为0或1至8的整数,n为0或1至4的整数,以及一种含有化合物[1′]作为活性成分的镇痛剂。由于其镇痛剂作用,化合物[1′]对于术后疼痛等尖锐疼痛具有镇痛效果。本发明还涉及某些酰胺衍生物的使用,其中包括化合物[1′]作为镇痛剂或镇痛剂拮抗剂。