发明申请
- 专利标题: Novel 4-(2-furoyl) aminopiperidines, intermediates in synthesizing the same, process for producing the same and medicinal use of the same
- 专利标题(中): 新型4-(2-糠酰基)氨基哌啶,其合成中间体,其制备方法及其医药用途
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申请号: US10492065申请日: 2002-10-08
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公开(公告)号: US20050085508A1公开(公告)日: 2005-04-21
- 发明人: Ryuuta Fukutomi , Hitoshi Inoue , Koji Kawamura , Takuya Kishimoto , Masashi Suzuki , Rie Shibayama , Kazuko Kojima , Kouichirou Hagihara
- 申请人: Ryuuta Fukutomi , Hitoshi Inoue , Koji Kawamura , Takuya Kishimoto , Masashi Suzuki , Rie Shibayama , Kazuko Kojima , Kouichirou Hagihara
- 国际申请: PCT/JP02/10449 WO 20021008
- 主分类号: A61P1/04
- IPC分类号: A61P1/04 ; A61P1/08 ; A61P1/10 ; A61P17/04 ; A61P43/00 ; C07D211/58 ; C07D401/12 ; C07D405/12 ; C07D405/14 ; C07D413/14 ; A61K31/445
摘要:
There are provided novel 4-(2-furoyl)aminopiperidines represented by the general formula (I), their synthetic intermediates, processes for their preparation and medicaments containing them. In the above formula, X is CH or N, and Y is a group of the following general formula (II), formula (II-a) or formula (III): wherein a, b and c are each an integer of 0-6; Z is CH2 or NH; W is O or S; T is O or N—R15 wherein R15 is H, a C1-C6 alkyl group, a benzyl group or a phenethyl group; and R1 is H, a C1-C6 alkoxycarbonyl group, a benzyloxycarbonyl group, or the like. The 4-(2-furoyl)aminopiperidine derivatives according to this invention possess opioid μ antagonistic activity and are useful for the treatment or prevention of side effects which are caused by μ receptors agonist and which are selected from constipation, nausea/emesis or itch, or for the treatment or prevention of idiopathic constipation, postoperative ileus, paralytic ileus, irritable bowel syndrome or chronic pruritus.
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