发明授权
US6025374A Azetidine, pyrrolidine and piperidine derivatives as 5HT1 receptor
agonists
失效
氮杂环丁烷,吡咯烷和哌啶衍生物作为5HT1受体激动剂
- 专利标题: Azetidine, pyrrolidine and piperidine derivatives as 5HT1 receptor agonists
- 专利标题(中): 氮杂环丁烷,吡咯烷和哌啶衍生物作为5HT1受体激动剂
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申请号: US849700申请日: 1997-05-28
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公开(公告)号: US6025374A公开(公告)日: 2000-02-15
- 发明人: Jose Luis Castro Pineiro , Caroline Henry , Victor Giulio Matassa , Austin John Reeve , Francine Sternfeld , Leslie Joseph Street
- 申请人: Jose Luis Castro Pineiro , Caroline Henry , Victor Giulio Matassa , Austin John Reeve , Francine Sternfeld , Leslie Joseph Street
- 申请人地址: GBX Hoddesdon
- 专利权人: Merck Sharp & Dohme, Ltd.
- 当前专利权人: Merck Sharp & Dohme, Ltd.
- 当前专利权人地址: GBX Hoddesdon
- 优先权: GBX9424627 19941206; GBX9505871 19950323
- 主分类号: A61K31/40
- IPC分类号: A61K31/40 ; A61K31/42 ; A61K31/445 ; A61P25/04 ; A61P25/06 ; A61P43/00 ; C07D403/06 ; C07D413/14 ; C07D209/02 ; C07D263/58 ; C07D401/00
摘要:
A class of substituted azetidine, pyrrolidine and piperidine derivatives are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.alpha. receptor subtype whilst possessing at least a 10-fold selective affinity for the 5-HT.sub.1D.alpha. receptor subtype relative to the 5-HT.sub.1D.beta. subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT.sub.1D receptors is indicated, whilst eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT.sub.1D receptor agonists.
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