发明授权
US5998415A Bicyclic heteroaryl-alkylene-(homo)piperazinones and thione analogues
thereof, their preparation, and their use of as selective agonists of
5-HT.sub.1 -like receptors
失效
双环杂芳基 - 亚烷基 - (同)哌嗪酮及其硫酮类似物,其制备及其作为5-HT1样受体选择性激动剂的用途
- 专利标题: Bicyclic heteroaryl-alkylene-(homo)piperazinones and thione analogues thereof, their preparation, and their use of as selective agonists of 5-HT.sub.1 -like receptors
- 专利标题(中): 双环杂芳基 - 亚烷基 - (同)哌嗪酮及其硫酮类似物,其制备及其作为5-HT1样受体选择性激动剂的用途
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申请号: US065020申请日: 1998-04-17
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公开(公告)号: US5998415A公开(公告)日: 1999-12-07
- 发明人: Mark Stuart Chambers , Sarah Christine Hobbs , Leslie Joseph Street
- 申请人: Mark Stuart Chambers , Sarah Christine Hobbs , 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: GBX9522473 19951102; GBX9523907 19951122
- 主分类号: C07D403/06
- IPC分类号: C07D403/06 ; C07D521/00 ; A61K31/495 ; C07D403/14
摘要:
A class of piperazinones, homopiperazinones and thione analogues thereof, substituted at the 1-position by an optionally substituted alkenyl, alkynyl, aryl-alkyl or heteroaryl-alkyl moiety, and linked at the 4-position via an alkylene spacer to a fused bicyclic heteroaromatic moiety, typically indolyl, are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.alpha. receptor subtype while 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, while eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT.sub.1D receptor agonists.
公开/授权文献
- USD390837S Multipurpose access control reader 公开/授权日:1998-02-17
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