发明名称 |
PIPERAZINE, PIPERIDINE AND TETRAHYDROPYRIDINE DERIVATIVES AS 5-HT RECEPTOR AGONISTS |
摘要 |
A class of N-substituted piperazine, piperidine and tetrahydropyridine derivatives, further substituted at the 4-position by an optionally substituted alkenyl, alkynyl, aryl-alkyl or heteroaryl-alkyl moiety, are selective agonists of 5-HT1-like receptors, being potent agonists of the human 5-HT1D alpha receptor subtype whilst possessing at least a 10-fold selective affinity for the 5-HT1D alpha receptor subtype relative to the 5-HT1D 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-HT1D receptors is indicated, whilst eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT1D receptor agonists.
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申请公布号 |
WO9745432(A1) |
申请公布日期 |
1997.12.04 |
申请号 |
WO1997GB01329 |
申请日期 |
1997.05.15 |
申请人 |
MERCK SHARP & DOHME LIMITED;BOURRAIN, SYLVIE;MACLEOD, ANGUS, MURRAY;SHOWELL, GRAHAM, ANDREW;STREET, LESLIE, JOSEPH |
发明人 |
BOURRAIN, SYLVIE;MACLEOD, ANGUS, MURRAY;SHOWELL, GRAHAM, ANDREW;STREET, LESLIE, JOSEPH |
分类号 |
C07D405/04;C07D405/14;(IPC1-7):C07D521/00;A61K31/41 |
主分类号 |
C07D405/04 |
代理机构 |
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