摘要 |
A class of substituted piperidine and tetrahydropyridine derivatives, linked through the 4-position thereof via an alkylene chain to a fused bicyclic heteroaromatic moiety such as indolyl, and further substituted at the 1position by an optionally substituted alkyl, alkenyl, alkynyl, cycloalkylalkyl, 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 processing at least a 10-fold selective affinity for the 5HT1D.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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申请人 |
MERCK SHARP & DOHME LIMITED |
发明人 |
CHAMBERS, MARK STUART;HOBBS, SARAH CHRISTINE;LADDUWAHETTY, TAMARA;MERCHANT, KEVIN JOHN;MACLEOD, ANGUS MURRAY |