| 摘要 |
PCT No. PCT/GB96/02624 Sec. 371 Date Apr. 17, 1998 Sec. 102(e) Date Apr. 17, 1998 PCT Filed Oct. 28, 1996 PCT Pub. No. WO97/16446 PCT Pub. Date May 9, 1997A 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-HT1-like receptors, being potent agonists of the human 5-HT1D alpha receptor subtype while 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, while eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT1D receptor agonists.
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