发明名称 Piperazine, piperidine and tetrahydropyridine derivatives
摘要 PCT No. PCT/GB96/02762 Sec. 371 Date May 12, 1998 Sec. 102(e) Date May 12, 1998 PCT Filed Nov. 13, 1996 PCT Pub. No. WO97/18203 PCT Pub. Date May 22, 1997A class of N-substituted piperazine, piperidine and tetrahydropyridine derivatives, linked by a fluoro-substituted alkylene chain to a fused bicyclic heteroaromatic moiety such as indolyl, and 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 recptor agonists.
申请公布号 US5977116(A) 申请公布日期 1999.11.02
申请号 US19980068680 申请日期 1998.05.12
申请人 MERCK SHARP & DOHME LTD. 发明人 CASTRO PINEIRO, JOSE LUIS;MACLEOD, ANGUS MURRAY;ROWLEY, MICHAEL;VAN NIEL, MONIQUE BODIL
分类号 C07D521/00;(IPC1-7):A01N43/60;C07D401/00;C07D403/00;C07D413/00 主分类号 C07D521/00
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