发明名称 Substituted 1-indolylpropyl-4-benzylpiperazine derivatives
摘要 PCT No. PCT/GB96/02682 Sec. 371 Date Apr. 28, 1998 Sec. 102(e) Date Apr. 28, 1998 PCT Filed Nov. 4, 1996 PCT Pub. No. WO97/17338 PCT Pub. Date May 15, 1997A class of 1-[3-(1H-indol-3-yl)propyl]-4-benzylpiperazine derivatives of formula I, substituted at the 5-position of the indole nucleus by a 1,2,4-triazol-4-yl moiety, and on the methylene linkage of the benzyl moiety by a range of substituted alkyl groups, 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.
申请公布号 AU7322896(A) 申请公布日期 1997.05.29
申请号 AU19960073228 申请日期 1996.11.04
申请人 MERCK SHARP & DOHME LIMITED 发明人 MARK STUART CHAMBERS;SARAH CHRISTINE HOBBS;LESLIE JOSEPH STREET
分类号 C07D521/00 主分类号 C07D521/00
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