发明名称 Substituted 1-indolylpropyl-4-benzyl-tetrahydropyridine derivatives
摘要 PCT No. PCT/GB96/02684 Sec. 371 Date May 8, 1998 Sec. 102(e) Date May 8, 1998 PCT Filed Nov. 4, 1996 PCT Pub. No. WO97/17337 PCT Pub. Date May 15, 1997A class of 1-[3-(1H-indol-3-yl)propyl]-4-benzyl-1,2,5,6-tetrahydropyridine derivatives, 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 an alkyl, alkoxy, or alkoxy-alkoxy substituent, 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 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 alpha receptors is indicated, and are expected to have fewer undesirable cardiovascular and other side effects.
申请公布号 AU7322996(A) 申请公布日期 1997.05.29
申请号 AU19960073229 申请日期 1996.11.04
申请人 MERCK SHARP & DOHME LIMITED 发明人 SYLVIE BOURRAIN;ANGUS MURRAY MACLEOD;JOSEPH GEORGE NEDUVELIL;GRAHAM ANDREW SHOWELL
分类号 C07D521/00 主分类号 C07D521/00
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