发明名称 Indoline and azaindoline derivatives as 5-HT1D alpha receptor agonists
摘要 PCT No. PCT/GB95/01756 Sec. 371 Date Jan. 21, 1997 Sec. 102(e) Date Jan. 21, 1997 PCT Filed Jul. 24, 1995 PCT Pub. No. WO96/04269 PCT Pub. Date Feb. 15, 1996Compounds of formula (I), or a salt or prodrug thereof, wherein Z represents an optionally substituted five-membered heteroaromatic ring selected from furan, thiophene, pyrrole, oxazole, thiazole, isoxazole, isothiazole, imidazole, pyrazole, oxadiazole, thiadiazole, triazole, and tetrazole; E represents a chemical bond or a straight or branched alkylene chain containing from 1-4 carbon atoms; Q represents a straight or branched alkylene chain containing from 1-6 carbon atoms; T represents nitrogen or CH; R1 represents aryl(C1-6)alkyl or heteroaryl(C1-6)alkyl, either of which groups may be optionally substituted; and R2 represents hydrogen or C1-6 alkyl 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 US5919783(A) 申请公布日期 1999.07.06
申请号 US19970776626 申请日期 1997.01.21
申请人 MERCK SHARP & DOHME LTD. 发明人 CHAMBERS, MARK STUART;MATASSA, VICTOR GIULIO;STREET, LESLIE JOSEPH
分类号 C07D521/00;(IPC1-7):A61K31/495;C07D403/14;C07D471/04 主分类号 C07D521/00
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