发明授权
US5919783A Indoline and azaindoline derivatives as 5-HT.sub.1D alpha receptor
agonists
失效
二氢吲哚和唑啉衍生物作为5-HT1Dα受体激动剂
- 专利标题: Indoline and azaindoline derivatives as 5-HT.sub.1D alpha receptor agonists
- 专利标题(中): 二氢吲哚和唑啉衍生物作为5-HT1Dα受体激动剂
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申请号: US776626申请日: 1997-01-21
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公开(公告)号: US5919783A公开(公告)日: 1999-07-06
- 发明人: Mark Stuart Chambers , Victor Giulio Matassa , Leslie Joseph Street
- 申请人: Mark Stuart Chambers , Victor Giulio Matassa , Leslie Joseph Street
- 申请人地址: GBX Hoddesdon
- 专利权人: Merck Sharp & Dohme Ltd.
- 当前专利权人: Merck Sharp & Dohme Ltd.
- 当前专利权人地址: GBX Hoddesdon
- 优先权: GBX9415575 19940802
- 主分类号: C07D521/00
- IPC分类号: C07D521/00 ; A61K31/495 ; C07D403/14 ; C07D471/04
摘要:
Compounds 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; R.sup.1 represents aryl(C.sub.1-6)alkyl or heteroaryl(C.sub.1-6)alkyl, either of which groups may be optionally substituted; and R.sup.2 represents hydrogen or C.sub.1-6 alkyl are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.alpha. receptor subtype whilst possessing at least a 10-fold selective affinity for the 5-HT.sub.1D.alpha. receptor subtype relative to the 5-HT.sub.1D.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-HT.sub.1D receptors is indicated, whilst eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT.sub.1D receptor agonists. ##STR1##
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