Patent · US Expired

Azetidine, pyrrolidine and piperidine derivatives

US5998440A · kind A · utility

8Cited by
2References
11Claims
0Family size

Assignee

Inventors

Key dates

Filing dateMay 8, 1998
Grant dateDec 7, 1999
Priority date
Expiry dateMay 8, 2018

Classification

  • Technology area (CPC C)Chemistry; Metallurgy
  • CPC primaryC07D249/08
  • WIPO fieldOrganic fine chemistry
  • WIPO sectorChemistry

Abstract

A class of substituted azetidine, pyrrolidine and piperidine derivatives, linked by a fluoro-substituted alkylene chain to a fused bicyclic heteroaromatic moiety such as indolyl, are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.alpha. receptor subtype while 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, while eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT.sub.1D receptor agonists.

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.