Patent · US Expired

Substituted 1-indolylpropyl-4-benzyl-tetrahydropyridine derivatives

US5994374A · kind A · utility

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1References
14Claims
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Assignee

Inventors

Key dates

Filing dateMay 8, 1998
Grant dateNov 30, 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 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-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 5HT.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.alpha. receptors is indicated, and are expected to have fewer undesirable cardiovascular and other side effects.

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