Patent · US Expired

Phenylmethyl derivatives having lipoxygenase inhibitory activity

US5354865A · kind A · utility

12Cited by
6References
7Claims
0Family size

Assignee

Inventors

Key dates

Filing dateSep 10, 1992
Grant dateOct 11, 1994
Priority date
Expiry dateSep 10, 2012

Classification

  • Technology area (CPC C)Chemistry; Metallurgy
  • CPC primaryC07D309/10
  • WIPO fieldOrganic fine chemistry
  • WIPO sectorChemistry

Abstract

Compounds of the structure ##STR1## where Ar is optionally substituted carbocyclic aryl, 5- or 6-membered heterocyclic aryl, 10-membered bicyclic heterocyclic aryl containing one or two nitrogen atoms, 9- or 10-membered heterocyclic containing one or two nitrogen atoms and optionally containing a further nitrogen or oxygen atom and one oxo or thioxo substituent, benzo[b]furyl, benzo[b]thienyl, A.sub.1 is propynylene, methylene, or a valence bond, X is O, S, SO.sub.2, or NR.sub.2, Y is selected from alkyl, haloalkyl, alkoxy, halogen, and hydrogen, A.sub.2 is selected from ##STR2## and methylene where Z is OR.sub.5 or NHR.sub.5 where R.sub.5 is hydrogen or alkyl, R.sub.1 is hydrogen, alkyl, or OR.sub.5, and m and n are integers having a value of 1 or 2 are potent inhibitors of lipoxygenase enzymes and thus inhibit the biosynthesis of leukotrienes. These compounds are useful in the treatment or amelioration of allergic and inflammatory disease states.

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