US 5,476,873 A · Acetylene derivatives having lipoxygenase inhibitory activity

Abstract

Compounds of the structure ##STR1## where p and q are zero or one, but cannot both be the same, M is a pharmaceutically acceptable cation or a metabolically cleavable group, B is a valence bond or a straight or branched alkylene group, R is alkyl, cycloalkyl or --NR.sup.1 R.sup.2, where R.sup.1 and R.sup.2 are hydrogen, alkyl, cycloalkyl or alkanoyl, and A is optionally substituted carbocyclic aryl, furyl, benzo[b]furyl, thienyl, or benzo[b]thienyl 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.

Claims7

Dependent claims

A compound having the structure ##STR14## wherein B is a valence bond or is a straight or branched divalent alkylene group of one to twelve carbon atoms,

M represents hydrogen or a pharmaceutically acceptable cation,
R.sup.2 is selected from the group consisting of
hydrogen,
alkyl of from one to six carbon atoms,
hydroxyalkyl of from one to six carbon atoms,
alkoxyalkyl in which the alkoxy portion and the alkyl portion each contain, independently, from one to six carbon atoms,
alkanoyl of from two to eight carbon atoms,
A is optionally substituted phenyl;
wherein the optional substituent on the phenyl group is
phenoxy, optionally substituted with alkyl of from one to six carbon atoms, haloalkyl of from one to six carbon atoms, alkoxy of from one to six carbon atoms, hydroxy or halogen;
and
the pharmaceutically acceptable salts thereof.

9 more elements

Dependencies are inferred from the claim text.

Acetylene derivatives having lipoxygenase inhibitory activity

Life of this patent

Acetylene derivatives having lipoxygenase inhibitory activity

Life of this patent

Abstract

Claims7