Indole iminooxy derivatives which inhibit leukotriene biosynthesis
First Claim
1. A compound having the formula ##STR10## or a pharmaceutically acceptable salt thereof wherein A1 is alkenylene of one to twelve carbon atoms;
- R1 is alkylthio of one to six carbon atoms;
R2 is selected from the group consisting ofphenylakyl in which the alkyl portion is of one to six carbon atoms, andthe phenyl group is optionally substituted with up to three substituents selected from the group consisting ofalkyl of one to six carbon atoms,halogen,haloalkyl of one to six carbon atoms, and alkoxy of one to twelve carbon atoms;
R3 is selected from the group consisting of optionally substituted heteroaryl,wherein the heteroaryl group is selected from the group consisting ofpyridyl,quinolyl,thiazolyl,benzothiazolyl,wherein the optional substituents on the heteroaryl groups are selected from the group consisting ofalkyl of one to six carbon atoms,halogen,alkoxy of one to six carbon atoms, andhaloalkyl of one to six carbon atoms; and
R4 is selected from the group consisting ofhydrogen, andalkyl of one to six carbons optionally substituted with hydroxy.
1 Assignment
0 Petitions
Accused Products
Abstract
Compounds of the structure ##STR1## where A1 is alkylene or cycloalkylene; A2 is a valence bond, alkylene, or cycloalkylene; R1 is selected from hydrogen, alkylthio, optionally substituted phenylthio, optionally substituted phenylalkylthio, optionally substituted 2-, 3- and 4-pyridylthio, optionally substituted 2- and 3-thienylthio, and optionally substituted 2-thiazolylthio; R2 is selected from optionally substituted phenylalkyl and optionally substituted heteroarylakyl; R3 is selected from alkyl, alkoxy, optionally substituted phenyl, optionally substituted phenoxy, optionally substituted phenylalkyl, optionally substituted phenylalkoxy, optionally substituted naphthyl,optionally substituted naphthyloxy, optionally substituted naphthylalkyl, optionally substituted naphthylalkoxy, optionally substituted heteroaryl, optionally substituted heteroaryloxy, optionally substituted heteroarylalkyl, and optionally substituted heteroarylalkoxy; R4 is selected from hydrogen and optionally substituted alkyl; and Z is selected from --COOB, --C(OB)R6 R6, --COOalkyl, --COOalkylaryl, --CONR5 R6, and --COR6 are potent inhibitors of lipoxygenase enzymes and thus inhibit the biosynthesis of leukotrienes. These compounds are useful in the treatment of amelioration of allergic and inflammatory disease states.
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Citations
4 Claims
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1. A compound having the formula ##STR10## or a pharmaceutically acceptable salt thereof wherein A1 is alkenylene of one to twelve carbon atoms;
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R1 is alkylthio of one to six carbon atoms; R2 is selected from the group consisting of phenylakyl in which the alkyl portion is of one to six carbon atoms, and the phenyl group is optionally substituted with up to three substituents selected from the group consisting of alkyl of one to six carbon atoms, halogen, haloalkyl of one to six carbon atoms, and alkoxy of one to twelve carbon atoms; R3 is selected from the group consisting of optionally substituted heteroaryl, wherein the heteroaryl group is selected from the group consisting of pyridyl, quinolyl, thiazolyl, benzothiazolyl, wherein the optional substituents on the heteroaryl groups are selected from the group consisting of alkyl of one to six carbon atoms, halogen, alkoxy of one to six carbon atoms, and haloalkyl of one to six carbon atoms; and R4 is selected from the group consisting of hydrogen, and alkyl of one to six carbons optionally substituted with hydroxy. - View Dependent Claims (2, 3, 4)
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Specification