Indole iminooxy derivatives which inhibit leukotriene biosynthes

Details Indole iminooxy derivatives which inhibit leukotriene biosynthes Indole iminooxy derivatives which inhibit leukotriene biosynthes

1994-01-24

1995-03-21

Springer, David B.

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

546273, 548159, C07D40102, C07D41702, A61K 31425, A61K 3147

Patent

active

053996992

ABSTRACT:
Compounds of the structure ##STR1## where A.sub.1 is alkylene or cycloalkylene; A.sub.2 is a valence bond, alkylene, or cycloalkylene; R.sub.1 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; R.sup.2 is selected from optionally substituted phenylalkyl and optionally substituted heteroarylakyl; R.sup.3 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; R.sup.4 is selected from hydrogen and optionally substituted alkyl; and Z is selected from --COOB, --C(OB)R.sup.6 R.sup.6, --COOalkyl, --COOalkylaryl, --CONR.sup.5 R.sup.6, and --COR.sup.6 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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