2-substituted-1-naphthols as 5-lipoxygenase inhibitors
AssigneeThe Du Pont Merck Pharmaceutical Company
InventorDouglas G. Batt
Life of this patent
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Abstract
2-Substituted-1-naphthols are 5-lipoxygenase inhibitors which make them useful in the treatment of inflammation, obstructive lung diseases and/or psoriasis. Useful 2-substituent groups are alkyls, alkenyls, alkynyls, cycloalkyls, cycloalkenyls, the groups CH.sub.2 --C.tbd.C--(CH.sub.2).sub.m R.sup.5 and CH.dbd.CH--(CH.sub.2).sub.n R.sup.5 (where m is 1-4, n is 0-3 and R.sup.5 includes phenyl, COOR.sup.9, where R.sup.9 is H or alkyl of 1-4 carbons, AR.sup.6 (where A is a methylene chain and R.sup.6 is a variety of groups including Cl, Br, I, CHO, CN, COOR.sup.9, NH.sub.2, SC(NH)NH.sub.2, phenyl, P(O)(OR.sup.9).sub.2, etc.), and CHR.sup.7 R.sup.21 (where R.sup.7 is a variety of aromatic and heterocyclic groups and R.sup.21 is H, optionally substituted phenyl and a variety of heterocyclic groups).
Claims15
A compound having the formula:
- ##STR45## wherein R.sup.2 and R.sup.3 independently are H, CH.sub.3, C.sub.2 H.sub.5, CH.sub.3 O, or C.sub.2 H.sub.5 O;
- ##STR46## where X is S, O, or NR.sup.10, and Y is CH or N;
- R.sup.9 and R.sup.10 independently are H or C.sub.9, --C.sub.4 alkyl;
- and R.sup.21 is H, lower alkyl, or phenyl, optionally monosubstituted with Cl, Br, F, CH.sub.3 or CH.sub.3 O.
Dependencies are inferred from the claim text.