4-(oxygen, sulfur or nitrogen substituted)-methyl 5-hydroxy-2(5H

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Phosphorus containing other than solely as part of an...

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514313, 514318, 549214, 549222, 549213, 549318, A61K 31665, A61K 3147, C07D30512, C07D 906

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active

050378112

ABSTRACT:
Compounds of the formula ##STR1## in which R.sub.1 is H or alkyl of 1 to 20 carbons, CO--R.sub.1.sup.* CO--O--R.sub.1.sup.* CO--NH--R.sub.1.sup.* or PO(OR.sub.1.sup.*).sub.2 or PO(OR.sub.1.sup.*)R.sub.1.sup.* where R.sub.1.sup.* independently is H, alkyl of 1 to 20 carbons, phenyl, or substituted phenyl; X is O, S, SO--, SO.sub.2, NH--, or NR.sub.2 where R.sub.2 is phenyl, substituted phenyl or alkyl of 1 to 20 carbons, and Y is alkyl having at least 6 carbon atoms, arylalkyl, aryl, substituted aryl, substituted arylalkyl, alkenyl containing one or more olephinic bonds and at least 6 carbon atoms, CO--R.sub.3, CO--OR.sub.3, CONHR.sub.3, SO.sub.2 R.sub.3, SO.sub.2 NHR.sub.3 where R.sub.3 is aryl, substituted aryl, substituted arylalkyl, alkyl, alkenyl containing one or more olephinic bonds, further Y is (CH.sub.2).sub.n --O--R.sub.4, or (CH.sub.2).sub.n --O--(CH.sub.2).sub.m --O--R.sub.4, where n, and m, are integers and are independently 1 to 25 and R.sub.4 is phenyl, substituted phenyl or alkyl of one to 20 carbons, still further Y is PO(OH).sub.2, PO(OH)OR.sub.5, PO(OH)R.sub.5 PO(OR.sub.5).sub.2, where R.sub.5 is independently phenyl, substituted phenyl, alkyl or 1 to 20 carbons or R.sub.5 is (CH.sub.2).sub.n --N(R.sub.5.sup.*).sub.3 where R.sub.5.sup.* is alkyl of 1 to 20 carbons, or Y is NH--R.sub.6 where R.sub.6 is phenyl, substituted phenyl or alkyl of at least 6 carbon atoms with the proviso that when X is O, S, then Y is not NH--R.sub.6, and with the further proviso that when X is SO or SO.sub.2 then Y is not SO.sub.2 R.sub.3 or SO.sub.2 NHR.sub.3, are disclosed. The compounds possess anti-inflammatory activity.

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