10-substituted 1,8-dihydroxy-9 (10H) anthracenone pharmaceuticals
AssigneeTeva Pharmaceutical Industries Ltd.
InventorsKlaus Muller, Wolfgang Wiegrebe, Dieter Gurster, Susanne Peters, nee Piwek
Life of this patent
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Abstract
Therapeutic compositions comprising 1,8-dihyroxy-9(10H) anthracenones substituted at position 10 thereof with phenylalkylidene or arylacyl blocking moieties, said compounds having substantial therapeutic activity and minimal inflammatory effect.
Claims13
A compound according to formula II, ##STR7## said compound containing one or more substituents (R);
- wherein (R) is one or more groups selected from the group consisting of hydrogen, methyl, trifluoromethyl, nitro, cyano, methoxy, carboxyl, methoxycarbonyl, hydroxy, bromo, iodo, fluoro, amino, substituted amino, mercapto, substituted mercapto, aryloxy and arylmethoxy;
- and wherein (n) is an integer of from 0 to 4.
A pharmaceutical composition comprising:
- (a) a pharmaceutically acceptable carrier;
- and
- (b) a therapeutically effective amount of a 10-substituted 1,8-dihydroxy-9(10H) anthracenone compound which inhibits lipoxygenase activity, wherein the substituent at the 10 position is a phenylalkylidene C-10 blocking moiety stable to metabolic degradation, and wherein the activity of the compound inhibiting lipoxygenase is not made ineffective by an inflammatory effect caused by said compound.
A 9-anthracenone compound which is capable of inhibiting lipoxygenase activity in a patient when provided in the form of a therapeutic composition, said inhibitory activity thereof not being made ineffective by an inflammatory effect caused by said compound, characterized by having an arylacyl C- 10 blocking moiety and a 5-LO inhibition, expressed in terms of IC.sub.50 .mu.M, of less than 11 or characterized by having a phenylalkylidene C-10 blocking moiety and a 5-LO inhibition, expressed in terms of IC.sub.50 .mu.M, of less than 6, wherein said IC.sub.50 .mu.M represents the inhibition of 5-hydroxyeicosatetraenoic acid and leukotriene B.sub.4 biosynthesis in bovine PMNL.
Dependencies are inferred from the claim text.