Patent ID: 6274559
Filing Date: 2001-08-14
Classification: A61K,A61P,Y10S

Abstract:
A method of treating or preventing hepatotoxicity, said method comprising administering to a patient in need of such treatment, a therapeutically effective amount of a compound, or a pharmaceutically acceptable salt or ester thereof, represented by Formula 1 ##STR14##wherein:R.sub.1 is chosen from --H, a hydroxy group, a hydroxy group protected by an acetyl or benzoyl group, a methyl group, an ethyl group, a methoxy group, an ethoxy group, a vinyl group, an ethinyl group, a cyano group, an azide group, an ethoxymethyloxy group, an octyloxymethyloxy group, a methanesulfonyloxy group, a phenylthio group and a (methylthio)thiocarbonyloxy group, orR.sub.1 and R.sub.2 taken together may form an oxo group;R.sub.2 is chosen from --H, a methoxy group, an ethoxy group, a hydroxy group and a hydroxy group protected by an acetyl or benzoyl group, orR.sub.2 and R.sub.4 taken together may form an epoxy group;R.sub.3 is chosen from --H, a vinyl group, a methyl group, an ethyl group, a hydroxy group and a hydroxy group protected by an acetyl or benzoyl group orR.sub.3 and R.sub.4 taken together may form an oxo group;R.sub.4 is chosen from --H, a methyl group, an ethyl group, a vinyl group, a hydroxy group and a hydroxy group protected by an acetyl or benzoyl group;R.sub.5 is chosen from a methyl group, a hydroxymethyl group wherein the hydroxy group may be protected by an acetyl or benzoyl group, a t-butyldimethylsilyloxymethyl group, a carboxylic group, a carboxylic ester moiety, a carboxylic amide moiety and an aldehyde group, orR.sub.4 and R.sub.5 taken together may form --OCR.sub.6 R.sub.7 OCH.sub.2 --, whereinR.sub.6 is chosen from --H, a lower alkyl group having 1-4 carbon atoms and a phenyl group;R.sub.7 is chosen from --H, a lower alkyl group having 1-4 carbon atoms and a phenyl group, orR.sub.6 and R.sub.7 taken together may form --(CH.sub.2).sub.5 ;R.sub.8 is chosen from --H and a methyl group;R.sub.9 is chosen from --CH.sub.2 COOR and --COOR, whereinR is chosen from --H, a lower alkyl group having 1-4 carbon atoms, a 2-tetrahydropyranyl group, CH(OR.sub.11)R.sub.10, CH(OR.sub.13)CH.sub.2 R.sub.12, whereinR.sub.10 is chosen from --H, a methyl group and an ethyl group;R.sub.11 is chosen from a lower alkyl group having 1-4 carbon atoms, an octyl group, a benzyl group, a methoxymethyl group and a methoxyethyl group;R.sub.12 is chosen from --H, a methyl group and an ethyl group; andR.sub.13 is chosen from a methyl group and an ethyl group, orR.sub.12 and R.sub.13 taken together may form --CH.sub.2 CH.sub.2 CH.sub.2 --,a glucosyl or a rhamnosyl group, wherein the hydroxy group may be protected by an acetyl or benzoyl group,a hydroxymethyl group wherein the hydroxy group may be protected by an acetyl or a benzoyl group, a methanesulfonyloxymethyl group and a cyanomethyl group; andR.sub.14 and R.sub.15 are independently --H, or R.sub.14 and R,.sub.5 taken together form an oxo group, with the provisos that:when R.sub.1 and R.sub.4 are hydroxy, R.sub.2 and R.sub.3 are --H, R.sub.5 is hydroxymethyl and R.sub.8 is methyl,R is not --H or methyl and R.sub.10 is not --H; andwhen R.sub.1 is --OH, R.sub.2 is --H, R.sub.3 or R.sub.4 form with R.sub.5 --OC(R.sub.6)(R.sub.7)OCH.sub.2 --, and R.sub.6 is methyl,R is not methyl,and a pharmaceutically acceptable carrier.