Patent ID: 6140310
Filing Date: 2000-10-31
Classification: A61K,C07C,C07F,C07H

Abstract:
A prodrug compound for a parent drug, wherein the parent drug has the structure: ##STR31## wherein X is oxygen or sulfur; n is 1 or 2; andY is defined by the remainder of the parent drug; such that the parent drug is not phosphoric acid; wherein the prodrug compound has the structure: ##STR32## wherein X, n and Y are defined above; and ""A"" is of the formula: ##STR33## wherein: R.sub.1, R.sub.3 and R.sub.6 are independently a (--O--CO--R8) group; a (--O--CO.sub.2 --R8) group; an N-substituted amino carbonyl oxy; a (--O--C(O)--NHCH.sub.3) group; a (--O--C(O)--N(CH.sub.3).sub.2) group; hydrogen; a halogen; a (--CO.sub.2 R9) group; a methyl group; a hydroxymethyl group(HO--CH.sub.2 --); a hydroxyethyl; a --CH.sub.2 --CO.sub.2 R.sub.11 group or a group which undergoes biotransformation in vivo to yield a hydroxy group;R.sub.2 and R.sub.7 are independently hydrogen; a (--CO.sub.2 --R10) group; a methyl group; a halogen; a methoxy group; (--O--CO--R8); or a hydroxymethyl group (HO--CH.sub.2);R.sub.4 and R.sub.5 are independently hydrogen; a methyl group; a methoxy-methyl (--CH.sub.2 --O--CH.sub.3); a (--CH.sub.2 --CO.sub.2 --R12) group; a (--CH.sub.2 --CO--CH.sub.3) group; a (--CH(CH.sub.3)--CO.sub.2 --R12) group; a (--CH.sub.2 --CO--NH.sub.2) group; a (--CH.sub.2 --NO.sub.2) group; or a (--CH.sub.2 --SO.sub.2 --CH.sub.3) group;R8 is an alkyl; a substituted or unsubstituted phenyl group, or wherein R8 can also be selected such that R8--CO.sub.2 H is an amino acid, lactic acid, glycolic acid, glyceric acid, or acetoacetic acid;R9, R10, R11 and R12, independently are methyl, ethyl, phenyl, or benzyl; and wherein at least one of the groups: R.sub.1, R.sub.3 or R.sub.6 is a (--O--CO--R8); a (--OCO.sub.2 R8) group; a (--O--CO--NHCH.sub.3) group; or a (--O--CO--N(CH.sub.3).sub.2) group; or a group which undergoes biotransformation in vivo to yield a hydroxy group.