Anthracycline derivatives as solubilized pro-drugs
AssigneeAmerican Cyanamid Company
InventorsKeith C. Murdock, Ving J. Lee
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Abstract
The N-phosphorylation of basic nitrogenous drug compounds to produce pro-drugs with enhanced water solubility or lipid solubility, or reduced toxicity, is disclosed. Drugs containing amine, amidine, guanidine, isourea, isothiourea and biguanide functions may be converted to such pro-drugs. The pro-drugs are hydrolyzed in the body, regenerating the original drugs with the release of a salt of phosphoric acid.
Claims1
A compound of the formula ##STR39## where R.sub.13 is hydrogen, --OH or ##STR40## Y is C.sub.1 -C.sub.6 alkyl and A is ##STR41## such that R' and R" may be the same or different and are R (where R is C.sub.1 -C.sub.6 alkyl, C.sub.6 H.sub.5, C.sub.6 H.sub.5 --CH.sub.2 --, NC--CH.sub.2 CH.sub.2 --, ##STR42## Cl.sub.3 C--CH.sub.2 -- or R.sub.7 OCH.sub.2 CH.sub.2 --, where R.sub.7 is hydrogen or C.sub.1 -C.sub.6 alkyl), hydrogen, or a pharmaceutically acceptable cation or R' and R" are linked to form a --CH.sub.2 --CH.sub.2 -- or a ##STR43## group.
Dependencies are inferred from the claim text.