PRODRUGS OF PHOSPHOROUS-CONTAINING PHARMACEUTICALS

摘要

Pharmaceutical compounds with the formula: Drug-P(=O)-O-Linker(-R2')k-R2 where Drug-P(=O)-O- is the residue of a drug comprising a phosphonate, phosphinate or phosphoryl function, such as alendronate or foscarnet, R2 and R2' (if present) are independently the acyl residue of an aliphatic amino acid; Linker is an at least difunctional moiety comprising a first function ester-bonded to the phosphonate, phosphinate or phosphoryl function spaced from a second function ester-bonded to R2; and k is 1 or zero; have enhanced bioavailability or other pharmacokinetic performance relative to the parent drug.