Polymeric conjugates of antitumor agents

Abstract

Water soluble polymeric conjugates of antitumor agents of formula (A) P-[W2]p-S0-[W1]r-[D] wherein: P is a water soluble polymer; [W1] is a residue of formula —HN-Z1-CO— in which Z1 represents a linear or branched C2-C12 alkylene chain or the residue of formula —C6HC—CH2—O—; [W2] is a residue of formula —HN-Z2-CO— in which Z2 represents a C2-C12 linear or branched alkylene chain; p and r are 0 or 1; S0 is a peptide that selectively is cleaved at the tumor site mainly by the action of the matrix metalloproteinases gelatinase; [D] is the residue of an antitumor agent. The conjugates possess enhanced antitumor activity and decreased toxicity with respect to the free drug. A process for their preparation, useful intermediates and pharmaceutical compositions containing them are also described.

Dependencies are inferred from the claim text.