POLYMERIC CONJUGATES OF ANTITUMOR AGENTS
    95.
    发明公开
    POLYMERIC CONJUGATES OF ANTITUMOR AGENTS 审中-公开
    聚合物复合物致癌CONNECTIONS

    公开(公告)号:EP1317287A2

    公开(公告)日:2003-06-11

    申请号:EP01969356.3

    申请日:2001-07-09

    IPC分类号: A61K47/48

    摘要: 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 -C6H4-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.