Patent ID: 7037898
Filing Date: 2006-05-02
Classification: A61K,A61P,C07K

Abstract:
1. A compound, W-Z-M, comprising a component, M, wherein M is a therapeutic agent, said M being linked to a ligand, W-Z, said ligand comprising an arm, Z, linked to a terminal group, W, wherein linkage in the arm, Z, of the ligand, W-Z, or between the arm, Z, and the component, M, prevents intracellular entry of the compound, W-Z-M, and wherein said linkage can be selectively cleaved by a factor or factors secreted by a target cell so as to permit entry of the therapeutic agent into said target cell, and further wherein the terminal group, W, includes β-alanyl, and further wherein M is selected from the group consisting of anthracyclines, including doxorubicin and daunorubicin, folic acid derivatives, vinca alkaloids, calicheamycin, mitoxantrone, methotrexate, cytosine arabinosides (ARA-C) or adenosine arabinosides (ARA-A), fludarabine phosphate, melphalan, bleomycin, mitomycin, L-canavanine, taxoids, camptothecin and their derivatives, especially 9-dimethylaminomethyl-10-hydroxycamphtothecin hydrochloride, and their derivatives, optionally linked to a substituted or unsubstituted amino acid.