ANTHRACYCLINE CONJUGATES, THEIR PREPARATION AND THEIR USE AS ANTITUMOR AGENTS

摘要

The present invention provides polymer-bound anthracyclines of formula A which consists essentially of three units represented by formulae 1, 2 and 3: (see formula 1) (see formula 2) (see formula 3) wherein: Gly represents glycine; n is 0 or 1: x is from 70 to 98 mol %, y is from 1 to 29 mol %, z is from 1 to 29 mol %, R1 is a C1-C6 alkyl group substituted by one or more hydroxy groups; Y is an amino acid residue or a peptide spacer; [NH-D] is the residue of an anthracycline aminoglycoside [NH2-D]; and Z is a hydroxy group or a residue of formula -NHR1 wherein R1 is as defined above. Methods for their preparation and pharmaceutical compositions containing them are also provided.