POLYMERGEBUNDENE CAMPTOTHECIN-DERIVATE

摘要

PCT No. PCT/EP94/03154 Sec. 371 Date Jun. 8, 1995 Sec. 102(e) Date Jun. 8, 1995 PCT Filed Sep. 21, 1994 PCT Pub. No. WO95/10304 PCT Pub. Date Apr. 20, 1995A polymeric conjugate consists essentially of: (i) from 60 to 99 mol % of N-(2-hydroxypropyl) methacryloylamide units represented by formula 1: ethacryloylglycyl-aminoacyl) camptothecin units represented by formula 2 2 wherein [A] is a spacer group having respective terminal amino and carbonyl groups which are separated by at least three atoms and O-CPT represents a residue of a camptothecin, the C-20 hydroxy group of the camptothecin being linked to the terminal carbonyl group of the spacer group [A]; and (iii) from 0 to 10 mol % of N-methacryloylglycine or N-(2-hydroxy-propyl)methacryloylglycinamide units represented by formula 3: 3 wherein Z represents hydroxy or a residue of formula -NH-CH2-CH(OH)-CH3.