Patent ID: 6328953
Filing Date: 2001-12-11
Classification: A61K,A61P

Abstract:
A polymeric conjugate which consists of:(i) from 85 to 97 mol % of N-(2-hydroxypropyl)methacryloylamide units represented by formula (3) ##STR9##(ii) from 3 to 15 mol % of 20-O-(N-methacryloyl-glycyl-aminoacyl-glycyl)camptothecin units represented by formula (4) ##STR10##wherein n is from 2 to 8, --[O-CPT] represents the residue of a camptothecin of formula (2) ##STR11##which is linked at the C-20 position and in which each of R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5, which are the same or different, is hydrogen, C.sub.1 -C.sub.12 linear or branched alkyl, nitro, amino, (CH.sub.2).sub.a NR.sub.6 R.sub.7 in which a is from 0 to 4 and R.sub.6 and R.sub.7 are hydrogen or one of R.sub.6 or R.sub.7 is hydrogen and the other of R.sub.6 or R.sub.7 is C.sub.1 -C.sub.6 alkyl, or NR.sub.6 R.sub.7 represents a piperazino or N-alkyl-piperazino ring optionally substituted with C.sub.1 -C.sub.6 linear or branched alkyl, or a piperidino ring, (CH.sub.2).sub.a NHCOR.sub.8 in which a is as above defined and R.sub.8 is C.sub.1 -C.sub.8 linear or branched alkyl or a group NR.sub.6 R.sub.7 as above, hydroxy or O--CO--R.sub.8 in which R.sub.8 is as above defined or represents a 1-piperidino ring or 1,4'-bipiperidine, or R.sub.2 and R.sub.3 taken together represent the residue O--(CH.sub.2).sub.b --O, in which b is 1 or 2, or R.sub.4 and R.sub.5 represent the residue (CH.sub.2).sub.m, in which m is from 2 to 4, or the residue CH.sub.2 --O--CH.sub.2 or CH.sub.2 NHCH.sub.2and (iii) from 0 to 12 mol % of N-methacryloyl-glycine or N-(2-hydroxypropyl)methacryloyl-glycinamide units represented by formula (5) ##STR12##wherein [Z] represents a hydroxy group or a residue of formula --NH--CH.sub.2 --CH(OH)--CH.sub.3.