Polymer-bound camptothecin derivatives

Details Polymer-bound camptothecin derivatives Polymer-bound camptothecin derivatives

C - Chemistry, Metallurgy

07

K

C07K 5/04 (2006.01) A61K 47/48 (2006.01) C07K 7/06 (2006.01)

Patent

CA 2150132

A polymeric conjugate consists essentially of: (i) from 60 to 99 mol % of N-(2- hydroxypropyl)methacryloylamide units represented by formula (1); (ii) from 1 to 40 mol % of 20-0-(N-methacryloylglycylaminoacyl)camptothecin units represented by formula (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) wherein Z represents hydroxy or a residue of formula -NH-CH2-CH(OH)-CH3.

Un conjugué polymère est essentiellement constitué de: (i) de 60 à 99 % en mole d'unités de N-(2-hydroxypropyl)méthacryloylamide répondant à la formule (1); (ii) de 1 à 40 % en mole d'unités de 20-O-(N-méthacryloylglycylaminoacyl)camptothécine répondant à la formule (2) dans laquelle [A] est un groupe d'espacement ayant des groupes terminaux respectivement amino et carbonyle qui sont séparés par au moins trois atomes, et O-CPT représente un reste d'une camptothécine, le groupe hydroxy C-20 de la camptothécine étant lié au groupe carbonyle terminal du groupe d'espacement [A]; et (iii) de 0 à 10 % en mole d'unités de N-méthacryloylglycine ou N-(2-hydroxy-propyl)méthacryloylglycinamide répondant à la formule (3) dans laquelle Z représente hydroxy ou un reste de formule -NH-CH¿2?-CH(OH)-CH¿3?.

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