DERIVADOS DE LA CAMPTOTECINA UNIDOS A POLIMEROS

UN CONJUGADO POLIMERICO QUE CONSISTE ESENCIALMENTE DE: (I) DE 60 A 99 MOL % DE UNIDADES DE N-(2-HIDROXIPROPILO)METACRILOLAMIDA REPRESENTADAS EN LA FORMULA (1); (II) DE 1 A 40 MOL % DE UNIDADES DE 20-0-(N-METACRILOILGLICILAMINOACILO)CAMPTOTECINA REPRESENTADAS EN LA FORMULA (2), DONDE [A] ES UN GRUPO SE SEPARACION QUE TIENE GRUPOS RESPECTIVOS DE TERMINAL AMINO Y CARBONILOS LOS CUALES ESTAN SEPARADOS POR AL MENOS 3 ATOMOS Y O-CPT REPRESENTA UN RESIDUO DE UNA CAPTOTECINA, EL GRUPO HIDROXI C-20 DE LA CAMPTOTECINA, ESTANDO LIGADO A UN GRUPO DE TERMINAL CARBONILO DEL GRUPO SE SEPARACION; Y (III) DE 0 A 10 MOL % DE UNIDADES DE NMETACRILOILGLICINA O N-(2.HIDROXIPROPIL)METACRILOILGLICINAMIDA REPRESENTADAS EN LA FORMULA (3) DONDE Z REPRESENTA HIDROXI O UN RESIDUO DE LA FORMULA NH-CH2-CH(OH)-CH3. 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.