A conjugated polymer of 20 - 0 - - Aminoacyl glycyl glycyl camptothecin, a procedure for producing such conjugated Polymer, a Derivative of 20 - 0 - acylamino - glycyl - camptothecin,A Derivative of 20 - 0 - - - (metacriloil glycyl glycyl - Aminoacyl) camptothecin Derivatives, processes for producing these

摘要

A conjugated polymer of [0 - 20 - camptothecin glycyl glycyl - Aminoacyl] consisting of: (i) between 85 and 97 mol% units of N - (2-hydroxypropyl) represented by the formula (3 metacriloilamida; (i)(i) between 3 and 15 mol% of unidadesd and 20 - 0 - (N - glycyl glycyl - metacriloil - Aminoacyl) - camptotecinarepresentadas BY FORMULA (4), in which n is between 2 and 8- [CPT] represents the residue of a camptothecin of formula (2), which is the encuentraunida c-20 position Q and the EU each R1, R2, R3, R4 and R5 can be equal or different,Is Hydrogen, C1 - 12 oramificado linear alkyl, Nitro, amino, (CH2) anr6r7, which ranges between 0 and 4 and R6 and R7 are Hydrogen or a hydrogen between R6 and R7 is the Mong and R6 and R7 is alquiloc1 - 6Or nr6r7 represents a Ring of N - alkyl - or piperazino piperazino optionally replaced with linear or branched alkyl C1 - 6 or a piperidino ring,Anhcor8 (CH2) where a is defined as before, and R8 is C1 - 8 linear or branched alkyl group or a nr6r7 as mentioned before, Hydroxy or co - R8,Where R8 is as defined before or represents a 1 - 1.4 - piperidino Ring or bipiperidino R2 and R3, or taken in formaconjunta represents the residue of N, o - (CH2) B - or,Where B is 1 or 2; R4 and R5 represents the residue of (CH2) m, where M is between 2 and 4The residuoch2 CH2 or - or - or ch2nhch2; and (iii) between 0 and 12 mol% units of metacriloil Glycine N - or N - (2 - hydroxy - propyl) - metacriloil glycinamide representadaspor formula (5),In the [z] represents a Hydroxy group or a residue of the Formula - NH - CH2 CH (OH) - CH3.This conjugated Polymer has a actividadantitumoralmejorada and reduced toxicity compared with the free Drug. A procedure to produce this conjugated Polymer, a Derivative of