| 摘要 |
The present invention relates in general to the field of targeted drug delivery of anti-cancer drugs. More precisely, the present invention concerns polymer drug conjugates, namely, conjugates of poly(organo)phosphazenes and anti-cancer drugs, wherein the conjugates are suitable to selectively release anti-cancer drugs in tumor tissue. In addition, the present invention relates to a method for manufacturing such poly(organo)phosphazene molecule conjugates, to poly(organo)phosphazene molecule conjugates for use in medicine, in particular, to poly(organo)phosphazene molecule conjugates for use in the treatment of cancer, and to pharmaceutical compositions comprising such poly(organo)phosphazene molecule conjugates. |
| 主权项 |
1. A poly(organo)phosphazene molecule conjugate represented by formula 1, wherein, a represents a degree of polymerisation of the poly(organo)phosphazenes in a range of 1 to 150; m is an integer between 1 and 150; n and l are the same or different and each of n and l is independently an integer between 0 and 149; X represents O, S or NH; Y represents a pH sensitive functional group, wherein the pH sensitive functional group is selected from the group consisting of hydrazide, hydroxamate, imine, cyclic acetal and aconityl; R1 is selected from the group consisting of (C1 to C10)-alkyl, (C1 to C10)-alkenyl, (C1 to C10)-alkynyl, (C1 to C10)-alkoxy, (C1 to C10)-alkenoxy, (C1 to C10)-acyl, cycloalkyl, cycloalkenyl, aryl, arylalkyl, arylalkenyl, (C1 to C10)-heteroalkyl, (C1 to C10)-heteroalkenyl, (C1 to C10)-heteroalkynyl, (C1 to C10)-heteroalkoxy, (C1 to C10)-heteroalkenoxy, (C1 to C10)-heteroacyl, heterocycloalkyl, heterocycloalkenyl, heteroaryl, heteroarylalkenyl, heteroarylalkyl, and polyalkylene oxide; R2 represents an anti-cancer drug; R3, R4, R5, R6 and R7 are the same or different and each of R3, R4, R5, R6 and R7 is independently selected from the group consisting of R1—Y—R2, polyalkylene oxide, depsipeptide, amino acid alkyl ester, and a tumor targeting ligand. |
