ELONGATED AND MULTIPLE SPACERS IN ACTIVATIBLE PRODRUGS

摘要

This invention is directed to prodrugs that can be activated at the preferre d site of action in order to selectively deliver the corresponding therapeutic parent drugs to target cells or to the target site. This invention will therefore primarily but not exclusively relate to tumor cells as target cell s. More specifically the prodrugs are compounds of the formula V-(W)k-(X)1-A-Z, wherein: V is a specifier; (W)k-(X)1-A is an elongated self-elimination spac er system; W and X are each a 1,(4+2n) electronic cascade spacer, being the sam e or different; A is either a spacer group of formula (Y)m wherein: Y is a 1,(4+2n) electronic cascade spacer, or a group of formula U being a cyclisation elimination spacer; Z is a therapeutic drug; k, 1 and m are integers from 0 (included) to 5 (included); n is an integer of 0 (included) to 10 (included), with the provisos that: - when A is (Y)m: k+1+m >= 1, and if k+1+m = 1; - when A is U: k+1 >= 1.