发明授权
EP1370298B1 ELONGATED AND MULTIPLE SPACERS IN ACTIVATIBLE PRODRUGS 有权
细长且多ABSTANDSHALTER含有活性药物前体

ELONGATED AND MULTIPLE SPACERS IN ACTIVATIBLE PRODRUGS
摘要:
This invention is directed to prodrugs that can be activated at the preferred 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 cells. 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 spacer system; W and X are each a 1,(4+2n) electronic cascade spacer, being the same 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.
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