The present invention relates to a prodrug or a pharmaceutically acceptable salt thereof comprising a biologically active moiety-linker conjugate D-L, wherein D is a hydroxyl-comprising biologically active moiety; and L is a promoiety comprising a moiety L1 represented by formula (I) and wherein L1 is substituted with one to four groups L2-Z and optionally further substituted, provided that the hydrogen marked with the asterisk in formula (I) is not replaced by a substituent; wherein L2 is a single chemical bond or a spacer and Z is a carrier group. The invention also relates to pharmaceutical compositions comprising said prodrugs and their use as medicaments.
本发明涉及一种前药或其药学上可接受的盐,包括
生物活性基团-连接物D-L的共轭物,其中D是含有羟基的
生物活性基团;L是包含由式(I)表示的基团L1的前基团,其中L1被一个到四个基团
L2-Z取代,并且可选择进一步取代,前提是式(I)中带星号标记的氢未被取代;其中
L2是一个
化学键或一个间隔物,Z是一个载体基团。该发明还涉及包含所述前药的药物组合物及其作为药物的用途。