Lipid derivative in which hydrophilic polymer is bound through cyclic benzylidene acetal linker
申请人:NOF CORPORATION
公开号:US10626217B2
公开(公告)日:2020-04-21
A lipid derivative in which a hydrophilic polymer is bound through a cyclic benzylidene acetal linker, and which can accurately control a hydrolysis rate in the weakly acidic environment of a living body to detach the hydrophilic polymer from a lipid membrane structure. The lipid derivative is represented by formula (1):
wherein, R1 and R6 are each independently a hydrogen atom or a hydrocarbon group; R2, R3, R4 and R5 are each independently an electron-withdrawing or electron-donating substituent or a hydrogen atom; R7 is a hydrocarbon group having from 8 to 24 carbon atoms, an acyl group having from 8 to 24 carbon atoms, a cholesterol derivative, a glycerolipid, a phospholipid or a sphingolipid; P is a hydrophilic polymer; s is 1 or 2, t is 0 or 1, and s+t is 1 or 2; and Z1 and Z2 are each independently a selected divalent spacer.
一种脂质衍生物,其中的亲水性聚合物通过环状亚苄基乙缩醛连接体结合,并能在生物体的弱酸性环境中精确控制水解速度,使亲水性聚合物从脂质膜结构中脱离。脂质衍生物由式(1)表示:
其中,R1 和 R6 各自独立地为氢原子或烃基;R2、R3、R4 和 R5 各自独立地为取电子或供电子取代基或氢原子;R7 是具有 8 至 24 个碳原子的烃基、具有 8 至 24 个碳原子的酰基、胆固醇衍生物、甘油酯、磷脂或鞘磷脂;P 是亲水性聚合物;s 是 1 或 2,t 是 0 或 1,s+t 是 1 或 2;以及 Z1 和 Z2 各自独立地是选定的二价间隔物。