申请人:FUJIFILM Corporation
公开号:EP3805198A1
公开(公告)日:2021-04-14
An object of the present invention is to provide a compound or a salt thereof constituting lipid particles that can achieve a high nucleic acid encapsulation rate and excellent delivery of nucleic acids, and to provide lipid particles that can achieve a high nucleic acid encapsulation rate and excellent delivery of nucleic acids. According to an aspect of the present invention, a compound represented by Formula (1) or a salt thereof is provided.
In the formula, X represents -NR1- or -O-, R1 represents a hydrogen atom, a hydrocarbon group, or the like, R2 and R3 each independently represent a hydrogen atom, a hydrocarbon group, or the like, R4, R5, R6, R7, R8, R9, R10, R11, and R12 each independently represent a hydrogen atom or an alkyl group,
groups in any one or more pairs among R4 and R5, R10 and R5, R5 and R12, R4 and R6, R5 and R6, R6 and R7, R6 and R10, R12 and R7, and R7 and R8 may be linked to each other to form a 4- to 7-membered ring which may contain an O atom, a, b, c, and d are each independently represent an integer of 0 to 3, a + b is equal to or greater than 1, and c + d is equal to or greater than 1.
本发明的目的是提供一种化合物或其盐类构成的脂质微粒,该脂质微粒可实现较高的核酸包封率和核酸的良好递送,并提供可实现较高的核酸包封率和核酸的良好递送的脂质微粒。根据本发明的一个方面,提供了一种由式(1)代表的化合物或其盐。
式中,X代表-NR1-或-O-,R1代表氢原子、烃基或类似物,R2和R3各自独立地代表氢原子、烃基或类似物,R4、R5、R6、R7、R8、R9、R10、R11和R12各自独立地代表氢原子或烷基、R4和R5之间任意一对或多对的基团、R10 和 R5、R5 和 R12、R4 和 R6、R5 和 R6、R6 和 R7、R6 和 R10、R12 和 R7 以及 R7 和 R8 中的任意一对或多对基团可彼此相连,形成可包含 O 原子的 4 至 7 元环,a、b、c 和 d 各自独立地代表 0 至 3 的整数,a + b 等于或大于 1,c + d 等于或大于 1。