申请人:Gifu University
公开号:EP3556764A1
公开(公告)日:2019-10-23
To provide a nucleoside that is more practical for RNA pharmaceuticals and other applications and use thereof. A nucleoside derivative represented by formula (1) or (2) below, or a salt thereof.
[C1]
(In formula (1), R1 represents a hydrogen atom, a hydroxyl group, a hydroxyl group in which a hydrogen atom is substituted by an alkyl group or alkenyl group, or a protected group, and in formula (2), X represent a halogen atom. In formula (1) and formula (2), R2 and R4 may be the same or different, and each represents a hydrogen atom, a hydroxyl protecting group, a phosphate group, a protected phosphate group, or -P(=O)nR5R6 (in which n is 0 or 1, and R5 and R6 may be the same or different, with each representing a hydrogen atom, hydroxyl group, protected hydroxyl group, mercapto group, protected mercapto group, lower alkoxy group, cyano lower alkoxy group, amino group or substituted amino group, but when n is 1, R5 and R6 are not both hydrogen atoms), R3 represents NHR7 (in which R7 represents a hydrogen atom, an alkyl group, an alkenyl group or a protecting group for an amino group), an azide group, an amidino group or a guanidino group, each having a linking group (but when R7 is hydrogen atom, the linking group is an alkylene group which has at least 2 carbon atoms), and B represents any of a purine-9-yl group, 2-oxo-pyrimidin-1-yl group, substituted purine-9-yl group or substituted 2-oxo-pyrimidin-1-yl group.)
提供一种更实用的核苷,用于 RNA 制药和其他应用及其用途。一种由下式(1)或(2)代表的核苷衍生物或其盐。
[C1]
(在式(1)中,R1代表氢原子、羟基、氢原子被烷基或烯基取代的羟基或被保护基,在式(2)中,X代表卤素原子。在式 (1) 和式 (2) 中,R2 和 R4 可以相同或不同,各自代表氢原子、羟基保护基团、磷酸基团、受保护的磷酸基团或 -P(=O)nR5R6 (其中 n 为 0 或 1,R5 和 R6 可以相同或不同、各自代表氢原子、羟基、受保护羟基、巯基、受保护巯基、低级烷氧基、氰基低级烷氧基、氨基或取代氨基,但当 n 为 1 时,R5 和 R6 不能同时代表氢原子、羟基、受保护羟基、巯基、低级烷氧基、氰基低级烷氧基、氨基或取代氨基、R3代表NHR7(其中R7代表氢原子、烷基、烯基或氨基的保护基)、叠氮基、脒基或胍基、B代表嘌呤-9-基、2-氧代嘧啶-1-基、取代的嘌呤-9-基或取代的 2-氧代嘧啶-1-基中的任一基团。)