申请人:Sankyo Company, Limited
公开号:EP1568704A1
公开(公告)日:2005-08-31
A 2-5A analog represented by the formula (1):
[wherein m is 0 or 1; n is 0 to 2; R1 represents an alkoxy group having from 1 to 6 carbon atoms which may have a substituent, a mercapto group, a mercapto group protected by a nucleic acid synthesis protecting group, or an alkylthio group having from 1 to 4 carbon atoms which may have a substituent; R2, R3, R4, R5 and R6 represent a hydroxyl group, a hydroxyl group protected by a nucleic acid synthesis protecting group, an alkoxy group having from 1 to 6 carbon atoms which may have a substituent, a mercapto group, a mercapto group protected by a nucleic acid synthesis protecting group, or an alkylthio group having from 1 to 4 carbon atoms which may have a substituent; R7 represents an oxygen atom, or a -O(CH2CH2O)q- group (q is 2 to 6); R8 represents a hydrogen atom, an alkyl group having from 1 to 6 carbon atoms which may have a substituent, or 5'-phosphorylated oligonucleotide analogs which do not have one hydroxyl group on a 5'-phosphoric acid group; E1, E2, E3 and E4 represent a naturally occurring or modified nucleic acid unit], and a pharmacologically acceptable salt thereof.
由式(1)表示的 2-5A 类似物:
[其中 m 为 0 或 1;n 为 0 至 2;R1 代表具有 1 至 6 个碳原子且可能具有取代基的烷氧基、巯基、受核酸合成保护基保护的巯基或具有 1 至 4 个碳原子且可能具有取代基的烷硫基;R2、R3、R4、R5 和 R6 代表羟基、受核酸合成保护基团保护的羟基、具有 1 至 6 个碳原子且可能具有取代基的烷氧基、巯基、受核酸合成保护基团保护的巯基或具有 1 至 4 个碳原子且可能具有取代基的烷硫基;R7代表氧原子,或-O(CH2CH2O)q-基团(q为2至6);R8代表氢原子、具有1至6个碳原子且可具有取代基的烷基,或在5'-磷酸基上不具有一个羟基的5'-磷酸化寡核苷酸类似物;E1、E2、E3和E4代表天然存在的或修饰的核酸单元],及其药理学上可接受的盐。