Nye nukleosider og oligonukleotidanaloger

摘要

The object of the present invention is to provide novel oligonucleotide analogues, which exhibit antisense or antigene activity having excellent stability, or exhibit excellent activity as a detection agent (probe) for a specific gene or as a primer for starting amplification, and to novel nucleoside analogues which are intermediates for their production. ÄSolutionÜ A compound of the formula (1): Äwherein R<1> and R<2> are the same or different and represent a hydrogen atom, a hydroxyl protecting group, a phosphoric acid group, or -P(R<3>)R<4> Äwherein R<3> and R<4> are the same or different and represent a hydroxyl group, an amino group, an alkoxy group having from 1 to 4 carbon atoms, a cyanoalkoxy group having from 1 to 5 carbon atoms or an amino group substituted by an alkyl group having from 1 to 4 carbon atomsÜ; A represents an alkylene group having from 1 to 4 carbon atoms; and B represents a purin-9-yl group, a 2-oxo-pyrimidin-1-yl group or a substituted purin-9-yl group or a substituted 2-oxo-pyrimidin-1-yl group having a substituent selected from the following alpha groupÜ; or the salt thereof; ( alpha group> a hydroxyl group which may be protected, an alkoxy group having from 1 to 4 carbon atoms, a mercapto group which may be protected, an alkylthio group having from 1 to 4 carbon atoms, an alkoxy group having from 1 to 4 carbon atoms, an amino group which may be protected, a mono- or di-alkylamino group which may be substituted by an alkyl group having from 1 to 4 carbon atoms, an alkyl group having from 1 to 4 carbon atoms and a halogen atom. A compound of the formula (I), and the pharmacologically acceptable salts or derivatives thereof.