Novel nucleosides and oligonucleotide analogues

Details Novel nucleosides and oligonucleotide analogues Novel nucleosides and oligonucleotide analogues

C - Chemistry, Metallurgy

07

H

C07H 19/20 (2006.01) A61K 31/7064 (2006.01) A61K 31/7076 (2006.01) C07H 19/06 (2006.01) C07H 19/067 (2006.01) C07H 19/10 (2006.01) C07H 19/16 (2006.01) C07H 19/167 (2006.01) C07H 21/02 (2006.01)

Patent

CA 2361318

[Subject] 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. [Solution] A compound of the formula (1): (see formula 1) [wherein R1 and R2 are the same or different and represent a hydrogen atom, a hydroxyl protecting group, a phosphoric acid group, or -P(R3)R4 [wherein R3 and R4 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 atoms]; 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 a group]; 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.

L'invention porte sur des composés de formule générale (1) et leurs sels, et sur de nouveaux analogues d'oligonucléotides préparés en les utilisant comme intermédiaires, et présentant d'excellentes activités antisens. Dans la formule: R<1> et R<2> sont chacun indépendamment H, un groupe protecteur hydroxyle, un groupe acide phosphorique, ou P(R<3>)R<4> (dans lequel R<3> et R<4> sont chacun indépendamment C1-C5 cyanoaloxy substitué par C1-C4 alkyle, ou analogue); A est C1-C4 alkylène; et B est purin-9-yl ou 2-oxopyrimidin-1yl.

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