OLIGONUCLEOTIDE AND ARTIFICIAL NUCLEOSIDE HAVING GUANIDINE BRIDGE

摘要

An oligonucleotide or a pharmacologically acceptable salt thereof of the present invention contains a compound represented by formula I or II or a salt thereof, and at least one of nucleoside structures represented by formula I′ or II′. According to the present invention, provided is a nucleic acid molecule for oligonucleotides having high binding affinity and specificity to a target nucleic acid, and exhibiting high nuclease resistance.

主权项

1. A compound represented by formula I or II below or a salt thereof: (wherein B1 represents a purine-9-yl group or a 2-oxo-1,2-dihydropyrimidine-1-yl group that may have any one or more substituents selected from a group α, wherein the group α consists of a hydroxyl group, a hydroxyl group protected by a protecting group in nucleic acid synthesis, a C1 to C6 linear alkyl group, a C1 to C6 linear alkoxy group, a mercapto group, a mercapto group protected by a protecting group in nucleic acid synthesis, a C1 to C6 linear alkylthio group, an amino group, a C1 to C6 linear alkylamino group, an amino group protected by a protecting group in nucleic acid synthesis, and a halogen atom; R1, R12, and R13 each independently represent a hydrogen atom, a C1 to C7 alkyl group that may be branched or form a ring, a protecting group for an amino group, orand
R2 and R3 each independently represent a hydrogen atom, a protecting group for a hydroxyl group in nucleic acid synthesis, a C1 to C7 alkyl group that may be branched or form a ring, a C2 to C7 alkenyl group that may be branched or form a ring, a C3 to C12 aryl group that may have any one or more substituents selected from the group α and that may have a hetero atom, an aralkyl group having a C3 to C12 aryl moiety that may have any one or more substituents selected from the group α and that may be a hetero atom, an acyl group that may have any one or more substituents selected from the group α, a silyl group that may have any one or more substituents selected from the group α, a phosphate group that may have any one or more substituents selected from the group α, a phosphate group protected by a protecting group in nucleic acid synthesis, or —P(R4)R5 (wherein R4 and R5 each independently represent a hydroxyl group, a hydroxyl group protected by a protecting group in nucleic acid synthesis, a mercapto group, a mercapto group protected by a protecting group in nucleic acid synthesis, an amino group, a C1 to C5 alkoxy group, a C1 to C5 alkylthio group, a C1 to C6 cyanoalkoxy group, and/or an amino group substituted with a C1 to C6 alkyl group)).