申请人:Kyowa Hakko Kirin Co., Ltd.
公开号:US20150376611A1
公开(公告)日:2015-12-31
The present invention provides an oligonucleotide having improved affinity for AGO2, and the like. The oligonucleotide has a nucleotide residue or a nucleoside residue represented by formula (I) wherein X
1
is an oxygen atom or the like, R
1
is formula (IIA) (wherein R
5A
is halogen or the like, and R
6A
is a hydrogen atom or the like) or formula (IVA) (wherein Y
3A
is a nitrogen atom or the like, and Y
4A
is CH or the like), or the like, R
2
is a hydrogen atom, hydroxy, halogen, or optionally substituted lower alkoxy, and R
3
is a hydrogen atom or the like} at the 5′ end thereof, and the nucleotide residue or the nucleoside residue binds to an adjacent nucleotide residue through the oxygen atom at position 3.
本发明提供了一种具有改善对AGO2亲和力的寡核苷酸等。该寡核苷酸在其5'端具有由式(I)表示的核苷酸残基或核苷酸残基其中X
1
是氧原子或类似物,R
1
是式(IIA)(其中R
5A
是卤素或类似物,而R
6A
是氢原子或类似物)或式(IVA)(其中Y
3A
是氮原子或类似物,而Y
4A
是CH或类似物),或类似物,R
2
是氢原子、羟基、卤素或可选择地取代的较低烷氧基,而R
3
是氢原子或类似物},并且该核苷酸残基或核苷酸残基通过位于位置3的氧原子与相邻核苷酸残基结合。