公开(公告)号：US20170044528A1

公开(公告)日：2017-02-16

申请号：US15118546

申请日：2015-02-17

申请人： OSAKA UNIVERSITY

发明人： Satoshi OBIKA ,  Takao YAMAGUCHI ,  Masahiko HORIBA ,  Reiko WAKI

IPC分类号： C12N15/113 ,  C07H19/16 ,  C07H19/06

CPC分类号： C12N15/113 ,  C07H19/06 ,  C07H19/16 ,  C07H21/00 ,  C12N2310/31

摘要： Disclosed are bridged nucleosides and nucleotides. The nucleosides of the present invention have a 2′,4′-bridged structure and are represented by formula I below: An oligonucleotide containing a 2′,4′-bridged artificial nucleotide of the present invention has a binding affinity for single-stranded RNA comparable to that of known 2′,4′-BNA/LNA and higher nuclease resistance than LNA. In particular, since the oligonucleotide has a much higher binding affinity for single-stranded RNA than S-oligo, it is expected that the oligonucleotide is applicable to nucleic acid drugs.

摘要翻译： 含有本发明的2'，4'-桥接人造核苷酸的寡核苷酸对于单链RNA具有与已知的2'，4'-BNA / LNA和比NNA更高的核酸酶抗性相当的结合亲和力。 特别是，由于寡核苷酸对单链RNA的结合亲和力高于S-寡聚体，所以预期该寡核苷酸适用于核酸药物。

公开(公告)号：US20220169671A1

公开(公告)日：2022-06-02

申请号：US17667988

申请日：2022-02-09

申请人： Osaka University

发明人： Satoshi OBIKA ,  Kosuke ITO ,  Takaki HABUCHI ,  Masahiko HORIBA

IPC分类号： C07H19/10 ,  C07H21/02 ,  C12N15/113

摘要： The present invention aims to provide a nucleic acid compound that hardly forms non-Watson-Crick base pairs, and an oligonucleotide containing the nucleic acid compound and showing reduced non-specific binding with nucleic acids other than the target nucleic acid. The nucleic acid compound according to the present invention is characterized in that the 2-position carbonyl group of the pyrimidine base is functionally converted (X1 and X2 are each independently S or Se), and that the 2′-position and the 4′-position are bridged in a particular structure. The oligonucleotide according to the present invention is characterized in that at least one of thymidine and uridine is the nucleic acid compound.

公开(公告)号：US20200055890A1

公开(公告)日：2020-02-20

申请号：US16487785

申请日：2018-02-20

申请人： Osaka University

发明人： Satoshi OBIKA ,  Kosuke ITO ,  Takaaki HABUCHI ,  Masahiko HORIBA

IPC分类号： C07H19/10 ,  C12N15/113 ,  C07H21/02

摘要： The present invention aims to provide a nucleic acid compound that hardly forms non-Watson-Crick base pairs, and an oligonucleotide containing the nucleic acid compound and showing reduced non-specific binding with nucleic acids other than the target nucleic acid. The nucleic acid compound according to the present invention is characterized in that the 2-position carbonyl group of the pyrimidine base is functionally converted (X1 and X2 are each independently S or Se), and that the 2′-position and the 4′-position are bridged in a particular structure. The oligonucleotide according to the present invention is characterized in that at least one of thymidine and uridine is the nucleic acid compound.