公开(公告)号：US20220170020A1

公开(公告)日：2022-06-02

申请号：US17666341

申请日：2022-02-07

Applicant: Osaka University

Inventor： Satoshi OBIKA ,  Reiko WAKI ,  Takao INOUE ,  Tokuyuki YOSHIDA ,  Kunihiko MORIHIRO ,  Yuya KASAHARA ,  Atsushi MIKAMI

IPC: C12N15/113 ,  A61K31/7115 ,  A61K31/712

Abstract: The present invention aims to provide an antisense oligonucleic acid with reduced hepatotoxicity. The antisense oligonucleic acid according to the present invention is characterized in that it has a base length of not less than 7 nt and not more than 30 nt, wherein nucleic acid residues of not less than 1 nt and not more than 5 nt respectively from the both terminals are 2′,4′-bridged nucleic acids, 2′,4′-non-bridged nucleic acid residue(s) is(are) present between the above-mentioned both terminals, and one or more bases in the nucleic acid residue(s) of the above-mentioned 2′,4′-non-bridged nucleic acid residue(s) is/are modified.

公开(公告)号：US20200056178A1

公开(公告)日：2020-02-20

申请号：US16487762

申请日：2018-02-20

Applicant: Osaka University

Inventor： Satoshi OBIKA ,  Reiko WAKI ,  Takao INOUE ,  Tokuyuki YOSHIDA ,  Kunihiko MORIHIRO ,  Yuya KASAHARA ,  Atsushi MIKAMI

IPC: C12N15/113 ,  A61K31/7115 ,  A61K31/712

Abstract: The present invention aims to provide an antisense oligonucleic acid with reduced hepatotoxicity. The antisense oligonucleic acid according to the present invention is characterized in that it has a base length of not less than 7 nt and not more than 30 nt, wherein nucleic acid residues of not less than 1 nt and not more than 5 nt respectively from the both terminals are 2′,4′-bridged nucleic acids, 2′,4′-non-bridged nucleic acid residue(s) is(are) present between the above-mentioned both terminals, and one or more bases in the nucleic acid residue(s) of the above-mentioned 2′,4′-non-bridged nucleic acid residue(s) is/are modified.

公开(公告)号：US20170044528A1

公开(公告)日：2017-02-16

申请号：US15118546

申请日：2015-02-17

Applicant: OSAKA UNIVERSITY

Inventor： Satoshi OBIKA ,  Takao YAMAGUCHI ,  Masahiko HORIBA ,  Reiko WAKI

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

CPC classification number: C12N15/113 ,  C07H19/06 ,  C07H19/16 ,  C07H21/00 ,  C12N2310/31

Abstract: 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.

Abstract translation: 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。