公开(公告)号：US20150266917A1

公开(公告)日：2015-09-24

申请号：US14428646

申请日：2013-09-19

Applicant: OSAKA UNIVERSITY

Inventor： Satoshi Obika ,  Yutaro Kotobuki ,  Reiko Waki

IPC: C07H19/10 ,  C07H19/06 ,  C07H21/02 ,  C07H21/04

CPC classification number: C07H19/10 ,  C07H19/06 ,  C07H21/00 ,  C07H21/02 ,  C07H21/04 ,  C07H23/00

Abstract: 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.

Abstract translation: 本发明的寡核苷酸或其药理学上可接受的盐含有由式I或II表示的化合物或其盐，以及由式I'或II'表示的至少一种核苷结构。 根据本发明，提供了对靶核酸具有高结合亲和性和特异性，并具有高核酸酶抗性的寡核苷酸的核酸分子。

公开(公告)号：US10377789B2

公开(公告)日：2019-08-13

申请号：US14428646

申请日：2013-09-19

Applicant: OSAKA UNIVERSITY

Inventor： Satoshi Obika ,  Yutaro Kotobuki ,  Reiko Waki

IPC: C07H19/06 ,  C07H19/10 ,  C07H21/00 ,  C07H21/02 ,  C07H21/04 ,  C07H23/00

Abstract: A compound represented by formula I or II below or a salt thereof: wherein B1 represents a purin-9-yl group or a 2-oxo-1,2-dihydropyrimidin-1-yl group that has any one or more substituents selected from the group consisting 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.

公开(公告)号：US09611479B2

公开(公告)日：2017-04-04

申请号：US15118546

申请日：2015-02-17

Applicant: OSAKA UNIVERSITY

Inventor： Satoshi Obika ,  Takao Yamaguchi ,  Masahiko Horiba ,  Reiko Waki

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

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.

公开(公告)号：US12104154B2

公开(公告)日：2024-10-01

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

CPC classification number: 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：US11261440B2

公开(公告)日：2022-03-01

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.