公开(公告)号：US20220127300A1

公开(公告)日：2022-04-28

申请号：US17428998

申请日：2020-02-10

Applicant: Osaka University

Inventor： Satoshi OBIKA ,  Takao YAMAGUCHI ,  Takaki HABUCHI ,  Go KATO ,  Takao INOUE ,  Tokuyuki YOSHIDA ,  Md Ariful ISLAM

IPC: C07H21/04

Abstract: Disclosed are a 5′-modified nucleoside and a nucleotide using the same. The nucleoside of the present invention is represented by the formula (I) below. The 5′-modified nucleoside of the present invention is usable as a substitute for a phosphorothioate-modified nucleic acid, which has a risk of, for example, accumulation in a specific organ. The 5′-modified nucleoside also has excellent industrial productivity because a diastereomer separation step is not involved in the production process thereof.

公开(公告)号：US20230340008A1

公开(公告)日：2023-10-26

申请号：US17791799

申请日：2021-02-18

Applicant: Osaka University ,  Japan Represented by Director General of National Institute of Health Sciences

Inventor： Satoshi OBIKA ,  Takao YAMAGUCHI ,  Hibiki KOMINE ,  Takaya SUGIURA ,  Takao INOUE ,  Tokuyuki YOSHIDA

IPC: C07H21/02

CPC classification number: C07H21/02

Abstract: Disclosed are a bridged nucleoside and a nucleotide using the same. The nucleoside of the present invention is represented by the formula (I) below. The bridged nucleoside of the present invention is usable as a substitute for a phosphorothioate-modified nucleic acid, which has a risk of, for example, accumulation in a specific organ. The bridged nucleoside also has excellent industrial productivity.

公开(公告)号：US20230124641A1

公开(公告)日：2023-04-20

申请号：US17800339

申请日：2021-02-17

Applicant: Osaka University ,  Japan as Represented by Director General of National Institute of health Sciences

Inventor： Satoshi OBIKA ,  Takao YAMAGUCHI ,  Yota SAKURAI ,  Chika YAMAMOTO ,  Kei SUGITA ,  Takao INOUE ,  Tokuyuki YOSHIDA

IPC: C07D493/08 ,  C07H21/04 ,  C07D239/10

Abstract: A cross-linked nucleoside of the present invention is a compound represented by the formula (I) below. The cross-linked nucleoside of the present invention is usable as a substitute for a phosphorothioate-modified nucleic acid, which has a risk of, for example, accumulation in a specific organ. The cross-linked nucleoside also has excellent industrial productivity.

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：US20220372060A1

公开(公告)日：2022-11-24

申请号：US17427134

申请日：2020-01-31

Applicant: Osaka University

Inventor： Satoshi OBIKA ,  Takao YAMAGUCHI ,  Takaki HABUCHI ,  Go KATO ,  Takao INOUE ,  Tokuyuki YOSHIDA ,  Takaya SUGIURA

IPC: C07H19/10 ,  C07H19/20 ,  C07H21/00

Abstract: Disclosed are a 5′-modified nucleoside and a nucleotide using the same. The nucleoside of the present invention is represented by the formula (I) below. The 5′-modified nucleoside of the present invention is usable as a substitute for a phosphorothioate-modified nucleic acid, which has a risk of, for example, accumulation in a specific organ. The 5′-modified nucleoside also has excellent industrial productivity because a diastereomer separation step is not involved in the production process thereof.

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.