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：US20220002336A1

公开(公告)日：2022-01-06

申请号：US17292963

申请日：2019-11-11

Applicant: MITSUBISHI TANABE PHARMA CORPORATION ,  OSAKA UNIVERSITY

Inventor： Hiroaki SAWAMOTO ,  Shinji KUMAGAI ,  Hiroyuki FURUKAWA ,  Tomo ARAKI ,  Masayuki UTSUGI ,  Satoshi OBIKA

IPC: C07H19/20 ,  C07H19/10 ,  C07H21/04

Abstract: The present invention provides a novel bridged artificial nucleic acid and an oligomer containing the same as a monomer. The present invention provides specifically a compound represented by general formula (I) (wherein each symbol is the same as defined in the specification) or salts thereof; as well as an oligonucleotide compound represented by general formula (I′) (wherein each symbol is the same as defined in the specification) or salts thereof.

公开(公告)号：US20180251488A1

公开(公告)日：2018-09-06

申请号：US15760513

申请日：2016-09-20

Applicant: MITSUBISHI TANABE PHARMA CORPORATION ,  OSAKA UNIVERSITY

Inventor： Satoshi OBIKA ,  Eiji KAWANISHI ,  Hiroaki SAWAMOTO ,  Shuhei YAMAKOSHI ,  Yuuki ARAI ,  Shinji KUMAGAI

IPC: C07H19/06 ,  C07H9/06

CPC classification number: C07H19/06 ,  C07C279/16 ,  C07D498/04 ,  C07D498/08 ,  C07H1/00 ,  C07H9/06 ,  C07H19/16 ,  C07H21/00

Abstract: The present invention provides a method for producing guanidine crosslinked artificial nucleic acid (abbreviated hereinafter as GuNA), and an intermediate compound for the production thereof. Specifically, the present invention provides a method for producing a compound represented by general formula I: (in the formula, R1, R2, R3, R4, R5, R6, m and ring A are as defined in the specification) or a salt thereof wherein a reducing agent is reacted with a compound represented by general formula II: (in the formula, R1, R2, R3, R4, R5, R6, m, and ring A′ are as defined in the specification).

公开(公告)号：US20240409919A1

公开(公告)日：2024-12-12

申请号：US18733430

申请日：2024-06-04

Applicant: SHIMADZU CORPORATION ,  OSAKA UNIVERSITY

Inventor： Satoshi OBIKA ,  Takao YAMAGUCHI ,  Momoka HAYASHIDA ,  Junichi MASUDA ,  Shinosuke HORIE ,  Risa SUZUKI

IPC: C12N15/10 ,  B01D15/40

Abstract: A method for separating components using a supercritical fluid chromatograph, including: injecting a sample into a mobile phase containing a supercritical fluid and a modifier to introduce the sample into a column; and separating components in the sample during passing through the column; wherein the sample contains an oligonucleotide as a target component; the supercritical fluid contains carbon dioxide; and the modifier contains a solution containing at least one selected from the group consisting of ammonium, an alkylamine, and an amino alcohol, and an acid.

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：US20220169671A1

公开(公告)日：2022-06-02

申请号：US17667988

申请日：2022-02-09

Applicant: Osaka University

Inventor： Satoshi OBIKA ,  Kosuke ITO ,  Takaki HABUCHI ,  Masahiko HORIBA

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

Abstract: 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：US20210317459A1

公开(公告)日：2021-10-14

申请号：US17250806

申请日：2019-09-04

Applicant: OSAKA UNIVERSITY ,  NATIONAL INSTITUTES OF BIOMEDICAL INNOVATION, HEALTH AND NUTRITION ,  NATIONAL UNIVERSITY CORPORATION KOBE UNIVERSITY

Inventor： Akira KIKUCHI ,  Shinji MATSUMOTO ,  Satoshi OBIKA ,  Yuya KASAHARA ,  Takumi FUKUMOTO

IPC: C12N15/113 ,  A61P35/04

Abstract: The purpose of the present invention is to provide an antisense oligonucleotide that targets an ARL4C molecule and exerts an antitumor effect in vivo, and a nucleic acid drug using the antisense oligonucleotide. An antisense oligonucleotide that has a base sequence consisting of at least 10 consecutive bases contained in the base sequence represented by SEQ ID NO: 1. This antisense oligonucleotide targets an ARL4C molecule and thus can inhibit the expression of ARL4C in a tumor cell in vitro and suppress the migration and proliferation thereof. When systemically administered, moreover, the antisense oligonucleotide can exert an excellent antitumor effect in vivo too.

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：US20200055890A1

公开(公告)日：2020-02-20

申请号：US16487785

申请日：2018-02-20

Applicant: Osaka University

Inventor： Satoshi OBIKA ,  Kosuke ITO ,  Takaaki HABUCHI ,  Masahiko HORIBA

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

Abstract: 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：US20250136613A1

公开(公告)日：2025-05-01

申请号：US18835370

申请日：2022-11-04

Applicant: Osaka University

Inventor： Satoshi OBIKA ,  Osamu NAKAGAWA ,  Ryohei YAMAJI ,  Haruhiko KAMADA ,  Taisuke NAKAYAMA

IPC: C07D498/04 ,  A61K47/54 ,  C07F9/6561 ,  C07H19/23

Abstract: A compound or a pharmaceutically acceptable salt thereof according to the present invention has a structure represented by Formula (I) and can form a ligand for a drug delivery system formulation. The drug delivery system formulation according to the present invention can improve, for example, an ability to make a delivery to the skeletal muscle.