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：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。

公开(公告)号：US20240240183A1

公开(公告)日：2024-07-18

申请号：US18563128

申请日：2022-05-24

Applicant: NATIONAL UNIVERSITY CORPORATION TOKYO MEDICAL AND DENTAL UNIVERSITY ,  OSAKA UNIVERSITY

Inventor： Takanori YOKOTA ,  Tetsuya NAGATA ,  Kotaro YOSHIOKA ,  Satoshi OBIKA

IPC: C12N15/113 ,  A61K9/00 ,  A61P29/00 ,  A61P37/06

CPC classification number: C12N15/113 ,  A61K9/0019 ,  A61P29/00 ,  A61P37/06 ,  C12N2310/11 ,  C12N2310/321 ,  C12N2310/341 ,  C12N2310/343 ,  C12N2320/30

Abstract: A problem to be solved by the present invention is to provide a double-stranded nucleic acid complex having a reduced toxicity whose effectiveness is not impaired. Provided is a double-stranded nucleic acid complex comprising a first nucleic acid strand and a second nucleic acid strand, wherein: said first nucleic acid strand is capable of hybridizing to at least part of a target gene or a transcription product thereof, and has an antisense effect on said target gene or transcription product thereof, said second nucleic acid strand comprises a base sequence complementary to said first nucleic acid strand, and said first nucleic acid strand and/or said second nucleic acid strand comprises at least one bridged non-natural nucleoside represented by formula (I) or formula (II) (wherein R represents a hydrogen atom or a methyl group).

公开(公告)号：US20230159924A1

公开(公告)日：2023-05-25

申请号：US17905442

申请日：2021-03-02

Applicant: MITSUBISHI TANABE PHARMA CORPORATION ,  KYOTO UNIVERSITY ,  OSAKA UNIVERSITY ,  NATIONAL INSTITUTES OF BIOMEDICAL INNOVATION, HEALTH AND NUTRITION

Inventor： Jun KOTERA ,  Koh ONO ,  Takahiro HORIE ,  Tomohiro YAMASAKI ,  Satoshi KOYAMA ,  Satoshi OBIKA ,  Yuya KASAHARA

IPC: C12N15/113 ,  A61P9/00

CPC classification number: C12N15/113 ,  A61P9/00 ,  C12N2310/11 ,  C12N2310/32 ,  C12N2310/3341 ,  C12N2310/315

Abstract: A prophylactic or therapeutic agent for an aneurysm comprising a miR-33b inhibiting substance, preferably an antisense oligonucleotide against miR-33b, as an active ingredient.

公开(公告)号：US20230113556A1

公开(公告)日：2023-04-13

申请号：US17907323

申请日：2021-03-26

Applicant: NATIONAL CEREBRAL AND CARDIOVASCULAR CENTER ,  OSAKA UNIVERSITY

Inventor： Mariko SHIBA ,  Tsuyoshi YAMAMOTO ,  Fumito WADA ,  Tadayuki KOBAYASHI ,  Keisuke TACHIBANA ,  Satoshi OBIKA

IPC: C12N15/113 ,  A61P3/06

Abstract: The present invention provides an antisense oligomer having the base sequence depicted in SEQ ID NO: 26, an antisense oligomer having a base sequence resulting from substitution, deletion, insertion, or addition of 1 to 6 bases in the base sequence depicted in SEQ ID NO: 26, a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable hydrate thereof, an oligonucleotide conjugate in which the antisense oligomer is bound with a molecule capable of binding to an asialoglycoprotein receptor, and a pharmaceutical composition containing the same.

公开(公告)号：US20200172903A1

公开(公告)日：2020-06-04

申请号：US16616743

申请日：2018-07-03

Applicant: OSAKA UNIVERSITY ,  DAIICHI SANKYO COMPANY, LIMITED

Inventor： Masayuki NAKAMORI ,  Hideki MOCHIZUKI ,  Satoshi OBIKA ,  Makoto KOIZUMI ,  Akifumi NAKAMURA ,  Kiyosumi TAKAISHI ,  Yumiko ASAHI

IPC: C12N15/113 ,  A61P25/16 ,  A61P25/28

Abstract: The objective of the present invention is to provide nucleic acid therapeutics which exhibits more excellent effect and which shows a substantivity for a prolonged period to suppress an expression of α-synuclein. The oligonucleotide or a pharmacologically acceptable salt thereof according to the present invention is characterized in comprising at least one 2′-O,4′-C-ethylene nucleoside, wherein the oligonucleotide can hybridize with α-synuclein gene, has an activity to suppress an expression of the α-synuclein gene, and is complementary to the α-synuclein gene, 5′ end of the oligonucleotide is a nucleotide complementary to the specific nucleotide, the oligonucleotide is complementary to at least a part of SEQ ID NO: 1, and the oligonucleotide has a length of 13 or more and 15 or less nucleotides.

公开(公告)号：US20190008886A1

公开(公告)日：2019-01-10

申请号：US16068163

申请日：2017-01-05

Applicant: OSAKA UNIVERSITY ,  NATIONAL UNIVERSITY CORPORATION TOKYO MEDICAL AND DENTAL UNIVERSITY ,  NATIONAL INSTITUTES OF BIOMEDICAL INNOVATION, HEALTH AND NUTRITION

Inventor： Masayuki NAKAMORI ,  Hideki MOCHIZUKI ,  Satoshi OBIKA ,  Takanori YOKOTA ,  Tetuya NAGATA ,  Yuya KASAHARA

IPC: A61K31/712 ,  C12N15/113 ,  C07K14/47 ,  A61P25/28 ,  A61P25/16

Abstract: The present invention can provide a nucleic acid medicine which has a higher effect and a more prolonged effect of inhibiting the expression of α-synudein can be provided. Disclosed is the oligonucleotide or a pharmacologically acceptable salt thereof, the oligonucleotide containing at least one nucleoside structure represented by Formula (I): (where each of Base and A are defined substituent or structure), can bind to an α-synudein gene, has activity for inhibiting expression of the α-synudein gene, and is complementary to the α-synudein gene, and the oligonucleotide has a length of twelve to twenty bases.

公开(公告)号：US20240240176A1

公开(公告)日：2024-07-18

申请号：US18288887

申请日：2022-04-28

Applicant: KYOTO UNIVERSITY ,  OSAKA UNIVERSITY ,  MITSUBISHI TANABE PHARMA CORPORATION ,  NATIONAL INSTITUTES OF BIOMEDICAL INNOVATION, HEALTH AND NUTRITION

Inventor： Jun KOTERA ,  Koh ONO ,  Takahiro HORIE ,  Naoya SOWA ,  Yuya IDE ,  Satoshi OBIKA ,  Yuya KASAHARA

IPC: C12N15/113 ,  A61P21/00

CPC classification number: C12N15/113 ,  A61P21/00 ,  C12N2310/11 ,  C12N2310/14 ,  C12N2310/323 ,  C12N2310/531

Abstract: A prophylactic or therapeutic agent for a myopathy, including a miR-33b inhibitor, preferably an antisense oligonucleotide against miR-33b, as an effective component.

公开(公告)号：US20240148775A1

公开(公告)日：2024-05-09

申请号：US18547071

申请日：2022-02-25

Applicant: Osaka University

Inventor： Masahito SHIMOJO ,  Satoshi OBIKA ,  Keishiro MISHIMA ,  Misa YOSHIDA

IPC: A61K31/713 ,  A61P35/00 ,  C12N15/113

CPC classification number: A61K31/713 ,  A61P35/00 ,  C12N15/113

Abstract: An oligonucleotide or a pharmacologically acceptable salt thereof according to the present invention contains a nucleotide sequence complementary to a continuous sequence of at least 12 bases in a target region constituted by a base sequence of SEQ ID No. 1, and induces N-exon skipping in human REST pre-mRNA processing. Such oligonucleotides are useful for manufacturing medicines for treatment of cancer, for example.

公开(公告)号：US20220177509A1

公开(公告)日：2022-06-09

申请号：US17601326

申请日：2020-03-31

Applicant: NIPPON SHOKUBAI CO., LTD. ,  OSAKA UNIVERSITY

Inventor： Takeshi BABA ,  Hiroshi OKAMOTO ,  Yumi NOMURA ,  Satoshi OBIKA ,  Takao YAMAGUCHI

IPC: C07H19/16 ,  C07H19/06 ,  C07H1/00

Abstract: Provided is a method for producing a compound represented by formula (III) from a compound represented by formula (I) as a starting material.