5'-MODIFIED NUCLEOSIDE AND NUCLEOTIDE USING SAME

Title:

5'-MODIFIED NUCLEOSIDE AND NUCLEOTIDE USING SAME

Document Type and Number:

WIPO Patent Application WO/2023/167094

Kind Code:

A1

Abstract:

Disclosed are a 5'-modified nucleoside and a nucleotide using the same. The nucleoside of the present invention is a compound represented by formula (I) or a salt thereof. The nucleoside of the present invention has suitable duplex-forming ability for a target RNA and excellent nuclease resistance and can be produced efficiently without requiring a diastereomer separation operation in its synthesis pathway. The nucleoside of the present invention is usable as a substitute for a phosphorothioate-modified nucleic acid with concerns of accumulation in a specific organ, etc. Moreover, this nucleoside has high industrial productivity.

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Inventors:

OBIKA SATOSHI (JP)
YAMAGUCHI TAKAO (JP)
SAKAUE SHIORI (JP)
INOUE TAKAO (JP)
YOSHIDA TOKUYUKI (JP)

Application Number:

PCT/JP2023/006672

Publication Date:

September 07, 2023

Filing Date:

February 24, 2023

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Assignee:

UNIV OSAKA (JP)
JAPAN AS REPRESENTED BY DIRECTOR GENERAL OF NAT INSTITUTE OF HEALTH SCIENCES (JP)

International Classes:

C07H19/073; A61K9/06; A61K9/08; A61K31/7088; A61K48/00; A61P21/00; A61P21/04; A61P31/12; A61P35/00; A61P43/00; C07H19/10; C07H19/173; C07H21/04; C12N5/10; C12N15/10; C12N15/11; C12N15/113

Domestic Patent References:

WO2021167029A1	2021-08-26
WO2020158910A1	2020-08-06
WO2022004388A1	2022-01-06

Other References:

ALEXANDER V. KEL′IN, IVAN ZLATEV, JOEL HARP, MUTHUSAMY JAYARAMAN, ANNA BISBE, JONATHAN O′SHEA, NATE TANEJA, RAJAR M. M: "Structural Basis of Duplex Thermodynamic Stability and Enhanced Nuclease Resistance of 5′- C -Methyl Pyrimidine-Modified Oligonucleotides", THE JOURNAL OF ORGANIC CHEMISTRY, AMERICAN CHEMICAL SOCIETY, vol. 81, no. 6, 18 March 2016 (2016-03-18), pages 2261 - 2279, XP055737137, ISSN: 0022-3263, DOI: 10.1021/acs.joc.5b02375

Attorney, Agent or Firm:

NAKAMICHI, Yoshihiro (JP)

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