JP7678994B2 - 架橋型ヌクレオシドおよびそれを用いたヌクレオチド - Google Patents

架橋型ヌクレオシドおよびそれを用いたヌクレオチド Download PDF

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JP7678994B2
JP7678994B2 JP2022501990A JP2022501990A JP7678994B2 JP 7678994 B2 JP7678994 B2 JP 7678994B2 JP 2022501990 A JP2022501990 A JP 2022501990A JP 2022501990 A JP2022501990 A JP 2022501990A JP 7678994 B2 JP7678994 B2 JP 7678994B2
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group
carbon atoms
amino
nucleic acid
substituted
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JPWO2021167029A1 (https=
Inventor
聡 小比賀
卓男 山口
飛々暉 小峯
隆也 杉浦
貴雄 井上
徳幸 吉田
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National Institute of Health Sciences
University of Osaka NUC
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Osaka University NUC
National Institute of Health Sciences
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/06Pyrimidine radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H21/00Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
    • C07H21/02Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with ribosyl as saccharide radical
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H1/00Processes for the preparation of sugar derivatives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/16Purine radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H21/00Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12NMICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N15/00Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
    • C12N15/09Recombinant DNA-technology
    • C12N15/11DNA or RNA fragments; Modified forms thereof; Non-coding nucleic acids having a biological activity
    • C12N15/113Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides; Antisense DNA or RNA; Triplex- forming oligonucleotides; Catalytic nucleic acids, e.g. ribozymes; Nucleic acids used in co-suppression or gene silencing
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12NMICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N2310/00Structure or type of the nucleic acid
    • C12N2310/10Type of nucleic acid
    • C12N2310/11Antisense
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12NMICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N2310/00Structure or type of the nucleic acid
    • C12N2310/30Chemical structure
    • C12N2310/31Chemical structure of the backbone
    • C12N2310/315Phosphorothioates
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12NMICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N2310/00Structure or type of the nucleic acid
    • C12N2310/30Chemical structure
    • C12N2310/32Chemical structure of the sugar
    • C12N2310/323Chemical structure of the sugar modified ring structure
    • C12N2310/3231Chemical structure of the sugar modified ring structure having an additional ring, e.g. LNA, ENA
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00Technologies relating to chemical industry
    • Y02P20/50Improvements relating to the production of bulk chemicals
    • Y02P20/55Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • General Health & Medical Sciences (AREA)
  • Biomedical Technology (AREA)
  • General Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Wood Science & Technology (AREA)
  • Zoology (AREA)
  • Physics & Mathematics (AREA)
  • Biophysics (AREA)
  • Plant Pathology (AREA)
  • Microbiology (AREA)
  • Saccharide Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
JP2022501990A 2020-02-19 2021-02-18 架橋型ヌクレオシドおよびそれを用いたヌクレオチド Active JP7678994B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
JP2020026646 2020-02-19
JP2020026646 2020-02-19
PCT/JP2021/006222 WO2021167029A1 (ja) 2020-02-19 2021-02-18 架橋型ヌクレオシドおよびそれを用いたヌクレオチド

Publications (2)

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JPWO2021167029A1 JPWO2021167029A1 (https=) 2021-08-26
JP7678994B2 true JP7678994B2 (ja) 2025-05-19

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JP2022501990A Active JP7678994B2 (ja) 2020-02-19 2021-02-18 架橋型ヌクレオシドおよびそれを用いたヌクレオチド

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Country Link
US (1) US12606589B2 (https=)
EP (1) EP4108670A4 (https=)
JP (1) JP7678994B2 (https=)
CN (1) CN115151555B (https=)
WO (1) WO2021167029A1 (https=)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20250179109A1 (en) * 2022-03-01 2025-06-05 Osaka University 5'-modified nucleoside and nucleotide using same

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009006478A2 (en) 2007-07-05 2009-01-08 Isis Pharmaceuticals, Inc. 6-disubstituted bicyclic nucleic acid analogs
WO2015125783A1 (ja) 2014-02-18 2015-08-27 国立大学法人大阪大学 架橋型ヌクレオシドおよびヌクレオチド
WO2017119463A1 (ja) 2016-01-07 2017-07-13 国立大学法人大阪大学 α-シヌクレイン発現抑制剤
WO2018155451A1 (ja) 2017-02-21 2018-08-30 国立大学法人大阪大学 核酸化合物およびオリゴヌクレオチド
WO2019009298A1 (ja) 2017-07-05 2019-01-10 国立大学法人大阪大学 α-シヌクレイン発現抑制剤
WO2020027227A1 (ja) 2018-07-31 2020-02-06 国立大学法人大阪大学 オリゴヌクレオチドを含有する小細胞肺癌治療薬

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009006478A2 (en) 2007-07-05 2009-01-08 Isis Pharmaceuticals, Inc. 6-disubstituted bicyclic nucleic acid analogs
WO2015125783A1 (ja) 2014-02-18 2015-08-27 国立大学法人大阪大学 架橋型ヌクレオシドおよびヌクレオチド
WO2017119463A1 (ja) 2016-01-07 2017-07-13 国立大学法人大阪大学 α-シヌクレイン発現抑制剤
WO2018155451A1 (ja) 2017-02-21 2018-08-30 国立大学法人大阪大学 核酸化合物およびオリゴヌクレオチド
WO2019009298A1 (ja) 2017-07-05 2019-01-10 国立大学法人大阪大学 α-シヌクレイン発現抑制剤
WO2020027227A1 (ja) 2018-07-31 2020-02-06 国立大学法人大阪大学 オリゴヌクレオチドを含有する小細胞肺癌治療薬

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Publication number Publication date
CN115151555B (zh) 2026-03-17
CN115151555A (zh) 2022-10-04
EP4108670A4 (en) 2024-04-17
EP4108670A1 (en) 2022-12-28
WO2021167029A1 (ja) 2021-08-26
JPWO2021167029A1 (https=) 2021-08-26
US12606589B2 (en) 2026-04-21
US20230340008A1 (en) 2023-10-26

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