JP6048982B2 - グアニジン架橋を有する人工ヌクレオシドおよびオリゴヌクレオチド - Google Patents

グアニジン架橋を有する人工ヌクレオシドおよびオリゴヌクレオチド Download PDF

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JP6048982B2
JP6048982B2 JP2014536921A JP2014536921A JP6048982B2 JP 6048982 B2 JP6048982 B2 JP 6048982B2 JP 2014536921 A JP2014536921 A JP 2014536921A JP 2014536921 A JP2014536921 A JP 2014536921A JP 6048982 B2 JP6048982 B2 JP 6048982B2
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carbon atoms
nucleic acid
oxo
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JPWO2014046212A1 (ja
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聡 小比賀
聡 小比賀
悠太朗 壽
悠太朗 壽
玲子 脇
玲子 脇
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University of Osaka NUC
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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
    • C07H19/10Pyrimidine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids
    • 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
    • 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
    • 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
    • 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
    • C07H21/04Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with deoxyribosyl as saccharide radical
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H23/00Compounds containing boron, silicon or a metal, e.g. chelates or vitamin B12
    • 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
    • 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)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Engineering & Computer Science (AREA)
  • Biotechnology (AREA)
  • General Health & Medical Sciences (AREA)
  • Wood Science & Technology (AREA)
  • Biomedical Technology (AREA)
  • General Engineering & Computer Science (AREA)
  • Zoology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Microbiology (AREA)
  • Physics & Mathematics (AREA)
  • Biophysics (AREA)
  • Plant Pathology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
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JP2014536921A 2012-09-21 2013-09-19 グアニジン架橋を有する人工ヌクレオシドおよびオリゴヌクレオチド Active JP6048982B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
JP2012208906 2012-09-21
JP2012208906 2012-09-21
JP2013022360 2013-02-07
JP2013022360 2013-02-07
PCT/JP2013/075370 WO2014046212A1 (ja) 2012-09-21 2013-09-19 グアニジン架橋を有する人工ヌクレオシドおよびオリゴヌクレオチド

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JPWO2014046212A1 JPWO2014046212A1 (ja) 2016-08-18
JP6048982B2 true JP6048982B2 (ja) 2016-12-21

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Country Status (9)

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US (1) US10377789B2 (enExample)
EP (1) EP2899197B1 (enExample)
JP (1) JP6048982B2 (enExample)
KR (1) KR101707437B1 (enExample)
CN (1) CN104768964B (enExample)
CA (1) CA2885719C (enExample)
ES (1) ES2622716T3 (enExample)
IN (1) IN2015DN02238A (enExample)
WO (1) WO2014046212A1 (enExample)

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US9315535B2 (en) 2013-02-18 2016-04-19 Shionogi & Co., Ltd. Nucleoside and nucleotide having nitrogen-containing heterocycle structure
TW201718618A (zh) * 2015-09-18 2017-06-01 田邊三菱製藥股份有限公司 架橋型核酸GuNA,其製造方法,及中間體化合物
US11234995B2 (en) 2016-01-07 2022-02-01 Osaka University α-synuclein expression inhibitor
EP3587432A4 (en) 2017-02-21 2021-01-06 Osaka University NUCLEIC ACID COMPOUND AND OLIGONUCLEOTIDE
US11261440B2 (en) 2017-02-21 2022-03-01 Osaka University Antisense oligonucleic acid
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
CN115920032A (zh) 2017-08-31 2023-04-07 田边三菱制药株式会社 含有il-33拮抗剂的子宫内膜异位症治疗剂
EP3792269A4 (en) * 2018-05-10 2022-06-22 Nippon Shinyaku Co., Ltd. PROCESS FOR PREPARING AN OLIGONUCLEIC ACID COMPOUND
JP7473113B2 (ja) * 2018-07-31 2024-04-23 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
JP7396577B2 (ja) 2018-09-05 2023-12-12 国立大学法人大阪大学 Arl4cを標的分子とするアンチセンスオリゴヌクレオチド、及び当該アンチセンスオリゴヌクレオチドを使用した核酸医薬
EP3881851A4 (en) 2018-11-12 2023-02-15 Mitsubishi Tanabe Pharma Corporation CROSSLINKED ARTIFICIAL NUCLEIC ACID ALNA
WO2020203880A1 (ja) 2019-03-29 2020-10-08 田辺三菱製薬株式会社 Dux4の発現を調節するための化合物、方法及び医薬組成物
EP3967328A4 (en) 2019-03-29 2022-12-28 Sysmex Corporation NEW ARTIFICIAL NUCLEIC ACID, METHOD FOR MAKING IT, AND USE THEREOF
US11466274B2 (en) 2019-05-31 2022-10-11 Aligos Therapeutics, Inc. Modified gapmer oligonucleotides and methods of use
KR102899410B1 (ko) * 2019-06-19 2025-12-12 야마사 쇼유 가부시키가이샤 가교형 뉴클레오시드 중간체의 결정 및 그의 제조 방법, 그리고 가교형 뉴클레오시드 아미다이트의 제조 방법
CA3140410A1 (en) * 2019-06-20 2020-12-24 Martin Edelmann Radiolabeled moem type oligonucleotides and process for their preparation
CN115667513A (zh) 2020-05-12 2023-01-31 田边三菱制药株式会社 用于调节Ataxin 3表达的化合物、方法和药物组合物
EP4219517A4 (en) 2020-09-25 2024-09-25 Riken Genesis Co., Ltd. NOVEL ARTIFICIAL NUCLEIC ACID, METHOD FOR PRODUCING THE SAME AND USE THEREOF
EP4252846A4 (en) 2020-11-06 2025-12-03 Sumitomo Pharma Co Ltd REGULATOR FOR THE EXPRESSION AND/OR FUNCTION OF THE RPS25 GENE
US20240148775A1 (en) 2021-02-25 2024-05-09 Osaka University Oligonucleotide for inducing n-exon skipping during rest mrna precursor processing
JP2024105742A (ja) * 2021-05-26 2024-08-07 ルクサナバイオテク株式会社 心疾患治療薬
EP4349987A1 (en) 2021-05-28 2024-04-10 Sumitomo Pharma Co., Ltd. Antisense nucleic acid
CN113552198B (zh) * 2021-05-31 2024-03-26 武汉维尔博生物科技有限公司 一种基于高响应葡萄糖适配体的电化学传感器及其制备方法
US20240390508A1 (en) 2021-08-21 2024-11-28 Takeda Pharmaceutical Company Limited Human transferrin receptor binding peptide-drug conjugate
WO2023093960A1 (en) * 2021-11-26 2023-06-01 Syddansk Universitet Modified peptide-oligonucleotide conjugate
EP4458836A4 (en) 2021-12-27 2025-05-21 Riken Genesis Co., Ltd. Novel artificial nucleic acid, method for producing same, and use of same
AU2023236560A1 (en) * 2022-03-17 2024-10-03 Aligos Therapeutics, Inc. Modified gapmer oligomers and methods of use thereof
WO2024101446A1 (ja) 2022-11-10 2024-05-16 ルクサナバイオテク株式会社 架橋部にグアニジノ構造を有する修飾ヌクレオシドおよびそれを用いたオリゴヌクレオチドの製造方法
JPWO2024181416A1 (enExample) 2023-02-28 2024-09-06
EP4678626A1 (en) 2023-03-06 2026-01-14 Spera Pharma, Inc. Long-chain alkenyloxy-substituted benzoyl derivative and oligonucleotide synthesis method using same
WO2024257847A1 (ja) 2023-06-16 2024-12-19 住友ファーマ株式会社 Rps25遺伝子の発現及び/又はその機能を調節するアンチセンスオリゴヌクレオチド
WO2025240506A1 (en) 2024-05-14 2025-11-20 Aligos Therapeutics, Inc. Modified antisense oligonucleotides for treating hepatitis b virus

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Also Published As

Publication number Publication date
EP2899197B1 (en) 2017-03-22
KR20150056647A (ko) 2015-05-26
CA2885719A1 (en) 2014-03-27
EP2899197A4 (en) 2016-03-09
WO2014046212A1 (ja) 2014-03-27
CN104768964B (zh) 2017-03-29
IN2015DN02238A (enExample) 2015-08-21
CA2885719C (en) 2017-07-11
CN104768964A (zh) 2015-07-08
JPWO2014046212A1 (ja) 2016-08-18
ES2622716T3 (es) 2017-07-07
US10377789B2 (en) 2019-08-13
EP2899197A1 (en) 2015-07-29
KR101707437B1 (ko) 2017-02-16
US20150266917A1 (en) 2015-09-24

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