CN104768964B - 具有胍桥的人工核苷和寡核苷酸 - Google Patents

具有胍桥的人工核苷和寡核苷酸 Download PDF

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CN104768964B
CN104768964B CN201380057335.0A CN201380057335A CN104768964B CN 104768964 B CN104768964 B CN 104768964B CN 201380057335 A CN201380057335 A CN 201380057335A CN 104768964 B CN104768964 B CN 104768964B
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carbon atoms
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nucleic acid
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CN104768964A (zh
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小比贺聪
寿悠太朗
胁玲子
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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)
  • Veterinary Medicine (AREA)
CN201380057335.0A 2012-09-21 2013-09-19 具有胍桥的人工核苷和寡核苷酸 Active CN104768964B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
JP2012208906 2012-09-21
JP2012-208906 2012-09-21
JP2013022360 2013-02-07
JP2013-022360 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

Publications (2)

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CN104768964A CN104768964A (zh) 2015-07-08
CN104768964B true CN104768964B (zh) 2017-03-29

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

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WO2014126229A1 (ja) * 2013-02-18 2014-08-21 塩野義製薬株式会社 含窒素複素環構造を有するヌクレオシド及びヌクレオチド
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
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
EP3587576A4 (en) 2017-02-21 2021-01-06 Osaka University ANTISENSE OLIGONUCLEIC ACID
US11286275B2 (en) 2017-02-21 2022-03-29 Osaka University Nucleic acid compound and oligonucleotide
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
IL272864B2 (en) 2017-08-31 2024-03-01 Mitsubishi Tanabe Pharma Corp Il-33 antagonist-containing therapeutic agent for endometriosis
CA3099778A1 (en) * 2018-05-10 2019-11-14 Nippon Shinyaku Co., Ltd. Method for preparing 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
WO2020050307A1 (ja) 2018-09-05 2020-03-12 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
US12338265B2 (en) 2018-11-12 2025-06-24 Mitsubishi Tanabe Pharma Corporation Crosslinked artificial nucleic acid ALNA
WO2020203896A1 (ja) 2019-03-29 2020-10-08 シスメックス株式会社 新規人工核酸、その製造方法及び用途
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
SG11202112741XA (en) 2019-05-31 2021-12-30 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
CN114008061B (zh) * 2019-06-20 2024-03-12 豪夫迈·罗氏有限公司 放射性标记的moem型寡核苷酸及其制备方法
JP7776420B2 (ja) 2020-05-12 2025-11-26 田辺三菱製薬株式会社 Ataxin 3発現を調節するための化合物、方法及び医薬組成物
CN116322706B (zh) 2020-09-25 2025-12-05 株式会社理真思 新人工核酸、其制造方法和用途
CN116507727A (zh) 2020-11-06 2023-07-28 住友制药株式会社 Rps25基因的表达和/或功能调节剂
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
TW202313975A (zh) 2021-05-28 2023-04-01 日商住友製藥股份有限公司 反義核酸
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
KR20240158340A (ko) * 2022-03-17 2024-11-04 알리고스 테라퓨틱스 인코포레이티드 변형 갭머 올리고머 및 이의 사용 방법
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 (https=) 2023-02-28 2024-09-06
JPWO2024185775A1 (https=) 2023-03-06 2024-09-12
JPWO2024257847A1 (https=) 2023-06-16 2024-12-19
US20250368996A1 (en) 2024-05-14 2025-12-04 Aligos Therapeutics, Inc. Modified antisense oligonucleotides for treating hepatitis b virus

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WO1996000575A1 (en) * 1994-06-30 1996-01-11 The Regents Of The University Of California Polynucleoside chain having multiple nucleosides, the nucleosides coupled by guanidyl linkages
CN1376161A (zh) * 1999-07-22 2002-10-23 三共株式会社 新型双环核苷类似物
CN102596983A (zh) * 2009-10-29 2012-07-18 国立大学法人大阪大学 交联型人工核苷和核苷酸

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Publication number Publication date
EP2899197B1 (en) 2017-03-22
EP2899197A1 (en) 2015-07-29
CA2885719A1 (en) 2014-03-27
KR20150056647A (ko) 2015-05-26
WO2014046212A1 (ja) 2014-03-27
CN104768964A (zh) 2015-07-08
IN2015DN02238A (https=) 2015-08-21
JP6048982B2 (ja) 2016-12-21
US20150266917A1 (en) 2015-09-24
EP2899197A4 (en) 2016-03-09
KR101707437B1 (ko) 2017-02-16
JPWO2014046212A1 (ja) 2016-08-18
US10377789B2 (en) 2019-08-13
CA2885719C (en) 2017-07-11
ES2622716T3 (es) 2017-07-07

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