JP7164540B2 - 立体的に規定されたホスホロチオエートオリゴヌクレオチドの調製のための直交保護基 - Google Patents

立体的に規定されたホスホロチオエートオリゴヌクレオチドの調製のための直交保護基 Download PDF

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JP7164540B2
JP7164540B2 JP2019553219A JP2019553219A JP7164540B2 JP 7164540 B2 JP7164540 B2 JP 7164540B2 JP 2019553219 A JP2019553219 A JP 2019553219A JP 2019553219 A JP2019553219 A JP 2019553219A JP 7164540 B2 JP7164540 B2 JP 7164540B2
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JP2020512360A (ja
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コンラッド ブライヒャー
エリク ダー フンダー
デニス ジュル ハンセン
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ロシュ イノベーション センター コペンハーゲン エーエス
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H21/00—Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
    • C07H21/02—Compounds 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H21/00—Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
    • C07H21/04—Compounds 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H1/00—Processes for the preparation of sugar derivatives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/06—Pyrimidine radicals
    • C07H19/10—Pyrimidine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids
    • Y—GENERAL 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
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Biochemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Biotechnology (AREA)
  • General Health & Medical Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Saccharide Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2019553219A 2017-03-29 2018-03-20 立体的に規定されたホスホロチオエートオリゴヌクレオチドの調製のための直交保護基 Active JP7164540B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP17163506.3 2017-03-29
EP17163506 2017-03-29
PCT/EP2018/057069 WO2018177825A1 (en) 2017-03-29 2018-03-20 Orthogonal protecting groups for the preparation of stereodefined phosphorothioate oligonucleotides

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JP2020512360A JP2020512360A (ja) 2020-04-23
JP2020512360A5 JP2020512360A5 (https=) 2021-04-08
JP7164540B2 true JP7164540B2 (ja) 2022-11-01

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JP2019553219A Active JP7164540B2 (ja) 2017-03-29 2018-03-20 立体的に規定されたホスホロチオエートオリゴヌクレオチドの調製のための直交保護基

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US (1) US11591362B2 (https=)
EP (1) EP3601309A1 (https=)
JP (1) JP7164540B2 (https=)
KR (1) KR20190135494A (https=)
CN (1) CN110475784B (https=)
WO (1) WO2018177825A1 (https=)

Families Citing this family (7)

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Publication number Priority date Publication date Assignee Title
WO2019002237A1 (en) * 2017-06-28 2019-01-03 Roche Innovation Center Copenhagen A/S METHOD OF MULTIPLE COUPLING AND OXIDATION
PT3717646T (pt) 2017-12-01 2025-07-28 Texas A & M Univ Sys Tratamento antisense da síndrome de angelman
EP3883941A1 (en) * 2018-11-22 2021-09-29 Roche Innovation Center Copenhagen A/S Pyridinium salts as activators in the synthesis of stereodefined oligonucleotides
CN113748116A (zh) 2019-03-20 2021-12-03 波涛生命科学有限公司 可用于寡核苷酸制备的技术
CN113661168A (zh) * 2019-04-16 2021-11-16 罗氏创新中心哥本哈根有限公司 用于制备核苷酸p(v)单体的新方法
CN116867795A (zh) * 2021-02-01 2023-10-10 第一三共株式会社 抗体－免疫刺激剂偶联物的新型制造方法
TW202241454A (zh) * 2021-02-01 2022-11-01 日商第一三共股份有限公司 抗體－免疫賦活化劑共軛物之新穎製造方法

Citations (1)

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Publication number Priority date Publication date Assignee Title
JP2015528002A (ja) 2012-07-13 2015-09-24 ウェイブ ライフ サイエンス プライベート リミテッド キラル制御

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US6465628B1 (en) 1999-02-04 2002-10-15 Isis Pharmaceuticals, Inc. Process for the synthesis of oligomeric compounds
US6492171B2 (en) 2000-05-16 2002-12-10 Isis Pharmaceuticals, Inc. Antisense modulation of TERT expression
WO2005092909A1 (ja) 2004-03-25 2005-10-06 Toudai Tlo, Ltd. 立体規則性の高いリボヌクレオチド類縁体及びデオキシリボヌクレオチド類縁体の製造法
JP5342881B2 (ja) 2006-01-27 2013-11-13 アイシス ファーマシューティカルズ， インコーポレーテッド ６−修飾された二環式核酸類似体
CA2648132C (en) 2006-04-03 2019-05-28 Santaris Pharma A/S Pharmaceutical composition comprising anti-mirna antisense oligonucleotides
EP2623599B1 (en) 2007-10-04 2019-01-02 Roche Innovation Center Copenhagen A/S Micromirs
DK2285819T3 (da) 2008-04-04 2013-12-02 Isis Pharmaceuticals Inc Oligomere forbindelser omfattende neutralt bundne, terminale bicykliske nukleosider
WO2010036698A1 (en) 2008-09-24 2010-04-01 Isis Pharmaceuticals, Inc. Substituted alpha-l-bicyclic nucleosides
RU2572826C2 (ru) * 2008-12-02 2016-01-20 Чиралджен, Лтд. Способ синтеза модифицированных по атому фосфора нуклеиновых кислот
CA2767253A1 (en) 2009-07-06 2011-01-13 Ontorii, Inc. Novel nucleic acid prodrugs and methods of use thereof
JP5868324B2 (ja) 2010-09-24 2016-02-24 株式会社Wave Life Sciences Japan 不斉補助基
WO2017157672A1 (en) 2016-03-18 2017-09-21 Roche Innovation Center Copenhagen A/S Acyl-protected l-lna-guanosine monomers
CN109311925B (zh) 2016-05-12 2022-06-03 罗氏创新中心哥本哈根有限公司 立体限定的氧杂氮杂磷杂环戊烷亚磷酰胺单体与核苷或寡核苷酸的增强的偶联
US10882884B2 (en) * 2016-05-18 2021-01-05 Eth Zurich Stereoselective synthesis of phosphorothioate oligoribonucleotides

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JP2015528002A (ja) 2012-07-13 2015-09-24 ウェイブ ライフ サイエンス プライベート リミテッド キラル制御

Non-Patent Citations (2)

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Title
OKA,N. et al，Solid-Phase Synthesis of Stereoregular Oligodeoxyribonucleoside Phosphorothioates Using Bicyclic Oxazaphospholidine Derivatives as Monomer Units，Journal of the American Chemical Society，2008年，Vol.130, No.47，p.16031-16037
Protective Groups in Organic Synthesis FIFTH Edition，2014年，pp.895-899, 907-921

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Publication number Publication date
JP2020512360A (ja) 2020-04-23
CN110475784A (zh) 2019-11-19
US11591362B2 (en) 2023-02-28
KR20190135494A (ko) 2019-12-06
US20210179658A1 (en) 2021-06-17
CN110475784B (zh) 2024-07-16
EP3601309A1 (en) 2020-02-05
WO2018177825A1 (en) 2018-10-04

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