CN110475784B - 用于制备立体限定硫代磷酸酯寡核苷酸的正交保护基 - Google Patents

用于制备立体限定硫代磷酸酯寡核苷酸的正交保护基 Download PDF

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Publication number
CN110475784B
CN110475784B CN201880022722.3A CN201880022722A CN110475784B CN 110475784 B CN110475784 B CN 110475784B CN 201880022722 A CN201880022722 A CN 201880022722A CN 110475784 B CN110475784 B CN 110475784B
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alkyl
aryl
amine
chiral auxiliary
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CN110475784A (zh
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K·布莱谢尔
E·D·丰德
D·J·汉森
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Roche Innovation Center Copenhagen AS
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Roche Innovation Center Copenhagen AS
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    • 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
    • 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
    • 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)
CN201880022722.3A 2017-03-29 2018-03-20 用于制备立体限定硫代磷酸酯寡核苷酸的正交保护基 Active CN110475784B (zh)

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

Publications (2)

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CN110475784A CN110475784A (zh) 2019-11-19
CN110475784B true CN110475784B (zh) 2024-07-16

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

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* Cited by examiner, † Cited by third party
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
KR102723989B1 (ko) 2017-12-01 2024-11-01 더 텍사스 에이 & 엠 유니버시티 시스템 엔젤만 증후군 안티센스 치료
WO2020104492A1 (en) * 2018-11-22 2020-05-28 Roche Innovation Center Copenhagen A/S Pyridinium salts as activators in the synthesis of stereodefined oligonucleotides
JP2022525541A (ja) 2019-03-20 2022-05-17 ウェイブ ライフ サイエンシズ リミテッド オリゴヌクレオチド調製に有用な技術
US12421268B2 (en) * 2019-04-16 2025-09-23 Roche Innovation Center Copenhagen A/S Process for preparing nucleotide P(V) monomers
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
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

Citations (1)

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CN104661664A (zh) * 2012-07-13 2015-05-27 威尔生命科学私人有限公司 手性控制

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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
WO2007090071A2 (en) 2006-01-27 2007-08-09 Isis Pharmaceuticals, Inc. 6-modified bicyclic nucleic acid analogs
EP2007888A2 (en) 2006-04-03 2008-12-31 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
US9290534B2 (en) 2008-04-04 2016-03-22 Ionis Pharmaceuticals, Inc. Oligomeric compounds having at least one neutrally linked terminal bicyclic nucleoside
DK2356129T3 (da) 2008-09-24 2013-05-13 Isis Pharmaceuticals Inc Substituerede alpha-L-bicykliske nukleosider
CN102282155B (zh) 2008-12-02 2017-06-09 日本波涛生命科学公司 磷原子修饰的核酸的合成方法
RU2612521C2 (ru) * 2009-07-06 2017-03-09 Онтории, Инк. Новые пролекарства нуклеиновых кислот и способы их применения
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
EP3455232B1 (en) * 2016-05-12 2020-05-06 Roche Innovation Center Copenhagen A/S Enhanced coupling of stereodefined oxazaphospholidine phosphoramidite monomers to nucleoside or oligonucleotide
EP3458464B1 (en) * 2016-05-18 2026-04-15 ETH Zurich Stereoselective synthesis of phosphorothioate oligoribonucleotides

Patent Citations (1)

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Publication number Priority date Publication date Assignee Title
CN104661664A (zh) * 2012-07-13 2015-05-27 威尔生命科学私人有限公司 手性控制

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Solid-Phase Synthesis of Stereoregular Oligodeoxyribonucleoside Phosphorothioates Using Bicyclic Oxazaphospholidine Derivatives as Monomer Units;Natsuhisa Oka, et al.;《Journal of the American Chemical Society》;20081231;第130卷(第47期);第16031-16037 *

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WO2018177825A1 (en) 2018-10-04
US11591362B2 (en) 2023-02-28
JP2020512360A (ja) 2020-04-23
CN110475784A (zh) 2019-11-19
JP7164540B2 (ja) 2022-11-01
US20210179658A1 (en) 2021-06-17
EP3601309A1 (en) 2020-02-05
KR20190135494A (ko) 2019-12-06

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