DK3455232T3 - Forbedret kobling af stereodefinerede oxazaphospholidin-phosphoramidit-monomerer til nukleosid eller oligonukleotid - Google Patents

Forbedret kobling af stereodefinerede oxazaphospholidin-phosphoramidit-monomerer til nukleosid eller oligonukleotid Download PDF

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Publication number
DK3455232T3
DK3455232T3 DK17725886.0T DK17725886T DK3455232T3 DK 3455232 T3 DK3455232 T3 DK 3455232T3 DK 17725886 T DK17725886 T DK 17725886T DK 3455232 T3 DK3455232 T3 DK 3455232T3
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Denmark
Prior art keywords
stereodefined
oxazaphospholidine
nucleoside
oligonucleotide
improved coupling
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Application number
DK17725886.0T
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English (en)
Inventor
Jacob Ravn
Erik Funder
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Roche Innovation Ct Copenhagen As
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Publication of DK3455232T3 publication Critical patent/DK3455232T3/da

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    • 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
    • C07H19/06Pyrimidine 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
    • C07H19/06Pyrimidine 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
    • C07H19/16Purine 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
    • C07H19/20Purine radicals with the saccharide radical esterified by phosphoric or polyphosphoric 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

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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)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
DK17725886.0T 2016-05-12 2017-05-09 Forbedret kobling af stereodefinerede oxazaphospholidin-phosphoramidit-monomerer til nukleosid eller oligonukleotid DK3455232T3 (da)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
EP16169429 2016-05-12
EP17163513 2017-03-29
EP17163604 2017-03-29
PCT/EP2017/060985 WO2017194498A1 (en) 2016-05-12 2017-05-09 Enhanced coupling of stereodefined oxazaphospholidine phosphoramidite monomers to nucleoside or oligonucleotide

Publications (1)

Publication Number Publication Date
DK3455232T3 true DK3455232T3 (da) 2020-07-06

Family

ID=58772850

Family Applications (1)

Application Number Title Priority Date Filing Date
DK17725886.0T DK3455232T3 (da) 2016-05-12 2017-05-09 Forbedret kobling af stereodefinerede oxazaphospholidin-phosphoramidit-monomerer til nukleosid eller oligonukleotid

Country Status (6)

Country Link
US (1) US11261209B2 (da)
EP (1) EP3455232B1 (da)
JP (1) JP7097820B2 (da)
CN (1) CN109311925B (da)
DK (1) DK3455232T3 (da)
WO (1) WO2017194498A1 (da)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
CN103796657B (zh) 2011-07-19 2017-07-11 波涛生命科学有限公司 合成官能化核酸的方法
PL2872485T3 (pl) 2012-07-13 2021-05-31 Wave Life Sciences Ltd. Asymetryczna grupa pomocnicza
KR102213609B1 (ko) 2012-07-13 2021-02-08 웨이브 라이프 사이언시스 리미티드 키랄 제어
JPWO2015108047A1 (ja) 2014-01-15 2017-03-23 株式会社新日本科学 免疫誘導活性を有するキラル核酸アジュバンド及び免疫誘導活性剤
JPWO2015108048A1 (ja) 2014-01-15 2017-03-23 株式会社新日本科学 抗腫瘍作用を有するキラル核酸アジュバンド及び抗腫瘍剤
BR112016016400A2 (pt) 2014-01-16 2017-10-03 Wave Life Sciences Ltd Composições de oligonucleotídeos quiralmente controlados, seu uso, sua composição farmacêutica, e métodos
KR20190135494A (ko) * 2017-03-29 2019-12-06 로슈 이노베이션 센터 코펜하겐 에이/에스 입체한정된 포스포로티오에이트 올리고뉴클레오티드의 제조를 위한 직교 보호기
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
US12421268B2 (en) 2019-04-16 2025-09-23 Roche Innovation Center Copenhagen A/S Process for preparing nucleotide P(V) monomers
EP4047004B1 (en) * 2019-10-18 2024-03-06 FUJIFILM Wako Pure Chemical Corporation Phosphoramidite activator
IL293327B2 (en) * 2019-11-27 2026-04-01 Alnylam Pharmaceuticals Inc Synthesis of 3'-RNA oligonucleotides
CN112898363B (zh) * 2021-01-25 2024-06-04 苏州金唯智生物科技有限公司 一种亚磷酰胺单体组合物及其制备方法和应用

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
JP2009536222A (ja) * 2006-05-05 2009-10-08 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 Pcsk9の発現を調節するための化合物および方法
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
KR102213609B1 (ko) * 2012-07-13 2021-02-08 웨이브 라이프 사이언시스 리미티드 키랄 제어
PL2872485T3 (pl) * 2012-07-13 2021-05-31 Wave Life Sciences Ltd. Asymetryczna grupa pomocnicza
PL231078B1 (pl) * 2012-08-05 2019-01-31 Inst Chemii Bioorganicznej Polskiej Akademii Nauk Sposób syntezy polifosforanów
AU2015217221A1 (en) * 2014-02-13 2016-08-11 Ligand Pharmaceuticals, Inc. Prodrug compounds and their uses

Also Published As

Publication number Publication date
JP2019514999A (ja) 2019-06-06
WO2017194498A1 (en) 2017-11-16
US11261209B2 (en) 2022-03-01
EP3455232B1 (en) 2020-05-06
CN109311925A (zh) 2019-02-05
CN109311925B (zh) 2022-06-03
EP3455232A1 (en) 2019-03-20
JP7097820B2 (ja) 2022-07-08
US20190153012A1 (en) 2019-05-23

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