JP7235512B2 - キャッピング工程を有さないチオール化オリゴヌクレオチドの合成 - Google Patents

キャッピング工程を有さないチオール化オリゴヌクレオチドの合成 Download PDF

Info

Publication number
JP7235512B2
JP7235512B2 JP2018567264A JP2018567264A JP7235512B2 JP 7235512 B2 JP7235512 B2 JP 7235512B2 JP 2018567264 A JP2018567264 A JP 2018567264A JP 2018567264 A JP2018567264 A JP 2018567264A JP 7235512 B2 JP7235512 B2 JP 7235512B2
Authority
JP
Japan
Prior art keywords
formula
compound
oligonucleotide
agent
steps
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Active
Application number
JP2018567264A
Other languages
English (en)
Japanese (ja)
Other versions
JP2019518778A5 (https=
JP2019518778A (ja
Inventor
シー，シアーンリン
ヤン，ジミン
キースマン，ウィリアム・エフ
フィロン，ヤニック
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Biogen MA Inc
Original Assignee
Biogen MA Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Biogen MA Inc filed Critical Biogen MA Inc
Publication of JP2019518778A publication Critical patent/JP2019518778A/ja
Publication of JP2019518778A5 publication Critical patent/JP2019518778A5/ja
Application granted granted Critical
Publication of JP7235512B2 publication Critical patent/JP7235512B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • 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
    • 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
    • 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
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N15/00—Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
    • C12N15/09—Recombinant DNA-technology
    • C12N15/11—DNA or RNA fragments; Modified forms thereof; Non-coding nucleic acids having a biological activity
    • C12N15/113—Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides; Antisense DNA or RNA; Triplex- forming oligonucleotides; Catalytic nucleic acids, e.g. ribozymes; Nucleic acids used in co-suppression or gene silencing
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N2310/00—Structure or type of the nucleic acid
    • C12N2310/10—Type of nucleic acid
    • C12N2310/11—Antisense
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N2310/00—Structure or type of the nucleic acid
    • C12N2310/30—Chemical structure
    • C12N2310/34—Spatial arrangement of the modifications
    • C12N2310/341—Gapmers, i.e. of the type ===---===
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Genetics & Genomics (AREA)
  • Biotechnology (AREA)
  • General Health & Medical Sciences (AREA)
  • Biomedical Technology (AREA)
  • General Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Wood Science & Technology (AREA)
  • Zoology (AREA)
  • Physics & Mathematics (AREA)
  • Biophysics (AREA)
  • Plant Pathology (AREA)
  • Microbiology (AREA)
  • Saccharide Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
JP2018567264A 2016-06-24 2017-06-22 キャッピング工程を有さないチオール化オリゴヌクレオチドの合成 Active JP7235512B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662354433P 2016-06-24 2016-06-24
US62/354,433 2016-06-24
PCT/US2017/038643 WO2017223258A1 (en) 2016-06-24 2017-06-22 Synthesis of thiolated oligonucleotides without a capping step

Publications (3)

Publication Number Publication Date
JP2019518778A JP2019518778A (ja) 2019-07-04
JP2019518778A5 JP2019518778A5 (https=) 2020-07-30
JP7235512B2 true JP7235512B2 (ja) 2023-03-08

Family

ID=59276874

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2018567264A Active JP7235512B2 (ja) 2016-06-24 2017-06-22 キャッピング工程を有さないチオール化オリゴヌクレオチドの合成

Country Status (7)

Country Link
US (1) US11142545B2 (https=)
EP (1) EP3475292B1 (https=)
JP (1) JP7235512B2 (https=)
KR (2) KR102722183B1 (https=)
CN (1) CN109689668B (https=)
ES (1) ES2999138T3 (https=)
WO (1) WO2017223258A1 (https=)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR112017004056A2 (pt) 2014-09-12 2017-12-05 Biogen Ma Inc composições e métodos para detecção da proteína smn em um indivíduo e tratamento de um indivíduo
MA49555A (fr) 2017-07-10 2021-04-28 Geron Corp Procédé amélioré de préparation d'imetelstat
CN114072501A (zh) 2019-05-06 2022-02-18 马萨诸塞大学 抗c9orf72寡核苷酸及相关方法
CN110468171B (zh) * 2019-09-20 2021-10-29 凯莱英医药集团（天津）股份有限公司 核酸的合成方法
CR20220485A (es) 2020-02-28 2022-11-10 Ionis Pharmaceuticals Inc Compuestos y métodos para modular smn2
CN114685572B (zh) * 2022-06-02 2022-08-30 上海百力格生物技术有限公司 用于mgb核酸探针合成的氧化剂组合物及探针的合成方法
US20260001902A1 (en) 2022-09-19 2026-01-01 Bachem Holding Ag Improved oligonucleotide synthesis
KR20260049191A (ko) 2023-08-02 2026-04-13 닛토덴코 가부시키가이샤 올리고뉴클레오티드를 제조하는 방법
CN121729420A (zh) * 2023-08-14 2026-03-24 箭头药业股份有限公司 寡核苷酸合成方法
WO2025165064A1 (ko) * 2024-02-02 2025-08-07 에스티팜 주식회사 올리고뉴클레오티드 합성을 위한 개선된 방법
WO2025234897A1 (ru) * 2024-05-07 2025-11-13 Акционерное общество "ГЕНЕРИУМ" Способ получения тиофосфатных олигонуклеотидов для терапевтического применения
WO2025235761A1 (en) 2024-05-09 2025-11-13 Biogen Ma Inc. Reagents and processes for preparing oligonucleotides

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6087491A (en) * 1993-01-08 2000-07-11 Hybridon, Inc. Extremely high purity oligonucleotides and methods of synthesizing them using dimer blocks
US5614621A (en) * 1993-07-29 1997-03-25 Isis Pharmaceuticals, Inc. Process for preparing oligonucleotides using silyl-containing diamino phosphorous reagents
US6809195B1 (en) * 2000-08-16 2004-10-26 Isis Pharmaceuticals, Inc. Process for the preparation of oligonucleotides
EP1386925A1 (en) * 2002-07-31 2004-02-04 Girindus AG Method for preparing oligonucleotides
SI2548560T1 (sl) 2005-06-23 2015-12-31 Isis Pharmaceuticals, Inc. Sestavki in postopki za moduliranje izrezovanja smn2
PT3305302T (pt) 2009-06-17 2018-12-14 Biogen Ma Inc Composições e métodos de modulação de excisões de smn2 em um sujeito
US8642755B2 (en) * 2009-06-30 2014-02-04 Agilent Technologies, Inc. Use of thioacetic acid derivatives in the sulfurization of oligonucleotides with phenylacetyl disulfide
US9725716B2 (en) * 2011-12-06 2017-08-08 Ohio State Innovation Foundation and Research Institute at Nationwide Children's Hospital Non-ionic, low osmolar contrast agents for delivery of antisense oligonucleotides and treatment of disease
WO2015061246A1 (en) * 2013-10-21 2015-04-30 Isis Pharmaceuticals, Inc. Method for solution phase detritylation of oligomeric compounds
RS60707B1 (sr) 2014-04-01 2020-09-30 Biogen Ma Inc Kompozicije za modulaciju ekspresije sod-1
HK1248603A1 (zh) * 2015-03-10 2018-10-19 Aduro Biotech, Inc. 用於活化"干扰素基因的刺激剂"依懒性信号传导的组合物和方法
JOP20190218A1 (ar) * 2017-03-22 2019-09-22 Boehringer Ingelheim Int مركبات ثنائية النيوكليوتيدات حلقية معدلة

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
ZACHARIA S CHERUVALLATH，ORGANIC PROCESS RESEARCH AND DEVELOPMENT，米国，2000年05月，VOL:4, NR:3，PAGE(S):199 - 204

Also Published As

Publication number Publication date
ES2999138T3 (en) 2025-02-24
US11142545B2 (en) 2021-10-12
KR20230133947A (ko) 2023-09-19
CN109689668A (zh) 2019-04-26
US20190161513A1 (en) 2019-05-30
KR102722183B1 (ko) 2024-10-24
KR20190020743A (ko) 2019-03-04
WO2017223258A1 (en) 2017-12-28
EP3475292B1 (en) 2024-09-18
CN109689668B (zh) 2023-02-17
JP2019518778A (ja) 2019-07-04
EP3475292A1 (en) 2019-05-01

Similar Documents

Publication Publication Date Title
JP7235512B2 (ja) キャッピング工程を有さないチオール化オリゴヌクレオチドの合成
JP7824080B2 (ja) オリゴヌクレオチドの収束液相合成
CN112004928A (zh) 寡核苷酸组合物及其使用方法
US20100331533A1 (en) Use Of Thioacetic Acid Derivatives In The Sulfurization Of Oligonucleotides With Phenylacetyl Disulfide
CN120129688A (zh) 用于制备高度纯化的5′-加帽寡核苷酸的高效方法
JP7085739B2 (ja) 人工ヌクレオシド及び人工ヌクレオチド並びに人工オリゴヌクレオチド
WO2019131719A1 (ja) 高脂溶性ホスホラミダイトの製造
JP7777452B2 (ja) 核酸オリゴマーの製造方法
AU2022291626A1 (en) Improved process for preparing imetelstat
CN100484949C (zh) 用于rna寡核苷酸合成中的核苷亚磷酰胺及其合成方法
HK40008182B (en) Synthesis of thiolated oligonucleotides without a capping step
HK40008182A (en) Synthesis of thiolated oligonucleotides without a capping step
EP3154996B1 (en) Protecting groups for "z nucleotide" and methods thereof
JP4709959B2 (ja) ヌクレオシドホスホロアミダイト化合物
WO2024019137A1 (ja) オリゴヌクレオチドの製造方法
KR100448211B1 (ko) 시티딘유도체의 제조방법
JP7423533B2 (ja) 配糖体化合物の製造方法
WO2006095739A1 (ja) リボヌクレオシドの２’水酸基の脱保護方法
WO2025244124A1 (ja) 核酸オリゴマーの製造方法
CN114835765A (zh) 一种2,-o-(2-甲氧乙基)鸟苷的合成工艺
CN118076620A (zh) 2’修饰嘧啶核苷的制造方法
US20100010069A1 (en) Extended Length Borane Phosphonate Nucleic Acid Compounds
Eritja Casadellà et al. Synthesis and Properties of Oligodeoxynucleotides Carrying 2-Aminopurine
HK40026576A (en) Improved process for preparing imetelstat
WO2005085271A1 (ja) ２ ‘水酸基を修飾された新規人工ｒｎａ

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20200618

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20200618

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20210728

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20211027

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20220318

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20220617

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20220927

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20221220

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20230201

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20230224

R150 Certificate of patent or registration of utility model

Ref document number: 7235512

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150