JP6048982B2 - 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 - Google Patents

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 Download PDF

Info

Publication number
JP6048982B2
JP6048982B2 JP2014536921A JP2014536921A JP6048982B2 JP 6048982 B2 JP6048982 B2 JP 6048982B2 JP 2014536921 A JP2014536921 A JP 2014536921A JP 2014536921 A JP2014536921 A JP 2014536921A JP 6048982 B2 JP6048982 B2 JP 6048982B2
Authority
JP
Japan
Prior art keywords
group
amino
carbon atoms
nucleic acid
oxo
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
JP2014536921A
Other languages
English (en)
Japanese (ja)
Other versions
JPWO2014046212A1 (ja
Inventor
聡 小比賀
聡 小比賀
悠太朗 壽
悠太朗 壽
玲子 脇
玲子 脇
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.)
University of Osaka NUC
Original Assignee
Osaka University NUC
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 Osaka University NUC filed Critical Osaka University NUC
Publication of JPWO2014046212A1 publication Critical patent/JPWO2014046212A1/ja
Application granted granted Critical
Publication of JP6048982B2 publication Critical patent/JP6048982B2/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
    • 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
    • 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
    • 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
    • C07H19/16—Purine radicals
    • 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
    • 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
    • C07H23/00—Compounds containing boron, silicon or a metal, e.g. chelates or vitamin B12
    • 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
    • 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)
  • Zoology (AREA)
  • Biomedical Technology (AREA)
  • General Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Wood Science & Technology (AREA)
  • Biophysics (AREA)
  • Plant Pathology (AREA)
  • Microbiology (AREA)
  • Physics & Mathematics (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)
JP2014536921A 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 Active JP6048982B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
JP2012208906 2012-09-21
JP2012208906 2012-09-21
JP2013022360 2013-02-07
JP2013022360 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)

Publication Number Publication Date
JPWO2014046212A1 JPWO2014046212A1 (ja) 2016-08-18
JP6048982B2 true JP6048982B2 (ja) 2016-12-21

Family

ID=50341516

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2014536921A Active JP6048982B2 (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

Country Status (9)

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

Families Citing this family (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9315535B2 (en) 2013-02-18 2016-04-19 Shionogi & Co., Ltd. Nucleoside and nucleotide having nitrogen-containing heterocycle structure
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
EP3415524A4 (en) 2016-01-07 2019-09-04 Osaka University INHIBITOR OF α-SYNNUCLEINE EXPRESSION
JP7095893B2 (ja) 2017-02-21 2022-07-05 国立大学法人大阪大学 アンチセンスオリゴ核酸
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
TWI850773B (zh) 2017-08-31 2024-08-01 日商田邊三菱製藥股份有限公司 可溶性il-33受體的用途
JP7394749B2 (ja) * 2018-05-10 2023-12-08 日本新薬株式会社 オリゴ核酸化合物の製造方法
EP3831837A4 (en) 2018-07-31 2023-06-14 Osaka University OLIGONUCLEOTIDE THERAPEUTIC AGENT FOR SMALL CELL LUNG CANCER
JP7396577B2 (ja) 2018-09-05 2023-12-12 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
KR102886120B1 (ko) 2018-11-12 2025-11-14 미쓰비시 타나베 파마 코퍼레이션 가교형 인공 핵산 alna
CA3198199A1 (en) 2019-03-29 2020-10-08 Mitsubishi Tanabe Pharma Corporation Compound, method and pharmaceutical composition for modulating expression of dux4
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
AU2020282828A1 (en) 2019-05-31 2022-01-27 Aligos Therapeutics, Inc. Modified gapmer oligonucleotides and methods of use
JPWO2020256084A1 (enExample) * 2019-06-19 2020-12-24
US20230087946A1 (en) * 2019-06-20 2023-03-23 Hoffmann-La Roche Inc. Radiolabeled moem type oligonucleotides and process for their preparation
WO2021230286A1 (ja) 2020-05-12 2021-11-18 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
JP7725490B2 (ja) 2020-09-25 2025-08-19 株式会社理研ジェネシス 新規人工核酸、その製造方法及び用途
JPWO2022097727A1 (enExample) 2020-11-06 2022-05-12
WO2022181807A1 (ja) 2021-02-25 2022-09-01 国立大学法人大阪大学 ＲＥＳＴ ｍＲＮＡ前駆体のプロセシングにおけるＮエキソンのスキッピングを誘導するオリゴヌクレオチド
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
CA3221758A1 (en) 2021-05-28 2022-12-01 Sumitomo Pharma Co., Ltd. Antisense nucleic acid
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
JPWO2023026994A1 (enExample) 2021-08-21 2023-03-02
WO2023093960A1 (en) * 2021-11-26 2023-06-01 Syddansk Universitet Modified peptide-oligonucleotide conjugate
WO2023127857A1 (ja) 2021-12-27 2023-07-06 株式会社理研ジェネシス 新規人工核酸、その製造方法及び用途
EP4493694A1 (en) * 2022-03-17 2025-01-22 Aligos Therapeutics, Inc. Modified gapmer oligomers and methods of use thereof
EP4617279A1 (en) 2022-11-10 2025-09-17 Luxna Biotech Co., Ltd. Modified nucleoside having guanidino structure in bridged part and method for producing oligonucleotide using same
JPWO2024181416A1 (enExample) 2023-02-28 2024-09-06
CN120813558A (zh) 2023-03-06 2025-10-17 斯佩拉制药株式会社 长链烯氧基取代的苯甲酰衍生物及使用该衍生物的寡核苷酸合成方法
CN121311591A (zh) 2023-06-16 2026-01-09 住友制药株式会社 调节rps25基因的表达和/或其功能的反义寡核苷酸
WO2025240506A1 (en) 2024-05-14 2025-11-20 Aligos Therapeutics, Inc. Modified antisense oligonucleotides for treating hepatitis b virus

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4458066A (en) * 1980-02-29 1984-07-03 University Patents, Inc. Process for preparing polynucleotides
US5132418A (en) * 1980-02-29 1992-07-21 University Patents, Inc. Process for preparing polynucleotides
US4500707A (en) * 1980-02-29 1985-02-19 University Patents, Inc. Nucleosides useful in the preparation of polynucleotides
US4973679A (en) * 1981-03-27 1990-11-27 University Patents, Inc. Process for oligonucleo tide synthesis using phosphormidite intermediates
US4668777A (en) * 1981-03-27 1987-05-26 University Patents, Inc. Phosphoramidite nucleoside compounds
US5696253A (en) * 1994-06-30 1997-12-09 The Regents Of The University Of California Polynucleoside chain with 3'→5' guanidyl linkages
JP3756313B2 (ja) 1997-03-07 2006-03-15 武 今西 新規ビシクロヌクレオシド及びオリゴヌクレオチド類縁体
JP4151751B2 (ja) * 1999-07-22 2008-09-17 第一三共株式会社 新規ビシクロヌクレオシド類縁体
JP4383176B2 (ja) 2002-02-13 2009-12-16 武 今西 ヌクレオシド類縁体およびそのヌクレオチド類縁体を含むオリゴヌクレオチド誘導体
JP4731324B2 (ja) 2003-08-28 2011-07-20 武 今西 Ｎ−ｏ結合性架橋構造型新規人工核酸
WO2007026824A1 (ja) * 2005-08-31 2007-03-08 Osaka University オリゴヌクレオチド類縁体
CN102596983B (zh) * 2009-10-29 2016-06-15 国立大学法人大阪大学 交联型人工核苷和核苷酸
US8536323B2 (en) * 2010-04-21 2013-09-17 Pierce Biotechnology, Inc. Modified nucleotides
US9206216B2 (en) * 2010-04-21 2015-12-08 Pierce Biotechnology, Inc. Modified nucleotides methods and kits

Also Published As

Publication number Publication date
EP2899197A1 (en) 2015-07-29
WO2014046212A1 (ja) 2014-03-27
US10377789B2 (en) 2019-08-13
CA2885719C (en) 2017-07-11
KR20150056647A (ko) 2015-05-26
EP2899197A4 (en) 2016-03-09
EP2899197B1 (en) 2017-03-22
IN2015DN02238A (enExample) 2015-08-21
KR101707437B1 (ko) 2017-02-16
JPWO2014046212A1 (ja) 2016-08-18
US20150266917A1 (en) 2015-09-24
CN104768964B (zh) 2017-03-29
CN104768964A (zh) 2015-07-08
CA2885719A1 (en) 2014-03-27
ES2622716T3 (es) 2017-07-07

Similar Documents

Publication Publication Date Title
JP6048982B2 (ja) 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
JP7485642B2 (ja) 治療化合物用の標的化リガンド
US9611479B2 (en) Crosslinked nucleoside and nucleotide
JP5669073B2 (ja) 架橋型人工ヌクレオシドおよびヌクレオチド
CN103619356B (zh) 肽寡核苷酸缀合物
US12398171B2 (en) 5′-modified nucleoside and nucleotide using same
WO2016017422A1 (ja) 架橋型ヌクレオシドおよびヌクレオチド
US20220127300A1 (en) 5'-modified nucleoside and nucleotide using same
WO2015125845A1 (ja) 含窒素非芳香族複素環を含む核酸のリン酸部位修飾
EP4477655A1 (en) Phenoxazine derivative and drug delivery system formulation using same
JP7751302B2 (ja) 架橋型ヌクレオシドおよびヌクレオチド
WO2024101446A1 (ja) 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
WO2023167094A1 (ja) ５'位修飾ヌクレオシドおよびそれを用いたヌクレオチド
CN118946575A (zh) 5'位修饰核苷和使用其的核苷酸

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A821

Effective date: 20160519

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20160628

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20160927

A911 Transfer to examiner for re-examination before appeal (zenchi)

Free format text: JAPANESE INTERMEDIATE CODE: A911

Effective date: 20161006

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: 20161101

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20161115

R150 Certificate of patent or registration of utility model

Ref document number: 6048982

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

RD04 Notification of resignation of power of attorney

Free format text: JAPANESE INTERMEDIATE CODE: R3D04

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250