CN104768964B - 具有胍桥的人工核苷和寡核苷酸 - Google Patents

具有胍桥的人工核苷和寡核苷酸 Download PDF

Info

Publication number
CN104768964B
CN104768964B CN201380057335.0A CN201380057335A CN104768964B CN 104768964 B CN104768964 B CN 104768964B CN 201380057335 A CN201380057335 A CN 201380057335A CN 104768964 B CN104768964 B CN 104768964B
Authority
CN
China
Prior art keywords
group
carbon atoms
amino
substituted
nucleic acid
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
CN201380057335.0A
Other languages
English (en)
Chinese (zh)
Other versions
CN104768964A (zh
Inventor
小比贺聪
寿悠太朗
胁玲子
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.)
The University of Osaka
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 CN104768964A publication Critical patent/CN104768964A/zh
Application granted granted Critical
Publication of CN104768964B publication Critical patent/CN104768964B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

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)
CN201380057335.0A 2012-09-21 2013-09-19 具有胍桥的人工核苷和寡核苷酸 Active CN104768964B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
JP2012-208906 2012-09-21
JP2012208906 2012-09-21
JP2013022360 2013-02-07
JP2013-022360 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
CN104768964A CN104768964A (zh) 2015-07-08
CN104768964B true CN104768964B (zh) 2017-03-29

Family

ID=50341516

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201380057335.0A Active CN104768964B (zh) 2012-09-21 2013-09-19 具有胍桥的人工核苷和寡核苷酸

Country Status (9)

Country Link
US (1) US10377789B2 (cg-RX-API-DMAC10.html)
EP (1) EP2899197B1 (cg-RX-API-DMAC10.html)
JP (1) JP6048982B2 (cg-RX-API-DMAC10.html)
KR (1) KR101707437B1 (cg-RX-API-DMAC10.html)
CN (1) CN104768964B (cg-RX-API-DMAC10.html)
CA (1) CA2885719C (cg-RX-API-DMAC10.html)
ES (1) ES2622716T3 (cg-RX-API-DMAC10.html)
IN (1) IN2015DN02238A (cg-RX-API-DMAC10.html)
WO (1) WO2014046212A1 (cg-RX-API-DMAC10.html)

Families Citing this family (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014126229A1 (ja) * 2013-02-18 2014-08-21 塩野義製薬株式会社 含窒素複素環構造を有するヌクレオシド及びヌクレオチド
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
US11234995B2 (en) 2016-01-07 2022-02-01 Osaka University α-synuclein expression inhibitor
US11261440B2 (en) 2017-02-21 2022-03-01 Osaka University Antisense oligonucleic acid
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
WO2019045075A1 (ja) 2017-08-31 2019-03-07 田辺三菱製薬株式会社 Ｉｌ－３３アンタゴニストを含む子宮内膜症治療剤
US11560401B2 (en) * 2018-05-10 2023-01-24 Nippon Shinyaku Co., Ltd. Method for preparing oligonucleic acid compound
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
CA3119580A1 (en) 2018-11-12 2020-05-22 Mitsubishi Tanabe Pharma Corporation Crosslinked artificial nucleic acid alna
TW202104595A (zh) 2019-03-29 2021-02-01 日商田邊三菱製藥股份有限公司 用來調節ｄｕｘ４的表現之化合物、方法及醫藥組成物
JP7413362B2 (ja) 2019-03-29 2024-01-15 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
KR20220024192A (ko) 2019-05-31 2022-03-03 알리고스 테라퓨틱스 인코포레이티드 변형된 갭머 올리고뉴클레오타이드 및 사용 방법
CN113924308B (zh) * 2019-06-19 2024-09-13 雅玛山酱油株式会社 交联型核苷中间体的结晶及其制造方法以及交联型核苷亚磷酰胺的制造方法
MX2021015541A (es) * 2019-06-20 2022-02-10 Hoffmann La Roche Oligonucleotidos tipo metoxietilen maleimida (moem) radiomarcados y proceso para su preparacion.
JP7776420B2 (ja) 2020-05-12 2025-11-26 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
EP4219517A4 (en) 2020-09-25 2024-09-25 Riken Genesis Co., Ltd. NOVEL ARTIFICIAL NUCLEIC ACID, METHOD FOR PRODUCING THE SAME AND USE THEREOF
TWI910261B (zh) 2020-11-06 2026-01-01 日商住友製藥股份有限公司 Ｒｐｓ２５基因之表現及／或功能調節劑
US20240148775A1 (en) 2021-02-25 2024-05-09 Osaka University Oligonucleotide for inducing n-exon skipping during rest mrna precursor processing
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
AU2022279820A1 (en) 2021-05-28 2023-12-14 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
WO2023026994A1 (ja) 2021-08-21 2023-03-02 武田薬品工業株式会社 ヒトトランスフェリンレセプター結合ペプチド－薬物コンジュゲート
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
JP2025509552A (ja) * 2022-03-17 2025-04-11 アリゴス セラピューティクス，インコーポレーテッド 修飾ギャップマーオリゴマー及びその使用方法
JPWO2024101446A1 (cg-RX-API-DMAC10.html) 2022-11-10 2024-05-16
EP4674962A1 (en) 2023-02-28 2026-01-07 The University of Osaka Oligonucleotide, and rest expression suppressing agent and pharmaceutical composition using same
EP4678626A1 (en) 2023-03-06 2026-01-14 Spera Pharma, Inc. Long-chain alkenyloxy-substituted benzoyl derivative and oligonucleotide synthesis method using same
JPWO2024257847A1 (cg-RX-API-DMAC10.html) 2023-06-16 2024-12-19
US20250368996A1 (en) 2024-05-14 2025-12-04 Aligos Therapeutics, Inc. Modified antisense oligonucleotides for treating hepatitis b virus

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1996000575A1 (en) * 1994-06-30 1996-01-11 The Regents Of The University Of California Polynucleoside chain having multiple nucleosides, the nucleosides coupled by guanidyl linkages
CN1376161A (zh) * 1999-07-22 2002-10-23 三共株式会社 新型双环核苷类似物
CN102596983A (zh) * 2009-10-29 2012-07-18 国立大学法人大阪大学 交联型人工核苷和核苷酸

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
US4458066A (en) * 1980-02-29 1984-07-03 University Patents, Inc. Process for preparing polynucleotides
US4668777A (en) * 1981-03-27 1987-05-26 University Patents, Inc. Phosphoramidite nucleoside compounds
US4973679A (en) * 1981-03-27 1990-11-27 University Patents, Inc. Process for oligonucleo tide synthesis using phosphormidite intermediates
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
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
DK1661905T3 (da) 2003-08-28 2012-07-23 Takeshi Imanishi Hidtil ukendte syntetiske nukleinsyrer af N-O-krydsbindingstype
WO2007026824A1 (ja) 2005-08-31 2007-03-08 Osaka University オリゴヌクレオチド類縁体
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

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1996000575A1 (en) * 1994-06-30 1996-01-11 The Regents Of The University Of California Polynucleoside chain having multiple nucleosides, the nucleosides coupled by guanidyl linkages
CN1376161A (zh) * 1999-07-22 2002-10-23 三共株式会社 新型双环核苷类似物
CN102596983A (zh) * 2009-10-29 2012-07-18 国立大学法人大阪大学 交联型人工核苷和核苷酸

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
Development of potential anticancer agents that target the telomere sequence;Myunji Park et al.;《Bioorganic & Medicinal Chemistry Letters》;20100506;第20卷;3982-3986 *
Synthesis, RNA selective hybridization and high nuclease resistance of an oligonucleotide containing novel bridged nucleic acid with cyclic urea structure;Masaru Nishida et al.;《Chemical Communications》;20100622;第46卷;5283-5285 *

Also Published As

Publication number Publication date
EP2899197A1 (en) 2015-07-29
ES2622716T3 (es) 2017-07-07
JPWO2014046212A1 (ja) 2016-08-18
KR101707437B1 (ko) 2017-02-16
WO2014046212A1 (ja) 2014-03-27
EP2899197A4 (en) 2016-03-09
EP2899197B1 (en) 2017-03-22
US20150266917A1 (en) 2015-09-24
KR20150056647A (ko) 2015-05-26
IN2015DN02238A (cg-RX-API-DMAC10.html) 2015-08-21
CA2885719A1 (en) 2014-03-27
CA2885719C (en) 2017-07-11
US10377789B2 (en) 2019-08-13
CN104768964A (zh) 2015-07-08
JP6048982B2 (ja) 2016-12-21

Similar Documents

Publication Publication Date Title
CN104768964A (zh) 具有胍桥的人工核苷和寡核苷酸
AU2023255025B2 (en) Targeting ligands
JP5669073B2 (ja) 架橋型人工ヌクレオシドおよびヌクレオチド
JP6233903B2 (ja) 架橋型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
KR102142689B1 (ko) 기능적으로-변형된 올리고뉴클레오티드 및 이의 서브유니트
EP3919620A1 (en) Short interfering nucleic acid (sina) compositions
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
CN108137638A (zh) 桥连型核酸GuNA、其制造方法及中间体化合物
US20220127300A1 (en) 5'-modified nucleoside and nucleotide using same
US12606589B2 (en) Bridged nucleoside and nucleotide using same
EP4477655A1 (en) Phenoxazine derivative and drug delivery system formulation using same
WO2026023273A1 (ja) リガンド－核酸コンジュゲート体およびそれを用いた医薬組成物
BR122021011374B1 (pt) Uso de um oligômero antissenso ou sal farmaceuticamente aceitável ou hidrato do mesmo e um carreador ou aditivo farmaceuticamente aceitável
BR112018004970B1 (pt) Oligômero antissenso, composição farmacêutica, e, uso do oligômero antissenso ou sal farmaceuticamente aceitável ou hidrato do mesmo

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
EXSB Decision made by sipo to initiate substantive examination
SE01 Entry into force of request for substantive examination
GR01 Patent grant
GR01 Patent grant