KR102886120B1 - 가교형 인공 핵산 alna - Google Patents

가교형 인공 핵산 alna

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Publication number
KR102886120B1
KR102886120B1 KR1020217017322A KR20217017322A KR102886120B1 KR 102886120 B1 KR102886120 B1 KR 102886120B1 KR 1020217017322 A KR1020217017322 A KR 1020217017322A KR 20217017322 A KR20217017322 A KR 20217017322A KR 102886120 B1 KR102886120 B1 KR 102886120B1
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South Korea
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group
methyl
compound
substituents
optionally substituted
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English (en)
Korean (ko)
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KR20210090659A (ko
Inventor
히로아키 사와모토
신지 구마가이
히로유키 후루카와
도모 아라키
마사유키 우츠기
사토시 오비카
Original Assignee
미쓰비시 타나베 파마 코퍼레이션
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7088—Compounds having three or more nucleosides or nucleotides
    • A61K31/712—Nucleic acids or oligonucleotides having modified sugars, i.e. other than ribose or 2'-deoxyribose
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07H19/06—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
    • C07H19/16—Purine 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
    • C07H19/20—Purine 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
    • 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
    • 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
    • C12N2310/30—Chemical structure
    • C12N2310/31—Chemical structure of the backbone
    • C12N2310/315—Phosphorothioates
    • 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)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • General Health & Medical Sciences (AREA)
  • Biotechnology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Engineering & Computer Science (AREA)
  • Zoology (AREA)
  • Wood Science & Technology (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biophysics (AREA)
  • Physics & Mathematics (AREA)
  • Plant Pathology (AREA)
  • Microbiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
KR1020217017322A 2018-11-12 2019-11-11 가교형 인공 핵산 alna Active KR102886120B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
JP2018212424 2018-11-12
JPJP-P-2018-212424 2018-11-12
PCT/JP2019/044182 WO2020100826A1 (ja) 2018-11-12 2019-11-11 架橋型人工核酸ａｌｎａ

Publications (2)

Publication Number Publication Date
KR20210090659A KR20210090659A (ko) 2021-07-20
KR102886120B1 true KR102886120B1 (ko) 2025-11-14

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020217017322A Active KR102886120B1 (ko) 2018-11-12 2019-11-11 가교형 인공 핵산 alna

Country Status (14)

Country Link
US (2) US12338265B2 (https=)
EP (3) EP4275690A3 (https=)
JP (1) JP7356448B2 (https=)
KR (1) KR102886120B1 (https=)
CN (4) CN119119156A (https=)
AU (1) AU2019381386C1 (https=)
BR (1) BR112021009168A2 (https=)
CA (1) CA3119580A1 (https=)
IL (2) IL283103B2 (https=)
MX (1) MX2021005537A (https=)
MY (1) MY208522A (https=)
PH (1) PH12021551082A1 (https=)
SG (1) SG11202104901VA (https=)
WO (1) WO2020100826A1 (https=)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
JP2023130528A (ja) * 2020-06-24 2023-09-21 田辺三菱製薬株式会社 Ｐｌｐ１発現を調節するための化合物、方法及び医薬組成物
JPWO2022014703A1 (https=) 2020-07-17 2022-01-20
WO2024101446A1 (ja) 2022-11-10 2024-05-16 ルクサナバイオテク株式会社 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
CN120418261A (zh) 2022-12-21 2025-08-01 田边三菱制药株式会社 制造中间体的制造方法、该制造中间体及使用其的桥连型人工核酸中间体的制造方法
WO2025206092A1 (ja) * 2024-03-27 2025-10-02 田辺三菱製薬株式会社 Ｍｙｏｒｅｇｕｌｉｎ発現を調節するための化合物及び医薬組成物

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP4236812B2 (ja) * 1997-09-12 2009-03-11 エクシコン エ／エス オリゴヌクレオチド類似体
AU9393798A (en) 1997-09-17 1999-04-05 Affymetrix, Inc. Genetic compositions and methods
WO2007145593A1 (en) * 2006-06-15 2007-12-21 Jyoti Chattopadhyaya Conformationally constrained 2' -n,4' -c-ethylene-bridged thymidine (aza-ena-t)
EP2580228B1 (en) * 2010-06-08 2016-03-23 Ionis Pharmaceuticals, Inc. Substituted 2'-amino and 2'-thio-bicyclic nucleosides and oligomeric compounds prepared therefrom
BR112013026345A2 (pt) 2011-04-13 2019-04-24 Merck Sharp & Dohe Corp. composto, composição farmacêutica, uso de um composto, e, método para tratar um paciente infectado com hcv
BR112014001075A2 (pt) 2011-07-19 2016-11-29 Univ Idaho sonda, seu uso, método in vitro para associar uma sonda com um alvo e kit
KR101707437B1 (ko) * 2012-09-21 2017-02-16 고꾸리쯔 다이가꾸 호우징 오사까 다이가꾸 구아니딘 가교를 갖는 인공 뉴클레오시드 및 올리고뉴클레오티드
WO2014124952A1 (en) 2013-02-12 2014-08-21 Syddansk Universitet "clickable" alkyne-lna oligonucleotides
WO2016128583A2 (en) 2015-02-15 2016-08-18 Ribo Task Aps Acyl-amino-lna and/or hydrocarbyl-amino-lna oligonucleotides
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
WO2020203880A1 (ja) 2019-03-29 2020-10-08 田辺三菱製薬株式会社 Ｄｕｘ４の発現を調節するための化合物、方法及び医薬組成物

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Astakhove et al. ChemBioChem: Volume 13, Issue 10, Jul 2012, p1377-1523*

Also Published As

Publication number Publication date
PH12021551082A1 (en) 2021-11-22
IL283103A (en) 2021-06-30
WO2020100826A1 (ja) 2020-05-22
JPWO2020100826A1 (ja) 2021-09-30
KR20210090659A (ko) 2021-07-20
EP3881851A4 (en) 2023-02-15
BR112021009168A2 (pt) 2021-08-17
CN112996522A (zh) 2021-06-18
MY208522A (en) 2025-05-14
US20250340584A1 (en) 2025-11-06
CN112996522B (zh) 2024-09-20
IL316158B1 (en) 2026-04-01
CN117964673A (zh) 2024-05-03
MX2021005537A (es) 2021-09-10
CA3119580A1 (en) 2020-05-22
CN117964674A (zh) 2024-05-03
EP4275690A2 (en) 2023-11-15
AU2019381386A1 (en) 2021-06-17
EP4275690A3 (en) 2023-11-22
SG11202104901VA (en) 2021-06-29
AU2019381386C1 (en) 2025-11-27
AU2019381386B2 (en) 2025-06-26
IL283103B2 (en) 2025-04-01
US12338265B2 (en) 2025-06-24
EP4275689A2 (en) 2023-11-15
EP4275689A3 (en) 2023-11-22
JP7356448B2 (ja) 2023-10-04
IL316158A (en) 2024-12-01
US20220002336A1 (en) 2022-01-06
IL283103B1 (en) 2024-12-01
CN119119156A (zh) 2024-12-13
EP3881851A1 (en) 2021-09-22

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