JP2024526730A - ２，６－ジアミノプリン及び２－アミノアデニンのコンジュゲートをオリゴヌクレオチドに導入するための簡便な化学的アプローチ - Google Patents

２，６－ジアミノプリン及び２－アミノアデニンのコンジュゲートをオリゴヌクレオチドに導入するための簡便な化学的アプローチ Download PDF

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JP2024526730A
JP2024526730A JP2024501665A JP2024501665A JP2024526730A JP 2024526730 A JP2024526730 A JP 2024526730A JP 2024501665 A JP2024501665 A JP 2024501665A JP 2024501665 A JP2024501665 A JP 2024501665A JP 2024526730 A JP2024526730 A JP 2024526730A
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ムタイア マノハラン
ミムナ マダウイ
デゥルバジョティ ダッタ
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Alnylam Pharmaceuticals Inc
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    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/549—Sugars, nucleosides, nucleotides or nucleic acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K49/00—Preparations for testing in vivo
    • A61K49/001—Preparation for luminescence or biological staining
    • A61K49/0013—Luminescence
    • A61K49/0017—Fluorescence in vivo
    • A61K49/005—Fluorescence in vivo characterised by the carrier molecule carrying the fluorescent agent
    • A61K49/0054—Macromolecular compounds, i.e. oligomers, polymers, dendrimers
    • 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
    • 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
    • C07H19/167—Purine radicals with ribosyl as the saccharide radical
    • 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
    • C07H19/173—Purine radicals with 2-deoxyribosyl as the 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
    • C07H21/02—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

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Biotechnology (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Biomedical Technology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Saccharide Compounds (AREA)
JP2024501665A 2021-07-15 2022-07-15 ２，６－ジアミノプリン及び２－アミノアデニンのコンジュゲートをオリゴヌクレオチドに導入するための簡便な化学的アプローチ Pending JP2024526730A (ja)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US202163222269P 2021-07-15 2021-07-15
US63/222,269 2021-07-15
US202163236022P 2021-08-23 2021-08-23
US63/236,022 2021-08-23
US202163246479P 2021-09-21 2021-09-21
US63/246,479 2021-09-21
PCT/US2022/037260 WO2023288045A2 (en) 2021-07-15 2022-07-15 Simple chemical approaches to introduce 2,6-diaminopurine and 2-aminoadenine conjugates into oligonucleotides

Publications (2)

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JP2024526730A true JP2024526730A (ja) 2024-07-19
JP2024526730A5 JP2024526730A5 (https=) 2025-07-14

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JP2024501665A Pending JP2024526730A (ja) 2021-07-15 2022-07-15 ２，６－ジアミノプリン及び２－アミノアデニンのコンジュゲートをオリゴヌクレオチドに導入するための簡便な化学的アプローチ

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US (1) US20250025564A1 (https=)
EP (1) EP4370136A4 (https=)
JP (1) JP2024526730A (https=)
WO (1) WO2023288045A2 (https=)

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2002523519A (ja) * 1998-09-01 2002-07-30 アイシス・ファーマシューティカルス・インコーポレーテッド ２−アミノアデノシンを取り込んでいるオリゴヌクレオチドの合成の改良法
WO2009099942A2 (en) * 2008-01-31 2009-08-13 Alnylam Pharmaceuticals, Inc. Chemically modified oligonucleotides and uses thereof

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5681941A (en) * 1990-01-11 1997-10-28 Isis Pharmaceuticals, Inc. Substituted purines and oligonucleotide cross-linking
JP3681338B2 (ja) * 2001-03-14 2005-08-10 独立行政法人科学技術振興機構 シクロプロピル基導入塩基を含有したｄｎａ
US6921812B1 (en) * 2001-07-03 2005-07-26 Isis Pharmaceuticals, Inc. Methods of modulating pharmacokinetics of oligonucleotides
WO2008100447A2 (en) * 2007-02-09 2008-08-21 Gilead Sciences, Inc. Nucleoside analogs for antiviral treatment
EP2270021A1 (en) * 2009-06-18 2011-01-05 Centre National de la Recherche Scientifique Phosphonates synthons for the synthesis of phosphonates derivatives showing better bioavailability
WO2019123339A1 (en) * 2017-12-20 2019-06-27 Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. 2'3' cyclic dinucleotides with phosphonate bond activating the sting adaptor protein

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2002523519A (ja) * 1998-09-01 2002-07-30 アイシス・ファーマシューティカルス・インコーポレーテッド ２−アミノアデノシンを取り込んでいるオリゴヌクレオチドの合成の改良法
WO2009099942A2 (en) * 2008-01-31 2009-08-13 Alnylam Pharmaceuticals, Inc. Chemically modified oligonucleotides and uses thereof

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
TETRAHEDRON LETTERS, vol. 37, no. 43, JPN6026014958, 1996, pages 7675 - 7678, ISSN: 0005841347 *

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WO2023288045A2 (en) 2023-01-19
US20250025564A1 (en) 2025-01-23
WO2023288045A3 (en) 2023-03-02
EP4370136A4 (en) 2025-10-29
EP4370136A2 (en) 2024-05-22

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