EA202090719A1 - Модифицированные нуклеозидные амидофосфиты - Google Patents

Модифицированные нуклеозидные амидофосфиты

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Publication number
EA202090719A1
EA202090719A1 EA202090719A EA202090719A EA202090719A1 EA 202090719 A1 EA202090719 A1 EA 202090719A1 EA 202090719 A EA202090719 A EA 202090719A EA 202090719 A EA202090719 A EA 202090719A EA 202090719 A1 EA202090719 A1 EA 202090719A1
Authority
EA
Eurasian Patent Office
Prior art keywords
amidophosphites
modified nucleoside
amidophosphite
substituents
formulas
Prior art date
Application number
EA202090719A
Other languages
English (en)
Inventor
Сергей Грязнов
Цзинь Хун
Вивек Кумар Раджванши
Original Assignee
Янссен Байофарма, Инк.
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 Янссен Байофарма, Инк. filed Critical Янссен Байофарма, Инк.
Publication of EA202090719A1 publication Critical patent/EA202090719A1/ru

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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
    • C07H19/067—Pyrimidine radicals with ribosyl as the 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
    • 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
    • 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
    • C07H19/20—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
    • 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
    • C07H19/23—Heterocyclic radicals containing two or more heterocyclic rings condensed among themselves or condensed with a common carbocyclic ring system, not provided for in groups C07H19/14 - C07H19/22
    • 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
    • C07H19/24—Heterocyclic radicals containing oxygen or sulfur as ring hetero atom
    • 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
    • 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)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Biotechnology (AREA)
  • General Health & Medical Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Saccharide Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Изобретение относится к соединениям и композициям, содержащим нуклеозидные 5'-амидофосфитные мономеры формул (I) и (II), а также к способам получения и применения, причем заместители определены, как указано в прилагаемой формуле изобретения.
EA202090719A 2017-09-14 2018-09-14 Модифицированные нуклеозидные амидофосфиты EA202090719A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201762558763P 2017-09-14 2017-09-14
PCT/IB2018/057077 WO2019053659A1 (en) 2017-09-14 2018-09-14 PHOSPHORAMIDITES OF MODIFIED NUCLEOSIDES

Publications (1)

Publication Number Publication Date
EA202090719A1 true EA202090719A1 (ru) 2020-07-01

Family

ID=63713969

Family Applications (1)

Application Number Title Priority Date Filing Date
EA202090719A EA202090719A1 (ru) 2017-09-14 2018-09-14 Модифицированные нуклеозидные амидофосфиты

Country Status (16)

Country Link
US (1) US11180524B2 (ru)
EP (1) EP3681894A1 (ru)
JP (2) JP7478660B2 (ru)
KR (1) KR20200100033A (ru)
CN (1) CN111465610A (ru)
AU (1) AU2018332214B2 (ru)
BR (1) BR112020005067A2 (ru)
CA (1) CA3075718A1 (ru)
CL (2) CL2020000657A1 (ru)
EA (1) EA202090719A1 (ru)
IL (2) IL303486A (ru)
MX (1) MX2020002882A (ru)
PH (1) PH12020550127A1 (ru)
SG (1) SG11202002294VA (ru)
UA (1) UA127737C2 (ru)
WO (1) WO2019053659A1 (ru)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114685560B (zh) * 2020-12-31 2024-05-14 沈阳药科大学 含哌啶骨架亚磷酰胺单体及寡聚核苷酸的合成和应用

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK1210357T3 (da) 1999-09-10 2008-07-21 Geron Corp Oligonukleotid-N3' -P5' -thiophosphoramidater: syntese og anvendelse deraf
US20020127598A1 (en) * 2000-03-27 2002-09-12 Wenqiang Zhou Solution-phase combinatorial library synthesis and pharmaceutically active compounds produced thereby
JP4255227B2 (ja) * 2000-11-21 2009-04-15 武 今西 Ｎ３’−ｐ５’結合を有する２’，４’−ｂｎａオリゴヌクレオチド
WO2005047506A1 (en) 2003-11-04 2005-05-26 Geron Corporation Rna amidates and thioamidates for rnai
US8138330B2 (en) * 2006-09-11 2012-03-20 Sigma-Aldrich Co. Llc Process for the synthesis of oligonucleotides
US8309707B2 (en) * 2008-09-06 2012-11-13 Chemgenes Corporation RNA synthesis-phosphoramidites for synthetic RNA in the reverse direction, and application in convenient introduction of ligands, chromophores and modifications of synthetic RNA at the 3′-end
US8541569B2 (en) * 2008-09-06 2013-09-24 Chemgenes Corporation Phosphoramidites for synthetic RNA in the reverse direction, efficient RNA synthesis and convenient introduction of 3'-end ligands, chromophores and modifications of synthetic RNA
WO2011133871A2 (en) * 2010-04-22 2011-10-27 Alnylam Pharmaceuticals, Inc. 5'-end derivatives
MX2018008266A (es) * 2016-01-11 2019-01-31 Innate Tumor Immunity Inc Dinucleotidos ciclicos para tratar condiciones asociadas con actividad del estimulador de genes del interferon (sting) tales como cancer.
CN109952378A (zh) * 2016-09-14 2019-06-28 詹森生物制药有限公司 经修饰的寡核苷酸及使用方法

Also Published As

Publication number Publication date
JP2020533387A (ja) 2020-11-19
CL2021000381A1 (es) 2021-07-02
IL303486A (en) 2023-08-01
US11180524B2 (en) 2021-11-23
IL273274A (en) 2020-04-30
PH12020550127A1 (en) 2021-02-08
US20220048941A1 (en) 2022-02-17
JP2024054157A (ja) 2024-04-16
SG11202002294VA (en) 2020-04-29
AU2018332214A1 (en) 2020-04-02
CL2020000657A1 (es) 2020-10-23
BR112020005067A2 (pt) 2020-09-15
AU2018332214B2 (en) 2023-11-02
MX2020002882A (es) 2020-10-05
UA127737C2 (uk) 2023-12-20
EP3681894A1 (en) 2020-07-22
US20200255468A1 (en) 2020-08-13
IL273274B2 (en) 2023-12-01
WO2019053659A1 (en) 2019-03-21
CN111465610A (zh) 2020-07-28
KR20200100033A (ko) 2020-08-25
AU2018332214A8 (en) 2021-10-07
CA3075718A1 (en) 2019-03-21
IL273274B1 (en) 2023-08-01
JP7478660B2 (ja) 2024-05-07

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