JP7419259B2 - 癌の治療のための4’-チオ-ヌクレオチドおよび-ヌクレオシドプロドラッグ - Google Patents

癌の治療のための4’-チオ-ヌクレオチドおよび-ヌクレオシドプロドラッグ Download PDF

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JP7419259B2
JP7419259B2 JP2020557913A JP2020557913A JP7419259B2 JP 7419259 B2 JP7419259 B2 JP 7419259B2 JP 2020557913 A JP2020557913 A JP 2020557913A JP 2020557913 A JP2020557913 A JP 2020557913A JP 7419259 B2 JP7419259 B2 JP 7419259B2
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オマー モウカ-シャフィク
コリンヌ イー アウジェッリ-サフラン
マーク ジェイ スト
ドゥ ヨン チョン
ヒョニョン チョ
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サウザーン リサーチ インスチチュート
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    • 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
    • C07H19/12—Triazine radicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • 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
    • C07H19/073—Pyrimidine radicals with 2-deoxyribosyl 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
    • C07H19/06—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
    • C07H19/10—Pyrimidine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids
    • C07H19/11—Pyrimidine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids containing cyclic phosphate
    • 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)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2020557913A 2018-04-19 2019-04-18 癌の治療のための4’-チオ-ヌクレオチドおよび-ヌクレオシドプロドラッグ Active JP7419259B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862660208P 2018-04-19 2018-04-19
US62/660,208 2018-04-19
PCT/US2019/028168 WO2019204637A1 (en) 2018-04-19 2019-04-18 4'-thio-nucleotide and -nucleoside prodrugs for the treatment of cancer

Publications (3)

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JP2021522197A JP2021522197A (ja) 2021-08-30
JP2021522197A5 JP2021522197A5 (enExample) 2022-04-25
JP7419259B2 true JP7419259B2 (ja) 2024-01-22

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JP2020557913A Active JP7419259B2 (ja) 2018-04-19 2019-04-18 癌の治療のための4’-チオ-ヌクレオチドおよび-ヌクレオシドプロドラッグ

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US (1) US20210363170A1 (enExample)
EP (2) EP4209498A1 (enExample)
JP (1) JP7419259B2 (enExample)
KR (1) KR102810546B1 (enExample)
CN (1) CN112513061B (enExample)
AU (2) AU2019256465B2 (enExample)
CA (1) CA3097003A1 (enExample)
WO (1) WO2019204637A1 (enExample)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113993521A (zh) 2019-06-05 2022-01-28 南方研究院 基于噻拉滨和噻拉滨前药的治疗
AU2021260964A1 (en) 2020-04-23 2022-12-01 Pinotbio, Inc. Composition for treating blood cancer using 4'-thio-5-aza-2'-deoxycytidine and uses thereof
CN111393314A (zh) * 2020-04-30 2020-07-10 安徽红杉生物医药科技有限公司 2-烷基-2-氨基丙酸酯盐酸盐的制备方法
BR112023001236A2 (pt) * 2020-07-23 2023-04-04 Southern Res Inst Polimorfos de 5-aza-4'-tio-2-desoxicitidina
WO2022031150A1 (ko) * 2020-08-07 2022-02-10 주식회사 피노바이오 데옥시사이티딘계 항암제 및 실릴 에테르 함유 링커를 포함하는 접합체 및 이의 용도
CN114685558A (zh) * 2020-12-28 2022-07-01 尚科生物医药(上海)有限公司 一种瑞德西韦中间体的制备方法
KR102891437B1 (ko) * 2021-08-02 2025-11-26 주식회사 피노바이오 잘 설계된 다중 표적 억제제로 선정된 4'-티오-5-아자-2'-디옥시사이티딘의 의약 용도

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004018494A1 (ja) 2002-08-22 2004-03-04 Geneticlab Co., Ltd. 4’−チオヌクレオチド
WO2016068341A1 (ja) 2014-10-31 2016-05-06 富士フイルム株式会社 チオヌクレオシド誘導体またはその塩および医薬組成物
WO2016155593A1 (zh) 2015-04-03 2016-10-06 四川科伦药物研究院有限公司 4'-硫代核苷的新型化合物及其制备方法、药物组合物和应用
WO2016189055A1 (en) 2015-05-27 2016-12-01 Idenix Pharmaceuticals Llc Nucleotides for the treatment of cancer
WO2019152459A1 (en) 2018-02-01 2019-08-08 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Stereoselective synthesis and process for the manufacturing of 2'-deoxynucleosides

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US6020322A (en) * 1993-11-09 2000-02-01 Pro-Neuron, Inc. Acyl deoxyribonucleoside derivatives and uses thereof
US5591722A (en) * 1989-09-15 1997-01-07 Southern Research Institute 2'-deoxy-4'-thioribonucleosides and their antiviral activity
NZ509405A (en) * 1998-07-23 2004-10-29 Southern Res Inst Preparation of 1-(4-thio-thioarabinofuranosyl) cytosine derivatives and their use as anticancer agents and DNA replication inhibitors
IL144032A0 (en) 1999-01-13 2002-04-21 Genentech Inc Serine protease inhibitors
MX2010003261A (es) * 2007-09-26 2010-08-18 Sinai School Medicine Analogos de azacitidina y usos de los mismos.
US20110218170A1 (en) * 2010-03-02 2011-09-08 Southern Research Institute Use of 2'-deoxy-4'-thiocytidine and its analogues as dna hypomethylating anticancer agents
US9156874B2 (en) * 2011-01-03 2015-10-13 Nanjing Molecular Research, Inc. Double-liver-targeting phosphoramidate and phosphonoamidate prodrugs
HRP20190572T1 (hr) * 2012-08-13 2019-05-17 Fujifilm Corporation POSREDNIK ZA SINTEZU 1-(2-DEOKSI-2 FLUORO-4-TIO-beta-D-ARABINOFURANOZIL) CITOZINA, POSREDNIK ZA SINTEZU TIONUKLEOZIDA, I METODE ZA PROIZVODNJU OVIH POSREDNIKA
US20160312261A1 (en) * 2015-04-24 2016-10-27 Plasmia Biotech, S.L. Enzymatic production of cytosinic nucleoside analogues
AU2021260964A1 (en) * 2020-04-23 2022-12-01 Pinotbio, Inc. Composition for treating blood cancer using 4'-thio-5-aza-2'-deoxycytidine and uses thereof

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004018494A1 (ja) 2002-08-22 2004-03-04 Geneticlab Co., Ltd. 4’−チオヌクレオチド
WO2016068341A1 (ja) 2014-10-31 2016-05-06 富士フイルム株式会社 チオヌクレオシド誘導体またはその塩および医薬組成物
WO2016155593A1 (zh) 2015-04-03 2016-10-06 四川科伦药物研究院有限公司 4'-硫代核苷的新型化合物及其制备方法、药物组合物和应用
WO2016189055A1 (en) 2015-05-27 2016-12-01 Idenix Pharmaceuticals Llc Nucleotides for the treatment of cancer
WO2019152459A1 (en) 2018-02-01 2019-08-08 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Stereoselective synthesis and process for the manufacturing of 2'-deoxynucleosides

Non-Patent Citations (3)

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Cancer Chemother. Pharmacol.,2014年,74,291-302
J. Am. Chem. Soc.,2007年,129,15424-15425
J. Phys. Chem. A,2006年,110,2308-2313

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Publication number Publication date
CN112513061A (zh) 2021-03-16
AU2024278376A1 (en) 2025-01-09
AU2019256465B2 (en) 2024-10-03
KR20210005638A (ko) 2021-01-14
CN112513061B (zh) 2025-01-24
KR102810546B1 (ko) 2025-05-20
WO2019204637A1 (en) 2019-10-24
EP3781584A1 (en) 2021-02-24
AU2019256465A1 (en) 2020-11-26
US20210363170A1 (en) 2021-11-25
EP4209498A1 (en) 2023-07-12
JP2021522197A (ja) 2021-08-30
EP3781584A4 (en) 2022-05-11
CA3097003A1 (en) 2019-10-24

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