CN112513061B - 用于治疗癌症的4’-硫代-核苷酸和-核苷前药 - Google Patents

用于治疗癌症的4’-硫代-核苷酸和-核苷前药 Download PDF

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CN112513061B
CN112513061B CN201980037108.9A CN201980037108A CN112513061B CN 112513061 B CN112513061 B CN 112513061B CN 201980037108 A CN201980037108 A CN 201980037108A CN 112513061 B CN112513061 B CN 112513061B
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CN112513061A (zh
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O·穆哈-查菲克
C·E·奥盖利-萨夫兰
M·J·苏托
郑斗瑛
赵显龙
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Southern Research Institute
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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
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • 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
    • 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)
CN201980037108.9A 2018-04-19 2019-04-18 用于治疗癌症的4’-硫代-核苷酸和-核苷前药 Active CN112513061B (zh)

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 (2)

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CN112513061A CN112513061A (zh) 2021-03-16
CN112513061B true CN112513061B (zh) 2025-01-24

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US (1) US20210363170A1 (https=)
EP (2) EP3781584A4 (https=)
JP (1) JP7419259B2 (https=)
KR (1) KR102810546B1 (https=)
CN (1) CN112513061B (https=)
AU (2) AU2019256465B2 (https=)
CA (1) CA3097003A1 (https=)
WO (1) WO2019204637A1 (https=)

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AU2020287343A1 (en) * 2019-06-05 2021-12-09 Southern Research Institute Thiarabine- and thiarabine prodrug-based treatments
EP4138843A4 (en) * 2020-04-23 2024-07-10 Southern Research Institute COMPOSITION FOR THE TREATMENT OF 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
WO2022020747A1 (en) * 2020-07-23 2022-01-27 Southern Research Institute Polymorophs of 5-aza-4'-thio-2-deoxycytidine
KR102810379B1 (ko) * 2020-08-07 2025-05-21 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 (2)

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EP1541581A1 (en) * 2002-08-22 2005-06-15 Geneticlab Co., Ltd. 4 -thionucleotide
CN107148423A (zh) * 2014-10-31 2017-09-08 富士胶片株式会社 硫代核苷衍生物或其盐及医药组合物

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US5591722A (en) * 1989-09-15 1997-01-07 Southern Research Institute 2'-deoxy-4'-thioribonucleosides and their antiviral activity
ES2402799T3 (es) * 1998-07-23 2013-05-09 Southern Research Institute Prepreparación de compuestos de tioarabinofuranosilo y utilización de los mismos
WO2000041531A2 (en) 1999-01-13 2000-07-20 Genentech, Inc. Serine protease inhibitors
UA99308C2 (ru) * 2007-09-26 2012-08-10 Маунт Синай Скул Оф Медсин Аналог азацитидина и его применение
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Publication number Publication date
EP4209498A1 (en) 2023-07-12
KR20210005638A (ko) 2021-01-14
EP3781584A4 (en) 2022-05-11
CA3097003A1 (en) 2019-10-24
WO2019204637A1 (en) 2019-10-24
JP7419259B2 (ja) 2024-01-22
CN112513061A (zh) 2021-03-16
EP3781584A1 (en) 2021-02-24
AU2024278376A1 (en) 2025-01-09
US20210363170A1 (en) 2021-11-25
AU2019256465B2 (en) 2024-10-03
KR102810546B1 (ko) 2025-05-20
AU2019256465A1 (en) 2020-11-26
JP2021522197A (ja) 2021-08-30

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