CN109553651B - 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 - Google Patents

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 Download PDF

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CN109553651B
CN109553651B CN201811577363.6A CN201811577363A CN109553651B CN 109553651 B CN109553651 B CN 109553651B CN 201811577363 A CN201811577363 A CN 201811577363A CN 109553651 B CN109553651 B CN 109553651B
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pharmaceutical composition
tumor
pharmaceutically acceptable
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CN109553651A (zh
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叶红
刘钢
郁楠
曾宏
赵明亮
卿燕
邓华
李雯佳
李栋宏
苏东海
钟维
李少华
巫循伟
王利春
王晶翼
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Sichuan Kelun Biotech Biopharmaceutical Co Ltd
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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
    • C07H19/06—Pyrimidine radicals
    • C07H19/10—Pyrimidine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids
    • 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
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7068—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
    • 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
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7076—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • C07F9/65586—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system at least one of the hetero rings does not contain nitrogen as ring hetero atom
    • 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
    • C07H19/20—Purine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Biochemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Saccharide Compounds (AREA)
CN201811577363.6A 2015-04-03 2016-03-28 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 Active CN109553651B (zh)

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CN201510157772 2015-04-03
CN2015101577720 2015-04-03
CN201680001812.5A CN106661077B (zh) 2015-04-03 2016-03-28 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

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CN201680001812.5A Active CN106661077B (zh) 2015-04-03 2016-03-28 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

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US (2) US10662214B2 (https=)
EP (1) EP3279207B1 (https=)
JP (1) JP6769000B2 (https=)
CN (2) CN109553651B (https=)
AU (1) AU2016240117C1 (https=)
CA (1) CA2975990A1 (https=)
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WO (1) WO2016155593A1 (https=)

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AU2013241341B2 (en) 2012-03-28 2016-09-08 Fujifilm Corporation Salt of 1-(2-deoxy-2-fluoro-4-thio-beta-D-arabinofuranosyl)cytosine
DK2883866T3 (da) 2012-08-13 2019-05-13 Fujifilm Corp MELLEMPRODUKT TIL SYNTESE AF 1-(2-DEOXY-2-FLUOR-4-THIO-beta-D- ARABINOFURANOSYL)CYTOSIN, MELLEMPRODUKT TIL SYNTESE AF THIONUKLEOSID OG FREMGANGSMÅDER TIL FREMSTILLING AF DISSE MELLEMPRODUKTER
TWI678373B (zh) 2014-10-31 2019-12-01 日商富士軟片股份有限公司 硫代核苷衍生物或其鹽及醫藥組合物
US10662214B2 (en) * 2015-04-03 2020-05-26 Sichuan Keiun-Biotech Biopharmaceutical Co., Ltd. Compound of 4′-thionucleoside, as well as preparation method therefor, pharmaceutical composition thereof and application thereof
EP3508205B1 (en) 2016-08-31 2022-05-18 FUJIFILM Corporation Anti-tumor agent, anti-tumor effect enhancer, and anti-tumor kit
JP2020502043A (ja) * 2016-12-22 2020-01-23 シチュアン ケルン−バイオテック バイオファーマシューティカル カンパニー リミテッド ４’−チオ−２’−フルオロヌクレオシドホスファミド化合物の固体形態及びそのための調製方法及びその使用
WO2019001292A1 (zh) * 2017-06-29 2019-01-03 四川科伦博泰生物医药股份有限公司 4'-硫代核苷的新型化合物的制备方法和此制备方法中的中间体
US11266674B2 (en) * 2017-09-01 2022-03-08 Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. Pharmaceutical composition for tumor treatment or prevention, method, and use thereof
MX2018002611A (es) 2018-01-29 2019-07-30 Fujifilm Corp Agente antitumoral para cancer del tracto biliar y metodo para tratar cancer del tracto biliar.
CA3097003A1 (en) * 2018-04-19 2019-10-24 Southern Research Institute 4'-thio-nucleotide and -nucleoside prodrugs for the treatment of cancer
WO2020108343A1 (zh) * 2018-11-28 2020-06-04 四川科伦博泰生物医药股份有限公司 以4'-硫代核苷类化合物为活性成分的口服药物组合物、其制备方法及其用途
CN114341149A (zh) * 2019-07-30 2022-04-12 匹诺生物股份有限公司 用于治疗癌症的二核苷酸化合物及其医学用途
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

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US5128458A (en) 1990-04-20 1992-07-07 Southern Research Institute 2',3'-dideoxy-4'-thioribonucleosides as antiviral agents
JPH1087687A (ja) 1996-04-09 1998-04-07 Yamasa Shoyu Co Ltd ５−置換−１−（２−デオキシ−２−フルオロ−４−チオ−β−Ｄ−アラビノフラノシル）ウラシル
DK0841344T3 (da) * 1996-04-09 2002-12-23 Yamasa Corp 1-(2-Desoxy-2-fluor-4-thio-Beta-D-arabinofuranosyl)cytosiner
GB0317009D0 (en) * 2003-07-21 2003-08-27 Univ Cardiff Chemical compounds
WO2005027962A1 (en) 2003-09-18 2005-03-31 Isis Pharmaceuticals, Inc. 4’-thionucleosides and oligomeric compounds
US7888330B2 (en) * 2005-11-09 2011-02-15 Wayne State University Phosphoramidate derivatives of FAU
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WO2014124430A1 (en) * 2013-02-11 2014-08-14 Emory University Nucleotide and nucleoside therapeutic compositions and uses related thereto
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US10662214B2 (en) * 2015-04-03 2020-05-26 Sichuan Keiun-Biotech Biopharmaceutical Co., Ltd. Compound of 4′-thionucleoside, as well as preparation method therefor, pharmaceutical composition thereof and application thereof

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US20180079770A1 (en) 2018-03-22
AU2016240117A1 (en) 2017-08-24
AU2016240117B2 (en) 2020-08-06
EP3279207B1 (en) 2024-01-24
CN109553651A (zh) 2019-04-02
US20200262860A1 (en) 2020-08-20
EA034375B1 (ru) 2020-01-31
JP2018513832A (ja) 2018-05-31
EP3279207A1 (en) 2018-02-07
CN106661077B (zh) 2019-02-12
US10662214B2 (en) 2020-05-26
WO2016155593A1 (zh) 2016-10-06
EP3279207A4 (en) 2018-11-14
JP6769000B2 (ja) 2020-10-14
EA201791535A1 (ru) 2018-01-31
HK1232229A1 (zh) 2018-01-05
CA2975990A1 (en) 2016-10-06
AU2016240117C1 (en) 2020-11-26
HK1243424A1 (en) 2018-07-13
CN106661077A (zh) 2017-05-10

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