CN106661077B - 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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CN106661077B
CN106661077B CN201680001812.5A CN201680001812A CN106661077B CN 106661077 B CN106661077 B CN 106661077B CN 201680001812 A CN201680001812 A CN 201680001812A CN 106661077 B CN106661077 B CN 106661077B
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compound
pharmaceutical composition
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base
pharmaceutically acceptable
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CN106661077A (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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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)
  • Saccharide Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201680001812.5A 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 CN106661077B (zh)

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CN2015101577720 2015-04-03
CN201510157772 2015-04-03
PCT/CN2016/077519 WO2016155593A1 (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 (enExample)
EP (1) EP3279207B1 (enExample)
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AU (1) AU2016240117C1 (enExample)
CA (1) CA2975990A1 (enExample)
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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN109553651A (zh) * 2015-04-03 2019-04-02 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及其制备方法、药物组合物和应用

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KR20170082650A (ko) 2012-03-28 2017-07-14 후지필름 가부시키가이샤 1-(2-디옥시-2-플루오로-4-티오-β-D-아라비노푸라노실)시토신의 염
KR101770248B1 (ko) 2012-08-13 2017-08-22 후지필름 가부시키가이샤 1-(2-데옥시-2-플루오로-4-티오-β-D-아라비노푸라노실)시토신의 합성 중간체, 티오뉴클레오시드의 합성 중간체, 및 그들의 제조법
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
RU2752172C2 (ru) 2016-08-31 2021-07-23 Фуджифилм Корпорэйшн Противоопухолевый агент, усилитель противоопухолевого действия и противоопухолевый набор
CA3041420A1 (en) * 2016-12-22 2018-06-28 Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. Solid form of 4'-thio-2'-fluoronucleoside phosphamide compound and preparation method therefor and use thereof
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
CN110831604B (zh) * 2017-09-01 2023-05-02 四川科伦博泰生物医药股份有限公司 用于肿瘤治疗或预防的药物组合物、方法及其用途
AU2018404329B2 (en) 2018-01-29 2021-09-09 Fujifilm Corporation Antitumor agent for biliary tract cancer and method for treating biliary tract cancer
EP4209498A1 (en) * 2018-04-19 2023-07-12 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
US12208112B2 (en) 2020-04-23 2025-01-28 Southern Research Institute Composition for treating blood cancer using 4′-thio-5-Aza-2′-deoxycytidine and uses thereof

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US6147058A (en) * 1996-04-09 2000-11-14 Yamasa Corporation 1-(2-deoxy-2-fluoro-4-thio-beta-D-arabinofuranosyl)cytosine
WO2005012327A2 (en) * 2003-07-21 2005-02-10 University College Cardiff Consultants Limited Nucleotide phosphoramidates as anticancer agents
WO2007056596A2 (en) * 2005-11-09 2007-05-18 Wayne State University Phosphoramidate derivatives of fau
WO2012045999A1 (en) * 2010-10-06 2012-04-12 Nucana Biomed Limited Phosphoramidite derivatives of gemcitabine for use in the treatment cancer
WO2014197578A1 (en) * 2013-06-05 2014-12-11 Idenix Pharmaceuticals, Inc. 1',4'-thio nucleosides for the treatment of hcv
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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US6147058A (en) * 1996-04-09 2000-11-14 Yamasa Corporation 1-(2-deoxy-2-fluoro-4-thio-beta-D-arabinofuranosyl)cytosine
WO2005012327A2 (en) * 2003-07-21 2005-02-10 University College Cardiff Consultants Limited Nucleotide phosphoramidates as anticancer agents
WO2007056596A2 (en) * 2005-11-09 2007-05-18 Wayne State University Phosphoramidate derivatives of fau
WO2012045999A1 (en) * 2010-10-06 2012-04-12 Nucana Biomed Limited Phosphoramidite derivatives of gemcitabine for use in the treatment cancer
WO2014197578A1 (en) * 2013-06-05 2014-12-11 Idenix Pharmaceuticals, Inc. 1',4'-thio nucleosides for the treatment of hcv
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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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN109553651A (zh) * 2015-04-03 2019-04-02 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及其制备方法、药物组合物和应用

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AU2016240117B2 (en) 2020-08-06
EA201791535A1 (ru) 2018-01-31
JP6769000B2 (ja) 2020-10-14
EP3279207B1 (en) 2024-01-24
AU2016240117C1 (en) 2020-11-26
US20200262860A1 (en) 2020-08-20
CN109553651A (zh) 2019-04-02
EP3279207A4 (en) 2018-11-14
US10662214B2 (en) 2020-05-26
CA2975990A1 (en) 2016-10-06
CN109553651B (zh) 2021-08-06
HK1232229A1 (zh) 2018-01-05
AU2016240117A1 (en) 2017-08-24
US20180079770A1 (en) 2018-03-22
HK1243424A1 (en) 2018-07-13
EA034375B1 (ru) 2020-01-31
CN106661077A (zh) 2017-05-10
EP3279207A1 (en) 2018-02-07
JP2018513832A (ja) 2018-05-31
WO2016155593A1 (zh) 2016-10-06

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