JP6769000B2 - ４’−チオヌクレオシドの新規な化合物、並びにその調製方法、その医薬組成物及びその用途 - Google Patents

４’−チオヌクレオシドの新規な化合物、並びにその調製方法、その医薬組成物及びその用途 Download PDF

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JP6769000B2
JP6769000B2 JP2017541855A JP2017541855A JP6769000B2 JP 6769000 B2 JP6769000 B2 JP 6769000B2 JP 2017541855 A JP2017541855 A JP 2017541855A JP 2017541855 A JP2017541855 A JP 2017541855A JP 6769000 B2 JP6769000 B2 JP 6769000B2
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compound
pharmaceutical composition
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amino
pharmaceutically acceptable
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JP2018513832A5 (enExample
JP2018513832A (ja
Inventor
フン イェ，
フン イェ，
ガン リュウ，
ガン リュウ，
ナン ユ，
ナン ユ，
フン ツェン，
フン ツェン，
ミンリャン ツァオ，
ミンリャン ツァオ，
ヤン チン，
ヤン チン，
フワ デン，
フワ デン，
ウェンジァ リ，
ウェンジァ リ，
ドンフン リ，
ドンフン リ，
ドンハイ スー，
ドンハイ スー，
ウェイ ツゥン，
ウェイ ツゥン，
シャオフワ リ，
シャオフワ リ，
シュンウェイ ウー，
シュンウェイ ウー，
リチュン ワン，
リチュン ワン，
ジンイ ワン，
ジンイ ワン，
Original Assignee
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
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
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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
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    • C07—ORGANIC CHEMISTRY
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    • 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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  • Medicinal Chemistry (AREA)
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  • Animal Behavior & Ethology (AREA)
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  • Genetics & Genomics (AREA)
  • Biotechnology (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Communicable Diseases (AREA)
  • Virology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2017541855A 2015-04-03 2016-03-28 ４’−チオヌクレオシドの新規な化合物、並びにその調製方法、その医薬組成物及びその用途 Expired - Fee Related JP6769000B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201510157772 2015-04-03
CN201510157772.0 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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JP2018513832A JP2018513832A (ja) 2018-05-31
JP2018513832A5 JP2018513832A5 (enExample) 2019-03-28
JP6769000B2 true JP6769000B2 (ja) 2020-10-14

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JP2017541855A Expired - Fee Related JP6769000B2 (ja) 2015-04-03 2016-03-28 ４’−チオヌクレオシドの新規な化合物、並びにその調製方法、その医薬組成物及びその用途

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US (2) US10662214B2 (enExample)
EP (1) EP3279207B1 (enExample)
JP (1) JP6769000B2 (enExample)
CN (2) CN109553651B (enExample)
AU (1) AU2016240117C1 (enExample)
CA (1) CA2975990A1 (enExample)
EA (1) EA034375B1 (enExample)
WO (1) WO2016155593A1 (enExample)

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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
CN107011168B (zh) 2012-08-13 2020-06-09 富士胶片株式会社 胞嘧啶类的合成中间体和硫代核苷的合成中间体
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
CN109553651B (zh) * 2015-04-03 2021-08-06 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
CA3035334C (en) 2016-08-31 2022-05-10 Fujifilm Corporation Combination of paclitaxel and 1-(2-deoxy-2-fluoro-4-thio-beta-d-arabinofuranosyl)-cytosine as anti-tumor agent
EA201990780A1 (ru) * 2016-12-22 2019-11-29 Твердая форма соединения 4'-тио-2'-фторнуклеозид фосфамида и способ его получения и применения
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
EP3677267A4 (en) * 2017-09-01 2021-06-02 Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. PHARMACEUTICAL COMPOSITION FOR TREATMENT OR PREVENTION OF TUMORS, METHOD AND USES THEREOF
CA3089728C (en) * 2018-01-29 2023-01-10 Fujifilm Corporation Antitumor agent for biliary tract cancer and method for treating biliary tract cancer
AU2019256465B2 (en) * 2018-04-19 2024-10-03 Southern Research Institute 4'-thio-nucleotide and -nucleoside prodrugs for the treatment of cancer
CN112770731A (zh) * 2018-11-28 2021-05-07 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
JP2022542697A (ja) * 2019-07-30 2022-10-06 ピノットバイオ，インコーポレイテッド 癌治療用ジヌクレオチド化合物及びその医薬用途
WO2021216936A1 (en) 2020-04-23 2021-10-28 Southern Research Institute Composition for treating 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
EP0841344B1 (en) * 1996-04-09 2002-09-25 Yamasa Corporation 1-(2-deoxy-2-fluoro-4-thio-beta-d-arabinofuranosyl)cytosines
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
WO2007056596A2 (en) * 2005-11-09 2007-05-18 Wayne State University Phosphoramidate derivatives of fau
GB201016855D0 (en) 2010-10-06 2010-11-17 Nucana Biomed Ltd Chemical compounds
EP2734535A4 (en) * 2011-07-19 2014-10-22 Nanjing Molecular Res Inc 2 ', 3'-DIDEOXY-2'-ALPHA-FLUOR-2'-BETA-C-METHYL NUCLEOSIDE AND PRODRUGS THEREOF
WO2014124430A1 (en) * 2013-02-11 2014-08-14 Emory University Nucleotide and nucleoside therapeutic compositions and uses related thereto
US10005779B2 (en) * 2013-06-05 2018-06-26 Idenix Pharmaceuticals Llc 1′,4′-thio nucleosides for the treatment of HCV
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
CN109553651B (zh) * 2015-04-03 2021-08-06 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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Publication number Publication date
WO2016155593A1 (zh) 2016-10-06
CN106661077B (zh) 2019-02-12
US20200262860A1 (en) 2020-08-20
EP3279207A4 (en) 2018-11-14
EA034375B1 (ru) 2020-01-31
AU2016240117B2 (en) 2020-08-06
CA2975990A1 (en) 2016-10-06
CN109553651A (zh) 2019-04-02
CN106661077A (zh) 2017-05-10
US20180079770A1 (en) 2018-03-22
US10662214B2 (en) 2020-05-26
HK1243424A1 (en) 2018-07-13
EP3279207A1 (en) 2018-02-07
HK1232229A1 (zh) 2018-01-05
JP2018513832A (ja) 2018-05-31
EP3279207B1 (en) 2024-01-24
AU2016240117C1 (en) 2020-11-26
EA201791535A1 (ru) 2018-01-31
AU2016240117A1 (en) 2017-08-24
CN109553651B (zh) 2021-08-06

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