JP5496899B2 - シチジンデアミナーゼ阻害剤としての2’−フルオロ−2’−デオキシテトラヒドロウリジン - Google Patents

シチジンデアミナーゼ阻害剤としての2’−フルオロ−2’−デオキシテトラヒドロウリジン Download PDF

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JP5496899B2
JP5496899B2 JP2010530110A JP2010530110A JP5496899B2 JP 5496899 B2 JP5496899 B2 JP 5496899B2 JP 2010530110 A JP2010530110 A JP 2010530110A JP 2010530110 A JP2010530110 A JP 2010530110A JP 5496899 B2 JP5496899 B2 JP 5496899B2
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compound
cancer
pharmaceutically acceptable
acceptable salt
fluoro
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JP2011500713A (ja
JP2011500713A5 (https=
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グレゴリー エス ハミルトン
尚 塚本
ダナ ヴィー ファラリス
ブリジェット デュヴァル
レナ ラピダス
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エイザイ インコーポレイテッド
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/06Pyrimidine radicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706Compounds 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
    • A61K31/7064Compounds 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
    • A61K31/7068Compounds 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H1/00Processes for the preparation of sugar derivatives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/06Pyrimidine radicals
    • C07H19/073Pyrimidine radicals with 2-deoxyribosyl as the saccharide radical
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
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  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
JP2010530110A 2007-10-16 2008-10-16 シチジンデアミナーゼ阻害剤としての2’−フルオロ−2’−デオキシテトラヒドロウリジン Active JP5496899B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US98039707P 2007-10-16 2007-10-16
US60/980,397 2007-10-16
PCT/US2008/080163 WO2009052287A1 (en) 2007-10-16 2008-10-16 2 ' -flu0r0-2 ' -deoxytetrahydrouridines as cytidine deaminase inhibitors

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JP2014043175A Division JP5859588B2 (ja) 2007-10-16 2014-03-05 シチジンデアミナーゼ阻害剤としての2’−フルオロ−2’−デオキシテトラヒドロウリジン

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JP2011500713A JP2011500713A (ja) 2011-01-06
JP2011500713A5 JP2011500713A5 (https=) 2011-12-01
JP5496899B2 true JP5496899B2 (ja) 2014-05-21

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JP2014043175A Active JP5859588B2 (ja) 2007-10-16 2014-03-05 シチジンデアミナーゼ阻害剤としての2’−フルオロ−2’−デオキシテトラヒドロウリジン

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US (4) US8268800B2 (https=)
EP (2) EP2447272B1 (https=)
JP (2) JP5496899B2 (https=)
KR (1) KR101543049B1 (https=)
CN (1) CN101827856B (https=)
AT (1) ATE548374T1 (https=)
BR (1) BRPI0818672B8 (https=)
CA (1) CA2702274C (https=)
CO (1) CO6270330A2 (https=)
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DK (1) DK2207786T3 (https=)
EA (1) EA018757B1 (https=)
EC (1) ECSP10010095A (https=)
ES (2) ES2616566T3 (https=)
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FR (2) FR23C1051I2 (https=)
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UA (1) UA99476C2 (https=)
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JP2012522842A (ja) * 2009-04-06 2012-09-27 エーザイ インコーポレイテッド シチジンベースの抗新生物薬とシチジンデアミナーゼ阻害薬との組合せ、および癌の治療におけるその使用
JP2014177455A (ja) * 2007-10-16 2014-09-25 Eisai Inc シチジンデアミナーゼ阻害剤としての2’−フルオロ−2’−デオキシテトラヒドロウリジン

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US11116782B2 (en) 2002-10-15 2021-09-14 Celgene Corporation Methods of treating myelodysplastic syndromes with a combination therapy using lenalidomide and azacitidine
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JP5687687B2 (ja) 2009-04-06 2015-03-18 大塚製薬株式会社 癌を治療するための(2’−デオキシ−リボフラノシル)−1,3,4,7−テトラヒドロ−(1,3)ジアゼピン−2−オン誘導体
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WO2020080912A1 (ko) * 2018-10-19 2020-04-23 인터올리고 주식회사 치료 효능을 개선한 핵산 변형체 및 이를 포함하는 항암용 약학 조성물
PH12022550795A1 (en) * 2019-10-08 2023-09-25 Otsuka Pharma Co Ltd 2`-deoxy-2`,2`-difluorotetrahydrouridines with high purity and methods of making the same
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