TWI860279B - 作為hcv rna複製抑制劑之經4'-氟-2'-甲基取代之核苷衍生物 - Google Patents

作為hcv rna複製抑制劑之經4'-氟-2'-甲基取代之核苷衍生物 Download PDF

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Publication number
TWI860279B
TWI860279B TW107133372A TW107133372A TWI860279B TW I860279 B TWI860279 B TW I860279B TW 107133372 A TW107133372 A TW 107133372A TW 107133372 A TW107133372 A TW 107133372A TW I860279 B TWI860279 B TW I860279B
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Taiwan
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formula
amino
compound
methyltetrahydrofuran
difluoro
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TW107133372A
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English (en)
Chinese (zh)
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TW201919649A (zh
Inventor
馬克 史密斯
克勞斯 G 克朗普
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美商里伯賽恩斯有限責任公司
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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
    • 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
    • A61K31/7068—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
    • A61K31/7072—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 having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
    • 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
    • A61P31/14—Antivirals for RNA viruses
    • 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
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Molecular Biology (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Virology (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Biotechnology (AREA)
  • Engineering & Computer Science (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
TW107133372A 2017-09-21 2018-09-21 作為hcv rna複製抑制劑之經4'-氟-2'-甲基取代之核苷衍生物 TWI860279B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201762561237P 2017-09-21 2017-09-21
US62/561,237 2017-09-21

Publications (2)

Publication Number Publication Date
TW201919649A TW201919649A (zh) 2019-06-01
TWI860279B true TWI860279B (zh) 2024-11-01

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TW107133372A TWI860279B (zh) 2017-09-21 2018-09-21 作為hcv rna複製抑制劑之經4'-氟-2'-甲基取代之核苷衍生物

Country Status (12)

Country Link
US (2) US10682369B2 (enExample)
EP (1) EP3684374B1 (enExample)
JP (1) JP7299897B2 (enExample)
KR (1) KR102735678B1 (enExample)
CN (1) CN111194217B (enExample)
AR (1) AR112702A1 (enExample)
AU (1) AU2018335411B2 (enExample)
CA (1) CA3075645A1 (enExample)
IL (1) IL273398B2 (enExample)
SG (1) SG11202002431SA (enExample)
TW (1) TWI860279B (enExample)
WO (1) WO2019060740A1 (enExample)

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EP3684374B1 (en) 2017-09-21 2025-07-30 Riboscience LLC 4'-fluoro-2'-methyl substituted nucleoside derivatives as inhibitors of hcv rna replication
EP3865535A1 (en) 2020-02-11 2021-08-18 Bosti Trading Ltd. New method of synthesis of chitosan derivatives and uses thereof
TW202144465A (zh) 2020-02-11 2021-12-01 瑞士商諾和席卓股份有限公司 合成聚葡萄胺糖衍生物之新方法及其用途
WO2022174179A1 (en) * 2021-02-15 2022-08-18 Emory University 4'-halogen containing nucleotide and nucleoside therapeutic compositions and uses related thereto
AR126678A1 (es) 2021-08-06 2023-11-01 Novochizol Sa Composiciones para el cuidado de las plantas y usos de las mismas
CN117835822A (zh) 2021-08-06 2024-04-05 诺和席卓股份有限公司 包含可溶性交联壳聚糖的复合凝胶、聚合物支架、聚集体和薄膜的制备及其用途

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Publication number Publication date
CN111194217B (zh) 2024-01-12
US10682369B2 (en) 2020-06-16
WO2019060740A1 (en) 2019-03-28
US20190231804A1 (en) 2019-08-01
EP3684374A1 (en) 2020-07-29
IL273398B1 (en) 2024-10-01
AR112702A1 (es) 2019-11-27
US20210046100A1 (en) 2021-02-18
TW201919649A (zh) 2019-06-01
AU2018335411B2 (en) 2024-06-27
US11351186B2 (en) 2022-06-07
SG11202002431SA (en) 2020-04-29
JP2020534374A (ja) 2020-11-26
CA3075645A1 (en) 2019-03-28
EP3684374A4 (en) 2021-06-16
JP7299897B2 (ja) 2023-06-28
IL273398B2 (en) 2025-02-01
AU2018335411A1 (en) 2020-03-26
CN111194217A (zh) 2020-05-22
KR102735678B1 (ko) 2024-11-27
IL273398A (en) 2020-05-31
EP3684374B1 (en) 2025-07-30
KR20200056420A (ko) 2020-05-22

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