JP6938637B2 - テノホビルの抗ウイルス性脂肪族エステルプロドラッグ - Google Patents

テノホビルの抗ウイルス性脂肪族エステルプロドラッグ Download PDF

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Publication number
JP6938637B2
JP6938637B2 JP2019533490A JP2019533490A JP6938637B2 JP 6938637 B2 JP6938637 B2 JP 6938637B2 JP 2019533490 A JP2019533490 A JP 2019533490A JP 2019533490 A JP2019533490 A JP 2019533490A JP 6938637 B2 JP6938637 B2 JP 6938637B2
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amino
methyl
oxy
propan
phosphoryl
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Expired - Fee Related
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Japanese (ja)
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JP2020504733A5 (enExample
JP2020504733A (ja
Inventor
ラヒーム,イザット
パパラン,ジャン−ローラン
ラハリ,フシーヌ
ダ・コスタ,ダニエル
ドゥハーン,デイビッド
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Merck Sharp & Dohme LLC
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    • 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
    • C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
    • C07F9/65616—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings containing the ring system having three or more than three double bonds between ring members or between ring members and non-ring members, e.g. purine or analogs
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
    • 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
    • A61K31/66—Phosphorus compounds
    • A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • 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
    • A61P31/18—Antivirals for RNA viruses for HIV
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32—Nitrogen atom
    • C07D473/34—Nitrogen atom attached in position 6, e.g. adenine
    • 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
    • C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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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)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Virology (AREA)
  • Molecular Biology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biochemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
JP2019533490A 2016-12-22 2017-12-20 テノホビルの抗ウイルス性脂肪族エステルプロドラッグ Expired - Fee Related JP6938637B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201662437753P 2016-12-22 2016-12-22
US62/437,753 2016-12-22
US201762574493P 2017-10-19 2017-10-19
US62/574,493 2017-10-19
PCT/US2017/067470 WO2018119013A1 (en) 2016-12-22 2017-12-20 Antiviral aliphatic ester prodrugs of tenofovir

Publications (3)

Publication Number Publication Date
JP2020504733A JP2020504733A (ja) 2020-02-13
JP2020504733A5 JP2020504733A5 (enExample) 2021-01-28
JP6938637B2 true JP6938637B2 (ja) 2021-09-22

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JP2019533490A Expired - Fee Related JP6938637B2 (ja) 2016-12-22 2017-12-20 テノホビルの抗ウイルス性脂肪族エステルプロドラッグ

Country Status (13)

Country Link
US (1) US10519159B2 (enExample)
EP (1) EP3559011B1 (enExample)
JP (1) JP6938637B2 (enExample)
KR (1) KR20190100250A (enExample)
CN (1) CN110099912B (enExample)
AU (1) AU2017379850B2 (enExample)
BR (1) BR112019013017A2 (enExample)
CA (1) CA3047573A1 (enExample)
MA (1) MA47094A (enExample)
MX (1) MX388757B (enExample)
RU (1) RU2759902C2 (enExample)
TW (1) TW201829412A (enExample)
WO (1) WO2018119013A1 (enExample)

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RU2019122414A3 (enExample) 2021-04-26
MX388757B (es) 2025-03-20
KR20190100250A (ko) 2019-08-28
MA47094A (fr) 2021-05-26
WO2018119013A1 (en) 2018-06-28
EP3559011B1 (en) 2022-04-13
CN110099912B (zh) 2021-10-15
RU2759902C2 (ru) 2021-11-18
CN110099912A (zh) 2019-08-06
US10519159B2 (en) 2019-12-31
AU2017379850A1 (en) 2019-06-13
TW201829412A (zh) 2018-08-16
US20180179208A1 (en) 2018-06-28
MX2019007585A (es) 2019-09-09
BR112019013017A2 (pt) 2020-01-14
CA3047573A1 (en) 2018-06-28
RU2019122414A (ru) 2021-01-25
EP3559011A1 (en) 2019-10-30
AU2017379850B2 (en) 2022-03-24
JP2020504733A (ja) 2020-02-13

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