AU2017379850B2 - Antiviral aliphatic ester prodrugs of tenofovir - Google Patents

Antiviral aliphatic ester prodrugs of tenofovir Download PDF

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Publication number
AU2017379850B2
AU2017379850B2 AU2017379850A AU2017379850A AU2017379850B2 AU 2017379850 B2 AU2017379850 B2 AU 2017379850B2 AU 2017379850 A AU2017379850 A AU 2017379850A AU 2017379850 A AU2017379850 A AU 2017379850A AU 2017379850 B2 AU2017379850 B2 AU 2017379850B2
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AU
Australia
Prior art keywords
hiv
methyl
amino
oxy
mmol
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Ceased
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AU2017379850A
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AU2017379850A1 (en
Inventor
Daniel Da Costa
David Dukhan
Jean-Laurent Paparin
Houcine Rahali
Izzat RAHEEM
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MSD International GmbH
Merck Sharp and Dohme LLC
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MSD International Holdings GmbH
Merck Sharp and Dohme LLC
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Publication of AU2017379850A1 publication Critical patent/AU2017379850A1/en
Application granted granted Critical
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Assigned to MSD INTERNATIONAL GMBH reassignment MSD INTERNATIONAL GMBH Request for Assignment Assignors: IDENIX PHARMACEUTICALS LLC, MERCK SHARP & DOHME CORP.
Ceased legal-status Critical Current
Anticipated expiration legal-status Critical

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561Heterocyclic 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
    • C07F9/65616Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52Purines, e.g. adenine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/66Phosphorus compounds
    • A61K31/675Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • 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
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D473/00Heterocyclic compounds containing purine ring systems
    • C07D473/26Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32Nitrogen atom
    • C07D473/34Nitrogen atom attached in position 6, e.g. adenine
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • YGENERAL 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
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against 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)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Virology (AREA)
  • Molecular Biology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Communicable Diseases (AREA)
  • Oncology (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)
AU2017379850A 2016-12-22 2017-12-20 Antiviral aliphatic ester prodrugs of tenofovir Ceased AU2017379850B2 (en)

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 (2)

Publication Number Publication Date
AU2017379850A1 AU2017379850A1 (en) 2019-06-13
AU2017379850B2 true AU2017379850B2 (en) 2022-03-24

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Application Number Title Priority Date Filing Date
AU2017379850A Ceased AU2017379850B2 (en) 2016-12-22 2017-12-20 Antiviral aliphatic ester prodrugs of tenofovir

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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RU2759902C2 (ru) 2021-11-18
CN110099912B (zh) 2021-10-15
EP3559011A1 (en) 2019-10-30
US10519159B2 (en) 2019-12-31
MX388757B (es) 2025-03-20
WO2018119013A1 (en) 2018-06-28
JP2020504733A (ja) 2020-02-13
RU2019122414A (ru) 2021-01-25
US20180179208A1 (en) 2018-06-28
CA3047573A1 (en) 2018-06-28
RU2019122414A3 (enExample) 2021-04-26
EP3559011B1 (en) 2022-04-13
MX2019007585A (es) 2019-09-09
CN110099912A (zh) 2019-08-06
BR112019013017A2 (pt) 2020-01-14
MA47094A (fr) 2021-05-26
TW201829412A (zh) 2018-08-16
AU2017379850A1 (en) 2019-06-13
JP6938637B2 (ja) 2021-09-22
KR20190100250A (ko) 2019-08-28

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