CA2958546C - 2'-chloro aminopyrimidinone and pyrimidine dione nucleosides - Google Patents

2'-chloro aminopyrimidinone and pyrimidine dione nucleosides Download PDF

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Publication number
CA2958546C
CA2958546C CA2958546A CA2958546A CA2958546C CA 2958546 C CA2958546 C CA 2958546C CA 2958546 A CA2958546 A CA 2958546A CA 2958546 A CA2958546 A CA 2958546A CA 2958546 C CA2958546 C CA 2958546C
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Prior art keywords
reaction
compound
pharmaceutically acceptable
acceptable salt
formula
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CA2958546A
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English (en)
French (fr)
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CA2958546A1 (en
Inventor
Michael O'neil Hanrahan Clarke
Richard L. Mackman
Dustin Siegel
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Gilead Sciences Inc
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Gilead Sciences Inc
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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
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • 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
    • 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
    • C07H19/073—Pyrimidine radicals with 2-deoxyribosyl as the saccharide radical
    • 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

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Genetics & Genomics (AREA)
  • Biotechnology (AREA)
  • Biochemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Virology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CA2958546A 2014-08-21 2015-08-19 2'-chloro aminopyrimidinone and pyrimidine dione nucleosides Active CA2958546C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201462040349P 2014-08-21 2014-08-21
US62/040,349 2014-08-21
PCT/US2015/045849 WO2016028866A1 (en) 2014-08-21 2015-08-19 2'-chloro aminopyrimidinone and pyrimidine dione nucleosides

Publications (2)

Publication Number Publication Date
CA2958546A1 CA2958546A1 (en) 2016-02-25
CA2958546C true CA2958546C (en) 2020-06-23

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CA2958546A Active CA2958546C (en) 2014-08-21 2015-08-19 2'-chloro aminopyrimidinone and pyrimidine dione nucleosides

Country Status (17)

Country Link
US (6) US9617295B2 (enExample)
EP (2) EP3738969A1 (enExample)
JP (2) JP6765364B2 (enExample)
KR (1) KR102528928B1 (enExample)
CN (1) CN106573954A (enExample)
AR (1) AR101561A1 (enExample)
AU (1) AU2015305593C1 (enExample)
BR (1) BR112017003242A2 (enExample)
CA (1) CA2958546C (enExample)
EA (1) EA201790234A1 (enExample)
ES (1) ES2808868T3 (enExample)
IL (1) IL250426A0 (enExample)
MX (1) MX2017002288A (enExample)
NZ (1) NZ728707A (enExample)
SG (1) SG11201700810SA (enExample)
TW (1) TWI673283B (enExample)
WO (1) WO2016028866A1 (enExample)

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Publication number Publication date
BR112017003242A2 (pt) 2017-11-28
JP2017525699A (ja) 2017-09-07
MX2017002288A (es) 2017-05-22
US20200087337A1 (en) 2020-03-19
TWI673283B (zh) 2019-10-01
CN106573954A (zh) 2017-04-19
US20160052953A1 (en) 2016-02-25
EP3183261B1 (en) 2020-06-17
KR102528928B1 (ko) 2023-05-08
KR20170042643A (ko) 2017-04-19
US20190202852A1 (en) 2019-07-04
WO2016028866A1 (en) 2016-02-25
JP2020111608A (ja) 2020-07-27
US9982006B2 (en) 2018-05-29
US20180340004A1 (en) 2018-11-29
AU2015305593A1 (en) 2017-02-23
AU2015305593B2 (en) 2018-05-17
US9617295B2 (en) 2017-04-11
EA201790234A1 (ru) 2017-07-31
TW201619178A (zh) 2016-06-01
SG11201700810SA (en) 2017-03-30
NZ728707A (en) 2018-06-29
EP3183261A1 (en) 2017-06-28
JP6765364B2 (ja) 2020-10-07
AU2015305593C1 (en) 2018-11-15
US20170327526A1 (en) 2017-11-16
US20200157137A1 (en) 2020-05-21
EP3738969A1 (en) 2020-11-18
IL250426A0 (en) 2017-03-30
AR101561A1 (es) 2016-12-28
CA2958546A1 (en) 2016-02-25
ES2808868T3 (es) 2021-03-02

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