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WO2022256490A3 - Improved synthesis of phosphoramidates for the treatment of hepatitis b virus - Google Patents

Improved synthesis of phosphoramidates for the treatment of hepatitis b virus Download PDF

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Publication number
WO2022256490A3
WO2022256490A3 PCT/US2022/031904 US2022031904W WO2022256490A3 WO 2022256490 A3 WO2022256490 A3 WO 2022256490A3 US 2022031904 W US2022031904 W US 2022031904W WO 2022256490 A3 WO2022256490 A3 WO 2022256490A3
Authority
WO
WIPO (PCT)
Prior art keywords
treatment
hepatitis
virus
phosphoramidates
improved synthesis
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
PCT/US2022/031904
Other languages
French (fr)
Other versions
WO2022256490A9 (en
WO2022256490A2 (en
Inventor
Mark Andrew LOCKWOOD
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Antios Therapeutics Inc
Original Assignee
Antios Therapeutics Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Antios Therapeutics Inc filed Critical Antios Therapeutics Inc
Publication of WO2022256490A2 publication Critical patent/WO2022256490A2/en
Publication of WO2022256490A3 publication Critical patent/WO2022256490A3/en
Publication of WO2022256490A9 publication Critical patent/WO2022256490A9/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H1/00—Processes for the preparation of sugar derivatives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H1/00—Processes for the preparation of sugar derivatives
    • C07H1/02—Phosphorylation
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H13/00—Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids
    • C07H13/02—Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids by carboxylic acids
    • C07H13/08—Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids by carboxylic acids having the esterifying carboxyl radicals directly attached to carbocyclic rings
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H23/00—Compounds containing boron, silicon or a metal, e.g. chelates or vitamin B12

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • General Health & Medical Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)

Abstract

The synthesis of phosphoramidate prodrugs useful in the treatment of viral infections is disclosed. Specifically, an improved synthesis of phosphoramidate nucleotides useful in the treatment of Hepatitis B virus is disclosed.
PCT/US2022/031904 2021-06-03 2022-06-02 Improved synthesis of phosphoramidates for the treatment of hepatitis b virus Ceased WO2022256490A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US202163196418P 2021-06-03 2021-06-03
US63/196,418 2021-06-03

Publications (3)

Publication Number Publication Date
WO2022256490A2 WO2022256490A2 (en) 2022-12-08
WO2022256490A3 true WO2022256490A3 (en) 2023-01-05
WO2022256490A9 WO2022256490A9 (en) 2023-08-17

Family

ID=84323546

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2022/031904 Ceased WO2022256490A2 (en) 2021-06-03 2022-06-02 Improved synthesis of phosphoramidates for the treatment of hepatitis b virus

Country Status (1)

Country Link
WO (1) WO2022256490A2 (en)

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5672697A (en) * 1991-02-08 1997-09-30 Gilead Sciences, Inc. Nucleoside 5'-methylene phosphonates
US20190062364A1 (en) * 2014-12-15 2019-02-28 Emory University Phosphoramidates for the treatment of hepatitis b virus
US20190350954A1 (en) * 2016-06-24 2019-11-21 Emory University Phosphoramidates for the treatment of hepatitis b virus

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5672697A (en) * 1991-02-08 1997-09-30 Gilead Sciences, Inc. Nucleoside 5'-methylene phosphonates
US20190062364A1 (en) * 2014-12-15 2019-02-28 Emory University Phosphoramidates for the treatment of hepatitis b virus
US20190350954A1 (en) * 2016-06-24 2019-11-21 Emory University Phosphoramidates for the treatment of hepatitis b virus

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
DATABASE PUBCHEM SUBSTANCE 2 June 2019 (2019-06-02), ANONYMOUS : "AKOS015951181", XP093021754, retrieved from PUBCHEM Database accession no. 152090600 *
S QUIRES ET AL.: "ATI-2173, a Novel Liver-Targeted Non-Chain-Terminating Nucleotide for Hepatitis B Virus Cure Regimens", ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, vol. 64, no. 9, 2020, pages e00836 - 20, XP093013378, DOI: 10.1128/AAC.00836-20 *

Also Published As

Publication number Publication date
WO2022256490A9 (en) 2023-08-17
WO2022256490A2 (en) 2022-12-08

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