JP2019525905A - Ｂ型肝炎ウイルスの治療のためのホスホロアミデート - Google Patents

Ｂ型肝炎ウイルスの治療のためのホスホロアミデート Download PDF

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JP2019525905A
JP2019525905A JP2018567034A JP2018567034A JP2019525905A JP 2019525905 A JP2019525905 A JP 2019525905A JP 2018567034 A JP2018567034 A JP 2018567034A JP 2018567034 A JP2018567034 A JP 2018567034A JP 2019525905 A JP2019525905 A JP 2019525905A
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substituted
alkyl
amino
alkynyl
aryl
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ラ ローザ，アベル デ
ラ ローザ，アベル デ
ペインター，ジョージ
アール． ブルームリング，グレゴリー
アール． ブルームリング，グレゴリー
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エモリー ユニバーシティー
エモリー ユニバーシティー
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Publication of JP2019525905A5 publication Critical patent/JP2019525905A5/ja
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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
    • 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
    • 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
    • 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
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • 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
    • A61K31/522—Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
    • 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
    • A61K31/661—Phosphorus acids or esters thereof not having P—C bonds, e.g. fosfosal, dichlorvos, malathion or mevinphos
    • 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
    • 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
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/10—Dispersions; Emulsions
    • A61K9/127—Synthetic bilayered vehicles, e.g. liposomes or liposomes with cholesterol as the only non-phosphatidyl surfactant
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P31/20—Antivirals for DNA viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • 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)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Virology (AREA)
  • Biotechnology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Dispersion Chemistry (AREA)
  • Gastroenterology & Hepatology (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)
  • Medicinal Preparation (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
  • Materials For Medical Uses (AREA)
JP2018567034A 2016-06-24 2017-06-23 Ｂ型肝炎ウイルスの治療のためのホスホロアミデート Pending JP2019525905A (ja)

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JP2022077781A JP2022116024A (ja) 2016-06-24 2022-05-10 Ｂ型肝炎ウイルスの治療のためのホスホロアミデート

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US201662354471P 2016-06-24 2016-06-24
US62/354,471 2016-06-24
PCT/US2017/038963 WO2017223421A1 (en) 2016-06-24 2017-06-23 Phosphoramidates for the treatment of hepatitis b virus

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JP2022077781A Division JP2022116024A (ja) 2016-06-24 2022-05-10 Ｂ型肝炎ウイルスの治療のためのホスホロアミデート

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JP2019525905A true JP2019525905A (ja) 2019-09-12
JP2019525905A5 JP2019525905A5 (https=) 2020-09-10

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JP2018567034A Pending JP2019525905A (ja) 2016-06-24 2017-06-23 Ｂ型肝炎ウイルスの治療のためのホスホロアミデート
JP2022077781A Withdrawn JP2022116024A (ja) 2016-06-24 2022-05-10 Ｂ型肝炎ウイルスの治療のためのホスホロアミデート

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US (2) US11364257B2 (https=)
EP (1) EP3474863A4 (https=)
JP (2) JP2019525905A (https=)
KR (1) KR20190057277A (https=)
CN (1) CN109689065A (https=)
AU (1) AU2017281531A1 (https=)
BR (1) BR112018076913A2 (https=)
CA (1) CA3029315A1 (https=)
EA (1) EA201990059A1 (https=)
IL (1) IL263859B2 (https=)
PH (1) PH12018550207A1 (https=)
SG (1) SG11201811316YA (https=)
WO (1) WO2017223421A1 (https=)
ZA (1) ZA201900156B (https=)

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JP2023520826A (ja) * 2020-04-08 2023-05-19 北京君科華元医薬科技有限公司 エンテカビルモノホスフェートアラニンアミドフェノールエステル及びその医薬用途

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WO2020103929A1 (zh) * 2018-11-23 2020-05-28 正大天晴药业集团股份有限公司 低聚核苷酸及前体药物
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CN110642910B (zh) * 2019-09-02 2020-10-30 南开大学 胸苷衍生物及其制备方法和用途
WO2021067480A1 (en) * 2019-10-02 2021-04-08 University Of Washington Compositions and methods for treatment of hepatitis b virus infection
CN111087421B (zh) * 2019-12-24 2022-10-18 南京正大天晴制药有限公司 一种用于手性药物合成的磷酰胺化合物的制备方法
US12516080B2 (en) 2020-04-02 2026-01-06 The Regents Of The University Of Michigan Remdesivir and remdesivir analogs, solutions, and nanoparticle, liposomal, and microparticle compositions for treating viral infections
US12552820B2 (en) 2020-04-21 2026-02-17 Ligand Pharmaceuticals Incorporated Benzyloxy phosph(on)ate compounds
WO2021253376A1 (zh) * 2020-06-19 2021-12-23 南京正大天晴制药有限公司 一种用于手性药物合成的磷酰胺化合物的制备方法
WO2022251594A1 (en) * 2021-05-27 2022-12-01 Antios Therapeutics, Inc. Pharmacokinetics and dose-related improvments in subjects treated with phosphoramidate clevudine prodrugs
WO2022256490A2 (en) * 2021-06-03 2022-12-08 Antios Therapeutics, Inc. Improved synthesis of phosphoramidates for the treatment of hepatitis b virus
CN113501853B (zh) * 2021-09-13 2021-12-07 南京颐媛生物医学研究院有限公司 4-硫代尿嘧啶脱氧核苷磷酸酯及其抗病毒药物用途
CA3243401A1 (en) * 2022-01-28 2023-08-03 Glaxosmithkline Intellectual Property Development Limited Polytherapy for the treatment of hepatitis B virus infections
CN115260263B (zh) * 2022-05-23 2025-02-21 浙江扬厉医药技术有限公司 烷基硫芳基克拉夫定磷酰胺类化合物及其应用

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Cited By (2)

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Publication number Priority date Publication date Assignee Title
JP2023520826A (ja) * 2020-04-08 2023-05-19 北京君科華元医薬科技有限公司 エンテカビルモノホスフェートアラニンアミドフェノールエステル及びその医薬用途
JP7452903B2 (ja) 2020-04-08 2024-03-19 北京君科華元医薬科技有限公司 エンテカビルモノホスフェートアラニンアミドフェノールエステル及びその医薬用途

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KR20190057277A (ko) 2019-05-28
US20190350954A1 (en) 2019-11-21
WO2017223421A1 (en) 2017-12-28
CN109689065A (zh) 2019-04-26
IL263859A (en) 2019-01-31
US20220280542A1 (en) 2022-09-08
EA201990059A1 (ru) 2019-07-31
JP2022116024A (ja) 2022-08-09
ZA201900156B (en) 2019-08-28
US11364257B2 (en) 2022-06-21
SG11201811316YA (en) 2019-01-30
AU2017281531A1 (en) 2019-01-17
PH12018550207A1 (en) 2019-04-15
EP3474863A1 (en) 2019-05-01
IL263859B1 (en) 2023-03-01
CA3029315A1 (en) 2017-12-28
IL263859B2 (en) 2023-07-01
BR112018076913A2 (pt) 2019-04-02
EP3474863A4 (en) 2020-03-25

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