CA3029315A1 - Phosphoramidates for the treatment of hepatitis b virus - Google Patents

Phosphoramidates for the treatment of hepatitis b virus Download PDF

Info

Publication number
CA3029315A1
CA3029315A1 CA3029315A CA3029315A CA3029315A1 CA 3029315 A1 CA3029315 A1 CA 3029315A1 CA 3029315 A CA3029315 A CA 3029315A CA 3029315 A CA3029315 A CA 3029315A CA 3029315 A1 CA3029315 A1 CA 3029315A1
Authority
CA
Canada
Prior art keywords
substituted
alkyl
amino
alkynyl
alkenyl
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.)
Pending
Application number
CA3029315A
Other languages
English (en)
French (fr)
Inventor
Abel De La Rosa
George Painter
Gregory R. Bluemling
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.)
Emory University
Original Assignee
Emory University
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 Emory University filed Critical Emory University
Publication of CA3029315A1 publication Critical patent/CA3029315A1/en
Pending legal-status Critical Current

Links

Classifications

    • 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
    • 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Virology (AREA)
  • Biotechnology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (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)
CA3029315A 2016-06-24 2017-06-23 Phosphoramidates for the treatment of hepatitis b virus Pending CA3029315A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
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

Publications (1)

Publication Number Publication Date
CA3029315A1 true CA3029315A1 (en) 2017-12-28

Family

ID=60783488

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3029315A Pending CA3029315A1 (en) 2016-06-24 2017-06-23 Phosphoramidates for the treatment of hepatitis b virus

Country Status (14)

Country Link
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=)

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN107428792B (zh) * 2014-12-15 2023-01-24 埃默里大学 用于治疗乙型肝炎病毒的磷酰胺
KR102708995B1 (ko) * 2018-01-10 2024-09-23 누코리온 파마슈티컬스, 인코포레이티드. 포스포르(포스포론)아미다타세탈 및 포스프(온)아탈세탈 화합물
CA3096264A1 (en) * 2018-04-12 2019-10-17 Modis Therapeutics Inc. Prodrugs of deoxynucleosides for treatment of diseases cased by unbalanced nucleotide pools
JP7496132B2 (ja) * 2018-08-31 2024-06-06 国立大学法人 鹿児島大学 核酸アナログ及び抗ｂ型肝炎ウイルス剤
US11166976B2 (en) 2018-11-08 2021-11-09 Aligos Therapeutics, Inc. S-antigen transport inhibiting oligonucleotide polymers and methods
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
MX2022000573A (es) 2019-07-17 2022-02-10 Nucorion Pharmaceuticals Inc Compuestos ciclicos de desoxirribonucleotido.
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
CN115715190B (zh) * 2020-04-02 2025-08-29 密歇根大学董事会 用于治疗病毒感染的瑞德西韦和瑞德西韦类似物、溶液剂以及纳米粒子、脂质体和微粒组合物
CN113493481B (zh) 2020-04-08 2025-02-18 北京君科华元医药科技有限公司 单磷酸恩替卡韦丙氨酰胺酚酯及其医药用途
WO2021216431A1 (en) 2020-04-21 2021-10-28 Ligand Pharmaceuticals, Inc. 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
US20250092401A1 (en) * 2022-01-28 2025-03-20 Glaxosmithkline Intellectual Property Development Limited Combination therapy for treating 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

Family Cites Families (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3687931A (en) 1970-03-19 1972-08-29 Syntex Corp Halogenated purine and pyrimidine nucleosides and process therefor
US5587362A (en) 1994-01-28 1996-12-24 Univ. Of Ga Research Foundation L-nucleosides
US7462605B2 (en) 1998-01-23 2008-12-09 Celmed Oncology (Usa), Inc. Phosphoramidate compounds and methods of use
MY164523A (en) 2000-05-23 2017-12-29 Univ Degli Studi Cagliari Methods and compositions for treating hepatitis c virus
US20040229839A1 (en) 2003-05-14 2004-11-18 Biocryst Pharmaceuticals, Inc. Substituted nucleosides, preparation thereof and use as inhibitors of RNA viral polymerases
GB0317009D0 (en) 2003-07-21 2003-08-27 Univ Cardiff Chemical compounds
WO2006063149A1 (en) 2004-12-09 2006-06-15 Regents Of The University Of Minnesota Nucleosides with antiviral and anticancer activity
EA016838B1 (ru) 2005-06-07 2012-07-30 Йельский Университет Способы лечения рака и других заболеваний или патологических состояний с применением клевудина (lfmau) и телбивудина (ldt)
US7888330B2 (en) 2005-11-09 2011-02-15 Wayne State University Phosphoramidate derivatives of FAU
US7964580B2 (en) 2007-03-30 2011-06-21 Pharmasset, Inc. Nucleoside phosphoramidate prodrugs
HUE025528T2 (en) 2008-04-23 2016-05-30 Gilead Sciences Inc 1'-substituted carba-nucleoside analogs for antiviral treatment
SG184324A1 (en) 2010-03-31 2012-11-29 Gilead Pharmasset Llc Nucleoside phosphoramidates
NZ607996A (en) 2010-09-22 2014-07-25 Alios Biopharma Inc Substituted nucleotide analogs
WO2012078416A2 (en) * 2010-12-06 2012-06-14 Rfs Pharma, Llc Monophosphate prodrugs of dapd and analogs thereof
WO2013013009A2 (en) 2011-07-19 2013-01-24 Nanjing Molecular Research, Inc. 2',3'-DIDEOXY-2'-α-FLUORO-2'-β-C-METHYLNUCLEOSIDES AND PRODRUGS THEREOF
HK1214270A1 (zh) * 2012-10-29 2016-07-22 共晶制药股份有限公司 用於治療病毒感染和癌症的嘧啶核苷及其單磷酸酯前藥
US20140140951A1 (en) 2012-11-14 2014-05-22 Idenix Pharmaceuticals, Inc. D-Alanine Ester of Rp-Nucleoside Analog
WO2014160484A1 (en) 2013-03-13 2014-10-02 Idenix Pharmaceuticals, Inc. Amino acid phosphoramidate pronucleotides of 2'-cyano, azido and amino nucleosides for the treatment of hcv
US9447132B2 (en) 2013-04-12 2016-09-20 Achillion Pharmaceuticals, Inc. Highly active nucleoside derivative for the treatment of HCV
CN107428792B (zh) * 2014-12-15 2023-01-24 埃默里大学 用于治疗乙型肝炎病毒的磷酰胺

Also Published As

Publication number Publication date
ZA201900156B (en) 2019-08-28
PH12018550207A1 (en) 2019-04-15
AU2017281531A1 (en) 2019-01-17
US20220280542A1 (en) 2022-09-08
EP3474863A4 (en) 2020-03-25
CN109689065A (zh) 2019-04-26
JP2019525905A (ja) 2019-09-12
US20190350954A1 (en) 2019-11-21
IL263859B2 (en) 2023-07-01
EA201990059A1 (ru) 2019-07-31
JP2022116024A (ja) 2022-08-09
SG11201811316YA (en) 2019-01-30
IL263859A (en) 2019-01-31
WO2017223421A1 (en) 2017-12-28
BR112018076913A2 (pt) 2019-04-02
KR20190057277A (ko) 2019-05-28
EP3474863A1 (en) 2019-05-01
IL263859B1 (en) 2023-03-01
US11364257B2 (en) 2022-06-21

Similar Documents

Publication Publication Date Title
US11981699B2 (en) Phosphoramidates for the treatment of hepatitis B virus
US20220280542A1 (en) Phosphoramidates for the treatment of hepatitis b virus
JP6757294B2 (ja) フィロウイルス科ウイルス感染症を処置するための方法
US11192914B2 (en) Alkyne containing nucleotide and nucleoside therapeutic compositions and uses related thereto
WO2023044104A1 (en) Phosphoramidates for the treatment of hepatitis b virus
EA039123B1 (ru) Фосфорамидаты для лечения вируса гепатита в
HK1244812B (en) Phosphoramidates for the treatment of hepatitis b virus

Legal Events

Date Code Title Description
EEER Examination request

Effective date: 20220525