CO2022005128A2 - Profármacos antivirales y formulaciones de los mismos - Google Patents

Profármacos antivirales y formulaciones de los mismos

Info

Publication number
CO2022005128A2
CO2022005128A2 CONC2022/0005128A CO2022005128A CO2022005128A2 CO 2022005128 A2 CO2022005128 A2 CO 2022005128A2 CO 2022005128 A CO2022005128 A CO 2022005128A CO 2022005128 A2 CO2022005128 A2 CO 2022005128A2
Authority
CO
Colombia
Prior art keywords
formulations
antiviral prodrugs
prodrugs
antiviral
efda
Prior art date
Application number
CONC2022/0005128A
Other languages
English (en)
Inventor
Arnab Kumar Chatterjee
Anil Kumar Gupta
Anders Mikal Eliasen
Sean Barry Joseph
Original Assignee
Scripps Research Inst
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 Scripps Research Inst filed Critical Scripps Research Inst
Publication of CO2022005128A2 publication Critical patent/CO2022005128A2/es

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
    • 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
    • A61K31/7076—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 containing purines, e.g. adenosine, adenylic 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5365—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/38—Cellulose; Derivatives thereof
    • 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
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • 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
    • 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
    • A61P31/18—Antivirals for RNA viruses for HIV
    • 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
    • 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
    • C07H19/16—Purine radicals
    • 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
    • C07H19/16—Purine radicals
    • C07H19/173—Purine 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
    • C07H19/16—Purine radicals
    • C07H19/20—Purine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Virology (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Genetics & Genomics (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Inorganic Chemistry (AREA)
  • Dispersion Chemistry (AREA)
  • Dermatology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)

Abstract

En la presente se proporcionan compuestos, composiciones y métodos para usar los mismos para el tratamiento y/o la prevención de infecciones de virus tales como VIH y VHB al administrar ciertos ésteres y otros derivados de 4'-etinil-2-fluoro-2'-desoxiadenosina (EFdA) o una sal farmacéuticamente aceptable de los mismos.
CONC2022/0005128A 2019-09-11 2022-04-25 Profármacos antivirales y formulaciones de los mismos CO2022005128A2 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201962898679P 2019-09-11 2019-09-11
PCT/US2020/050519 WO2021050961A1 (en) 2019-09-11 2020-09-11 Antiviral prodrugs and formulations thereof

Publications (1)

Publication Number Publication Date
CO2022005128A2 true CO2022005128A2 (es) 2022-05-10

Family

ID=74866690

Family Applications (2)

Application Number Title Priority Date Filing Date
CONC2022/0005128A CO2022005128A2 (es) 2019-09-11 2022-04-25 Profármacos antivirales y formulaciones de los mismos
CONC2022/0004681A CO2022004681A2 (es) 2019-09-11 2022-06-22 Profármacos antivirales y composiciones farmacéuticas de los mismos

Family Applications After (1)

Application Number Title Priority Date Filing Date
CONC2022/0004681A CO2022004681A2 (es) 2019-09-11 2022-06-22 Profármacos antivirales y composiciones farmacéuticas de los mismos

Country Status (15)

Country Link
US (3) US20220323476A1 (es)
EP (2) EP4028019A4 (es)
JP (2) JP2022547978A (es)
KR (2) KR20220066302A (es)
CN (2) CN114793421A (es)
AU (2) AU2020346908A1 (es)
BR (2) BR112022004417A2 (es)
CA (2) CA3150418A1 (es)
CL (2) CL2022000601A1 (es)
CO (2) CO2022005128A2 (es)
CR (2) CR20220110A (es)
IL (2) IL290861A (es)
MX (2) MX2022002899A (es)
PE (2) PE20221036A1 (es)
WO (2) WO2021050961A1 (es)

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US10675296B2 (en) 2017-07-11 2020-06-09 Gilead Sciences, Inc. Compositions comprising an RNA polymerase inhibitor and cyclodextrin for treating viral infections
US20230045509A1 (en) * 2019-12-09 2023-02-09 Viiv Healthcare Company Pharmaceutical compositions comprising cabotegravir
KR20220132608A (ko) 2020-01-27 2022-09-30 길리애드 사이언시즈, 인코포레이티드 SARS CoV-2 감염증을 치료하기 위한 방법
JP2023516087A (ja) 2020-03-12 2023-04-17 ギリアード サイエンシーズ， インコーポレイテッド １’－シアノヌクレオシドを調製する方法
WO2021188959A1 (en) * 2020-03-20 2021-09-23 Gilead Sciences, Inc. Prodrugs of 4'-c-substituted-2-halo-2'-deoxyadenosine nucleosides and methods of making and using the same
CA3172483A1 (en) 2020-04-06 2021-10-14 Scott Ellis Inhalation formulations of 1'-cyano substituted carbanucleoside analogs
AU2021281351A1 (en) 2020-05-29 2023-01-19 Gilead Sciences, Inc. Remdesivir treatment methods
PE20230618A1 (es) 2020-06-24 2023-04-14 Gilead Sciences Inc Analogos de nucleosido de 1'-ciano y usos de los mismos
IL300453A (en) 2020-08-27 2023-04-01 Gilead Sciences Inc COMPOSITIONS AND METHODS FOR THE TREATMENT OF VIRAL INFECTIONS
TW202400185A (zh) 2022-03-02 2024-01-01 美商基利科學股份有限公司 用於治療病毒感染的化合物及方法

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CA2502109C (en) * 2004-03-24 2010-02-23 Yamasa Corporation 4'-c-substituted-2-haloadenosine derivative
CN100532388C (zh) * 2007-07-16 2009-08-26 郑州大学 2’-氟-4’-取代-核苷类似物、其制备方法及应用
US20090274686A1 (en) * 2008-05-02 2009-11-05 Yat Sun Or Nucleoside phosphonate derivatives
US20130244966A1 (en) * 2011-12-12 2013-09-19 Catabasis Pharmaceuticals, Inc. Fatty acid antiviral conjugates and their uses
WO2015143712A1 (en) * 2014-03-28 2015-10-01 Merck Sharp & Dohme Corp. 4'-substituted nucleoside reverse transcriptase inhibitors
KR102185996B1 (ko) * 2015-09-23 2020-12-02 머크 샤프 앤드 돔 코포레이션 4'-치환된 뉴클레오시드 리버스 트랜스크립타제 억제제 및 그의 제조법
WO2017100108A1 (en) * 2015-12-10 2017-06-15 Merck Sharp & Dohme Corp. Antiviral phosphodiamide prodrugs of tenofovir
EP3706762A4 (en) * 2017-12-07 2021-09-01 Emory University N4-HYDROXYCYTIDINE AND DERIVATIVES AND ANTIVIRAL USES IN RELATION TO IT
WO2019171285A1 (en) * 2018-03-07 2019-09-12 Glaxosmithkline Intellectual Property (No.2) Limited Compounds useful in hiv therapy
WO2021021717A1 (en) * 2019-07-27 2021-02-04 Brii Biosciences, Inc. Adenosine derivative and pharmaceutical composition comprising the same

Also Published As

Publication number Publication date
CN114793421A (zh) 2022-07-26
CA3150418A1 (en) 2021-03-18
AU2020346907A1 (en) 2022-03-24
EP4028019A1 (en) 2022-07-20
PE20221036A1 (es) 2022-06-17
CA3150467A1 (en) 2021-03-18
CR20220110A (es) 2022-06-16
EP4028019A4 (en) 2024-04-17
AU2020346908A1 (en) 2022-03-24
IL290919A (en) 2022-04-01
JP2022547978A (ja) 2022-11-16
CO2022004681A2 (es) 2022-07-19
US20230390318A1 (en) 2023-12-07
US20220323476A1 (en) 2022-10-13
KR20220066302A (ko) 2022-05-24
EP4028020A4 (en) 2023-09-27
CL2022000601A1 (es) 2022-10-28
MX2022002899A (es) 2022-05-16
CL2022000587A1 (es) 2022-10-28
BR112022004424A2 (pt) 2022-05-31
EP4028020A1 (en) 2022-07-20
WO2021050956A1 (en) 2021-03-18
WO2021050961A1 (en) 2021-03-18
KR20220066303A (ko) 2022-05-24
BR112022004417A2 (pt) 2022-06-21
CR20220109A (es) 2022-06-07
US20220332751A1 (en) 2022-10-20
IL290861A (en) 2022-04-01
JP2022547558A (ja) 2022-11-14
PE20221037A1 (es) 2022-06-17
CN114929236B (zh) 2024-06-07
AU2020346908A2 (en) 2022-06-16
AU2020346907A2 (en) 2022-06-16
CN114929236A (zh) 2022-08-19
MX2022002897A (es) 2022-05-16

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