ECSP21080535A - Compuestos y métodos para el tratamiento de covid-19 - Google Patents

Compuestos y métodos para el tratamiento de covid-19

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Publication number
ECSP21080535A
ECSP21080535A ECSENADI202180535A ECDI202180535A ECSP21080535A EC SP21080535 A ECSP21080535 A EC SP21080535A EC SENADI202180535 A ECSENADI202180535 A EC SENADI202180535A EC DI202180535 A ECDI202180535 A EC DI202180535A EC SP21080535 A ECSP21080535 A EC SP21080535A
Authority
EC
Ecuador
Prior art keywords
compounds
methods
covid
treatment
cov
Prior art date
Application number
ECSENADI202180535A
Other languages
English (en)
Inventor
Paul Sullivan Bradley
Richard Lillis Jonathan
Louis Hoffman Robert
Louise Hawking Emma
Dimitrova Pencheva Klimentina
Forrest Sammons Matthew
John Thiel Andrew
Rhys Owen Dafydd
Bezawada Padmavani
Youngjin Pettersson Martin
David Ticehurst Martyn
Luthra Suman
Steven Kania Robert
JAINI Rohit
Bryce Tuttle Jamison
Mahadeo Rane Anil
Nathan O'brien Laramy Matthew
Kulkarni Samir
Original Assignee
Pfizer
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 Pfizer filed Critical Pfizer
Publication of ECSP21080535A publication Critical patent/ECSP21080535A/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0821Tripeptides with the first amino acid being heterocyclic, e.g. His, Pro, Trp
    • C07K5/0823Tripeptides with the first amino acid being heterocyclic, e.g. His, Pro, Trp and Pro-amino acid; Derivatives thereof
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/572Five-membered rings
    • C07F9/5728Five-membered rings condensed with carbocyclic rings or carbocyclic ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • C07F9/65583Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/66Phosphorus compounds
    • A61K31/675Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/06Tripeptides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/12Carboxylic acids; Salts or anhydrides thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/08Solutions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/141Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
    • A61K9/145Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/141Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
    • A61K9/146Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic macromolecular compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/19Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles lyophilised, i.e. freeze-dried, solutions or dispersions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Molecular Biology (AREA)
  • Virology (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biochemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biophysics (AREA)
  • Immunology (AREA)
  • Genetics & Genomics (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Cephalosporin Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)

Abstract

La invención se refiere a compuestos de la fórmula I (Ver gráfico línea 3, pagina 154) I en donde R1, R2 y ----- son como se definen en el presente documento, a composiciones farmacéuticas que comprenden los compuestos y a métodos para el tratamiento de COVID-19 en un paciente mediante la administración de cantidades terapéuticamente eficaces de los compuestos y métodos para la inhibición o prevención de la replicación del SARS-CoV-2 con los compuestos.
ECSENADI202180535A 2020-04-05 2021-11-12 Compuestos y métodos para el tratamiento de covid-19 ECSP21080535A (es)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US202063005407P 2020-04-05 2020-04-05
US202063038454P 2020-06-12 2020-06-12
US202063061628P 2020-08-05 2020-08-05
US202063065658P 2020-08-14 2020-08-14
US202063073145P 2020-09-01 2020-09-01
US202063114289P 2020-11-16 2020-11-16
US202163163635P 2021-03-19 2021-03-19

Publications (1)

Publication Number Publication Date
ECSP21080535A true ECSP21080535A (es) 2022-03-31

Family

ID=75478095

Family Applications (1)

Application Number Title Priority Date Filing Date
ECSENADI202180535A ECSP21080535A (es) 2020-04-05 2021-11-12 Compuestos y métodos para el tratamiento de covid-19

Country Status (20)

Country Link
US (1) US11926642B2 (es)
EP (1) EP3953361A1 (es)
JP (1) JP2023519035A (es)
KR (1) KR20210151949A (es)
CN (1) CN114641485A (es)
AU (1) AU2021253796B2 (es)
BR (1) BR112021022778A2 (es)
CA (1) CA3140164A1 (es)
CO (1) CO2021015318A2 (es)
CR (1) CR20210563A (es)
EC (1) ECSP21080535A (es)
IL (1) IL288061A (es)
MX (1) MX2021013934A (es)
PE (1) PE20220765A1 (es)
PH (1) PH12021552872A1 (es)
PY (1) PY2126213A (es)
TW (1) TWI807291B (es)
UY (1) UY39149A (es)
WO (1) WO2021205298A1 (es)
ZA (1) ZA202109010B (es)

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BR112022018793A2 (pt) * 2020-03-20 2022-11-29 Abivax Uso de um composto de fórmula (i) ou (ii) para tratar ou previnir uma infecção por coronaviridae e condições relacionadas, composição farmacêutica e medicamento compreendendo os mesmos, uso de um mirna como um biomarcador de uma infecção por coronaviridae, e método para avaliar uma infecção por coronaviridae
US11124497B1 (en) 2020-04-17 2021-09-21 Pardes Biosciences, Inc. Inhibitors of cysteine proteases and methods of use thereof
US11174231B1 (en) 2020-06-09 2021-11-16 Pardes Biosciences, Inc. Inhibitors of cysteine proteases and methods of use thereof
US12577240B2 (en) 2020-07-11 2026-03-17 Pfizer Inc. Antiviral heteroaryl ketone derivatives
US11351149B2 (en) * 2020-09-03 2022-06-07 Pfizer Inc. Nitrile-containing antiviral compounds
US20220204476A1 (en) * 2020-12-21 2022-06-30 The Governors Of The University Of Alberta Rna virus inhibitor compounds and uses thereof
EP4282420A4 (en) * 2021-01-20 2024-11-27 National University Corporation Hokkaido University ANTIVIRAL AGENT
KR102522788B1 (ko) 2021-01-28 2023-04-18 (주)아이엠디팜 카모스타트 및 니클로사마이드를 포함하는 공결정, 이를 포함하는 약학 조성물 및 이의 제조 방법
HRP20250770T1 (hr) 2021-04-14 2025-08-29 Shionogi & Co., Ltd. Derivati triazina koji imaju inhibirajuće djelovanje na replikaciju virusa i farmaceutski pripravak koji ih sadrži
US20230033285A1 (en) * 2021-06-16 2023-02-02 The Scripps Research Institute Protease Inhibitors for Treatment of Coronavirus Infections
AU2022353486A1 (en) 2021-09-28 2024-05-02 National University Corporation Hokkaido University Pharmaceutical composition containing triazine derivative
WO2023054292A1 (ja) 2021-09-28 2023-04-06 塩野義製薬株式会社 トリアジン誘導体を含有する医薬組成物
EP4289432A4 (en) 2021-11-24 2025-01-15 Shionogi & Co., Ltd PREPARATION FOR ORAL ADMINISTRATION CONTAINING TRIAZINE DERIVATIVES
WO2023095860A1 (ja) * 2021-11-26 2023-06-01 塩野義製薬株式会社 3clプロテアーゼ阻害剤及びcovid-19治療用薬剤を組み合わせることを特徴とするcovid-19治療用医薬
WO2023182840A1 (ko) * 2022-03-25 2023-09-28 주식회사 미토이뮨테라퓨틱스 항바이러스용 약학적 조성물 및 이의 용도
WO2023196412A1 (en) * 2022-04-06 2023-10-12 Nobias Therapeutics, Inc. Liquid formulations comprising mitogen-activated protein kinase kinase (mek) inhibitors and methods using same
US12545687B2 (en) 2022-04-08 2026-02-10 Shionogi & Co., Ltd. Uracil derivatives having virus replication inhibitory activity and pharmaceutical composition comprising the same
CN114773405B (zh) * 2022-06-21 2022-09-23 和鼎(南京)医药技术有限公司 一种莫那比拉韦的制备方法
CN115054593B (zh) * 2022-07-15 2023-02-03 深圳市人民医院 防治新型冠状病毒肺炎或检测新冠病毒及突变株的药物及应用
WO2024089159A1 (en) 2022-10-27 2024-05-02 Ubiq Holding B.V. Main protease inhibitors
CN115785080B (zh) * 2022-12-16 2024-10-11 陕西盘龙药业集团股份有限公司 一种尿嘧啶母核类化合物及其制备方法和应用
TW202523308A (zh) * 2023-10-05 2025-06-16 日商塩野義製藥股份有限公司 含有尿嘧啶衍生物之製劑
JP7674711B1 (ja) * 2023-10-05 2025-05-12 塩野義製薬株式会社 ウラシル誘導体を含有する医薬組成物

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KR20060118486A (ko) 2003-11-20 2006-11-23 노보 노르디스크 헬스 케어 악티엔게젤샤프트 인자 xi의 치료적 사용
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US10316021B2 (en) * 2016-11-28 2019-06-11 Pfizer Inc. Heteroarylphenoxy benzamide kappa opioid ligands

Also Published As

Publication number Publication date
IL288061A (en) 2022-01-01
TW202202148A (zh) 2022-01-16
JP2023519035A (ja) 2023-05-10
PE20220765A1 (es) 2022-05-16
TWI807291B (zh) 2023-07-01
WO2021205298A1 (en) 2021-10-14
CN114641485A (zh) 2022-06-17
US11926642B2 (en) 2024-03-12
BR112021022778A2 (pt) 2022-11-22
CO2021015318A2 (es) 2021-11-19
AU2021253796A1 (en) 2021-12-09
EP3953361A1 (en) 2022-02-16
MX2021013934A (es) 2021-12-15
US20220017548A1 (en) 2022-01-20
PH12021552872A1 (en) 2022-03-21
UY39149A (es) 2021-10-29
CR20210563A (es) 2022-01-24
CA3140164A1 (en) 2021-10-14
ZA202109010B (en) 2023-09-27
PY2126213A (es) 2022-10-12
AU2021253796B2 (en) 2023-06-01
KR20210151949A (ko) 2021-12-14

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