CN115916806A - 作为sars-cov-2抗病毒药物的脂质-肽融合抑制剂 - Google Patents

作为sars-cov-2抗病毒药物的脂质-肽融合抑制剂 Download PDF

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Publication number
CN115916806A
CN115916806A CN202180044021.1A CN202180044021A CN115916806A CN 115916806 A CN115916806 A CN 115916806A CN 202180044021 A CN202180044021 A CN 202180044021A CN 115916806 A CN115916806 A CN 115916806A
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peptide
lipid
seq
cov
sars
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CN202180044021.1A
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English (en)
Chinese (zh)
Inventor
M·波罗托
A·莫斯科纳
S·格尔曼
V·奥特洛
Z·于
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Columbia University in the City of New York
Wisconsin Alumni Research Foundation
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Columbia University in the City of New York
Wisconsin Alumni Research Foundation
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Publication of CN115916806A publication Critical patent/CN115916806A/zh
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    • 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
    • A61K47/50—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/554—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being a steroid plant sterol, glycyrrhetic acid, enoxolone or bile acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/005—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from viruses
    • 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
    • A61K47/50—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/542—Carboxylic acids, e.g. a fatty acid or an amino acid
    • 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
    • A61K47/50—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/543—Lipids, e.g. triglycerides; Polyamines, e.g. spermine or spermidine
    • 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
    • A61K47/50—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/545—Heterocyclic compounds
    • A—HUMAN NECESSITIES
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    • 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
    • A61K47/50—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/56—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
    • A61K47/59—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
    • A61K47/60—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
    • 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
    • A61K47/50—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/62—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid
    • A61K47/64—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
    • A61K47/645—Polycationic or polyanionic oligopeptides, polypeptides or polyamino acids, e.g. polylysine, polyarginine, polyglutamic acid or peptide TAT
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2319/00—Fusion polypeptide
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2319/00—Fusion polypeptide
    • C07K2319/01—Fusion polypeptide containing a localisation/targetting motif
    • C07K2319/10—Fusion polypeptide containing a localisation/targetting motif containing a tag for extracellular membrane crossing, e.g. TAT or VP22
    • C—CHEMISTRY; METALLURGY
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    • C12N2760/00011—Details
    • C12N2760/14011—Filoviridae
    • C12N2760/14111—Ebolavirus, e.g. Zaire ebolavirus
    • C12N2760/14122—New viral proteins or individual genes, new structural or functional aspects of known viral proteins or genes
    • C—CHEMISTRY; METALLURGY
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    • C12N2760/14011—Filoviridae
    • C12N2760/14111—Ebolavirus, e.g. Zaire ebolavirus
    • C12N2760/14133—Use of viral protein as therapeutic agent other than vaccine, e.g. apoptosis inducing or anti-inflammatory
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    • C12N2760/00011—Details
    • C12N2760/16011—Orthomyxoviridae
    • C12N2760/16111—Influenzavirus A, i.e. influenza A virus
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    • C12N2760/00011—Details
    • C12N2760/18011—Paramyxoviridae
    • C12N2760/18411—Morbillivirus, e.g. Measles virus, canine distemper
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    • C12N2770/00011—Details
    • C12N2770/20011—Coronaviridae
    • C12N2770/20033—Use of viral protein as therapeutic agent other than vaccine, e.g. apoptosis inducing or anti-inflammatory

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  • Proteomics, Peptides & Aminoacids (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Communicable Diseases (AREA)
  • Gastroenterology & Hepatology (AREA)
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  • Genetics & Genomics (AREA)
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CN202180044021.1A 2020-04-24 2021-04-22 作为sars-cov-2抗病毒药物的脂质-肽融合抑制剂 Pending CN115916806A (zh)

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Application Number Priority Date Filing Date Title
US202063015479P 2020-04-24 2020-04-24
US63/015,479 2020-04-24
PCT/US2021/028667 WO2021216891A2 (en) 2020-04-24 2021-04-22 Lipid-peptide fusion inhibitors as sars-cov-2 antivirals

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CN115916806A true CN115916806A (zh) 2023-04-04

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CN202180044021.1A Pending CN115916806A (zh) 2020-04-24 2021-04-22 作为sars-cov-2抗病毒药物的脂质-肽融合抑制剂

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US (1) US20230159597A1 (https=)
EP (1) EP4139330A4 (https=)
JP (1) JP2023524911A (https=)
KR (1) KR20230028719A (https=)
CN (1) CN115916806A (https=)
BR (1) BR112022021528A2 (https=)
CA (1) CA3175831A1 (https=)
IL (1) IL297498A (https=)
WO (1) WO2021216891A2 (https=)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA3235784A1 (en) * 2021-10-22 2023-04-27 Wisconsin Alumni Research Foundation Peptides that inhibit infection by sars-cov-2, the virus that causes covid-19 disease
WO2024016011A2 (en) * 2022-07-15 2024-01-18 The Trustees Of Columbia University In The City Of New York Broad spectrum inhibition of human coronaviruses by lipopeptides derived from the c-terminal heptad repeat of betacoronaviruses
WO2025231157A2 (en) * 2024-04-30 2025-11-06 Decoy Therapeutics Inc. New anti-viral therapeutic peptides, conjugates, and methods of use thereof

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US20080027006A1 (en) * 2004-02-12 2008-01-31 The Regents Of The University Of Colorado Compositions And Methods For Modification And Prevention Of Sars Coronavirus Infectivity
WO2010089129A1 (en) * 2009-02-06 2010-08-12 Cormus Srl Inhibitors of viral fusion and uses thereof
WO2012020108A2 (en) * 2010-08-11 2012-02-16 Cormus Srl Multimeric inhibitors of viral fusion and uses thereof
CN104151403A (zh) * 2013-04-08 2014-11-19 中国医学科学院药物研究所 一类多肽或其衍生物、及其在流感病毒感染中的应用
WO2015171924A2 (en) * 2014-05-07 2015-11-12 Cornell University Inhibitors of fusion between viral and cell membranes as well as compositions and methods of using them
WO2017015457A1 (en) * 2015-07-21 2017-01-26 Modernatx, Inc. Ebola vaccine
US20180243225A1 (en) * 2017-01-25 2018-08-30 Modernatx, Inc. Ebola/marburg vaccines

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WO2005032453A2 (en) * 2003-04-28 2005-04-14 Sequoia Pharmaceuticals, Inc. Antiviral agents for the treatment, control and prevention of infections by coronaviruses
GB0720503D0 (en) * 2007-10-22 2007-11-28 Angeletti P Ist Richerche Bio New compound
CA3173973A1 (en) * 2020-03-04 2021-09-10 Dana-Farber Cancer Institute, Inc. Antiviral structurally-stabilized sars-cov-2 peptides and uses thereof

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US20080027006A1 (en) * 2004-02-12 2008-01-31 The Regents Of The University Of Colorado Compositions And Methods For Modification And Prevention Of Sars Coronavirus Infectivity
WO2010089129A1 (en) * 2009-02-06 2010-08-12 Cormus Srl Inhibitors of viral fusion and uses thereof
WO2012020108A2 (en) * 2010-08-11 2012-02-16 Cormus Srl Multimeric inhibitors of viral fusion and uses thereof
CN104151403A (zh) * 2013-04-08 2014-11-19 中国医学科学院药物研究所 一类多肽或其衍生物、及其在流感病毒感染中的应用
WO2015171924A2 (en) * 2014-05-07 2015-11-12 Cornell University Inhibitors of fusion between viral and cell membranes as well as compositions and methods of using them
US20170216448A1 (en) * 2014-05-07 2017-08-03 Cornell University Inhibitors of fusion between viral and cell membranes as well as compositions and methods of using them
WO2017015457A1 (en) * 2015-07-21 2017-01-26 Modernatx, Inc. Ebola vaccine
US20180243225A1 (en) * 2017-01-25 2018-08-30 Modernatx, Inc. Ebola/marburg vaccines

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Title
FIGUEIRA TIAGO ET AL: "Structure-stability-function mechanistic links in the anti-measles virus action of tocopherol-derivatized peptide nanoparticles", ACS NANO, vol. 12, no. 10, 9 September 2018 (2018-09-09) *
KELLY K. LEE ET AL: "Capturing a fusion intermediate of influenza hemagglutinin with a cholesterol-conjugated peptide, a new antiviral strategy for influenza virus", JBC, vol. 286, no. 49, 9 December 2011 (2011-12-09) *
MARCELO AUGUSTO ET AL: "Antiviral lipopeptide-cell membrane interaction is influenced by PEG linker length", MOLECULES, vol. 22, no. 7, 15 July 2017 (2017-07-15) *
XIA ET AL: "Inhibitionof SARS-CoV-2(previously2019-nCoV) infection by a highly potent pan-coronavirus fusion inhibitor targeting its spike protein that harbors a high capacity to mediate membrane fusion", CELL RESEARCH, vol. 30, 30 March 2020 (2020-03-30), pages 345 *
孟广鹏;梁国栋;张培宇;王潮;刘克良;: "基于Ⅰ类包膜病毒膜融合机制的肽类抗病毒药物研究进展", 国际药学研究杂志, no. 11, 30 November 2017 (2017-11-30) *

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WO2021216891A2 (en) 2021-10-28
KR20230028719A (ko) 2023-03-02
IL297498A (en) 2022-12-01
BR112022021528A2 (pt) 2023-04-04
WO2021216891A3 (en) 2021-12-09
EP4139330A2 (en) 2023-03-01
CA3175831A1 (en) 2021-10-28
US20230159597A1 (en) 2023-05-25
EP4139330A4 (en) 2024-10-23
JP2023524911A (ja) 2023-06-13

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