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EA201800065A1 - Пан-геномные ингибиторы белка ns5a вируса гепатита с, фармацевтические композиции, промежуточные продукты для синтеза ингибиторов и способы их получения и применения - Google Patents

Пан-геномные ингибиторы белка ns5a вируса гепатита с, фармацевтические композиции, промежуточные продукты для синтеза ингибиторов и способы их получения и применения

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Publication number
EA201800065A1
EA201800065A1 EA201800065A EA201800065A EA201800065A1 EA 201800065 A1 EA201800065 A1 EA 201800065A1 EA 201800065 A EA201800065 A EA 201800065A EA 201800065 A EA201800065 A EA 201800065A EA 201800065 A1 EA201800065 A1 EA 201800065A1
Authority
EA
Eurasian Patent Office
Prior art keywords
optionally substituted
inhibitors
hepatitis
genomic
virus
Prior art date
Application number
EA201800065A
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English (en)
Other versions
EA034084B1 (ru
Inventor
Александр Васильевич ИВАЩЕНКО
Олег Дмитриевич МИТЬКИН
Original Assignee
ИВАЩЕНКО, Андрей Александрович
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.)
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Application filed by ИВАЩЕНКО, Андрей Александрович filed Critical ИВАЩЕНКО, Андрей Александрович
Publication of EA201800065A1 publication Critical patent/EA201800065A1/ru
Publication of EA034084B1 publication Critical patent/EA034084B1/ru

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/7056—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-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
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/19—Cytokines; Lymphokines; Interferons
    • A61K38/21—Interferons [IFN]
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    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/43—Enzymes; Proenzymes; Derivatives thereof
    • A61K38/46—Hydrolases (3)
    • A61K38/48—Hydrolases (3) acting on peptide bonds (3.4)
    • A61K38/482—Serine endopeptidases (3.4.21)
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    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
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    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
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    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
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    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
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    • 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C12Y304/00—Hydrolases acting on peptide bonds, i.e. peptidases (3.4)
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  • Immunology (AREA)
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  • Oncology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Настоящее изобретение относится к новому соединению общей формулы (1)или его фармацевтически приемлемой соли, гидрату, кристаллической форме или стереоизомеру, где R1 представляет собой водород, третбутоксикарбонил; R2 представляет собой водород, галоген, C-C-алкил; R3 представляет собой необязательно замещенный арил, необязательно замещенный арилокси, необязательно замещенный арилсульфанил, необязательно замещенный ариламино или необязательно замещенный азотсодержащий гетарил; R4 представляет собой йод;где R11 представляет собой необязательно замещенный C-C-алкил, необязательно замещенный C-C-циклоалкил или необязательно замещенный C-C-алкилокси; стрелки (←) указывают место присоединения заместителей;где R41 представляет собой необязательно замещенный C-C-алкил, необязательно замещенный C-C-циклоалкил или необязательно замещенный C-C-алкилокси; X представляет собой бута-1,3-диинилен или 1,4-фенилен; стрелки (←) указывают место присоединения заместителей.
EA201800065A 2015-09-04 2016-06-24 Пан-геномные ингибиторы белка ns5a вируса гепатита с, фармацевтические композиции, промежуточные продукты для синтеза ингибиторов и способы их получения и применения EA034084B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US14/845,333 US9790207B2 (en) 2015-09-04 2015-09-04 Pan-genomic inhibitors of NS5A protein encoded by HCV, pharmaceutical compositions, intermediates for inhibitor synthesis, and their synthesis and application methods
PCT/US2016/039152 WO2017039791A1 (en) 2015-09-04 2016-06-24 Pan-genomic inhibitors of ns5a protein encoded by hcv, pharmaceutical compositions, intermediates for inhibitor synthesis, and their synthesis and application methods.

Publications (2)

Publication Number Publication Date
EA201800065A1 true EA201800065A1 (ru) 2018-08-31
EA034084B1 EA034084B1 (ru) 2019-12-25

Family

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EA201800065A EA034084B1 (ru) 2015-09-04 2016-06-24 Пан-геномные ингибиторы белка ns5a вируса гепатита с, фармацевтические композиции, промежуточные продукты для синтеза ингибиторов и способы их получения и применения

Country Status (5)

Country Link
US (1) US9790207B2 (ru)
EP (1) EP3344617A4 (ru)
EA (1) EA034084B1 (ru)
RU (1) RU2669919C1 (ru)
WO (1) WO2017039791A1 (ru)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11648300B1 (en) * 2022-03-31 2023-05-16 Asavi Llc Pharmaceutical combination therapy and prevention with aprotinin + nirmatrelvir of SARS-CoV-2 and/or disease associated with this infection, including COVID-19

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20100158862A1 (en) * 2006-08-11 2010-06-24 Bristol-Myers Squibb Company Hepatitis C Virus Inhibitors
NZ587323A (en) * 2008-02-12 2012-02-24 Bristol Myers Squibb Co Hepatitis c virus inhibitors
US8653070B2 (en) * 2009-12-14 2014-02-18 Enanta Pharmaceuticals, Inc. Hepatitis C virus inhibitors
RU2452735C1 (ru) * 2010-11-30 2012-06-10 Александр Васильевич Иващенко Замещенные азолы, противовирусный активный компонент, фармацевтическая композиция, способ получения и применения

Also Published As

Publication number Publication date
EA034084B1 (ru) 2019-12-25
EP3344617A4 (en) 2019-06-12
US20170066746A1 (en) 2017-03-09
EP3344617A1 (en) 2018-07-11
US9790207B2 (en) 2017-10-17
RU2669919C1 (ru) 2018-10-17
WO2017039791A1 (en) 2017-03-09

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