EA023423B1 - Ингибиторы репликации вирусов гриппа - Google Patents

Ингибиторы репликации вирусов гриппа Download PDF

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Publication number
EA023423B1
EA023423B1 EA201490396A EA201490396A EA023423B1 EA 023423 B1 EA023423 B1 EA 023423B1 EA 201490396 A EA201490396 A EA 201490396A EA 201490396 A EA201490396 A EA 201490396A EA 023423 B1 EA023423 B1 EA 023423B1
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EA
Eurasian Patent Office
Prior art keywords
fluoro
mmol
compound
pyrrolo
solution
Prior art date
Application number
EA201490396A
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English (en)
Russian (ru)
Other versions
EA201490396A1 (ru
Inventor
Пол С. Чарифсон
Майкл П. Кларк
Упул К. Бандарадже
Рэнди С. Бетил
Майкл Дж. Бойд
Иоана Дейвис
Хунбо Дэн
Джон П. Даффи
Люк Дж. Фармер
Хуай Гао
Вэньсинь Гу
Джозеф М. Кеннеди
Брайан Ледфорд
Марк В. Ледебур
Франсуа Мальте
Эмануэле Перола
Тяньшэн Ван
Original Assignee
Вертекс Фармасьютикалз Инкорпорейтед
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Application filed by Вертекс Фармасьютикалз Инкорпорейтед filed Critical Вертекс Фармасьютикалз Инкорпорейтед
Publication of EA201490396A1 publication Critical patent/EA201490396A1/ru
Publication of EA023423B1 publication Critical patent/EA023423B1/ru

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed 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
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/351—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom not condensed with another ring
    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines 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
    • A61K31/495—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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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
    • A61P31/16—Antivirals for RNA viruses for influenza or rhinoviruses
    • 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
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings

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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)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Virology (AREA)
  • Molecular Biology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Biochemistry (AREA)
  • Emergency Medicine (AREA)
  • Pulmonology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Micro-Organisms Or Cultivation Processes Thereof (AREA)
EA201490396A 2011-08-01 2012-08-01 Ингибиторы репликации вирусов гриппа EA023423B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201161513793P 2011-08-01 2011-08-01
PCT/US2012/049097 WO2013019828A1 (en) 2011-08-01 2012-08-01 Inhibitors of influenza viruses replication

Publications (2)

Publication Number Publication Date
EA201490396A1 EA201490396A1 (ru) 2014-06-30
EA023423B1 true EA023423B1 (ru) 2016-06-30

Family

ID=46650922

Family Applications (3)

Application Number Title Priority Date Filing Date
EA201500265A EA027210B1 (ru) 2011-08-01 2012-08-01 Ингибиторы репликации вирусов гриппа
EA201692506A EA037372B1 (ru) 2011-08-01 2012-08-01 Ингибиторы репликации вирусов гриппа
EA201490396A EA023423B1 (ru) 2011-08-01 2012-08-01 Ингибиторы репликации вирусов гриппа

Family Applications Before (2)

Application Number Title Priority Date Filing Date
EA201500265A EA027210B1 (ru) 2011-08-01 2012-08-01 Ингибиторы репликации вирусов гриппа
EA201692506A EA037372B1 (ru) 2011-08-01 2012-08-01 Ингибиторы репликации вирусов гриппа

Country Status (37)

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US (5) US9051319B2 (cg-RX-API-DMAC7.html)
EP (2) EP3147284B1 (cg-RX-API-DMAC7.html)
JP (3) JP5917692B2 (cg-RX-API-DMAC7.html)
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CN (3) CN105503862B (cg-RX-API-DMAC7.html)
AP (1) AP3867A (cg-RX-API-DMAC7.html)
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CA (1) CA2844054C (cg-RX-API-DMAC7.html)
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IL (2) IL230618A (cg-RX-API-DMAC7.html)
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SG (2) SG10201503835TA (cg-RX-API-DMAC7.html)
SI (1) SI2739623T1 (cg-RX-API-DMAC7.html)
TW (3) TWI594997B (cg-RX-API-DMAC7.html)
UA (2) UA118010C2 (cg-RX-API-DMAC7.html)
UY (1) UY34234A (cg-RX-API-DMAC7.html)
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KR101903354B1 (ko) 2009-06-17 2018-10-04 버텍스 파마슈티칼스 인코포레이티드 인플루엔자 바이러스 복제의 억제제
EP2729465A2 (en) 2011-07-05 2014-05-14 Vertex Pharmaceuticals Incorporated Processes and intermediates for producing azaindoles
UA118010C2 (uk) 2011-08-01 2018-11-12 Вертекс Фармасьютікалз Інкорпорейтед Інгібітори реплікації вірусів грипу
US9296727B2 (en) 2013-10-07 2016-03-29 Vertex Pharmaceuticals Incorporated Methods of regioselective synthesis of 2,4-disubstituted pyrimidines
HRP20191525T1 (hr) 2013-11-13 2019-11-29 Vertex Pharma Inhibitori replikacije virusa influence
LT3421468T (lt) 2013-11-13 2021-01-11 Vertex Pharmaceuticals Incorporated Gripo virusų replikacijos inhibitorių paruošimo būdai
CN103922966B (zh) * 2014-04-14 2015-10-21 武汉大学 作为甲型流感病毒抑制剂的甲酰胺和异腈类化合物及其制备与应用
MX381488B (es) * 2014-08-08 2025-03-12 Janssen Sciences Ireland Uc Indoles para su uso en la infección por el virus de la gripe.
JP6718451B2 (ja) * 2014-09-08 2020-07-08 ヤンセン・サイエンシズ・アイルランド・アンリミテッド・カンパニー インフルエンザウィルス感染に使用するためのピロロピリミジン
MA40772A (fr) * 2014-10-02 2017-08-08 Vertex Pharma Variants du virus de la grippe a
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WO2016183120A1 (en) 2015-05-13 2016-11-17 Vertex Pharmaceuticals Incorporated Inhibitors of influenza viruses replication
JP6704416B2 (ja) * 2015-05-13 2020-06-03 バーテックス ファーマシューティカルズ インコーポレイテッドＶｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ インフルエンザウイルスの複製の阻害剤を調製する方法
AU2016359907B2 (en) 2015-11-27 2021-04-01 Janssen Sciences Ireland Uc Heterocyclic indoles for use in influenza virus infection
RU2737190C2 (ru) * 2015-12-09 2020-11-25 Саншайн Лейк Фарма Ко., Лтд. Ингибиторы репликации вируса гриппа, способы их применения и использование
HRP20211749T1 (hr) * 2016-01-07 2022-02-18 Janssen Sciences Ireland Unlimited Company Pentanske kiseline supstituirane pirolo-[2-3,b]pirimidin-piridinima za liječenje virusnih infekcija influencom
EA201891666A1 (ru) 2016-01-20 2019-01-31 Янссен Сайенсиз Айрлэнд Юси Арилзамещенные пиримидины для применения при инфекции, вызванной вирусом гриппа
KR102598246B1 (ko) * 2016-07-26 2023-11-02 톈진 롱보진 파마시우티컬 씨오., 엘티디. Jak 저해제로서 헤테로사이클릭 화합물, 및 이의 염 및 치료학적 용도
WO2018033082A1 (en) 2016-08-16 2018-02-22 Sunshine Lake Pharma Co., Ltd. Inhibitors of influenza virus replication, application methods and uses thereof
US10647693B2 (en) 2016-08-30 2020-05-12 North & South Brother Pharmacy Investment Company Limited Inhibitors of influenza virus replication, application methods and uses thereof
CN106478460B (zh) * 2016-09-28 2018-06-12 衢州学院 一种手性N-Boc-3-氨基-4-芳基-丁酸的合成方法
CN108218873B (zh) 2016-12-15 2020-07-07 广东东阳光药业有限公司 流感病毒复制抑制剂及其用途
US11098042B2 (en) 2017-01-05 2021-08-24 Sunshine Lake Pharma Co., Ltd. Inhibitors of influenza virus replication and uses thereof
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WO2018170147A1 (en) 2017-03-14 2018-09-20 The Regents Of The University Of California Genome-wide identification of immune evasion functions in a virus
CN109384783A (zh) * 2017-08-09 2019-02-26 银杏树药业(苏州)有限公司 新型杂环化合物及其作为抗流感病毒抑制剂的医药用途
TWI821343B (zh) 2018-07-27 2023-11-11 美商共結晶製藥公司 流感病毒複製之抑制劑
CN112979647B (zh) * 2021-03-12 2022-05-20 浙江大学 含氮杂氨基酸的氮杂吲哚衍生物及制备和应用

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