EA201390362A1 - Новые аналоги пиперазина в качестве противовирусных препаратов широкого спектра действия против гриппа - Google Patents

Новые аналоги пиперазина в качестве противовирусных препаратов широкого спектра действия против гриппа

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Publication number
EA201390362A1
EA201390362A1 EA201390362A EA201390362A EA201390362A1 EA 201390362 A1 EA201390362 A1 EA 201390362A1 EA 201390362 A EA201390362 A EA 201390362A EA 201390362 A EA201390362 A EA 201390362A EA 201390362 A1 EA201390362 A1 EA 201390362A1
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EA
Eurasian Patent Office
Prior art keywords
piperazin
wide range
action against
virus drugs
new analogues
Prior art date
Application number
EA201390362A
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English (en)
Other versions
EA023258B1 (ru
Inventor
Кристофер В. Сианси
Самюэл Герритц
Гуо Ли
Бредли С. Пирс
Аннапурна Пендри
Шухао Ши
Вэйсюй Чжай
Шижун Чжу
Original Assignee
Бристол-Маерс Сквибб Компани
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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Publication date
Application filed by Бристол-Маерс Сквибб Компани filed Critical Бристол-Маерс Сквибб Компани
Publication of EA201390362A1 publication Critical patent/EA201390362A1/ru
Publication of EA023258B1 publication Critical patent/EA023258B1/ru

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D261/00Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/02Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
    • C07D261/06Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
    • C07D261/10Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D261/18Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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
    • 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
    • A61P31/16Antivirals for RNA viruses for influenza or rhinoviruses
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/32Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D207/325Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms with substituted hydrocarbon radicals directly attached to the ring nitrogen atom
    • C07D207/327Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D233/90Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D249/00Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/041,2,3-Triazoles; Hydrogenated 1,2,3-triazoles
    • C07D249/061,2,3-Triazoles; Hydrogenated 1,2,3-triazoles with aryl radicals directly attached to ring atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pulmonology (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Предложено соединение формулы (I), в том числе его фармацевтически приемлемые соли:в котором Het представляет собой 5- или 6-членный гетероцикл с -N, -О или -S, смежным с -Ar заместителем или смежный с точкой присоединения -Ar заместителя; Ar представляет собой арил или гетероарил; R представляет собой -СН, -CHF или -СН=СН; W представляет собой -NO, -Cl, -Br, -СНО, -СН=СНили -CN; X представляет собой -Cl, -СНили -CN; Y представляет собой -СН или -N; Z представляет собой C-Cалкил, C-Cциклоалкил, замещенный арил, замещенный гетероарил, ORили NHR, в которых Rвыбран из группы Н, арила, гетероарила, C-Cалкила и C-Cциклоалкила. Данное соединение в составе композиций пригодно для предупреждения и лечения вируса гриппа.
EA201390362A 2010-09-08 2011-09-06 1,4-пиперазиновые производные в качестве средства от вирусного гриппа EA023258B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US38072810P 2010-09-08 2010-09-08
PCT/US2011/050504 WO2012033736A1 (en) 2010-09-08 2011-09-06 Novel piperazine analogs as broad-spectrum influenza antivirals

Publications (2)

Publication Number Publication Date
EA201390362A1 true EA201390362A1 (ru) 2013-07-30
EA023258B1 EA023258B1 (ru) 2016-05-31

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EA201390362A EA023258B1 (ru) 2010-09-08 2011-09-06 1,4-пиперазиновые производные в качестве средства от вирусного гриппа

Country Status (17)

Country Link
US (1) US8362004B2 (ru)
EP (1) EP2614052B1 (ru)
JP (1) JP5902172B2 (ru)
CN (1) CN103201268B (ru)
BR (1) BR112013005552A2 (ru)
CA (1) CA2809624A1 (ru)
DK (1) DK2614052T3 (ru)
EA (1) EA023258B1 (ru)
ES (1) ES2533068T3 (ru)
HR (1) HRP20150228T1 (ru)
MX (1) MX2013002557A (ru)
PL (1) PL2614052T3 (ru)
PT (1) PT2614052E (ru)
RS (1) RS53844B1 (ru)
SI (1) SI2614052T1 (ru)
SM (1) SMT201500068B (ru)
WO (1) WO2012033736A1 (ru)

Families Citing this family (7)

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KR101369584B1 (ko) 2011-04-19 2014-03-06 일양약품주식회사 페닐-이속사졸 유도체 및 그의 제조방법
CN105101959B (zh) * 2012-11-05 2018-04-17 南特知识产权控股有限责任公司 作为刺猬信号传导通路的抑制剂的含有环状磺酰胺的衍生物
KR102089122B1 (ko) * 2016-08-25 2020-03-13 주식회사 엘지화학 디아민 화합물 및 이를 이용하여 제조된 플렉시블 소자용 기판
US11040963B2 (en) 2017-02-02 2021-06-22 Janssen Vaccines & Prevention B.V. Piperazine derivatives for influenza virus inhibitions
WO2018141854A1 (en) 2017-02-02 2018-08-09 Janssen Vaccines & Prevention B.V. Piperazine derivatives for influenza virus inhibition
WO2021204923A1 (en) * 2020-04-09 2021-10-14 Vironova Medical Ab Antiviral agents
WO2021204924A1 (en) * 2020-04-09 2021-10-14 Vironova Medical Ab Compounds for use in the treatment of hypercytokinemia

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GB9914371D0 (en) * 1999-06-18 1999-08-18 Smithkline Beecham Plc Novel compounds
KR20040010713A (ko) * 2001-06-15 2004-01-31 야마노우치세이야쿠 가부시키가이샤 페닐피리딘 카보닐 피페라진 유도체
AU2003246972A1 (en) 2002-08-06 2004-02-23 Astrazeneca Ab Condensed pyridines and pyrimidines with tie2 (tek) activity
WO2004078732A1 (fr) 2003-01-28 2004-09-16 Aventis Pharma S.A. Produits n-aryl-heteroaromatiques, compositions les contenant et utilisation
US6949865B2 (en) * 2003-01-31 2005-09-27 Betabatt, Inc. Apparatus and method for generating electrical current from the nuclear decay process of a radioactive material
GB0428235D0 (en) 2004-12-23 2005-01-26 Glaxo Group Ltd Novel compounds
EP1834954A1 (en) * 2006-03-15 2007-09-19 4Sc Ag Thiazoles as NF-kB Inhibitors (proteasome inhibitors)
AU2010281265A1 (en) * 2009-08-05 2012-03-22 Versitech Limited Antiviral compounds and methods of making and using thereof

Also Published As

Publication number Publication date
PT2614052E (pt) 2015-03-31
PL2614052T3 (pl) 2015-06-30
SMT201500068B (it) 2015-05-05
WO2012033736A1 (en) 2012-03-15
US20120238539A1 (en) 2012-09-20
CN103201268B (zh) 2015-08-12
BR112013005552A2 (pt) 2016-05-03
EP2614052B1 (en) 2014-12-31
SI2614052T1 (sl) 2015-04-30
EP2614052A1 (en) 2013-07-17
DK2614052T3 (en) 2015-04-07
ES2533068T3 (es) 2015-04-07
RS53844B1 (en) 2015-08-31
CN103201268A (zh) 2013-07-10
JP2013537193A (ja) 2013-09-30
JP5902172B2 (ja) 2016-04-13
HRP20150228T1 (hr) 2015-04-10
US8362004B2 (en) 2013-01-29
EA023258B1 (ru) 2016-05-31
CA2809624A1 (en) 2012-03-15
MX2013002557A (es) 2013-05-28

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Legal Events

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MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG MD TJ TM

MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): RU