EA200601178A1 - Морфолинилсодержащие бензимидазолы в качестве ингибиторов репликации респираторно-синцитиального вируса - Google Patents

Морфолинилсодержащие бензимидазолы в качестве ингибиторов репликации респираторно-синцитиального вируса

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Publication number
EA200601178A1
EA200601178A1 EA200601178A EA200601178A EA200601178A1 EA 200601178 A1 EA200601178 A1 EA 200601178A1 EA 200601178 A EA200601178 A EA 200601178A EA 200601178 A EA200601178 A EA 200601178A EA 200601178 A1 EA200601178 A1 EA 200601178A1
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EA
Eurasian Patent Office
Prior art keywords
hydrogen
substituted
morpholinyl
halogen
alkyl
Prior art date
Application number
EA200601178A
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English (en)
Other versions
EA009876B1 (ru
Inventor
Жан-Франсуа Бонфанти
Кунрад Йозеф Лодевейк Андрис
Жером Мишель Клод Фортэн
Филипп Мюллер
Фредерик Марк Морис Дубле
Кристоф Мейер
Руди Эдмонд Виллебрордс
Том Валериус Жозефа Жевер
Филип Мария Марта Берн Тиммерман
Original Assignee
Тиботек Фармасьютикалз Лтд.
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=34704695&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=EA200601178(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Тиботек Фармасьютикалз Лтд. filed Critical Тиботек Фармасьютикалз Лтд.
Publication of EA200601178A1 publication Critical patent/EA200601178A1/ru
Publication of EA009876B1 publication Critical patent/EA009876B1/ru

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles 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 in position 2
    • C07D235/30—Nitrogen atoms not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic 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
    • C07D413/12—Heterocyclic 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
    • 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
    • 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
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/06—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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Virology (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Настоящее изобретение относится к морфолинилсодержащим бензимидазолам, имеющим ингибирующую активность в отношении репликации респираторно-синцитиального вируса и имеющим формулу (I), к его пролекарству, N-оксиду, аддитивной соли, четвертичному амину, комплексу с металлом или стереохимически изомерной форме, где G представляет собой прямую связь или необязательно замещенный Cалкандиил; Rпредставляет собой Arили моноциклический или бициклический гетероцикл, Q представляет собой R, пирролидинил, замещенный R, пиперидинил, замещенный Rили гомопиперидинил, замещенный R; один из Rи Rвыбирается из галогена, необязательно моно- или полизамещенного Cалкила, необязательно моно- или полизамещенного Салкенила, нитро, гидрокси, Ar, N(RR), N(RR)сульфонила, N(RR)карбонила, Cалкилокси, Arокси, ArCалкилокси, карбоксила, Cалкилоксикарбонила или -C(=Z)Ar; и другой из Rи Rпредставляет собой водород; в случае, когда Rявляется отличным от водорода, тогда Rпредставляет собой водород, Cалкил или галоген, и Rпредставляет собой водород; в случае, когда Rявляется отличным от водорода, тогда Rпредставляет собой водород, Cалкил или галоген и Rпредставляет собой водород. Кроме того, изобретение относится к получению указанных соединений и композиций, содержащих эти соединения, а также к применению их в качестве лекарственного средства.
EA200601178A 2003-12-18 2004-12-20 Морфолинилсодержащие бензимидазолы в качестве ингибиторов репликации респираторно-синцитиального вируса EA009876B1 (ru)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
EP03104810 2003-12-18
US56718204P 2004-04-30 2004-04-30
EP04105312 2004-10-26
PCT/EP2004/053620 WO2005058871A1 (en) 2003-12-18 2004-12-20 Morpholinyl containing benzimidazoles as inhibitors of respiratory syncytial virus replication

Publications (2)

Publication Number Publication Date
EA200601178A1 true EA200601178A1 (ru) 2006-10-27
EA009876B1 EA009876B1 (ru) 2008-04-28

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EA200601178A EA009876B1 (ru) 2003-12-18 2004-12-20 Морфолинилсодержащие бензимидазолы в качестве ингибиторов репликации респираторно-синцитиального вируса

Country Status (33)

Country Link
US (2) US7449463B2 (ru)
EP (1) EP1697345B1 (ru)
JP (1) JP4951348B2 (ru)
KR (1) KR100967406B1 (ru)
CN (2) CN101412709B (ru)
AP (1) AP2150A (ru)
AR (1) AR046959A1 (ru)
AT (1) ATE388950T1 (ru)
AU (1) AU2004298460B2 (ru)
BR (1) BRPI0417268B8 (ru)
CA (1) CA2548668C (ru)
CY (1) CY1108142T1 (ru)
DE (1) DE602004012448T2 (ru)
DK (1) DK1697345T3 (ru)
EA (1) EA009876B1 (ru)
EG (1) EG25799A (ru)
ES (1) ES2303653T3 (ru)
HK (1) HK1130799A1 (ru)
HR (1) HRP20080245T3 (ru)
IL (1) IL175910A (ru)
ME (1) ME01042B (ru)
MX (1) MXPA06007112A (ru)
MY (1) MY143573A (ru)
NO (1) NO339314B1 (ru)
NZ (1) NZ547479A (ru)
PL (1) PL1697345T3 (ru)
PT (1) PT1697345E (ru)
RS (1) RS50584B (ru)
SI (1) SI1697345T1 (ru)
TW (1) TWI351401B (ru)
UA (1) UA84718C2 (ru)
WO (1) WO2005058871A1 (ru)
ZA (1) ZA200605894B (ru)

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AR046959A1 (es) * 2003-12-18 2006-01-04 Tibotec Pharm Ltd Morfolinilo que contiene bencimidazoles como inhibidores de la replicacion del virus sincitial respiratorio
TWI370820B (en) 2005-04-27 2012-08-21 Takeda Pharmaceutical Fused heterocyclic compounds
US8034835B2 (en) * 2005-06-20 2011-10-11 Tibotec Pharmaceuticals Ltd. 1-[[2-amino-3-(substituted alkyl)-3H-benzimidazolyl[methyl]-3-substituted-1,3-dihydro-benzoimidazol-2-ones and structural analogs
BRPI0611744B8 (pt) * 2005-06-20 2021-05-25 Janssen R & D Ireland benzimidazóis heterociclilaminoalquila substituída, seu processo de preparação e composição farmacêutica
US20120148678A1 (en) 2010-12-08 2012-06-14 Advanced Technologies And Regenerative Medicine, Llc. Sustained release of poorly water soluble active compounds
TWI650321B (zh) 2011-10-14 2019-02-11 美商安比特生物科學公司 雜環化合物及其使用方法
UA119050C2 (uk) * 2013-11-11 2019-04-25 Ґілеад Саєнсиз, Інк. ПІРОЛО[1.2-f][1.2.4]ТРИАЗИНИ, ЯКІ ВИКОРИСТОВУЮТЬСЯ ДЛЯ ЛІКУВАННЯ РЕСПІРАТОРНО-СИНЦИТІАЛЬНИХ ВІРУСНИХ ІНФЕКЦІЙ
JO3637B1 (ar) 2015-04-28 2020-08-27 Janssen Sciences Ireland Uc مركبات بيرازولو- وترايازولو- بيريميدين مضادة للفيروسات rsv
US10906899B2 (en) 2016-05-10 2021-02-02 Georgia State University Research Foundation, Inc. Bicyclic fused pyrazole derivatives for the treatment of RSV
TW201815787A (zh) 2016-09-23 2018-05-01 美商基利科學股份有限公司 磷脂醯肌醇3-激酶抑制劑
TW201825465A (zh) 2016-09-23 2018-07-16 美商基利科學股份有限公司 磷脂醯肌醇3-激酶抑制劑
TW201813963A (zh) 2016-09-23 2018-04-16 美商基利科學股份有限公司 磷脂醯肌醇3-激酶抑制劑
MX2018014032A (es) 2017-03-20 2019-08-21 Forma Therapeutics Inc Composiciones de pirrolopirrol como activadores de piruvato cinasa (pkr).
TW201932470A (zh) 2017-11-29 2019-08-16 愛爾蘭商健生科學愛爾蘭無限公司 具有抗ｒｓｖ活性之吡唑并嘧啶
EP3746444B1 (en) 2018-01-31 2023-09-27 Janssen Sciences Ireland Unlimited Company Cycloalkyl substituted pyrazolopyrimidines having activity against rsv
EA202092439A1 (ru) 2018-04-23 2021-03-05 Янссен Сайенсиз Айрлэнд Анлимитед Компани Гетероароматические соединения, обладающие активностью против rsv
CN113226356A (zh) 2018-09-19 2021-08-06 福马治疗股份有限公司 活化丙酮酸激酶r
EP3853206B1 (en) 2018-09-19 2024-04-10 Novo Nordisk Health Care AG Treating sickle cell disease with a pyruvate kinase r activating compound
GB201820751D0 (en) * 2018-12-19 2019-01-30 Bp Oil Int Methods for preparing intermediates
CA3147397A1 (en) 2019-07-22 2021-01-28 Lupin Limited Macrocyclic compounds as sting agonists and methods and uses thereof
JP7329239B2 (ja) 2019-09-20 2023-08-18 株式会社タマディック フライトシミュレーター
WO2023018560A1 (en) * 2021-08-13 2023-02-16 Georgia State University Research Foundation, Inc. Bicyclic fused pyrazole derivatives for the treatment of respiratory infections including rsv

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ATE258928T1 (de) * 1999-06-28 2004-02-15 Janssen Pharmaceutica Nv Respiratorisches syncytialvirus replikation inhibitoren
AP1552A (en) * 1999-06-28 2006-01-17 Janssen Pharmaceutica Nv Respiratory syncytial virus replication inhibitors.
DE60033859T2 (de) * 1999-06-28 2007-11-08 Janssen Pharmaceutica N.V. Hemmer des Respiratorischen Syncytial Virus
WO2005058869A1 (en) * 2003-12-18 2005-06-30 Tibotec Pharmaceuticals Ltd. Aminobenzimidazoles and benzimidazoles as inhibitors of respiratory syncytial virus replication
AR046959A1 (es) * 2003-12-18 2006-01-04 Tibotec Pharm Ltd Morfolinilo que contiene bencimidazoles como inhibidores de la replicacion del virus sincitial respiratorio

Also Published As

Publication number Publication date
US20070043022A1 (en) 2007-02-22
EA009876B1 (ru) 2008-04-28
US7449463B2 (en) 2008-11-11
CA2548668A1 (en) 2005-06-30
IL175910A (en) 2013-08-29
TW200531972A (en) 2005-10-01
EP1697345A1 (en) 2006-09-06
PT1697345E (pt) 2008-06-12
BRPI0417268B8 (pt) 2021-05-25
ATE388950T1 (de) 2008-03-15
UA84718C2 (ru) 2008-11-25
ME01042B (me) 2012-10-20
MY143573A (en) 2011-05-31
NO20063322L (no) 2006-09-18
TWI351401B (en) 2011-11-01
JP4951348B2 (ja) 2012-06-13
RS50584B (sr) 2010-05-07
IL175910A0 (en) 2006-10-05
CN101412709A (zh) 2009-04-22
CY1108142T1 (el) 2014-02-12
HRP20080245T3 (en) 2008-07-31
CN101412709B (zh) 2015-03-25
US8883837B2 (en) 2014-11-11
KR100967406B1 (ko) 2010-07-01
US20080280881A1 (en) 2008-11-13
NZ547479A (en) 2009-03-31
KR20070015507A (ko) 2007-02-05
MXPA06007112A (es) 2006-08-23
CA2548668C (en) 2011-09-20
AU2004298460A1 (en) 2005-06-30
EP1697345B1 (en) 2008-03-12
HK1130799A1 (en) 2010-01-08
DK1697345T3 (da) 2008-06-23
EG25799A (en) 2012-08-06
CN1894237A (zh) 2007-01-10
BRPI0417268A (pt) 2007-03-13
JP2007514720A (ja) 2007-06-07
PL1697345T3 (pl) 2008-08-29
DE602004012448D1 (de) 2008-04-24
NO339314B1 (no) 2016-11-28
ZA200605894B (en) 2008-01-08
AP2150A (en) 2010-09-04
AU2004298460B2 (en) 2009-03-19
ES2303653T3 (es) 2008-08-16
WO2005058871A1 (en) 2005-06-30
SI1697345T1 (sl) 2008-08-31
AR046959A1 (es) 2006-01-04
AP2006003640A0 (en) 2006-06-30
BRPI0417268B1 (pt) 2018-10-23
DE602004012448T2 (de) 2009-03-26

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