EA201590391A1 - Пиразолилмочевины в качестве ингибиторов киназы - Google Patents

Пиразолилмочевины в качестве ингибиторов киназы

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Publication number
EA201590391A1
EA201590391A1 EA201590391A EA201590391A EA201590391A1 EA 201590391 A1 EA201590391 A1 EA 201590391A1 EA 201590391 A EA201590391 A EA 201590391A EA 201590391 A EA201590391 A EA 201590391A EA 201590391 A1 EA201590391 A1 EA 201590391A1
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EA
Eurasian Patent Office
Prior art keywords
utie
pyrazolyl
kinase inhibitors
kinases
inflammatory diseases
Prior art date
Application number
EA201590391A
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English (en)
Other versions
EA025393B1 (ru
Inventor
Клэр Энн Мари Кариу
Кэтрин Элизабет Чаррон
Юэн Александер Фрэйзер Фордайс
Дэниел Хамза
Мэттью Колин Тор Файф
Кадзухиро Ито
Джон Кинг-Андервуд
Питер Джон Мюррей
Стюарт Томас Онионз
Стефен Малкольм Том
Хейли Теган Анджела Уотсон
Джонатан Гарет Уилльямс
Original Assignee
Респайверт Лимитед
Топайверт Фарма Лимитед
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Application filed by Респайверт Лимитед, Топайверт Фарма Лимитед filed Critical Респайверт Лимитед
Publication of EA201590391A1 publication Critical patent/EA201590391A1/ru
Publication of EA025393B1 publication Critical patent/EA025393B1/ru

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms 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
    • A61K31/495—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
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
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    • A61P11/02—Nasal agents, e.g. decongestants
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61P31/12—Antivirals
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    • A61P37/02—Immunomodulators
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • 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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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
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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
    • C07D403/12—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 linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (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)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Virology (AREA)
  • Diabetes (AREA)
  • Rheumatology (AREA)
  • Oncology (AREA)
  • Cardiology (AREA)
  • Communicable Diseases (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Molecular Biology (AREA)
  • Hospice & Palliative Care (AREA)
  • Obesity (AREA)
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  • Emergency Medicine (AREA)
  • Otolaryngology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Предоставлены соединения формулы Iгде R, R, R, R, Q, X и Y имеют значения, приведенные в описании изобретения, которые обладают противовоспалительной активностью (например, в результате ингибирования ими одного или более представителей семейства ферментов р38 митоген-активируемых протеинкиназ; Syk киназы; и представителей Src семейства тирозинкиназ) и применяются в терапии, в том числе в фармацевтических комбинациях, в частности, при лечении воспалительных заболеваний, включая воспалительные заболевания легких, глаз и кишечника.
EA201590391A 2012-08-17 2013-08-16 Пиразолилмочевины в качестве ингибиторов киназы EA025393B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GBGB1214750.0A GB201214750D0 (en) 2012-08-17 2012-08-17 Compounds
US201361782793P 2013-03-14 2013-03-14
PCT/GB2013/052184 WO2014027209A1 (en) 2012-08-17 2013-08-16 Pyrazolyl-ureas as kinase inhibitors

Publications (2)

Publication Number Publication Date
EA201590391A1 true EA201590391A1 (ru) 2015-06-30
EA025393B1 EA025393B1 (ru) 2016-12-30

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EA201590391A EA025393B1 (ru) 2012-08-17 2013-08-16 Пиразолилмочевины в качестве ингибиторов киназы

Country Status (12)

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US (2) US9701670B2 (ru)
EP (1) EP2885284B1 (ru)
JP (1) JP2015524837A (ru)
KR (1) KR20150056777A (ru)
CN (1) CN105073725A (ru)
AU (1) AU2013303922A1 (ru)
BR (1) BR112015003218A2 (ru)
CA (1) CA2881914A1 (ru)
EA (1) EA025393B1 (ru)
GB (1) GB201214750D0 (ru)
MX (1) MX2015002044A (ru)
WO (1) WO2014027209A1 (ru)

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EP2578582A1 (en) 2011-10-03 2013-04-10 Respivert Limited 1-Pyrazolyl-3-(4-((2-anilinopyrimidin-4-yl)oxy)napththalen-1-yl)ureas as p38 MAP kinase inhibitors
JP6128449B2 (ja) 2011-12-09 2017-05-17 チエシ ファルマスーティシ エス．ピー．エー． キナーゼ阻害剤
GB201214750D0 (en) 2012-08-17 2012-10-03 Respivert Ltd Compounds
WO2014033446A1 (en) 2012-08-29 2014-03-06 Respivert Limited Kinase inhibitors
WO2014033449A1 (en) 2012-08-29 2014-03-06 Respivert Limited Kinase inhibitors
WO2014033447A2 (en) 2012-08-29 2014-03-06 Respivert Limited Kinase inhibitors
GB201215357D0 (en) 2012-08-29 2012-10-10 Respivert Ltd Compounds
EP2925742B1 (en) 2012-11-16 2016-10-26 Respivert Limited Kinase inhibitors
EP2970190A1 (en) 2013-03-14 2016-01-20 Respivert Limited Kinase inhibitors
EP2981534B1 (en) 2013-04-02 2017-07-19 Topivert Pharma Limited Kinase inhibitors based upon n-alkyl pyrazoles
EP2981526B1 (en) 2013-04-02 2021-11-03 Oxular Acquisitions Limited Intermediates useful in the preparation of naphthylurea derivatives useful as kinase inhibitors
CN106164067B (zh) 2014-02-14 2019-09-10 瑞斯比维特有限公司 作为抗炎化合物的芳族杂环化合物
MA40774A (fr) 2014-10-01 2017-08-08 Respivert Ltd Dérivés de diaryle-urée en tant qu'inhibiteurs de kinase p38

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BR112015003218A2 (pt) 2019-09-24
EA025393B1 (ru) 2016-12-30
GB201214750D0 (en) 2012-10-03
AU2013303922A1 (en) 2015-02-19
US20140057915A1 (en) 2014-02-27
MX2015002044A (es) 2016-01-22
US9701670B2 (en) 2017-07-11
KR20150056777A (ko) 2015-05-27
EP2885284B1 (en) 2016-11-02
CN105073725A (zh) 2015-11-18
JP2015524837A (ja) 2015-08-27
US20150218137A1 (en) 2015-08-06
CA2881914A1 (en) 2014-02-20
EP2885284A1 (en) 2015-06-24

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