CA2938924C - Pyrazolyl-ureas as kinase inhibitors - Google Patents

Pyrazolyl-ureas as kinase inhibitors Download PDF

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Publication number
CA2938924C
CA2938924C CA2938924A CA2938924A CA2938924C CA 2938924 C CA2938924 C CA 2938924C CA 2938924 A CA2938924 A CA 2938924A CA 2938924 A CA2938924 A CA 2938924A CA 2938924 C CA2938924 C CA 2938924C
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Prior art keywords
tert
buty1
pyrazol
pyridin
naphthalen
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CA2938924A
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English (en)
French (fr)
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CA2938924A1 (en
Inventor
Alistair Ian Longshaw
Euan Alexander Fraser Fordyce
Stuart Thomas Onions
John King-Underwood
Jennifer Diane Venable
Iain Walters
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Respivert Ltd
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Respivert Ltd
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    • 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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    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/007—Pulmonary tract; Aromatherapy
    • A61K9/0073—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
    • A61K9/0075—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy for inhalation via a dry powder inhaler [DPI], e.g. comprising micronized drug mixed with lactose carrier particles
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    • 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
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    • 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
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    • 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
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    • 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
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    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
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    • C—CHEMISTRY; METALLURGY
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    • 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
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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
    • 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
    • C—CHEMISTRY; METALLURGY
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    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Diabetes (AREA)
  • Otolaryngology (AREA)
  • Emergency Medicine (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Rheumatology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Virology (AREA)
  • Endocrinology (AREA)
  • Cardiology (AREA)
  • Obesity (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
CA2938924A 2014-02-14 2015-02-13 Pyrazolyl-ureas as kinase inhibitors Active CA2938924C (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201461940282P 2014-02-14 2014-02-14
US61/940,282 2014-02-14
US201461941064P 2014-02-18 2014-02-18
US61/941,064 2014-02-18
PCT/GB2015/050401 WO2015121660A1 (en) 2014-02-14 2015-02-13 Pyrazolyl-ureas as kinase inhibitors

Publications (2)

Publication Number Publication Date
CA2938924A1 CA2938924A1 (en) 2015-08-20
CA2938924C true CA2938924C (en) 2023-01-31

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CA2938924A Active CA2938924C (en) 2014-02-14 2015-02-13 Pyrazolyl-ureas as kinase inhibitors

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US (8) US9447076B2 (enExample)
EP (4) EP3105222B1 (enExample)
JP (4) JP6630280B2 (enExample)
KR (1) KR102413704B1 (enExample)
CN (4) CN113264921B (enExample)
AU (3) AU2015216957B2 (enExample)
BR (1) BR112016015838B1 (enExample)
CA (1) CA2938924C (enExample)
DK (2) DK3357919T3 (enExample)
EA (1) EA034927B1 (enExample)
ES (2) ES2677595T3 (enExample)
JO (1) JO3392B1 (enExample)
MX (2) MX371353B (enExample)
PL (2) PL3357919T3 (enExample)
PT (2) PT3105222T (enExample)
SG (1) SG11201607058PA (enExample)
TR (1) TR201809072T4 (enExample)
TW (2) TWI751099B (enExample)
UY (1) UY35998A (enExample)
WO (2) WO2015121444A1 (enExample)

Families Citing this family (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UA105763C2 (uk) 2007-12-19 2014-06-25 Кансер Рісерч Текнолоджі Лімітед 8-ЗАМІЩЕНІ ПІРИДО[2,3-b]ПІРАЗИНИ ТА ЇХ ЗАСТОСУВАННЯ
NZ706154A (en) 2010-02-01 2016-09-30 Cancer Rec Tech Ltd 1-(5-tert-butyl-2-phenyl-2h-pyrazol-3-yl)-3-[2-fluoro-4-(1-methyl-2-oxo-2,3-dihydro-1h-imidazo[4,5-b]pyridin-7-yloxy)-phenyl]-urea and related compounds and their use in therapy
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
JP2014528404A (ja) 2011-10-03 2014-10-27 レスピバート・リミテツド ｐ３８ＭＡＰキナーゼ阻害剤としての１−ピラゾリル−３−（４−（（２−アニリノピリミジン−４−イル）オキシ）ナフタレン−１−イル）尿素
GB201214750D0 (en) 2012-08-17 2012-10-03 Respivert Ltd Compounds
EP2890695A2 (en) 2012-08-29 2015-07-08 Respivert Limited Kinase inhibitors
EP2890460B1 (en) 2012-08-29 2017-02-22 Respivert Limited Kinase inhibitors
US9783556B2 (en) 2012-08-29 2017-10-10 Respivert Limited Kinase inhibitors
EP2925742B1 (en) 2012-11-16 2016-10-26 Respivert Limited Kinase inhibitors
WO2014140582A1 (en) 2013-03-14 2014-09-18 Respivert Limited Kinase inhibitors
MX363949B (es) 2013-04-02 2019-04-08 Topivert Pharma Ltd Inhibidor de quinasa.
US9771353B2 (en) 2013-04-02 2017-09-26 Topivert Pharma Limited Kinase inhibitors based upon N-alkyl pyrazoles
GB201320732D0 (en) 2013-11-25 2014-01-08 Cancer Rec Tech Ltd Methods of chemical synthesis
GB201320729D0 (en) 2013-11-25 2014-01-08 Cancer Rec Tech Ltd Therapeutic compounds and their use
WO2015092423A1 (en) 2013-12-20 2015-06-25 Respivert Limited Urea derivatives useful as kinase inhibitors
EP3105222B1 (en) 2014-02-14 2018-04-11 Respivert Limited Aromatic heterocyclic compounds as antiinflammatory compounds
MA40774A (fr) 2014-10-01 2017-08-08 Respivert Ltd Dérivés de diaryle-urée en tant qu'inhibiteurs de kinase p38
CN105801486A (zh) * 2016-03-31 2016-07-27 常州大学 一种1-（2,4二溴苯基）-3-吡唑醇的合成方法
CA3015978A1 (en) 2016-04-06 2017-10-12 Topivert Pharma Limited Kinase inhibitors
EP3474835B1 (en) 2016-06-23 2023-07-05 University of Maryland, Baltimore Non-catalytic substrate-selective p38 -specific mapk inhibitors with endothelial-stabilizing and anti-inflammatory activity, and methods of use thereof
EP3824906A1 (en) 2016-12-21 2021-05-26 Amgen Inc. Anti-tnf alpha antibody formulations
US10342786B2 (en) 2017-10-05 2019-07-09 Fulcrum Therapeutics, Inc. P38 kinase inhibitors reduce DUX4 and downstream gene expression for the treatment of FSHD
JP2021501130A (ja) 2017-10-05 2021-01-14 フルクラム セラピューティクス，インコーポレイテッド ＤＵＸ４の発現を低減するためのｐ３８阻害剤の使用
CA3122371A1 (en) 2018-12-07 2020-06-11 University Of Maryland, Baltimore Non-atp/catalytic site p38 mitogen activated protein kinase inhibitors
CA3125039A1 (en) * 2019-01-23 2020-07-30 Theravance Biopharma R&D Ip, Llc Imidazo[1,5-a]pyridine, 1,2,4-triazolo[4,3-a]pyridine and imidazo[1,5-a]pyrazine as jak inhibitors
US11286260B2 (en) * 2020-05-18 2022-03-29 Gen1E Lifesciences Inc. P38α mitogen-activated protein kinase inhibitors
CN111889025B (zh) * 2020-09-01 2022-01-11 山东大学 一种耐酸碱耐盐超两亲分子乳化剂及其制备方法和乳液
AU2021370893B2 (en) 2020-10-29 2024-03-07 Gen1E Lifesciences Inc. Crystalline 5-(dimethylamino) -n- (4-(morpholinomethyl)phenyl) naphthalene-1-sulfonamide di-hydrochloride di-hydrate
CA3205921A1 (en) * 2021-02-03 2022-08-11 Sheng CUI Formulation of furin inhibitor for inhalation
IL306101A (en) 2021-03-23 2023-11-01 Gen1E Lifesciences Inc Naphthyl-mutated p38 alpha mitogen-activated protein kinase inhibitors
CN116655608B (zh) * 2023-05-30 2025-08-19 成都瑞芬思德丹生物科技有限公司 一种具有抗炎活性的吡咯烷酮类化合物及其制备方法和应用

Family Cites Families (53)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE69836563T2 (de) 1997-12-22 2007-05-16 Bayer Pharmaceuticals Corp., West Haven INHIBIERUNG DER p38 KINASE-AKTIVITÄT DURCH DIE VERWENDUNG VON ARYL- UND HETEROARYL-SUBSTITUIERTEN HARNSTOFFEN
US7329670B1 (en) 1997-12-22 2008-02-12 Bayer Pharmaceuticals Corporation Inhibition of RAF kinase using aryl and heteroaryl substituted heterocyclic ureas
DE69834842T2 (de) 1997-12-22 2007-05-10 Bayer Pharmaceuticals Corp., West Haven Hemmung von raf-kinase unter verwendung von aryl- und heteroarylsubstituierten heterocyclischen harnstoffen
US20080300281A1 (en) 1997-12-22 2008-12-04 Jacques Dumas Inhibition of p38 Kinase Activity Using Aryl and Heteroaryl Substituted Heterocyclic Ureas
UA73492C2 (en) 1999-01-19 2005-08-15 Aromatic heterocyclic compounds as antiinflammatory agents
EP1200411B1 (en) 1999-07-09 2005-12-14 Boehringer Ingelheim Pharmaceuticals Inc. Process for synthesis of heteroaryl-substituted urea compounds
JP4955171B2 (ja) 1999-11-16 2012-06-20 ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド 抗炎症剤としての尿素誘導体
US6492529B1 (en) 2000-01-18 2002-12-10 Boehringer Ingelheim Pharmaceuticals, Inc. Bis pyrazole-1H-pyrazole intermediates and their synthesis
US6525046B1 (en) 2000-01-18 2003-02-25 Boehringer Ingelheim Pharmaceuticals, Inc. Aromatic heterocyclic compounds as antiinflammatory agents
AU2001250783A1 (en) 2000-02-29 2001-09-12 Cor Therapeutics, Inc. Benzamides and related inhibitors of factor xa
CA2445003A1 (en) 2001-05-16 2002-11-21 Boehringer Ingelheim Pharmaceuticals, Inc. Diarylurea derivatives useful as anti-inflammatory agents
ES2284887T3 (es) 2001-07-11 2007-11-16 Boehringer Ingelheim Pharmaceuticals Inc. Metodos para tratar enfermedades transmitidas por citocinas.
US20030216396A1 (en) 2002-02-11 2003-11-20 Bayer Corporation Pyridine, quinoline, and isoquinoline N-oxides as kinase inhibitors
US7838541B2 (en) 2002-02-11 2010-11-23 Bayer Healthcare, Llc Aryl ureas with angiogenesis inhibiting activity
JP4629978B2 (ja) * 2002-02-25 2011-02-09 ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド サイトカイン媒介疾患の治療に有用な１，４−二置換ベンゾ縮合シクロアルキル尿素化合物
AU2003243921B2 (en) 2002-06-27 2009-05-07 Novo Nordisk A/S Aryl carbonyl derivatives as therapeutic agents
EP1541563A4 (en) 2002-07-10 2007-11-07 Ono Pharmaceutical Co ANTAGONIST OF CCR4 AND CORRESPONDING MEDICINAL USE
ATE489379T1 (de) 2003-02-28 2010-12-15 Bayer Healthcare Llc 2-oxo-1,3,5-perhydrotriazapinderivate, die sich zur behandlung von hyperproliferativen, angiogenen und entzündlichen erkrankungen eignen
UY28213A1 (es) 2003-02-28 2004-09-30 Bayer Pharmaceuticals Corp Nuevos derivados de cianopiridina útiles en el tratamiento de cáncer y otros trastornos.
ATE517885T1 (de) 2004-04-30 2011-08-15 Bayer Healthcare Llc Substituierte pyrazolyl-harnstoff-derivate zur behandlung von krebs
GB0500435D0 (en) 2005-01-10 2005-02-16 Novartis Ag Organic compounds
ATE485269T1 (de) 2005-06-27 2010-11-15 Bristol Myers Squibb Co C-verknüpfte zyklische antagonisten des p2y1- rezeptors mit eignung bei der behandlung thrombotischer leiden
UA95310C2 (ru) 2006-10-20 2011-07-25 Айкос Корпорейшен Композиция, содержащая ингибитор chk1 и циклодекстрин, для лечения рака
HUE025197T2 (en) 2008-03-17 2016-02-29 Ambit Biosciences Corp Quinazoline derivatives as RAF kinase modulators and methods for their use
BRPI0920707A2 (pt) 2008-10-02 2015-12-29 Respivert Ltd compostos
GB0818033D0 (en) 2008-10-02 2008-11-05 Respivert Ltd Novel compound
WO2010067130A1 (en) 2008-12-11 2010-06-17 Respivert Limited P38 map kinase inhibitors
GB0905955D0 (en) * 2009-04-06 2009-05-20 Respivert Ltd Novel compounds
GB0921731D0 (en) 2009-12-11 2010-01-27 Respivert Ltd Theraputic uses
GB0921730D0 (en) 2009-12-11 2010-01-27 Respivert Ltd Method of treatment
EP2548862B1 (en) 2010-03-15 2016-06-08 Ube Industries, Ltd. Method for producing amide compound
GB201005589D0 (en) 2010-04-01 2010-05-19 Respivert Ltd Novel compounds
US9024041B2 (en) 2010-04-08 2015-05-05 Respivert Ltd. P38 MAP kinase inhibitors
JP5787976B2 (ja) * 2010-04-08 2015-09-30 レスピバート・リミテツド Ｐ３８ｍａｐキナーゼ阻害剤としてのピラゾリルウレア
GB201010196D0 (en) 2010-06-17 2010-07-21 Respivert Ltd Methods
GB201010193D0 (en) 2010-06-17 2010-07-21 Respivert Ltd Medicinal use
EP2582700B1 (en) 2010-06-17 2016-11-02 Respivert Limited Respiratory formulations containing p38 mapk inhibitors
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
JP2014528404A (ja) 2011-10-03 2014-10-27 レスピバート・リミテツド ｐ３８ＭＡＰキナーゼ阻害剤としての１−ピラゾリル−３−（４−（（２−アニリノピリミジン−４−イル）オキシ）ナフタレン−１−イル）尿素
PE20141370A1 (es) 2011-12-09 2014-10-17 Chiesi Farma Spa Inhibidores de quinasa
GB201214750D0 (en) 2012-08-17 2012-10-03 Respivert Ltd Compounds
GB201215357D0 (en) 2012-08-29 2012-10-10 Respivert Ltd Compounds
EP2890460B1 (en) 2012-08-29 2017-02-22 Respivert Limited Kinase inhibitors
EP2890695A2 (en) 2012-08-29 2015-07-08 Respivert Limited Kinase inhibitors
US9783556B2 (en) 2012-08-29 2017-10-10 Respivert Limited Kinase inhibitors
EP2925742B1 (en) 2012-11-16 2016-10-26 Respivert Limited Kinase inhibitors
WO2014140582A1 (en) 2013-03-14 2014-09-18 Respivert Limited Kinase inhibitors
MX363949B (es) 2013-04-02 2019-04-08 Topivert Pharma Ltd Inhibidor de quinasa.
US9771353B2 (en) 2013-04-02 2017-09-26 Topivert Pharma Limited Kinase inhibitors based upon N-alkyl pyrazoles
WO2015092423A1 (en) 2013-12-20 2015-06-25 Respivert Limited Urea derivatives useful as kinase inhibitors
EP3105222B1 (en) 2014-02-14 2018-04-11 Respivert Limited Aromatic heterocyclic compounds as antiinflammatory compounds
MA40774A (fr) 2014-10-01 2017-08-08 Respivert Ltd Dérivés de diaryle-urée en tant qu'inhibiteurs de kinase p38
EP3201189A1 (en) 2014-10-01 2017-08-09 Respivert Limited N-phenyl-3-quinazolin-6-yl-benzamide derivatives as p38 kinase inhibitors

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