JP6495238B2 - キナーゼ阻害剤として有用な尿素誘導体 - Google Patents

キナーゼ阻害剤として有用な尿素誘導体 Download PDF

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JP6495238B2
JP6495238B2 JP2016505888A JP2016505888A JP6495238B2 JP 6495238 B2 JP6495238 B2 JP 6495238B2 JP 2016505888 A JP2016505888 A JP 2016505888A JP 2016505888 A JP2016505888 A JP 2016505888A JP 6495238 B2 JP6495238 B2 JP 6495238B2
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methoxy
oxy
tert
butyl
ethoxy
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JP2016515606A (ja
JP2016515606A5 (enExample
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マシュー コリン ソー ファイフ，
マシュー コリン ソー ファイフ，
ステファン マルコム トム，
ステファン マルコム トム，
トーマス マシュー ベーカー，
トーマス マシュー ベーカー，
ガレス ウィリアム ハーボトル，
ガレス ウィリアム ハーボトル，
ヴェドラン ハシンベゴヴィック，
ヴェドラン ハシンベゴヴィック，
プレムジ メグハニ，
プレムジ メグハニ，
アーロン リグビー，
アーロン リグビー，
コリン サムブルック−スミス，
コリン サムブルック−スミス，
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トピバート ファーマ リミテッド
トピバート ファーマ リミテッド
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Priority claimed from GB201305945A external-priority patent/GB201305945D0/en
Priority claimed from GBGB1322678.2A external-priority patent/GB201322678D0/en
Priority claimed from GB201402647A external-priority patent/GB201402647D0/en
Application filed by トピバート ファーマ リミテッド, トピバート ファーマ リミテッド filed Critical トピバート ファーマ リミテッド
Publication of JP2016515606A publication Critical patent/JP2016515606A/ja
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
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    • C07C317/00—Sulfones; Sulfoxides
    • C07C317/44—Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton
    • C07C317/48—Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton the carbon skeleton being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
    • A—HUMAN NECESSITIES
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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
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    • 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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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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    • 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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    • C07C311/08—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
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    • C07D211/80—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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
    • C07D211/84—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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 hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen directly attached to ring carbon atoms
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    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2016505888A 2013-04-02 2014-04-01 キナーゼ阻害剤として有用な尿素誘導体 Expired - Fee Related JP6495238B2 (ja)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
GB201305945A GB201305945D0 (en) 2013-04-02 2013-04-02 New compounds
GB1305945.6 2013-04-02
GB1322678.2 2013-12-20
GBGB1322678.2A GB201322678D0 (en) 2013-12-20 2013-12-20 New compounds
GB201402647A GB201402647D0 (en) 2014-02-14 2014-02-14 New compounds
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Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2229391B1 (en) 2007-12-19 2014-08-06 Cancer Research Technology Limited Pyrido[2,3-b]pyrazine-8-substituted compounds and their use
CA2786834C (en) 2010-02-01 2018-10-16 Cancer Research Technology Limited 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
PH12014500547A1 (en) 2011-10-03 2014-04-21 Respivert Ltd 1-pyrazolyl-3-(-4-((2-anilinopyrimidin-4-yl)oxy)napththalen-1-yl)ureas as p38 map kinase 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
GB201214750D0 (en) 2012-08-17 2012-10-03 Respivert Ltd Compounds
EP2890695A2 (en) 2012-08-29 2015-07-08 Respivert Limited Kinase inhibitors
US20150210722A1 (en) 2012-08-29 2015-07-30 Respivert Limited Kinase inhibitors
WO2014033449A1 (en) 2012-08-29 2014-03-06 Respivert Limited Kinase inhibitors
WO2014076484A1 (en) 2012-11-16 2014-05-22 Respivert Limited Kinase inhibitors
WO2014140582A1 (en) 2013-03-14 2014-09-18 Respivert Limited Kinase inhibitors
EP2981534B1 (en) 2013-04-02 2017-07-19 Topivert Pharma Limited Kinase inhibitors based upon n-alkyl pyrazoles
ES2856902T3 (es) * 2013-04-02 2021-09-28 Oxular Acquisitions Ltd Derivados de urea útiles como inhibidores de quinasa
GB201320729D0 (en) 2013-11-25 2014-01-08 Cancer Rec Tech Ltd Therapeutic compounds and their use
GB201320732D0 (en) 2013-11-25 2014-01-08 Cancer Rec Tech Ltd Methods of chemical synthesis
CN113717162A (zh) 2013-12-20 2021-11-30 奥苏拉收购有限公司 用作激酶抑制剂的脲衍生物
JP6586098B2 (ja) 2014-02-14 2019-10-02 レスピバート・リミテツド キナーゼ阻害剤としてのピラゾリル尿素
MA40774A (fr) * 2014-10-01 2017-08-08 Respivert Ltd Dérivés de diaryle-urée en tant qu'inhibiteurs de kinase p38
AR107165A1 (es) 2015-12-23 2018-03-28 Chiesi Farm Spa Inhibidores de quinasa
MA44607A (fr) * 2016-04-06 2021-05-19 Oxular Acquisitions Ltd Inhibiteurs de kinase
CN114748622B (zh) 2017-10-05 2024-09-24 弗尔康医疗公司 P38激酶抑制剂降低dux4和下游基因表达以用于治疗fshd
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
CN110878055B (zh) * 2018-09-06 2021-02-05 中国科学院化学研究所 一种制备羰基杂环类化合物的方法
JP7594787B2 (ja) 2018-12-07 2024-12-05 ユニバーシティ オブ メリーランド、ボルチモア 非ＡＴＰ／触媒部位ｐ３８マイトジェン活性化プロテインキナーゼ阻害剤
EP4313959A1 (en) * 2021-03-23 2024-02-07 GEN1E Lifesciences Inc. Substituted naphthyl p38alpha mitogen-activated protein kinase inhibitors

Family Cites Families (64)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2290520C (en) 1997-05-23 2009-01-27 Bayer Corporation Inhibition of p38 kinase activity by aryl ureas
CA2308428A1 (en) 1997-11-03 1999-05-14 Boehringer Ingelheim Pharmaceuticals, Inc. Aromatic heterocyclic compounds as anti-inflammatory agents
EP1140840B1 (en) 1999-01-13 2006-03-22 Bayer Pharmaceuticals Corp. -g(v)-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors
ATE538794T1 (de) 1999-01-13 2012-01-15 Bayer Healthcare Llc Gamma carboxyarylsubstituierte diphenylharnstoffverbindungen als p38 kinasehemmer
UA73492C2 (en) 1999-01-19 2005-08-15 Aromatic heterocyclic compounds as antiinflammatory agents
HUP0202248A3 (en) 1999-03-12 2006-06-28 Boehringer Ingelheim Pharma Compounds useful as anti-inflammatory agents
WO2001004115A2 (en) 1999-07-09 2001-01-18 Boehringer Ingelheim Pharmaceuticals, Inc. Novel process for synthesis of heteroaryl-substituted urea compounds
CA2389360C (en) 1999-11-16 2008-06-03 Steffen Breitfelder Urea derivatives as anti-inflammatory agents
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
JP2005507367A (ja) * 2001-04-13 2005-03-17 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 １，４−二置換ベンゾ縮合化合物
MXPA03009361A (es) 2001-04-13 2004-01-29 Boehringer Ingelheim Pharma Compuestos de urea utilies como agentes anti-inflamatorios.
EP1392661A1 (en) 2001-05-16 2004-03-03 Boehringer Ingelheim Pharmaceuticals Inc. Diarylurea derivatives useful as anti-inflammatory agents
MXPA03010724A (es) 2001-05-25 2004-03-02 Boehringer Ingelheim Pharma Compuestos de carbamato y oxamida como inhibidores de la produccion de citocina.
CA2453147A1 (en) 2001-07-11 2003-01-23 Boehringer Ingelheim Pharmaceuticals, Inc. Methods of treating cytokine mediated diseases
DK1478358T3 (da) 2002-02-11 2013-10-07 Bayer Healthcare Llc Sorafenibtosylat til behandling af sygdomme kendetegnet ved unormal angiogenese
AU2003210969A1 (en) 2002-02-11 2003-09-04 Bayer Corporation Aryl ureas with raf kinase and angiogenesis inhibiting activity
AU2003213806A1 (en) 2002-02-25 2003-09-09 Boehringer Ingelheim Pharmaceuticals, Inc. 1,4-disubstituted benzofused cycloalkyl urea compounds useful in treating cytokine mediated diseases
AR037647A1 (es) 2002-05-29 2004-12-01 Novartis Ag Derivados de diarilurea utiles para el tratamiento de enfermedades dependientes de la cinasa de proteina
CA2494824A1 (en) * 2002-08-08 2004-02-19 Boehringer Ingelheim Pharmaceuticals, Inc. Fluorinated phenyl-naphthalenyl-urea compounds as inhibitors of cytokines involved in inflammatory processes
US20050014753A1 (en) 2003-04-04 2005-01-20 Irm Llc Novel compounds and compositions as protein kinase inhibitors
WO2004113352A1 (en) 2003-06-19 2004-12-29 Amedis Pharmaceuticals Ltd. Silylated heterocyclylurea derivatives as cytokine-inhibitors
WO2005005396A1 (en) 2003-06-30 2005-01-20 Boehringer Ingelheim Pharmaceuticals, Inc. Process of making di-aryl urea compounds
BRPI0413757A (pt) 2003-08-22 2006-10-31 Boehringer Ingelheim Pharma métodos para o tratamento de copd e da hipertensão pulmonar
EP1670787B1 (en) 2003-09-11 2012-05-30 iTherX Pharma, Inc. Cytokine inhibitors
WO2005044825A1 (en) 2003-10-21 2005-05-19 Amedis Pharmaceuticals Ltd. Silicon compounds and their use
KR20060110307A (ko) 2003-11-28 2006-10-24 노파르티스 아게 단백질 키나아제 의존성 질환의 치료에서의 디아릴 우레아유도체
US20060035893A1 (en) 2004-08-07 2006-02-16 Boehringer Ingelheim International Gmbh Pharmaceutical compositions for treatment of respiratory and gastrointestinal disorders
GB0423554D0 (en) 2004-10-22 2004-11-24 Cancer Rec Tech Ltd Therapeutic compounds
TW200740820A (en) 2005-07-05 2007-11-01 Takeda Pharmaceuticals Co Fused heterocyclic derivatives and use thereof
AR056582A1 (es) 2005-10-28 2007-10-10 Lilly Co Eli COMPUESTOS DE PIRAZOLIL UREA CON ACTIVIDAD INHIBITORIA DE CINASA P38 Y FORMULACIoN FARMACÉUTICA QUE LO COMPRENDE
US7790756B2 (en) 2006-10-11 2010-09-07 Deciphera Pharmaceuticals, Llc Kinase inhibitors useful for the treatment of myleoproliferative diseases and other proliferative diseases
US8293748B2 (en) 2008-10-02 2012-10-23 Respivert Ltd. p38 MAP kinase inhibitors
GB0818033D0 (en) 2008-10-02 2008-11-05 Respivert Ltd Novel compound
JP5670912B2 (ja) 2008-12-11 2015-02-18 レスピバート・リミテツド ｐ３８ＭＡＰキナーゼ阻害剤
GB0905955D0 (en) 2009-04-06 2009-05-20 Respivert Ltd Novel compounds
RU2725140C2 (ru) * 2009-06-10 2020-06-30 Чугаи Сейяку Кабусики Кайся Тетрациклические соединения
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
ES2664098T3 (es) 2010-03-15 2018-04-18 Ube Industries, Ltd. Método para producir un compuesto de amida
GB201005589D0 (en) 2010-04-01 2010-05-19 Respivert Ltd Novel compounds
WO2011124923A2 (en) 2010-04-08 2011-10-13 Respivert Limited Novel compounds
WO2011124930A1 (en) 2010-04-08 2011-10-13 Respivert Limited P38 map kinase inhibitors
GB201009731D0 (en) * 2010-06-10 2010-07-21 Pulmagen Therapeutics Inflamma Kinase inhibitors
GB201010196D0 (en) 2010-06-17 2010-07-21 Respivert Ltd Methods
US8933228B2 (en) 2010-06-17 2015-01-13 Respivert, Ltd. Respiratory formulations and compounds for use therein
GB201010193D0 (en) 2010-06-17 2010-07-21 Respivert Ltd Medicinal use
KR20130141500A (ko) * 2010-09-29 2013-12-26 크리스탈지노믹스(주) 단백질 키나제 억제 활성을 갖는 신규한 아미노퀴나졸린 화합물
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
PH12014500547A1 (en) 2011-10-03 2014-04-21 Respivert Ltd 1-pyrazolyl-3-(-4-((2-anilinopyrimidin-4-yl)oxy)napththalen-1-yl)ureas as p38 map kinase inhibitors
MY170656A (en) * 2011-12-09 2019-08-24 Chiesi Farm Spa Kinase inhibitors
GB201214750D0 (en) 2012-08-17 2012-10-03 Respivert Ltd Compounds
WO2014033449A1 (en) 2012-08-29 2014-03-06 Respivert Limited Kinase inhibitors
EP2890695A2 (en) 2012-08-29 2015-07-08 Respivert Limited Kinase inhibitors
GB201215357D0 (en) 2012-08-29 2012-10-10 Respivert Ltd Compounds
US20150210722A1 (en) 2012-08-29 2015-07-30 Respivert Limited Kinase inhibitors
WO2014076484A1 (en) 2012-11-16 2014-05-22 Respivert Limited Kinase inhibitors
WO2014140582A1 (en) 2013-03-14 2014-09-18 Respivert Limited Kinase inhibitors
EP2981534B1 (en) 2013-04-02 2017-07-19 Topivert Pharma Limited Kinase inhibitors based upon n-alkyl pyrazoles
ES2856902T3 (es) * 2013-04-02 2021-09-28 Oxular Acquisitions Ltd Derivados de urea útiles como inhibidores de quinasa
CN113717162A (zh) 2013-12-20 2021-11-30 奥苏拉收购有限公司 用作激酶抑制剂的脲衍生物
JP6586098B2 (ja) 2014-02-14 2019-10-02 レスピバート・リミテツド キナーゼ阻害剤としてのピラゾリル尿素
MA40774A (fr) 2014-10-01 2017-08-08 Respivert Ltd Dérivés de diaryle-urée en tant qu'inhibiteurs de kinase p38
MA44607A (fr) * 2016-04-06 2021-05-19 Oxular Acquisitions Ltd Inhibiteurs de kinase

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