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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JP2016515606A5 (enExample
JP2016515606A (ja
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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
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • 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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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
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    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
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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
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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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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    • 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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    • C07D213/04—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
    • 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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    • C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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  • 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
GB1305945.6 2013-04-02
GB201305945A GB201305945D0 (en) 2013-04-02 2013-04-02 New compounds
GBGB1322678.2A GB201322678D0 (en) 2013-12-20 2013-12-20 New compounds
GB1322678.2 2013-12-20
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
NZ586418A (en) 2007-12-19 2012-09-28 Cancer Rec Tech Ltd Pyrido[2,3-b]pyrazine-8-substituted compounds and their use
JP5760010B2 (ja) 2010-02-01 2015-08-05 キャンサー・リサーチ・テクノロジー・リミテッド １−（５−ｔｅｒｔ−ブチル−２−フェニル−２Ｈ−ピラゾール−３−イル）−３−［２−フルオロ−４−（１−メチル−２−オキソ−２，３−ジヒドロ−１Ｈ−イミダゾ［４，５−Ｂ］ピリジン−７−イルオキシ）−フェニル］−尿素および関連化合物ならびに治療におけるそれらの使用
KR101995274B1 (ko) 2011-10-03 2019-07-02 레스피버트 리미티드 P38 map 키나제 저해제인 1-피라졸릴-3-(4-((2-아닐리노피리미딘-4-일)옥시)나프탈렌-1-일) 우레아
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
US20150225373A1 (en) 2012-08-29 2015-08-13 Respivert Limited Kinase inhibitors
US9783556B2 (en) 2012-08-29 2017-10-10 Respivert Limited Kinase inhibitors
EP2890460B1 (en) 2012-08-29 2017-02-22 Respivert Limited Kinase inhibitors
US9732063B2 (en) 2012-11-16 2017-08-15 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
AU2014246866B2 (en) 2013-04-02 2018-05-10 Oxular Acquisitions Limited Kinase inhibitor
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
CA2934199A1 (en) 2013-12-20 2015-06-25 Respivert Limited Urea derivatives useful as kinase inhibitors
PT3357919T (pt) 2014-02-14 2020-02-20 Respivert Ltd Compostos heterocíclicos aromáticos como compostos antiinflamatórios
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
EA201892213A1 (ru) 2016-04-06 2019-05-31 Топайверт Фарма Лимитед Ингибиторы киназ
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
BR112020006677A2 (pt) 2017-10-05 2020-10-06 Fulcrum Therapeutics, Inc. uso de inibidores p38 para reduzir a expressão de dux4
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
IL283755B2 (en) 2018-12-07 2026-04-01 Univ Maryland N-(Phenyl-4-methylamino)-5-naphthalene-1-sulfonamide compounds and pharmaceutical preparations containing them
WO2022204046A1 (en) * 2021-03-23 2022-09-29 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
DE69826695T2 (de) 1997-05-23 2006-02-02 Bayer Pharmaceuticals Corp., West Haven Arylharnstoffderivate zur behandlung von inflammatorischen oder immunomodulatorischen erkrankungen
EP1028953A1 (en) 1997-11-03 2000-08-23 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
EP1158985B1 (en) 1999-01-13 2011-12-28 Bayer HealthCare LLC OMEGA-CARBOXY ARYL SUBSTITUTED DIPHENYL UREAS AS p38 KINASE INHIBITORS
UA73492C2 (en) 1999-01-19 2005-08-15 Aromatic heterocyclic compounds as antiinflammatory agents
ATE278674T1 (de) 1999-03-12 2004-10-15 Boehringer Ingelheim Pharma Heterocyklischer harnstoff und verwandte verbindungen als entzündungshemmende mittel
CA2374737C (en) 1999-07-09 2008-02-12 Boehringer Ingelheim Pharmaceuticals, Inc. Novel process for synthesis of heteroaryl-substituted urea compounds
EP1232150B1 (en) 1999-11-16 2007-10-10 Boehringer Ingelheim Pharmaceuticals Inc. Urea derivatives as anti-inflammatory agents
US6525046B1 (en) 2000-01-18 2003-02-25 Boehringer Ingelheim Pharmaceuticals, Inc. Aromatic heterocyclic compounds as antiinflammatory agents
US6492529B1 (en) 2000-01-18 2002-12-10 Boehringer Ingelheim Pharmaceuticals, Inc. Bis pyrazole-1H-pyrazole intermediates and their synthesis
WO2002083628A1 (en) 2001-04-13 2002-10-24 Boehringer Ingelheim Pharmaceuticals, Inc. 1,4-disubstituted benzo-fused compounds
WO2002083642A1 (en) 2001-04-13 2002-10-24 Boehringer Ingelheim Pharmaceuticals, Inc. Compounds useful as anti-inflammatory agents
JP2004530690A (ja) 2001-05-16 2004-10-07 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 抗炎症性薬剤として有用なジアリールウレア誘導体
EP1395561A1 (en) 2001-05-25 2004-03-10 Boehringer Ingelheim Pharmaceuticals Inc. Carbamate and oxamide compounds as inhibitors of cytokine production
WO2003005999A2 (en) 2001-07-11 2003-01-23 Boehringer Ingelheim Pharmaceuticals, Inc. Methods of treating cytokine mediated diseases
SI1478358T1 (sl) 2002-02-11 2013-09-30 Bayer Healthcare Llc Sorafenib tozilat za zdravljenje bolezni, značilnih po abnormalni angiogenezi
US20040023961A1 (en) 2002-02-11 2004-02-05 Bayer Corporation Aryl ureas with raf kinase and angiogenisis inhibiting activity
EP1480973B1 (en) 2002-02-25 2008-02-13 Boehringer Ingelheim Pharmaceuticals Inc. 1,4-disubstituted benzofused cycloalkyl urea compounds useful in treating cytokine mediated diseases
PE20040522A1 (es) 2002-05-29 2004-09-28 Novartis Ag Derivados de diarilurea dependientes de la cinasa de proteina
EP1549621A1 (en) 2002-08-08 2005-07-06 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
CA2536293A1 (en) 2003-08-22 2005-03-03 Boehringer Ingelheim Pharmaceuticals, Inc. Methods of treating copd and pulmonary hypertension
WO2005023761A2 (en) 2003-09-11 2005-03-17 Kemia, Inc. Cytokine inhibitors
WO2005044825A1 (en) 2003-10-21 2005-05-19 Amedis Pharmaceuticals Ltd. Silicon compounds and their use
PE20051046A1 (es) 2003-11-28 2006-01-11 Novartis Ag Derivados de diaril-urea en el tratamiento de enfermedades dependientes de la quinasa de proteina
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
PE20070795A1 (es) 2005-10-28 2007-08-24 Lilly Co Eli Compuestos pirazol-urea-heterociclicos como inhibidores de cinasa
US7790756B2 (en) 2006-10-11 2010-09-07 Deciphera Pharmaceuticals, Llc Kinase inhibitors useful for the treatment of myleoproliferative diseases and other proliferative diseases
GB0818033D0 (en) 2008-10-02 2008-11-05 Respivert Ltd Novel compound
JP2012504591A (ja) 2008-10-02 2012-02-23 レスピバート・リミテツド ｐ３８ＭＡＰキナーゼ阻害剤
MX2011006219A (es) 2008-12-11 2011-06-28 Respivert Ltd Inhibidores de la proteina cinasa activada por el mitogeno p38.
GB0905955D0 (en) 2009-04-06 2009-05-20 Respivert Ltd Novel compounds
ES2575084T3 (es) * 2009-06-10 2016-06-24 Chugai Seiyaku Kabushiki Kaisha Compuesto tetracíclico
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
JP5708637B2 (ja) 2010-03-15 2015-04-30 宇部興産株式会社 アミド化合物の製造方法
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
GB201009731D0 (en) * 2010-06-10 2010-07-21 Pulmagen Therapeutics Inflamma Kinase inhibitors
GB201010193D0 (en) 2010-06-17 2010-07-21 Respivert Ltd Medicinal use
WO2011158044A2 (en) 2010-06-17 2011-12-22 Respivert Limited Respiratory formulations and compounds for use therein
GB201010196D0 (en) * 2010-06-17 2010-07-21 Respivert Ltd Methods
WO2012044090A2 (ko) * 2010-09-29 2012-04-05 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
KR101995274B1 (ko) * 2011-10-03 2019-07-02 레스피버트 리미티드 P38 map 키나제 저해제인 1-피라졸릴-3-(4-((2-아닐리노피리미딘-4-일)옥시)나프탈렌-1-일) 우레아
UA115320C2 (uk) 2011-12-09 2017-10-25 К'Єзі Фармачеутічі С.П.А. Інгібітори кінази
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
US20150225373A1 (en) 2012-08-29 2015-08-13 Respivert Limited Kinase inhibitors
US9783556B2 (en) 2012-08-29 2017-10-10 Respivert Limited Kinase inhibitors
US9732063B2 (en) 2012-11-16 2017-08-15 Respivert Limited Kinase inhibitors
WO2014140582A1 (en) 2013-03-14 2014-09-18 Respivert Limited Kinase inhibitors
AU2014246866B2 (en) * 2013-04-02 2018-05-10 Oxular Acquisitions Limited Kinase inhibitor
EP2981534B1 (en) 2013-04-02 2017-07-19 Topivert Pharma Limited Kinase inhibitors based upon n-alkyl pyrazoles
CA2934199A1 (en) 2013-12-20 2015-06-25 Respivert Limited Urea derivatives useful as kinase inhibitors
PT3357919T (pt) 2014-02-14 2020-02-20 Respivert Ltd Compostos heterocíclicos aromáticos como compostos antiinflamatórios
MA40774A (fr) 2014-10-01 2017-08-08 Respivert Ltd Dérivés de diaryle-urée en tant qu'inhibiteurs de kinase p38
EA201892213A1 (ru) * 2016-04-06 2019-05-31 Топайверт Фарма Лимитед Ингибиторы киназ

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