JP5908493B2 - インドール - Google Patents

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Publication number
JP5908493B2
JP5908493B2 JP2013542121A JP2013542121A JP5908493B2 JP 5908493 B2 JP5908493 B2 JP 5908493B2 JP 2013542121 A JP2013542121 A JP 2013542121A JP 2013542121 A JP2013542121 A JP 2013542121A JP 5908493 B2 JP5908493 B2 JP 5908493B2
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JP
Japan
Prior art keywords
methyl
oxo
pyridinyl
indole
dihydro
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Fee Related
Application number
JP2013542121A
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English (en)
Japanese (ja)
Other versions
JP2013544840A5 (enExample
JP2013544840A (ja
Inventor
スティーブン、デイビッド、ナイト
ウィリアム、ヘンリー、ミラー
ケネス、アレン、ニューランダー
シャラド、クマール、ベルマ
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
GlaxoSmithKline LLC
Original Assignee
GlaxoSmithKline LLC
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by GlaxoSmithKline LLC filed Critical GlaxoSmithKline LLC
Publication of JP2013544840A publication Critical patent/JP2013544840A/ja
Publication of JP2013544840A5 publication Critical patent/JP2013544840A5/ja
Application granted granted Critical
Publication of JP5908493B2 publication Critical patent/JP5908493B2/ja
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2013542121A 2010-12-01 2011-11-30 インドール Expired - Fee Related JP5908493B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US41847010P 2010-12-01 2010-12-01
US61/418,470 2010-12-01
PCT/US2011/062537 WO2012075080A1 (en) 2010-12-01 2011-11-30 Indoles

Publications (3)

Publication Number Publication Date
JP2013544840A JP2013544840A (ja) 2013-12-19
JP2013544840A5 JP2013544840A5 (enExample) 2015-01-22
JP5908493B2 true JP5908493B2 (ja) 2016-04-26

Family

ID=46172248

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2013542121A Expired - Fee Related JP5908493B2 (ja) 2010-12-01 2011-11-30 インドール

Country Status (5)

Country Link
US (1) US8765792B2 (enExample)
EP (1) EP2646020B1 (enExample)
JP (1) JP5908493B2 (enExample)
ES (1) ES2607064T3 (enExample)
WO (1) WO2012075080A1 (enExample)

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US20130102477A1 (en) 2010-06-23 2013-04-25 Ryan D. Morin Biomarkers for non-hodgkin lymphomas and uses thereof
JP6389036B2 (ja) 2010-09-10 2018-09-12 エピザイム インコーポレイテッド ヒトezh2の阻害剤、およびその使用方法
US9175331B2 (en) 2010-09-10 2015-11-03 Epizyme, Inc. Inhibitors of human EZH2, and methods of use thereof
EP3323820B1 (en) 2011-02-28 2023-05-10 Epizyme, Inc. Substituted 6,5-fused bicyclic heteroaryl compounds
TW201733984A (zh) 2011-04-13 2017-10-01 雅酶股份有限公司 經取代之苯化合物
JO3438B1 (ar) 2011-04-13 2019-10-20 Epizyme Inc مركبات بنزين مستبدلة بأريل أو أريل غير متجانس
CN103987842A (zh) 2011-09-30 2014-08-13 葛兰素史密斯克莱有限责任公司 治疗癌症的方法
US9206128B2 (en) 2011-11-18 2015-12-08 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
EP2780013A4 (en) 2011-11-18 2015-07-01 Constellation Pharmaceuticals Inc MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF
EP2812001B1 (en) 2012-02-10 2017-06-14 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
PL3184523T3 (pl) 2012-04-13 2019-12-31 Epizyme Inc Bromowodorek N-((4,6-dimetylo-2-okso-1,2-dihydropirydyn-3-ylo)metylo)-5- (etylo(tetrahydro-2H-piran-4-ylo)amino)-4-metylo-4'-(morfolinometylo)-[1,1'- bifenylo]-3-karboksyamidu do zastosowania w leczeniu zaburzenia proliferacji komórkowej układu hematologicznego
WO2013173441A2 (en) 2012-05-16 2013-11-21 Glaxosmithkline Llc Enhancer of zeste homolog 2 inhibitors
SG10201705989YA (en) 2012-10-15 2017-08-30 Epizyme Inc Substituted benzene compounds
BR112015008447A2 (pt) * 2012-10-15 2017-07-04 Epizyme Inc métodos para tratar câncer
EP2935214B1 (en) * 2012-12-21 2019-02-20 Epizyme, Inc. 1,4-pyridone compounds
WO2014100665A1 (en) * 2012-12-21 2014-06-26 Epizyme, Inc. 1,4-pyridone bicyclic heteroaryl compounds
WO2014153208A1 (en) 2013-03-14 2014-09-25 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
US9120757B2 (en) 2013-03-14 2015-09-01 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
US20160031839A1 (en) 2013-03-14 2016-02-04 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
EP2970136A1 (en) 2013-03-14 2016-01-20 Epizyme, Inc. Arginine methyl transferase inhibtors and uses thereof
EP2970133B1 (en) 2013-03-14 2018-10-24 Epizyme, Inc. Pyrazole derivatives as prmt1 inhibitors and uses thereof
AU2014260433A1 (en) 2013-03-14 2015-09-10 Epizyme, Inc. Pyrazole derivatives as arginine methyltransferase inhibitors and uses thereof
US9394258B2 (en) 2013-03-14 2016-07-19 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
SG11201506972PA (en) 2013-03-14 2015-10-29 Epizyme Inc Arginine methyltransferase inhibitors and uses thereof
EP2970134B1 (en) 2013-03-14 2018-02-28 Epizyme, Inc. Pyrazole derivatives as prmt1 inhibitors and uses thereof
WO2014144659A1 (en) 2013-03-14 2014-09-18 Epizyme, Inc. Pyrazole derivatives as prmt1 inhibitors and uses thereof
EP2970305B1 (en) 2013-03-15 2017-02-22 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
CA2910873A1 (en) 2013-04-30 2014-11-06 Glaxosmithkline Intellectual Property (No.2) Limited Enhancer of zeste homolog 2 inhibitors
RU2015155595A (ru) * 2013-06-06 2017-07-14 Глэксосмитклайн Интеллекчуал Проперти (No.2) Лимитед Ингибиторы энхансера zeste гомолога 2 область техники, к которой относится изобретение
JP2016523955A (ja) 2013-07-10 2016-08-12 グラクソスミスクライン、インテレクチュアル、プロパティー、ナンバー2、リミテッドGlaxosmithkline Intellectual Property No.2 Limited Zesteホモログ2エンハンサー阻害剤
EP3033334A1 (en) 2013-08-15 2016-06-22 Constellation Pharmaceuticals, Inc. Indole derivatives as modulators of methyl modifying enzymes, compositions and uses thereof
EP4324525A3 (en) 2013-10-16 2024-07-17 Epizyme, Inc. Hydrochloride salt form for ezh2 inhibition
WO2015077194A1 (en) * 2013-11-22 2015-05-28 Bristol-Myers Squibb Company Inhibitors of lysine methyl transferase
WO2015128837A1 (en) 2014-02-26 2015-09-03 Glaxosmithkline Intellectual Property (No.2) Limited Methods of treating cancer patients responding to ezh2 inhibitor gsk126
TW201636344A (zh) 2014-12-05 2016-10-16 美國禮來大藥廠 Ezh2抑制劑
WO2016102493A1 (en) * 2014-12-22 2016-06-30 Bayer Pharma Aktiengesellschaft Imidazopyridine ezh2 inhibitors
US20180271857A1 (en) 2014-12-23 2018-09-27 University Of Copenhagen Treatment of cancer by inhibiting ezh2 activity
US10493076B2 (en) 2015-08-24 2019-12-03 Epizyme, Inc. Method for treating cancer
TW201718598A (zh) 2015-08-27 2017-06-01 美國禮來大藥廠 Ezh2抑制劑
WO2017040190A1 (en) 2015-08-28 2017-03-09 Constellation Pharmaceuticals, Inc. Crystalline forms of (r)-n-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1h-indole-3-carboxamide
CN105801463A (zh) * 2016-03-31 2016-07-27 常州大学 一种2-甲酸-3-丙氧基-5-甲基吡咯的合成方法
CN107573327B (zh) * 2016-07-05 2020-03-31 四川大学 吲唑-甲酰胺-吡啶酮衍生物及其制备方法和用途
KR102351782B1 (ko) * 2016-09-07 2022-01-17 상하이 하이헤 파마수티컬 컴퍼니 리미티드 피리도 5원 방향족 고리계 화합물, 이의 제조 방법 및 용도
EP3529242A1 (en) 2016-10-19 2019-08-28 Constellation Pharmaceuticals, Inc. Synthesis of inhibitors of ezh2
WO2018086590A1 (zh) * 2016-11-11 2018-05-17 上海海雁医药科技有限公司 砜基取代的苯并杂环衍生物、其制法与医药上的用途
WO2018137639A1 (zh) * 2017-01-25 2018-08-02 恩瑞生物医药科技(上海)有限公司 一种组蛋白甲基转移酶ezh2抑制剂、其制备方法及其医药用途
CA3104209A1 (en) 2018-07-09 2020-01-16 Fondation Asile Des Aveugles Inhibition of prc2 subunits to treat eye disorders
JP7721501B2 (ja) 2019-07-31 2025-08-12 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Cd38の阻害剤としてのヘテロ二環式アミド
CN113666920B (zh) * 2020-04-14 2025-10-03 浙江华海药业股份有限公司 苯并恶唑类化合物制备方法及其在医药领域的应用
JP2024503280A (ja) * 2020-12-29 2024-01-25 レボリューション メディシンズ インコーポレイテッド Sos1阻害剤及びその使用
MX2023008701A (es) 2021-01-29 2023-11-29 Boehringer Ingelheim Int Quinolinas y azaquinolinas como inhibidores de cumulo de diferenciacion 38 (cd38).
EP4392034A1 (en) 2021-08-25 2024-07-03 Institut National de la Santé et de la Recherche Médicale (INSERM) Use of ezh2 inhibitors for the treatment of aortic valve stenosis

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US5330986A (en) 1992-11-24 1994-07-19 Hoechst-Roussel Pharmaceuticals Inc. Indole-7-carboxamide derivatives
DE10022925A1 (de) * 2000-05-11 2001-11-15 Basf Ag Substituierte Indole als PARP-Inhibitoren
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WO2009006577A2 (en) 2007-07-03 2009-01-08 The Regents Of The University Of Michigan Compositions and methods for inhibiting ezh2
CN102369204A (zh) * 2008-09-26 2012-03-07 新加坡科技研究局 3-脱氮瓶菌素衍生物
ES2528269T3 (es) 2010-05-07 2015-02-06 Glaxosmithkline Llc Azaindazoles
HRP20170736T1 (hr) 2010-05-07 2017-07-28 Glaxosmithkline Llc Indoli
ES2534804T3 (es) 2010-05-07 2015-04-28 Glaxosmithkline Llc Indazoles
EP3323820B1 (en) 2011-02-28 2023-05-10 Epizyme, Inc. Substituted 6,5-fused bicyclic heteroaryl compounds

Also Published As

Publication number Publication date
EP2646020A1 (en) 2013-10-09
EP2646020A4 (en) 2014-04-23
JP2013544840A (ja) 2013-12-19
US20130245016A1 (en) 2013-09-19
EP2646020B1 (en) 2016-09-21
ES2607064T3 (es) 2017-03-29
US8765792B2 (en) 2014-07-01
WO2012075080A1 (en) 2012-06-07

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