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
Authority
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
JP2013544840A (ja
JP2013544840A5 (OSRAM
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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Classifications

    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/14—Heterocyclic 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)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Hematology (AREA)
  • Oncology (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 (OSRAM) 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 (OSRAM)
EP (1) EP2646020B1 (OSRAM)
JP (1) JP5908493B2 (OSRAM)
ES (1) ES2607064T3 (OSRAM)
WO (1) WO2012075080A1 (OSRAM)

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RU2765155C2 (ru) 2010-09-10 2022-01-26 Эпизайм, Инк. Ингибиторы ezh2 человека и способы их применения
EP3323820B1 (en) 2011-02-28 2023-05-10 Epizyme, Inc. Substituted 6,5-fused bicyclic heteroaryl compounds
JO3438B1 (ar) 2011-04-13 2019-10-20 Epizyme Inc مركبات بنزين مستبدلة بأريل أو أريل غير متجانس
TW201733984A (zh) 2011-04-13 2017-10-01 雅酶股份有限公司 經取代之苯化合物
EP2760452A4 (en) 2011-09-30 2015-04-01 Glaxosmithkline Llc METHODS OF TREATING CANCER
EP2780014A4 (en) 2011-11-18 2015-07-01 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
SG10201608577RA (en) 2012-04-13 2016-12-29 Epizyme Inc Salt form of a human hi stone methyltransf erase ezh2 inhibitor
WO2013173441A2 (en) 2012-05-16 2013-11-21 Glaxosmithkline Llc Enhancer of zeste homolog 2 inhibitors
NZ706738A (en) 2012-10-15 2018-10-26 Epizyme Inc Substituted benzene compounds
AU2013331368A1 (en) * 2012-10-15 2015-04-30 Epizyme, Inc. Methods of treating cancer
WO2014100646A1 (en) * 2012-12-21 2014-06-26 Epizyme, Inc. 1,4-pyridone compounds
CA2894222A1 (en) * 2012-12-21 2014-06-26 Epizyme, Inc. 1,4-pyridone bicyclic heteroaryl compounds
US9365527B2 (en) 2013-03-14 2016-06-14 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
WO2014153214A1 (en) 2013-03-14 2014-09-25 Epizyme, Inc. Arginine methyl transferase inhibtors and uses thereof
US9023883B2 (en) 2013-03-14 2015-05-05 Epizyme, Inc. PRMT1 inhibitors and uses thereof
US9120757B2 (en) 2013-03-14 2015-09-01 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
US9447079B2 (en) 2013-03-14 2016-09-20 Epizyme, Inc. PRMT1 inhibitors and uses thereof
WO2014153090A1 (en) 2013-03-14 2014-09-25 Epizyme, Inc. Pyrazole derivatives asprmt1 inhibitors and uses thereof
CA2903264A1 (en) 2013-03-14 2014-11-06 Epizyme, Inc. Pyrazole derivatives as arginine methyltransferase inhibitors and uses thereof
HRP20202008T1 (hr) 2013-03-14 2021-02-19 Epizyme, Inc. Inhibitori arginin-metiltransferaze i njihove uporabe
WO2014153235A2 (en) 2013-03-14 2014-09-25 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
EP2970181B1 (en) 2013-03-14 2017-06-07 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
WO2014151142A1 (en) 2013-03-15 2014-09-25 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
CN105308038B (zh) 2013-04-30 2018-05-29 葛兰素史密斯克莱知识产权（第2 号）有限公司 Zeste增强子同源物2的抑制剂
KR20160018594A (ko) * 2013-06-06 2016-02-17 글락소스미스클라인 인털렉츄얼 프로퍼티 (넘버 2) 리미티드 제스트 인핸서 상동체 2 억제제
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
LT3057962T (lt) 2013-10-16 2023-12-11 Epizyme, Inc. Hidrochlorido druskos forma, skirta ezh2 inhibavimui
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
AR102767A1 (es) 2014-12-05 2017-03-22 Lilly Co Eli Inhibidores de ezh2
WO2016102493A1 (en) * 2014-12-22 2016-06-30 Bayer Pharma Aktiengesellschaft Imidazopyridine ezh2 inhibitors
WO2016101956A2 (en) 2014-12-23 2016-06-30 University Of Copenhagen Treatment of cancer by inhibiting ezh2 activity
WO2017035234A1 (en) 2015-08-24 2017-03-02 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
US10577350B2 (en) 2015-08-28 2020-03-03 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
EA038701B1 (ru) * 2016-09-07 2021-10-07 Хайхэ Биофарма Ко., Лтд. Пиридо пятичленное ароматическое циклическое соединение, способ его получения и применение
WO2018075598A1 (en) 2016-10-19 2018-04-26 Constellation Pharmaceuticals, Inc. Synthesis of inhibitors of ezh2
US10793549B2 (en) 2016-11-11 2020-10-06 Shanghai Haiyan Pharmaceutical Technology Co., Ltd. Sulfuryl-substituted benzoheterocyclic derivative, preparation method and medical use thereof
US11214561B2 (en) * 2017-01-25 2022-01-04 Ancureall Pharmaceutical (Shanghai) Co., Ltd. Histone methyltransferase EZH2 inhibitor, preparation method and pharmaceutical use thereof
EP3823671B1 (en) 2018-07-09 2024-02-07 Fondation Asile Des Aveugles Inhibition of prc2 subunits to treat eye disorders
MX2022001019A (es) * 2019-07-31 2022-02-22 Ribon Therapeutics Inc Amidas heterobiciclicas como inhibidoras del cumulo de diferenciacion 38 (cd38).
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
CN116916914A (zh) * 2020-12-29 2023-10-20 锐新医药公司 Sos1抑制剂及其用途
US11952377B2 (en) 2021-01-29 2024-04-09 Boehringer Ingelheim International Gmbh Quinolines and azaquinolines as inhibitors of CD38
US20240350508A1 (en) 2021-08-25 2024-10-24 INSERM (Institut National de la Santé et de la Recherche Médicale) 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
GB0400895D0 (en) * 2004-01-15 2004-02-18 Smithkline Beecham Corp Chemical compounds
WO2009006577A2 (en) * 2007-07-03 2009-01-08 The Regents Of The University Of Michigan Compositions and methods for inhibiting ezh2
US20110237606A1 (en) * 2008-09-26 2011-09-29 Agency Of Science, Technology And Research 3-Deazaneplanocin Derivatives
PT2566327T (pt) * 2010-05-07 2017-05-26 Glaxosmithkline Llc Indoles
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EP3323820B1 (en) 2011-02-28 2023-05-10 Epizyme, Inc. Substituted 6,5-fused bicyclic heteroaryl compounds

Also Published As

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

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