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
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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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 (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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US9175331B2 (en) 2010-09-10 2015-11-03 Epizyme, Inc. Inhibitors of human EZH2, and methods of use thereof
EP2681216B1 (en) 2011-02-28 2017-09-27 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
CA2850570A1 (en) 2011-09-30 2013-04-04 Glaxosmithkline Llc Methods of treating cancer
US9206128B2 (en) 2011-11-18 2015-12-08 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
US9051269B2 (en) 2011-11-18 2015-06-09 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
RS59392B1 (sr) 2012-04-13 2019-11-29 Epizyme Inc N-((4,6-dimetil-2-okso-l,2-dihidropiridin-3-il)metil)-5-(etil(tetrahidro-2h-piran-4-il)amino)-4-metil-4’ (morfolinometil)-[l,1’-bifenil]-3-karboksamid hidrobromid za upotrebu u lečenju proliferativnih poremećaja ćelija hematološkog sistema
US9562041B2 (en) 2012-05-16 2017-02-07 Glaxosmithkline Llc Enhancer of zeste homolog 2 inhibitors
HK1213552A1 (zh) 2012-10-15 2016-07-08 Epizyme, Inc. 经取代的苯化合物
RS59541B1 (sr) * 2012-10-15 2019-12-31 Epizyme Inc Metodi lečenja kancera
US20150344427A1 (en) * 2012-12-21 2015-12-03 Epizyme, Inc. 1,4-pyridone compounds
WO2014100665A1 (en) 2012-12-21 2014-06-26 Epizyme, Inc. 1,4-pyridone bicyclic heteroaryl compounds
EP2970220A2 (en) 2013-03-14 2016-01-20 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
WO2014144659A1 (en) 2013-03-14 2014-09-18 Epizyme, Inc. Pyrazole derivatives as prmt1 inhibitors and uses thereof
US9365527B2 (en) 2013-03-14 2016-06-14 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
US9133189B2 (en) 2013-03-14 2015-09-15 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
WO2014153172A1 (en) 2013-03-14 2014-09-25 Epizyme, Inc. Pyrazole derivatives as prmt1 inhibitors and uses thereof
CA2903264A1 (en) 2013-03-14 2014-11-06 Epizyme, Inc. Pyrazole derivatives as arginine methyltransferase inhibitors and uses thereof
US9120757B2 (en) 2013-03-14 2015-09-01 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
US8952026B2 (en) 2013-03-14 2015-02-10 Epizyme, Inc. PRMT1 inhibitors and uses thereof
US9045455B2 (en) 2013-03-14 2015-06-02 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
ES2837034T3 (es) 2013-03-14 2021-06-29 Epizyme Inc Inhibidores de arginina metiltransferasa y usos de los mismos
WO2014151142A1 (en) 2013-03-15 2014-09-25 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
HK1214815A1 (zh) 2013-04-30 2016-08-05 Glaxosmithkline Intellectual Property (No. 2) Limited Zeste增强子同源物2的抑制剂
JP2016520645A (ja) * 2013-06-06 2016-07-14 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
WO2015004618A1 (en) 2013-07-10 2015-01-15 Glaxosmithkline Intellectual Property (No.2) Limited Enhancer of zeste homolog 2 inhibitors
EP3033334A1 (en) 2013-08-15 2016-06-22 Constellation Pharmaceuticals, Inc. Indole derivatives as modulators of methyl modifying enzymes, compositions and uses thereof
CN105829302B (zh) 2013-10-16 2020-09-08 Epizyme股份有限公司 用于ezh2抑制的盐酸盐形式
WO2015077194A1 (en) * 2013-11-22 2015-05-28 Bristol-Myers Squibb Company Inhibitors of lysine methyl transferase
EP3111222A1 (en) 2014-02-26 2017-01-04 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
WO2016101956A2 (en) 2014-12-23 2016-06-30 University Of Copenhagen Treatment of cancer by inhibiting ezh2 activity
EP3341080A4 (en) 2015-08-24 2019-03-20 Epizyme Inc METHOD FOR THE TREATMENT OF 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
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
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
CN112399857A (zh) 2018-07-09 2021-02-23 盲人庇护基金会 Prc2亚单位的抑制治疗眼失调
WO2021021986A1 (en) * 2019-07-31 2021-02-04 Ribon Therapeutics, Inc. Heterobicyclic amides as inhibitors of 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
HRP20251111T1 (hr) 2021-01-29 2025-11-21 Boehringer Ingelheim International Gmbh Azakinolini kao inhibitori 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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DE10022925A1 (de) * 2000-05-11 2001-11-15 Basf Ag Substituierte Indole als PARP-Inhibitoren
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JP5889875B2 (ja) 2010-05-07 2016-03-22 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニーＧｌａｘｏＳｍｉｔｈＫｌｉｎｅ ＬＬＣ アザインダゾール
JP5864546B2 (ja) * 2010-05-07 2016-02-17 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニーＧｌａｘｏＳｍｉｔｈＫｌｉｎｅ ＬＬＣ インダゾール
EP2681216B1 (en) 2011-02-28 2017-09-27 Epizyme, Inc. Substituted 6,5-fused bicyclic heteroaryl compounds

Also Published As

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

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