JP6373973B2 - Zesteホモログ2エンハンサー阻害剤 - Google Patents

Zesteホモログ2エンハンサー阻害剤 Download PDF

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Publication number
JP6373973B2
JP6373973B2 JP2016511152A JP2016511152A JP6373973B2 JP 6373973 B2 JP6373973 B2 JP 6373973B2 JP 2016511152 A JP2016511152 A JP 2016511152A JP 2016511152 A JP2016511152 A JP 2016511152A JP 6373973 B2 JP6373973 B2 JP 6373973B2
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JP
Japan
Prior art keywords
alkyl
methyl
oxo
dimethyl
dihydropyridin
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
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JP2016511152A
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English (en)
Japanese (ja)
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JP2016517878A (ja
JP2016517878A5 (enExample
Inventor
チャールズ、ウィリアム、ブラックリッジ、ジュニア
ジョエル、ロレイン、バージェス
ニール、ダブリュ.ジョンソン
ジリ、カスパレク
スティーブン、デイビッド、ナイト
ルイス、ブイ.ラフランス、ザ、サード
フアン、アイ.ルエンゴ
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
ステュアート、ポール、ロメリル
マーク、シュルツ
ダイ−シ、ス
シンロン、ティアン
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 Intellectual Property No 2 Ltd
Original Assignee
GlaxoSmithKline Intellectual Property No 2 Ltd
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Filing date
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Application filed by GlaxoSmithKline Intellectual Property No 2 Ltd filed Critical GlaxoSmithKline Intellectual Property No 2 Ltd
Publication of JP2016517878A publication Critical patent/JP2016517878A/ja
Publication of JP2016517878A5 publication Critical patent/JP2016517878A5/ja
Application granted granted Critical
Publication of JP6373973B2 publication Critical patent/JP6373973B2/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
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • C07D401/02—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Epidemiology (AREA)
JP2016511152A 2013-04-30 2014-04-25 Zesteホモログ2エンハンサー阻害剤 Expired - Fee Related JP6373973B2 (ja)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
US201361817436P 2013-04-30 2013-04-30
US61/817,436 2013-04-30
US201361842038P 2013-07-02 2013-07-02
US61/842,038 2013-07-02
US201361907024P 2013-11-21 2013-11-21
US61/907,024 2013-11-21
US201461936460P 2014-02-06 2014-02-06
US61/936,460 2014-02-06
PCT/IB2014/061012 WO2014177982A1 (en) 2013-04-30 2014-04-25 Enhancer of zeste homolog 2 inhibitors

Publications (3)

Publication Number Publication Date
JP2016517878A JP2016517878A (ja) 2016-06-20
JP2016517878A5 JP2016517878A5 (enExample) 2017-06-01
JP6373973B2 true JP6373973B2 (ja) 2018-08-15

Family

ID=50877537

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2016511152A Expired - Fee Related JP6373973B2 (ja) 2013-04-30 2014-04-25 Zesteホモログ2エンハンサー阻害剤

Country Status (20)

Country Link
US (2) US9505745B2 (enExample)
EP (1) EP2991980B1 (enExample)
JP (1) JP6373973B2 (enExample)
KR (1) KR20160003115A (enExample)
CN (1) CN105308038B (enExample)
AU (1) AU2014261075B2 (enExample)
BR (1) BR112015027527A2 (enExample)
CA (1) CA2910873A1 (enExample)
CL (1) CL2015003200A1 (enExample)
DO (1) DOP2015000270A (enExample)
EA (1) EA030196B1 (enExample)
ES (1) ES2717680T3 (enExample)
HK (1) HK1214815A1 (enExample)
MX (1) MX2015015144A (enExample)
NZ (1) NZ630205A (enExample)
PE (1) PE20151981A1 (enExample)
PH (1) PH12015502414A1 (enExample)
SG (1) SG11201508203TA (enExample)
WO (1) WO2014177982A1 (enExample)
ZA (1) ZA201507398B (enExample)

Families Citing this family (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9085583B2 (en) * 2012-02-10 2015-07-21 Constellation—Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
KR20190105669A (ko) 2012-10-15 2019-09-17 에피자임, 인코포레이티드 암을 치료하는 방법
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
CA2917463A1 (en) 2013-07-10 2015-01-15 Glaxosmithkline Intellectual Property (No.2) Limited Enhancer of zeste homolog 2 inhibitors
RU2685230C2 (ru) 2014-02-06 2019-04-17 Хептарес Терапьютикс Лимитед Бициклические азотсодержащие соединения как агонисты М1 мускариновых рецепторов
MA40848A (fr) * 2014-10-28 2021-05-05 Glaxosmithkline Ip No 2 Ltd Inhibiteurs d'ezh2 (enhancer of zeste homolog 2)
TW201636344A (zh) 2014-12-05 2016-10-16 美國禮來大藥廠 Ezh2抑制劑
TW201708210A (zh) * 2015-06-30 2017-03-01 葛蘭素史克智慧財產(第二)有限公司 Zeste同源物2增強子之抑制劑
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
WO2017079757A1 (en) * 2015-11-06 2017-05-11 Epizyme, Inc. Pediatric dosing for treatment of cancer with an ezh2 inhibitor
SI3378859T1 (sl) 2015-11-19 2020-03-31 Jiangsu Hengrui Medicine Co., Ltd., Derivat benzofurana, postopek za njegovo pripravo in njegova uporaba v medicini
WO2017191545A1 (en) * 2016-05-05 2017-11-09 Glaxosmithkline Intellectual Property (No.2) Limited Enhancer of zeste homolog 2 inhibitors
US20170337814A1 (en) * 2016-05-20 2017-11-23 Donald Edward Morgan Safety alerting drivers device and system
US10968215B2 (en) 2016-09-07 2021-04-06 Shanghai Haihe Pharmaceutical Co., Ltd. Pyrido five-element aromatic ring compound, preparation method therefor and use thereof
US20190367457A1 (en) 2016-12-30 2019-12-05 Mitobridge, Inc. Oxopyridine derivatives useful as aminocarboxymuconate semialdehyde decarboxylase (acmsd) inhibitors
US10266542B2 (en) 2017-03-15 2019-04-23 Mirati Therapeutics, Inc. EZH2 inhibitors
DK3746446T3 (da) 2018-01-31 2022-06-27 Mirati Therapeutics Inc PRC2-inhibitorer
WO2020011607A1 (en) 2018-07-09 2020-01-16 Fondation Asile Des Aveugles Inhibition of prc2 subunits to treat eye disorders
US12421228B2 (en) 2019-04-22 2025-09-23 Mirati Therapeutics, Inc. Naphthyridine derivatives as PRC2 inhibitors
CN118027041A (zh) * 2019-05-31 2024-05-14 西藏海思科制药有限公司 一种btk抑制剂环衍生物及其制备方法和药学上的应用
CN114269748A (zh) 2019-06-05 2022-04-01 米拉蒂医疗股份有限公司 作为用于治疗癌症的PRC2抑制剂的咪唑并[1,2-c]嘧啶衍生物
KR20220066892A (ko) 2019-08-22 2022-05-24 주노 쎄러퓨티크스 인코퍼레이티드 T 세포 요법 및 제스트 동족체 2의 인핸서 (ezh2) 억제제의 병용 요법 및 관련 방법
CN110964200A (zh) * 2019-12-19 2020-04-07 新纳奇材料科技江苏有限公司 一种基于聚硅氧烷馏出物的羟基封端聚硅氧烷的制备方法
CN114787143A (zh) * 2019-12-23 2022-07-22 四川海思科制药有限公司 Zeste增强子同源物2抑制剂及其用途
CN111233768B (zh) * 2020-03-18 2021-08-03 徐州圣元化工有限公司 一种3-(二氟甲基)-1-甲基-1h-吡唑-4-羧酸乙酯的制备方法
CN119768393A (zh) 2022-05-25 2025-04-04 医肯纳肿瘤学公司 Mek抑制剂和其用途

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20080293716A1 (en) * 2004-01-30 2008-11-27 Smithkline Beecham Corporation Chemical Compounds
WO2005095386A1 (en) * 2004-03-30 2005-10-13 Chiron Corporation Substituted thiophene derivatives as anti-cancer agents
US7696352B2 (en) * 2004-06-18 2010-04-13 Millennium Pharmaceuticals, Inc. Factor Xa inhibitors
AU2006325746A1 (en) 2005-12-14 2007-06-21 Bristol-Myers Squibb Company Six-membered heterocycles useful as serine protease inhibitors
ES2654332T3 (es) * 2009-08-07 2018-02-13 Merck Patent Gmbh Nuevos compuestos azaheterocíclicos
MX2012012966A (es) 2010-05-07 2013-01-22 Glaxosmithkline Llc Indoles.
US8846935B2 (en) 2010-05-07 2014-09-30 Glaxosmithkline Llc Indazoles
WO2012005805A1 (en) * 2010-05-07 2012-01-12 Glaxosmithkline Llc Azaindazoles
EP2646020B1 (en) 2010-12-01 2016-09-21 Glaxosmithkline LLC Indoles
WO2012118812A2 (en) 2011-02-28 2012-09-07 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
JO3363B1 (ar) 2011-04-13 2019-03-13 Epizyme Inc مركبات بنزين مستبدلة بأريل أو أريل غير متجانس
US9730925B2 (en) * 2011-09-30 2017-08-15 Glaxomithkline Llc Methods of treating cancer
US9085583B2 (en) 2012-02-10 2015-07-21 Constellation—Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
ES2617379T3 (es) 2012-04-13 2017-06-16 Epizyme, Inc. Forma de sal de un inhibidor de histona metiltransferasa EZH2 humana
US9562041B2 (en) 2012-05-16 2017-02-07 Glaxosmithkline Llc Enhancer of zeste homolog 2 inhibitors
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

Also Published As

Publication number Publication date
SG11201508203TA (en) 2015-11-27
AU2014261075A1 (en) 2015-11-05
EA201592068A1 (ru) 2016-05-31
BR112015027527A2 (pt) 2017-07-25
KR20160003115A (ko) 2016-01-08
US20170029412A1 (en) 2017-02-02
AU2014261075B2 (en) 2017-01-19
CN105308038B (zh) 2018-05-29
PE20151981A1 (es) 2016-01-14
ES2717680T3 (es) 2019-06-24
DOP2015000270A (es) 2016-02-15
US9505745B2 (en) 2016-11-29
US9790212B2 (en) 2017-10-17
JP2016517878A (ja) 2016-06-20
PH12015502414A1 (en) 2016-02-22
US20160102083A1 (en) 2016-04-14
MX2015015144A (es) 2016-02-18
HK1214815A1 (zh) 2016-08-05
CN105308038A (zh) 2016-02-03
ZA201507398B (en) 2017-01-25
EP2991980A1 (en) 2016-03-09
CA2910873A1 (en) 2014-11-06
NZ630205A (en) 2017-03-31
CL2015003200A1 (es) 2016-04-22
WO2014177982A1 (en) 2014-11-06
EP2991980B1 (en) 2019-01-02
EA030196B1 (ru) 2018-07-31

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