CN105308038B - Zeste增强子同源物2的抑制剂 - Google Patents

Zeste增强子同源物2的抑制剂 Download PDF

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Publication number
CN105308038B
CN105308038B CN201480033093.6A CN201480033093A CN105308038B CN 105308038 B CN105308038 B CN 105308038B CN 201480033093 A CN201480033093 A CN 201480033093A CN 105308038 B CN105308038 B CN 105308038B
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China
Prior art keywords
methyl
oxo
dihydropyridin
dimethyl
carboxamide
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Expired - Fee Related
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CN201480033093.6A
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English (en)
Chinese (zh)
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CN105308038A (zh
Inventor
小查尔斯.W.布莱克利奇
J.L.伯吉斯
N.W.约翰逊
J.卡斯帕雷克
S.D.奈特
L.V.拉弗朗斯第三
J.I.卢恩戈
W.H.米勒
K.A.纽兰德
S.P.罗默里尔
M.舒尔茨
D-S.苏
田新荣
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GlaxoSmithKline Intellectual Property No 2 Ltd
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GlaxoSmithKline Intellectual Property No 2 Ltd
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic 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
    • 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
    • C07D401/02Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/06Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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

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  • 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)
CN201480033093.6A 2013-04-30 2014-04-25 Zeste增强子同源物2的抑制剂 Expired - Fee Related CN105308038B (zh)

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 (2)

Publication Number Publication Date
CN105308038A CN105308038A (zh) 2016-02-03
CN105308038B true CN105308038B (zh) 2018-05-29

Family

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Family Applications (1)

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CN201480033093.6A Expired - Fee Related CN105308038B (zh) 2013-04-30 2014-04-25 Zeste增强子同源物2的抑制剂

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)

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BR112015008447A2 (pt) 2012-10-15 2017-07-04 Epizyme Inc métodos para tratar câncer
BR112015027527A2 (pt) * 2013-04-30 2017-07-25 Glaxosmithkline Ip No 2 Ltd intensificador de inibidores do homólogo zeste 2
WO2015004618A1 (en) 2013-07-10 2015-01-15 Glaxosmithkline Intellectual Property (No.2) Limited Enhancer of zeste homolog 2 inhibitors
JP6479029B2 (ja) 2014-02-06 2019-03-06 ヘプタレス セラピューティクス リミテッドHeptares Therapeutics Limited ムスカリンm1受容体アゴニストとしての二環式アザ化合物
JP6571180B2 (ja) * 2014-10-28 2019-09-04 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
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
KR20180042356A (ko) 2015-08-24 2018-04-25 에피자임, 인코포레이티드 암 치료 방법
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
ES2760510T3 (es) 2015-11-19 2020-05-14 Jiangsu Hengrui Medicine Co Derivado de benzofurano, método de preparación del mismo y uso del mismo en medicina
ES2801423T3 (es) 2016-05-05 2021-01-11 Glaxosmithkline Ip No 2 Ltd Potenciador de inhibidores del homólogo Zeste 2
US20170337814A1 (en) * 2016-05-20 2017-11-23 Donald Edward Morgan Safety alerting drivers device and system
CN109790160B (zh) 2016-09-07 2022-11-15 上海海和药物研究开发股份有限公司 吡啶并五元芳香环类化合物、其制备方法及用途
WO2018125983A1 (en) 2016-12-30 2018-07-05 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
JP2021531340A (ja) 2018-07-09 2021-11-18 フォンダシヨン、アジール、デ、アブグルスFondation Asile Des Aveugles 眼障害を治療するためのprc2サブユニットの阻害
US12421228B2 (en) 2019-04-22 2025-09-23 Mirati Therapeutics, Inc. Naphthyridine derivatives as PRC2 inhibitors
CN113544130B (zh) * 2019-05-31 2024-01-09 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
CA3142711A1 (en) 2019-06-05 2020-12-10 Mirati Therapeutics, Inc. Imidazo[1,2-c]pyrimidine derivatives as prc2 inhibitors for treating cancer
EP4017527A1 (en) 2019-08-22 2022-06-29 Juno Therapeutics, Inc. Combination therapy of a t cell therapy and an enhancer of zeste homolog 2 (ezh2) inhibitor and related methods
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
WO2021129629A1 (zh) * 2019-12-23 2021-07-01 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
TW202404581A (zh) 2022-05-25 2024-02-01 美商醫肯納腫瘤學公司 Mek抑制劑及其用途

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WO2012142513A1 (en) * 2011-04-13 2012-10-18 Epizyme, Inc. Substituted benzene compounds
CN102970869A (zh) * 2010-05-07 2013-03-13 葛兰素史密斯克莱有限责任公司 吲哚
WO2013049770A2 (en) * 2011-09-30 2013-04-04 Glaxosmithkline Llc Methods of treating cancer

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WO2012005805A1 (en) * 2010-05-07 2012-01-12 Glaxosmithkline Llc Azaindazoles
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Also Published As

Publication number Publication date
HK1214815A1 (zh) 2016-08-05
ES2717680T3 (es) 2019-06-24
WO2014177982A1 (en) 2014-11-06
PE20151981A1 (es) 2016-01-14
AU2014261075B2 (en) 2017-01-19
US20160102083A1 (en) 2016-04-14
ZA201507398B (en) 2017-01-25
US20170029412A1 (en) 2017-02-02
JP6373973B2 (ja) 2018-08-15
EA201592068A1 (ru) 2016-05-31
NZ630205A (en) 2017-03-31
EP2991980A1 (en) 2016-03-09
EA030196B1 (ru) 2018-07-31
CL2015003200A1 (es) 2016-04-22
SG11201508203TA (en) 2015-11-27
DOP2015000270A (es) 2016-02-15
EP2991980B1 (en) 2019-01-02
AU2014261075A1 (en) 2015-11-05
JP2016517878A (ja) 2016-06-20
PH12015502414A1 (en) 2016-02-22
KR20160003115A (ko) 2016-01-08
BR112015027527A2 (pt) 2017-07-25
CN105308038A (zh) 2016-02-03
US9505745B2 (en) 2016-11-29
CA2910873A1 (en) 2014-11-06
MX2015015144A (es) 2016-02-18
US9790212B2 (en) 2017-10-17

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