JP6370368B2 - Brd4阻害剤としてのインドリノン類似体 - Google Patents

Brd4阻害剤としてのインドリノン類似体 Download PDF

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JP6370368B2
JP6370368B2 JP2016504660A JP2016504660A JP6370368B2 JP 6370368 B2 JP6370368 B2 JP 6370368B2 JP 2016504660 A JP2016504660 A JP 2016504660A JP 2016504660 A JP2016504660 A JP 2016504660A JP 6370368 B2 JP6370368 B2 JP 6370368B2
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mmol
phenyl
alkyl
methyl
hplc
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JP2016515560A5 (enExample
JP2016515560A (ja
Inventor
ハラルド エンゲルハルト
ハラルド エンゲルハルト
ダヴィデ ジャンニ
ダヴィデ ジャンニ
アンドレアス マントウリディス
アンドレアス マントウリディス
クリスティアン スメサースト
クリスティアン スメサースト
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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
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
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04Ortho-condensed systems
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
JP2016504660A 2013-03-27 2014-03-26 Brd4阻害剤としてのインドリノン類似体 Active JP6370368B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP13161486 2013-03-27
EP13161486.9 2013-03-27
PCT/EP2014/056079 WO2014154760A1 (en) 2013-03-27 2014-03-26 Indolinone analogues as brd4 inhibitors

Publications (3)

Publication Number Publication Date
JP2016515560A JP2016515560A (ja) 2016-05-30
JP2016515560A5 JP2016515560A5 (enExample) 2017-04-27
JP6370368B2 true JP6370368B2 (ja) 2018-08-08

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JP2016504660A Active JP6370368B2 (ja) 2013-03-27 2014-03-26 Brd4阻害剤としてのインドリノン類似体

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US (1) US9102684B2 (enExample)
EP (1) EP2978757B1 (enExample)
JP (1) JP6370368B2 (enExample)
WO (1) WO2014154760A1 (enExample)

Families Citing this family (40)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9266891B2 (en) 2012-11-16 2016-02-23 Boehringer Ingelheim International Gmbh Substituted [1,2,4]triazolo[4,3-A]pyrazines that are BRD4 inhibitors
WO2014080291A2 (en) 2012-11-21 2014-05-30 Rvx Therapeutics Inc. Biaryl derivatives as bromodomain inhibitors
US9073878B2 (en) 2012-11-21 2015-07-07 Zenith Epigenetics Corp. Cyclic amines as bromodomain inhibitors
WO2014096965A2 (en) 2012-12-21 2014-06-26 Rvx Therapeutics Inc. Novel heterocyclic compounds as bromodomain inhibitors
MX366703B (es) 2013-03-15 2019-07-22 Incyte Holdings Corp Heterociclos tricíclicos como inhibidores de la proteína bet.
CA2901083A1 (en) 2013-04-26 2014-10-30 Beigene, Ltd. Substituted 5-(3,5-dimethylisoxazol-4-yl)indoline-2-ones
WO2015004533A2 (en) 2013-06-21 2015-01-15 Zenith Epigenetics Corp. Novel substituted bicyclic compounds as bromodomain inhibitors
SG11201510409QA (en) 2013-06-21 2016-01-28 Zenith Epigenetics Corp Novel bicyclic bromodomain inhibitors
WO2015006193A1 (en) 2013-07-08 2015-01-15 Incyte Corporation Tricyclic heterocycles as bet protein inhibitors
WO2015015318A2 (en) 2013-07-31 2015-02-05 Zenith Epigenetics Corp. Novel quinazolinones as bromodomain inhibitors
US9315501B2 (en) 2013-11-26 2016-04-19 Incyte Corporation Bicyclic heterocycles as BET protein inhibitors
WO2015081203A1 (en) 2013-11-26 2015-06-04 Incyte Corporation Bicyclic heterocycles as bet protein inhibitors
US9309246B2 (en) 2013-12-19 2016-04-12 Incyte Corporation Tricyclic heterocycles as BET protein inhibitors
UA119870C2 (uk) 2014-04-23 2019-08-27 Інсайт Корпорейшн 1H-ПІРОЛО[2,3-c]ПІРИДИН-7(6H)-ОНИ ТА ПІРАЗОЛО[3,4-c]ПІРИДИН-7(6H)-ОНИ ЯК ІНГІБІТОРИ БІЛКІВ BET
US9902702B2 (en) * 2014-07-15 2018-02-27 Bristol-Myers Squibb Company Spirocycloheptanes as inhibitors of rock
ES2855225T3 (es) 2014-09-15 2021-09-23 Incyte Corp Heterociclos tricíclicos para su uso como inhibidores de proteínas BET
DK3212789T3 (da) 2014-10-31 2020-07-27 Massachusetts Inst Technology Massiv parallel kombinatorisk genetik til crispr
US10710992B2 (en) 2014-12-01 2020-07-14 Zenith Epigenetics Ltd. Substituted pyridinones as bromodomain inhibitors
EP3227280B1 (en) * 2014-12-01 2019-04-24 Zenith Epigenetics Ltd. Substituted pyridines as bromodomain inhibitors
JP2017537946A (ja) 2014-12-11 2017-12-21 ゼニス・エピジェネティクス・リミテッドZenith Epigenetics Ltd. ブロモドメイン阻害剤としての置換複素環
HK1245247A1 (zh) 2014-12-17 2018-08-24 恒翼生物医药科技(上海)有限公司 溴结构域的抑制剂
CA2988209A1 (en) * 2015-06-16 2016-12-22 Orion Corporation Spiro[cyclobutane-1,3'-indolin]-2'-one derivatives as bromodomain inhibitors
WO2016203335A1 (en) 2015-06-18 2016-12-22 Pfizer Inc. Novel pyrido[2,3-b]pyrazinones as bet-family bromodomain inhibitors
TW201722966A (zh) 2015-10-29 2017-07-01 英塞特公司 Bet蛋白質抑制劑之非晶固體形式
AU2017281286B2 (en) 2016-06-20 2021-05-20 Incyte Corporation Crystalline solid forms of a bet inhibitor
WO2018109271A1 (en) * 2016-12-13 2018-06-21 Orion Corporation New bromodomain inhibitors
CN107739370B (zh) * 2017-10-26 2021-03-30 中国药科大学 吡咯酮类brd4蛋白抑制剂的制备方法以及用途
CN109928979B (zh) * 2017-12-15 2021-08-06 四川科伦博泰生物医药股份有限公司 吲哚酮类衍生物及其制备方法和用途
CN108383771A (zh) * 2018-01-08 2018-08-10 华东师范大学 手性3,3-二取代异吲哚啉-1-酮衍生物及其合成方法和应用
ES3053198T3 (en) * 2018-08-27 2026-01-20 Arcus Biosciences Inc Cd73 inhibitors
WO2020102216A1 (en) 2018-11-13 2020-05-22 Incyte Corporation Substituted heterocyclic derivatives as pi3k inhibitors
WO2020102150A1 (en) 2018-11-13 2020-05-22 Incyte Corporation Heterocyclic derivatives as pi3k inhibitors
WO2020102198A1 (en) 2018-11-13 2020-05-22 Incyte Corporation Heterocyclic derivatives as pi3k inhibitors
CN113710668B (zh) * 2019-04-09 2025-01-07 Opna生物公司 用于ep300或cbp调节及其适应症的缩合吖嗪
WO2021065980A1 (ja) 2019-09-30 2021-04-08 協和キリン株式会社 Bet分解剤
WO2021175432A1 (en) 2020-03-04 2021-09-10 Boehringer Ingelheim International Gmbh Method for administration of an anti cancer agent
EP3912625A1 (en) 2020-05-20 2021-11-24 Kaerus Bioscience Limited Novel maxi-k potassium channel openers for the treatment of fragile x associated disorders
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
EP4580618A2 (en) * 2022-08-30 2025-07-09 Pannex Therapeutics Inc. Pannexin-1 modulators and methods of treating disorders in which pannexin-1 is implicated
WO2025233532A1 (en) 2024-05-10 2025-11-13 Les Laboratoires Servier Maxi-k potassium channel openers and therapeutic applications thereof

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0919423D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds

Also Published As

Publication number Publication date
US9102684B2 (en) 2015-08-11
EP2978757B1 (en) 2017-02-08
US20140296229A1 (en) 2014-10-02
WO2014154760A1 (en) 2014-10-02
JP2016515560A (ja) 2016-05-30
EP2978757A1 (en) 2016-02-03

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