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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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic 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
    • C07D498/04—Ortho-condensed systems
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D413/02—Heterocyclic 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
    • C07D413/04—Heterocyclic 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
    • 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

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (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

Country Status (4)

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

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US9073878B2 (en) 2012-11-21 2015-07-07 Zenith Epigenetics Corp. Cyclic amines as bromodomain inhibitors
US9765039B2 (en) 2012-11-21 2017-09-19 Zenith Epigenetics Ltd. Biaryl derivatives as bromodomain inhibitors
CN105073744B (zh) 2012-12-21 2019-11-08 齐尼思表观遗传学有限公司 作为溴结构域抑制剂的新型杂环化合物
BR112015022942B1 (pt) 2013-03-15 2022-02-22 Incyte Holdings Corporation Compostos heterocíciclos tricíclicos, método para inibir proteína bet in vitro e composição farmacêutica compreendendo os referidos compostos
EA027139B1 (ru) 2013-04-26 2017-06-30 Бейджин, Лтд. Замещенные 5-(3,5-диметилизоксазол-4-ил)индолин-2-оны
SG10201710705UA (en) 2013-06-21 2018-02-27 Zenith Epigenetics Ltd Novel bicyclic bromodomain inhibitors
WO2015004533A2 (en) 2013-06-21 2015-01-15 Zenith Epigenetics Corp. Novel substituted bicyclic compounds as bromodomain inhibitors
ES2635560T3 (es) 2013-07-08 2017-10-04 Incyte Holdings Corporation Heterociclos tricíclicos como inhibidores de la proteína NET
EP3027604B1 (en) 2013-07-31 2019-02-20 Zenith Epigenetics Ltd. Novel quinazolinones as bromodomain inhibitors
US9315501B2 (en) 2013-11-26 2016-04-19 Incyte Corporation Bicyclic heterocycles as BET protein inhibitors
US9399640B2 (en) 2013-11-26 2016-07-26 Incyte Corporation Substituted pyrrolo[2,3-c]pyridines and pyrazolo[3,4-c]pyridines as BET protein inhibitors
WO2015095492A1 (en) 2013-12-19 2015-06-25 Incyte Corporation Tricyclic heterocycles as bet protein inhibitors
NZ725930A (en) 2014-04-23 2023-04-28 Incyte Holdings Corp 1h-pyrrolo[2,3-c]pyridin-7(6h)-ones and pyrazolo[3,4-c]pyridin-7(6h)-ones as inhibitors of bet proteins
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
CN107429246B (zh) 2014-10-31 2021-06-01 麻省理工学院 用于crispr的大规模并行组合遗传学
HK1246273B (en) 2014-12-01 2019-12-06 恒翼生物医药(上海)股份有限公司 Substituted pyridines as bromodomain inhibitors
HK1245246A1 (zh) 2014-12-01 2018-08-24 恒翼生物医药科技(上海)有限公司 作为溴域抑制剂的取代吡啶酮
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
CA2966450A1 (en) 2014-12-17 2016-06-23 Olesya KHARENKO Inhibitors of bromodomains
JP2018527293A (ja) * 2015-06-16 2018-09-20 オリオン コーポレーション ブロモドメイン阻害剤としてのスピロ［シクロブタン−１，３’−インドリン］−２’−オン誘導体
WO2016203335A1 (en) 2015-06-18 2016-12-22 Pfizer Inc. Novel pyrido[2,3-b]pyrazinones as bet-family bromodomain inhibitors
AR106520A1 (es) 2015-10-29 2018-01-24 Incyte Corp Forma sólida amorfa de un inhibidor de proteína bet
EP3472157B1 (en) 2016-06-20 2023-04-12 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
EP3843714B1 (en) 2018-08-27 2025-11-12 Arcus Biosciences, Inc. Cd73 inhibitors
US11396502B2 (en) 2018-11-13 2022-07-26 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
BR112021019957A2 (pt) 2019-04-09 2021-12-07 Plexxikon Inc Azinas condensadas para modulação de ep300 ou cbp e indicações da mesma
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

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GB0919423D0 (en) * 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds

Also Published As

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

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