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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Publication number
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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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (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
EP13161486.9 2013-03-27
EP13161486 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)

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

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US9765039B2 (en) 2012-11-21 2017-09-19 Zenith Epigenetics Ltd. Biaryl derivatives as bromodomain inhibitors
US9073878B2 (en) 2012-11-21 2015-07-07 Zenith Epigenetics Corp. Cyclic amines as bromodomain inhibitors
JP2016507496A (ja) 2012-12-21 2016-03-10 ゼニス・エピジェネティクス・コーポレイションZenith Epigenetics Corp. ブロモドメイン阻害剤としての新規複素環式化合物
EA035469B1 (ru) 2013-03-15 2020-06-22 Инсайт Холдингс Корпорейшн Трициклические гетероциклы как ингибиторы белков бэт
EA027139B1 (ru) * 2013-04-26 2017-06-30 Бейджин, Лтд. Замещенные 5-(3,5-диметилизоксазол-4-ил)индолин-2-оны
KR102307566B1 (ko) 2013-06-21 2021-10-05 제니쓰 에피제네틱스 리미티드 신규한 바이사이클릭 브로모도메인 억제제
CN105473581B (zh) 2013-06-21 2019-04-23 齐尼思表观遗传学有限公司 作为溴结构域抑制剂的新取代的双环化合物
EP3019502B1 (en) 2013-07-08 2017-05-17 Incyte Holdings Corporation Tricyclic heterocycles as bet protein inhibitors
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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
US9315501B2 (en) 2013-11-26 2016-04-19 Incyte Corporation Bicyclic heterocycles as BET protein inhibitors
US9309246B2 (en) 2013-12-19 2016-04-12 Incyte Corporation Tricyclic heterocycles as BET protein inhibitors
SMT202000133T1 (it) 2014-04-23 2020-05-08 Incyte Corp 1h-pirrolo[2,3-c]piridin-7(6h)-oni e pirazolo[3,4-c]piridin-7(6h)-oni come inibitori di proteine bet
US9902702B2 (en) * 2014-07-15 2018-02-27 Bristol-Myers Squibb Company Spirocycloheptanes as inhibitors of rock
JP6599979B2 (ja) 2014-09-15 2019-10-30 インサイト・コーポレイション Betタンパク質阻害剤として用いるための三環式複素環化合物
TWI716367B (zh) 2014-10-31 2021-01-21 麻省理工學院 用於常間回文重複序列叢集(crispr)之大量平行組合性基因學
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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
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CN107406438B (zh) 2014-12-17 2021-05-14 恒翼生物医药科技(上海)有限公司 溴结构域的抑制剂
KR20180012861A (ko) * 2015-06-16 2018-02-06 오리온 코포레이션 브로모도메인 억제제로서의 스피로[사이클로부탄-1,3'-인돌린]-2'-온 유도체
WO2016203335A1 (en) 2015-06-18 2016-12-22 Pfizer Inc. Novel pyrido[2,3-b]pyrazinones as bet-family bromodomain inhibitors
WO2017075377A1 (en) 2015-10-29 2017-05-04 Incyte Corporation Amorphous solid form of a bet protein inhibitor
CN109715625B (zh) 2016-06-20 2022-04-19 因赛特公司 Bet抑制剂的结晶固体形式
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
US11161838B2 (en) 2018-11-13 2021-11-02 Incyte Corporation Heterocyclic derivatives as PI3K inhibitors
WO2020102198A1 (en) 2018-11-13 2020-05-22 Incyte Corporation Heterocyclic derivatives as pi3k inhibitors
JP7636646B2 (ja) 2019-04-09 2025-02-27 オプナ バイオ ソシエテ アノニム Ep300またはcbpの調節のための縮合アジンおよびその適応
CN114502534A (zh) 2019-09-30 2022-05-13 协和麒麟株式会社 Bet降解剂
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
US9102684B2 (en) 2015-08-11
WO2014154760A1 (en) 2014-10-02
EP2978757A1 (en) 2016-02-03
EP2978757B1 (en) 2017-02-08
US20140296229A1 (en) 2014-10-02
JP2016515560A (ja) 2016-05-30

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