JP6453845B2 - Ｂｒｄ４阻害薬としてのジヒドロキナゾリノン類似体 - Google Patents

Ｂｒｄ４阻害薬としてのジヒドロキナゾリノン類似体 Download PDF

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JP6453845B2
JP6453845B2 JP2016504661A JP2016504661A JP6453845B2 JP 6453845 B2 JP6453845 B2 JP 6453845B2 JP 2016504661 A JP2016504661 A JP 2016504661A JP 2016504661 A JP2016504661 A JP 2016504661A JP 6453845 B2 JP6453845 B2 JP 6453845B2
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phenyl
methyl
mmol
mixture
hplc
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JP2016515561A (ja
JP2016515561A5 (enExample
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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
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
ウルリヒ ライザー
ウルリヒ ライザー
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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
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—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
    • 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)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2016504661A 2013-03-27 2014-03-26 Ｂｒｄ４阻害薬としてのジヒドロキナゾリノン類似体 Active JP6453845B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP13161487 2013-03-27
EP13161487.7 2013-03-27
PCT/EP2014/056081 WO2014154762A1 (en) 2013-03-27 2014-03-26 Dihydroquinazolinone analogues as brd4 inhibitors

Publications (3)

Publication Number Publication Date
JP2016515561A JP2016515561A (ja) 2016-05-30
JP2016515561A5 JP2016515561A5 (enExample) 2017-05-18
JP6453845B2 true JP6453845B2 (ja) 2019-01-16

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JP2016504661A Active JP6453845B2 (ja) 2013-03-27 2014-03-26 Ｂｒｄ４阻害薬としてのジヒドロキナゾリノン類似体

Country Status (4)

Country Link
US (1) US9199988B2 (enExample)
EP (1) EP2978758B1 (enExample)
JP (1) JP6453845B2 (enExample)
WO (1) WO2014154762A1 (enExample)

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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
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
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
CA2919948C (en) 2013-07-31 2020-07-21 Zenith Epigenetics Corp. Novel quinazolinones as bromodomain 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
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
WO2015095370A1 (en) * 2013-12-19 2015-06-25 Gilead Sciences, Inc. Fused heterocyclic compounds as ion channel modulators
KR102394518B1 (ko) 2014-01-09 2022-05-06 오리온 코포레이션 브로모도메인 억제제로서의 비사이클릭 헤테로사이클릭 유도체
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
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
US10179125B2 (en) 2014-12-01 2019-01-15 Zenith Epigenetics Ltd. 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
WO2016092375A1 (en) 2014-12-11 2016-06-16 Zenith Epigenetics Corp. Substituted heterocycles as bromodomain inhibitors
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
WO2016203335A1 (en) 2015-06-18 2016-12-22 Pfizer Inc. Novel pyrido[2,3-b]pyrazinones as bet-family bromodomain inhibitors
CN105130880B (zh) * 2015-09-18 2017-07-11 上海皓伯化工科技有限公司 一种制备1‑(3‑甲氧丙基)哌啶‑4‑胺的方法
WO2017075377A1 (en) 2015-10-29 2017-05-04 Incyte Corporation Amorphous solid form of a bet protein inhibitor
CN105541825A (zh) * 2015-12-28 2016-05-04 中国药科大学 三氮唑衍生物制备方法及其作为药物的用途
CN109715625B (zh) 2016-06-20 2022-04-19 因赛特公司 Bet抑制剂的结晶固体形式
CN107056771A (zh) * 2017-01-23 2017-08-18 中国药科大学 Bromodomain蛋白二价抑制剂及其制备方法和应用
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
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
US12527741B2 (en) 2021-06-17 2026-01-20 Wisconsin Alumni Research Foundation Modular dendron micelles for treatment of pulmonary diseases related to fibrosis and viral infection including COVID-19
WO2023274418A1 (zh) * 2021-07-02 2023-01-05 南京明德新药研发有限公司 蛋白降解靶向嵌合体类化合物
CN114437041B (zh) * 2022-02-25 2023-11-10 湖北科技学院 一类具有抗肿瘤活性的4-四唑基取代-3，4-二氢喹唑啉衍生物及其制备方法和应用
CN121248481B (zh) * 2025-11-25 2026-08-11 渭南师范学院 一种2-(2-氨基-5-溴-苯甲酰基)吡啶的合成方法

Family Cites Families (2)

* 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
GB0919432D0 (en) * 2009-11-05 2009-12-23 Glaxosmithkline Llc Use

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Publication number Publication date
JP2016515561A (ja) 2016-05-30
WO2014154762A1 (en) 2014-10-02
US9199988B2 (en) 2015-12-01
US20140296230A1 (en) 2014-10-02
EP2978758B1 (en) 2017-02-08
EP2978758A1 (en) 2016-02-03

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