JP6999688B2 - Ｂｃｌ６阻害剤としての新規の６－アミノキノリノン化合物および誘導体 - Google Patents

Ｂｃｌ６阻害剤としての新規の６－アミノキノリノン化合物および誘導体 Download PDF

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JP6999688B2
JP6999688B2 JP2019551728A JP2019551728A JP6999688B2 JP 6999688 B2 JP6999688 B2 JP 6999688B2 JP 2019551728 A JP2019551728 A JP 2019551728A JP 2019551728 A JP2019551728 A JP 2019551728A JP 6999688 B2 JP6999688 B2 JP 6999688B2
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JP2020503374A5 (enExample
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シュテファン シュトイラー
ゲオルク ダーマン
ニーナ ケレス
マンフレッド ケーグル
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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
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/12—Heterocyclic 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
    • A—HUMAN NECESSITIES
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    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/02—Inorganic compounds
    • A—HUMAN NECESSITIES
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    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K9/08—Solutions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • A—HUMAN NECESSITIES
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    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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 three or more hetero rings
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/113—Spiro-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
    • 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
    • C07D498/08—Bridged systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Inorganic Chemistry (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2019551728A 2016-12-13 2017-12-07 Ｂｃｌ６阻害剤としての新規の６－アミノキノリノン化合物および誘導体 Active JP6999688B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP16203746 2016-12-13
EP16203746.9 2016-12-13
PCT/EP2017/081899 WO2018108704A1 (en) 2016-12-13 2017-12-07 New 6-amino-quinolinone compounds and derivatives as bcl6 inhibitors

Publications (3)

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JP2020503374A JP2020503374A (ja) 2020-01-30
JP2020503374A5 JP2020503374A5 (enExample) 2021-01-21
JP6999688B2 true JP6999688B2 (ja) 2022-02-10

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JP2019551728A Active JP6999688B2 (ja) 2016-12-13 2017-12-07 Ｂｃｌ６阻害剤としての新規の６－アミノキノリノン化合物および誘導体

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US (1) US11001570B2 (enExample)
EP (1) EP3555063B1 (enExample)
JP (1) JP6999688B2 (enExample)
WO (1) WO2018108704A1 (enExample)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3630749B9 (en) 2017-05-26 2024-05-29 Cancer Research Technology Limited 2-quinolone derived inhibitors of bcl6
EP3630291B9 (en) 2017-05-26 2024-05-29 Cancer Research Technology Limited Benzimidazolone derived inhibitors of bcl6
EP3728232B1 (en) * 2017-12-22 2023-08-30 Ontario Institute for Cancer Research (OICR) Novel quinolone compounds as inhibitors of the bcl6 btb domain protein-protein interaction and/or as bcl6 degraders
CA3086368A1 (en) 2017-12-22 2019-06-27 Ontario Institute For Cancer Research (Oicr) Novel deuterated compounds as inhibitors of the bcl6 btb domain protein-protein interaction and/or as bcl6 degraders
IL296734B2 (en) * 2018-04-13 2025-06-01 The Institute Of Cancer Res Royal Cancer Hospital Bcl6 inhibitors
EP3820500A4 (en) * 2018-07-13 2022-04-13 Teqla Therapeutics, Inc. USE OF BCL6 INHIBITORS TO TREAT AUTOIMMUNE DISEASES
GB201819126D0 (en) * 2018-11-23 2019-01-09 Cancer Research Tech Ltd Inhibitor compounds
GB201909573D0 (en) 2019-07-03 2019-08-14 Cancer Research Tech Ltd Modulation of T cell cytotoxicity and related therapy
GB201914860D0 (en) 2019-10-14 2019-11-27 Cancer Research Tech Ltd Inhibitor compounds
MX2022004526A (es) 2019-10-17 2022-07-21 Arvinas Operations Inc Moléculas bifuncionales que contienen una porción de unión a la ligasa de ubiquitina e3 unida a una porción de direccionamiento a bcl6.
CN117377664A (zh) * 2020-12-23 2024-01-09 贝勒医学院 孤儿核受体tlx的小分子调节剂
CN118388454A (zh) 2021-04-16 2024-07-26 阿尔维纳斯运营股份有限公司 Bcl6蛋白水解的调节剂和其相关使用方法
US20250074890A1 (en) * 2021-08-02 2025-03-06 Dana-Farber Cancer Institute, Inc. Cyanopyridine and cyanopyrimidine bcl6 degraders
US20250066326A1 (en) * 2021-12-17 2025-02-27 Dana-Farber Cancer Institute, Inc. Bcl6 degraders and uses thereof
CA3251059A1 (en) 2022-05-02 2023-11-09 The Board Of Trustees Of The Leland Stanford Junior University Compositions, systems and methods for modulating a target gene
KR20250020448A (ko) * 2022-06-02 2025-02-11 시젱 하이스코 파마수티칼 씨오., 엘티디. Bcl6을 억제하거나 분해하는 화합물 및 의약학에서의 응용
WO2023240038A1 (en) 2022-06-06 2023-12-14 Treeline Biosciences, Inc. Tricyclic quinolone bcl6 bifunctional degraders
KR20250023483A (ko) 2022-06-13 2025-02-18 트리라인 바이오사이언시스, 인크. 퀴놀론 bcl6 이작용성 분해제
AU2023295387A1 (en) 2022-06-13 2025-01-09 Treeline Biosciences, Inc. 1,8-naphthyridin-2-one heterobifunctional bcl6 degraders
EP4558487A1 (en) * 2022-07-19 2025-05-28 Dana-Farber Cancer Institute, Inc. Quinoxalinedione and pyrido [2, 3-b]pyrazine-2, 3-dione b cell lymphoma 6 (bcl6) degraders and uses thereof
KR20250044657A (ko) * 2022-08-09 2025-04-01 다나-파버 캔서 인스티튜트 인크. 거대고리 bcl6 분해제
WO2024193464A1 (zh) * 2023-03-17 2024-09-26 西藏海思科制药有限公司 一种含氮三并环衍生物及其在医药上的应用
CN117003735B (zh) * 2023-08-08 2025-12-26 西南交通大学 一种靶向bcl6蛋白降解的二价配体分子及其应用
AU2024330272A1 (en) * 2023-09-01 2026-03-19 Treeline Biosciences, Inc. Tricyclic quinolone and 1,8-naphthyridin-2-one bcl6 bifunctional degraders
AU2024331602A1 (en) * 2023-09-01 2026-03-19 Treeline Biosciences, Inc. Bcl6 bifunctional degraders
CN120987969A (zh) * 2024-05-21 2025-11-21 中国药科大学 一类蛋白靶向降解嵌合体及其用途

Citations (6)

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Publication number Priority date Publication date Assignee Title
WO2007136592A2 (en) 2006-05-18 2007-11-29 Amphora Discovery Corporation 2-0x0-l,2-dihydr0quin0line derivatives, compositions, and uses thereof as antiproliferative agents
WO2008066887A2 (en) 2006-11-30 2008-06-05 Albert Einstein College Of Medicine Of Yeshiva University Small molecule inhibitors of bcl6
JP2008543778A (ja) 2005-06-08 2008-12-04 ライジェル ファーマシューティカルズ， インコーポレイテッド Ｊａｋ経路の阻害のための組成物および方法
JP2009519249A (ja) 2005-12-09 2009-05-14 アムジエン・インコーポレーテツド プロリルヒドロキシラーゼ阻害活性を示すキノロンベースの化合物、およびこの組成物、およびこの使用
JP2011518157A (ja) 2008-04-16 2011-06-23 ポートラ ファーマシューティカルズ， インコーポレイテッド Ｓｙｋ又はｊａｋキナーゼ阻害剤としての２，６−ジアミノ−ピリミジン−５−イル−カルボキサミド類
CN105037265A (zh) 2015-05-20 2015-11-11 南京大学 一类含查尔酮骨架的喹啉酮衍生物的制备方法及在抗癌药物中的应用

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA3086368A1 (en) * 2017-12-22 2019-06-27 Ontario Institute For Cancer Research (Oicr) Novel deuterated compounds as inhibitors of the bcl6 btb domain protein-protein interaction and/or as bcl6 degraders
EP3728232B1 (en) * 2017-12-22 2023-08-30 Ontario Institute for Cancer Research (OICR) Novel quinolone compounds as inhibitors of the bcl6 btb domain protein-protein interaction and/or as bcl6 degraders

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2008543778A (ja) 2005-06-08 2008-12-04 ライジェル ファーマシューティカルズ， インコーポレイテッド Ｊａｋ経路の阻害のための組成物および方法
JP2009519249A (ja) 2005-12-09 2009-05-14 アムジエン・インコーポレーテツド プロリルヒドロキシラーゼ阻害活性を示すキノロンベースの化合物、およびこの組成物、およびこの使用
WO2007136592A2 (en) 2006-05-18 2007-11-29 Amphora Discovery Corporation 2-0x0-l,2-dihydr0quin0line derivatives, compositions, and uses thereof as antiproliferative agents
WO2008066887A2 (en) 2006-11-30 2008-06-05 Albert Einstein College Of Medicine Of Yeshiva University Small molecule inhibitors of bcl6
JP2011518157A (ja) 2008-04-16 2011-06-23 ポートラ ファーマシューティカルズ， インコーポレイテッド Ｓｙｋ又はｊａｋキナーゼ阻害剤としての２，６−ジアミノ−ピリミジン−５−イル−カルボキサミド類
CN105037265A (zh) 2015-05-20 2015-11-11 南京大学 一类含查尔酮骨架的喹啉酮衍生物的制备方法及在抗癌药物中的应用

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EP3555063A1 (en) 2019-10-23
WO2018108704A1 (en) 2018-06-21
EP3555063B1 (en) 2020-09-16
JP2020503374A (ja) 2020-01-30
US20200071297A1 (en) 2020-03-05
US11001570B2 (en) 2021-05-11

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