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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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
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    • A61K9/2004—Excipients; Inactive ingredients
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    • A—HUMAN NECESSITIES
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    • A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • A—HUMAN NECESSITIES
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    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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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
    • C07D401/14—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
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    • 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
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    • 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
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    • 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)
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  • General Health & Medical Sciences (AREA)
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  • Inorganic Chemistry (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Other In-Based 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

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JP2020503374A JP2020503374A (ja) 2020-01-30
JP2020503374A5 JP2020503374A5 (https=) 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 (https=)
EP (1) EP3555063B1 (https=)
JP (1) JP6999688B2 (https=)
WO (1) WO2018108704A1 (https=)

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US11161839B2 (en) 2017-05-26 2021-11-02 The Institute Of Cancer Research: Royal Cancer Hospital 2-quinolone derived inhibitors of BCL6
JP7202315B2 (ja) 2017-05-26 2023-01-11 キャンサー・リサーチ・テクノロジー・リミテッド ベンズイミダゾロン由来のｂｃｌ６阻害剤
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
WO2019119138A1 (en) * 2017-12-22 2019-06-27 Ontario Institute For Cancer Research (Oicr) Novel quinolone compounds as inhibitors of the bcl6 btb domain protein-protein interaction and/or as bcl6 degraders
CA3095371A1 (en) * 2018-04-13 2019-10-17 Cancer Research Technology Limited Bcl6 inhibitors
EP3820500A4 (en) * 2018-07-13 2022-04-13 Teqla Therapeutics, Inc. USE OF BCL6 INHIBITORS FOR THE TREATMENT OF 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
CA3154386A1 (en) * 2019-10-17 2021-04-22 Michael Berlin Bifunctional molecules containing an e3 ubiquitine ligase binding moiety linked to a bcl6 targeting moiety
KR20230171979A (ko) 2021-04-16 2023-12-21 아비나스 오퍼레이션스, 인코포레이티드 Bcl6 단백질 분해의 조절제 및 관련 사용 방법
AU2022325137A1 (en) * 2021-08-02 2024-02-01 Dana-Farber Cancer Institute, Inc. Cyanopyridine and cyanopyrimidine bcl6 degraders
EP4448487A4 (en) * 2021-12-17 2025-12-03 Dana Farber Cancer Inst Inc BCL6 DEGRADING AGENTS AND THEIR USES
AU2023278399A1 (en) * 2022-06-02 2024-12-19 Xizang Haisco Pharmaceutical Co., Ltd. Compound for inhibiting or degrading bcl6 and use thereof in pharmaceutics
PE20250756A1 (es) 2022-06-06 2025-03-13 Treeline Biosciences Inc Degradadores bifuncionales de bcl6 de quinolona triciclica
EP4536649A1 (en) 2022-06-13 2025-04-16 Treeline Biosciences, Inc. Quinolone bcl6 bifunctional degraders
KR20250023481A (ko) 2022-06-13 2025-02-18 트리라인 바이오사이언시스, 인크. 1,8-나프티리딘-2-온 이종이작용성 bcl6 분해제
CN119497710A (zh) * 2022-07-19 2025-02-21 丹娜-法伯癌症研究院 喹喔啉二酮和吡啶并[2,3-b]吡嗪-2,3-二酮b细胞淋巴瘤6(bcl6)降解剂及其用途
JP2025526656A (ja) * 2022-08-09 2025-08-15 ダナ－ファーバー キャンサー インスティテュート，インコーポレイテッド 大環状ｂｃｌ６分解剤
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)

* Cited by examiner, † Cited by third party
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

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2019119138A1 (en) * 2017-12-22 2019-06-27 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

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

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