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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JP2020503374A (ja
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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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    • A61K47/02—Inorganic compounds
    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A61K9/2004—Excipients; Inactive ingredients
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    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • A—HUMAN NECESSITIES
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    • 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
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    • 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
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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
    • 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
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    • 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)
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  • General Health & Medical Sciences (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Inorganic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (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 (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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US11161839B2 (en) 2017-05-26 2021-11-02 The Institute Of Cancer Research: Royal Cancer Hospital 2-quinolone derived inhibitors of BCL6
AU2018274723B2 (en) 2017-05-26 2024-01-18 Cancer Research Technology Limited Benzimidazolone derived inhibitors of BCL6
US11505539B2 (en) 2017-12-22 2022-11-22 Ontario Institute For Cancer Research (Oicr) Deuterated compounds as inhibitors of the BCL6 BTB domain protein-protein interaction and/or as BCL6 degraders
US11192880B2 (en) 2017-12-22 2021-12-07 Ontario Institute For Cancer Research (Oicr) Quinolone compounds as inhibitors of the BCL6 BTB domain protein-protein interaction and/or as BCL6 degraders
AU2019253510B2 (en) * 2018-04-13 2023-08-10 Cancer Research Technology Limited BCL6 inhibitors
US20210330672A1 (en) * 2018-07-13 2021-10-28 Teqla Therapeutics Inc. Use of bcl6 inhibitors for treating 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
US12310975B2 (en) 2019-10-17 2025-05-27 Arvinas Operations, Inc. Modulators of BCL6 proteolysis and associated methods of use
US12545657B2 (en) * 2020-12-23 2026-02-10 Baylor College Of Medicine Small-molecule modulators of the orphan nuclear receptor TLX
CA3214806A1 (en) 2021-04-16 2022-10-20 Arvinas Operations, Inc. Modulators of bcl6 proteolysis and associated methods of use
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
JP2025518252A (ja) * 2022-06-02 2025-06-12 シーザン ハイスーク ファーマシューティカル カンパニー リミテッド Ｂｃｌ６を阻害又は分解する化合物及びその医薬的な応用
CR20250001A (es) 2022-06-06 2025-05-14 Treeline Biosciences Inc Degradadores bifuncionales de bcl6 de quinolona tricíclica
JP2025525324A (ja) 2022-06-13 2025-08-05 ツリーライン バイオサイエンシズ インコーポレイテッド １，８－ナフチリジン－２－オンヘテロ二官能性ｂｃｌ６分解剤
AU2023292893A1 (en) 2022-06-13 2025-01-02 Treeline Biosciences, Inc. Quinolone bcl6 bifunctional degraders
JP2025524835A (ja) * 2022-07-19 2025-08-01 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 キノキサリンジオンおよびピリド［２，３－ｂ］ピラジン－２，３－ジオンｂ細胞リンパ腫６（ｂｃｌ６）分解剤ならびにその使用
CN119585240A (zh) * 2022-08-09 2025-03-07 丹娜-法伯癌症研究院 大环bcl6降解剂
CN120813582A (zh) * 2023-03-17 2025-10-17 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
WO2025049964A1 (en) * 2023-09-01 2025-03-06 Treeline Biosciences, Inc. Bcl6 bifunctional degraders
AU2024330272A1 (en) * 2023-09-01 2026-03-19 Treeline Biosciences, Inc. Tricyclic quinolone and 1,8-naphthyridin-2-one 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
US11505539B2 (en) * 2017-12-22 2022-11-22 Ontario Institute For Cancer Research (Oicr) Deuterated compounds as inhibitors of the BCL6 BTB domain protein-protein interaction and/or as BCL6 degraders
US11192880B2 (en) * 2017-12-22 2021-12-07 Ontario Institute For Cancer Research (Oicr) 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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US20200071297A1 (en) 2020-03-05
JP2020503374A (ja) 2020-01-30
EP3555063B1 (en) 2020-09-16
EP3555063A1 (en) 2019-10-23
WO2018108704A1 (en) 2018-06-21
US11001570B2 (en) 2021-05-11

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