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 PDFInfo
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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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- BFXPUIUKFVPUKI-UHFFFAOYSA-N Oc1nc(Cl)ncc1Cl Chemical compound Oc1nc(Cl)ncc1Cl BFXPUIUKFVPUKI-UHFFFAOYSA-N 0.000 description 1
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Classifications
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- 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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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- 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
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- A—HUMAN NECESSITIES
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- A61K9/00—Medicinal preparations characterised by special physical form
- 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
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- 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
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
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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
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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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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- 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)
- Veterinary Medicine (AREA)
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- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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- Engineering & Computer Science (AREA)
- Biophysics (AREA)
- Hematology (AREA)
- Oncology (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)
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| EP16203746.9 | 2016-12-13 | ||
| EP16203746 | 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 |
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| JP (1) | JP6999688B2 (https=) |
| WO (1) | WO2018108704A1 (https=) |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| WO2018215798A1 (en) * | 2017-05-26 | 2018-11-29 | 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 |
| 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 |
| EP3728231A4 (en) | 2017-12-22 | 2021-05-19 | Ontario Institute for Cancer Research (OICR) | NOVEL DEUTERATED COMPOUNDS AS INHIBITORS OF THE PROTEIN-PROTEIN INTERACTION OF THE BCL6-BTB DOMAIN AND / OR AS BCL6 DEGRADERS |
| ES3060268T3 (en) | 2018-04-13 | 2026-03-25 | Cancer Research Tech Ltd | 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 |
| CN115397821B (zh) | 2019-10-17 | 2024-09-03 | 阿尔维纳斯运营股份有限公司 | 含有与bcl6靶向部分连接的e3泛素连接酶结合部分的双官能分子 |
| CN117279910A (zh) | 2021-04-16 | 2023-12-22 | 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 |
| CA3226724A1 (en) * | 2021-08-02 | 2023-02-09 | Lyn Howard Jones | Cyanopyridine and cyanopyrimidine bcl6 degraders |
| US20250066326A1 (en) * | 2021-12-17 | 2025-02-27 | Dana-Farber Cancer Institute, Inc. | Bcl6 degraders and uses thereof |
| KR20250020448A (ko) * | 2022-06-02 | 2025-02-11 | 시젱 하이스코 파마수티칼 씨오., 엘티디. | Bcl6을 억제하거나 분해하는 화합물 및 의약학에서의 응용 |
| MA69177B1 (fr) | 2022-06-06 | 2026-03-31 | Treeline Biosciences, Inc. | Agents de dégradation bifonctionnels de quinolone-bcl6 tricycliques |
| EP4536658A1 (en) | 2022-06-13 | 2025-04-16 | Treeline Biosciences, Inc. | 1,8-naphthyridin-2-one heterobifunctional bcl6 degraders |
| WO2023244918A1 (en) | 2022-06-13 | 2023-12-21 | Treeline Biosciences, Inc. | Quinolone bcl6 bifunctional 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 |
| IL317937A (en) * | 2022-08-09 | 2025-02-01 | Dana Farber Cancer Inst Inc | Macrocyclic BCL6 joints |
| 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 |
| WO2025049964A1 (en) * | 2023-09-01 | 2025-03-06 | 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 |
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| 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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| EP3728231A4 (en) * | 2017-12-22 | 2021-05-19 | Ontario Institute for Cancer Research (OICR) | NOVEL DEUTERATED COMPOUNDS AS INHIBITORS OF THE PROTEIN-PROTEIN INTERACTION OF THE BCL6-BTB DOMAIN AND / OR AS BCL6 DEGRADERS |
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| 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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| JP2020503374A (ja) | 2020-01-30 |
| EP3555063B1 (en) | 2020-09-16 |
| WO2018108704A1 (en) | 2018-06-21 |
| EP3555063A1 (en) | 2019-10-23 |
| US20200071297A1 (en) | 2020-03-05 |
| US11001570B2 (en) | 2021-05-11 |
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