JP2020503374A5 - - Google Patents
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- Publication number
- JP2020503374A5 JP2020503374A5 JP2019551728A JP2019551728A JP2020503374A5 JP 2020503374 A5 JP2020503374 A5 JP 2020503374A5 JP 2019551728 A JP2019551728 A JP 2019551728A JP 2019551728 A JP2019551728 A JP 2019551728A JP 2020503374 A5 JP2020503374 A5 JP 2020503374A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- group
- substituted
- hydrogen
- heterocyclyl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
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- 125000000217 alkyl group Chemical group 0.000 claims description 198
- 125000000623 heterocyclic group Chemical group 0.000 claims description 92
- 239000001257 hydrogen Substances 0.000 claims description 50
- 229910052739 hydrogen Inorganic materials 0.000 claims description 50
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 46
- 150000003839 salts Chemical class 0.000 claims description 36
- 150000001875 compounds Chemical class 0.000 claims description 35
- 125000001072 heteroaryl group Chemical group 0.000 claims description 28
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 26
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims description 24
- 229910052736 halogen Inorganic materials 0.000 claims description 16
- 150000002367 halogens Chemical class 0.000 claims description 16
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 16
- 229910052757 nitrogen Inorganic materials 0.000 claims description 14
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 12
- -1 -C 1-6 haloalkyl Chemical group 0.000 claims description 10
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 10
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 8
- 125000001424 substituent group Chemical group 0.000 claims description 8
- 239000008194 pharmaceutical composition Substances 0.000 claims description 6
- 239000013543 active substance Substances 0.000 claims description 5
- 201000010099 disease Diseases 0.000 claims description 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 5
- 102100021631 B-cell lymphoma 6 protein Human genes 0.000 claims description 4
- 101000971234 Homo sapiens B-cell lymphoma 6 protein Proteins 0.000 claims description 4
- 230000009286 beneficial effect Effects 0.000 claims description 4
- 125000001188 haloalkyl group Chemical group 0.000 claims description 4
- 150000002431 hydrogen Chemical class 0.000 claims description 4
- 230000005764 inhibitory process Effects 0.000 claims description 4
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 4
- 230000002265 prevention Effects 0.000 claims description 4
- 206010028980 Neoplasm Diseases 0.000 claims description 3
- 201000011510 cancer Diseases 0.000 claims description 3
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims description 2
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims description 2
- 125000003342 alkenyl group Chemical group 0.000 claims description 2
- 125000000304 alkynyl group Chemical group 0.000 claims description 2
- 239000000460 chlorine Substances 0.000 claims description 2
- 229910052801 chlorine Inorganic materials 0.000 claims description 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 2
- 231100000433 cytotoxic Toxicity 0.000 claims description 2
- 230000001472 cytotoxic effect Effects 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 239000011737 fluorine Substances 0.000 claims description 2
- 229910052731 fluorine Inorganic materials 0.000 claims description 2
- 230000002401 inhibitory effect Effects 0.000 claims description 2
- 125000002757 morpholinyl group Chemical group 0.000 claims description 2
- 125000004193 piperazinyl group Chemical group 0.000 claims description 2
- 125000003386 piperidinyl group Chemical group 0.000 claims description 2
- TVEXGJYMHHTVKP-UHFFFAOYSA-N 6-oxabicyclo[3.2.1]oct-3-en-7-one Chemical compound C1C2C(=O)OC1C=CC2 TVEXGJYMHHTVKP-UHFFFAOYSA-N 0.000 claims 1
- 230000010261 cell growth Effects 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 4
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 4
- 239000000203 mixture Substances 0.000 description 3
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 3
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 2
- 239000003708 ampul Substances 0.000 description 2
- 239000001913 cellulose Substances 0.000 description 2
- 229920002678 cellulose Polymers 0.000 description 2
- 239000008101 lactose Substances 0.000 description 2
- 235000019359 magnesium stearate Nutrition 0.000 description 2
- 239000011780 sodium chloride Substances 0.000 description 2
- 239000000243 solution Substances 0.000 description 2
- 0 NOCC(OCC*1CCOCC1)=O Chemical compound NOCC(OCC*1CCOCC1)=O 0.000 description 1
- 230000004663 cell proliferation Effects 0.000 description 1
- 239000000706 filtrate Substances 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 229940127557 pharmaceutical product Drugs 0.000 description 1
- 239000008215 water for injection Substances 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| 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 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020503374A JP2020503374A (ja) | 2020-01-30 |
| JP2020503374A5 true JP2020503374A5 (https=) | 2021-01-21 |
| JP6999688B2 JP6999688B2 (ja) | 2022-02-10 |
Family
ID=57544344
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| 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 |
Country Status (4)
| Country | Link |
|---|---|
| US (1) | US11001570B2 (https=) |
| EP (1) | EP3555063B1 (https=) |
| JP (1) | JP6999688B2 (https=) |
| WO (1) | WO2018108704A1 (https=) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2006133426A2 (en) * | 2005-06-08 | 2006-12-14 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the jak pathway |
| JP5202327B2 (ja) * | 2005-12-09 | 2013-06-05 | 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 |
| EP2040711A2 (en) | 2006-05-18 | 2009-04-01 | Amphora Discovery Corporation | 2-oxo-1,2-dihydroquinoline derivatives, compositions, and uses thereof as antiproliferative agents |
| US8338464B2 (en) | 2006-11-30 | 2012-12-25 | Albert Einstein College Of Medicine Of Yeshiva University | Small molecule inhibitors of BCL6 |
| SG2014015085A (en) * | 2008-04-16 | 2014-06-27 | Portola Pharm Inc | 2,6-diamino-pyrimidin-5-yl-carboxamides as syk or jak kinases inhibitors |
| 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 |
| 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 |
-
2017
- 2017-12-07 JP JP2019551728A patent/JP6999688B2/ja active Active
- 2017-12-07 WO PCT/EP2017/081899 patent/WO2018108704A1/en not_active Ceased
- 2017-12-07 EP EP17811299.1A patent/EP3555063B1/en active Active
- 2017-12-07 US US16/469,071 patent/US11001570B2/en active Active
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