JP2020503374A5 - - Google Patents
Download PDFInfo
- 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
Links
- 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 | 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)
| 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 |
|---|---|---|---|---|
| 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 |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BRPI0610876B8 (pt) * | 2005-06-08 | 2021-05-25 | Rigel Pharmaceuticals Inc | composto, formulação farmacêutica, e métodos de inibir uma atividade de uma jak cinase, e de inibir uma cascata de transdução de sinal em que jak3 cinase desempenha um papel |
| EP1960363B1 (en) * | 2005-12-09 | 2014-01-22 | Amgen, Inc. | Quinolone based compounds exhibiting prolyl hydroxylase inhibitory activity, compositions and uses thereof |
| US20070287706A1 (en) * | 2006-05-18 | 2007-12-13 | Dickson John K Jr | Certain substituted quinolones, compositions, and uses thereof |
| WO2008066887A2 (en) | 2006-11-30 | 2008-06-05 | Albert Einstein College Of Medicine Of Yeshiva University | Small molecule inhibitors of bcl6 |
| SG165655A1 (en) * | 2008-04-16 | 2010-11-29 | 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 |
| 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 |
-
2017
- 2017-12-07 US US16/469,071 patent/US11001570B2/en active Active
- 2017-12-07 WO PCT/EP2017/081899 patent/WO2018108704A1/en not_active Ceased
- 2017-12-07 JP JP2019551728A patent/JP6999688B2/ja active Active
- 2017-12-07 EP EP17811299.1A patent/EP3555063B1/en active Active
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2020503374A5 (https=) | ||
| HRP20241553T1 (hr) | 4-(4-(4-(((2-(2,6-dioksopiperidin-3-il)-l-oksoizoindolin-4-il)oksi)metil)benzil)piperazin-l-il)-3-fluorobenzonitril kao antiproliferativni spoj | |
| CA2662320C (en) | Bcl inhibitors treating platelet excess | |
| CN100471842C (zh) | 喹诺酮衍生物或其盐 | |
| JP2014500295A5 (https=) | ||
| IL205501A (en) | Preparation of preparations for the treatment of arthritis | |
| JP2007519649A5 (https=) | ||
| JP2012522847A5 (https=) | ||
| NO20056007L (no) | Dobbel NK1/NK3 antagonister for behandling av schizofreni | |
| ES2142861T3 (es) | Derivados de 4-(1h-2-metilimidazo(4,5-c)piridinilmetil)fenilsulfonamida como antagonistas del paf. | |
| RU2018106498A (ru) | Производные 5-(N-конденсированный трициклический арил-тетрагидроизохинолин-6-ил) пиридин-3-ил-уксусной кислоты в качестве ингибиторов репликации вируса иммунодефицита человека | |
| MA46268B1 (fr) | Dérivés de 5-[2-(pyridin-2-ylamino)-1 ,3-thiazol-5-yl]-2,3-dihydro-1h-isoindol-1-one et leur utilisation en tant qu'inhibiteurs doubles de phosphatidylinositol 3-kinase delta & gamma | |
| JP2018522927A5 (https=) | ||
| MX2024014315A (es) | Compuestos amido heteroaromaticos utiles en el tratamiento de enfermedades hepaticas | |
| CA3101878A1 (en) | Acyl sulfonamides that are bcl family antagonists for use in clinical management of conditions caused or mediated by senescent cells and for treating cancer | |
| JP2015517514A5 (https=) | ||
| JP2008521929A5 (https=) | ||
| BR0306701A (pt) | Composto, sal do composto, sal de cálcio, método de preparação de um sal, composição farmacêutica, método de preparação de uma composição, e, uso de um sal | |
| JP2016512501A5 (https=) | ||
| JP5461084B2 (ja) | 崩壊遅延が抑制されたパロキセチン塩酸塩水和物の経口投与用医薬組成物 | |
| SE9901572D0 (sv) | New compounds | |
| JP2021510168A5 (https=) | ||
| HU9303082D0 (en) | Process for production of 3,4-dihydro-2(1h)-quinolyne-derivatives with neuroprotective action and of pharmaceutical compositions containing them as medical agent | |
| BG64819B1 (bg) | Комбиниране на тетрахидропиридини и средства, инхибиращи ацетилхолинестераза, за лечение на сенилнадеменция от алцхаймеров тип | |
| WO2016156330A1 (en) | Solid pharmaceutical composition comprising amorphous sofosbuvir and a phospholipid |