JP2018507238A5 - - Google Patents
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- Publication number
- JP2018507238A5 JP2018507238A5 JP2017546629A JP2017546629A JP2018507238A5 JP 2018507238 A5 JP2018507238 A5 JP 2018507238A5 JP 2017546629 A JP2017546629 A JP 2017546629A JP 2017546629 A JP2017546629 A JP 2017546629A JP 2018507238 A5 JP2018507238 A5 JP 2018507238A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- salt
- membered
- compound
- substituted
- 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 211
- 229910052736 halogen Inorganic materials 0.000 claims description 48
- 150000001875 compounds Chemical class 0.000 claims description 45
- 150000002367 halogens Chemical class 0.000 claims description 43
- 150000003839 salts Chemical class 0.000 claims description 43
- 125000006568 (C4-C7) heterocycloalkyl group Chemical group 0.000 claims description 33
- 125000003118 aryl group Chemical group 0.000 claims description 32
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims description 31
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 28
- 125000001072 heteroaryl group Chemical group 0.000 claims description 23
- PIGFYZPCRLYGLF-UHFFFAOYSA-N Aluminum nitride Chemical compound [Al]#N PIGFYZPCRLYGLF-UHFFFAOYSA-N 0.000 claims description 21
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 19
- 125000002619 bicyclic group Chemical group 0.000 claims description 9
- 125000002950 monocyclic group Chemical group 0.000 claims description 9
- 229910052739 hydrogen Inorganic materials 0.000 claims description 7
- 239000001257 hydrogen Substances 0.000 claims description 7
- 125000001424 substituent group Chemical group 0.000 claims description 7
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 4
- 150000002431 hydrogen Chemical class 0.000 claims description 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 15
- 229910052757 nitrogen Inorganic materials 0.000 claims 9
- UHOVQNZJYSORNB-UHFFFAOYSA-N Benzene Chemical compound C1=CC=CC=C1 UHOVQNZJYSORNB-UHFFFAOYSA-N 0.000 claims 6
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical group C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 6
- 125000005843 halogen group Chemical group 0.000 claims 5
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims 2
- 150000002390 heteroarenes Chemical group 0.000 claims 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 239000013543 active substance Substances 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 239000000969 carrier Substances 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 125000003386 piperidinyl group Chemical group 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 0 CC(*=C1*)=**(**)C1=O Chemical compound CC(*=C1*)=**(**)C1=O 0.000 description 5
- FLNMQGISZVYIIK-UHFFFAOYSA-N CC[n]1nccc1 Chemical compound CC[n]1nccc1 FLNMQGISZVYIIK-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP15157879 | 2015-03-05 | ||
| EP15157879.6 | 2015-03-05 | ||
| EP15199403.5 | 2015-12-10 | ||
| EP15199403 | 2015-12-10 | ||
| PCT/EP2016/054713 WO2016139361A1 (en) | 2015-03-05 | 2016-03-04 | New pyridinones and isoquinolinones as inhibitors of the bromodomain brd9 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018507238A JP2018507238A (ja) | 2018-03-15 |
| JP2018507238A5 true JP2018507238A5 (https=) | 2020-08-06 |
| JP6857606B2 JP6857606B2 (ja) | 2021-04-14 |
Family
ID=55521687
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017546629A Active JP6857606B2 (ja) | 2015-03-05 | 2016-03-04 | ブロモドメインｂｒｄ９の阻害剤としての新規ピリジノンおよびイソキノリノン |
Country Status (4)
| Country | Link |
|---|---|
| US (1) | US11319318B2 (https=) |
| EP (1) | EP3265453B1 (https=) |
| JP (1) | JP6857606B2 (https=) |
| WO (1) | WO2016139361A1 (https=) |
Families Citing this family (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105473147A (zh) | 2013-04-24 | 2016-04-06 | 萨克生物研究学院 | 维生素d受体/smad基因组回路门纤维化反应 |
| AR104259A1 (es) | 2015-04-15 | 2017-07-05 | Celgene Quanticel Res Inc | Inhibidores de bromodominio |
| WO2019023149A1 (en) | 2017-07-24 | 2019-01-31 | Salk Institute For Biological Studies | USE OF BROMODOMAIN-CONTAINING PROTEIN-9 ANTAGONISTS IN ASSOCIATION WITH VITAMIN D RECEPTOR AGONISTS IN THE TREATMENT OF DIABETES |
| WO2019120234A2 (zh) * | 2017-12-20 | 2019-06-27 | 贝达药业股份有限公司 | 作为溴结构域蛋白质抑制剂的化合物和组合物 |
| JP2021512167A (ja) | 2018-01-30 | 2021-05-13 | フォグホーン セラピューティクス インコーポレイテッドＦｏｇｈｏｒｎ Ｔｈｅｒａｐｅｕｔｉｃｓ Ｉｎｃ． | 障害を治療するための方法及び化合物 |
| EP3774804A1 (en) | 2018-03-26 | 2021-02-17 | Novartis AG | N-(3-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)phenyl)benzamide derivatives |
| US10442799B1 (en) | 2018-04-07 | 2019-10-15 | Fuqiang Ruan | Heterocyclic compounds and uses thereof |
| CN110776508B (zh) * | 2018-07-27 | 2021-07-16 | 海创药业股份有限公司 | 一种brd4抑制剂及其制备方法和用途 |
| EP3917517A4 (en) | 2019-01-29 | 2023-01-25 | Foghorn Therapeutics Inc. | CONNECTIONS AND USES THEREOF |
| CN113874016A (zh) * | 2019-01-29 | 2021-12-31 | 福宏治疗公司 | 化合物及其用途 |
| US12384776B2 (en) | 2019-01-29 | 2025-08-12 | Foghorn Therapeutics Inc. | Compounds and uses thereof |
| WO2020160193A2 (en) * | 2019-01-29 | 2020-08-06 | Foghorn Therapeutics Inc. | Compounds and uses thereof |
| GB201905721D0 (en) * | 2019-04-24 | 2019-06-05 | Univ Dundee | Compounds |
| CN110003204B (zh) * | 2019-04-30 | 2020-08-11 | 上海勋和医药科技有限公司 | 一种bet蛋白抑制剂、其制备方法及用途 |
| EP3978480A4 (en) * | 2019-05-29 | 2023-10-25 | ST Pharm Co., Ltd. | Phthalazinone compounds and use thereof |
| WO2021022163A2 (en) * | 2019-07-31 | 2021-02-04 | Foghorn Therapeutics Inc. | Compounds and uses thereof |
| CR20220105A (es) * | 2019-09-16 | 2022-06-13 | Novartis Ag | Degradadores bifuncionales de brd9 y sus métodos de uso |
| US12528825B2 (en) | 2020-01-29 | 2026-01-20 | Foghorn Therapeutics Inc. | Compounds and uses thereof |
| AU2021214767A1 (en) * | 2020-01-29 | 2022-07-28 | Foghorn Therapeutics Inc. | Compounds and uses thereof |
| AU2021231898A1 (en) | 2020-03-05 | 2022-10-27 | C4 Therapeutics, Inc. | Compounds for targeted degradation of BRD9 |
| US11787800B2 (en) | 2020-07-29 | 2023-10-17 | Foghorn Therapeutics Inc. | BRD9 degraders and uses thereof |
| JP2023536139A (ja) * | 2020-07-29 | 2023-08-23 | フォグホーン セラピューティクス インコーポレイテッド | 化合物及びその使用 |
| US20240150755A1 (en) * | 2021-02-26 | 2024-05-09 | Salk Institute For Biological Studies | Modulating regulatory t cell function in autoimmune disease and cancer |
| WO2023283263A1 (en) | 2021-07-06 | 2023-01-12 | Foghorn Therapeutics Inc. | Citrate salt, pharmaceutical compositions, and methods of making and using the same |
| WO2023010354A1 (zh) * | 2021-08-04 | 2023-02-09 | 四川大学华西医院 | 一种具有egfr抑制活性的小分子化合物及其制备方法与应用 |
| CN119384408A (zh) | 2022-06-16 | 2025-01-28 | 安菲斯塔治疗有限责任公司 | 用于靶向蛋白降解的双功能分子 |
| EP4587126A1 (en) | 2022-09-13 | 2025-07-23 | Amphista Therapeutics Ltd | Compounds for targeted protein degradation |
| WO2024163641A2 (en) * | 2023-02-01 | 2024-08-08 | Foghorn Therapeutics Inc. | Formulations for treating cancer |
| WO2024238871A1 (en) * | 2023-05-18 | 2024-11-21 | Rectify Pharmaceuticals, Inc. | Aryl sulfonamide compounds and their use in treating medical conditions |
| CN117229202B (zh) * | 2023-11-15 | 2024-01-26 | 苏州美诺医药科技有限公司 | 一种brd9靶向降解化合物的中间体的制备方法 |
| GB202319256D0 (en) | 2023-12-15 | 2024-01-31 | Amphista Therapeutics Ltd | Novel compounds for targeted protein degradation |
| WO2025191109A1 (en) | 2024-03-13 | 2025-09-18 | Amphista Therapeutics Limited | Combinations comprising brd9 bifunctional compounds and their use in the treatment of cancer |
| WO2026052822A1 (en) | 2024-09-06 | 2026-03-12 | Amphista Therapeutics Limited | Tetrahydroisoquinoline compounds for targeted protein degradation |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HUT66969A (en) * | 1991-10-09 | 1995-01-30 | Syntex Inc | Benzo- and pyrido-pyridazinone- and pyridazin-thion derivatives, pharmaceutical compositions containing the same and process for the production of thereof |
| US5716954A (en) * | 1991-10-09 | 1998-02-10 | Syntex U.S.A. Inc. | Benzopyridazinone and pyridopyridazinone compounds |
| US5466697A (en) * | 1994-07-13 | 1995-11-14 | Syntex (U.S.A.) Inc. | 8-phenyl-1,6-naphthyridin-5-ones |
| ES2232306B1 (es) * | 2003-11-10 | 2006-08-01 | Almirall Prodesfarma, S.A. | Nuevos derivados de piridazin-3(2h)-ona. |
| AR063706A1 (es) * | 2006-09-11 | 2009-02-11 | Cgi Pharmaceuticals Inc | Determinadas amidas sustituidas, el uso de las mismas para el tratamiento de enfermedades mediadas por la inhibicion de la actividad de btk y composiciones farmaceuticas que las comprenden. |
| CL2008002793A1 (es) * | 2007-09-20 | 2009-09-04 | Cgi Pharmaceuticals Inc | Compuestos derivados de amidas sustituidas, inhibidores de la actividad de btk; composicion farmaceutica que los comprende; utiles en el tratamiento del cancer, trastornos oseos, enfermedades autoinmunes, entre otras |
| EP2196465A1 (en) | 2008-12-15 | 2010-06-16 | Almirall, S.A. | (3-oxo)pyridazin-4-ylurea derivatives as PDE4 inhibitors |
| WO2013142390A1 (en) * | 2012-03-21 | 2013-09-26 | Gtx, Inc. | Aldo-keto reductase subfamily 1c3 (akr1c3) inhibitors |
| WO2014201173A1 (en) * | 2013-06-12 | 2014-12-18 | Amgen Inc. | Bicyclic sulfonamide compounds as sodium channel inhibitors |
| EP3010918B1 (en) | 2013-06-21 | 2018-08-15 | Zenith Epigenetics Ltd. | Novel substituted bicyclic compounds as bromodomain inhibitors |
| CN103396774B (zh) | 2013-08-09 | 2017-09-19 | 西南石油大学 | 堵漏剂及其制备方法 |
| EP3290407B1 (en) * | 2013-10-18 | 2020-01-01 | Celgene Quanticel Research, Inc | Bromodomain inhibitors |
| WO2015081246A1 (en) | 2013-11-26 | 2015-06-04 | Incyte Corporation | Bicyclic heterocycles as bet protein inhibitors |
| US9399640B2 (en) * | 2013-11-26 | 2016-07-26 | Incyte Corporation | Substituted pyrrolo[2,3-c]pyridines and pyrazolo[3,4-c]pyridines as BET protein inhibitors |
| MA40940A (fr) | 2014-11-10 | 2017-09-19 | Constellation Pharmaceuticals Inc | Pyrrolopyridines substituées utilisées en tant qu'inhibiteurs de bromodomaines |
| MA40943A (fr) * | 2014-11-10 | 2017-09-19 | Constellation Pharmaceuticals Inc | Pyrrolopyridines substituées utilisées en tant qu'inhibiteurs de bromodomaines |
-
2016
- 2016-03-04 EP EP16708994.5A patent/EP3265453B1/en active Active
- 2016-03-04 WO PCT/EP2016/054713 patent/WO2016139361A1/en not_active Ceased
- 2016-03-04 JP JP2017546629A patent/JP6857606B2/ja active Active
- 2016-03-04 US US15/554,440 patent/US11319318B2/en active Active
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