JPWO2020227325A5 - - Google Patents
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- JPWO2020227325A5 JPWO2020227325A5 JP2021565854A JP2021565854A JPWO2020227325A5 JP WO2020227325 A5 JPWO2020227325 A5 JP WO2020227325A5 JP 2021565854 A JP2021565854 A JP 2021565854A JP 2021565854 A JP2021565854 A JP 2021565854A JP WO2020227325 A5 JPWO2020227325 A5 JP WO2020227325A5
- Authority
- JP
- Japan
- Prior art keywords
- amino
- oxoindolin
- dioxopiperidin
- dioxoisoindolin
- ylidene
- 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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- QORWEDPACXFHBR-SLMZUGIISA-N CC1=C(NC(=C1C(=O)NCCCN2CCN(CC2)C(=O)CCCCNC3=CC=CC4=C3C(=O)N(C4=O)C5CCC(=O)NC5=O)C)/C=C\6/C7=C(C=CC(=C7)F)NC6=O Chemical compound CC1=C(NC(=C1C(=O)NCCCN2CCN(CC2)C(=O)CCCCNC3=CC=CC4=C3C(=O)N(C4=O)C5CCC(=O)NC5=O)C)/C=C\6/C7=C(C=CC(=C7)F)NC6=O QORWEDPACXFHBR-SLMZUGIISA-N 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 1
Claims (1)
ｈ． （Ｚ）－Ｎ－（３－（４－（２－（（５－（（２－（２，６－ジオキソピペリジン－３－イル）－１，３－ジオキソイソインドリン－４－イル）アミノ）ペンチル）アミノ）－２－オキソエチル）ピペラジン－１－イル）プロピル）－５－（（５－フルオロ－２－オキソインドリン－３－イリデン）メチル）－２，４－ジメチル－１Ｈ－ピロール－３－カルボキサミド（ＨＣ５８－７５）；
ｉ． （Ｚ）－Ｎ－（３－（４－（２－（（６－（（２－（２，６－ジオキソピペリジン－３－イル）－１，３－ジオキソイソインドリン－４－イル）アミノ）ヘキシル）アミノ）－２－オキソエチル）ピペラジン－１－イル）プロピル）－５－（（５－フルオロ－２－オキソインドリン－３－イリデン）メチル）－２，４－ジメチル－１Ｈ－ピロール－３－カルボキサミド（ＨＣ５８－７６）；および
ｊ． （Ｚ）－Ｎ－（３－（４－（２－（（８－（（２－（２，６－ジオキソピペリジン－３－イル）－１，３－ジオキソイソインドリン－４－イル）アミノ）オクチル）アミノ）－２－オキソエチル）ピペラジン－１－イル）プロピル）－５－（（５－フルオロ－２－オキソインドリン－３－イリデン）メチル）－２，４－ジメチル－１Ｈ－ピロール－３－カルボキサミド（ＨＣ５８－７８）、
ならびにその薬学的に許容される塩、からなる群から選択される化合物。
g. (Z)-N-(3-(4-(5-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)pentanoyl) Piperazin-1-yl)propyl)-5-((5-fluoro-2-oxoindolin-3-ylidene)methyl)-2,4-dimethyl-1H-pyrrole-3-carboxamide (HC58-38);
h. (Z)-N-(3-(4-(2-((5-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl) amino)pentyl)amino)-2-oxoethyl)piperazin-1-yl)propyl)-5-((5-fluoro-2-oxoindolin-3-ylidene)methyl)-2,4-dimethyl-1H-pyrrole- 3-carboxamide (HC58-75);
i. (Z)-N-(3-(4-(2-((6-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl) amino)hexyl)amino)-2-oxoethyl)piperazin-1-yl)propyl)-5-((5-fluoro-2-oxoindolin-3-ylidene)methyl)-2,4-dimethyl-1H-pyrrole- 3-carboxamide (HC58-76); and j. (Z)-N-(3-(4-(2-((8-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl) amino)octyl)amino)-2-oxoethyl)piperazin-1-yl)propyl)-5-((5-fluoro-2-oxoindolin-3-ylidene)methyl)-2,4-dimethyl-1H-pyrrole- 3-carboxamide (HC58-78),
and pharmaceutically acceptable salts thereof.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962843816P | 2019-05-06 | 2019-05-06 | |
| US62/843,816 | 2019-05-06 | ||
| PCT/US2020/031527 WO2020227325A1 (en) | 2019-05-06 | 2020-05-05 | Heterobifunctional compounds as degraders of hpk1 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2022531446A JP2022531446A (en) | 2022-07-06 |
| JPWO2020227325A5 true JPWO2020227325A5 (en) | 2023-05-15 |
| JP7503851B2 JP7503851B2 (en) | 2024-06-21 |
Family
ID=73051660
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021565854A Active JP7503851B2 (en) | 2019-05-06 | 2020-05-05 | Heterobifunctional compounds as degraders of HPK1 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US20230022524A1 (en) |
| EP (1) | EP3965824A4 (en) |
| JP (1) | JP7503851B2 (en) |
| CN (1) | CN114423463A (en) |
| CA (1) | CA3137916A1 (en) |
| WO (1) | WO2020227325A1 (en) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11071730B2 (en) | 2018-10-31 | 2021-07-27 | Gilead Sciences, Inc. | Substituted 6-azabenzimidazole compounds |
| LT3873903T (en) | 2018-10-31 | 2024-05-10 | Gilead Sciences, Inc. | Substituted 6-azabenzimidazole compounds as hpk1 inhibitors |
| EP3972695A1 (en) | 2019-05-23 | 2022-03-30 | Gilead Sciences, Inc. | Substituted exo-methylene-oxindoles which are hpk1/map4k1 inhibitors |
| TW202208381A (en) * | 2020-05-06 | 2022-03-01 | 美商紐力克斯醫療股份有限公司 | Bifunctional degraders of hematopoietic progenitor kinase and therapeutic uses thereof |
| AU2022207648A1 (en) | 2021-01-13 | 2023-07-27 | Monte Rosa Therapeutics Ag | Isoindolinone compounds |
| WO2022199652A1 (en) * | 2021-03-24 | 2022-09-29 | Impact Therapeutics (Shanghai) , Inc | Five-membered heteroaryl-pyrimidine compounds as usp1 inhibitors and the use thereof |
| CN117693503A (en) | 2021-07-20 | 2024-03-12 | 阿斯利康(瑞典)有限公司 | Substituted pyrazine-2-carboxamides as HPK1 inhibitors for the treatment of cancer |
| WO2023006063A1 (en) * | 2021-07-30 | 2023-02-02 | Beigene, Ltd. | PYRROLO [2, 3-b] PYRAZINE-BASED BIFUNCTIONAL COMPOUNDS AS HPK1 DEGRADERS AND THE USE THEREOF |
| WO2023023941A1 (en) * | 2021-08-24 | 2023-03-02 | Biofront Ltd (Cayman) | Hpk1 degraders, compositions comprising the hpki degrader, and methods of using the same |
| AU2022388571A1 (en) * | 2021-11-10 | 2024-05-09 | Gilead Sciences, Inc. | Bifunctional degraders of hematopoietic progenitor kinase and therapeutic uses thereof |
| AU2022398484A1 (en) * | 2021-11-23 | 2024-06-13 | Cullinan Oncology, Inc. | Heterobifunctional compounds as hpk1 degraders |
| WO2023151559A1 (en) * | 2022-02-08 | 2023-08-17 | 和径医药科技（上海）有限公司 | Heterocyclic compound, pharmaceutical composition containing same, and anti-tumor use thereof |
| WO2024017372A1 (en) * | 2022-07-22 | 2024-01-25 | 成都百裕制药股份有限公司 | Indolone derivative and use thereof |
| WO2024027755A1 (en) * | 2022-08-05 | 2024-02-08 | 杭州中美华东制药有限公司 | Protac chimeric compound, preparation method therefor and use thereof |
| CN118206559A (en) * | 2022-12-16 | 2024-06-18 | 杭州中美华东制药有限公司 | PROTAC chimeric compounds, preparation method and use thereof |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CZ303705B6 (en) | 2000-02-15 | 2013-03-27 | Sugen, Inc. | Pyrrole substituted 2-indolinone compound for use as protein kinase inhibitor and pharmaceutical composition containing thereof |
| US9938264B2 (en) | 2015-11-02 | 2018-04-10 | Yale University | Proteolysis targeting chimera compounds and methods of preparing and using same |
| EP3454856A4 (en) | 2016-05-10 | 2019-12-25 | C4 Therapeutics, Inc. | Heterocyclic degronimers for target protein degradation |
| TW201811799A (en) | 2016-09-09 | 2018-04-01 | 美商英塞特公司 | Pyrazolopyrimidine compounds and uses thereof |
| AR109596A1 (en) * | 2016-09-09 | 2018-12-26 | Incyte Corp | PIRAZOLOPIRIDINE COMPOUNDS AND THEIR USES |
| WO2018098280A1 (en) * | 2016-11-22 | 2018-05-31 | Dana-Farber Cancer Institute, Inc. | Degradation of protein kinases by conjugation of protein kinase inhibitors with e3 ligase ligand and methods of use |
| CN110267659A (en) | 2016-12-08 | 2019-09-20 | 西奈山伊坎医学院 | For treating the composition and method of the cancer of CDK4/6 mediation |
| AU2018215212B2 (en) | 2017-01-31 | 2022-06-02 | Arvinas Operations, Inc. | Cereblon ligands and bifunctional compounds comprising the same |
| WO2019084030A1 (en) | 2017-10-24 | 2019-05-02 | Genentech, Inc. | (4-hydroxypyrrolidin-2-yl)-hydroxamate compounds and methods of use thereof |
| JP7385284B2 (en) | 2018-01-22 | 2023-11-22 | バイオベンチャーズ・リミテッド・ライアビリティ・カンパニー | BCL-2 proteolytic agents for cancer treatment |
| CN112154146A (en) | 2018-03-06 | 2020-12-29 | 西奈山伊坎医学院 | Serine threonine kinase (AKT) degradation/disruption compounds and methods of use |
-
2020
- 2020-05-05 CA CA3137916A patent/CA3137916A1/en active Pending
- 2020-05-05 CN CN202080049386.9A patent/CN114423463A/en active Pending
- 2020-05-05 EP EP20802303.6A patent/EP3965824A4/en active Pending
- 2020-05-05 US US17/604,636 patent/US20230022524A1/en active Pending
- 2020-05-05 WO PCT/US2020/031527 patent/WO2020227325A1/en unknown
- 2020-05-05 JP JP2021565854A patent/JP7503851B2/en active Active
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