JPWO2021053495A5 - - Google Patents
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- Publication number
- JPWO2021053495A5 JPWO2021053495A5 JP2022516375A JP2022516375A JPWO2021053495A5 JP WO2021053495 A5 JPWO2021053495 A5 JP WO2021053495A5 JP 2022516375 A JP2022516375 A JP 2022516375A JP 2022516375 A JP2022516375 A JP 2022516375A JP WO2021053495 A5 JPWO2021053495 A5 JP WO2021053495A5
- Authority
- JP
- Japan
- Prior art keywords
- ligase
- targeting
- binding
- formula
- group capable
- 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.)
- Pending
Links
Claims (1)
- 式（Ｉ）：
（式中、
前記標的化リガンドは、標的タンパク質に結合できる基であり；
前記リンカーは、前記標的化リガンドを前記標的化リガーゼバインダーに共有結合的に連結する基であり；及び
前記標的化リガーゼバインダーは、リガーゼ（例えば、セレブロンＥ３ユビキチンリガーゼ）に結合できる基である）
の二機能性化合物、又はその薬学的に許容される塩、水和物、溶媒和物、プロドラッグ、立体異性体、若しくは互変異性体。
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962901161P | 2019-09-16 | 2019-09-16 | |
| US62/901,161 | 2019-09-16 | ||
| US201962905849P | 2019-09-25 | 2019-09-25 | |
| US62/905,849 | 2019-09-25 | ||
| PCT/IB2020/058535 WO2021053495A1 (en) | 2019-09-16 | 2020-09-14 | Bifunctional degraders and their methods of use |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2022547716A JP2022547716A (ja) | 2022-11-15 |
| JPWO2021053495A5 true JPWO2021053495A5 (ja) | 2023-09-22 |
Family
ID=72603497
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022516375A Pending JP2022547716A (ja) | 2019-09-16 | 2020-09-14 | 二機能性分解誘導薬及びそれらの使用方法 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US20220387602A1 (ja) |
| EP (1) | EP4031247A1 (ja) |
| JP (1) | JP2022547716A (ja) |
| CN (1) | CN114521196A (ja) |
| WO (1) | WO2021053495A1 (ja) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX2022010952A (es) | 2020-03-05 | 2022-10-07 | C4 Therapeutics Inc | Compuestos para la degradacion dirigida de brd9. |
| WO2022143856A1 (en) * | 2020-12-31 | 2022-07-07 | Beigene, Ltd. | Degradation of bruton's tyrosine kinase (btk) by conjugation of btk inhibitors with e3 ligase ligand and methods of use |
| WO2022189859A1 (en) * | 2021-03-12 | 2022-09-15 | Novartis Ag | Fatty acid-bifunctional degrader conjugates and their methods of use |
| EP4334302A1 (en) * | 2021-05-03 | 2024-03-13 | Nurix Therapeutics, Inc. | Compounds for inhibiting or degrading target proteins, compositions, comprising the same, methods of their making, and methods of their use |
| AR125768A1 (es) * | 2021-05-05 | 2023-08-09 | Biogen Ma Inc | Compuestos para la degradación dirigida de la tirosina cinasa de bruton |
| WO2023031801A1 (en) | 2021-09-01 | 2023-03-09 | Novartis Ag | Bifunctional degraders comprising a tead binder |
| WO2023115150A1 (en) * | 2021-12-22 | 2023-06-29 | Anaxis Pharma Pty Ltd | Bifunctional arylsulphonamide compounds |
| WO2023125908A1 (en) * | 2021-12-30 | 2023-07-06 | Beigene, Ltd. | Degradation of bruton's tyrosine kinase (btk) by conjugation of btk inhibitors with e3 ligase ligand and methods of use |
| WO2024020221A1 (en) * | 2022-07-21 | 2024-01-25 | Arvinas Operations, Inc. | Modulators of tyk2 proteolysis and associated methods of use |
| WO2024043319A1 (ja) * | 2022-08-26 | 2024-02-29 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | 抗体薬物複合体 |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5141943A (en) * | 1990-04-12 | 1992-08-25 | Brown University Research Foundation | 5-benzyl barbiturate derivatives |
| KR101736521B1 (ko) | 2009-11-03 | 2017-05-16 | 글락소스미스클라인 엘엘씨 | 퀴나졸린 화합물 |
| WO2013157021A1 (en) * | 2012-04-20 | 2013-10-24 | Advinus Therapeutics Limited | Bicyclic compounds, compositions and medicinal applications thereof |
| EP3445760B1 (en) * | 2016-04-22 | 2022-02-23 | Dana-Farber Cancer Institute, Inc. | Degradation of cyclin-dependent kinase 9 (cdk9) by conjugation of cdk9 inhibitors with e3 ligase ligand and methods of use |
| CA3020543A1 (en) * | 2016-04-22 | 2017-10-26 | Dana-Farber Cancer Institute, Inc. | Degradation of cyclin-dependent kinase 8 (cdk8) by conjugation of cdk8 inhibitors with e3 ligase ligand and methods of use |
| CN109071552B (zh) * | 2016-04-22 | 2022-06-03 | 达纳－法伯癌症研究所公司 | 细胞周期蛋白依赖性激酶4/6(cdk4/6)通过cdk4/6抑制剂与e3连接酶配体的缀合的降解及使用方法 |
| AU2017281903B2 (en) * | 2016-06-23 | 2020-12-24 | Dana-Farber Cancer Institute, Inc. | Degradation of bromodomain-containing protein 9 (BRD9) by conjugation of BRD9 inhibitors with E3 ligase ligand and methods of use |
| DK3660004T3 (da) * | 2016-10-11 | 2023-05-08 | Arvinas Operations Inc | Forbindelser og fremgangsmåder til målrettet degradering af androgenreceptor |
| KR20190080956A (ko) * | 2016-11-22 | 2019-07-08 | 다나-파버 캔서 인스티튜트 인크. | Ｅ3 리가아제 리간드와 브루톤 티로신 키나아제(ｂｔｋ) 억제제의 컨쥬게이션에 의한 ｂｔｋ의 분해 및 사용 방법 |
| EP3652329B1 (en) * | 2017-07-12 | 2023-10-04 | Dana-Farber Cancer Institute, Inc. | Compounds for tau protein degradation |
| CN109518406B (zh) | 2017-09-18 | 2021-11-16 | 青岛海尔洗涤电器有限公司 | 一种衣物洗干一体机及其控制方法 |
| WO2019140387A1 (en) * | 2018-01-12 | 2019-07-18 | Kymera Therapeutics, Inc. | Crbn ligands and uses thereof |
| CN111936498B (zh) * | 2018-03-26 | 2024-04-16 | 诺华股份有限公司 | N-(3-(7H-吡咯并[2,3-d]嘧啶-4-基)苯基)苯甲酰胺衍生物 |
| CN117186108A (zh) * | 2018-03-26 | 2023-12-08 | 诺华股份有限公司 | 布鲁顿酪氨酸激酶降解剂 |
| EP3897631A4 (en) * | 2018-12-20 | 2022-11-23 | C4 Therapeutics, Inc. | TARGETED PROTEIN DEGRADATION |
| US20220281876A1 (en) * | 2019-07-26 | 2022-09-08 | Beigene, Ltd. | Degradation of bruton's tyrosine kinase (btk) by conjugation of btk inhibitors with e3 ligase ligand and methods of use |
-
2020
- 2020-09-14 EP EP20775721.2A patent/EP4031247A1/en active Pending
- 2020-09-14 US US17/642,285 patent/US20220387602A1/en active Pending
- 2020-09-14 CN CN202080064750.9A patent/CN114521196A/zh active Pending
- 2020-09-14 WO PCT/IB2020/058535 patent/WO2021053495A1/en unknown
- 2020-09-14 JP JP2022516375A patent/JP2022547716A/ja active Pending
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