CN115708410A - 靶向降解Btk的化合物及其抗肿瘤用途 - Google Patents
靶向降解Btk的化合物及其抗肿瘤用途 Download PDFInfo
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- CN115708410A CN115708410A CN202180040932.7A CN202180040932A CN115708410A CN 115708410 A CN115708410 A CN 115708410A CN 202180040932 A CN202180040932 A CN 202180040932A CN 115708410 A CN115708410 A CN 115708410A
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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- A—HUMAN NECESSITIES
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Abstract
本发明提供了靶向降解Btk的化合物及其抗肿瘤用途，具体地，本发明制备并筛选了一系列的化合物，并验证了这些化合物对布鲁顿酪氨酸蛋白激酶(Btk)抑制和降解活性，最终发现了具备良好成药性的化合物，可以用于治疗与布鲁顿酪氨酸蛋白激酶(Btk)活性或表达量相关的疾病。
Description
PCT国内申请，说明书已公开。
Claims (10)
- PCT国内申请，权利要求书已公开。
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN202011160099.3A CN114478532A (zh) | 2020-10-26 | 2020-10-26 | 靶向降解Btk的化合物及其抗肿瘤用途 |
| CN2020111600993 | 2020-10-26 | ||
| PCT/CN2021/126315 WO2022089400A1 (zh) | 2020-10-26 | 2021-10-26 | 靶向降解Btk的化合物及其抗肿瘤用途 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN115708410A true CN115708410A (zh) | 2023-02-21 |
| CN115708410B CN115708410B (zh) | 2023-05-23 |
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| CN202011160099.3A Pending CN114478532A (zh) | 2020-10-26 | 2020-10-26 | 靶向降解Btk的化合物及其抗肿瘤用途 |
| CN202180040932.7A Active CN115708410B (zh) | 2020-10-26 | 2021-10-26 | 靶向降解Btk的化合物及其抗肿瘤用途 |
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| CN202011160099.3A Pending CN114478532A (zh) | 2020-10-26 | 2020-10-26 | 靶向降解Btk的化合物及其抗肿瘤用途 |
Country Status (3)
| Country | Link |
|---|---|
| US (1) | US20240002389A1 (zh) |
| CN (2) | CN114478532A (zh) |
| WO (1) | WO2022089400A1 (zh) |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CN115611902A (zh) * | 2021-07-15 | 2023-01-17 | 标新生物医药科技(上海)有限公司 | 基于布鲁顿酪氨酸激酶配体设计的蛋白降解化合物及其应用 |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2019177902A1 (en) * | 2018-03-10 | 2019-09-19 | Yale University | Modulators of btk proteolysis and methods of use |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2017117473A1 (en) * | 2015-12-30 | 2017-07-06 | Dana-Farber Cancer Institute, Inc. | Bifunctional molescules for her3 degradation and methods of use |
| 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 |
| CN109422753B (zh) * | 2017-09-03 | 2021-12-31 | 上海美志医药科技有限公司 | 一类具有抑制并降解酪氨酸蛋白激酶jak1或jak2活性的化合物 |
| CN109422751B (zh) * | 2017-09-03 | 2022-04-22 | 上海美志医药科技有限公司 | 一类具有降解酪氨酸蛋白激酶jak3活性的化合物 |
| CN109422752B (zh) * | 2017-09-03 | 2023-04-07 | 上海美志医药科技有限公司 | 一类具有抑制并降解布鲁顿酪氨酸蛋白激酶Btk活性的化合物 |
| CN109422733A (zh) * | 2017-09-03 | 2019-03-05 | 上海美志医药科技有限公司 | 一类抑制并降解酪氨酸蛋白激酶alk的化合物 |
| WO2019127008A1 (zh) * | 2017-12-26 | 2019-07-04 | 清华大学 | 一种靶向降解btk的化合物及其应用 |
| CA3085457C (en) * | 2018-01-29 | 2023-05-23 | Dana-Farber Cancer Institute, Inc. | Degradation of bruton's tyrosine kinase (btk) by conjugation of btk inhibitors with e3 ligase ligand and methods of use |
| CN111662294A (zh) * | 2019-03-05 | 2020-09-15 | 上海美志医药科技有限公司 | 一类具有降解Btk活性的化合物 |
-
2020
- 2020-10-26 CN CN202011160099.3A patent/CN114478532A/zh active Pending
-
2021
- 2021-10-26 WO PCT/CN2021/126315 patent/WO2022089400A1/zh active Application Filing
- 2021-10-26 US US18/250,477 patent/US20240002389A1/en active Pending
- 2021-10-26 CN CN202180040932.7A patent/CN115708410B/zh active Active
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2019177902A1 (en) * | 2018-03-10 | 2019-09-19 | Yale University | Modulators of btk proteolysis and methods of use |
Non-Patent Citations (1)
| Title |
|---|
| SAUL JAIME-FIGUEROA A等: "Design,Synthesisi and Biological Evaluation of Proteolysis Targeting Chimeras", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS * |
Also Published As
| Publication number | Publication date |
|---|---|
| US20240002389A1 (en) | 2024-01-04 |
| CN114478532A (zh) | 2022-05-13 |
| CN115708410B (zh) | 2023-05-23 |
| WO2022089400A1 (zh) | 2022-05-05 |
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