JP2019514882A5 - - Google Patents
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- JP2019514882A5 JP2019514882A5 JP2018555278A JP2018555278A JP2019514882A5 JP 2019514882 A5 JP2019514882 A5 JP 2019514882A5 JP 2018555278 A JP2018555278 A JP 2018555278A JP 2018555278 A JP2018555278 A JP 2018555278A JP 2019514882 A5 JP2019514882 A5 JP 2019514882A5
- Authority
- JP
- Japan
- Prior art keywords
- cancer
- alkyl
- disease
- formula
- linker
- 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.)
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- 0 CC(Bc1c(*)nc(*C2CC*(C)CC2)[s]1)c1nc(*)c(*)[o]1 Chemical compound CC(Bc1c(*)nc(*C2CC*(C)CC2)[s]1)c1nc(*)c(*)[o]1 0.000 description 8
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662326581P | 2016-04-22 | 2016-04-22 | |
| US62/326,581 | 2016-04-22 | ||
| PCT/US2017/028924 WO2017185023A1 (en) | 2016-04-22 | 2017-04-21 | Degradation of cyclin-dependent kinase 9 (cdk9) by conjugation of cdk9 inhibitors with e3 ligase ligand and methods of use |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019514882A JP2019514882A (ja) | 2019-06-06 |
| JP2019514882A5 true JP2019514882A5 (enExample) | 2020-05-07 |
| JP6927999B2 JP6927999B2 (ja) | 2021-09-01 |
Family
ID=60117046
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018555278A Active JP6927999B2 (ja) | 2016-04-22 | 2017-04-21 | サイクリン依存性キナーゼ９（ｃｄｋ９）阻害剤のｅ３リガーゼリガンドとのコンジュゲーションによるｃｄｋ９の分解および使用法 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US10532103B2 (enExample) |
| EP (1) | EP3445760B1 (enExample) |
| JP (1) | JP6927999B2 (enExample) |
| CN (1) | CN109153675B (enExample) |
| AU (1) | AU2017254702B2 (enExample) |
| WO (1) | WO2017185023A1 (enExample) |
Families Citing this family (38)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11883381B2 (en) | 2016-05-12 | 2024-01-30 | The Regents Of The University Of Michigan | ASH1L inhibitors and methods of treatment therewith |
| US11173211B2 (en) | 2016-12-23 | 2021-11-16 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides |
| US10513515B2 (en) | 2017-08-25 | 2019-12-24 | Biotheryx, Inc. | Ether compounds and uses thereof |
| WO2019094772A1 (en) | 2017-11-10 | 2019-05-16 | The Regents Of The University Of Michigan | Ash1l degraders and methods of treatment therewith |
| US20200377477A1 (en) * | 2018-02-20 | 2020-12-03 | Dana-Farber Cancer Institute, Inc. | Degraders of egfr and methods of use thereof |
| JP2021514012A (ja) * | 2018-02-20 | 2021-06-03 | デイナ ファーバー キャンサー インスティチュート，インコーポレイテッド | Ｅｇｆｒの分解誘導剤およびその使用法 |
| JP2021514400A (ja) * | 2018-02-20 | 2021-06-10 | デイナ ファーバー キャンサー インスティチュート，インコーポレイテッド | Ｅｇｆｒの阻害剤およびその使用法 |
| CN118754858A (zh) | 2018-03-26 | 2024-10-11 | 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 |
| US12539292B2 (en) | 2018-04-01 | 2026-02-03 | Arvinas Operations, Inc. | BRM targeting compounds and associated methods of use |
| CA3106239A1 (en) * | 2018-07-27 | 2020-01-30 | Biotheryx, Inc. | Bifunctional compounds as cdk modulators |
| US11707452B2 (en) | 2018-08-20 | 2023-07-25 | Arvinas Operations, Inc. | Modulators of alpha-synuclein proteolysis and associated methods of use |
| US12186400B2 (en) | 2018-11-09 | 2025-01-07 | Yipeng Wang | Micromolecular compound specifically degrading tau protein, and application thereof |
| CN113423701A (zh) | 2018-11-13 | 2021-09-21 | 拜欧斯瑞克斯公司 | 取代的异吲哚啉酮 |
| WO2020173440A1 (en) * | 2019-02-27 | 2020-09-03 | Cullgen (Shanghai), Inc. | Cyclic-amp response element binding protein (cbp) and/or adenoviral e1a binding protein of 300 kda (p300) degradation compounds and methods of use |
| CA3133314A1 (en) | 2019-03-21 | 2020-09-24 | Codiak Biosciences, Inc. | Extracellular vesicle conjugates and uses thereof |
| US12233356B2 (en) | 2019-03-21 | 2025-02-25 | Lonza Sales Ag | Process for preparing extracellular vesicles |
| EP3947368B1 (en) * | 2019-04-04 | 2025-09-03 | Dana-Farber Cancer Institute, Inc. | Bifunctional compounds comprising a cdk2/5 ligand, a linker and a e3 ubiquitin ligase binding degron for the treatment of cancer |
| AU2020263390B2 (en) * | 2019-04-23 | 2026-01-08 | Dana-Farber Cancer Institute, Inc. | Degraders of cyclin-dependent kinase 12 (CDK12) and uses thereof |
| WO2021011913A1 (en) | 2019-07-17 | 2021-01-21 | Arvinas Operations, Inc. | Tau-protein targeting compounds and associated methods of use |
| US12491251B2 (en) | 2019-08-05 | 2025-12-09 | Dana-Farber Cancer Institute, Inc. | Degraders of cyclin-dependent kinase 7 (CDK7) and uses thereof |
| CN114521196A (zh) * | 2019-09-16 | 2022-05-20 | 诺华股份有限公司 | 双官能团降解剂及其使用方法 |
| US12310975B2 (en) | 2019-10-17 | 2025-05-27 | Arvinas Operations, Inc. | Modulators of BCL6 proteolysis and associated methods of use |
| US20230158159A1 (en) * | 2020-04-24 | 2023-05-25 | Massachusetts Institute Of Technology | Chimeric degraders of cyclin-dependent kinase 9 and uses thereof |
| WO2021222150A2 (en) | 2020-04-28 | 2021-11-04 | Anwita Biosciences, Inc. | Interleukin-2 polypeptides and fusion proteins thereof, and their pharmaceutical compositions and therapeutic applications |
| WO2021237100A1 (en) | 2020-05-21 | 2021-11-25 | Codiak Biosciences, Inc. | Methods of targeting extracellular vesicles to lung |
| CN116507333B (zh) * | 2020-08-27 | 2025-05-09 | 上海睿跃生物科技有限公司 | 环amp反应元件结合蛋白(cbp)和/或300kda腺病毒e1a结合蛋白(p300)降解化合物和使用方法 |
| EP4204418A1 (en) | 2020-08-28 | 2023-07-05 | Arvinas Operations, Inc. | Rapidly accelerating fibrosarcoma protein degrading compounds and associated methods of use |
| WO2022051616A1 (en) * | 2020-09-03 | 2022-03-10 | Board Of Regents Of The University Of Nebraska | Cdk targeted heterobifunctional small molecule proteolysis targeting chimeras |
| US20240241020A1 (en) | 2020-09-23 | 2024-07-18 | Lonza Sales Ag | Process for preparing extracellular vesicles |
| CN114349738B (zh) * | 2020-10-14 | 2023-05-05 | 清华大学 | 一类靶向降解cdk2的小分子缀合物及其应用 |
| JP7814386B2 (ja) * | 2020-11-05 | 2026-02-16 | クロノス バイオ インコーポレイテッド | Ｃｄｋ９活性を調節するための化合物および方法 |
| CA3214806A1 (en) | 2021-04-16 | 2022-10-20 | Arvinas Operations, Inc. | Modulators of bcl6 proteolysis and associated methods of use |
| US20240376096A1 (en) * | 2021-07-16 | 2024-11-14 | Dana-Farber Cancer Institute, Inc. | Small molecule cyclin dependent kinase 4/6 (cdk4/6) and ikzf2 (helios) degraders and methods of use thereof |
| WO2023030453A1 (zh) * | 2021-09-01 | 2023-03-09 | 四川海思科制药有限公司 | 一种降解Bcl-2家族蛋白的化合物及其在医药上的应用 |
| US12084453B2 (en) | 2021-12-10 | 2024-09-10 | Incyte Corporation | Bicyclic amines as CDK12 inhibitors |
| EP4584258A1 (en) | 2022-09-07 | 2025-07-16 | Arvinas Operations, Inc. | Rapidly accelerated fibrosarcoma (raf) degrading compounds and associated methods of use |
| EP4428133A1 (en) * | 2023-03-07 | 2024-09-11 | Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. | Bifunctional protein targeting chimeras (protacs) comprising arylidene-indolinone scaffold as dcaf11 ligand and use thereof |
| WO2025137613A1 (en) * | 2023-12-22 | 2025-06-26 | Ganymede Oncology, Inc. | Cycloalkylene nrf2 protein degraders |
Family Cites Families (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20080221132A1 (en) * | 2006-09-11 | 2008-09-11 | Xiong Cai | Multi-Functional Small Molecules as Anti-Proliferative Agents |
| WO2008049856A2 (en) * | 2006-10-25 | 2008-05-02 | Ingenium Pharmaceuticals Gmbh | Methods of treating pain using cdk inhibitors |
| TW200922564A (en) * | 2007-09-10 | 2009-06-01 | Curis Inc | CDK inhibitors containing a zinc binding moiety |
| JP2015508414A (ja) * | 2012-01-12 | 2015-03-19 | イエール ユニバーシティ | Ｅ３ユビキチンリガーゼによる標的タンパク質および他のポリペプチドの分解増強のための化合物および方法 |
| GB201311888D0 (en) * | 2013-07-03 | 2013-08-14 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| EP3805218A1 (en) * | 2014-04-05 | 2021-04-14 | Syros Pharmaceuticals, Inc. | Inhibitors of cyclin-dependent kinase 7 (cdk7) |
| CN119591582A (zh) * | 2014-04-14 | 2025-03-11 | 阿尔维纳斯运营股份有限公司 | 基于酰亚胺的蛋白水解调节剂和相关使用方法 |
| US10071164B2 (en) * | 2014-08-11 | 2018-09-11 | Yale University | Estrogen-related receptor alpha based protac compounds and associated methods of use |
| JP6815318B2 (ja) * | 2014-12-23 | 2021-01-20 | 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 | 二官能性分子によって標的化タンパク質分解を誘導する方法 |
| KR20240119196A (ko) * | 2015-06-04 | 2024-08-06 | 아비나스 오퍼레이션스, 인코포레이티드 | 단백질분해의 이미드계 조절인자 및 관련된 이용 방법 |
| WO2017007612A1 (en) * | 2015-07-07 | 2017-01-12 | Dana-Farber Cancer Institute, Inc. | Methods to induce targeted protein degradation through bifunctional molecules |
| JP7028766B2 (ja) * | 2015-09-09 | 2022-03-02 | 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 | サイクリン依存性キナーゼの阻害剤 |
| GB201516243D0 (en) * | 2015-09-14 | 2015-10-28 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| AU2016349781A1 (en) * | 2015-11-02 | 2018-05-10 | Yale University | Proteolysis targeting chimera compounds and methods of preparing and using same |
| WO2017117473A1 (en) * | 2015-12-30 | 2017-07-06 | Dana-Farber Cancer Institute, Inc. | Bifunctional molescules for her3 degradation and methods of use |
| WO2017117474A1 (en) * | 2015-12-30 | 2017-07-06 | Dana-Farber Cancer Institute, Inc. | Bifunctional compounds for her3 degradation and methods of use |
| JP6921114B2 (ja) * | 2016-04-22 | 2021-08-18 | デイナ ファーバー キャンサー インスティチュート，インコーポレイテッド | サイクリン依存性キナーゼ８（ｃｄｋ８）阻害剤のｅ３リガーゼリガンドとのコンジュゲーションによるｃｄｋ８の分解および使用法 |
| WO2017185031A1 (en) * | 2016-04-22 | 2017-10-26 | Dana-Farber Cancer Institute, Inc. | Degradation of cyclin-dependent kinase 4/6 (cdk4/6) by conjugation of cdk4/6 inhibitors with e3 ligase ligand and methods of use |
| EP3892272B1 (en) * | 2016-04-22 | 2024-07-24 | Dana-Farber Cancer Institute, Inc. | Bifunctional molecules for degradation of egfr and methods of use |
| CN109562107A (zh) * | 2016-05-10 | 2019-04-02 | C4医药公司 | 用于靶蛋白降解的杂环降解决定子体 |
| EP4483875A3 (en) * | 2016-05-10 | 2025-04-02 | C4 Therapeutics, Inc. | Spirocyclic degronimers for target protein degradation |
| EP3455219A4 (en) * | 2016-05-10 | 2019-12-18 | C4 Therapeutics, Inc. | AMINE-RELATED C3-GLUTARIMIDE DEGRONIMERS FOR TARGET PROTEIN REDUCTION |
| CN109641874A (zh) * | 2016-05-10 | 2019-04-16 | C4医药公司 | 用于靶蛋白降解的c3-碳连接的戊二酰亚胺降解决定子体 |
| CA3025805A1 (en) * | 2016-06-23 | 2017-12-28 | James Bradner | Degradation of tripartite motif-containing protein 24 (trim24) by conjugation of trim24 inhibitors with e3 ligase ligand and methods of use |
| WO2018064589A1 (en) * | 2016-09-29 | 2018-04-05 | Dana-Farber Cancer Institute, Inc. | Targeted protein degradation using a mutant e3 ubiquitin ligase |
-
2017
- 2017-04-21 AU AU2017254702A patent/AU2017254702B2/en active Active
- 2017-04-21 EP EP17786750.4A patent/EP3445760B1/en active Active
- 2017-04-21 WO PCT/US2017/028924 patent/WO2017185023A1/en not_active Ceased
- 2017-04-21 US US16/094,102 patent/US10532103B2/en active Active
- 2017-04-21 CN CN201780024826.3A patent/CN109153675B/zh active Active
- 2017-04-21 JP JP2018555278A patent/JP6927999B2/ja active Active
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