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
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- 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 (https=) | 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 (7)
| Country | Link |
|---|---|
| US (1) | US10532103B2 (https=) |
| EP (1) | EP3445760B1 (https=) |
| JP (1) | JP6927999B2 (https=) |
| CN (1) | CN109153675B (https=) |
| AU (1) | AU2017254702B2 (https=) |
| CA (1) | CA3018429A1 (https=) |
| WO (1) | WO2017185023A1 (https=) |
Families Citing this family (38)
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| ES2910787T3 (es) | 2016-05-12 | 2022-05-13 | Univ Michigan Regents | Inhibidores de ASH1L y métodos de tratamiento con los mismos |
| 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 |
| WO2019094773A1 (en) * | 2017-11-10 | 2019-05-16 | The Regents Of The University Of Michigan | Ash1l inhibitors and methods of treatment therewith |
| WO2019164948A1 (en) * | 2018-02-20 | 2019-08-29 | Dana-Farber Cancer Institute, Inc. | Inhibitors of egfr and methods of use thereof |
| CA3088561A1 (en) * | 2018-02-20 | 2019-08-29 | Dana-Farber Cancer Institute, Inc. | Degraders of egfr and methods of use thereof |
| EP3755697A4 (en) * | 2018-02-20 | 2021-10-27 | Dana-Farber Cancer Institute, Inc. | EGFR DEGRADATION AGENTS AND METHODS FOR USING THEM |
| 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 |
| 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 |
| JP7297053B2 (ja) | 2018-08-20 | 2023-06-23 | アルビナス・オペレーションズ・インコーポレイテッド | 神経変性疾患を治療するためのｅ３ユビキチンリガーゼ結合活性を有するキメラ（ｐｒｏｔａｃ）化合物を標的とし、アルファ－シヌクレインタンパク質を標的とするタンパク質分解 |
| WO2020093370A1 (zh) * | 2018-11-09 | 2020-05-14 | 汪义朋 | 一种特异性降解tau蛋白的小分子化合物及其应用 |
| WO2020102195A1 (en) | 2018-11-13 | 2020-05-22 | Biotheryx, Inc. | Substituted isoindolinones |
| 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 |
| EP3941607A1 (en) | 2019-03-21 | 2022-01-26 | Codiak BioSciences, Inc. | Process for preparing extracellular vesicles |
| US20240108747A1 (en) | 2019-03-21 | 2024-04-04 | Lonza Sales Ag | Extracellular vesicle conjugates and uses thereof |
| 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 |
| WO2020219650A1 (en) * | 2019-04-23 | 2020-10-29 | Dana-Farber Cancer Institute, Inc. | Degraders of cyclin-dependent kinase 12 (cdk12) and uses thereof |
| EP3999182A1 (en) | 2019-07-17 | 2022-05-25 | Arvinas Operations, Inc. | Tau-protein targeting compounds and associated methods of use |
| ES3031581T3 (en) * | 2019-08-05 | 2025-07-09 | Dana Farber Cancer Inst 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 |
| CA3154386A1 (en) | 2019-10-17 | 2021-04-22 | Michael Berlin | Bifunctional molecules containing an e3 ubiquitine ligase binding moiety linked to a bcl6 targeting moiety |
| 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 |
| WO2022042707A1 (en) * | 2020-08-27 | 2022-03-03 | 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 |
| WO2022047145A1 (en) | 2020-08-28 | 2022-03-03 | 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 |
| WO2022066928A2 (en) | 2020-09-23 | 2022-03-31 | Codiak Biosciences, Inc. | 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 |
| KR20230171979A (ko) | 2021-04-16 | 2023-12-21 | 아비나스 오퍼레이션스, 인코포레이티드 | Bcl6 단백질 분해의 조절제 및 관련 사용 방법 |
| CN117396208A (zh) * | 2021-07-16 | 2024-01-12 | 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)和ikzf2(helios)的小分子降解剂及其使用方法 |
| JP2024534223A (ja) * | 2021-09-01 | 2024-09-18 | シーザン ハイスーク ファーマシューティカル カンパニー リミテッド | Ｂｃｌ－２ファミリータンパク質を分解する化合物及びその医薬的な応用 |
| US12084453B2 (en) | 2021-12-10 | 2024-09-10 | Incyte Corporation | Bicyclic amines as CDK12 inhibitors |
| WO2024054591A1 (en) | 2022-09-07 | 2024-03-14 | 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 |
|---|---|---|---|---|
| WO2008033747A2 (en) * | 2006-09-11 | 2008-03-20 | Curis, Inc. | 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 |
| KR102668696B1 (ko) * | 2012-01-12 | 2024-05-29 | 예일 유니버시티 | E3 유비퀴틴 리가아제에 의한 표적 단백질 및 다른 폴리펩티드의 증진된 분해를 위한 화합물 및 방법 |
| GB201311888D0 (en) * | 2013-07-03 | 2013-08-14 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| EP3129371B1 (en) * | 2014-04-05 | 2020-07-29 | Syros Pharmaceuticals, Inc. | Inhibitors of cyclin-dependent kinase 7 (cdk7) |
| RU2738833C9 (ru) * | 2014-04-14 | 2022-02-28 | Арвинас, Оперэйшнз, Инк. | Имидные модуляторы протеолиза и способы их применения |
| US10071164B2 (en) * | 2014-08-11 | 2018-09-11 | Yale University | Estrogen-related receptor alpha based protac compounds and associated methods of use |
| WO2016105518A1 (en) * | 2014-12-23 | 2016-06-30 | Dana-Farber Cancer Institute, Inc. | Methods to induce targeted protein degradation through bifunctional molecules |
| CA2988414C (en) * | 2015-06-04 | 2023-09-26 | Arvinas, Inc. | Imide-based modulators of proteolysis and associated methods of use |
| WO2017007612A1 (en) * | 2015-07-07 | 2017-01-12 | Dana-Farber Cancer Institute, Inc. | Methods to induce targeted protein degradation through bifunctional molecules |
| AU2016319125B2 (en) * | 2015-09-09 | 2021-04-08 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinases |
| GB201516243D0 (en) * | 2015-09-14 | 2015-10-28 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| BR112018008918A8 (pt) * | 2015-11-02 | 2019-02-26 | Univ Yale | compostos de quimera proteólise dirigida e métodos para preparação e uso dos mesmos |
| WO2017117474A1 (en) * | 2015-12-30 | 2017-07-06 | Dana-Farber Cancer Institute, Inc. | Bifunctional compounds for her3 degradation and methods of use |
| WO2017117473A1 (en) * | 2015-12-30 | 2017-07-06 | Dana-Farber Cancer Institute, Inc. | Bifunctional molescules for her3 degradation and methods of use |
| AU2017254713C1 (en) * | 2016-04-22 | 2021-04-29 | Dana-Farber Cancer Institute, Inc. | Bifunctional molecules for degradation of EGFR and methods of use |
| US10865205B2 (en) * | 2016-04-22 | 2020-12-15 | 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 |
| EP3445765A4 (en) * | 2016-04-22 | 2019-09-18 | Dana Farber Cancer Institute, Inc. | DECREASE OF CYCLINE-DEPENDENT KINASE 4/6 (CDK4 / 6) BY CONJUGATION OF CDK4 / 6 INHIBITORS WITH E3-LIGASE LIGANDS AND METHODS OF USE |
| EP3454856B1 (en) * | 2016-05-10 | 2024-09-11 | C4 Therapeutics, Inc. | Heterocyclic degronimers for target protein degradation |
| ES2990061T3 (es) * | 2016-05-10 | 2024-11-28 | C4 Therapeutics Inc | Degronímeros espirocíclicos para la degradación de proteínas diana |
| 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 |
| CN109790143A (zh) * | 2016-05-10 | 2019-05-21 | C4医药公司 | 用于靶蛋白降解的胺连接的c3-戊二酰亚胺降解决定子体 |
| WO2017223415A1 (en) * | 2016-06-23 | 2017-12-28 | Dana-Farber Cancer Institute, Inc. | 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 CA CA3018429A patent/CA3018429A1/en active Pending
- 2017-04-21 JP JP2018555278A patent/JP6927999B2/ja active Active
- 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 WO PCT/US2017/028924 patent/WO2017185023A1/en not_active Ceased
- 2017-04-21 EP EP17786750.4A patent/EP3445760B1/en active Active
- 2017-04-21 AU AU2017254702A patent/AU2017254702B2/en active Active
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