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 (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 (40)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109414596B (zh) | 2016-05-12 | 2023-09-29 | 密歇根大学董事会 | Ash1l抑制剂和用其进行治疗的方法 |
| 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 |
| US10632209B2 (en) | 2017-11-10 | 2020-04-28 | The Regents Of The University Of Michigan | ASH1L inhibitors and methods of treatment therewith |
| WO2019164932A1 (en) * | 2018-02-20 | 2019-08-29 | Dana-Farber Cancer Institute, Inc. | Degraders of egfr and methods of use thereof |
| CA3087288A1 (en) * | 2018-02-20 | 2019-08-29 | Dana-Farber Cancer Institute, Inc. | Inhibitors 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 |
| EP3774804A1 (en) | 2018-03-26 | 2021-02-17 | Novartis AG | N-(3-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)phenyl)benzamide derivatives |
| US12539292B2 (en) | 2018-04-01 | 2026-02-03 | Arvinas Operations, Inc. | BRM targeting compounds and associated methods of use |
| WO2020023782A1 (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 |
| 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 |
| JP2022507267A (ja) | 2018-11-13 | 2022-01-18 | バイオセリックス， インコーポレイテッド | 置換イソインドリノン |
| CN113646002A (zh) * | 2019-02-27 | 2021-11-12 | 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 |
| KR20210141554A (ko) | 2019-03-21 | 2021-11-23 | 코디악 바이오사이언시즈, 인크. | 세포외 소포 접합체 및 이의 용도 |
| EP3941607A1 (en) | 2019-03-21 | 2022-01-26 | Codiak BioSciences, Inc. | Process for preparing extracellular vesicles |
| ES3055186T3 (en) * | 2019-04-04 | 2026-02-10 | Dana Farber Cancer Inst Inc | Bifunctional compounds comprising a cdk2/5 ligand, a linker and a e3 ubiquitin ligase binding degron for the treatment of cancer |
| JP2022529700A (ja) * | 2019-04-23 | 2022-06-23 | 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１２（ｃｄｋ１２）の分解剤およびその使用 |
| EP3999182A1 (en) | 2019-07-17 | 2022-05-25 | Arvinas Operations, Inc. | Tau-protein targeting compounds and associated methods of use |
| CN114174281B (zh) * | 2019-08-05 | 2025-02-07 | 达纳-法伯癌症研究公司 | 细胞周期蛋白依赖性激酶7(cdk7)的降解剂及其用途 |
| EP4031247A1 (en) * | 2019-09-16 | 2022-07-27 | Novartis AG | Bifunctional degraders and their methods of use |
| MX2022004526A (es) | 2019-10-17 | 2022-07-21 | Arvinas Operations Inc | Moléculas bifuncionales que contienen una porción de unión a la ligasa de ubiquitina e3 unida a una porción de direccionamiento a bcl6. |
| US20230158159A1 (en) * | 2020-04-24 | 2023-05-25 | Massachusetts Institute Of Technology | Chimeric degraders of cyclin-dependent kinase 9 and uses thereof |
| EP4143329A4 (en) | 2020-04-28 | 2024-10-16 | 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 |
| 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 |
| WO2022098843A1 (en) * | 2020-11-05 | 2022-05-12 | Kronos Bio, Inc. | Compounds and methods for modulating cdk9 activity |
| CN118388454A (zh) | 2021-04-16 | 2024-07-26 | 阿尔维纳斯运营股份有限公司 | Bcl6蛋白水解的调节剂和其相关使用方法 |
| 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 |
| US20240408085A1 (en) * | 2021-09-01 | 2024-12-12 | Xizang Haisco Pharmaceutical Co., Ltd. | Compound for degradation of bcl-2 family proteins and medical application thereof |
| TW202329937A (zh) | 2021-12-03 | 2023-08-01 | 美商英塞特公司 | 雙環胺ｃｋ１２抑制劑 |
| US12084453B2 (en) | 2021-12-10 | 2024-09-10 | Incyte Corporation | Bicyclic amines as CDK12 inhibitors |
| CA3251059A1 (en) | 2022-05-02 | 2023-11-09 | The Board Of Trustees Of The Leland Stanford Junior University | Compositions, systems and methods for modulating a target gene |
| 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 |
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|---|---|---|---|---|
| SG174772A1 (en) * | 2006-09-11 | 2011-10-28 | 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 |
| KR102438072B1 (ko) * | 2012-01-12 | 2022-08-31 | 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 |
| EP3805218A1 (en) * | 2014-04-05 | 2021-04-14 | Syros Pharmaceuticals, Inc. | Inhibitors of cyclin-dependent kinase 7 (cdk7) |
| EP4649963A3 (en) * | 2014-04-14 | 2026-05-13 | Arvinas Operations, Inc. | Imide-based modulators of proteolysis and associated methods of use |
| 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 |
| 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 |
| WO2017044858A2 (en) * | 2015-09-09 | 2017-03-16 | 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 |
| 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 |
| WO2017185036A1 (en) * | 2016-04-22 | 2017-10-26 | 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 |
| WO2017197046A1 (en) * | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | C3-carbon linked glutarimide degronimers for target protein degradation |
| CN121974842A (zh) * | 2016-05-10 | 2026-05-05 | 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 |
| 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 |
| CN109562113A (zh) * | 2016-05-10 | 2019-04-02 | C4医药公司 | 用于靶蛋白降解的螺环降解决定子体 |
| AU2017281525B2 (en) * | 2016-06-23 | 2021-01-21 | 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 AU AU2017254702A patent/AU2017254702B2/en active Active
- 2017-04-21 US US16/094,102 patent/US10532103B2/en active Active
- 2017-04-21 JP JP2018555278A patent/JP6927999B2/ja active Active
- 2017-04-21 WO PCT/US2017/028924 patent/WO2017185023A1/en not_active Ceased
- 2017-04-21 CN CN201780024826.3A patent/CN109153675B/zh active Active
- 2017-04-21 EP EP17786750.4A patent/EP3445760B1/en active Active
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