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
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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)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2017263574B2 (en) | 2016-05-12 | 2022-11-17 | 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 |
| CA3087288A1 (en) * | 2018-02-20 | 2019-08-29 | Dana-Farber Cancer Institute, Inc. | Inhibitors of egfr and methods of use thereof |
| AU2019225811A1 (en) * | 2018-02-20 | 2020-07-09 | Dana-Farber Cancer Institute, Inc. | Degraders of EGFR and methods of use thereof |
| 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 |
| AU2019309894A1 (en) * | 2018-07-27 | 2021-01-28 | Biotheryx, Inc. | Bifunctional compounds as CDK modulators |
| EP3841100A1 (en) | 2018-08-20 | 2021-06-30 | Arvinas Operations, Inc. | Proteolysis targeting chimeric (protac) compound with e3 ubiquitin ligase binding activity and targeting alpha-synuclein protein for treating neurodegenerative diseases |
| 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 |
| WO2020191369A1 (en) | 2019-03-21 | 2020-09-24 | Codiak Biosciences, Inc. | Process for preparing extracellular vesicles |
| KR20210141554A (ko) | 2019-03-21 | 2021-11-23 | 코디악 바이오사이언시즈, 인크. | 세포외 소포 접합체 및 이의 용도 |
| 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 |
| CN119954801A (zh) | 2019-07-17 | 2025-05-09 | 阿尔维纳斯运营股份有限公司 | Tau蛋白靶向化合物及相关使用方法 |
| ES3031581T3 (en) * | 2019-08-05 | 2025-07-09 | Dana Farber Cancer Inst Inc | Degraders of cyclin-dependent kinase 7 (cdk7) and uses thereof |
| JP7785663B2 (ja) * | 2019-09-16 | 2025-12-15 | ノバルティス アーゲー | 二機能性分解誘導薬及びそれらの使用方法 |
| CN115397821B (zh) | 2019-10-17 | 2024-09-03 | 阿尔维纳斯运营股份有限公司 | 含有与bcl6靶向部分连接的e3泛素连接酶结合部分的双官能分子 |
| WO2021216828A1 (en) * | 2020-04-24 | 2021-10-28 | Massachusetts Institute Of Technology | Chimeric degraders of cyclin-dependent kinase 9 and uses thereof |
| US11897930B2 (en) | 2020-04-28 | 2024-02-13 | 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 |
| US20240100170A1 (en) * | 2020-08-27 | 2024-03-28 | 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 |
| JP7834721B2 (ja) | 2020-08-28 | 2026-03-24 | アルビナス・オペレーションズ・インコーポレイテッド | 急速進行性線維肉腫タンパク質分解化合物及び関連する使用方法 |
| 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 |
| EP4240422A4 (en) * | 2020-11-05 | 2025-05-07 | Kronos Bio, Inc. | Compounds and methods for modulating CDK9 activity |
| CN117279910A (zh) | 2021-04-16 | 2023-12-22 | 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 |
| CA3231175A1 (en) * | 2021-09-01 | 2023-03-09 | Xizang Haisco Pharmaceutical Co., Ltd. | Compound for degradation of bcl-2 family proteins and medical application thereof |
| WO2023107705A1 (en) | 2021-12-10 | 2023-06-15 | 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 |
|---|---|---|---|---|
| EP2061772A4 (en) * | 2006-09-11 | 2011-06-29 | Curis Inc | MULTIFUNCTIONAL SMALL MOLECULES AS PROLIFERATION-ACTIVE ACTIVE SUBSTANCES |
| US20080188524A1 (en) | 2006-10-25 | 2008-08-07 | Martin Augustin | Methods of treating pain |
| TW200922564A (en) * | 2007-09-10 | 2009-06-01 | Curis Inc | CDK inhibitors containing a zinc binding moiety |
| CA2861066C (en) * | 2012-01-12 | 2024-01-02 | Yale University | Compounds and methods for the enhanced degradation of targeted proteins and other polypeptides by an e3 ubiquitin ligase |
| 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) |
| AU2015247817C1 (en) * | 2014-04-14 | 2022-02-10 | 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 |
| HUE054149T2 (hu) * | 2015-06-04 | 2021-08-30 | Arvinas Operations Inc | Proteolízis imid-alapú modulátorai és ezekkel kapcsolatos felhasználási eljárások |
| WO2017007612A1 (en) * | 2015-07-07 | 2017-01-12 | Dana-Farber Cancer Institute, Inc. | Methods to induce targeted protein degradation through bifunctional molecules |
| EP3347018B1 (en) * | 2015-09-09 | 2021-09-01 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinases |
| 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 |
| US20190016703A1 (en) * | 2015-12-30 | 2019-01-17 | Dana-Farber Cancer Institute, Inc. | Bifunctional compounds for her3 degradation and methods of use |
| US20200216454A1 (en) * | 2015-12-30 | 2020-07-09 | Dana-Farber Cancer Institute, Inc. | Bifunctional molecules for her3 degradation and methods of use |
| EP3445357B1 (en) * | 2016-04-22 | 2021-05-26 | Dana-Farber Cancer Institute, Inc. | Bifunctional molecules for degradation of egfr 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 |
| CN109311869B (zh) * | 2016-04-22 | 2022-12-23 | 达纳－法伯癌症研究所公司 | 通过细胞周期蛋白-依赖性激酶8(cdk8)抑制剂与e3连接酶配体的缀合降解cdk8和使用方法 |
| 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 |
| EP3454862B1 (en) * | 2016-05-10 | 2024-09-11 | C4 Therapeutics, Inc. | Spirocyclic degronimers for target protein degradation |
| 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 |
| EP4491236A3 (en) * | 2016-05-10 | 2025-04-02 | C4 Therapeutics, Inc. | Heterocyclic degronimers for target protein degradation |
| 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 CN CN201780024826.3A patent/CN109153675B/zh active Active
- 2017-04-21 WO PCT/US2017/028924 patent/WO2017185023A1/en not_active Ceased
- 2017-04-21 JP JP2018555278A patent/JP6927999B2/ja active Active
- 2017-04-21 EP EP17786750.4A patent/EP3445760B1/en active Active
- 2017-04-21 AU AU2017254702A patent/AU2017254702B2/en active Active
- 2017-04-21 US US16/094,102 patent/US10532103B2/en active Active
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