AU2017254702B2 - Degradation of cyclin-dependent kinase 9 (CDK9) by conjugation of CDK9 inhibitors with E3 ligase ligand and methods of use - Google Patents
Degradation of cyclin-dependent kinase 9 (CDK9) by conjugation of CDK9 inhibitors with E3 ligase ligand and methods of use Download PDFInfo
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- AU2017254702B2 AU2017254702B2 AU2017254702A AU2017254702A AU2017254702B2 AU 2017254702 B2 AU2017254702 B2 AU 2017254702B2 AU 2017254702 A AU2017254702 A AU 2017254702A AU 2017254702 A AU2017254702 A AU 2017254702A AU 2017254702 B2 AU2017254702 B2 AU 2017254702B2
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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 (2)
| Publication Number | Publication Date |
|---|---|
| AU2017254702A1 AU2017254702A1 (en) | 2018-10-11 |
| AU2017254702B2 true AU2017254702B2 (en) | 2020-12-24 |
Family
ID=60117046
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2017254702A Active AU2017254702B2 (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 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US10532103B2 (enExample) |
| EP (1) | EP3445760B1 (enExample) |
| JP (1) | JP6927999B2 (enExample) |
| CN (1) | CN109153675B (enExample) |
| AU (1) | AU2017254702B2 (enExample) |
| CA (1) | CA3018429A1 (enExample) |
| WO (1) | WO2017185023A1 (enExample) |
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| WO2017197240A1 (en) | 2016-05-12 | 2017-11-16 | 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 |
| US10632209B2 (en) * | 2017-11-10 | 2020-04-28 | The Regents Of The University Of Michigan | ASH1L inhibitors 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 |
| US20200390783A1 (en) * | 2018-02-20 | 2020-12-17 | Dana-Farber Cancer Institute, Inc. | Inhibitors 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 |
| 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 |
| WO2020023782A1 (en) * | 2018-07-27 | 2020-01-30 | Biotheryx, Inc. | Bifunctional compounds as cdk modulators |
| CN112912376A (zh) | 2018-08-20 | 2021-06-04 | 阿尔维纳斯运营股份有限公司 | 用于治疗神经变性疾病的具有E3泛素连接酶结合活性并靶向α-突触核蛋白的蛋白水解靶向嵌合(PROTAC)化合物 |
| US12186400B2 (en) | 2018-11-09 | 2025-01-07 | Yipeng Wang | Micromolecular compound specifically degrading tau protein, and application thereof |
| US10844039B2 (en) | 2018-11-13 | 2020-11-24 | Biotheryx, Inc. | Substituted isoindolinones |
| CN119330963A (zh) * | 2019-02-27 | 2025-01-21 | 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 |
| AU2020241903A1 (en) | 2019-03-21 | 2021-10-14 | Lonza Sales Ag | Extracellular vesicle conjugates and uses thereof |
| EP3941607A1 (en) | 2019-03-21 | 2022-01-26 | Codiak BioSciences, Inc. | Process for preparing extracellular vesicles |
| AU2020256220A1 (en) * | 2019-04-04 | 2021-09-16 | Dana-Farber Cancer Institute, Inc. | CDK2/5 degraders and uses thereof |
| US20220227734A1 (en) * | 2019-04-23 | 2022-07-21 | 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 |
| WO2021026109A1 (en) * | 2019-08-05 | 2021-02-11 | 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 |
| NZ787624A (en) | 2019-10-17 | 2025-07-25 | Arvinas Operations Inc | Bifunctional molecules containing an e3 ubiquitine ligase binding moiety linked to a bcl6 targeting moiety |
| WO2021216828A1 (en) * | 2020-04-24 | 2021-10-28 | 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 |
| US12180193B2 (en) | 2020-08-28 | 2024-12-31 | Arvinas Operations, Inc. | 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 |
| JP2023548335A (ja) * | 2020-11-05 | 2023-11-16 | 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 |
| PE20240639A1 (es) | 2021-04-16 | 2024-04-04 | Arvinas Operations Inc | Moduladores de la proteolisis bcl6 y metodos de uso asociados |
| AU2022311961A1 (en) * | 2021-07-16 | 2023-11-09 | Dana-Farber Cancer Institute, Inc. | Small molecule cyclin dependent kinase 4/6 (cdk4/6) and ikzf2 (helios) degraders and methods of use thereof |
| AU2022336575A1 (en) * | 2021-09-01 | 2024-03-28 | Xizang Haisco Pharmaceutical Co., Ltd. | Compound for degradation of bcl-2 family proteins and medical application thereof |
| 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 |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20150291562A1 (en) * | 2014-04-14 | 2015-10-15 | Arvinas, Inc. | Imide-based modulators of proteolysis and associated methods of use |
Family Cites Families (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2010502743A (ja) * | 2006-09-11 | 2010-01-28 | キュリス,インコーポレイテッド | 抗増殖薬剤としての多機能性低分子 |
| 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 |
| EP2802608A4 (en) * | 2012-01-12 | 2015-08-05 | Univ Yale | COMPOUNDS AND METHODS FOR ENHANCED DEGRADATION OF TARGET PROTEINS AND OTHER POLYPEPTIDES BY E3 UBIQUITIN LIGASE |
| GB201311888D0 (en) * | 2013-07-03 | 2013-08-14 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| US10336760B2 (en) * | 2014-04-05 | 2019-07-02 | Syros Pharmaceuticals, Inc. | Inhibitors of cyclin-dependent kinase 7 (CDK7) |
| US10071164B2 (en) * | 2014-08-11 | 2018-09-11 | Yale University | Estrogen-related receptor alpha based protac compounds and associated methods of use |
| EP3256470B1 (en) * | 2014-12-23 | 2023-07-26 | Dana-Farber Cancer Institute, Inc. | Methods to induce targeted protein degradation through bifunctional molecules |
| MX389264B (es) * | 2015-06-04 | 2025-03-20 | Arvinas Operations Inc | Moduladores de proteolisis basados en imida y metodos de uso asociados. |
| WO2017007612A1 (en) * | 2015-07-07 | 2017-01-12 | Dana-Farber Cancer Institute, Inc. | Methods to induce targeted protein degradation through bifunctional molecules |
| CA2996978A1 (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 |
| WO2017079267A1 (en) * | 2015-11-02 | 2017-05-11 | Yale University | Proteolysis targeting chimera compounds and methods of preparing and using same |
| 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 |
| 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 |
| 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 |
| ES2989988T3 (es) * | 2016-05-10 | 2024-11-28 | C4 Therapeutics Inc | Degronímeros heterorocíclicos para la degradación de proteínas diana |
| 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 |
| 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 |
| WO2017197036A1 (en) * | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | Spirocyclic degronimers for target protein degradation |
| EP3474899A4 (en) * | 2016-06-23 | 2020-01-22 | Dana Farber Cancer Institute, Inc. | DEGRADATION OF PROTEIN 24 WITH THREE-PIECE MOTIVE (TRIM24) BY CONJUGATING TRIM24 INHIBITORS WITH E3 LIGASELIGAND AND METHOD FOR USE |
| WO2018064589A1 (en) * | 2016-09-29 | 2018-04-05 | Dana-Farber Cancer Institute, Inc. | Targeted protein degradation using a mutant e3 ubiquitin ligase |
-
2017
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Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20150291562A1 (en) * | 2014-04-14 | 2015-10-15 | Arvinas, Inc. | Imide-based modulators of proteolysis and associated methods of use |
Non-Patent Citations (2)
| Title |
|---|
| FAN JUNFA ET AL, "Modifications of the isonipecotic acid fragment of SNS-032: Analogs with improved permeability and lower efflux ratio", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, (2008-10-02), vol. 18, no. 23, pages 6236 - 6239 * |
| R. E. KIERNAN ET AL, "Interaction between Cyclin T1 and SCFSKP2 Targets CDK9 for Ubiquitination and Degradation by the Proteasome", MOLECULAR AND CELLULAR BIOLOGY, (2001-12-01), vol. 21, no. 23, pages 7956 - 7970 * |
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| US10532103B2 (en) | 2020-01-14 |
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| WO2017185023A1 (en) | 2017-10-26 |
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| CA3018429A1 (en) | 2017-10-26 |
| EP3445760B1 (en) | 2022-02-23 |
| CN109153675B (zh) | 2023-05-02 |
| CN109153675A (zh) | 2019-01-04 |
| JP2019514882A (ja) | 2019-06-06 |
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