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 PDF

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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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cancer
alkyl
disease
cdk9
bifunctional compound
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AU2017254702A1 (en
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Nathanael Gray
Nicholas KWIATKOWSKI
Yanke LIANG
Calla M. OLSON
Tinghu Zhang
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Dana Farber Cancer Institute Inc
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AU2017254702A 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 Active AU2017254702B2 (en)

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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

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Families Citing this family (37)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3454945B1 (en) 2016-05-12 2022-01-19 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
JP7424637B2 (ja) 2017-11-10 2024-01-30 ザ リージェンツ オブ ザ ユニバーシティ オブ ミシガン Ash1l分解剤及びそれを用いた治療方法
AU2019225806A1 (en) * 2018-02-20 2020-07-16 Dana-Farber Cancer Institute, Inc. Inhibitors of EGFR and methods of use thereof
EP3755698A4 (en) * 2018-02-20 2021-10-27 Dana-Farber Cancer Institute, Inc. EGFR DEGRADATION AGENTS AND METHODS FOR USING THEM
EP3755697A4 (en) * 2018-02-20 2021-10-27 Dana-Farber Cancer Institute, Inc. EGFR DEGRADATION AGENTS AND METHODS FOR USING THEM
EP4166557A1 (en) 2018-03-26 2023-04-19 Novartis AG Intermediates of n-(3-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)phenyl)benzamide derivatives
US11236103B2 (en) 2018-07-27 2022-02-01 Biotheryx, Inc. Bifunctional compounds
WO2020041331A1 (en) 2018-08-20 2020-02-27 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
WO2020102195A1 (en) 2018-11-13 2020-05-22 Biotheryx, Inc. Substituted isoindolinones
US20230073777A1 (en) * 2019-02-27 2023-03-09 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
CA3133314A1 (en) 2019-03-21 2020-09-24 Codiak Biosciences, Inc. Extracellular vesicle conjugates and uses thereof
WO2020206137A1 (en) 2019-04-04 2020-10-08 Dana-Farber Cancer Institute, Inc. Cdk2/5 degraders and uses thereof
EP3958861A4 (en) * 2019-04-23 2023-05-03 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
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
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
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
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
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
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
US11986532B2 (en) 2021-04-16 2024-05-21 Arvinas Operations, Inc. Modulators of BCL6 proteolysis and associated methods of use
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
EP4397661A4 (en) * 2021-09-01 2025-08-27 Xizang Haisco Pharmaceutical Co Ltd COMPOUND FOR DEGRADING BCL-2 FAMILY PROTEINS AND ASSOCIATED MEDICAL USE
US12084453B2 (en) 2021-12-10 2024-09-10 Incyte Corporation Bicyclic amines as CDK12 inhibitors
TW202432544A (zh) 2022-09-07 2024-08-16 美商亞文納營運公司 快速加速纖維肉瘤降解化合物及相關使用方法
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)

* Cited by examiner, † Cited by third party
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)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20090077914A (ko) * 2006-09-11 2009-07-16 쿠리스 인코퍼레이션 항증식제로서의 다작용성 소분자
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
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
EP3129371B1 (en) * 2014-04-05 2020-07-29 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
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
US11142507B2 (en) * 2015-09-09 2021-10-12 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
GB201516243D0 (en) * 2015-09-14 2015-10-28 Glaxosmithkline Ip Dev Ltd Novel compounds
CN108366992A (zh) * 2015-11-02 2018-08-03 耶鲁大学 蛋白水解靶向嵌合体化合物及其制备和应用方法
US20200216454A1 (en) * 2015-12-30 2020-07-09 Dana-Farber Cancer Institute, Inc. Bifunctional molecules for her3 degradation and methods of use
US20190016703A1 (en) * 2015-12-30 2019-01-17 Dana-Farber Cancer Institute, Inc. Bifunctional compounds for her3 degradation and methods of use
US10865204B2 (en) * 2016-04-22 2020-12-15 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
WO2017185034A1 (en) * 2016-04-22 2017-10-26 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
WO2017185036A1 (en) * 2016-04-22 2017-10-26 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
WO2017197046A1 (en) * 2016-05-10 2017-11-16 C4 Therapeutics, Inc. C3-carbon linked glutarimide degronimers for target protein degradation
EP3454862B1 (en) * 2016-05-10 2024-09-11 C4 Therapeutics, Inc. Spirocyclic degronimers for target protein degradation
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
EP3474899A4 (en) * 2016-06-23 2020-01-22 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

Patent Citations (1)

* Cited by examiner, † Cited by third party
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)

* Cited by examiner, † Cited by third party
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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