JP6921114B2 - サイクリン依存性キナーゼ８（ｃｄｋ８）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ｃｄｋ８の分解および使用法 - Google Patents

サイクリン依存性キナーゼ８（ｃｄｋ８）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ｃｄｋ８の分解および使用法 Download PDF

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JP6921114B2
JP6921114B2 JP2018555152A JP2018555152A JP6921114B2 JP 6921114 B2 JP6921114 B2 JP 6921114B2 JP 2018555152 A JP2018555152 A JP 2018555152A JP 2018555152 A JP2018555152 A JP 2018555152A JP 6921114 B2 JP6921114 B2 JP 6921114B2
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cancer
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bifunctional compound
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JP2019514876A (ja
JP2019514876A5 (OSRAM
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ナサナエル グレイ
ナサナエル グレイ
ティンフー チャン
ティンフー チャン
カラー エム． オルソン
カラー エム． オルソン
ヤンケ リャン
ヤンケ リャン
ニコラス クフャトコフスキ
ニコラス クフャトコフスキ
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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
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
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JP2018555152A 2016-04-22 2017-04-21 サイクリン依存性キナーゼ８（ｃｄｋ８）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ｃｄｋ８の分解および使用法 Active JP6921114B2 (ja)

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US201662326584P 2016-04-22 2016-04-22
US62/326,584 2016-04-22
PCT/US2017/028948 WO2017185034A1 (en) 2016-04-22 2017-04-21 Degradation of cyclin-dependent kinase 8 (cdk8) by conjugation of cdk8 inhibitors with e3 ligase ligand and methods of use

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JP2019514876A JP2019514876A (ja) 2019-06-06
JP2019514876A5 JP2019514876A5 (OSRAM) 2020-05-28
JP6921114B2 true JP6921114B2 (ja) 2021-08-18

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US (3) US10865205B2 (OSRAM)
EP (2) EP3985006A1 (OSRAM)
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AU (1) AU2017254711B2 (OSRAM)
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Families Citing this family (31)

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Publication number Priority date Publication date Assignee Title
AU2017254702B2 (en) * 2016-04-22 2020-12-24 Dana-Farber Cancer Institute, Inc. Degradation of cyclin-dependent kinase 9 (CDK9) by conjugation of CDK9 inhibitors with E3 ligase ligand 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
HUE061847T2 (hu) 2016-10-11 2023-08-28 Arvinas Operations Inc Androgén receptor célzott degradálására alkalmas vegyületek és eljárások
CA3042260C (en) * 2016-11-01 2023-10-03 Arvinas, Inc. Tau-protein targeting protacs and associated methods of use
US11173211B2 (en) 2016-12-23 2021-11-16 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides
CN108187035B (zh) * 2018-01-05 2020-12-15 杭州师范大学 E3连接酶fbw7在延缓衰老及相关疾病方面的医药用途
US12325725B2 (en) 2018-02-13 2025-06-10 Dana-Farber Cancer Institute, Inc. Cyclin-dependent kinase degraders and methods of use
WO2019226213A2 (en) 2018-03-08 2019-11-28 Incyte Corporation AMINOPYRAZINE DIOL COMPOUNDS AS PI3K-y INHIBITORS
WO2019186343A1 (en) 2018-03-26 2019-10-03 Novartis Ag N-(3-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)phenyl)benzamide derivatives
WO2020010003A1 (en) 2018-07-02 2020-01-09 Incyte Corporation AMINOPYRAZINE DERIVATIVES AS PI3K-γ INHIBITORS
US11707452B2 (en) 2018-08-20 2023-07-25 Arvinas Operations, Inc. Modulators of alpha-synuclein proteolysis and associated methods of use
CN111018857B (zh) * 2018-10-09 2023-06-02 嘉兴优博生物技术有限公司 靶向蛋白酶降解平台(ted)
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
EP3880669A1 (en) 2018-11-13 2021-09-22 Biotheryx, Inc. Substituted isoindolinones
US12233356B2 (en) 2019-03-21 2025-02-25 Lonza Sales Ag Process for preparing extracellular vesicles
CN113747925B (zh) 2019-03-21 2024-10-15 隆萨销售股份公司 胞外囊泡缀合物及其用途
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
CN114867727B (zh) 2019-07-17 2025-02-21 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
WO2021053495A1 (en) * 2019-09-16 2021-03-25 Novartis Ag Bifunctional degraders and their methods of use
EP4045496A1 (en) 2019-10-17 2022-08-24 Arvinas Operations, Inc. Bifunctional molecules containing an e3 ubiquitine ligase binding moiety linked to a bcl6 targeting moiety
KR20220103753A (ko) 2019-11-19 2022-07-22 브리스톨-마이어스 스큅 컴퍼니 헬리오스 단백질의 억제제로서 유용한 화합물
CN115605488B (zh) * 2020-05-06 2024-08-09 新锐思生物制药股份有限公司 造血祖细胞激酶的双功能降解剂及其治疗用途
AU2021273458A1 (en) 2020-05-09 2022-12-01 Arvinas Operations, Inc. Methods of manufacturing a bifunctional compound, ultrapure forms of the bifunctional compound, and dosage forms comprising the same
WO2021237100A1 (en) 2020-05-21 2021-11-25 Codiak Biosciences, Inc. Methods of targeting extracellular vesicles to lung
US12180193B2 (en) 2020-08-28 2024-12-31 Arvinas Operations, Inc. Accelerating fibrosarcoma protein degrading compounds and associated methods of use
US20240241020A1 (en) 2020-09-23 2024-07-18 Lonza Sales Ag Process for preparing extracellular vesicles
AU2022253242A1 (en) 2021-04-06 2023-11-23 Bristol-Myers Squibb Company Pyridinyl substituted oxoisoindoline compounds
AU2022259683A1 (en) 2021-04-16 2023-10-19 Arvinas Operations, Inc. Modulators of bcl6 proteolysis and associated methods of use
CN117715904A (zh) 2021-05-07 2024-03-15 凯麦拉医疗公司 Cdk2降解剂和其用途
US11957759B1 (en) 2022-09-07 2024-04-16 Arvinas Operations, Inc. Rapidly accelerated fibrosarcoma (RAF) degrading compounds and associated methods of use
WO2025122895A1 (en) 2023-12-08 2025-06-12 Arvinas Operations, Inc. Use of androgen receptor degrader for the treatment of spinal and bulbar muscular atrophy

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10000483B2 (en) 2012-10-19 2018-06-19 Dana-Farber Cancer Institute, Inc. Bone marrow on X chromosome kinase (BMX) inhibitors and uses thereof
KR20250127179A (ko) * 2014-04-14 2025-08-26 아비나스 오퍼레이션스, 인코포레이티드 단백질분해의 이미드-기초된 조절인자 및 연관된 이용 방법
US10071164B2 (en) * 2014-08-11 2018-09-11 Yale University Estrogen-related receptor alpha based protac compounds and associated methods of use

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