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
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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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JP2019514876A5 JP2019514876A5 (enExample) 2020-05-28
JP6921114B2 true JP6921114B2 (ja) 2021-08-18

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Families Citing this family (33)

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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
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
LT3660004T (lt) * 2016-10-11 2023-06-12 Arvinas Operations, Inc. Junginiai ir metodai, skirti tikslinei androgeno receptoriaus degradacijai
EP3535265A4 (en) * 2016-11-01 2020-07-08 Arvinas, Inc. PROTACS TARGETING ON TAU PROTEIN AND RELATED METHODS FOR 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
AU2019222652B2 (en) * 2018-02-13 2021-09-02 Dana-Farber Cancer Institute, Inc. Cyclin-dependent kinase degraders and methods of use
MD3762368T2 (ro) 2018-03-08 2022-07-31 Incyte Corp Compuși diol aminopirazină ca inhibitori ai PI3K-Y
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
US12539292B2 (en) 2018-04-01 2026-02-03 Arvinas Operations, Inc. BRM targeting compounds and associated methods of use
US11046658B2 (en) 2018-07-02 2021-06-29 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)
US12186400B2 (en) 2018-11-09 2025-01-07 Yipeng Wang Micromolecular compound specifically degrading tau protein, and application thereof
CN113423701A (zh) 2018-11-13 2021-09-21 拜欧斯瑞克斯公司 取代的异吲哚啉酮
US12233356B2 (en) 2019-03-21 2025-02-25 Lonza Sales Ag Process for preparing extracellular vesicles
CA3133314A1 (en) 2019-03-21 2020-09-24 Codiak Biosciences, Inc. Extracellular vesicle conjugates and uses thereof
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
WO2021011913A1 (en) 2019-07-17 2021-01-21 Arvinas Operations, Inc. Tau-protein targeting compounds and associated methods of use
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
US12310975B2 (en) 2019-10-17 2025-05-27 Arvinas Operations, Inc. Modulators of BCL6 proteolysis and associated methods of use
KR20220103753A (ko) 2019-11-19 2022-07-22 브리스톨-마이어스 스큅 컴퍼니 헬리오스 단백질의 억제제로서 유용한 화합물
TW202140441A (zh) 2020-03-23 2021-11-01 美商必治妥美雅史谷比公司 經取代之側氧基異吲哚啉化合物
JP7857232B2 (ja) * 2020-05-06 2026-05-12 ニューリックス セラピューティクス，インコーポレイテッド 造血前駆体キナーゼの二官能性分解物質およびその治療的使用
EP4146642A1 (en) 2020-05-09 2023-03-15 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
EP4204418A1 (en) 2020-08-28 2023-07-05 Arvinas Operations, Inc. Rapidly 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
PT4320112T (pt) 2021-04-06 2025-07-07 Bristol Myers Squibb Co Compostos de oxoisoindolina substituídos por piridinilo
CA3214806A1 (en) 2021-04-16 2022-10-20 Arvinas Operations, Inc. Modulators of bcl6 proteolysis and associated methods of use
AU2022271290A1 (en) 2021-05-07 2023-11-23 Kymera Therapeutics, Inc. Cdk2 degraders and uses thereof
EP4584258A1 (en) 2022-09-07 2025-07-16 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
CN119591582A (zh) * 2014-04-14 2025-03-11 阿尔维纳斯运营股份有限公司 基于酰亚胺的蛋白水解调节剂和相关使用方法
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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