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

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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
JP6927999B2 (ja) * 2016-04-22 2021-09-01 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 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
KR20250044800A (ko) * 2016-10-11 2025-04-01 아비나스 오퍼레이션스, 인코포레이티드 안드로겐 수용체의 표적 분해용 화합물 및 방법
JP7286539B2 (ja) * 2016-11-01 2023-06-05 アルビナス・オペレーションズ・インコーポレイテッド タウタンパク質標的化ｐｒｏｔａｃ、および関連使用方法
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
CA3087286C (en) * 2018-02-13 2023-06-27 Dana-Farber Cancer Institute, Inc. Cyclin-dependent kinase degraders and methods of use
IL277071B2 (en) 2018-03-08 2024-07-01 Incyte Corp AMINOPYRAZINE DIOL COMPOUNDS AS PI3K-y INHIBITORS
CN111936498B (zh) 2018-03-26 2024-04-16 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
US11046658B2 (en) 2018-07-02 2021-06-29 Incyte Corporation Aminopyrazine derivatives as PI3K-γ inhibitors
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
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
WO2020102195A1 (en) 2018-11-13 2020-05-22 Biotheryx, Inc. Substituted isoindolinones
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
CA3130706A1 (en) 2019-04-04 2020-10-08 Dana-Farber Cancer Institute, Inc. Cdk2/5 degraders and uses thereof
US11912699B2 (en) 2019-07-17 2024-02-27 Arvinas Operations, Inc. Tau-protein targeting compounds and associated
WO2021053495A1 (en) * 2019-09-16 2021-03-25 Novartis Ag Bifunctional degraders and their methods of use
CN119019369A (zh) 2019-10-17 2024-11-26 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
KR20220103753A (ko) 2019-11-19 2022-07-22 브리스톨-마이어스 스큅 컴퍼니 헬리오스 단백질의 억제제로서 유용한 화합물
WO2021226262A1 (en) * 2020-05-06 2021-11-11 Nurix Therapeutics, Inc. Bifunctional degraders of hematopoietic progenitor kinase and therapeutic uses thereof
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
JP2023539663A (ja) 2020-08-28 2023-09-15 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
US20240241020A1 (en) 2020-09-23 2024-07-18 Lonza Sales Ag Process for preparing extracellular vesicles
AR125298A1 (es) 2021-04-06 2023-07-05 Bristol Myers Squibb Co Compuestos de oxoisoindolina sustituidos con piridinilo
CN118388454A (zh) 2021-04-16 2024-07-26 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
US12097261B2 (en) 2021-05-07 2024-09-24 Kymera Therapeutics, Inc. CDK2 degraders and uses thereof
US11957759B1 (en) 2022-09-07 2024-04-16 Arvinas Operations, Inc. Rapidly accelerated fibrosarcoma (RAF) degrading compounds and associated methods of use

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014063054A1 (en) * 2012-10-19 2014-04-24 Dana-Farber Cancer Institute, Inc. Bone marrow on x chromosome kinase (bmx) inhibitors and uses thereof
JP6778114B2 (ja) * 2014-04-14 2020-10-28 アルビナス・オペレーションズ・インコーポレイテッドＡｒｖｉｎａｓ Ｏｐｅｒａｔｉｏｎｓ， Ｉｎｃ． イミド系タンパク質分解モジュレーター及び関連する使用方法
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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