JP2019514883A5 - - Google Patents

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JP2019514883A5
JP2019514883A5 JP2018555281A JP2018555281A JP2019514883A5 JP 2019514883 A5 JP2019514883 A5 JP 2019514883A5 JP 2018555281 A JP2018555281 A JP 2018555281A JP 2018555281 A JP2018555281 A JP 2018555281A JP 2019514883 A5 JP2019514883 A5 JP 2019514883A5
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cancer
alkyl
disease
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formula
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JP2018555281A
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JP6921115B2 (ja
JP2019514883A (ja
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Priority claimed from PCT/US2017/028941 external-priority patent/WO2017185031A1/en
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JP2018555281A 2016-04-22 2017-04-21 サイクリン依存性キナーゼ4/6(cdk4/6)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cdk4/6の分解および使用法 Active JP6921115B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662326571P 2016-04-22 2016-04-22
US62/326,571 2016-04-22
PCT/US2017/028941 WO2017185031A1 (en) 2016-04-22 2017-04-21 Degradation of cyclin-dependent kinase 4/6 (cdk4/6) by conjugation of cdk4/6 inhibitors with e3 ligase ligand and methods of use

Publications (3)

Publication Number Publication Date
JP2019514883A JP2019514883A (ja) 2019-06-06
JP2019514883A5 true JP2019514883A5 (enExample) 2020-05-28
JP6921115B2 JP6921115B2 (ja) 2021-08-18

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JP2018555281A Active JP6921115B2 (ja) 2016-04-22 2017-04-21 サイクリン依存性キナーゼ4/6(cdk4/6)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cdk4/6の分解および使用法

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US (1) US10865204B2 (enExample)
EP (1) EP3445765A4 (enExample)
JP (1) JP6921115B2 (enExample)
CN (1) CN109071552B (enExample)
AU (1) AU2017254708B2 (enExample)
CA (1) CA3018434A1 (enExample)
WO (1) WO2017185031A1 (enExample)

Families Citing this family (62)

* Cited by examiner, † Cited by third party
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
SI3526202T1 (sl) 2016-10-11 2025-04-30 Arvinas Operations, Inc. Spojine in postopki za ciljno razgradnjo androgenskih receptorjev
MX2019004950A (es) 2016-10-28 2019-09-26 Icahn School Med Mount Sinai Composiciones y metodos para tratar el cancer mediado por el potenciador del homologo zeste 2.
CA3045037A1 (en) * 2016-12-08 2018-06-14 Icahn School Of Medicine At Mount Sinai Compositions and methods for treating cdk4/6-mediated cancer
US11173211B2 (en) 2016-12-23 2021-11-16 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides
CN109516989B (zh) * 2017-09-17 2021-12-31 上海美志医药科技有限公司 一类抑制并降解cdk的化合物
WO2019126731A1 (en) 2017-12-22 2019-06-27 Petra Pharma Corporation Aminopyridine derivatives as phosphatidylinositol phosphate kinase inhibitors
EP3752517B1 (en) 2018-02-13 2025-04-09 Dana-Farber Cancer Institute, Inc. Cyclin-dependent kinase degraders and methods of use
WO2019161224A1 (en) 2018-02-15 2019-08-22 GiraFpharma LLC Heterocyclic compounds as kinase inhibitors
CA3091041A1 (en) * 2018-02-22 2019-08-29 Ichan School Of Medicine At Mount Sinai Protein arginine methyltransferase 5 (prmt5) degradation / disruption compounds and methods of use
JP2021515013A (ja) * 2018-03-06 2021-06-17 アイカーン スクール オブ メディスン アット マウント シナイ セリンスレオニンキナーゼ(akt)分解/破壊化合物および使用方法
EP3774804A1 (en) 2018-03-26 2021-02-17 Novartis AG N-(3-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)phenyl)benzamide derivatives
US12539292B2 (en) 2018-04-01 2026-02-03 Arvinas Operations, Inc. BRM targeting compounds and associated methods of use
EP3778590A4 (en) 2018-04-09 2021-12-22 ShanghaiTech University ANTI PROTEIN DEGRADATION COMPOUND, ANTITUMOR APPLICATION, INTERMEDIATE THEREOF, AND INTERMEDIATE USE
JP2021527666A (ja) * 2018-06-21 2021-10-14 アイカーン スクール オブ メディスン アット マウント シナイ Wd40反復ドメインタンパク質5(wdr5)分解/破壊化合物および使用の方法
WO2020010204A1 (en) 2018-07-05 2020-01-09 Icahn School Of Medicine At Mount Sinai Protein tyrosine kinase 6 (ptk6) degradation / disruption compounds and methods of use
AU2019309909A1 (en) * 2018-07-23 2021-02-04 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
US11707452B2 (en) 2018-08-20 2023-07-25 Arvinas Operations, Inc. Modulators of alpha-synuclein proteolysis and associated methods of use
WO2020092662A1 (en) * 2018-11-02 2020-05-07 The Wistar Institute Of Anatomy And Biology Proteolysis-targeting chimeras
JP2022507267A (ja) 2018-11-13 2022-01-18 バイオセリックス, インコーポレイテッド 置換イソインドリノン
EP3932922A4 (en) 2019-02-25 2022-05-11 ShanghaiTech University SULPHUR-CONTAINING COMPOUND BASED ON A GLUTARIMIDE FRAMEWORK AND ITS USE
KR20210141554A (ko) 2019-03-21 2021-11-23 코디악 바이오사이언시즈, 인크. 세포외 소포 접합체 및 이의 용도
EP3941607A1 (en) 2019-03-21 2022-01-26 Codiak BioSciences, Inc. Process for preparing extracellular vesicles
JP2022521825A (ja) * 2019-03-28 2022-04-12 エッサ ファーマ,インコーポレイテッド アンドロゲン受容体モジュレーター及びタンパク質分解誘導キメラリガンドとして使用するための方法
ES3055186T3 (en) * 2019-04-04 2026-02-10 Dana Farber Cancer Inst Inc Bifunctional compounds comprising a cdk2/5 ligand, a linker and a e3 ubiquitin ligase binding degron for the treatment of cancer
JP7667742B2 (ja) 2019-04-09 2025-04-23 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 Atp競合性akt阻害剤gdc-0068とe3リガーゼリガンドとの結合によるaktの分解および使用方法
JP2022529700A (ja) * 2019-04-23 2022-06-23 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 サイクリン依存性キナーゼ12(cdk12)の分解剤およびその使用
CN114423463B (zh) 2019-05-06 2025-09-26 西奈山伊坎医学院 作为hpk1的降解剂的异双功能化合物
EP3976621A4 (en) * 2019-06-03 2023-11-15 Regents of the University of Minnesota COMPOUNDS THAT DEGRADE KINASES AND THEIR USES
TW202112767A (zh) 2019-06-17 2021-04-01 美商佩特拉製藥公司 作為磷脂酸肌醇磷酸激酶抑制劑之胺基吡啶衍生物
TWI769382B (zh) * 2019-06-21 2022-07-01 長庚大學 利博西林用於製備治療罹患磷酸二酯酶4介導疾病的患者的醫藥組合物及用途
CN110143948B (zh) * 2019-06-21 2021-05-14 上海博悦生物科技有限公司 Cdk4/6抑制剂、其药物组合物、制备方法及应用
EP3999182A1 (en) 2019-07-17 2022-05-25 Arvinas Operations, Inc. Tau-protein targeting compounds and associated methods of use
WO2021023233A1 (zh) 2019-08-05 2021-02-11 上海科技大学 Egfr蛋白降解剂及其抗肿瘤应用
EP4031247A1 (en) * 2019-09-16 2022-07-27 Novartis AG Bifunctional degraders and their methods of use
MX2022004526A (es) 2019-10-17 2022-07-21 Arvinas Operations Inc Moléculas bifuncionales que contienen una porción de unión a la ligasa de ubiquitina e3 unida a una porción de direccionamiento a bcl6.
PH12022551482A1 (en) 2019-12-18 2023-11-29 Novartis Ag 3-(5-methoxy-1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof
CN115380026B (zh) * 2020-03-17 2023-11-07 南京明德新药研发有限公司 蛋白降解调节剂与其使用方法
TWI918648B (zh) * 2020-05-06 2026-03-21 美商新銳思生物製藥股份有限公司 造血前驅細胞激酶之雙官能降解劑及其治療用途
CN115996918A (zh) 2020-05-09 2023-04-21 阿尔维纳斯运营股份有限公司 制造双官能团化合物的方法、双官能团化合物的超纯形式以及包括所述双官能团化合物的剂型
WO2021237100A1 (en) 2020-05-21 2021-11-25 Codiak Biosciences, Inc. Methods of targeting extracellular vesicles to lung
US12103924B2 (en) 2020-06-01 2024-10-01 Icahn School Of Medicine At Mount Sinai Mitogen-activated protein kinase kinase (MEK) degradation compounds and methods of use
CN111909155B (zh) * 2020-08-21 2022-10-18 东莞理工学院 蛋白水解靶向嵌合体、提高其口服生物利用度的前药分子及应用
WO2022047145A1 (en) 2020-08-28 2022-03-03 Arvinas Operations, Inc. Rapidly accelerating fibrosarcoma protein degrading compounds and associated methods of use
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
EP4259128A4 (en) * 2020-12-09 2025-04-30 Kymera Therapeutics, Inc. Irak degraders and uses thereof
CN116783205A (zh) * 2020-12-22 2023-09-19 尼坎治疗公司 用于通过泛素蛋白酶体途径降解细胞周期蛋白依赖性激酶2的化合物
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
WO2022254362A1 (en) 2021-06-03 2022-12-08 Novartis Ag 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives and medical uses thereof
AU2022362494A1 (en) * 2021-10-14 2024-05-23 Cullgen (Shanghai), Inc. Modified proteins and protein degraders
WO2023178130A1 (en) * 2022-03-16 2023-09-21 Biotheryx, Inc. Sos1 protein degraders, pharmaceutical compositions, and therapeutic applications
WO2023207875A1 (en) * 2022-04-25 2023-11-02 Onquality Pharmaceuticals China Ltd. Cdk inhibitors, pharmaceutical compositions, and therapeutic applications
CN119451967A (zh) * 2022-06-22 2025-02-14 霖康疗法公司 用于经由泛素蛋白酶体途径降解细胞周期蛋白依赖性激酶2的含有吡啶并[2,3-d]嘧啶-7(8H)-酮衍生物的双功能化合物
CN115364100B (zh) * 2022-08-25 2023-08-29 杭州天玑济世生物科技有限公司 Ly2835219作为线粒体自噬诱导剂的用途
EP4584258A1 (en) 2022-09-07 2025-07-16 Arvinas Operations, Inc. Rapidly accelerated fibrosarcoma (raf) degrading compounds and associated methods of use
WO2024083257A1 (zh) * 2022-10-21 2024-04-25 上海领泰生物医药科技有限公司 Sos1蛋白降解剂及其应用
CN121358732A (zh) * 2023-03-07 2026-01-16 睿跃生物科技有限公司 治疗癌症的化合物和方法
AU2024392985A1 (en) 2023-12-08 2026-06-04 Arvinas Operations, Inc. Use of androgen receptor degrader for the treatment of spinal and bulbar muscular atrophy
WO2025222132A1 (en) * 2024-04-19 2025-10-23 Foghorn Therapeutics Inc. Compounds and uses thereof
WO2025231380A1 (en) * 2024-05-02 2025-11-06 University Of Maryland, Baltimore Proteolysis targeting chimeras and methods of use thereof
WO2026067249A1 (en) * 2024-09-29 2026-04-02 K2 Medicines (Nanjing) Co., Ltd. Cdk4 or cdk4/6 dual degrader and use thereof

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ534069A (en) * 2002-01-22 2007-03-30 Warner Lambert Co 2-(Pyridin-2-ylamino)-pyrido[2,3-d]pyrimidin-7-ones to be used to treat neurodegenerative disorders, viruses and cancer
AU2009284098B2 (en) * 2008-08-22 2012-03-29 Astex Therapeutics Ltd. Pyrrolopyrimidine compounds as CDK inhibitors
PA8852901A1 (es) * 2008-12-22 2010-07-27 Lilly Co Eli Inhibidores de proteina cinasa
EP4649963A3 (en) * 2014-04-14 2026-05-13 Arvinas Operations, Inc. Imide-based modulators of proteolysis and associated methods of use
WO2016015604A1 (en) * 2014-07-26 2016-02-04 Sunshine Lake Pharma Co., Ltd. Compounds as cdk small-molecule inhibitors and uses thereof
WO2016040848A1 (en) * 2014-09-12 2016-03-17 G1 Therapeutics, Inc. Treatment of rb-negative tumors using topoisomerase inhibitors in combination with cyclin dependent kinase 4/6 inhibitors
EP3191098A4 (en) 2014-09-12 2018-04-25 G1 Therapeutics, Inc. Combinations and dosing regimes to treat rb-positive tumors
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
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
AU2019309909A1 (en) * 2018-07-23 2021-02-04 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

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