JP6968823B2 - Egfrの分解のための二官能性分子、及び使用方法 - Google Patents

Egfrの分解のための二官能性分子、及び使用方法 Download PDF

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JP6968823B2
JP6968823B2 JP2018554702A JP2018554702A JP6968823B2 JP 6968823 B2 JP6968823 B2 JP 6968823B2 JP 2018554702 A JP2018554702 A JP 2018554702A JP 2018554702 A JP2018554702 A JP 2018554702A JP 6968823 B2 JP6968823 B2 JP 6968823B2
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cancer
formula
egfr
pharmaceutically acceptable
alkyl
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ナサニエル グレイ
ジェボン ジャン
クラーク ドリス デ
マイケル エック
パシ ヤンネ
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Dana Farber Cancer Institute Inc
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/16Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
    • A61K47/18Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/545Heterocyclic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents

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  • Life Sciences & Earth Sciences (AREA)
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  • Animal Behavior & Ethology (AREA)
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  • Proteomics, Peptides & Aminoacids (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
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US201662326574P 2016-04-22 2016-04-22
US62/326,574 2016-04-22
PCT/US2017/028950 WO2017185036A1 (en) 2016-04-22 2017-04-21 Bifunctional molecules for degradation of egfr and methods of use

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EP (2) EP3892272B1 (show.php)
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CN (1) CN109475528B (show.php)
AU (1) AU2017254713C1 (show.php)
CA (1) CA3021358A1 (show.php)
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Families Citing this family (78)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3256470B1 (en) 2014-12-23 2023-07-26 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
US9694084B2 (en) 2014-12-23 2017-07-04 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
US12312316B2 (en) 2015-01-20 2025-05-27 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor
WO2016149668A1 (en) 2015-03-18 2016-09-22 Arvinas, Inc. Compounds and methods for the enhanced degradation of targeted proteins
EP3302482A4 (en) 2015-06-05 2018-12-19 Arvinas, Inc. Tank-binding kinase-1 protacs 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
WO2017185036A1 (en) 2016-04-22 2017-10-26 Dana Farber Cancer Institute, Inc. Bifunctional molecules for degradation of egfr and methods of use
CA3018429A1 (en) * 2016-04-22 2017-10-26 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
CA3087528C (en) 2016-09-15 2024-01-30 Arvinas, Inc. Indole derivatives as estrogen receptor degraders
WO2018064589A1 (en) 2016-09-29 2018-04-05 Dana-Farber Cancer Institute, Inc. Targeted protein degradation using a mutant e3 ubiquitin ligase
MX2019005007A (es) 2016-11-01 2019-07-18 Arvinas Inc Protac dirigidos a la proteína tau y métodos asociados de uso.
JP6957620B2 (ja) 2016-12-01 2021-11-02 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. エストロゲン受容体分解物質としてのテトラヒドロナフタレン誘導体およびテトラヒドロイソキノリン誘導体
US11173211B2 (en) 2016-12-23 2021-11-16 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides
MX2019007646A (es) * 2016-12-23 2019-09-06 Arvinas Operations Inc Moleculas quimericas dirigidas a la proteolisis del egfr y metodos asociados de uso.
CN110741004B (zh) 2016-12-23 2023-10-17 阿尔维纳斯运营股份有限公司 用于迅速加速性纤维肉瘤多肽的靶向降解的化合物和方法
WO2018118598A1 (en) 2016-12-23 2018-06-28 Arvinas, Inc. Compounds and methods for the targeted degradation of fetal liver kinase polypeptides
US11191741B2 (en) 2016-12-24 2021-12-07 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of enhancer of zeste homolog 2 polypeptide
CA3049912A1 (en) 2017-01-26 2018-08-02 Arvinas Operations, Inc. Modulators of estrogen receptor proteolysis and associated methods of use
EP3577109A4 (en) 2017-01-31 2020-11-18 Arvinas Operations, Inc. CEREMONY LIGANDS AND BIFUNCTIONAL COMPOUNDS CONTAINING THEM
US12023385B2 (en) 2017-02-08 2024-07-02 Dana-Farber Cancer Institute, Inc. Tunable endogenous protein degradation with heterobifunctional compounds
EP3710443A1 (en) 2017-11-17 2020-09-23 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of interleukin-1 receptor-associated kinase 4 polypeptides
WO2019121562A1 (en) 2017-12-18 2019-06-27 F. Hoffmann-La Roche Ag Bifunctional inhibitors with egfr having a e3 ubiquitin ligase moiety
JP2021512059A (ja) 2018-01-29 2021-05-13 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 ブルトン型チロシンキナーゼ(btk)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btkの分解および使用方法
TW201945357A (zh) 2018-02-05 2019-12-01 瑞士商赫孚孟拉羅股份公司 化合物
US11542251B2 (en) 2018-02-14 2023-01-03 Dana-Farber Cancer Institute, Inc. IRAK degraders and uses thereof
EP3755330A4 (en) * 2018-02-20 2021-11-24 Dana-Farber Cancer Institute, Inc. PHARMACEUTICAL COMBINATIONS OF EGFR INHIBITORS AND THEIR METHODS OF USE
WO2019183523A1 (en) * 2018-03-23 2019-09-26 Genentech, Inc. Hetero-bifunctional degrader compounds and their use as modulators of targeted ubiquination (vhl)
US11161841B2 (en) 2018-04-04 2021-11-02 Arvinas Operations, Inc. Modulators of proteolysis and associated methods of use
CN108610333B (zh) * 2018-06-08 2020-04-03 绍兴文理学院 诱导MDM2自我降解E3泛素连接酶二聚体酰胺类小分子PROTACs
CN108610332B (zh) * 2018-06-08 2020-04-03 绍兴文理学院 诱导MDM2自我降解E3泛素连接酶二聚体酯类小分子PROTACs
US11667621B2 (en) 2018-06-11 2023-06-06 Stevens Institute Of Technology Antiestrogen compounds
CN112533898A (zh) 2018-07-31 2021-03-19 日商泛美克斯股份有限公司 杂环化合物
CN112912376A (zh) 2018-08-20 2021-06-04 阿尔维纳斯运营股份有限公司 用于治疗神经变性疾病的具有E3泛素连接酶结合活性并靶向α-突触核蛋白的蛋白水解靶向嵌合(PROTAC)化合物
US20210338825A1 (en) * 2018-09-28 2021-11-04 Dana-Farber Cancer Institute, Inc. Degraders of hepatitis c virus ns3/4a protein
US10844039B2 (en) 2018-11-13 2020-11-24 Biotheryx, Inc. Substituted isoindolinones
AU2020241903A1 (en) 2019-03-21 2021-10-14 Lonza Sales Ag Extracellular vesicle conjugates and uses thereof
EP3941607A1 (en) 2019-03-21 2022-01-26 Codiak BioSciences, Inc. Process for preparing extracellular vesicles
CA3252762A1 (en) 2019-04-12 2025-07-08 C4 Therapeutics, Inc. Tricyclic degraders of ikaros and aiolos
CN110204532B (zh) * 2019-05-15 2022-03-08 浙江工业大学 一种靶向egfr蛋白降解的化合物及其制备方法和应用
AU2020298293A1 (en) 2019-06-21 2022-01-20 Dana-Farber Cancer Institute, Inc. Allosteric EGFR inhibitors and methods of use 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
US20220313829A1 (en) * 2019-08-05 2022-10-06 Shanghaitech University Egfr protein degradant and anti-tumor application thereof
IL290789B2 (en) 2019-08-26 2025-09-01 Arvinas Operations Inc Methods for treating breast cancer with a history of tetrahydronaphthalene as estrogen receptor-disrupting agents
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
ES3041635T3 (en) * 2019-12-16 2025-11-13 Beijing Tide Pharmaceutical Co Ltd Macrocyclic compounds for inhibiting and inducing degradation of egfr kinase in the treatment of cancer
AU2020405129A1 (en) 2019-12-19 2022-06-23 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor
EP4681715A2 (en) * 2019-12-20 2026-01-21 C4 Therapeutics, Inc. Isoindolinone and indazole compounds for the degradation of egfr
WO2021152113A1 (en) * 2020-01-31 2021-08-05 Bayer Aktiengesellschaft Substituted 2,3-benzodiazepines derivatives
WO2021237100A1 (en) 2020-05-21 2021-11-25 Codiak Biosciences, Inc. Methods of targeting extracellular vesicles to lung
CN111592535B (zh) * 2020-06-22 2021-07-20 通化师范学院 一种抗egfr突变的抑制剂eai045的制备方法
US11839659B2 (en) 2020-07-02 2023-12-12 Northwestern University Proteolysis-targeting chimeric molecules (PROTACs) that induce degradation of indoleamine 2,3-dioxygenase (IDO) protein
CN114057770B (zh) * 2020-08-06 2023-05-02 成都先导药物开发股份有限公司 靶向egfr蛋白降解的双功能化合物
US12180193B2 (en) 2020-08-28 2024-12-31 Arvinas Operations, Inc. Accelerating fibrosarcoma protein degrading compounds and associated methods of use
CA3191532A1 (en) * 2020-09-11 2022-03-17 Hyung-Chul Ryu Compounds for suppressing egfr mutant cancer and pharmaceutical use thereof
TW202214236A (zh) 2020-09-14 2022-04-16 美商亞文納營運公司 用於靶向降解雌激素受體之化合物之結晶及非晶形形式
WO2022066928A2 (en) 2020-09-23 2022-03-31 Codiak Biosciences, Inc. Process for preparing extracellular vesicles
CN112608302B (zh) * 2020-12-28 2022-05-24 郑州大学第一附属医院 低氧还原激活靶向泛素化降解egfr蛋白的喹唑啉类衍生物及其应用
CN113004251B (zh) * 2021-03-05 2022-09-27 郑州大学第一附属医院 含2-硝基咪唑的喹唑啉类衍生物及其应用
CN117337175A (zh) * 2021-04-02 2024-01-02 密歇根大学董事会 癌症治疗的组合疗法
PE20240639A1 (es) 2021-04-16 2024-04-04 Arvinas Operations Inc Moduladores de la proteolisis bcl6 y metodos de uso asociados
US11981678B2 (en) 2021-04-29 2024-05-14 Northwestern University Substituted [1,2,4]triazolo[4,3-c]pyrimidin-5-amines and proteolysis-targeting chimeric derivatives thereof (PROTACs) that induce degradation of embryonic ectoderm development (EED) protein
US12042543B2 (en) 2021-04-30 2024-07-23 Northwestern University Substituted 3-amino-5-phenylbenzamide compounds as covalent inhibitors of enhancer zeste homolog 2 (EZH2) and proteolysis-targeting chimeric derivatives thereof (PROTACs) that induce degradation of EZH2
US20250129047A1 (en) 2021-07-04 2025-04-24 Newave Pharmaceutical Inc. Isoquinoline derivatives as mutant egfr modulators and uses thereof
WO2023034411A1 (en) 2021-09-01 2023-03-09 Oerth Bio Llc Compositions and methods for targeted degradation of proteins in a plant cell
CN115160311B (zh) * 2022-05-26 2024-03-15 北京康辰药业股份有限公司 一种用于egfr降解的双功能化合物及其应用
CN115109055B (zh) * 2022-05-26 2023-11-28 北京康辰药业股份有限公司 一种用于egfr降解的双功能化合物及其应用
WO2024050016A1 (en) 2022-08-31 2024-03-07 Oerth Bio Llc Compositions and methods for targeted inhibition and degradation of proteins in an insect cell
CN115286643B (zh) * 2022-09-02 2023-09-01 南京大学 蛋白质靶向降解化合物及其制备方法和应用
EP4584258A1 (en) 2022-09-07 2025-07-16 Arvinas Operations, Inc. Rapidly accelerated fibrosarcoma (raf) degrading compounds and associated methods of use
WO2024073507A1 (en) 2022-09-28 2024-04-04 Theseus Pharmaceuticals, Inc. Macrocyclic compounds and uses thereof
WO2024086132A1 (en) * 2022-10-17 2024-04-25 Ohio University Protacs targeting viral enzymes for precise treatment of covid-19
TW202444727A (zh) 2023-01-26 2024-11-16 美商艾維納斯手術有限公司 基於cereblon之kras降解protac及其相關用途
CN119317636A (zh) * 2023-03-07 2025-01-14 艾博生物科技(上海)有限公司 编码活化EGFR突变肽的免疫调节治疗性mRNA组合物
TW202448898A (zh) 2023-05-31 2024-12-16 瑞士商百濟神州瑞士有限責任公司 用於egfr激酶降解之化合物
WO2025006902A2 (en) * 2023-06-29 2025-01-02 Dana-Farber Cancer Institute, Inc. Synthesis and in vitro characterization of proteolysis targeting chimeras (protacs) for degradation of dna methyltransferase 1 (dnmt1)
WO2025049555A1 (en) 2023-08-31 2025-03-06 Oerth Bio Llc Compositions and methods for targeted inhibition and degradation of proteins in an insect cell
WO2025137613A1 (en) * 2023-12-22 2025-06-26 Ganymede Oncology, Inc. Cycloalkylene nrf2 protein degraders
WO2025235298A1 (en) * 2024-05-07 2025-11-13 Nikang Therapeutics, Inc. Bifunctional compounds containing thiazolyl derivatives for degrading certain cyclin-dependent kinase via ubiquitin proteasome pathway

Family Cites Families (50)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA154303A (en) 1913-06-27 1914-03-10 Albert C. Campbell Fire alarm
US6306663B1 (en) 1999-02-12 2001-10-23 Proteinex, Inc. Controlling protein levels in eucaryotic organisms
US7041298B2 (en) 2000-09-08 2006-05-09 California Institute Of Technology Proteolysis targeting chimeric pharmaceutical
US7208157B2 (en) 2000-09-08 2007-04-24 California Institute Of Technology Proteolysis targeting chimeric pharmaceutical
AU2009298877A1 (en) * 2008-09-23 2010-04-08 Georgetown University Viral and fungal inhibitors
EP2588129A4 (en) 2010-06-30 2014-07-09 Univ Brandeis ON SMALL MOLECULES TARGETED PROTEIN REMOVAL
CN103502275A (zh) 2010-12-07 2014-01-08 耶鲁大学 融合蛋白的小分子疏水性标记和引起的其降解
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
WO2013106646A2 (en) * 2012-01-12 2013-07-18 Yale University Compounds and methods for the inhibition of vcb e3 ubiquitin ligase
EP2846784A4 (en) 2012-05-11 2016-03-09 Univ Yale COMPOUNDS FOR PROMOTING PROTEIN REMOVAL AND PROCESS THEREFOR
USRE48175E1 (en) 2012-10-19 2020-08-25 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged small molecules as inducers of protein degradation
GB201311888D0 (en) * 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compounds
US20160058872A1 (en) 2014-04-14 2016-03-03 Arvinas, Inc. Imide-based modulators of proteolysis and associated methods of use
US20150291562A1 (en) * 2014-04-14 2015-10-15 Arvinas, Inc. Imide-based modulators of proteolysis and associated methods of use
US20160022642A1 (en) 2014-07-25 2016-01-28 Yale University Compounds Useful for Promoting Protein Degradation and Methods Using Same
US10071164B2 (en) 2014-08-11 2018-09-11 Yale University Estrogen-related receptor alpha based protac compounds and associated methods of use
WO2016065139A1 (en) 2014-10-24 2016-04-28 Fl Therapeutics Llc 3-substituted piperidine-2, 6-diones and non-covalent complexes with albumin
CN107108613B (zh) 2014-11-10 2020-02-25 基因泰克公司 布罗莫结构域抑制剂及其用途
MA40940A (fr) 2014-11-10 2017-09-19 Constellation Pharmaceuticals Inc Pyrrolopyridines substituées utilisées en tant qu'inhibiteurs de bromodomaines
US9694084B2 (en) 2014-12-23 2017-07-04 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
EP3256470B1 (en) 2014-12-23 2023-07-26 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
MX390189B (es) 2015-01-20 2025-03-20 Arvinas Operations Inc COMPUESTOS Y METODOS PARA LA DEGRADACION DIRIGIDA DE RECEPTOR DE ANDROGENOs.
GB201504314D0 (en) 2015-03-13 2015-04-29 Univ Dundee Small molecules
WO2016149668A1 (en) 2015-03-18 2016-09-22 Arvinas, Inc. Compounds and methods for the enhanced degradation of targeted proteins
GB201506871D0 (en) 2015-04-22 2015-06-03 Glaxosmithkline Ip Dev Ltd Novel compounds
JP6629885B2 (ja) 2015-05-22 2020-01-15 バイオセリックス, インコーポレイテッド タンパク質を標的とする化合物、その組成物、方法、および使用
MX389264B (es) 2015-06-04 2025-03-20 Arvinas Operations Inc Moduladores de proteolisis basados en imida y metodos de uso asociados.
EP3302482A4 (en) 2015-06-05 2018-12-19 Arvinas, Inc. Tank-binding kinase-1 protacs and associated methods of use
CN107849034B (zh) 2015-06-30 2021-09-03 达纳-法伯癌症研究所公司 Egfr抑制剂及其使用方法
WO2017007612A1 (en) * 2015-07-07 2017-01-12 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
JP2018526430A (ja) 2015-07-10 2018-09-13 アルヴィナス・インコーポレイテッド タンパク質分解のmdm2系修飾因子および関連の使用方法
HK1255697A1 (zh) 2015-07-13 2019-08-23 Arvinas, Inc. 基於丙氨酸的蛋白水解调节剂和相关的使用方法
WO2017024319A1 (en) 2015-08-06 2017-02-09 Dana-Farber Cancer Institute, Inc. Tunable endogenous protein degradation
WO2017024317A2 (en) 2015-08-06 2017-02-09 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
EP3337476A4 (en) 2015-08-19 2019-09-04 Arvinas, Inc. Compounds and methods for the targeted degradation of bromodomain-containing proteins
WO2017117474A1 (en) 2015-12-30 2017-07-06 Dana-Farber Cancer Institute, Inc. Bifunctional compounds for her3 degradation and methods of use
US20170281784A1 (en) 2016-04-05 2017-10-05 Arvinas, Inc. Protein-protein interaction inducing technology
EP3440066B1 (en) 2016-04-06 2022-11-30 The Regents of The University of Michigan Mdm2 protein degraders
SG11201808729WA (en) 2016-04-12 2018-11-29 Univ Michigan Regents Bet protein degraders
WO2017185036A1 (en) 2016-04-22 2017-10-26 Dana Farber Cancer Institute, Inc. Bifunctional molecules for degradation of egfr and methods of use
WO2017197036A1 (en) 2016-05-10 2017-11-16 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
WO2017197056A1 (en) 2016-05-10 2017-11-16 C4 Therapeutics, Inc. Bromodomain targeting degronimers for target protein degradation
CN109641874A (zh) 2016-05-10 2019-04-16 C4医药公司 用于靶蛋白降解的c3-碳连接的戊二酰亚胺降解决定子体
ES2989988T3 (es) 2016-05-10 2024-11-28 C4 Therapeutics Inc Degronímeros heterorocíclicos para la degradación de proteínas diana
WO2017197240A1 (en) 2016-05-12 2017-11-16 The Regents Of The University Of Michigan Ash1l inhibitors and methods of treatment therewith
WO2017201069A1 (en) 2016-05-18 2017-11-23 Biotheryx, Inc. Oxoindoline derivatives as protein function modulators
CN118436801A (zh) 2016-05-20 2024-08-06 豪夫迈·罗氏有限公司 Protac抗体缀合物及其使用方法
US10646488B2 (en) 2016-07-13 2020-05-12 Araxes Pharma Llc Conjugates of cereblon binding compounds and G12C mutant KRAS, HRAS or NRAS protein modulating compounds and methods of use thereof
MX2019007646A (es) * 2016-12-23 2019-09-06 Arvinas Operations Inc Moleculas quimericas dirigidas a la proteolisis del egfr y metodos asociados de uso.

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