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
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JP2019519476A (ja
JP2019519476A5 (cg-RX-API-DMAC10.html
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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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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/14—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/16—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
    • A61K47/18—Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal 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
    • A61K47/51—Medicinal 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
    • A61K47/54—Medicinal 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
    • A61K47/545—Heterocyclic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
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  • Oil, Petroleum & Natural Gas (AREA)
  • 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)
JP2018554702A 2016-04-22 2017-04-21 Ｅｇｆｒの分解のための二官能性分子、及び使用方法 Active JP6968823B2 (ja)

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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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Families Citing this family (78)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2016105518A1 (en) 2014-12-23 2016-06-30 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
EP3270917A4 (en) 2015-03-18 2018-08-08 Arvinas, Inc. Compounds and methods for the enhanced degradation of targeted proteins
WO2016197114A1 (en) 2015-06-05 2016-12-08 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
EP3892272B1 (en) 2016-04-22 2024-07-24 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
KR102570992B1 (ko) * 2016-11-01 2023-08-28 아비나스 오퍼레이션스, 인코포레이티드 타우(Tau)-단백질 표적화 프로탁(PROTAC) 및 관련 사용 방법
CN110291087B (zh) 2016-12-01 2024-07-09 阿尔维纳斯运营股份有限公司 作为雌激素受体降解剂的四氢萘和四氢异喹啉衍生物
US11173211B2 (en) 2016-12-23 2021-11-16 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides
EP3559006A4 (en) 2016-12-23 2021-03-03 Arvinas Operations, Inc. COMPOUNDS AND METHODS FOR TARGETED DEGRADATION OF F TAL LIVER KINASE POLYPEPTIDES
US10723717B2 (en) 2016-12-23 2020-07-28 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of rapidly accelerated fibrosarcoma polypeptides
WO2018119441A1 (en) * 2016-12-23 2018-06-28 Arvinas, Inc. Egfr proteolysis targeting chimeric molecules and associated methods of use
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
US10604506B2 (en) 2017-01-26 2020-03-31 Arvinas Operations, Inc. Modulators of estrogen receptor proteolysis and associated methods of use
IL312367A (en) 2017-01-31 2024-06-01 Arvinas Operations Inc Cereblon ligands and bifunctional compounds comprising the same
EP3579847A4 (en) * 2017-02-08 2020-12-09 Dana Farber Cancer Institute, Inc. MODULAR DEGRADATION OF ENDOGENOUS PROTEIN 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
EP3728251A1 (en) 2017-12-18 2020-10-28 F. Hoffmann-La Roche AG Bifunctional inhibitors with egfr having a e3 ubiquitin ligase moiety
EP3746426A4 (en) 2018-01-29 2021-12-29 Dana Farber Cancer Institute, Inc. Degradation of bruton's tyrosine kinase (btk) by conjugation of btk inhibitors with e3 ligase ligand and methods of use
TW201945357A (zh) 2018-02-05 2019-12-01 瑞士商赫孚孟拉羅股份公司 化合物
WO2019160915A1 (en) 2018-02-14 2019-08-22 Dana-Farber Cancer Institute, Inc. Irak degraders and uses thereof
AU2019225803A1 (en) * 2018-02-20 2020-07-23 Dana-Farber Cancer Institute, Inc. Pharmaceutical combinations of EGFR inhibitors and methods of use thereof
WO2019183523A1 (en) * 2018-03-23 2019-09-26 Genentech, Inc. Hetero-bifunctional degrader compounds and their use as modulators of targeted ubiquination (vhl)
CN112218859B (zh) 2018-04-04 2024-10-29 阿尔维纳斯运营股份有限公司 蛋白水解调节剂及相关使用方法
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
JP7515175B2 (ja) 2018-07-31 2024-07-12 ファイメクス株式会社 複素環化合物
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
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
US12233356B2 (en) 2019-03-21 2025-02-25 Lonza Sales Ag Process for preparing extracellular vesicles
MX2021011242A (es) 2019-03-21 2022-01-19 Codiak Biosciences Inc Conjugados de vesícula extracelular y usos de estos.
EA202192738A1 (ru) 2019-04-12 2022-03-17 С4 Терапьютикс, Инк. Трициклические соединения, обеспечивающие разрушение белка ikaros и белка 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
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
KR20220054347A (ko) 2019-08-26 2022-05-02 아비나스 오퍼레이션스, 인코포레이티드 에스트로겐 수용체 분해제로서의 테트라히드로나프탈렌 유도체로 유방암을 치료하는 방법
JP2022552006A (ja) 2019-10-17 2022-12-14 アルヴィナス・オペレーションズ・インコーポレイテッド Ｂｃｌ６標的化部分に連結されたｅ３ユビキチンリガーゼ結合部分を含有する二官能性分子
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
CA3165168A1 (en) 2019-12-19 2021-06-24 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor
PE20221724A1 (es) 2019-12-20 2022-11-04 C4 Therapeutics Inc Compuestos de isoindolinona e indazol para la degradacion del receptor del factor de crecimiento epidermico (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
WO2022047145A1 (en) 2020-08-28 2022-03-03 Arvinas Operations, Inc. Rapidly accelerating fibrosarcoma protein degrading compounds and associated methods of use
KR102539755B1 (ko) * 2020-09-11 2023-06-05 제이투에이치바이오텍 (주) Egfr 돌연변이 암의 억제용 화합물 및 이들의 의약 용도
AR123492A1 (es) 2020-09-14 2022-12-07 Arvinas Operations Inc Formas cristalinas y amorfas de un compuesto para la degradación dirigida del receptor de estrógeno
US20240241020A1 (en) 2020-09-23 2024-07-18 Lonza Sales Ag 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
MX2023011597A (es) * 2021-04-02 2023-10-30 Univ Michigan Regents Terapia combinada para el tratamiento del cáncer.
MX2023011940A (es) 2021-04-16 2023-12-07 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
WO2023283130A1 (en) 2021-07-04 2023-01-12 Newave Pharmaceutical Inc. Isoquinoline derivatives as mutant egfr modulators and uses thereof
EP4395549A1 (en) 2021-09-01 2024-07-10 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
WO2024054591A1 (en) 2022-09-07 2024-03-14 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
IL322247A (en) 2023-01-26 2025-09-01 Arvinas Operations Inc Cerebellon-based KRAS-disrupting proteins and related uses
WO2024183741A1 (en) * 2023-03-07 2024-09-12 Abogen Biosciences (Shanghai) Co., Ltd. Immunomodulatory therapeutic mrna compositions encoding activating egfr mutation peptides
AR132818A1 (es) 2023-05-31 2025-07-30 Beigene Switzerland Gmbh Compuestos para la degradación de la cinasa egfr
CN121368481A (zh) * 2023-06-29 2026-01-20 丹娜-法伯癌症研究院 用于降解dna甲基转移酶1 (dnmt1)的蛋白水解靶向嵌合体(protacs)的合成和体外表征
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
AU2001295041A1 (en) 2000-09-08 2002-03-22 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
US9765019B2 (en) 2010-06-30 2017-09-19 Brandeis University Small-molecule-targeted protein degradation
CA2823837A1 (en) 2010-12-07 2012-06-14 Yale University Small-molecule hydrophobic tagging of fusion proteins and induced degradation of same
WO2013106646A2 (en) * 2012-01-12 2013-07-18 Yale University Compounds and methods for the inhibition of vcb e3 ubiquitin ligase
CA2861066C (en) * 2012-01-12 2024-01-02 Yale University Compounds and methods for the enhanced degradation of targeted proteins and other polypeptides by an 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
KR20220101015A (ko) * 2014-04-14 2022-07-18 아비나스 오퍼레이션스, 인코포레이티드 단백질분해의 이미드-기초된 조절인자 및 연관된 이용 방법
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
MA40940A (fr) 2014-11-10 2017-09-19 Constellation Pharmaceuticals Inc Pyrrolopyridines substituées utilisées en tant qu'inhibiteurs de bromodomaines
WO2016077375A1 (en) 2014-11-10 2016-05-19 Genentech, Inc. Bromodomain inhibitors and uses thereof
US9694084B2 (en) 2014-12-23 2017-07-04 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
WO2016105518A1 (en) 2014-12-23 2016-06-30 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
WO2016118666A1 (en) 2015-01-20 2016-07-28 Arvinas, Inc. Compounds and methods for the targeted degradation of the androgen receptor
GB201504314D0 (en) 2015-03-13 2015-04-29 Univ Dundee Small molecules
EP3270917A4 (en) 2015-03-18 2018-08-08 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
CN107787320B (zh) 2015-05-22 2020-12-04 拜欧赛里克斯公司 靶向蛋白质的化合物、其组合物、方法和用途
CN108136044B (zh) 2015-06-04 2021-08-10 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
WO2016197114A1 (en) 2015-06-05 2016-12-08 Arvinas, Inc. Tank-binding kinase-1 protacs and associated methods of use
EP3317273B1 (en) * 2015-06-30 2021-12-29 Dana-Farber Cancer Institute, Inc. Inhibitors of egfr and methods of use thereof
WO2017007612A1 (en) 2015-07-07 2017-01-12 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
CN108137507A (zh) 2015-07-10 2018-06-08 阿尔维纳斯股份有限公司 基于mdm2的蛋白水解调节剂和相关的使用方法
CA2988436A1 (en) 2015-07-13 2017-01-19 Arvinas, Inc. Alanine-based modulators of proteolysis and associated methods of use
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
WO2017030814A1 (en) 2015-08-19 2017-02-23 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
JP7037500B2 (ja) 2016-04-06 2022-03-16 ザ リージェンツ オブ ザ ユニヴァシティ オブ ミシガン Ｍｄｍ２タンパク質分解剤
KR20180132861A (ko) 2016-04-12 2018-12-12 더 리젠츠 오브 더 유니버시티 오브 미시간 Bet 단백질 분해제
EP3892272B1 (en) 2016-04-22 2024-07-24 Dana-Farber Cancer Institute, Inc. Bifunctional molecules for degradation of egfr and methods of use
ES2990061T3 (es) 2016-05-10 2024-11-28 C4 Therapeutics Inc Degronímeros espirocíclicos para la degradación de proteínas diana
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
CN109562107A (zh) 2016-05-10 2019-04-02 C4医药公司 用于靶蛋白降解的杂环降解决定子体
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
CA3024556A1 (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
ES2858151T3 (es) 2016-05-20 2021-09-29 Hoffmann La Roche Conjugados de PROTAC-anticuerpo y procedimientos de uso
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
WO2018119441A1 (en) * 2016-12-23 2018-06-28 Arvinas, Inc. Egfr proteolysis targeting chimeric molecules and associated methods of use

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EP3445357A1 (en) 2019-02-27
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EP3445357B1 (en) 2021-05-26
US11161842B2 (en) 2021-11-02
AU2017254713B2 (en) 2020-11-19
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