CA3021358A1 - Bifunctional molecules for degradation of egfr and methods of use - Google Patents
Bifunctional molecules for degradation of egfr and methods of use Download PDFInfo
- Publication number
- CA3021358A1 CA3021358A1 CA3021358A CA3021358A CA3021358A1 CA 3021358 A1 CA3021358 A1 CA 3021358A1 CA 3021358 A CA3021358 A CA 3021358A CA 3021358 A CA3021358 A CA 3021358A CA 3021358 A1 CA3021358 A1 CA 3021358A1
- Authority
- CA
- Canada
- Prior art keywords
- cancer
- formula
- egfr
- bifunctional compound
- alkyl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 0 CC(*)=*(C)N*C=* Chemical compound CC(*)=*(C)N*C=* 0.000 description 2
Classifications
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- 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)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| 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 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA3021358A1 true CA3021358A1 (en) | 2017-10-26 |
Family
ID=60116448
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA3021358A Pending CA3021358A1 (en) | 2016-04-22 | 2017-04-21 | Bifunctional molecules for degradation of egfr and methods of use |
Country Status (7)
| Country | Link |
|---|---|
| US (3) | US10450310B2 (enExample) |
| EP (2) | EP3445357B1 (enExample) |
| JP (1) | JP6968823B2 (enExample) |
| CN (1) | CN109475528B (enExample) |
| AU (1) | AU2017254713C1 (enExample) |
| CA (1) | CA3021358A1 (enExample) |
| WO (1) | WO2017185036A1 (enExample) |
Families Citing this family (78)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| 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 |
| HK1249058A1 (zh) | 2015-03-18 | 2018-10-26 | Arvinas, Inc. | 用於增强靶向蛋白质降解的化合物和方法 |
| 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 |
| 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 |
| JP6968823B2 (ja) | 2016-04-22 | 2021-11-17 | 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 | Ｅｇｆｒの分解のための二官能性分子、及び使用方法 |
| WO2018053354A1 (en) | 2016-09-15 | 2018-03-22 | 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 |
| KR20230127371A (ko) | 2016-11-01 | 2023-08-31 | 아비나스 오퍼레이션스, 인코포레이티드 | 타우(Tau)-단백질 표적화 프로탁(PROTAC) 및 관련 사용 방법 |
| IL297717A (en) | 2016-12-01 | 2022-12-01 | Arvinas Operations Inc | History of tetrahydronaphthalene and tetrahydroisoquinoline as estrogen receptor antagonists |
| WO2018118598A1 (en) | 2016-12-23 | 2018-06-28 | Arvinas, Inc. | Compounds and methods for the targeted degradation of fetal liver kinase polypeptides |
| US11173211B2 (en) | 2016-12-23 | 2021-11-16 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides |
| MX2019007649A (es) | 2016-12-23 | 2019-09-10 | Arvinas Operations Inc | Compuestos y metodos para la degradacion dirigida de polipeptidos de fibrosarcoma acelerado rapidamente. |
| 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 |
| IL300417A (en) | 2017-01-26 | 2023-04-01 | Arvinas Operations Inc | Bifunctional benzothiophene compounds, preparations containing them and their use in therapy |
| EP3577109A4 (en) | 2017-01-31 | 2020-11-18 | Arvinas Operations, Inc. | CEREMONY LIGANDS AND BIFUNCTIONAL COMPOUNDS CONTAINING THEM |
| CA3053008A1 (en) | 2017-02-08 | 2018-08-16 | Dana-Farber Cancer Institute, Inc. | Tunable endogenous protein degradation with heterobifunctional compounds |
| US11065231B2 (en) | 2017-11-17 | 2021-07-20 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of interleukin-1 receptor- associated kinase 4 polypeptides |
| CN111491933A (zh) * | 2017-12-18 | 2020-08-04 | 豪夫迈·罗氏有限公司 | 具有e3泛素连接酶部分的egfr双功能抑制剂 |
| CA3085457C (en) | 2018-01-29 | 2023-05-23 | 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 |
| EP3752504A4 (en) | 2018-02-14 | 2021-06-09 | Dana Farber Cancer Institute, Inc. | IRAQ DEGRADER AND USES THEREOF |
| CA3088972A1 (en) * | 2018-02-20 | 2019-08-29 | 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) |
| JP7720698B2 (ja) | 2018-04-04 | 2025-08-08 | アルビナス・オペレーションズ・インコーポレイテッド | タンパク質分解の調節因子および関連する使用方法 |
| 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 |
| 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 |
| US11667621B2 (en) | 2018-06-11 | 2023-06-06 | Stevens Institute Of Technology | Antiestrogen compounds |
| EP3831811A4 (en) | 2018-07-31 | 2022-04-20 | Fimecs, Inc. | HETEROCYCLIC COMPOUND |
| 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 |
| WO2020069125A1 (en) * | 2018-09-28 | 2020-04-02 | Dana-Farber Cancer Institute, Inc. | Degraders of hepatitis c virus ns3/4a protein |
| CA3119343C (en) | 2018-11-13 | 2024-01-16 | Biotheryx, Inc. | Substituted isoindolinones |
| US12233356B2 (en) | 2019-03-21 | 2025-02-25 | Lonza Sales Ag | Process for preparing extracellular vesicles |
| US20240108747A1 (en) | 2019-03-21 | 2024-04-04 | Lonza Sales Ag | Extracellular vesicle conjugates and uses thereof |
| KR20210152515A (ko) | 2019-04-12 | 2021-12-15 | 씨4 테라퓨틱스, 인코포레이티드 | 이카로스 및 아이올로스의 트리시클릭 분해제 |
| 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 |
| WO2020257607A1 (en) | 2019-06-21 | 2020-12-24 | Dana-Farber Cancer Institute, Inc. | Allosteric egfr inhibitors and methods of use thereof |
| US11912699B2 (en) | 2019-07-17 | 2024-02-27 | Arvinas Operations, Inc. | Tau-protein targeting compounds and associated |
| CN112321566B (zh) * | 2019-08-05 | 2022-06-10 | 上海科技大学 | Egfr蛋白降解剂及其抗肿瘤应用 |
| EP4021450B1 (en) | 2019-08-26 | 2025-11-05 | Arvinas Operations, Inc. | Methods of treating breast cancer with tetrahydronaphthalene derivatives as estrogen receptor degraders |
| AU2020368542B2 (en) | 2019-10-17 | 2024-02-29 | 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 |
| MX2022007659A (es) | 2019-12-20 | 2022-07-19 | 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 |
| EP4204418A1 (en) | 2020-08-28 | 2023-07-05 | 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 |
| EP4211128A1 (en) | 2020-09-14 | 2023-07-19 | Arvinas Operations, Inc. | Crystalline forms of a compound for the targeted degradation of estrogen receptor |
| 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 |
| WO2022212806A1 (en) * | 2021-04-02 | 2022-10-06 | The Regents Of The University Of Michigan | Combination therapy for cancer treatment |
| EP4323352A1 (en) | 2021-04-16 | 2024-02-21 | Arvinas Operations, Inc. | Modulators of bcl6 proteolysis and associated methods of use |
| 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 |
| 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 |
| TW202432544A (zh) | 2022-09-07 | 2024-08-16 | 美商亞文納營運公司 | 快速加速纖維肉瘤降解化合物及相關使用方法 |
| 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 |
| WO2024183741A1 (en) * | 2023-03-07 | 2024-09-12 | Abogen Biosciences (Shanghai) Co., Ltd. | Immunomodulatory therapeutic mrna compositions encoding activating egfr mutation peptides |
| WO2024246838A1 (en) | 2023-05-31 | 2024-12-05 | Beigene Switzerland Gmbh | Compounds for the degradation of egfr kinase |
| 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)
| 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 |
| WO2002020740A2 (en) | 2000-09-08 | 2002-03-14 | 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 |
| AU2011272860A1 (en) | 2010-06-30 | 2013-02-07 | Brandeis University | Small-molecule-targeted protein degradation |
| EP2649099A4 (en) | 2010-12-07 | 2016-10-19 | Univ Yale | SMALL MOLECULAR HYDROPHOBIC LABELING OF FUSION PROTEINS AND INDUCED REMOVAL FROM THIS |
| WO2013106646A2 (en) * | 2012-01-12 | 2013-07-18 | Yale University | Compounds and methods for the inhibition of vcb e3 ubiquitin ligase |
| KR102438072B1 (ko) | 2012-01-12 | 2022-08-31 | 예일 유니버시티 | E3 유비퀴틴 리가아제에 의한 표적 단백질 및 다른 폴리펩티드의 증진된 분해를 위한 화합물 및 방법 |
| EP2846784A4 (en) | 2012-05-11 | 2016-03-09 | Univ Yale | COMPOUNDS FOR PROMOTING PROTEIN REMOVAL AND PROCESS THEREFOR |
| US9758522B2 (en) | 2012-10-19 | 2017-09-12 | 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 |
| KR20250127179A (ko) | 2014-04-14 | 2025-08-26 | 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 |
| 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 |
| 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 |
| US11352351B2 (en) | 2015-01-20 | 2022-06-07 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of androgen receptor |
| GB201504314D0 (en) | 2015-03-13 | 2015-04-29 | Univ Dundee | Small molecules |
| HK1249058A1 (zh) | 2015-03-18 | 2018-10-26 | Arvinas, Inc. | 用於增强靶向蛋白质降解的化合物和方法 |
| GB201506871D0 (en) | 2015-04-22 | 2015-06-03 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| RU2694895C2 (ru) | 2015-05-22 | 2019-07-18 | Биотерикс, Инк. | Нацеленные на белки соединения, их композиции, способы и применения |
| WO2016197032A1 (en) | 2015-06-04 | 2016-12-08 | Arvinas, Inc. | Imide-based modulators of proteolysis and associated methods of use |
| WO2016197114A1 (en) | 2015-06-05 | 2016-12-08 | Arvinas, Inc. | Tank-binding kinase-1 protacs and associated methods of use |
| US10385019B2 (en) * | 2015-06-30 | 2019-08-20 | 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 |
| CA2988430A1 (en) | 2015-07-10 | 2017-01-19 | Arvinas, Inc. | Mdm2-based modulators of proteolysis and associated methods of use |
| RU2018105094A (ru) | 2015-07-13 | 2019-08-14 | Арвинас, Инк. | Модуляторы протеолиза на основе аланина и связанные с ними способы применения |
| WO2017024317A2 (en) | 2015-08-06 | 2017-02-09 | Dana-Farber Cancer Institute, Inc. | Methods to induce targeted protein degradation through bifunctional molecules |
| EP3331905B1 (en) | 2015-08-06 | 2022-10-05 | Dana-Farber Cancer Institute, Inc. | Targeted protein degradation to attenuate adoptive t-cell therapy associated adverse inflammatory responses |
| US10772962B2 (en) | 2015-08-19 | 2020-09-15 | Arvinas Operations, 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 |
| KR102387316B1 (ko) | 2016-04-06 | 2022-04-15 | 더 리젠츠 오브 더 유니버시티 오브 미시간 | Mdm2 단백질 분해제 |
| RU2752677C2 (ru) | 2016-04-12 | 2021-07-29 | Дзе Риджентс Оф Дзе Юниверсити Оф Мичиган | Деструкторы белка вет |
| JP6968823B2 (ja) | 2016-04-22 | 2021-11-17 | 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 | Ｅｇｆｒの分解のための二官能性分子、及び使用方法 |
| EP4491236A3 (en) | 2016-05-10 | 2025-04-02 | C4 Therapeutics, Inc. | Heterocyclic degronimers for target protein degradation |
| WO2017197036A1 (en) | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | Spirocyclic degronimers for target protein degradation |
| EP3455218A4 (en) | 2016-05-10 | 2019-12-18 | C4 Therapeutics, Inc. | C3 CARBON-BASED GLUTARIMIDE DEGRONIMERS FOR TARGET PROTEIN REDUCTION |
| EP3455219A4 (en) | 2016-05-10 | 2019-12-18 | C4 Therapeutics, Inc. | AMINE-RELATED C3-GLUTARIMIDE DEGRONIMERS FOR TARGET PROTEIN REDUCTION |
| WO2017197056A1 (en) | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | Bromodomain targeting degronimers for target protein degradation |
| US11883381B2 (en) | 2016-05-12 | 2024-01-30 | 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 |
| PL3458101T3 (pl) | 2016-05-20 | 2021-05-31 | F. Hoffmann-La Roche Ag | Koniugaty PROTAC-przeciwciało i sposoby ich stosowania |
| 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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2017
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- 2017-04-21 CA CA3021358A patent/CA3021358A1/en active Pending
- 2017-04-21 EP EP17786758.7A patent/EP3445357B1/en active Active
- 2017-04-21 CN CN201780025159.0A patent/CN109475528B/zh active Active
- 2017-04-21 AU AU2017254713A patent/AU2017254713C1/en active Active
- 2017-04-21 WO PCT/US2017/028950 patent/WO2017185036A1/en not_active Ceased
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2018
- 2018-10-17 US US16/163,254 patent/US10450310B2/en active Active
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2019
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| EP3445357A1 (en) | 2019-02-27 |
| AU2017254713C1 (en) | 2021-04-29 |
| JP6968823B2 (ja) | 2021-11-17 |
| WO2017185036A1 (en) | 2017-10-26 |
| US20190106417A1 (en) | 2019-04-11 |
| US10450310B2 (en) | 2019-10-22 |
| EP3445357A4 (en) | 2019-11-06 |
| EP3445357B1 (en) | 2021-05-26 |
| CN109475528A (zh) | 2019-03-15 |
| AU2017254713B2 (en) | 2020-11-19 |
| US20220017510A1 (en) | 2022-01-20 |
| US11161842B2 (en) | 2021-11-02 |
| AU2017254713A1 (en) | 2018-10-18 |
| EP3892272A1 (en) | 2021-10-13 |
| JP2019519476A (ja) | 2019-07-11 |
| US20200102298A1 (en) | 2020-04-02 |
| CN109475528B (zh) | 2022-01-11 |
| EP3892272B1 (en) | 2024-07-24 |
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