JP2022540935A5 - - Google Patents

Info

Publication number
JP2022540935A5
JP2022540935A5 JP2022502929A JP2022502929A JP2022540935A5 JP 2022540935 A5 JP2022540935 A5 JP 2022540935A5 JP 2022502929 A JP2022502929 A JP 2022502929A JP 2022502929 A JP2022502929 A JP 2022502929A JP 2022540935 A5 JP2022540935 A5 JP 2022540935A5
Authority
JP
Japan
Prior art keywords
disease
tau
compound
disorder
pharmaceutically acceptable
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.)
Granted
Application number
JP2022502929A
Other languages
English (en)
Japanese (ja)
Other versions
JP7548992B2 (ja
JP2022540935A (ja
Filing date
Publication date
Application filed filed Critical
Priority claimed from PCT/US2020/042645 external-priority patent/WO2021011913A1/en
Publication of JP2022540935A publication Critical patent/JP2022540935A/ja
Publication of JP2022540935A5 publication Critical patent/JP2022540935A5/ja
Priority to JP2024146579A priority Critical patent/JP2024178191A/ja
Application granted granted Critical
Publication of JP7548992B2 publication Critical patent/JP7548992B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

JP2022502929A 2019-07-17 2020-07-17 タウタンパク質標的化化合物および関連する使用方法 Active JP7548992B2 (ja)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP2024146579A JP2024178191A (ja) 2019-07-17 2024-08-28 タウタンパク質標的化化合物および関連する使用方法

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962875500P 2019-07-17 2019-07-17
US62/875,500 2019-07-17
PCT/US2020/042645 WO2021011913A1 (en) 2019-07-17 2020-07-17 Tau-protein targeting compounds and associated methods of use

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2024146579A Division JP2024178191A (ja) 2019-07-17 2024-08-28 タウタンパク質標的化化合物および関連する使用方法

Publications (3)

Publication Number Publication Date
JP2022540935A JP2022540935A (ja) 2022-09-20
JP2022540935A5 true JP2022540935A5 (https=) 2023-07-25
JP7548992B2 JP7548992B2 (ja) 2024-09-10

Family

ID=71996063

Family Applications (2)

Application Number Title Priority Date Filing Date
JP2022502929A Active JP7548992B2 (ja) 2019-07-17 2020-07-17 タウタンパク質標的化化合物および関連する使用方法
JP2024146579A Pending JP2024178191A (ja) 2019-07-17 2024-08-28 タウタンパク質標的化化合物および関連する使用方法

Family Applications After (1)

Application Number Title Priority Date Filing Date
JP2024146579A Pending JP2024178191A (ja) 2019-07-17 2024-08-28 タウタンパク質標的化化合物および関連する使用方法

Country Status (5)

Country Link
US (2) US11912699B2 (https=)
EP (1) EP3999182A1 (https=)
JP (2) JP7548992B2 (https=)
CN (2) CN119954801A (https=)
WO (1) WO2021011913A1 (https=)

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK2767532T3 (en) 2012-12-21 2016-09-12 Nat Inst For Quantum And Radiological Science And Tech New connection for reproduction of tau protein heavy in the brain.
WO2019195609A2 (en) 2018-04-04 2019-10-10 Arvinas Operations, Inc. Modulators of proteolysis and associated methods of use
TW201946624A (zh) 2018-05-09 2019-12-16 新旭生技股份有限公司 雜芳基化合物及其用途
EP3999182A1 (en) * 2019-07-17 2022-05-25 Arvinas Operations, Inc. Tau-protein targeting compounds and associated methods of use
CN114728071B (zh) 2019-11-13 2024-12-06 新旭生技股份有限公司 用于降解tau蛋白聚集体的化合物及其用途
EP4121046A4 (en) * 2020-03-18 2024-04-24 Dana-Farber Cancer Institute, Inc. Targeted degraders of aberrant tau based on the pet tracer pbb3
AU2021337466A1 (en) 2020-09-01 2023-03-30 Enveric Biosciences Canada Inc. Halogenated psilocybin derivatives and methods of using
AU2022207648A1 (en) 2021-01-13 2023-07-27 Monte Rosa Therapeutics Ag Isoindolinone compounds
WO2022251614A1 (en) * 2021-05-28 2022-12-01 Beth Israel Deaconess Medical Center, Inc. Protacs with transcription factor targeting moieties
CA3226162A1 (en) 2021-07-09 2023-01-12 Plexium, Inc. Aryl compounds and pharmaceutical compositions that modulate ikzf2
CA3235512A1 (en) * 2021-10-22 2023-04-27 Xiaobao Yang Crbn e3 ligase ligand compound, protein degrader developed based thereon and their applications
CN115385908B (zh) * 2022-07-26 2024-04-12 阿茨可利(杭州)医学科技有限公司 靶向促进tau蛋白去磷酸化的小分子嵌合体及其应用
CN115028679B (zh) * 2022-08-11 2022-11-15 深圳湾实验室 一种具有Cyclophilin A降解活性的PROTAC化合物及其制备方法与应用
WO2024097948A1 (en) 2022-11-04 2024-05-10 Roivant Discovery, Inc. Degraders of mdm2 and uses thereof
WO2024140638A1 (zh) * 2022-12-27 2024-07-04 标新生物医药科技(上海)有限公司 基于硫/氧取代戊二酰亚胺基异吲哚啉酮骨架的化合物及其应用
US12448399B2 (en) 2023-01-26 2025-10-21 Arvinas Operations, Inc. Cereblon-based KRAS degrading PROTACs and uses related thereto
US20240327381A1 (en) * 2023-02-08 2024-10-03 Celgene Corporation Compounds and Compositions for Selective Degradation of Engineered Proteins
CN116283512B (zh) * 2023-02-24 2025-04-25 博诺康源(北京)药业科技有限公司 一种合成维兰特罗及其盐的方法
WO2024182633A2 (en) * 2023-03-01 2024-09-06 The Regents Of The University Of California Targeted dephosphorylation of tau
EP4720071A1 (en) 2023-05-31 2026-04-08 Beone Medicines I GmbH Compounds for the degradation of egfr kinase
WO2025011624A1 (en) * 2023-07-11 2025-01-16 Etern Biopharma (Shanghai) Co., Ltd. Bifunctional compounds for androgen receptor degradation and methods of use
WO2025085387A1 (en) * 2023-10-16 2025-04-24 University Of Pittsburgh - Of The Commonwealth System Of Higher Education Substituted-alkenyl-indazoles for imaging aggregated tau in tauopathies
CN119285633A (zh) * 2024-10-11 2025-01-10 中国药科大学 一种靶向降解Tau蛋白的疏水标签化合物及其制备和应用

Family Cites Families (144)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4522811A (en) 1982-07-08 1985-06-11 Syntex (U.S.A.) Inc. Serial injection of muramyldipeptides and liposomes enhances the anti-infective activity of muramyldipeptides
CA2287387C (en) 1997-05-14 2010-02-16 Sloan-Kettering Institute For Cancer Research Methods and compositions for destruction of selected proteins
US6306663B1 (en) 1999-02-12 2001-10-23 Proteinex, Inc. Controlling protein levels in eucaryotic organisms
EP1176959B1 (en) 1999-05-05 2006-03-08 Merck & Co., Inc. Novel prolines as antimicrobial agents
US7208157B2 (en) 2000-09-08 2007-04-24 California Institute Of Technology Proteolysis targeting chimeric pharmaceutical
WO2002020740A2 (en) 2000-09-08 2002-03-14 California Institute Of Technology Proteolysis targeting chimeric pharmaceutical
US7091353B2 (en) 2000-12-27 2006-08-15 Celgene Corporation Isoindole-imide compounds, compositions, and uses thereof
JP2005507363A (ja) 2001-02-16 2005-03-17 イー・アイ・デュポン・ドウ・ヌムール・アンド・カンパニー 血管新生阻害トリペプチド、組成物およびそれらの使用方法
GB0106953D0 (en) 2001-03-20 2001-05-09 Univ Aberdeen Neufofibrillary labels
HN2002000136A (es) 2001-06-11 2003-07-31 Basf Ag Inhibidores de la proteasa del virus hiv, compuestos que contienen a los mismos, sus usos farmaceuticos y los materiales para su sintesis
US7030141B2 (en) 2001-11-29 2006-04-18 Christopher Franklin Bigge Inhibitors of factor Xa and other serine proteases involved in the coagulation cascade
WO2004005248A1 (en) 2002-07-02 2004-01-15 Novartis Ag Peptide inhibitors of smac protein binding to inhibitor of apoptosis proteins (iap)
WO2005016326A2 (en) 2003-07-11 2005-02-24 The Government Of The United States Of America As Represented By The Secretary Of The Department Of Health And Human Services Analogs of thalidomide as potential angiogenesis inhibitors
BRPI0506883A (pt) 2004-01-16 2007-05-29 Univ Michigan miméticos de smac conformacionalmente comprimidos e seus usos
AU2005228950B2 (en) 2004-03-23 2012-02-02 Genentech, Inc. Azabicyclo-octane inhibitors of IAP
DK2253614T3 (da) 2004-04-07 2013-01-07 Novartis Ag IAP-inhibitorer
KR100984459B1 (ko) 2004-07-02 2010-09-29 제넨테크, 인크. Iap의 억제제
DK1836201T4 (da) 2004-12-20 2013-11-11 Genentech Inc Pyrrolidininhibitorer af IAP.
MX2007010371A (es) 2005-02-25 2008-01-11 Tetralogic Pharmaceuticals Inhibidores dimericos iap.
CN100383139C (zh) 2005-04-07 2008-04-23 天津和美生物技术有限公司 可抑制细胞释放肿瘤坏死因子的哌啶-2,6-二酮衍生物
WO2006113942A2 (en) 2005-04-20 2006-10-26 Schering Corporation Method of inhibiting cathepsin activity
UA91560C2 (ru) 2005-08-31 2010-08-10 Селджин Корпорэйшн Соединения ряда изоиндолимидов, их композиция и применение
AU2007226715A1 (en) 2006-03-03 2007-09-20 Novartis Ag N-formyl hydroxylamine compounds
WO2007101347A1 (en) 2006-03-07 2007-09-13 Aegera Therapeutics Inc. Bir domain binding compounds
CA2644143C (en) 2006-04-05 2013-10-01 Novartis Ag Combinations comprising bcr-abl/c-kit/pdgf-r tk inhibitors for treating cancer
NZ572531A (en) 2006-05-05 2011-09-30 Univ Michigan Bivalent smac mimetics and the uses thereof
AU2007275415A1 (en) 2006-07-20 2008-01-24 Ligand Pharmaceuticals Incorporated Proline urea CCR1 antagonists for the treatment of autoimmune diseases or inflammation
US20100056495A1 (en) 2006-07-24 2010-03-04 Tetralogic Pharmaceuticals Corporation Dimeric iap inhibitors
CL2007002513A1 (es) 2006-08-30 2008-04-04 Celgene Corp Soc Organizada Ba Compuestos derivados de isoindolina sustituidos, compuestos intermediarios; composicion farmaceutica; y uso en el tratamiento y prevencion de enfermedades tales como cancer, dolor, degeneracion macular, entre otras.
RU2448101C2 (ru) 2006-08-30 2012-04-20 Селджин Корпорейшн 5-замещенные изоиндолиновые соединения
US8877780B2 (en) 2006-08-30 2014-11-04 Celgene Corporation 5-substituted isoindoline compounds
CA2668286C (en) 2006-11-03 2014-09-16 Pharmacyclics, Inc. Bruton's tyrosine kinase activity probe and method of using
WO2008109057A1 (en) 2007-03-02 2008-09-12 Dana-Farber Cancer Institute, Inc. Organic compounds and their uses
JP5454943B2 (ja) 2007-04-12 2014-03-26 ジョイアント ファーマスーティカルズ、インク. 抗癌剤として有用なsmac模倣二量体及び三量体
WO2008128171A2 (en) 2007-04-13 2008-10-23 The Regents Of The University Of Michigan Diazo bicyclic smac mimetics and the uses thereof
WO2008134679A1 (en) 2007-04-30 2008-11-06 Genentech, Inc. Inhibitors of iap
US20100203012A1 (en) 2007-05-30 2010-08-12 Aegera Therapeutics, Inc. Iap bir domain binding compounds
US8415340B2 (en) 2007-07-25 2013-04-09 Bristol-Myers Squibb Company Triazine kinase inhibitors
EP2058312A1 (en) 2007-11-09 2009-05-13 Universita' degli Studi di Milano SMAC mimetic compounds as apoptosis inducers
PT2358697E (pt) 2008-10-29 2016-02-03 Celgene Corp Compostos de isoindolina para utilização no tratamento do cancro
US8691187B2 (en) 2009-03-23 2014-04-08 Eli Lilly And Company Imaging agents for detecting neurological disorders
WO2010141805A1 (en) 2009-06-05 2010-12-09 Janssen Pharmaceutica Nv Heterocyclic amides as modulators of trpa1
AU2010273220B2 (en) 2009-07-13 2015-10-15 President And Fellows Of Harvard College Bifunctional stapled polypeptides and uses thereof
US8551955B2 (en) 2009-10-28 2013-10-08 Joyant Pharmaceuticals, Inc. Dimeric Smac mimetics
PL3202460T3 (pl) 2010-02-11 2019-12-31 Celgene Corporation Pochodne arylometoksyizoindoliny i zawierające je kompozycje oraz sposoby ich zastosowania
US8198300B2 (en) 2010-04-29 2012-06-12 Universidad De Chile Method for preventing tau protein aggregation and treating Alzheimer's disease with a quinoline derivative compound
CN103153335A (zh) 2010-06-30 2013-06-12 布兰代斯大学 小分子靶定的蛋白质降解
WO2012040527A2 (en) 2010-09-24 2012-03-29 The Regents Of The University Of Michigan Deubiquitinase inhibitors and methods for use of the same
AR084070A1 (es) 2010-12-02 2013-04-17 Constellation Pharmaceuticals Inc Inhibidores del bromodominio y usos de los mismos
CA2823837A1 (en) 2010-12-07 2012-06-14 Yale University Small-molecule hydrophobic tagging of fusion proteins and induced degradation of same
WO2012090104A1 (en) 2010-12-31 2012-07-05 Kareus Therapeutics, Sa Methods and compositions for designing novel conjugate therapeutics
AU2012249491B2 (en) 2011-04-29 2016-12-15 Celgene Corporation Methods for the treatment of cancer and inflammatory diseases using cereblon as a predictor
EP2776409B1 (en) 2011-11-09 2016-02-03 Ensemble Therapeutics Corporation Macrocyclic compounds for inhibition of inhibitors of apoptosis
WO2013071039A1 (en) 2011-11-09 2013-05-16 Ensemble Therapeutics Macrocyclic compounds for inhibition of inhibitors of apoptosis
WO2013106646A2 (en) 2012-01-12 2013-07-18 Yale University Compounds and methods for the inhibition of vcb e3 ubiquitin ligase
KR102668696B1 (ko) 2012-01-12 2024-05-29 예일 유니버시티 E3 유비퀴틴 리가아제에 의한 표적 단백질 및 다른 폴리펩티드의 증진된 분해를 위한 화합물 및 방법
WO2013170147A1 (en) 2012-05-11 2013-11-14 Yale University Compounds useful for promoting protein degradation and methods using same
CN104781234A (zh) 2012-05-22 2015-07-15 伊莱利利公司 用于检测神经功能障碍的基于咔啉和咔唑的成像剂
US9345740B2 (en) 2012-07-10 2016-05-24 Bristol-Myers Squibb Company IAP antagonists
US9453048B2 (en) 2012-08-09 2016-09-27 Bristol-Myers Squibb Company IAP antagonists
US9783573B2 (en) 2012-09-18 2017-10-10 Bristol-Myers Squibb Company IAP antagonists
US9603889B2 (en) 2012-10-02 2017-03-28 Bristol-Myers Squibb Company IAP antagonists
GB201218864D0 (en) 2012-10-19 2012-12-05 Astex Therapeutics Ltd Bicyclic heterocycle compounds and their uses in therapy
CA2930030A1 (en) 2012-11-09 2014-05-15 Ensemble Therapeutics Corporation Macrocyclic compounds for inhibition of inhibitors of apoptosis
GB201311910D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel Compounds
NL2011274C2 (en) 2013-08-06 2015-02-09 Illumicare Ip B V 51 Groundbreaking platform technology for specific binding to necrotic cells.
GB201311891D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compound
GB201311888D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compounds
US9637518B2 (en) 2013-07-12 2017-05-02 Bristol-Myers Squibb Company IAP antagonists
WO2015110263A1 (en) 2014-01-21 2015-07-30 Ac Immune Sa Carbazole and carboline compounds for use in the diagnosis, treatment, alleviation or prevention of disorders associated with amyloid or amyolid-like proteins
US20180228907A1 (en) 2014-04-14 2018-08-16 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same
US20160058872A1 (en) 2014-04-14 2016-03-03 Arvinas, Inc. Imide-based modulators of proteolysis and associated methods of use
RU2738833C9 (ru) 2014-04-14 2022-02-28 Арвинас, Оперэйшнз, Инк. Имидные модуляторы протеолиза и способы их применения
HUE053939T2 (hu) 2014-05-13 2021-08-30 Hoffmann La Roche Deuterált heterociklikus vegyületek és képalkotó kontrasztanyagként való használatuk
TW201613916A (en) 2014-06-03 2016-04-16 Gilead Sciences Inc TANK-binding kinase inhibitor compounds
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
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
JP6817962B2 (ja) 2015-01-20 2021-01-20 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. ターゲティングされたアンドロゲン受容体分解のための化合物および方法
US12312316B2 (en) 2015-01-20 2025-05-27 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor
EA036518B1 (ru) 2015-02-02 2020-11-18 Юсб Байофарма Спрл Производные 9h-пирролодипиридина
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
GB201506872D0 (en) 2015-04-22 2015-06-03 Ge Oil & Gas Uk Ltd Novel compounds
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
EP3319944A4 (en) 2015-07-10 2019-04-24 Arvinas, Inc. MDM2-BASED MODULATORS OF PROTEOLYSIS AND RELATED USE METHODS
BR112017028269A2 (pt) 2015-07-13 2018-09-04 Arvinas Inc composto, composição farmacêutica, uso de uma quantidade efetiva de um composto, estado ou condição de doença, e, método para identificar um composto.
WO2017024318A1 (en) 2015-08-06 2017-02-09 Dana-Farber Cancer Institute, Inc. Targeted protein degradation to attenuate adoptive t-cell therapy associated adverse inflammatory responses
WO2017024317A2 (en) 2015-08-06 2017-02-09 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
US10772962B2 (en) 2015-08-19 2020-09-15 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of bromodomain-containing proteins
GB201516243D0 (en) 2015-09-14 2015-10-28 Glaxosmithkline Ip Dev Ltd Novel compounds
BR112018008918A8 (pt) 2015-11-02 2019-02-26 Univ Yale compostos de quimera proteólise dirigida e métodos para preparação e uso dos mesmos
WO2017117474A1 (en) 2015-12-30 2017-07-06 Dana-Farber Cancer Institute, Inc. Bifunctional compounds for her3 degradation and methods of use
WO2017117473A1 (en) 2015-12-30 2017-07-06 Dana-Farber Cancer Institute, Inc. Bifunctional molescules for her3 degradation and methods of use
BR112018068906A2 (pt) 2016-03-16 2019-01-22 H. Lee Moffitt Cancer Center And Research Institute, Inc. composição, método, método de redução de risco, prevenção ou tratamento de um indivíduo que tem uma doença ou distúrbio autoimune, método de indução de degradação de uma proteína-alvo numa célula, método para reduzir o risco, prevenir ou tratar um estado da doença ou afecção num paciente em que a atividade proteica desregulada é responsável pelo referido estado da doença ou afecção, método para reduzir o risco, prevenir ou tratar câncer num indivíduo e método de tratamento de uma doença ou distúrbio genético num indivíduo
US20170281784A1 (en) 2016-04-05 2017-10-05 Arvinas, Inc. Protein-protein interaction inducing technology
US10759808B2 (en) 2016-04-06 2020-09-01 The Regents Of The University Of Michigan Monofunctional intermediates for ligand-dependent target protein degradation
SG11201808728QA (en) 2016-04-06 2018-11-29 Univ Michigan Regents Mdm2 protein degraders
CN109152933B (zh) * 2016-04-21 2022-12-02 生物风险投资有限责任公司 诱导抗细胞凋亡bcl-2家族蛋白的降解的化合物及其用途
AU2017254713C1 (en) 2016-04-22 2021-04-29 Dana-Farber Cancer Institute, Inc. Bifunctional molecules for degradation of EGFR and methods of use
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
EP3445765A4 (en) 2016-04-22 2019-09-18 Dana Farber Cancer Institute, Inc. DECREASE OF CYCLINE-DEPENDENT KINASE 4/6 (CDK4 / 6) BY CONJUGATION OF CDK4 / 6 INHIBITORS WITH E3-LIGASE LIGANDS 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
WO2017197056A1 (en) 2016-05-10 2017-11-16 C4 Therapeutics, Inc. Bromodomain targeting 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
EP3454856B1 (en) 2016-05-10 2024-09-11 C4 Therapeutics, Inc. Heterocyclic degronimers for target protein degradation
GB201610147D0 (en) 2016-06-10 2016-07-27 Glaxosmithkline Ip Dev Ltd Novel compounds
WO2017223415A1 (en) 2016-06-23 2017-12-28 Dana-Farber Cancer Institute, Inc. Degradation of tripartite motif-containing protein 24 (trim24) by conjugation of trim24 inhibitors with e3 ligase ligand and methods of use
WO2017223452A1 (en) 2016-06-23 2017-12-28 Dana-Farber Cancer Institute, Inc. Degradation of bromodomain-containing protein 9 (brd9) by conjugation of brd9 inhibitors with e3 ligase ligand and methods of use
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
CA3036834A1 (en) 2016-09-13 2018-03-22 The Regents Of The University Of Michigan Fused 1,4-oxazepines as bet protein degraders
CA3036841A1 (en) 2016-09-13 2018-03-22 The Regents Of The University Of Michigan Fused 1,4-diazepines as bet protein degraders
US20180072711A1 (en) 2016-09-15 2018-03-15 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
CN110506039A (zh) 2016-10-11 2019-11-26 阿尔维纳斯股份有限公司 用于雄激素受体靶向降解的化合物和方法
MX2019005007A (es) 2016-11-01 2019-07-18 Arvinas Inc Protac dirigidos a la proteína tau y métodos asociados de uso.
US10925868B2 (en) 2016-11-10 2021-02-23 Dana-Farber Cancer Institute, Inc. Degradation of protein kinases by conjugation of protein kinase inhibitors with E3 ligase ligand and methods of use
WO2018098280A1 (en) 2016-11-22 2018-05-31 Dana-Farber Cancer Institute, Inc. Degradation of protein kinases by conjugation of protein kinase inhibitors with e3 ligase ligand and methods of use
CA3042297A1 (en) 2016-11-22 2018-05-31 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
CA3042294A1 (en) 2016-11-22 2018-05-31 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
BR112019011200B1 (pt) 2016-12-01 2021-12-28 Arvinas Operations, Inc Derivados de tetrahidronaftaleno e tetrahidroisoquinolina como degradadores do receptor de estrogênio
WO2018106870A1 (en) 2016-12-08 2018-06-14 Icahn School Of Medicine At Mount Sinai Compositions and methods for treating cdk4/6-mediated cancer
US10806737B2 (en) 2016-12-23 2020-10-20 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of fetal liver kinase polypeptides
KR20250117470A (ko) 2016-12-23 2025-08-04 아비나스 오퍼레이션스, 인코포레이티드 급속 진행성 섬유육종 폴리펩티드의 표적화 분해를 위한 화합물 및 방법
JP2020505327A (ja) 2016-12-23 2020-02-20 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. Egfrタンパク質分解標的化キメラ分子およびその関連する使用方法
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
BR112019015312A2 (pt) 2017-01-26 2020-03-10 Arvinas Operations, Inc. Moduladores da proteólise pelo receptor de estrogênio e métodos de uso associados
IL312367A (en) * 2017-01-31 2024-06-01 Arvinas Operations Inc Cereblon ligands and bifunctional compounds comprising the same
JP7227912B2 (ja) 2017-02-08 2023-02-24 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 キメラ抗原受容体の調節
WO2018226542A1 (en) 2017-06-09 2018-12-13 Arvinas, Inc. Modulators of proteolysis and associated methods of use
ES2965049T3 (es) * 2017-07-12 2024-04-10 Dana Farber Cancer Inst Inc Compuestos para la degradación de la proteína tau
WO2019060742A1 (en) 2017-09-22 2019-03-28 Kymera Therapeutics, Inc AGENTS FOR DEGRADING PROTEINS AND USES THEREOF
WO2019084030A1 (en) 2017-10-24 2019-05-02 Genentech, Inc. (4-HYDROXYPYRROLIDIN-2-YL) -HYDROXAMATE COMPOUNDS AND METHODS OF USE
WO2019084026A1 (en) 2017-10-24 2019-05-02 Genentech, Inc. (4-HYDROXYPYRROLIDIN-2-YL) -HETEROCYCLIC COMPOUNDS AND METHODS OF USE
CN111372585A (zh) 2017-11-16 2020-07-03 C4医药公司 用于靶蛋白降解的降解剂和降解决定子
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
US20190300521A1 (en) 2018-04-01 2019-10-03 Arvinas Operations, Inc. Brm targeting compounds and associated methods of use
IL302595A (en) 2018-04-13 2023-07-01 Arvinas Operations Inc Servalon ligands and bifunctional compounds containing them
JP7297053B2 (ja) 2018-08-20 2023-06-23 アルビナス・オペレーションズ・インコーポレイテッド 神経変性疾患を治療するためのe3ユビキチンリガーゼ結合活性を有するキメラ(protac)化合物を標的とし、アルファ-シヌクレインタンパク質を標的とするタンパク質分解
US11389438B2 (en) * 2019-02-25 2022-07-19 Chdi Foundation, Inc. Compounds for targeting mutant huntingtin protein and uses thereof
EP3999182A1 (en) * 2019-07-17 2022-05-25 Arvinas Operations, Inc. Tau-protein targeting compounds and associated methods of use

Similar Documents

Publication Publication Date Title
JP2022540935A5 (https=)
Hubbard et al. The role of aquaporin-4 in synaptic plasticity, memory and disease
JP2020502248A5 (https=)
JP2016199576A5 (https=)
JP2019507781A5 (https=)
MY178082A (en) Solid pharmaceutical compositions and processes for their production
RU2018114447A (ru) Введение дейтерированных усилителей cftr
JP2018531941A5 (https=)
JP2023153807A5 (https=)
SI3099684T1 (en) HETEROARIL AMIDI AS PROTEIN AGGREGATIVE INHIBITORS
WO2014160871A8 (en) Methods and agents for treating alzheimer's disease
JP2017518355A5 (https=)
EP4233901A3 (en) Pharmaceutical compositions containing anti-beta amyloid antibodies
JP2022513449A5 (https=)
JP2019529514A5 (https=)
JP2018505205A5 (https=)
JP2017505809A5 (https=)
BR112013016818A2 (pt) formulação
JP2018515506A5 (https=)
JP2022539152A5 (https=)
JP2019505549A5 (https=)
JP2016523969A5 (https=)
JP2011251985A5 (https=)
WO2018027037A3 (en) Reelin compositions for treatment of neurological disorders
RU2020115710A (ru) Терапевтические агенты для нейродегенеративных заболеваний