MX2023010341A - Moduladores de la proteolisis y metodos asociados de uso. - Google Patents

Moduladores de la proteolisis y metodos asociados de uso.

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Publication number
MX2023010341A
MX2023010341A MX2023010341A MX2023010341A MX2023010341A MX 2023010341 A MX2023010341 A MX 2023010341A MX 2023010341 A MX2023010341 A MX 2023010341A MX 2023010341 A MX2023010341 A MX 2023010341A MX 2023010341 A MX2023010341 A MX 2023010341A
Authority
MX
Mexico
Prior art keywords
target protein
present disclosure
modulators
binds
inhibition
Prior art date
Application number
MX2023010341A
Other languages
English (en)
Inventor
Craig M Crews
Andrew P Crew
Hanqing Dong
Keith R Hornberger
Michael Berlin
Jing Wang
Original Assignee
Arvinas Operations Inc
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Arvinas Operations Inc filed Critical Arvinas Operations Inc
Publication of MX2023010341A publication Critical patent/MX2023010341A/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10—Tetrapeptides
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/07—Tetrapeptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • C07D417/02—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 two hetero rings
    • C07D417/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Biophysics (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Wood Science & Technology (AREA)
  • Zoology (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Biomedical Technology (AREA)
  • Biotechnology (AREA)
  • Microbiology (AREA)
  • General Engineering & Computer Science (AREA)

Abstract

La presente descripción hace referencia a compuestos bifuncionales, que son útiles como moduladores de la proteína de sarcoma de rata Kirsten (proteína diana). En particular, la presente descripción se dirige a compuestos bifuncionales, que contienen en un extremo un ligando de Von Hippel-Lindau, cereblon, inhibidores de las proteínas de apoptosis u homólogo diminuto doble de ratón 2 que se une a la ubiquitina ligasa E3 respectiva y en el otro extremo un resto que se une a una proteína diana, de forma tal que la proteína diana se ubique cerca de la ubiquitina ligasa para efectuar la degradación (e inhibición) de la proteína diana. La presente descripción presenta una amplia variedad de actividades farmacológicas asociadas a la degradación/inhibición de la proteína diana. Las enfermedades o los trastornos que resultan de la agregación, acumulación y/o sobreactivación de la proteína diana se tratan o previenen con compuestos y composiciones de la presente descripción.
MX2023010341A 2018-04-04 2020-10-02 Moduladores de la proteolisis y metodos asociados de uso. MX2023010341A (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201862652676P 2018-04-04 2018-04-04

Publications (1)

Publication Number Publication Date
MX2023010341A true MX2023010341A (es) 2023-09-15

Family

ID=66770522

Family Applications (2)

Application Number Title Priority Date Filing Date
MX2020010420A MX2020010420A (es) 2018-04-04 2019-04-04 Moduladores de la proteólisis y métodos asociados de uso.
MX2023010341A MX2023010341A (es) 2018-04-04 2020-10-02 Moduladores de la proteolisis y metodos asociados de uso.

Family Applications Before (1)

Application Number Title Priority Date Filing Date
MX2020010420A MX2020010420A (es) 2018-04-04 2019-04-04 Moduladores de la proteólisis y métodos asociados de uso.

Country Status (12)

Country Link
US (2) US11161841B2 (es)
EP (1) EP3774777A2 (es)
JP (1) JP2021521112A (es)
KR (3) KR20230130752A (es)
CN (1) CN112218859A (es)
AU (2) AU2019249231B2 (es)
BR (1) BR112020020307A2 (es)
CA (1) CA3095494C (es)
CO (1) CO2020013864A2 (es)
IL (1) IL277729A (es)
MX (2) MX2020010420A (es)
WO (1) WO2019195609A2 (es)

Families Citing this family (46)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR102548191B1 (ko) * 2018-04-09 2023-06-28 상하이테크 유니버시티 표적 단백질 분해 화합물, 이의 항종양 응용, 이의 중간체 및 중간체의 응용
CN110698378B (zh) * 2019-11-19 2021-03-19 上海皓元生物医药科技有限公司 2-(羟基-(甲基环丙基)苯基氨基)-1-哌嗪基乙酮衍生物的制备方法
JP7480298B2 (ja) * 2019-12-02 2024-05-09 シャンハイ インリー ファーマシューティカル カンパニー リミテッド 酸素含有複素環化合物、その製造方法及び使用
JOP20220152A1 (ar) 2019-12-18 2023-01-30 Novartis Ag مشتقات 3-(5- ميثوكسي -1- أوكسو أيزو إندولين -2- يل) بيبريدين -2، 6- دايون واستخداماتها
CN113045565A (zh) * 2019-12-27 2021-06-29 微境生物医药科技(上海)有限公司 新型K-Ras G12C抑制剂
WO2021201577A1 (en) * 2020-03-30 2021-10-07 Uppthera Hmg-coa reductase degradation inducing compound
US20220370416A1 (en) * 2020-04-06 2022-11-24 Arvinas Operations, Inc. Compounds and methods for targeted degradation of kras
WO2021255089A1 (en) 2020-06-19 2021-12-23 Bayer Aktiengesellschaft 1,3,4-oxadiazole pyrimidines and 1,3,4-oxadiazole pyridines as fungicides
EP4204418A1 (en) 2020-08-28 2023-07-05 Arvinas Operations, Inc. Rapidly accelerating fibrosarcoma protein degrading compounds and associated methods of use
EP4208455A1 (en) * 2020-09-02 2023-07-12 The United States of America, as represented by the Secretary, Department of Health and Human Services Lzk-targeting degraders and methods of use
CN113633780B (zh) * 2020-09-11 2023-08-29 上海邈基生物科技有限公司 一种小分子偶联物及其用途
IL302081A (en) * 2020-10-14 2023-06-01 Ranok Therapeutics Hangzhou Co Ltd Methods and preparations for targeted protein degradation
EP4228700A1 (en) * 2020-10-14 2023-08-23 Ranok Therapeutics (Hangzhou) Co. Ltd. Methods and compositions for targeted protein degradation
AU2022207648A1 (en) 2021-01-13 2023-07-27 Monte Rosa Therapeutics Ag Isoindolinone compounds
AR124870A1 (es) 2021-02-15 2023-05-17 Astellas Pharma Inc Compuesto de quinazolina para inducir la degradación de la proteína kras mutante g12d
CN115043817A (zh) * 2021-03-09 2022-09-13 苏州泽璟生物制药股份有限公司 Sos1蛋白水解调节剂及其制备方法和应用
CN115232114B (zh) * 2021-04-23 2023-12-19 上海领泰生物医药科技有限公司 Sos1降解剂及其制备方法和应用
CN115260158A (zh) * 2021-04-30 2022-11-01 上海医药集团股份有限公司 一种靶向蛋白调节剂的化合物及其应用
WO2022251588A1 (en) * 2021-05-27 2022-12-01 Halda Therapeutics Opco, Inc. Heterobifunctional compounds and methods of treating disease
WO2022266206A1 (en) * 2021-06-16 2022-12-22 Erasca, Inc. Kras inhibitor conjugates
CN117460737A (zh) * 2021-07-05 2024-01-26 四川科伦博泰生物医药股份有限公司 杂芳环化合物、其制备方法及用途
AU2022370021A1 (en) * 2021-10-22 2024-05-09 Gluetacs Therapeutics (Shanghai) Co., Ltd. Crbn e3 ligase ligand compound, protein degrading agent developed on the basis of ligand compound, and their applications
WO2023077441A1 (en) * 2021-11-05 2023-05-11 Ranok Therapeutics (Hangzhou) Co. Ltd. Methods and compositions for targeted protein degradation
WO2023099620A1 (en) * 2021-12-01 2023-06-08 Boehringer Ingelheim International Gmbh Kras degrading compounds comprising annulated 2-amino-3-cyano thiophenes
CN116332959A (zh) * 2021-12-24 2023-06-27 苏州泽璟生物制药股份有限公司 Krasg12d蛋白水解调节剂及其制备方法和应用
WO2023130012A1 (en) * 2021-12-29 2023-07-06 Development Center For Biotechnology Compounds for mutant kras protein degradation and uses thereof
WO2023138524A1 (zh) * 2022-01-24 2023-07-27 贝达药业股份有限公司 Kras g12d降解剂及其在医药上的应用
CN116891514A (zh) * 2022-04-06 2023-10-17 润佳（苏州）医药科技有限公司 一种双官能化合物及其用途
WO2023185864A1 (en) * 2022-03-28 2023-10-05 Jingrui Biopharma Co., Ltd. Compounds for Targeted Degradation of KRAS
JP7440710B1 (ja) 2022-07-21 2024-02-28 アステラス製薬株式会社 Ｇ１２ｄ変異ｋｒａｓタンパクに作用する複素環化合物
WO2024022471A1 (zh) * 2022-07-28 2024-02-01 上海湃隆生物科技有限公司 Kras抑制剂化合物
WO2024029613A1 (ja) * 2022-08-05 2024-02-08 アステラス製薬株式会社 変異ｋｒａｓタンパクの分解を誘導するための複素環化合物
TW202413346A (zh) * 2022-08-09 2024-04-01 日商安斯泰來製藥股份有限公司 用於誘導g12v突變kras蛋白之分解之雜環化合物
TW202412809A (zh) 2022-08-12 2024-04-01 日商安斯泰來製藥股份有限公司 包含標靶療法的抗癌組合
WO2024033538A1 (en) 2022-08-12 2024-02-15 Astellas Pharma Inc. Combination of anticancer agents comprising a bifunctional compound with g12d mutant kras inhibitory activity
WO2024034123A1 (ja) * 2022-08-12 2024-02-15 アステラス製薬株式会社 複素環化合物を含む医薬組成物
WO2024054625A2 (en) * 2022-09-08 2024-03-14 Nikang Therapeutics, Inc. Bifunctional compounds for degrading kras g12d via ubiquitin proteasome pathway
WO2024050742A1 (en) * 2022-09-08 2024-03-14 Nikang Therapeutics, Inc. Bifunctional compounds for degrading kras g12d via ubiquitin proteasome pathway
CN118027067A (zh) * 2022-09-13 2024-05-14 润佳（苏州）医药科技有限公司 一种双官能化合物及其用途
CN117917410A (zh) * 2022-10-21 2024-04-23 上海领泰生物医药科技有限公司 pan-KRAS降解剂及其制备方法和应用
US20240189315A1 (en) 2022-11-09 2024-06-13 Boehringer Ingelheim International Gmbh Cyclic Pyridine Derivatives as cGAS Inhibitors
CN115873018B (zh) * 2022-11-18 2024-03-15 中国药科大学 苯并嘧啶和苯并三嗪类造血祖细胞激酶1降解剂及其应用
WO2024118960A1 (en) * 2022-11-30 2024-06-06 Tiger Biotherapeutics Inc. Glutarimide-containing kras-mutant degrader compounds and uses thereof
US20240217972A1 (en) * 2022-11-30 2024-07-04 Tiger Biotherapeutics Inc. Glutarimide-containing pan-kras-mutant degrader compounds and uses thereof
WO2024120424A1 (zh) * 2022-12-07 2024-06-13 贝达药业股份有限公司 一种靶向泛kras蛋白降解剂的化合物及其应用
CN118165068A (zh) * 2022-12-08 2024-06-11 润佳(上海)医药工程有限公司 一种双官能化合物及其用途

Family Cites Families (131)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998003502A1 (en) 1996-07-24 1998-01-29 Celgene Corporation Substituted 2(2,6-dioxopiperidin-3-yl)phthalimides and -1-oxoisoindolines and method of reducing tnf-alpha levels
CA2287387C (en) 1997-05-14 2010-02-16 Sloan-Kettering Institute For Cancer Research Methods and compositions for destruction of selected proteins
KR100301507B1 (ko) 1998-12-28 2001-11-17 구자홍 리니어압축기의오일공급장치
US6306663B1 (en) 1999-02-12 2001-10-23 Proteinex, Inc. Controlling protein levels in eucaryotic organisms
DE60026514T2 (de) 1999-05-05 2006-11-09 Merck & Co., Inc. Neue prolinverbindungen als mikrobizide mittel
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
US20030045552A1 (en) 2000-12-27 2003-03-06 Robarge Michael J. Isoindole-imide compounds, compositions, and uses thereof
EP1360205A1 (en) 2001-02-16 2003-11-12 E.I. Dupont De Nemours And Company Angiogenesis-inhibitory tripeptides, compositions and their methods of use
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
BR0312408A (pt) 2002-07-02 2005-04-19 Novartis Ag Inibidores de peptìdeo de ligação de proteìna smac a inibidor de apoptose de proteìnas (iap)
WO2005007621A2 (en) 2003-05-30 2005-01-27 Rigel Pharmaceuticals, Inc. Ubiquitin ligase inhibitors
US7932382B2 (en) 2004-01-16 2011-04-26 The Regents Of The University Of Michigan Conformationally constrained Smac mimetics and the uses thereof
AU2005228950B2 (en) 2004-03-23 2012-02-02 Genentech, Inc. Azabicyclo-octane inhibitors of IAP
KR20080083220A (ko) 2004-04-07 2008-09-16 노파르티스 아게 Ｉａｐ 억제제
KR100984459B1 (ko) 2004-07-02 2010-09-29 제넨테크, 인크. Ｉａｐ의 억제제
JP5007235B2 (ja) 2004-12-20 2012-08-22 ジェネンテック， インコーポレイテッド Ｉａｐのピロリジンインヒビター
KR101317661B1 (ko) 2005-02-25 2013-10-15 테트랄로직 파마슈티칼스 코포레이션 이량체성 ｉａｐ 억제제
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
AU2006285144A1 (en) 2005-08-31 2007-03-08 Celgene Corporation Isoindole-imide compounds and compositions comprising and methods of using the same
BRPI0708524A2 (pt) 2006-03-03 2011-05-31 Novartis Ag compostos de n-formil hidroxilamina
WO2007101347A1 (en) 2006-03-07 2007-09-13 Aegera Therapeutics Inc. Bir domain binding compounds
MX2008012728A (es) 2006-04-05 2008-10-14 Novartis Ag Combinaciones de agentes terapeuticos para el tratamiento de cancer.
CA2648518C (en) 2006-04-11 2012-06-26 Ramot At Tel Aviv University Ltd. Treatment of hematological malignancies with fts and a bcr-abl tyrosine kinase inhibitor
WO2007130626A2 (en) 2006-05-05 2007-11-15 The Regents Of The University Of Michigan Bivalent smac mimetics and the uses thereof
JP2009544620A (ja) 2006-07-20 2009-12-17 リガンド・ファーマシューティカルズ・インコーポレイテッド 自己免疫疾患及び炎症のためのプロリン尿素ｃｃｒ１アンタゴニスト
US20100056495A1 (en) 2006-07-24 2010-03-04 Tetralogic Pharmaceuticals Corporation Dimeric iap inhibitors
KR20090060314A (ko) 2006-08-30 2009-06-11 셀진 코포레이션 5-치환 이소인돌린 화합물
RU2448101C2 (ru) 2006-08-30 2012-04-20 Селджин Корпорейшн 5-замещенные изоиндолиновые соединения
ES2403546T3 (es) 2006-11-03 2013-05-20 Pharmacyclics, Inc. Sonda de actividad de la tirosina-cinasa de Bruton y procedimiento de utilización
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
DK2139490T3 (da) 2007-04-13 2014-09-08 Univ Michigan Diazo-bicykliske smac-mimetiske stoffer og anvendelser deraf
US8907092B2 (en) 2007-04-30 2014-12-09 Genentech, Inc. Inhibitors of IAP
US20100203012A1 (en) 2007-05-30 2010-08-12 Aegera Therapeutics, Inc. Iap bir domain binding compounds
US8762458B2 (en) * 2007-06-29 2014-06-24 Microsoft Corporation Providing sender-selected sound items to conversation participants
ES2551352T3 (es) * 2007-07-05 2015-11-18 Array Biopharma, Inc. Pirimido ciclopentanos útiles para el tratamiento de enfermedades inflamatorias o hiperproliferativas
ES2392003T3 (es) 2007-07-25 2012-12-03 Bristol-Myers Squibb Company Inhibidores de la triazina quinasa
EP2058312A1 (en) 2007-11-09 2009-05-13 Universita' degli Studi di Milano SMAC mimetic compounds as apoptosis inducers
WO2010025337A1 (en) * 2008-08-29 2010-03-04 Enzon Pharmaceuticals, Inc. Method of treating ras associated cancer
PE20140963A1 (es) 2008-10-29 2014-08-06 Celgene Corp Compuestos de isoindolina para el tratamiento de cancer
US20120135089A1 (en) 2009-03-17 2012-05-31 Stockwell Brent R E3 ligase inhibitors
WO2010141805A1 (en) 2009-06-05 2010-12-09 Janssen Pharmaceutica Nv Heterocyclic amides as modulators of trpa1
WO2011008260A2 (en) 2009-07-13 2011-01-20 President And Fellows Of Harvard College Bifunctional stapled polypeptides and uses thereof
WO2011059763A2 (en) 2009-10-28 2011-05-19 Joyant Pharmaceuticals, Inc. Dimeric smac mimetics
NZ717149A (en) 2010-02-11 2017-06-30 Celgene Corp Arylmethoxy isoindoline derivatives and compositions comprising and methods of using the same for treating various diseases
WO2012003281A2 (en) 2010-06-30 2012-01-05 Brandeis University Small-molecule-targeted protein degradation
US20120010235A1 (en) 2010-07-12 2012-01-12 Xin-Jie Chu N-substituted pyrrolidines
EP2619184B1 (en) 2010-09-24 2018-05-23 The Regents of the University of Michigan Deubiquitinase inhibitors and methods for use of the same
EP2635286A4 (en) 2010-11-05 2014-11-12 Glaxosmithkline Ip No 2 Ltd METHOD FOR THE TREATMENT OF CANCER
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
KR20140024914A (ko) 2011-04-29 2014-03-03 셀진 코포레이션 예측인자로 세레브론을 사용하는 암 및 염증성 질환의 치료를 위한 방법
US9376425B2 (en) 2011-09-27 2016-06-28 Amgen, Inc. Heterocyclic compounds as MDM2 inhibitors for the treatment of cancer
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
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
US20150119435A1 (en) 2012-05-11 2015-04-30 Yale University Compounds useful for promoting protein degradation and methods using same
JP6171003B2 (ja) 2012-05-24 2017-07-26 ノバルティス アーゲー ピロロピロリジノン化合物
SG11201406889WA (en) 2012-05-30 2015-02-27 Hoffmann La Roche Substituted pyrrolidine-2-carboxamides
WO2014011712A1 (en) 2012-07-10 2014-01-16 Bristol-Myers Squibb Company Iap antagonists
ES2742285T3 (es) 2012-07-31 2020-02-13 Novartis Ag Marcadores asociados con la sensibilidad a inhibidores del doble minuto humano 2 (MDM2)
WO2014025759A1 (en) 2012-08-09 2014-02-13 Bristol-Myers Squibb Company Iap antagonists
TWI586668B (zh) 2012-09-06 2017-06-11 第一三共股份有限公司 二螺吡咯啶衍生物之結晶
WO2014047024A1 (en) 2012-09-18 2014-03-27 Bristol-Myers Squibb Company Iap antagonists
WO2014055461A1 (en) 2012-10-02 2014-04-10 Bristol-Myers Squibb Company Iap antagonists
EP2917218B1 (en) 2012-11-09 2017-01-04 Ensemble Therapeutics Corporation Macrocyclic compounds for inhibition of inhibitors of apoptosis
RU2690663C2 (ru) 2012-12-20 2019-06-05 Мерк Шарп И Доум Корп. Замещенные имидазопиридины в качестве ингибиторов hdm2
US9637493B2 (en) 2012-12-20 2017-05-02 Merck Sharp & Dohme Corp. Substituted pyrrolopyrimidines as HDM2 inhibitors
EP2752191A1 (en) 2013-01-07 2014-07-09 Sanofi Compositions and methods using hdm2 antagonist and mek inhibitor
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.
WO2014134201A1 (en) 2013-02-28 2014-09-04 Amgen Inc. A benzoic acid derivative mdm2 inhibitor for the treatment of cancer
CA2906538C (en) 2013-03-14 2021-02-02 Ana Gonzalez Buenrostro Heteroaryl acid morpholinone compounds as mdm2 inhibitors for the treatment of cancer
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
WO2015006524A1 (en) 2013-07-12 2015-01-15 Bristol-Myers Squibb Company Iap antagonists
JO3805B1 (ar) 2013-10-10 2021-01-31 Araxes Pharma Llc مثبطات كراس جي12سي
EP3055290B1 (en) * 2013-10-10 2019-10-02 Araxes Pharma LLC Inhibitors of kras g12c
US20160339023A1 (en) 2013-12-23 2016-11-24 Fang Li Pharmaceutical Combinations
EP3104861A4 (en) * 2014-02-14 2017-10-04 Warrell, Raymond P., Jr. Bifunctional compounds and use for reducing uric acid levels
US20180228907A1 (en) 2014-04-14 2018-08-16 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same
KR20210132233A (ko) * 2014-04-14 2021-11-03 아비나스 오퍼레이션스, 인코포레이티드 단백질분해의 이미드-기초된 조절인자 및 연관된 이용 방법
US20160058872A1 (en) 2014-04-14 2016-03-03 Arvinas, Inc. Imide-based modulators of proteolysis and associated methods of use
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
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
CN107428734A (zh) 2015-01-20 2017-12-01 阿尔维纳斯股份有限公司 用于雄激素受体的靶向降解的化合物和方法
US20170327469A1 (en) 2015-01-20 2017-11-16 Arvinas, Inc. Compounds and methods for the targeted degradation of androgen receptor
US10017540B2 (en) 2015-03-11 2018-07-10 California Institute Of Technology Cyclic peptide binder against oncogenic K-Ras
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
US20180147202A1 (en) 2015-06-05 2018-05-31 Arvinas, Inc. TANK-BINDING KINASE-1 PROTACs AND ASSOCIATED METHODS OF USE
KR20180035828A (ko) 2015-07-10 2018-04-06 아비나스 인코포레이티드 단백질 분해의 mdm2계 조절인자 및 관련된 이용 방법
US20170037004A1 (en) 2015-07-13 2017-02-09 Arvinas, Inc. Alanine-based modulators of proteolysis and associated methods of use
CA2995036A1 (en) 2015-08-06 2017-02-09 Dana-Farber Cancer Institute, Inc. Tunable endogenous protein degradation
WO2017030814A1 (en) 2015-08-19 2017-02-23 Arvinas, 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
WO2017058807A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
US9938264B2 (en) 2015-11-02 2018-04-10 Yale University Proteolysis targeting chimera compounds and methods of preparing and using same
MX2018011216A (es) 2016-03-16 2019-08-29 H Lee Moffitt Cancer Ct & Res Moléculas pequeñas contra cereblon para mejorar la función efectora de los linfocitos t.
WO2017172979A1 (en) * 2016-03-30 2017-10-05 Araxes Pharma Llc Substituted quinazoline compounds and methods of use
US20170281784A1 (en) 2016-04-05 2017-10-05 Arvinas, Inc. Protein-protein interaction inducing technology
CA3021358A1 (en) 2016-04-22 2017-10-26 Dana-Farber Cancer Institute, Inc. Bifunctional molecules for degradation of egfr and methods of use
EP3455219A4 (en) 2016-05-10 2019-12-18 C4 Therapeutics, Inc. AMINE-LINKED C3-GLUTARIMIDE DEGRONIMERS FOR THE DEGRADATION OF TARGET PROTEINS
JP7039489B2 (ja) * 2016-05-18 2022-03-22 ミラティ セラピューティクス， インコーポレイテッド Ｋｒａｓ ｇ１２ｃ阻害剤
US11285218B2 (en) * 2016-06-23 2022-03-29 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
US20180072711A1 (en) 2016-09-15 2018-03-15 Arvinas, Inc. Indole derivatives as estrogen receptor degraders
US10584101B2 (en) 2016-10-11 2020-03-10 Arvinas, Inc. Compounds and methods for the targeted degradation of androgen receptor
CA3209295A1 (en) 2016-11-01 2018-06-07 Arvinas, Inc. Tau-protein targeting protacs and associated methods of use
HRP20231537T1 (hr) 2016-12-01 2024-03-15 Arvinas Operations, Inc. Derivati tetrahidronaftalena i tetrahidroizokinolina kao degradatori estrogenskih receptora
EP3559006A4 (en) * 2016-12-23 2021-03-03 Arvinas Operations, Inc. COMPOUNDS AND METHODS FOR TARGETED DEGRADATION OF FETAL LIVER KINASE POLYPEPTIDES
CA3047586A1 (en) 2016-12-23 2018-06-28 Arvinas Operations, Inc. Egfr proteolysis targeting chimeric molecules and associated methods of use
US10723717B2 (en) 2016-12-23 2020-07-28 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of rapidly accelerated fibrosarcoma 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
US10604506B2 (en) 2017-01-26 2020-03-31 Arvinas Operations, Inc. Modulators of estrogen receptor proteolysis and associated methods of use
AU2018215212B2 (en) 2017-01-31 2022-06-02 Arvinas Operations, Inc. Cereblon ligands and bifunctional compounds comprising the same
EP4119552A1 (en) 2017-02-08 2023-01-18 Dana-Farber Cancer Institute, Inc. Regulating chimeric antigen receptors
JOP20190272A1 (ar) 2017-05-22 2019-11-21 Amgen Inc مثبطات kras g12c وطرق لاستخدامها
EP3630746A1 (en) 2017-05-25 2020-04-08 Araxes Pharma LLC Compounds and methods of use thereof for treatment of cancer
EP3630745A2 (en) 2017-05-25 2020-04-08 Araxes Pharma LLC Covalent inhibitors of kras
US20180353501A1 (en) * 2017-06-09 2018-12-13 Arvinas, Inc. Modulators of proteolysis and associated methods of use
EP3774789A1 (en) 2018-04-01 2021-02-17 Arvinas Operations, Inc. Brm targeting compounds and associated methods of use

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