JP2017513862A5 - - Google Patents

Download PDF

Info

Publication number
JP2017513862A5
JP2017513862A5 JP2016563103A JP2016563103A JP2017513862A5 JP 2017513862 A5 JP2017513862 A5 JP 2017513862A5 JP 2016563103 A JP2016563103 A JP 2016563103A JP 2016563103 A JP2016563103 A JP 2016563103A JP 2017513862 A5 JP2017513862 A5 JP 2017513862A5
Authority
JP
Japan
Prior art keywords
syndrome
disease
alkyl
dioxo
dihydro
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
JP2016563103A
Other languages
English (en)
Japanese (ja)
Other versions
JP6778114B2 (ja
JP2017513862A (ja
Filing date
Publication date
Application filed filed Critical
Priority claimed from PCT/US2015/025813 external-priority patent/WO2015160845A2/en
Publication of JP2017513862A publication Critical patent/JP2017513862A/ja
Publication of JP2017513862A5 publication Critical patent/JP2017513862A5/ja
Application granted granted Critical
Publication of JP6778114B2 publication Critical patent/JP6778114B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

JP2016563103A 2014-04-14 2015-04-14 イミド系タンパク質分解モジュレーター及び関連する使用方法 Active JP6778114B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201461979351P 2014-04-14 2014-04-14
US61/979,351 2014-04-14
PCT/US2015/025813 WO2015160845A2 (en) 2014-04-14 2015-04-14 Imide-based modulators of proteolysis and associated methods of use

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2020170865A Division JP7169327B2 (ja) 2014-04-14 2020-10-09 イミド系タンパク質分解モジュレーター及び関連する使用方法

Publications (3)

Publication Number Publication Date
JP2017513862A JP2017513862A (ja) 2017-06-01
JP2017513862A5 true JP2017513862A5 (enExample) 2017-07-13
JP6778114B2 JP6778114B2 (ja) 2020-10-28

Family

ID=54264534

Family Applications (5)

Application Number Title Priority Date Filing Date
JP2016563103A Active JP6778114B2 (ja) 2014-04-14 2015-04-14 イミド系タンパク質分解モジュレーター及び関連する使用方法
JP2020170865A Active JP7169327B2 (ja) 2014-04-14 2020-10-09 イミド系タンパク質分解モジュレーター及び関連する使用方法
JP2022172961A Pending JP2022191517A (ja) 2014-04-14 2022-10-28 イミド系タンパク質分解モジュレーター及び関連する使用方法
JP2024199445A Pending JP2025020416A (ja) 2014-04-14 2024-11-15 イミド系タンパク質分解モジュレーター及び関連する使用方法
JP2026035833A Pending JP2026094376A (ja) 2014-04-14 2026-03-06 イミド系タンパク質分解モジュレーター及び関連する使用方法

Family Applications After (4)

Application Number Title Priority Date Filing Date
JP2020170865A Active JP7169327B2 (ja) 2014-04-14 2020-10-09 イミド系タンパク質分解モジュレーター及び関連する使用方法
JP2022172961A Pending JP2022191517A (ja) 2014-04-14 2022-10-28 イミド系タンパク質分解モジュレーター及び関連する使用方法
JP2024199445A Pending JP2025020416A (ja) 2014-04-14 2024-11-15 イミド系タンパク質分解モジュレーター及び関連する使用方法
JP2026035833A Pending JP2026094376A (ja) 2014-04-14 2026-03-06 イミド系タンパク質分解モジュレーター及び関連する使用方法

Country Status (10)

Country Link
US (2) US20150291562A1 (enExample)
EP (2) EP4649963A3 (enExample)
JP (5) JP6778114B2 (enExample)
KR (6) KR20210132233A (enExample)
CN (2) CN106458993B (enExample)
AU (5) AU2015247817C1 (enExample)
CA (1) CA2945975C (enExample)
MX (2) MX387318B (enExample)
RU (2) RU2020139890A (enExample)
WO (1) WO2015160845A2 (enExample)

Families Citing this family (371)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HUE035389T2 (en) 2006-09-26 2018-05-02 Celgene Corp 5-substituted quinazolinone derivatives as anticancer agents
KR100987051B1 (ko) * 2008-12-23 2010-10-11 한국수력원자력 주식회사 입자추적법을 이용한 복잡흐름장에서의 오염 물질 이동 수치모사 방법
RU2611007C2 (ru) 2011-03-11 2017-02-17 Селджин Корпорейшн Твердые формы 3-(5-амино-2-метил-4-оксо-4н-хиназолин-3-ил)пиперидин-2, 6-диона и их фармацевтические композиции и применение
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
WO2014039421A1 (en) 2012-09-04 2014-03-13 Celgene Corporation Isotopologues of 3-(5-amino-2-methyl-4-oxoquinazolin-3(4h)-yl) piperidine-2-6-dione and methods of preparation thereof
AU2013204922B2 (en) 2012-12-20 2015-05-14 Celgene Corporation Chimeric antigen receptors
WO2014121033A1 (en) 2013-02-04 2014-08-07 Fl Therapeutics Llc Soluble complexes of drug analogs and albumin
EP2970372B1 (en) 2013-03-15 2020-09-30 Celgene Corporation Modified t lymphocytes
GB201311888D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compounds
GB201311891D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compound
EP3964507A1 (en) 2013-10-04 2022-03-09 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
CN106456628A (zh) 2014-03-19 2017-02-22 无限药品股份有限公司 用于治疗PI3K‑γ介导的障碍的杂环化合物
EP4649963A3 (en) * 2014-04-14 2026-05-13 Arvinas Operations, Inc. Imide-based modulators of proteolysis and associated methods of use
US20180228907A1 (en) * 2014-04-14 2018-08-16 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same
CN106456699B (zh) 2014-05-05 2021-07-02 生物风险投资有限责任公司 作为抗老化剂抑制抗凋亡的Bcl-2蛋白的组合物和方法
US9937259B2 (en) 2014-06-27 2018-04-10 Zhuhai Beihai Biotech Co., Ltd. Abiraterone derivatives and non-covalent complexes with albumin
CA2955972A1 (en) 2014-07-22 2016-01-28 Bioventures, Llc. Compositions and methods for selectively depleting senescent cells
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
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
US12312316B2 (en) 2015-01-20 2025-05-27 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor
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
AU2016232705C1 (en) 2015-03-18 2021-06-17 Arvinas, Inc. Compounds and methods for the enhanced degradation of targeted proteins
GB201506872D0 (en) 2015-04-22 2015-06-03 Ge Oil & Gas Uk Ltd Novel compounds
GB201506871D0 (en) * 2015-04-22 2015-06-03 Glaxosmithkline Ip Dev Ltd Novel compounds
CA2988414C (en) * 2015-06-04 2023-09-26 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
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
CA2994969A1 (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
EP3337476A4 (en) * 2015-08-19 2019-09-04 Arvinas, Inc. Compounds and methods for the targeted degradation of bromodomain-containing proteins
WO2017040304A1 (en) 2015-08-28 2017-03-09 Cornell University Malt1 inhibitors and uses thereof
CN114230571B (zh) 2015-09-14 2025-07-08 无限药品股份有限公司 异喹啉酮的固体形式、其制备方法、包含其的组合物及其使用方法
BR112018008918A8 (pt) 2015-11-02 2019-02-26 Univ Yale compostos de quimera proteólise dirigida e métodos para preparação e uso dos mesmos
WO2017117473A1 (en) * 2015-12-30 2017-07-06 Dana-Farber Cancer Institute, Inc. Bifunctional molescules for her3 degradation and methods of use
WO2017117474A1 (en) * 2015-12-30 2017-07-06 Dana-Farber Cancer Institute, Inc. Bifunctional compounds for her3 degradation and methods of use
CA3014644A1 (en) 2016-02-15 2017-08-24 The Regents Of The University Of Michigan Fused 1,4-oxazepines and related analogs as bet bromodomain inhibitors
CN109153644B (zh) 2016-03-16 2022-10-21 H·李·莫菲特癌症中心研究有限公司 用以增强效应t细胞功能的针对cereblon的小分子
US20170281784A1 (en) 2016-04-05 2017-10-05 Arvinas, Inc. Protein-protein interaction inducing technology
EP3440082A1 (en) * 2016-04-06 2019-02-13 The Regents of The University of Michigan Monofunctional intermediates for ligand-dependent target protein degradation
AU2017246452C1 (en) * 2016-04-06 2021-06-03 The Regents Of The University Of Michigan MDM2 protein degraders
AU2017250076B2 (en) * 2016-04-12 2021-07-22 The Regents Of The University Of Michigan Bet 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
WO2017185036A1 (en) 2016-04-22 2017-10-26 Dana Farber Cancer Institute, Inc. Bifunctional molecules for degradation of egfr and methods of use
WO2017185031A1 (en) * 2016-04-22 2017-10-26 Dana-Farber Cancer Institute, Inc. Degradation of cyclin-dependent kinase 4/6 (cdk4/6) by conjugation of cdk4/6 inhibitors with e3 ligase ligand and methods of use
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
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
CN121974842A (zh) 2016-05-10 2026-05-05 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
WO2017197046A1 (en) * 2016-05-10 2017-11-16 C4 Therapeutics, Inc. C3-carbon linked glutarimide degronimers for target protein degradation
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
CN109562113A (zh) 2016-05-10 2019-04-02 C4医药公司 用于靶蛋白降解的螺环降解决定子体
CN109414596B (zh) 2016-05-12 2023-09-29 密歇根大学董事会 Ash1l抑制剂和用其进行治疗的方法
CN109152843A (zh) 2016-05-20 2019-01-04 豪夫迈·罗氏有限公司 Protac抗体缀合物及其使用方法
GB201610156D0 (en) 2016-06-10 2016-07-27 Otsuka Pharma Co Ltd Cliptac compositions
AU2017281525B2 (en) * 2016-06-23 2021-01-21 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
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
GB201614134D0 (en) * 2016-08-18 2016-10-05 Glaxosmithkline Ip Dev Ltd Novel compounds
CA3036834A1 (en) * 2016-09-13 2018-03-22 The Regents Of The University Of Michigan Fused 1,4-oxazepines as bet protein degraders
ES2857743T3 (es) * 2016-09-13 2021-09-29 Univ Michigan Regents 1,4-diazepinas fusionadas como degradadores de proteína BET
GB2554071A (en) * 2016-09-14 2018-03-28 Univ Dundee Small molecules
EP3512842B1 (en) 2016-09-15 2024-01-17 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
SI3526202T1 (sl) 2016-10-11 2025-04-30 Arvinas Operations, Inc. Spojine in postopki za ciljno razgradnjo androgenskih receptorjev
CN109983027A (zh) * 2016-10-20 2019-07-05 细胞基因公司 基于cereblon的可异二聚化嵌合抗原受体
EP3530652A4 (en) * 2016-10-21 2020-03-25 Keio University MODIFIED PHENYLPHTHALIMIDE AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME AS ACTIVE INGREDIENT
MX2019004950A (es) 2016-10-28 2019-09-26 Icahn School Med Mount Sinai Composiciones y metodos para tratar el cancer mediado por el potenciador del homologo zeste 2.
MX2019005007A (es) * 2016-11-01 2019-07-18 Arvinas Inc Protac dirigidos a la proteína tau y métodos asociados de uso.
US10689366B2 (en) 2016-11-01 2020-06-23 Cornell University Compounds for MALT1 degredation
AU2017363257B2 (en) * 2016-11-22 2021-08-19 Dana-Farber Cancer Institute, Inc. Degradation of protein kinases by conjugation of protein kinase inhibitors with E3 ligase ligand and methods of use
US10842878B2 (en) * 2016-11-22 2020-11-24 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
IL266842B (en) 2016-12-01 2022-09-01 Arvinas Operations Inc History of tetrahydronaphthalene and tetrahydroisoquinoline as estrogen receptor antagonists
CA3045037A1 (en) 2016-12-08 2018-06-14 Icahn School Of Medicine At Mount Sinai Compositions and methods for treating cdk4/6-mediated cancer
IL325835A (en) * 2016-12-23 2026-03-01 Univ Yale Compounds and methods for the targeted degradation of rapidly accelerated fibrosarcoma polypeptides
CN110753693A (zh) * 2016-12-23 2020-02-04 阿尔维纳斯运营股份有限公司 Egfr蛋白水解靶向嵌合分子和相关使用方法
US11173211B2 (en) 2016-12-23 2021-11-16 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides
US10806737B2 (en) 2016-12-23 2020-10-20 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of fetal liver kinase polypeptides
US11191741B2 (en) * 2016-12-24 2021-12-07 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of enhancer of zeste homolog 2 polypeptide
CN107056772A (zh) * 2017-01-23 2017-08-18 中国药科大学 基于cereblon配体诱导BET降解的双功能分子及其制备和应用
IL300417A (en) * 2017-01-26 2023-04-01 Arvinas Operations Inc Bifunctional benzothiophene compounds, preparations containing them and their use in therapy
IL319363A (en) * 2017-01-31 2025-05-01 Arvinas Operations Inc Cervalon ligands and bifunctional compounds containing them
EP4119552A1 (en) 2017-02-08 2023-01-18 Dana-Farber Cancer Institute, Inc. Regulating chimeric antigen receptors
JP6773915B2 (ja) * 2017-02-13 2020-10-21 カング バイオファーマシューティカルズ リミテッド 前立腺癌を治療する組み合わせ、薬物組成物および治療方法
CN110573507B (zh) * 2017-04-14 2023-11-14 邓迪大学 小分子
CN107033147B (zh) * 2017-04-25 2018-08-21 东南大学 一种bet/hdac双靶点抑制剂及其制备方法和应用
WO2018200981A1 (en) * 2017-04-28 2018-11-01 Quartz Therapeutics, Inc. Raf-degrading conjugate compounds
CN108947888B (zh) * 2017-05-23 2021-05-07 南京理工大学 一种在水相中钯催化合成3-取代异吲哚啉酮的方法
EP4717317A3 (en) 2017-06-20 2026-06-03 C4 Therapeutics, Inc. N/o-linked degrons and degronimers for protein degradation
US10716858B2 (en) 2017-06-30 2020-07-21 Massachusetts Institute Of Technology Branched multi-functional macromonomers and uses thereof
GB201710620D0 (en) * 2017-07-03 2017-08-16 Glaxosmithkline Intellectual Property Ltd Targeted protein degradation
US20210154184A1 (en) * 2017-07-12 2021-05-27 Dana-Farber Cancer Institute, Inc. Compounds for tau protein degradation
WO2019023553A1 (en) * 2017-07-28 2019-01-31 Arvinas, Inc. COMPOUNDS AND METHODS FOR TARGETED DEGRADATION OF THE ANDROGEN RECEPTOR
TWI793151B (zh) * 2017-08-23 2023-02-21 瑞士商諾華公司 3-(1-氧異吲哚啉-2-基)之氫吡啶-2,6-二酮衍生物及其用途
CN109422751B (zh) * 2017-09-03 2022-04-22 上海美志医药科技有限公司 一类具有降解酪氨酸蛋白激酶jak3活性的化合物
CN109422733A (zh) * 2017-09-03 2019-03-05 上海美志医药科技有限公司 一类抑制并降解酪氨酸蛋白激酶alk的化合物
WO2019043217A1 (en) 2017-09-04 2019-03-07 F. Hoffmann-La Roche Ag DIHYDROBENZIMIDAZOLONES
WO2019043208A1 (en) 2017-09-04 2019-03-07 F. Hoffmann-La Roche Ag DIHYDROQUINOLINONES
CN118108706A (zh) 2017-09-04 2024-05-31 C4医药公司 戊二酰亚胺
MX2020003190A (es) 2017-09-22 2020-11-11 Kymera Therapeutics Inc Degradadores de proteinas y usos de los mismos.
WO2019060693A1 (en) 2017-09-22 2019-03-28 Kymera Therapeutics, Inc. CRBN LIGANDS AND USES THEREOF
SG11202003415XA (en) * 2017-10-18 2020-05-28 Novartis Ag Compositions and methods for selective protein degradation
EP3676268A1 (en) * 2017-10-20 2020-07-08 Dana-Farber Cancer Institute, Inc. Heterobifunctional compounds with improved specificityfor the bromodomain of brd4
WO2019084026A1 (en) 2017-10-24 2019-05-02 Genentech, Inc. (4-HYDROXYPYRROLIDIN-2-YL) -HETEROCYCLIC COMPOUNDS AND METHODS OF USE
WO2019084030A1 (en) 2017-10-24 2019-05-02 Genentech, Inc. (4-HYDROXYPYRROLIDIN-2-YL) -HYDROXAMATE COMPOUNDS AND METHODS OF USE
US10632209B2 (en) * 2017-11-10 2020-04-28 The Regents Of The University Of Michigan ASH1L inhibitors and methods of treatment therewith
EP3710002A4 (en) 2017-11-16 2021-07-07 C4 Therapeutics, Inc. DEGRADER AND DEGRONE FOR TARGETED PROTEIN DEGRADATION
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
WO2019109415A1 (zh) * 2017-12-04 2019-06-13 清华大学 一种靶向降解hmgcr的化合物及其应用
EP3724180B1 (en) 2017-12-13 2023-02-22 Dana-Farber Cancer Institute, Inc. Compounds for the degradation of stk4 and treatment of hematologic malignancies
WO2019114770A1 (zh) * 2017-12-13 2019-06-20 上海科技大学 Alk蛋白降解剂及其抗肿瘤应用
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
IL315310A (en) 2017-12-26 2024-10-01 Kymera Therapeutics Inc Irak degraders and uses thereof
CN119792569A (zh) * 2018-01-10 2025-04-11 财团法人生物技术开发中心 抗体protac偶联物
EP3737666A4 (en) 2018-01-12 2022-01-05 Kymera Therapeutics, Inc. PROTEIN DEGRADATION AGENTS AND ASSOCIATED USES
US11512080B2 (en) 2018-01-12 2022-11-29 Kymera Therapeutics, Inc. CRBN ligands and uses thereof
ES3041854T3 (en) 2018-01-22 2025-11-17 Bioventures Llc Bcl-2 proteins degraders for cancer treatment
JP2021512153A (ja) 2018-01-26 2021-05-13 イエール ユニバーシティ タンパク質分解のイミド系モジュレーターおよび使用方法
TW201945357A (zh) 2018-02-05 2019-12-01 瑞士商赫孚孟拉羅股份公司 化合物
US11702402B2 (en) * 2018-02-23 2023-07-18 Dana-Farber Cancer Institute, Inc. Small molecules that block proteasome-associated ubiquitin receptor RPN13 function and uses thereof
JP2021515013A (ja) 2018-03-06 2021-06-17 アイカーン スクール オブ メディスン アット マウント シナイ セリンスレオニンキナーゼ(akt)分解/破壊化合物および使用方法
WO2019170150A1 (zh) 2018-03-09 2019-09-12 上海科技大学 蛋白降解靶向bcr-abl化合物及其抗肿瘤应用
WO2019177902A1 (en) 2018-03-10 2019-09-19 Yale University Modulators of btk proteolysis and methods of use
WO2019183523A1 (en) 2018-03-23 2019-09-26 Genentech, Inc. Hetero-bifunctional degrader compounds and their use as modulators of targeted ubiquination (vhl)
CN111902141A (zh) * 2018-03-26 2020-11-06 C4医药公司 用于ikaros降解的羟脑苷脂结合剂
CN110317192A (zh) * 2018-03-28 2019-10-11 上海美志医药科技有限公司 一类具有降解雄激素受体活性的化合物
AU2019249849C1 (en) * 2018-04-01 2022-09-29 Arvinas Operations, Inc. BRM targeting compounds and associated methods of use
US12539292B2 (en) 2018-04-01 2026-02-03 Arvinas Operations, Inc. BRM targeting compounds and associated methods of use
BR112020020307A2 (pt) 2018-04-04 2021-01-12 Arvinas Operations, Inc. Moduladores de proteólise e métodos de uso associados
EP3778590A4 (en) 2018-04-09 2021-12-22 ShanghaiTech University ANTI PROTEIN DEGRADATION COMPOUND, ANTITUMOR APPLICATION, INTERMEDIATE THEREOF, AND INTERMEDIATE USE
CA3303472A1 (en) 2018-04-13 2026-05-13 Massachusetts Institute Of Technology Brush prodrugs and uses thereof
CA3095912A1 (en) * 2018-04-13 2019-10-17 Arvinas Operations, Inc. Cereblon ligands and bifunctional compounds comprising the same
WO2019204354A1 (en) 2018-04-16 2019-10-24 C4 Therapeutics, Inc. Spirocyclic compounds
EP3556760A1 (en) 2018-04-19 2019-10-23 F. Hoffmann-La Roche AG Spiro compounds
CN111741769B (zh) * 2018-04-20 2022-09-16 四川科伦博泰生物医药股份有限公司 一种多功能化合物、其制备方法及其在医药上的应用
WO2019221755A1 (en) 2018-05-18 2019-11-21 Bioventures, Llc Piperlongumine analogues and uses thereof
EP3578561A1 (en) 2018-06-04 2019-12-11 F. Hoffmann-La Roche AG Spiro compounds
CA3103185A1 (en) 2018-06-13 2019-12-19 Amphista Therapeutics Ltd Bifunctional molecules for targeting rpn11
JP2021527666A (ja) * 2018-06-21 2021-10-14 アイカーン スクール オブ メディスン アット マウント シナイ Wd40反復ドメインタンパク質5(wdr5)分解/破壊化合物および使用の方法
AU2019294835B2 (en) * 2018-06-29 2025-04-17 Dana-Farber Cancer Institute, Inc. Ligands to cereblon (CRBN)
CN110372693B (zh) * 2018-07-04 2022-05-03 清华大学 一种靶向降解bet蛋白的化合物及其应用
WO2020010204A1 (en) 2018-07-05 2020-01-09 Icahn School Of Medicine At Mount Sinai Protein tyrosine kinase 6 (ptk6) degradation / disruption compounds and methods of use
CN108794453A (zh) * 2018-07-05 2018-11-13 清华大学 一种靶向降解fak蛋白的化合物及其应用
US11292792B2 (en) 2018-07-06 2022-04-05 Kymera Therapeutics, Inc. Tricyclic CRBN ligands and uses thereof
US12454520B2 (en) 2018-07-06 2025-10-28 Kymera Therapeutics, Inc. Protein degraders and uses thereof
BR122022012697B1 (pt) 2018-07-10 2023-04-04 Novartis Ag Usos de derivados de 3-(5-hidróxi-1-oxoisoindolin-2-il)piperidina-2,6- diona, e kit
AR116109A1 (es) 2018-07-10 2021-03-31 Novartis Ag Derivados de 3-(5-amino-1-oxoisoindolin-2-il)piperidina-2,6-diona y usos de los mismos
EP3820532A4 (en) * 2018-07-11 2022-04-06 H. Lee Moffitt Cancer Center & Research Institute, Inc. DIMERE IMMUNOMODULATORY COMPOUNDS AGAINST CEREBLON-BASED MECHANISMS
US12011432B2 (en) 2018-07-18 2024-06-18 Case Western Reserve University Method of modulating ribonucleotide reductase
US20200038513A1 (en) 2018-07-26 2020-02-06 Arvinas Operations, Inc. Modulators of fak proteolysis and associated methods of use
WO2020027225A1 (ja) 2018-07-31 2020-02-06 ファイメクス株式会社 複素環化合物
US11707452B2 (en) 2018-08-20 2023-07-25 Arvinas Operations, Inc. Modulators of alpha-synuclein proteolysis and associated methods of use
MX2021001957A (es) * 2018-08-22 2021-07-15 Cullgen Shanghai Inc Compuestos de degradacion y metodos de uso del receptor de tropomiosina quinasa (trk).
US11969472B2 (en) 2018-08-22 2024-04-30 Cullgen (Shanghai), Inc. Tropomyosin receptor kinase (TRK) degradation compounds and methods of use
WO2020051235A1 (en) 2018-09-04 2020-03-12 C4 Therapeutics, Inc. Compounds for the degradation of brd9 or mth1
CN119219628A (zh) 2018-09-07 2024-12-31 阿尔维纳斯运营股份有限公司 用于迅速加速性纤维肉瘤多肽的靶向降解的多环化合物和方法
CN111018857B (zh) * 2018-10-09 2023-06-02 嘉兴优博生物技术有限公司 靶向蛋白酶降解平台(ted)
AU2019365238A1 (en) 2018-10-24 2021-05-13 F. Hoffmann-La Roche Ag Conjugated chemical inducers of degradation and methods of use
AU2019389174A1 (en) 2018-11-30 2021-07-01 Kymera Therapeutics, Inc. Irak degraders and uses thereof
BR112021011968A2 (pt) 2018-12-19 2021-09-08 Celgene Corporation Compostos de 3-((3-aminofenil)amino)piperidina-2,6-diona substituídos, composições dos mesmos e métodos de tratamento com os mesmos
AU2019404022A1 (en) 2018-12-19 2021-07-08 Celgene Corporation Substituted 3-((3-aminophenyl)amino)piperidine-2,6-dione compounds, compositions thereof, and methods of treatment therewith
EP3897631A4 (en) 2018-12-20 2022-11-23 C4 Therapeutics, Inc. TARGETED PROTEIN BREAKDOWN
US20220081435A1 (en) * 2019-01-03 2022-03-17 The Regents Of The University Of Michigan Androgen receptor protein degraders
WO2020160295A1 (en) * 2019-01-30 2020-08-06 Montelino Therapeutics, Llc Bi-functional compounds and methods for targeted ubiquitination of androgen receptor
JP7394140B2 (ja) * 2019-02-02 2023-12-07 シーエスピーシー ゾンチー ファーマシューティカル テクノロジー(シージアチュアン)カンパニー,リミテッド 標的ユビキチン化分解brd4タンパク質化合物、その調製方法および応用
WO2020163170A1 (en) * 2019-02-05 2020-08-13 The Board Of Regents Of The University Of Texas System Trapping-free parp inhibitors
KR102876423B1 (ko) * 2019-02-07 2025-10-24 한국화학연구원 표적 단백질 eed 분해 유도 데그라듀서, 이의 제조방법 및 이를 유효성분으로 함유하는 eed, ezh2, 또는 prc2 관련 질환의 예방 또는 치료용 약학적 조성물
WO2020176424A1 (en) * 2019-02-25 2020-09-03 Chdi Foundation, Inc. Compounds for targeting mutant huntingtin protein and uses thereof
EP3932922A4 (en) 2019-02-25 2022-05-11 ShanghaiTech University SULPHUR-CONTAINING COMPOUND BASED ON A GLUTARIMIDE FRAMEWORK AND ITS USE
US12186401B2 (en) 2019-03-01 2025-01-07 Ontario Institute for Cancer Research (OICR) and Sinai Health System Amide-based proteolysis modulators of B-rapidly accelerated fibrosarcoma (BRAF) and associated uses
ES2995214T3 (en) 2019-03-06 2025-02-07 C4 Therapeutics Inc Heterocyclic compounds for medical treatment
KR102980990B1 (ko) 2019-04-05 2026-06-25 카이메라 쎄라퓨틱스 인코포레이티드 Stat 분해제 및 이의 용도
JP7667742B2 (ja) 2019-04-09 2025-04-23 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 Atp競合性akt阻害剤gdc-0068とe3リガーゼリガンドとの結合によるaktの分解および使用方法
KR102947433B1 (ko) 2019-04-12 2026-04-06 씨4 테라퓨틱스, 인코포레이티드 이카로스 및 아이올로스의 트리시클릭 분해제
WO2020214555A1 (en) 2019-04-16 2020-10-22 Northwestern University Bifunctional compounds comprising apcin-a and their use in the treatment of cancer
BR112021020775A2 (pt) * 2019-04-18 2021-12-14 Hinova Pharmaceuticals Inc Classe de compostos heterocíclicos quiméricos bifuncionais para a degradação direcionada de receptores de andrógeno e uso dos mesmos
CN114423463B (zh) 2019-05-06 2025-09-26 西奈山伊坎医学院 作为hpk1的降解剂的异双功能化合物
CR20210587A (es) 2019-05-31 2022-02-11 Janssen Pharmaceutica Nv Inhibidores de molécula pequeña de quinasa inductora de nf-kb
US12624044B2 (en) 2019-06-10 2026-05-12 Kymera Therapeutics, Inc. SMARCA degraders and uses thereof
WO2020251972A1 (en) 2019-06-10 2020-12-17 Kymera Therapeutics, Inc. Smarca degraders and uses thereof
EP4029499A4 (en) 2019-06-12 2023-07-26 Shanghaitech University Alk protein regulator and anti-tumor application thereof
WO2020253711A1 (zh) * 2019-06-17 2020-12-24 中国科学院上海药物研究所 一种吡咯并吡啶酮类化合物、其制备方法、其组合物和用途
CN110372669B (zh) * 2019-06-19 2020-11-24 浙江省医学科学院 一种基于crbn配体诱导egfr降解的化合物及其制备方法、药物组合物和应用
WO2020263989A1 (en) 2019-06-24 2020-12-30 University Of Iowa Research Foundation Jnk inhibitors as anticancer agents
PH12022500002A1 (en) 2019-06-28 2023-04-03 Kymera Therapeutics Inc Irak degraders and uses thereof
EP3999182A1 (en) 2019-07-17 2022-05-25 Arvinas Operations, Inc. Tau-protein targeting compounds and associated methods of use
US12558427B2 (en) 2019-07-17 2026-02-24 Kymera Therapeutics, Inc. IRAK degraders and uses thereof
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
US12636370B2 (en) 2019-08-08 2026-05-26 Institute For Cancer Research Combination therapy for treatment of cancer
WO2021041348A1 (en) * 2019-08-26 2021-03-04 Arvinas Operations, Inc. Methods of treating breast cancer with tetrahydronaphthalene derivatives as estrogen receptor degraders
CN114761400B (zh) * 2019-09-12 2024-08-13 南京明德新药研发有限公司 一种可降解蛋白的并环类化合物及其应用
CN110563703B (zh) * 2019-09-18 2021-04-09 浙江省医学科学院 基于crbn配体诱导parp-1降解的化合物及制备方法和应用
EP3795570B1 (en) * 2019-09-23 2022-02-23 Accutar Biotechnology Inc. Substituted quinoline-8-carbonitrile derivatives having androgen receptor degradation activity and uses thereof
EP4034114A4 (en) 2019-09-23 2023-07-26 Accutar Biotechnology Inc. Novel ureas having androgen receptor degradation activity and uses thereof
JP7502425B2 (ja) 2019-10-01 2024-06-18 アルヴィナス・オペレーションズ・インコーポレイテッド Brm標的化化合物および関連使用方法
CA3154334A1 (en) 2019-10-16 2021-04-22 Jeremiah A. Johnson Brush prodrugs and uses thereof
MX2022004526A (es) * 2019-10-17 2022-07-21 Arvinas Operations Inc Moléculas bifuncionales que contienen una porción de unión a la ligasa de ubiquitina e3 unida a una porción de direccionamiento a bcl6.
US20210113557A1 (en) * 2019-10-22 2021-04-22 Arvinas Operations, Inc. Methods of treating prostate cancer
CN112707900B (zh) * 2019-10-24 2022-06-10 上海科技大学 蛋白降解剂及其在疾病治疗中的应用
CN110713480B (zh) * 2019-10-28 2021-02-26 浙江省医学科学院 AChE蛋白降解物及其制备方法和应用
CN110746400B (zh) * 2019-11-07 2021-12-17 郑州大学 一种靶向雄激素受体的荧光探针及其制备方法
CN110790750B (zh) * 2019-11-07 2021-09-21 郑州大学 一种邻苯二甲酰亚胺类选择性雄激素受体降解剂及其制备方法和用途
WO2021119159A1 (en) 2019-12-10 2021-06-17 Kymera Therapeutics, Inc. Irak degraders and uses thereof
KR20220114615A (ko) 2019-12-16 2022-08-17 베이징 타이드 파마슈티컬 코퍼레이션 리미티드 Egfr 키나제의 분해를 억제 및 유도하는 화합물
CA3161878A1 (en) 2019-12-17 2021-06-24 Matthew M. Weiss Irak degraders and uses thereof
US20230099031A1 (en) * 2019-12-17 2023-03-30 Orionis Biosciences, Inc. Bifunctional agents for protein recruitment and/or degradation
EP4076524A4 (en) 2019-12-17 2023-11-29 Kymera Therapeutics, Inc. IRAQ DEGRADERS AND USES THEREOF
WO2021127443A1 (en) * 2019-12-19 2021-06-24 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor
EP4681715A3 (en) 2019-12-20 2026-01-28 C4 Therapeutics, Inc. Isoindolinone and indazole compounds for the degradation of egfr
AU2020414151A1 (en) 2019-12-23 2022-08-25 Jiangxi Jemincare Group Co., Ltd Protein degradation agent compound preparation method and application
US11679109B2 (en) 2019-12-23 2023-06-20 Kymera Therapeutics, Inc. SMARCA degraders and uses thereof
US20230117831A1 (en) * 2020-01-08 2023-04-20 The Broad Institute, Inc. Multi-functional chimeric molecules
WO2021141662A1 (en) * 2020-01-10 2021-07-15 Massachusetts Institute Of Technology Proteolysis targeting chimeric molecules (protacs) with functional handles and uses thereof
MX2022009419A (es) 2020-01-31 2022-08-25 Avilar Therapeutics Inc Compuestos de union al asgpr para la degradacion de proteinas extracelulares.
CN113248484A (zh) * 2020-02-13 2021-08-13 上海强睿生物科技有限公司 一种特异性降解tau蛋白的小分子化合物及其应用
KR20210103973A (ko) * 2020-02-14 2021-08-24 보로노이 주식회사 단백질 키나아제 분해 유도 화합물 및 이의 용도
JP7815127B2 (ja) 2020-02-19 2026-02-17 ニューリックス セラピューティクス,インコーポレイテッド インターロイキン-1受容体関連キナーゼの二機能性分解剤およびその治療的使用
BR112022016901A2 (pt) * 2020-02-26 2022-12-06 Cullgen Shanghai Inc Compostos de degradação do receptor de tropomiosina quinase (trk) e métodos de uso
CN115210227A (zh) 2020-03-04 2022-10-18 基因泰克公司 作为tead抑制剂的异双功能分子
CN119823124A (zh) 2020-03-05 2025-04-15 C4医药公司 用于brd9的靶向降解的化合物
CN113387930B (zh) 2020-03-11 2022-07-12 苏州开拓药业股份有限公司 一种双官能化合物及其制备方法和用途
CN115380026B (zh) * 2020-03-17 2023-11-07 南京明德新药研发有限公司 蛋白降解调节剂与其使用方法
WO2021188948A1 (en) 2020-03-19 2021-09-23 Kymera Therapeutics, Inc. Mdm2 degraders and uses thereof
KR102624481B1 (ko) * 2020-03-20 2024-01-16 (주)프레이저테라퓨틱스 p38 제거능을 갖는 화합물, 이의 제조방법 및 이를 포함하는 만성 염증성 질환 치료용 조성물
KR20230004511A (ko) 2020-03-21 2023-01-06 아비나스 오퍼레이션스, 인코포레이티드 인다졸계 화합물 및 관련된 사용 방법
CN115605267B (zh) 2020-03-21 2025-07-29 阿维纳斯企业公司 突变体lrrk2蛋白水解的选择性调节剂和相关使用方法
US20230158158A1 (en) 2020-03-27 2023-05-25 Uppthera Pyrazolo quinazoline derivative compounds inducing selective degradation of plk1
US20220370416A1 (en) 2020-04-06 2022-11-24 Arvinas Operations, Inc. Compounds and methods for targeted degradation of kras
KR102185390B1 (ko) * 2020-04-17 2020-12-01 (주) 업테라 세포 투과성 세레블론 재조합 융합 단백질 및 이의 용도
WO2021217036A1 (en) * 2020-04-23 2021-10-28 Salem Aliasger K Gper proteolytic targeting chimeras
ES3014370T3 (en) * 2020-04-28 2025-04-22 Rhizen Pharmaceuticals Ag Novel compounds useful as poly(adp-ribose) polymerase (parp) inhibitors
WO2021219077A1 (zh) * 2020-04-29 2021-11-04 泰比棣医药科技(石家庄)有限公司 一种组织靶向的蛋白靶向降解化合物及其用途
CN113582974B (zh) * 2020-04-30 2022-05-17 江西济民可信集团有限公司 一类作为蛋白降解剂的化合物及其制备方法和医药用途
CN115996918A (zh) 2020-05-09 2023-04-21 阿尔维纳斯运营股份有限公司 制造双官能团化合物的方法、双官能团化合物的超纯形式以及包括所述双官能团化合物的剂型
GB202007106D0 (en) 2020-05-14 2020-07-01 Ucl Business Plc Cyclosporine analogues
US12103924B2 (en) 2020-06-01 2024-10-01 Icahn School Of Medicine At Mount Sinai Mitogen-activated protein kinase kinase (MEK) degradation compounds and methods of use
EP4161521A4 (en) 2020-06-03 2024-07-10 Kymera Therapeutics, Inc. DEUTERED IRAQ DEGRADERS AND USES THEREOF
TW202210483A (zh) 2020-06-03 2022-03-16 美商凱麥拉醫療公司 Irak降解劑之結晶型
KR20230024328A (ko) 2020-06-12 2023-02-20 상하이 제민케어 파마슈티칼스 컴퍼니 리미티드 프탈라지논 화합물, 이의 제조 방법 및 이의 의학적 용도
WO2021255212A1 (en) 2020-06-19 2021-12-23 F. Hoffmann-La Roche Ag Braf degraders
CN115916769B (zh) * 2020-06-28 2024-09-10 深圳扬厉医药技术有限公司 并环吲唑类化合物
CN114341128B (zh) * 2020-07-24 2024-06-25 恩瑞生物医药科技(上海)有限公司 双功能蛋白降解靶向嵌合体类化合物及其制备方法和医药用途
CN116490186B (zh) 2020-08-05 2025-10-31 C4医药公司 用于ret的靶向降解的化合物
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
CN114163444B (zh) * 2020-09-11 2023-07-14 江苏恒瑞医药股份有限公司 一种用于雄激素受体蛋白靶向降解的嵌合体化合物、其制备方法及其在医药上的应用
AU2021342287A1 (en) 2020-09-14 2023-04-13 Arvinas Operations, Inc. Crystalline forms of a compound for the targeted degradation of estrogen receptor
IL302037A (en) * 2020-10-14 2023-06-01 C4 Therapeutics Inc Tricyclic heterobifunctional compounds for degradation of targeted proteins
WO2022087125A1 (en) 2020-10-21 2022-04-28 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor protein
EP4240733A1 (en) * 2020-11-06 2023-09-13 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor and associated methods of use
CN112341436A (zh) * 2020-11-20 2021-02-09 中国药科大学 基于靶向抑制和降解alk的苯并咔唑类蛋白水解靶向嵌合分子、制备方法及用途
WO2022120355A1 (en) 2020-12-02 2022-06-09 Ikena Oncology, Inc. Tead degraders and uses thereof
TW202237095A (zh) 2020-12-03 2022-10-01 德商艾斯巴赫生物有限公司 Alc1抑制劑及與parpi之協同性
CN112480081B (zh) * 2020-12-07 2022-02-22 沈阳药科大学 一种基于Cereblon配体诱导SHP2蛋白降解的双功能分子化合物
US12606568B2 (en) 2020-12-09 2026-04-21 Kymera Therapeutics, Inc. SMARCA degraders and uses thereof
US20240124418A1 (en) * 2020-12-14 2024-04-18 Biotheryx, Inc. Pde4 degraders, pharmaceutical compositions, and therapeutic applications
AR124547A1 (es) 2020-12-30 2023-04-05 Kymera Therapeutics Inc Degradadores de irak y sus usos
WO2022146151A1 (en) * 2020-12-30 2022-07-07 Captor Therapeutics S.A. Novel compounds which bind to cereblon, and methods of use thereof
US12152035B2 (en) 2020-12-30 2024-11-26 Industrial Technology Research Institute Androgen receptor binding molecule and use thereof
CN117242060B (zh) 2021-01-13 2026-07-17 蒙特罗莎治疗股份有限公司 异吲哚啉酮化合物
US12569564B2 (en) 2021-01-23 2026-03-10 Newave Pharmaceutical Inc. Spirocyclic MDM2 modulator and uses thereof
JP2024505562A (ja) 2021-02-02 2024-02-06 レス ラボラトイレス セルビエル 選択的bcl-xl protac化合物及び使用の方法
LT4293024T (lt) 2021-02-15 2026-05-25 Astellas Pharma Inc. Chinazolino junginys, skirtas g12d mutantinio kras baltymo degradacijai sukelti
MX2023009178A (es) 2021-02-15 2023-08-21 Kymera Therapeutics Inc Degradadores de la cinasa 4 asociada al receptor de interleucina 1 (irak4) y usos de los mismos.
WO2022174268A1 (en) 2021-02-15 2022-08-18 Kymera Therapeutics, Inc. Irak4 degraders and uses thereof
CA3211347A1 (en) 2021-03-19 2022-09-22 Erika Araujo Indazole based compounds and associated methods of use
CN117321046A (zh) * 2021-03-19 2023-12-29 阿维纳斯企业公司 基于吲唑的化合物和相关使用方法
JP2024512544A (ja) * 2021-03-29 2024-03-19 江▲蘇▼恒瑞医▲薬▼股▲フン▼有限公司 テトラヒドロナフタレン系化合物、その製造方法及びその医薬的応用
CN118388454A (zh) 2021-04-16 2024-07-26 阿尔维纳斯运营股份有限公司 Bcl6蛋白水解的调节剂和其相关使用方法
MX2023012981A (es) * 2021-05-03 2024-01-11 Nurix Therapeutics Inc Compuestos para inhibir o degradar proteinas objetivo, composiciones que los comprenden, metodos para su preparacion y metodos para usarlos.
AU2022268925A1 (en) 2021-05-03 2023-11-16 Avilar Therapeutics, Inc. Potent asgpr-binding compounds for the degradation of immunoglobulins and other proteins
US20240287076A1 (en) 2021-05-05 2024-08-29 Biogen Ma Inc. Compounds for targeting degradation of bruton's tyrosine kinase
CA3217792A1 (en) 2021-05-07 2022-11-10 Kymera Therapeutics, Inc Cdk2 degraders and uses thereof
BR112023024507A2 (pt) 2021-05-26 2024-02-15 C4 Therapeutics Inc Método para tratar um câncer mediado por receptor do fator de crescimento epidérmico mutante que sofreu metástase para o cérebro ou sistema nervoso central
AU2022290851A1 (en) 2021-06-08 2023-11-23 C4 Therapeutics, Inc. Therapeutics for the degradation of mutant braf
WO2022266258A1 (en) 2021-06-15 2022-12-22 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of irak-4
CN113481289B (zh) * 2021-06-22 2022-03-29 天津见康华美医学诊断技术有限公司 一种铁粒幼红细胞性贫血检测引物组合物及应用
CN113354619B (zh) * 2021-06-24 2024-03-19 皖南医学院 一种靶向泛素化降解酪氨酸酶的化合物及其制备方法和应用
JP2024526259A (ja) 2021-07-02 2024-07-17 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング 抗protac抗体および複合体
US20250129047A1 (en) 2021-07-04 2025-04-24 Newave Pharmaceutical Inc. Isoquinoline derivatives as mutant egfr modulators and uses thereof
WO2023283372A1 (en) 2021-07-07 2023-01-12 Biogen Ma Inc. Compounds for targeting degradation of irak4 proteins
CA3224732A1 (en) 2021-07-07 2023-01-12 Kevin M. Guckian Compounds for targeting degradation of irak4 proteins
CN113278023B (zh) * 2021-07-22 2021-10-15 上海睿跃生物科技有限公司 含氮杂环化合物及其制备方法和应用
EP4384828A4 (en) * 2021-08-12 2025-09-17 Univ Ramot MARKERS OF DISEASE RESISTANCE AND TOLERANCE AND THEIR USES
HUE070709T2 (hu) 2021-08-18 2025-06-28 Nurix Therapeutics Inc Interleukin-1 receptorhoz kapcsolódó kinázok kétfunkciós lebontói és terápiás alkalmazásuk
EP4395549A1 (en) 2021-09-01 2024-07-10 Oerth Bio LLC Compositions and methods for targeted degradation of proteins in a plant cell
CN115772210A (zh) * 2021-09-08 2023-03-10 苏州开拓药业股份有限公司 硫代乙内酰脲化合物或其药用盐的无定形物、晶体、药物组合物、制备方法和用途
WO2023038500A1 (ko) * 2021-09-13 2023-03-16 주식회사 유빅스테라퓨틱스 Enl 단백질 분해용 화합물 및 이들의 의약 용도
WO2023056443A1 (en) * 2021-10-01 2023-04-06 Dana-Farber Cancer Institute, Inc. Binders of cereblon and methods of use thereof
KR20240111312A (ko) 2021-10-25 2024-07-16 카이메라 쎄라퓨틱스 인코포레이티드 Tyk2 분해제 및 이의 용도
WO2023074780A1 (ja) * 2021-10-27 2023-05-04 国立大学法人愛媛大学 治療薬組成物
JP2024540080A (ja) 2021-10-29 2024-10-31 カイメラ セラピューティクス, インコーポレイテッド Irak4分解剤およびその合成
JP2024541479A (ja) 2021-11-24 2024-11-08 アルビナス・オペレーションズ・インコーポレイテッド Brm標的化化合物及び関連使用方法
CN118679160A (zh) 2021-11-24 2024-09-20 阿维纳斯运营公司 Brm靶向化合物和相关的使用方法
WO2023093845A1 (zh) 2021-11-25 2023-06-01 江苏恒瑞医药股份有限公司 一种用于雄激素受体蛋白靶向降解的嵌合体化合物、其制备方法及其在医药上的应用
WO2023121753A1 (en) 2021-12-20 2023-06-29 Massachusetts Institute Of Technology Biomolecule-polymer-pharmaceutical agent conjugates for delivering the pharmaceutical agent
WO2023119677A1 (en) 2021-12-24 2023-06-29 Astellas Pharma Inc. Pharmaceutical composition comprising a quinazoline compound
AR128330A1 (es) 2022-01-26 2024-04-17 Genentech Inc Inductores químicos de degradación conjugados con anticuerpo y métodos de estos
CN114410773B (zh) * 2022-01-27 2024-05-03 宁波大学 用于预测或诊断抑郁症复发的标志物组合及其应用
EP4472967A4 (en) 2022-01-31 2026-04-15 Kymera Therapeutics Inc Iraqi Degradation Agents and Their Uses
CA3255513A1 (en) 2022-03-11 2025-03-04 Astellas Pharma Inc. HETEROCYCLIC COMPOUND TO INDUCE DETERIORATION OF G12D MUTATION KRAS PROTEIN
CN114907386B (zh) * 2022-03-11 2023-03-31 山东大学 一种hemtac小分子降解剂及其应用
CN114560908B (zh) * 2022-03-11 2024-10-25 国家纳米科学中心 一种多肽protac分子及其制备方法和应用
CN116789636B (zh) * 2022-03-14 2026-01-30 北京康辰药业股份有限公司 双功能化合物及其制备方法、药物组合物和用途
CN119301111A (zh) 2022-03-24 2025-01-10 葛兰素史密斯克莱知识产权发展有限公司 作为protac中的降解决定子的2,4-二氧代四氢嘧啶基衍生物
EP4511128A1 (en) 2022-04-20 2025-02-26 Kumquat Biosciences Inc. Macrocyclic heterocycles and uses thereof
US20240050577A1 (en) * 2022-04-27 2024-02-15 Risen (Suzhou) Pharma Tech Co., Ltd. Cdk inhibitors and pharmaceutical uses thereof
CN119365198A (zh) 2022-05-02 2025-01-24 艾斯巴赫生物有限公司 ALC1抑制剂的用途和与PARPi的协同作用
US20260014260A1 (en) * 2022-05-24 2026-01-15 Newave Pharmaceutical Inc. Mdm2 degrader
IL316803A (en) 2022-06-06 2025-01-01 C4 Therapeutics Inc Bicyclic glutarimide-modified cervalon-binding agents
WO2024006776A1 (en) 2022-06-27 2024-01-04 Relay Therapeutics, Inc. Estrogen receptor alpha degraders and medical use thereof
CA3260847A1 (en) 2022-06-27 2024-01-04 Relay Therapeutics, Inc. Estrogen Alpha Receptor Degrading Agents and Their Uses
WO2024002205A1 (en) * 2022-06-30 2024-01-04 Anhorn Medicines Co., Ltd. Bifunctional compound and pharmaceutical composition comprising the bifunctional compound, and method for treating androgen receptor related disease by using the same
WO2024020221A1 (en) 2022-07-21 2024-01-25 Arvinas Operations, Inc. Modulators of tyk2 proteolysis and associated methods of use
WO2024019103A1 (ja) * 2022-07-21 2024-01-25 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
TW202415653A (zh) * 2022-08-02 2024-04-16 大陸商北京星奇原生物科技有限公司 Bcl-xl降解化合物
TW202412789A (zh) 2022-08-05 2024-04-01 日商安斯泰來製藥股份有限公司 用於誘導突變kras蛋白分解之雜環化合物
WO2024035780A1 (en) * 2022-08-09 2024-02-15 Board Of Regents Of The University Of Nebraska Akr1c3 targeted heterobifunctional small molecule proteolysis targeting chimeras
CN119604495A (zh) 2022-08-09 2025-03-11 安斯泰来制药株式会社 用于诱导g12v突变kras蛋白分解的杂环化合物
EP4568674A1 (en) 2022-08-12 2025-06-18 Astellas Pharma Inc. Combination of anticancer agents comprising a bifunctional compound with g12d mutant kras inhibitory activity
AU2023322690A1 (en) 2022-08-12 2025-03-20 Astellas Pharma Inc. Anti cancer combinations comprising chemotherapy
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
EP4584258A1 (en) 2022-09-07 2025-07-16 Arvinas Operations, Inc. Rapidly accelerated fibrosarcoma (raf) degrading compounds and associated methods of use
WO2024054954A1 (en) * 2022-09-08 2024-03-14 Halda Therapeutics Opco, Inc. Heterobifunctional compounds and methods of treating disease
WO2024064358A1 (en) 2022-09-23 2024-03-28 Ifm Due, Inc. Compounds and compositions for treating conditions associated with sting activity
WO2024073507A1 (en) 2022-09-28 2024-04-04 Theseus Pharmaceuticals, Inc. Macrocyclic compounds and uses thereof
JP2025533592A (ja) * 2022-09-29 2025-10-07 江▲蘇▼恒瑞医▲薬▼股▲フン▼有限公司 テトラリン系誘導体の薬学的に許容される塩、結晶型及び調製方法
CN117801051A (zh) * 2022-09-30 2024-04-02 苏州德亘生物医药有限公司 一类eRF3a靶向蛋白降解机制治疗人类肿瘤的药物
KR20250079173A (ko) 2022-10-03 2025-06-04 고리츠다이가쿠호진 요코하마시리츠다이가쿠 이환성 구조를 갖는 이미다조피리딘 유도체
EP4428134A1 (en) 2023-03-10 2024-09-11 Dark Blue Therapeutics Ltd Protac degraders of mllt1 and/or mllt3
IL321713A (en) 2022-12-27 2025-08-01 Merck Patent Gmbh Anti-PROTAC VHH antibodies and complexes
IL321942A (en) 2023-01-09 2025-09-01 Arvinas Operations Inc Modulators of BCL6 proteolysis and related methods of use
CN120530094A (zh) 2023-01-12 2025-08-22 田边三菱制药株式会社 Cereblon E3连接酶结合化合物、包含其的药物组合物及其制造方法
CN120569372A (zh) 2023-01-24 2025-08-29 第一三共株式会社 经取代的苯化合物
PE20260006A1 (es) 2023-01-26 2026-01-06 Arvinas Operations Inc Protacs degradadores de kras basados en cereblon y usos relacionados con los mismos
WO2024178348A2 (en) 2023-02-24 2024-08-29 Ppm Biopharma Llc Pleiotropic pathway modifier compounds and method of treating diseases
CN116854667A (zh) * 2023-05-17 2023-10-10 浙江工业大学 一种靶向降解pd-l1的蛋白水解靶向嵌合体及其应用
JP2026519279A (ja) * 2023-05-18 2026-06-15 アジュ ユニバーシティー インダストリー-アカデミック コーオペレイション ファウンデーション 骨分化誘導可能な新規化合物
WO2024240078A1 (en) * 2023-05-19 2024-11-28 The Chinese University Of Hong Kong Compositions and methods related to protein labeling
WO2024240858A1 (en) 2023-05-23 2024-11-28 Valerio Therapeutics Protac molecules directed against dna damage repair system and uses thereof
WO2024243441A1 (en) 2023-05-24 2024-11-28 Kumquat Biosciences Inc. Heterocyclic compounds and uses thereof
AR133028A1 (es) 2023-06-22 2025-08-20 Astellas Pharma Inc Composición farmacéutica que comprende un degradador de todas las kras
AR133027A1 (es) 2023-06-22 2025-08-20 Astellas Pharma Inc Composición farmacéutica que comprende un compuesto de quinazolina
CN122206684A (zh) 2023-06-30 2026-06-12 默克专利有限公司 用于kras蛋白降解的异双功能化合物
JP2026524477A (ja) 2023-06-30 2026-07-22 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング Krasの分解のためのヘテロ二官能性化合物
EP4735451A1 (en) 2023-06-30 2026-05-06 Kumquat Biosciences Inc. Substituted condensed tricyclic amine compounds and uses thereof as ras inhibitors
CN117263865B (zh) * 2023-08-04 2026-03-27 南开大学 以6,6-二甲基双环[3.1.1]-2-甲胺为疏水基团的蛋白降解剂及其制备方法、药物组合物和应用
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
GB202314126D0 (en) 2023-09-15 2023-11-01 Univ Oxford Innovation Ltd Compound and method
AU2024352092A1 (en) 2023-09-28 2026-04-09 Arvinas Operations, Inc. Benzimidazole and benzimidazolone based protac compounds for the targeted degradation of leucine rich repeat kinase 2 (lrrk2)
TW202530189A (zh) 2023-09-29 2025-08-01 日商第一三共股份有限公司 3-苯基丙基胺衍生物
WO2025085738A1 (en) 2023-10-18 2025-04-24 Halda Therapeutics Opco, Inc. Heterobifunctional compounds and methods of treating disease
CN122228262A (zh) 2023-11-02 2026-06-16 金橘生物科技公司 降解剂及其用途
AU2024392985A1 (en) 2023-12-08 2026-06-04 Arvinas Operations, Inc. Use of androgen receptor degrader for the treatment of spinal and bulbar muscular atrophy
CN122555560A (zh) 2023-12-21 2026-08-11 丹娜-法伯癌症研究院 激酶抑制和降解
WO2025184594A1 (en) 2024-02-29 2025-09-04 Arvinas Operations, Inc. Modulators of bcl6 proteolysis and associated methods of use
WO2025189056A1 (en) 2024-03-08 2025-09-12 Halda Therapeutics Opco, Inc. Heterobifunctional compounds and their use in treating disease
WO2025213104A1 (en) 2024-04-05 2025-10-09 Arvinas Operations, Inc. Crystalline forms of a compound for the targeted degradation of bcl6
CN118161490B (zh) * 2024-05-10 2024-07-23 昆明医科大学 一种去泛素化酶抑制剂在制备预防或者治疗炎症药物中的应用
WO2025262295A1 (en) 2024-06-21 2025-12-26 Dark Blue Therapeutics Ltd Protac degraders of mllt1 and/or mllt3
EP4667467A1 (en) 2024-06-21 2025-12-24 Dark Blue Therapeutics Ltd Protac degraders of mllt1 and/or mllt3
EP4667466A1 (en) 2024-06-21 2025-12-24 Dark Blue Therapeutics Ltd Protac degraders of mllt1 and/or mllt3
CN118459478B (zh) * 2024-07-09 2024-10-29 深圳大学 一种brd4蛋白靶向降解剂及其制备方法与应用
WO2026107062A1 (en) 2024-11-13 2026-05-21 Recludix Pharma, Inc. Stat6 degraders and uses thereof
WO2026117543A1 (en) 2024-11-26 2026-06-04 Arvinas Operations, Inc. Combination therapy for the targeted degradation of bcl6
WO2026117542A1 (en) 2024-11-26 2026-06-04 Arvinas Operations, Inc. Combination therapy for the targeted degradation of bcl6
WO2026136623A1 (en) 2024-12-19 2026-06-25 Genentech, Inc. Ire1 degrader compounds and methods of use
WO2026129303A1 (zh) * 2024-12-20 2026-06-25 上海壹迪生物技术有限公司 一种靶向雄激素受体蛋白降解的双功能化合物及其应用
WO2026139448A1 (en) 2024-12-23 2026-07-02 Merck Patent Gmbh Heterobifunctional compounds for the degradation of kras protein
CN120154610B (zh) * 2025-05-19 2025-09-02 深圳大学 抗血栓小分子化合物bptu作为黏菌素佐剂协同抗革兰氏阴性菌的应用
CN121895289A (zh) * 2026-03-23 2026-04-21 四川大学 一种哌啶-2,6-二酮类化合物、药物组合物及其制备方法和用途
CN122234044A (zh) * 2026-05-14 2026-06-19 四川大学华西医院 靶向乳酸脱氢酶的protac化合物及其制备方法和应用

Family Cites Families (27)

* 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
DE69740140D1 (de) * 1996-07-24 2011-04-14 Celgene Corp Substituierte 2-(2,6-Dioxopiperidin-3-yl)-phthalimide und Oxoisoindoline und Verfahren zur Verringerung der TNF-Alpha-Stufen
PE20020354A1 (es) 2000-09-01 2002-06-12 Novartis Ag Compuestos de hidroxamato como inhibidores de histona-desacetilasa (hda)
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
JP4361273B2 (ja) * 2001-02-27 2009-11-11 アメリカ合衆国 潜在的な血管形成阻害剤としてのサリドマイド類似体
DE10244453A1 (de) * 2002-09-24 2004-04-01 Phenomiques Gmbh Hemmung der Proteinkinase C-alpha zur Behandlung von Krankheiten
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
FR2885904B1 (fr) * 2005-05-19 2007-07-06 Aventis Pharma Sa Nouveaux derives du fluorene, compositions les contenant et utilisation
CA2822094C (en) * 2005-08-31 2015-10-27 Celgene Corporation Isoindole-imide compounds and compositions comprising and methods of using the same
RU2448101C2 (ru) * 2006-08-30 2012-04-20 Селджин Корпорейшн 5-замещенные изоиндолиновые соединения
AU2007290407A1 (en) * 2006-08-30 2008-03-06 Celgene Corporation 5-substituted isoindoline compounds
CA2957226C (en) * 2008-10-29 2018-08-14 Celgene Corporation Isoindoline compounds for use in the treatment of cancer
WO2011008260A2 (en) * 2009-07-13 2011-01-20 President And Fellows Of Harvard College Bifunctional stapled polypeptides and uses thereof
SG183257A1 (en) * 2010-02-11 2012-09-27 Celgene Corp Arylmethoxy isoindoline derivatives and compositions comprising and methods of using the same
CN103154246B (zh) 2010-05-14 2015-11-25 达那-法伯癌症研究所 用于治疗白血病的组合物和方法
ES2606958T3 (es) * 2010-05-14 2017-03-28 Dana-Farber Cancer Institute, Inc. Compuestos de tienotriazolodiazepina para tratar una neoplasia
JP2013528206A (ja) * 2010-06-09 2013-07-08 ジェネリクス・[ユーケー]・リミテッド 結晶形態のサリドマイド及びその調製方法
JP5852658B2 (ja) * 2010-09-24 2016-02-03 ザ リージェンツ オブ ザ ユニバーシティー オブ ミシガン デユビキチナーゼ阻害剤およびその使用方法
EP2649099A4 (en) 2010-12-07 2016-10-19 Univ Yale SMALL MOLECULAR HYDROPHOBIC LABELING OF FUSION PROTEINS AND INDUCED REMOVAL FROM THIS
WO2012090104A1 (en) * 2010-12-31 2012-07-05 Kareus Therapeutics, Sa Methods and compositions for designing novel conjugate therapeutics
WO2012149299A2 (en) * 2011-04-29 2012-11-01 Celgene Corporaiton Methods for the treatment of cancer and inflammatory diseases using cereblon as a predictor
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
EP4649963A3 (en) * 2014-04-14 2026-05-13 Arvinas Operations, Inc. Imide-based modulators of proteolysis and associated methods of use
US20160058872A1 (en) * 2014-04-14 2016-03-03 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
SI3526202T1 (sl) * 2016-10-11 2025-04-30 Arvinas Operations, Inc. Spojine in postopki za ciljno razgradnjo androgenskih receptorjev

Similar Documents

Publication Publication Date Title
RU2020139890A (ru) Имидные модуляторы протеолиза и способы их применения
RU2018105094A (ru) Модуляторы протеолиза на основе аланина и связанные с ними способы применения
JP2023175957A5 (enExample)
AU2020273338B2 (en) Compounds and methods for the enhanced degradation of targeted proteins
JP2021521192A5 (enExample)
AU2020245350A1 (en) Bridged tricyclic carbamoylpyridone compounds and their pharmaceutical use
EP3455219A1 (en) Amine-linked c3-glutarimide degronimers for target protein degradation
BR112017028394A2 (en) compound, composition, and methods for inducing degradation of a target protein in a cell and for treating a diseased condition or a diseased condition.
WO2008076278A4 (en) Methods of cancer treatment with igf1r inhibitors
TW202342442A (zh) Raf激酶抑制劑及其使用方法
WO2025137105A1 (en) Dual raf and tubulin inhibitors and methods of use thereof
JP2025509736A5 (enExample)
RU2022126566A (ru) Соединения и способы для улучшенного расщепления специфических белков
RU2019123462A (ru) Лиганды цереблона и бифункциональные соединения, содержащие их
HK40107897A (en) Compounds and methods for the enhanced degradation of targeted proteins
AU2024311847A1 (en) Dual raf and tubulin inhibitors and methods of use thereof
RU2020136948A (ru) Лиганды цереблона и содержащие их бифункциональные соединения
HK40085013A (en) Bridged tricyclic carbamoylpyridone compounds and their pharmaceutical use
RU2023100284A (ru) Лиганды цереблона и бифункциональные соединения, содержащие их
BR122021002241B1 (pt) Composto bifuncional, composto, composição farmacêutica, e, uso de um composto para preparar um medicamento