HK1208875A1 - Compounds & methods for the enhanced degradation of targeted proteins & other polypeptides by an e3 ubiquitin ligase e3 - Google Patents
Compounds & methods for the enhanced degradation of targeted proteins & other polypeptides by an e3 ubiquitin ligase e3Info
- Publication number
- HK1208875A1 HK1208875A1 HK15109544.5A HK15109544A HK1208875A1 HK 1208875 A1 HK1208875 A1 HK 1208875A1 HK 15109544 A HK15109544 A HK 15109544A HK 1208875 A1 HK1208875 A1 HK 1208875A1
- Authority
- HK
- Hong Kong
- Prior art keywords
- polypeptides
- compounds
- methods
- ubiquitin ligase
- targeted proteins
- Prior art date
Links
- 102000006275 Ubiquitin-Protein Ligases Human genes 0.000 title 1
- 108010083111 Ubiquitin-Protein Ligases Proteins 0.000 title 1
- 230000015556 catabolic process Effects 0.000 title 1
- 150000001875 compounds Chemical class 0.000 title 1
- 238000006731 degradation reaction Methods 0.000 title 1
- 238000000034 method Methods 0.000 title 1
- 229920001184 polypeptide Polymers 0.000 title 1
- 102000004196 processed proteins & peptides Human genes 0.000 title 1
- 108090000765 processed proteins & peptides Proteins 0.000 title 1
- 102000004169 proteins and genes Human genes 0.000 title 1
- 108090000623 proteins and genes Proteins 0.000 title 1
Classifications
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Families Citing this family (289)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
KR20130124291A (ko) | 2010-07-02 | 2013-11-13 | 길리애드 사이언시즈, 인코포레이티드 | Hiv 항바이러스 화합물로서의 2-퀴놀리닐-아세트산 유도체 |
SG186820A1 (en) | 2010-07-02 | 2013-02-28 | Gilead Sciences Inc | Napht- 2 -ylacetic acid derivatives to treat aids |
WO2012045018A1 (en) | 2010-09-30 | 2012-04-05 | St. Jude Children's Research Hospital | Aryl-substituted imidazoles |
PT2699558T (pt) | 2011-04-21 | 2016-12-29 | Gilead Sciences Inc | Compostos de benzotiazole e a sua utilização farmacêutica |
US9284323B2 (en) | 2012-01-04 | 2016-03-15 | Gilead Sciences, Inc. | Naphthalene acetic acid derivatives against HIV infection |
WO2013103724A1 (en) | 2012-01-04 | 2013-07-11 | Gilead Sciences, Inc. | 2- (tert - butoxy) -2- (7 -methylquinolin- 6 - yl) acetic acid derivatives for treating aids |
EP2800738B1 (en) * | 2012-01-06 | 2020-04-08 | Novartis AG | Heterocyclic compounds and methods for their use |
RU2666530C2 (ru) | 2012-01-12 | 2018-09-11 | Йейл Юниверсити | Соединения и способы усиления деградации белков-мишеней и других полипептидов с помощью е3 убиквитин лигазы |
WO2013159064A1 (en) | 2012-04-20 | 2013-10-24 | Gilead Sciences, Inc. | Benzothiazol- 6 -yl acetic acid derivatives and their use for treating an hiv infection |
GB201311910D0 (en) * | 2013-07-03 | 2013-08-14 | Glaxosmithkline Ip Dev Ltd | Novel Compounds |
WO2014187777A1 (en) * | 2013-05-21 | 2014-11-27 | Mediapharma S.R.L. | Novel inhibitors of pvhl-elongin c binding |
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 |
RU2738833C9 (ru) * | 2014-04-14 | 2022-02-28 | Арвинас, Оперэйшнз, Инк. | Имидные модуляторы протеолиза и способы их применения |
US20180228907A1 (en) * | 2014-04-14 | 2018-08-16 | Arvinas, Inc. | Cereblon ligands and bifunctional compounds comprising the same |
WO2015171591A1 (en) | 2014-05-05 | 2015-11-12 | Board Of Trustees Of The University Of Arkansas | COMPOSITIONS AND METHODS FOR INHIBITING ANTIAPOPTOTIC Bcl-2 PROTEINS AS ANTI-AGING AGENTS |
WO2015184383A1 (en) * | 2014-05-29 | 2015-12-03 | St. Jude Children's Research Hospital | Aryl-substituted imidazoles and methods of making and using same |
EP3177144A4 (en) | 2014-07-22 | 2018-01-24 | 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 |
WO2016045115A1 (zh) * | 2014-09-28 | 2016-03-31 | 姜凡 | Hiv-1整合酶抑制剂 |
US9694084B2 (en) | 2014-12-23 | 2017-07-04 | Dana-Farber Cancer Institute, Inc. | Methods to induce targeted protein degradation through bifunctional molecules |
WO2016105518A1 (en) | 2014-12-23 | 2016-06-30 | Dana-Farber Cancer Institute, Inc. | Methods to induce targeted protein degradation through bifunctional molecules |
EP3247708A4 (en) * | 2015-01-20 | 2018-09-12 | Arvinas, Inc. | Compounds and methods for the targeted degradation of the androgen receptor |
US20170327469A1 (en) | 2015-01-20 | 2017-11-16 | Arvinas, Inc. | Compounds and methods for the targeted degradation of androgen receptor |
GB201504314D0 (en) * | 2015-03-13 | 2015-04-29 | Univ Dundee | Small molecules |
EP4414369A3 (en) * | 2015-03-18 | 2024-10-16 | Arvinas, Inc. | Compounds and methods for the enhanced degradation of targeted proteins |
JP6708661B2 (ja) | 2015-03-30 | 2020-06-10 | ミッション セラピューティクス リミティド | Usp30阻害剤としての1−シアノ−ピロリジン化合物 |
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 |
JP6873433B2 (ja) * | 2015-06-04 | 2021-05-19 | アルヴィナス・オペレーションズ・インコーポレイテッド | タンパク質分解のイミド系修飾因子および関連の使用方法 |
US20180147202A1 (en) | 2015-06-05 | 2018-05-31 | Arvinas, Inc. | TANK-BINDING KINASE-1 PROTACs AND ASSOCIATED METHODS OF USE |
JP6954619B2 (ja) * | 2015-06-19 | 2021-10-27 | 学校法人東京理科大学 | タンパク質分解誘導タグ及びその用途 |
CN105085620B (zh) * | 2015-06-25 | 2018-05-08 | 中山大学附属第一医院 | 一种靶向泛素化降解Smad3的化合物 |
WO2017007612A1 (en) | 2015-07-07 | 2017-01-12 | Dana-Farber Cancer Institute, Inc. | Methods to induce targeted protein degradation through bifunctional molecules |
MX2018000360A (es) * | 2015-07-10 | 2018-06-11 | Arvinas Inc | Moduladores basados en mdm2 de proteolisis y metodos de uso asociados. |
MX2018000471A (es) * | 2015-07-13 | 2018-04-10 | Arvinas Inc | Moduladores de proteolisis basados en alanina y metodos de uso asociados. |
WO2017009650A1 (en) * | 2015-07-14 | 2017-01-19 | Mission Therapeutics Limited | Cyanopyrrolidines as dub inhibitors for the treatment of cancer |
EP3331906A1 (en) | 2015-08-06 | 2018-06-13 | 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 |
KR20220082095A (ko) | 2015-10-30 | 2022-06-16 | 팀버 파마슈티칼스 엘엘씨 | 이소트레티노인 제형 및 이의 용도 및 사용 방법 |
CN108366992A (zh) | 2015-11-02 | 2018-08-03 | 耶鲁大学 | 蛋白水解靶向嵌合体化合物及其制备和应用方法 |
GB201522768D0 (en) * | 2015-12-23 | 2016-02-03 | Mission Therapeutics Ltd | Novel compounds |
WO2017180417A1 (en) * | 2016-04-12 | 2017-10-19 | The Regents Of The University Of Michigan | Bet protein degraders |
US10781205B2 (en) | 2016-04-20 | 2020-09-22 | Glaxosmithkline Intellectual Property Development Limited | Conjugates comprising RIPK2 inhibitors |
JP6936498B2 (ja) * | 2016-04-21 | 2021-09-15 | バイオベンチャーズ・リミテッド・ライアビリティ・カンパニーBioVentures, LLC | 抗アポトーシス性Bcl−2ファミリータンパク質の分解を誘導する化合物及びその使用 |
CA3021358A1 (en) | 2016-04-22 | 2017-10-26 | Dana-Farber Cancer Institute, Inc. | Bifunctional molecules for degradation of egfr and methods of use |
EP3445760B1 (en) * | 2016-04-22 | 2022-02-23 | 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 |
CN107305202B (zh) * | 2016-04-22 | 2020-04-17 | 北京睿创康泰医药研究院有限公司 | 分析甲磺酸乐伐替尼及其制剂杂质的hplc方法及杂质作参比标准的用途 |
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 |
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 |
CN109641874A (zh) | 2016-05-10 | 2019-04-16 | C4医药公司 | 用于靶蛋白降解的c3-碳连接的戊二酰亚胺降解决定子体 |
EP3454862B1 (en) | 2016-05-10 | 2024-09-11 | C4 Therapeutics, Inc. | Spirocyclic degronimers for target protein degradation |
CN105943526B (zh) * | 2016-05-18 | 2018-08-14 | 上海交通大学医学院附属上海儿童医学中心 | Pd0325901在维持动脉导管开放中的应用 |
PL3458101T3 (pl) | 2016-05-20 | 2021-05-31 | F. Hoffmann-La Roche Ag | Koniugaty PROTAC-przeciwciało i sposoby ich stosowania |
KR101825065B1 (ko) * | 2016-05-24 | 2018-02-05 | 한국화학연구원 | Alk 단백질의 분해를 유도하는 약학적 조성물 및 이를 유효성분으로 함유하는 암의 예방 또는 치료용 약학적 조성물 |
GB201610156D0 (en) * | 2016-06-10 | 2016-07-27 | Otsuka Pharma Co Ltd | Cliptac compositions |
GB201610147D0 (en) * | 2016-06-10 | 2016-07-27 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
CA3025805A1 (en) * | 2016-06-23 | 2017-12-28 | James Bradner | Degradation of tripartite motif-containing protein 24 (trim24) by conjugation of trim24 inhibitors with e3 ligase ligand and methods of use |
EP3474900A4 (en) * | 2016-06-23 | 2020-03-11 | Dana-Farber Cancer Institute, Inc. | DEGRADATION OF PROTEIN 9 (BRD9) CONTAINING BROMANOMAIN BY CONJUGATING BRD9 INHIBITORS WITH E3 LIGASE LIGAND AND METHOD FOR USE THEREOF |
CN108495618B (zh) | 2016-07-12 | 2019-08-16 | 冰洲石生物科技公司 | 新的化合物及其用途 |
CN106279120A (zh) * | 2016-07-15 | 2017-01-04 | 谢阳 | 一种n‑芳基氨基甲酰基脯氨酸类化合物及其药物组合物和应用 |
CA3034326A1 (en) | 2016-08-19 | 2018-02-22 | Beigene, Ltd. | Use of a combination comprising a btk inhibitor for treating cancers |
CN106318920B (zh) * | 2016-09-14 | 2019-10-11 | 中国科学院天津工业生物技术研究所 | 黄酮-6-羟化酶及其在灯盏乙素合成中的应用 |
GB2554071A (en) * | 2016-09-14 | 2018-03-28 | Univ Dundee | Small molecules |
ES2975558T3 (es) | 2016-09-15 | 2024-07-09 | Arvinas Inc | Derivados de indol como degradantes de receptor de estrógeno |
US12129248B2 (en) | 2016-09-26 | 2024-10-29 | Dana-Farber Cancer Institute, Inc. | Chromobox protein inhibitors and uses thereof |
WO2018064589A1 (en) | 2016-09-29 | 2018-04-05 | Dana-Farber Cancer Institute, Inc. | Targeted protein degradation using a mutant e3 ubiquitin ligase |
JP6899993B2 (ja) * | 2016-10-04 | 2021-07-07 | 国立医薬品食品衛生研究所長 | 複素環化合物 |
MX2019004278A (es) | 2016-10-11 | 2019-08-05 | Arvinas Inc | Compuestos y metodos para la degradacion dirigida del receptor de angrogenos. |
EA201991071A1 (ru) | 2016-10-28 | 2019-11-29 | Композиции и способы для лечения ezh2-опосредованного рака | |
KR20230127371A (ko) | 2016-11-01 | 2023-08-31 | 아비나스 오퍼레이션스, 인코포레이티드 | 타우(Tau)-단백질 표적화 프로탁(PROTAC) 및 관련 사용 방법 |
CN106749060B (zh) * | 2016-11-11 | 2019-07-23 | 湖北龙翔药业科技股份有限公司 | 一种帕托珠利的精制方法 |
BR112019009565A2 (pt) * | 2016-11-15 | 2019-10-08 | Univ Tokyo Science Found | método de avaliação da cinética molecular e método de rastreamento |
CN110035775A (zh) | 2016-11-15 | 2019-07-19 | 学校法人东京理科大学 | Ras蛋白分解诱导分子和药物组合物 |
US11007269B2 (en) | 2016-11-15 | 2021-05-18 | Tokyo University Of Science Foundation | P53 degradation inducing molecule and pharmaceutical composition |
JP7038712B2 (ja) * | 2016-11-22 | 2022-03-18 | デイナ ファーバー キャンサー インスティチュート,インコーポレイテッド | ブルトン型チロシンキナーゼ(btk)阻害剤のe3リガーゼリガンドとのコンジュゲーションによるbtkの分解および使用法 |
CN118834201A (zh) | 2016-12-01 | 2024-10-25 | 阿尔维纳斯运营股份有限公司 | 作为雌激素受体降解剂的四氢萘和四氢异喹啉衍生物 |
US11541051B2 (en) | 2016-12-08 | 2023-01-03 | Icahn School Of Medicine At Mount Sinai | Compositions and methods for treating CDK4/6-mediated cancer |
US10954210B2 (en) | 2016-12-08 | 2021-03-23 | Hangzhou Solipharma Co., Ltd. | Crystal form of tipifarnib and preparation method and pharmaceutical composition thereof |
US11173211B2 (en) | 2016-12-23 | 2021-11-16 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides |
IL294423B2 (en) * | 2016-12-23 | 2024-01-01 | Univ Yale | Compounds and methods for targeted reduction of rapidly accelerated polypeptide fibrosarcoma |
MX2019007646A (es) * | 2016-12-23 | 2019-09-06 | Arvinas Operations Inc | Moleculas quimericas dirigidas a la proteolisis del egfr y metodos asociados de uso. |
EP3559006A4 (en) | 2016-12-23 | 2021-03-03 | Arvinas Operations, Inc. | COMPOUNDS AND METHODS FOR 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 |
CN106749513A (zh) * | 2017-01-23 | 2017-05-31 | 中国药科大学 | 基于vhl配体诱导bet降解的双功能分子及其制备和应用 |
US10604506B2 (en) | 2017-01-26 | 2020-03-31 | Arvinas Operations, Inc. | Modulators of estrogen receptor proteolysis and associated methods of use |
IL312367A (en) * | 2017-01-31 | 2024-06-01 | Arvinas Operations Inc | Servalon ligands and bifunctional compounds containing them |
AU2018219292B2 (en) * | 2017-02-08 | 2024-09-26 | Dana-Farber Cancer Institute, Inc. | Tunable endogenous protein degradation with heterobifunctional compounds |
EP3580212A4 (en) | 2017-02-08 | 2021-03-17 | Dana Farber Cancer Institute, Inc. | REGULATION OF CHIMERIC ANTIGEN RECEPTORS |
CA3059671A1 (en) * | 2017-04-14 | 2018-10-18 | University Of Dundee | Small molecules |
JP2020518660A (ja) * | 2017-04-28 | 2020-06-25 | クォーツ セラピューティクス,インコーポレイティド | Raf分解性結合体化合物 |
CN108976278B (zh) * | 2017-06-05 | 2021-04-06 | 海创药业股份有限公司 | 一种嵌合分子及其制备和应用 |
JP2020523319A (ja) * | 2017-06-07 | 2020-08-06 | シルバーバック セラピューティックス インコーポレイテッド | 免疫調節化合物の抗体コンジュゲートおよびその使用 |
CA3060372C (en) * | 2017-06-09 | 2022-04-05 | Dana-Farber Cancer Institute, Inc. | Improved methods for generating small molecule degraders and dimerizers |
CN118440096A (zh) | 2017-06-20 | 2024-08-06 | C4医药公司 | 用于蛋白降解的n/o-连接的降解决定子和降解决定子体 |
MX2019015402A (es) | 2017-06-22 | 2020-07-20 | Catalyst Biosciences Inc | Polipeptidos de serina proteasa 1 de tipo membrana modificada (mtsp-1) y metodos de uso. |
CA3066518A1 (en) | 2017-06-26 | 2019-01-03 | Beigene, Ltd. | Immunotherapy for hepatocellular carcinoma |
JP2020528918A (ja) | 2017-07-28 | 2020-10-01 | 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. | アンドロゲン受容体の標的化分解のための化合物および方法 |
EP3668976A1 (en) * | 2017-08-18 | 2020-06-24 | Cambridge Enterprise Limited | Modular binding proteins |
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 |
CN118108706A (zh) | 2017-09-04 | 2024-05-31 | C4医药公司 | 戊二酰亚胺 |
EP3679028A1 (en) | 2017-09-04 | 2020-07-15 | C4 Therapeutics, Inc. | Dihydroquinolinones |
CN111315735B (zh) | 2017-09-04 | 2024-03-08 | C4医药公司 | 二氢苯并咪唑酮 |
CA3075669A1 (en) * | 2017-09-13 | 2019-03-21 | Amgen Inc. | Bisamide sarcomere activating compounds and uses thereof |
IL273432B (en) | 2017-09-22 | 2022-09-01 | Kymera Therapeutics Inc | Protein compounds and their uses |
US11358948B2 (en) | 2017-09-22 | 2022-06-14 | Kymera Therapeutics, Inc. | CRBN ligands and uses thereof |
US10342786B2 (en) | 2017-10-05 | 2019-07-09 | Fulcrum Therapeutics, Inc. | P38 kinase inhibitors reduce DUX4 and downstream gene expression for the treatment of FSHD |
WO2019071144A1 (en) | 2017-10-05 | 2019-04-11 | Fulcrum Therapeutics, Inc. | USE OF P38 INHIBITORS TO REDUCE DUX4 EXPRESSION |
KR102129367B1 (ko) | 2017-10-20 | 2020-07-03 | 한국화학연구원 | 세레브론 단백질의 분해 유도 화합물, 이의 제조방법 및 이를 유효성분으로 함유하는 암의 예방 또는 치료용 약학적 조성물 |
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 |
EP3706737A4 (en) | 2017-11-10 | 2021-10-20 | The Regents of the University of Michigan | ASH11 INHIBITORS AND METHOD OF TREATING THEREOF |
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 |
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 |
JP2021014409A (ja) * | 2017-11-21 | 2021-02-12 | 京都薬品工業株式会社 | タンパク質結合性薬物 |
US11786529B2 (en) | 2017-11-29 | 2023-10-17 | Beigene Switzerland Gmbh | Treatment of indolent or aggressive B-cell lymphomas using a combination comprising BTK inhibitors |
CN109912655B (zh) * | 2017-12-13 | 2021-12-10 | 上海科技大学 | Alk蛋白降解剂及其抗肿瘤应用 |
EP3728251A1 (en) | 2017-12-18 | 2020-10-28 | F. Hoffmann-La Roche AG | Bifunctional inhibitors with egfr having a e3 ubiquitin ligase moiety |
IL315310A (en) | 2017-12-26 | 2024-10-01 | Kymera Therapeutics Inc | IRAK joints and used in them |
US11512080B2 (en) | 2018-01-12 | 2022-11-29 | Kymera Therapeutics, Inc. | CRBN ligands and uses thereof |
EP3737666A4 (en) | 2018-01-12 | 2022-01-05 | Kymera Therapeutics, Inc. | PROTEIN DEGRADANTS AND USES THEREOF |
JP7385284B2 (ja) | 2018-01-22 | 2023-11-22 | バイオベンチャーズ・リミテッド・ライアビリティ・カンパニー | 癌処置のためのbcl-2タンパク質分解剤 |
WO2019148055A1 (en) | 2018-01-26 | 2019-08-01 | Yale University | Imide-based modulators of proteolysis and methods of use |
TW201945357A (zh) | 2018-02-05 | 2019-12-01 | 瑞士商赫孚孟拉羅股份公司 | 化合物 |
US20210261538A1 (en) * | 2018-02-22 | 2021-08-26 | Icahn School Of Medicine At Mount Sinai | Protein arginine methyltransferase 5 (prmt5) degradation / disruption compounds and methods of use |
CN112154146A (zh) | 2018-03-06 | 2020-12-29 | 西奈山伊坎医学院 | 丝氨酸苏氨酸激酶(akt)降解/破坏化合物和使用方法 |
CN110240629B (zh) * | 2018-03-09 | 2023-10-03 | 上海科技大学 | 蛋白降解靶向bcr-abl化合物及其抗肿瘤应用 |
EP3765026A4 (en) | 2018-03-10 | 2021-12-22 | Yale University | BTK PROTEOLYSIS MODULATORS AND METHODS FOR USE |
WO2019183523A1 (en) | 2018-03-23 | 2019-09-26 | Genentech, Inc. | Hetero-bifunctional degrader compounds and their use as modulators of targeted ubiquination (vhl) |
WO2019183600A1 (en) | 2018-03-23 | 2019-09-26 | The Regents Of The University Of California | Methods and compounds for targeted autophagy |
KR20210018199A (ko) | 2018-03-26 | 2021-02-17 | 씨4 테라퓨틱스, 인코포레이티드 | 이카로스의 분해를 위한 세레블론 결합제 |
SG11202008898UA (en) * | 2018-04-01 | 2020-10-29 | Arvinas Operations Inc | Brm targeting compounds and associated methods of use |
WO2019195609A2 (en) | 2018-04-04 | 2019-10-10 | Arvinas Operations, Inc. | Modulators of proteolysis and associated methods of use |
WO2019199816A1 (en) | 2018-04-13 | 2019-10-17 | Arvinas Operations, Inc. | Cereblon ligands and bifunctional compounds comprising the same |
US11998606B2 (en) | 2018-04-13 | 2024-06-04 | Board Of Regents, The University Of Texas System | Compounds and methods for selective proteolysis of glucocorticoid receptors |
CN112312904A (zh) | 2018-04-16 | 2021-02-02 | C4医药公司 | 螺环化合物 |
EP3556760A1 (en) | 2018-04-19 | 2019-10-23 | F. Hoffmann-La Roche AG | Spiro compounds |
TWI813666B (zh) * | 2018-04-20 | 2023-09-01 | 大陸商四川科倫博泰生物醫藥股份有限公司 | 一種多功能化合物、其製備方法及其在醫藥上的應用 |
WO2019218904A1 (zh) * | 2018-05-18 | 2019-11-21 | 四川科伦博泰生物医药股份有限公司 | 非天然氨基酸类衍生物、其制备方法及用途 |
US12084423B2 (en) | 2018-05-18 | 2024-09-10 | Bioventures, Llc | Piperlongumine analogues and uses thereof |
EP3578561A1 (en) | 2018-06-04 | 2019-12-11 | F. Hoffmann-La Roche AG | Spiro compounds |
WO2019238886A1 (en) | 2018-06-13 | 2019-12-19 | University Of Dundee | Bifunctional molecules for targeting usp14 |
WO2019238817A1 (en) | 2018-06-13 | 2019-12-19 | University Of Dundee | Bifunctional molecules for targeting rpn11 |
EP3807263A1 (en) | 2018-06-13 | 2021-04-21 | Amphista Therapeutics Ltd | Bifunctional molecules for targeting uchl5 |
CN112996518A (zh) * | 2018-06-21 | 2021-06-18 | 西奈山伊坎医学院 | Wd40重复结构域蛋白5(wdr5)降解/破坏化合物和使用方法 |
CN112714646A (zh) * | 2018-07-05 | 2021-04-27 | 西奈山伊坎医学院 | 蛋白酪氨酸激酶6(ptk6)降解/破坏化合物和使用方法 |
US11292792B2 (en) | 2018-07-06 | 2022-04-05 | Kymera Therapeutics, Inc. | Tricyclic CRBN ligands and uses thereof |
US11981618B2 (en) * | 2018-07-24 | 2024-05-14 | Autotac Inc. | P62 ligand compound, and composition for preventing, ameliorating or treating proteinopathies comprising the same |
US20200038513A1 (en) * | 2018-07-26 | 2020-02-06 | Arvinas Operations, Inc. | Modulators of fak proteolysis and associated methods of use |
CN112533898A (zh) | 2018-07-31 | 2021-03-19 | 日商泛美克斯股份有限公司 | 杂环化合物 |
WO2020041331A1 (en) | 2018-08-20 | 2020-02-27 | Arvinas Operations, Inc. | Proteolysis targeting chimeric (protac) compound with e3 ubiquitin ligase binding activity and targeting alpha-synuclein protein for treating neurodegenerative diseases |
CN112888681A (zh) | 2018-08-22 | 2021-06-01 | 上海睿跃生物科技有限公司 | 原肌球蛋白受体激酶(trk)降解化合物及使用方法 |
US11969472B2 (en) | 2018-08-22 | 2024-04-30 | Cullgen (Shanghai), Inc. | Tropomyosin receptor kinase (TRK) degradation compounds and methods of use |
AU2019335516B2 (en) | 2018-09-07 | 2022-06-16 | Arvinas Operations, Inc. | Polycyclic compounds and methods for the targeted degradation of rapidly accelerated fibrosarcoma polypeptides |
US20220047596A1 (en) * | 2018-09-12 | 2022-02-17 | Board Of Regents, The University Of Texas System | Combination of parp inhibitor and brd4 inhibitor for the treatment of cancer |
JP2022501388A (ja) * | 2018-09-19 | 2022-01-06 | ラホヤ インスティチュート フォー イミュノロジー | 関節リウマチにおけるptprs及びプロテオグリカン |
KR20210077719A (ko) | 2018-10-15 | 2021-06-25 | 누릭스 테라퓨틱스 인코포레이티드 | 유비퀴틴 프로테오좀 경로를 통해 btk를 분해시키기 위한 이작용성 화합물 |
CN113056287A (zh) * | 2018-10-24 | 2021-06-29 | 豪夫迈·罗氏有限公司 | 缀合的化学降解诱导剂及使用方法 |
US20220001017A1 (en) * | 2018-11-09 | 2022-01-06 | Shanghai Qiangrui Biotech Co., Ltd. | Micromolecular compound specificallydegrading tau protein, and application thereof |
CN111171113B (zh) * | 2018-11-09 | 2023-05-16 | 汪义朋 | 一种特异性降解tau蛋白的小分子化合物及其应用 |
CN111233661B (zh) * | 2018-11-29 | 2023-03-31 | 暨南大学 | 靶向泛素化降解ERRα蛋白的化合物及其药用组合物和应用 |
JP2022516401A (ja) | 2018-11-30 | 2022-02-28 | カイメラ セラピューティクス, インコーポレイテッド | Irak分解剤およびそれらの使用 |
SG11202106507RA (en) | 2018-12-19 | 2021-07-29 | Celgene Corp | Substituted 3-((3-aminophenyl)amino)piperidine-2,6-dione compounds, compositions thereof, and methods of treatment therewith |
KR20210118828A (ko) | 2018-12-19 | 2021-10-01 | 셀진 코포레이션 | 치환된 3-((3-아미노페닐)아미노)피페리딘-2,6-디온 화합물, 이의 조성물, 및 이를 사용한 치료 방법 |
US11547759B2 (en) | 2019-01-30 | 2023-01-10 | Montelino Therapeutics, Inc. | Bi-functional compounds and methods for targeted ubiquitination of androgen receptor |
EP3917916A4 (en) | 2019-01-30 | 2022-12-14 | Montelino Therapeutics, Inc. | BIFUNCTIONAL COMPOUNDS AND METHODS FOR TARGETING ANDROGEN RECEPTOR UBIQUITINATION |
EP3922632A4 (en) * | 2019-02-07 | 2023-02-15 | Korea Research Institute of Chemical Technology | DEGRADATION AGENT THAT INDUCES DEGRADATION OF A TARGET EED PROTEIN, METHOD FOR ITS MANUFACTURE AND PHARMACEUTICAL COMPOSITION FOR THE PREVENTION OR TREATMENT OF DISEASES ASSOCIATED WITH EED, EZH2 OR PRC2 USING SUCH AGENT AS THE ACTIVE SUBSTANCE |
WO2020168172A1 (en) * | 2019-02-15 | 2020-08-20 | Zamboni Chem Solutions Inc. | Conjugate compounds for the degradation of raf |
WO2020181232A1 (en) | 2019-03-06 | 2020-09-10 | C4 Therapeutics, Inc. | Heterocyclic compounds for medical treatment |
AU2020241903A1 (en) | 2019-03-21 | 2021-10-14 | Lonza Sales Ag | Extracellular vesicle conjugates and uses thereof |
EP3941607A1 (en) | 2019-03-21 | 2022-01-26 | Codiak BioSciences, Inc. | Process for preparing extracellular vesicles |
WO2020206424A1 (en) | 2019-04-05 | 2020-10-08 | Kymera Therapeutics, Inc. | Stat degraders and uses thereof |
BR112021019722A2 (pt) | 2019-04-09 | 2021-12-14 | Nurix Therapeutics Inc | Compostos de piperidina 3-substituídos para inibição de cbl-b, e uso de inibidor de cbl-b em combinação com vacina contra câncer e/ou vírus oncolítico |
WO2020206608A1 (en) * | 2019-04-09 | 2020-10-15 | Ranok Therapeutics (Hangzhou) Co., Ltd. | Methods and compositions for targeted protein degradation |
AU2020272978A1 (en) | 2019-04-12 | 2021-09-16 | C4 Therapeutics, Inc. | Tricyclic degraders of Ikaros and Aiolos |
CA3132387A1 (en) * | 2019-04-23 | 2020-10-29 | Dana-Farber Cancer Institute, Inc. | Degraders of cyclin-dependent kinase 12 (cdk12) and uses thereof |
CN110151767B (zh) * | 2019-05-08 | 2022-10-18 | 武汉威立得生物医药有限公司 | Gnf-7在制备治疗流感病毒感染的药物中的应用 |
US11826430B2 (en) | 2019-05-14 | 2023-11-28 | Nuvation Bio Inc. | Anti-cancer nuclear hormone receptor-targeting compounds |
JP2022533147A (ja) * | 2019-05-17 | 2022-07-21 | ヒノバ ファーマシューティカルズ インコーポレイテッド | 芳香族アミン類のar及びbetを標的とするタンパク質分解キメラ化合物及び使用 |
EP3969447A1 (en) | 2019-05-17 | 2022-03-23 | Nurix Therapeutics, Inc. | Cyano cyclobutyl compounds for cbl-b inhibition and uses thereof |
US20220233702A1 (en) * | 2019-06-03 | 2022-07-28 | Regents Of The University Of Minnesota | Compounds that degrade kinases and uses thereof |
US11890346B2 (en) | 2019-06-12 | 2024-02-06 | Northwestern University | Proteolysis-targeting chimeric molecules (PROTACs) that induce degradation of c-MYC protein |
EP3989966A4 (en) | 2019-06-28 | 2023-09-27 | Kymera Therapeutics, Inc. | IRAQ DEGRADERS AND USES THEREOF |
US11912699B2 (en) | 2019-07-17 | 2024-02-27 | Arvinas Operations, Inc. | Tau-protein targeting compounds and associated |
US20220281876A1 (en) * | 2019-07-26 | 2022-09-08 | Beigene, Ltd. | Degradation of bruton's tyrosine kinase (btk) by conjugation of btk inhibitors with e3 ligase ligand and methods of use |
EP4010336A4 (en) * | 2019-08-05 | 2023-08-23 | Dana-Farber Cancer Institute, Inc. | CYCLIN-DEPENDENT KINASE 7 (CDK7) DEGRADING AGENTS AND THEIR USES |
EP4038066A1 (en) | 2019-10-01 | 2022-08-10 | Arvinas Operations, Inc. | Brm targeting compounds and associated methods of use |
CA3154386A1 (en) | 2019-10-17 | 2021-04-22 | Michael Berlin | Bifunctional molecules containing an e3 ubiquitine ligase binding moiety linked to a bcl6 targeting moiety |
IL292387A (en) | 2019-10-23 | 2022-06-01 | Stichting Het Nederlands Kanker Inst Antoni Van Leeuwenhoek Ziekenhuis | A chimeric polypeptide for immune cell regulation |
WO2021078301A1 (zh) * | 2019-10-24 | 2021-04-29 | 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 |
CN110684022B (zh) * | 2019-11-01 | 2022-07-08 | 海南一龄医疗产业发展有限公司 | Set8赖氨酸甲基转移酶抑制剂及其中间体、制备方法和用途 |
CN110759902B (zh) * | 2019-11-01 | 2022-04-22 | 海南一龄医疗产业发展有限公司 | Set8赖氨酸甲基转移酶抑制剂及其制备方法和用途 |
EP4054546A4 (en) * | 2019-11-06 | 2023-10-18 | Dana-Farber Cancer Institute, Inc. | SELECTIVE HISTONE DEACETYLASE (HDAC) DEGRADATION PRODUCTS AND METHOD FOR THE USE THEREOF |
WO2021097046A1 (en) | 2019-11-13 | 2021-05-20 | Nuvation Bio Inc. | Anti-cancer nuclear hormone receptor-targeting compounds |
WO2021113686A1 (en) | 2019-12-04 | 2021-06-10 | Omeros Corporation | Masp-2 inhibitors and methods of use |
EP4069676A1 (en) | 2019-12-04 | 2022-10-12 | Omeros Corporation | Masp-2 inhibitors and methods of use |
JP2023504543A (ja) | 2019-12-04 | 2023-02-03 | オメロス コーポレーション | Masp-2阻害剤および使用方法 |
JP2023504147A (ja) | 2019-12-04 | 2023-02-01 | 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 | ユビキチンプロテオソーム経路を介したbtkの分解のための二官能性化合物 |
US11904006B2 (en) | 2019-12-11 | 2024-02-20 | University Of Iowa Research Foundation | Poly(diaminosulfide) particle-based vaccine |
CN112979747A (zh) * | 2019-12-16 | 2021-06-18 | 江苏恒瑞医药股份有限公司 | 用于制备蛋白降解靶向嵌合体的羟脯氨酸衍生物 |
US11591332B2 (en) | 2019-12-17 | 2023-02-28 | Kymera Therapeutics, Inc. | IRAK degraders and uses thereof |
EP4076520A4 (en) | 2019-12-17 | 2024-03-27 | Kymera Therapeutics, Inc. | IRAQ DEGRADERS AND USES THEREOF |
US11883393B2 (en) | 2019-12-19 | 2024-01-30 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of androgen receptor |
EP4076450A4 (en) | 2019-12-20 | 2024-01-10 | C4 Therapeutics, Inc. | ISOINDOLINONE AND INDAZOLE COMPOUNDS FOR DEGRADING EGFR |
WO2021133920A1 (en) | 2019-12-23 | 2021-07-01 | Kymera Therapeutics, Inc. | Smarca degraders and uses thereof |
JP2023516645A (ja) * | 2020-03-04 | 2023-04-20 | ジェネンテック, インコーポレイテッド | Tead阻害剤としてのヘテロ二官能性分子 |
CA3165309A1 (en) | 2020-03-05 | 2021-09-10 | Christopher G. Nasveschuk | Compounds for targeted degradation of brd9 |
TW202200543A (zh) | 2020-03-19 | 2022-01-01 | 美商凱麥拉醫療公司 | Mdm2降解劑及其用途 |
KR20230004511A (ko) | 2020-03-21 | 2023-01-06 | 아비나스 오퍼레이션스, 인코포레이티드 | 인다졸계 화합물 및 관련된 사용 방법 |
WO2021194878A1 (en) | 2020-03-21 | 2021-09-30 | Arvinas Operations, Inc. | Selective modulators of mutant lrrk2 proteolysis and associated methods of use |
KR102337029B1 (ko) | 2020-03-27 | 2021-12-09 | (주) 업테라 | Plk1 선택적 분해 유도 화합물 |
CN115298173A (zh) * | 2020-03-31 | 2022-11-04 | 田边三菱制药株式会社 | 羟基吡咯烷衍生物及其医药用途 |
CN115803030A (zh) | 2020-04-06 | 2023-03-14 | 阿维纳斯企业公司 | 用于kras靶向降解的化合物和方法 |
CA3176547A1 (en) * | 2020-04-23 | 2021-10-28 | Milad ROUHIMOGHADAM | Gper proteolytic targeting chimeras |
US20240270780A1 (en) * | 2020-04-29 | 2024-08-15 | Tai Bi Di Pharmaceutical Technology (Shijiazhuang) Co. Ltd | Proteolysis targeting compound with tissue targeting capability and use thereof |
PE20231204A1 (es) | 2020-05-09 | 2023-08-17 | Arvinas Operations Inc | Metodos para fabricar un compuesto bifuncional, formas ultrapuras del compuesto bifuncional y formas de dosificacion que comprenden el mismo |
CN111606969B (zh) * | 2020-05-13 | 2023-02-03 | 四川大学 | 一种parp1蛋白降解剂及其在抗肿瘤中的应用 |
GB202007106D0 (en) | 2020-05-14 | 2020-07-01 | Ucl Business Plc | Cyclosporine analogues |
WO2021237100A1 (en) | 2020-05-21 | 2021-11-25 | Codiak Biosciences, Inc. | Methods of targeting extracellular vesicles to lung |
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 |
US20230183197A1 (en) * | 2020-06-01 | 2023-06-15 | Neophore Limited | Inhibitors of mlh1 and/or pms2 for cancer treatment |
CN113321700B (zh) * | 2020-06-02 | 2022-07-01 | 泰比瑞医药科技(石家庄)有限公司 | 一种降解靶蛋白的双功能化合物及其用途 |
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 |
WO2022047145A1 (en) | 2020-08-28 | 2022-03-03 | Arvinas Operations, Inc. | Rapidly accelerating fibrosarcoma protein degrading compounds and associated methods of use |
US20240241020A1 (en) | 2020-09-23 | 2024-07-18 | Lonza Sales Ag | Process for preparing extracellular vesicles |
WO2022087125A1 (en) | 2020-10-21 | 2022-04-28 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of androgen receptor protein |
CN112174999A (zh) * | 2020-11-02 | 2021-01-05 | 兰州理工大学 | 一种具有抗癌活性的钛金属配合物后修饰产物及其制备方法与应用 |
US20220144809A1 (en) | 2020-11-06 | 2022-05-12 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of androgen receptor and associated methods of use |
CA3197092A1 (en) * | 2020-11-11 | 2022-05-19 | Jakob FUHRMANN | 1-(2-(4-cyclopropyl-1h-1,2,3-triazol-1-yl)acetyl)-4-hydroxy-n-(benzyl)pyrrolidin e-2-carboxamide derivatives as vhl inhibitors for the treatment of anemia and cancer |
AR124189A1 (es) * | 2020-11-30 | 2023-02-22 | Genentech Inc | Compuestos y procedimientos de uso de los mismos |
WO2022120355A1 (en) | 2020-12-02 | 2022-06-09 | Ikena Oncology, Inc. | Tead degraders and uses thereof |
WO2022169780A1 (en) | 2021-02-02 | 2022-08-11 | Les Laboratoires Servier | Selective bcl-xl protac compounds and methods of use |
BR112023015067A2 (pt) | 2021-02-15 | 2023-10-03 | Astellas Pharma Inc | Composto de quinazolina para induzir a degradação de proteína kras g12d mutante |
WO2022187650A1 (en) * | 2021-03-04 | 2022-09-09 | The Scripps Research Institute | Heterobifunctional compositions for targeted protein degradation and methods for their use |
US20240159737A1 (en) * | 2021-03-09 | 2024-05-16 | Baylor College Of Medicine | Cellular selectivity profiling against rna helicases and splicing regulators |
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 |
AU2022238476A1 (en) | 2021-03-19 | 2023-10-05 | Arvinas Operations, Inc. | Indazole based compounds and associated methods of use |
MX2023011241A (es) | 2021-03-23 | 2023-10-03 | Nuvation Bio Inc | Compuestos dirigidos a receptores de hormonas nucleares contra el cancer. |
CA3214729A1 (en) | 2021-04-08 | 2022-10-13 | Marilena GALLOTTA | Combination therapies with cbl-b inhibitor compounds |
MX2023011940A (es) | 2021-04-16 | 2023-12-07 | Arvinas Operations Inc | Moduladores de la proteolisis bcl6 y metodos de uso asociados. |
CN115232111A (zh) * | 2021-04-23 | 2022-10-25 | 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 |
CN113603676B (zh) * | 2021-04-28 | 2022-05-24 | 浙江工业大学 | 基于厄洛替尼靶向降解egfr蛋白小分子化合物及其制备方法和应用 |
EP4334360A2 (en) | 2021-05-03 | 2024-03-13 | Avilar Therapeutics, Inc. | Potent asgpr-binding compounds for the degradation of immunoglobulins and other proteins |
CA3218577A1 (en) | 2021-05-03 | 2022-11-10 | Nuvation Bio Inc. | Anti-cancer nuclear hormone receptor-targeting compounds |
IL308314A (en) | 2021-05-07 | 2024-01-01 | Kymera Therapeutics Inc | CDK2 compounds and their uses |
EP4089103A1 (en) | 2021-05-12 | 2022-11-16 | Universität Duisburg-Essen | Clpcp protease-binding cyclic heptapeptides |
WO2022266258A1 (en) | 2021-06-15 | 2022-12-22 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of irak-4 |
WO2023283130A1 (en) | 2021-07-04 | 2023-01-12 | Newave Pharmaceutical Inc. | Isoquinoline derivatives as mutant egfr modulators and uses thereof |
WO2023034411A1 (en) | 2021-09-01 | 2023-03-09 | Oerth Bio Llc | Compositions and methods for targeted degradation of proteins in a plant cell |
US11981672B2 (en) | 2021-09-13 | 2024-05-14 | Montelino Therapeutics Inc. | Bi-functional compounds and methods for targeted ubiquitination of androgen receptor |
WO2023056069A1 (en) | 2021-09-30 | 2023-04-06 | Angiex, Inc. | Degrader-antibody conjugates and methods of using same |
JP2024539280A (ja) | 2021-10-25 | 2024-10-28 | カイメラ セラピューティクス, インコーポレイテッド | Tyk2分解剤およびそれらの使用 |
CN118574827A (zh) | 2021-11-24 | 2024-08-30 | 阿维纳斯运营公司 | Brm靶向化合物和相关的使用方法 |
EP4436966A1 (en) | 2021-11-24 | 2024-10-02 | Arvinas Operations, Inc. | Brm targeting compounds and associated methods of use |
GB202117225D0 (en) * | 2021-11-29 | 2022-01-12 | Neophore Ltd | Protac compounds |
CN113979999B (zh) * | 2021-12-23 | 2022-05-20 | 北京鑫开元医药科技有限公司 | 靶向泛素化降解bcr-abl激酶的化合物及其制备方法、组合物和用途 |
WO2023119677A1 (en) | 2021-12-24 | 2023-06-29 | Astellas Pharma Inc. | Pharmaceutical composition comprising a quinazoline compound |
WO2023141570A2 (en) * | 2022-01-21 | 2023-07-27 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of kras |
AR128330A1 (es) | 2022-01-26 | 2024-04-17 | Genentech Inc | Inductores químicos de degradación conjugados con anticuerpo y métodos de estos |
TW202339738A (zh) | 2022-01-31 | 2023-10-16 | 美商凱麥拉醫療公司 | Irak降解物及其用途 |
CN116676273A (zh) * | 2022-02-22 | 2023-09-01 | 中国科学院深圳先进技术研究院 | 一种蛋白水解靶向流感病毒及其制备方法和应用 |
WO2023171781A1 (ja) | 2022-03-11 | 2023-09-14 | アステラス製薬株式会社 | G12d変異krasタンパクの分解を誘導するための複素環化合物 |
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 |
WO2023205701A1 (en) | 2022-04-20 | 2023-10-26 | Kumquat Biosciences Inc. | Macrocyclic heterocycles and uses thereof |
WO2023220425A1 (en) * | 2022-05-12 | 2023-11-16 | Kymera Therapeutics, Inc. | Bcl-xl/bcl-2 degraders and uses thereof |
WO2024006776A1 (en) | 2022-06-27 | 2024-01-04 | Relay Therapeutics, Inc. | Estrogen receptor alpha degraders and medical use thereof |
TW202417425A (zh) | 2022-06-27 | 2024-05-01 | 美商傳達治療有限公司 | 雌激素受體α降解劑及其使用方法 |
WO2024020221A1 (en) | 2022-07-21 | 2024-01-25 | Arvinas Operations, Inc. | Modulators of tyk2 proteolysis and associated methods of use |
WO2024035780A1 (en) * | 2022-08-09 | 2024-02-15 | Board Of Regents Of The University Of Nebraska | Akr1c3 targeted heterobifunctional small molecule proteolysis targeting chimeras |
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 |
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 |
WO2024033537A1 (en) | 2022-08-12 | 2024-02-15 | Astellas Pharma Inc. | Combination of anticancer agents comprising a bifunctional compound with g12d mutant kras inhibitory activity |
WO2024039210A1 (ko) * | 2022-08-17 | 2024-02-22 | 한국화학연구원 | Cdk2 및/또는 cdk9의 억제 또는 분해용 화합물 및 이들의 의약 용도 |
WO2024040080A1 (en) * | 2022-08-19 | 2024-02-22 | Erasca, Inc. | Kras inhibitor conjugates |
CN115475164B (zh) * | 2022-08-22 | 2024-06-04 | 西安交通大学 | 一种可降解PDGFR-β的蛋白降解靶向嵌合体及其制备方法和应用 |
WO2024050016A1 (en) | 2022-08-31 | 2024-03-07 | Oerth Bio Llc | Compositions and methods for targeted inhibition and degradation of proteins in an insect cell |
US11957759B1 (en) | 2022-09-07 | 2024-04-16 | Arvinas Operations, Inc. | Rapidly accelerated fibrosarcoma (RAF) degrading compounds and associated methods of use |
WO2024064358A1 (en) | 2022-09-23 | 2024-03-28 | Ifm Due, Inc. | Compounds and compositions for treating conditions associated with sting activity |
WO2024075051A1 (en) | 2022-10-07 | 2024-04-11 | Pfizer Inc. | Hsd17b13 inhibitors and/or degraders |
WO2024081913A1 (en) * | 2022-10-14 | 2024-04-18 | 76Bio, Inc. | Dual-specific bifunctional fusion proteins for ubiquitin-mediated degradation |
WO2024127297A1 (en) | 2022-12-16 | 2024-06-20 | Pfizer Inc. | 3-fluoro-4-hydroxybenzmide-containing inhibitors and/or degraders and uses thereof |
EP4428134A1 (en) | 2023-03-10 | 2024-09-11 | Dark Blue Therapeutics Ltd | Protac degraders of mllt1 and/or mllt3 |
US20240335444A1 (en) | 2023-01-09 | 2024-10-10 | Arvinas Operations, Inc. | Modulators of bcl6 proteolysis and associated methods of use |
US20240287101A1 (en) | 2023-01-26 | 2024-08-29 | Arvinas Operations, Inc. | Cereblon-based kras degrading protacs and uses related thereto |
CN117024413B (zh) * | 2023-10-07 | 2024-01-09 | 天津匠新致成科技有限公司 | 3-氨基吡嗪-2-甲酰胺类靶向蛋白水解嵌合体及其制备方法、药物组合物和应用 |
CN117402178B (zh) * | 2023-12-15 | 2024-03-08 | 英矽智能科技(上海)有限公司 | 作为jak抑制剂和phd抑制剂的嘧啶类化合物 |
CN118515785B (zh) * | 2024-07-24 | 2024-11-08 | 上海青煜医药科技有限公司 | 融合蛋白、包含其的泛素化系统及其应用 |
Family Cites Families (97)
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 |
ES2116591T3 (es) | 1993-04-07 | 1998-07-16 | Pfizer | Cicloalquilhidroxiureas y su uso como inhibidores de la lipoxigenasa. |
DE69705838T2 (de) * | 1996-04-24 | 2002-04-11 | Medivir Uk Ltd., Cambridge | Substrate und inhibitoren von proteolytischen enzymen |
CA2204082A1 (en) * | 1996-05-03 | 1997-11-03 | Michael William John Urquhart | Pharmaceutical compounds |
US6218425B1 (en) * | 1996-08-06 | 2001-04-17 | Eli Lilly And Company | 8-substituted B-nor-6-Thiaequilenin compounds having activity as selective estrogen receptor modulators |
CA2218756A1 (en) * | 1996-10-25 | 1998-04-25 | Kristin Sue Marron | Substituted benzo¢b!thiophene compounds having activity as selective estrogen receptor modulators |
HRP970566A2 (en) | 1996-10-30 | 1998-08-31 | Jones Deborah Defeo | Conjugates useful in the treatment of prostate canser |
ATE460423T1 (de) | 1997-05-14 | 2010-03-15 | Sloan Kettering Inst Cancer | Verfahren und zubereitungen zur zerstörung bestimmter proteine |
AU740597B2 (en) | 1997-07-10 | 2001-11-08 | Merck & Co., Inc. | Conjugates useful in the treatment of prostate cancer |
WO2000008001A1 (en) * | 1998-08-07 | 2000-02-17 | Chiron Corporation | Substituted isoxazole as estrogen receptor modulators |
US7223556B1 (en) | 1998-10-09 | 2007-05-29 | President And Fellows Of Harvard College | Targeted proteolysis by recruitment to ubiquitin protein ligases |
US6306663B1 (en) | 1999-02-12 | 2001-10-23 | Proteinex, Inc. | Controlling protein levels in eucaryotic organisms |
EP1155030A4 (en) * | 1999-02-26 | 2005-12-14 | Oklahoma Med Res Found | NEW COMPOUND VON HIPPEL-LINDAU TUMOR SUPPRESSOR COMPLEX AND SCF UBIQUITIN LIGASE |
EP1176959B1 (en) | 1999-05-05 | 2006-03-08 | Merck & Co., Inc. | Novel prolines as antimicrobial agents |
US6552166B1 (en) | 1999-10-19 | 2003-04-22 | Merck & Co., Inc. | Process for the preparation of conjugates useful in the treatment of prostate cancer |
US6740495B1 (en) * | 2000-04-03 | 2004-05-25 | Rigel Pharmaceuticals, Inc. | Ubiquitin ligase assay |
US6417394B2 (en) * | 2000-04-05 | 2002-07-09 | Bristol Myers Squibb Pharma Company | Specific salt forms of triphenylethylene derivatives as selective estrogen receptor modulators |
WO2002000617A2 (en) * | 2000-06-28 | 2002-01-03 | Bristol-Myers Squibb Company | Selective androgen receptor modulators and methods for their identification, design and use |
CN1230418C (zh) * | 2000-08-24 | 2005-12-07 | 田纳西大学研究公司 | 选择性雄激素受体调节剂及其使用方法 |
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 |
AU2001295041A1 (en) | 2000-09-08 | 2002-03-22 | California Institute Of Technology | Proteolysis targeting chimeric pharmaceutical |
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 |
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 |
ATE491701T1 (de) * | 2001-08-03 | 2011-01-15 | Vertex Pharma | Von pyrazol abgeleitete kinaseinhibitoren und deren verwendung |
US20030133927A1 (en) | 2001-10-10 | 2003-07-17 | Defeo-Jones Deborah | Conjugates useful in the treatment of prostate cancer |
US7030141B2 (en) * | 2001-11-29 | 2006-04-18 | Christopher Franklin Bigge | Inhibitors of factor Xa and other serine proteases involved in the coagulation cascade |
US7053046B2 (en) | 2001-12-21 | 2006-05-30 | Mcgrath Kevin | Peptide activators of VEGF |
US20060128632A1 (en) | 2002-07-02 | 2006-06-15 | Sharma Sushil K | Peptide inhibitors of smac protein binding to inhibitor of apoptosis proteins (iap) |
US20030143590A1 (en) | 2002-11-18 | 2003-07-31 | Shyam Ramakrishnan | Regulation of human dopamine-like g protein- coupled receptor |
US7915293B2 (en) * | 2003-05-30 | 2011-03-29 | Rigel Pharmaceuticals, Inc. | Ubiquitin ligase inhibitors |
CN1835937B (zh) * | 2003-06-13 | 2012-07-18 | 詹森药业有限公司 | 作为选择性雄激素受体调节剂(sarms)的噻唑啉衍生物 |
WO2005111028A1 (en) * | 2004-05-03 | 2005-11-24 | Janssen Pharmaceutica N.V. | Novel indole derivatives as selective androgen receptor modulators (sarms) |
WO2006006065A1 (en) | 2004-07-08 | 2006-01-19 | Warner-Lambert Company Llc | Androgen modulators |
DE102008020113A1 (de) | 2008-04-23 | 2009-10-29 | Bayer Schering Pharma Aktiengesellschaft | Substituierte Dihydropyrazolone und ihre Verwendung |
US20060167066A1 (en) | 2004-12-20 | 2006-07-27 | Genentech, Inc. | Pyrrolidine inhibitors of IAP |
US20060252698A1 (en) * | 2005-04-20 | 2006-11-09 | Malcolm Bruce A | Compounds for inhibiting cathepsin activity |
US7718846B2 (en) | 2005-05-16 | 2010-05-18 | Gideon Koren | Animal models of long QT syndrome and uses thereof |
CA2620414A1 (en) | 2005-08-26 | 2007-03-01 | Methylgene Inc. | Benzodiazepine and benzopiperazine analog inhibitors of histone deacetylase |
JP5175191B2 (ja) | 2005-08-30 | 2013-04-03 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | グリコピラノシル置換ベンジルベンゼン誘導体、該化合物を含有する医薬品及びその使用と製造方法 |
CN101410381B (zh) * | 2006-01-24 | 2011-08-03 | 詹森药业有限公司 | 作为选择性雄激素受体调节剂(sarms)的2-取代的苯并咪唑 |
CA2643267A1 (en) | 2006-03-03 | 2007-09-20 | Novartis Ag | N-formyl hydroxylamine compounds |
US7989487B2 (en) * | 2006-07-06 | 2011-08-02 | University Of Medicine And Dentistry Of New Jersey | Estrogen receptor modulators and uses thereof |
WO2008011392A2 (en) * | 2006-07-20 | 2008-01-24 | Ligand Pharmacueticals Incorporated | Proline urea ccr1 antagonists for the treatment of autoimmune diseases or inflammation |
ES2403546T3 (es) | 2006-11-03 | 2013-05-20 | Pharmacyclics, Inc. | Sonda de actividad de la tirosina-cinasa de Bruton y procedimiento de utilización |
US8518891B2 (en) | 2006-11-29 | 2013-08-27 | Longqin Hu | Chemotherapeutic conjugates and methods of use |
US20080233850A1 (en) * | 2007-03-20 | 2008-09-25 | 3M Innovative Properties Company | Abrasive article and method of making and using the same |
CL2008001234A1 (es) | 2007-04-30 | 2008-09-22 | Genentech Inc | Compuestos derivados de heterociclos nitrogenados, inhibidores de las proteinas de apoptosis; y uso en el tratamiento del cancer. |
US8415340B2 (en) * | 2007-07-25 | 2013-04-09 | Bristol-Myers Squibb Company | Triazine kinase inhibitors |
KR101595238B1 (ko) * | 2007-12-21 | 2016-02-18 | 리간드 파마슈티칼스 인코포레이티드 | 선택적 안드로겐 수용체 조절제(sarm) 및 이의 용도 |
CN101910182B (zh) | 2007-12-28 | 2013-07-17 | 田边三菱制药株式会社 | 抗癌剂 |
WO2010027564A2 (en) | 2008-07-18 | 2010-03-11 | Glaxosmithkline Llc | Amido anti-viral compounds, compositions, and methods of use |
CN101768155B (zh) | 2008-12-30 | 2012-09-05 | 天津药物研究院 | 一类含(氨甲基-五元芳香杂环-4-羰基)-吡咯烷-2-羧酸的衍生物、其制备方法和用途 |
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 |
WO2011005510A2 (en) * | 2009-06-22 | 2011-01-13 | Cerapedics, Inc. | Peptide conjugates and uses thereof |
CN102510755A (zh) | 2009-07-13 | 2012-06-20 | 哈佛大学校长及研究员协会 | 双功能钉接多肽和其用途 |
US8362020B2 (en) | 2009-12-30 | 2013-01-29 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
US20110164191A1 (en) * | 2010-01-04 | 2011-07-07 | Microvision, Inc. | Interactive Projection Method, Apparatus and System |
JP5935030B2 (ja) | 2010-05-14 | 2016-06-15 | 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 | 白血病を治療するための組成物および方法 |
DK2571503T3 (en) | 2010-05-14 | 2015-04-20 | Dana Farber Cancer Inst Inc | COMPOSITIONS AND THEIR USE IN THE TREATMENT OF NEOPLASIA, INFLAMMATORY DISEASE AND OTHER DISORDERS |
WO2011160016A2 (en) * | 2010-06-17 | 2011-12-22 | The Trustees Of Columbia University In The City Of New York | E3 binding pockets and identification and use of e3 ligase inhibitors |
EP2588129A4 (en) * | 2010-06-30 | 2014-07-09 | Univ Brandeis | ON SMALL MOLECULES TARGETED PROTEIN REMOVAL |
JP5823514B2 (ja) | 2010-07-07 | 2015-11-25 | アーデリクス,インコーポレーテッド | リン酸輸送を阻害する化合物及び方法 |
WO2012009649A1 (en) | 2010-07-16 | 2012-01-19 | Anderson Gaweco | Mif inhibitors and their uses |
US8809377B2 (en) | 2010-09-24 | 2014-08-19 | 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 |
EP2696682B1 (en) | 2011-04-13 | 2018-03-21 | Innovimmune Biotherapeutics, Inc. | Mif inhibitors and their uses |
RU2666530C2 (ru) | 2012-01-12 | 2018-09-11 | Йейл Юниверсити | Соединения и способы усиления деградации белков-мишеней и других полипептидов с помощью е3 убиквитин лигазы |
WO2013106646A2 (en) | 2012-01-12 | 2013-07-18 | Yale University | Compounds and methods for the inhibition of vcb e3 ubiquitin ligase |
US20150141470A1 (en) | 2012-05-08 | 2015-05-21 | The Broad Institute, Inc. | Diagnostic and treatment methods in patients having or at risk of developing resistance to cancer therapy |
US20150119435A1 (en) | 2012-05-11 | 2015-04-30 | Yale University | Compounds useful for promoting protein degradation and methods using same |
AU2013283378B2 (en) | 2012-06-25 | 2017-07-13 | Oncoethix Gmbh | Method of treating lymphoma using thienotriazolodiazepine compounds |
KR101738063B1 (ko) | 2012-09-21 | 2017-05-19 | 아로그 파마슈티칼스, 인코퍼레이티드 | 구조적으로 활성인 인산화된 flt3 키나제의 억제 방법 |
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. |
EP2958923A1 (de) | 2013-02-22 | 2015-12-30 | Bayer Pharma Aktiengesellschaft | 4-substituierte pyrrolo- und pyrazolo-diazepine |
US9492460B2 (en) | 2013-02-27 | 2016-11-15 | Bristol-Myers Squibb Company | Carbazole compounds useful as bromodomain inhibitors |
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 |
NZ720004A (en) | 2013-11-18 | 2020-03-27 | Forma Therapeutics Inc | Tetrahydroquinoline compositions as bet bromodomain inhibitors |
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 |
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 |
EP3201199A1 (en) | 2014-10-02 | 2017-08-09 | Glaxosmithkline Intellectual Property (No. 2) Limited | Compound |
EA033325B1 (ru) | 2014-10-27 | 2019-09-30 | Тэнша Терапеутикс, Инк. | Ингибиторы бромодомена |
EP3247708A4 (en) | 2015-01-20 | 2018-09-12 | Arvinas, Inc. | Compounds and methods for the targeted degradation of the androgen receptor |
GB201504314D0 (en) | 2015-03-13 | 2015-04-29 | Univ Dundee | Small molecules |
EP4414369A3 (en) | 2015-03-18 | 2024-10-16 | 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 |
US20180147202A1 (en) | 2015-06-05 | 2018-05-31 | Arvinas, Inc. | TANK-BINDING KINASE-1 PROTACs AND ASSOCIATED METHODS OF USE |
CN108366992A (zh) * | 2015-11-02 | 2018-08-03 | 耶鲁大学 | 蛋白水解靶向嵌合体化合物及其制备和应用方法 |
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