CA3020281A1 - Monofunctional intermediates for ligand-dependent target protein degradation - Google Patents
Monofunctional intermediates for ligand-dependent target protein degradation Download PDFInfo
- Publication number
- CA3020281A1 CA3020281A1 CA3020281A CA3020281A CA3020281A1 CA 3020281 A1 CA3020281 A1 CA 3020281A1 CA 3020281 A CA3020281 A CA 3020281A CA 3020281 A CA3020281 A CA 3020281A CA 3020281 A1 CA3020281 A1 CA 3020281A1
- Authority
- CA
- Canada
- Prior art keywords
- group
- compound
- optionally substituted
- another embodiment
- hydrogen
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/10—Spiro-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D495/14—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicinal Preparation (AREA)
- Plural Heterocyclic Compounds (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Applications Claiming Priority (15)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662318974P | 2016-04-06 | 2016-04-06 | |
| US62/318,974 | 2016-04-06 | ||
| US201662321499P | 2016-04-12 | 2016-04-12 | |
| US62/321,499 | 2016-04-12 | ||
| US201662393874P | 2016-09-13 | 2016-09-13 | |
| US201662393935P | 2016-09-13 | 2016-09-13 | |
| US201662393888P | 2016-09-13 | 2016-09-13 | |
| US62/393,874 | 2016-09-13 | ||
| US62/393,935 | 2016-09-13 | ||
| US62/393,888 | 2016-09-13 | ||
| US201662409571P | 2016-10-18 | 2016-10-18 | |
| US201662409592P | 2016-10-18 | 2016-10-18 | |
| US62/409,571 | 2016-10-18 | ||
| US62/409,592 | 2016-10-18 | ||
| PCT/US2017/026275 WO2017176958A1 (en) | 2016-04-06 | 2017-04-06 | Monofunctional intermediates for ligand-dependent target protein degradation |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA3020281A1 true CA3020281A1 (en) | 2017-10-12 |
Family
ID=58549317
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA3020281A Pending CA3020281A1 (en) | 2016-04-06 | 2017-04-06 | Monofunctional intermediates for ligand-dependent target protein degradation |
Country Status (7)
| Country | Link |
|---|---|
| US (2) | US10759808B2 (enExample) |
| EP (1) | EP3440082A1 (enExample) |
| JP (2) | JP7001614B2 (enExample) |
| CN (1) | CN109311900A (enExample) |
| AU (2) | AU2017246453A1 (enExample) |
| CA (1) | CA3020281A1 (enExample) |
| WO (1) | WO2017176958A1 (enExample) |
Families Citing this family (113)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| WO2017197046A1 (en) | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | C3-carbon linked glutarimide degronimers for target protein degradation |
| 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 |
| 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 |
| 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 |
| 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 |
| MX2019005007A (es) * | 2016-11-01 | 2019-07-18 | Arvinas Inc | Protac dirigidos a la proteína tau y métodos asociados de uso. |
| US11173211B2 (en) | 2016-12-23 | 2021-11-16 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides |
| EP3577120A1 (en) | 2017-02-03 | 2019-12-11 | The Regents of The University of Michigan | Fused 1,4-diazepines as bet bromodomain inhibitors |
| EP4717317A3 (en) | 2017-06-20 | 2026-06-03 | C4 Therapeutics, Inc. | N/o-linked degrons and degronimers for protein degradation |
| 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 |
| WO2019043208A1 (en) | 2017-09-04 | 2019-03-07 | F. Hoffmann-La Roche Ag | DIHYDROQUINOLINONES |
| WO2019043217A1 (en) | 2017-09-04 | 2019-03-07 | F. Hoffmann-La Roche Ag | DIHYDROBENZIMIDAZOLONES |
| CN118108706A (zh) | 2017-09-04 | 2024-05-31 | C4医药公司 | 戊二酰亚胺 |
| WO2019060693A1 (en) | 2017-09-22 | 2019-03-28 | Kymera Therapeutics, Inc. | CRBN LIGANDS AND USES THEREOF |
| MX2020003190A (es) | 2017-09-22 | 2020-11-11 | Kymera Therapeutics Inc | Degradadores de proteinas y usos de los mismos. |
| 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 |
| IL315310A (en) | 2017-12-26 | 2024-10-01 | Kymera Therapeutics Inc | Irak degraders and uses thereof |
| 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 |
| EP3752517B1 (en) * | 2018-02-13 | 2025-04-09 | Dana-Farber Cancer Institute, Inc. | Cyclin-dependent kinase degraders and methods of use |
| 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 |
| CN110357850A (zh) * | 2018-03-26 | 2019-10-22 | 广东东阳光药业有限公司 | 一种含硫杂环化合物的制备方法 |
| US12539292B2 (en) | 2018-04-01 | 2026-02-03 | Arvinas Operations, Inc. | BRM targeting compounds and associated methods of use |
| EP3778590A4 (en) * | 2018-04-09 | 2021-12-22 | ShanghaiTech University | ANTI PROTEIN DEGRADATION COMPOUND, ANTITUMOR APPLICATION, INTERMEDIATE THEREOF, AND INTERMEDIATE USE |
| WO2019204354A1 (en) | 2018-04-16 | 2019-10-24 | C4 Therapeutics, Inc. | Spirocyclic compounds |
| EP3578561A1 (en) | 2018-06-04 | 2019-12-11 | F. Hoffmann-La Roche AG | Spiro compounds |
| WO2019242625A1 (zh) * | 2018-06-20 | 2019-12-26 | 上海科技大学 | 制备来那度胺衍生物的方法 |
| US12454520B2 (en) | 2018-07-06 | 2025-10-28 | Kymera Therapeutics, Inc. | Protein degraders and uses thereof |
| US11292792B2 (en) | 2018-07-06 | 2022-04-05 | Kymera Therapeutics, Inc. | Tricyclic CRBN ligands and uses thereof |
| 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 |
| 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 |
| 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 |
| CN110963958B (zh) * | 2018-09-30 | 2025-10-10 | 上海长森药业有限公司 | 一种mdm2抑制剂，及其制备方法、药物组合物和应用 |
| CA3121667A1 (en) * | 2018-09-30 | 2020-04-02 | Shanghai Institute Of Materia Medica, Chinese Academy Of Sciences | Isoindoline compound, preparation method, pharmaceutical composition and use thereof |
| BR112021006647A2 (pt) * | 2018-10-08 | 2021-07-13 | The Regents Of The University Of Michigan | degradores de proteína mdm2 de pequenas moléculas |
| 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) |
| JP2022507267A (ja) * | 2018-11-13 | 2022-01-18 | バイオセリックス， インコーポレイテッド | 置換イソインドリノン |
| WO2020103922A1 (en) * | 2018-11-23 | 2020-05-28 | Ascentage Pharma (Suzhou) Co., Ltd. | Novel pharmaceutical composition and use thereof |
| AU2019389174A1 (en) | 2018-11-30 | 2021-07-01 | Kymera Therapeutics, Inc. | Irak degraders and uses thereof |
| AU2019392231B2 (en) * | 2018-12-06 | 2022-10-20 | Shanghai Institute Of Materia Medica, Chinese Academy Of Sciences | Isoindoline compound, and preparation method, pharmaceutical composition, and application of isoindoline compound |
| EP3897631A4 (en) | 2018-12-20 | 2022-11-23 | C4 Therapeutics, Inc. | TARGETED PROTEIN BREAKDOWN |
| EP3932922A4 (en) | 2019-02-25 | 2022-05-11 | ShanghaiTech University | SULPHUR-CONTAINING COMPOUND BASED ON A GLUTARIMIDE FRAMEWORK AND ITS USE |
| CN113646002A (zh) * | 2019-02-27 | 2021-11-12 | 上海睿跃生物科技有限公司 | 环amp反应元件结合蛋白(cbp)和/或300kda腺病毒e1a结合蛋白(p300)降解化合物和使用方法 |
| 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 |
| WO2020251972A1 (en) | 2019-06-10 | 2020-12-17 | Kymera Therapeutics, Inc. | Smarca degraders and uses thereof |
| US12624044B2 (en) | 2019-06-10 | 2026-05-12 | Kymera Therapeutics, Inc. | SMARCA degraders and uses thereof |
| PH12022500002A1 (en) | 2019-06-28 | 2023-04-03 | Kymera Therapeutics Inc | Irak degraders and uses thereof |
| US12558427B2 (en) | 2019-07-17 | 2026-02-24 | 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 |
| 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 |
| EP4017850A1 (en) * | 2019-08-21 | 2022-06-29 | Kalvista Pharmaceuticals Limited | Enzyme inhibitors |
| 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. |
| IL292375A (en) | 2019-10-21 | 2022-06-01 | Celgene Corp | Solid forms include (s)-2-(2,6-dioxopiperidin-3-yl)-4-((2-fluoro-4-((3-morpholinoazetidin-1-yl)metyl)benzyl)amino)isoindoline-1 3- Discussion and salts from them, and preparations that include the same and their use |
| AU2020372333B2 (en) * | 2019-10-21 | 2026-08-06 | Celgene Corporation | Methods for treating a hematological cancer and the use of companion biomarkers for 2-(2,6-Dioxopiperidin-3-yl)-4-((2-fluoro-4-((3-morpholinoazetidin-1-yl)methyl)benzyl)amino)isoindoline-1,3-dione |
| WO2021119159A1 (en) | 2019-12-10 | 2021-06-17 | Kymera Therapeutics, Inc. | Irak degraders and uses thereof |
| AU2020398965A1 (en) * | 2019-12-12 | 2022-06-30 | Biotheryx, Inc. | PDE4 inhibitors, pharmaceutical compositions, and therapeutic applications |
| EP4076524A4 (en) | 2019-12-17 | 2023-11-29 | Kymera Therapeutics, Inc. | IRAQ DEGRADERS AND USES THEREOF |
| CA3161878A1 (en) | 2019-12-17 | 2021-06-24 | Matthew M. Weiss | Irak degraders and uses thereof |
| US11850239B2 (en) | 2019-12-19 | 2023-12-26 | Ascentage Pharma (Suzhou) Co., Ltd. | MDM2 inhibitor and a platinum compound for cancer treatment |
| US11679109B2 (en) | 2019-12-23 | 2023-06-20 | Kymera Therapeutics, Inc. | SMARCA degraders and uses thereof |
| GB201919219D0 (en) | 2019-12-23 | 2020-02-05 | Otsuka Pharma Co Ltd | Cancer biomarkers |
| US20230064976A1 (en) * | 2020-01-23 | 2023-03-02 | Ascentage Pharma (Suzhou) Co., Ltd. | Amorphous form or crystalline form of 2-indolinolinololylspironone compounds or their salts, solvent complexes |
| AU2021226514B2 (en) * | 2020-02-25 | 2023-10-19 | Shanghaitech University | Glutarimide skeleton-based compounds and application thereof |
| BR112022016901A2 (pt) | 2020-02-26 | 2022-12-06 | Cullgen Shanghai Inc | Compostos de degradação do receptor de tropomiosina quinase (trk) e métodos de uso |
| WO2021188948A1 (en) | 2020-03-19 | 2021-09-23 | Kymera Therapeutics, Inc. | Mdm2 degraders and uses thereof |
| AU2021247685A1 (en) * | 2020-03-31 | 2022-10-27 | Bristol-Myers Squibb Company | Conjugates |
| CN113509557A (zh) * | 2020-04-09 | 2021-10-19 | 嘉兴优博生物技术有限公司 | 靶向蛋白酶降解平台(ted) |
| 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 |
| EP4161521A4 (en) | 2020-06-03 | 2024-07-10 | Kymera Therapeutics, Inc. | DEUTERED IRAQ DEGRADERS AND USES THEREOF |
| CN116507333B (zh) * | 2020-08-27 | 2025-05-09 | 上海睿跃生物科技有限公司 | 环amp反应元件结合蛋白(cbp)和/或300kda腺病毒e1a结合蛋白(p300)降解化合物和使用方法 |
| JP2023539867A (ja) | 2020-08-27 | 2023-09-20 | 大塚製薬株式会社 | Ｍｄｍ２アンタゴニストを用いた癌治療に関するバイオマーカー |
| WO2022047145A1 (en) | 2020-08-28 | 2022-03-03 | Arvinas Operations, Inc. | Rapidly accelerating fibrosarcoma protein degrading compounds and associated methods of use |
| WO2022120355A1 (en) | 2020-12-02 | 2022-06-09 | Ikena Oncology, Inc. | Tead degraders and uses thereof |
| US12606568B2 (en) | 2020-12-09 | 2026-04-21 | Kymera Therapeutics, Inc. | SMARCA degraders and uses thereof |
| AR124547A1 (es) | 2020-12-30 | 2023-04-05 | Kymera Therapeutics Inc | Degradadores de irak y sus usos |
| 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 |
| CN112979657A (zh) * | 2021-02-03 | 2021-06-18 | 福建医科大学 | 一种靶向降解Hsp90蛋白的化合物及其制备方法与应用 |
| WO2022174268A1 (en) | 2021-02-15 | 2022-08-18 | Kymera Therapeutics, Inc. | Irak4 degraders and uses thereof |
| GB202103080D0 (en) | 2021-03-04 | 2021-04-21 | Otsuka Pharma Co Ltd | Cancer biomarkers |
| 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 |
| CN115232108B (zh) | 2021-04-23 | 2025-04-18 | 领泰生物医药(绍兴)有限公司 | Sos1降解剂及其制备方法和应用 |
| CA3217792A1 (en) | 2021-05-07 | 2022-11-10 | Kymera Therapeutics, Inc | Cdk2 degraders and uses thereof |
| TW202317546A (zh) | 2021-07-09 | 2023-05-01 | 美商普萊克斯姆公司 | 調節ikzf2之芳基化合物及醫藥組合物 |
| KR20240111312A (ko) | 2021-10-25 | 2024-07-16 | 카이메라 쎄라퓨틱스 인코포레이티드 | Tyk2 분해제 및 이의 용도 |
| 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 |
| AU2022405474B2 (en) * | 2021-12-08 | 2026-08-13 | Gluetacs Therapeutics (Shanghai) Co., Ltd. | E3 ubiquitin ligase ligand compound, protein degrader developed based thereon and their applications |
| EP4472967A4 (en) | 2022-01-31 | 2026-04-15 | Kymera Therapeutics Inc | Iraqi Degradation Agents and Their Uses |
| WO2023192534A1 (en) * | 2022-03-30 | 2023-10-05 | Ohio State Innovation Foundation | Cyclin-dependent kinase 9 (cdk9) degraders and methods of using thereof |
| EP4511128A1 (en) | 2022-04-20 | 2025-02-26 | Kumquat Biosciences Inc. | Macrocyclic heterocycles and uses thereof |
| US20250270202A1 (en) * | 2022-06-24 | 2025-08-28 | Shanghai Institute Of Materia Medica, Chinese Academy Of Sciences | Substituted 4-aminoisoindoline compound, preparation method therefor, pharmaceutical composition thereof, and use thereof |
| JP2025522795A (ja) * | 2022-06-27 | 2025-07-17 | ピン セラピューティクス、インコーポレイテッド | カゼインキナーゼ１アルファを分解するための化合物及び方法 |
| 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 |
| 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 |
| CN118019736A (zh) * | 2022-09-08 | 2024-05-10 | 标新生物医药科技(上海)有限公司 | 基于cereblon蛋白设计的分子胶化合物及其应用 |
| WO2024064316A1 (en) | 2022-09-23 | 2024-03-28 | Regents Of The University Of Michigan | Compounds and compositions as smarca2/4 inhibitors and uses thereof |
| WO2024064358A1 (en) | 2022-09-23 | 2024-03-28 | Ifm Due, Inc. | Compounds and compositions for treating conditions associated with sting activity |
| WO2024243441A1 (en) | 2023-05-24 | 2024-11-28 | Kumquat Biosciences Inc. | Heterocyclic compounds and uses thereof |
| EP4735451A1 (en) | 2023-06-30 | 2026-05-06 | Kumquat Biosciences Inc. | Substituted condensed tricyclic amine compounds and uses thereof as ras inhibitors |
| 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 |
| CN122228262A (zh) | 2023-11-02 | 2026-06-16 | 金橘生物科技公司 | 降解剂及其用途 |
| WO2026107062A1 (en) | 2024-11-13 | 2026-05-21 | Recludix Pharma, Inc. | Stat6 degraders and uses thereof |
| WO2026151924A1 (en) * | 2025-01-09 | 2026-07-16 | Triana Biomedicines, Inc. | 2-(2, 6-dioxopiperidine-3-yl)-1, 3-dioxoisoindoline derivatives bearing an heteroaryl group as anaplastic lymphoma kinase (alk) degraders and uses thereof |
Family Cites Families (78)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7083983B2 (en) | 1996-07-05 | 2006-08-01 | Cancer Research Campaign Technology Limited | Inhibitors of the interaction between P53 and MDM2 |
| WO1998011111A1 (en) | 1996-09-13 | 1998-03-19 | Yoshitomi Pharmaceutical Industries, Ltd. | Thienotriazolodiazepine compounds and medicinal uses thereof |
| US6831155B2 (en) | 1999-12-08 | 2004-12-14 | President And Fellows Of Harvard College | Inhibition of p53 degradation |
| US20030045552A1 (en) * | 2000-12-27 | 2003-03-06 | Robarge Michael J. | Isoindole-imide compounds, compositions, and uses thereof |
| US7091353B2 (en) * | 2000-12-27 | 2006-08-15 | Celgene Corporation | Isoindole-imide compounds, compositions, and uses thereof |
| KR100650966B1 (ko) | 2001-12-18 | 2006-11-30 | 에프. 호프만-라 로슈 아게 | 시스-2,4,5-트리페닐-이미다졸린 및 종양 치료에서의 그의용도 |
| JP4361798B2 (ja) | 2001-12-18 | 2009-11-11 | エフ．ホフマン−ラ ロシュ アーゲー | Ｍｄｍ２インヒビターとしてのシス−イミダゾリン |
| AU2003243594A1 (en) | 2002-06-13 | 2003-12-31 | Johns Hopkins University | Novel boronic chalcone derivatives and uses thereof |
| WO2004043371A2 (en) | 2002-11-08 | 2004-05-27 | Irm Llc | Methods and compositions for modulating p53 transcription factor |
| US20050227932A1 (en) | 2002-11-13 | 2005-10-13 | Tianbao Lu | Combinational therapy involving a small molecule inhibitor of the MDM2: p53 interaction |
| WO2004073615A2 (en) | 2003-02-13 | 2004-09-02 | Government Of The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Deazaflavin compounds and methods of use thereof |
| US6916833B2 (en) | 2003-03-13 | 2005-07-12 | Hoffmann-La Roche Inc. | Substituted piperidines |
| US7425638B2 (en) | 2003-06-17 | 2008-09-16 | Hoffmann-La Roche Inc. | Cis-imidazolines |
| US7132421B2 (en) | 2003-06-17 | 2006-11-07 | Hoffmann-La Roche Inc. | CIS-imidazoles |
| US7829742B2 (en) | 2003-12-22 | 2010-11-09 | Johns Hopkins University | Boronic acid aryl analogs |
| WO2005097820A1 (en) | 2004-04-06 | 2005-10-20 | Korea Research Institute Of Bioscience And Biotechnology | Peptides for inhibiting mdm2 function |
| KR20080027969A (ko) | 2004-05-18 | 2008-03-28 | 에프. 호프만-라 로슈 아게 | 신규 ｃｉｓ-이미다졸린 |
| GB0419481D0 (en) | 2004-09-02 | 2004-10-06 | Cancer Rec Tech Ltd | Isoindolin-1-one derivatives |
| MX2007003375A (es) | 2004-09-22 | 2007-05-07 | Janssen Pharmaceutica Nv | Inhibidores de la interaccion entre mdm2 y p53. |
| US7759383B2 (en) | 2005-02-22 | 2010-07-20 | The Regents Of The University Of Michigan | Small molecule inhibitors of MDM2 and the uses thereof |
| KR101139263B1 (ko) | 2005-03-16 | 2012-05-16 | 에프. 호프만-라 로슈 아게 | 시스-２，４，５-트리아릴-이미다졸린 및 항암 약제로서의그의 용도 |
| WO2006129623A1 (ja) | 2005-05-30 | 2006-12-07 | Mitsubishi Tanabe Pharma Corporation | チエノトリアゾロジアゼピン化合物及びその医薬としての用途 |
| US7576082B2 (en) | 2005-06-24 | 2009-08-18 | Hoffman-La Roche Inc. | Oxindole derivatives |
| CA2822094C (en) * | 2005-08-31 | 2015-10-27 | Celgene Corporation | Isoindole-imide compounds and compositions comprising and methods of using the same |
| US7495007B2 (en) | 2006-03-13 | 2009-02-24 | Hoffmann-La Roche Inc. | Spiroindolinone derivatives |
| WO2007107543A1 (en) | 2006-03-22 | 2007-09-27 | Janssen Pharmaceutica N.V. | Inhibitors of the interaction between mdm2 and p53 |
| AU2007290407A1 (en) * | 2006-08-30 | 2008-03-06 | Celgene Corporation | 5-substituted isoindoline compounds |
| US7737174B2 (en) | 2006-08-30 | 2010-06-15 | The Regents Of The University Of Michigan | Indole inhibitors of MDM2 and the uses thereof |
| US8648096B2 (en) * | 2006-09-15 | 2014-02-11 | Celgene Corporation | N-methylaminomethyl isoindole compounds and compositions comprising and methods of using the same |
| US7638548B2 (en) | 2006-11-09 | 2009-12-29 | Hoffmann-La Roche Inc. | Spiroindolinone derivatives |
| CN101605798A (zh) | 2006-12-14 | 2009-12-16 | 第一三共株式会社 | 咪唑并噻唑衍生物 |
| PT2118074E (pt) | 2007-02-01 | 2014-03-20 | Resverlogix Corp | Compostos para a prevenção e tratamento de doenças cardiovasculares |
| WO2008106507A2 (en) | 2007-02-27 | 2008-09-04 | University Of South Florida | Mdm2/mdmx inhibitor peptide |
| BRPI0810082A2 (pt) | 2007-03-29 | 2014-10-21 | Novartis Ag | 3-imidazolil-indóis para o tratamento de doenças proliferativas |
| US7625895B2 (en) | 2007-04-12 | 2009-12-01 | Hoffmann-Le Roche Inc. | Diphenyl-dihydro-imidazopyridinones |
| WO2008130614A2 (en) | 2007-04-20 | 2008-10-30 | University Of Pittsburg-Of The Commonwealth System Of Higher Education | Selective and dual-action p53/mdm2/mdm4 antagonists |
| US7553833B2 (en) | 2007-05-17 | 2009-06-30 | Hoffmann-La Roche Inc. | 3,3-spiroindolinone derivatives |
| US8288377B2 (en) | 2007-09-21 | 2012-10-16 | Janssen Pharmaceutica N.V. | Inhibitors of the interaction between MDM2 and p53 |
| CN101910182B (zh) | 2007-12-28 | 2013-07-17 | 田边三菱制药株式会社 | 抗癌剂 |
| JPWO2009151069A1 (ja) | 2008-06-12 | 2011-11-17 | 第一三共株式会社 | ４，７−ジアザスピロ［２．５］オクタン環構造を有するイミダゾチアゾール誘導体 |
| GB0811643D0 (en) | 2008-06-25 | 2008-07-30 | Cancer Rec Tech Ltd | New therapeutic agents |
| US8114995B2 (en) | 2008-06-26 | 2012-02-14 | Resverlogix Corp. | Methods of preparing quinazolinone derivatives |
| US9757368B2 (en) | 2009-04-22 | 2017-09-12 | Resverlogix Corp. | Anti-inflammatory agents |
| GB0919432D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Use |
| GB0919434D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| GB0919423D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| AU2010317096B2 (en) | 2009-11-05 | 2015-03-26 | Glaxosmithkline Llc | Benzodiazepine bromodomain inhibitor |
| GB0919426D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| CN104876938A (zh) | 2009-11-12 | 2015-09-02 | 密歇根大学董事会 | 螺-吲哚酮mdm2拮抗剂 |
| SG183257A1 (en) * | 2010-02-11 | 2012-09-27 | Celgene Corp | Arylmethoxy isoindoline derivatives and compositions comprising and methods of using the same |
| ES2606958T3 (es) | 2010-05-14 | 2017-03-28 | Dana-Farber Cancer Institute, Inc. | Compuestos de tienotriazolodiazepina para tratar una neoplasia |
| 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 |
| WO2011143651A1 (en) | 2010-05-14 | 2011-11-17 | Dana-Farber Cancer Institute, Inc. | Compositions and methods for modulating metabolism |
| EP2585465B1 (en) | 2010-06-22 | 2014-11-12 | GlaxoSmithKline LLC | Benzotriazolodiazepine compounds inhibitors of bromodomains |
| PE20140408A1 (es) | 2010-11-12 | 2014-04-10 | Univ Michigan | Derivados espiro-oxindol como antagonistas de mdm2 |
| AR084070A1 (es) | 2010-12-02 | 2013-04-17 | Constellation Pharmaceuticals Inc | Inhibidores del bromodominio y usos de los mismos |
| WO2012075456A1 (en) | 2010-12-02 | 2012-06-07 | Constellation Pharmaceuticals | Bromodomain inhibitors and uses thereof |
| EP2677865A4 (en) | 2011-02-23 | 2015-04-22 | Icahn School Med Mount Sinai | BROMODOMAIN INHIBITORS AS MODULATORS OF GENE EXPRESSION |
| WO2012151512A2 (en) | 2011-05-04 | 2012-11-08 | Constellation Pharmaceuticals, Inc. | Bromodomain inhibitors and uses thereof |
| MX346375B (es) | 2011-05-11 | 2017-03-16 | Univ Michigan Regents | Antagonistas de espiro-oxindol de mdm2. |
| WO2012174487A2 (en) | 2011-06-17 | 2012-12-20 | Constellation Pharmaceuticals, Inc. | Bromodomain inhibitors and uses thereof |
| GB201114103D0 (en) | 2011-08-17 | 2011-09-28 | Glaxosmithkline Llc | Novel compounds |
| WO2013027168A1 (en) | 2011-08-22 | 2013-02-28 | Pfizer Inc. | Novel heterocyclic compounds as bromodomain inhibitors |
| WO2013033268A2 (en) | 2011-08-29 | 2013-03-07 | Coferon, Inc. | Bivalent bromodomain ligands, and methods of using same |
| DE102011082013A1 (de) | 2011-09-01 | 2013-03-07 | Bayer Pharma AG | 6H-Thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine |
| WO2013097052A1 (en) | 2011-12-30 | 2013-07-04 | Abbott Laboratories | Bromodomain inhibitors |
| US20140079636A1 (en) * | 2012-04-16 | 2014-03-20 | Dinesh U. Chimmanamada | Targeted therapeutics |
| US20130281399A1 (en) | 2012-04-19 | 2013-10-24 | Rvx Therapeutics Inc. | Treatment of diseases by epigenetic regulation |
| WO2013155695A1 (en) | 2012-04-20 | 2013-10-24 | Abbott Laboratories | Isoindolone derivatives |
| HK1208681A1 (en) | 2012-06-12 | 2016-03-11 | Abbvie Inc. | Pyridinone and pyridazinone derivatives |
| EP2970312B1 (en) | 2013-03-11 | 2017-11-15 | The Regents of The University of Michigan | Bet bromodomain inhibitors and therapeutic methods using the same |
| WO2015077058A2 (en) * | 2013-11-08 | 2015-05-28 | The Broad Institute, Inc. | Compositions and methods for selecting a treatment for b-cell neoplasias |
| US9580430B2 (en) | 2014-02-28 | 2017-02-28 | The Regents Of The University Of Michigan | 9H-pyrimido[4,5-B]indoles and related analogs as BET bromodomain inhibitors |
| 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 |
| NZ731789A (en) * | 2014-10-30 | 2019-04-26 | Kangpu Biopharmaceuticals Ltd | Isoindoline derivative, intermediate, preparation method, pharmaceutical composition and use thereof |
| 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 |
| WO2017007612A1 (en) * | 2015-07-07 | 2017-01-12 | Dana-Farber Cancer Institute, Inc. | Methods to induce targeted protein degradation through bifunctional molecules |
-
2017
- 2017-04-06 EP EP17718291.2A patent/EP3440082A1/en not_active Withdrawn
- 2017-04-06 CA CA3020281A patent/CA3020281A1/en active Pending
- 2017-04-06 CN CN201780035311.3A patent/CN109311900A/zh active Pending
- 2017-04-06 WO PCT/US2017/026275 patent/WO2017176958A1/en not_active Ceased
- 2017-04-06 JP JP2018552788A patent/JP7001614B2/ja not_active Expired - Fee Related
- 2017-04-06 AU AU2017246453A patent/AU2017246453A1/en not_active Abandoned
- 2017-04-06 US US16/091,544 patent/US10759808B2/en active Active
-
2020
- 2020-08-31 US US17/007,191 patent/US20210002289A1/en not_active Abandoned
-
2021
- 2021-09-15 AU AU2021232732A patent/AU2021232732A1/en not_active Abandoned
- 2021-12-24 JP JP2021210079A patent/JP2022050469A/ja not_active Withdrawn
Also Published As
| Publication number | Publication date |
|---|---|
| US20210002289A1 (en) | 2021-01-07 |
| EP3440082A1 (en) | 2019-02-13 |
| JP2019513746A (ja) | 2019-05-30 |
| AU2021232732A1 (en) | 2021-10-14 |
| JP2022050469A (ja) | 2022-03-30 |
| AU2017246453A1 (en) | 2018-11-08 |
| US20190119289A1 (en) | 2019-04-25 |
| JP7001614B2 (ja) | 2022-02-03 |
| WO2017176958A1 (en) | 2017-10-12 |
| CN109311900A (zh) | 2019-02-05 |
| US10759808B2 (en) | 2020-09-01 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AU2017246453A1 (en) | Monofunctional intermediates for ligand-dependent target protein degradation | |
| EP3409276B1 (en) | Ire-1a inhibitors | |
| CA2748251C (en) | Bicyclic heterocyclic compound for use as a sensory neuron specific sodium channel inhibitor | |
| AU2002219555B2 (en) | VLA-4 Inhibitors | |
| EP0634169B1 (en) | Quinoline or quinazoline derivatives and their use in the manufacture of a medicament for the treatment of osteoporosis | |
| CA2900695A1 (en) | Heterocyclic amides as kinase inhibitors | |
| JP6268276B2 (ja) | ＰＥＲＫ阻害剤としての新規なＮ（２，３−ジヒドロ−１Ｈ−ピロロ［２，３−ｂ］ピリジン−５−イル）−４−キナゾリンアミン誘導体およびＮ−（２，３−ジヒドロ−１Ｈ−インドール−５−イル）−４−キナゾリンアミン誘導体 | |
| WO2012176763A1 (ja) | 新規インダゾール誘導体 | |
| MXPA05000336A (es) | Antagonistas del receptor 1 de hormona de concentracion de melanina (mchir). | |
| CN106536491B (zh) | 作为盐皮质激素受体调节剂的苯并噁嗪酮酰胺 | |
| CA2870407A1 (en) | Aminoquinazoline and pyridopyrimidine derivatives | |
| WO2017006953A1 (ja) | ＴｒｋＡ阻害活性を有する複素環誘導体 | |
| CA2927182A1 (en) | Quinolinyl modulators of ror.gamma.t | |
| JP7778750B2 (ja) | ３－（５－フルオロベンゾフラン－３－イル）－４－（５－メチル－５Ｈ－［１，３］ジオキソロ［４，５－ｆ］インドール－７－イル）ピロール－２，５－ジオンの固体形態 | |
| CA2897417A1 (en) | New dihydroquinoline-2-one derivatives as aldosterone synthase (cyp11b2 or cyp11b1) inhibitors | |
| CA2800521A1 (en) | Fused imidazole derivative | |
| MX2012005189A (es) | Inhibidores de ire-1-alfa. | |
| AU2006298164A1 (en) | Novel fused pyrrole derivative | |
| JPWO2016098793A1 (ja) | 環状グアニジル基を有するチアゾール誘導体 | |
| JP2000514078A (ja) | 骨吸収阻害剤として有用なヘテロ芳香族ペンタジエン酸誘導体 | |
| CN107614498A (zh) | 二氮杂‑苯并荧蒽类化合物 | |
| CA3181583A1 (en) | Methods of use for pyrimidines as ferroportin inhibitors | |
| JP4685307B2 (ja) | ビトロネクチン受容体アンタゴニスト | |
| KR20200100615A (ko) | 3-(5-플루오로벤조푸란-3-일)-4-(5-메틸-5H-[1,3]디옥솔로[4,5-f]인돌-7-일)피롤-2,5-디온의 고체 형태 | |
| WO2014024119A1 (en) | Heterocyclic amides as itk inhibitors |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| EEER | Examination request |
Effective date: 20220309 |