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 | |
| US201662393888P | 2016-09-13 | 2016-09-13 | |
| US201662393935P | 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 (100)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SG11201808728QA (en) * | 2016-04-06 | 2018-11-29 | Univ Michigan Regents | Mdm2 protein degraders |
| UA123168C2 (uk) * | 2016-04-12 | 2021-02-24 | Дзе Ріджентс Оф Дзе Юніверсіті Оф Мічіган | Деструктори білка вет |
| WO2017197055A1 (en) | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | Heterocyclic degronimers for target protein degradation |
| EP3454862B1 (en) | 2016-05-10 | 2024-09-11 | C4 Therapeutics, Inc. | Spirocyclic degronimers for target protein degradation |
| 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 |
| 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 |
| EP3512855B1 (en) * | 2016-09-13 | 2022-07-27 | The Regents of the University of Michigan | Fused 1,4-oxazepines as bet protein degraders |
| US10975093B2 (en) * | 2016-09-13 | 2021-04-13 | The Regents Of The University Of Michigan | Fused 1,4-diazepines as BET protein degraders |
| EP3535265A4 (en) * | 2016-11-01 | 2020-07-08 | Arvinas, Inc. | PROTACS TARGETING ON TAU PROTEIN AND RELATED METHODS FOR USE |
| US11173211B2 (en) | 2016-12-23 | 2021-11-16 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides |
| WO2018144789A1 (en) * | 2017-02-03 | 2018-08-09 | The Regents Of The University Of Michigan | Fused 1,4-diazepines as bet bromodomain inhibitors |
| CN110769822A (zh) | 2017-06-20 | 2020-02-07 | 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 |
| 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 |
| EP3679028A1 (en) | 2017-09-04 | 2020-07-15 | C4 Therapeutics, Inc. | Dihydroquinolinones |
| CN111278815B (zh) | 2017-09-04 | 2024-03-08 | C4医药公司 | 戊二酰亚胺 |
| WO2019043217A1 (en) | 2017-09-04 | 2019-03-07 | F. Hoffmann-La Roche Ag | DIHYDROBENZIMIDAZOLONES |
| WO2019060693A1 (en) | 2017-09-22 | 2019-03-28 | Kymera Therapeutics, Inc. | CRBN LIGANDS AND USES THEREOF |
| CA3076613A1 (en) | 2017-09-22 | 2019-03-28 | Kymera Therapeutics, Inc. | Protein degraders and uses thereof |
| WO2019094772A1 (en) | 2017-11-10 | 2019-05-16 | The Regents Of The University Of Michigan | Ash1l degraders and methods of treatment therewith |
| 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 |
| IL315310A (en) | 2017-12-26 | 2024-10-01 | Kymera Therapeutics Inc | Irak degraders and uses thereof |
| US11485743B2 (en) | 2018-01-12 | 2022-11-01 | Kymera Therapeutics, Inc. | Protein degraders and uses thereof |
| EP3737675A4 (en) | 2018-01-12 | 2022-01-05 | 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 |
| 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 |
| JP2021519337A (ja) * | 2018-03-26 | 2021-08-10 | シー４ セラピューティクス， インコーポレイテッド | Ｉｋａｒｏｓの分解のためのセレブロン結合剤 |
| KR102548191B1 (ko) * | 2018-04-09 | 2023-06-28 | 상하이테크 유니버시티 | 표적 단백질 분해 화합물, 이의 항종양 응용, 이의 중간체 및 중간체의 응용 |
| EP3781156A4 (en) | 2018-04-16 | 2022-05-18 | 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 |
| WO2020010227A1 (en) | 2018-07-06 | 2020-01-09 | 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 |
| PL3820573T3 (pl) * | 2018-07-10 | 2024-02-19 | Novartis Ag | Pochodne 3-(5-hydroksy-1-oksoizoindolin-2-ylo)piperydyno-2,6-dionu i ich zastosowanie w leczeniu chorób zależnych od palca cynkowego z rodziny ikaros 2 (ikzf2) |
| 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 |
| JP7297053B2 (ja) | 2018-08-20 | 2023-06-23 | アルビナス・オペレーションズ・インコーポレイテッド | 神経変性疾患を治療するためのｅ３ユビキチンリガーゼ結合活性を有するキメラ（ｐｒｏｔａｃ）化合物を標的とし、アルファ－シヌクレインタンパク質を標的とするタンパク質分解 |
| US11969472B2 (en) | 2018-08-22 | 2024-04-30 | Cullgen (Shanghai), Inc. | Tropomyosin receptor kinase (TRK) degradation compounds and methods of use |
| CN112888681B (zh) | 2018-08-22 | 2025-11-18 | 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 |
| EP3846800A4 (en) | 2018-09-04 | 2022-08-24 | 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 |
| EP3862348A4 (en) * | 2018-09-30 | 2022-06-22 | Shanghai Institute of Materia Medica, Chinese Academy of Sciences | ISOINDOLINE COMPOUND, PROCESS OF MANUFACTURE, PHARMACEUTICAL COMPOSITION AND USE THEREOF |
| MX2021003999A (es) * | 2018-10-08 | 2021-06-23 | Univ Michigan Regents | Moleculas de bajo peso molecular degradadoras de la proteina mdm2. |
| 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) |
| EP3880669A1 (en) | 2018-11-13 | 2021-09-22 | Biotheryx, Inc. | Substituted isoindolinones |
| AU2019384292A1 (en) | 2018-11-23 | 2021-01-14 | Ascentage Pharma (Suzhou) Co., Ltd. | Novel pharmaceutical composition and use thereof |
| JP7623943B2 (ja) | 2018-11-30 | 2025-01-29 | 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 |
| 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 |
| CN120698985A (zh) | 2018-12-20 | 2025-09-26 | C4医药公司 | 靶向蛋白降解 |
| WO2020173440A1 (en) * | 2019-02-27 | 2020-09-03 | Cullgen (Shanghai), Inc. | Cyclic-amp response element binding protein (cbp) and/or adenoviral e1a binding protein of 300 kda (p300) degradation compounds and methods of use |
| MX2021012216A (es) | 2019-04-05 | 2022-01-24 | Kymera Therapeutics Inc | Degradadores de transductores de señal y activadores de transcripción (stat) y usos de los mismos. |
| CA3144805A1 (en) | 2019-06-28 | 2020-12-30 | Kymera Therapeutics, Inc. | Irak degraders and uses thereof |
| CN114867727B (zh) | 2019-07-17 | 2025-02-21 | 阿尔维纳斯运营股份有限公司 | Tau蛋白靶向化合物及相关使用方法 |
| 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 |
| CN114258392A (zh) * | 2019-08-21 | 2022-03-29 | 卡尔维斯塔制药有限公司 | 酶抑制剂 |
| 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 |
| EP4048668A4 (en) * | 2019-10-21 | 2024-03-13 | 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 |
| WO2021119571A1 (en) * | 2019-12-12 | 2021-06-17 | Biotheryx, Inc. | Pde4 inhibitors, pharmaceutical compositions, and therapeutic applications |
| US11591332B2 (en) | 2019-12-17 | 2023-02-28 | Kymera Therapeutics, Inc. | IRAK degraders and uses thereof |
| KR20220145325A (ko) | 2019-12-17 | 2022-10-28 | 카이메라 쎄라퓨틱스 인코포레이티드 | Irak 분해제 및 이의 용도 |
| US11850239B2 (en) | 2019-12-19 | 2023-12-26 | Ascentage Pharma (Suzhou) Co., Ltd. | MDM2 inhibitor and a platinum compound for cancer treatment |
| WO2021133920A1 (en) | 2019-12-23 | 2021-07-01 | 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 |
| WO2023205701A1 (en) | 2022-04-20 | 2023-10-26 | Kumquat Biosciences Inc. | Macrocyclic heterocycles and uses thereof |
| US20230096517A1 (en) * | 2020-02-25 | 2023-03-30 | Shanghaitech University | Glutarimide skeleton-based compounds and application thereof |
| AU2021225981A1 (en) | 2020-02-26 | 2022-09-29 | Cullgen (Shanghai) , Inc. | Tropomyosin receptor kinase (TRK) degradation compounds and methods of use |
| WO2021188948A1 (en) * | 2020-03-19 | 2021-09-23 | Kymera Therapeutics, Inc. | Mdm2 degraders and uses thereof |
| EP4126068A4 (en) * | 2020-03-31 | 2024-12-04 | Orum Therapeutics Inc. | 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 |
| US20230313313A1 (en) | 2020-08-27 | 2023-10-05 | Otsuka Pharmaceutical Co., Ltd. | Biomarkers for cancer therapy using mdm2 antagonists |
| 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 |
| US12180193B2 (en) | 2020-08-28 | 2024-12-31 | Arvinas Operations, Inc. | 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 |
| AR124547A1 (es) | 2020-12-30 | 2023-04-05 | Kymera Therapeutics Inc | Degradadores de irak y sus usos |
| CA3208313A1 (en) | 2021-01-13 | 2022-07-21 | Monte Rosa Therapeutics Ag | Isoindolinone compounds |
| 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 |
| MX2023009527A (es) | 2021-02-15 | 2023-08-24 | Kymera Therapeutics Inc | Degradadores de la cinasa 4 asociada al receptor de interleucina 1 (irak4) y usos de los mismos. |
| GB202103080D0 (en) | 2021-03-04 | 2021-04-21 | Otsuka Pharma Co Ltd | Cancer biomarkers |
| AU2022259683A1 (en) | 2021-04-16 | 2023-10-19 | Arvinas Operations, Inc. | Modulators of bcl6 proteolysis and associated methods of use |
| 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 |
| AR125798A1 (es) | 2021-05-07 | 2023-08-16 | Kymera Therapeutics Inc | Degradadores cdk2 y usos de los mismos |
| AU2022306297A1 (en) | 2021-07-09 | 2024-02-08 | Plexium, Inc. | Aryl compounds and pharmaceutical compositions that modulate ikzf2 |
| US20250051338A1 (en) | 2021-10-25 | 2025-02-13 | Kymera Therapeutics, Inc. | Tyk2 degraders and uses thereof |
| EP4422635A4 (en) | 2021-10-29 | 2025-11-26 | Kymera Therapeutics Inc | IRAQ4 DEGRADATION AGENTS AND THEIR SYNTHESIS |
| CA3243560A1 (en) | 2022-01-31 | 2023-08-03 | Kymera Therapeutics, Inc. | Iraqi Degradation Agents and Their Uses |
| US20250236607A1 (en) * | 2022-03-30 | 2025-07-24 | Ohio State Innovation Foundation | Cyclin-dependent kinase 9 (cdk9) degraders and methods of using thereof |
| CN117285524A (zh) * | 2022-06-24 | 2023-12-26 | 中国科学院上海药物研究所 | 一类取代的4-氨基异吲哚啉类化合物、其制备方法、药物组合物及应用 |
| JP2025521686A (ja) | 2022-06-27 | 2025-07-10 | リレー セラピューティクス， インコーポレイテッド | エストロゲン受容体アルファ分解剤及びその使用 |
| WO2024003749A1 (en) * | 2022-06-27 | 2024-01-04 | Pin Therapeutics, Inc. | Compounds and methods for degrading casein kinase 1 alpha |
| WO2024006776A1 (en) | 2022-06-27 | 2024-01-04 | Relay Therapeutics, Inc. | Estrogen receptor alpha degraders and medical use thereof |
| 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 |
| WO2024051766A1 (zh) * | 2022-09-08 | 2024-03-14 | 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 |
| WO2024064358A1 (en) | 2022-09-23 | 2024-03-28 | Ifm Due, Inc. | Compounds and compositions for treating conditions associated with sting activity |
| WO2024064316A1 (en) | 2022-09-23 | 2024-03-28 | Regents Of The University Of Michigan | Compounds and compositions as smarca2/4 inhibitors and uses thereof |
| CN120981456A (zh) | 2023-05-24 | 2025-11-18 | 金橘生物科技公司 | 杂环化合物及其用途 |
| WO2025007000A1 (en) | 2023-06-30 | 2025-01-02 | 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 |
| WO2025096855A1 (en) | 2023-11-02 | 2025-05-08 | Kumquat Biosciences Inc. | 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 |
| EP0989131B1 (en) | 1996-09-13 | 2002-11-13 | Mitsubishi Pharma Corporation | 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 |
| CA2468783A1 (en) | 2001-12-18 | 2003-06-26 | F. Hoffmann-La Roche Ag | Cis-imidazolines as mdm2 inhibitors |
| WO2003051359A1 (en) | 2001-12-18 | 2003-06-26 | F.Hoffmann-La Roche Ag | Cis-2,4,5- triphenyl-imidazolines and their use in the treatment of tumors |
| WO2003106384A2 (en) | 2002-06-01 | 2003-12-24 | Johns Hopkins University | Novel boronic chalcone derivatives and uses thereof |
| AU2003291269A1 (en) | 2002-11-08 | 2004-06-03 | 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 |
| AU2004212928A1 (en) | 2003-02-13 | 2004-09-02 | Bioveris Corporation | 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 |
| WO2005063774A1 (en) | 2003-12-22 | 2005-07-14 | Johns Hopkins University | Boronic acid aryl analogs |
| US8598127B2 (en) | 2004-04-06 | 2013-12-03 | Korea Research Institute Of Bioscience & Biotechnology | Peptides for inhibiting MDM2 function |
| JP4814228B2 (ja) | 2004-05-18 | 2011-11-16 | エフ．ホフマン−ラ ロシュ アーゲー | 新規ｃｉｓ−イミダゾリン |
| GB0419481D0 (en) | 2004-09-02 | 2004-10-06 | Cancer Rec Tech Ltd | Isoindolin-1-one derivatives |
| KR101331786B1 (ko) | 2004-09-22 | 2013-11-21 | 얀센 파마슈티카 엔.브이. | Ｍｄｍ2 및 ｐ53간의 상호작용 저해제 |
| US7759383B2 (en) | 2005-02-22 | 2010-07-20 | The Regents Of The University Of Michigan | Small molecule inhibitors of MDM2 and the uses thereof |
| JP4955646B2 (ja) | 2005-03-16 | 2012-06-20 | エフ．ホフマン−ラ ロシュ アーゲー | シス−２，４，５−トリアリール−イミダゾリン及びそれらの抗癌薬としての使用 |
| 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 |
| MX2008002765A (es) * | 2005-08-31 | 2008-04-07 | Celgene Corp | Compuestos de isoindol-imida y composiciones que la comprenden y metodos para usar los mismos. |
| US7495007B2 (en) | 2006-03-13 | 2009-02-24 | Hoffmann-La Roche Inc. | Spiroindolinone derivatives |
| CA2644643C (en) | 2006-03-22 | 2015-05-19 | Janssen Pharmaceutica N.V. | Inhibitors of the interaction between mdm2 and p53 |
| US7737174B2 (en) | 2006-08-30 | 2010-06-15 | The Regents Of The University Of Michigan | Indole inhibitors of MDM2 and the uses thereof |
| CA2660806C (en) * | 2006-08-30 | 2015-06-16 | Celgene Corporation | 5-substituted isoindoline compounds |
| RS51725B (sr) * | 2006-09-15 | 2011-10-31 | Celgene Corporation | Jedinjenja n-metilaminometil izoindola i kompozicije koje ih sadrže i upotreba istih |
| 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 |
| SI2118074T1 (sl) | 2007-02-01 | 2014-05-30 | Resverlogix Corp. | Spojine za preprečevanje in zdravljenje kardiovaskularnih bolezni |
| WO2008106507A2 (en) | 2007-02-27 | 2008-09-04 | University Of South Florida | Mdm2/mdmx inhibitor peptide |
| EA200901212A1 (ru) | 2007-03-29 | 2010-04-30 | Новартис Аг | 3-имидазолилиндолы, предназначенные для лечения пролиферативных заболеваний |
| 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 |
| JP5438008B2 (ja) | 2007-09-21 | 2014-03-12 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | ＭＤＭ２とｐ５３の間の相互作用の阻害剤 |
| JP5478262B2 (ja) | 2007-12-28 | 2014-04-23 | 田辺三菱製薬株式会社 | 抗癌剤 |
| WO2009151069A1 (ja) | 2008-06-12 | 2009-12-17 | 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 |
| AU2009262252B2 (en) | 2008-06-26 | 2013-05-02 | Resverlogix Corp. | Methods of preparing quinazolinone derivatives |
| BRPI1014956B8 (pt) | 2009-04-22 | 2021-05-25 | Resverlogix Corp | agentes anti-inflamatórios |
| GB0919434D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| GB0919432D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Use |
| HUE026967T2 (en) | 2009-11-05 | 2016-07-28 | Glaxosmithkline Llc | Benzodiazepine Bromodomain inhibitor |
| GB0919426D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| GB0919423D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| AU2010319595B2 (en) | 2009-11-12 | 2015-09-17 | The Regents Of The University Of Michigan | Spiro-oxindole MDM2 antagonists |
| RS56232B1 (sr) * | 2010-02-11 | 2017-11-30 | Celgene Corp | Derivati arilmetoksi izoindolina i kompozicije koje ih obuhvataju i postupci njihove primene |
| JP5913292B2 (ja) | 2010-05-14 | 2016-04-27 | 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 | 代謝を調節する組成物および方法 |
| CA2799403C (en) | 2010-05-14 | 2020-01-21 | Dana-Farber Cancer Institute, Inc. | Compositions and methods for treating leukemia |
| 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 |
| ES2526671T3 (es) | 2010-06-22 | 2015-01-14 | Glaxosmithkline Llc | Compuestos de benzotriazoldiazepina inhibidores de bromodominios |
| CA2817585A1 (en) | 2010-11-12 | 2012-05-18 | The Regents Of The University Of Michigan | Spiro-oxindole mdm2 antagonists |
| US9249161B2 (en) | 2010-12-02 | 2016-02-02 | Constellation Pharmaceuticals, Inc. | Bromodomain inhibitors and uses thereof |
| AR084070A1 (es) | 2010-12-02 | 2013-04-17 | Constellation Pharmaceuticals Inc | Inhibidores del bromodominio y usos de los mismos |
| CA2828212A1 (en) | 2011-02-23 | 2012-08-30 | Shiraz Mujtaba | Inhibitors of bromodomains as modulators of gene expression |
| EP2705039B1 (en) | 2011-05-04 | 2017-07-26 | Constellation Pharmaceuticals, Inc. | Bromodomain inhibitors and uses thereof |
| CA2835422C (en) | 2011-05-11 | 2016-10-11 | The Regents Of The University Of Michigan | Spiro-oxindole mdm2 antagonists |
| 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 |
| WO2013033270A2 (en) | 2011-08-29 | 2013-03-07 | Coferon, Inc. | Bromodomain ligands capable of dimerizing in an aqueous solution, 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 |
| SG11201408324QA (en) | 2012-06-12 | 2015-01-29 | Abbvie Inc | Pyridinone and pyridazinone derivatives |
| AU2014249192B2 (en) | 2013-03-11 | 2017-12-21 | The Regents Of The University Of Michigan | BET bromodomain inhibitors and therapeutic methods using the same |
| US20160282354A1 (en) * | 2013-11-08 | 2016-09-29 | The Broad Institute, Inc. | Compositions and methods for selecting a treatment for b-cell neoplasias |
| CA2940554A1 (en) | 2014-02-28 | 2015-09-03 | The Regents Of The University Of Michigan | 9h-pyrimido[4,5-b]indoles and related analogs as bet bromodomain inhibitors |
| US20160058872A1 (en) * | 2014-04-14 | 2016-03-03 | Arvinas, Inc. | Imide-based modulators of proteolysis and associated methods of use |
| MX387318B (es) * | 2014-04-14 | 2025-03-18 | Arvinas Operations Inc | Moduladores de la proteólisis basados en imida y métodos de uso asociados. |
| ES2812877T3 (es) * | 2014-10-30 | 2021-03-18 | Kangpu Biopharmaceuticals Ltd | Derivado de isoindolina, producto intermedio, método de preparación, composición farmacéutica y uso del mismo |
| 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 CA CA3020281A patent/CA3020281A1/en active Pending
- 2017-04-06 EP EP17718291.2A patent/EP3440082A1/en not_active Withdrawn
- 2017-04-06 WO PCT/US2017/026275 patent/WO2017176958A1/en not_active Ceased
- 2017-04-06 CN CN201780035311.3A patent/CN109311900A/zh active Pending
- 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 |
|---|---|
| AU2021232732A1 (en) | 2021-10-14 |
| AU2017246453A1 (en) | 2018-11-08 |
| JP7001614B2 (ja) | 2022-02-03 |
| US20190119289A1 (en) | 2019-04-25 |
| US20210002289A1 (en) | 2021-01-07 |
| EP3440082A1 (en) | 2019-02-13 |
| JP2022050469A (ja) | 2022-03-30 |
| CN109311900A (zh) | 2019-02-05 |
| JP2019513746A (ja) | 2019-05-30 |
| US10759808B2 (en) | 2020-09-01 |
| WO2017176958A1 (en) | 2017-10-12 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CA3020281A1 (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 | |
| MXPA05000336A (es) | Antagonistas del receptor 1 de hormona de concentracion de melanina (mchir). | |
| WO2012176763A1 (ja) | 新規インダゾール誘導体 | |
| 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 | |
| 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 | |
| CA2927182A1 (en) | Quinolinyl modulators of ror.gamma.t | |
| AU2022202463A1 (en) | Tetrahydroisoquinoline compound, preparation method therefor, pharmaceutical composition containing same, and use thereof | |
| 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 | |
| KR20200083529A (ko) | 파르네소이드 x 수용체 조정제로서의 알켄 스피로시클릭 화합물 | |
| CA2800521A1 (en) | Fused imidazole derivative | |
| CA2897417A1 (en) | New dihydroquinoline-2-one derivatives as aldosterone synthase (cyp11b2 or cyp11b1) inhibitors | |
| 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 | |
| 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 | |
| CA3181583A1 (en) | Methods of use for pyrimidines as ferroportin inhibitors | |
| JPH0769890A (ja) | キノリンまたはキナゾリン誘導体を含んでなる医薬組成物 |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| EEER | Examination request |
Effective date: 20220309 |
|
| EEER | Examination request |
Effective date: 20220309 |
|
| EEER | Examination request |
Effective date: 20220309 |
|
| EEER | Examination request |
Effective date: 20220309 |