AR114244A1 - Compuestos que degradan efgr útiles en el tratamiento del cáncer - Google Patents
Compuestos que degradan efgr útiles en el tratamiento del cáncerInfo
- Publication number
- AR114244A1 AR114244A1 ARP190100272A ARP190100272A AR114244A1 AR 114244 A1 AR114244 A1 AR 114244A1 AR P190100272 A ARP190100272 A AR P190100272A AR P190100272 A ARP190100272 A AR P190100272A AR 114244 A1 AR114244 A1 AR 114244A1
- Authority
- AR
- Argentina
- Prior art keywords
- heterocyclyl
- piperidyl
- pyridinyl
- heteroaryl
- aryl
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- 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
- C07D401/14—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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
Reivindicación 1: Compuesto de fórmula (1), o una sal farmacéuticamente aceptable del mismo, en la que: L se selecciona del grupo que consiste en: i) -aril-(CH₂)₁₋₂-heterociclil-C(=O)-(CH₂)₁₋₁₀-NH-, en particular a) -fenil-(CH₂)₁₋₂-piperazinil-C(=O)-(CH₂)₁₋₁₀-NH-; ii) -heteroaril-C(=O)-NH-heterociclil-C(=O)-(CH₂)₁₋₁₀-NH-, en particular a) -piridinil-C(=O)-NH-piperidil-C(=O)-(CH₂)₁₋₁₀-NH-; iii) -heteroaril-(CH₂)₁₋₂-heterociclil-C(=O)-(CH₂)₁₋₁₀-NH-, en particular a) -piridinil-(CH₂)₁₋₂-piperazinil-C(=O)-(CH₂)₁₋₁₀-NH-; iv) -heteroaril-C(=O)-NH-heterociclil-(CH₂)₁₋₁₀-NH-, en particular a) -piridinil-C(=O)-NH-piperidil-(CH₂)₁₋₁₀-NH-; v) -heteroaril-C(=O)-NH-heterociclil-(CH₂)₁₋₁₀-heterociclilo, en particular a) -piridinil-C(=O)-NH-piperidil-(CH₂)₁₋₁₀-piperidilo; y vi) -heteroaril-(CH₂)₁₋₂-heterociclil-C(=O)-(CH₂)₁₋₁₀-heterociclil-, en particular a) -piridinil-(CH₂)₁₋₂-piperidil-C(=O)-(CH₂)₁₋₁₀-piperidilo, o b) -piridinil-(CH₂)₁₋₂-piperazinil-C(=O)-(CH₂)₁₋₁₀-piperidilo, de manera que cada fracción arilo o heteroarilo puede sustituirse independientemente por un a) halógeno, en particular F, o b) alquilo C₁₋₆, en particular metilo; R¹ es H; A es heteroarilo, en particular a) tiazolilo, o b) piridinilo; B es arilo, en particular fenilo, en el que el arilo a) está no sustituido, o b) sustituido con 1 - 2 sustituyentes seleccionados independientemente i) de halógeno, en particular F, ii) alquilo C₁₋₆, en particular metilo; e iii) hidroxi.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP18155128 | 2018-02-05 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR114244A1 true AR114244A1 (es) | 2020-08-12 |
Family
ID=61163580
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP190100272A AR114244A1 (es) | 2018-02-05 | 2019-02-05 | Compuestos que degradan efgr útiles en el tratamiento del cáncer |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US20200361930A1 (es) |
| EP (1) | EP3749664A1 (es) |
| JP (1) | JP2021525219A (es) |
| CN (1) | CN111615512A (es) |
| AR (1) | AR114244A1 (es) |
| TW (1) | TW201945357A (es) |
| WO (1) | WO2019149922A1 (es) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2018237026A1 (en) | 2017-06-20 | 2018-12-27 | C4 Therapeutics, Inc. | N / O-LINKED DEGRONS AND DEGRONIMERS FOR DEGRADATION OF PROTEINS |
| CN118108706A (zh) | 2017-09-04 | 2024-05-31 | C4医药公司 | 戊二酰亚胺 |
| WO2019099868A2 (en) | 2017-11-16 | 2019-05-23 | C4 Therapeutics, Inc. | Degraders and degrons for targeted protein degradation |
| WO2020051235A1 (en) | 2018-09-04 | 2020-03-12 | C4 Therapeutics, Inc. | Compounds for the degradation of brd9 or mth1 |
| CN113557235A (zh) | 2019-03-06 | 2021-10-26 | C4医药公司 | 用于药物治疗的杂环化合物 |
| AU2020298293A1 (en) * | 2019-06-21 | 2022-01-20 | Dana-Farber Cancer Institute, Inc. | Allosteric EGFR inhibitors and methods of use thereof |
| BR112022011827A2 (pt) | 2019-12-20 | 2022-08-30 | C4 Therapeutics Inc | Composto, composição farmacêutica, uso de um composto, métodos para tratamento ou profilaxia de câncer e para tratar um paciente com um distúrbio mediado por receptor do fator de crescimento epidérmico, e, invenção |
| AR120799A1 (es) * | 2019-12-20 | 2022-03-16 | Hoffmann La Roche | 2-[4-cloro-6-[2-[4-[[4-(hidroximetil)-1-piperidil]metil]fenil]etinil]-1-oxoisoindolin-2-il]-2-(6,7-dihidro-5h-pirrolo[1,2-c]imidazol-1-il)-n-tiazol-2-il-acetamida como inhibidor de egfr |
| AR120800A1 (es) * | 2019-12-20 | 2022-03-16 | Hoffmann La Roche | Derivados de 6,7-dihidro-5h-pirrolo[1,2-c]imidazol como inhibidores de egfr |
| IL295709A (en) | 2020-03-05 | 2022-10-01 | C4 Therapeutics Inc | Compounds for targeted knockdown of brd9 |
| EP4361153A1 (en) | 2021-06-25 | 2024-05-01 | Korea Research Institute of Chemical Technology | Novel bifunctional heterocyclic compound having btk degradation function via ubiquitin proteasome pathway, and use thereof |
| WO2023283130A1 (en) | 2021-07-04 | 2023-01-12 | Newave Pharmaceutical Inc. | Isoquinoline derivatives as mutant egfr modulators and uses thereof |
| WO2023088385A1 (zh) | 2021-11-17 | 2023-05-25 | 浙江同源康医药股份有限公司 | 用于egfr蛋白降解的化合物及其用途 |
| WO2023208165A1 (zh) * | 2022-04-29 | 2023-11-02 | 四川海思科制药有限公司 | 一种含氮杂环衍生物及其组合物和药学上的应用 |
| CN115160311B (zh) * | 2022-05-26 | 2024-03-15 | 北京康辰药业股份有限公司 | 一种用于egfr降解的双功能化合物及其应用 |
| CN115109055B (zh) * | 2022-05-26 | 2023-11-28 | 北京康辰药业股份有限公司 | 一种用于egfr降解的双功能化合物及其应用 |
| WO2024064358A1 (en) | 2022-09-23 | 2024-03-28 | Ifm Due, Inc. | Compounds and compositions for treating conditions associated with sting activity |
| WO2024073507A1 (en) | 2022-09-28 | 2024-04-04 | Theseus Pharmaceuticals, Inc. | Macrocyclic compounds and uses thereof |
Family Cites Families (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2013020557A1 (en) | 2011-08-08 | 2013-02-14 | Syddansk Universitet | Method and antibodies for the identification of ubiquitinated proteins and sites of ubiquitination |
| WO2013063560A2 (en) | 2011-10-27 | 2013-05-02 | New York University | INHIBITION OF c-MYC UBIQUITINATION TO PREVENT CANCER INITIATION AND PROGRESSION |
| EP3608317A1 (en) | 2012-01-12 | 2020-02-12 | Yale University | Compounds & methods for the enhanced degradation of targeted proteins & other polypeptides by an e3 ubiquitin ligase |
| KR20150087850A (ko) | 2012-11-20 | 2015-07-30 | 제넨테크, 인크. | Egfr 돌연변이체를 함유하는 t790m의 억제제로서의 아미노피리미딘 화합물 |
| EP3052494B1 (en) | 2013-06-28 | 2018-12-26 | H. Hoffnabb-La Roche Ag | Azaindazole compounds as inhibitors of t790m containing egfr mutants |
| KR20240038809A (ko) | 2014-04-14 | 2024-03-25 | 아비나스 오퍼레이션스, 인코포레이티드 | 단백질분해의 이미드-기초된 조절인자 및 연관된 이용 방법 |
| CN105327350A (zh) | 2014-07-23 | 2016-02-17 | 中国科学院上海巴斯德研究所 | 泛素化途径相关因子在调控辅助性t细胞功能中的应用 |
| US9694084B2 (en) * | 2014-12-23 | 2017-07-04 | Dana-Farber Cancer Institute, Inc. | Methods to induce targeted protein degradation through bifunctional molecules |
| CN107257800B (zh) | 2014-12-23 | 2020-06-30 | 达纳-法伯癌症研究所股份有限公司 | 通过双功能分子诱导靶蛋白降解的方法 |
| WO2017004383A1 (en) * | 2015-06-30 | 2017-01-05 | Dana-Farber Cancer Institute, Inc. | Inhibitors of egfr and methods of use thereof |
| WO2017007612A1 (en) | 2015-07-07 | 2017-01-12 | Dana-Farber Cancer Institute, Inc. | Methods to induce targeted protein degradation through bifunctional molecules |
| CA2995036A1 (en) | 2015-08-06 | 2017-02-09 | Dana-Farber Cancer Institute, Inc. | Tunable endogenous protein degradation |
| US20200216454A1 (en) | 2015-12-30 | 2020-07-09 | Dana-Farber Cancer Institute, Inc. | Bifunctional molecules for her3 degradation and methods of use |
| EP3892272B1 (en) | 2016-04-22 | 2024-07-24 | Dana-Farber Cancer Institute, Inc. | Bifunctional molecules for degradation of egfr and methods of use |
| 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 |
| WO2017197056A1 (en) * | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | Bromodomain targeting degronimers for target protein degradation |
| WO2017197036A1 (en) * | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | Spirocyclic degronimers for target protein degradation |
| CN109562107A (zh) * | 2016-05-10 | 2019-04-02 | C4医药公司 | 用于靶蛋白降解的杂环降解决定子体 |
| 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 |
-
2019
- 2019-02-01 TW TW108104122A patent/TW201945357A/zh unknown
- 2019-02-04 EP EP19702906.9A patent/EP3749664A1/en not_active Withdrawn
- 2019-02-04 WO PCT/EP2019/052585 patent/WO2019149922A1/en unknown
- 2019-02-04 JP JP2020541782A patent/JP2021525219A/ja active Pending
- 2019-02-04 CN CN201980009141.0A patent/CN111615512A/zh active Pending
- 2019-02-05 AR ARP190100272A patent/AR114244A1/es unknown
-
2020
- 2020-08-04 US US16/984,987 patent/US20200361930A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| CN111615512A (zh) | 2020-09-01 |
| US20200361930A1 (en) | 2020-11-19 |
| EP3749664A1 (en) | 2020-12-16 |
| WO2019149922A1 (en) | 2019-08-08 |
| TW201945357A (zh) | 2019-12-01 |
| JP2021525219A (ja) | 2021-09-24 |
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