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)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (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 (17)
| 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 |
| EP3679026A1 (en) | 2017-09-04 | 2020-07-15 | C4 Therapeutics, Inc. | Glutarimide |
| WO2019099868A2 (en) | 2017-11-16 | 2019-05-23 | C4 Therapeutics, Inc. | Degraders and degrons for targeted protein degradation |
| EP3846800A4 (en) | 2018-09-04 | 2022-08-24 | C4 Therapeutics, Inc. | COMPOUNDS FOR THE DEGRADATION OF BRD9 OR MTH1 |
| EP3935050A4 (en) | 2019-03-06 | 2023-01-04 | C4 Therapeutics, Inc. | HETEROCYCLIC COMPOUNDS FOR MEDICAL TREATMENT |
| AU2020298293A1 (en) * | 2019-06-21 | 2022-01-20 | Dana-Farber Cancer Institute, Inc. | Allosteric EGFR inhibitors and methods of use thereof |
| 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 |
| CA3154073A1 (en) * | 2019-12-20 | 2021-06-24 | Christopher G. Nasveschuk | Isoindolinone and indazole compounds for the degradation of egfr |
| 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 |
| JP2023516073A (ja) | 2020-03-05 | 2023-04-17 | シーフォー セラピューティクス， インコーポレイテッド | Ｂｒｄ９の標的分解のための化合物 |
| CA3223447A1 (en) | 2021-06-25 | 2022-12-29 | 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 |
| 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 |
| 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 |
| 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 |
| 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 |
|---|---|---|---|---|
| US9476888B2 (en) | 2011-08-08 | 2016-10-25 | 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 |
| JP6430390B2 (ja) | 2012-11-20 | 2018-11-28 | ジェネンテック， インコーポレイテッド | Ｔ７９０ｍを含むｅｇｆｒ変異体の阻害剤としてのアミノピリミジン化合物 |
| EP3052494B1 (en) | 2013-06-28 | 2018-12-26 | H. Hoffnabb-La Roche Ag | Azaindazole compounds as inhibitors of t790m containing egfr mutants |
| KR102320082B1 (ko) | 2014-04-14 | 2021-10-29 | 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 |
| EP3256470B1 (en) | 2014-12-23 | 2023-07-26 | Dana-Farber Cancer Institute, Inc. | Methods to induce targeted protein degradation through bifunctional molecules |
| US9694084B2 (en) * | 2014-12-23 | 2017-07-04 | Dana-Farber Cancer Institute, Inc. | Methods to induce targeted protein degradation through bifunctional molecules |
| CA2987914C (en) * | 2015-06-30 | 2022-09-13 | 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 |
| EP3331905B1 (en) | 2015-08-06 | 2022-10-05 | Dana-Farber Cancer Institute, Inc. | Targeted protein degradation to attenuate adoptive t-cell therapy associated adverse inflammatory responses |
| WO2017117473A1 (en) | 2015-12-30 | 2017-07-06 | Dana-Farber Cancer Institute, Inc. | Bifunctional molescules for her3 degradation and methods of use |
| CA3021358A1 (en) | 2016-04-22 | 2017-10-26 | Dana-Farber Cancer Institute, Inc. | Bifunctional molecules for degradation of egfr and methods of use |
| WO2017197036A1 (en) * | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | Spirocyclic degronimers for target protein degradation |
| EP3455218A4 (en) * | 2016-05-10 | 2019-12-18 | C4 Therapeutics, Inc. | C3 CARBON-BASED GLUTARIMIDE DEGRONIMERS FOR TARGET PROTEIN REDUCTION |
| EP3454856A4 (en) * | 2016-05-10 | 2019-12-25 | C4 Therapeutics, Inc. | HETEROCYCLIC DEGRONIMERS FOR TARGET PROTEIN REDUCTION |
| WO2017197056A1 (en) * | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | Bromodomain targeting degronimers for target protein degradation |
| WO2017197051A1 (en) * | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | Amine-linked c3-glutarimide degronimers for target protein degradation |
-
2019
- 2019-02-01 TW TW108104122A patent/TW201945357A/zh unknown
- 2019-02-04 WO PCT/EP2019/052585 patent/WO2019149922A1/en unknown
- 2019-02-04 CN CN201980009141.0A patent/CN111615512A/zh active Pending
- 2019-02-04 JP JP2020541782A patent/JP2021525219A/ja active Pending
- 2019-02-04 EP EP19702906.9A patent/EP3749664A1/en not_active Withdrawn
- 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 |
|---|---|
| JP2021525219A (ja) | 2021-09-24 |
| CN111615512A (zh) | 2020-09-01 |
| WO2019149922A1 (en) | 2019-08-08 |
| US20200361930A1 (en) | 2020-11-19 |
| TW201945357A (zh) | 2019-12-01 |
| EP3749664A1 (en) | 2020-12-16 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AR114244A1 (es) | Compuestos que degradan efgr útiles en el tratamiento del cáncer | |
| CL2021000038A1 (es) | Derivados de 3-(5-hidroxi-1-oxoisoindolin-2-il)piperidina-2,6-diona y su uso en el tratamiento de trastornos dependientes de la proteína con dedos de zinc 2 de la familia ikaros (ikzf2) | |
| AR103064A1 (es) | Compuestos moduladores de fxr (nr1h4) | |
| AR106237A2 (es) | Inhibidores heterocíclicos de la aspartil proteasa, sus sales farmacéuticamente aceptables | |
| AR119057A1 (es) | Compuestos de 1-oxo-isoindolin-5-carboxamida sustituida, composiciones de estos y métodos de tratamiento con dichos compuestos | |
| AR114803A1 (es) | Compuestos de 4-aminoisoindolin-1,3-diona sustituida, composiciones de estos y métodos de tratamiento con dichos compuestos | |
| AR110405A1 (es) | Compuestos | |
| AR104884A1 (es) | Compuestos de 4-hidroxi-3-(heteroaril)piridin-2-ona como agonistas de apj | |
| UY38296A (es) | Derivados de 3–(5–amino–1–oxoisoindolin–2–il)piperidin–2,6–diona y sus usos | |
| SA515361086B1 (ar) | Fasn مركبات وتركيبات جديدة لتثبيط | |
| AR094784A1 (es) | Compuestos de tubulisina, métodos para obtenerlos y uso | |
| AR100645A1 (es) | Derivados de pirazolo-pirimidina | |
| AR094812A1 (es) | Derivado de piridina monocíclico como inhibidor del fgfr | |
| AR097082A1 (es) | Compuestos terapéuticamente activos y sus métodos de uso | |
| AR080859A1 (es) | Derivados 1,2,4 triazolo-piridinicos inhibidores no nucleosidicos de la transcriptasa inversa, utiles para tratar infecciones por vih y composiciones farmaceuticas que los contienen. | |
| AR112831A1 (es) | Terapia de combinación usando un antagonista del receptor 2 de quimiocina (ccr2) y un inhibidor de pd-1 / pd-l1 | |
| AR119672A1 (es) | Inhibidor de 15-pgdh | |
| AR109296A1 (es) | Derivados de oxadiazolopiridina para el uso como inhibidores de ghrelin o-aciltransferasa (goat) | |
| AR109706A1 (es) | INHIBIDORES DUALES DE FOSFATIDILINOSITOL 3 QUINASA d / g | |
| RU2019131147A (ru) | Новые хиназолиноновые производные, ингибирующие pi3k, и содержащая их фармацевтическая композиция | |
| AR125026A1 (es) | Inhibidores del sarcómero cardíaco | |
| AR101798A1 (es) | Quinolinas herbicidas | |
| CO2019005165A2 (es) | Compuesto de piridona como inhibidor de c-met | |
| AR096160A1 (es) | Inhibidores de nicotamida fosforibosiltransferasa, composiciones, productos y usos de los mismos | |
| AR112463A1 (es) | Derivados de propanamina para tratar el dolor y estados relacionados con dolor |