MX2023009031A - Compuestos y metodos para la degradacion dirigida de polipeptidos de fibrosarcoma acelerado rapidamente. - Google Patents
Compuestos y metodos para la degradacion dirigida de polipeptidos de fibrosarcoma acelerado rapidamente.Info
- Publication number
- MX2023009031A MX2023009031A MX2023009031A MX2023009031A MX2023009031A MX 2023009031 A MX2023009031 A MX 2023009031A MX 2023009031 A MX2023009031 A MX 2023009031A MX 2023009031 A MX2023009031 A MX 2023009031A MX 2023009031 A MX2023009031 A MX 2023009031A
- Authority
- MX
- Mexico
- Prior art keywords
- target protein
- raf
- present disclosure
- compounds
- rapidly accelerated
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 4
- 230000015556 catabolic process Effects 0.000 title abstract 3
- 238000006731 degradation reaction Methods 0.000 title abstract 3
- 201000008808 Fibrosarcoma Diseases 0.000 title abstract 2
- 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 abstract 7
- 108090000623 proteins and genes Proteins 0.000 abstract 7
- 102000006275 Ubiquitin-Protein Ligases Human genes 0.000 abstract 2
- 108010083111 Ubiquitin-Protein Ligases Proteins 0.000 abstract 2
- 230000001588 bifunctional effect Effects 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 230000005764 inhibitory process Effects 0.000 abstract 2
- 101000941994 Homo sapiens Protein cereblon Proteins 0.000 abstract 1
- 102100032783 Protein cereblon Human genes 0.000 abstract 1
- 102000018471 Proto-Oncogene Proteins B-raf Human genes 0.000 abstract 1
- 108010091528 Proto-Oncogene Proteins B-raf Proteins 0.000 abstract 1
- 238000009825 accumulation Methods 0.000 abstract 1
- 230000002776 aggregation Effects 0.000 abstract 1
- 238000004220 aggregation Methods 0.000 abstract 1
- 230000006552 constitutive activation Effects 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 239000003446 ligand Substances 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 230000000144 pharmacologic effect Effects 0.000 abstract 1
Classifications
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- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- 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
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- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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Abstract
La presente descripción se refiere a compuestos bifuncionales, que encuentran utilidad como moduladores de Fibrosarcoma Acelerado Rápidamente (RAF, tal como c-RAF, A-RAF y/o B-RAF; la proteína diana). En particular, la presente descripción se dirige a compuestos bifuncionales, que contienen en un extremo un ligando Von Hippel-Lindau, cereblon, Inhibidores de las Proteínas de Apoptosis, u homólogo 2 doble minuto de ratón que se une a la respectiva ligasa de ubiquitina E3 y en el otro extremo una porción que se une a la proteína diana RAF, de manera que la proteína diana se ubica en la proximidad de la ligasa de ubiquitina para efectuar la degradación (e inhibición) de la proteína diana. La presente descripción exhibe una amplia gama de actividades farmacológicas, asociadas con la degradación/inhibició n de la proteína diana. Las enfermedades o trastornos que resultan de la agregación o acumulación de la proteína diana o de la activación constitutiva de la proteína diana, se tratan o se previenen con los compuestos y composiciones de la presente descripción.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201662438803P | 2016-12-23 | 2016-12-23 | |
US201762582698P | 2017-11-07 | 2017-11-07 |
Publications (1)
Publication Number | Publication Date |
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MX2023009031A true MX2023009031A (es) | 2023-08-09 |
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Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
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MX2019007649A MX2019007649A (es) | 2016-12-23 | 2017-12-22 | Compuestos y metodos para la degradacion dirigida de polipeptidos de fibrosarcoma acelerado rapidamente. |
MX2023009031A MX2023009031A (es) | 2016-12-23 | 2019-06-21 | Compuestos y metodos para la degradacion dirigida de polipeptidos de fibrosarcoma acelerado rapidamente. |
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MX2019007649A MX2019007649A (es) | 2016-12-23 | 2017-12-22 | Compuestos y metodos para la degradacion dirigida de polipeptidos de fibrosarcoma acelerado rapidamente. |
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US (1) | US10723717B2 (es) |
EP (1) | EP3558994A4 (es) |
JP (2) | JP2020504741A (es) |
KR (2) | KR102564201B1 (es) |
CN (2) | CN117510491A (es) |
AU (2) | AU2017382436C1 (es) |
BR (1) | BR112019012878A2 (es) |
CA (1) | CA3047784A1 (es) |
CO (1) | CO2019007894A2 (es) |
IL (3) | IL294423B2 (es) |
MX (2) | MX2019007649A (es) |
WO (1) | WO2018119448A1 (es) |
Families Citing this family (101)
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KR102053484B1 (ko) | 2012-12-21 | 2019-12-06 | 국립연구개발법인 양자과학기술연구개발기구 | 뇌 안에 축적된 타우 단백질을 이미징하기 위한 신규한 화합물 |
KR20220029783A (ko) | 2015-01-20 | 2022-03-08 | 아비나스 오퍼레이션스, 인코포레이티드 | 안드로겐 수용체의 표적화된 분해를 위한 화합물 및 방법 |
US20170327469A1 (en) | 2015-01-20 | 2017-11-16 | Arvinas, Inc. | Compounds and methods for the targeted degradation of androgen receptor |
EP3302482A4 (en) | 2015-06-05 | 2018-12-19 | Arvinas, Inc. | Tank-binding kinase-1 protacs and associated methods of use |
WO2017030814A1 (en) | 2015-08-19 | 2017-02-23 | Arvinas, Inc. | Compounds and methods for the targeted degradation of bromodomain-containing proteins |
WO2017197055A1 (en) | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | Heterocyclic degronimers for target protein degradation |
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 |
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IL294423B2 (en) | 2024-01-01 |
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AU2017382436C1 (en) | 2021-05-27 |
BR112019012878A2 (pt) | 2019-11-26 |
US20180179183A1 (en) | 2018-06-28 |
KR20190102019A (ko) | 2019-09-02 |
JP2020504741A (ja) | 2020-02-13 |
IL267410A (en) | 2019-08-29 |
US10723717B2 (en) | 2020-07-28 |
MX2019007649A (es) | 2019-09-10 |
CN110741004A (zh) | 2020-01-31 |
JP2023065395A (ja) | 2023-05-12 |
CO2019007894A2 (es) | 2019-10-09 |
AU2021200099A1 (en) | 2021-03-18 |
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