PE20221724A1 - Compuestos de isoindolinona e indazol para la degradacion del receptor del factor de crecimiento epidermico (egfr) - Google Patents

Compuestos de isoindolinona e indazol para la degradacion del receptor del factor de crecimiento epidermico (egfr)

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Publication number
PE20221724A1
PE20221724A1 PE2022001139A PE2022001139A PE20221724A1 PE 20221724 A1 PE20221724 A1 PE 20221724A1 PE 2022001139 A PE2022001139 A PE 2022001139A PE 2022001139 A PE2022001139 A PE 2022001139A PE 20221724 A1 PE20221724 A1 PE 20221724A1
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PE
Peru
Prior art keywords
egfr
compounds
growth factor
factor receptor
epidermal growth
Prior art date
Application number
PE2022001139A
Other languages
English (en)
Inventor
Christopher G Nasveschuk
Martin Duplessis
Jae Young Ahn
Alexander W Hird
Ryan E Michael
Kiel Lazarski
Yanke Liang
Georg Jaeschke
Antonio Ricci
Annick Goergler
Daniel Rueher
Original Assignee
C4 Therapeutics Inc
Priority date (The priority date 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 date listed.)
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Publication date
Application filed by C4 Therapeutics Inc filed Critical C4 Therapeutics Inc
Publication of PE20221724A1 publication Critical patent/PE20221724A1/es

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    • 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
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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
    • A61K31/425—Thiazoles
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
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    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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  • Health & Medical Sciences (AREA)
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  • Animal Behavior & Ethology (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biochemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Peptides Or Proteins (AREA)

Abstract

Referida a compuestos de formula (I) que degradan el Receptor del Factor de Crecimiento Epidermico (EGFR), en donde A se selecciona de los sistemas de anillo AF, AG y AH; y B se selecciona del sistema del anillo AD y AE. Estos compuestos son seleccionados del grupo que consiste en 5-((2-(1-(6,7-dihidro-5H-pirrolo[1,2-c]imidazol-1-il)-2-oxo-2-(tiazol-2-ilamino)etil)-7-fluoro-3-oxoisoindolin-5-il)etinil)-N-(1-(2-(4-(4-((2,6-dioxopiperidin-3-il)amino)fenil)piperidin-1-il)acetil)piperidin-4-il)picolinamida, entre otros. Asimismo, la accion de dichos compuestos consiste en la ubiquitinacion de la proteina EGFR con una o mas mutaciones, tales como L858R, T790M o C797S, para finalizar con su degradacion proteasomica; ademas, los compuestos reclamados son utiles para el tratamiento o profilaxis del cancer de pulmon no pequeno con mutacion de EGFR en pacientes humanos.
PE2022001139A 2019-12-20 2020-12-18 Compuestos de isoindolinona e indazol para la degradacion del receptor del factor de crecimiento epidermico (egfr) PE20221724A1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962951464P 2019-12-20 2019-12-20
US201962951467P 2019-12-20 2019-12-20
PCT/US2020/066211 WO2021127561A1 (en) 2019-12-20 2020-12-18 Isoindolinone and indazole compounds for the degradation of egfr

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PE20221724A1 true PE20221724A1 (es) 2022-11-04

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US (2) US11673902B2 (es)
EP (1) EP4076450A4 (es)
JP (1) JP2023509375A (es)
KR (1) KR20220119415A (es)
CN (1) CN114901277B (es)
AU (1) AU2020405237A1 (es)
BR (1) BR112022011827A2 (es)
CA (1) CA3154073A1 (es)
CL (1) CL2022001641A1 (es)
CO (1) CO2022008604A2 (es)
IL (1) IL293999A (es)
MX (1) MX2022007659A (es)
PE (1) PE20221724A1 (es)
TW (1) TW202136265A (es)
WO (1) WO2021127561A1 (es)

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