NEW BRAF INHIBITORS AS "PARADOX BREAKERS" Russian patent published in 2024 - IPC C07D239/88 C07D239/90 C07D403/12 A61K31/517 A61P35/00 

FIELD: chemistry.

SUBSTANCE: invention relates to a compound selected from 6-[2-cyano-3-[[ethyl(methyl)sulfamoyl]amino]-6-fluorophenoxy]-3-methyl-4-oxoquinazoline; 6-[6-chloro-2-cyano-3-[[ethyl(methyl)sulfamoyl]amino]phenoxy]-3-methyl-4-oxoquinazoline; (3R)-N-[4-chloro-2-cyano-3-(3-methyl-4-oxoquinazolin-6-yl)oxyphenyl]-3-fluoropyrrolidine-1-sulphonamide; N-[4-chloro-2-cyano-3-(3-methyl-4-oxoquinazolin-6-yl)oxyphenyl]pyrrolidine-1-sulphonamide; 6-[2-cyano-3-[[ethyl(methyl)sulfamoyl]amino]phenoxy]-3-methyl-4-oxoquinazoline; N-[2-cyano-3-(3-methyl-4-oxoquinazolin-6-yl)oxyphenyl]pyrrolidine-1-sulphonamide; (3R)-N-[2-cyano-3-(3-methyl-4-oxoquinazolin-6-yl)oxyphenyl]-3-fluoropyrrolidine-1-sulphonamide; N-[2-cyano-3-(3-methyl-4-oxoquinazolin-6-yl)oxyphenyl]cyclopentane sulphonamide; N-[2-cyano-3-(3-methyl-4-oxoquinazolin-6-yl)oxyphenyl]cyclohexane sulphonamide; N-[2-cyano-3-(3-methyl-4-oxoquinazolin-6-yl)oxyphenyl]butane-2-sulphonamide; 6-[2-cyano-3-[[ethyl(methyl)sulfamoyl]amino]anilino]-3-methyl-4-oxoquinazoline; (3R)-N-[2-cyano-3-[(3-methyl-4-oxoquinazolin-6-yl)amino]phenyl]-3-fluoropyrrolidine-1-sulphonamide; 6-[6-chloro-2-cyano-3-[[ethyl(methyl)sulfamoyl]amino]anilino]-3-methyl-4-oxoquinazoline; N-[4-chloro-2-cyano-3-[(3-methyl-4-oxoquinazolin-6-yl)amino]phenyl]pyrrolidine-1-sulphonamide; N-[2-cyano-4-fluoro-3-(3-methyl-4-oxoquinazolin-6-yl)oxyphenyl]pyrrolidine-1-sulphonamide; N-[2-cyano-4-fluoro-3-(3-methyl-4-oxoquinazolin-6-yl)oxyphenyl]cyclopentane sulphonamide and 6-[2-cyano-3-(dimethylsulfamoylamino)-6-fluorophenoxy]-3-methyl-4-oxoquinazoline; or a pharmaceutically acceptable salt thereof, which are BRAF inhibitors. Invention also relates to a pharmaceutical composition containing said compound, use thereof for the treatment or prevention of BRAF mutation cancer selected from thyroid cancer, colorectal cancer, brain cancer, melanoma and non-small cell lung cancer (NSCLC), and for preparing a medicament for treating or preventing said types of cancer, as well as a method of treating them.

EFFECT: disclosed are new braf inhibitors as "paradox breakers".

8 cl, 9 tbl, 17 ex