FIELD: organic chemistry.
SUBSTANCE: group of inventions relates to a compound of formula (IIa), its pharmaceutically acceptable salt, pharmaceutical composition, the use and a method of preventing MEK reactivation by bypassing CRAF based on it. Where in formula (IIa) R2 represents L; R3 represents fluorine; R6 represents H, halogen or C1-C6 alkyl; R8 represents C1-C6 alkyl; L represents -Z1-Z2; Z1 represents -CH2; Z 2 is selected from C 3 -C 8 heterocyclyl having 1–2 heteroatoms selected from O and N, optionally substituted by one or more substituents individually and independently selected from C 1 -C 4 alkyl, cyano, halogen, amino, amino( C1-C4 alkyl), amido, oxo; or -NR 5 R 5´ ; each R 5 and R 5' independently represents C1-C6 alkyl; X represents O; Y represents O; Z represents either C or N.
EFFECT: compounds of formula (IIa) having MEK inhibitor properties that maximize reversal of the pathological MAPK/ERK pathway and are effective agents against cancer.
30 cl, 22 dwg, 16 tbl, 126 ex
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