4,5-DIHYDRO-[1,2,4]TRIAZOLO[4,3-F]PTERIDINES AS PROTEIN KINASE Plk1 INHIBITORS FOR TREATING PROLIFERATIVE DISEASES Russian patent published in 2012 - IPC C07D491/12 A61K31/519 A61P35/00 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to compounds of formula (I) exhibiting the properties of proteinkinase Plk1 inhibitors. In formula (I): the ring A is a 5-member heteroaryl ring which contains atoms N as heteroatoms where the ring is optionally substituted by C_1-6alkyl; X¹ is NR⁸-; R¹ is H, C_1-10 aliphatic, C_3-10 cycloaliphatic, phenyl, 5-6- member heteroaryl group containing atom S, N as a heteroatom where said R¹ is optionally substituted by 0-5 J¹; each R² and R³, is independently H, C_1-10 aliphatic group; R⁴ is C_3-10 cycloaliphatic group; R⁸ is H, -C(O)OR; each J¹ is independently C_1-6 halogenalkyl, halogen, Q or -Z-Q; each Z is independently C_1-6 aliphatic group where 0-3 -CH₂- links in the specified C_1-6 aliphatic group are optionally replaced by -NR-, -O-, -C(O)-, where any of the unsubstituted -CH₂- links in the specified C_1-6 aliphatic group is optionally substituted by 0-2 J^z ; each Q is independently H, C_1-6 aliphatic group, 3-8- member aromatic or non-aromatic monocyclic ring having 0-3 heteroatoms independently selected from O and N where each Q is independently and optionally substituted by 0-2 J^Q; J^z is halogen; J^Q is -M; each M is independently H, C_1-6 aliphatic group, halogen; each R is independently H or unsubstituted C_1-6 aliphatic group.

EFFECT: preparing the pharmaceutical composition and method for inhibiting proteinkinase Plk1 activity.

31 cl, 43 ex, 1 tbl