| 摘要 |
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 C1-6alkyl; X1 is NR8-; R1 is H, C1-10 aliphatic, C3-10 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, C1-10 aliphatic group; R4 is C3-10 cycloaliphatic group; R8 is H, -C(O)OR; each J1 is independently C1-6 halogenalkyl, halogen, Q or -Z-Q; each Z is independently C1-6 aliphatic group where 0-3 -CH2- links in the specified C1-6 aliphatic group are optionally replaced by -NR-, -O-, -C(O)-, where any of the unsubstituted -CH2- links in the specified C1-6 aliphatic group is optionally substituted by 0-2 Jz ; each Q is independently H, C1-6 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 JQ; Jz is halogen; JQ is -M; each M is independently H, C1-6 aliphatic group, halogen; each R is independently H or unsubstituted C1-6 aliphatic group. ^ EFFECT: preparing the pharmaceutical composition and method for inhibiting proteinkinase Plk1 activity. ^ 31 cl, 43 ex, 1 tbl |
