DERIVATIVES OF PYRROLO[3,2-c]PYRIDIN-4-ONE 2-INDOLINONE AS PROTEINKINASE INHIBITORS Russian patent published in 2011 - IPC C07D471/04 A61K31/437 A61P33/00 

FIELD: medicine, pharmaceutics.

SUBSTANCE: claimed invention relates to compounds of pyrrolo[3,2-c]pyridine-4-one 2-indolinone of formula (I). Compound of formula (I): , where: represents single or binary bond; X and Y independently on each other are selected from C or N; X and Y represent N, then R₅ and R₇ are absent; R₁ and R₂ represent H; R₃ is selected from alkyl, trifluormethyl, aryl and aralkyl, where said alkyl, aryl or aralkyl iis substituted by one or more halogens or hydroxyls; R₄ is selected from alkyl, cycloalkyl, heterocycloalkyl, -[CH₂CH(OH)]_rCH₂NR₉R₁₀ and -(CH₂)_nNR₉R₁₀, where said alkyl or heterocycloalkyl is probably substituted by one or more groups, selected from group, consisting of hydroxyl, amino, aminoalkyl, hydroxyalkyl and -NR₉R₁₀; X and Y represent C, then R₅, R₆, R₇, R₈ are independently on each other selected from hydrogen, halo, alkyl, heterocycloalkyl, aryl, heteroaryl, hydroxyl, -OR₉, -NR₉R₁₀, -NSO₂R₉, -NR₉COR₁₀, -NHCO₂R₁₀, where said aryl, heteroaryl, heterocycloalkyl are substituted by one or more groups, consisting of alkyl, alkoxyl and halogen; R₉ and R₁₀ independently on each other are selected from hydrogen, alkyl, cycloalkyl, where said alkyl, aryl, independently on each other are substituted by one or more groups, consisting of alkyl, aryl, hydroxyl, alkoxyl; R₉ and R₁₀ together with atom, to which they are bound, form 4-6-member rings, where 4-6-member rings can, in addition, contain one-two heteroatoms, selected from group, consisting of N and O, and each 4-6-member ring, formed in said way, is probably substituted by one or more groups, consisting of alkyl; n represents 2-6 and their pharmaceutically acceptable salts, where R₁, R₂, R₃, R₄, R₅, R₆, R₇, R₈, X, Y and -have values given in description. Also described is pharmaceutical composition, containing said compounds and possessing activity of proteinkinase inhibitor, methods of obtaining and pharmaceutical applications.

EFFECT: obtained and described are novel compounds, which can be useful as proteinkinase inhibitors.

20 cl, 131 ex, 6 tbl