QUINOLINE DERIVATIVES AND MELK INHIBITORS CONTAINING SAME Russian patent published in 2016 - IPC C07D215/46 C07D215/54 C07D401/04 C07D401/10 C07D401/12 C07D409/04 C07D409/06 C07D409/14 C07D401/14 A61K31/47 A61K31/4709 A61P35/00 

FIELD: chemistry.

SUBSTANCE: invention relates to organic chemistry, namely to a heterocyclic compound of general formula (I) or its pharmaceutically acceptable salt thereof, where: R¹ is C₁-C₆ alkyl sulphonyl or -CO-R⁵, where R⁵ is C₁-C-₆ alkyl or C₃-C₅ cycloalkyl; R² represents phenyl which can contain group substitute selected from group of substitutes C, or -NR^6AR^7A, where R^6A is hydrogen atom and R^7A is -(CH₂)_n-R^10A (where n equals whole number from 0 to 2 and R^10A represents mono- or tricyclic C₃-C₁₀ cycloalkyl, which can contain group substitute selected from group of substitutes D, phenyl, which can contain group substitute selected from a group of substitutes E, aliphatic heterocyclic group which is selected from piperidinil, piperazinil and azabicyclooctanil and can be substituted C₁-C-₆ alkyl, aromatic heterocyclic group which is selected from a pyridinyl, pyrimidinyl and pirazolil and can contain group substitute selected from a group of substitutes I), or R^6A and R^7A is formed with adjacent nitrogen atom aliphatic heterocyclic group that is selected from piperidinil and piperazinil and may contain group substitute selected from a group of substitutes F; R³ is C₆-C₁₀ aryl, which can contain group substitute selected from a group of substitutes G, or aromatic heterocyclic group which is selected from a pyridinyl, pyrimidinyl, tiofenil, isoxazolyl, pyrrolyl and pirazolil and can contain group substitute selected from a group of substitutes H; R⁴ is hydrogen atom or halogen; R is hydrogen atom or halogen; and R¹⁰¹ is hydrogen atom; where said substitutes C - I are one-three substitutes are given in claim. Invention also relates to pharmaceutical composition, an inhibitor of MELK, agent, which simulates the expression MELK, anticancer agent based on compounds of formula (I), method of treating and/or preventing diseases, which includes MELK overexpression, using compound of formula (I).

EFFECT: obtained are novel heterocyclic compounds effective as anti-tumour agent.

19 cl, 4 tbl, 1200 ex