HETEROCYCLIC MEK INHIBITORS AND METHODS OF APPLICATION Russian patent published in 2009 - IPC C07D231/02 C07D237/26 C07D401/00 C07D413/00 C07D417/00 A61K31/44 A61K31/50 A61K31/655 A61P35/00 A61P29/00 

FIELD: chemistry.

SUBSTANCE: invention refers to new componds including its separated enantiomers, diastereoisomers, solvates and to pharmaceutically acceptable salts of formula: , where X represents N or CR¹⁰; Y represents NR³; R¹, R², R⁸, R⁹ and R¹⁰ independently represent hydrogen, hdroxy, halogen, -SR¹¹, -OR³, -NR³R⁴, C₁-C₁₀alkyl, C₃-C₁₀cycloalkyl, C₃-C₁₀cycloalkylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, heterocyclyl or heterocyclylalkyl; R⁷ represents hydrogen, C₁-C₁₀alkyl, C₃-C₁₀cycloalkyl, C₃-C₁₀cycloalkylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, heterocyclyl or heterocyclylalkyl, where any of specified alkyl, cycloalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, heterocyclyl and heterocyclylalkyl fragments are optionally substituted with one or more groups independently chosen from oxo (provided it is not substituted for aryl or heteroaryl), halogen, cyano, nitro, SO₂NR¹¹R¹², -C(O)R¹¹, C(O)OR¹¹, -C(O)NR¹¹R¹² , -SR¹¹, -S(O)R¹⁴, -SO₂R¹⁴, -NR¹¹R¹², -OR¹¹, C₁-C₁₀alkyl and C₃-C₁₀cycloalkyl; R³ represents hydrogen, C₁-C₁₀alkyl, C₃-C₁₀cycloalkyl, C₃-C₁₀cycloalkylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, heterocyclyl or heterocyclylalkyl, where any of specified alkyl, cycloalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, heterocyclyl and heterocyclylalkyl fragments are optionally substituted with one or more groups independently chosen from oxo (provided it is not substituted for aryl or heteroaryl), halogen, cyano, nitro, -SO₂NR¹¹R¹², -C(O)R¹¹, C(O)OR¹¹, -C(O)NR¹¹R¹², -SR¹¹, -S(O)R¹⁴, -SO₂R¹⁴, -NR¹¹R¹² and -OR¹¹; R⁴ represents hydrogen or C₁-C₆alkyl; R¹¹ and R¹² independently represent hydrogen and lower alkyl, and R¹⁴ represents lower alkyl; W represents heteroaryl, heterocyclyl, -C(O)OR³, -C(O)NR³R⁴, -C(O)NR⁴OR³, -C(O)NR⁴SO₂R³, -C(O)(C₃-C₁₀cycloalkyl), -C(O)(C₁-C₁₀alkyl), -C(O)(aryl), -C(O)(heteroaryl) or C(O)(heterocyclyl), where any of specified heteroaryl, heterocyclyl, C(O)OR³, -C(O)NR³R⁴, -C(O)NR⁴OR³, -C(O)NR⁴SO₂R³, -C(O)(C₃-C₁₀cycloalkyl), -C(O)(C₁-C₁₀alkyl), -C(O)(aryl), -C(O)(heteroaryl) and -C(O)(heterocyclyl) are optionally substituted with one or more groups independently chosen from halogen, -NR³R⁴, -OR³ and C₁-C₁₀alkyl; where heteroaryl represents univalent aromatic radical of 5-, 6- or 7-merous rings containing at least, one to four heteroatoms chosen of nitrogen, oxygen or sulphur, and heterocyclyl represents saturated or partially unsaturated carbocyclic radical of 5-6 ring atoms where at least one ring atom represents heteroatom chosen from nitrogen, oxygen and sulphur, while other ring atoms represent C. Besides, the invention refers to compositions, to method of MEK activity inhibition, to application of compound under any of cl. 1-21 and 23-41, as well as to methods of producing intermediate compounds.

EFFECT: production of new biologically active compounds of activity as a MEK inhibitor.

55 cl, 34 dwg, 165 ex