1,3-DIARYL-SUBSTITUTED UREAS AS KINASE ACTIVITY MODULATORS Russian patent published in 2010 - IPC C07D401/06 C07D401/14 A61K31/404 A61K31/44 A61P35/00 A61P15/08 

FIELD: chemistry.

SUBSTANCE: invention relates to novel compounds which have inhibiting properties on activity of at least one kinase selected from veGFR2, EphB₄, PDGFRβ and c-Kit, having general formula I , where R denotes 0-1 substitutes independently selected from halogen, (C₁-C₆)-alkyl, (C₁-C₆) -alkoxy; R₇ and R₈ together with carbon atoms with which they are bonded form a condensed 5-member heteroaryl ring substituted with a -(Z₁)_mR₁ group, where the heteroaryl ring contains at least one nitrogen atom and optionally an extra nitrogen atom; R₁ is pyridinyl which can be substituted, where the substitutes are independently selected from hydroxy, cyano, halogen, (C₁-C₆)-alkyl, (C₁-C₆) - alkoxy, morpholinyl, imidazolyl, tetrazolyl, aminocarbonyl and -NHR10, where R10 is selected from hydrogen; (C₁-C₆)-alkyl; allyl, phenyl or pyrimidinyl, which may be substituted with CN; thiazolyl, pyridinyl, sulphonyl which is substituted with (C₁-C₆)-alkyl, an acyl which may be substituted with (C₁-C₆)-alkoxy, imidazolyl, cyclopropyl, (C₁-C₆)-alkyl, possibly substituted with NH₂, NH(C₁-C₄-alkyl), N((C₁-C₄)-alkyl (C₁-C₄-alkyl)), hydroxy, (C₁-C₄)alkoxy, morpholinyl, pyrrolidinyl; Z₁ is - CR₅R₆-, where each of R₅ and R6 is selected from hydrogen; and m equals 1; R₂ is benzo[1,3]dioxo-5-lyl or phenyl, which may be substituted with (C₁-C₆)-alkyl, halogen(C₁-C₆)-alkyl, halogen, phenyl, (C₁-C₆)-alkylsulphonyl or (C₁-C₆)-alkoxy, whose alkyl part may be substituted with hydroxyl, halogen, dioxanyl; and each of R₃ and R₄ is selected from hydrogen; provided that the formula 1 compound is not 5-(phenylcarbamoylamino)-3-(2-(4-pyridyl)ethyl)indole, 1-(4-chloro-3-(trifluoromethyl)phenyl)-3-(1-(pyridin-4-yl)-1H-indol-5-yl)urea and 1(2-methoxy-5-(trifluoromethyl)phenyl)-3-(1-pyridin-4-yl)-1H-indol-5-yl)urea, as well as their pharmaceutically acceptable salts. The invention also relates to a pharmaceutical composition, an inhibiting method and a method of preparing a pharmaceutical composition.

EFFECT: more effective use of the compounds.

29 cl, 1 dwg, 6 ex