INHIBITORS OF AKT ACTIVITY Russian patent published in 2016 - IPC C07D471/04 C07D498/04 C07D498/14 A61K31/4741 A61K31/4375 A61K31/519 A61K31/5383 A61K31/551 A61P35/00 

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula

,

where each R¹ and R² is independently selected from hydrogen, C₁-C₁₀alkyl, optionally substituted OH and OR³, where R³ represents C₁-C₁₀alkyl, or R¹ and R² together represent oxo or optionally C₁-C₁₀alkyl O-substituted oxime; W represents O, NR′ or CR^aR^b, where R′ represents either hydrogen, or C₁-C₁₀alkyl; X is either absent or represents CR⁴R⁵, where each R^a, R^b, R⁴ and R⁵ are independently selected from substituents, given for R¹ and R²; Y and Z independently represent substituted or non-substituted nitrogen or carbon (substituents for which are given in i. 1 of the invention formula), or Y and Z together form optionally substituted pyrazolyl, imidazolyl, pyriminidyl, 1,2,4-triazolyl (substituents for which are given in i. 1 of the invention formula); R^7a and R^7b represent H; R^6a and R^6b represent H or R^6a and R^6b can be combined with formation of C₃-C₆cycloalkyl, optionally substituted with one or two substituents, selected from C₁-C₆alkyl and OH; Cy is selected from C_1-6alkyl(C₃-C₈)cycloalkyl, phenyl, pyridinyl and thienyl; m equals 0 or 1; R⁸ represents F. the invention also relates to particular compounds, given in i. 1 of the invention formula, to pharmaceutical composition and method for treating malignant tumour.

EFFECT: novel methods for Akt inhibition.

19 cl, 1 dwg, 153 ex