DIFLUOROMETHYLAMINOPYRIDINES AND DIFLUOROMETHYLAMINOPYRIMIDINES Russian patent published in 2020 - IPC C07D401/04 C07D401/14 C07D403/04 C07D405/14 C07D413/14 C07D491/48 C07D491/56 C07D491/20 C07D498/08 C07D519/00 A61K31/53 A61K31/506 A61P35/00 

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula (I),

,

where X¹, X² and X³ are independently of each other N or CH, provided that at least two of X¹, X² and X³ are N; Y is N or CH; R¹ and R² independently of each other are (i) morpholinyl of formula (II)

(II), where the arrow denotes a bond in formula (I); and where R³ and R⁴ independently of each other are H, C₁-C₃alkyl, optionally substituted with one or two OH, C₁-C₂fluoroalkyl groups, C₁-C₂alkoxy, C₁-C₂alkoxy-C₁-C₃alkyl, CN or C(O)OC₁-C₂alkyl; or R³ and R⁴ together form divalent residue -R⁵R⁶-, selected from C₁-C₃alkylene, optionally substituted with 1–4 F, -CH₂-O-CH₂-, -CH₂-NH-CH₂- or any of structures , where the arrows denote bonds in formula (II); (ii) saturated 5–6 membered heterocyclic ring Z containing 1 to 2 heteroatoms independently selected from N, O and S, optionally containing from 1 to 3 substituents R⁹; wherein R⁹ independently in each case is halogen, -OH, C₁-C₃alkyl, CH₂OH, CH₂CH₂OH, CH₂F, CHF₂, CF₃, CH₂CF₃, C₁-C₂alkoxy, C₁-C₂alkoxy-C₁-C₃alkyl, C₃-C₆cycloalkyl, = O, -NH₂, NHCH₃ or N(CH₃)₂; or two R⁹ substituents together form divalent residue -R¹⁰R¹¹-, selected from C₁-C₃alkylene, optionally substituted with 1-4 F, -CH₂-O-CH₂- or -O-CH₂CH₂-O-; which are inhibitors of phosphoinositol-3-kinases (PI3K), targets of rapamycin in mammals (mTOR) and kinases related to PI3K- (PIKK).

EFFECT: disclosed are difluoromethylaminopyridines and difluoromethylaminopyrimidines.

24 cl, 13 tbl, 67 ex