BROMDOMAIN INHIBITORS Russian patent published in 2018 - IPC C07D471/04 C07D487/04 A61K31/437 A61K31/5025 A61K31/5377 A61P13/12 A61P15/16 A61P25/28 A61P31/18 A61P35/00 

FIELD: pharmaceutics.

SUBSTANCE: invention relates to compounds of formula (I) or pharmaceutically acceptable salts thereof (I)

,

in which R^x is hydrogen or C₁-C₃ alkyl; R^y is C₁-C₃ alkyl; X¹ is N or CR^x1; X² represents the CR^x2; Y¹ is N or CR^u; where R^u represents hydrogen; A¹ represents the CR¹, A² represents the CR², A³ is CR³ and A⁴ represents N or CR⁴, provided that zero, one of the A¹, A², A³ and A⁴ is N; L¹ absent or means CH₂, C(O), C(H)(OH), (CH₂)_mO or (CH₂)_mN(R^z), where R^z represents hydrogen; G¹ is C₁-C₆ alkyl, C₁-C₆ alkoxy C₁-C₆ alkyl, G^1a or -(C₁-C₆ alkylenyl)-G^1a; where each G^1a is independently phenyl, 9-10-membered bicyclic aryl, optionally partially unsaturated; 5-6-membered heteroaryl with one to two heteroatoms selected from N; bicyclic 9-10-membered heteroaryl with one to three heteroatoms selected from N, S; 4-6-membered heterocycle with one to two heteroatoms selected independently from N, O and S; 10-membered spirocyclic heterocyclyl with two heteroatoms selected from O; C₃-C₇cycloalkyl; bicyclic 7-membered cycloalkyl, tricyclic 10-membered cycloalkyl, and each G^1a is independently unsubstituted or substituted by 1, 2, 3 R^w. Values of other radicals are given in the patent claim. Invention also relates to pharmaceutical composition, methods of treatment and contraceptive method in men.

EFFECT: technical result: new compounds of formula (I) with BET-inhibitory activity are obtained.

57 cl, 8 tbl, 354 ex