CDK8/19 INHIBITORS Russian patent published in 2021 - IPC C07D471/04 A61K31/4375 A61P35/00 

FIELD: pharmaceutics.

SUBSTANCE: invention relates to a compound of the formula I or its pharmaceutically acceptable salt, which can be used as inhibitors of the activity of cyclin-dependent protein kinases CDK8/19. In the formula I, L is -[CH₂]_0-3-, - [CH₂]_0-2-C(O)-, -C(O)-[CH₂]_0-2-; R is -NR⁴R⁵, -OR⁶; R¹ is -NR²R³; R² and R³ are independently H; C_1-6 alkyl, unsubstituted or substituted with one or several substituents of R⁷; C_3-7 cycloalkyl, unsubstituted or substituted with one or several substituents of R⁸; or R² and R³, together with a nitrogen atom to which they are attached, form 4-7-element heterocyclic ring with 1-3 heteroatoms selected from N, where heterocyclic ring formed by R² and R³ can be unsubstituted or substituted with one or several substituents of R⁹; R⁴ and R⁵ are independently H; C_1-6 alkyl, unsubstituted or substituted with one or several substituents of R¹², or R⁴ and R⁵, together with a nitrogen atom to which they are attached, form 4-7-element heterocyclic ring with 1-3 heteroatoms selected from N, where heterocyclic ring formed by R⁴ and R⁵ can be unsubstituted or substituted by one or several substituents of R¹⁴; R⁶ is H; C_1-6 alkyl; R⁷ and R¹², each independently, is H, -OR¹⁸, C_3-7 cycloalkyl, unsubstituted or substituted by one or several radicals selected from C_1-6 alkyl, halogen; R⁸ is H, Hal; R⁹ and R¹⁴, each independently, is H, C_1-6 alkyl; R¹⁸ is H, C₁-C₆ alkyl. The invention also relates to a pharmaceutical composition containing therapeutically effective amount of a compound of the formula I and intended for the prevention or treatment of a disease or disorder mediated by the activation of cyclin-dependent protein kinases CDK8/19, and to a method for treating a disease or disorder mediated by the activation of cyclin-dependent protein kinases CDK8/19, including the injection of therapeutically effective amount of the specified compound.

EFFECT: obtaining CDK8/19 inhibitors.

11 cl, 6 tbl, 12 ex