ROR GAMMA MODULATORS (RORγ) Russian patent published in 2020 - IPC C07C311/37 C07C317/32 C07D213/81 C07D261/08 A61K31/10 A61K31/166 A61K31/18 A61K31/42 A61K31/44 A61P19/02 A61P29/00 A61P37/00 

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to a compound of formula I, in which A₁₁-A₁₄ are CR₁₁, CR₁₂, CR₁₃ and CR₁₄, respectively; R₁ is C(2-6)alkyl, C(3-6)cycloalkyl, C(3-6)cycloalkylC(1-3)alkyl, (di)C(3-6)cycloalkylamino or (di)(C(3-6)cycloalkylC(1-3)alkyl) amino, where all carbon atoms of alkyl groups are optionally substituted with one or more F and where all carbon atoms of cycloalkyl groups are optionally substituted with one or more F or methyl; R₂ and R₃ are independently H, methyl or ethyl, where all alkyl groups, if present, optionally substituted with one or more F; R₄ is H; R₅ is H, C(1-6)alkyl, C(6-10)aryl, C(6-10)arylC(1-3)alkyl, C(1-9)heteroaryl, C(1-9)heteroarylC(1-3)alkyl, C(3-6)cycloalkyl, C(3-6)cycloalkylC(1-3)alkyl, C(2-5)heterocycloalkyl or C(2-5)heterocycloalkyl-C(1-3)alkyl, all groups are optionally substituted with one or more F, Cl, C(1-2)alkyl, C(1-2)alkoxy or cyano; sulphonyl group with R₁ is represented by R₈; remaining R₆-R₁₄ are independently H or C(1-6)alkyl, all alkyl groups are optionally substituted with one or more F; R₁₅ is H, C(1-6)alkyl, C(3-6)cycloalkyl, C(3-6)cycloalkylC(1-3)alkyl, C(6-10)aryl, C(6-10)arylC(1-3)alkyl, C(1-9)heteroaryl, C(1-9)heteroarylC(1-3)alkyl, C(2-5)heterocycloalkyl or C(2-5)heterocycloalkylC(1-3)alkyl, all groups are optionally substituted with one or more F, Cl, C(1-2)alkyl, C(1-2)alkoxy or cyano; and R₁₆ is C(1-6)alkyl, C(3-6)cycloalkyl, C(3-6)cycloalkylC(1-3)alkyl, C(6-10)aryl, C(6-10)arylC(1-3)alkyl, C(1-9)heteroaryl, C(1-9)heteroarylC(1-3)alkyl, C(2-5)heterocycloalkyl or C(2-5)heterocycloalkylC(1-3)alkyl, all groups are optionally substituted with one or more F, Cl, C(1-2)alkyl, C(1-2)alkoxy or cyano. Invention also relates to individual compounds and to a pharmaceutical composition.

(Formula I).

EFFECT: obtaining novel compounds of formula I, which can be used as RORγ inhibitors, as well as for treating RORγ-mediated diseases.

12 cl, 40 ex