BIARYL DERIVATIVE, METHOD FOR PRODUCTION THEREOF AND PHARMACEUTICAL APPLICATION THEREOF Russian patent published in 2022 - IPC C07D401/12 C07D401/14 C07D405/14 C07D409/14 C07D413/14 A61K31/444 A61P31/00 A61P35/00 A61P37/02 

FIELD: chemistry.

SUBSTANCE: invention relates to a compound by the formula (III), a stereoisomer or a pharmacologically acceptable salt thereof, applicable in preventing and/or treating a disease mediated by a PD-1/PD-L1 signalling pathway. In the formula (III), R₁ is selected from the group consisting of hydrogen and a _1-10 alkyl; R₂ is selected from the group consisting of hydrogen, a C_1-10 alkyl, a C_3-10 cycloalkyl, a C_3-10 cycloalkyl, a C_1-8 alkyl and a 3-10-membered heterocyclyl, or R₁ and R₂ together with the nitrogen atom directly attached thereto form a 3-10-membered heterocyclyl, the above groups are unsubstituted or substituted by one or more substituents selected from the group consisting of halogen, a C_1-10 alkyl, a C_1-10 haloalkyl, a C_3-10 cycloalkyl, a 3-10-membered heterocyclyl, =O, -C_0-8-S(O)(=N-R₇)R₉, -C_0-8-N=S(O)R₉R₁₀, -C_0-8-S(O)_rR₁₂, -C_0-8-O-R₁₃, -C_0-8-C(O)OR₁₃, -C_0-8-C(O)R₁₄, -C_0-8-C(O)NR₁₅R₁₆ , and -C_0-8-N(R₁₅)-C(O)R₁₄; R₅ is selected from the group consisting of hydrogen, methyl, and methoxy; R₆ constitutes methyl; R₇ constitutes hydrogen; R₉ is selected from a _1-10 alkyl; R₁₀ is selected from a _1-10 alkyl, or R₉ and R₁₀ together with the sulphur atom directly attached thereto form a 3-10-membered heterocyclyl with one heteroatom S; each R₁₂ is selected from a _1-10 alkyl; each R₁₃ is selected from hydrogen and a _1-10 alkyl, wherein the C_1-10 alkyl is unsubstituted or substituted by one or more substituents selected from a halogen; each R₁₄ is selected from a _1-10 alkyl; R₁₅ is selected from hydrogen and a _1-10 alkyl; R₁₆ is selected from hydrogen and a _1-10 alkyl, and each r constitutes 1 or 2; unless otherwise defined, the heterocyclyl contains 1 or 2 heteroatoms selected from nitrogen and oxygen. The invention relates also to a method for producing compounds by the formula (III), a pharmaceutical composition, an application thereof in medicine for preventing and/or treating a disease mediated by a PD-1/PD-L1-dependent signalling pathway, as well as to methods for preventing and/or treating diseases and disorders mediated by a PD-1/PD-L1-dependent signalling pathway.

EFFECT: creation of a biuryl compound applicable for preventing and/or treating diseases and disorders mediated by a PD-1/PD-L1 signalling pathway.

17 cl, 3 tbl, 141 ex