HETEROARYL-BIPHENYL AMINES FOR TREATING PD-L1 DISEASES Russian patent published in 2025 - IPC C07D471/04 C07D519/00 A61K31/42 A61K31/422 A61K31/4985 A61K45/06 A61P31/00 A61P35/00 A61P37/00 

FIELD: medicine; pharmaceutics.

SUBSTANCE: invention relates to a compound of formula (Ia), or its pharmaceutically acceptable salt and which can be used as PD-L1 inhibitors for treating diseases associated with such activity. In formula (Ia), A is selected from the group consisting of pyridinyl, pyrimidinyl, pyrazinyl and pyrazolyl, each of which is unsubstituted or has from one to two substitutes independently selected from the group consisting of C_1-3 alkyl, C_1-3 haloalkyl and C_1-3 alkoxy groups; X¹ represents C_1-3 alkylene; R^2a and R^2b are each independently selected from a group consisting of H, C_1-8 alkyl, -Y, -X²-CO₂R^a, -X²OR^a, -X²C(O)NR^aR^b and -X²Y, where each X² represents C_1-6 alkylene, and any C_1-8 alkyl or C_1-6 alkylene is unsubstituted or has from one to two substituents independently selected from the group consisting of OH, C(O)NH₂ and CO₂H, and each Y is selected from a group consisting of C_3-6 cycloalkyl, C_4-8 heterocyclyl containing 1-2 heteroatoms selected from N and O, and 5-6-member heteroaryl containing 1–2 heteroatoms selected from N, each of which is unsubstituted or has from one to three substitutes independently selected from a group, consisting of oxo group and OH; or R^2a and R^2b are combined to form 4–9-membered ring containing 1–2 heteroatoms selected from N and O, or a spirocyclic ring containing in ring from 0 to 2 additional heteroatoms selected from O and N; where 4–9-membered ring or spirocyclic ring formed by combining R^2a and R^2b is unsubstituted or has from 1 to 3 substitutes independently selected from the group consisting of oxo group, C_1-8 alkyl, -X³-CO₂R^a and -X³OR^a, where X³ is a bond; R³ and R⁴ are each independently selected from the group consisting of F, Cl, CN and CH₃; Z is a fused bicyclic heteroaryl ring selected from the following fragments, which is unsubstituted or has from one to three substituents R^c; every R^a is independently H; every R^b is independently H; every R^c is independently selected from a group consisting of C_1-6 alkyl and C_1-6 haloalkyl. Invention also relates to a pharmaceutical composition containing said compounds and use thereof in a method for modulating an immune response in a subject via a PD-1 signaling pathway.

EFFECT: disclosed are heteroaryl-biphenyl amines for treating pd-l1 diseases.

16 cl, 1 tbl, 84 ex