PYRIMIDINE DERIVATIVES AS INHIBITORS OF PD1/PD-L1 ACTIVATION Russian patent published in 2022 - IPC C07D401/14 A61P35/00 C07D239/52 C07D401/06 C07D405/14 

FIELD: biotechnology.

SUBSTANCE: invention relates to new compounds of the formula I, their stereoisomers and their pharmaceutically acceptable salts, where R₁, R₂, R₃, and R₄ are independently selected from hydrogen, C_1-10 alkyl, C_1-10 alkoxy, C_1-6 halogenalkyl, C₆ aryl, and 6 or 10-element monocyclic or bicyclic heteroaryl with 1-2 heteroatoms selected from N or O, where C_1-10 alkyl, C₆ aryl, and 6 or 10-element monocyclic or bicyclic heteroaryl are optionally substituted with one or more groups selected from hydrogen, halogen, hydroxyl, cyano, C_1-6 alkyl, or C_1-6 alkoxy, where C_1-6 alkoxy is optionally substituted with C_4-5 heterocyclyl with one nitrogen heteroatom, where C_4-5 heterocyclyl is optionally substituted with one or more groups selected from halogen; O is absent or is oxygen; R₅ is selected from

; and R₆ is selected from a group consisting of hydrogen, C(O)C_1-6 alkyl. A method for the production of compounds of the formula I is also described.

EFFECT: described compounds are 2-(benzyloxy)pyrimidine derivatives, which are inhibitors of PD-1/PD-L1 activation.

formula I

11 cl, 1 dwg, 4 tbl, 8 ex