COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS OF 2-AMINOPYRIMIDINE AND THEIR USE Russian patent published in 2023 - IPC C07D471/04 A61K31/519 A61P31/00 A61P31/12 A61P35/00 A61P37/00 

FIELD: pharmaceutical chemistry.

SUBSTANCE: includes 2-aminopyrimidine derivative of formula I, its stereoisomer or pharmaceutically acceptable salt, pharmaceutical composition and application. In formula I, X is N; Y is NH; Z is selected from the group consisting of -N(H)C(O)R₄ and -OH; R₁ and R₃ are hydrogen; R₂ is selected from the group consisting of -NR₈R₉, -CONR₁₀R₁₁, -COR₁₀ and -S(O)₂NR₁₀R₁₁; R₄, R₅ and R₆ are independently selected from the group consisting of C₁-C₆ alkyl, C₃-C₁₀ heterocycloalkyl; heterocycloalkyl includes 1, 2 or 3 heteroatoms selected from N, O or S; R₈ is C₃-C₁₀ cycloalkyl; R₉, R₁₀ and R₁₁ are independently selected from the group consisting of hydrogen, hydroxyl, C₁-C₆ alkyl, C₃-C₁₀ heteroaryl; heteroaryl includes 1, 2 or 3 heteroatoms selected from N, O or S; alkyl, heteroaryl optionally substituted with 1-3 substituents selected from the group consisting of (C₁-C₆ alkyl)₂N-, C₁-C₆ alkyl; or R₁₀ and R₁₁ and N, to which they are appropriately linked, form a C₃-C₁₀ heterocycloalkyl containing 1 or 2 heteroatoms selected from N or O; heterocycloalkyl is optionally substituted with 1-3 substituents selected from the group consisting of halogen, hydroxyl, (C₁-C₆ alkyl)₂N-, C₁-C₆ alkoxy and C₆-C₁₂ aryl.

EFFECT: 2-aminopyrimidine derivative of formula I with selective TLR8 activator properties.

10 cl, 2 tbl, 22 ex