NEW COMPOUND AS A PROTEIN KINASE INHIBITOR AND PHARMACEUTICAL COMPOSITION CONTAINING SAID COMPOUND Russian patent published in 2022 - IPC C07D401/04 C07D401/14 C07D405/14 C07D409/14 C07D417/14 A61K31/4439 

FIELD: chemistry.

SUBSTANCE: invention relates to a compound by the formula 1, stereoisomers or pharmaceutically acceptable salts thereof exhibiting the ability to inhibit the activity of Janus kinase 1 (JAK1). In formula 1, R₁ constitutes H, a C_1-6alkyl, or a C_1-6alkoxy; X constitutes C-A₁ or N, Y constitutes C-A₂ or N-A₄, Z constitutes C-A₃ or N-A₅, wherein at least one from X, Y, and Z includes N; at least one bond between X and Y or bond between Y and Z is a double bond, and if the bond between X and Y is a double bond, A₁ or A₄ is absent; each of substitutes from A₁ to A₄ independently constitutes H; A₅ independently constitutes H, a C_1-6alkyl, or a -C(=O)-NH-C_1-6halogenalkyl; R₂ constitutes H or a C_1-6alkyl; each of n and m independently equals 0, 1, 2, or 3; B₁ constitutes -C(=O)-; B₂ constitutes a C_3-7cycloalkyl; B₃ constitutes H; D₁ constitutes -NR₃-; D₂ constitutes -C(=O)-; D₃ constitutes -NR₃-, , , or a single bond; D₄ constitutes H, a C_1-6alkyl, a C_1-6alkenyl, a C_1-6halogenalkyl, a C_1-6cyanoalkyl, a C_3-7cycloalkyl, a 5-6-membered heterocycloalkyl, a C_1-6alkyl, wherein one H is substituted with methylpiperazine, a 6-membered aryl, or a 5-6-membered heteroaryl; wherein when D₄ constitutes a C_1-6alkyl wherein one H is substituted with methylpiperazine, then D₃ constitutes a single bond, where at least one H contained in the C_1-6alkyl or C_1-6alkenyl can be substituted with a C_3-7cycloalkyl, a 6-membered aryl, a 5-6-membered heteroaryl, or cyano, at least one H contained in the C_3-7cycloalkyl or 5-6-membered heterocycloalkyl can be substituted with a C_1-6alkyl or cyano, and at least one H contained in the 6-membered aryl or 5-6-membered heteroaryl can be substituted with a C_1-6alkyl, C_1-6alkoxy, C_1-6halogenalkyl, cyano or halogen; and each of R₃ and R₄ independently constitutes H or a C_1-6alkyl, and where the 5-6-membered heterocycloalkyl contains 1 to 3 heteroatoms selected from N, O, and S, the 5-6-membered heteroaryl contains 1 to 3 heteroatoms selected from N, O, and S, and wherein the remaining ring atoms are carbon atoms. Invention also relates to a pharmaceutical composition containing said compounds, an application thereof for preventing or treating diseases associated with Janus kinase 1, and a method for preventing or treating diseases associated with Janus kinase 1.

EFFECT: creation of a compound applicable in treatment of diseases associated with Janus kinase 1.

14 cl, 1 tbl, 63 ex