NEW CDK8/19 INHIBITORS Russian patent published in 2021 - IPC C07D403/12 C07D401/12 C07D471/04 C07D413/12 C07D215/38 C07D239/86 C07D241/04 A61K31/497 A61K31/517 A61K31/502 A61K31/5377 A61P35/00 A61P35/02 

FIELD: medicine.

SUBSTANCE: invention relates to a compound of the formula I or to its pharmaceutically acceptable salt, where X₁ is CR₁, N; X₂ is CR₂, N; X₃, X₄, X₅, X₆, each independently, is CH, N; R₁ is H, Hal; R₂ is H, -OR₁₀, -NR₁₁R₁₂, R₃ and R₄ together with a nitrogen atom, to which they are attached, can be 4-7-element heterocycle with 1-2 heteroatoms selected from N and/or O that can be unsubstituted or substituted with one substituent selected from C₁-C₆ alkyl unsubstituted or substituted with one or several halogens; Y is -N(R₁₃)-, -O- or -S-; Z is -C(R₁₄)₂- or -C(O)-; R₁₀ is H, C₁-C₆ alkyl; R₁₁, R₁₂, each independently, is H, C₁-C₆ alkyl; R₁₃ is H; R₁₄, each independently, is H; not including compounds, where X₁, X₃ are N, X₂, X₄, X₅, X₆ are CH, R₃ and R₄ together with a nitrogen atom, to which they are attached, are R is H, C₁-C₆ alkyl. The invention also relates to a pharmaceutical composition intended for the treatment of a disease or a disorder mediated by the activation of cyclin-dependent protein kinases CDK8/9 based on the specified compounds.

EFFECT: new compounds and a pharmaceutical composition based on them are obtained that can be used in medicine for the treatment of such diseases as colorectal cancer, melanoma, metastatic melanoma, breast cancer, triple negative breast cancer (TNBC), prostate cancer, metastatic ovarian cancer, metastatic gastric cancer, leukemia, acute myeloid leukemia, pancreatic cancer (PC).

(I)

11 cl, 11 tbl, 18 ex