INHIBITOR CONTAINING A TRICYCLIC DERIVATIVE, A METHOD OF ITS PRODUCTION AND ITS USE Russian patent published in 2023 - IPC C07D498/04 C07D498/14 A61K31/553 A61K31/4162 A61K31/4188 A61K31/4196 A61P35/00 

FIELD: medicine.

SUBSTANCE: invention relates to a compound of formula (VI), its stereoisomer, or a pharmaceutically acceptable salt thereof, wherein ring B is selected from the group consisting of the following:

L is nitrogen; G is oxygen; Q is N; Z is -CR_aa; R_aa is selected from the group consisting of hydrogen and deuterium; each R^y is independently selected from the group consisting of hydrogen and deuterium; each of R₅, R₆ and R₁₄ is independently selected from the group consisting of hydrogen, deuterium and halogen; each of R₃ and R₄ is independently selected from the group consisting of hydrogen, deuterium, C_1-6 alkyl, C_1-6 deuterated alkyl and -(CH₂)_n1OR_bb, wherein each of the said C_1-6 alkyl and C_1-6 deuterated alkyl is optionally further substituted with one or more substituents selected from the group consisting of deuterium and C_1-6 alkoxy; R₂ is selected from the group consisting of hydrogen, deuterium and C_1-6 alkyl; or R₂ and R₃ are associated with the formation of a 4–6-membered heterocyclyl containing nitrogen, where the number of nitrogen atoms is equal to one or two; R^z is selected from the group consisting of hydrogen, deuterium, C_1-6 alkyl, C_1-6 deuterated alkyl and C_1-6 haloalkyl, wherein the said C_1-6 alkyl is optionally further substituted with one or more substituents selected from the group, consisting of deuterium, halogen, cyano; R_bb is selected from the group consisting of hydrogen, C_1-6 alkyl and cyano; n₁ is 0.1, 2 or 3; m is 1; t is 1; n is 1; and q is either 0, 1, 2, 3, 4, 5, or 6. The invention also relates to methods of preparing a compound of formula (VI), a pharmaceutical composition for inhibiting the activity of phosphatidylinositol-3-kinase (PI3K) based on it.

EFFECT: new compounds and a pharmaceutical composition based on them have been obtained, which can be used in medicine in the treatment of cancer and diseases or conditions mediated or dependent on PI3K imbalance.

24 cl, 4 tbl, 129 ex