CONDENSED TRICYCLIC COMPOUND AND USE THEREOF IN MEDICINE Russian patent published in 2025 - IPC C07D471/04 C07D471/14 C07D487/14 C07D498/14 A61K31/424 A61K31/437 A61K31/4985 A61K31/506 A61K31/519 A61P3/04 A61P3/06 A61P3/10 A61P9/04 A61P9/10 A61P9/12 A61P11/00 A61P13/12 A61P25/28 A61P27/02 A61P27/06 A61P35/00 

FIELD: chemistry; pharmaceutics.

SUBSTANCE: group of inventions relates to organic chemistry and pharmaceutics and includes a tricyclic compound of formula [I-a], pharmaceutically acceptable salts thereof, individual compounds and pharmaceutically acceptable salts thereof, specified in the claim, a pharmaceutical composition containing such compounds, a PDHC inhibitor, a PDHC2 inhibitor, agent for treating a disease associated with inhibitory action on PDHC activity, a method of inhibiting PDHC activity, a method of treating a disease associated with an inhibitory effect on PDHC activity, and use of the compounds. In formula [I-a], the bond indicated by the dotted line is a single bond or a double bond, provided that the ring formed by the dotted lines is an aromatic ring, X¹, X², X³ and X⁴ each independently represents CH or N, Y¹ and Y² each independently represents CH, N or O (where the total amount of N and O for X², X³, X⁴, Y¹ or Y² is 0–3), R^A is C_1-4 alkyl, R^B is (1) halogen, (2) cyano, (3) hydroxy, (4) oxo, (5) -COR¹, (6) C_1-8 alkyl, (7) C_1-8 alkoxy, (8) -Cy², (9) -OCy³, m equals 0 or 1, n equals 0, 1 or 2, when n equals 2, all R^B can be identical or different, other substitutes are as presented in claims.

EFFECT: condensed tricyclic derivatives of formula [Ia] have inhibitory action on PDHA.

38 cl, 28 tbl, 107 ex