NITROGEN-CONTAINING HETEROCYCLIC AMIDE AND ITS USE FOR MEDICAL PURPOSES Russian patent published in 2023 - IPC C07D487/04 C07D498/04 C07D519/00 A61K31/437 A61K31/4985 A61K31/506 A61P3/10 A61P9/04 A61P9/12 A61P43/00 

FIELD: medicine.

SUBSTANCE: invention relates to a compound of the formula [I-a] or the formula [II] or its pharmaceutically acceptable salt, where a dotted line bond is a single bond or a double bond, X¹ is a carbon atom, a nitrogen atom, or an oxygen atom, X² is a carbon atom or a nitrogen atom, R^1a is C_1-4 alkyl or C_1-4 alkyl carbonyl, R² is halogen, cyano group, or C_1-4 alkyl, m is 0 or 1, n is 0, 1, or 2, if n is 2, all R² are the same or different, A¹, A², A³, A⁴, A⁵, A⁶, and A⁷ are all independently selected from a group including a carbon atom, a nitrogen atom, and an oxygen atom, A⁸ is selected from a group including a carbon atom and a nitrogen atom, and the total number of nitrogen atoms and oxygen atoms contained in the structural formula of a fragment (a) is 0, 1, 2, or 3, t is 0 or 1, r is 0, 1, or 2, and the sum of t and r is 1 or 2, w is 0 or 1, R³ and R⁴, all independently, are hydrogen or C_1-4 alkyl; Cy¹ is (1) (i) C_4-6 cycloalkyl or (ii) 4-6-element saturated or partially saturated heterocyclyl containing one nitrogen atom, C_4-6 cycloalkyl and saturated or partially saturated heterocyclyl is optionally substituted with one substitute independently selected from a group including C_1-4 alkyl and an oxo group, or (2) (i) phenyl or (ii) 5- or 6-element heteroaryl containing 1, 2, or 3 heteroatoms independently selected from a group including a nitrogen atom and an oxygen atom, phenyl and heteroaryl are optionally substituted with 1 or 2 substitutes independently selected from a group including halogen, cyano group, carboxy group, C_1-4 alkyl, halogen-C_1-4 alkyl, and C_3-6 cycloalkyl; Cy² is (1) (i) C_3-6 cycloalkyl or (ii) 4-6-element saturated heterocyclyl containing 1 or 2 heteroatoms independently selected from a group including a nitrogen atom and an oxygen atom, and C_3-6 cycloalkyl and saturated heterocyclyl are optionally substituted with 1 or 2 substitutes independently selected from a group including halogen, hydroxy group, and C_1-4 alkyl, or (2) (i) phenyl or (ii) 5- or 6-element heteroaryl containing 1, 2, 3, or 4 nitrogen atoms, and phenyl and heteroaryl are optionally substituted with 1 or 2 substitutes independently selected from a group including halogen, cyano group, C_1-4 alkyl, C_1-4 alkoxy group, and C_1-4 alkyl sulfonyl, and v is 0 or 1. The invention also relates to a pharmaceutical composition having an inhibitory effect on the activity of PDHK1 and 2, containing effective amount of a compound, according to the invention, or its pharmaceutically acceptable salt and a pharmaceutically acceptable carrier. Compounds, according to the invention, are intended for use in the treatment of diseases associated with an inhibitory effect on the activity of PDHK1 and 2.

EFFECT: nitrogen-containing heterocyclic amide, which has an inhibitory effect on pyruvate dehydrogenase kinase (PDHK 1 and 2).

, ,

46 cl, 26 tbl, 140 ex