ION CHANNEL INHIBITORS, PHARMACEUTICAL FORMULATIONS AND APPLICATIONS Russian patent published in 2021 - IPC C07D221/20 C07D401/12 C07D409/12 A61K31/4747 A61K31/44 A61P25/00 

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to a compound of Formula I, or its pharmacologically acceptable salts:

wherein R1 is a C6-C10 aryl, optionally substituted with 1-4 substituents selected from a group consisting of halogen, cyano, C1-C6 alkyl and C1-C6 haloalkyl, benzyl, optionally substituted with 1-4 substituents selected from a group consisting of halogen and C1-C6 haloalkyl, or adamant-1-yl, optionally substituted with 1-4 halogen atoms; X is selected from -N(R14)-C(=O)-, or -N(R14)-S(=O)k-, or -CH2-N(R14)-C(=O)-, or -CH2-N(R14)-S(=O)k-, or -C(=O)-N(R14), и -CH2-C(=O)-N(R14); k is selected from 1 and 2; and R14 represents

or ;

each of R3, R4, R5, R6, R7, R8, R9 and R10 independently represents hydrogen, C1-6 alkyl or C1-6haloalkyl; each of R12 and R13 independently represents hydrogen, fluorine, C1-6 alkyl or C1-6 haloalkyl; R11 and either R12, or R13, together with the carbon atoms to which they are attached, form 3-, 4-, 5-, 6- or 7-memebered cycloalkyl group, which inhibit human T-type calcium channels and differentially modulate other key ion channels to control cell excitability and abnormal neuronal activity, particularly those involved in the development and maintenance of persistent or chronic pain and /or neurological disorders. The invention also relates to a pharmaceutical composition containing these compounds.

EFFECT: effective treatment of persistent or chronic pain and /or neurological disorders.

32 cl, 2 tbl, 158 ex, 12 dwg