SPIROCYCLIC PYRROLOPYRAZINE(PIPERIDINE)AMIDES AS IONIC CHANNELS MODULATORS Russian patent published in 2017 - IPC C07D471/20 A61K31/4985 A61P25/00 

FIELD: pharmacology.

SUBSTANCE: invention relates to a compound of formula

or its pharmaceutically acceptable salts. In formula I R¹ is C₁-C₈alkyl, C₁-C₈hydroxyalkyl, CO₂R⁸, or two R¹ together form an oxo group, or a 3- to 7-membered fused cycloalkyl ring; R² is halogen, C₁-C₈haloalkyl, C₁-C₈hydroxyhaloalkyl, CN, SO₂CH₃, CO₂R⁸, CON(R⁸)₂ or COR⁸; R³ is H, C₁-C₈alkyl, C₃-C₈cycloalkyl, CO₂R⁸, COR⁸, CON(R⁸)₂, CF₃, CH₂CF₃, CH₂CHF₂, CH₂-phenyl, CH₂-CN, CH₂-CO₂R⁸, CH₂-CON(R⁸)₂, CH₂-C₃-C₈cycloalkyl, C₁-C₈alkoxy-C₁-C₈alkyl or C₁-C₈hydroxyalkyl; R⁴ is C₁-C₈alkyl or halogen; A is phenyl substituted by 1 to 2 substituents; or 5-membered heteroaryl, wherein the three ring atoms are N, substituted by fluorophenyl-C₁-C₈alkyl; or 6-membered heteroaryl, wherein one ring atom is N substituted by 1 to 2 substituents; or a 9-10 membered bicyclic heteroaryl, wherein 2 to 3 ring atoms are independently heteroatoms selected from N, O, optionally substituted by 1 to 2 substituents; m is an integer from 1 to 2; n is an integer from 1 to 2; and o is an integer from 0 to 1; the values of the remaining substituents are indicated in the claims. The invention also relates to pharmaceutical compositions, to methods for inhibition of a potential-dependent sodium ion channel, to methods of treatment, to individual compounds.

EFFECT: new compounds having inhibitory activity with respect to the potential-dependent sodium ion channel are obtained.

42 cl, 3 tbl, 752 ex