SUBSTITUTED NICOTINAMIDES AS KCNQ2-3 MODULATORS Russian patent published in 2014 - IPC C07D213/82 C07D401/12 C07D405/12 C07D413/12 A61K31/465 A61K31/4436 A61P29/00 

FIELD: medicine, pharmaceutics.

SUBSTANCE: in general formula A¹ stands for CR¹⁰R¹¹ or S; A² stands for CR¹²R¹³, C(=O), O, S or S(=O)₂; R¹ stands for C_1-10-alkyl, saturated or unsaturated, branched or non-branched, non-substituted, or monosubstituted, or polysubstituted; C_3-10-cycloalkyl or 5- or 6-membered heterocyclyl with the O-atom, each time saturated or unsaturated, non-substituted, or monosubstituted, or polysubstituted; C_6-10-aryl or C_5-10-heteroaryl with 1-3 heteroatoms, selected from N, O or S, each time non-substituted, or monosubstituted, or polysubstituted; through C_1-8-alkyl or C_2-8-heteroalkyl bound by the bridge bond C_3-10-cycloalkyl, each time saturated, non-substituted, and the alkyl or heteroalkyl chain each time can be branched or non-branched, saturated, non-substituted; or through C_1-8-alkyl, bound by the bridge bond aryl or heteroaryl, each time non-substituted, or monosubstituted, or polysubstituted, and the alkyl chain each time can be branched or non-branched, saturated or unsaturated, non-substituted, or monosubstituted, or polysubstituted; R², R³ and R⁴ each time independently on each other stand for H; F; Cl; Br; I; methyl; O-C_1-6-alkyl or NR^aR^b, and R^a and R^b together with the nitrogen atom that binds them form heterocyclyl, saturated, non-branched, non-substituted; R⁵, R⁶, R⁷, R⁸, R¹⁰, R¹¹, R¹² and R¹³each time independently on each other stand for H; F; Cl; Br; I; OH or C_1-10-alkul; or R⁵ and R⁶ or R⁷ and R¹¹ together with carbon atom(s), that bind(s) them form C_3-8-cycloalkyl, each time saturated or non-saturated, non-substituted, or monosubstituted, or polysubstituted; with respective remaining substituents R⁵, R⁶, R⁷, R⁸, R¹⁰, R¹¹, R¹² and R¹³ having the value given above; R⁹ stands for C_3-10-cycloalkyl, saturated, non-substituted; C_6-10-aryl or 5- or 6-membered heteroaryl with heteroatom, selected from N and S, each time non-substituted or monosubstituted.

EFFECT: invention relates to substituted nicotinamides of general formula (1), to a medication based on them and their application for treating KCNQ2/3-mediated diseases.

13 cl, 3 tbl, 224 ex