SUBSTITUTED TETRAHYDROPYRROLOPYRAZINE COMPOUNDS AND USE THEREOF IN DRUG PREPARATIONS (TRADEMARK GRA 3 363) Russian patent published in 2012 - IPC C07D487/04 A61K31/4985 A61P25/00 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to substituted tetrahydropyrrolopyrazines of general formula I, wherein R¹, R² and R³ in each case independently mean hydrogen or groups R¹ and R² or R² and R³ form a common cycle ; R⁴ and R⁵ in each case independently mean H; R⁶ means branched or unbranched saturated, unsubstituted C_1-6-alkyl, or unsubstituted heteroaryl wherein heteroaryl is a 5- or 6-member aromatic residue containing 1 heteroatom specified in a group consisting of N, O and S, or means phenyl wherein phenyl is unsubstituted or single-substituted or double-substituted by 1 or 2 substitutes which in each case are independently specified in a group consisting of F, Cl, Br, I, CF₃, C_1-6-alkyl, O-C_1-6-alkyl, and , or means unsubstituted phenyl attached through C_1-3-alkyl chain; R^4a, R^5a and R^6a in each case independently mean H; R⁷ means (CH₂)_tC(=O)R⁸, wherein t is equal to 1, (C=O)(CH₂)_mNR¹¹R¹², wherein m is equal to 1 or 2, C(=O)(CH₂)_n(C=O)R⁸, wherein n is equal to 1, 2 or 3, (CH₂)_sNHC(=O)R⁸, wherein s is equal to 1 or 2; R⁸ means NR⁹R¹⁰ or saturated, branched or unbranched, unsubstituted C_1-6-alkyl; wherein R⁹ and R¹⁰ in each case independently mean H, saturated, branched or unbranched, unsubstituted C_1-6-alkyl, or unsubstituted or saturated C_3-8-cycloalkyl, or phenyl, or phenyl attached through C_1-3-alkyl wherein the alkyl chain is saturated, branched or unbranched, and wherein phenyl in each case is unsaturated or single or double saturated by 1 or 2 substitutes which independently specified in a group consisting of F, Cl, Br, I, CF₃, C_1-6-alkyl, O-C_1-6-alkyl, pyridyl, and , or unsubstituted heteroaryl attached through C_1-3-alkyl wherein heteroaryl is a 5-member aromatic residue 1 heteroatom of which are specified in a group consisting of O and S, wherein the alkyl chain is saturated, branched or unbranched, or heterocyclyl, or heterocyclyl attached through C_1-3-alkyl wherein the alkyl chain is saturated, branched or unbranched, and wherein heterocyclyl in each case is saturated, unsubstituted or single substituted by benzyl, and heterocyclyl contains cycloalkyl containing 5 to 6 atoms in a cycle wherein 1 or 2 carbon atoms are substituted by 1 or 2 heteroatoms which are specified in a group consisting of N; or both groups R⁹ and R¹⁰ mean (CH₂)_3-6, CH₂CH₂OCH₂CH₂ or CH₂CH₂NR¹⁴CH₂CH₂; wherein R¹⁴ means phenyl or phenyl attached through C_1-3-alkyl wherein phenyl in each case is unsaturated or single substituted by a substitute whih is specified in a group consisting of F, Cl, Br, I, O-C_1-6-alkyl, and , or R¹⁴ means C(=O)R¹³; wherein R¹³ means saturated and unbranched C_1-6-alkyl or means phenyl condensed with heteroaryl wherein heteroaryl is a 6-member aromatic residue 1 heteroatom of which is specified in a group consisting of N; R¹¹ and R¹² in each case independently mean H, saturated, branched or unbranched C_1-6-alkyl, or unsubstituted, saturated C_3-8-cycloalkyl, C(=O)R²⁰ or S(=O)₂R¹³; wherein R²⁰ means NR²¹NR²², or R²⁰ means saturated, branched or unbranched C_1-6-alkyl, or means saturated C_3-8-cycloalkyl, unsubstituted or single substituted by phenyl, or means unsaturated heteroaryl wherein heteroaryl is a 5-member aromatic residue 1 heteroatom of which is specified in a group consisting of O, or means phenyl wherein phenyl is unsubstituted or single substituted by C_1-6-alkyl or means phenyl attached through C_1-6-alkyl which is unsubstituted or single substituted by a substitute specified in a group consisting of F, Cl, Br, I and CF₃, wherein the alkyl chain is saturated or unsaturated, branched or unbranched; wherein R²¹ and R²² in each case independently mean H or saturated, branched or unbranched, unsubstituted C_1-6-alkyl; in the form of bases and salts of physiologically acceptable acids. The invention also refers to methods for preparing them, to drug preparations for treating disorders or diseases related with at least partially KCNQ2/3 K⁺ canals containing such compounds.

EFFECT: there are prepared new compounds and based drug preparations which can find application in medicine for managing pain, epilepsy, migraine, panic conditions and urinary incontinence.

17 cl, 2 tbl, 91 ex