ARYLAMIDE DERIVATIVES AS TTX-S BLOCKERS Russian patent published in 2014 - IPC C07D213/81 C07D213/64 C07D239/42 C07D401/12 C07D401/14 C07D405/12 C07D413/12 C07D417/14 A61K31/44 A61K31/4427 A61K31/444 A61K31/506 A61P25/00 A61P29/00 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to compounds of formula (I) and (II), which possess the blocking activity on voltage-sensitive sodium channels, such as TTX-S channels, and their pharmaceutically salts. In general formula (I) and (II), R¹ represents -CF₃, -CHF₂, -OCF₃, -OCHF₂, -OCH₂CHF_2/ -OCH₂CF₃, -OCF₂CHF₂; -OCF₂CF₃, -OCH₂CH₂CF₃, -OCH(CH₃)CF₃, -OCH₂C(CH₃)F₂, -OCH₂CF₂CHF₂, -OCH₂CF₂CF₃, OCH₂CH₂OCH₂CF₃, -NHCH₂CF₃, -SCF₃, -SCH₂CF₃, -CH₂CF₃ -CH₂CH₂CF₃, -CH₂OCH₂CF₃ and -OCH₂CH₂OCF₃; R² is specified in (1) hydrogen, (2) halogen (3) -O_n-C_1-6 alkyl, (4) -O_n-C_3-6 cycloalkyl, (5) -O_n-phenyl, (6) -O_n-heterocyclic group, (7) -NR⁷ (C=O)R⁸; wherein n is equal to 0 or 1, p is equal to 1, 2; R³ and R⁴ represents hydrogen or C_1-6 alkyl, X represents carbon atom; Y represents hydrogen or C_1-6 alkyl; Ar represents 4-pyridyl, 4-pyrimidyl or 6-pyrimidyl, which is substituted in the 2^nd position by a substitute, which is independently specified in (1) -(C=O)-NR⁷R⁸, (2) -NR⁷(C=O)R⁸; R⁹ is specified in: (1) hydrogen, (2) halogen, (3) -O_n-C_1-6 alkyl, wherein alkyl is unsubstituted or substituted by hydroxyl; q is equal to 1, 2 or 3; R¹⁰ independently represents hydrogen, C_1-6 alkyl, C_2-6alkenyl, C_3-7 cycloalkyl or phenyl, which is unsubstituted or substituted by one or substitutes independently specified in hydroxyl, -O_n-C_1-6 alkyl and -C_3-7 cycloalkyl.

EFFECT: preparing the compounds possessing the blocking activity on voltage-sensitive sodium channels.

7 cl, 2 tbl, 1281 ex