SUBSTITUTED BENZO[d]ISOXAZOL-3-YLAMINE COMPOUNDS AND USE THEREOF AS ANALGESICS Russian patent published in 2011 - IPC C07D261/20 C07D413/12 A61K31/423 A61K31/4439 A61P29/00 

FIELD: chemistry.

SUBSTANCE: invention relates to novel benzo[d]isoxazol-3-ylamine compounds of formula I in free form or in form of salts with physiologically compatible acids, having antagonistic effect on KCNQ2/3 ion channel. In formula I , R¹, R², R³ and R⁴ independently denote H, F, CI, Br, I, -NR⁷R⁸, -OR⁹ or C₁-C₁₀alkyl, R⁵ denotes -C(=S)NR²¹R²² or (CHR⁶)_n-R²⁵, where n equals 1, 2 or 3, R⁶ denotes H or C₁-C₆ alkyl, R²⁵ denotes aryl or heteroaryl, R⁷ and R⁸ independently denote H or C₁-C₁₀ alkyl, R⁹ denotes H, C₁-C₁₀alkyl or -(C₁-C₅alkylene)aryl, R²¹ denotes H, R²² denotes C₁-C₁₀alkyl, C₂-C₁₀alkenyl, C₃-C₈cycloalkyl, -(C₁-C₅alkylene)-C₃-C₈cycloalkyl, -(C₁-C₃alkylene)heterocycloalkyl, aryl, heteroaryl or -(C₁-C₅alkylene)aryl, wherein each of the heterocycloalkyl residues has 5-6 members, contains 1 or 2 heteroatoms in the ring, independently selected from oxygen and nitrogen, each of the aryl residues is phenyl, anthracenyl or naphthyl, each of the heteroaryl residues has 5 or 6 members and contains 1 or 2 heteroatoms in the ring, independently selected from oxygen, sulphur and nitrogen.

EFFECT: said compounds can be used to prepare a medicinal agent for curing pain, migraine, anxiety, uroclepsia or epilepsy.

17 cl, 203 ex