NOCICEPTINE ANTAGONISTS, AMIDE DERIVATIVES, ANALGETIC AGENT, METHOD OF INITIATION OF ANTAGONISTIC EFFECT TO NOCICEPTINE, METHOD OF PAIN TREATMENT, PHARMACEUTICAL COMPOSITIONS

摘要

FIELD: organic chemistry, medicine, pharmacy. SUBSTANCE: invention describes antagonist of nociceptine comprising amide derivative and its pharmaceutically acceptable salts of the formula [1] where R¹ and R² are similar or different and each is hydrogen atom, lower alkyl optionally substituted with hydroxy-group, amino-group, lower alkyl- -amino-group or di-(lower)-alkylamino-group; R³, R⁴ mean hydrogen atom; ring A is quinolyl, 5,6,7,8-tetrahydroacridinyl, 2,3-dihydro-1H-cyclopenta[b] quinolyl; ring B is phenyl, thienyl, furyl, pyrrolyl, pyrrolidinyl or oxazolyl; X means group of the formula: where E is single linkage or -O-; ring G is phenyl, naphthyl, benzofuranyl, 2,3-dihydrobenzofuranyl, cyclohexyl or 5,6,7,8-tetrahydro-2- naphthyl; R⁵ has different values; t = 0 or from 1 to 5; m = 0 or 1-8; n = 0 or 1-4. Invention describes also derivatives of amide of the formula [1'] and [1''] and also analgetic agent based on compounds of the formula [1'] and [1''], method of initiation of antagonistic effect to nociceptine including administration of compound of the formula [1], method of pain treatment including administration of compound of the formula [1'] or [1''] and pharmaceutical compositions containing compounds of the formula [1], [1'] or [1'']. Owing to antagonistic effect to nociceptine compounds show analgetic effect against acute pain. EFFECT: improved method of treatment, valuable medicinal properties of compounds. 14 cl, 48 tbl, 133 ex