DERIVATIVES OF N-ACYL-2-ARYLCYCLOALKYLAMINE STIMULATING MELATONIN SYNTHESIS, PHARMACEUTICAL COMPOSITION, METHOD OF MELATONIN-STIMULATING BINDING

摘要

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention describes novel derivatives of N-acyl-2-arylcycloalkylamine of the formula (I) or (II) that stimulate synthesis of melatonin where X is halogen, hydrogen atom, C_1-4-alkyl or OR₅ where R₅ means hydrogen atom, C_1-4-perfluoroalkyl, C_1-4-fluoroalkyl, C_1-4-perdeuterium-alkyl, C_1-20-alkyl, C_4-20-alkylcycloalkyl, C_2-20-carbonitriloalkyl, C_3-22- -carboalkoxyalkyl, C_3-20-alkenyl, C_3-20-alkynyl, C_9-20-phenylalkyl, C_9-20-phenylalkenyl, C_9-20-phenylalkynyl, C_2-20-hydroxyalkyl, C_8-20- -phenylhydroxyalkyl, C_7-20-pyridylalkyl or C_6-20-pyrrylalkyl; Y is hydrogen or halogen atom; Z is hydrogen, halogen atom, cyano- -group, phenyl, C_7-20-phenylalkyl, C_8-20-phenylalkynyl or C_2-20- -alkylamido-group; R is hydrogen, halogen atom or C_1-4-alkyl in both cases; n = 1 or 2; G is bivalent methylene, ethylene or C_1-4-alkylmethylene residue; R₁ is hydrogen atom, C_1-4-alkyl or benzyl-group; R₂ is C_1-6-alkyl, C_2-6-alkenyl, C_3-6/ -cycloalkyl, C_2-4-alkoxyalkyl, C_1-4-trifluoromethylalkyl, C_2-8-alkylthioalkyl or NR₃R₄ where R₃ and R₄ are taken independently each of other among hydrogen atom and C_1-4-alkyl but R₃ and R₄ can not mean hydrogen atom simultaneously. New derivatives of N-acyl-2-aryl- -cyclopropylmethylamine show medicinal and biologically active properties. These compounds stimulate synthesis of melatonin and they are useful therefore for treatment of patients with some diseases. Invention describes method of their synthesis also. EFFECT: new compounds indicated above, improved method of synthesis, valuable medicinal properties. 19 cl, 6 tbl