N-TRIAZOLYL-2-INDOLECARBOXAMIDES, METHOD OF THEIR SYNTHESIS (VARIANTS), PHARMACEUTICAL COMPOSITION CONTAINING THEREOF (VARIANTS) AND 1-SUBSTITUTED 3-AMINOTRIAZOLES Russian patent published in 2001 - IPC

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention describes N-tri-azolyl-2-indolecarboxamides of the general formula (I) where R¹ means (C₂-C₆)-alkyl, group -(CH₂)_n-G with n = 0-5 and G that means nonaromatic monocyclic or polycyclic C₃-C₁₃-hydrocarbon group, phenyl-C₁-C₃-alkyl where phenyl group can be substituted once with halogen atom or C₁-C₃-alkoxy-group, group -(CH₂)_nNR₂R₃ where n = 1-6 and R₂ and R₃ can be similar or different and they mean C₁-C₃-alkyl or with nitrogen atom to which they are bound form morpholino-group or piperidino-group; X₁ X₂, X₃, X₄, each means independently hydrogen or halogen atom, (C₁-C₆)-alkyl or (C₁-C₃)-alkoxy-group under condition that only one of X₁ X₂, X₃, X₄, means possibly hydrogen atom; R₄ means hydrogen atom, group (CH₂)_nCOOR₅ where n is determined above and R₅ means hydrogen atom or (C₁-C₆)-alkyl; (C₁-C₆)-alkyl; group -(CH₂)_nOR₅ or group (CH₂)_nOR₂R₅, where n, R₂, R₃ and R₅ are determined above; group -(CH₂)_n-tetrazolyl where n is determined above and R₄ means one of these groups as alkaline metal salt; Y₁, Y₂, Y₃ each means independently hydrogen, halogen atom, (C₁-C₃)-alkyl, -alkoxy-group or carbamoyl-group; or one of their salts or solvents. Invention relates to also methods of their synthesis, to pharmaceutical composition containing these compounds and 1-substituted 3-aminotriazoles of the formula (7) as intermediate compounds used for synthesis of compounds of the formula (I). Synthesized compounds show activity of partial or complete agonist of CCK-A-receptors and they can be used for treatment of patients with disorders of nutrition, obesity, later dyskinesia and gastroenteric tract. EFFECT: improved method of synthesis, valuable medicinal properties. 13 cl, 7 tbl, 512 ex