DERIVATIVES OF 1,5-BENZODIAZEPINE, METHOD OF THEIR SYNTHESIS, PHARMACEUTICAL COMPOSITION Russian patent published in 1998 - IPC

FIELD: organic chemistry and technology, pharmacy. SUBSTANCE: invention relates to derivatives of 1,5-benzodiazepine of the formula (I) where R¹ is a bridge C_7-11--cycloalkyl or C_1-6--alkyl possibly substituted with hydroxyl, phenyl, alkoxycarbonyl, C_3-7--cycloalkyl or a bridge C_7-11--cycloalkyl; R² - free or substituted phenyl where halogen, C_1-4--alkyl, nitro-, cyano- trifluoromethoxy-, alkylthio-group or (CH₂)_nR⁴ can be substituents; R⁴ is hydroxy, alkoxy, CO₂R⁵ or NR⁶R⁷; R³ - is phenyl possibly substituted with one or two halogen atoms; R⁵ - - hydrogen or C_1-4--alkyl; R⁶ and R⁷ are C_1-4--alkyl; R⁸ - hydrogen or halogen; m = 0, 1 or 2; n = 0 or 1, or their pharmaceutically acceptable salts and solvates. Synthesized compounds are strong and specific antagonists of gastrin and/or cholecystokinin. EFFECT: improved method of synthesis, enhanced effectiveness of compounds. 14 cl, 2 tbl, 149 ex