| 摘要 |
FIELD: organic chemistry and technology, pharmacy. SUBSTANCE: invention relates to derivatives of 1,5-benzodiazepine of the formula (I) <EMI ID=0.340 HE=30 WI=72 TI=CHI> where R is a bridge C<SB>7-11</SB>--cycloalkyl or C<SB>1-6</SB>--alkyl possibly substituted with hydroxyl, phenyl, alkoxycarbonyl, C<SB>3-7</SB>--cycloalkyl or a bridge C<SB>7-11</SB>--cycloalkyl; R - free or substituted phenyl where halogen, C<SB>1-4</SB>--alkyl, nitro-, cyano- trifluoromethoxy-, alkylthio-group or (CH<SB>2</SB>)<SB>n</SB>R can be substituents; R is hydroxy, alkoxy, CO<SB>2</SB>R or NR<SP>6</SP>R ; R<SP>3</SP> - is phenyl possibly substituted with one or two halogen atoms; R<SP>5</SP> - - hydrogen or C<SB>1-4</SB>--alkyl; R and R are C<SB>1-4</SB>--alkyl; R - 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 exs
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