FIELD: organic chemistry, pharmacy. SUBSTANCE: invention relates to new derivatives of benzodiazepines of the formula (I) where R′ means the group -CH2CH(OH)(CH2)aR4 or ketone group -CH2CO(CH2)aR5 where a = 0 or 1; R4 is C1-C7-alkyl of the direct or branched chain or C3-C8-cycloalkyl; R5 is C1-C8-alkyl, C3-C8-cycloalkyl, C3-C8-cycloalkyl-C1-C8-alkyl, C1-C8-alkyl-C3-C8-cyclo- -C1-C8-alkyl, pyrrolidyl possibly substituted with C1-C8-acyl, carbamoyl, C1-C8-alkylamino-C1-C8-alkyl or adamantyl-radical; R2 - phenyl substituted with C1-C8-alkyl, C1-C8-alkoxyl, nitro-, cyano- -group, amine, halogen atom, C1-C8-alkylamino-group, di-C1-C8- -alkylamino-group, carboxy-, C1-C8-acylamino-group, carboxyamido- -group, carboxy-(C1-C8)-alkyl or pyridyl-radical possibly substituted with C1-C8-alkyl; R3 - unsubstituted phenyl or phenyl substituted with C1-C8-alkyl or halogen atom or pyridyl-radical; X - hydrogen or halogen atom at position 7 of benzodiazepine ring; W - hydrogen atom or C1-C8-alkyl at position 8 of benzodiazepine ring, or their pharmaceutically acceptable salts. Synthesized compounds are useful as drugs showing an antagonistic effect with respect to gastrin and/or CCK-B receptors. EFFECT: improved method of synthesis, valuable medicinal properties. 14 cl, 7 ex
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Authors
Dates
1999-10-10—Published
1993-02-26—Filed