5-HETEROCYCLO-1,5-BENZODIAZEPINES AND THEIR PHARMACEUTICALLY ACCEPTABLE SALTS Russian patent published in 2000 - IPC

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention describes the novel compounds - 5-hetero- -cyclo-1,5-benzodiazepines of the general formula (I) and their pharmaceutically salts where X is hydrogen or halogen atom; R¹ is the group NR⁴R⁵ where R⁴ means C_3-6-alkyl and R⁵ means phenyl substituted in para-position with methoxyl; R₂ is indole, phenyl or the group NHR¹¹ where R¹¹ is phenyl or phenyl substituted with carboxyl-group; R³ is heterocyclic group bound to nitrogen atom through carbon atom of its cyclic ring taken among pyridyl, pyrimidinyl or pyrazolyl and the latter is substituted three-fold with C_1-4-alkyl; z = 1. Compounds show agonistic activity with respect to cholecysto-kinin-A receptors that implies the possibility to modulate hormones gastrin and cholecystokinin in mammals. Some of these compounds show also agonistic activity with respect to chole-cystokinin-B receptors. EFFECT: new compounds indicated above, valuable hormonal activity. 6 cl, 43 ex