| 摘要 |
This invention relates to novel derivatives of 1-[2-(substituted vinyl)]-5H-2,3-benzodiazepine, a method for producing thereof , pharmaceutical composition, a method for producing the same and a method for treatment of central nervous system diseases. Compounds according to the invention have a general formula (I) , (I) wherein A and B together form a group of formula =C=N- or =CH-NH-; R1 represents phenyl which may contain between 2 and 3 hydroxyl groups or between 1 and 3 same or different substitutes selected of the group comprising halogen, trifluoromethyl, nitro-, cyano-, amino-, C1-3 alkylamino-, di-(C1-3 alkyl)amino-, C1-4 alkanoylamino-, C1-4 alkyl. C1-4 alkoxy-, carboxyl, (C1-4 alkoxy)carbonyl, C1-4 alkoxycarbonyloxy and methylenedioxyl, naphtyl, which may contain substituent , selected of the group comprising hydroxyl. C1-4 alkoxy- and C1-4 acyloxygroup, furyl, thienyl or indole; R2 represents hydrogen or C1-4 alkyl; R3 and R4 represents each C1-4 alkoxygroup, attached in thepositions 7 or 8 of benzodiazepine ring , or R3 and R4 together form 7,8- or 8,9-methylenedioxyl group, and have a considerable activity relative to the central nervous system. |
