Benzodiazepine compounds and their use as pharmaceuticals

Details Benzodiazepine compounds and their use as pharmaceuticals Benzodiazepine compounds and their use as pharmaceuticals

C - Chemistry, Metallurgy

07

D

260/239.5

C07D 487/04 (2006.01) C07D 249/04 (2006.01)

Patent

CA 1167839

G.1181 -1- ABSTRACT These are described compounds of formula(I) Image or an acid addition salt thereof; in which R1, R2, R3 and R4 independently represent hydrogen,C1-4 alkyl, C2-4 alkenyl, halogen, C1-4 haloalkyl, nitro, C1-4 alkoxy,C1-4 haloaDkoxy, C1-4 alkylthio or phenylsulphonyl; in which R5 is a group ofthe formula Image where R7 is hydrogen or C1-6 alkyl is hydrogen or C1-4 alkyl and n is 0 or 1, provided that when R7 is hydrogen n is 0; and in which R6 is attached to the l, 2 or 3-position of the triazole ring and is hydrogen, C1-10 alkyl, C3-7 cycloalkyl, C3-7 cycloalkyl C1-4 alkyl, phenyl, benzyl or acyl. These compounds are pharmaceutically active and are especially useful in the G.1181 -2- treatment of disorders of the central nervous system. They are prepared by reacting an amine of formula R5H with a triazolobenzodiazepine intermediate appropriately substituted at the 10-position or by ring-closing the appropriate anilinotriazole.

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