Benzodiazepine compounds and their use as pharmaceuticals

C - Chemistry – Metallurgy – 07 – D

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260/239.5

C07D 487/04 (2006.01) C07D 231/38 (2006.01)

Patent

CA 1159056

ABSTRACT Compounds are described of the formula Image or an acid addition salt thereof; in which R1, R2, R3 and R4 independently represent hydrogen, C1-4 alkyl, C2-4 alkenyl, C3-7 cycloalkyl, C3-7 cycloalkyl C1-4 alkyl, halogen, C1-4 haloalkyl, C1-4 alkanoyl, nitro, amino, C2-4 acylamino, cyano, hydroxyl, C1-4 alkoxy, C1-4 alkylthio, C1-4 haloalkoxy or a group of the formula -SO2N(R8)2, -SO2R8, or -SO3R8 where R8 is C1-4 alkyl, C1-4 haloalkyl or optionally substituted phenyl; in which R5 is a group of the formula Image where R9 is hydrogen,C1-4 alkyl, C3-7 cycloalkyl, C3-7 cycloalkyl C1-4 alkyl, C1-4 haloalkyl, C2-4 alkenyl, C1-4 alkanoyl, benzyl, cyano or optionally substituted phenyl, where R10 is hydrogen, C1-4 alkyl or optionally substituted phenyl and where n is 0 or l; in which R6 is hydrogen, C1-10 alkyl, C3-7 cycloalkyl, C3-7 cycloalkyl C1-4 alkyl, C1-4 haloalkyl, benzyl, C1-6 alkanoyl, C1-4 carbalkoxy or benzoyl; and in which R7 is one of the values of R6 or halogen, nitro, cyano, amino or C1-4 acylamino. The compounds have neuroleptic, sedative, relaxant, anxiolytic or anti-emetic properties, while at the same tine have low toxicity, and thus are useful in the treatment of disorders of the central nervous system.

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