Substituted benzazepines, their preparation and...

C - Chemistry – Metallurgy – 07 – D

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C07D 223/16 (2006.01) A61K 31/55 (2006.01) C07D 223/32 (2006.01) C07D 401/04 (2006.01) C07D 403/04 (2006.01) C07D 521/00 (2006.01)

Patent

CA 1321195

ABSTRACT OF THE DISCLOSURE Disclosed herein are novel 1-substituted- 2,3,4,5-tetrahydro-1?-3-benzazepines of the general formula I: Image I wherein R1, R2, R3, R4 and R5 are specified substituents. R1 is preferably -X6, -CHR7R8, cycloalkyl, cycloalkenyl, Image or pyrrolyl where m is 1, R6 represents =H, phenyl, substituted phenyl, aralkyl, alkyl, cycloalkyl, haloalkyl or alkoxyalkyl, R7 represents H or alkyl preferably H, R8 represents cycloalkyl, cycloalkenyl, haloalkyl, alkoxyalkyl, alkenyl or alkynyl and R9 represents alkyl, alkoxy or alkoxyalkyl. R2 preferably represents -H and R3 -CH3, R4 is preferably halogen and R5 is preferably OH, OCO?R9 or -O(CR7)2-?OCO?-R13 where R7 represents hydrogen, R9 is as defined above and R13 represents alkyl. The compounds of the formula I are indicated as being useful in the treatment of psychoses, depression and pain. Also disclosed are process for the preparation of the novel compounds as well as pharmaceutical compositions comprising them.

562352

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