3-amino-1-benzoxepin derivatives, their salts and...

C - Chemistry – Metallurgy – 07 – D

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260/390, 260/355

C07D 313/08 (2006.01) C07D 405/12 (2006.01) C07D 413/12 (2006.01)

Patent

CA 1161857

ABSTRACT OF THE DISCLOSURE Novel 3-amino-1-benzoxepine derivatives and methods for their production are disclosed. These derivatives correspond to the Formula I Image I wherein: R1 and R2 independently of one another are hydrogen, C1-C5 alkyl, C1-C5 alkyl substituted with a term- inal phenyl, or a phenyl containing one or two halogens, methyl or methoxy groups, a 3,4-methylenedioxy or a 3,4- ethylenedioxy group, C2-C5 alkyl substituted with terminal hydroxy or methoxy or, C3-C4 alkenyl; or one of R1 and R2 are hydrogen or a C1-C5 alkyl and the other is a C2-C5 alkyl substituted with a terminal NR7R8; R7 and R8 independently of one another are hydrogen or C1-C5 alkyl; or R7 and R8 are together a 5 to 7 member ring or said ring having heterogeneous oxygen, sulfur or nitrogen, or R1 and R2 are together a 5 to 7 member ring or said ring having heterogeneous oxygen, sulfur or NR9; R9 is hydrogen, methyl, benzyl, or phenyl; one of R3 and R4 is hydrogen and the other hydroxy, or R3 and R4 together are oxygen; R5 and R6 independently of one another are hydrogen, halogen, C1-C4 alkyl, C1-C4 alkoxy or C1-C4 alkylthio; or one of R5 and R6 is trifluoromethyl or nitro and the other is hydrogen; the stereo isomers and the pharmaceutically acceptable acid addition salts thereof. These compounds have a favourable effect upon the motility of the gastro-intestinal tract and, therefore, constitute the active ingredient of pharma- ceutical compositions and methods for the treatment of motility disorders.

357545

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