1-benzoxepin-5(2h)-one derivatives, salts, intermediate...

C - Chemistry – Metallurgy – 07 – D

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260/355.5, 260/3

C07D 313/08 (2006.01) C07D 405/04 (2006.01)

Patent

CA 1162553

ABSTRACT OF THE DISCLOSURE Novel, 3-amino-1-benzoxepin-5(2H)-one derivatives and methods for their production are disclosed. These deri- vatives 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 terminal 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 NR5R6; R5 and R6 independently of one another are hydrogen or C1-C5 alkyl; or R5 and R6 are together a 5 to 7 member ring, or R5 and R6 are together a 5 to 7 member ring having heterogeneous oxygen, sulfur or nitrogen; R1 and R2 are together a 5 to 7 member ring or R1 and R2 are together a 5 to 7 member ring having heterogeneous oxygen, sulfur or NR7; R7 is hydrogen, methyl, benzyl or phenyl; R3 and R4 independently of one another are hydrogen, halogen, C1-C4 alkyl, C1-C4 alkoxy or C1-C4 alkylthio; or one of R3 and R4 is trifluoromethyl or nitro and the other is hydrogen; and the pharmaceutically acceptable acid addition salts there- of. These compounds have a favourable effect on the treatment of spasms of the stomach-intestinal tract and, therefore, constitute the active ingredient of pharmaceutical compo- sitions and methods for the treatment of disorders of the stomach and intestinal tract. Pocesses for the preparation of the derivatives and their acid additions salts and inter- mediate products for their preparation are also described.

357544

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