Use of new and known 3-amino-tetra:hydro-1-benzoxepine derivs. - to control gastrointestinal motility, especially in colon

摘要

The use of benzoxepin derivatives of formula (I) and their acid addition salts is claimed in pharmaceuticals for mammals. R1, R2 = independently H, halogen, OH, alkyl or alkoxy, R3 = H, or 1-5C alkyl which is optionally substituted on a C atom not bound to the N atom by alkoxy, OH, NH2, mono- or di-alkylamino or (when R4 is not H), by OCOR5. R4 = H or 1-5C alkyl, which is substituted on a C atom not bound to the N atom by alkoxy or OH, or R3 and R4 together form 4-5C alkylene. R5 = alkyl or phenyl, which is optionally substituted with halogen or alkoxy. Also claimed are new cpds. of formula (I) where R4 = ethyl, n-propyl, 4-5C alkyl, 1-5C alkyl (substituted on a C atom not bound to the N atom, by lower alkoxy or OH). If R1 and R2 are not H and/or R3 is not H, isopropyl, dimethylamino propyl or diethylaminoethyl, R4 can also be H. If R1 and R2 are not H and/or R3 are not CH3, R4 can also be CH3. If R1 and R2 are not H and/or R3 are not H, R4 can also be isopropyl. 3-pentylamino-2,3,4,5-tetrahydro-1-benzoxepin and its acid addition salts are specifically claimed, as is 3-diphenylamno-2,3,4,5- tetrahydro-1-benzoxepin. Also claimed is the corresponding 4,5-dihydro-1-benzoxepin- 3(2H)-one intermediate for (I). USE/ADVANTAGE - (I) are used to regulate gastrointestinal motlity esp. of the colon. In animal experiments, (I) were found to increase peristaltic wave amplitude in the stomach but to decrease peristalsis in the colon.