SUBSTITUTED BENZAMIDE DERIVATIVES,PROCESSES FOR THE PREPARATION THEREOF,AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME

摘要

o-Substd.-N-morpholinyl alkylbenzamide derivs. and analogues of formula (I) and their acid-addn. or quat. ammonium salts and N-oxides are new. R is H, 2-5C alkoxycarbonyl, benzyloxycarbonyl, furyl-, thienyl-, pyridyl- or 1,2-benzisoxazolyl-(1-3C) alkyl, Ph-(3-5C) alkenyl or T-(Y)p-R6; T is single bond or 1-6C alkylene; X is O, S or CO; R6 is Ph opt. substd. by 1-5 halogen, 1-4C alkyl, CF3, 1-4C alkoxy, NO2, CN or NH2 or naphthyl or Ph2CH; p is 0 or 1, but it is 0 when T is single bond; R1 is halogen, OH, 1-12C alkoxy, 3-6C cycloalkoxy, 3-8C alkenyloxy, 3-8C alkynyloxy, 2-6C alk interrupted by 1 or 2 O or CO, 1-4C alkylthio, NH2, mono-substd. NH2 in which the substit. is 1-8C alkyl, Ph-(1-3)alkyl or 3-6C cycloalkyl, 2-6C alkoxy in which a C atom other than in the 1-position is substd. by one OH or NH2 or 1-6C alkoxy substd. by a halogen, CN, 2-5C alkoxycarbonyl, phthalimido, 3-6C cycloalkyl, Ph opt. substd. by one halogen, PhO opt. substd. by one halogen or PhCO opt. substd. by one halogen; R2 is H; R3 is H, halogen, NH2, mono- or di-(1-4C) alkylamino, 2-5C alkanoylamino or NO2; R4 is H, halogen, NO2, SO2NH2, mono- or di-(1-4C)alkylsulphamoyl; or 2 of R1-R4 form 1-3C alkylenedioxy and the other 2 are H; R5 is H or 1-4C alkyl; X is 1-3C alkylene, m, n are 1 or 2. If at least one of R2-R4 is other than H.