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substituerade benzamidderivat, foerfarande foer deras framstaellning och (innehaollande farmaceutiska blandningar.

机译:取代的苯甲酰胺衍生物,其制备方法和(包含药物混合物)。

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.
机译:邻-取代-N-吗啉基烷基苯甲酰胺衍生物。和式(I)的类似物及其酸加成基。或铵盐和N-氧化物是新的。 R为H,2-5C烷氧羰基,苄氧羰基,呋喃基,噻吩基,吡啶基或1,2-苯并恶唑基-(1-3C)烷基,Ph-(3-5C)烯基或T-(Y)p-R6 ; T是单键或1-6C亚烷基; X为O,S或CO; R6是Ph opt。取代1-5个卤素,1-4C烷基,CF 3,1-4C烷氧基,NO 2,CN或NH 2或萘基或Ph 2 CH。 p为0或1,但当T为单键时为0。 R 1是卤素,OH,1-12C烷氧基,3-6C环烷氧基,3-8C烯氧基,3-8C炔氧基,被1或2 O或CO中断的2-6C烷,1-4C烷硫基,NH 2单取代。 NH2在其中替代。取代基是在1位以外的碳原子被取代的1-8C烷基,Ph-(1-3)烷基或3-6C环烷基,2-6C烷氧基。由一种OH或NH 2或1-6C烷氧基取代。由卤素,CN,2-5C烷氧羰基,邻苯二甲酰亚胺基,3-6C环烷基,Ph opt。取代由一个卤素,PhO选择。取代由一种卤素或PhCO选择。取代一卤素R2为H; R3是H,卤素,NH2,单或二(1-4C)烷基氨基,2-5C烷酰基氨基或NO2; R4为H,卤素,NO2,SO2NH2,单或二(1-4C)烷基磺酰基; R1-R4中的2个为1-3C亚烷基二氧基,另外2个为H; R5是H或1-4C烷基; X为1-3C亚烷基,m,n为1或2。如果R 2 -R 4中的至少一个不是H。

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