申请人:A. H. Robins Company, Incorporated
公开号:US03963745A1
公开(公告)日:1976-06-15
A method is disclosed for controlling emesis utilizing N-(1-substituted-3-pyrrolidinyl)benzamides and thiobenzamides of the formula: ##SPC1## Wherein R is cycloalkyl, phenyl and phenyllower-alkyl; R.sup.1 is hydrogen, lower alkyl of 1 to 8 carbon atoms and phenyl; R.sup.2 is halogen, lower-alkyl, lower-alkoxy, amino, nitro, monoalkylamino, dialkylamino, mercaptomethyl, acetamido, sulfamoyl, cyano, hydroxy, benzyloxy, and trifluoromethyl; X is oxygen and sulfur; n is an integer from zero to three inclusive and pharmaceutically acceptable acid addition salts thereof. The benzamide compounds wherein R is cyclohexyl and R.sup.1 is lower-alkyl are particularly effective as antiemetics and have minimal side effects.
本发明公开了一种利用N-(1-取代的-3-吡咯烷基)苯甲酰胺和硫代苯甲酰胺控制呕吐的方法,其化学式为:##SPC1##,其中R为环烷基、苯基和苯基低级烷基;R1为氢、1至8个碳原子的低级烷基和苯基;R2为卤素、低级烷基、低级烷氧基、氨基、硝基、单烷基氨基、二烷基氨基、巯基甲基、乙酰氨基、磺酰氨基、氰基、羟基、苄氧基和三氟甲基;X为氧和硫;n为0至3的整数,以及其药学上可接受的酸加成盐。当R为环己基,R1为低级烷基时,这些苯甲酰胺化合物作为止吐剂特别有效,且副作用最小。