Cis- and trans-N-(2-aminocycloaliphatic)-2-arylacetamide derivative compounds of the formula ##STR1## e.g., N-\x9b2-(N', \n" N'-dimethylamino)cyclohexyl!-N-methyl-2-(4-bromophenyl)acetamide and trans-N-methyl-N-\x9b2-(1-pyrrolidinyl)cyclohexyl!acetamide, \n' 2-(3,4-dichlorophenyl) and their pharmaceutically acceptable salts, have been found to have potent analgesic activity, and the preferred compounds have in addition only low to moderate apparent physical dependence liability, compared to morphine and methadone. As analgesics they would be useful also as antitussives. Processes for preparation of these compounds are also disclosed. This invention also includes compositions containing these compounds useful in pharmaceutical dosage unit form for alleviating pain in humans and animals, as well as methods for alleviating pain in animals and humans with these compositions.
式子为##STR1##的顺式和反式N-(2-
氨基环脂肪基)-2-芳基乙酰胺衍
生物化合物,例如N-\x9b2-(N',\n" N'-二甲基
氨基)环己基!-N-甲基-2-(4-
溴苯基)乙酰胺和反式N-甲基-N-\x9b2-(1-
吡咯烷基)环己基!乙酰胺,2-(3,4-二
氯苯基)及其药物可接受的盐,已发现具有强效镇痛活性,并且与
吗啡和
美沙酮相比,优选化合物仅具有低至中度的明显身体依赖性。作为镇痛剂,它们也可以作为止咳剂使用。还公开了制备这些化合物的方法。本发明还包括含有这些化合物的组合物,其以制药剂量形式对于缓解人和动物的疼痛有用,以及使用这些组合物缓解动物和人的疼痛的方法。