申请人:The Upjohn Company
公开号:US04145435A1
公开(公告)日:1979-03-20
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.
式为##STR1##的顺式和反式N-(2-氨基环脂肪族)-2-芳基乙酰胺衍生物化合物,例如N-\x9b2-(N', \n" N'-二甲氨基)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)及其药学上可接受的盐,已发现具有强效的镇痛活性,而优选的化合物除了与吗啡和美沙酮相比仅具有低至中等的明显物理依赖性,作为镇咳剂,它们也将是有用的。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,用于制备用于缓解人和动物的疼痛的药物剂量单位形式,以及使用这些组合物缓解动物和人的疼痛的方法。