申请人:American Home Products Corporation
公开号:US05962465A1
公开(公告)日:1999-10-05
The compounds of formula I: ##STR1## wherein R.sup.1 and R.sup.2 are, independently, hydrogen, alkyl, phenyl or benzyl; or R.sup.1 and R.sup.2, taken together, are benzylidene optionally substituted with R.sup.3 as defined below or alkylidene, or R.sup.1 and R.sup.2, taken together with the carbon to which they are attached, form a carbonyl moiety or a cycloalkyl group; R.sup.3 is hydrogen, hydroxy, halo, trifluoromethyl, trifluoromethoxy, alkyl, alkoxy, aralkoxy, alkanoyloxy, amino, mono- or di-alkylamino, alkanamido or alkanesulfonamido; R.sup.4 is hydrogen or alkyl; m is an integer 0, 1 or 2; n is an integer from 0 to 6, inclusive; Z is hydrogen, hydroxy, alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, polycyclo-alkyl, phenyl optionally substituted with R.sup.3 as defined above, phenoxy optionally substituted with R.sup.3 as defined above, naphthyl optionally substituted with R.sup.3 as defined above or naphthyloxy optionally substituted with R.sup.3 as defined above, heteroaryl or heteroaryloxy, in which the heterocyclic ring of the heteroaryl or heteroaryloxy group is selected from thiophene, furan, pyridine, pyrazine, pyrimidine, indole, indazole, imidazole, chroman, coumarin, carbostyril, quinoline, benzisoxazole, benzoxazole, pyrazole, pyrrole, thiazole, oxazole, or isoxazole and the heterocyclic ring is optionally substituted by R.sup.3 as defined above; or a pharmaceutically acceptable salt thereof, are useful in treating disorders of the dopaminergic system.
化学式为I的化合物:##STR1##
其中R.sup.1和R.sup.2分别为氢、烷基、苯基或苄基;或R.sup.1和R.sup.2连在一起,是苄基亚甲基,可选地用下面定义的R.sup.3取代,或烷基亚甲基,或R.sup.1和R.sup.2与它们连接的碳形成羰基基团或环烷基;R.sup.3为氢、羟基、卤素、三
氟甲基、三
氟甲氧基、烷基、烷氧基、芳基氧基、烷酰氧基、
氨基、单烷基或二烷基
氨基、烷基酰胺或烷基磺酰胺;R.sup.4为氢或烷基;m为0、1或2的整数;n为0到6的整数,包括0和6;Z为氢、羟基、烷基、烯基、炔基、烷氧基、环烷基、多环环烷基、苯基(可选地用上述定义的R.sup.3取代)、苯氧基(可选地用上述定义的R.sup.3取代)、
萘基(可选地用上述定义的R.sup.3取代)或
萘氧基(可选地用上述定义的R.sup.3取代)、杂环芳基或杂环芳基氧基,其中杂环芳基或杂环芳基氧基的杂环环选自
噻吩、
呋喃、
吡啶、
吡嗪、
嘧啶、
吲哚、
吲唑、
咪唑、色
甘醇、
香豆素、
喹啉、苯并
异噁唑、苯并
噁唑、
吡唑、
吡咯、
噻唑、
噁唑或
异噁唑,且杂环环可选地由上述定义的R.sup.3取代;或其药学上可接受的盐,适用于治疗
多巴胺系统疾病。