摘要:
The present invention discloses compound of formula (I) or any of its enantiomers or any mixture thereof, a pharmaceutically acceptable addition salt thereof or the N-oxide thereof wherein X and Y together form =O, =S, =NOR , =CR R , =N-CN, =N-NR R , -(CH2)m-, or -W'-(CH2)p-W"-, or one of X and Y is hydrogen and the other is -OR , -SR , or -NR R , Z is hydrogen, -COOR ; R and R are independently hydrogen, halogen, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, alcoxy, aryl, arylalkyl, or -(CH2)q-COOR ; R , R and R are independently hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, aryl, or arylalkyl, -CO-alkyl, or -SO2-alkyl; R and R are independently hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, aryl or arylalkyl; R is alkyl, alkenyl or alkynyl; R is alkyl, alkenyl, alkynyl, aryl, or arylalkyl; where said aryl groups may be substituted one or more times with substituents selected from the group consisting of halogen, CF3, CN, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, amino and nitro; W' and W" are each independently O or S; n is 1, 2, 3 or 4; m is 2, 3, 4 or 5; p is 1, 2, 3, 4, or 5; and q is 0, 1, 2, 3, or 4. The compounds possess valuable properties as monoamine neurotransmitter, i.e dopamine, and serotonine, reuptake inhibitors.
摘要(中):
本发明公开了式(I)化合物或其任何对映体或其任何混合物,其药学上可接受的加成盐或其N-氧化物,其中X和Y一起形成= O,= S,= NOR 2, = CR 3 R 4,= N-CN,= N-NR 7 R 8, - (CH 2)m - 或-W' - (CH 2)p W“ 并且Y是氢,另一个是-OR 5,-SR 5或-NR 5 R 6,Z是氢,-COOR 9; R 3和R 4, 独立地是氢,卤素,烷基,环烷基,环烷基烷基,烯基,炔基,烷氧基,芳基,芳基烷基或 - (CH 2)q -COOR 2; R 2,R 5和R 6独立地是 氢,烷基,环烷基,环烷基烷基,烯基,炔基,芳基或芳烷基,-CO-烷基或-SO2-烷基; R 7和R 8独立地为氢,烷基,环烷基,环烷基烷基,烯基,炔基 ,芳基或芳基烷基; R 9是烷基,烯基或炔基; R 1是烷基,烯基,炔基,芳基或芳烷基;其中所述芳基可以被取代基选自以下基团: 卤素,CF 3,CN,烷氧基,环烷氧基,烷基,环烷基,烯基,炔基,氨基和硝基的取代基; W'和W“各自独立地为O或S; n为1,2,3或4; m为2,3,4或5; p为1,2,3,4或5; q为0, 该化合物具有作为单胺神经递质(即多巴胺和5-羟色胺)再摄取抑制剂的有价值的性质。