公开(公告)号：US20050131051A1

公开(公告)日：2005-06-16

申请号：US10362164

申请日：2001-08-21

Applicant: Shaomeng Wang ,  Sukumar Sakamuri ,  Istvan Enyedey ,  Alan Kozikowski

Inventor： Shaomeng Wang ,  Sukumar Sakamuri ,  Istvan Enyedey ,  Alan Kozikowski

IPC: C07D453/02 ,  A61K31/407 ,  A61K31/439 ,  A61K39/00 ,  A61K47/48 ,  A61P25/00 ,  A61P25/04 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/32 ,  A61P25/36 ,  A61P43/00 ,  C07B57/00 ,  C07D211/52 ,  C07D487/04 ,  C07D491/04

CPC classification number: C07D491/04 ,  C07D211/52 ,  C07D453/02

Abstract: The present invention relates to a class of compounds of formula (I) and (II): wherein R1 is hydrogen; linear or branched C1-C15 alkyl; C1-C15 alkenyl; C3-C6 cycloalkyl; mono, di, tri, tetra, penta substituted aryl or heteroaryl; COOR3; —(CH2)n-aryl; —COO—(CH2)nR3; —(CH2)n—COOR3; —C(O)R3; —C(O)NHR3; or an unsubstituted or substituted oxadiazole; and R2 is hydrogen; linear or branched C1-C15 alkyl; C1-C15 alkenyl; C3-C6 cycloalkyl; mono, di, tri, tetra, penta substituted aryl or heteroaryl; unsubstituted or substituted naphthyl; 1,3-Benzodioxole; fluorene; indole; isoquinoline; quinoline; pyridine; pyrimidine; onnthracene; or —(CH2)n-Ph; wherein the heteroaryl comprises N, O, or S, the mono or multi substituents on the aryl or heteroaryl are independently C1-C5 alkyl, C1-C5 alkenyl, H, F, Cl, Br, I, —NO2, NHR, or —OR, R is C1-C7 alkyl; R3 is C1-C5 alkyl, C1-C5 alkenyl, benzyl, substituted aryl or heteroaryl; and n=1-7. These compounds are discovered, synthesized and confirmed as potent inhibitors of dopamine (DA), serotonin (5-HT), and norepinephrine inhibitors. These compounds are therefore particularly useful in the treatment conditions or diseases wherein modulation of the monoamine neurotransmitter system involving dopamine (DA), serotonin (5-HT), and norepinephrine plays a role.