| 摘要 |
The present disclosure relates to certain amine derivatives of fused bicyclic heterocycles that inhibit the amine reuptake function of the biogenic amine transporters, dopamine transporter (DAT), serotonin transporter (SERT) and norepinephrine transporter (NET). Compounds of the present disclosure are potent inhibitors of the reuptake of dopamine (DA), serotonin (5-hydroxytryptamine, 5-HT) and norepinephrine (NE) with full or partial maximal efficacy. The compounds with partial maximal efficacy in inhibiting reuptake of all three biogenic amines are herein referred to as partial triple uptake inhibitors (PTRIs). Compounds of the present disclosure are useful for treating depression, pain and substance abuse and relapse to substance abuse and addiction to substances such as cocaine, methamphetamine, nicotine and alcohol. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. |
| 主权项 |
1. A compound represented by the formula (I): wherein: n is 0, 1 or 2; m is 0, 1 or 2; R1 is a heterocycle; R2 is H or lower alkyl group; Ar is a phenyl or heterocyclic group; R3 is H, alkyl, cycloalkyl, heterocycloalkyl, aryl, aralkyl, heteroaryl, or heteroarylalkyl; R4 is H, alkyl, hydroxy, alkoxy, aryloxy, heteroaryloxy, amino, alkylamino or dialkylamino; R3 and R4 together form a carbocycle or heterocycle; R5 is H, halogen, alkyl, aryl, hydroxy, alkoxy, aryloxy, amino, alkylamino or dialkylamino; pharmaceutically acceptable salts thereof, deuterated forms thereof, isomers thereof, solvates thereof, and mixtures thereof. |
