[EN] HETEROCYCLIC COMPOUNDS AS BIOGENIC AMINE TRANSPORT MODULATORS<br/>[FR] COMPOSÉS HÉTÉROCYCLIQUES EN TANT QUE MODULATEURS DU TRANSPORT D'AMINES BIOGÈNES
申请人:ANANTHAN SUBRAMANIAM
公开号:WO2016090296A1
公开(公告)日:2016-06-09
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.
本公开涉及抑制生物胺转运体多巴胺转运体(DAT)、5-羟色胺转运体(SERT)和去甲肾上腺素转运体(NET)的某些融合双环杂环生物胺衍生物的化合物。本公开的化合物是多巴胺(DA)、5-羟色胺(5-HT)和去甲肾上腺素(NE)的重摄取的有效抑制剂,具有完全或部分最大效力。在抑制所有三种生物胺的重摄取中具有部分最大效力的化合物在此被称为部分三重摄取抑制剂(PTRIs)。本公开的化合物可用于治疗抑郁症、疼痛、物质滥用、物质滥用复发以及对可卡因、甲基苯丙胺、尼古丁和酒精等物质的成瘾。本摘要旨在作为在特定领域进行搜索的扫描工具,并不意在限制本发明。