申请人:Abbott Laboratories
公开号:US05128362A1
公开(公告)日:1992-07-07
The present invention provides compounds of the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein R.sub.1 is selected from hydrogen, halo, lower alkyl, lower alkoxy, or thioalkoxy; and R.sub.2 is lower alkoxy; or R.sub.1 and R.sub.2 together form a methylenedioxy or ethylenedioxy ring; R.sub.3 and R.sub.4 are independently selected from hydrogen, hydroxy, lower alkyl, lower alkoxy, lower alkylthio, (lower alkyl)amino, (lower alkylsulfonyl)amino, and halo; and R.sub.7 is selected from the group consisting of 2- or 3-thienyl, 2- or 3-furyl, and ##STR2## where R.sub.13 and R.sub.14 are independently selected from the group consisting of hydrogen, hydroxy, halogen, amino, lower alkyl, lower alkoxy, lower alkylthio, methylenedioxy, or ethylenedioxy. The compounds of the present invention selectively inhibit .alpha..sub.2 -adrenergic receptors as well as inhibit the uptake of biogenic amines and are thus useful in the treatment of certain cardiovascular and psychiatric disorders.
本发明提供了以下结构的化合物##STR1##或其药学上可接受的盐,其中R.sub.1从氢、卤素、较低的烷基、较低的烷氧基或硫代烷氧基中选择;而R.sub.2是较低的烷氧基;或者R.sub.1和R.sub.2一起形成一个亚甲二氧基或乙二氧基环;R.sub.3和R.sub.4独立地从氢、羟基、较低的烷基、较低的烷氧基、较低的烷硫基、(较低的烷基)氨基、(较低的烷基磺酰基)氨基和卤素中选择;而R.sub.7从2-或3-噻吩基、2-或3-呋喃基和##STR2##中选择,其中R.sub.13和R.sub.14独立地从氢、羟基、卤素、氨基、较低的烷基、较低的烷氧基、较低的烷硫基、亚甲二氧基或乙二氧基中选择。本发明的化合物选择性地抑制α2-肾上腺素受体,并抑制生物胺的摄取,因此在治疗某些心血管和精神疾病方面具有用处。