申请人:UNIVERSITY OF FLORIDA
公开号:EP0218300A2
公开(公告)日:1987-04-15
The invention provides compounds adapted for the site-specific/sustained delivery of a centrally acting drug species to the brain having the formula [D-DHC] and the non- toxic pharmaceutically acceptable salts thereof, wherein [D] is a centrally acting drug species containing at least one reactive -OH, -COOH, -SH, -NH- or -NH2 functional group and [DHC] is the reduced, biooxidizable, blood-brain barrier penetrating lipoidal form of a dihydropyridine ⇒ pyridinium salt redox carrier comprising a dihydroquinoline or dihydroisoquinoline ring system, a carbon atom of the nitrogen-containing ring portion of said ring system being connected via a bridging group to a reactive -OH, -COOH, -SH, -NH- or -NH2 functional group in the centrally acting drug species. The corresponding quaternary derivatives are also described.
本发明提供了适用于向脑部定点/持续递送具有式[D-DHC]的中枢作用药物种类的化合物及其无毒药学上可接受的盐,其中[D]是含有至少一个活性-OH、-COOH、-SH、-NH-或-NH2官能团的中枢作用药物种类,[DHC]是还原的、可生物氧化的、二氢吡啶⇒吡啶鎓盐氧化还原载体的脂质形式,该载体包含二氢喹啉或二氢异喹啉环系统,所述环系统含氮环部分的碳原子通过桥基与中枢作用药物种类中的活性-OH、-COOH、-SH、-NH-或-NH2 官能团相连。还描述了相应的季衍生物。