发明名称 Brain-specific drug delivery of steroid sex hormones cleaved from pyridinium carboxylates and dihydro-pyridine carboxylate precursors
摘要 The subject compounds, which are adapted for the site-specific/sustained delivery of centrally acting drug species to the brain, are: (a) compounds of the formula [D-DHC](I) wherein [D] is a centrally acting drug species, and [DHC] is the reduced, biooxidizable, blood-brain barrier penetrating lipoidal form of a dihydropyridine-><-pyridinium salt redox carrier, with the proviso that when [DHC] is <IMAGE> wherein R is lower alkyl or benzyl and [D] is a drug species containing a single NH2 or OH functional group, the single OH group when present being a primary or secondary OH group, said drug species being linked directly through said NH2 or OH function group to the carbonyl function of [DHC], then [D] must be other than a sympathetic stimulant, steroid sex hormone or long chain alkanol; and (b) non-toxic pharmaceutically acceptable salts of compounds of formula (I) wherein [D] is a centrally acting drug species and [DHC] is the reduced, biooxidizable, blood-brain barrier penetrating lipoidal form of a dihydropyridine-><-pyridinium salt redox carrier. The corresponding ionic pyridinium salt type drug/carrier entitles [D-QC]+X- are also disclosed.
申请公布号 US4900837(A) 申请公布日期 1990.02.13
申请号 US19870076191 申请日期 1987.07.21
申请人 UNIVERSITY OF FLORIDA 发明人 BODOR, NICHOLAS S.
分类号 A61K38/00;C07D209/32;C07D211/90;C07D213/80;C07D213/82;C07D401/12;C07J43/00;C07K14/70 主分类号 A61K38/00
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