发明授权
- 专利标题: Brain-specific drug delivery
- 专利标题(中): 脑特异性药物递送
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申请号: US665940申请日: 1984-10-29
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公开(公告)号: US4824850A公开(公告)日: 1989-04-25
- 发明人: Nicholas S. Bodor
- 申请人: Nicholas S. Bodor
- 申请人地址: FL Gainesville
- 专利权人: University of Florida
- 当前专利权人: University of Florida
- 当前专利权人地址: FL Gainesville
- 优先权: CAX428192 19830516
- 主分类号: A61K38/00
- IPC分类号: A61K38/00 ; C07D209/32 ; C07D211/90 ; C07D213/80 ; C07D213/82 ; C07D401/12 ; C07J43/00 ; C07K14/70 ; A61K31/515 ; A61K31/40 ; A61K31/44 ; A61K31/47
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.revreaction.pyridinium salt redox carrier, with the proviso that when [DHC] is ##STR1## wherein R is lower alkyl or benzyl and [D] is a drug species containing a single NH.sub.2 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 NH.sub.2 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.revreaction.pyridinium salt redox carrier. The corresponding ionic pyridinium salt type drug/carrier entitles [D--QC].sup.+ X.sup.- are also disclosed.
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