C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
260/111, 167/179
C07D 211/90 (2006.01) C07D 209/32 (2006.01) C07D 213/80 (2006.01) C07D 213/82 (2006.01) C07D 401/12 (2006.01) C07J 43/00 (2006.01) C07K 14/70 (2006.01) A61K 38/00 (2006.01)
Patent
CA 1253856
Abstract of the Disclosure 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 Image 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 functional group to the carbonyl function of [DHC], then [D] must be other than a sympathetic stimulant, steroid sex hormone, memory enhancer, long chain alkanol or anticancer or antitumor agent; 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, bio- oxidizable, blood-brain barrier penetrating lipoidal form of a dihydropyridine Image pyridinium salt redox carrier. The corresponding ionic pyridinium salt type drug/carrier entities [D-QC]+ are also disclosed, as are derivatives of testicularly acting drug species capable of penetrating the blood-testis barrier.
428192
Ogilvy Renault Llp/s.e.n.c.r.l.,s.r.l.
University Of Florida
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