http://rdf.ncbi.nlm.nih.gov/pubchem/patent/EP-0110955-B1

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filingDate 1983-05-12^^<http://www.w3.org/2001/XMLSchema#date>
grantDate 1995-08-23^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_c7aac89d703d61ee5be2780f60072363
publicationDate 1995-08-23^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber EP-0110955-B1
titleOfInvention Brain-specific drug delivery
abstract Dihydropyridine deriv.-drug cpds. of formula D'-DHC (I) and their salts are new, (D' is a centrally or testicularly acting drug species; and DHC is the reduced bio-oxidisable blood-brain barrier penetrating lipoidal form of a dihydropyridine in equilibrium with a pyridinium salt redox carrier. Provided that when DHC is 1-R-1,4-dihydro-3-pyridinylcarbonyl (R is lower alkyl or benzyl) and D' is a drug species contg. a single NH2 or OH gp. (as a p- or s-OH) linked directly through the NH2 or OH to the carbonyl function of DHC, then D' is not a sympathetic stimulant, steroid sex hormone, memory enhancer, long chain alkanol or anticancer or antitumour agent). (I) give site specific and sustained delivery of the centrally acting drug to the brain. They readily and easily penetrate the blood-brain barrier so that increased concns. are present in the brain; oxidn. of the dihydropyridine carrier in vivo to an ionic pyridinium salt prevents its elimination from the brain, while elimination from the general circulatory system is accelerated. This action ensures prolonged brain-specific action, while any systemic toxic effects are decreased and central toxicity is reduced. Site specific and sustained delivery to the testes is also achieved, esp. with drugs that cannot themselves penetrate the blood-testis barrier; they are useful for male contraception, improving sexual function esp. in veterinary use, etc.
priorityDate 1982-05-18^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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