C - Chemistry – Metallurgy – 07 – K
Patent
C - Chemistry, Metallurgy
07
K
C07K 7/02 (2006.01) A61K 38/08 (2006.01) A61K 38/33 (2006.01) A61K 47/48 (2006.01) C07K 5/083 (2006.01) C07K 5/097 (2006.01) C07K 5/103 (2006.01) C07K 5/117 (2006.01) C07K 7/06 (2006.01) C07K 14/70 (2006.01) A61K 38/00 (2006.01)
Patent
CA 2144773
The invention provides novel peptide derivatives which are designed to deliver pharmacologically active peptides into the central nervous svstem by sequential metabolism. The peptide is placed in a molecular environment which disguises its peptide nature and provides biolabile, lipophilic functions to penetrate the blood-brain barrier by passive transport. The design incorpo- rates a dihydropyridine-type redox targetor moiety, an amino acid or di- or tripeptide spacer inserted between the targetor and N- terminal amino acid unit of the peptide and a bulky, lipophilic substitutent protecting the C-terminal amino acid unit of the pep- tide. The dihydropyridine-type targetor undergoes an enzymatically mediated oxidation to a hydrophilic, membrane-imperme- able pyridinium salt. That polar targetor-peptide conjugate is trapped behind the lipoidal blood-brain barrier. Over time, cleavage of the lipophilic ester from the peptide by esterase and/or lipase enzymes and enzymatic cleavage of the targetor-spacer from the peptide results in release of the desired peptide in the brain.
Na
University Of Florida
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