BETA-AMYLOID PEPTIDE INHIBITORS

The present invention relates to compounds which inhibit the binding of meta l ions to a region in the N-terminal loop of the .beta.-amyloid peptide which includes a cluster of histidine residues. In addition, the invention relates to pharmaceutical compositions including these compounds as the acti...

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Bibliographic Details
Main Authors PALLICH, SUSANNE, MCCARTHY, THOMAS DAVID, MATTHEWS, BARRY ROSS, BARNHAM, KEVIN JEFFREY, CHERNY, ROBERT ALAN
Format Patent
LanguageEnglish
French
Published 01.02.2001
Edition7
Subjects
CHEMISTRY
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PEPTIDES
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Summary:The present invention relates to compounds which inhibit the binding of meta l ions to a region in the N-terminal loop of the .beta.-amyloid peptide which includes a cluster of histidine residues. In addition, the invention relates to pharmaceutical compositions including these compounds as the active agent , and to methods of treatment involving the administration of these compounds. The compounds of the invention are useful in the treatment of Alzheimer's disease and other amyloid-related conditions. In a first aspect the present invention provides a compound which interacts with the .beta.-amyloid peptid e in such a way that the N-terminal loop of the peptide (amino acid residues 1 - 15) is blocked or destabilised, thereby inhibiting the binding of one or mor e metal ions to at least one histidine residue within the N-terminal loop. Preferably the compound inhibits binding of Cu2+, Zn2+ and Fe3+ ions, but no t Mg2+ or Ca2+ ions.
Bibliography:Application Number: CA20002379858