The Open University

Radmila Mileusnic

Steven Peter Russell Rose

The invention provides a compound having formula X-Arg-Xaa-Arg-Xin which Xand Xare up to 30 amino acid residues and Xaa is an amino acid residue. A preferred compound is the tripeptide Arg-Glu-Arg which corresponds to amino acid residues 328 to 330 of human amyloid precursor protein. The invention further provides a derivative of a polypeptide having the formula: X-Arg-Xaa-Arg-Xwherein Xand X, which may be the same or different, each represents from zero to 30 natural or synthetic amino acid residues or derivatives thereof and Xaa represents a natural or synthetic amino acid residue or derivative thereof, at least one functional group of at least one said amino acid residue or derivative thereof being protected by a protective group. The compounds of the invention are believed to be useful in the treatment of Alzheimer's disease and as cognitive enhancers.

Polypeptides, derivatives and uses thereof

The invention provides compounds having formulae comprisingX-Ser-Met-Arg-Glu-Arg-Xin which Xand Xare up to 30 amino acid residues and the formula represents a reverse-order sequence corresponding to amino acid residues 332 to 328 of human APP and from zero to 30 successive amino acid residues of human APP extending in each direction therefrom, The invention also provides the pentapeptide Ser-Met-Arg-Glu-Arg, corresponding to residues 332 to 328 of human amyloid precursor protein in reverse order, and the tripeptide Arg-Glu-Arg which corresponds residues 328 to 330 of human amyloid precursor protein, the tripeptide and pentapeptide being provided as pharmaceutical compositions. The invention further provides conjugates of the foregoing compounds which can cross the blood-brain barrier and pharmaceutical compositions containing such conjugates. The compounds and compositions of the invention are believed to be useful in the treatment of Alzheimer's disease and as cognitive enhancers and appropriate methods of medical treatment are disclosed.

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Milton Keynes, United Kingdom

Radmila Mileusnic