Polypeptides, derivatives and uses thereof

A polypeptide derivative according to any preceding claim, in which at least one protective group is an acyl group represented by the formula

• 3
• wherein R represents a substituted or unsubstituted straight- or branched-chain alkyl group, a substituted or unsubstituted cycloalkyl group, a substituted or unsubstituted straight or branched-chain aralkyl group or a substituted or unsubstituted aryl group, the groups R being the same or different when both said hydrogen are replaced by acyl groups.

A polypeptide derivative according to any preceding claim, in which X1 is from zero to 20 and/or X2 is from zero to 20.

A compound having the formula

• 4
• in which X1 is a protective group and X2 is H or a protective group.

A compound having the formula

• 5
• in which R represents a substituted or unsubstituted straight- or branched-chain alkyl group, a substituted or unsubstituted cycloalkyl group, a substituted or unsubstituted straight or branched-chain aralkyl group or a substituted or unsubstituted aryl group.

A compound having the formula

• 6

A compound having a formula comprising:

• X1-Arg-Glu-Arg-X2 (II)
• wherein X1 and X2, which may be the same or different, each represents from zero to 32 natural or synthetic amino acid residues or derivatives thereof, and Xaa represents a natural or synthetic amino acid residue or a derivative thereof, provided that the compound is none of the following (as hereinbefore defined):
• APP 296-335, APP 319-335, APP 317-332, APP 321-335, APP 319-332, APP 321-332, APP 321-331, APP 325-335, APP 321-330, APP 327-332, APP 328-332, APP 328-331, APP 328-330, APP 335-319 and APP 316-337.

A compound having a formula comprising:

• X1-Arg-Xaa-Arg-X2 (III)
• wherein X1 and X2, which may be the same or different, each represents from zero to 32 natural or synthetic amino acid residues or derivatives thereof and Xaa represents a natural or synthetic amino acid residue or a derivative thereof, for use in medicine.

Use of a compound having a formula comprising:

• X1-Arg-Xaa-Arg-X2 (III)
• wherein X1 and X2, which may be the same or different, each represents from zero to 32 natural or synthetic amino acid residues or derivatives thereof and Xaa represents a natural or synthetic amino acid residue or a derivative thereof, in the preparation of a medicament for use in the treatment of a neurodegenerative disease or as a cognitive enhancer.

A pharmaceutical composition comprising a compound having a formula comprising:

• X1-Arg-Xaa-Arg-X2 (III)
• wherein X1 and X2, which may be the same or different, each represents from zero to 32 natural or synthetic amino acid residues or derivatives thereof and Xaa represents a natural or synthetic amino acid residue or a derivative thereof, and a pharmaceutically acceptable carrier.

A pharmaceutical composition in which a compound having a formula comprising:

• X1-Arg-xaa-Arg-X2 (III)
• wherein X1 and X2, which may be the same or different, each represents from zero to 32 natural or synthetic amino acid residues or derivatives thereof and Xaa represents a natural or synthetic amino acid residue or a derivative thereof, is chemically or physically linked to a further molecule or vehicle to form a complex for pharmaceutical delivery of said compound.

A compound having any of the following formulae:

• 12 Arg-Glu-Arg (SEQ ID NO 9) Arg-Glu-Arg-Met (SEQ ID NO 10) Met-Arg-Glu-Arg (SEQ ID NO 11) Arg-Glu-Arg-Met-Ser (SEQ ID NO 3) Ser-Met-Arg-Glu-Arg (SEQ ID NO 4)
• for use in medicine.

Use of a compound having any of the following formulae:

• 13 Arg-Glu-Arg (SEQ ID NO 9) Arg-Glu-Arg-Met (SEQ ID NO 10) Met-Arg-Glu-Arg (SEQ ID NO 11) Arg-Glu-Arg-Met-Ser (SEQ ID NO 3) Ser-Met-Arg-Glu-Arg (SEQ ID NO 4)
• in the preparation of a medicament for use in the treatment of a neurodegenerative disease or as a cognitive enhancer.

A pharmaceutical composition comprising a compound having any of the following formulae:

• 14 Arg-Glu-Arg (SEQ ID NO 9) Arg-Glu-Arg-Met (SEQ ID NO 10) Met-Arg-Glu-Arg (SEQ ID NO 11) Arg-Glu-Arg-Met-Ser (SEQ ID NO 3) Ser-Met-Arg-Glu-Arg (SEQ ID NO 4)
• and a pharmaceutically-acceptable carrier.

A pharmaceutical composition in which a compound having any of the following formulae:

• 15 Arg-Glu-Arg (SEQ ID NO 9) Arg-Glu-Arg-Met (SEQ ID NO 10) Met-Arg-Glu-Arg (SEQ ID NO 11) Arg-Glu-Arg-Met-Ser (SEQ ID NO 3) Ser-Met-Arg-Glu-Arg (SEQ ID NO 4)
• is chemically or physically linked to a further molecule or vehicle to form a complex for pharmaceutical delivery of said compound.