Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai
Reexamination Certificate
2007-10-30
2007-10-30
Borin, Michael (Department: 1631)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Peptide containing doai
C514S017400, C514S002600, C530S328000, C530S329000
Reexamination Certificate
active
10721774
ABSTRACT:
The invention relates to compounds of formula (I) or (II), which are of interest especially for inhibition of polymerization of amyloid β peptide, as model substances for synthesis of amyloid β peptide-ligands, as tools for the identification of other organic compounds with similar functional properties and/or as ligands for detection of amyloid deposits using e.g., positron emission tomography (PET). Formula (II) is: R1-A′-Y′-Leu-X′-Z′-B′-R2in which X′ means any group or amino acid imparting to the compound according to formula (I) the ability to bind to the KLVFF-sequence in amyloid β peptide, or two amino acids imparting the same ability, but with the proviso that one is not proline; Y′ means any amino acid; Z′ means any non-acidic amino acid; A′ means a direct bond or an α-amino acid bonded at the carboxyl terminal of the α-carboxy group or a di-, tri-, tetra- or pentapeptide bonded at the carboxyl terminal of the α-carboxy group; B′ means a direct bond or an α-amino acid bonded at the α-nitrogen or a di-, tri, tetra- or pentapeptide bonded at the α-nitrogen of the N-terminal α-amino acid; R1is H or —CO—R3bonded at the α-amino group of A′; R2is H, —OR4or NR5R6, all bonded to the α-carboxyl group of the α-carboxyterminal of B′; R3and R4are straight or branched carbon chain of 1-4 carbon atoms; R5and R6are independently H, alkyl, cycloalyl, aryl or substituted aryl or together are —(CH2)n— where n is 4-5; and R1and R2together can form a hydrocarbon ring or heterocyclic ring; all α-amino acids being either D- or L-isomers.
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Näslund Jan
Nordstedt Christer
Terenius Lars
Thyberg Johan
Tjernberg Lars O.
Borin Michael
Clark & Elbing LLP
Neurochem (International) Limited
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