Template fixed beta-hairpin loop mimetics and their use in...

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai

Reexamination Certificate

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C514S021100

Reexamination Certificate

active

07994118

ABSTRACT:
Template-fixed β-hairpin mimetics and libraries including a plurality of these mimetics are provided. The template-fixed β-hairpin mimetics are of the following general formula:in-line-formulae description="In-line Formulae" end="lead"?R1-Cys-Z-Cys-R2  (I)in-line-formulae description="In-line Formulae" end="tail"?wherein the two cysteine residues are bridged by a disulfide bond, thereby forming a cyclic peptide; R1and R2are di- or tripeptide moieties of certain types, as defined herein; and Z is a chain of n amino acid residues with n being an integer from 4 to 20 and with each of these n amino acid residues being, independently, derived from any naturally occurring L-α-amino acid.

REFERENCES:
patent: WO 0062815 (2000-10-01), None
patent: WO 00/77194 (2000-12-01), None
patent: WO 03/054000 (2003-07-01), None
N.C Wrighton et al. Science (1996) 273(5274), pp. 458-463.
Wrighton et al.; Small Peptides as Potent Mimetics of the Protein Hormone Erythropoietin; Science; vol. 273, pp. 458-463, Jul. 26, 1996.
Dimarcq et al.; Cystein-Rich Antimicrobial Peptides in Invertebrates; Biopolymers (Peptide Science), vol. 47, pp. 465-477; 1998.
Skelton et al.; Amino Acid Determinants of β-Hairpin conformation in Erythropoeitin Receptor Agonist Peptides Derived from a Phage Display Library; J. Mol. Biol.; vol. 316, pp. 1111-1125; 2002.
Lowman; Bacteriophage Display and Discovery of Peptide Leads for Drug Development; Annu. Rev. Biomol. Struct. 1997; vol. 26, pp. 401-424; 1997.
Shankaramma et al.; Macrocyclic Hairpin Mimetics of the Cationic Antimicrobial Peptide Protegrin I: A New Family of Broad-Spectrum Antibiotics; ChemBioChem; vol. 3, pp. 1126-1133; 2002.

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