Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai
Reexamination Certificate
2001-12-11
2008-08-26
Russel, Jeffrey Edwin (Department: 1654)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Peptide containing doai
C530S321000
Reexamination Certificate
active
07417024
ABSTRACT:
Template-fixed β-hairpin peptidomimetics of the general formulae (I), wherein Z is a template-fixed chain of 7 to 11 α-amino acid residues which, depending on their positions in the chain (counted starting from the N-terminal amino acid) are Gly, or Pro, or of certain types which, as the remaining symbols in the above formulae, are defined in the description and the claims, and salts thereof, have the property to inhibit proteases, in particular serine proteases. These β-hairpin peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.
REFERENCES:
patent: WO 01/16161 (2001-03-01), None
Spath et al. Stabilization of a beta-Hairpin in a Cyclic Peptide . . . Helvetica Chimica Acta. 1998, vol. 81, pp. 1726-1738.
Hollosi et al. Ion Binding Properties In Acetonitrile of Cyclopeptides Built Up From Proline And Glycine Residues. International Journal of Peptide and Protein Reserch. 1977, vol. 10, pp. 329-341.
Obrecht et al.; Novel Peptide Mimetic Buliding Blocks and Strategies for Effcient Lead Finding; Advances in Medicinal Chemistry, JAI Press, U.S.; Apr. 1999, pp. 1-68.
Robinson; The Design, Synthesis and Conformation of Some New beta-Hairpin Mimetics: Novel Reagents for Drug and Vaccine Discolvery; Synlett, vol. 1999, No. 4, Apr. 2000, pp. 429-441.
Jiang, et la., Combinatorial Biomimetic Chemistry: Parallel Syntheis of a Small Library of beta-Hairpin Mimetics Based on Loop III from Human Platelet-Derived Growth Factor B; Helvetica Chimica Acta; vol. 83, No. 12, Dec. 2000; pp. 3097-3112.
Pfeifer et al.; Stabilization of beta-hairpin conformations in a protein surface mimetic using a bicycle template derived from (2S,3R, 4R)-diaminoproline; Chem. Commun.; Cmabridge; 1998, vol. 18, pp. 1977-1978.
Spath et al.; Stabilization of a β-Hairpin Comformation in a Cyclic Peptide Using the Templating Effect of a Heterochiral Diproline Unit; Helvetica Chimica Acta, vol. 81, 1998, pp. 1726-1738.
Descours et al.; A New Family of β-Hairpin Mimetics Based on a Tyrpsin Inhibitor fomr Sunflower Seeds; ChemBioChem 2002, 3, pp. 318-323.
Descours Anne
Obrecht Daniel
Robinson John Anthony
Hoffmann & Baron , LLP
Polyphor Ltd.
Russel Jeffrey Edwin
Universität Zürich
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