Peptides having protected amines of untargeted sites,...

Chemistry: natural resins or derivatives; peptides or proteins; – Peptides of 3 to 100 amino acid residues – Synthesis of peptides

Reexamination Certificate

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C530S333000, C530S334000, C530S339000

Reexamination Certificate

active

07662915

ABSTRACT:
The present invention relates to synthetic peptides having selectively protected amines of untargeted sites and to methods for production thereof and for specifically conjugating PEG to targeted sites of the synthetic peptides using the same. The present invention provides a much higher yield of PEG conjugated peptides in which PEG is specifically combined to amines at targeted sites.

REFERENCES:
patent: 6528485 (2003-03-01), Veronese et al.
patent: 922446 (1999-06-01), None
T. Shi and D.L. Rabenstein. Bioorg. Med. Chem. Letters (2002) 12(16), pp. 2237-2240.
F. Alberecio. Biopolymers (2000) 55, pp. 123-139.
D. Kadereit et al. Chem. Eur. J. (2001) 7(6), pp. 1184-1193.
K. Barlos and M. Gatos. Biopolymers (1999) 51, pp. 266-278.
J. Wilken and S.B.H. Kent. Curr. Opinion Biotech. (1998) 9, pp. 412-426.
Lee et al., “Site-specific PEGylated Peptide Drugs for Enhanced Therapeutic Efficacy,” Presentation, Controlled Release Society 29th Annual Meeting Proceedings, Jul. 20-25, 2002, 2 pps.
Lee et al., “Preparation of Site-specific PEGylated Growth Hormone-Releasing Factor 1-29,” Presentation, American Association of Pharmaceutical Scientists, Annual Meeting, Nov. 11, 2002 (Abstract only) (2 pps.).

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