Cyclic peptides as G-protein-coupled receptor antagonists

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

Reexamination Certificate

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C514S009100

Reexamination Certificate

active

07579432

ABSTRACT:
The invention relates to novel cyclic compounds which have the ability to modulate the activity of G protein-coupled receptors. The compounds preferably act as antagonists. In preferred embodiments, the invention provides cyclic peptidic and peptidomimetic antagonists of C5a receptors, which are active against C5a receptors on polymorphonuclear leukocytes and macrophages. The compounds of the invention are both potent and selective, and are useful in the treatment of a variety of inflammatory conditions.

REFERENCES:
patent: 5807824 (1998-09-01), van Oostrum et al.
patent: WO 99/00406 (1999-01-01), None
patent: WO 9900406 (1999-01-01), None
Finch et al., J. Med. Chem., 1999, vol. 42, pp. 1965-1974.
Paczkowski et al., “Pharmacological Characterization of Antagonists of the C5a Receptor,”Brit. J. Pharmacol., 128:1461-1466, 1999.
Strachan et al., “A New Small Molecule C5a Receptor Antagonist Inhibits the Reverse-Passive Arthus Reaction and Endotoxic Shock in Rats,”J. Immunol., 164:6560-6565, 2000.
International Search Report for PCT/AU02/01427, mailed Dec. 20, 2002.
Finch et al., “Low -Molecular-Weight Peptidic and Cyclic Antagonists of the Receptor for the Complement Factor C5a,”J. Med. Chem., 42:1965-1974, 1999.
European Search Report; EP 02771873; Nov. 9, 2005.

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