PAR-2 agonist

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

Reexamination Certificate

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C514S001100, C530S330000

Reexamination Certificate

active

07910556

ABSTRACT:
A compound, or a salt or solvate thereof having a structure of Ar—CO-AA1-AA2-AA3-AA4-NH—X—NR1R2is disclosed. Ar represents an optionally substituted phenyl group or an aromatic heterocyclic group; AA1represents a hydrophobic amino acid; AA2represents an unsubstituted amino acid containing 2 or more carbon atoms; AA3represents an unsubstituted amino acid containing 2 or more carbon atoms; AA4represents a hydrophobic amino acid; X represents a divalent saturated aliphatic hydrocarbon group having 2-6 carbon atoms; and R1and R2represent a saturated or unsubstituted aliphatic hydrocarbon group having 1-8 carbon atoms, or alternatively R1and R2may form a ring together with an adjacent nitrogen atom. A pharmaceutical composition for prevention/treatment of diseases associated with PAR-2 is also disclosed. The pharmaceutical composition includes the above compound, a salt or a solvate thereof and a pharmaceutically acceptable carrier.

REFERENCES:
patent: 5763575 (1998-06-01), Sundelin et al.
patent: 5874400 (1999-02-01), Sundelin et al.
patent: 5888529 (1999-03-01), Bunnett et al.
patent: 5958407 (1999-09-01), Bunnett et al.
patent: 7056942 (2006-06-01), Hildesheim et al.
patent: 2003/0166553 (2003-09-01), Araki et al.
patent: 2003/0203849 (2003-10-01), Araki et al.
patent: 2004/0077612 (2004-04-01), Mercep et al.
patent: 2005/0222384 (2005-10-01), Ramage et al.
patent: 2006/0019904 (2006-01-01), Araki et al.
patent: 2001-64203 (2001-03-01), None
patent: 2001-181208 (2001-07-01), None
patent: 2001-233790 (2001-08-01), None
patent: WO 96/23225 (1996-08-01), None
patent: 01-47556 (2001-07-01), None
patent: 01-62291 (2001-08-01), None
patent: 03-104268 (2003-12-01), None
patent: WO 2006/104190 (2006-10-01), None
Vippagunta SR, Brittain HG, Grant DJW, “Crystalline solids,” Advanced Drug Delivery Reviews, 2001, 48: 3-26.
John J. McGuirre et al.; “2-Furoyl-LIGRLO-amide: A Potent and Selective Proteinase-Activated Receptor 2 Agonist”, The Journal of Pharmacology and Experimental Therapeutics, vol. 309, No. 3, Jun. 2004, pp. 1124-1131. Cited in the ISR.
Hashem N. Alshurafa et al.; “A protease activated receptor-2 (PAR-2) activating peptide, tc-LIGRLO-NH2, induces protease relase from mast-cells: role in TNF degradation”, BMC Pharmacology, vol. 4, No. 12, Jul. 2004, pp. 1-9. Cited in the ISR.
Graeme S. Cottrell et al.; “Trypsin IV, a Novel Agonist of Protease-activated Receptors 2 and 4”, The Journal of Biological Chemistry, vol. 279, No. 14, Apr. 2004, pp. 13532 to 13539. Cited in the ISR.
International Search Report of PCT/JP2005/023852, date of mailing Mar. 28, 2006.
Santagada, V. et al.: Minimal Strcuctural Requirements for Agonist Activity of PAR-2 Activating Peptides; Bioorg. Med. Chem. Lett. 12; pp. 21-24, 2002.
Nystedt, S. et al.; Molecular Cloning of a Potential Proteinase Activated Receptor; Proceeding of the National Academy of Sciences USA, 91: pp. 9208-9212, 1994.
Macfarlane, Scott R.. et al.; Proteinase-Activated Receptors; Pharmacological Reviews, 53; pp. 245-282, 2001.
Roy, Samir S.; Dual endothelium-dependent vascular activities of proteinase-activated receptor-2-activating peptides: evidence for receptor heterogeneity; Br J Pharmacol, 123; 1434-1440, 1998.
Kawabata, A. et al.; Increased vascular permeability by a specific agonist of protease-activated receptor-2 in rat hindpaw; Br J Pharmacol, 125; 419-422,1998.
Al-ani, B. et al.; Proteinase-Activated Receptor 2 (PAR2): Development of a Ligand-Binding Assay Correlating with Activation of PAR2by Par1- and PAR2- Derived Peptide Ligands1; The Journal of Pharamacology and Experimental Therapeutics, vol. 290; pp. 753-760, 1999.
Hollenberg, Morley D. et. al.; Proteinase-Activated Receptor-2 in Rat Aorta: Structural Requirements for Agonist Activity of Receptor-Activating Peptides; Molecular Pharmacology, 49, 229-233, 1996.
Translation of International Preliminary Report on Patentability mailed Jul. 12, 2007 of International Application No. PCT/JP2005/023852.
European Search Report dated Jun. 17, 2009 issued in corresponding European Application No. 06730381.8.
Hollenberg M. D. et al., “Proteinase-Activated Receptors: Structural Requirements for Activity, Receptor Cross-Reactivity, and Receptor Selectivity of Receptor-Activating Peptides”, Canadian Journal of Physiology and Pharmacology, 1997, pp. 832-841, vol. 75, abstract only.
European Search Report dated Jul. 6, 2009 issued in corresponding European Application No. 5822433.8.
Hollenberg, M. D. et al., “Proteinase-Activated Receptors: Structural Requirements for Activity, Receptor Cross-Reactivity, and Receptor Selectivity of Receptor-Activating Peptides”, Canadian Journal of Physiology and Pharmacology, Jul. 1997, pp. 832-841, vol. 75.
Lashuel, H. A. et al., “Protofilaments, Filaments, Ribbons, and Fibrils from Peptidomimetic Self-Assembly: Implication for Amyloid Fibril Formation and Materials Science”, Journal of The American Chemical Society, May 19, 2000, pp. 5262-5277, vol. 122, American Chemical Society.
Toru Sugaya et al.(Toru Kanke) ; “Characterization of Potent Protease-Activated Receptor-2 (PAR-2) Activating Peptide, 2-furoyl-LIGRL-NH2” Nov. 2004, p. 116, Dai 12 Kai The Pharmaceutical Society of Japan Iyakuhin Kagakubukai Nenkai.

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