Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
2011-06-14
2011-06-14
Balasubramanian, Venkataraman (Department: 1624)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
C514S269000, C544S324000, C544S319000
Reexamination Certificate
active
07960393
ABSTRACT:
The present invention relates to a pyrimidine derivative of the formula (I) and salts thereof which is useful as an active ingredient of pharmaceutical preparations. The pyrimidine derivative of the present invention has excellent CRTH2 (G-protein-coupled chemoattractant receptor, expressed on Th2 cells) antagonistic activity and can be used for the prophylaxis and treatment of diseases associated with CRTH2 activity, in particular for the treatment of allergic diseases, such as asthma, allergic rhinitis, atopic dermatitis, and allergic conjunctivitis; eosinophil-related diseases, such as Churg-Strauss syndrome and sinusitis; basophil-related diseases, such as basophilic leukemia, chronic urticaria and basophilic leukocytosis in human and other mammals; and inflammatory diseases characterized by T lymphocytes and profuse leukocyte infiltrates such as psoriasis, eczema, inflammatory bowel disease, ulcerative colitis, Crohn's disease, COPD (chronic obstructive pulmonary disorder) and arthritis.
REFERENCES:
patent: 7812160 (2010-10-01), Ly et al.
patent: 2007/0129355 (2007-06-01), Ly et al.
patent: 42 39 440 (1993-06-01), None
patent: 1 170 594 (2002-01-01), None
patent: 1 413 306 (2004-04-01), None
patent: 1471057 (2004-10-01), None
patent: 1356834 (1974-06-01), None
patent: 2 262 096 (1992-03-01), None
patent: WO 01/83485 (2001-11-01), None
patent: WO 03/066047 (2003-08-01), None
patent: WO 2004/058164 (2004-07-01), None
patent: WO 2004/096777 (2004-11-01), None
patent: WO 2008/156780 (2008-12-01), None
patent: WO 2008/156781 (2008-12-01), None
Pettipher R., British Journal of Pharmacology, 153, $191-$199, 2008.
Hata et al., Pharmacology & Therapeutics 103, 147-166, 2004.
International Search Report of International Application No. PCT/EP2004/003910 having a Publication No. WO 04/096777.
U.S. Appl. No. 12/665,705, filed Dec. 18, 2009, Tai Wei Ly.
U.S. Appl. No. 12/665,706, filed Dec. 18, 2009, Tai Wei Ly et al.
Sugimoto, H., et al, An Orally Bioavailable Small Molecule Antagonist of CRTH2, Ramatroban (Bay U3405), Inhibits Prostaglandin D2-Induced Eosinophil Migration In Vitro, J. Pharmacology & Experimental Therapeutics, Am. Soc. for Pharmacology and, U.S., vol. 305, No. 1, pp. 347-352 (2003).
Ulven, T., et al, Novel Selective Orally Active CRTH2 Antagonists for Allergic Inflammation Developed from In Silico Derived Hits, J. Med. Chem., 49, pp. 6638-6641 (2006).
Ordukhanyan, A. A., et al, Khimiko-Farmatsevticheskii Zhurnal, 13(9): 36-40 (1979) (English abstract provided).
Ly, T. W., et al, Small-Molecule CRTH2 Antagonists for the Treatment of Allergic Inflammation: An Overview, Expert Opin. Investig. Drugs, 14(7): 769-773 (2005).
Yamamoto et al., “The orally available spleen tyrosine kinase inhibitor 2-[7-(3,4-dimethoxyphenyl)-imidazo [1,2-c] pyrimidin-5-ylamino]-nicotinamide dihydrochloride (Bay 61-3606) blocks antigen-induced airway inflammation in rodents,”J Pharmacol Exp Therapeutics306(3):1174-1181 (2003).
Romagnani, S., “The Th1/Th2 paradigm,”Immunology Today, vol. 18, pp. 263-266 (2001).
Sanz et al., “IL-4-Induced Eosinophil Accumulation in Rat Skin Is Dependent on Endogenous TNF-αand α4 Integrin/VCAM-1 Adhesion Pathways,”J. Immunol., vol. 160, pp. 5637-5634 (1998).
Nagata et al., “CRTH2, an orphan receptor of T-helper-2-cells, is express on basophils and eosinophils and response to mast cell-derived factor(s),”FEBS Lett., vol. 459, pp. 195-199 (1999).
Hirai, H. et al., “Prostaglandin D2 Selectivity Induces Chemotaxis in T Helper Type 2 Cells, Eosinophils, and Basophils via Seven-Transmembrane Receptor CRTH2,”J. Exp. Med., vol. 193, pp. 255-261 (2001).
Leath, T.M. et al.,Drug Discovery Today, vol. 10, pp. 1647-1655 (2005).
Hata, A.N & Breyer, R.M.,Pharmacology&Therapeutics, vol. 103, pp. 147-166 (2004).
Inpharma Weekly, Issue 1236, p. 22, May 6, 2000.
Office Action mailed Dec. 9, 2009 in U.S. Appl. No. 10/554,668.
Notice of Allowance mailed May 25, 2010 in U.S. Appl. No. 10/554,668.
Bacon Kevin
Koriyama Yuji
Ly Tai-wei
Manabe Yoshihisa
Sato Hiroki
Actimis Pharmaceuticals, Inc.
Balasubramanian Venkataraman
Jones Day
LandOfFree
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