2,5-substituted pyrimidine derivatives-CCR-3 receptor...

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

Reexamination Certificate

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C514S274000, C514S275000, C544S316000, C544S332000, C544S335000

Reexamination Certificate

active

06984643

ABSTRACT:
Compounds of Formula (I):wherein Ar1is aryl; Ar2is hydrogen, cycloalkyl, aryl or heteroaryl; Z is —C(═O) or a single bond; R1, R2, R3, R4and R5are independently hydrogen or alkyl optionally substituted with hydroxy; alk is an alkylene chain of one to six carbon atoms; X is —O—, —NRh(where Rhis hydrogen or alkyl), (CR6R7)m(where R6and R7are independently in each occurrence hydrogen or alkyl and m is an integer from 0 to 3), or —S(O)n(wherein n is an integer from 0 to 2); or prodrugs thereof, and pharmaceutically acceptable salts thereof,are inhibitors of CCR3 useful for treating eosinophil induced diseases such as asthma.

REFERENCES:
patent: 4716166 (1987-12-01), Abou-Gharbia et al.
patent: 0 640 599 (1994-08-01), None
patent: 1 201 239 (2002-05-01), None
patent: 2 343 893 (2000-05-01), None
patent: WO 97/36875 (1997-10-01), None
patent: WO 97/36901 (1997-10-01), None
patent: WO 00/31032 (2000-06-01), None
patent: WO 00/73278 (2000-12-01), None
patent: WO 01/00617 (2001-01-01), None
Barnes, Peter J., Ann. Rev. Pharmacol. Toxicol., 2002, 42, 81-98.
Stella, Valentino J, Expert. Opin. Ther. Patents, 14, 2004, 277-280.
Wolff, Manfred E. “Buger's Medicinal Chemistry, 5ed, Part 1”, John Wiley & Sons, 1995, pp. 975-977.
Banker, G.S. et al, “Modern Pharmaceutics, 3ed.”, Marcel Dekker, New York, 1996, pp. 451 and 596.
West, Anthony R., Solid State Chemistry and its Applications, Wiley, New York, 1988, pp. 358 & 365.
Barnes PJ., Annu Rev Pharmacol Toxicol. 2002;42:81-98, Medline abstract PMID: 11807165.
Owen C., Pulm Pharmacol Ther. 2001;14(3):193-202., abstract only.
Lloyd CM, Rankin SM., Curr Opin Pharmacol. Aug. 2003;3(4):443-8. abstract only.
Naya, Akira et al., Discovery of a Novel CCR3 Selective Antagonist,Bioorganic & Medicinal Chemistry Letters, 2001, pp. 1219-1223, vol. 11, No. 9, Pergamon, Elsevier Science Lld.
Banwell, M.E. et al., “Regulation of Human Eotaxin-3/CCL26 Expression: Modulation by Cytokines and Glucocorticoids”,Cytokine, (2002) 17(6):317-323.
Barnes, P.J., “Cytokine-directed therapies for the treatment of chronic airway diseases”,Cytokine&Growth Factor Reviews(2003) 14:511-522.
Ettmayer, P., et al., “Lessons Learned from Marketed and Investigational Prodrugs”,J Med Chem, (2004) 47(10); 2393-2404.
Kim, Y.J., et al., “Eosinophil-Induced Chronic Hepatitis”,J. Korean Med Sci(1998) 13:219-222.
Lampinen, M., et al., “Cytokine-regulated accumulation of eosinophils in inflammatory disease”,Allergy(2004) 59:793-805.
Owen, C., “Chemokine Receptors in Airway Disease: Which Receptors to Target?”,Pulm Pharmacol&Therap(2001) 14:193-202.
Poulsen, L.K., et al., “Biomolecular Regulation of the IgE Immune Response III. Cytokine Profiles in Atopic Dermatitis, Inhalant Allergy and Non-Allergic Donors”,Cytokine, (1996) 8(8):651-657.
Radinger, M., et al., “Eotaxin-2 regulates newly produced and CD34* airway eosinophils after allergen exposure”,J. Allergy Clin Immunol(2004) 113:1109-16.
Rothenberg, M.E., “Eosinophilic gastrointestinal disorders (EGID)”,J Allergy Clin Immunol(Jan. 2004) pp 11-28.
Shakoory, B., et al., “The Role of Human Mast Cell-Derived Cytokines in Eosinophil Biology”,J Interferon Cytokine Res(2004) 24:271-81.
Straumann, A., et al., The physiological and pathophysiological roles of eosinophils in the gastrointestinal tract,Allergy(2004) 59:15-25.
Webb, D.C., et al., “Distinct spatial requirement for eosinophil-induced airways hyperreactivity”,Immunol Cell Biol(2001) 79:165-69.
Sabroe, I., et al., “A Small Molecule Antagonist of Chemokine Receptors CCR1 and CCR3”,J Biol Chem, (2000) 275(34):25985-25992.
White, J.R., et al., :Identification of Potent, Selective Non-peptide CC Chemokine Receptor-3 Atnagonist That Inhibits Eotaxin-, Eotaxin-2-, and Monocyte chemotactic Protein-4-Induced Eosinophil Migration,J Biol Chem, (2000) 275(47): 36626-36631.
Ying, S., et al., “Eosinophil Chemotactic Chemokines (Eotaxin, Eotaxin-2, RANTES, Monocyte Chemoattractant Protein-3 (MCP-3), and MCP-4), and C-C Chemokine Receptor 3 Expression in Bronchial Biopsies from Atopic and Nonatopic (Intrinsic) Asthmatics”,J Immunol, (1999) pp 6322-6329.

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