Organic compounds -- part of the class 532-570 series – Organic compounds – Nitrogen attached directly or indirectly to the purine ring...
Patent
1995-09-14
2000-02-08
Raymond, Richard L.
Organic compounds -- part of the class 532-570 series
Organic compounds
Nitrogen attached directly or indirectly to the purine ring...
540460, 540575, 546180, 546189, 546190, 546191, C07D29532, C07D295205
Patent
active
060229691
ABSTRACT:
Novel compounds, compositions and methods effective for the prevention and treatment of mast-cell mediated inflammatory disorders are described. The compounds, compositions and methods are effective for the prevention and treatment of inflammatory diseases associated with the respiratory tract, such as asthma and allergic rhinitis, as well as other types of immunomediated inflammatory disorders, such as rheumatoid arthritis, conjunctivitis and inflammatory bowel disease, various dermatological conditions, as well as certain viral conditions. The compounds comprise potent and selective inhibitors of the mast cell protease tryptase. The compositions for treating these conditions include oral, inhalant, topical and parenteral preparations as well as devices comprising such preparations.
REFERENCES:
patent: 4220646 (1980-09-01), Cotrel et al.
patent: 4746737 (1988-05-01), Fujii et al.
patent: 5525623 (1996-06-01), Spear et al.
patent: 5656660 (1997-08-01), Lum et al.
Castells, et al., "Tryptase levels in nasal-lavage fluid as an indicator of the immediate allergic response," 1988, J. Allergy Clin. Immunol., 82:348-355.
Caughey, et al., "Substance P and Vasoactive Intestinal Peptide Degradation by Mast Cell Tryptase and Chymase," 1988, J. Pharmacol. Exp Ther., 244:133-137.
Caughey, "The Structure and Airway Biology of Mast Cell Proteinases," 1991, Am. J. Respir Cell Mol. Biol., 4:387-394.
Chiu, et al., "Gastric Cytoprotective Properties of SCH 32761, a Novel Antiulcer Agent," 1984, Arch, Int, Pharmacodyn., 270:128-140.
Franconi, et al., "Mast Cell Tryptase and Chymase Reverse Airway Smooth Muscle Relaxation Induced by Vasoactive Intestinal Peptide in the Ferret," 1988, J. Pharmacol. Exp. Ther., 248(3):947-951.
Kalenderian, et al., "Elevated Histamine and Tryptase Levels in Smokers' Bronchoalveolar Lavage Fluid--Do Lung Mast Cells Contribute to Smokers' Emphysema?" 1988, Chest, 94:119-123.
Larsen, "Experimental Models of Reversible Airway Obstruction," 1991, The Lung: Scientific Foundations, 953-965.
Miller, et al., "Cloning and Characterization of Complementary DNA for Human Tryptase," 1989, J. Clin, Invest., 84:1188-1195.
Miller, et al., "Cloning and Characterization of Complementary DNA for Human Tryptase," 1990, J. Clin, Invest., 86:864-870.
Ruoss, et al., "Mast Cell Tryptase Is a Mitogen for Cultured Fibroblasts,," 1991, J. Clin, Invest., 88:493-499.
Schwartz, et al., "Tryptase Levels as an Indicator of Mast-Cell Activation in Systemic Anaphylaxis and Mastocytosis," 1987, N. Engl. J. Med., 316:1622-1626.
Sekizawa, et al., "Mast Cell Tryptase Causes Airway Smooth Muscle Hyperresponsiveness in Dogs," 1989, J. Clin, Invest., 83:175-179.
Sturzebecher, et al., "Inhibition of Human Mast Cell Tryptase by Benzamidine Derivatives," 1992, Biol. Chem Hoppe-Seyler, 373:1025-1030.
Tam, et al., "Degradation of Airway Neuropeptides by Human Lung Tryptase," 1990, Am. J. Respir, Cell Mol Biol., 3:27-32.
Tidwell, et al., "Aromatic Amidines: Comparison of Their Ability to Block Respiratory Syncytial Virus Induced Cell Fusion and the Inhibit Plasmin, Urokinase, Thrombin, and Trypsin," 1983, J. Med. Chem., 26:294-298.
Tidwell, et al., "Suppression of Respiratory Syncytial Virus Infection in Cotton Rats by Bis (5-Amindino-2-Benzimidazolyl) Methane," 1984, Antimicrobial Agents and Chemotherapy 26:591-593.
Vanderslice, et al., "Molecular Cloning of Dog Mast Cell Tryptase and Related Protease: Structural Evidence of a Unique Mode of Serine Protease Activation," 1989, Biochemistry, 28:4148-4155.
Vanderslice, et al., "Human mast cell tryptase: Multiple cDNAs and genes reveal a multigene serine protease family," 1990, Proc. Natl. Acad, Sci. USA, 87:3811-3815.
Wanner, et al., "Models of Airway Hyperresponsiveness," 1990, Am. Rev. Respir, Dis., 141:253-257.
Wenzel, et al., "Activation of Pulmonary Mast Cells by Bronchoalveolar Allergen Challenge," 1988, Am. Rev. Resp. Dis., 141:1002-1008.
Cotrel et al., "Heterocyclic compounds and compositions containing them," Chemical Abstracts, vol. 85, 1976, No. 46758m.
Jeanmart et al. "Dithiepino [1,4] [2,3-c] pyrrole derivatives," Chemical Abstracts, vol. 87, 1977, No. 184560h.
Cotrel et al., "Heterocyclic compounds for pharmaceutical compositions," Chemical Abstracts, vol. 94, 1981, No. 156973w.
Farge et al. "Dithiepino [1,4] [2,3-c] pyrrole derivatives and pharmaceutical compositions containing them," Chemical Abstracts, vol. 95, 1981, No. 43190r.
Chemical Abstracts, Document No. 125:114691, 1996.
Chemical Abstracts, Document No. 124:260612, 1996.
Chemical Abstracts, Document No. 122:290875, 1995.
Dener Jeffrey Mark
Gangloff Anthony Robert
Kuo Elaine Yee-Lin
Rice Ken Duane
AxyS Pharmaceuticals, Inc.
Raymond Richard L.
LandOfFree
Compositions and methods for treating mast-cell mediated conditi does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Compositions and methods for treating mast-cell mediated conditi, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Compositions and methods for treating mast-cell mediated conditi will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-1682291