Mucin synthesis inhibitors

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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C514S471000, C514S579000, C546S350000, C549S302000, C564S305000

Reexamination Certificate

active

07345051

ABSTRACT:
The claimed invention relates to methods of modulating mucin synthesis and the therapeutic application of compounds of Formula II in controlling mucin over-production associated with diseases such as chronic obstructive pulmonary diseases (COPD) including asthma and chronic bronchitis, inflammatory lung diseases, cystic fibrosis and acute or chronic respiratory infectious diseases.whereinX is S, N, O or CR;Y is CRR′, O, NR6, CRR′—CRR′ or CR═CR;Z is NR6, O, S, CRR′ or CRR′—CRR′;R1-R3are independently selected from the group consisting of H, C1-C8alkyl, C1-C8alkoxy, amino, hydroxy, halosubstituted alky and halo;R4isQ is CR, NR6orR5is H or benzyl;R6is H, C1-C8alkyl, C1-C8alkoxy, OH or halo; andR and R′ are independently H, C1-C8alkyl, C1-C8alkoxy, OH or halo,or a pharmaceutically acceptable salt thereof.

REFERENCES:
patent: 3138636 (1964-06-01), Scherrer
patent: 3144387 (1964-08-01), Jones
patent: 4168313 (1979-09-01), Bago
patent: 4515980 (1985-05-01), Bailey
patent: 4921875 (1990-05-01), Englert et al.
patent: 4931459 (1990-06-01), Connor et al.
patent: 4994493 (1991-02-01), Greger et al.
patent: 5066668 (1991-11-01), Boschelli et al.
patent: 5114958 (1992-05-01), Boschelli et al.
patent: 5143929 (1992-09-01), Belliotti et al.
patent: 5155110 (1992-10-01), Connor et al.
patent: 5212189 (1993-05-01), Belliotti et al.
patent: 5360925 (1994-11-01), de Lassauniere et al.
patent: 5480999 (1996-01-01), de Lassauniere et al.
patent: 5733748 (1998-03-01), Yu
patent: 5875776 (1999-03-01), Vaghefi
patent: 5908839 (1999-06-01), Levitt et al.
patent: 6737427 (2004-05-01), Zhou et al.
patent: 2928546 (1981-01-01), None
patent: 42 44 539 (1993-07-01), None
patent: 0 174 006 (1986-03-01), None
patent: 0 210 574 (1987-02-01), None
patent: 0 242 559 (1987-10-01), None
patent: 1553171 (1979-09-01), None
patent: WO 85/04589 (1985-10-01), None
patent: WO 96/39419 (1996-12-01), None
patent: WO 97/03659 (1997-02-01), None
patent: WO 98/37881 (1998-09-01), None
patent: WO 98/42708 (1998-10-01), None
patent: WO 99/01421 (1999-01-01), None
patent: WO 99/44620 (1999-09-01), None
patent: WO 00/40235 (2000-07-01), None
patent: WO 00/42003 (2000-07-01), None
patent: WO 00/42029 (2000-07-01), None
patent: WO 01/22935 (2001-04-01), None
patent: WO 01/85146 (2001-11-01), None
[R] O'Neil et al. (eds.), The Merck Index—An Encyclopedia of Chemicals, Drugs and Biologicals, 13th Edition, Merck & Co., Whitehouse Station, NJ, 2001, only entries No. 1034 (bendroflumethiazide), No. 4158 (flufenamic acid), No. 5821 (mefenamic acid), No. 6557 (niflumic acid) and No. 9134 (talniflumate) supplied.
Aikawa et al., “Marked goblet cell hyperplasic with mucus accumlation in the airways of patients who died of severe acute asthma attack,”Chest(1992), vol. 101, pp. 916-921.
Alexander et al., “Trial of cyclosporin in corticosteroid-dependent chronic severe asthma,”Lancet(1992), vol. 339, pp. 324-328.
Beasley et al., “Cellular events in bronchi in mild asthma and after bronchial provocation,”Am. Rev. Respir. Dis.(1989), vol. 139, pp. 806-817.
Borchers et al., “Monocyte inflammation augments acrolein-induced Muc5ac expression in mouse lung,”Am. J. Physiol.(1999), vol. 277, pp. L489-L497.
Bousquet et al., “Eosinophilic inflammation in asthma,”N. Engl. J. Med.(1990), vol. 323, pp. 1033-1039.
Burrows et al., “Association of asthma with serum IgE levels and skin-test reactivity to allergens,”N. Eng. J. Med.(1989), vol. 320, pp. 271-277.
Cardell et al., “Death in asthmatics,”Thorax(1959), vol. 14, pp. 341-352.
Chaumeil, “Micronization: a method of improving the bioavailability of poorly soluble drugs,”Method. Find. Exp. Clin. Pharmacol.(1998), vol. 20, pp. 211-215.
Chu et al., “Glycophorin A interacts with interleukin-2 and inhibits interleukin-2-depedent T-lymphocyte proliferation,”Cell. Immunol.(1992), vol. 145, pp. 223-239.
Clifford et al., “Symptoms, atopy and bronchial response to methacholine in parents with asthma and their children,”Arch. Dis. Childhood(1987), vol. 62, pp. 66-73.
Cunningham et al., “Cloning of an epithelial chloride channel from bovine trachea,”J. Biol. Chem.(1995), vol. 29, pp. 31016-31026.
Cutz et al., “Ultrastructure of airways in children with asthma,”Histopathology(1978), vol. 2, pp. 407-421.
Dong et al., “IL-9 induces chemokine expression in lung epithelial cells and baseline airway eosinophilia in transgenic mice,”Eur. J. Immunol.(1999), vol. 29, pp. 2130-2139.
Doucet et al., “Interleukin (IL) 4 and IL-13 act on human lung fibroblasts: Implication in asthma,”J. Clin. Invest.(1998), vol. 101, pp. 2129-2139.
Doull et al., “Allelic association of gene markers on chromosomes 5q and 11q with atopy and bronchial hyperresponsiveness,”Am. J. Respir. Crit. Care Med.(1996), vol. 153, pp. 1280-1284.
Dugas et al., “Interleukin-9 potentiates the interleukin-4-induced immunoglobulin (IgG, IgM and IgE production by normal human B lymphocytes,”Eur. J. Immunol.(1993), vol. 23, pp. 1687-1692.
Dunnill et al., “A comparison of the quantitative anatomy of the bronchi in normal subjects, in asthmaticus, in chronic bronchitis, and in emphysema,”Thorax(1969), vol. 24, pp. 176-179.
Earle et al., “Fatal bronchial asthma,”Thorax(1953), vol. 8, pp. 195-206.
Eklund et al., “Induction by IL-9 and suppression by IL-3 and IL-4 of the levels of chromosome 14-derived transcripts that encode late-expressed mouse mast cell proteases,”J. Immunol.(1993), vol. 151, pp. 4266-4273.
Eng et al., “Short-term efficacy of ultrasonically nebulized hypertonic saline in cystic fibrosis,”Pediatr. Pulmonol.(1996), vol. 21, pp. 77-83.
Ewart et al., “Respiratory system mechanics in mice measured by end-inflation occlusion,”J. Appl. Phys.(1995), vol. 79, pp. 560-566.
Gergen et al., “The increasing problem of asthma in the United States,”Am. Rev. Respir. Dis.(1992), vol. 146, pp. 823-824.
Gergen et al., “The association of allergen skin test reactivity and respiratory disease among whites in the U.S. population,”Arch. Intern. Med.(1991), vol. 151, pp. 487-492.
Glynn et al., “Bronchial biopsy in chronic bronchitis and asthma,”Thorax(1960), vol. 15, pp. 142-153.
Halonen et al., “The predicitive relationship between serum IgE levels at birth and subsequent incidences of lower respiratory illnesses and eczema in infants,”Am. Rev. Respir. Dis.(1992), vol. 146, pp. 866-870.
Holgate et al., “The bronchial epithelium as a key regulator of airway inflammation and remodeling in asthma,”Clin. Exp. Allergy(1999), vol. 29, pp. 90-95.
Jeffery et al., “Morphology of the airway wall in asthma and in chronic obstructive pulmonary disease,”Am. Rev. Respir. Dis.(1991), vol. 143, pp. 1152-1158.
Kleeberger et al., “A genetic model for evaluation of susceptibility to ozone-induced inflammation,”Am. J. Physiol.(1990), vol. 258, pp. L313-L320.
Kreitman et al., “Site-specific conjugation to interleukin 4 containing mutated cysteine residues produces interleukin 4-toxin conjugates with improved binding and activity,”Biochem.(1994), vol. 33, pp. 11637-11644.
Levitt et al., “Genetic susceptibility to atracurium-induced bronchoconstriction,”Am. J. Respir. Crit. Care. Med.(1995), vol. 151, pp. 1537-1542.
Levitt et al., “Autosomal recessive inheritance of airway hyper-reactivity to 5-hydroxytryptamine,”J. Appl. Physiol.(1989), vol. 67, pp. 1125-1132.
Levitt et al., “Expression of airway hyper-reactivity to acetylcholine as a simple autosomal recessive trait in mice,”FASEB J.(1988), vol. 2, pp. 2605-2608.
Levitt, “Understanding biological variability in susceptibility to respiratory disease”,Pharmacogenetics(1991), vol. 1, pp. 94-97.
Li et al., “act

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