Quinolones and their therapeutic use

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

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514255, 514256, 514291, 514312, 544238, 544333, 544405, 546 90, 546156, A61K 3147, A61K 3150, A61K 31505

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active

058918787

ABSTRACT:
1-Alkyl-substituted-quinolone-3-carboxamides have therapeutic utility via inhibition of Phosphodiesterase IV esterase and/or Tumour Necrosis Factor activity. The compounds of the invention have the general formula (I): ##STR1## The compounds of the invention encompassed by formula (I) include enantiomers, diastereoisomers and mixtures, including racemic mixtures.

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Nicholson, C.D. et al, `Differential Modulation of Tissue Function and Therapeutic Potential of Selective Inhibitors of Cyclic Nucleotide Phosphodiesterase Isoenzymes`, Trends Pharm. Sci. 1991, 12(1) pages 19-27.
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Hall, I.P., `Isoenzyme Selective Phosphodiesterase Inhibitors: Potential Clinical Uses`, Brit. J. Clin. Pharm., 1993, 35(1), pp. 1-7.
Giembycz, M.A. et al, `Prospects for Selective Cyclic Nucleotide Phosphodiesterase Inhibitors in the Treatment of Bronchial Asthma`, Clin. Exp. Allergy, 1992, 22(3), pp. 337-344.
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Palfreyman, M.N. (1995) "Phosphodiesterase type IV inhibitors as antiflammatory agents" Drugs of the Future 20(8):793-804.
Schudt, C. et al, "Zardaverine: A Cyclic AMPP Specific PDE III/IV Inhibitor" Agents and Actions, Suppl., 1991, 34, pp. 379-402, abstract only.
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