Methods and compositions of (2R,4S) itraconazole for treating fu

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

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A61K 31495, A61K 3150

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active

054749972

ABSTRACT:
Methods and compositions are disclosed utilizing the optically pure (2R,4S) isomer of itraconazole. This compound is a potent drug for the treatment of local and systemic fungal, yeast, and dermatophyte infections, while avoiding the concomitant liability of adverse effects associated with the racemic mixture of itraconazole.

REFERENCES:
patent: 4267179 (1981-11-01), Heeres et al.
patent: 4490530 (1984-12-01), Heeres et al.
"Pharmacokinetics of Itraconazole following Oral Administration to Normal Volunteers," by T. Hardin, J. Graybill, R. Fetchick, R. Woestenborghs, M. Rinaldi and J. Kuhn; Antimicrobial Agents and Chemotherapy, vol. 32, No. 9, (1988), pp. 1310-1313.
"In vitro Antifungal Spectrum of Itraconazole and Treatment of Systemic Mycoses with Old and New Antimycotic Agents," by J. Van Cutsem; Journal of Chemotheraphy, vol. 38, Supplement 1, (1992), pp. 3-11.
"Activity of Orally, Topically, and Parenterally Administered Itraconazole in the Treatment of Superficial and Deep Mycoses: Animal Modes," by J. Van Cutsem, F. Van Gerven and P. A. J. Janssen; Reviews of Infectious Diseases, vol. 9, Supplement 1, (1987), pp. S15-S32.
"Antimycotic Azoles. 7. Synthesis and Antifungal Properties of a Series of Novel Triazol-3-ones," by J. Heeres, L. J. J. Backx and J. Van Cutsem; Journal of Medical Chemistry, vol. 27, No. 7, (1984), pp. 894-900.

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