Itraconazole and stereoisomers

Details Itraconazole and stereoisomers Itraconazole and stereoisomers

1996-07-09

1999-12-07

Lee, Howard C.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

514384, 544359, 544367, A61K 31495, A61K 3150, C07D40314

Patent

active

059984139

ABSTRACT:
Anti-infective compositions for the treatment of a human in need of therapy for a systemic or topical fungal infection which comprise a pharmaceutically acceptable carrier and a therapeutically effective amount of (2R,4S) itraconazole or a pharmaceutically acceptable salt thereof, substantially free of its (2S,4R) stereoisomer.

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Nerurkar et al. J. Clin. Pharm., vol. 32(10):935-943, (1992). Abstract only.
Hardin, et al., "Pharmacokinetics of Itraconazole following Oral Administration to Normal Volunteers", Antimicrobial Agents and Chemotherapy, 32, No. 9, 1988, 1310-1313.
J. Heeres, et al., "Antimycotic Azoles. 7. Synthesis and Antifungal Properties of a Series of Novel Triazol-3-ones", J. Med. Chem., 27, No. 7, 1984, 894-900.
Hostetler, et al., "Effect of cyclodextrin on the pharmacology of antifungal oral azoles", Antimicrobial Agents and Chemother., 36, (2), 1992, 477-480.
Stinson, "Wave of new enantiomer products set to flood the market as chemists develop chiral technology for large-scale production processes", C&EN, 71(39), Sep. 27, pp. 38-63.
Stinson, "New single-isomer products on the chiral drug market create demand for enantiomeric intermediates and enantioselective technologies", C&EN, 72(38), Sep. 19, 1994, pp. 38-72.
J. Van Cutsem, et al., "Oral and parenteral therapy with saperconazole (R 66905) of invasive aspergillosis in normal and immunocompromised animals", Antimicrobial Agents and Chemo., 33, No. 12, 1989, 2063-2068.
J. Van Cutsem, et al., "Antimycotic Azoles. 7. Synthesis and Antifungal Properties of a Series of Novel Triazol-3-ones", J. Med. Chem., 27, No. 7, 1984, 894-900.
J. Van Cutsem, et al., "In vitro Antifungal Spectrum of Itraconazole and Treatment of Systemic Mycoses with Old and New Antimycotic Agents", J. Chemother., 38, Supp. 1, 1992, 3-11.

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