Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai
Patent
1996-08-16
1997-12-09
Robinson, Douglas W.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Peptide containing doai
530317, A61K 3800, A61K 3812, C07K 500
Patent
active
056960840
ABSTRACT:
Disclosed are novel antifungal agents having the formula: ##STR1## or a pharmaceutically acceptable acid, ester or prodrug thereof, wherein preferred compounds include those compounds wherein R.sub.1 is selected from the group consisting of --NH.sub.2 ; R.sub.2 is selected from the group consisting of hydrogen, fluoro, and hydroxyl; R.sub.3 is selected from the group consisting of --CH.sub.2 (p-C.sub.6 H.sub.4).sub.3 O(CH.sub.2).sub.3 CH.sub.3, --CH.sub.2 (p-C.sub.6 H.sub.4)O(CH.sub.2).sub.6 CH.sub.3, --COO(p-C.sub.6 H.sub.4)O(CH.sub.2).sub.6 CH.sub.3, --CO(Piperazinyl)(p-C.sub.6 H.sub.4).sub.2 OCH.sub.3, --CO(p-C.sub.6 H.sub.4)O(CH.sub.2).sub.6 CH.sub.3, --CO(p-C.sub.6 H.sub.4)(Piperazinyl)(p-C.sub.6 H.sub.4)O(CH.sub.2).sub.4 CH.sub.3, --CO(p-C.sub.6 H.sub.4)(Piperazinyl)(p-C.sub.6 H.sub.4)O(CH.sub.2).sub.6 CH.sub.3, --CO(p-C.sub.6 H.sub.4)(Piperazinyl)(p-C.sub.6 H.sub.4)OCH.sub.3, and --CO(p-C.sub.6 H.sub.4)(Piperazinyl)O(CH.sub.2).sub.6 CH.sub.3 ; and R.sub.4 is selected from the group consisting of --CH(OH)CH.sub.3, --CH.sub.2 OH, --CH.sub.2 CH.sub.3, --CH.sub.2 CH.sub.2 CH.sub.2 NH.sub.2, --CH.sub.2 (CH.sub.2)NH.sub.2, --CH.sub.2 NH.sub.2, --CH.sub.2 (CH.sub.2).sub.2 (NH)C.dbd.(NH)--NH.sub.2, --CH.sub.3, --CH.sub.2 (Ph)OH, hydrogen, --CH.sub.2 CH.sub.2 COOH, and --CH.sub.2 COOH. Also disclosed are pharmaceutical compositions containing such compounds and the use of the same in the treatment of fungal infections.
REFERENCES:
patent: 5502033 (1996-03-01), Iwamoto et al.
Zambias, R. A., et al., "Preparation and Structure-Activity Relationships of Simplified Analogues of the Antifungal Agent Cilofungin: A Total Synthesis Approach", J. Med. Chem., vol. 35, No. 15, 1992, pp. 2843-2855.
Kurokawa, N., et al., "Total Synthesis of Echinocandins. 1. Sterocontrolled Syntheses of the Constituent Amino Acids", J. Am. Chem. Soc., 108, No. 19, 1986, pp.6041-6045.
Balkovec, J. M., "Lipopeptide antifungal agents", Section Review-Anti-infectives, Expert. Opin. Invest. Drugs, (1994) 3(2), pp. 65-82.
Degoey David Allen
Grampovnik David J.
Klein Larry Lewis
Lartey Paul A.
Leone Christina Louise
Abbott Laboratories
Anand Mona
Bell Kent L.
Robinson Douglas W.
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