Drug resistance and multidrug resistance modulators

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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544381, A01N 4360, C07D24104

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active

057769397

ABSTRACT:
Drug and multidrug resistant modulators of Formula (C): ##STR1## where Z is selected from the group consisting of --S--, --S(O).sub.w --, and --CH.sub.2 --, where w is 1 or 2; and pharmaceutically acceptable salts or solvates thereof are described and claimed.
Use of the new compounds in the preparation of pharmaceutical compositions is described and claimed. In addition, methods for treating drug and multidrug resistance in various diseases using a compound of this invention are described and claimed. Also, methods of enhancing oral bioavailability of a drug and methods of enhancing bioavailability of a drug to the brain using a compound of this invention are described and claimed.

REFERENCES:
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patent: 5596002 (1997-01-01), Hofheinz et al.
patent: 5654304 (1997-08-01), Pfister et al.
Ruetz, Stephan, et al., "The pfmdrl gene of Plasmodium falciparum confers cellular resistance to antimalarial drugs in yeast cells," Proc. Natl. Acad. Sci. USA, vol. 93, pp. 9942-9947, (1996).
Terao, Toshimitsu, et al., "Active Secretion of Drugs from the Small Intestinal Epithelium in Rats by P-Glycoprotein Functioning as an Absorption Barrier," J. Pharm. Pharmacol, 48:1083-1089 (1996).
Pfister, J. R., et al., "Methanodibenzosuberylpiperazines as Potent Multidrug Resistance Reversal Agents," Bioorganic & Medicinal Chemistry Letters, vol. 5, No. 21, pp. 2473-2476 (1995).

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