Taxane-based prodrugs

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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549510, 549511, 528421, A61K 31335, C07D30514

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active

058247017

ABSTRACT:
Taxane-based compositions of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of aryls, substituted aryls, aralkyls, substituted aralkyls, alkyls and substituted alkyls;

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Georg, G. et al., "Selective C-2 and C-4 Deacylation and Acylation of Taxol: The First Synthesis of a C-4, Substituted Taxol Analogue", Tetrahedron Letters, vol. 35, No. 48; pp. 8931-8934, (1994).
Ueda Y. et al., "Synthesis and Antitumor Evaluation of 2'-Oxycarbonylpaclitaxels (Paclitaxel-2'-Carbonates)", Bioorganic and Med. Chem. Letters; vol. 4, No. 15; pp. 1861-1864, (1994).
Ueda Y. et al., "Novel, Water-Soluble Phosphate Derivaties of 2'-Ethoxy Carbonylpaclitaxel as Potential Prodrugs of Paclitaxel: Syntheses and Antitumor Evaluation",Bioorg.& Med. Chem. Ltrs; vol. 5 No. 3: pp. 247-252; (1995).

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