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AssigneesEnsuiko Sugar Refining Co., Ltd., Bio Research Corporation of Yokohama, Tadakatsu Mandai, Kaken Pharmaceutical Co., Ltd.
InventorsTadakatsu Mandai, Hiroshi Okumoto, Koji Hara, Katsuhiko Mikuni, Kozo Hara, Yoshinori Tsuchiya, Kosho Nakamura, Teruhiko Umetsu
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An object of the invention is to develop galactose or mannose derivatives of docetaxel, etc. having improved solubility and physiological activity, to alleviate burden imposed on patients and to provide effective therapeutic drug for tumors. The present invention provides taxoid derivatives comprising any of paclitaxel, docetaxel and 10-deacetyl-baccatin III to which galactose or mannose is linked through a spacer, and methods for producing taxoid derivatives comprising reacting paclitaxel, docetaxel or 10-deacetyl-baccatin III with tetrabenzyl acetyloxygalactoside or tetrabenzyl acetyloxymannoside, subjecting the product to debenzylation reaction, and optionally to detriethylsilylation reaction.
A taxoid derivative comprising any one of paclitaxel, docetaxel and 10-deacetyl-baccatin III to which galactose or mannose is linked through a glycolate which is a spacer.
An antitumor agent comprising galactosyloxyacetyl-10-docetaxel as an active ingredient
An antitumor agent comprising mannosyloxyacetyl-10-docetaxel as an active ingredient
Dependencies are inferred from the claim text.