Paclitaxel prodrugs, method for preparation as well as their use in selective chemotherapy
AssigneePharmachemie B.V.
InventorsHendricus B. A. de Bont, Ruben G. G. Leenders, Johan W. Scheeren, Hidde J. Haisma, Dick de Vos
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Abstract
A paclitaxel prodrug has a paclitaxel portion coupled to a cleavable N-(aliphatic or aromatic)-O-glycosyl carbamate spacer group, and can be administered orally, topically or by injection to provide an anti-tumor effect, the prodrug being activated by a hydrolizing enzyme, an endogeneous enzyme or an exogeneous enzyme.
Claims5
An anti-tumor composition for administration orally, topically or by injection, containing as active ingredient a paclitaxel prodrug, consisting of paclitaxel coupled to a cleavable N-(aliphatic or aromatic)-O-glycosyl carbamate spacer group, said prodrug having formula 1 or 2a,b ##STR5## wherein R.sup.1, R.sup.2, R.sup.3 =--H or --CH.sub.3
- R.sup.4 =--CH.sub.2 OH, --C(O)O.sup.- Z.sup.+
- R.sup.5 =--H, --CX.sub.3, --OY, --NHY,
- --S(O).sub.2 Y, --C(O)Y, --C(O)OY
- X=halogen
- Y=C.sub.1 -C.sub.3 alkyl, aryl
- Z=H, Li, Na, K
- n=1(a) or 2(b),
- or an acid addition salt thereof.
Dependencies are inferred from the claim text.