C - Chemistry – Metallurgy – 07 – H
Patent
C - Chemistry, Metallurgy
07
H
C07H 13/12 (2006.01) A61K 31/70 (2006.01) A61K 47/48 (2006.01) C07C 263/12 (2006.01) C12N 9/96 (2006.01)
Patent
CA 2192424
The invention relates to novel, water-soluble paclitaxel prodrugs wherein paclitaxel is, through its 2'-hydroxyl functionality, connected to a cleavable spacer group, which is in turn attached to a preferably enzymatically cleavable sugar group. Such prodrugs are relatively non-toxic and can be used in cancer treatment. They can be selectively activated at the tumor site by the action of endogeneous enzymes or targeted enzymes, or via a non-enzymatic process. The enzyme is preferably.beta.-glucuronidase,.beta.-glucosidase or.beta.-galactosidase. The invention also relates to a process for preparing a pharmaceutical composition containing a paclitaxel prodrug as defined herein, which comprises said prodrug with a pharmaceutically acceptable carrier to provide a solid or liquid formulation for administration.
de Bont Hendricus Barthelomeas Andreas
de Vos Dick
Haisma Hidde Jacob
Leenders Ruben Gerardus George
Scheeren Johan Wilhelm
Gowling Lafleur Henderson Llp
Pharmachemie B.v.
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