Hydrolysis-promoting hydrophobic taxane derivatives
申请(专利)号:
US19990249004
申请日期:
1999-02-12
公开/公告号:
US6107332A
公开/公告日期:
2000-08-22
申请(专利权)人:
THE LIPOSOME COMPANY, INC.
被引量:
摘要:
Provided herein is a taxane having a hydrocarbon attached at the 2′ and/or 7 positions, the hydrocarbon's alpha position being occupied by a “hydrolysis-promoting group” (“HPG”). In one embodiment, the hydrolysis promoting group is stereospecifically attached to the &agr;-carbon of the hydrophobic taxane. The Substitution of an HPG for the methylene unit ordinarily occupying the alpha position allows for enhanced in vivo hydrolysis of the hydrocarbon-taxane bond, and hence, for enhanced taxane therapeutic activity. Also provided herein are taxane-containing compositions, and methods of administering taxanes to animals, including those afflicted with cancers or inflammatory diseases.
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