Back to results
US 5,489,589 AGranted
Amino acid derivatives of paclitaxel
AssigneeBristol-Myers Squibb Company
InventorsMark D. Wittman, John F. Kadow
Life of this patent
Estimating the term…
Abstract
The present invention concerns water-soluble amino acid derivatives of paclitaxel, their use as antitumor agents, and pharmaceutical compositions containg the compounds.
Claims11
A compound of the formula (I):
- ##STR30## wherein R.sup.1 or R.sup.2 are independently hydrogen or --(CH.sub.2 O)).sub.n COCH.sub.2 Y;
- R.sup.6 is hydrogen, C.sub.1-8 alkanoyl or --(CH.sub.2 O).sub.n COCH.sub.2 Y;
- n is one to six;
- p is zero or one;
- R.sup.4 and R.sup.5 are independently C.sub.1-8 alkyl, C.sub.2-8 alkenyl, C.sub.2-8 alkynyl, or --Z--R.sup.7 ;
- Z is a direct bond, C.sub.1-8 alkylene or C.sub.2-8 alkenediyl;
- R.sup.7 is aryl, substituted aryl, C.sub.3-8 cycloalkyl or heteroaryl;
- R.sup.3 is hydrogen, C.sub.1-8 alkyl, C.sub.2-8 alkenyl, C.sub.2-8 alkynyl, C.sub.3-8 cycloalkyl, aryl or heteroaryl;
- Y is a radical of the formula ##STR31## in which q is one to three;
- R.sup.r is hydrogen or C.sub.1-8 alkyl;
- and with the proviso at least one of R.sup.1, R.sup.2 and R.sup.6 is --(CH.sub.2 O).sub.n COCH.sub.2 Y;
- or a pharmaceutically acceptable salt thereof.
9 more elements
Dependencies are inferred from the claim text.