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US 4,942,184 AGranted
Water soluble, antineoplastic derivatives of taxol
AssigneeThe United States of America as represented by the Department of Health and Human Services
InventorsRudiger D. Haugwitz, Leon Zalkow, Jan Glinski, Mathew Suffness, Howard M. Deutsch, Venkatachala Narayanan
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Abstract
Antineoplastic, water soluble, taxol derivatives and methods for preparing the same are described.
Claims8
Antineoplastic water soluble derivatives of taxol having the following formula:
- ##STR4## wherein:
- Z=ethylene, propylene, CHCH, 1,2-cyclohexane, 1,2-phenylene,
- R.sup.1 =OH base, NR.sup.2 R.sup.3, OR.sup.3, SR.sup.3, OCH.sub.2 CONR.sup.4 R.sup.5, OH
- R.sup.2 =hydrogen, methyl
- R.sup.3 =(CH.sub.2).sub.n NR.sup.6 R.sup.7 ;
- (CH.sub.2).sub.n NR.sup..sym.6 R.sup.7 R.sup.8 X.sup..crclbar.
- n=1 to 3
- R.sup.4 =hydrogen, lower alkyl containing 1 to 4 carbons
- R.sup.5 =hydrogen, lower alkyl containing 1 to 4 carbons, benzyl, hydroxyethyl, CH.sub.2 CO.sub.2 H, dimethylaminoethyl
- R.sup.6 R.sup.7 =lower alkyl containing 1 or 2 carbons, benzyl or R.sup.6 and R.sup.7 together with the nitrogen atom of NR.sup.6 R.sup.7 form the following rings ##STR5## R.sup.8 =lower alkyl containing 1 or 2 carbons, benzyl X.sup..crclbar. =halide
- base=NH.sub.3, (HOC.sub.2 H.sub.4).sub.3 N, N(CH.sub.3).sub.3, CH.sub.3 N(C.sub.2 H.sub.4 OH).sub.2, NH.sub.2 (CH.sub.2).sub.6 NH.sub.2, N-methylglucamine, NaOH, KOH.
8 more elements
Dependencies are inferred from the claim text.