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US 4,904,768 AGranted
Epipodophyllotoxin glucoside 4'-phosphate derivatives
AssigneeBristol-Myers Company
InventorsMark G. Saulnier, Peter D. Senter, John F. Kadow
Life of this patent
Estimating the term…
Abstract
Phosphate derivatives of 4'-demethylepipodophyllotoxin glucosides are novel antitumor agents and the salts thereof offer the pharmaceutical advantage of high water solubility.
Claims31
A compound having the formula ##STR10## wherein R.sup.6 is H and R.sup.1 is selected from the group consistng of (C.sub.1-10)alkyl;
- (C.sub.2-10)alkenyl;
- (C.sub.5-6)cycloalkyl;
- 2-furyl;
- 2-thienyl;
- (C.sub.6-10)aryl;
- (C.sub.7-14)aralkyl;
- and (C.sub.8-14)aralkenyl wherein each of the aromatic rings may be unsubstituted or substituted with one or more groups selected from halo, (C.sub.1-8)alkyl, (C.sub.1-8)alkoxy, hydroxy, nitro, and amino;
- or R.sup.1 and R.sup.6 are each (C.sub.1-8)alkyl;
- or R.sup.1 and R.sup.6 and the carbon to which they are attached join to form a (C.sub.5-6)cycloalkyl group;
- X is oxygen or sulfur;
- R.sup.7 and R.sup.8 are independently selected from the group consisting of H, (C.sub.1-5)alkyl, halo-substituted (C.sub.1-5)alkyl, cyano-substituted (C.sub.1-5)alkyl, (C.sub.3-6)cycloalkyl, (C.sub.6-10)aryl, (C.sub.7-14)aralkyl, wherein the ring portion of said aryl and aralkyl groups is unsubstituted or substituted with a group selected from the group consisting of alkyl, halo, and nitro;
- or a pharmaceutically acceptable salt thereof.
9 more elements
The compound etoposide 4'-phosphate disodium salt ##STR12##
The compound etoposide 4'-thiophosphate disodium salt ##STR13##
Dependencies are inferred from the claim text.