C - Chemistry – Metallurgy – 07 – H
Patent
C - Chemistry, Metallurgy
07
H
167/202, 260/228
C07H 15/26 (2006.01) A61K 31/70 (2006.01) C07H 17/04 (2006.01)
Patent
CA 1310637
ABSTRACT Phosphate derivatives of 4'-demethylepipodophyllotoxin glucosides are novel antitumor agents and the salts thereof offer the pharmaceutical advantage of high water solubility. Such agents have the following formula: Image wherein R6 is H and R1 is selected from the group consisting of (C1-10)alkyl; (C2-10) alkenyl; (C56)cycloalkyl; 2-furyl; 2- thienyl; (C6-10)aryl; (C7-14)aralkyl; and (C8-14)aralkenyl wherein each of the aromatic rings may be unsubstituted or substituted with one or more groups selected from halo, (C1-8)alkyl, (C1-8)alkoxy, hydroxy, nitro, and amino; or R1 and R6 are each (C1-8) alkyl; or R1 and R6 and the carbon to which they are attached join to form a (C5-6) cycloalkyl group; X is oxygen or sulfur; R7 and R8 are independently selected from the group consisting of H, (C1-5) alkyl, A-substituted (C1-5)alkyl, (C3-6)cycloalkyl, A-substituted (C36)cycloalkyl, (C~1O)aryl, A-substituted aryl, alkyl-substituted aryl, (C7-14)aralkyl, A-substituted aralkyl, and alkyl-substituted aralkyl; wherein said A-substituents are one or more groups selected from hydroxy, alkoxy, alkanoyloxy, cyano, amino, alkylamino, dialkylamino, carboxy, alkylthio, mercapto, mercaptothio, nitropyridyl disulfide, alkanoylamino, alkanoyl, carbamoyl, nitro, and halo.
573861
Kadow John F.
Saulnier Mark G.
Senter Peter D.
Bristol-Myers Squibb Company
Cassan Maclean
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