ANTI-TUMORMEDEL

摘要

The invention pertains to anthraquinone derivatives of the following general formula: the tautomeric forms and the pharmacologically acceptable acid-addition salts thereof, wherein A-B is selected from CH-CH and CH2-CH2; Q is a divalent optionally branched C2-C4 alkylene moiety, wherein R1 and R2 are each individually hydrogen, C1-C4 alkyl monohydroxy C2-C4 alkyl wherein the carbon atom alpha to the nitrogen atom may not bear an hydroxy group, dihydroxy C3-C6 alkyl wherein the carbon atom alpha to the nitrogen atom may not bear an hydroxy group, formyl, C2-C4 alkanoyl trifluoroacetyl and moieties of the formulae: -(CH2)n-CN, -(CH2)n-O-R and wherein n is an integer from 2 to 4, inclusive, R is C1-C4 alkyl and R3 and R4 are each individually hydrogen, C1-C4 alkyl and monohydroxy C2-C4 alkyl wherein the carbon atom alpha to the nitrogen atom may not bear an hydroxy group; and R1 and R2 taken together with their associated N atom and R3 and R4 taken together with their associated N atom is morpholino, thiomorpholino, piperazino, 4-methyl-1 -piperazino or a moiety of the formula: wherein m is an integer from 2 to 6, inclusive; with the proviso that the ratio of the total number of carbon atoms to the sum of the total number of oxygen atoms plus the total number of nitrogen atoms in the side chains at the 1-position and the 4-position may not exceed 4; R5 is hydrogen, hydroxy, chloro and C1-C6 alkanoyloxy; R6 is hydrogen and hydroxy; R7 is hydrogen, hydroxy, chloro, C1-C6 alkanoyloxy and a moiety of the formula wherein R8 and R9 are each individually methyl, ethyl, and beta -hydroxy- ethyl; provided that when R5 is OH then one of R6 and R7 must be H, and when R5 is H then both of R6 and R7 must be H. The above-defined anthraquinone derivatives, many of which are novel per se, have a number of useful properties, including in many cases activity as anti-tumor agents.