Open chain-morpholino adriamycins

Claim 1

A compound of the formula: ##STR4## and the pharmaceutically acceptable salts thereof wherein R is: --CO--CH 3 , --CHOH--CH 3 , --CO--CH 2 OH, --CHOH--CH 2 OH, hydrogen, hydroxy, 1 to 3 carbon alkyl, 1 to 3 carbon terminal hydroxyalkyl; or, a 2 to 7 carbon ester or diester of said --CO--CH 2 OH, --CHOH--CH 2 OH, --CHOH--CH 3 or of said 1 to 3 carbon terminal hydroxyalkyl; or said --CO--CH 2 OH, --CHOH--CH 2 OH, or --CHOH--CH 3 or said 1 to 3 C-terminal hydroxyalkyl having 1 to 6 carbon alkyl or aryl ether replacements of one or more of the hydroxyls; or 13-ketimine derivatives of --CO--CH 3 and --CO--CH 2 OH; Y is hydrogen, hydroxy, or methoxy, X is O or NH, but when Y is hydrogen or hydroxy, X must be O; at least one of R 1 and R 2 is hydrogen and the other is hydrogen, hydroxy, or methoxy; B is H, alkyl (1-6) or aryl (6-15) which is unsubstituted or which contains substituents selected from the group consisting of halo, lower alkyl (1-4) nitro or lower alkoxy; lower alkyl (1-4), said alkyl or said unsubstituted or substituted aryl lower alkyl also being unsubstituted or substituted with hydroxy, alkoxy, carbonyl, cyano or ester group substitutions; or B and R 2 taken together, in order, are the methylene-oxygen bridge --CH 2 --O--; and A is --CHR 3 CN wherein R 3 is H, aryl (6-15), which is unsubstituted or which contains substituents selected from the group consisting of halo, lower alkyl (1-4) nitro or lower alkoxy; alkyl (1-6) or aryl lower alkyl (1-4), wherein the aryl is unsubstituted or contains substituents selected from the group consisting of halo, lower alkyl (1-4) nitro or lower alkoxy; said alkyl or aryl lower alkyl is unsubstituted or contains hydroxy, alkoxy, carbonyl, or ester group substitutions.