Imino-aza-anthracyclinone derivatives for the treatment of amyloidosis

摘要

A compound of formula I wherein: R1 is selected from hydrogen, hydroxyl, alkyl, alkoxyl, cycloalkoxyl, halogen, amino which may be unsubstituted or mono- or di- substituted by acyl, trifluoroacyl, aralkyl, aryl, OSO2(R4) wherein R4 is alkyl or aryl; R2 is selected from hydrogen, RB-CH2- wherein RB represents an aryl group, a heterocyclyl group or a group of formula Rc-CH=CH- , wherein Rc is hydrogen, alkyl, alkenyl or cycloalkyl, alkyl, cycloalkyl, aryl-alkyl, aryloxy-alkyl, acyl of formula C-(R5)=O wherein R5 is selected from hydrogen, alkyl, alkenyl, cycloalkyl, aryl, heterocyclyl, an acyl residue of an amino acid: R3 is selected from a group of formula OR6 wherein R6 represents hydrogen, alkyl, alkenyl, cycloalkyl, aryl-alkyl, aryl, a group of formula NR7R8 wherein R7 and R8 which can be the same or different, represent hydrogen, alkyl, aralkyl, alkenyl, cycloalkyl, heterocyclyl, acyl of formula -C(R5)=O wherein R5 is as above defined, or R7 and R8 together with the N atom to which they are attached, represent heterocyclyl, the term "aryl" includes mono- or bicyclic aromatic groups optionally substituted by one or more substituents selected from alkyl, alkoxy, trifluoromethyl, halogen, hydroxy or aryloxy, an alkyl group may be substituted with one or more substituents selected from cycloalkyl, heterocyclyl, halogen, CF3, hydroxy, alkoxy, aryloxy, amino, mono- or di-alkylamino, carboxy and alkyloxycarbonyl, a heterocyclyl group may be optionally substituted with one or more alkyl substituents; with the proviso that when R, is a methoxyl group and R3 is a hydroxyl group then R2 is not 4-pyridinmethyl, or a pharmaceutically acceptable salt thereof. These compounds are useful in the treatment of amyloidosis.