Compounds for treating diseases wherein inhibition of Fas-mediated apoptosis is indicated

摘要

The compounds of Formula (I) may be used in the manufacture of medicaments for inhibiting the expression of Fas, for treating autoimmune diseases and for inhibiting tumor growth and metastasis. In formula (I); R7-R13 are independently H or OH; and A is a moiety of Formula (II), wherein; R1 is hydrogen, lower alkanoyl of up to 6 carbon atoms or aroyl selected from benzoyl and naphthoy!; R2 is hydrogen, lower alkyl of up to 6 carbon atoms or arylalkyl selected from benzyl, phenylethyl and phenylpropyl; R3 is hydrogen or lower alkyl of up to 6 carbon atoms; R4 is hydrogen or lower alkyl of up to 6 carbon atoms, or when X is oxygen, R4 together with R5 can represent CH2O; X is a single bond, CH2, oxygen or sulfur; Ar is selected from phenyl, naphthyl, indanyl and tetrahydronaphthyl; R5 and R6 are individually selected from hydrogen, fluorine, chlorine, bromine, hydroxyl, lower alkyl of up to 6 carbon atoms, a CONH2 group, lower alkoxy of up to 6 carbon atoms, benzyloxy, lower alkylthio of up to 6 carbon atoms, lower alkysulphinyl of up to 6 carbon atoms and lower alkylsulphonyl of up to 6 carbon atoms; or R5 and R6 together represent methylenedioxy. A preferred compound of the formula above is carvedilol (1-(carbazol-4-yloxy-3-[(2-(o-methoxyphenoxy)ethyl]amino]-2-propanol).