| 摘要 |
The invention concerns a compound of the structure <CHEM> wherein R<1> and R<2> are each independently, hydrogen or <CHEM> X is -(CH2)m- or -Ar<1>- ; R<3> and R<4> are each, independently, hydrogen, alkyl, -(CH2)n-Ar, -(CH2)p-NR<5>R<6>, or -(CH2)p-N<+>R<5>R<6>R<7>Y<-> ; R<5> and R<6> are each, independently, hydrogen, alkyl, or -(CH2)n-Ar; Ar- and -Ar<1>- are each optionally substituted mono- or bivalent radicals respectively of groups selected from <CHEM> <CHEM> in which the optional substituents are selected from the group consisting of alkyl, aralkyl, alkoxy, cyano, halo, nitro, carbalkoxy, or perfluoroalkyl; R<7> is alkyl; Y is a halide, sulfate, phosphate, or p-toluenesulfonate anion; m = 1 -6; n = 1-6; p = 1 -6; with the proviso that R<1> and R<2> are not both hydrogen; or a pharmaceutically acceptable salt thereof, which by virtue of its immunosuppressive activity is useful in treating transplantation rejection, host vs. graft disease, autoimmune diseases and diseases of inflammation; by virtue of its antitumor activity is useful in treating solid tumors; and by virtue of its antifungal activity is useful in treating fungal infections. |
