Amide esters of rapamycin

Details Amide esters of rapamycin Amide esters of rapamycin

C - Chemistry, Metallurgy

07

H

C07H 19/01 (2006.01) C07D 498/18 (2006.01)

Patent

CA 2068567

ABSTRACT A compound of the structure Image wherein R1 and R2 are each independently, hydrogen or Image ; X is -(CH2)m- or -Ar-; R3 and R4 are each, independently, hydrogen, alkyl, -(CH2)n-Ar, -(CH2)p-NR5R6, or-(CH2)p-N+R5R6R7Y-; R5 and R6 are each, independently, hydrogen, alkyl, or -(CH2)n-Ar; Ar is an optionally substituted group selected from Image , Image , Image , Image , Image , Image ,or Image in which the optional substituents are selected from the group consisting of alkyl, aralkyl, alkoxy, cyano, halo, nitro, carbalkoxy, or perfluoroalkyl; R7 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 R1 and R2 are not both hydrogen; or a pharmaceutically acceptable salt thereof, which by virtue of its immunosuppressive activity is useful in treatingtransplantation 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.

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