Carbamates of rapamycin

Details Carbamates of rapamycin Carbamates of rapamycin

C - Chemistry, Metallurgy

07

H

C07H 19/01 (2006.01) A61K 31/70 (2006.01) C07D 498/18 (2006.01) C07H 23/00 (2006.01)

Patent

CA 2065790

ABSTRACT A compound of the structure Image wherein R1 and R2 are each, independently, hydrogen or -CONH(CR3R4)n-X; R3 and R4 are each, independently, hydrogen, alkyl, aralkyl, cycloalkyl, halogen, or trifluoromethyl; X is hydrogen, lower alkyl, cycloalkyl, trifluoromethyl, nitro, alkoxy, carboalkoxy, aralkyl, halo, dialkylamino, thioalkyl, or Y; Y is a phenyl group which may be optionally mono-, di-, or tri- substituted with a group selected from alkyl, aralkyl, alkoxy, cyano, halo, nitro, carbalkoxy, trifluoromethyl, dialkylamino, or alkylthio; n=0-5; with the proviso that R1 and R2 are not both hydrogen and when n = 0, X is lower alkyl, cycloalkyl, aralkyl, or Y; or a pharmaceutically acceptable salt thereof when X is dialkylamino, 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.

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