Carboxylic acid esters of rapamycin

C - Chemistry – Metallurgy – 07 – H

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C07H 19/24 (2006.01) A61K 31/70 (2006.01)

Patent

CA 2051781

AHP-9580 ABSTRACT A compound of the structure Image wherein R1, R2, and R3 are each, independently, hydrogen or Image with the proviso that R1, R2, and R3 are not all hydrogen; R4 is -(CH2)mX(CH2)nCO2R5 or Image ; R5 and R6 are each, independently, alkyl, aralkyl, or phenyl which is optionallymono-, di-, or tri-substituted with a substituent selected from alkyl, alkoxy, hydroxy, cyano, halo, nitro, carbalkoxy, trifluoromethyl, amino, or a carboxylic acid; X is Image , O, or S; R7 and R8 are each, independently, hydrogen or alkyl; Y is CH or N; m is 0-4; n is 0-4; with the proviso that m and n are not both O when X is O or S; or a pharmaceutically acceptable salt thereof, which is by virtue of its immunosuppressive activity is useful in treating transplantation rejection, host vs. graft disease, autoimmune diseases, and diseases of inflammation, and by virtue of itsantifungal activity is useful in treating fungal infections.

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