Sulfonyl carbamates of rapamycin

C - Chemistry – Metallurgy – 07 – H

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

Patent

CA 2065791

ABSTRACT A compound of the structure Image wherein R1 and R2 are each, independently, hydrogen or -CONHSO2-Ar; and Ar is phenyl, naphthyl, pyridyl, quinolyl, isoquinolyl, quinoxalyl, thienyl, thionaphthyl, furyl, benzofuryl, benzodioxyl, benzoxazolyl, benzoisoxazolyl, or benzodioxolyl; wherein the Ar group may be optionally mono-, di-, or tri- substituted; 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 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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