Sulfonylcarbamates of rapamycin
AssigneeAmerican Home Products Corporation
InventorWenling Kao
Life of this patent
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Abstract
A compound of the structure ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen or --CONHSO.sub.2 -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 provision that R.sup.1 and R.sup.2 are not hydrogen; or 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.
Claims7
A compound of the formula ##STR4## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen or --CONHSO.sub.2 -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 a group selected from alkyl of 1-6 carbon atoms, phenylalkyl of 7-10 carbon atoms, alkoxy of 1-6 carbon atoms, cyano, halo, nitro, carbalkoxy of 2-7 carbon atoms, trifluoromethyl, amino, dialkylamino of 1-6 carbon atoms per alkyl group, alkylthio of 1-6 carbon atoms, --SO.sub.3 H, --PO.sub.3 H, and --CO.sub.2 H;
- with the proviso that R.sup.1 and R.sup.2 are not both hydrogen;
- or a pharmaceutically acceptable salt thereof when the Ar group contains a basic nitrogen or when the Ar group is substituted by dialklyamino of 1-6 carbon atoms per alkyl group, --SO.sub.3 H, --PO.sub.3 H, or --CO.sub.2 H.
A compound which is rapamycin 42-tertbutyldimethylsilyl ether-31-ester with phenylsulfonylcarbamic acid.
Dependencies are inferred from the claim text.