Carbamates of rapamycin
AssigneeAmerican Home Products Corporation
InventorsAmedeo A. Failli, Oleg I. Bleyman, Wenling Kao, Magid A. Abou-Gharbia
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AssigneeAmerican Home Products Corporation
InventorsAmedeo A. Failli, Oleg I. Bleyman, Wenling Kao, Magid A. Abou-Gharbia
Estimating the term…
A compound of the structure ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen, or --CONH--O--(CR.sup.3 R.sup.4).sub.m Z; R.sup.3 and R.sup.4 are each, independently, hydrogen, alkyl, cycloalkyl, --CF.sub.3, or F; Z is hydrogen, alkyl, --OR.sup.5, --SR.sup.5, --NRSR.sup.6, --CN, --CF3, --OAr, --Ar, or R.sup.7 ; R.sup.5 and R.sup.6 are each, independently, hydrogen, alkyl, arylalkyl, alkenyl, alkynyl, alkoxyalkyl, alkylthioalkyl, alkylaminoalkyl, dialkylaminoalkyl, cycloalkyl, or Ar; R.sup.7 ##STR2## or --C.tbd.C--R.sup.11 ; R.sup.8, R.sup.9, R.sup.10, and R.sup.11 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, halogen, or phenyl, wherein the phenyl group may be optionally mono-, di-, or tri-substituted; Ar is an aryl radical that may be optionally mono-, di-, or tri-substituted; and m=1-6; with the proviso that R.sup.1 and R.sup.2 are both not hydrogen, or a pharmaceutically acceptable salt thereof which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.
A compound of the structure ##STR9## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen, or --CONH--O--(CR.sup.3 R.sup.4).sub.m Z;
The compound of claim I which is 42-O-(allyloxyaminocarbonyl)rapamycin or a pharmaceutically acceptable salt thereof.
The compound of claim I which is 42-O-(pyridine-2ylmethoxyaminocarbonyl)rapamycin or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.