Hindered esters of rapamycin and their use as pharmaceuticals

摘要

A compound of the structure wherein R and R1 are each, independently, or hydrogen; R2 and R3 are each, independently, alkyl, arylalkyl, or R2 and R3 may be taken together to form a cycloalkyl ring; R4 is a heterocyclic radical which may be optionally substituted; R5 is alkyl or arylalkyl; R6 and R7 are taken together to form a saturated heterocyclic ring which may be optionally substituted; k=0-1, m=0-1; n=1-6; with the proviso that R and R1 are not both hydrogen, or a pharmaceutically acceptable salt thereof, which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.