RAPAMYCIN ARYLCARBONYL UND ALKOXYCARBONYL CARBAMATE ALS IMMUNOSUPPRESIVE UND ANTIFUNGALE MITTEL

摘要

N-arylcarbonyl and N-alkylcarbonyl carbamates of rapamycin of the formula shown below wherein R1 and R2 are both and where A is lower alkoxy or aryl or heteroaryl, R3 is H or methyl and R4 is C1-C6 alkyl, C2-C6 alkenyl or C2-C6 alkynyl possess immunosuppressive and/or antifungal and/or antitumor and/or antiinflammatory activity in vitro and/or inhibit thymocyte proliferation in vivo. These compounds are thus expected to be useful in the treatment of transplantation rejection, autoimmune diseases, fungal infections, cancer, and diseases of inflammation.