Biotin esters of rapamycin

A method of inducing immunosuppression in a mammal in need thereof which comprises administering to said mammal an immunosuppressive amount of a compound of the structure ##STR18## R.sup.1 and R.sup.2 are each, independently, hydrogen or ##STR19## X is ##STR20## Y is ##STR21## Z is --CH.sub.2 --, --S--S--, or ##STR22## R.sup.3 is hydrogen, alkyl of 1-6 carbon atoms, arylalkyl of 7-10 carbon atoms, alkenyl of 2-7 carbon atoms, alkynyl of 2-7 carbon atoms, --(CH.sub.2).sub.q CO.sub.2 R.sup.5, --(CH.sub.2).sub.r NR.sup.6 R.sup.7, carbamylalkyl of 2-3 carbon atoms, aminoalkyl of 1-4 carbon atoms, hydroxyalkyl of 1-4 carbon atoms, guanylalkyl of 2-4 carbon atoms, mercaptoalkyl of 1-4 carbon atoms, alkylthioalkyl of 2-6 carbon atoms, indolylmethyl, hydroxyphenylmethyl, imidazoylmethyl, halo, trifluoromethyl, or phenyl which is optionally mono-, di-, or tri-substituted with a substituent selected from alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, hydroxy, cyano, halo, nitro, carbalkoxy of 2-7 carbon atoms, trifluoromethyl, amino, or --CO.sub.2 H;

• R.sup.4, R.sup.6, and R.sup.7 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, or arylalkyl of 7-10 carbon atoms;
• R.sup.5 is hydrogen, alkyl of 1-6 carbon atoms, arylalkyl of 7-10 carbon atoms, alkenyl of 2-7 carbon atoms, alkynyl of 2-7 carbon atoms, or phenyl which is optionally mono-, di-, or tri-substituted with a substituent selected from alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, hydroxy, cyano, halo, nitro, carbalkoxy of 2-7 carbon atoms, trifluoromethyl, amino, or --CO.sub.2 H;
• h=0-1;
• j=0-1;
• m=0-6;
• n=0-6;
• p=0-10;
• q=0-10;
• r=0-6;
• with the proviso that R.sup.1 and R.sup.2 are not both hydrogen, or a pharmaceutically acceptable salt thereof.

A pharmaceutical composition which comprises, a compound of the structure ##STR23## R.sup.1 and R.sup.2 are each, independently, hydrogen or ##STR24## X is ##STR25## Y is ##STR26## Z is --CH.sub.2 --, --S--S--, or ##STR27## R.sup.3 is hydrogen, alkyl of 1-6 carbon atoms, arylalkyl of 7-10 carbon atoms, alkenyl of 2-7 carbon atoms, alkynyl of 2-7 carbon atoms, --(CH.sub.2).sub.q CO.sub.2 R.sup.5, --(CH.sub.2).sub.r NR.sup.6 R.sup.7, carbamylalkyl of 2-3 carbon atoms, aminoalkyl of 1-4 carbon atoms, hydroxyalkyl of 1-4 carbon atoms, guanylalkyl of 2-4 carbon atoms, mercaptoalkyl of 1-4 carbon atoms, alkylthioalkyl of 2-6 carbon atoms, indolylmethyl, hydroxyphenylmethyl, imidazoylmethyl, halo, trifluoromethyl, or phenyl which is optionally mono-, di-, or tri-substituted with a substituent selected from alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, hydroxy, cyano, halo, nitro, carbalkoxy of 2-7 carbon atoms, trifluoromethyl, amino, or --CO.sub.2 H;

• R.sup.4, R.sup.6, and R.sup.7 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, or arylalkyl of 7-10 carbon atoms;
• R.sup.5 is hydrogen, alkyl of 1-6 carbon atoms, arylalkyl of 7-10 carbon atoms, alkenyl of 2-7 carbon atoms, alkynyl of 2-7 carbon atoms, or phenyl which is optionally mono-, di-, or tri-substituted with a substituent selected from alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, hydroxy, cyano, halo, nitro, carbalkoxy of 2-7 carbon atoms, trifluoromethyl, amino, or --CO.sub.2 H;
• h=0-1;
• j=0-1;
• m=0-6;
• n=0-6;
• p=0-10;
• q=0-10;
• r=0-6;
• with the proviso that R.sup.1 and R.sup.2 are not both hydrogen, or a pharmaceutically acceptable salt thereof, and a pharmaceutical carrier.