Aminoesters of rapamycin

A method of treating transplantation rejection, host vs. graft disease, autoimmune diseases, and diseases of inflammation in a mammal by administering an effective amount of a compound having the formula ##STR11## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen or ##STR12## with the proviso that R.sup.1 and R.sup.2 are not both hydrogen;

• R.sup.3 is hydrogen, alkyl of 1-6 carbon atoms, phenylalkyl of 7-10 carbon atoms, --(CH.sub.2).sub.q CO.sub.2 R.sup.6, --(CH.sub.2).sub.r NR.sup.7 CO.sub.2 R.sup.8, 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 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 and R.sup.7 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, or phenylalkyl of 7-10 carbon atoms;
• R.sup.5, R.sup.6, and R.sup.8 are each, independently, alkyl of 1-6 carbon atoms, phenylalkyl of 7-10 carbon atoms, fluorenylmethyl, or phenyl which is optionally mono-, di-, or trisubstituted with a substituent 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;
• m is 0-4;
• n is 0-4;
• p is 1-2;
• q is 0-4;
• r is 0-4;
• wherein R.sup.3, R.sup.4, m, and n are independent in each of the ##STR13## subunits when p=2;
• or a pharmaceutically acceptable salt thereof.