O-allylated rapamycin derivs. of formula (I) are new. X = (H,H) or O Y = (H, OH) or O R1 and R2 = each H, alkyl, thioalkyl, arylalkyl, hydroxyalkyl, dihydroxyalkyl, hydroxyalkylarylalkyl, dihydroxyalkylaralkyl, alkoxyalkyl, acyloxyalkyl, aminoalkyl, alkylaminoalkyl, alkoxycarbonylamino-alkyl, acylaminoalkyl, arylosulphonamido-alkyl, allyl, dihydroxyalkylallyl, dioxolanyl-allyl, carbalkoxyallyl or (R3)3Si R3 = each H, Me, Et, i-Pr, t-Bu or Ph R4 = Me or R4 and R1 together form 2-6C alkylene alk- or alkyl refer to 1-6C alkyl, branched or linear, esp. 1-3C alkyl, in which the carbon chain is opt. interrupted by an ether linkage provided that T1 and R2 are not both it and provided that when R1 is carboxyalkyl or (R3)3Si, X and Y are not both O. Dose is 0.05-10 mg/kg p.o. or 0.01-5 mg/kg. i.r.
