Rapamycin derivatives

Claim 1

A compound of Formula I: ##STR4## wherein R 1 is: optionally hydroxy-substituted alkynyl; R 2 is of Formula II or Formula III: ##STR5## R 3 is: H, alkyl, alkyenyl, (optionally hydroxy-substituted) alkynyl, aryl, thioalkyl, arylalkyl, hydroxyarylalkyl, hydroxyaryl, hydroxyalkyl, dihydroxyalkyl, hydroxyalkoxyalkyl, hydroxyalkylarylalkyl, dihydroxyalkylarylalkyl, alkoxyalkyl, aminoalkyl, alkylaminoalkyl, alkoxycarbonylamidoalkyl, arylsulfonamidoalkyl, allyl, dihydroxyalkylallyl, dioxolanylallyl, carbalkoxyalkyl, or alkylsilyl; R 4 is H or methyl, or R 4 together with R 3 forms C 2-6 alkylene; R 5 is: R 6 O--CH 2 -- wherein R 6 is H, alkyl, alkenyl, alkynyl, aryl, amino, alkylcarbonyl, arylcarbonyl, heteroarylcarbonyl, hydroxyalkylcarbonyl, aminoalkylcarbinyl, formyl, thioalkyl, arylalkyl, hydroxyarylalkyl, hydroxyaryl, hydroxyalkyl, dihydroxyalkyl, hydroxyalkoxyalkyl, hydroxyalkylarylalkyl, dihydroxyalkylarylalkyl, alkoxyalkyl, aminoalkyl, alkylaminoalkyl, alkoxycarbonylamidoalkyl, arylsulfonamidoalkyl, allyl, dihydroxyalkylallyl, dioxolanylallyl, carbalkoxyalkyl or alkylsilyl, R 7 CO-- where R 7 is H, alkyl, hydroxy, alkoxy, aryloxy, amido, alkamido, a residue of an amino acid, or N,N-disubstituted-amido wherein each substituent of N is independently alkyl, aryl, arylakyl or alkylaryl, or both such substituents together form morpholino or piperazino, R 8 NCH-- where R 8 is alkyl, aryl, amino, alkylamino, arylamino, or arylsulfonylamino, or O,O-(alkylyne) dioxymethylyne; each X and Y is independently O, (H, OH), or (H, OR 9 ); and R 9 is: alkyl, alkylcarbonyl, arylcarbonyl, heteroarylcarbonyl, hydroxyalkylcarbonyl, aminoalkylcarbonyl, formyl or aryl; "alk" or "alkyl" refer to a C 1-10 aliphatic substituent, each such "alk" or "alkyl" being optionally interrupted by an oxy (--O--) linkage; and "ar" or "aryl" refer to substituted or unsubstituted tolyl, phenyl, benzyl, or pyridyl.