Rapamycin carbonate esters as immuno-suppressant agents

A method of treating organ and tissue transplant rejection which comprises administration to a warm-blooded animal in need thereof of a therapeutically effective amount of a compound according to the formula:

• ##STR4## wherein:
• R.sup.1 and R.sup.2 are independently H or --COOR.sup.3 but both R.sup.1 and R.sup.2 cannot be H, and
• R.sup.3 is C.sub.1 -C.sub.6 alkyl where 1 to 3 hydrogens may be replaced by fluorine, chlorine, bromine or iodine, C.sub.3 -C.sub.8 cycloalkyl, C.sub.2 -C.sub.6 alkenyl, or Ar--(CH.sub.2).sub.n --where n is 0 to 6 and Ar is phenyl, phenyl substituted by fluorine, chlorine, bromine, iodine, trifluoromethyl, nitro, cyano, C.sub.1 -C.sub.6 alkyl or C.sub.1 -C.sub.6 alkoxy;
• pyridinyl, indolyl, quinolyl or furanyl;
• or a pharmaceutically acceptable salt thereof.

A method of treating autoimmune diseases which comprises administration to a warm-blooded animal in need thereof of a therapeutically effective amount of a compound according to the formula:

• ##STR5## wherein:
• R.sup.1 and R.sup.2 are independently H or --COOR.sup.3 but both R.sup.1 and R.sup.2 cannot be H, and
• R.sup.3 is C.sub.1 -C.sub.6 alkyl where 1 to 3 hydrogens may be replaced by fluorine, chlorine, bromine or iodine, C.sub.3 -C.sub.8 cycloalkyl, C.sub.2 -C.sub.6 alkenyl, or Ar--(CH.sub.2).sub.n --where n is 0 to 6 and Ar is phenyl, phenyl substituted by fluorine, chlorine, bromine, iodine, trifluoromethyl, nitro, cyano, C.sub.1 -C.sub.6 alkyl or C.sub.1 -C.sub.6 alkoxy;
• pyridinyl, indolyl, quinolyl or furanyl;
• or a pharmaceutically acceptable salt thereof.

A pharmaceutical composition for the treatment of organ and tissue transplant rejection and autoimmune diseases which comprises a pharmaceutical carrier and an effective amount of a compound having the formula:

• ##STR6## wherein:
• R.sup.1 and R.sup.2 are independently H or --COOR.sup.3 but both R.sup.1 and R.sup.2 cannot be H, and
• R.sup.3 is C.sub.1 -C.sub.6 alkyl where 1 to 3 hydrogens may be replaced by fluorine, chlorine, bromine or iodine, C.sub.3 -C.sub.8 cycloalkyl, C.sub.2 -C.sub.6 alkenyl, or Ar--(CH.sub.2).sub.n --where n is 0 to 6 and Ar is phenyl, phenyl substituted by fluorine, chlorine, bromine, iodine, trifluoromethyl, nitro, cyano, C.sub.1 -C.sub.6 alkyl or C.sub.1 -C.sub.6 alkoxy;
• pyridinyl, indolyl, quinolyl or furanyl;
• or a pharmaceutically acceptable salt thereof.