Rapamycin oximes
AssigneeAmerican Home Products Corporation
InventorsCraig E. Caufield, Amedeo A. Failli
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Abstract
A derivative of rapamycin in which the 27-position has the structure ##STR1## wherein R.sup.1 is hydrogen, alkyl, or --CH.sub.2 Ar; Ar is ##STR2## wherein R.sup.2, R.sup.3, and R.sup.4 are each, independently, hydrogen, alkyl, aralkyl, alkoxy, hydroxy, cyano, halo, nitro, carbalkoxy, trifluoromethyl, amino, or a carboxylic acid; X is N, O, or S; or a pharmaceutically acceptable salt thereof, which is by virtue of its immunosuppresive activity is useful in treating transplantation rejection host vs. graft disease, autoimmune diseases, and diseases of inflammation.
Claims9
A derivative of rapamycin in which the 27-position has the structure ##STR7## wherein R.sup.1 is hydrogen, alkyl of 1-6 carbon atoms, or --CH.sub.2 Ar;
- Ar is ##STR8## wherein R.sup.2, R.sup.3, and R.sup.4 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, aralkyl of 7-10 carbon atoms, alkoxy of 1-6 carbon atoms, hydroxy, cyano, halo, nitro, carbalkoxy of 2-7 carbon atoms, trifluoromethyl, amino, or a carboxylic acid;
- X is N, O, or S;
- or a pharmaceutically acceptable salt thereof.
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 which is a derivative of rapamycin in which the 27-position has the structure;
- ##STR10## wherein R.sup.1 is hydrogen, alkyl of 1-6 carbon atoms, or --CH.sub.2 Ar;
- Ar is ##STR11## wherein R.sup.2, R.sup.3, and R.sup.4 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, aralkyl of 7-10 carbon atoms, alkoxy of 1-6 carbon atoms, hydroxy, cyano, halo, nitro, carbalkoxy of 2-7 carbon atoms, trifluoromethyl, amino, or a carboxylic acid;
- X is N, O, or S;
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.