Rapamycin oximes

Details Rapamycin oximes Rapamycin oximes

C - Chemistry, Metallurgy

07

H

C07H 17/00 (2006.01) A61K 31/70 (2006.01)

Patent

CA 2046105

AHP-9665 ABSTRACT A derivative of rapamycin in which the 27-position has the structure Image wherein R1 is hydrogen, alkyl, or -CH2Ar; A1 is Image , Image , Image , or Image ; wherein R2, R3, and R4 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.

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