Rapamycin hydrazones

Details Rapamycin hydrazones Rapamycin hydrazones

C - Chemistry, Metallurgy

07

H

C07H 17/00 (2006.01) A61K 31/70 (2006.01) C07D 498/18 (2006.01)

Patent

CA 2046102

AHP-9722 ABSTRACT A compound of the structure Image wherein R1 is hydrogen, alkyl or aralkyl; R2 is hydrogen, alkyl, cycloalkyl, aralkyl, -COR3,- CO2R3, -SO2R3, -CONR4R5, -CSNR4R5, -COCONR4R5, or Ar; R3 is alkyl, aralkyl, or Ar; R4 and R5 are each, independently, hydrogen, alkyl, cycloalkyl, allyl, aralkyl, or Ar; Ar is , , Image , Image Image , , or Image ; R6, R7, R8 are each, independently, hydrogen, alkyl, alkoxy, hydroxy, cyano, halo, nitro, carbalkoxy, trifluoromethyl, trifluoromethoxy, amino, or a carboxylic acid; X is CH or N; Y is NH, O, or S; or a pharmaceutically acceptable salt thereof, which by virtue of its immunosuppressive activity is useful in treating transplantation rejection, host vs. graft disease, autoimmune diseases and diseases of inflammation; by virtue of its antitumor activity is useful in treating solid tumors; and by virtue of its antifungal activity is useful in treating fungal infections.

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