C - Chemistry – Metallurgy – 07 – H
Patent
C - Chemistry, Metallurgy
07
H
C07H 19/24 (2006.01) A61K 31/70 (2006.01) A61K 38/05 (2006.01) C07K 5/06 (2006.01)
Patent
CA 2051782
AHP-9675/9675-1-N1 ABSTRACT A compound of the structure Image wherein R1 and R2 are each, independently, hydrogen or Image with the proviso that R1 and R2 are not both hydrogen; R3 is hydrogen, alkyl, aralkyl, -(CH2)qCO2R6, -(CH2)r,NR7CO2R8, carbamylalkyl, aminoalkyl, hydroxyalkyl, guanylalkyl, mercaptoalkyl, alkylthioalkyl, indolylmethyl, hydroxyphenylmethyl, imidazoylmethyl or phenyl which is optionally mono-, di-, or tri-substituted with a substituent selected from alkyl, alkoxy, hydroxy, cyano, halo, nitro, carbalkoxy, trifluoromethyl, amino, or a carboxylic acid; R4 and R7 are each, independently, hydrogen, alkyl, or aralkyl; R5, R6, and R8 are each, independently, alkyl, aralkyl, fluorenylmethyl, or phenyl which is optionally mono-, di-, or tri-substituted with a substituent selected from alkyl, alkoxy, hydroxy, cyano, halo, nitro, carbalkoxy, trifluoromethyl, amino, or a carboxylic acid; m is 0-4; n is 0-4; AHP-9675/9675-1-Nl p is 1-2; q is 0-4; r is 0-4; wherein R3, R4, m, and n are independent in each of the Image subunits when p = 2; or a pharmaceutically acceptable salt thereof, which by virtue of its immuno- suppressive activity is useful in treating transplantation rejection, host vs. graft disease, autoimmune diseases, and diseases of inflammation, and by virtue of its antifungal activity is useful in treating fungal infections.
Caufield Craig E.
Failli Amedeo A.
Steffan Robert J.
American Home Products Corporation
Ridout & Maybee Llp
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