Heterocyclic derivatives

C - Chemistry – Metallurgy – 07 – D

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167/215, 167/235

C07D 261/18 (2006.01) A61K 31/42 (2006.01) A61K 31/535 (2006.01) C07D 413/12 (2006.01)

Patent

CA 2035544

ABSTRACT OF THE DISCLOSURE Compounds of the formula (I): Image (I) wherein R1 is -OR4 (where R4 is hydrogen, lower alkyl, lower hydroxyalkyl, phenyl, phenyl-lower-alkyl, or -(CH2)nY where n is an integer from 1 to 4 and Y is morpholino, -SR5, -C(O)OR5, -C(O)N(R6)2, -N(R6)2, or -N+(R6)3X-, in which R5 is lower alkyl, each R6 is independently selected from hydrogen or lower alkyl, and X is halogen) or -SR7 (where R7 is lower alkyl, phenyl-lower-alkyl, or -(CH2)nW where W is -N(R6)2, or -N+(R6)3X-, and n, R6 and X are as previously defined); or R1-CO- is replaced with -CN; R2 is lower alkyl, phenyl or phenyl-lower-alkyl; R3 is halo, hydroxy, lower alkyl, lower alkoxy, lower haloalkyl, lower haloalkoxy, or -C(O)OR5 where R5 is as previously defined; and 1-FF26960 -19- Z is a bond, 2,5-thienyl or 2,5-furanyl; and pharmaceutically acceptable salts thereof are useful in treating inflammation, autoimmune disease, allograft rejection or related disease states in mammals. 1-FF26960

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