| 摘要 |
The present invention relates to new orally active azole derivatives with antifungal activity of formula I <IMAGE> I wherein: X is CH or N; Ar represents phenyl substituted with halogen and/or trifluoromethyl; Z is -C(=O)- or -SO2-; R1 is CN, CO2H, CO2R7, CONR8R9 or CH2Y and then R3 is hydrogen, or R1 together with R3 forms a ring of formmula I' <IMAGE> I' wherein B is O, hydroxy or hydrogen; R4 is C1-4 alkyl; R5, R6, R8 and R9 are hydrogen or C1-4 alkyl; Y is -OH,-OR7, -OC(=O)R7, -NR8R9, -NHC(=O)OR7; R7 is C1-C4-alkyl, phenyl-C1-C4-alkyl or optionally substituted phenyl; when Z is -C(=O)-, R2 is optionally substituted phenyl, or naphtyl; when Z is -SO2-, R2 is C1-4 alkyl, phenyl-C1-4-alkyl or optionally substituted phenyl.
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