Orally active azole derivatives

Details Orally active azole derivatives Orally active azole derivatives

C - Chemistry, Metallurgy

07

D

C07D 413/06 (2006.01) A01N 43/653 (2006.01) A01N 43/76 (2006.01) A01N 43/84 (2006.01) A01N 47/12 (2006.01) C07D 233/60 (2006.01) C07D 233/61 (2006.01) C07D 249/08 (2006.01) C07D 303/38 (2006.01) C07D 403/12 (2006.01) C07D 405/12 (2006.01) C07D 407/12 (2006.01) C07D 521/00 (2006.01)

Patent

CA 2129455

The present invention relates to new orally active azole derivatives with antifungal activity of formula I Image 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 formula I' Image 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 Cl-C4-alkyl, phenyl-C1-C4-alkyl or optionally substituted phenyl; when Z is -C(=O)-, R2 is optionally susbtituted phenyl, naphtyl, or an heterocycle; when Z is -SO2-, R2 is C1-4 alkyl, phenyl-C1-4-alkyl or optionally susbtituted phenyl.

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