Triazole antifungal agents

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 401/14 (2006.01) A01N 43/653 (2006.01) A01N 43/74 (2006.01) A01N 43/84 (2006.01) C07D 413/14 (2006.01) C07D 417/14 (2006.01) C07D 521/00 (2006.01)

Patent

CA 1306253

Abstract Title: Antifungal Agents An antifungal agent of the formula:- Image ----- (I) where R is a phenyl group optionally substituted by 1 to 3 substituents each independently selected from halo and CF3; R1 is either (a) a phenyl group substituted by a group of the formula -N=CH-N(Cl-C4 alkyl)2, Image or Image or (b) a 5- or 6-membered aromatic heterocyclic group which is optionally benzo-fused and optionally substituted by 1 or 2 substituents each independently selected from halo, Cl-C4 alkyl and halo-(Cl or C2 alkyl), said heterocyclic group being attached to the nitrogen atom of the piperazine ring by a carbon atom; and R2 is H or CH3 ; PLC 459 or an O-ester or O-ether thereof which is a C2-C4 alkanoyl or benzoyl ester, or a Cl-C4 alkyl, C2-C4 alkenyl, phenyl-(Cl-C4 alkyl) or phenyl ether, said phenyl and benzoyl groups of said O-esters and O-ethers being optionally substituted by one or two substituetns each selected from Cl-C4 alkyl, halo and halo-(Cl or C2 alkyl); or a pharmaceutically acceptable salt thereof. PLC 459

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