Triazole derivatives having antimycotic activity

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 249/08 (2006.01) A01N 43/653 (2006.01) A61K 31/41 (2006.01) A61K 31/44 (2006.01) A61K 31/495 (2006.01) C07C 251/32 (2006.01) C07C 251/42 (2006.01) C07C 251/54 (2006.01) C07D 213/53 (2006.01) C07D 233/61 (2006.01) C07D 295/13 (2006.01) C07D 303/36 (2006.01) C07D 401/12 (2006.01) C07D 403/12 (2006.01) C07D 405/12 (2006.01) C07D 521/00 (2006.01)

Patent

CA 2141782

Novel triazole derivatives represented by the formula (I): Image (I) (where Ar is a phenyl group substituted by 1 or 2 halogen atoms; R1 and R2 are typically such that, when taken together with the adjacent carbon atom, they form a cyclopropylidene group; R3 is a straight-chained, branched or cyclic alkyl group having 1 - 4 carbon atoms; R4 is typically an optionally substituted straight-chained or branched alkyl group having 1 - 4 carbon atoms; and the wavy line represents either an E- or Z-type bond) or salts thereof. The triazole derivatives exhibit a marked therapeutic effects not only in in vitro experiments but also in vivo experiments using laboratory animal models such as Aspergillus infected mice. The derivatives are also safe to use. Therefore, they are extremely useful as therapeutics for various superficial dermatomycoses, deep dermatomycoses and deep mycoses (mycoses in internal organs).

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