CYCLOHEXAPEPTIDE COMPOUNDS, PROCESS FOR THEIR PRODUCTION AND THEIR USE AS A PHARMACEUTICAL

摘要

A cyclohexapeptide compound of general formula (I), wherein R¹ is C₁-C₂₀ alkyl; C₉-C₂₀ alkenyl; C₉-C₂₀ alkoxyphenyl; an aryl group selected from: phenyl, biphenyl, terphenyl and naphthyl; C₁-C₁₂ alkylphenyl, C₂-C₁₂ alkenylphenyl, C₁-C₁₂ alkoxyphenyl; linoleoyl; palmitoyl; 12-methylmyristoyl; 10,12-dimethylmyristoyl; or -COC₆H₄(p)OC₈H₁₇, R₁ and R₃ are independently -OH; -CN; -CH₂NH₂; -N₃; aryl; substituted aryl; heterocyclyl and substituted heterocyclic with 1-3 of the same or different heteroatoms; aminoalkylamino; mono or di-substituted linear or cyclic aminoalkylamino; -OR, wherein, R is C₁-C₁₂ alkyl; substituted alkyl of the type -(CH₂)_n-X, where n is 1-5 and X is Cl, Br, I, COOY, CN, NH₂ or a heterocyclic and where Y is C₁-C₆ linear or branched alkyl; C₂-C₁₂-alkenyl; aryl; fused aryl; substituted aryl; a heterocyclic containing 1-3 heteroatoms; mono or di-substituted aminoalkyl; or a hydroxy protecting group; and R₃ may additionally be imidazolyl; R₂ and R₄ are independently -H or -OH; R₅ is -H or -CH₃, R₆ is -H, -CH₃ or -CH₂CONH₂. R₇ is -H, -CH₃ or -OH. R₈ and R₉ are independently -H or -CH₂-Sec.amine in which the sec.amine is attached to -CH₂ through its N linkage; and its pharmaceutically acceptable salts. The compounds are useful as antifungal agents.