Cyclic peptide antifungal agents

Details Cyclic peptide antifungal agents Cyclic peptide antifungal agents

C - Chemistry, Metallurgy

07

K

C07K 7/56 (2006.01) A61K 38/12 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2217048

Provided are pharmaceutical formulations, and methods of inhibiting fungal and parasitic activity using a compound of formula (I) wherein: R' is hydrogen, methyl or NH2C(O)CH2-; R" and R''' are independently methyl or hydrogen; Rx1, Rx2, Ry1, Ry2, Ry3, and Ry4 are independently hydroxy or hydrogen; R0 is a group of formula (1); R1 is C1-C6 alkyl, C1-C6 alkoxy, phenyl, p-halo-phenyl, p-nitrophenyl, phenoxy, benzyl, p-halo-benzyl, or p-nitro-benzyl; and R2 is an acyl side chain as defined herein.

On décrit des formulations, pharmaceutiques et des procédés permettant d'inhiber une activité fongique et parasitaire à l'aide d'un composé de formule (I) où R' représente hydrogène, méthyle ou NH¿2?C(O)CH¿2?-; R" et R''' représentent indépendemment méthyle ou hydrogène; R?x1¿, R?x2¿, R?y1¿, R?y2¿, R?y3¿ et R?y4¿ représentent indépendemment hydroxy ou hydrogène; R?0¿ représente un groupe de formule (1); R¿1? représente alkyle C¿1?-C¿6?, alcoxy C¿1?-C¿6?, phényle, p-halo-phényle, p-nitrophényle, phénoxy, benzyle, p-halo-benzyle ou p-nitro-benzyle; et R¿2? représente une chaîne latérale acyle correspondant à la définition.

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