Cyclic peptide antifungal agents

C - Chemistry – Metallurgy – 07 – K

Patent

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Details

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

Patent

CA 2220688

Provided are pharmaceutical formulations, and methods of inhibiting fungal and parasitic activity using a compound of formula (I), where R', R", R''', Rx1, Rx2, Ry1, Ry2, Ry3, Ry4 and R0 are as defined hereinabove; and R2 is (II), or (III); R3 is (IV), or (V); R3a is C1-C6 alkyl or C1-C6 alkoxy; R3b and R3c are independently phenyl or naphthyl; R3d is C1-C12 alkyl, C1-C12 alkoxy or -O- (CH2)m-[O-(CH2)n]p-O-(C1-C12 alkyl);m is 2, 3 or 4; n is 2, 3 or 4; p is 0 or 1; or a pharmaceutically acceptable salt thereof.

L'invention porte sur des formulations pharmaceutiques et des procédés qui permettent de bloquer l'activité fongique et parasitaire grâce à un composé de la formule (I), dans laquelle R', R", R''', R?x1¿, R?x2?, R?y1¿, R?y2¿, R?y3¿, R?y4¿ et R?0¿ sont tels que définis ci-dessus; et R?2¿ représente (II), ou (III); R?3¿ représente (IV), ou (V); R?3a¿ représente C¿1?-C¿6? alkyle ou C¿1?-C¿6? alcoxy; R?3b¿ et R?3c¿ représentent indépendamment phényle ou naphtyle; R?3d¿ représente C¿1?-C¿12? alkyle, C¿1?-C¿12? alcoxy ou -O-(CH¿2?)¿m?-[O-(CH¿2?)¿n?]¿p?-O-(C¿1?-C¿12? alkyle); m vaut 2, 3, ou 4; n vaut 2, 3, ou 4: p vaut 0 ou 1; ou un de ses sels acceptables sur le plan pharmaceutique.

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