C - Chemistry – Metallurgy – 07 – K
Patent
C - Chemistry, Metallurgy
07
K
C07K 7/56 (2006.01) A61K 38/12 (2006.01) A61K 38/00 (2006.01)
Patent
CA 2220944
Provided are pharmaceutical formulations, and methods of inhibiting fungal and parasitic activity using a compound of formula (I), wherein R', R", R''', Rx1, Rx2, Ry1, Ry2, Ry3, Ry4 and R0 are as defined hereinabove; and R2 is (i); R3 is (ii), (iii), (iv) or (v); R3a, R3b, R3c and R3d are independently hydrogen, C1-12 alkyl, C2-C12 alkynyl, C1-C12 alkoxy, C1-C12 alkylthio, halo, or -O- (CH2)m-[O-(CH2)n]p-O-(C1-C12 alkyl) or -O-(CH2)q-X-R4; m is 2, 3 or 4; n is 2, 3, or 4; p is 0 or 1; q is 2, 3, or 4; X is pyrrolidino, piperidino or piperazino; and R4 is hydrogen, C1-C12 alkyl, C3-C12 cycloalkyl, benzyl or C3- C12-cycloalkylmethyl; or a pharmaceutically acceptable salt thereof.
L'invention se rapporte à des formulations pharmaceutiques et à des procédés d'inhibition de l'activité fongique et parasite au moyen d'un composé de la formula (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 dans cette formule; et R?2¿ représente (i); R?3¿ représente (ii), (iii), (iv) ou (v); R?3a¿, R?3b¿, R?3c¿ et R?3d¿ représentent indépendamment hydrogène, alkyle en C¿1?-¿12?, alkynyle en C¿2?-C¿12?, alcoxy en C¿1?-C¿12?, alkylthio en C¿1?-C¿12?, halo ou -O-(CH¿2?)¿m?-[O-(CH¿2?)¿n?]¿p?-O-(alkyle en C¿1?-C¿12?) ou -O-(CH¿2?)¿q?-X-R?4¿: m vaut 2, 3 ou 4; n vaut 2, 3 ou 4; p vaut 0 ou 1; q vaut 2, 3, ou 4; X représente pyrrolidino, pipéridino or pipérazino; R?4¿ représente hydrogène, alkyle en C¿1?-C¿12?, cycloalkyle en C¿3?-C¿12?, benzyle ou cycloalkylméthyle en C¿3?-C¿12?; ou d'un sel pharmaceutiquement acceptable de ce composé.
Jamison James Andrew
Rodriguez Michael John
Eli Lilly And Company
Gowling Lafleur Henderson Llp
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