Terbenzimidazoles useful for medical therapy (topoisomerase...

C - Chemistry – Metallurgy – 07 – D

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C07D 235/18 (2006.01) A61K 31/415 (2006.01) C07D 401/14 (2006.01)

Patent

CA 2278452

The invention provides a topoisomerase poision of formula (I) wherein Ar is aryl or a nitrogen-, sulfur- or oxygen-containing heteroaromatic group; X is H, CN, CHO, OH, acetyl, CF3, O(C1-C4)alkyl, NO2, NH2, halogen or halo-(C1- C4)alkyl; each Y is individually H, (C1-C4)alkyl or aralkyl; Y' is phenyl, or methoxyphenyl; n is 0 or 1; and each Z is individually H, (C1-C4)alkyl, halogen or halo(C1-C4)alkyl; or a pharmaceutically acceptable salt thereof; for use in medical therapy (e.g. the treatment of fungal infection or cancer). The invention also provides novel compounds of formula (I); pharmaceutical compositions comprising compounds of formula (I); and therapeutic methods, comprising treating fungal infection or treating cancer by administering at least one compound of formula (I).

L'invention concerne un inhibiteur de topoisomérase de la formule (I) dans laquelle Ar représente un aryle ou un groupe hétéroaromatique contenant de l'azote, du soufre ou de l'oxygène; X représente H, CN, CHO, OH, un acétyle, CF¿3?, O(C¿1?-C¿4?)alkyle, NO¿2?, NH¿2?, un halogène ou un halo-(C¿1?-C¿4?)alkyle; chaque Y représente individuellement H, (C¿1?-C¿4?)alkyle ou un aralkyle; Y' représente un phényle, ou un méthoxyphényle; n représente 0 ou 1, et chaque Z représente individuellement H, (C¿1?-C¿4?)alkyle, un halogène ou un halo(C¿1?-C¿4?)alkyle; ou un sel du composé de la formule (I) acceptable du point de vue pharmaceutique, et est destinée à être utilisée dans un traitement médical (par exemple dans le traitement d'une infection mycosique ou d'un cancer). L'invention concerne également de nouveaux composés de la formule (I), des compositions pharmaceutiques comprenant des composés de la formule (I), et des méthodes thérapeutiques, comprenant le traitement d'une infection mycosique ou d'un cancer par administration d'au moins un composé de la formule (I).

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