Kinesin inhibitors as cancer therapeutics

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 233/64 (2006.01) A61K 31/417 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2708822

The invention provides novel imidazole compounds that inhibit the activity of kinesin spindle protein (KSP, also called Eg5). Inhibitors of KSP can reduce undesired cellular proliferation and provide other therapeutic effects. The invention also provides pharmaceutical compositions containing these novel compounds, and methods of using the novel KSP inhibitors and their pharmaceutical compositions to treat various types of cancers. The compounds, compositions and methods of the invention are especially useful for treating certain classes of cancers that are resistant to conventional drug treatments, because such cancers are shown to remain sensitive to the compounds of the invention.

L'invention porte sur de nouveaux composés imidazoles qui inhibent l'activité de protéine du fuseau kinésine (KSP, également appelée Eg5). Des inhibiteurs de KSP peuvent réduire une prolifération cellulaire non souhaitée et fournir d'autres effets thérapeutiques. L'invention porte également sur des compositions pharmaceutiques contenant ces nouveaux composés, et sur des procédés d'utilisation des nouveaux inhibiteurs de KSP et de leurs compositions pharmaceutiques pour traiter divers types de cancers. Les composés, compositions et procédés de l'invention sont particulièrement utiles pour traiter certaines classes de cancers qui sont résistants à des traitements par les médicaments classiques, en raison du fait qu'il a été démontré que de tels cancers restent sensibles aux composés de l'invention.

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