Inhibitors of farnesyl-protein transferase

Details Inhibitors of farnesyl-protein transferase Inhibitors of farnesyl-protein transferase

C - Chemistry, Metallurgy

07

K

C07K 5/062 (2006.01) A61K 38/05 (2006.01)

Patent

CA 2201351

The present invention comprises analogs of the CAAX motif of the protein Ras that is modified by farnesylation in vivo. These CAAX analogs inhibit the farnesylation of Ras. Furthermore, these CAAX analogues differ from those previously described as inhibitors of Ras farnesyl transferase in that they do not have a thiol moiety. The lack of the thiol offers unique advantages in terms of improved pharmacokinetic behavior in animals, prevention of thiol- dependant chemical reactions, such as rapid auto-oxidation and disulfide formation with endogenous thiols, and reduced systemic toxicity. Further contained in this invention are chemotherapeutic compositions containg these farnesyl transferase inhibitors and methods for their production.

La présente invention se rapporte à des analogues du motif CAAX de la protéine Ras qui est modifiée par farnésylation in vivo. Ces analogues de CAAX inhibent la farnésylation de Ras. De plus, ils diffèrent de ceux précédemment décrits se présentant sous forme d'inhibiteurs de farnésyle transférase de Ras modifiée en ce qu'ils ne possèdent pas de fraction thiol. L'absence de thiol offre des avantages uniques sur le plan du comportement pharmacocinétique amélioré chez les animaux, de la prévention des réactions chimiques dépendant de thiol, telle que l'auto-oxydation rapide et la formation de bisulfure avec des thiols endogènes, et de la toxicité systémique réduite. L'invention se rapporte en outre à des compositions chimiothérapeutiques contenant ces inhibiteurs de farnésyle transférase et à leurs procédés de production.

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