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 31/415 (2006.01) A61K 31/445 (2006.01) A61K 38/05 (2006.01) C07D 401/02 (2006.01) C07D 403/02 (2006.01)

Patent

CA 2201349

The present invention comprises analogs of the CAAX motif of the protein Ras that is modified by farnesylation in vivo. These CAAX analogs inhibit farnesyl- protein transferase. Furthermore, these CAAX analogs differ from those previously described as inhibitors of farnesyl-protein 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-dependent chemical reactions, such as rapid autoxidation and disulfide formation with endogenous thiols, and reduced systemic toxicity. Further contained in this invention are chemotherapeutic compositions containing these farnesyl transferase inhibitors and methods for their production.

Analogues du motif CAAX de la protéine Ras modifiée par farnésylation in vivo. Ces analogues CAAX interdisent la transférase de la farnésyl-protéine. Ils diffèrent en outre de ceux décrits antérieurement en tant qu'inhibiteurs de transférase de la farnésyl-protéine par le fait qu'ils ne comprennent pas de fraction thiol. L'absence de thiol présente des avantages particuliers sur le plan du comportement pharmacocinétique chez les animaux, de la prévention des réactions chimiques dépendantes d'un thiol, telles que l'auto-oxydation rapide et la formation de disulfure avec des thiols endogènes, ainsi qu'une toxicité systémique réduite. L'invention porte également sur des compositions chimiothérapeutiques renfermant de tels inhibiteurs de farnésyl-transférase et sur leurs procédés de production.

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