Inhibitors of farnesyl-protein transferase

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

C - Chemistry, Metallurgy

07

K

C07K 5/097 (2006.01) A61K 31/40 (2006.01) A61K 31/445 (2006.01) A61K 38/05 (2006.01) A61K 38/06 (2006.01) C07D 207/27 (2006.01) C07D 211/76 (2006.01) C07D 405/12 (2006.01) C07K 5/06 (2006.01) C07K 5/078 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2172126

The present invention comprises analogs of the CAAX motif of the protein Ras that is modified by farnesylation vivo. These CAAX analogs inhibit the farnesylation of Ras. Furthermore, these CAAX analogs differ from those previously described as inhibitors of Ras famesyl transferase in that they do not bave 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.

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, ces analogues de CAAX se distinguent de ceux décrits précédemment comme inhibiteurs de la farnésyle-transférase de RAS, en ce qu'ils ne possèdent pas une fraction thiol. L'absence de thiol offre des avantaes uniques, tels qu'un comportement pharmacocinétique amélioré chez les animaux, la prévention des réactions chimiques dépendantes du thiol, notamment l'autoxydation et la formation de disulfure avec des thiols endogènes, et une toxicité systémique réduite. L'invention se rapporte également à des compositions chimiothérapeutiques contenant ces inhibiteurs de la farnésyle transférase et à leur procédés de production.

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