Inhibitors of farnesyl-protein transferase

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

C - Chemistry, Metallurgy

07

K

C07K 5/04 (2006.01) A61K 31/40 (2006.01) A61K 31/415 (2006.01) A61K 31/44 (2006.01) A61K 38/04 (2006.01) C07D 207/28 (2006.01) C07D 213/81 (2006.01) C07D 213/82 (2006.01) C07D 233/54 (2006.01) C07D 233/64 (2006.01) C07D 233/90 (2006.01) C07D 405/12 (2006.01) C07K 5/02 (2006.01) C07K 5/097 (2006.01) C07K 5/117 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2172125

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 farnsylation of Ras. Furthermore, these CAAX analogs differ from those previously described as inhibitors of Ras farnsyl 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 are chemotherapeutic compositions containing these farnesyl transferase inhibitors and methods for their production.

L'invention concerne des analogues de la séquence CAAX de la protéine Ras modifiée par farnésylation in vivo. Ces analogues de CAAX inhibent la farnésylation de Ras et se distinguent, par ailleurs, de celles décrites précédemment en tant qu'inhibiteurs de la Ras farnésyl-transférase par le fait qu'ils ne comprennent pas de fraction thiol. L'absence de thiol présente des avantages uniques en termes de comportement pharmacocinétique amélioré chez l'animal, de prévention des réactions chimiques dues au thiol telles que l'autoxydation et la formation de bisulfure avec des thiols endogènes, et de toxicité systémique réduite. L'invention concerne également des compositions chimiothérapeutiques contenant ces inihibiteurs de la farnésyl-transférase et leurs procédés de production.

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