Inhibitors of farnesyl-protein transferase

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

C - Chemistry, Metallurgy

07

D

C07D 233/64 (2006.01) A61K 31/395 (2006.01) A61K 31/40 (2006.01) A61K 31/415 (2006.01) A61K 31/44 (2006.01) C07D 207/09 (2006.01) C07D 213/38 (2006.01) C07D 233/54 (2006.01) C07D 401/00 (2006.01) C07D 401/14 (2006.01) C07D 403/06 (2006.01) C07D 403/14 (2006.01) C07D 405/00 (2006.01) C07D 409/00 (2006.01) C07D 413/00 (2006.01) C07D 417/00 (2006.01) C07D 471/04 (2006.01) C07D 495/04 (2006.01)

Patent

CA 2223561

The present invention comprises low molecular weight peptidyl compounds that inhibit the farnesyl-protein transferase. Furthermore, these compounds differ from the mono- or dipeptidyl analogs 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.

L'invention porte sur des composés peptidyliques de faible poids moléculaire inhibiteurs de la farnésyl transférase. Lesdits composés diffèrent de leurs analogues mono et di-peptidilyques préalablement décrits comme inhibiteurs de la farnésyl transférase en ce qu'ils ne présentent pas de fraction thiol. Cette absence de thiol offre de grands avantages: amélioration du comportement pharmacocinétique chez l'animal, prévention des réactions chimiques suscitées par le thiol tels qu'une auto-oxydation rapide et la formation de bisulfure avec les thiols endogènes, ainsi que réduction de la toxicité systémique. L'invention porte également sur des compositions chimiothérapeutiques contenant lesdits inhibiteurs, et leurs procédés d'obtention.

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