Inhibitors of farnesyl-protein transferase

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

C - Chemistry, Metallurgy

07

C

C07C 323/58 (2006.01) A61K 31/13 (2006.01) A61K 31/16 (2006.01) A61K 31/27 (2006.01) A61K 31/275 (2006.01) A61K 31/325 (2006.01) A61K 31/33 (2006.01) C07C 323/59 (2006.01) C07D 209/20 (2006.01) C07D 211/76 (2006.01) C07D 213/56 (2006.01) C07D 215/14 (2006.01) C07D 217/16 (2006.01) C07D 233/54 (2006.01) C07D 233/64 (2006.01) C07D 277/30 (2006.01) C07D 333/24 (2006.01) C07D 405/12 (2006.01) C07D 405/14 (2006.01) C07D 409/12 (2006.01) C07D 417/12 (2006.01) C07D 471/04 (2006.01) C07D 495/04 (2006.01)

Patent

CA 2216564

The present invention comprises peptidomimetic compounds which comprise a suitably substituted aminoalkylbenzamide moiety. The instant compounds inhibit the farnesyl protein transferase enzyme and the farnesylation of certain proteins. Furthermore, the instant farnesyl protein transferase inhibitors 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.

L'invention porte sur des composés peptidomimétiques comportant une fraction aminoalkylbenzamide adéquatement substituée. Ces composés instantanés inhibent la farnésyl-protéine transférase et la farnésylation de certaines protéines. De plus, ces inhibiteurs instantanés de farnésyl-protéine transférase différent de ceux préalablement décrits en ce qu'ils ne présentent pas de fraction thiol. Cette absence de thiol offre des avantages uniques en terme de comportement pharacocinétique amélioré chez l'animal, de prévention des réactions chimiques liées au thiol telles que la rapidité d'auto-oxydation ou la formation de disulfures avec des thiols endogènes, et une toxicité systémique réduite. L'invention porte également sur des compositions chimiothérapeutiques contenant lesdits inhibiteurs de farnésyl-protéine transférase et leurs procédés de production.

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