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) C07D 207/09 (2006.01) C07D 211/34 (2006.01) C07D 223/04 (2006.01) C07D 403/00 (2006.01) C07K 5/065 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2201350

The present invention comprises analogs of the CA1A2X motif of the protein Ras that is modified by farnesylation in vivo. These CA1A2X analogs inhibit the farnesylation of Ras. Furthermore, these CA1A2X analogs differ from those previously described as inhibitors of Ras farnesly transferase in that they have a prolyl like moiety in the A1 position. Further contained in this invention are chemotherapeutic compositions containing these farnesyl transferase inhibitors and methods for their production.

La présente invention comprend des analogues du motif CA1A2X de la protéine Ras qui est modifiée par farnésylation in vivo. Ces analogues de CA1A2X inhibent la farnésylation de Ras. De plus, ces analogues de CA1A2X diffèrent de ceux qui ont antérieurement été décrits comme des inhibiteurs de la Ras farnésyl-transférase du fait que la fraction apparentée à la prolyle est dans la position A1. De plus, la présente invention porte également sur des compositions chimiothérapeutiques contenant ces inhibiteurs de la farnésyl-transférase et sur les méthodes de production de ces dernières.

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