Inhibitors of geranylgeranyl-protein transferase

Details Inhibitors of geranylgeranyl-protein transferase Inhibitors of geranylgeranyl-protein transferase

C - Chemistry, Metallurgy

07

K

C07K 5/08 (2006.01) A61K 31/195 (2006.01) A61K 31/22 (2006.01) A61K 38/06 (2006.01) C07C 323/25 (2006.01) C07C 323/41 (2006.01) C07K 5/083 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2180528

The compounds disclosed are analogs of the CAAX motif of proteins that can be modified by geranylgeranylation vivo that selectively inhibit the geranylgeranylation of several proteins. The relatively poor activity of the compounds against the farnesyl protein transferase, which modifies several proteins important in cellular replication, allows the use of the compounds of the instant invention to treat diseases which are regulated by the function of a geranylgeranylated protein, such as certain cancers and inflammatory diseases. Further contained in this invention are chemotherapeutic compositions containing these geranylgeranyl protein transferase type I inhibitors and methods for their production.

Les composés décrits sont des analogues du motif CAAX de protéines pouvant être modifiées par géranylgéranylation in vivo, qui inhibent sélectivement la géranylgéranylation de plusieurs protéines. L'activité relativement faible desdits composés contre la farnésyle-protéine transférase, qui modifie plusieurs protéines importantes dans la réplication cellulaire, permet l'utilisation des composés de la présente invention pour traiter des maladies qui sont régulées par la fonction d'une protéine géranylgéranylée, telle que dans certains cancers et certaines maladies imflammatoires. Des compositions chimiothérapeutiques contenant lesdits inhibiteurs de géranylgéranyle-protéine transférase de type I et des procédés de production desdites compositions sont également décrits.

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