[EN] SUBSTITUTED BICYCLIC PYRIMIDINE-BASED COMPOUNDS AND COMPOSITIONS AND USES THEREOF<br/>[FR] COMPOSÉS BICYCLIQUES SUBSTITUÉS À BASE DE PYRIMIDINE, COMPOSITIONS ET UTILISATIONS ASSOCIÉES
申请人:THE ROYAL INSTITUTION FOR THE ADVANCEMENT OF LEARNING / MCGILL UNIV
公开号:WO2018137036A1
公开(公告)日:2018-08-02
Novel C-2-substituted bicyclic compounds of Formula I have been prepared and found to be useful as potent inhibitors of hGGPPS by inhibiting geranylgeranylation of proteins and inhibiting the biosynthesis of GGPP. The application is directed to these compounds, to compositions comprising these compounds, and to their use, in particular as medicaments for use in the treatment of cancer and other conditions which are treatable by inhibiting human geranylgeranylation pyrophosphate hGGPPS activity.
已经制备了Formula I的新型C-2取代双环化合物,并发现它们作为hGGPPS的有效抑制剂,通过抑制蛋白质的戊二烯基酰基化和抑制GGPP的生物合成而被发现是有用的。该申请涉及这些化合物,包括这些化合物的组合物,以及它们的用途,特别是作为用于治疗癌症和其他可通过抑制人类戊二烯基酰基化焦磷酸盐hGGPPS活性的药物。