Inhibitors of prenyl-protein transferase
    1.
    发明授权
    Inhibitors of prenyl-protein transferase 失效
    异戊烯基蛋白转移酶的抑制剂

    公开(公告)号:US06355643B1

    公开(公告)日:2002-03-12

    申请号:US09516757

    申请日:2000-03-01

    IPC分类号: A61K31496

    CPC分类号: C07D233/64 A61K31/496

    摘要: The present invention comprises unsubstituted and substituted piperazine-containing compounds having alkanoyl, alkylsulfonyl, alkylamido or alkoxycarbonyl substituents, and having the formula A, which inhibit prenyl-protein transferases. In particular, the invention relates to prenyl-protein transferase inhibitors which are efficacious in vivo as inhibitors of geranylgeranyl-protein transferase type I (GGTase-I) and that inhibit the cellular processing of both the H-Ras protein and the K4B-Ras protein. Such therapeutic compounds are useful in the treatment of cancer.

    摘要翻译: 本发明包括具有烷酰基,烷基磺酰基,烷基酰氨基或烷氧基羰基取代基的未取代和取代的含哌嗪化合物,并且具有抑制异戊烯基 - 蛋白质转移酶的式A。 特别地,本发明涉及在体内作为er牛儿基ger牛蛋白转移酶I型(GGTase-I)抑制剂有效的异戊烯基 - 蛋白转移酶抑制剂,并且抑制H-Ras蛋白和K4B-Ras蛋白两者的细胞加工 。 这些治疗化合物可用于治疗癌症。