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    • 9. 发明申请
    • PRODUCT CONTAINING AT LEAST ONE PHOSPHATASE CDC25 INHIBITOR COMBINED WITH AT LEAST ONE OTHER ANTICANCER AGENT
    • 含有至少一种磷酸酯酶的产品CDC25抑制剂与至少一种其他抗感染剂
    • WO2005000852A3
    • 2005-06-30
    • PCT/FR2004001586
    • 2004-06-24
    • SOD CONSEILS RECH APPLICPREVOST GREGOIREBREZAK PANNETIER MARIE-CHRISTIDIOLEZ CHRISTIAN
    • PREVOST GREGOIREBREZAK PANNETIER MARIE-CHRISTINEDIOLEZ CHRISTIAN
    • A61K45/06A61P35/00C07D263/56C07D263/57C07D277/66C07D413/04C07D413/12C07D417/04C07D417/12C07D519/00A61K31/425A61K31/42C07D277/64
    • A61K45/06C07D519/00
    • The invention relates to a product containing at least one phosphatase Cdc25 inhibitor combined with at least one other anticancer agent for simultaneous, separate or staggered therapeutic use during treatment for cancer. According to the invention, the other anticancer agent is preferably selected from: DNA base analogs such as 5-fluorouracil; inhibitors of type I and/or type II topoisomerases, such as camptothecin and the analogs thereof, doxorubicin or amsacrine; compounds interacting with the cellular spindle, for example, paclitaxel (Taxol); compounds acting on the cytoskeleton, such as vinblastine; inhibitors of the transduction of the signal passing via the heterotrimeric G proteins; prenyltransferase inhibitors, and especially farnesyltransferase inhibitors; cyclin-dependent kinase (CDKs) inhibitors; alkylating agents such as cisplatin; folic acid antagonists such as methotrexate; and inhibitors of DNA synthesis and cellular division, such as mitomycin C. The invention also relates to (1R)-1-[({(2R)-2-amino--3-[(8S)-8-(cyclohexylmethyl)-2-phenyl-5,6-dihydroimidazo[1,2-a]pyrazin-7(8H)-yl]--3-oxopropyl}dithio)methyl]-2-[(8S)-8-(cyclohexylmethyl)-2-phenyl--5,6-dihydroimidazo[1,2-a]pyrazin-7(8H)-yl]-2-oxoethylamine, or the pharmaceutically acceptable salts thereof, that can be used as anticancer agents.
    • 本发明涉及含有至少一种磷酸酶Cdc25抑制剂与至少一种其他抗癌剂组合的产品,用于癌症治疗期间的同时,分离或交错的治疗用途。 根据本发明,其它抗癌剂优选选自:DNA碱基类似物,如5-氟尿嘧啶; I型和/或II型拓扑异构酶的抑制剂,如喜树碱及其类似物,多柔比星或amsacrine; 与细胞纺锤体相互作用的化合物,例如紫杉醇(紫杉醇); 作用于细胞骨架的化合物,如长春花碱; 通过异源三聚体G蛋白的信号转导的抑制剂; 异戊烯转移酶抑制剂,特别是法呢基转移酶抑制剂; 细胞周期蛋白依赖性激酶(CDKs)抑制剂; 烷化剂如顺铂; 叶酸拮抗剂如甲氨蝶呤; 以及DNA合成和细胞分裂的抑制剂,例如丝裂霉素C.本发明还涉及(1R)-1 - [({(2R)-2-氨基-3 - [(8S)-8-(环己基甲基) 2-苯基-5,6-二氢咪唑并[1,2-a]吡嗪-7(8H) - 基] - 3-氧代丙基}二硫代)甲基] -2 - [(8S)-8-(环己基甲基)-2 - 苯基-5,6-二氢咪唑并[1,2-a]吡嗪-7(8H) - 基] -2-氧代乙基胺或其药学上可接受的盐,可用作抗癌剂。