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Analogs of indole-3-carbinol metabolites as chemotherapeutic and chemopreventive agents

机译:吲哚-3-甲醇代谢产物的类似物作为化学治疗和化学预防剂

摘要

Novel compounds useful as chemotherapeutic and chemopreventive agents are provided. The compounds are analogs of indole-3-carbinol metabolites wherein the structures and substituents of the compounds are selected to enhance the compounds' overall efficacy, particularly with respect to therapeutic activity, oral bioavailability, long-term safety, patient tolerability, and therapeutic window. The compounds are useful not only in treatment of cancer but also in prevention of cancer. One preferred class of the novel compounds has the structure of formula (IV); embedded image wherein:R1, R2, R3, R4, R5, R6, R7, R8, R5A, R6A, R7A, R8A, R22 and R23 are defined herein. Pharmaceutical compositions are provided as well, as are methods of synthesis and use.
机译:提供了用作化学治疗剂和化学预防剂的新型化合物。化合物是吲哚-3-甲醇代谢物的类似物,其中选择化合物的结构和取代基以增强化合物的整体功效,特别是在治疗活性,口服生物利用度,长期安全性,患者耐受性和治疗范围方面。该化合物不仅可用于治疗癌症,而且可用于预防癌症。一类优选的新型化合物具有式(IV)的结构; “嵌入式图像” 其中: R 1 ,R 2 ,R < Sup> 3 ,R 4 ,R 5 ,R 6 ,R 7 ,R < Sup> 8 ,R 5A ,R 6A ,R 7A ,R 8A ,R <在此定义了Sup> 22 和R 23 。还提供了药物组合物,以及合成和使用方法。

著录项

  • 公开/公告号US7666897B2

    专利类型

  • 公开/公告日2010-02-23

    原文格式PDF

  • 申请/专利权人 LING JONG;WAN-RU CHAO;

    申请/专利号US20080205532

  • 发明设计人 LING JONG;WAN-RU CHAO;

    申请日2008-09-05

  • 分类号A61K31/40;C07D209;

  • 国家 US

  • 入库时间 2022-08-21 18:49:04

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