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    • 1. 发明申请
    • COMPOSITIONS AND METHODS TO IMPROVE THE THERAPEUTIC BENEFIT OF INDIRUBIN AND ANALOGS THEREOF, INCLUDING MEISOINDIGO
    • 组合物和改善靛蓝及其类似物的治疗效果的方法,包括MEISOINDIGO
    • US20160243077A1
    • 2016-08-25
    • US14250958
    • 2014-04-11
    • Dennis M. BROWNIan Nisbet
    • Dennis M. BROWNIan Nisbet
    • A61K31/404A61K45/06C07K16/40C12N15/113A61K31/7056A61K39/395
    • A61K31/404A61K31/7056A61K39/3955A61K45/06C07D209/34C07K16/40C12N15/1137C12N2310/141C12N2320/31
    • The present invention describes methods and compositions for improving the therapeutic efficacy of therapeutically active agents previously limited by suboptimal therapeutic performance by either improving efficacy as monotherapy or reducing side effects. Such methods and compositions are particularly applicable to therapeutically active agents selected from the group consisting of: (i) indirubin; (ii) an analog of indirubin; (iii) a derivative of indirubin or of an analog of indirubin; and (iv) a pharmaceutical composition comprising indirubin, an analog of indirubin, or a derivative of indirubin or of an analog of indirubin, especially meisoindigo. In particular, the therapeutically active agents selected from the group consisting of: (i) indirubin; (ii) an analog of indirubin; (iii) a derivative of indirubin or of an analog of indirubin; and (iv) a pharmaceutical composition comprising indirubin, an analog of indirubin, or a derivative of indirubin or of an analog of indirubin, especially meisoindigo, are effective Nek9 inhibitors. The active agent, such as meisoindigo, can act as a Nek9 inhibitor. The active agent can be used together with Nek9 inhibitors or agents that inhibit the expression of Nek9.
    • 本发明描述了通过改善作为单一疗法或减少副作用的功效而改善先前受次优治疗性能限制的治疗活性剂的治疗功效的方法和组合物。 这些方法和组合物特别适用于选自以下的治疗活性剂:(i)靛玉红; (ii)靛玉红类似物; (iii)靛玉红或靛玉红类似物的衍生物; 和(iv)包含靛玉红,靛玉红类似物或靛玉红衍生物或靛玉红类似物,特别是异靛红的药物组合物。 特别地,选自以下的治疗活性剂:(i)靛玉红; (ii)靛玉红类似物; (iii)靛玉红或靛玉红类似物的衍生物; 和(iv)包含靛玉红,靛玉红类似物或靛玉红衍生物或靛玉红类似物,特别是异靛红的药物组合物是有效的Nek9抑制剂。 活性剂,例如meisoindigo,可以作为Nek9抑制剂。 活性剂可与Nek9抑制剂或抑制Nek9表达的试剂一起使用。