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    • 16. 发明授权
    • Halogenated triptolide derivatives as immunomodulators and anticancer agents
    • 卤代雷公藤内酯衍生物作为免疫调节剂和抗癌剂
    • US07417069B2
    • 2008-08-26
    • US11210677
    • 2005-08-23
    • Dongcheng DaiJohn H. Musser
    • Dongcheng DaiJohn H. Musser
    • A61K31/36C07D493/14
    • C07D493/22
    • Compounds having the structure I: are useful for inducing cell death (apoptosis) and in immunosuppression. In structure I, CR1R2 is selected from CHOH, C═O, CHF, CF2 and C(CF3)OH; CR6 and CR13 are selected from CH, COH and CF; CR7R8, CR9R10 and CR11R12 are selected from CH2, CHOH, C═O, CHF and CF2; and CR3R4R5 is selected from CH3, CH2OH, C═O, COOH, CH2F, CHF2 and CF3; such that: at least one of R1-R13 comprises fluorine; no more than two of CR3R4R5, CR6, CR7R8, CR9R10, CR11R12, and CR13 comprises fluorine or oxygen; and, when CR1R2 is CHOH, CR3R4R5 is not CH2F.
    • 具有结构I的化合物可用于诱导细胞死亡(凋亡)和免疫抑制。 在结构I中,CR 1,R 2选自CHOH,CO,CHF,CF 2和C(CF 3) OH); CR 6和CR 13选自CH,COH和CF; R&lt; 9&gt; 8&lt; 9&gt;&lt; 9&lt; 10&gt;和&lt; 11&gt; > 12 选自CH 2,CHOH,CO,CHF和CF 2; 和CR 3 R 4选自CH 3,CH 2,CH 2, OH,CO,COOH,CH 2,F,CHF 2和CF 3; 使得:R 1〜R 13中的至少一个包含氟; 不超过两个CR 3,R 4,R 5,CR 6,CR 7, 其中,R 8,R 9,R 10,R 11,R 12, 并且CR 13包括氟或氧; 当CR <1> 2 2时为CHOH时,CR 3 R 4 R 5 O >不是CH 2。