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    • 8. 发明授权
    • Tricyclic-bis-enone derivatives and methods of use thereof
    • 三环 - 双烯酮衍生物及其使用方法
    • US08067465B2
    • 2011-11-29
    • US12722053
    • 2010-03-11
    • Tadashi HondaFrank G. FavaloroGordon W. GribbleMichael B. SpornNanjoo Suh
    • Tadashi HondaFrank G. FavaloroGordon W. GribbleMichael B. SpornNanjoo Suh
    • A61K31/275C07C255/47
    • C07C62/38C07C225/12C07C255/47C07C271/18C07C2603/00C07C2603/26C07F7/1804
    • Novel tricyclic-bis-enone derivatives (TBEs) as well as the process for the preparation of such TBEs are provided. Also provided are methods for prevention and/or treatment of cancer, Alzheimer's disease, Parkinson's disease, multiple sclerosis, amyotropic lateral sclerosis, rheumatoid arthritis, inflammatory bowel disease, and all other diseases whose pathogenesis is believed to involve excessive production of either nitric oxide (NO) or prostaglandins or the overexpression of iNOS or COX-2 genes or gene products. Further, methods for the synthesis of the TBE compounds of the invention utilize cheap commercially available reagents and are highly cost effective and amenable to scale-up. Additional high efficiency synthetic methods that utilize novel intermediates as well as the synthesis of these intermediates are also provided. Furthermore, the invention also provides methods for designing novel and water-soluble TBEs.
    • 提供了新的三环双烯衍生物(TBE)以及制备这种TBE的方法。 还提供了用于预防和/或治疗癌症,阿尔茨海默氏病,帕金森病,多发性硬化,肌萎缩性侧索硬化,类风湿性关节炎,炎症性肠病以及其发病机制被认为涉及过量产生一氧化氮的所有其它疾病的方法 NO)或前列腺素或iNOS或COX-2基因或基因产物的过表达。 此外,用于合成本发明的TBE化合物的方法使用便宜的市售试剂,并且是高成本有效的并且适于放大。 还提供了利用新型中间体以及这些中间体的合成的其它高效合成方法。 此外,本发明还提供了设计新型和水溶性TBE的方法。