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HISTONE DEACETYLASE AND TUBULIN DEACETYLASE INHIBITORS

机译:组蛋白去乙酰化酶和微管蛋白去乙酰化酶抑制剂

摘要

In recognition of the need to develop novel therapeutic agents and efficient methods for the synthesis thereof, the present invention provides novel inhibitors of histone deacetylases, tubulin deacetylases, and/or aggresome inhibitors, and pharmaceutically acceptable salts and derivatives thereof. The inventive compounds fall into two classes ~ "isorubacin" class and "isoisotubacin" class- ~ all of which include a 1,3-dioxane core. The present invention further provides methods for treating disorders regulated by histone deacetylase activity, tubulin deacetylase activity, and/or the aggresome (e.g., proliferative diseases, cancer, inflammatory diseases, protozoal infections, protein degradation disorders, protein deposition disorders, etc.) comprising administering a therapeutically effective amount of an inventive compound to a subject in need thereof. The present invention also provides methods for preparing compounds of the invention.
机译:认识到需要开发新型治疗剂及其有效方法,本发明提供了组蛋白脱乙酰基酶,微管蛋白脱乙酰基酶和/或聚集体抑制剂的新型抑制剂,及其药学上可接受的盐和衍生物。本发明的化合物分为两类:“异柔红霉素”类和“异异丁星”类,所有这些均包括1,3-二恶烷核心。本发明进一步提供了用于治疗由组蛋白脱乙酰基酶活性,微管蛋白脱乙酰基酶活性和/或聚集体(例如,增生性疾病,癌症,炎性疾病,原生动物感染,蛋白质降解疾病,蛋白质沉积疾病等)调节的疾病的方法,包括:将治疗有效量的本发明化合物给予有此需要的受试者。本发明还提供了制备本发明化合物的方法。

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