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    • 6. 发明公开
    • UBIQUITIN LIGASE INHIBITORS
    • 泛素连接酶抑制剂
    • EP1833807A1
    • 2007-09-19
    • EP06717448.2
    • 2006-01-05
    • Rigel Pharmaceuticals, Inc.
    • SINGH, RajinderRAMESH, UshaISSAKANI, Sarkiz, D.HUANG, JianingKINOSHITA, TaiseiGURURAJA, Tarikere
    • C07D277/42A61K31/426A61P35/00
    • C07D277/38C07D277/42
    • This invention describes compounds and pharmaceutical compositions useful as ubiquitin agent inhibitors, particularly ubiquitin ligase inhibitors. The compounds and pharmaceutical compositions of the invention are useful as inhibitors of the biochemical pathways of organisms in which ubiquitination is involved, such as signal transduction pathways. The invention also comprises the use of the compounds and pharmaceutical compositions of the invention for the treatment of conditions that require inhibition of ubiquitination. Furthermore, the invention comprises methods of inhibiting ubiquitination in a cell comprising contacting a cell in which inhibition of ubiquitination is desired with a compound or pharmaceutical composition according to the invention. Particularly, the compounds and pharmaceutical compositions are useful to inhibit the ubiquitin ligase activity of MDM2.
    • 本发明描述了用作泛蛋白剂抑制剂,特别是泛素连接酶抑制剂的化合物和药物组合物。 本发明的化合物和药物组合物可用作涉及泛素化的生物体的生物化学途径的抑制剂,例如信号转导途径。 本发明还包括本发明的化合物和药物组合物用于治疗需要抑制泛素化的病症的用途。 此外,本发明包括抑制细胞中泛素化的方法,包括使需要抑制泛素化的细胞与本发明的化合物或药物组合物接触。 特别地,所述化合物和药物组合物可用于抑制MDM2的泛素连接酶活性。