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    • 6. 发明授权
    • Benzothiophene derivatives
    • 苯并噻吩衍生物
    • US07834034B2
    • 2010-11-16
    • US11918913
    • 2006-04-14
    • Dawn M. MampreianThomas A. MillerDavid L. SlomanMatthew G. StantonKevin J. WilsonDavid J. Witter
    • Dawn M. MampreianThomas A. MillerDavid L. SlomanMatthew G. StantonKevin J. WilsonDavid J. Witter
    • A61K31/445C07D409/12
    • C07D333/70C07D409/06C07D409/12C07D409/14C07D413/06C07D413/14
    • The present invention relates to a novel class of benzothiophene amide derivatives. The hydroxamic acid compounds can be used to treat cancer. The benzothiophene amide compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the hydroxamic acid derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the hydroxamic acid derivatives in vivo.
    • 本发明涉及一类新型的苯并噻吩酰胺衍生物。 异羟肟酸化合物可用于治疗癌症。 苯并噻吩酰胺化合物也可以抑制组蛋白脱乙酰酶,适用于选择性诱导末端分化,阻止肿瘤细胞的细胞生长和/或凋亡,从而抑制这些细胞的增殖。 因此,本发明的化合物可用于治疗具有以肿瘤细胞增殖为特征的肿瘤的患者。 本发明的化合物还可用于预防和治疗TRX介导的疾病,例如自身免疫性,过敏性和炎性疾病,以及预防和/或治疗中枢神经系统(CNS)的疾病,例如 神经退行性疾病 本发明进一步提供包含异羟肟酸衍生物和这些药物组合物的安全投药方案的药物组合物,它们易于遵循,并且其在体内导致治疗有效量的异羟肟酸衍生物。