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    FLUORINATED ARYLAMIDE DERIVATIVES
    2.
    发明公开
    FLUORINATED ARYLAMIDE DERIVATIVES 审中-公开
    氟化芳酰胺衍生物

    公开(公告)号：EP1976511A2

    公开(公告)日：2008-10-08

    申请号：EP07762514.3

    申请日：2007-01-09

    申请人： Merck & Co., Inc.

    发明人： MILLER, Thomas, A. ,  SLOMAN, David, L. ,  STANTON, Matthew, G. ,  WILSON, Kevin, J. ,  WITTER, David, J.

    IPC分类号： A61K31/38

    CPC分类号： C07D231/40 ,  C07D333/20 ,  C07D333/70 ,  C07D409/12 ,  C07D409/14 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14

    摘要： The present invention relates to a novel class of fluorinated arylamide derivatives. The instant compounds can be used to treat cancer. The fluorinated arylamide derivatives 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.

    HYDROXYALKYLARYLAMIDE DERIVATIVES
    4.
    发明公开
    HYDROXYALKYLARYLAMIDE DERIVATIVES 审中-公开
    羟基烷基酰胺衍生物

    公开(公告)号：EP1973405A2

    公开(公告)日：2008-10-01

    申请号：EP07716310.3

    申请日：2007-01-08

    申请人： Merck & Co., Inc.

    发明人： HEIDEBRECHT, Richard, W., Jr. ,  MILLER, Thomas, A. ,  WILSON, Kevin, J. ,  WITTER, David, J. ,  GRIMM, Jonathan

    IPC分类号： A01N43/00 ,  A61K31/33

    CPC分类号： C07D333/70 ,  C07D333/20 ,  C07D413/12

    摘要： The present invention relates to a novel class of hydroxyalkylarylamide derivatives. The instant compounds can be used to treat cancer. The fluorinated arylamide derivatives 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.

    摘要翻译： 本发明涉及一类新的羟烷基芳酰胺衍生物。 本发明化合物可用于治疗癌症。 氟化芳基酰胺衍生物还可以抑制组蛋白脱乙酰酶，适用于选择性诱导终末分化，阻止肿瘤细胞的生长和/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。 本发明化合物还可用于预防和治疗TRX介导的疾病，如自身免疫性疾病，变应性疾病和炎性疾病，以及用于预防和/或治疗中枢神经系统（CNS）疾病，例如 神经退行性疾病。 本发明进一步提供了包含异羟肟酸衍生物和这些药物组合物的安全给药方案的药物组合物，其易于遵循并且导致治疗有效量的异羟肟酸衍生物在体内。