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    SILICON DERIVATIVES AS HISTONE DEACETYLASE INHIBITORS
    2.
    发明申请
    SILICON DERIVATIVES AS HISTONE DEACETYLASE INHIBITORS 审中-公开
    硅酮衍生物作为脱乙酰壳多糖抑制剂

    公开(公告)号：US20110130361A1

    公开(公告)日：2011-06-02

    申请号：US12672441

    申请日：2008-08-05

    申请人： Jonathan Grimm ,  Richard W. Heidebrecht, JR. ,  Dawn M. Mampreian ,  Joey L. Methot ,  Thomas A. Miller ,  Karin M. Otte ,  Scott Peterson ,  Phieng Siliphaivanh ,  Kevin J. Wilson ,  David J. Witter

    发明人： Jonathan Grimm ,  Richard W. Heidebrecht, JR. ,  Dawn M. Mampreian ,  Joey L. Methot ,  Thomas A. Miller ,  Karin M. Otte ,  Scott Peterson ,  Phieng Siliphaivanh ,  Kevin J. Wilson ,  David J. Witter

    IPC分类号： A61K31/695 ,  C07C271/28 ,  C07D333/22 ,  C07D209/32 ,  C07F7/02 ,  A61K31/24 ,  A61K31/381 ,  A61K31/4015 ,  A61P35/00

    CPC分类号： C07F7/0812

    摘要： The present invention relates to a novel class of Silicon derivatives. The Silicon compounds can be used to treat cancer. The Silicon 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 Silicon derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the Silicon derivatives in vivo.

    摘要翻译： 本发明涉及一类新型的硅衍生物。 硅化合物可用于治疗癌症。 硅化合物还可以抑制组蛋白脱乙酰酶，并且适用于选择性诱导末端分化，并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疾病（CNS），例如 神经退行性疾病 本发明还提供包含硅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，并且其在体内导致治疗有效量的硅衍生物。

    Hydroxyalkylarylamide Derivatives
    4.
    发明申请
    Hydroxyalkylarylamide Derivatives 审中-公开
    羟烷基芳基酰胺衍生物

    公开(公告)号：US20090062297A1

    公开(公告)日：2009-03-05

    申请号：US12087623

    申请日：2007-01-08

    申请人： Richard W. Heidebrecht ,  Thomas A. Miller ,  Kevin J. Wilson ,  David J. Witter ,  Jonathan Grimm

    发明人： Richard W. Heidebrecht ,  Thomas A. Miller ,  Kevin J. Wilson ,  David J. Witter ,  Jonathan Grimm

    IPC分类号： A61K31/496 ,  C07D333/24 ,  A61K31/381 ,  A61K31/422 ,  C07D413/12 ,  C07D333/70

    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基酰胺衍生物。 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，并且适用于选择性诱导终末分化，并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。

    Pyridyl derivatives as histone deacetylase inhibitors
    9.
    发明授权
    Pyridyl derivatives as histone deacetylase inhibitors 有权
    吡啶衍生物作为组蛋白脱乙酰酶抑制剂

    公开(公告)号：US08461189B2

    公开(公告)日：2013-06-11

    申请号：US12666415

    申请日：2008-06-24

    申请人： Richard W. Heidebrecht, Jr. ,  Thomas A. Miller ,  Matthew G. Stanton ,  David J. Witter

    发明人： Richard W. Heidebrecht, Jr. ,  Thomas A. Miller ,  Matthew G. Stanton ,  David J. Witter

    IPC分类号： A01N43/40 ,  A01N47/10 ,  A61K31/44 ,  C07D213/55

    CPC分类号： C07D213/75 ,  C07D409/04 ,  C07D409/14

    摘要： The present invention relates to a novel class of pyridyl and pyrimidinyl derivatives. The pyridyl and pyrimidinyl compounds can be used to treat cancer. The pyridyl and pyrimidinyl 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 pyridyl and pyrimidinyl derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the pyridyl and pyrimidinyl derivatives in vivo.

    摘要翻译： 本发明涉及一类新的吡啶基和嘧啶基衍生物。 吡啶基和嘧啶基化合物可用于治疗癌症。 吡啶基和嘧啶基化合物也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吡啶基和嘧啶基衍生物的药物组合物以及易于遵循的这些药物组合物的安全给药方案，并且其在体内导致治疗有效量的吡啶基和嘧啶基衍生物。