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    SILICON DERIVATIVES AS HISTONE DEACETYLASE INHIBITORS
    11.
    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。

    N-HYDROXY-NAPHTHALENE DICARBOXAMIDE AND N-HYDROXY-BIPHENYL-DICARBOXAMIDE COMPOUNDS AS HISTONE DEACETYLASE INHIBITORS
    13.
    发明申请
    N-HYDROXY-NAPHTHALENE DICARBOXAMIDE AND N-HYDROXY-BIPHENYL-DICARBOXAMIDE COMPOUNDS AS HISTONE DEACETYLASE INHIBITORS 审中-公开
    N-羟基萘甲酸二酰胺和N-羟基 - 联苯二甲酰胺化合物作为HISTONE脱乙酰壳多糖酶抑制剂

    公开(公告)号：US20100216796A1

    公开(公告)日：2010-08-26

    申请号：US12681634

    申请日：2008-09-30

    申请人： Solomon Kattar ,  Thomas A. Miller ,  Karin M. Otte ,  Phieng Siliphaivanh ,  Laura Surdi ,  Paul Tempest ,  Anna A. Zabierek

    发明人： Solomon Kattar ,  Thomas A. Miller ,  Karin M. Otte ,  Phieng Siliphaivanh ,  Laura Surdi ,  Paul Tempest ,  Anna A. Zabierek

    IPC分类号： A61K31/166 ,  C07C233/64 ,  C07D319/16 ,  C07D265/30 ,  A61K31/357 ,  A61K31/5375 ,  A61P35/00

    CPC分类号： C07D319/18 ,  C07C259/10 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2601/14 ,  C07D207/323 ,  C07D207/335 ,  C07D213/40 ,  C07D231/56 ,  C07D233/61 ,  C07D261/08 ,  C07D265/30 ,  C07D277/28 ,  C07D307/14 ,  C07D307/52 ,  C07D307/81 ,  C07D409/04 ,  C07D417/04 ,  C07D471/04

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

    摘要翻译： 本发明涉及新型的N-羟基 - 萘二甲酰胺和N-羟基 - 联苯二甲酰胺衍生物。 N-羟基 - 萘二甲酰胺和N-羟基 - 联苯二甲酰胺化合物可用于治疗癌症。 N-羟基 - 萘二甲酰胺和N-羟基 - 联苯二甲酰胺化合物也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，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 本发明还提供包含N-羟基 - 萘二甲酰胺和N-羟基 - 联苯二甲酰胺衍生物的药物组合物以及这些药物组合物的安全投药方案，其易于遵循，并且其导致治疗有效量的N - 羟基 - 萘二甲酰胺和N-羟基 - 联苯二甲酰胺衍生物。

    Benzothiophene derivatives
    14.
    发明授权
    Benzothiophene derivatives 有权
    苯并噻吩衍生物

    公开(公告)号：US07834034B2

    公开(公告)日：2010-11-16

    申请号：US11918913

    申请日：2006-04-14

    申请人： Dawn M. Mampreian ,  Thomas A. Miller ,  David L. Sloman ,  Matthew G. Stanton ,  Kevin J. Wilson ,  David J. Witter

    发明人： Dawn M. Mampreian ,  Thomas A. Miller ,  David L. Sloman ,  Matthew G. Stanton ,  Kevin J. Wilson ,  David J. Witter

    IPC分类号： A61K31/445 ,  C07D409/12

    CPC分类号： C07D333/70 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D413/06 ,  C07D413/14

    摘要： 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.

    摘要翻译： 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。

    Fluorinated Arylamide Derivatives
    15.
    发明申请
    Fluorinated Arylamide Derivatives 审中-公开
    氟化芳酰胺衍生物

    公开(公告)号：US20090012075A1

    公开(公告)日：2009-01-08

    申请号：US12087624

    申请日：2007-01-08

    申请人： Thomas A. Miller ,  David L. Sloman ,  Matthew G. Stanton ,  Kevin J. Wilson ,  David J. Witter

    发明人： Thomas A. Miller ,  David L. Sloman ,  Matthew G. Stanton ,  Kevin J. Wilson ,  David J. Witter

    IPC分类号： A61K31/381 ,  C07D409/12 ,  C07D333/50 ,  C07D409/14 ,  C07D413/10 ,  C07D413/14 ,  A61K31/4436 ,  A61K31/5377 ,  A61K31/4025 ,  A61K31/4245 ,  A61P35/00 ,  A61K31/415 ,  A61K31/496

    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.

    摘要翻译： 本发明涉及一类新型氟化芳基酰胺衍生物。 本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疾病（CNS），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。

    Diamine and Iminodiacetic Acid Hydroxamic Acid Derivatives
    17.
    发明申请
    Diamine and Iminodiacetic Acid Hydroxamic Acid Derivatives 审中-公开
    二胺和亚氨基二乙酸羟肟酸衍生物

    公开(公告)号：US20090023718A1

    公开(公告)日：2009-01-22

    申请号：US10580480

    申请日：2004-11-23

    申请人： Thomas A. Miller ,  David J. Witter ,  Sandro Belvedere

    发明人： Thomas A. Miller ,  David J. Witter ,  Sandro Belvedere

    IPC分类号： A61K31/5355 ,  A61K31/416 ,  A61K31/47 ,  A61K31/4965 ,  C07D231/54 ,  C07D215/38 ,  C07D265/30 ,  C07D241/04 ,  A61P35/00

    CPC分类号： C07D211/16 ,  C07C259/06 ,  C07C2601/14 ,  C07D209/14 ,  C07D215/38 ,  C07D215/40 ,  C07D217/06 ,  C07D231/56 ,  C07D277/82 ,  C07D295/185 ,  C07D317/66

    摘要： The present invention relates to a novel class of hydroxamic acid derivatives having a diamine or iminodiacetic acid backbone. The hydroxamic acid compounds can be used to treat cancer. The hydroxamic acid compounds can also inhibit histone deacetylase and are suitable for use in selectively including terminal differentiation, arresting cell growth and/or apoptosis of neo-plastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compound of the invention are also 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： 本发明涉及具有二胺或亚氨基二乙酸骨架的新一类异羟肟酸衍生物。 异羟肟酸化合物可用于治疗癌症。 异羟肟酸化合物还可以抑制组蛋白脱乙酰酶，并且适用于选择性地包括末端分化，阻止新塑料细胞的细胞生长和/或细胞凋亡，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，例如神经变性 疾病 本发明进一步提供包含异羟肟酸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的给药方案，并且其在体内导致治疗有效量的异羟肟酸衍生物。

    Benzothiophene hydroxamic acid derivatives with carbamate, urea, amide and sulfonamide substitutions
    18.
    发明授权
    Benzothiophene hydroxamic acid derivatives with carbamate, urea, amide and sulfonamide substitutions 有权
    苯并噻吩异羟肟酸衍生物与氨基甲酸酯，脲，酰胺和磺酰胺取代

    公开(公告)号：US07872024B2

    公开(公告)日：2011-01-18

    申请号：US11918911

    申请日：2006-04-14

    申请人： Joey Methot ,  Thomas A. Miller ,  David J. Witter

    发明人： Joey Methot ,  Thomas A. Miller ,  David J. Witter

    IPC分类号： A61K31/40 ,  A61K31/445 ,  C07D405/00 ,  C07D333/52

    CPC分类号： C07D333/70

    摘要： The present invention relates to a novel class of hydroxamic acid derivatives carbamate, urea, amide and sulfonamide substitutions. The hydroxamic acid compounds can be used to treat cancer. The hydroxamic acid 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 are also 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： 本发明涉及一类新型异羟肟酸衍生物氨基甲酸酯，脲，酰胺和磺酰胺取代物。 异羟肟酸化合物可用于治疗癌症。 异羟肟酸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，例如神经变性 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。

    Benzothiophene hydroxamic acid derivatives with carbamate, urea, amide and sulfonamide substitutions
    20.
    发明申请
    Benzothiophene hydroxamic acid derivatives with carbamate, urea, amide and sulfonamide substitutions 有权
    苯并噻吩异羟肟酸衍生物与氨基甲酸酯，脲，酰胺和磺酰胺取代

    公开(公告)号：US20090318541A1

    公开(公告)日：2009-12-24

    申请号：US11918911

    申请日：2006-04-14

    申请人： Joey Methot ,  Thomas A. Miller ,  David J. Witter

    发明人： Joey Methot ,  Thomas A. Miller ,  David J. Witter

    IPC分类号： A61K31/381 ,  C07D333/64 ,  A61P35/00 ,  A61P25/00

    CPC分类号： C07D333/70

    摘要： The present invention relates to a novel class of hydroxamic acid derivatives carbamate, urea, amide and sulfonamide substitutions. The hydroxamic acid compounds can be used to treat cancer. The hydroxamic acid 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 are also 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： 本发明涉及一类新型异羟肟酸衍生物氨基甲酸酯，脲，酰胺和磺酰胺取代物。 异羟肟酸化合物可用于治疗癌症。 异羟肟酸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，例如神经变性 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。