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44 条记录 (耗时 0.049 秒)

    PYRIDYL AND PYRIMIDINYL DERIVATIVES AS HISTONE DEACETYLASE INHIBITORS
    23.
    发明申请
    PYRIDYL AND PYRIMIDINYL DERIVATIVES AS HISTONE DEACETYLASE INHIBITORS 有权
    吡啶并吡啶并吡啶衍生物作为脱乙酰壳多糖酶抑制剂

    公开(公告)号：US20100324092A1

    公开(公告)日：2010-12-23

    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： A61K31/4418 ,  C07D213/74 ,  C07D401/12 ,  A61K31/444 ,  A61P35/00

    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 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疾病（CNS），例如 神经退行性疾病 本发明还提供包含吡啶基和嘧啶基衍生物的药物组合物和这些药物组合物的安全给药方案，其易于遵循，并且其导致治疗有效量的体内吡啶基和嘧啶基衍生物。

    Benzothiophene derivatives
    24.
    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。

    Hydroxyalkylarylamide Derivatives
    25.
    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。

    Fluorinated Arylamide Derivatives
    26.
    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。

    Pyrrolo[2,3d]pyrimidine compositions and their use
    29.
    发明授权
    Pyrrolo[2,3d]pyrimidine compositions and their use 失效
    吡咯并[2,3d]嘧啶组合物及其用途

    公开(公告)号：US06800633B2

    公开(公告)日：2004-10-05

    申请号：US09728229

    申请日：2000-12-01

    申请人： Arlindo L. Castelhano ,  Bryan McKibben ,  David J. Witter

    发明人： Arlindo L. Castelhano ,  Bryan McKibben ,  David J. Witter

    IPC分类号： C07D48704

    CPC分类号： C07D487/04 ,  A61K31/519

    摘要： This invention pertains to compounds having the structure: wherein R1 and R2 are each independently a hydrogen atom, substituted alkyl, or a substituted or unsubstituted aryl, or alkylaryl moiety or together form a substituted or unsubstituted heterocyclic ring, provided that both R1 and R2 are both not hydrogen atoms or that neither R1 or R2 is 1-phenylethyl; R3 is a substituted or unsubstituted aryl, or alkylaryl moiety; R4 is a hydrogen atom or a substituted or unsubstituted alkyl, aryl, or alkylaryl moiety; and R5 and R6 are each independently a halogen atom, a hydrogen atom or a substituted or unsubstituted alkyl, aryl, or alkylaryl moiety, and the use of these compounds to treat a disease associated with increased levels of adenosine in a subject.

    摘要翻译： 本发明涉及具有以下结构的化合物：其中R 1和R 2各自独立地为氢原子，取代的烷基或取代或未取代的芳基或烷基芳基部分，或一起形成取代或未取代的杂环，条件是R 1和R 2均为 不是氢原子，也不是R1或R2都是1-苯基乙基; R3是取代或未取代的芳基或烷基芳基部分; R4是氢原子或取代或未取代的烷基，芳基或烷芳基部分; 并且R 5和R 6各自独立地为卤素原子，氢原子或取代或未取代的烷基，芳基或烷基芳基部分，以及这些化合物用于治疗与受试者中腺苷水平升高相关的疾病的用途。