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    Inhibitors of janus kinases
    28.
    发明授权
    Inhibitors of janus kinases 有权
    痛风激酶抑制剂

    公开(公告)号：US07763634B2

    公开(公告)日：2010-07-27

    申请号：US12227959

    申请日：2007-06-05

    申请人： Jonathan R. Young ,  Andrew Haidle ,  Paul Tempest ,  Michelle Machacek

    发明人： Jonathan R. Young ,  Andrew Haidle ,  Paul Tempest ,  Michelle Machacek

    IPC分类号： A61K31/4745 ,  C07D471/02

    CPC分类号： C07D471/04

    摘要： The instant invention provides for tetracyclic compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.

    摘要翻译： 本发明提供抑制四种已知的哺乳动物JAK激酶（JAK1，JAK2，JAK3和TYK2）和PDK1的四环化合物。 本发明还提供了包含这种抑制化合物的组合物和通过向需要治疗骨髓增生性疾病或癌症的患者施用化合物来抑制JAK1，JAK2，JAK3 TYK2和PDK1的活性的方法。

    Aryl-Fused Spirocyclic Compounds
    29.
    发明申请
    Aryl-Fused Spirocyclic Compounds 有权
    芳基稠合的螺环化合物

    公开(公告)号：US20090239849A1

    公开(公告)日：2009-09-24

    申请号：US12227417

    申请日：2007-05-14

    申请人： Christopher Hamblett ,  Solomon Kattar ,  Dawn Mampreian ,  Joey Methot ,  Thomas Miller ,  Paul Tempest

    发明人： Christopher Hamblett ,  Solomon Kattar ,  Dawn Mampreian ,  Joey Methot ,  Thomas Miller ,  Paul Tempest

    IPC分类号： A61K31/551 ,  C07D471/10 ,  A61K31/438 ,  A61P35/00

    CPC分类号： C07D471/10 ,  C07D401/04 ,  C07D491/107

    摘要： The present invention relates to a novel class of aryl-fused spirocyclic compounds. These compounds can 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 compounds of the instant invention and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of these compounds in vivo.

    摘要翻译： 本发明涉及一类新颖的芳基稠合的螺环化合物。 这些化合物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 神经退行性疾病 本发明进一步提供包含本发明化合物和易于遵循的这些药物组合物的安全给药方案的药物组合物，并且其在体内导致治疗有效量的这些化合物。

    Spirocyclic Compounds
    30.
    发明申请
    Spirocyclic Compounds 有权
    螺环化合物

    公开(公告)号：US20090209566A1

    公开(公告)日：2009-08-20

    申请号：US12085396

    申请日：2006-11-17

    申请人： Scott C. Berk ,  Joshua Close ,  Christopher Hamblett ,  Richard W. Heidebrecht ,  Solomon D. Kattar ,  Laura T. Kliman ,  Dawn M. Mampreian ,  Joey L. Methot ,  Thomas Miller ,  David L. Sloman ,  Matthew G. Stanton ,  Paul Tempest ,  Anna A. Zabierek

    发明人： Scott C. Berk ,  Joshua Close ,  Christopher Hamblett ,  Richard W. Heidebrecht ,  Solomon D. Kattar ,  Laura T. Kliman ,  Dawn M. Mampreian ,  Joey L. Methot ,  Thomas Miller ,  David L. Sloman ,  Matthew G. Stanton ,  Paul Tempest ,  Anna A. Zabierek

    IPC分类号： A61K31/438 ,  C07D471/10 ,  C07D491/107 ,  C07D498/10 ,  C07D487/10 ,  A61K31/4439 ,  A61K31/506 ,  A61P35/00

    CPC分类号： C07D471/10 ,  C07D487/10 ,  C07D491/10 ,  C07D491/107 ,  C07D498/10

    摘要： The present invention relates to a novel class of substituted spirocyclic compounds, represented by the following structural Formula: I Wherein A, B and D are independently selected from CR12, NR1a, C(O) and O; E is selected from a bond, CR12, NR1a, C(O) and O; wherein at least one of A, B, D or E is CR12; and provided that when A is O, then E is not O; G is CR12; R is selected from NH2 and OH; These compounds can inhibit histone deacetylase and are suitable for use in selectively inducing termin 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 compounds of the instant invention and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of these compounds in vivo.

    摘要翻译： 本发明涉及由下列结构式表示的新一类取代的螺环化合物：其中A，B和D独立地选自CR12，NR1a，C（O）和O; E选自键，CR12，NR1a，C（O）和O; 其中A，B，D或E中的至少一个为CR 12; 并且条件是当A为O时，则E不为O; G是CR12; R选自NH 2和OH; 这些化合物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 本发明进一步提供包含本发明化合物和易于遵循的这些药物组合物的安全给药方案的药物组合物，并且其在体内导致治疗有效量的这些化合物。