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34 条记录 (耗时 0.062 秒)

    Substituted isoxazole compounds
    14.
    发明授权
    Substituted isoxazole compounds 有权
    取代的异恶唑化合物

    公开(公告)号：US08354398B2

    公开(公告)日：2013-01-15

    申请号：US13145730

    申请日：2010-01-22

    申请人： Scott Hunter Watterson ,  Alaric J. Dyckman ,  William J. Pitts ,  Steven H. Spergel

    发明人： Scott Hunter Watterson ,  Alaric J. Dyckman ,  William J. Pitts ,  Steven H. Spergel

    IPC分类号： A61K31/4245 ,  C07D413/14

    CPC分类号： C07D413/14

    摘要： Disclosed are compounds of Formula (I) or pharmaceutically acceptable salts thereof, wherein Q is R1 is alkyl or aryl, said aryl optionally substituted with one to five substituents independently selected from C1 to C6 alkyl, C1 to C4 haloalkyl, —OR4, and/or halogen; and R2, R3, R4, and n are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.

    摘要翻译： 公开了式（I）化合物或其药学上可接受的盐，其中Q为R 1为烷基或芳基，所述芳基任选被一至五个独立地选自C 1至C 6烷基，C 1至C 4卤代烷基，-OR 4和/ 或卤素; 并且R 2，R 3，R 4和n在本文中定义。 还公开了使用这种化合物作为G蛋白偶联受体S1P1的选择性激动剂的方法，以及包含这些化合物的药物组合物。 这些化合物可用于治疗，预防或减缓各种治疗领域（例如自身免疫性疾病和血管疾病）中的疾病或病症的进展。

    SUBSTITUTED HETEROCYCLIC COMPOUNDS
    15.
    发明申请
    SUBSTITUTED HETEROCYCLIC COMPOUNDS 有权
    取代的杂环化合物

    公开(公告)号：US20120022041A1

    公开(公告)日：2012-01-26

    申请号：US13145721

    申请日：2010-01-22

    申请人： William J. Pitts ,  Alaric J. Dyckman ,  Steven H. Spergel ,  Scott Hunter Watterson

    发明人： William J. Pitts ,  Alaric J. Dyckman ,  Steven H. Spergel ,  Scott Hunter Watterson

    IPC分类号： A61K31/4439 ,  A61P37/06 ,  A61P29/00 ,  C07D413/14

    CPC分类号： C07D413/14

    摘要： Disclosed are compounds of Formula (I) or pharmaceutically acceptable salts thereof, wherein Q is R1 is cycloalkyl, heteroaryl, or heterocyclyl, each optionally substituted with one to five substituents independently selected from C1 to C6 alkyl, C1 to C4 haloalkyl, —OR4, and/or halogen; and R2, R3, R4, and n are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as vascular disease and autoimmune diseases.

    摘要翻译： 公开了式（I）化合物或其药学上可接受的盐，其中Q为R 1为环烷基，杂芳基或杂环基，各自任选被一至五个独立地选自C 1至C 6烷基，C 1至C 4卤代烷基，-OR 4， 和/或卤素; 并且R 2，R 3，R 4和n在本文中定义。 还公开了使用这种化合物作为G蛋白偶联受体S1P1的选择性激动剂的方法，以及包含这些化合物的药物组合物。 这些化合物可用于治疗，预防或减缓各种治疗领域（例如血管疾病和自身免疫性疾病）中疾病或病症的发展。

    Substituted pyrazole compounds
    17.
    发明授权
    Substituted pyrazole compounds 有权
    取代的吡唑化合物

    公开(公告)号：US08389509B2

    公开(公告)日：2013-03-05

    申请号：US13145728

    申请日：2010-01-22

    申请人： Alaric J. Dyckman ,  William J. Pitts ,  Scott Hunter Watterson

    发明人： Alaric J. Dyckman ,  William J. Pitts ,  Scott Hunter Watterson

    IPC分类号： A61K31/4155 ,  A61K31/397 ,  A61K31/4245 ,  C07D231/10 ,  C07D271/06 ,  C07D205/04

    CPC分类号： C07D413/14

    摘要： Disclosed are compounds of Formula (I) or a pharmaceutically acceptable salt thereof, wherein: n is zero or an integer selected from 1 through 4; R1 is cycloalkyl, aryl, heteroaryl, or heterocyclyl, each optionally substituted with one to five substituents independently selected from C1 to C6 alkyl, C1 to C4 haloalkyl, benzyl, —OR4, and/or halogen; and R2, R3, R4, and n are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.

    摘要翻译： 公开了式（I）的化合物或其药学上可接受的盐，其中：n为0或选自1至4的整数; R 1是环烷基，芳基，杂芳基或杂环基，各自任选地被一至五个独立地选自C 1至C 6烷基，C 1至C 4卤代烷基，苄基，-OR 4和/或卤素的取代基取代。 并且R 2，R 3，R 4和n在本文中定义。 还公开了使用这种化合物作为G蛋白偶联受体S1P1的选择性激动剂的方法，以及包含这些化合物的药物组合物。 这些化合物可用于治疗，预防或减缓各种治疗领域（例如自身免疫疾病和血管疾病）中的疾病或病症的进展。

    Integrin inhibitor prodrugs
    20.
    发明授权
    Integrin inhibitor prodrugs 失效
    整联蛋白抑制剂前药

    公开(公告)号：US06214834B1

    公开(公告)日：2001-04-10

    申请号：US09049305

    申请日：1998-03-27

    申请人： Prabhakar K. Jadhav ,  Douglas G. Batt ,  Munir A. Hussain ,  William J. Pitts ,  Arnold J. Repta

    发明人： Prabhakar K. Jadhav ,  Douglas G. Batt ,  Munir A. Hussain ,  William J. Pitts ,  Arnold J. Repta

    IPC分类号： C07D23156

    CPC分类号： C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04

    摘要： This invention relates to novel heterocycles which are useful as antagonists of the &agr;v&bgr;3 integrin and related cell surface adhesive protein receptors, to pharmaceutical compositions containing such compounds, to iontophoretic delivery of such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of cell adhesion, the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.

    摘要翻译： 本发明涉及可用作αphavbeta3整联蛋白和相关细胞表面粘附蛋白受体的拮抗剂的新型杂环，含有这些化合物的药物组合物，这些化合物的离子电渗疗法，以及单独或与 用于抑制细胞粘附，血管生成障碍的治疗，炎症，骨退化，癌症转移，糖尿病性视网膜病变，血栓形成，再狭窄，黄斑变性和由细胞粘附和/或细胞迁移介导的其它病症和/或 血管生成。