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    Modulators of glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof
    25.
    发明授权
    Modulators of glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof 有权
    糖皮质激素受体，AP-1和/或NF-κB活性的调节剂及其用途

    公开(公告)号：US08067447B2

    公开(公告)日：2011-11-29

    申请号：US12513192

    申请日：2007-10-31

    申请人： James E. Sheppeck ,  John L. Gilmore ,  T. G. Murali Dhar ,  Hai-Yun Xiao

    发明人： James E. Sheppeck ,  John L. Gilmore ,  T. G. Murali Dhar ,  Hai-Yun Xiao

    IPC分类号： A61K31/433 ,  A61K31/416 ,  C07D285/135 ,  C07D231/56 ,  C07D231/40

    CPC分类号： C07D231/56 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07D417/14

    摘要： Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, and/or AP-1, and/or NF-κB activity including inflammatory and immune diseases, obesity and diabetes having the structure of formula (I), its enantiomers, diastereomers, or a pharmaceutically-acceptable salt, or hydrate, thereof, wherein (Ia) is heterocycle or heteroaryl; J, Ja, E, F, G, Ma, M, Q, Za and Z are as defined herein. Also provided are pharmaceutical compositions and methods of treating inflammatory- or immune-associated diseases and obesity and diabetes employing said compounds.

    摘要翻译： 提供了新的非甾体化合物，其可用于治疗与调节糖皮质激素受体，和/或AP-1和/或NF-κB活性相关的疾病，包括炎性和免疫疾病，肥胖症和糖尿病，其结构为 式（I），其对映异构体，非对映体或其药学上可接受的盐或水合物，其中（Ia）是杂环或杂芳基; J，Ja，E，F，G，Ma，M，Q，Za和Z如本文所定义。 还提供了使用所述化合物治疗炎性或免疫相关疾病和肥胖症和糖尿病的药物组合物和方法。

    Modulators of glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof
    30.
    发明授权
    Modulators of glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof 有权
    糖皮质激素受体，AP-1和/或NF-κB活性的调节剂及其用途

    公开(公告)号：US08198311B2

    公开(公告)日：2012-06-12

    申请号：US12513232

    申请日：2007-10-31

    申请人： James E. Sheppeck ,  John L. Gilmore ,  T. G. Murali Dhar ,  Hai-Yun Xiao ,  Jianmin Wang ,  Bingwei Vera Yang ,  Lidia M. Doweyko

    发明人： James E. Sheppeck ,  John L. Gilmore ,  T. G. Murali Dhar ,  Hai-Yun Xiao ,  Jianmin Wang ,  Bingwei Vera Yang ,  Lidia M. Doweyko

    IPC分类号： A61K31/416 ,  C07D231/56

    CPC分类号： C07D231/56 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12

    摘要： Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity including inflammatory and immune diseases, obesity and diabetes having the structure of formula (I), its enantiomers, diastereomers, or a pharmaceutically acceptable salt, or hydrate, thereof, wherein X is (Ia); or X is (Ib); or X is (Ic); (Id) is heterocycle or heteroaryl; E is —N—, —NR1—, —O—, —S—, —SO2— or —CR2—; F is —N—, —NR1a—, —O—, —S—, —SO2— or —CR2a—; G is N, —NR1b—, —O—, —S—, —SO2— or —CR2b—, provided that the E-F-G containing heterocyclic ring formed does not contain a S—S or S—O bond, and at least one of E, F and G is a heteroatom; J, Ja, M, Ma, Q, Rx, Ry, R1, R1a, R1b, R2, R2a, R2b, and R3 to R21, Z, Za, Zb, and Zc are as defined above.

    摘要翻译： 提供了新的非甾体化合物，其可用于治疗与调节糖皮质激素受体，AP-1和/或NF-κB活性相关的疾病，包括具有式（I）结构的炎性和免疫疾病，肥胖症和糖尿病 ），其对映异构体，非对映异构体或其药学上可接受的盐或水合物，其中X为（Ia）; 或X为（Ib）; 或X为（Ic）; （Id）是杂环或杂芳基; E是-N-，-NR1 - ， - O - ， - S - ， - SO2-或-CR2-; F是-N-，-NR1 - ， - O - ， - S - ， - SO2-或-CR2a-; G是N，-NR1b - ， - O - ， - S - ， - SO2-或-CR2b-，条件是所形成的含有EFG的杂环不含S-S或S-O键， E，F和G是杂原子; J，Ja，M，Ma，Q，Rx，Ry，R1，R1a，R1b，R2，R2a，R2b和R3至R21，Z，Za，Zb和Zc如上所定义。