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46 条记录 (耗时 0.048 秒)

    Modulators of the glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof
    33.
    发明授权
    Modulators of the 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：US08013004B2

    公开(公告)日：2011-09-06

    申请号：US12631179

    申请日：2009-12-04

    申请人： T. G. Murali Dhar ,  Hai-Yun Xiao ,  Bingwei Yang

    发明人： T. G. Murali Dhar ,  Hai-Yun Xiao ,  Bingwei Yang

    IPC分类号： C07D277/00 ,  C07D233/00 ,  A01N43/76 ,  A01N43/50

    CPC分类号： C07D401/10 ,  C07D249/14 ,  C07D277/46 ,  C07D401/04 ,  C07D401/14 ,  C07D403/10 ,  C07D417/10

    摘要： A class of 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 obesity, diabetes, inflammatory and immune diseases, and have the structure of formula (I) or (II): including a stereoisomer thereof, a tautomer thereof, a prodrug thereof, or a pharmaceutically acceptable salt thereof, where Q is selected from N, O, and S; Y is aryl or heteroaryl; Z is H, C2-6alkyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, halo, or alkoxy; and A, B, R, Ra, Rb, Rc and Rd are defined herein. Also provided are pharmaceutical compositions and methods of treating obesity, diabetes and inflammatory or immune associated diseases comprising said compounds.

    摘要翻译： 提供一类新型非甾体化合物，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，包括肥胖症，糖尿病，炎症和免疫疾病，并且具有 式（I）或（II）的结构：包括其立体异构体，其互变异构体，其前药或其药学上可接受的盐，其中Q选自N，O和S; Y是芳基或杂芳基; Z是H，C 2-6烷基，环烷基，杂环烷基，芳基，杂芳基，卤素或烷氧基; 并且A，B，R，Ra，Rb，Rc和Rd在本文中定义。 还提供了治疗肥胖症，糖尿病和包含所述化合物的炎性或免疫相关疾病的药物组合物和方法。

    Modulators of glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof
    34.
    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：US07994190B2

    公开(公告)日：2011-08-09

    申请号：US12513228

    申请日：2007-10-31

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

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

    IPC分类号： A61K31/437 ,  C07D401/02

    CPC分类号： C07D471/04

    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 the group X is O or (Rx)(Ry); is heterocyclo or heteroaryl; E is —N—, —NR1—, —O—, —C(═O), —S—, —SO2—, or —CR2—; F is —N—, —NR1a, —O—, —C(═O), —S—, —SO2—, or —CR2a—; G is independently N, —NR1b—, —O—, —C(═O), —S—, —SO2— or —CR2b— provided that the heterocyclic ring formed does not contain a S—S or S—O bond and at least one of E, F and G is a hetero atom; and Ma, Rx, Ry, R1, R1a, R1b, R2, R2a, R2b, R4, R5a, R6, R7, X, Za and Z are as defined herein. Also provided are pharmaceutical compositions and methods of treating inflammatory- or immune-associated diseases 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，包括具有结构式的炎性和免疫疾病，肥胖症和糖尿病 （I）：其对映体，非对映异构体或其药学上可接受的盐或水合物，其中基团X为O或（Rx）（Ry）; 是杂环基或杂芳基; E是-N-，-NR1-，-O - ， - C（= O）， - S - ， - SO 2 - 或-CR 2 - ; F是-N-，-NR1a，-O-，-C（= O），-S-，-SO2 - 或-CR2a; G独立地为N，-NR1b - ， - O - ， - C（= O）， - S - ， - SO2-或-CR2b-，条件是所形成的杂环不含S-S或S-O键， E，F和G中的至少一个是杂原子; 并且Ma，Rx，Ry，R1，R1a，R1b，R2，R2a，R2b，R4，R5a，R6，R7，X，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的药物组合物和方法。