Modulators of the glucocorticoid receptor, AP-1, and/or NF-kB activity and use thereof
    3.
    发明申请
    Modulators of the glucocorticoid receptor, AP-1, and/or NF-kB activity and use thereof 有权
    糖皮质激素受体,AP-1和/或NF-kB活性的调节剂及其用途

    公开(公告)号:US20060154975A1

    公开(公告)日:2006-07-13

    申请号:US11330748

    申请日:2006-01-12

    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): where X is S, O or N; Z is —T—COOR1 or —T—COR1; and T, R, R1, Ra, Rb, Rc, Rd, Z, A and B 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: 提供了一类新型非甾体化合物,其可用于治疗与糖皮质激素受体,AP-1和/或NF-κB活性的调节相关的疾病,包括肥胖症,糖尿病,炎症和免疫疾病,并且具有 式(I):其中X为S,O或N; Z是-T-COOR 1或-T-COR 1; 和T,R,R 1,R 2,R 2,R b,R d,R d, 本文定义了Z,A和B。 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。

    Compositions and methods involving nuclear hormone receptor site II
    5.
    发明申请
    Compositions and methods involving nuclear hormone receptor site II 失效
    涉及核激素受体位点II的组成和方法

    公开(公告)号:US20060223110A1

    公开(公告)日:2006-10-05

    申请号:US10621807

    申请日:2003-07-17

    摘要: A binding site in nuclear hormone receptors is described and its structural coordinates are provided. The invention provides machine-readable data storage media comprising structure coordinates of Site II and computer systems comprising the machine-readable data storage media. The invention provides methods used in the design and identification of ligands of Site II and of modulators of nuclear hormone receptors. The invention provides ligands of Site II, modulators of NHRs, pharmaceutical compositions comprising modulators of NHRs, methods of modulating NHRs, and methods of treating diseases by administering modulators of an NHR. Also provided are methods of designing mutants, mutant NHRs, Site II binding assays, and models of Site II.

    摘要翻译: 描述核激素受体中的结合位点并提供其结构坐标。 本发明提供了包括站点II的结构坐标和包括机器可读数据存储介质的计算机系统的机器可读数据存储介质。 本发明提供了用于设计和鉴定位点II配体和核激素受体调节剂的方法。 本发明提供了位点II的配体,NHR的调节剂,包含NHR调节剂的药物组合物,调节NHR的方法,以及通过施用NHR的调节剂治疗疾病的方法。 还提供了设计突变体,突变NHR,Site II结合测定和Site II模型的方法。

    Substituted heteroaryl amide modulators of glucocorticoid receptor, AP-1, and/or NF-kB activity and use thereof
    6.
    发明申请
    Substituted heteroaryl amide modulators of glucocorticoid receptor, AP-1, and/or NF-kB activity and use thereof 有权
    糖皮质激素受体,AP-1和/或NF-kB活性的取代的杂芳基酰胺调节剂及其用途

    公开(公告)号:US20060154973A1

    公开(公告)日:2006-07-13

    申请号:US11330553

    申请日:2006-01-12

    摘要: The present invention relates to new class of non-steroidal compounds 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-associated diseases, and have the structure including all stereoisomers thereof, tautomers thereof, or a prodrug thereof, or a pharmaceutically acceptable salt thereof, wherein X is selected from N, O, and S; Y is N or CR6; Z is a ring; and where R, Ra, Rb, Rc, Rd, R1, R2, R3, R4, and R5 are as 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: 本发明涉及新类型的非甾体化合物,其可用于治疗与糖皮质激素受体,AP-1和/或NF-κB活性调节有关的疾病,包括肥胖症,糖尿病,炎性和免疫相关疾病, 并且具有包括其所有立体异构体,其互变异构体或其前药或其药学上可接受的盐的结构,其中X选自N,O和S; Y是N或CR 6; Z是一个戒指 并且其中R,R a,R b,R b,R c,R d,R 1, R 2,R 3,R 4和R 5如本文所定义。 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。