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18 条记录 (耗时 0.069 秒)

    Substituted heteroaryl amide modulators of glucocorticoid receptor, AP-1, and/or NF-kB activity and use thereof
    3.
    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

    申请人： James Sheppeck ,  T.G. Dhar ,  Lidia Doweyko ,  John Gilmore ,  David Weinstein ,  Hai-Yun Xiao ,  Bingwei Yang ,  Arthur Doweyko

    发明人： James Sheppeck ,  T.G. Dhar ,  Lidia Doweyko ,  John Gilmore ,  David Weinstein ,  Hai-Yun Xiao ,  Bingwei Yang ,  Arthur Doweyko

    IPC分类号： A61K31/433 ,  A61K31/4245 ,  A61K31/4196

    CPC分类号： C07D233/91 ,  C07D277/46 ,  C07D417/06

    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。

    Heterocyclic modulators of the glucocorticoid receptor, AP-1, and/or NF-kB activity and use thereof
    7.
    发明申请
    Heterocyclic 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活性的杂环调节剂及其用途

    公开(公告)号：US20050182083A1

    公开(公告)日：2005-08-18

    申请号：US11035290

    申请日：2005-01-13

    申请人： David Weinstein ,  James Sheppeck ,  John Gilmore

    发明人： David Weinstein ,  James Sheppeck ,  John Gilmore

    IPC分类号： A61K31/4745 ,  C07D403/12 ,  C07D471/18 ,  C07D487/04

    CPC分类号： C07D471/18

    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 obesity, diabetes, inflammatory and immune diseases, and have the structure of formula (I) or stereoisomers or prodrugs or solvates or pharmaceutically acceptable salts thereof, wherein A, B, J, K, Z, 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： 提供了新的非甾体化合物，其可用于治疗与糖皮质激素受体，AP-1和/或NF-κB活性的调节相关的疾病，包括肥胖，糖尿病，炎症和免疫疾病，并且具有式（I ）或其立体异构体或前药或溶剂化物或其药学上可接受的盐，其中A，B，J，K，Z，R，R a，R b， C和/或D，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 the glucocorticoid receptor, AP-1, and/or NF-kappaB activity and use thereof
    8.
    发明申请
    Modulators of the glucocorticoid receptor, AP-1, and/or NF-kappaB 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：US20050176716A1

    公开(公告)日：2005-08-11

    申请号：US11034652

    申请日：2005-01-13

    申请人： Jingwu Duan ,  Bin Jiang ,  James Sheppeck ,  John Gilmore

    发明人： Jingwu Duan ,  Bin Jiang ,  James Sheppeck ,  John Gilmore

    IPC分类号： A01N43/58 ,  A01N43/60 ,  A61K31/495 ,  A61K31/498 ,  A61K31/50 ,  C07D241/36 ,  C07D403/12 ,  C07D417/02 ,  C07D417/12 ,  C07D417/14 ,  C07D43/02

    CPC分类号： C07D403/12 ,  C07D241/36 ,  C07D417/12 ,  C07D417/14

    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) its stereoisomers thereof, or a solvate thereof, or a prodrug thereof, or a pharmaceutically acceptable salt thereof, where Z is CONR1R2 or CH2NR1R2 and where at least two of X1-X4 and/or X5-X8 is N or NR18, and R, Ra, Rb, Rc, Rd, R1, R2 and R18 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）其立体异构体，或其溶剂化物，或其前药，或其药学上可接受的盐，其中Z为CONR 1，R 2或CH 2 > 2个NR 2 R 2，并且其中X 1 -X 4中的至少两个和 /或X 5 -X 8是N或NR 18，R，R a，R SUP R 1，R 2，R 2，R 2，R 2，R 2， > 18 。 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 the glucocorticoid receptor, AP-1, and/or NF-kB activity and use thereof
    9.
    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：US20050182082A1

    公开(公告)日：2005-08-18

    申请号：US11034822

    申请日：2005-01-13

    申请人： Jingwu Duan ,  James Sheppeck ,  Bin Jiang ,  John Gilmore

    发明人： Jingwu Duan ,  James Sheppeck ,  Bin Jiang ,  John Gilmore

    IPC分类号： A61K31/439 ,  A61K31/473 ,  A61K31/4748 ,  C07D221/28 ,  C07D401/12 ,  C07D401/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/08

    CPC分类号： C07D471/08 ,  C07D401/12 ,  C07D401/14 ,  C07D417/12 ,  C07D417/14

    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) its stereoisomers thereof, or a solvate thereof, or a prodrug thereof, or a pharmaceutically acceptable salt thereof, where Z is CONR1R2 or CH2NR1R2 and where at least one of X1-X8 is N, and 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）其立体异构体，或其溶剂化物，或其前药，或其药学上可接受的盐，其中Z为CONR 1，R 2或CH 2 > 2 1 2 其中X 1 -X 8中的至少一个为 N和R，R a，O，R b，R c和R d都在本文中定义。 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。

    Substituted 1,3-dihydro-imidazol-2-one and 1,3-dihydro-imidazol-2-thione derivatives as inhibitors of matrix metalloproteinases and/or TNF-alpha converting enzyme (TACE)
    10.
    发明申请
    Substituted 1,3-dihydro-imidazol-2-one and 1,3-dihydro-imidazol-2-thione derivatives as inhibitors of matrix metalloproteinases and/or TNF-alpha converting enzyme (TACE) 有权
    取代的1,3-二氢 - 咪唑-2-酮和1,3-二氢 - 咪唑-2-硫酮衍生物作为基质金属蛋白酶和/或TNF-α转化酶（TACE）的抑制剂，

    公开(公告)号：US20050075384A1

    公开(公告)日：2005-04-07

    申请号：US10946418

    申请日：2004-09-21

    申请人： James Sheppeck ,  John Gilmore

    发明人： James Sheppeck ,  John Gilmore

    IPC分类号： C07D401/12 ,  A61K31/4164 ,  C07D233/30

    CPC分类号： C04B35/632 ,  C07D401/12

    摘要： The present invention describes novel 1,3-dihydro-imidazol-2-one or 1,3-dihydro-imidazol-2-thione compounds of formula (I): or a stereoisomer or pharmaceutically acceptable salt or solvate thereof, wherein A, L R1, R2, R3 and R4 are defined in the present specification, which are useful as selective inhibitors of MMP, TACE, aggrecanase or a combination thereof. This invention also relates to pharmaceutical compositions comprising these compounds and methods of using the same.

    摘要翻译： 本发明描述了式（I）的新型1,3-二氢 - 咪唑-2-酮或1,3-二氢 - 咪唑-2-硫酮化合物或其立体异构体或药学上可接受的盐或溶剂化物，其中A，LR 本说明书中定义了R 2，R 3和R 4，其可用作MMP，TACE，聚蛋白聚糖蛋白聚糖酶或其组合的选择性抑制剂。 本发明还涉及包含这些化合物的药物组合物及其使用方法。