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    MODULATORS OF THE GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-kB ACTIVITY AND USE THEREOF
    1.
    发明申请
    MODULATORS OF THE GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-kB ACTIVITY AND USE THEREOF 有权
    GLUCOCORTICOID受体的调节剂，AP-1和/或NF-kB活性及其用途

    公开(公告)号：US20100113532A1

    公开(公告)日：2010-05-06

    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： A61K31/4196 ,  C07D249/14 ,  C07D401/10 ,  C07D417/10 ,  A61K31/4439 ,  A61P19/02 ,  A61P3/10 ,  A61P11/06

    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，其前体药物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 the glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof
    2.
    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：US07642273B2

    公开(公告)日：2010-01-05

    申请号：US11330749

    申请日：2006-01-12

    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： C07D401/00 ,  C07D249/08 ,  A61K31/44 ,  A01N43/64

    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）或（II）：其中Q选自N，O和S;其包括其立体异构体，其互变异构体，其前药或其药学上可接受的盐; 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 the glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof
    3.
    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 the glucocorticoid receptor, AP-1, and/or NF-kB activity and use thereof
    4.
    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：US20070179189A1

    公开(公告)日：2007-08-02

    申请号：US11330749

    申请日：2006-01-12

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

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

    IPC分类号： A61K31/4439 ,  A61K31/426 ,  A61K31/4184 ,  C07D403/02

    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）或（II）：其中Q选自N，O和S;其包括其立体异构体，其互变异构体，其前药或其药学上可接受的盐; 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; 并且本文定义了A，B，R，R a，R b，R b，R c和R d。 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 heteroaryl amide modulators of glucocorticoid receptor, AP-1, and/or NF-kB activity and use thereof
    5.
    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。

    Modulators of the glucocorticoid receptor, AP-1, and/or NF-kB activity and use thereof
    6.
    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

    申请人： Bingwei Yang ,  Lidia Doweyko ,  Arthur Doweyko

    发明人： Bingwei Yang ,  Lidia Doweyko ,  Arthur Doweyko

    IPC分类号： A61K31/421 ,  A61K31/426 ,  A61K31/4166

    CPC分类号： C07D277/46 ,  C07D233/90 ,  C07D277/56

    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。

    Heterocyclic modulators of the glucocorticoid receptor, AP-1, and/or NF-kB activity and use thereof
    9.
    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：US20060154962A1

    公开(公告)日：2006-07-13

    申请号：US11330511

    申请日：2006-01-12

    申请人： Bingwei Yang

    发明人： Bingwei Yang

    IPC分类号： A61K31/47 ,  A61K31/44 ,  A61K31/428 ,  A61K31/421 ,  A61K31/426 ,  A61K31/4196 ,  A61K31/4172

    CPC分类号： C07D277/56 ,  A61K31/135 ,  C07D233/88 ,  C07D277/46 ,  C07D417/10 ,  A61K2300/00

    摘要： The invention relates to a class of novel 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 diseases, and have the structure of formula (I) or stereoisomers or prodrugs or solvates or pharmaceutically acceptable salts thereof, wherein Z, R, R4, R5, 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： 本发明涉及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活性调节有关的疾病，包括肥胖症，糖尿病，炎症和免疫疾病，并且具有 式（I）的结构或其立体异构体或前药或溶剂合物或其药学上可接受的盐，其中Z，R，R 4，R 5，R a， 本文定义的，其中R b，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。