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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 GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-kB ACTIVITY AND USE THEREOF
    6.
    发明申请
    MODULATORS OF 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：US20100063051A1

    公开(公告)日：2010-03-11

    申请号：US12513187

    申请日：2007-10-31

    申请人： Bingwei Vera Yang ,  Lidia M. Doweyko ,  Wayne Vaccaro ,  Tram N. Huynh ,  David R. Tortolani ,  T.G. Murali Dhar

    发明人： Bingwei Vera Yang ,  Lidia M. Doweyko ,  Wayne Vaccaro ,  Tram N. Huynh ,  David R. Tortolani ,  T.G. Murali Dhar

    IPC分类号： A61K31/5377 ,  C07D277/38 ,  C07D417/12 ,  A61K31/426 ,  A61P37/00 ,  A61P29/00

    CPC分类号： C07D211/58 ,  C07C235/36 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07D213/75 ,  C07D231/40 ,  C07D233/88 ,  C07D239/42 ,  C07D277/46 ,  C07D277/82 ,  C07D285/08 ,  C07D285/135 ,  C07D417/04 ,  C07D417/10 ,  C07D417/12

    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) an enantiomer, diastereomer, tautomer, solvate (e.g. a hydrate), or a pharmaceutically-acceptable salt, thereof, wherein: M is selected from alkyl, substituted alkyl, cycloalkyl, aryl, heterocyclo, and heteroaryl, provided that if M is alkyl then R6 and R7 taken together with the carbon atom to which they are both attached are selected from a group other than cycloalkyl; Q is selected from (i) hydrogen, C1-C4 alkyl, and substituted C1-C4 alkyl; or (ii) Q and R6 are combined with the carbon atoms to which they are attached to form a 3- to 6-membered cycloalkyl; or (iii) Q and MaM are combined with the carbon atom(s) to which they are attached to form a 3- to 7-membered ring containing 1-2 heteroatoms which are independently selected from the group consisting of O, S, SO2, and N which ring may be optionally substituted with 0-2 R5 groups or carbonyl; Z is selected from cycloalkyl, heterocyclo, aryl, or heteroaryl; and Ma, Za, R1, R2, R3, R4, R6, R7, and R22 are as defined herein. Also provided are pharmaceutical compositions and methods of treating metabolic and inflammatory- or immune-associated diseases or disorders using 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，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 ），对映体，非对映体，互变异构体，溶剂合物（例如水合物）或其药学上可接受的盐，其中：M选自烷基，取代的烷基，环烷基，芳基，杂环和杂芳基，条件是如果M是烷基 那么R6和R7与它们所连接的碳原子一起选自除环烷基以外的基团; Q选自（i）氢，C 1 -C 4烷基和取代的C 1 -C 4烷基; 或（ii）Q和R 6与它们所连接的碳原子结合形成3-至6-元环烷基; 或（iii）Q和MaM与它们所连接的碳原子一起形成含有1-2个杂原子的3-至7-元环，其独立地选自O，S，SO 2 和N，该环可以任选地被0-2个R5基或羰基取代; Z选自环烷基，杂环基，芳基或杂芳基; 并且Ma，Za，R 1，R 2，R 3，R 4，R 6，R 7和R 22如本文所定义。 还提供了使用所述化合物治疗代谢和炎症或免疫相关疾病或病症的药物组合物和方法。

    MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-kB ACTIVITY AND USE THEREOF
    7.
    发明申请
    MODULATORS OF 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：US20090075995A1

    公开(公告)日：2009-03-19

    申请号：US11835438

    申请日：2007-08-08

    申请人： David S. Weinstein ,  Ping Chen ,  T.G. Murali Dhar ,  Jingwu Duan ,  Hua Gong ,  Bin Jiang ,  Bingwei Vera Yang ,  Arthur M. Doweyko

    发明人： David S. Weinstein ,  Ping Chen ,  T.G. Murali Dhar ,  Jingwu Duan ,  Hua Gong ,  Bin Jiang ,  Bingwei Vera Yang ,  Arthur M. Doweyko

    IPC分类号： A61K31/5377 ,  A61K31/436 ,  C07D491/052 ,  A61P31/12 ,  A61K31/427 ,  C07D417/12

    CPC分类号： C07D417/12 ,  C07D277/46 ,  C07D405/12 ,  C07D417/14 ,  C07D491/04

    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, having the structure of formula (I): an enantiomer, diastereomer, or tautomer thereof, or a prodrug ester thereof, or a pharmaceutically-acceptable salt thereof, in which: Z is heterocyclo or heteroaryl; A is a 5- to 8-membered carbocyclic ring or a 5- to 8-membered heterocyclic ring; B is a cycloalkyl, cycloalkenyl, aryl, heterocyclo, or heteroaryl ring, wherein each ring is fused to the A ring on adjacent atoms and optionally substituted by one to four groups which are the same or different and are independently selected from R5, R6, R7, and R8; J1, J2, and J3 are at each occurrence the same or different and are independently -A1QA2-; Q is a bond, O, S, S(O), or S(O)2; A1 and A2 are the same or different and are at each occurrence independently selected from a bond, C1-3alkylene, substituted C1-3alkylene, C2-4alkenylene, and substituted C2-4alkenylene, provided that A1 and A2 are chosen so that ring A is a 5- to 8-membered carbocyclic or heterocyclic ring; R1 to R11 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，其可用于治疗与式（I）结构的糖皮质激素受体，AP-1和/或NF-κB活性（包括炎症和免疫疾病）调节相关的疾病：对映异构体 ，非对映异构体或其互变异构体，或其前药酯或其药学上可接受的盐，其中：Z是杂环或杂芳基; A是5至8元碳环或5至8元杂环; B是环烷基，环烯基，芳基，杂环基或杂芳基环，其中每个环与相邻原子上的A环稠合并任选地被一至四个相同或不同的基团取代，并且独立地选自R5，R6， R7和R8; J1，J2和J3各自出现相同或不同，独立地为-A1QA2-; Q是键，O，S，S（O）或S（O）2; A1和A2相同或不同，并且在每次出现时独立地选自键，C1-3亚烷基，取代的C1-3亚烷基，C2-4亚烯基和取代的C2-4亚烯基，条件是选择A1和A2使得环A为 5-至8-元碳环或杂环; R1至R11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。