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    Modulators of glucocorticoid receptor, AP-1, and/or NF-kB activity, and use thereof
    3.
    发明申请
    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活性的调节剂及其用途

    公开(公告)号：US20070129400A1

    公开(公告)日：2007-06-07

    申请号：US11451660

    申请日：2006-06-13

    Applicant: Jingwu Duan ,  Zhonghui Lu ,  David Weinstein ,  Bin Jiang

    Inventor： Jingwu Duan ,  Zhonghui Lu ,  David Weinstein ,  Bin Jiang

    IPC: A61K31/4709 ,  A61K31/4439 ,  A61K31/428 ,  A61K31/427 ,  A61K31/416 ,  C07D417/02 ,  C07D403/02 ,  C07D405/02 ,  C07D409/02

    CPC classification number: C07D401/04 ,  C07D231/56 ,  C07D401/06 ,  C07D403/04 ,  C07D405/04 ,  C07D405/06 ,  C07D409/06 ,  C07D417/06 ,  C07D417/12

    Abstract: 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 an enantiomer, a diastereomer, a pharmaceutically acceptable salt, or hydrate thereof, where J is selected from NR1 or C(R4)(R4a); K is selected from NR2 or C(R5)(R5a); L is selected from NR3 or C(R6)(R6a); and A, X, Y, R1, R2, R3, R4, R4a, R5, R5a, R6, R6a, R8, R10, R11, and n are defined herein. Also provided are pharmaceutical compositions and methods of treating obesity, diabetes and inflammatory or immune associated diseases comprising said compounds.

    Abstract translation: 提供非甾体化合物，其可用于治疗与糖皮质激素受体，AP-1和/或NF-κB活性（包括肥胖症，糖尿病，炎症和免疫疾病）的调节相关的疾病，并且具有式（I）的结构， 或其对映异构体，非对映异构体，药学上可接受的盐或水合物，其中J选自NR 1或C（R 4 S 4）（R 4a） / SUB>）; K选自NR 2或C（R 5）（R 5a）; L选自NR 3或C（R 6 S）（R 6a）; 和A，X，Y，R 1，R 2，R 3，R 4，R SUB R 4a，R 5，R 5a，R 6，R 6a，R SUB， R 8，R 11，R 11和n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。

    FUSED HETEROARYL MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-kappaB ACTIVITY AND USE THEREOF
    4.
    发明申请
    FUSED HETEROARYL MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-kappaB ACTIVITY AND USE THEREOF 有权
    GLUCOCORTICOID受体，AP-1和/或NF-κB活性的融合血管调节剂及其用途

    公开(公告)号：US20110002952A1

    公开(公告)日：2011-01-06

    申请号：US12866270

    申请日：2009-02-05

    Applicant: Jingwu Duan ,  David S. Weinstein ,  Bin Jiang

    Inventor： Jingwu Duan ,  David S. Weinstein ,  Bin Jiang

    IPC: A61K31/5377 ,  C07D491/147 ,  A61K31/4375 ,  A61K38/26 ,  A61K38/28 ,  A61K39/00 ,  A61P37/00 ,  A61P29/00 ,  A61P3/00 ,  A61P37/06 ,  A61P19/02 ,  A61P25/00 ,  A61P11/06 ,  A61P1/00 ,  A61P17/06

    CPC classification number: C07D491/147

    Abstract: Novel non-steroidal compounds are provided which are useful in treating diseases or disorders associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity, including metabolic and inflammatory and immune diseases or disorders, 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; B1 and B2 rings are pyridyl rings, wherein the B1 and B2 rings are each fused to the A ring and the B1 ring is optionally substituted by one to three groups which are the same or different and are independently selected from R1, R2, and R4, and the B2 ring is optionally substituted by one to three groups which are the same or different and are independently selected from R3, R7, and R3 71, J2, and J3 are at each occurrence the same or different and are independently -AIQA2-; Q is a bond, O, S, S(0), or S(O)2; A1 and A2 are the same or different and are at each occurrence independently selected from a bond, C1-3 alkylene, substituted C1-3 alkylene, C24 alkenylene, and substituted C24 alkenylene, 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.

    Abstract translation: 提供新的非甾体化合物，其可用于治疗与调节糖皮质激素受体，AP-1和/或NF-κB活性相关的疾病或病症，包括具有结构的代谢和炎症和免疫疾病或病症 式（I）的化合物：其对映异构体，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是杂环基或杂芳基; -A是5-至8-元碳环或5-至8-元杂环; B1和B2环是吡啶环，其中B1和B2环各自与A环稠合，B1环任选被一至三个相同或不同并且独立地选自R 1，R 2和R 4的基团取代 并且B2环任选地被一至三个相同或不同并且独立地选自R3，R7和R371的基团取代，J2和J3在每次出现时相同或不同，并且独立地为-AIQA2- ; Q是键，O，S，S（0）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，C24亚烯基和取代的C24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。

    Indane modulators of glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof
    7.
    发明授权
    Indane 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活性的吲哚调节剂及其用途

    公开(公告)号：US08324401B2

    公开(公告)日：2012-12-04

    申请号：US12542762

    申请日：2009-08-18

    Applicant: Jingwu Duan ,  Bin Jiang

    Inventor： Jingwu Duan ,  Bin Jiang

    IPC: A61K31/4164 ,  A61K31/426 ,  C07D233/54

    CPC classification number: C07D285/135 ,  C07D233/76 ,  C07D249/12 ,  C07D277/46 ,  C07D285/08

    Abstract: Novel non-steroidal compounds are provided that 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 having the structure of formula (I): or enantiomers, diastereomers, or a pharmaceutically-acceptable salt, or hydrate, thereof, where X is A1QA2-; Q is a bond, —C(═O)—, —OC(O)—, —C(═O)NR5—, —SOp—, —SOpNR5—, —C(O)O—, —NR5C(O)—, —OC(O)NR5—, —NR5C(O)O—, —S(O)pNR5C(O)—, —C(O)NR5S(O)p— —NR5S(O)p—, or —NR5C(═O)NR6—. Y is selected from hydrogen, C1-6alkyl, OR16, substituted C1-6alkyl, cycloalkyl, aryl, heterocyclo and heteroaryl. A1 and A2 are independently selected from a bond, C1-3alkylene, or C1-3alkenylene, and R1-R11 are defined herein. Also provided are pharmaceutical compositions, combinations, and methods of treating obesity, diabetes and inflammatory- or immune-associated diseases comprising said compounds.

    Abstract translation: 提供新的非甾体化合物，其可用于治疗与糖皮质激素受体，AP-1和/或NF-κB活性相关的疾病，所述疾病包括具有式（I）结构的肥胖症，糖尿病，炎症和免疫疾病 ）：或其对映异构体，非对映体或其药学上可接受的盐或水合物，其中X为AlQA2-; Q是键，-C（= O） - ， - OC（O） - ， - C（= O）NR5-，-SOp-，-SOpNR5-，-C（O） - （O）NR 5 - ， - NR 5 C（O）O-，-S（O）pNR 5 C（O） - ， - C（O）NR 5 S（O） NR5C（= O）NR6-。 Y选自氢，C 1-6烷基，OR 16，取代的C 1-6烷基，环烷基，芳基，杂环和杂芳基。 A1和A2独立地选自键，C1-3亚烷基或C1-3亚烯基，R1-R11在本文中定义。 还提供了治疗包含所述化合物的肥胖症，糖尿病和炎性或免疫相关疾病的药物组合物，组合和方法。

    Modulators of the glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof
    8.
    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：US07625921B2

    公开(公告)日：2009-12-01

    申请号：US11034822

    申请日：2005-01-13

    Applicant: Jingwu Duan ,  James Sheppeck ,  Bin Jiang ,  John L. Gilmore

    Inventor： Jingwu Duan ,  James Sheppeck ,  Bin Jiang ,  John L. Gilmore

    IPC: A61K31/4748 ,  C07D401/14 ,  C07D417/12

    CPC classification number: C07D471/08 ,  C07D401/12 ,  C07D401/14 ,  C07D417/12 ,  C07D417/14

    Abstract: 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.

    Abstract translation: 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，或其溶剂合物或其前药，或其药学上可接受的盐，其中Z为CONR1R2或CH2NR1R2，并且其中X1-X8中的至少一个为N，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。

    Indane modulators of glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof
    9.
    发明授权
    Indane 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活性的吲哚调节剂及其用途

    公开(公告)号：US07592461B2

    公开(公告)日：2009-09-22

    申请号：US11642508

    申请日：2006-12-20

    Applicant: Jingwu Duan ,  Bin Jiang

    Inventor： Jingwu Duan ,  Bin Jiang

    IPC: A61K31/426 ,  A61K31/433 ,  C07D277/46 ,  C07D285/135

    CPC classification number: C07D285/135 ,  C07D233/76 ,  C07D249/12 ,  C07D277/46 ,  C07D285/08

    Abstract: Novel non-steroidal compounds are provided that 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 having the structure of formula (I): or enantiomers, diastereomers, or a pharmaceutically-acceptable salt, or hydrate, thereof, where X is -A1QA2-; Q is a bond, —C(═O)—, —OC(O)—, —C(═O)NR5—, —SOp—, —SOpNR5—, —C(O)O—, —NR5C(O)—, —OC(O)NR5—, —NR5C(O)O—, —S(O)pNR5C(O)—, —C(O)NR5S(O)p— —NR5S(O)p—, or —NR5C(═O)NR6—. Y is selected from hydrogen, C1-6alkyl, OR16, substituted C1-6alkyl, cycloalkyl, aryl, heterocyclo and heteroaryl. A1 and A2 are independently selected from a bond, C1-3alkylene, or C1-3alkenylene, and R1-R11 are defined herein. Also provided are pharmaceutical compositions, combinations, and methods of treating obesity, diabetes and inflammatory- or immune-associated diseases comprising said compounds.

    Abstract translation: 提供了新型非甾体化合物，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，包括具有式（I）结构的肥胖症，糖尿病，炎症和免疫疾病： 或对映异构体，非对映异构体或其药学上可接受的盐或水合物，其中X为-A1QA2-; Q是键，-C（-O） - ， - OC（O） - ， - C（-O）NR5-，-SOp-，-SOpNR5-，-C（O） - （O）NR 5 - ， - NR 5 C（O）O-，-S（O）p NR 15 C（O） - ， - C（O）NR 5 S（O）p - ， - -NR 5 C（-O）NR 6 - 。 Y选自氢，C 1-6烷基，OR 16，取代的C 1-6烷基，环烷基，芳基，杂环和杂芳基。 A1和A2独立地选自键，C1-3亚烷基或C1-3亚烯基，R1-R11在本文中定义。 还提供了治疗包含所述化合物的肥胖症，糖尿病和炎性或免疫相关疾病的药物组合物，组合和方法。

    Modulators of the glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof
    10.
    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：US07569689B2

    公开(公告)日：2009-08-04

    申请号：US11034652

    申请日：2005-01-13

    Applicant: Jingwu Duan ,  Bin Jiang ,  James Sheppeck ,  John L. Gilmore

    Inventor： Jingwu Duan ,  Bin Jiang ,  James Sheppeck ,  John L. Gilmore

    IPC: A61K31/498 ,  C07D417/14

    CPC classification number: C07D403/12 ,  C07D241/36 ,  C07D417/12 ,  C07D417/14

    Abstract: 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.

    Abstract translation: 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，或其溶剂合物，或其前药，或其药学上可接受的盐，其中Z为CONR1R2或CH2NR1R2，并且其中X1-X4和/或X5-X8中的至少两个为N或NR18 ，R，R a，R b，R c，R d，R 1，R 2和R 18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。

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