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

    Modulators of the glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof
    4.
    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
    5.
    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
    6.
    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 glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof
    8.
    发明授权
    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活性的调节剂及其用途

    公开(公告)号：US08067447B2

    公开(公告)日：2011-11-29

    申请号：US12513192

    申请日：2007-10-31

    申请人： James E. Sheppeck ,  John L. Gilmore ,  T. G. Murali Dhar ,  Hai-Yun Xiao

    发明人： James E. Sheppeck ,  John L. Gilmore ,  T. G. Murali Dhar ,  Hai-Yun Xiao

    IPC分类号： A61K31/433 ,  A61K31/416 ,  C07D285/135 ,  C07D231/56 ,  C07D231/40

    CPC分类号： C07D231/56 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07D417/14

    摘要： Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, and/or AP-1, and/or NF-κB activity including inflammatory and immune diseases, obesity and diabetes having the structure of formula (I), its enantiomers, diastereomers, or a pharmaceutically-acceptable salt, or hydrate, thereof, wherein (Ia) is heterocycle or heteroaryl; J, Ja, E, F, G, Ma, M, Q, Za and Z 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，其可用于治疗与调节糖皮质激素受体，和/或AP-1和/或NF-κB活性相关的疾病，包括炎性和免疫疾病，肥胖症和糖尿病，其结构为 式（I），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（Ia）是杂环或杂芳基; J，Ja，E，F，G，Ma，M，Q，Za和Z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。

    Process for preparing azacycloalkanoylaminothiazoles
    10.
    发明授权
    Process for preparing azacycloalkanoylaminothiazoles 有权
    制备氮杂环烷酰氨基噻唑的方法

    公开(公告)号：US06639074B2

    公开(公告)日：2003-10-28

    申请号：US10100129

    申请日：2002-03-18

    申请人： Bang-Chi Chen ,  Kyoung S. Kim ,  S. David Kimball ,  Raj N. Misra ,  Mark E. Salvati ,  Joseph E. Sundeen ,  Hai-Yun Xiao ,  Rulin Zhao

    发明人： Bang-Chi Chen ,  Kyoung S. Kim ,  S. David Kimball ,  Raj N. Misra ,  Mark E. Salvati ,  Joseph E. Sundeen ,  Hai-Yun Xiao ,  Rulin Zhao

    IPC分类号： C07D47100

    CPC分类号： C07D417/12 ,  A61K31/427 ,  A61K31/454 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D417/14

    摘要： The present invention relates to new, efficient processes for the preparation of 5-(2-oxazolylalkylthio)-2-azacycloalkanoylaminothiazole compounds of formula I or a pharmaceutically acceptable salt thereof, wherein: R is alkyl, aryl or heteroaryl; R1, R2, R3, R4 and R5 are each independently hydrogen, alkyl, aryl or heteroaryl; R6 and R7 are each independently hydrogen, alkyl, aryl, heteroaryl, halogen, hydroxy or alkoxy; R8 is hydrogen, alkyl, aryl, heteroaryl, CONR9R10, COR11 or COOR12; R9, R10, R11 and R12 are each independently hydrogen, alkyl or aryl; m equals 0 to 5; and n equals 0 to 5, which are novel, potent inhibitors of cyclin dependent kinases (cdks). The present invention further concerns new key intermediate compounds, a quaternary ammonium salt of formula III′ and a 2-oxazolylalkyl derivative of formula IX.

    摘要翻译： 本发明涉及制备式I的5-（2-恶唑基烷硫基）-2-氮杂环烷酰氨基噻唑化合物或其药学上可接受的盐的新的，有效的方法，其中：R是烷基，芳基或杂芳基; R 1，R 2 R 3，R 4和R 5各自独立地为氢，烷基，芳基或杂芳基; R 6和R 7各自独立地为氢，烷基，芳基，杂芳基，卤素 ，羟基或烷氧基; R 8是氢，烷基，芳基，杂芳基，CONR 9 R 10，COR 11或COOR 12; R 9，R 10，R 11 且R 12各自独立地为氢，烷基或芳基; m等于0至5; 和等于0至5，这是细胞周期蛋白依赖性激酶（cdks）的新型有效抑制剂。 本发明还涉及新的关键中间体化合物，式III'的季铵盐和式IX的2-恶唑基烷基衍生物。