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46 条记录 (耗时 0.035 秒)

    Heterobicyclic compounds useful as kinase inhibitors
    8.
    发明授权
    Heterobicyclic compounds useful as kinase inhibitors 有权
    用作激酶抑制剂的异双环化合物

    公开(公告)号：US08309571B2

    公开(公告)日：2012-11-13

    申请号：US13084622

    申请日：2011-04-12

    申请人： T. G. Murali Dhar ,  Stephen T. Wrobleski

    发明人： T. G. Murali Dhar ,  Stephen T. Wrobleski

    IPC分类号： A01N43/42 ,  A61K31/44 ,  C07D413/00

    CPC分类号： C07D487/04

    摘要： A compound of Formula (I) and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof. Also disclosed are pharmaceutical compositions containing compounds of Formula I, and methods of treating conditions associated with the activity of p38 kinase.

    摘要翻译： 式（I）的化合物及其对映异构体，非对映异构体和药学上可接受的盐。 还公开了含有式I化合物的药物组合物，以及治疗与p38激酶活性相关的病症的方法。

    Modulators of the glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof
    9.
    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。

    Crystalline forms and process for preparing spiro-hydantoin compounds
    10.
    发明授权
    Crystalline forms and process for preparing spiro-hydantoin compounds 有权
    结晶形式和制备螺 - 乙内酰脲化合物的方法

    公开(公告)号：US07381737B2

    公开(公告)日：2008-06-03

    申请号：US11238427

    申请日：2005-09-29

    申请人： Albert J. DelMonte ,  T. G. Murali Dhar ,  Yu Fan ,  Jack Z. Gougoutas ,  Mary F. Malley ,  Douglas D. McLeod ,  Robert E. Waltermire ,  Chenkou Wei

    发明人： Albert J. DelMonte ,  T. G. Murali Dhar ,  Yu Fan ,  Jack Z. Gougoutas ,  Mary F. Malley ,  Douglas D. McLeod ,  Robert E. Waltermire ,  Chenkou Wei

    IPC分类号： A61K31/4188 ,  C07D235/00

    CPC分类号： C07D487/10

    摘要： A process is provided for preparing spiro-hydantoin compounds of the formula II wherein Z is N or CR4b; K and L are independently O or S; Ar is an optionally substituted aryl or heteroaryl; A2 is a linker, G′ is a linker; Q is a linker; and R2, R4a, R4c, and Rh are defined in the specification. The process optionally includes the enantiomeric separation of intermediates to allow preparation of enantiomers of the spiro-hydantoin compounds of formula II. Substituted spiro-hydantoin compounds may be prepared from the spiro-hydantoin compounds of formula II. The spiro-hydantoin compound of formula II and the substituted spiro-hydantoin compounds are useful in the treatment of immune or inflammatory diseases. Also, provided are products made by the instant inventive process and crystalline forms (prepared by any process) of the substituted spiro-hydantoin compound, 5-[(5S,9R)-9-(4-Cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]non-7-ylmethyl]-thiophene-3-carboxylic acid, including solvates and salts thereof, as well as methods of use thereof. Crystalline forms of certain intermediates are provided.

    摘要翻译： 提供了制备式II的螺 - 乙内酰脲化合物的方法，其中Z是N或CR 4b; K和L独立地为O或S; Ar是任选取代的芳基或杂芳基; A 2是连接体，G'是连接体; Q是一个连接符; 和R 2，R 4a，R 4c和R h H在本说明书中定义。 该方法任选地包括中间体的对映异构体分离，以允许制备式II的螺 - 乙内酰脲化合物的对映异构体。 取代的螺 - 乙内酰脲化合物可以由式II的螺 - 乙内酰脲化合物制备。 式II的螺 - 乙内酰脲化合物和取代的螺 - 乙内酰脲化合物可用于治疗免疫或炎性疾病。 此外，提供的是本发明方法制备的产物和取代的螺 - 乙内酰脲化合物的5 - [（5S，9R）-9-（4-氰基苯基）-3-（3， 5-二氯苯基）-1-甲基-2,4-二氧代-1,3,7-三氮杂螺[4.4]壬-7-基甲基] - 噻吩-3-甲酸，包括其溶剂合物及其盐，以及 使用它。 提供某些中间体的结晶形式。