利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

30 条记录 (耗时 0.043 秒)

    Inhibitors of epoxide hydrolases for the treatment of hypertension
    3.
    发明申请
    Inhibitors of epoxide hydrolases for the treatment of hypertension 审中-公开
    环氧化物水解酶抑制剂治疗高血压

    公开(公告)号：US20060035869A1

    公开(公告)日：2006-02-16

    申请号：US11240444

    申请日：2005-09-29

    申请人： Bruce Hammock ,  Christophe Morisseau ,  Jiang Zheng ,  Marvin Goodrow ,  Tonya Severson ,  James Sanborn

    发明人： Bruce Hammock ,  Christophe Morisseau ,  Jiang Zheng ,  Marvin Goodrow ,  Tonya Severson ,  James Sanborn

    IPC分类号： A61K31/17 ,  A61K31/66

    CPC分类号： A61K31/325 ,  A61K31/00 ,  A61K31/336

    摘要： Biologically stable inhibitors of soluble epoxide hydrolases are provided. The inhibitors can be used, for example, to selectively inhibit epoxide hydrolase in therapeutic applications such as treating inflammation, for use in affinity separations of the epoxide hydrolases, and in agricultural applications. A preferred class of compounds for practicing the invention have the structure shown by Formula 1 wherein X and Y is each independently nitrogen, oxygen, or sulfur, and X can further be carbon, at least one of R1-R4 is hydrogen, R2 is hydrogen when X is nitrogen but is not present when X is sulfur or oxygen, R4 is hydrogen when Y is nitrogen but is not present when Y is sulfur or oxygen, R1 and R3 are each independently a substituted or unsubstituted alkyl, haloalkyl, cycloalkyl, aryl, acyl, or heterocyclic, or being a metabolite or degradation product thereof.

    摘要翻译： 提供了生物稳定的可溶性环氧化物水解酶抑制剂。 抑制剂可用于例如在治疗应用中选择性抑制环氧化物水解酶，例如治疗炎症，用于环氧化物水解酶的亲和分离，以及在农业应用中。 用于实施本发明的一类优选的化合物具有式1所示的结构，其中X和Y各自独立地为氮，氧或硫，X可以进一步为碳，R 1， -R 4是氢，当X是氮时，R 2是氢，但当X是硫或氧时，R 2不是存在的，R 4是氢 当Y为氮时，当Y为硫或氧时不存在，R 1和R 3各自独立地为取代或未取代的烷基，卤代烷基，环烷基，芳基，酰基 ，或杂环，或其代谢产物或降解产物。

    Inhibitors of epoxide hydrolases for the treatment of hypertension
    7.
    发明申请
    Inhibitors of epoxide hydrolases for the treatment of hypertension 审中-公开
    环氧化物水解酶抑制剂治疗高血压

    公开(公告)号：US20050282767A1

    公开(公告)日：2005-12-22

    申请号：US11189964

    申请日：2005-07-25

    申请人： Deanna Kroetz ,  Darryl Zeldin ,  Bruce Hammock ,  Christophe Morisseau

    发明人： Deanna Kroetz ,  Darryl Zeldin ,  Bruce Hammock ,  Christophe Morisseau

    IPC分类号： A61K31/00 ,  A61K31/325 ,  A61K31/336 ,  A61K48/00

    CPC分类号： A61K31/325 ,  A61K31/00 ,  A61K31/336

    摘要： The invention provides compounds that inhibit epoxide hydrolase in therapeutic applications for treating hypertension. A preferred class of compounds for practicing the invention have the structure shown by Formula I wherein Z is oxygen or sulfur, W is carbon phosphorous or sulfur, X and Y is each independently nitrogen, oxygen, or sulfur, and X can further be carbon, at least one of R1—R4 is hydrogen, R2 is hydrogen when X is nitrogen but is not present when X is sulfur or oxygen, R4 is hydrogen when Y is nitrogen but is not present when Y is sulfur or oxygen, R1 and R3 is each independently C1-C20 substituted or unsubstituted alkyl, cycloalkyl, aryl, acyl, or heterocyclic.

    摘要翻译： 本发明提供在治疗高血压的治疗应用中抑制环氧化物水解酶的化合物。 用于实施本发明的优选类化合物具有式I所示的结构，其中Z是氧或硫，W是碳磷或硫，X和Y各自独立地是氮，氧或硫，并且X还可以是碳， R 1至R 4中的至少一个为氢，当X为氮时，R 2为氢，但当X为硫或不存在时不存在 当Y为氮时，氧，R 4为氢，但当Y为硫或氧时不存在，R 1和R 3各自独立地为 C 1 -C 20取代或未取代的烷基，环烷基，芳基，酰基或杂环。

    Pyrazole inhibitors of COX-2 and sEH
    9.
    发明授权
    Pyrazole inhibitors of COX-2 and sEH 有权
    吡唑类抑制剂COX-2和sEH

    公开(公告)号：US09096532B2

    公开(公告)日：2015-08-04

    申请号：US13993317

    申请日：2011-12-12

    申请人： Bruce D. Hammock ,  Sung Hee Hwang ,  Karen Wagner ,  Christophe Morisseau ,  Aaron Wecksler ,  Guodong Zhang

    发明人： Bruce D. Hammock ,  Sung Hee Hwang ,  Karen Wagner ,  Christophe Morisseau ,  Aaron Wecksler ,  Guodong Zhang

    IPC分类号： A61K31/635 ,  C07D231/10 ,  C07D231/12 ,  C07D231/40 ,  C07D231/14

    CPC分类号： C07D231/12 ,  C07D231/14 ,  C07D231/40

    摘要： The present invention provides compounds and compositions, e.g., a series of compounds wherein a 1,5-biarylpyrazole group is conjugated to a urea group by a non-cleavable covalent chain, that are useful as dual COX-2/sEH inhibitors. The compounds disclosed herein have activity associated with the arachidonate cascade. The activity of these compounds was demonstrated using a lipopolysaccharide (LPS) induced model of pain in the rat. The compounds of the present invention demonstrated superior anti-allodynic activity as compared to the same dose of celecoxib, i.e., a COX-2 inhibitor, also as compared to the same dose of t-AUCB, i.e., a sEH inhibitor, and also as compared to the co-administered same dose of both celecoxib and t-AUCB. The dual inhibitors of the present invention demonstrate enhanced in vivo anti-allodynic activity in a nociceptive behavioral assay. In addition, the compounds of the present invention also demonstrated to have potent anti-angiogenic effects toward endothelial cells (HUVEC) and inhibit angiogenesis in vitro, ex vivo and in vivo. The dual inhibitors of the present invention also demonstrate anti-angiogenic effect to slow breast tumor growth in vivo.

    摘要翻译： 本发明提供化合物和组合物，例如一系列化合物，其中1,5-双芳基吡唑基团可通过不可裂解的共价链与脲基团缀合，其可用作双重COX-2 / sEH抑制剂。 本文公开的化合物具有与花生四烯酸级联相关的活性。 使用脂多糖（LPS）诱导的大鼠疼痛模型证明了这些化合物的活性。 与相同剂量的塞来昔布（即，COX-2抑制剂）相比，本发明的化合物与同样剂量的t-AUCB（即sEH抑制剂）相比，表现出优异的抗异常性疼痛活性，并且还作为 与联合给药相同剂量的塞来昔布和t-AUCB相比。 本发明的双重抑制剂在伤害性行为测定中表现出增强的体内抗异常性疼痛活性。 此外，本发明的化合物还证明对体内，体内和体内对内皮细胞（HUVEC）具有有效的抗血管生成作用并抑制血管生成。 本发明的双重抑制剂还表现出对血管内肿瘤生长缓慢的抗血管生成作用。