Use of cis-Epoxyeicosantrienoic acids and inhibitors of soluble epoxide hydrolase to reduce pulmonary infiltration by neutrophils
    4.
    发明申请
    Use of cis-Epoxyeicosantrienoic acids and inhibitors of soluble epoxide hydrolase to reduce pulmonary infiltration by neutrophils 审中-公开
    使用顺式 - 环氧二十碳三烯酸和可溶性环氧化物水解酶抑制剂来减少嗜中性粒细胞的肺部浸润

    公开(公告)号:US20050222252A1

    公开(公告)日:2005-10-06

    申请号:US10815425

    申请日:2004-03-31

    IPC分类号: A61K31/335

    摘要: It has now been discovered that inhibitors of soluble epoxide hydrolase (“sEH”) are useful in reducing the severity of or inhibiting the progression of obstructive pulmonary diseases, restrictive airway diseases, and asthma. Administering a cis-epoxyeicosantrienoic acid (“EET”) in addition to the inhibitor is at least additive, and may be synergistic, in reducing or inhibiting these conditions and diseases, as measured by reduced numbers of neutrophils present in the lung. The inhibitor of sEH may be a nucleic acid, such as a small interfering RNA.

    摘要翻译: 现在已经发现,可溶性环氧化物水解酶(“sEH”)的抑制剂可用于降低阻塞性肺疾病,限制性气道疾病和哮喘的严重性或抑制其进展。 除了抑制剂之外,还施用顺式 - 环氧二十碳三烯酸(“EET”)至少是添加剂,并且可以协同作用,以减少或抑制这些病症和疾病,如通过减少存在于肺中的嗜中性粒细胞数量所测量的。 sEH的抑制剂可以是核酸,如小干扰RNA。

    Inhibitors of epoxide hydrolases for the treatment of hypertension
    6.
    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

    IPC分类号: A61K31/17 A61K31/66

    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
    8.
    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

    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。