Inhibition of glutathione transferase by haloenol lactones
    5.
    发明授权
    Inhibition of glutathione transferase by haloenol lactones 失效
    通过卤代烯内酯抑制谷胱甘肽转移酶

    公开(公告)号:US06495370B1

    公开(公告)日:2002-12-17

    申请号:US09639392

    申请日:2000-08-15

    IPC分类号: G01N3300

    摘要: This invention relates to novel haloenol lactone compounds. These compounds have the following general structure: in which Ar is an aryl group and Y is a haloenol lactone moiety. The compounds of the invention are useful for the specific measurement of particular isoenzymes of glutathione S-transferase. Measurement of glutathione S-transferase isoenzymes has importance in diagnostic medicine. The compounds of the invention are also useful for treatment of drug resistance in cancer and for preventing herbicide resistance in plants.

    摘要翻译: 本发明涉及新的卤烯醇内酯化合物。 这些化合物具有以下一般结构:其中Ar是芳基,Y是卤代烯内酯部分。本发明的化合物可用于特异性测量谷胱甘肽S-转移酶的特定同工酶。 谷胱甘肽S-转移酶同工酶的测定在诊断医学中具有重要意义。 本发明的化合物还可用于治疗癌症中的耐药性和用于防止植物中的除草剂抗性。

    Inhibitors of epoxide hydrolases for the treatment of hypertension
    10.
    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。