USE OF CIS-EPOXYEICOSATRIENOIC ACIDS AND INHIBITORS OF SOLUBLE EPOXIDE HYDROLASE TO TREAT CONDITIONS MEDIATED BY PBR, CB2, AND NK2 RECEPTORS
    11.
    发明申请
    USE OF CIS-EPOXYEICOSATRIENOIC ACIDS AND INHIBITORS OF SOLUBLE EPOXIDE HYDROLASE TO TREAT CONDITIONS MEDIATED BY PBR, CB2, AND NK2 RECEPTORS 有权
    独联体环氧化合物酸和可溶性环氧化物水解酶的抑制剂用于治疗由PBR,CB2和NK2受体介导的病症

    公开(公告)号:US20100074852A1

    公开(公告)日:2010-03-25

    申请号:US12518549

    申请日:2007-01-04

    摘要: The invention relates to the discovery that cis-epoxyeicosatraenoic acids (EETs) bind to and act as agonists of peripheral benzodiazepine receptor and the cannabinoid CB2 receptor. The invention provides methods of reducing symptoms of conditions whose activity is mediated by these receptors, including inhibiting anxiety, inhibiting the growth of cancer cells expressing peripheral benzodiazepine receptors, and reducing oxygen radical damage to cells, by contacting the cells with a cis-epoxyeicosantrienoic acid, an inhibitor of soluble epoxide hydrolase (sEH), or both. The invention further provides methods of inhibiting irritable bowel syndrome by administering to individuals with inhibiting irritable bowel syndrome a cis-epoxyeicosantrienoic acid, an inhibitor of soluble epoxide hydrolase (sEH), or both. In some embodiments, the method comprises administering to the individual a nucleic acid which inhibits expression of sEH.

    摘要翻译: 本发明涉及顺式 - 环氧二十碳四烯酸(EETs)结合并作为外周苯并二氮杂受体和大麻素CB2受体的激动剂的发现。 本发明提供了减少活性由这些受体介导的病症症状的方法,包括抑制焦虑,抑制表达外周苯并二氮杂受体的癌细胞的生长,以及通过使细胞与顺式 - 环氧二十碳三烯酸 ,可溶性环氧化物水解酶(sEH)的抑制剂或两者。 本发明还提供了通过向具有抑制肠易激综合征的个体施用顺式环氧二十碳三烯酸,可溶性环氧化物水解酶(sEH)抑制剂或两者)来抑制肠易激综合征的方法。 在一些实施方案中,该方法包括向个体施用抑制sEH表达的核酸。

    Insect control method with genetically engineered biopesticides
    13.
    发明授权
    Insect control method with genetically engineered biopesticides 失效
    基因工程生物农药的昆虫控制方法

    公开(公告)号:US06344193B1

    公开(公告)日:2002-02-05

    申请号:US09206766

    申请日:1998-01-15

    IPC分类号: A01N6300

    摘要: Insect pests can be controlled by treating the pests or their loci with a combination of recombinant virus and organic insecticide. The recombinant virus preferably is a baculovirus. Combinations of recombinant baculovirus with chemical insecticides provide a dose-response in pests, such as insects, that is greater than additive. Preferred treatments of the invention are uses of recombinant baculoviruses that express a foreign protein or toxin, with pyrethroid insecticides. Treatments against pyrethroid resistant pests are especially useful.

    摘要翻译: 可以通过用重组病毒和有机杀虫剂的组合处理害虫或其基因座来控制昆虫害虫。 重组病毒优选为杆状病毒。 重组杆状病毒与化学杀虫剂的组合在害虫(如昆虫)中提供大于添加剂的剂量反应。 本发明的优选处理是用拟除虫菊酯杀虫剂表达外源蛋白或毒素的重组杆状病毒的用途。 对拟除虫菊酯抗性害虫的治疗特别有用。

    Pyrazole inhibitors of COX-2 and sEH
    17.
    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

    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。