Method for treating or preventing inflammatory disorders
    97.
    发明申请
    Method for treating or preventing inflammatory disorders 审中-公开
    治疗或预防炎性疾病的方法

    公开(公告)号:US20050080140A1

    公开(公告)日:2005-04-14

    申请号:US10923348

    申请日:2004-08-20

    摘要: According to the present invention, the gene for IL-13, an anti-inflammatory cytokine, was shown to be a target of prostacyclin (PGI2)-activated Peroxisome proliferator-activated receptor (PPAR) δ. Furthermore, the PGI2-PPARδ signaling pathway was revealed to regulate the expression of IL-13 gene in human vascular endothelial cells, and controls inflammatory responses induced by proinflammatory cytokines through the production of IL-13 in an autocrine or paracrine manner. Thus, the present invention provides a method for treating or preventing inflammatory disorders, which comprises administering a therapeutically effective amount of PPARδ agonist into a subject. Furthermore, the present invention provides a method for treating or preventing inflammatory disorders, which comprises administering a prostacyclin synthase gene or a protein encoded by the gene into a subject.

    摘要翻译: 根据本发明,IL-13的基因(抗炎细胞因子)显示为前列环素(PGI 2)活化的过氧化物酶体增生物激活受体(PPAR)三角洲的靶标。 此外,显示PGI2-PPARdelta信号通路调节人血管内皮细胞中IL-13基因的表达,并通过以自分泌或旁分泌的方式通过产生IL-13来控制由促炎细胞因子诱导的炎症反应。 因此,本发明提供了治疗或预防炎症性疾病的方法,其包括向受试者施用治疗有效量的PPARδ激动剂。 此外,本发明提供了治疗或预防炎症性疾病的方法,其包括将前列环素合酶基因或由该基因编码的蛋白质施用于受试者。

    Cyclopentane heptan(ene)oic acid, 2-heteroarylalkenyl derivatives as
therapeutic agents
    98.
    发明授权
    Cyclopentane heptan(ene)oic acid, 2-heteroarylalkenyl derivatives as therapeutic agents 有权
    环戊烷庚(烯)酸,2-杂芳基烯基衍生物作为治疗剂

    公开(公告)号:US6160129A

    公开(公告)日:2000-12-12

    申请号:US243344

    申请日:1999-02-01

    申请人: Robert M. Burk

    发明人: Robert M. Burk

    摘要: The invention relates to the use of derivatives of F-type prostaglandins as ocular hypotensives. The compounds used in accordance with the invention are represented by the following formula I: ##STR1## wherein wavy line attachments indicate either the alpha (.alpha.) or beta (.beta.) configuration; hatched segments indicate .alpha. configuration; the solid triangle is used to indicate .beta. configuration; dashed bonds represent a double bond, or a single bond; R is a substituted heteroaryl radical having at least two pendant substituents selected from the group consisting of C.sub.1 to C.sub.6 alkyl; halogen; trifluoromethyl; COR.sup.1 ; COCF.sub.3 ; SO.sub.2 NR.sup.1 ; NO.sub.2 and CN or at least one cyano group; R.sup.1 is hydrogen or a lower alkyl radical having up to six carbon atoms, X is selected from the group consisting of --OR.sup.1 and --N(R.sup.1).sub.2 ; Y is .dbd.O or represents 2 hydrogen radicals and the 9, 11 or 15 lower alkyl esters thereof; provided, however, when said heteroaryl radical is a dichlorothienyl radical, the compound is not a 1-carboxylic acid or amide thereof. Certain of the compounds represented by Formula I are novel and comprise another aspect of the present invention.

    摘要翻译: 本发明涉及使用F型前列腺素衍生物作为眼部低血压。 根据本发明使用的化合物由下式I表示:其中波浪线附着物指示α(α)或β(β)构型; 阴影线段表示alpha配置; 实心三角形用于指示beta配置; 虚线键代表双键或单键; R是具有至少两个选自C 1至C 6烷基的侧基取代基的取代的杂芳基; 卤素; 三氟甲基 COR1; COCF3; SO2NR1; NO 2和CN或至少一个氰基; R 1是氢或具有至多6个碳原子的低级烷基,X选自-OR 1和-N(R 1)2; Y为= O或代表2个氢原子及其9,11或15个低级烷基酯; 但是,当所述杂芳基为二氯噻吩基时,该化合物不是1-羧酸或其酰胺。 某些由式I表示的化合物是新的并且包括本发明的另一方面。