Ligands of nuclear receptor
    3.
    发明授权
    Ligands of nuclear receptor 失效
    核受体配体

    公开(公告)号:US06605639B1

    公开(公告)日:2003-08-12

    申请号:US09868059

    申请日:2001-06-14

    IPC分类号: A01N3710

    摘要: It has been newly found out that ascochlorin, which is a publicly known fat-soluble antibiotic, and its homologues serve as a ligand of retinoid X receptor and react in vivo with the amino group of serum protein to form Schiff bases without showing any side effect of retinoid. Ascochlorin and its homologues are usable in treating and/or preventing a disease or condition which can be relieved by the retinoid X receptor ligand-dependent gene transcriptional regulation (for example, diseases caused by the expression of insulin resistance, hypertension, cerebrovascular diseases, rheumatoid arthritis, autoimmune disease, Ca metabolic disorder, complication of diabetes, arteriosclerosis, etc.). Moreover, they can inhibit denaturation and/or necrosis of pancreatic Langerhans islet &bgr;-cells and, therefore, are usable in making these cells to sustain the insulin productivity.

    摘要翻译: 最近发现,作为公知的脂溶性抗生素的ascochlorin,其同系物作为类视黄醇X受体的配体,并与血清蛋白质的氨基反应形成希夫碱,而没有显示任何副作用 的类视黄醇。 异烟肼及其同系物可用于治疗和/或预防可被视黄酸X受体配体依赖性基因转录调节(例如,由胰岛素抵抗,高血压,脑血管疾病,类风湿病的表达引起的疾病)缓解的疾病或病症 关节炎,自身免疫性疾病,Ca代谢紊乱,糖尿病并发症,动脉硬化等)。 此外,它们可以抑制胰腺胰岛β细胞的变性和/或坏死,因此可用于使这些细胞维持胰岛素的生产力。

    New tunicamine derivatives and their preparation
    7.
    发明授权
    New tunicamine derivatives and their preparation 失效
    新型明胺衍生物及其制备方法

    公开(公告)号:US4202968A

    公开(公告)日:1980-05-13

    申请号:US920448

    申请日:1978-06-29

    摘要: New tunicamine derivatives are provided which exhibit antiviral activity against some virus, particularly Newcastle disease virus, and inhibitory activity against coccidiosis and which are also of particular value as intermediates for the preparation of a variety of useful antibacterial, antitumor and antiviral compounds. They have a structure of the formula: ##STR1## wherein R represents hydrogen or a fatty acid residue of the formula (CH.sub.3).sub.2 CH(CH.sub.2).sub.n CH.dbd.CHCO-- where n represents an integer of 8 to 11 inclusive. They are prepared either by fermentation methods or by acid hydrolysis of the known antibiotic tunicamycin.

    摘要翻译: 提供了对一些病毒,特别是新城疫病毒具有抗病毒活性和抗球虫病的抑制活性的新的明胺衍生物,并且它们作为制备各种有用的抗菌,抗肿瘤和抗病毒化合物的中间体也是特别有价值的。 它们具有下式的结构:其中R表示氢或式(CH3)2CH(CH2)nCH = CHCO-的脂肪酸残基,其中n表示8〜11的整数。 它们通过发酵方法或通过已知的抗生素衣霉素的酸水解来制备。