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    Use of phenylmethimazoles, methimazole derivatives, and tautomeric cyclic thiones for the treatment of autoimmune/inflammatory diseases associated with toll-like receptor overexpression
    1.
    发明申请
    Use of phenylmethimazoles, methimazole derivatives, and tautomeric cyclic thiones for the treatment of autoimmune/inflammatory diseases associated with toll-like receptor overexpression 审中-公开
    苯甲嘧啶，甲巯咪唑衍生物和互变异构环状硫堇用于治疗与同样受体过表达相关的自身免疫/炎性疾病

    公开(公告)号：US20060211752A1

    公开(公告)日：2006-09-21

    申请号：US11130922

    申请日：2005-05-17

    申请人： Leonard Kohn ,  Norikazu Harii ,  Uruguaysito Benavides-Peralta ,  Mariana Gonzalez-Murguiondo ,  Christopher Lewis ,  Giorgio Napolitano ,  Cesidio Giuliani ,  Ramiro Malgor ,  Douglas Goetz

    发明人： Leonard Kohn ,  Norikazu Harii ,  Uruguaysito Benavides-Peralta ,  Mariana Gonzalez-Murguiondo ,  Christopher Lewis ,  Giorgio Napolitano ,  Cesidio Giuliani ,  Ramiro Malgor ,  Douglas Goetz

    IPC分类号： A61K31/4166

    CPC分类号： A61K31/4164 ,  A61K31/4166 ,  A61K31/56 ,  A61K45/06 ,  Y02A50/411

    摘要： The present invention relates to the treatment of autoimmune and/or inflammatory diseases associated with overexpression of Toll-like receptor 3 (TLR3) as well as Toll-like receptor 4 (TLR4) and/or TLR3/TLR4 signaling in nonimmune cells, monocytes, macrophages, and/or dendritic cells in association with related pathologies. This invention also relates to the use of phenylmethimazoles, methimazole derivatives, and tautomeric cyclic thiones for the treatment of autoimmune and inflammatory diseases associated with Toll-like receptor 3 (TLR3) as well as Toll-like receptor 4 (TLR4) and/or TLR3/TLR4 signaling in nonimmune cells, monocytes, macrophages, and/or dendritic cells in association with related pathologies. This invention also relates to treating a subject having a disease or condition associated with abnormal Toll-like receptor 3 as well as Toll-like receptor 4 and/or TLR3/TLR4 signaling in nonimmune cells, monocytes, macrophages, and/or dendritic cells in association with related pathologies. The present invention also relates to the treatment of autoimmune-inflammatory pathologies and chemokine and cytokine-mediated diseases associated with TLR overexpression and signaling. This invention also relates to pharmaceutical formulations capable of inhibiting the IRF-3/Type 1 IFN/STAT/ISRE/IRF-1 pathway associated with Toll-like receptor overexpression or signaling.

    摘要翻译： 本发明涉及治疗与非免疫细胞，单核细胞中Toll样受体3（TLR3）和Toll样受体4（TLR4）和/或TLR3 / TLR4信号传导过度相关的自身免疫性和/或炎性疾病， 巨噬细胞和/或与相关病理学相关的树突状细胞。 本发明还涉及苯甲基咪唑，甲巯咪唑衍生物和互变异构环状硫堇用于治疗与Toll样受体3（TLR3）以及Toll样受体4（TLR4）和/或TLR3相关的自身免疫性和炎性疾病的用途 / TLR4信号传导在非免疫细胞，单核细胞，巨噬细胞和/或树突状细胞中，与相关病理学相关。 本发明还涉及在非免疫细胞，单核细胞，巨噬细胞和/或树突细胞中治疗具有与异常Toll样受体3以及Toll样受体4和/或TLR3 / TLR4信号传导相关的疾病或病症的受试者 与相关病理学关联。 本发明还涉及治疗与TLR过表达和信号传导相关的自身免疫性炎症病理和趋化因子和细胞因子介导的疾病。 本发明还涉及能够抑制与Toll样受体过表达或信号传导相关的IRF-3/1型IFN / STAT / ISRE / IRF-1途径的药物制剂。

    Compositions and methods for treatment of colitis
    3.
    发明申请
    Compositions and methods for treatment of colitis 有权
    用于治疗结肠炎的组合物和方法

    公开(公告)号：US20060058365A1

    公开(公告)日：2006-03-16

    申请号：US10912948

    申请日：2004-08-06

    申请人： Leonard Kohn ,  Douglas Goetz ,  Uruguaysito Benavides-Peralta ,  Mariana Gonzalez-Murguiondo ,  Norikazu Harii ,  Christopher Lewis ,  Giorgio Napolitano ,  Nilesh Dagia

    发明人： Leonard Kohn ,  Douglas Goetz ,  Uruguaysito Benavides-Peralta ,  Mariana Gonzalez-Murguiondo ,  Norikazu Harii ,  Christopher Lewis ,  Giorgio Napolitano ,  Nilesh Dagia

    IPC分类号： A61K31/4166

    CPC分类号： A61K31/4164 ,  Y02A50/402 ,  Y02A50/411

    摘要： The present invention relates to the treatment of inflammatory bowel disease (IBD) and related gastrointestinal pathologies. This invention also relates to the treatment of cytokine-mediated diseases, including tumor necrosis factor-α (TNFα)-induced diseases and/or chemokine-mediated diseases. This invention also relates to treating an animal having a disease or condition associated with Toll-like receptor 4. Specifically, the present invention relates to the treatment of inflammatory bowel disease (IBD) and related gastrointestinal pathologies that are cytokine-mediated or associated with Toll-like receptor 4. More specifically, this invention is directed to methods for treating or preventing IBD and related gastrointestinal pathologies using methimazole derivatives and tautomeric cyclic thiones. This invention is also directed to pharmaceutical compositions containing methimazole derivatives and tautomeric cyclic thiones, which are useful for the treatment or prophylaxis of IBD and related gastrointestinal pathologies. This invention also relates to pharmaceutical formulations capable of inhibiting tumor necrosis factor-α (TNFα)-induced vascular cell adhesion molecule-1 (VCAM-1) expression and the resulting leukocyte-endothelial cell adhesion for the inhibition and prevention of inflammatory bowel syndrome and related gastrointestinal pathologies.

    摘要翻译： 本发明涉及炎症性肠病（IBD）和相关胃肠道病理学的治疗。 本发明还涉及细胞因子介导的疾病的治疗，包括肿瘤坏死因子-α（TNFα）诱导的疾病和/或趋化因子介导的疾病。 本发明还涉及治疗具有与Toll样受体4相关的疾病或病症的动物。具体而言，本发明涉及炎症性肠病（IBD）的治疗以及细胞因子介导或与Toll相关的相关胃肠病理 类似受体4.更具体地，本发明涉及使用甲巯咪唑衍生物和互变异构环状硫堇治疗或预防IBD和相关胃肠道病理学的方法。 本发明还涉及含有甲巯咪唑衍生物和互变异构环状硫堇的药物组合物，其可用于治疗或预防IBD和相关的胃肠道病理。 本发明还涉及能够抑制肿瘤坏死因子-α（TNFα）诱导的血管细胞粘附分子-1（VCAM-1）表达的药物制剂以及由此产生的白细胞内皮细胞粘附以抑制和预防炎症性肠综合征和 相关的胃肠道病变。