利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

35 条记录 (耗时 0.024 秒)

    Novel Imino Sugar Derivatives Demonstrate Potent Antiviral Activity and Reducted Toxicity
    5.
    发明申请
    Novel Imino Sugar Derivatives Demonstrate Potent Antiviral Activity and Reducted Toxicity 有权
    新型伊米诺糖衍生物证明有效的抗病毒活性和减少的毒性

    公开(公告)号：US20110189771A1

    公开(公告)日：2011-08-04

    申请号：US13061734

    申请日：2009-09-02

    申请人： Timothy M. Block ,  Jinhong Chang ,  Xiaodong Xu

    发明人： Timothy M. Block ,  Jinhong Chang ,  Xiaodong Xu

    IPC分类号： C12N5/02 ,  C07D211/40

    CPC分类号： A61K31/47 ,  A61K31/7056 ,  C07D211/46 ,  Y02A50/393 ,  A61K2300/00

    摘要： Imino sugars, such as deoxynojirimycin (DNJ), are glucose analogues that selectively inhibit cellular α-glucosidase I and II (enzymes that process N-linked glycans in glycoprotein) and exhibit broad spectrum antiviral activities against many enveloped viruses. Previously we have reported a novel DNJ derivative, OSL-95II, with antiviral activity and reduced cytotoxicity. In order to develop imino sugars with more potent antiviral activity as well as improved toxicity profile, OSL-95II was modified by diversifying the nitrogen linked alkylated side chain. The antiviral activities were initially tested in bovine viral diarrhea virus (BVDV) infected MDBK cells, yielding several imino sugar derivatives with novel structure and superior antiviral activity and toxicity profile. Furthermore, these new compounds were shown to be active against Dengue virus (DV) and West Nile virus (WNV) infection in BHK cells where potent anti-DV activity having submicromolar EC50 values and SI of greater than 900. These compounds represent a new generation of iminio sugars and their analogues, having application in the clinical treatment of infection of DV and other members of flaviviridae.

    摘要翻译： 诸如脱氧野尻霉素（DNJ）的亚氨基糖是选择性抑制细胞α-葡萄糖苷酶I和II（在糖蛋白中处理N-连接聚糖的酶）并且对许多包膜病毒展现广谱抗病毒活性的葡萄糖类似物。 以前我们已经报道了具有抗病毒活性和降低的细胞毒性的新型DNJ衍生物OSL-95II。 为了开发具有更强的抗病毒活性和改善的毒性特征的亚氨基糖，OSL-95II通过使氮连接的烷基化侧链多样化而被修饰。 首先在牛病毒性腹泻病毒（BVDV）感染的MDBK细胞中测试抗病毒活性，产生几种具有新结构和优良抗病毒活性和毒性特征的亚氨基糖衍生物。 此外，这些新化合物被证明对BHK细胞中登革热病毒（DV）和西尼罗病毒（WNV）感染具有活性，其中具有亚微摩尔EC 50值和SI大于900的有效抗DV活性。这些化合物代表新一代 的亚氨基糖及其类似物，可用于临床治疗DV和其他黄病毒成分的感染。

    Imino sugar derivatives demonstrate potent antiviral activity and reduced toxicity
    6.
    发明授权
    Imino sugar derivatives demonstrate potent antiviral activity and reduced toxicity 有权
    亚氨基糖衍生物表现出强大的抗病毒活性和降低的毒性

    公开(公告)号：US09040488B2

    公开(公告)日：2015-05-26

    申请号：US13061734

    申请日：2009-09-02

    申请人： Timothy M. Block ,  Jinhong Chang ,  Xiaodong Xu

    发明人： Timothy M. Block ,  Jinhong Chang ,  Xiaodong Xu

    IPC分类号： C07D211/46 ,  A61K31/445 ,  A61K31/47 ,  A61K31/7056

    CPC分类号： A61K31/47 ,  A61K31/7056 ,  C07D211/46 ,  Y02A50/393 ,  A61K2300/00

    摘要： Imino sugars, such as deoxynojirimycin (DNJ), are glucose analogues that selectively inhibit cellular α-glucosidase I and II (enzymes that process N-linked glycans in glycoprotein) and exhibit broad spectrum antiviral activities against many enveloped viruses. Previously we have reported a novel DNJ derivative, OSL-95II, with antiviral activity and reduced cytotoxicity. In order to develop imino sugars with more potent antiviral activity as well as improved toxicity profile, OSL-95II was modified by diversifying the nitrogen linked alkylated side chain. The antiviral activities were initially tested in bovine viral diarrhea virus (BVDV) infected MDBK cells, yielding several imino sugar derivatives with novel structure and superior antiviral activity and toxicity profile. Furthermore, these new compounds were shown to be active against Dengue virus (DV) and West Nile virus (WNV) infection in BHK cells where potent anti-DV activity having submicromolar EC50 values and SI of greater than 900. These compounds represent a new generation of iminio sugars and their analogues, having application in the clinical treatment of infection of DV and other members of flaviviridae.

    摘要翻译： 诸如脱氧野尻霉素（DNJ）的亚氨基糖是选择性抑制细胞α-葡萄糖苷酶I和II（在糖蛋白中加工N-连接聚糖的酶）并且对许多包膜病毒展现广谱抗病毒活性的葡萄糖类似物。 以前我们已经报道了具有抗病毒活性和降低的细胞毒性的新型DNJ衍生物OSL-95II。 为了开发具有更强的抗病毒活性和改善的毒性特征的亚氨基糖，OSL-95II通过使氮连接的烷基化侧链多样化而被修饰。 首先在牛病毒性腹泻病毒（BVDV）感染的MDBK细胞中测试抗病毒活性，产生几种具有新结构和优良抗病毒活性和毒性特征的亚氨基糖衍生物。 此外，这些新化合物被证明对BHK细胞中登革热病毒（DV）和西尼罗病毒（WNV）感染具有活性，其中具有亚微摩尔EC 50值和SI大于900的有效抗DV活性。这些化合物代表新一代 的亚氨基糖及其类似物，可用于临床治疗DV和其他黄病毒成分的感染。