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公开(公告)号：US10143720B2
公开(公告)日：2018-12-04
申请号：US15483711
申请日：2017-04-10
IPC分类号： A01N37/18 , A61K38/00 , A61P1/16 , A61K38/12 , A61K31/16 , A61K31/165 , A61K31/166 , A61K45/06 , C07K5/12
摘要： The present invention provides small molecule inhibitors of hepatitis B virus (HBV) covalently closed circular (ccc) DNA, which are useful as therapeutics in the management of chronic HBV. The compounds of the invention achieve epigenetic modification of the cccDNA, histone modification and histone deacetylase activity inhibition, thus modulating HBV cccDNA. The present invention further provides methods for modulating HBV cccDNA, for treating or preventing HBV in a subject, and for modulating cccDNA transcription of hepatitis B in a subject.
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公开(公告)号：US09623071B2
公开(公告)日：2017-04-18
申请号：US14435675
申请日：2013-05-31
IPC分类号： A01N37/18 , A61K38/00 , A61P1/16 , A61K38/12 , A61K45/06 , C07K5/12 , A61K31/165 , A61K31/16 , A61K31/166
CPC分类号： A61K38/12 , A61K31/16 , A61K31/165 , A61K31/166 , A61K45/06 , C07K5/123 , C07K5/126
摘要： The present invention provides small molecule inhibitors of hepatitis B virus (HBV) covalently closed circular (ccc) DNA, which are useful as therapeutics in the management of chronic HBV. The compounds of the invention achieve epigenetic modification of the cccDNA, histone modification and histone deacetylase activity inhibition, thus modulating HBV cccDNA. The present invention further provides methods for modulating HBV cccDNA, for treating or preventing HBV in a subject, and for modulating cccDNA transcription of hepatitis B in a subject.
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公开(公告)号：US20150011537A1
公开(公告)日：2015-01-08
申请号：US14380546
申请日：2013-02-22
申请人： Baruch S. Blumberg Institute , Philadelphia Health & Education Corporation d/b/a Drexel University College of Medicine
发明人： Andrea Cuconati , Jinhong Chang , Timothy M. Block , Ju-Tao Guo
IPC分类号： C12Q1/02 , A61K31/5513
CPC分类号： A61K31/5513 , C07D243/24 , C12Q1/6897 , C12Q1/70 , G01N2500/04 , G01N2500/10 , Y02A50/385 , Y02A50/387
摘要： The present invention describes a unique antiviral screen system. The assay is based on quantitatively monitoring viral activation of host cell beta-interferon (IFN-β) gene expression in a HEK293-derived reporter cell line expressing a firefly luciferase gene under the control of a human IFN-β promoter. Unlike the traditional high throughput antiviral assays that measure either the reduction of viral components/yields or cytopathic effect, the readout of the reporter assay in the present invention is the virus-induced host cellular innate immune response. Hence, the assay allows for identification of compounds that inhibit virus infection. In addition, because induction of IFN is one of the most common attributes of viruses, the assay is applicable to all the viruses that are able to infect the reporter cell line and induce IFN-β expression. Compounds that interfere with viral mediated activation of the interferon pathway in a primary screen, can be further screened with virus-specific assay to confirm their antiviral activity.
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公开(公告)号：US10376502B2
公开(公告)日：2019-08-13
申请号：US14813931
申请日：2015-07-30
发明人： Yanming Du , Xiaodong Xu , Hong Ye , Jinhong Chang , Timothy M. Block
IPC分类号： A61K31/45 , A61K31/4015 , C07F9/59 , C07D207/12 , C07D211/44 , C07D211/46 , C07D413/06
摘要： Pharmaceutical compositions of the invention comprise alkylated imino sugars derivatives having a disease-modifying action in the treatment of diseases associated with glucosidase activity that include Viral hemorrhagic fevers, and any other diseases involving glucosidase activity.
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5.发明申请Novel Alkylated Imino Sugars Exhibiting Glucosidase Inhibition and Their Method of Use 审中-公开新型烷基化亚氨基糖显示葡萄糖苷酶抑制及其使用方法公开(公告)号：US20150335630A1
公开(公告)日：2015-11-26
申请号：US14813931
申请日：2015-07-30
发明人： Yanming Du , Xiaodong Xu , Hong Ye , Jinhong Chang , Timothy M. Block
IPC分类号： A61K31/45 , A61K31/4015
CPC分类号： A61K31/45 , A61K31/4015 , C07D207/12 , C07D211/44 , C07D211/46 , C07D413/06 , C07F9/59
摘要： Pharmaceutical compositions of the invention comprise alkylated imino sugars derivatives having a disease-modifying action in the treatment of diseases associated with glucosidase activity that include Viral hemorrhagic fevers, and any other diseases involving glucosidase activity.
摘要翻译： 本发明的药物组合物包含在治疗与葡萄糖苷酶活性相关的疾病（包括病毒性出血热）和涉及葡糖苷酶活性的任何其它疾病中具有疾病修饰作用的烷基化亚氨基糖衍生物。
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公开(公告)号：US20170305856A1
公开(公告)日：2017-10-26
申请号：US15492652
申请日：2017-04-20
发明人： Yanming Du , Jinhong Chang , Timothy Michael Block
IPC分类号： C07D211/40 , C07C9/15 , A61K31/13 , A61K31/45 , C07D419/12 , C07D211/36
摘要： Described herein are alkylated imino sugars derivatives having a disease-modifying action in the treatment of diseases associated with glucosidase activity that include viral hemorrhagic fevers and other enveloped viruses, and any other diseases involving glucosidase activity.
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公开(公告)号：US10421723B2
公开(公告)日：2019-09-24
申请号：US15492652
申请日：2017-04-20
发明人： Yanming Du , Jinhong Chang , Timothy Michael Block
IPC分类号： C07D211/40 , C07D211/36 , C07D419/12 , A61K31/45 , A61K31/13
摘要： Described herein are alkylated imino sugars derivatives having a disease-modifying action in the treatment of diseases associated with glucosidase activity that include viral hemorrhagic fevers and other enveloped viruses, and any other diseases involving glucosidase activity.
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8.发明授权Alkylated imino sugars exhibiting glucosidase inhibition and their method of use 有权显示葡糖苷酶抑制的烷基化亚氨基糖及其使用方法公开(公告)号：US09126937B2
公开(公告)日：2015-09-08
申请号：US14388175
申请日：2013-03-27
发明人： Yanming Du , Xiaodong Xu , Hong Ye , Jinhong Chang , Timothy M. Block
IPC分类号： C07D211/40 , A61K31/445 , C07D211/46 , C07D413/06 , C07F9/59
CPC分类号： A61K31/45 , A61K31/4015 , C07D207/12 , C07D211/44 , C07D211/46 , C07D413/06 , C07F9/59
摘要： Pharmaceutical compositions of the invention comprise alkylated imino sugars derivatives having a disease-modifying action in the treatment of diseases associated with glucosidase activity that include Viral hemorrhagic fevers, and any other diseases involving glucosidase activity.
摘要翻译： 本发明的药物组合物包含在治疗与葡萄糖苷酶活性相关的疾病（包括病毒性出血热）和涉及葡糖苷酶活性的任何其它疾病中具有疾病修饰作用的烷基化亚氨基糖衍生物。
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公开(公告)号：US09168260B2
公开(公告)日：2015-10-27
申请号：US14380546
申请日：2013-02-22
发明人： Andrea Cuconati , Jinhong Chang , Timothy M. Block , Ju-Tao Guo
IPC分类号： A61K31/5513 , C07D243/24 , C12Q1/70 , C12Q1/68
CPC分类号： A61K31/5513 , C07D243/24 , C12Q1/6897 , C12Q1/70 , G01N2500/04 , G01N2500/10 , Y02A50/385 , Y02A50/387
摘要： The present invention describes a unique antiviral screen system. The assay is based on quantitatively monitoring viral activation of host cell beta-interferon (IFN-β) gene expression in a HEK293-derived reporter cell line expressing a firefly luciferase gene under the control of a human IFN-β promoter. Unlike the traditional high throughput antiviral assays that measure either the reduction of viral components/yields or cytopathic effect, the readout of the reporter assay in the present invention is the virus-induced host cellular innate immune response. Hence, the assay allows for identification of compounds that inhibit virus infection. In addition, because induction of IFN is one of the most common attributes of viruses, the assay is applicable to all the viruses that are able to infect the reporter cell line and induce IFN-β expression. Compounds that interfere with viral mediated activation of the interferon pathway in a primary screen, can be further screened with virus-specific assay to confirm their antiviral activity.
摘要翻译： 本发明描述了一种独特的抗病毒屏幕系统。 该测定基于定量监测来自表达在人IFN-α的控制下的萤火虫荧光素酶基因的HEK293衍生的报道细胞系中宿主细胞β-干扰素（IFN-α）基因表达的病毒活化; 启动子。 不同于测量病毒成分/产量或细胞病变效应的降低的传统高通量抗病毒测定法，本发明中报道分析的读出是病毒诱导的宿主细胞先天免疫应答。 因此，该测定允许鉴定抑制病毒感染的化合物。 此外，由于IFN的诱导是病毒最常见的属性之一，所以该测定适用于能够感染报道细胞系并诱导IFN-α的所有病毒。 表达。 可以用病毒特异性测定进一步筛选干扰原代筛选中的干扰素途径的病毒介导的活化的化合物，以证实其抗病毒活性。
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公开(公告)号：US10045961B2
公开(公告)日：2018-08-14
申请号：US15483645
申请日：2017-04-10
申请人： DREXEL UNIVERSITY
发明人： Jinhong Chang , Fang Guo , Timothy M. Block , Ju-Tao Guo
IPC分类号： A61K31/35 , A61K31/352 , A61K31/473 , G01N33/50 , C12Q1/70
摘要： Provided herein are methods of treating a subject having hepatitis B viral (HBV) infection. More specifically, disclosed herein are methods of stimulating the innate cytokine response in macrophages, dendritic cells and/or liver non-parenchymal cells with small molecular agonists of STING to suppress HBV replication in hepatocytes. The methods are especially suitable for use in the treatment of chronic HBV infections. Also disclosed herein are methods of identifying compounds useful in the treatment of HBV infection.
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