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1.发明授权β-L-2′-deoxynucleosides for the treatment of resistant HBV strains and combination therapies 有权＆bgr; -L-2'-脱氧核苷用于治疗耐药性HBV病毒株和联合疗法公开(公告)号：US07928086B2
公开(公告)日：2011-04-19
申请号：US11651353
申请日：2007-01-09
IPC分类号： A01N43/04 , A61K31/70 , A61K31/715
CPC分类号： A61K45/06 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K38/21
摘要： It has been discovered that β-L-2′-deoxynucleosides are active against drug-resistant hepatitis B virus with mutations. A method for treating lamivudine resistant HBV (M552V) in a host is provided that includes administering a β-L-2′-deoxynucleoside or its pharmaceutically acceptable salt, ester or prodrug. In addition, a method for preventing lamivudine resistant HBV (M552V) mutation from occurring in a naïve host is provided that includes administering a β-L-2′-deoxynucleoside or its pharmaceutically acceptable salt, ester or prodrug. A method for preventing and/or suppressing the emergence of the HBV double mutant (L528M/M552V) in a host is also provided that includes administering a β-L-2′-deoxynucleoside or its pharmaceutically acceptable salt, ester or prodrug.
摘要翻译： 已经发现，-L-2'-脱氧核苷对具有突变的耐药性乙型肝炎病毒具有活性。 提供了一种治疗宿主中拉米夫定耐药HBV（M552V）的方法，其包括施用一种β-2'-2'-脱氧核苷或其药学上可接受的盐，酯或前药。 另外，提供了一种用于预防在初始宿主中发生拉米夫定耐药性HBV（M552V）突变的方法，其包括施用一种β-2'-脱氧核苷或其药学上可接受的盐，酯或前药。 还提供了用于预防和/或抑制宿主中HBV双突变体（L528M / M552V）的出现的方法，其包括施用＆bgr。-L-2'-脱氧核苷或其药学上可接受的盐，酯或前药。
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2.发明授权β-L-2′-deoxynucleosides for the treatment of resistant HBV strains and combination therapies 有权β-L-2'-脱氧核苷用于治疗耐药性HBV病毒株和组合疗法公开(公告)号：US07186700B2
公开(公告)日：2007-03-06
申请号：US10662641
申请日：2003-09-15
IPC分类号： A01N43/04 , A61K31/70 , A61K31/715
CPC分类号： A61K45/06 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K38/21
摘要： It has been discovered that β-L-2′-deoxynucleosides are active against drug-resistant hepatitis B virus with mutations. A method for treating lamivudine resistant HBV (M552V) in a host is provided that includes administering a β-L-2′-deoxynucleoside or its pharmaceutically acceptable salt, ester or prodrug. In addition, a method for preventing lamivudine resistant HBV (M552V) mutation from occurring in a naïve host is provided that includes administering a β-L-2′-deoxynucleoside or its pharmaceutically acceptable salt, ester or prodrug. A method for preventing and/or suppressing the emergence of the HBV double mutant (L528M/M552V) in a host is also provided that includes administering a β-L-2′-deoxynucleoside or its pharmaceutically acceptable salt, ester or prodrug.
摘要翻译： 已经发现β-L-2'-脱氧核苷对具有突变的耐药性乙型肝炎病毒具有活性。 提供了一种治疗宿主中拉米夫定耐药性HBV（M552V）的方法，其包括施用β-L-2'-脱氧核苷或其药学上可接受的盐，酯或前药。 此外，提供了一种用于预防在初始宿主中发生拉米夫定耐药性HBV（M552V）突变的方法，其包括施用β-L-2'-脱氧核苷或其药学上可接受的盐，酯或前药。 还提供了预防和/或抑制宿主中HBV双突变体（L528M / M552V）的出现的方法，其包括施用β-L-2'-脱氧核苷或其药学上可接受的盐，酯或前药。
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3.发明授权β-L-2′-deoxynucleosides for the treatment of resistant HBV strains and combination therapies 有权＆bgr; -L-2'-脱氧核苷用于治疗耐药性HBV病毒株和联合疗法公开(公告)号：US08158606B2
公开(公告)日：2012-04-17
申请号：US13052750
申请日：2011-03-21
IPC分类号： A01N43/04 , A61K31/70 , A61K31/715
CPC分类号： A61K45/06 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K38/21
摘要： It has been discovered that β-L-2′-deoxynucleosides are active against drug-resistant hepatitis B virus with mutations. A method for treating lamivudine resistant HBV (M552V) in a host is provided that includes administering a β-L-2′-deoxynucleoside or its pharmaceutically acceptable salt, ester or prodrug. In addition, a method for preventing lamivudine resistant HBV (M552V) mutation from occurring in a naïve host is provided that includes administering a β-L-2′-deoxynucleoside or its pharmaceutically acceptable salt, ester or prodrug. A method for preventing and/or suppressing the emergence of the HBV double mutant (L528M/M552V) in a host is also provided that includes administering a β-L-2′-deoxynucleoside or its pharmaceutically acceptable salt, ester or prodrug.
摘要翻译： 已经发现，-L-2'-脱氧核苷对具有突变的耐药性乙型肝炎病毒是有活性的。 提供了一种治疗宿主中拉米夫定耐药HBV（M552V）的方法，其包括施用一种β-2'-2'-脱氧核苷或其药学上可接受的盐，酯或前药。 另外，提供了一种用于预防在初始宿主中发生拉米夫定耐药性HBV（M552V）突变的方法，其包括施用一种β-2'-脱氧核苷或其药学上可接受的盐，酯或前药。 还提供了用于预防和/或抑制宿主中HBV双突变体（L528M / M552V）的出现的方法，其包括施用＆bgr。-L-2'-脱氧核苷或其药学上可接受的盐，酯或前药。
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4.发明申请Beta-L-2'-deoxynucleosides for the treatment of resistant HBV strains and combination therapies 有权β-L-2'-脱氧核苷用于治疗耐药性HBV病毒株和组合疗法公开(公告)号：US20080182814A1
公开(公告)日：2008-07-31
申请号：US11651353
申请日：2007-01-09
IPC分类号： A61K31/7064 , A61K31/7072 , A61K31/7076 , A61P31/20
CPC分类号： A61K45/06 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K38/21
摘要： It has been discovered that β-L-2′-deoxynucleosides are active against drug-resistant hepatitis B virus with mutations. A method for treating lamivudine resistant HBV (M552V) in a host is provided that includes administering a β-L-2′-deoxynucleoside or its pharmaceutically acceptable salt, ester or prodrug. In addition, a method for preventing lamivudine resistant HBV (M552V) mutation from occurring in a naïve host is provided that includes administering a β-L-2′-deoxynucleoside or its pharmaceutically acceptable salt, ester or prodrug. A method for preventing and/or suppressing the emergence of the HBV double mutant (L528M/M552V) in a host is also provided that includes administering a β-L-2′-deoxynucleoside or its pharmaceutically acceptable salt, ester or prodrug.
摘要翻译： 已经发现β-L-2'-脱氧核苷对具有突变的耐药性乙型肝炎病毒具有活性。 提供了一种治疗宿主中拉米夫定耐药性HBV（M552V）的方法，其包括施用β-L-2'-脱氧核苷或其药学上可接受的盐，酯或前药。 此外，提供了一种用于预防在初始宿主中发生拉米夫定耐药性HBV（M552V）突变的方法，其包括施用β-L-2'-脱氧核苷或其药学上可接受的盐，酯或前药。 还提供了预防和/或抑制宿主中HBV双突变体（L528M / M552V）的出现的方法，其包括施用β-L-2'-脱氧核苷或其药学上可接受的盐，酯或前药。
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5.发明申请Beta-L-2'-deoxynucleosides for the treatment of resistant HBV strains and combination therapies 有权β-L-2'-脱氧核苷用于治疗耐药性HBV病毒株和组合疗法公开(公告)号：US20050080034A1
公开(公告)日：2005-04-14
申请号：US10662641
申请日：2003-09-15
IPC分类号： A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K38/21 , A61K45/06 , A61P31/12 , A61K31/52
CPC分类号： A61K45/06 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K38/21
摘要： It has been discovered that β-L-2′-deoxynucleosides are active against drug-resistant hepatitis B virus with mutations. A method for treating lamivudine resistant HBV (M552V) in a host is provided that includes administering a β-L-2′-deoxynucleoside or its pharmaceutically acceptable salt, ester or prodrug. In addition, a method for preventing lamivudine resistant HBV (M552V) mutation from occurring in a naïve host is provided that includes administering a β-L-2′-deoxynucleoside or its pharmaceutically acceptable salt, ester or prodrug. A method for preventing and/or suppressing the emergence of the HBV double mutant (L528M/M552V) in a host is also provided that includes administering a β-L-2′-deoxynucleoside or its pharmaceutically acceptable salt, ester or prodrug.
摘要翻译： 已经发现β-L-2'-脱氧核苷对具有突变的耐药性乙型肝炎病毒具有活性。 提供了一种治疗宿主中拉米夫定耐药性HBV（M552V）的方法，其包括施用β-L-2'-脱氧核苷或其药学上可接受的盐，酯或前药。 此外，提供了一种用于预防在初始宿主中发生拉米夫定耐药性HBV（M552V）突变的方法，其包括施用β-L-2'-脱氧核苷或其药学上可接受的盐，酯或前药。 还提供了预防和/或抑制宿主中HBV双突变体（L528M / M552V）的出现的方法，其包括施用β-L-2'-脱氧核苷或其药学上可接受的盐，酯或前药。
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公开(公告)号：US06518014B1
公开(公告)日：2003-02-11
申请号：US08890735
申请日：1997-07-11
IPC分类号： C07K1402
CPC分类号： C12N7/00 , C12N2730/10023 , C12Q1/18
摘要： Provided in one embodiment is a non-infectious, recombinant hepadnavirus core particle composition comprising isolated hepadnavirus core particles, template RNA encapsidated in the same core particles and hepadnavirus polymerase encapsidated in the same core particles, wherein, upon addition of deoxynucleoside triphosphates to the composition, the hepadnavirus polymerase incorporates deoxynucleotides from the added deoxynucleosides into reverse transcripts of the template RNA beginning with the first deoxynucleotide of the reverse transcript or within about 10 deoxynucleotides of the first deoxynucleotide of the reverse transcript. Another embodiment provides hapadnaviral core particles with all three functional components: (1) P; (2) C; and (3) a nucleic acid that serves as a template. These core particles include for example (a) recombinant, insect-cell-derived core particles, (b) core particles produced in cells contacted with a reverse transcriptase inhibitor, and (c) core particles that are especially suitable for assays for (+)-strand synthesis.
摘要翻译： 在一个实施方案中提供了一种非感染性重组肝炎病毒核心颗粒组合物，其包含分离的肝炎病毒核心颗粒，包裹在相同核心颗粒中的模板RNA和包裹在相同核心颗粒中的肝炎病毒聚合酶，其中在向组合物中加入脱氧核苷三磷酸时， 肝炎病毒聚合酶将来自加入的脱氧核苷的脱氧核苷酸引入模板RNA的逆转录物，从逆转录物的第一脱氧核苷酸开始，或在逆转录物的第一脱氧核苷酸的约10个脱氧核苷酸内。 另一个实施方案提供了具有所有三种功能组分的半脱乙酰病毒核心颗粒：（1）P; （2）C; 和（3）作为模板的核酸。 这些核心颗粒包括例如（a）重组的昆虫细胞衍生的核心颗粒，（b）在与逆转录酶抑制剂接触的细胞中产生的核心颗粒，和（c）特别适用于（+） 品牌综合。
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7.发明申请BETA-L-2' DEOXYNUCLEOSIDES FOR THE TREATMENT OF RESISTANT HBV STRAINS AND COMBINATION THERAPIES 有权用于治疗耐药性HBV菌株和组合治疗的BETA-L-2'脱氧核糖核酸公开(公告)号：US20110172178A1
公开(公告)日：2011-07-14
申请号：US13052750
申请日：2011-03-21
IPC分类号： A61K31/7072 , A61K31/7068 , A61P31/20
CPC分类号： A61K45/06 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K38/21
摘要： It has been discovered that β-L-2′-deoxynucleosides are active against drug-resistant hepatitis B virus with mutations. A method for treating lamivudine resistant HBV (M552V) in a host is provided that includes administering a β-L-2′-deoxynucleoside or its pharmaceutically acceptable salt, ester or prodrug. In addition, a method for preventing lamivudine resistant HBV (M552V) mutation from occurring in a naïve host is provided that includes administering a β-L-2′-deoxynucleoside or its pharmaceutically acceptable salt, ester or prodrug. A method for preventing and/or suppressing the emergence of the HBV double mutant (L528M/M552V) in a host is also provided that includes administering a β-L-2′-deoxynucleoside or its pharmaceutically acceptable salt, ester or prodrug.
摘要翻译： 已经发现，-L-2'-脱氧核苷对具有突变的耐药性乙型肝炎病毒具有活性。 提供了一种治疗宿主中拉米夫定耐药HBV（M552V）的方法，其包括施用一种β-2'-2'-脱氧核苷或其药学上可接受的盐，酯或前药。 另外，提供了一种用于预防在初始宿主中发生拉米夫定耐药性HBV（M552V）突变的方法，其包括施用一种β-2'-脱氧核苷或其药学上可接受的盐，酯或前药。 还提供了用于预防和/或抑制宿主中HBV双突变体（L528M / M552V）的出现的方法，其包括施用＆bgr。-L-2'-脱氧核苷或其药学上可接受的盐，酯或前药。
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