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1.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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2.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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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：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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4.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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5.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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6.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：US07824851B2
公开(公告)日：2010-11-02
申请号：US10715729
申请日：2003-11-17
申请人： Jean-Pierre Sommadossi , Paolo LaColla , David Standring , Vadim Bichko , Lin Qu
发明人： Jean-Pierre Sommadossi , Paolo LaColla , David Standring , Vadim Bichko , Lin Qu
CPC分类号： A61K31/7072 , A61K31/7052 , A61K38/21 , A61K38/212 , A61K38/215 , A61K38/217 , A61K45/06 , C07H19/06 , C07H19/16 , C07K14/005 , C12N2770/24022 , C12N2770/24122 , C12N2770/24222 , C12Q1/04 , C12Q1/18 , C12Q1/701 , C12Q1/707 , C12Q2600/156 , C12Q2600/158 , G01N2333/186 , A61K2300/00
摘要： The present invention discloses a method for the treatment of Flaviviridae infection that includes the administration of a 2′-branched nucleoside, or a pharmaceutically acceptable prodrug and/or salt thereof, to a human in need of therapy in combination or alternation with a drug that directly or indirectly induces a mutation in the viral genome at a location other than a mutation of a nucleotide that results in a change from seine to a different amino acid in the highly conserved consensus sequence, XRXSGXXXT (Sequence ID No. 63), of domain B of the RNA polymerase region, or is associated with such a mutation. The invention also includes a method to detect a mutant strain of Flaviviridae and a method for its treatment.
摘要翻译： 本发明公开了一种治疗黄病毒科感染的方法，其包括将2支支链核苷或其药学上可接受的前药和/或盐给予需要与药物组合或替代的药物， 在高度保守的共有序列（XRXSGXXXT（序列号63））的区域中，在导致从seine到不同氨基酸的变化的核苷酸的突变以外的位置直接或间接诱导病毒基因组中的突变 B的RNA聚合酶区域，或与这样的突变有关。 本发明还包括检测黄病毒科突变菌株的方法及其治疗方法。
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公开(公告)号：US20050031588A1
公开(公告)日：2005-02-10
申请号：US10715729
申请日：2003-11-17
申请人： Jean-Pierre Sommadossi , Paolo LaColla , David Standring , Vadim Bichko , Lin Qu
发明人： Jean-Pierre Sommadossi , Paolo LaColla , David Standring , Vadim Bichko , Lin Qu
IPC分类号： A61K31/7052 , A61K38/21 , A61K45/06 , C07H19/06 , C07H19/16 , C07K14/18 , C12Q1/70 , A61K31/7056
CPC分类号： A61K31/7072 , A61K31/7052 , A61K38/21 , A61K38/212 , A61K38/215 , A61K38/217 , A61K45/06 , C07H19/06 , C07H19/16 , C07K14/005 , C12N2770/24022 , C12N2770/24122 , C12N2770/24222 , C12Q1/04 , C12Q1/18 , C12Q1/701 , C12Q1/707 , C12Q2600/156 , C12Q2600/158 , G01N2333/186 , A61K2300/00
摘要： The present invention discloses a method for the treatment of Flaviviridae infection that includes the administration of a 2′-branched nucleoside, or a pharmaceutically acceptable prodrug and/or salt thereof, to a human in need of therapy in combination or alternation with a drug that directly or indirectly induces a mutation in the viral genome at a location other than a mutation of a nucleotide that results in a change from serine to a different amino acid in the highly conserved consensus sequence, XRXSGXXXT, of domain B of the RNA polymerase region, or is associated with such a mutation. The invention also includes a method to detect a mutant strain of Flaviviridae and a method for its treatment.
摘要翻译： 本发明公开了一种治疗黄病毒科感染的方法，其包括将2支支链核苷或其药学上可接受的前药和/或盐给予需要与药物组合或替代的药物， 直接或间接地诱导病毒基因组中突变的位置，其不是导致在RNA聚合酶区域B的高度保守的共有序列XRXSGXXXT中从丝氨酸到不同氨基酸的变化的突变， 或与这种突变有关。 本发明还包括检测黄病毒科突变菌株的方法及其治疗方法。
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公开(公告)号：US07951789B2
公开(公告)日：2011-05-31
申请号：US12005937
申请日：2007-12-27
申请人： Jean-Pierre Sommadossi , Gilles Gosselin , Claire Pierra , Christian Perigaud , Suzanne Peyrottes
发明人： Jean-Pierre Sommadossi , Gilles Gosselin , Claire Pierra , Christian Perigaud , Suzanne Peyrottes
CPC分类号： C07H17/02 , A61K31/675 , A61K31/7056 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K31/708 , C07F9/65586 , C07F9/65616 , C07H19/00
摘要： Provided herein are compounds, compositions and methods for the treatment of liver disorder, including HCV and/or HBV infections. Specifically, compound and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents.
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公开(公告)号：US07625875B2
公开(公告)日：2009-12-01
申请号：US11005444
申请日：2004-12-06
CPC分类号： C07K9/003 , A61K31/7068 , A61K31/7072 , A61K38/00 , A61K45/06 , C07H19/06 , C07H19/067 , A61K2300/00
摘要： 2′ and 3′-Prodrugs of 1′, 2′, 3′ or 4′-branched β-D or β-L nucleosides, or their pharmaceutically acceptable salts and derivatives are described, which are useful in the prevention and treatment of Flaviviridae infections and other related conditions. These modified nucleosides provide superior results against flaviviruses and pestiviruses, including hepatitis C virus and viruses generally that replicate through an RNA dependent RNA reverse transcriptase. Compounds, compositions, methods and uses are provided for the treatment of Flaviviridae infection, including HCV infection, that include the administration of an effective amount of the prodrugs of the present invention, or their pharmaceutically acceptable salts or derivatives. These drugs may optionally be administered in combination or alteration with further anti-viral agents to prevent or treat Flaviviridae infections and other related conditions.
摘要翻译： 描述了1'，2'，3'或4'-支链β-D或β-L核苷的2'和3'-前药，或其药学上可接受的盐和衍生物，其可用于预防和治疗黄病毒科 感染等相关条件。 这些修饰的核苷对黄病毒和瘟病毒提供了优异的结果，包括丙型肝炎病毒和通常通过RNA依赖性RNA逆转录酶复制的病毒。 提供化合物，组合物，方法和用途用于治疗包括HCV感染在内的黄病毒科感染，包括施用有效量的本发明前药或其药学上可接受的盐或衍生物。 这些药物可以任选地与另外的抗病毒剂组合或改变来施用，以预防或治疗黄病毒科感染和其他相关病症。
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