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1. 发明申请

WO2011113579A2 INFLUENZA A 2009 PANDEMIC H1N1 POLYPEPTIDE FRAGMENTS COMPRISING ENDONUCLEASE ACTIVITY AND THEIR USE 审中-公开
标题翻译： INFLUENZA A 2009大流行H1N1多肽片段包含内切酶活性及其使用
公开(公告)号：WO2011113579A2
公开(公告)日：2011-09-22
申请号：PCT/EP2011/001274
申请日：2011-03-15
申请人： EUROPEAN MOLECULAR BIOLOGY LABORATORY (EMBL) , CUSACK, Stephen , KOWALINSKI, Eva , ZUBIETA, Chloe
发明人： CUSACK, Stephen , KOWALINSKI, Eva , ZUBIETA, Chloe
IPC分类号： C07K14/11
CPC分类号： C12N9/22 , A61K31/33 , A61K38/00 , C07D211/32 , C07D211/96 , C07D311/62 , C07H19/10 , C07K14/005 , C07K16/40 , C07K2299/00 , C07K2317/34 , C12N2760/16122 , G06F19/16
摘要： The present invention relates to polypeptide fragments comprising an amino-terminal fragment of the PA subunit of a viral RNA-dependent RNA polymerase possessing endonuclease activity, wherein said PA subunit is from Influenza A 2009 pandemic HlNl virus or is a variant thereof. This invention also relates to (i) crystals of the polypeptide fragments which are suitable for structure determination of said polypeptide fragments using X-ray crystallography and (ii) computational methods using the structural coordinates of said polypeptide to screen for and design compounds that modulate, preferably inhibit the endonucleolytically active site within the polypeptide fragment. In addition, this invention relates to methods identifying compounds that bind to the PA polypeptide fragments possessing endonuclease activity and preferably inhibit said endonucleolytic activity, preferably in a high throughput setting. This invention also relates to compounds which are able to modulate, preferably to inhibit, the endonuclease activity of the PA subunit polypeptide fragment or variant thereof of the present invention and pharmaceutical compositions comprising said compounds for the treatment of disease conditions caused by viral infections with viruses of the Orthomyxoviridae family, Bunyaviridae family and/or Arenviridae family, preferably caused by viral infections with Influenza A 2009 pandemic HlNl virus. Preferably, said compounds are identifiable by the methods disclosed herein or said pharmaceutical compositions are producible by the methods disclosed herein.
摘要翻译：本发明涉及包含具有核酸内切酶活性的病毒RNA依赖性RNA聚合酶的PA亚单位的氨基末端片段的多肽片段，其中所述PA亚单位来自A流感大流行H1N1病毒，或其变体。本发明还涉及（i）适合于使用X射线晶体学结构测定所述多肽片段的多肽片段的晶体，以及（ii）使用所述多肽的结构坐标筛选和设计调节的化合物的计算方法，优选抑制多肽片段内的核内解离活性位点。此外，本发明涉及鉴定结合具有核酸内切酶活性的PA多肽片段的化合物的方法，优选抑制所述内切核酸酶活性，优选以高通量设置。本发明还涉及能够调节，优选抑制本发明的PA亚基多肽片段或其变体的内切核酸酶活性的化合物和包含所述化合物的药物组合物，用于治疗由病毒感染引起的疾病状况的正粘病毒科，布尼亚病毒科和/或球虫病科，优选由2009年流感大流行H1N1流感病毒感染引起。优选地，所述化合物可以通过本文公开的方法鉴定，或者所述药物组合物可通过本文公开的方法生产。

2. 发明公开

EP2547696A2 FRAGMENTS OF THE PA SUBUNIT OF RNA DEPENDENT RNA POLYMERASE FROM PANDEMIC INFLUENZA VIRUS A 2009 H1N1, AND THEIR USE 有权
标题翻译： PA作者RNA依赖的RNA聚合酶从流行的流感病毒2009年的H1N1病毒及其用途HEIN意识FRAGMENTS
公开(公告)号：EP2547696A2
公开(公告)日：2013-01-23
申请号：EP11709643.8
申请日：2011-03-15
申请人： EUROPEAN MOLECULAR BIOLOGY LABORATORY (EMBL)
发明人： CUSACK, Stephen , KOWALINSKI, Eva , ZUBIETA, Chloe
IPC分类号： C07K14/11 , A61K31/428 , A61K31/33
CPC分类号： C12N9/22 , A61K31/33 , A61K38/00 , C07D211/32 , C07D211/96 , C07D311/62 , C07H19/10 , C07K14/005 , C07K16/40 , C07K2299/00 , C07K2317/34 , C12N2760/16122 , G06F19/16
摘要： The present invention relates to polypeptide fragments comprising an amino-terminal fragment of the PA subunit of a viral RNA-dependent RNA polymerase possessing endonuclease activity, wherein said PA subunit is from Influenza A 2009 pandemic H1N1 virus or is a variant thereof. This invention also relates to (i) crystals of the polypeptide fragments which are suitable for structure determination of said polypeptide fragments using X-ray crystallography and (ii) computational methods using the structural coordinates of said polypeptide to screen for and design compounds that modulate, preferably inhibit the endonucleolytically active site within the polypeptide fragment. In addition, this invention relates to methods identifying compounds that bind to the PA polypeptide fragments possessing endonuclease activity and preferably inhibit said endonucleolytic activity, preferably in a high throughput setting. This invention also relates to compounds which are able to modulate, preferably to inhibit, the endonuclease activity of the PA subunit polypeptide fragment or variant thereof of the present invention and pharmaceutical compositions comprising said compounds for the treatment of disease conditions caused by viral infections with viruses of the Orthomyxoviridae family, Bunyaviridae family and/or Arenviridae family, preferably caused by viral infections with Influenza A 2009 pandemic H1N1 virus. Preferably, said compounds are identifiable by the methods disclosed herein or said pharmaceutical compositions are producible by the methods disclosed herein.
摘要翻译：本发明涉及包括病毒RNA依赖性RNA聚合酶波塞PA亚基的氨基末端片段的唱核酸内切酶活，worin所述PA亚基多肽片段是从流感2009大流行的H1N1病毒或其变体。所以本发明涉及的多肽片段使用X-射线晶体学和（ii）使用所述多肽的结构坐标来筛选计算方法和设计的化合物并调节其适合于所述多肽片段的结构测定（I）的晶体，优选抑制多肽片段内核酸内切酶活。此外，本发明涉及识别并化合物结合到PA多肽片段波塞唱内切酶活性并优选抑制核酸内切说活性，优选以高通量设定方法。因此，这发明涉及能够调节，优选抑制，PA亚基多肽片段或本发明的变体，和药物组合物包含所述化合物的用于疾病状况通过用病毒的病毒感染引起的治疗的核酸内切酶活性的化合物正粘病毒科，布尼亚病毒科和/或沙粒家族的，优选通过用流感病毒感染2009大流行的H1N1病毒引起的。优选地，所述化合物是通过所述方法圆盘在游离缺失或所述药物组合物通过在游离缺失方法可生产的圆盘识别。

3. 发明授权

EP2547696B1 FRAGMENTS OF THE PA SUBUNIT OF RNA DEPENDENT RNA POLYMERASE FROM PANDEMIC INFLUENZA VIRUS A 2009 H1N1, AND THEIR USE 有权
公开(公告)号：EP2547696B1
公开(公告)日：2018-05-23
申请号：EP11709643.8
申请日：2011-03-15
申请人： EUROPEAN MOLECULAR BIOLOGY LABORATORY (EMBL)
发明人： CUSACK, Stephen , KOWALINSKI, Eva , ZUBIETA, Chloe
IPC分类号： A61K31/33 , C07K14/005 , A61K38/00 , C07D311/62 , C07H19/10 , C07K16/40 , C07D211/32 , C07D211/96 , C12N9/22 , G06F19/16
CPC分类号： C12N9/22 , A61K31/33 , A61K38/00 , C07D211/32 , C07D211/96 , C07D311/62 , C07H19/10 , C07K14/005 , C07K16/40 , C07K2299/00 , C07K2317/34 , C12N2760/16122 , G06F19/16
摘要： The present invention relates to polypeptide fragments comprising an amino-terminal fragment of the PA subunit of a viral RNA-dependent RNA polymerase possessing endonuclease activity, wherein said PA subunit is from Influenza A 2009 pandemic H1N1 virus or is a variant thereof. This invention also relates to (i) crystals of the polypeptide fragments which are suitable for structure determination of said polypeptide fragments using X-ray crystallography and (ii) computational methods using the structural coordinates of said polypeptide to screen for and design compounds that modulate, preferably inhibit the endonucleolytically active site within the polypeptide fragment. In addition, this invention relates to methods identifying compounds that bind to the PA polypeptide fragments possessing endonuclease activity and preferably inhibit said endonucleolytic activity, preferably in a high throughput setting. This invention also relates to compounds which are able to modulate, preferably to inhibit, the endonuclease activity of the PA subunit polypeptide fragment or variant thereof of the present invention and pharmaceutical compositions comprising said compounds for the treatment of disease conditions caused by viral infections with viruses of the Orthomyxoviridae family, Bunyaviridae family and/or Arenviridae family, preferably caused by viral infections with Influenza A 2009 pandemic H1N1 virus. Preferably, said compounds are identifiable by the methods disclosed herein or said pharmaceutical compositions are producible by the methods disclosed herein.

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