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1. 发明授权

US08080523B2 Analogs of ShK toxin and their uses in selective inhibition of Kv1.3 potassium channels 有权
标题翻译： ShK毒素类似物及其在Kv1.3钾通道选择性抑制中的应用
公开(公告)号：US08080523B2
公开(公告)日：2011-12-20
申请号：US11663398
申请日：2005-10-07
申请人： Christine Beeton , George K. Chandy , Michael William Pennington
发明人： Christine Beeton , George K. Chandy , Michael William Pennington
IPC分类号： A61K38/00 , A61K38/16 , A61K38/28 , A61P3/04 , A61P25/00 , A61P3/10 , A61P7/12
CPC分类号： A61K38/1767 , A61K47/48038 , A61K47/48261 , A61K47/542 , A61K47/6415 , G01N33/68 , G01N2015/149
摘要： Analogs of ShK toxin and methods for using such ShK analogs. The ShK analogs generally comprise ShK toxin attached to a chemical entity (e.g. an atom, molecule, group, residue, compound, moiety, etc.) that has an anionic charge. In some embodiments the chemical entity attached to the ShK toxin may comprise an amino acid residue. The ShK analogs may be administered to human or non-human animal subjects to cause inhibition of potassium channels or to otherwise treat diseases or disorders. In some embodiments, the chemical entity to which the ShK toxin is attached may be chosen to provide selective inhibition of certain potassium channels (e.g., Kv1.3 channels) over other potassium channels (e.g., Kv1.1 channels). In come embodiments, the chemical entity to which the ShK toxin is attached may include a fluorophore, thereby providing a fluorophore tagged ShK analog. Such fluorophore tagged ShK analogs may be used in flow cytometry alone, or in conjunction with class II tetramers that can detect autoreactive cells.
摘要翻译： ShK毒素的类似物和使用这种ShK类似物的方法。 ShK类似物通常包含与具有阴离子电荷的化学实体（例如原子，分子，基团，残基，化合物，部分等）连接的ShK毒素。在一些实施方案中，连接至ShK毒素的化学实体可以包含氨基酸残基。可以向人类或非人类动物受试者施用ShK类似物以引起钾通道的抑制或以其它方式治疗疾病或病症。在一些实施方案中，可以选择与其连接的ShK毒素的化学实体以提供对其它钾通道（例如Kv1.1通道）的某些钾通道（例如，Kv1.3通道）的选择性抑制。在实施方案中，ShK毒素所连接的化学实体可以包括荧光团，从而提供荧光标记的ShK类似物。这种荧光标记的ShK类似物可以单独使用在流式细胞术中，或与可以检测自身反应性细胞的II类四聚体结合使用。

2. 发明授权

US08440621B2 Analogs of ShK toxin and their uses in selective inhibition of Kv1.3 potassium channels 有权
标题翻译： ShK毒素类似物及其在Kv1.3钾通道选择性抑制中的应用
公开(公告)号：US08440621B2
公开(公告)日：2013-05-14
申请号：US13286939
申请日：2011-11-01
申请人： George K. Chandy , Christine Beeton , Michael William Pennington
发明人： George K. Chandy , Christine Beeton , Michael William Pennington
IPC分类号： A61K38/00 , A61K38/16 , A61P3/04 , A61P25/00
CPC分类号： A61K38/1767 , A61K47/48038 , A61K47/48261 , A61K47/542 , A61K47/6415 , G01N33/68 , G01N2015/149
摘要： Analogs of ShK toxin and methods for using such ShK analogs. The ShK analogs generally comprise ShK toxin attached to a chemical entity (e.g. an atom, molecule, group, residue, compound, moiety, etc.) that has an anionic charge. The ShK analogs may be administered to human or non-human animal subjects to cause inhibition of potassium channels or to otherwise treat diseases or disorders. In some embodiments, the chemical entity to which the ShK toxin is attached may be chosen to provide selective inhibition of certain potassium channels (e.g., Kv1.3 channels) over other potassium channels (e.g., Kv1.1 channels). In come embodiments, the chemical entity to which the ShK toxin is attached may include a fluorophore and such fluorophore-tagged ShK analogs may be used in flow cytometry alone, or in conjunction with class II tetramers that can detect autoreactive cells.
摘要翻译： ShK毒素的类似物和使用这种ShK类似物的方法。 ShK类似物通常包含与具有阴离子电荷的化学实体（例如原子，分子，基团，残基，化合物，部分等）连接的ShK毒素。可以向人类或非人类动物受试者施用ShK类似物以引起钾通道的抑制或以其它方式治疗疾病或病症。在一些实施方案中，可以选择与其连接的ShK毒素的化学实体以提供对其它钾通道（例如Kv1.1通道）的某些钾通道（例如，Kv1.3通道）的选择性抑制。在实施方案中，ShK毒素所连接的化学实体可以包括荧光团，并且此类荧光团标记的ShK类似物可以单独使用在流式细胞术中，或者与能够检测自身反应性细胞的II类四聚体结合使用。

3. 发明申请

US20120142600A1 Analogs of ShK Toxin and their Uses in Selective Inhibition of Kv1.3 Potassium Channels 有权
标题翻译： ShK毒素类似物及其在Kv1.3钾通道选择性抑制中的应用
公开(公告)号：US20120142600A1
公开(公告)日：2012-06-07
申请号：US13286939
申请日：2011-11-01
申请人： Christine Beeton , George K. Chandy , Michael William Pennington
发明人： Christine Beeton , George K. Chandy , Michael William Pennington
IPC分类号： A61K38/17 , A61P37/00
CPC分类号： A61K38/1767 , A61K47/48038 , A61K47/48261 , A61K47/542 , A61K47/6415 , G01N33/68 , G01N2015/149
摘要： Analogs of ShK toxin and methods for using such ShK analogs. The ShK analogs generally comprise ShK toxin attached to a chemical entity (e.g. an atom, molecule, group, residue, compound, moiety, etc.) that has an anionic charge. The ShK analogs may be administered to human or non-human animal subjects to cause inhibition of potassium channels or to otherwise treat diseases or disorders. In some embodiments, the chemical entity to which the ShK toxin is attached may be chosen to provide selective inhibition of certain potassium channels (e.g., Kv1.3 channels) over other potassium channels (e.g., Kv1.1 channels). In come embodiments, the chemical entity to which the ShK toxin is attached may include a fluorophore and such fluorophore-tagged ShK analogs may be used in flow cytometry alone, or in conjunction with class II tetramers that can detect autoreactive cells.
摘要翻译： ShK毒素的类似物和使用这种ShK类似物的方法。 ShK类似物通常包含与具有阴离子电荷的化学实体（例如原子，分子，基团，残基，化合物，部分等）连接的ShK毒素。可以向人类或非人类动物受试者施用ShK类似物以引起钾通道的抑制或以其它方式治疗疾病或病症。在一些实施方案中，可以选择与其连接的ShK毒素的化学实体以提供对其它钾通道（例如Kv1.1通道）的某些钾通道（例如，Kv1.3通道）的选择性抑制。在实施方案中，ShK毒素所连接的化学实体可以包括荧光团，并且此类荧光团标记的ShK类似物可以单独使用在流式细胞术中，或者与能够检测自身反应性细胞的II类四聚体结合使用。

4. 发明申请

US20080221024A1 Analogs of Shk Toxin and Their Uses in Selective Inhibittion of Kv1. 3 Potassium Channels 有权
标题翻译： Shk毒素的类似物及其在Kv1选择性抑制中的应用。 3钾通道
公开(公告)号：US20080221024A1
公开(公告)日：2008-09-11
申请号：US11663398
申请日：2005-10-07
申请人： George K. Chandy , Christine Beeton , William Michael Pennington
发明人： George K. Chandy , Christine Beeton , William Michael Pennington
IPC分类号： A61K38/17 , C07K14/435 , C12Q1/02 , A61P37/00
CPC分类号： A61K38/1767 , A61K47/48038 , A61K47/48261 , A61K47/542 , A61K47/6415 , G01N33/68 , G01N2015/149
摘要： Analogs of ShK toxin and methods for using such ShK analogs. The ShK analogs generally comprise ShK toxin attached to a chemical entity (e.g. an atom, molecule, group, residue, compound, moiety, etc.) that has an anionic charge. In some embodiments the chemical entity attached to the ShK toxin may comprise an amino acid residue. The ShK analogs may be administered to human or non-human animal subjects to cause inhibition of potassium channels or to otherwise treat diseases or disorders. In some embodiments, the chemical entity to which the ShK toxin is attached may be chosen to provide selective inhibition of certain potassium channels (e.g., Kv1.3 channels) over other potassium channels (e.g., Kv1.1 channels). In come embodiments, the chemical entity to which the ShK toxin is attached may include a fluorophore, thereby providing a fluorophore tagged ShK analog. Such fluorophore tagged ShK analogs may be used in flow cytometry alone, or in conjunction with class II tetramers that can detect autoreactive cells.
摘要翻译： ShK毒素的类似物和使用这种ShK类似物的方法。 ShK类似物通常包含与具有阴离子电荷的化学实体（例如原子，分子，基团，残基，化合物，部分等）连接的ShK毒素。在一些实施方案中，连接至ShK毒素的化学实体可以包含氨基酸残基。可以向人类或非人类动物受试者施用ShK类似物以引起钾通道的抑制或以其它方式治疗疾病或病症。在一些实施方案中，可以选择与其连接的ShK毒素的化学实体以提供对其它钾通道（例如，Kv1.1通道）的某些钾通道（例如，Kv1.3通道）的选择性抑制。在实施方案中，ShK毒素所连接的化学实体可以包括荧光团，从而提供荧光标记的ShK类似物。这种荧光标记的ShK类似物可以单独使用在流式细胞术中，或与可以检测自身反应性细胞的II类四聚体结合使用。

5. 发明申请

US20090306159A1 Inhibition of Intermediate-Conductance Calcium Activated Potassium Channels in the Treatment and/or Prevention of Atherosclerosis 审中-公开
标题翻译：中等电导钙激活钾通道在治疗和/或预防动脉粥样硬化中的抑制作用
公开(公告)号：US20090306159A1
公开(公告)日：2009-12-10
申请号：US12066381
申请日：2006-09-12
申请人： Heike Wulff , George K. Chandy , Hiroto Miura
发明人： Heike Wulff , George K. Chandy , Hiroto Miura
IPC分类号： A61K31/415 , A61K31/41 , A61P9/10
CPC分类号： A61K31/415 , A61K31/41
摘要： Methods for treating or preventing atherosclerosis in human or non-human animal subjects by inhibiting or blocking intermediate-conductance calcium activated potassium channels associated with vascular smooth muscle and/or other cells which play a role in the pathogenesis of atherosclerosis (e.g., KCa3.1, KCNN4, IKCa1, IK1, SK4 channels).
摘要翻译：通过抑制或阻断与在动脉粥样硬化发病机制中起作用的血管平滑肌和/或其它细胞相关的中间电导钙激活钾通道来治疗或预防人或非人动物受试者的动脉粥样硬化的方法（例如KCa3.1 ，KCNN4，IKCa1，IK1，SK4通道）。

6. 发明授权

US07507839B2 Therapeutic ion channel blocking agents and methods of use thereof 失效
标题翻译：治疗离子通道阻断剂及其使用方法
公开(公告)号：US07507839B2
公开(公告)日：2009-03-24
申请号：US10507925
申请日：2003-03-20
申请人： Jonathan B. Baell , Heike Wulff , Andrew J. Harvey , Raymond S. Norton , George K. Chandy
发明人： Jonathan B. Baell , Heike Wulff , Andrew J. Harvey , Raymond S. Norton , George K. Chandy
IPC分类号： C07D307/00 , A61K31/34
CPC分类号： C07D417/14 , C07D307/86 , C07D405/14 , C07D409/14
摘要： Various divalent ligands based on khellinone derivatives are described. These derivatives can be useful in the modulation of potassium channel activity in cells, including among others Kv1.3 channels found in T-cells. The compounds may also be useful in the treatment or prevention of autoimmune and inflammatory diseases, including multiple sclerosis.
摘要翻译：描述了基于凯芬酮衍生物的各种二价配体。这些衍生物可用于细胞中钾通道活性的调节，包括在T细胞中发现的Kv1.3通道。所述化合物还可用于治疗或预防自身免疫性和炎性疾病，包括多发性硬化。

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