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1.发明授权公开(公告)号：US09061070B2
公开(公告)日：2015-06-23
申请号：US13620438
申请日：2012-09-14
申请人： Michael P. Belmares , Jonathan David Garman , Peter S. Lu , Michael W. Salter , Michael Tymianski
发明人： Michael P. Belmares , Jonathan David Garman , Peter S. Lu , Michael W. Salter , Michael Tymianski
CPC分类号： A61K47/48246 , A61K38/00 , A61K47/645 , C07K7/06 , C07K14/70571 , C07K2319/10
摘要： The invention provides methods for treating stroke and compositions for use in the same. The methods employ a chimeric peptide of an active peptide and an internalization peptide. The internalization peptide is a tat variant that promotes uptake of itself and a linked active peptide into a cell without substantial binding to N-type calcium channels. Use of the tat variant allows treating of stroke free of certain side effects associated with binding to N-type calcium channels. Tat variant peptides can also be linked to other active agent for use in treating other diseases.
摘要翻译： 本发明提供了治疗中风和组合物的方法。 该方法采用活性肽和内化肽的嵌合肽。 内化肽是一种tat变体，其促进其自身的摄取和连接的活性肽进入细胞，而不与N型钙通道基本结合。 使用tat变体允许治疗与结合N-型钙通道相关的某些副作用。 Tat变体肽也可以连接到其他活性剂以用于治疗其它疾病。
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公开(公告)号：US20130267470A1
公开(公告)日：2013-10-10
申请号：US13816663
申请日：2011-08-12
IPC分类号： A61K38/07
CPC分类号： A61K38/07 , A61K38/08 , A61K38/1709 , A61K38/1787 , A61K47/645 , C07K7/06 , C07K2319/10 , C12N9/0075 , C12Y114/13039 , G01N33/573 , G01N33/6872 , G01N2333/70571 , G01N2333/90254 , G01N2500/02
摘要： The invention provides methods of treatment or prophylaxis of damaging effects of penetrative injury to the brain or other part of the central nervous system. The methods are based in part on results in a rodent model of penetrative ballistic injury showing that an inhibitor of PDF-95 NMDAR interaction is effective in inhibiting neurological deficits resulting from such injury. The methods are useful for treating subjects having or at risk of penetrative brain injury, including subjects who have been shot in the head or at risk of such injury (e.g., military or law enforcement personnel).
摘要翻译： 本发明提供了治疗或预防对大脑或中枢神经系统其他部分的穿透性损伤的损伤作用的方法。 该方法部分基于穿透性弹道损伤啮齿动物模型的结果，表明PDF-95 NMDAR相互作用的抑制剂有效抑制由此类损伤引起的神经功能缺损。 这些方法对于治疗具有或具有渗透性脑损伤风险的受试者是有用的，包括头部受到攻击或有受伤风险的受试者（例如军事或执法人员）。
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3.发明申请Treating Stroke and Other Diseases Without Inhibiting N-Type Calcium Channels 审中-公开治疗中风和其他疾病，不抑制N型钙通道公开(公告)号：US20130172230A1
公开(公告)日：2013-07-04
申请号：US13620438
申请日：2012-09-14
申请人： Michael P. Belmares , Jonathan David Garman , Peter S. Lu , Michael W. Salter , Michael Tymianski
发明人： Michael P. Belmares , Jonathan David Garman , Peter S. Lu , Michael W. Salter , Michael Tymianski
CPC分类号： A61K47/48246 , A61K38/00 , A61K47/645 , C07K7/06 , C07K14/70571 , C07K2319/10
摘要： The invention provides methods for treating stroke and compositions for use in the same. The methods employ a chimeric peptide of an active peptide and an internalization peptide. The internalization peptide is a tat variant that promotes uptake of itself and a linked active peptide into a cell without substantial binding to N-type calcium channels. Use of the tat variant allows treating of stroke free of certain side effects associated with binding to N-type calcium channels. Tat variant peptides can also be linked to other active agent for use in treating other diseases.
摘要翻译： 本发明提供了治疗中风和组合物的方法。 该方法采用活性肽和内化肽的嵌合肽。 内化肽是一种tat变体，其促进其自身的摄取和连接的活性肽进入细胞，而不与N型钙通道基本结合。 使用tat变体允许治疗与结合N-型钙通道相关的某些副作用。 Tat变体肽也可以连接到其他活性剂以用于治疗其它疾病。
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4.发明申请公开(公告)号：US20080274977A1
公开(公告)日：2008-11-06
申请号：US12040851
申请日：2008-02-29
申请人： Michael P. Belmares , Jonathan David Garman , Peter S. Lu , Michael W. Salter , Michael Tymianski
发明人： Michael P. Belmares , Jonathan David Garman , Peter S. Lu , Michael W. Salter , Michael Tymianski
CPC分类号： A61K47/48246 , A61K38/00 , A61K47/645 , C07K7/06 , C07K14/70571 , C07K2319/10
摘要： The invention provides methods for treating stroke and compositions for use in the same. The methods employ a chimeric peptide of an active peptide and an internalization peptide. The internalization peptide is a tat variant that promotes uptake of itself and a linked active peptide into a cell without substantial binding to N-type calcium channels. Use of the tat variant allows treating of stroke free of certain side effects associated with binding to N-type calcium channels. Tat variant peptides can also be linked to other active agent for use in treating other diseases.
摘要翻译： 本发明提供了治疗中风和组合物的方法。 该方法采用活性肽和内化肽的嵌合肽。 内化肽是一种tat变体，其促进其自身的摄取和连接的活性肽进入细胞，而不与N型钙通道基本结合。 使用tat变体允许治疗与结合N-型钙通道相关的某些副作用。 Tat变体肽也可以连接到其他活性剂以用于治疗其它疾病。
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公开(公告)号：US09629892B2
公开(公告)日：2017-04-25
申请号：US13816663
申请日：2011-08-12
IPC分类号： A61K38/07 , A61K38/08 , C07K7/06 , A61K47/48 , G01N33/573 , G01N33/68 , C12N9/02 , A61K38/17
CPC分类号： A61K38/07 , A61K38/08 , A61K38/1709 , A61K38/1787 , A61K47/645 , C07K7/06 , C07K2319/10 , C12N9/0075 , C12Y114/13039 , G01N33/573 , G01N33/6872 , G01N2333/70571 , G01N2333/90254 , G01N2500/02
摘要： The invention provides methods of treatment or prophylaxis of damaging effects of penetrative injury to the brain or other part of the central nervous system. The methods are based in part on results in a rodent model of penetrative ballistic injury showing that an inhibitor of PDF-95 NMDAR interaction is effective in inhibiting neurological deficits resulting from such injury. The methods are useful for treating subjects having or at risk of penetrative brain injury, including subjects who have been shot in the head or at risk of such injury (e.g., military or law enforcement personnel).
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公开(公告)号：US08324168B2
公开(公告)日：2012-12-04
申请号：US12553096
申请日：2009-09-03
申请人： Michael P. Belmares , Jonathan David Garman , Peter S. Lu , Michael W. Salter , Michael Tymianski
发明人： Michael P. Belmares , Jonathan David Garman , Peter S. Lu , Michael W. Salter , Michael Tymianski
IPC分类号： C07K14/435 , A61K38/16
摘要： The invention provides agents useful for treating pain. An exemplary agent comprises or consists of the a portion of a retroviral Tat protein. One such agent is the peptide Tat-NR2B9c. This peptide has previously been described as an agent for inhibiting damaging effects of stroke and similar conditions via inhibition of PSD95 interactions with NMDA receptors and/or NOS. The present application provides data showing that the Tat-NR2B9c peptides is effective in alleviation of pain. The alleviation of pain can be obtained at a dose of the peptide below the dose required to inhibit PSD-95 interactions with NMDAR or NOS.
摘要翻译： 本发明提供可用于治疗疼痛的药剂。 一个示例性药剂包含一部分逆转录病毒Tat蛋白或由其组成。 一种这样的药剂是Tat-NR2B9c肽。 此肽以前已经被描述为通过抑制与NMDA受体和/或NOS的PSD95相互作用来抑制中风和类似条件的损伤作用的药剂。 本申请提供了显示Tat-NR2B9c肽有效缓解疼痛的数据。 疼痛缓解可以在低于抑制PSD-95与NMDAR或NOS相互作用所需剂量的肽剂量下获得。
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7.发明授权公开(公告)号：US08288345B2
公开(公告)日：2012-10-16
申请号：US12040851
申请日：2008-02-29
申请人： Michael P. Belmares , Jonathan David Garman , Peter S. Lu , Michael W. Salter , Michael Tymianski
发明人： Michael P. Belmares , Jonathan David Garman , Peter S. Lu , Michael W. Salter , Michael Tymianski
CPC分类号： A61K47/48246 , A61K38/00 , A61K47/645 , C07K7/06 , C07K14/70571 , C07K2319/10
摘要： The invention provides methods for treating stroke and compositions for use in the same. The methods employ a chimeric peptide of an active peptide and an internalization peptide. The internalization peptide is a tat variant that promotes uptake of itself and a linked active peptide into a cell without substantial binding to N-type calcium channels. Use of the tat variant allows treating of stroke free of certain side effects associated with binding to N-type calcium channels. Tat variant peptides can also be linked to other active agent for use in treating other diseases.
摘要翻译： 本发明提供了治疗中风和组合物的方法。 该方法采用活性肽和内化肽的嵌合肽。 内化肽是一种tat变体，其促进其自身的摄取和连接的活性肽进入细胞，而不与N型钙通道基本结合。 使用tat变体允许治疗与结合N-型钙通道相关的某些副作用。 Tat变体肽也可以连接到其他活性剂以用于治疗其它疾病。
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公开(公告)号：US20100062985A1
公开(公告)日：2010-03-11
申请号：US12553096
申请日：2009-09-03
申请人： Michael P. Belmares , Jonathan David Garman , Peter S. Lu , Michael W. Salter , Michael Tymianski
发明人： Michael P. Belmares , Jonathan David Garman , Peter S. Lu , Michael W. Salter , Michael Tymianski
摘要： The invention provides agents useful for treating pain. An exemplary agent comprises or consists of the a portion of a retroviral Tat protein. One such agent is the peptide Tat-NR2B9c. This peptide has previously been described as an agent for inhibiting damaging effects of stroke and similar conditions via inhibition of PSD95 interactions with NMDA receptors and/or NOS. The present application provides data showing that the Tat-NR2B9c peptides is effective in alleviation of pain. The alleviation of pain can be obtained at a dose of the peptide below the dose required to inhibit PSD-95 interactions with NMDAR or NOS.
摘要翻译： 本发明提供可用于治疗疼痛的药剂。 一个示例性药剂包含一部分逆转录病毒Tat蛋白或由其组成。 一种这样的药剂是Tat-NR2B9c肽。 此肽以前已经被描述为通过抑制与NMDA受体和/或NOS的PSD95相互作用来抑制中风和类似条件的损伤作用的药剂。 本申请提供了显示Tat-NR2B9c肽有效缓解疼痛的数据。 疼痛缓解可以在低于抑制PSD-95与NMDAR或NOS相互作用所需剂量的肽剂量下获得。
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9.发明授权公开(公告)号：US08933013B2
公开(公告)日：2015-01-13
申请号：US13377519
申请日：2010-06-10
IPC分类号： A61K38/00 , A61K38/02 , A61K38/17 , A61K38/16 , A61K38/10 , C07K7/08 , A61K38/08 , A61K47/48 , A61K45/06 , A61K31/275
CPC分类号： A61K47/64 , A61K31/275 , A61K31/277 , A61K38/08 , A61K38/10 , A61K45/06 , A61K47/645 , C07K16/1072 , C07K2319/10 , A61K2300/00
摘要： The invention provides methods of delivering pharmacologic agents linked to an internalization peptide, in which an inflammatory response inducible by the internalization peptide is inhibited by co-administration of an anti-inflammatory or by linking the internalization peptide to biotin or similar molecule. Such methods are premised in part on the results described in the examples whereby administration of a pharmacological agent linked to tat at high dosages is closely followed by an inflammatory response, which includes mast cell degranulation, histamine release and the typical sequelae of histamine release, such as redness, heat, swelling, and hypotension.
摘要翻译： 本发明提供了递送与内化肽连接的药理学试剂的方法，其中通过共同给予抗炎剂或通过将内化肽与生物素或类似分子连接来抑制内化肽诱导的炎症反应。 这些方法部分地基于实施例中描述的结果，其中以高剂量施用与tat连接的药剂紧随其后是炎性反应，其包括肥大细胞脱粒，组胺释放和组胺释放的典型后遗症，例如 作为发红，发热，肿胀和低血压。
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公开(公告)号：US08680137B2
公开(公告)日：2014-03-25
申请号：US12966871
申请日：2010-12-13
IPC分类号： A01N43/12 , A61K31/38 , A01N43/06 , C07D333/00 , C07D311/02
CPC分类号： A61K31/551 , A61K31/122 , A61K31/353 , A61K31/381 , A61K31/4245 , A61K31/427 , A61K31/428 , A61K31/433 , A61K31/4704 , A61K31/4709 , A61K31/4725 , A61K31/496 , C07D209/08 , C07D215/08 , C07D215/233 , C07D277/36 , C07D277/82 , C07D311/18 , C07D333/38 , C07D333/60 , C07D339/00 , C07D403/06 , C07D409/04 , C07D409/06 , C07D417/04 , C40B40/04 , G01N33/6872 , G01N2510/00
摘要： This invention relates to methods of screening for modulators of mammalian cell injury cause by TRPM7 gene and protein activity, compounds that modulate TRPM7 gene and protein activity and methods of treatment of mammalian cell injury using modulators of TRPM7 gene and protein activity.
摘要翻译： 本发明涉及使用TRPM7基因和蛋白质活性的调节剂筛选TRPM7基因和蛋白质活性引起的哺乳动物细胞损伤调节剂，调节TRPM7基因的化合物和蛋白质活性的方法以及哺乳动物细胞损伤治疗方法。
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