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1. 发明授权

US07569536B2 Method for controlling SR protein phosphorylation, and antiviral agents whose active ingredients comprise agents that control SR protein activity 有权
标题翻译：用于控制SR蛋白磷酸化的方法，以及其活性成分包含控制SR蛋白活性的试剂的抗病毒剂
公开(公告)号：US07569536B2
公开(公告)日：2009-08-04
申请号：US10584482
申请日：2004-12-24
申请人： Masatoshi Hagiwara , Takeshi Fukuhara , Masaaki Suzuki , Takamitsu Hosoya
发明人： Masatoshi Hagiwara , Takeshi Fukuhara , Masaaki Suzuki , Takamitsu Hosoya
IPC分类号： A01N61/00 , A61K51/00 , C12N15/09 , C12N9/12
CPC分类号： A61K31/444 , A61K31/4409 , A61K31/4439 , A61K31/4453 , A61K31/4545 , A61K31/455 , A61K31/5377 , A61K31/55 , C07D211/14 , C07D213/81 , C07D213/82 , C07D401/12 , C12N15/1137 , Y02A50/385 , Y02A50/389 , Y02A50/463 , Y02A50/465 , Y02A50/467
摘要： The present invention provides: (1) antiviral agents that act by reducing or inhibiting the activity of SR proteins, more specifically, (i) antiviral agents that act by enhancing dephosphorylation of SR proteins, and (ii) antiviral agents that act by inhibiting proteins that phosphorylate SR proteins; (2) antiviral agents that act by inhibiting the expression of SR proteins, and (3) antiviral agents that act by activating proteins that antagonize SR proteins. The present invention also provides compounds that inhibit SRPKs, which phosphorylate SR proteins. Such compounds inhibit the activity of SR proteins and have antiviral activities. Various new viruses including SARS have emerged, and thus the present invention provides long-lasting broad-spectrum antiviral agents applicable to new viruses.
摘要翻译：本发明提供：（1）通过降低或抑制SR蛋白的活性而起作用的抗病毒剂，更具体地，（i）通过增强SR蛋白的去磷酸化作用的抗病毒剂，和（ii）通过抑制蛋白质起作用的抗病毒剂磷酸化SR蛋白; （2）通过抑制SR蛋白的表达起作用的抗病毒剂，和（3）通过激活拮抗SR蛋白的蛋白质起作用的抗病毒剂。本发明还提供抑制磷酸化SR蛋白的SRPK的化合物。这些化合物抑制SR蛋白的活性并具有抗病毒活性。出现了包括SARS在内的各种新病毒，因此本发明提供了适用于新病毒的长效广谱抗病毒剂。

2. 发明授权

US08338362B2 Methods for controlling SR protein phosphorylation, and antiviral agents whose active ingredients comprise agents that control SR protein activity 有权
标题翻译：用于控制SR蛋白磷酸化的方法，以及其活性成分包含控制SR蛋白活性的试剂的抗病毒剂
公开(公告)号：US08338362B2
公开(公告)日：2012-12-25
申请号：US12494102
申请日：2009-06-29
申请人： Masatoshi Hagiwara , Takeshi Fukuhara , Masaaki Suzuki , Takamitsu Hosoya
发明人： Masatoshi Hagiwara , Takeshi Fukuhara , Masaaki Suzuki , Takamitsu Hosoya
IPC分类号： A01N61/00 , A61K31/00 , A61K49/00 , C12N15/09 , C12N9/12
CPC分类号： A61K31/444 , A61K31/4409 , A61K31/4439 , A61K31/4453 , A61K31/4545 , A61K31/455 , A61K31/5377 , A61K31/55 , C07D211/14 , C07D213/81 , C07D213/82 , C07D401/12 , C12N15/1137 , Y02A50/385 , Y02A50/389 , Y02A50/463 , Y02A50/465 , Y02A50/467
摘要： The present invention provides: (1) antiviral agents that act by reducing or inhibiting the activity of SR proteins, more specifically, (i) antiviral agents that act by enhancing dephosphorylation of SR proteins, and (ii) antiviral agents that act by inhibiting proteins that phosphorylate SR proteins; (2) antiviral agents that act by inhibiting the expression of SR proteins, and (3) antiviral agents that act by activating proteins that antagonize SR proteins. The present invention also provides compounds that inhibit SRPKs, which phosphorylate SR proteins. Such compounds inhibit the activity of SR proteins and have antiviral activities. Various new viruses including SARS have emerged, and thus the present invention provides long-lasting broad-spectrum antiviral agents applicable to new viruses.
摘要翻译：本发明提供：（1）通过降低或抑制SR蛋白的活性而起作用的抗病毒剂，更具体地，（i）通过增强SR蛋白的去磷酸化作用的抗病毒剂，和（ii）通过抑制蛋白质起作用的抗病毒剂磷酸化SR蛋白; （2）通过抑制SR蛋白的表达起作用的抗病毒剂，和（3）通过激活拮抗SR蛋白的蛋白质起作用的抗病毒剂。本发明还提供抑制磷酸化SR蛋白的SRPK的化合物。这些化合物抑制SR蛋白的活性并具有抗病毒活性。出现了包括SARS在内的各种新病毒，因此本发明提供了适用于新病毒的长效广谱抗病毒剂。

3. 发明申请

US20130079369A1 METHODS FOR CONTROLLING SR PROTEIN PHOSPHORYLATION, AND ANTIVIRAL AGENTS WHOSE ACTIVE INGREDIENTS COMPRISE AGENTS THAT CONTROL SR PROTEIN ACTIVITY 有权
标题翻译：用于控制SR蛋白磷酸化的方法以及活性成分包含控制SR蛋白活性的试剂的抗病毒剂
公开(公告)号：US20130079369A1
公开(公告)日：2013-03-28
申请号：US13680538
申请日：2012-11-19
申请人： Masatoshi Hagiwara , Takeshi Fukuhara , Masaaki Suzuki , Takamitsu Hosoya
发明人： Masatoshi Hagiwara , Takeshi Fukuhara , Masaaki Suzuki , Takamitsu Hosoya
IPC分类号： A61K31/444
CPC分类号： A61K31/444 , A61K31/4409 , A61K31/4439 , A61K31/4453 , A61K31/4545 , A61K31/455 , A61K31/5377 , A61K31/55 , C07D211/14 , C07D213/81 , C07D213/82 , C07D401/12 , C12N15/1137 , Y02A50/385 , Y02A50/389 , Y02A50/463 , Y02A50/465 , Y02A50/467
摘要： The present invention provides: (1) antiviral agents that act by reducing or inhibiting the activity of SR proteins, more specifically, (i) antiviral agents that act by enhancing dephosphorylation of SR proteins, and (ii) antiviral agents that act by inhibiting proteins that phosphorylate SR proteins; (2) antiviral agents that act by inhibiting the expression of SR proteins, and (3) antiviral agents that act by activating proteins that antagonize SR proteins. The present invention also provides compounds that inhibit SRPKs, which phosphorylate SR proteins. Such compounds inhibit the activity of SR proteins and have antiviral activities. Various new viruses including SARS have emerged, and thus the present invention provides long-lasting broad-spectrum antiviral agents applicable to new viruses.
摘要翻译：本发明提供：（1）通过降低或抑制SR蛋白的活性而起作用的抗病毒剂，更具体地，（i）通过增强SR蛋白的去磷酸化起作用的抗病毒剂，和（ii）通过抑制蛋白质起作用的抗病毒剂磷酸化SR蛋白; （2）通过抑制SR蛋白的表达起作用的抗病毒剂，和（3）通过激活拮抗SR蛋白的蛋白质起作用的抗病毒剂。本发明还提供抑制磷酸化SR蛋白的SRPK的化合物。这些化合物抑制SR蛋白的活性并具有抗病毒活性。出现了包括SARS在内的各种新病毒，因此本发明提供了适用于新病毒的长效广谱抗病毒剂。

4. 发明申请

US20100016359A1 METHODS FOR CONTROLLING SR PROTEIN PHOSPHORYLATION, AND ANTIVIRAL AGENTS WHOSE ACTIVE INGREDIENTS COMPRISE AGENTS THAT CONTROL SR PROTEIN ACTIVITY 有权
标题翻译：用于控制SR蛋白磷酸化的方法以及活性成分包含控制SR蛋白活性的试剂的抗病毒剂
公开(公告)号：US20100016359A1
公开(公告)日：2010-01-21
申请号：US12494102
申请日：2009-06-29
申请人： Masatoshi Hagiwara , Takeshi Fukuhara , Masaaki Suzuki , Takamitsu Hosoya
发明人： Masatoshi Hagiwara , Takeshi Fukuhara , Masaaki Suzuki , Takamitsu Hosoya
IPC分类号： A61K31/4545 , A61P31/12
CPC分类号： A61K31/444 , A61K31/4409 , A61K31/4439 , A61K31/4453 , A61K31/4545 , A61K31/455 , A61K31/5377 , A61K31/55 , C07D211/14 , C07D213/81 , C07D213/82 , C07D401/12 , C12N15/1137 , Y02A50/385 , Y02A50/389 , Y02A50/463 , Y02A50/465 , Y02A50/467
摘要： The present invention provides: (1) antiviral agents that act by reducing or inhibiting the activity of SR proteins, more specifically, (i) antiviral agents that act by enhancing dephosphorylation of SR proteins, and (ii) antiviral agents that act by inhibiting proteins that phosphorylate SR proteins; (2) antiviral agents that act by inhibiting the expression of SR proteins, and (3) antiviral agents that act by activating proteins that antagonize SR proteins. The present invention also provides compounds that inhibit SRPKs, which phosphorylate SR proteins. Such compounds inhibit the activity of SR proteins and have antiviral activities. Various new viruses including SARS have emerged, and thus the present invention provides long-lasting broad-spectrum antiviral agents applicable to new viruses.
摘要翻译：本发明提供：（1）通过降低或抑制SR蛋白的活性而起作用的抗病毒剂，更具体地，（i）通过增强SR蛋白的去磷酸化作用的抗病毒剂，和（ii）通过抑制蛋白质起作用的抗病毒剂磷酸化SR蛋白; （2）通过抑制SR蛋白的表达起作用的抗病毒剂，和（3）通过激活拮抗SR蛋白的蛋白质起作用的抗病毒剂。本发明还提供抑制磷酸化SR蛋白的SRPK的化合物。这些化合物抑制SR蛋白的活性并具有抗病毒活性。出现了包括SARS在内的各种新病毒，因此本发明提供了适用于新病毒的长效广谱抗病毒剂。

5. 发明申请

US20070135367A1 Method for controlling sr protein phosphorylation, and antiviral agents whose active ingredients comprise agents that control sr protein activity 有权
标题翻译：用于控制SR蛋白磷酸化的方法，以及其活性成分包含控制sr蛋白活性的试剂的抗病毒剂
公开(公告)号：US20070135367A1
公开(公告)日：2007-06-14
申请号：US10584482
申请日：2004-12-24
申请人： Masatoshi Hagiwara , Takeshi Fukuhara , Masaaki Suzuki , Takamitsu Hosoya
发明人： Masatoshi Hagiwara , Takeshi Fukuhara , Masaaki Suzuki , Takamitsu Hosoya
IPC分类号： A61K31/445 , A61K48/00 , A61K31/24 , A61K31/44
CPC分类号： A61K31/444 , A61K31/4409 , A61K31/4439 , A61K31/4453 , A61K31/4545 , A61K31/455 , A61K31/5377 , A61K31/55 , C07D211/14 , C07D213/81 , C07D213/82 , C07D401/12 , C12N15/1137 , Y02A50/385 , Y02A50/389 , Y02A50/463 , Y02A50/465 , Y02A50/467
摘要： The present invention provides: (1) antiviral agents that act by reducing or inhibiting the activity of SR proteins, more specifically, (i) antiviral agents that act by enhancing dephosphorylation of SR proteins, and (ii) antiviral agents that act by inhibiting proteins that phosphorylate SR proteins; (2) antiviral agents that act by inhibiting the expression of SR proteins, and (3) antiviral agents that act by activating proteins that antagonize SR proteins. The present invention also provides compounds that inhibit SRPKs, which phosphorylate SR proteins. Such compounds inhibit the activity of SR proteins and have antiviral activities. Various new viruses including SARS have emerged, and thus the present invention provides long-lasting broad-spectrum antiviral agents applicable to new viruses.
摘要翻译：本发明提供：（1）通过降低或抑制SR蛋白的活性而起作用的抗病毒剂，更具体地，（i）通过增强SR蛋白的去磷酸化作用的抗病毒剂，和（ii）通过抑制蛋白质起作用的抗病毒剂磷酸化SR蛋白; （2）通过抑制SR蛋白的表达起作用的抗病毒剂，和（3）通过激活拮抗SR蛋白的蛋白质起作用的抗病毒剂。本发明还提供抑制磷酸化SR蛋白的SRPK的化合物。这些化合物抑制SR蛋白的活性并具有抗病毒活性。出现了包括SARS在内的各种新病毒，因此本发明提供了适用于新病毒的长效广谱抗病毒剂。

6. 发明申请

US20110059950A1 ANILINE DERIVATIVE HAVING ANTI-RNA VIRAL ACTIVITY 有权
标题翻译：具有抗RNA病毒活性的苯胺衍生物
公开(公告)号：US20110059950A1
公开(公告)日：2011-03-10
申请号：US12934206
申请日：2009-02-04
申请人： Hiroshi Onogi , Masatoshi Hagiwara , Masaaki Suzuki , Hiroko Koyama , Takamitsu Hosoya , Toshiyuki Hiramatsu
发明人： Hiroshi Onogi , Masatoshi Hagiwara , Masaaki Suzuki , Hiroko Koyama , Takamitsu Hosoya , Toshiyuki Hiramatsu
IPC分类号： A61K31/55 , A61K31/4545 , C07D401/12 , A61K31/4427 , A61K31/455 , C07D213/82 , A61K31/4709 , A61K31/4725 , A61P31/14
CPC分类号： C07D213/81 , A61K31/00 , A61K31/395 , A61K31/4545 , A61K31/455 , A61K31/55 , C07D213/82 , C07D213/83 , C07D225/02 , C07D401/12 , C07D405/12 , C07D409/12
摘要： Viruses, and particularly RNA viruses, have high mutation rates. Hence, antiviral agents that have been developed to date targeting protease or reverse transcriptase of viruses have quickly lost their effectiveness and resistant viruses have emerged. Also, in recent years, viral diseases caused by various new viruses such as SARS, avian influenza, and the hepatitis C have become social menaces. Therefore, the development of a novel antiviral agent that can cope with a virus resistant to an existing drug or a new virus and has a wide range of applications has been demanded. The present invention provides a novel anti-RNA viral agent and a method for use thereof. The present invention further provides an anti-RNA viral agent that is also effective against a new virus or a drug-resistant virus, and a method for use thereof.
摘要翻译：病毒，特别是RNA病毒，具有高突变率。因此，迄今为止开发的针对蛋白酶或病毒逆转录酶的抗病毒药物已经迅速丧失其有效性，并出现了抗性病毒。另外近年来，由SARS，禽流感，丙型肝炎等各种新病毒引起的病毒性疾病已成为社会威胁。因此，需要开发能够应对对现有药物或新病毒有抵抗性的病毒的新型抗病毒剂，并且具有广泛的应用。本发明提供了一种新的抗-RNA病毒剂及其使用方法。本发明还提供了对新病毒或耐药性病毒也有效的抗RNA病毒剂及其使用方法。

7. 发明授权

US08765941B2 Aniline derivative having anti-RNA viral activity 有权
标题翻译：具有抗RNA病毒活性的苯胺衍生物
公开(公告)号：US08765941B2
公开(公告)日：2014-07-01
申请号：US12934206
申请日：2009-02-04
申请人： Hiroshi Onogi , Masatoshi Hagiwara , Masaaki Suzuki , Hiroko Koyama , Takamitsu Hosoya , Toshiyuki Hiramatsu
发明人： Hiroshi Onogi , Masatoshi Hagiwara , Masaaki Suzuki , Hiroko Koyama , Takamitsu Hosoya , Toshiyuki Hiramatsu
IPC分类号： C07D225/02 , C07D401/00 , C07D401/12 , A61K31/395 , C07D213/83 , C07D405/12 , A61K31/55 , A61K31/00 , A61K31/4545 , C07D213/81 , A61K31/455 , C07D213/82 , C07D409/12
CPC分类号： C07D213/81 , A61K31/00 , A61K31/395 , A61K31/4545 , A61K31/455 , A61K31/55 , C07D213/82 , C07D213/83 , C07D225/02 , C07D401/12 , C07D405/12 , C07D409/12
摘要： Viruses, and particularly RNA viruses, have high mutation rates. Hence, antiviral agents that have been developed to date targeting protease or reverse transcriptase of viruses have quickly lost their effectiveness and resistant viruses have emerged. Also, in recent years, viral diseases caused by various new viruses such as SARS, avian influenza, and the hepatitis C have become social menaces. Therefore, the development of a novel antiviral agent that can cope with a virus resistant to an existing drug or a new virus and has a wide range of applications has been demanded. The present invention provides a novel anti-RNA viral agent and a method for use thereof. The present invention further provides an anti-RNA viral agent that is also effective against a new virus or a drug-resistant virus, and a method for use thereof.
摘要翻译：病毒，特别是RNA病毒，具有高突变率。因此，迄今为止开发的针对蛋白酶或病毒逆转录酶的抗病毒药物已经迅速丧失其有效性，并出现了抗性病毒。另外近年来，由SARS，禽流感，丙型肝炎等各种新病毒引起的病毒性疾病已成为社会威胁。因此，需要开发能够应对对现有药物或新病毒有抵抗性的病毒的新型抗病毒剂，并且具有广泛的应用。本发明提供了一种新的抗-RNA病毒剂及其使用方法。本发明还提供了对新病毒或耐药性病毒也有效的抗RNA病毒剂及其使用方法。

8. 发明授权

US07786151B2 Therapeutic composition of treating abnormal splicing caused by the excessive kinase induction 有权
标题翻译：治疗由过度激酶诱导引起的异常剪接的组合物
公开(公告)号：US07786151B2
公开(公告)日：2010-08-31
申请号：US11029470
申请日：2005-01-06
申请人： Masatoshi Hagiwara , Masaaki Suzuki
发明人： Masatoshi Hagiwara , Masaaki Suzuki
IPC分类号： A01N43/82 , A01N43/78 , A61K31/425
CPC分类号： A61K31/428 , A61K31/7052
摘要： The present invention provides a composition of treating, preventing abnormal splicing caused by the excessive kinase induction, which comprises TG003 and a method using the same of treating, preventing abnormal splicing caused by the excessive kinase induction.
摘要翻译：本发明提供了治疗，预防由过度激酶诱导引起的异常剪接的组合物，其包含TG003，以及使用该组合物治疗预防由过度激酶诱导引起的异常剪接的方法。

9. 发明申请

US20050171026A1 Therapeutic composition of treating abnormal splicing caused by the excessive kinase induction 有权
标题翻译：治疗由过度激酶诱导引起的异常剪接的组合物
公开(公告)号：US20050171026A1
公开(公告)日：2005-08-04
申请号：US11029470
申请日：2005-01-06
申请人： Masatoshi Hagiwara , Masaaki Suzuki
发明人： Masatoshi Hagiwara , Masaaki Suzuki
IPC分类号： A61K31/428 , A61K31/7052 , A61P35/00
CPC分类号： A61K31/428 , A61K31/7052
摘要： The present invention provides a composition of treating, preventing abnormal splicing caused by the excessive kinase induction, which comprises TG003 and a method using the same of treating, preventing abnormal splicing caused by the excessive kinase induction.
摘要翻译：本发明提供了治疗，预防由过度激酶诱导引起的异常剪接的组合物，其包含TG003，以及使用该组合物治疗预防由过度激酶诱导引起的异常剪接的方法。

10. 发明授权

US09273364B2 Transgenic reporter system that reveals expression profiles and regulation mechanisms of alternative splicing in mammalian organisms 有权
标题翻译：转基因报告系统，揭示哺乳动物生物体内可变剪接的表达谱和调节机制
公开(公告)号：US09273364B2
公开(公告)日：2016-03-01
申请号：US13700890
申请日：2011-05-31
申请人： Masatoshi Hagiwara , Akihide Takeuchi
发明人： Masatoshi Hagiwara , Akihide Takeuchi
IPC分类号： C12Q1/68 , C12N15/10 , C12N15/00 , C12N15/01
CPC分类号： C12Q1/6897 , C12N15/1086
摘要： An object of the present invention is to develop a new alternative splicing reporter system and to provide a method for detecting alternative splicing patterns in a mammalian multicellular organism more precisely, a method for identifying efficiently substances and gene regions that affect alternative splicing in a mammalian multicellular organism, and the like by utilizing the alternative splicing reporter system. Specifically, the present invention relates to a method for detecting alternative splicing in a mammalian multicellular organism, and a method for identifying substances and gene regions that affect alternative splicing in a mammalian multicellular organism, which use a DNA construct in which at least two different reporter genes are inserted into a specific gene that undergoes alternative splicing, or a combination of DNA constructs (a combination of at least two different DNA constructs) in which DNA construct a reporter gene is inserted into a specific gene that undergoes alternative splicing.
摘要翻译：本发明的一个目的是开发一种新的选择性剪接报道系统，并提供一种用于更准确地检测哺乳动物多细胞生物体中的选择性剪接模式的方法，一种用于有效识别影响哺乳动物多细胞中的选择性剪接的物质和基因区域的方法生物体等通过利用可变剪接报告系统。具体地，本发明涉及用于检测哺乳动物多细胞生物体中的选择性剪接的方法，以及用于鉴定影响哺乳动物多细胞生物体中的选择性剪接的物质和基因区域的方法，其使用DNA构建体，其中至少两个不同的报道子将基因插入到经历可选剪接的特定基因中，或将DNA构建体报告基因插入经历可选剪接的特定基因的DNA构建体（至少两种不同DNA构建体的组合）的组合中。

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