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1.发明授权Method for controlling SR protein phosphorylation, and antiviral agents whose active ingredients comprise agents that control SR protein activity 有权用于控制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
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。
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2.发明授权Methods for controlling SR protein phosphorylation, and antiviral agents whose active ingredients comprise agents that control SR protein activity 有权用于控制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
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。
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3.发明申请METHODS FOR CONTROLLING SR PROTEIN PHOSPHORYLATION, AND ANTIVIRAL AGENTS WHOSE ACTIVE INGREDIENTS COMPRISE AGENTS THAT CONTROL SR PROTEIN ACTIVITY 有权用于控制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
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。
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4.发明申请METHODS FOR CONTROLLING SR PROTEIN PHOSPHORYLATION, AND ANTIVIRAL AGENTS WHOSE ACTIVE INGREDIENTS COMPRISE AGENTS THAT CONTROL SR PROTEIN ACTIVITY 有权用于控制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
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。
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5.发明申请Method for controlling sr protein phosphorylation, and antiviral agents whose active ingredients comprise agents that control sr protein activity 有权用于控制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
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。
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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。
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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。
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8.发明申请Method of Rapid Methylation of Alkene Compound and Kit for PET Tracer Preparation Using the Same 失效用于使用其的PET示踪剂制备的烯化合物和试剂盒的快速甲基化方法公开(公告)号：US20090238759A1
公开(公告)日：2009-09-24
申请号：US12090642
申请日：2006-10-06
申请人： Masaaki Suzuki , Takamitsu Hosoya
发明人： Masaaki Suzuki , Takamitsu Hosoya
IPC分类号： A61K51/04 , C07C67/30 , C07C1/00 , A61K101/02
CPC分类号： C07C45/673 , C07B59/00 , C07B2200/05 , C07C1/325 , C07C29/32 , C07C67/343 , C07C2531/24 , C07C47/21 , C07C49/603 , C07C69/587 , C07C33/03
摘要： To provide a method of rapid methylation of alkenes, which is applicable to the preparation of a PET tracer and which enables alkenes to be methylated through cross coupling between SP2 (alkenyl) and SP3 (alkyl) carbon atoms rapidly and in a high yield. Methyl iodide and an alkenyltrialkylstannane are subjected to cross coupling in an aprotic polar solvent in the presence of a palladium complex having a valence of 0, a phosphine ligand, a cuprous halide, and a carbonate and/or alkali metal fluoride.
摘要翻译： 提供烯烃快速甲基化的方法，其适用于制备PET示踪剂，并且通过SP2（烯基）和SP3（烷基）碳原子之间的快速和高收率的交叉偶联使烯烃能甲基化。 甲基碘和烯基三烷基锡烷在非质子极性溶剂中，在化合价为0的钯络合物，膦配位体，卤化亚铜和碳酸盐和/或碱金属氟化物的存在下进行交联。
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公开(公告)号：US20120230914A1
公开(公告)日：2012-09-13
申请号：US13381078
申请日：2010-07-05
申请人： Yasuyoshi Watanabe , Hirotaka Onoe , Kayo Takahashi , Masaaki Suzuki , Hisashi Doi , Takamitsu Hosoya
发明人： Yasuyoshi Watanabe , Hirotaka Onoe , Kayo Takahashi , Masaaki Suzuki , Hisashi Doi , Takamitsu Hosoya
IPC分类号： A61K49/00 , A61K51/04 , C07F7/22 , C07D249/14 , C07F5/05
CPC分类号： C07D249/08 , A61K51/0453 , C07B2200/05
摘要： A labeling compound of the present invention includes a structure represented by formula (1) wherein X1 is 11CH3, CH218F, CF218F, 18F, 76Br or 124I, X2 is CN or NO2, and R is any one of groups represented by or a structure represented by formula (2) wherein X3 is CH3, CH2F, CF3, F, Br or I, and R is defined equally as in the formula (1). This allows realizing a labeling compound for PET, capable of quantifying aromatase with high accuracy.
摘要翻译： 本发明的标记化合物包括由式（1）表示的结构，其中X1为11CH3，CH218F，CF218F，18F，76Br或124I，X2为CN或NO2，R为由 通式（2）其中X 3是CH 3，CH 2 F，CF 3，F，Br或I，R与式（1）同样地定义。 这允许实现PET的标记化合物，能够以高精度定量芳香化酶。
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10.发明授权Method of rapid methylation of alkene compound and kit for PET tracer preparation using the same 失效烯烃化合物的快速甲基化方法和使用其的PET示踪剂制备试剂盒公开(公告)号：US08067631B2
公开(公告)日：2011-11-29
申请号：US12090642
申请日：2006-10-06
申请人： Masaaki Suzuki , Takamitsu Hosoya
发明人： Masaaki Suzuki , Takamitsu Hosoya
CPC分类号： C07C45/673 , C07B59/00 , C07B2200/05 , C07C1/325 , C07C29/32 , C07C67/343 , C07C2531/24 , C07C47/21 , C07C49/603 , C07C69/587 , C07C33/03
摘要： To provide a method of rapid methylation of alkenes, which is applicable to the preparation of a PET tracer and which enables alkenes to be methylated through cross coupling between SP2 (alkenyl) and SP3 (alkyl) carbon atoms rapidly and in a high yield. Methyl iodide and an alkenyltrialkylstannane are subjected to cross coupling in an aprotic polar solvent in the presence of a palladium complex having a valence of 0, a phosphine ligand, a cuprous halide, and a carbonate and/or alkali metal fluoride.
摘要翻译： 提供烯烃快速甲基化的方法，其适用于制备PET示踪剂，并且通过SP2（烯基）和SP3（烷基）碳原子之间的快速和高收率的交叉偶联使烯烃能甲基化。 甲基碘和烯基三烷基锡烷在非质子极性溶剂中，在化合价为0的钯络合物，膦配位体，卤化亚铜和碳酸盐和/或碱金属氟化物的存在下进行交联。
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