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1. 发明授权

US08466290B2 STAT3 inhibitor containing quinolinecarboxamide derivative as active ingredient 有权
标题翻译：含有喹啉甲酰胺衍生物的STAT3抑制剂作为活性成分
公开(公告)号：US08466290B2
公开(公告)日：2013-06-18
申请号：US13003441
申请日：2009-07-10
申请人： Akira Asai , Kenji Matsuno , Naohisa Ogo , Takane Yokotagawa , Osamu Takahashi , Yasuto Akiyama , Tadashi Ashizawa , Tadashi Okawara
发明人： Akira Asai , Kenji Matsuno , Naohisa Ogo , Takane Yokotagawa , Osamu Takahashi , Yasuto Akiyama , Tadashi Ashizawa , Tadashi Okawara
IPC分类号： C07D215/38
CPC分类号： C07D401/12 , A61K31/4709 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： The present invention provides a STATS inhibitor containing as an active ingredient, a quinolinecarboxamide derivative represented by the formula (I) (in the formula, W represents a bond or an alkylene chain; X represents O, S, or NR34; and R1 to R8 and R34 each represent H, halogen, alkyl, phenyl, furyl, thienyl, or the like), or a pharmacologically acceptable salt thereof.
摘要翻译：本发明提供含有作为活性成分的式（I）所示的喹啉甲酰胺衍生物的STATS抑制剂（式中，W表示键或亚烷基链; X表示O，S或NR34; R1〜R8 和R 34各自表示H，卤素，烷基，苯基，呋喃基，噻吩基等）或其药理学上可接受的盐。

2. 发明申请

US20120302524A1 1,3,4-OXADIAZOLE-2-CARBOXAMIDE COMPOUND 有权
标题翻译： 1,3,4-氧杂氮杂-2-羧酰胺化合物
公开(公告)号：US20120302524A1
公开(公告)日：2012-11-29
申请号：US13519707
申请日：2010-12-28
申请人： Akira Asai , Kenji Matsuno , Naohisa Ogo , Osamu Takahashi , Yoshiaki Masuda , Ayumu Muroya , Yasuto Akiyama , Tadashi Ashizawa , Tadashi Okawara
发明人： Akira Asai , Kenji Matsuno , Naohisa Ogo , Osamu Takahashi , Yoshiaki Masuda , Ayumu Muroya , Yasuto Akiyama , Tadashi Ashizawa , Tadashi Okawara
IPC分类号： A61K31/4245 , C07D413/14 , A61K31/4439 , C07F7/10 , A61K31/695 , A61K31/454 , A61K31/5377 , A61K31/496 , A61K31/4709 , A61K31/498 , C07D513/04 , A61K31/4545 , A61K31/541 , A61K31/437 , C07D487/04 , A61K31/55 , A61P35/00 , C07D413/04
CPC分类号： C07D413/04 , C07D413/14 , C07D417/14 , C07D487/04 , C07D498/04 , C07D513/04
摘要： Provided is a 1,3,4-oxadiazole-2-carboxamide compound which has STAT3 inhibitory activity and is useful as an anticancer agent. Provided is a 1,3,4-oxadiazole-2-carboxamide compound represented by formula (I) or a pharmacologically acceptable salt thereof (in the formula, Ar represents a furyl group or the like; R1 represents a hydrogen atom or the like; and —X—Y represents a diaryl group such as a biphenyl group).
摘要翻译：提供具有STAT3抑制活性并可用作抗癌剂的1,3,4-恶二唑-2-甲酰胺化合物。提供由式（I）表示的1,3,4-恶二唑-2-甲酰胺化合物或其药学上可接受的盐（在该式中，Ar表示呋喃基等; R 1表示氢原子等; -X-Y表示二苯基等二芳基）。

3. 发明申请

US20110172429A1 STAT3 INHIBITOR CONTAINING QUINOLINECARBOXAMIDE DERIVATIVE AS ACTIVE INGREDIENT 有权
标题翻译：含有喹啉甲酰胺衍生物的STAT3抑制剂作为活性成分
公开(公告)号：US20110172429A1
公开(公告)日：2011-07-14
申请号：US13003441
申请日：2009-07-10
申请人： Akira Asai , Kenji Matsuno , Naohisa Ogo , Takane Yokotagawa , Osamu Takahashi , Yasuto Akiyama , Tadashi Ashizawa , Tadashi Okawara
发明人： Akira Asai , Kenji Matsuno , Naohisa Ogo , Takane Yokotagawa , Osamu Takahashi , Yasuto Akiyama , Tadashi Ashizawa , Tadashi Okawara
IPC分类号： C07D215/14
CPC分类号： C07D401/12 , A61K31/4709 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： The present invention provides a STATS inhibitor containing as an active ingredient, a quinolinecarboxamide derivative represented by the formula (I) (in the formula, W represents a bond or an alkylene chain; X represents O, S, or NR34; and R1 to R8 and R34 each represent H, halogen, alkyl, phenyl, furyl, thienyl, or the like.), or a pharmacologically acceptable salt thereof.
摘要翻译：本发明提供含有作为活性成分的式（I）所示的喹啉甲酰胺衍生物的STATS抑制剂（式中，W表示键或亚烷基链; X表示O，S或NR34; R1〜R8 和R 34各自表示H，卤素，烷基，苯基，呋喃基，噻吩基等）或其药理学上可接受的盐。

4. 发明授权

US08796320B2 1,3,4-Oxadiazole-2-carboxamide compound 有权
标题翻译： 1,3,4-恶二唑-2-甲酰胺化合物
公开(公告)号：US08796320B2
公开(公告)日：2014-08-05
申请号：US13519707
申请日：2010-12-28
申请人： Akira Asai , Kenji Matsuno , Naohisa Ogo , Osamu Takahashi , Yoshiaki Masuda , Ayumu Muroya , Yasuto Akiyama , Tadashi Ashizawa , Tadashi Okawara
发明人： Akira Asai , Kenji Matsuno , Naohisa Ogo , Osamu Takahashi , Yoshiaki Masuda , Ayumu Muroya , Yasuto Akiyama , Tadashi Ashizawa , Tadashi Okawara
IPC分类号： A61K31/4245 , C07D271/10 , C07D413/14
CPC分类号： C07D413/04 , C07D413/14 , C07D417/14 , C07D487/04 , C07D498/04 , C07D513/04
摘要： Provided is a 1,3,4-oxadiazole-2-carboxamide compound which has STAT3 inhibitory activity and is useful as an anticancer agent. Provided is a 1,3,4-oxadiazole-2-carboxamide compound represented by formula (I) or a pharmacologically acceptable salt thereof (in the formula, Ar represents a furyl group or the like; R1 represents a hydrogen atom or the like; and —X—Y represents a diaryl group such as a biphenyl group).
摘要翻译：提供具有STAT3抑制活性并可用作抗癌剂的1,3,4-恶二唑-2-甲酰胺化合物。提供由式（I）表示的1,3,4-恶二唑-2-甲酰胺化合物或其药学上可接受的盐（在该式中，Ar表示呋喃基等; R 1表示氢原子等; -X-Y表示二苯基等二芳基）。

5. 发明申请

US20110091896A1 METHOD FOR ANALYSIS/IDENTIFICATION OF ANTIBODY GENE AT ONE-CELL LEVEL 审中-公开
标题翻译：用于单细胞水平分析/鉴定抗体基因的方法
公开(公告)号：US20110091896A1
公开(公告)日：2011-04-21
申请号：US12995404
申请日：2009-06-04
申请人： Yasuto Akiyama
发明人： Yasuto Akiyama
IPC分类号： C12Q1/68 , C12P21/00 , C12P19/34
CPC分类号： G01N33/56972 , G01N33/6854
摘要： Disclosed are: a method for identifying/analyzing a gene for an antibody in one cell derived from a human; a technique for producing an antibody derived from an identified one B cell; and others. A gene for an antibody specific to a melanoma antigen is analyzed/identified at a one-cell level by using an immortalized B cell produced from peripheral blood monocytes from a melanoma patient or a primary B cell included in the peripheral blood monocytes. It is found that B cells capable of producing a specific antibody can be separated on one cell by one cell basis by staining the B cells with a GST-labeled melanoma-specific cancer antigen MAGE1, an Alexa-labeled anti-GST antibody and a PE-labeled anti-human IgG antibody and carrying out the single cell sorting of the stained B cells. Further, a practical technique for extracting total RNA from the separated one B cell and cloning a gene for a specific antibody into the total RNA efficiently can be established.
摘要翻译：公开了一种用于鉴定/分析来源于人的一种细胞中的抗体基因的方法; 用于产生源自鉴定的一个B细胞的抗体的技术; 和别的。通过使用由来自黑素瘤患者或包含在外周血单核细胞中的原代B细胞的外周血单核细胞产生的永生化B细胞，在单细胞水平分析/鉴定用于黑素瘤抗原特异性抗体的基因。发现能够产生特异性抗体的B细胞可以通过用GST标记的黑素瘤特异性癌抗原MAGE1，Alexa标记的抗GST抗体和PE染色B细胞，在一个细胞上通过一个细胞分离标记的抗人IgG抗体，并进行染色的B细胞的单细胞分选。此外，可以建立从分离的一个B细胞中提取总RNA并将特异性抗体的基因有效克隆到总RNA中的实用技术。

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