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1. 发明申请

US20090239916A1 NOVEL DRUG DISCOVERY TARGET AND MEDICINE ACTING ON THE SAME 审中-公开
标题翻译：新药发现目标与药物相同
公开(公告)号：US20090239916A1
公开(公告)日：2009-09-24
申请号：US11569555
申请日：2005-05-26
申请人： Akito Tanaka , Akira Yamazaki , Akinobu Nakanishi , Mikio Takeuchi , Masayuki Haramura
发明人： Akito Tanaka , Akira Yamazaki , Akinobu Nakanishi , Mikio Takeuchi , Masayuki Haramura
IPC分类号： A61K31/428 , G01N33/53 , C12N9/04 , G01N33/68 , C07D311/22 , C07D277/68 , A61K31/352 , A61P29/00
CPC分类号： G01N33/6893 , A61K31/352 , A61K31/428 , C07D277/68 , C07D311/24 , G01N2500/00 , G01N2800/24
摘要： The present invention provides a pharmaceutical composition comprising as an active ingredient a compound that specifically binds to MFP-2 or a functional fragment thereof and a screening method for the compound; the compound and a pharmaceutical composition comprising the same are highly useful as anti-inflammatory agents and anti-allergic agents.
摘要翻译：本发明提供一种药物组合物，其包含与MFP-2或其功能片段特异性结合的化合物作为活性成分和该化合物的筛选方法; 该化合物和包含该化合物的药物组合物作为抗炎剂和抗过敏剂是非常有用的。

2. 发明申请

US20080176341A1 Method for Suppressing Intermolecular Nonspecific Interaction and for Intensifying Intermolecular Specific Interaction on Metal Surface 审中-公开
标题翻译：抑制分子间非特异性相互作用和加强金属表面分子间特异性相互作用的方法
公开(公告)号：US20080176341A1
公开(公告)日：2008-07-24
申请号：US11573868
申请日：2004-08-19
申请人： Akito Tanaka , Tomohiro Terada , Tsuruki Tamura , Takaaki Shiyama , Akira Yamazaki , Minoru Furuya , Masayuki Haramura
发明人： Akito Tanaka , Tomohiro Terada , Tsuruki Tamura , Takaaki Shiyama , Akira Yamazaki , Minoru Furuya , Masayuki Haramura
IPC分类号： G01N33/553
CPC分类号： G01N33/54393 , G01N33/553
摘要： The present invention provides a method of searching for a target molecule for a ligand immobilized on a metal surface or analyzing the interaction between a ligand and a target molecule, characterized in that the immobilization of the ligand on the metal surface via a hydrophilic spacers, and the method eliminates or suppresses a nonspecific interaction that prevents analysis of intermolecular interaction on a metal surface, and can intensify specific intermolecular interactions.
摘要翻译：本发明提供了一种搜索用于固定在金属表面上的配体的目标分子或分析配体和靶分子之间的相互作用的方法，其特征在于通过亲水间隔物将配体固定在金属表面上，以及该方法消除或抑制非特异性相互作用，其阻止金属表面上分子间相互作用的分析，并且可以加强特定的分子间相互作用。

3. 发明申请

US20090042318A1 METHOD FOR EFFECTIVE SEARCH FOR TARGET MOLECULE 审中-公开
标题翻译：有效搜索目标分子的方法
公开(公告)号：US20090042318A1
公开(公告)日：2009-02-12
申请号：US11814986
申请日：2006-01-26
申请人： Akito Tanaka , Akira Yamazaki , Masayuki Haramura
发明人： Akito Tanaka , Akira Yamazaki , Masayuki Haramura
IPC分类号： G01N33/545
CPC分类号： G01N33/54393 , B01J20/3227 , B01J20/3248 , B01J20/3253 , B01J20/3255 , B01J20/3285 , G01N33/54306
摘要： The present invention provides a solid phase carrier capable of adsorbing a highly hydrophobic target molecule, for example, a membrane associated protein, and a solid phase carrier optimized not only for a highly hydrophobic target molecule, but also for an optionally chosen target molecule. More specifically, the present invention provides a solid phase carrier having a ligand and a capping agent immobilized thereon, with the hydrophobic property of the surface thereof adjusted to enable the binding of the target molecule to the ligand, or to increase the amount of target molecule bound to the ligand; various methods using the solid phase carrier (for example, method of concentrating, isolating, or purifying a target molecule, a method of selectively adsorbing a particular target molecule to the solid phase carrier, or a method of analyzing the interaction between ligand and target molecule therefor); a production method for the solid phase carrier; and an improvement method for a solid phase carrier having a ligand and a capping agent immobilized thereon and the like.
摘要翻译：本发明提供了能够吸附高度疏水的靶分子例如膜相关蛋白的固相载体，以及不仅对于高度疏水的靶分子而且优选任选地选择的靶分子优化的固相载体。更具体地说，本发明提供一种具有固定在其上的配体和封端剂的固相载体，其表面的疏水性被调节以使靶分子与配体结合，或增加靶分子的量与配体结合; 使用固相载体的各种方法（例如，浓缩，分离或纯化靶分子的方法，将特定靶分子选择性吸附到固相载体上的方法或分析配体与靶分子之间的相互作用的方法为此）一种固相载体的制备方法; 以及其上固定有配体和封端剂等的固相载体的改进方法。

4. 发明申请

US20070082955A1 Novel target protein of anticancer agent and novel anticancer agent (spnal) corresponding thereto 失效
标题翻译：抗癌剂的新型靶蛋白和与其对应的新型抗癌剂（spnal）
公开(公告)号：US20070082955A1
公开(公告)日：2007-04-12
申请号：US10573166
申请日：2004-11-30
申请人： Akito Tanaka , Akira Yamazaki , Takeshi Tsutsumi , Tomohiro Terada , Masayuki Haramura
发明人： Akito Tanaka , Akira Yamazaki , Takeshi Tsutsumi , Tomohiro Terada , Masayuki Haramura
IPC分类号： A61K31/192 , C07C321/24 , G01N33/53
CPC分类号： C07D231/12 , A61K45/06 , C07C317/44 , C07C323/62
摘要： The present invention provides a pharmaceutical composition containing, as an active ingredient, a compound that specifically binds to KSRP or a functional fragment thereof, and a screening method for the compound. KSRP is a novel target protein for anticancer agents; a compound capable of regulating the expression and activity of such a protein and a pharmaceutical composition containing it are highly useful for proliferative diseases, particularly as anticancer agents. By providing the novel target protein, the mechanism behind the anticancer effect that has conventionally been unexplainable can be elucidated.
摘要翻译：本发明提供含有与KSRP或其功能片段特异性结合的化合物作为活性成分的药物组合物和该化合物的筛选方法。 KSRP是抗癌剂的新型靶蛋白; 能够调节这种蛋白质的表达和活性的化合物和含有该蛋白质的药物组合物对于增殖性疾病，特别是作为抗癌剂是非常有用的。通过提供新的靶蛋白，可以阐明通常不可解释的抗癌作用背后的机制。

5. 发明授权

US07456022B2 Solid support having ligand immobilized thereon by using photocleavable linker 有权
标题翻译：通过使用可光致发光的接头，其上固定有配体的固体支持物
公开(公告)号：US07456022B2
公开(公告)日：2008-11-25
申请号：US11572972
申请日：2005-07-28
申请人： Masayuki Haramura , Akito Tanaka
发明人： Masayuki Haramura , Akito Tanaka
IPC分类号： B01J20/26 , G01N33/547
CPC分类号： B01J20/289 , B01J20/261 , B01J20/286 , B01J20/321 , B01J20/3219 , B01J20/3251 , B01J20/3253 , B01J20/3255 , B01J2220/54 , G01N33/54353 , Y10T436/207497
摘要： The present invention provides a method of analyzing the interaction between a ligand and a target molecule, which uses a solid support wherein the ligand is immobilized via a linker cleavable by photoirradiation, particularly a method of searching and purifying a target molecule. By intervening a linker specifically cleavable by photoirradiation between the ligand molecule and the solid support, release and elution of the target molecule from the solid support without using a ligand or salt at a high concentration can be enabled, and suppression of release and elution of a nonspecific protein can be enabled.
摘要翻译：本发明提供了一种分析配体和靶分子之间的相互作用的方法，其使用固体支持物，其中通过光照射可切割的接头固定配体，特别是搜索和纯化靶分子的方法。通过插入通过配体分子和固体支持体之间的光照射可以特异性地切割的接头，可以使得目标分子从固体支持物中释放和洗脱而不使用高浓度的配体或盐，并且抑制释放和洗脱可以启用非特异性蛋白质。

6. 发明申请

US20110189789A1 NOVEL TARGET PROTEIN OF ANTICANCER AGENT AND NOVEL ANTICANCER AGENT (SPNAL) CORRESPONDING THERETO 审中-公开
标题翻译：新药抗体药剂和新型抗感染药物（SPNAL）相关药物的新目标蛋白
公开(公告)号：US20110189789A1
公开(公告)日：2011-08-04
申请号：US12632905
申请日：2009-12-08
申请人： Akito Tanaka , Akira Yamazaki , Takeshi Tsutsumi , Tomohiro Terada , Masayuki Haramura
发明人： Akito Tanaka , Akira Yamazaki , Takeshi Tsutsumi , Tomohiro Terada , Masayuki Haramura
IPC分类号： G01N33/53
CPC分类号： C07D231/12 , A61K45/06 , C07C317/44 , C07C323/62
摘要： The present invention provides a pharmaceutical composition containing, as an active ingredient, a compound that specifically binds to KSRP or a functional fragment thereof, and a screening method for the compound. KSRP is a novel target protein for anticancer agents; a compound capable of regulating the expression and activity of such a protein and a pharmaceutical composition containing it are highly useful for proliferative diseases, particularly as anticancer agents. By providing the novel target protein, the mechanism behind the anticancer effect that has conventionally been unexplainable can be elucidated.
摘要翻译：本发明提供含有与KSRP或其功能片段特异性结合的化合物作为活性成分的药物组合物和该化合物的筛选方法。 KSRP是抗癌剂的新型靶蛋白; 能够调节这种蛋白质的表达和活性的化合物和含有该蛋白质的药物组合物对于增殖性疾病，特别是作为抗癌剂是非常有用的。通过提供新的靶蛋白，可以阐明通常不可解释的抗癌作用背后的机制。

7. 发明申请

US20100094026A1 METHOD OF SCREENING COMPOUND USEFUL IN TREATING ALLERGIC DISEASE 审中-公开
标题翻译：筛选化合物可用于治疗过敏性疾病的方法
公开(公告)号：US20100094026A1
公开(公告)日：2010-04-15
申请号：US12092208
申请日：2006-08-11
申请人： Akito Tanaka , Akinobu Nakanishi , Masayuki Haramura , Mikio Takeuchi
发明人： Akito Tanaka , Akinobu Nakanishi , Masayuki Haramura , Mikio Takeuchi
IPC分类号： A61K31/35 , C07D407/12 , G01N33/566
CPC分类号： G01N33/6893 , G01N2500/00 , G01N2800/24
摘要： The present invention provides a method of screening for a compound useful for treatment of an allergic disease by identifying a molecule targeted by Intal upon exertion of its efficacy as an anti-allergic agent (hereinafter referred as a target) and using the target, as well as a new type of anti-allergic agent comprising a compound obtainable by the screening as an active ingredient for treatment of an allergic disease.
摘要翻译：本发明提供一种筛选用于治疗过敏性疾病的化合物的方法，其通过鉴定作为抗过敏剂（以下称为靶标）的功效的Intal作为靶标的分子，以及使用该靶标作为新型的抗过敏剂，其包含通过筛选获得的化合物作为治疗过敏性疾病的活性成分。

8. 发明授权

US07001887B2 Peptide derivatives 失效
标题翻译：肽衍生物
公开(公告)号：US07001887B2
公开(公告)日：2006-02-21
申请号：US10470801
申请日：2002-02-04
申请人： Takuya Shiraishi , Shojiro Kadono , Masayuki Haramura , Haruhiko Sato , Toshiro Kozono , Takaki Koga , Akihisa Sakamoto
发明人： Takuya Shiraishi , Shojiro Kadono , Masayuki Haramura , Haruhiko Sato , Toshiro Kozono , Takaki Koga , Akihisa Sakamoto
IPC分类号： C07K5/06 , C07D213/02 , C07D235/04 , C07D239/86 , C07D401/04
CPC分类号： G06F19/16 , A61K38/00 , C07K5/06078 , C07K5/06139 , C07K5/06156 , G01N33/68
摘要： A compound of Formula (1): wherein R1 represents an amidinophenyl group, etc.; R2 represents a hydrogen atom, etc.; R3 represents a carbamoylalkyl group, etc.; R4 represents a hydrogen atom, etc.; R5 represents a benzyl group, etc.; R6 represents a hydrogen atom, etc.; and R7 represents an alkylsulfonyl group, etc. A crystal of a complex between factor VIIa/human soluble tissue factor and a low-molecular weight reversible factor VIIa inhibitor. A medium carrying a part or all of structure coordinate data of a complex between human factor VIIa/human soluble tissue factor and a low-molecular weight reversible factor VIIa inhibitor, obtainable by X-ray crystal structure analysis of the crystal. A method for computationally designing a low-molecular weight reversible factor VIIa inhibitor using the coordinate data.
摘要翻译：式的化合物

9. 发明授权

US07919653B2 Method of inhibiting nonspecific interaction between molecules on solid phase support 有权
标题翻译：抑制固相载体上分子之间非特异性相互作用的方法
公开(公告)号：US07919653B2
公开(公告)日：2011-04-05
申请号：US10522716
申请日：2003-07-30
申请人： Akito Tanaka , Tomohiro Terada , Tsuruki Tamura , Takaaki Shiyama , Akira Yamazaki , Minoru Furuya , Masayuki Haramura
发明人： Akito Tanaka , Tomohiro Terada , Tsuruki Tamura , Takaaki Shiyama , Akira Yamazaki , Minoru Furuya , Masayuki Haramura
IPC分类号： G01N33/53 , G01N37/00 , G01N33/543
CPC分类号： C08G65/33396 , G01N33/54393
摘要： The present invention provides a method of suppressing the nonspecific interaction between molecules, characterized in that in a process to immobilize a molecule onto a solid phase carrier and analyze the specific interaction between the molecule and a molecule that specifically interacts with the molecule on the solid phase, the hydrophobic property of the solid phase surface in the solid phase carrier is regulated, particularly a hydrophilic spacer is interlaid at the time of immobilization of the molecule onto the solid phase carrier, which method makes it possible to suppress the nonspecific interaction between the molecules, and to reduce nonspecific adsorption to the solid phase.
摘要翻译：本发明提供了抑制分子之间非特异性相互作用的方法，其特征在于在将分子固定在固相载体上并分析分子与与固相分子特异性相互作用的分子之间的特异性相互作用的方法调节固相载体中固相表面的疏水性，特别是在将分子固定在固相载体上时，亲水间隔物被嵌入，该方法可以抑制分子之间的非特异性相互作用，并减少对固相的非特异性吸附。

10. 发明授权

US07659426B2 Target protein of anticancer agent and novel anticancer agent (spnal) corresponding thereto 失效
标题翻译：抗癌剂的靶蛋白和与其对应的新型抗癌剂（spnal）
公开(公告)号：US07659426B2
公开(公告)日：2010-02-09
申请号：US10573166
申请日：2004-11-30
申请人： Akito Tanaka , Akira Yamazaki , Takeshi Tsutsumi , Tomohiro Terada , Masayuki Haramura
发明人： Akito Tanaka , Akira Yamazaki , Takeshi Tsutsumi , Tomohiro Terada , Masayuki Haramura
IPC分类号： A01N41/10
CPC分类号： C07D231/12 , A61K45/06 , C07C317/44 , C07C323/62
摘要： The present invention provides a pharmaceutical composition containing, as an active ingredient, a compound that specifically binds to KSRP or a functional fragment thereof, and a screening method for the compound. KSRP is a novel target protein for anticancer agents; a compound capable of regulating the expression and activity of such a protein and a pharmaceutical composition containing it are highly useful for proliferative diseases, particularly as anticancer agents. By providing the novel target protein, the mechanism behind the anticancer effect that has conventionally been unexplainable can be elucidated.
摘要翻译：本发明提供含有与KSRP或其功能片段特异性结合的化合物作为活性成分的药物组合物和该化合物的筛选方法。 KSRP是抗癌剂的新型靶蛋白; 能够调节这种蛋白质的表达和活性的化合物和含有该蛋白质的药物组合物对于增殖性疾病，特别是作为抗癌剂是非常有用的。通过提供新的靶蛋白，可以阐明通常不可解释的抗癌作用背后的机制。

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