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1. 发明专利

JP2014118379A Antimicrobial agent and therapeutic agent for infection disease composed of the same 审中-公开
标题翻译：用于感染疾病的抗微生物剂和治疗药物
公开(公告)号：JP2014118379A
公开(公告)日：2014-06-30
申请号：JP2012274145
申请日：2012-12-15
申请人： Univ Of Tokyo , 国立大学法人東京大学 , Genome Soyaku Kenkyusho:Kk , 株式会社ゲノム創薬研究所
发明人： SEKIMIZU KAZUHISA , HAMAMOTO HIROSHI , KATAOKA KEIKO
IPC分类号： A61K31/499 , A01N43/90 , A01P3/00 , A61P31/04
摘要： PROBLEM TO BE SOLVED: To provide antimicrobial agents comprising a novel chemical structure, and a therapeutic agent for infection disease which has good in vivo kinetics, especially in mammals, of the antimicrobial agents, and excellent therapeutic effect.SOLUTION: An antimicrobial agent is represented by formula (1), and a therapeutic agent for infection disease is composed of the antimicrobial agent.
摘要翻译：要解决的问题：提供包含新型化学结构的抗微生物剂和具有良好体内动力学特别是哺乳动物的感染性疾病的治疗剂，以及优异的治疗效果。解决方案：抗微生物剂被代表通过式（1），感染性疾病的治疗剂由抗菌剂构成。

2. 发明专利

JP2013180952A Novel compound and antimicrobial agent comprising the novel compound 有权
标题翻译：新化合物和包含新化合物的抗微生物剂
公开(公告)号：JP2013180952A
公开(公告)日：2013-09-12
申请号：JP2012043480
申请日：2012-02-29
申请人： Univ Of Tokyo , 国立大学法人東京大学 , Genome Soyaku Kenkyusho:Kk , 株式会社ゲノム創薬研究所
发明人： SEKIMIZU KAZUHISA , OWADA TOMOHIKO , HAMAMOTO HIROSHI
IPC分类号： C07D231/16 , A01N43/08 , A01N43/10 , A01N43/30 , A01N43/56 , A01N47/02 , A01P3/00 , A61K31/345 , A61K31/381 , A61K31/415 , A61P31/04 , C07D307/71 , C07D333/40 , C07D333/44 , C07D409/12
摘要： PROBLEM TO BE SOLVED: To provide: a novel compound having applicability to various applications; an antimicrobial agent comprising the novel compound; and further an infectious disease therapeutic agent in which body kinetics is excellent and therapeutic effect is excellent in the antimicrobial agent.SOLUTION: Compounds or the like are represented by formula (1), antimicrobial agents comprise these compounds, and infectious disease therapeutic agents are these compounds, and are such that a structure is limited in the formula (1). In the formula (1), Xto Xeach independently denote H, F, Cl, Br, a methyl group, a dimethylamino group or a trifluoromethoxy group, provided that n (n is 2, 3 or 4) in Xto Xdenotes H; Ydenotes H or a methyl group; and Xdenotes a nitro group or an aldehyde group.
摘要翻译：要解决的问题：提供：适用于各种应用的新型化合物; 包含该新化合物的抗微生物剂; 还有一种感染性疾病治疗剂，其中动力学优异，治疗效果优异的抗微生物剂。解决方案：化合物等由式（1）表示，抗微生物剂包含这些化合物，感染性疾病治疗剂是这些化合物，并且使得式（1）中的结构受到限制。在式（1）中，Xto Xeach独立地表示H，F，Cl，Br，甲基，二甲基氨基或三氟甲氧基，条件是X至X表示H中的n（n为2,3或4） Y表示H或甲基; X代表硝基或醛基。

3. 发明专利

JP2013145250A Toxicity testing method 审中-公开
标题翻译：毒性测试方法
公开(公告)号：JP2013145250A
公开(公告)日：2013-07-25
申请号：JP2013092830
申请日：2013-04-25
申请人： Genome Soyaku Kenkyusho:Kk , 株式会社ゲノム創薬研究所
发明人： SEKIMIZU KAZUHISA , HAMAMOTO HIROSHI
IPC分类号： G01N33/15 , G01N33/66
摘要： PROBLEM TO BE SOLVED: To provide a toxicity testing method capable of substituting an acute toxicity test to various medicines, food materials or the like by mammals having not only economic and troublesome problems but also many ethical problems with little financial and ethical problems and without reducing test significance.SOLUTION: The toxicity testing method is a method for evaluating acute toxicity of cytotoxicity to mammals for an object to be tested showing cytotoxicity to mammals, a toxicity testing method to be performed by measuring a metabolic state of the object to be tested in a silkworm with the object to be tested administered thereto, a method for estimating a metabolic state in a mammal of the object to be tested, and is a drub metabolism estimation method which uses a silkworm as an experimental animal for substituted for a mammal.
摘要翻译：要解决的问题：提供一种毒性测试方法，其能够通过不仅经济和麻烦的问题的哺乳动物代替急性毒性试验，而且还具有许多伦理问题，几乎没有经济和伦理问题，而且没有减少测试意义。解决方案：毒性测试方法是评估对哺乳动物细胞毒性的急性毒性的方法，显示对哺乳动物的细胞毒性，通过测量待测物体的代谢状态进行的毒性测试方法具有待测试对象的蚕，用于估计待测试对象的哺乳动物中的代谢状态的方法，并且是使用蚕作为替代哺乳动物的实验动物的排泄代谢估计方法。

4. 发明专利

JP2012005480A Antibiotic-producing microorganism and antibiotic produced by the same 有权
标题翻译：抗生素生产微生物及其生产的抗生素
公开(公告)号：JP2012005480A
公开(公告)日：2012-01-12
申请号：JP2011116486
申请日：2011-05-25
申请人： Genome Soyaku Kenkyusho:Kk , Univ Of Tokyo , 国立大学法人東京大学 , 株式会社ゲノム創薬研究所
发明人： SEKIMIZU KAZUHISA , HAMAMOTO HIROSHI , MURAKAMI KAZUHISA
IPC分类号： C12N1/20 , A61K35/74 , A61K38/00 , A61P31/04 , C07G11/00 , C07K7/50 , C12P1/04
摘要： PROBLEM TO BE SOLVED: To provide a new microorganism producible of an antibiotic; to provide a new microorganism to be used in a method for producing the antibiotic; and especially to provide a new microorganism producible of a new antibiotic effective against multidrug-resistant bacteria, showing effectiveness at least against both MRSA (methicillin-resistant Staphylococcus aureus) and VRE (vancomycin-resistant enterococci).SOLUTION: The microorganism is a microorganism having an accession number NITE P-870 belonging to a genus Lysobacter, or a naturally or artificially mutated microorganism thereof. The microorganism has a capacity of producing the antibiotic having antibacterial activity, and has a base sequence in a 16S rRNA region represented by the sequence number 1 in a sequence list.
摘要翻译：要解决的问题：提供可生产抗生素的新型微生物; 提供用于生产抗生素的方法中的新微生物; 特别是提供一种能够有效抗多种耐药性细菌的新型抗生素的新型微生物，至少对MRSA（耐甲氧西林金黄色葡萄球菌）和VRE（万古霉素耐药性肠球菌）均有效。解决方案：微生物是属于溶血杆菌属的登录号为NITE P-870的微生物或其天然或人工突变的微生物。微生物具有生产具有抗菌活性的抗生素的能力，并且在序列表中由序列号1表示的16S rRNA区域中具有碱基序列。版权所有（C）2012，JPO＆INPIT

5. 发明专利

JP2010145113A Method for determining internal kinetics, and method for preparing library of compound favorable in internal kinetics using the same 审中-公开
标题翻译：用于确定内部动力学的方法和使用该方法制备内部动力学中化合物的图书馆的方法
公开(公告)号：JP2010145113A
公开(公告)日：2010-07-01
申请号：JP2008319566
申请日：2008-12-16
申请人： Genome Soyaku Kenkyusho:Kk , Univ Of Tokyo , 国立大学法人東京大学 , 株式会社ゲノム創薬研究所
发明人： SEKIMIZU KAZUHISA , HAMAMOTO HIROSHI , ASAMI YUKIHIRO , OGATA YASUSHI
IPC分类号： G01N30/88 , C40B30/06 , G01N30/62 , G01N33/15 , G01N33/50
摘要： PROBLEM TO BE SOLVED: To provide a method which can efficiently determine a possibility of an inspection target as a drug from an aspect of internal kinetics in a mammal without requiring much labor in the searching study stage of the development of medicines or experiments with animals using the mammal, a method for preparing a compound library favorable in internal kinetics constituted of a compound afv in internal kinetics by the method of the determination, and the compound library.
SOLUTION: In the method for determining internal kinetics, the inspection target is administered to the larva of a holometabolous insect to evaluate the internal kinetics in the larva of the holometabolous insect of the compound in the inspection target or a substance formed by the internal chemical change of the compound in the inspection target of the larva and the quality of the internal kinetics of the compound in the inspection target or the substance formed by the internal chemical change of the compound in the inspection target in the mammal is determined from the evaluation result. In the method for preparing the compound library, the compound in the inspection target is selected using the method for determining internal kinetics to prepare the compound library using the compound in the inspection target as a constituent element.
COPYRIGHT: (C)2010,JPO&INPIT
摘要翻译：要解决的问题：提供一种能够从哺乳动物的内部动力学方面有效地确定作为药物的检查对象的可能性的方法，而不需要在开发药物或实验的研究阶段中花费太多劳动使用哺乳动物的动物，通过测定方法制备在内部动力学中由化合物组成的内部动力学有利的化合物文库的方法和化合物文库。解决方案：在确定内部动力学的方法中，将检查目标施用于全息虫的幼虫，以评估检查对象中化合物的全息变性昆虫的幼虫的内部动力学或由化合物在幼虫检查对象中的内部化学变化以及化合物在检查对象中的内部动力学质量或由哺乳动物检查对象中化合物的内部化学变化形成的物质的质量由评价结果。在制备化合物文库的方法中，使用确定内部动力学的方法选择检查对象中的化合物，以使用检查对象中的化合物作为构成要素制备化合物文库。版权所有（C）2010，JPO＆INPIT

6. 发明专利

JP2010133975A Method of screening compound having antimicrobial activity on pathogenic microorganism infecting organism having acquired immune mechanism by using larva of insect having only natural immune mechanism, and method of evaluating antimicrobial activity by using larva of insect having only natural immune mechanism 有权
标题翻译：通过使用仅具有自然免疫机制的病人的拉伐病毒对具有获得性免疫机制的致病微生物感染有机体的抗微生物活性的筛选化合物的方法，以及通过使用仅具有自然免疫机制的小鼠进行评估抗微生物活性的方法
公开(公告)号：JP2010133975A
公开(公告)日：2010-06-17
申请号：JP2010037402
申请日：2010-02-23
申请人： Genome Soyaku Kenkyusho:Kk , 株式会社ゲノム創薬研究所
发明人： SEKIMIZU KAZUHISA
IPC分类号： G01N33/50 , C12Q1/02 , G01N33/15 , G01N33/48
CPC分类号： G01N33/5085 , G01N2333/21 , G01N2333/305 , G01N2333/43578
摘要： PROBLEM TO BE SOLVED: To provide an effective model for developing antimicrobial agent for microbe infection in an organism having acquired immune mechanism, wherein the model of microbe infection using the organism having only natural immune mechanism.
SOLUTION: Whether the larva of a silkworm is useful or not as an antimicrobial agent evaluation system is investigated. It is found out that the larva of the silkworm is died by infection on the injection of Staphylococcus aureus or Pseudomonas aeruginosa to the larva of the silkworm. The effect of the antimicrobial agent for the larva of the silkworm is surprisingly agrees with the clinical efficacy of these agent on human i.e. an organism having acquired immune mechanism.
COPYRIGHT: (C)2010,JPO&INPIT
摘要翻译：要解决的问题：提供一种在具有获得性免疫机制的生物体中开发用于微生物感染的抗微生物剂的有效模型，其中使用仅具有天然免疫机制的生物体的微生物感染模型。
解决方案：研究蚕的幼虫是否用作抗微生物剂评价系统。发现蚕的幼虫在金黄色葡萄球菌或铜绿假单胞菌注射感染后死于蚕的幼虫。抗微生物剂对蚕幼虫的效果令人惊奇地与这些药剂对人类即具有获得性免疫机制的生物体的临床疗效一致。版权所有（C）2010，JPO＆INPIT

7. 发明专利

JP2009058500A Evaluating method, screening method, and manufacturing method of matter for lowering blood sugar level 有权
标题翻译：评估方法，筛选方法和制造方法降低血糖水平
公开(公告)号：JP2009058500A
公开(公告)日：2009-03-19
申请号：JP2008178397
申请日：2008-07-08
申请人： Genome Soyaku Kenkyusho:Kk , 株式会社ゲノム創薬研究所
发明人： SEKIMIZU KAZUHISA , HAMAMOTO HIROSHI , MATSUMOTO YASUHIKO , SUMITANI ERIKO , SUGITA TAKUYA
IPC分类号： G01N33/50 , A01K67/033 , A61K45/00 , A61P3/10 , G01N33/15 , G01N33/66
摘要： PROBLEM TO BE SOLVED: To provide cost-effective methods for accurately and excellently screening, evaluating and manufacturing diabetic curative drugs in which few ethical problems exist, additionally also cost-effective laboratory animals under specific condition to preferably be used in the above methods with few ethical problems.
SOLUTION: This is the method for evaluating as to whether a test substance is the matter which lowers human blood sugar level or not, characterized by comprising a process (a) to raise glucose (B) concentration in fat body or blood of a target invertebrate animal by allowing this invertebrate animal to ingest glucose (A), a process (b) to administer the above test substance to the target invertebrate animal with its glucose (B) concentration in fat body or blood increased which is obtained from the above process (a), and a process (c) to measure the glucose (B) concentration in fat body or blood of the invertebrate animal injected with the above test substance.
COPYRIGHT: (C)2009,JPO&INPIT
摘要翻译：要解决的问题：为了准确，优良地筛选，评估和制造出几乎不存在伦理问题的糖尿病治疗药物，提供具有成本效益的方法，另外还有在上述条件下优选使用特定条件下的具有成本效益的实验室动物少有伦理问题的方法。解决方案：这是评估测试物质是否是降低人血糖水平的问题的方法，其特征在于包括以下步骤：（a）提高脂肪体或血液中的葡萄糖（B）浓度通过允许该无脊椎动物摄入葡萄糖（A）的目标无脊椎动物，将上述测试物质施用于其在脂肪体或血液中的葡萄糖（B）浓度增加的目标无脊椎动物的方法（b），其从上述方法（a）和（c）测量注射上述试验物质的无脊椎动物的脂肪体或血液中的葡萄糖（B）浓度。版权所有（C）2009，JPO＆INPIT

8. 发明专利

JP2009047552A Toxicity testing method 有权
标题翻译：毒性测试方法
公开(公告)号：JP2009047552A
公开(公告)日：2009-03-05
申请号：JP2007214006
申请日：2007-08-20
申请人： Genome Soyaku Kenkyusho:Kk , 株式会社ゲノム創薬研究所
发明人： SEKIMIZU KAZUHISA , HAMAMOTO HIROSHI
IPC分类号： G01N33/15 , G01N33/48
摘要： PROBLEM TO BE SOLVED: To provide a toxicity testing method which enables the replacement of an acute toxicity test with respect to various drugs or food materials of a mammal having not only a problem of economical efficiency or labor but also a moral problem without bringing about a problem from an aspect of cost and morals and reducing the meaning of the test. SOLUTION: The toxicity testing method is a method for evaluating the acute toxicity of the mammal by an examination target showing cytotoxicity with respect to the mammal and performed by administering the examination target to the larva of a holometabolous insect to calculate the LD 50 value of the larva. Further, this toxicity testing method is performed by measuring the metabolic state of the examination target in the larva of the holometabolous insect to which the examination target is administered. COPYRIGHT: (C)2009,JPO&INPIT
摘要翻译：要解决的问题：提供一种毒性测试方法，其能够替代不仅具有经济效率或劳动问题的哺乳动物的各种药物或食物材料的急性毒性试验，而且没有从成本和道德方面带来问题，减少测试的意义。毒性试验方法是一种评价哺乳动物的急性毒性的方法，该检查对象表现出对哺乳动物的细胞毒性，并通过将检查对象施用于全息型昆虫的幼虫来计算LD 50 幼虫的价值。此外，该毒性试验方法是通过测定施用检查对象的全息型昆虫的幼虫中的检查对象的代谢状态进行的。版权所有（C）2009，JPO＆INPIT

9. 发明专利

JP2014217322A 固相レジンを用いた環状ペプチド化合物の製造方法审中-公开
标题翻译：使用固体相树脂的环状磷酸酯化合物的生产方法
公开(公告)号：JP2014217322A
公开(公告)日：2014-11-20
申请号：JP2013098834
申请日：2013-05-08
申请人：株式会社ゲノム創薬研究所 , Genome Soyaku Kenkyusho:Kk , 国立大学法人東京大学 , Univ Of Tokyo , 国立大学法人東京大学
发明人： SEKIMIZU KAZUHISA , INOUE MASAYUKI , KURANAGA TAKESHI
IPC分类号： C12P21/04
摘要：【課題】環状ペプチド化合物の全合成による製造方法の提供。【解決手段】特定構造の環状ペプチド化合物を、Wangレジン又はトリチルレジンからなる固相レジンを用いて溶媒中、固相レジンと1個の基が結合し、結合していない基は、それぞれ独立して酸と反応させることによりt−ブチル(t−Bu)基、t−ブチルジメチルシリル(TBS)基、t−ブチルオキシカルボニル(Boc)基、及びトリチル(Tr)基等を脱保護として、特定構造で表される環状ペプチド化合物誘導体を製造する方法。【選択図】なし
摘要翻译：要解决的问题：提供通过全合成环状肽化合物的制造方法。溶解性：在具有特定结构的环状肽化合物的制造方法中，使用由Wang树脂或三苯甲基树脂构成的固相树脂。在溶剂中，固相树脂和一个基团键合，非键合基团各自独立地与叔丁基（t-Bu）基团的酸，叔丁基二甲基甲硅烷基（TBS）基团，叔丁氧羰基（Boc ）组，三苯甲基（Tr）基团等作为脱保护基。

10. 发明专利

JP2012249567A Method for identifying target protein of antimicrobial agent based on analysis of drug-resistant and temperature-sensitive mutant strain 有权
标题翻译：基于耐药和温敏敏感菌株分析鉴定抗微生物剂目标蛋白的方法
公开(公告)号：JP2012249567A
公开(公告)日：2012-12-20
申请号：JP2011124011
申请日：2011-06-02
申请人： Genome Soyaku Kenkyusho:Kk , 株式会社ゲノム創薬研究所 , Univ Of Tokyo , 国立大学法人東京大学
发明人： SEKIMIZU KAZUHISA , HAMAMOTO HIROSHI , MATSUMOTO YASUHIKO
IPC分类号： C12Q1/68 , A61K45/00 , A61P31/04 , C12N15/09 , C12Q1/02 , G01N33/15 , G01N33/50 , G01N33/68
摘要： PROBLEM TO BE SOLVED: To provide a method for identifying a target protein of "antimicrobial agent" such as an antibiotic, and a method of identifying a base substitution causing a drug resistance to be obtained.SOLUTION: The method for identifying the target protein of the antimicrobial agent includes: isolating a temperature-sensitive mutant strain from among drug-resistant mutant strains against the agent; identifying the protein into which an amino acid mutation in the temperature-sensitive mutant is introduced; and identifying a protein before the amino acid mutation is introduced, as the target protein of the antimicrobial agent.

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