公开(公告)号：US20070161604A1

公开(公告)日：2007-07-12

申请号：US10584283

申请日：2004-12-22

申请人： Akio Hayashi ,  Shinji Nakade ,  Hidehiro Suzuki

发明人： Akio Hayashi ,  Shinji Nakade ,  Hidehiro Suzuki

IPC分类号： A61K31/665 ,  G01N33/53 ,  C07F9/02 ,  C07F9/28 ,  C07K16/18

CPC分类号： A61K31/665 ,  A61K45/06 ,  C07F9/10 ,  C07F9/65742 ,  C07K16/18 ,  G01N33/92 ,  G01N2500/00 ,  A61K2300/00

摘要： There is provided a method of screening a preventive and/or therapeutic substance for diseases in which LPA takes part, characterized in that a compound represented by any of formula (I), (II) and (III): [wherein the meaning of characters are described in the description] is used. The compounds obtained by the screening method or the screening kit of the present invention, their salts, their solvates and prodrugs thereof would modulate the binding of highly active LPA with LPA receptor in human and other mammals, so that they can be used as a preventive and/or therapeutic agent for diseases in which LPA takes part, for example, urinary diseases, central nervous diseases, inflammatory diseases, circulatory diseases, cancer, diabetes, immune system disorders and alimentary diseases.

摘要翻译： 提供了一种筛选LPA参与的疾病的预防和/或治疗物质的方法，其特征在于由式（I），（II）和（III）中任何一种表示的化合物：[其中字符的含义 在描述中被描述]被使用。 通过本发明的筛选方法或筛选试剂盒获得的化合物，它们的盐，它们的溶剂合物和前体药物将调节人和其它哺乳动物中高活性LPA与LPA受体的结合，从而可以将其用作预防 和/或其中LPA参与的疾病的治疗剂，例如尿病，中枢神经疾病，炎性疾病，循环系统疾病，癌症，糖尿病，免疫系统疾病和消化性疾病。

公开(公告)号：US07700792B2

公开(公告)日：2010-04-20

申请号：US10584283

申请日：2004-12-22

申请人： Akio Hayashi ,  Shinji Nakade ,  Hidehiro Suzuki

发明人： Akio Hayashi ,  Shinji Nakade ,  Hidehiro Suzuki

IPC分类号： C07F9/02

CPC分类号： A61K31/665 ,  A61K45/06 ,  C07F9/10 ,  C07F9/65742 ,  C07K16/18 ,  G01N33/92 ,  G01N2500/00 ,  A61K2300/00

摘要： To provide a highly active LPA and a method of screening therewith.There is provided a method of screening a preventive and/or therapeutic substance for diseases in which LPA takes part, characterized in that a compound represented by any of formula (I), (II) and (III): [wherein the meaning of characters are described in the description] is used. The compounds obtained by the screening method or the screening kit of the present invention, their salts, their solvates and prodrugs thereof would modulate the binding of highly active LPA with LPA receptor in human and other mammals, so that they can be used as a preventive and/or therapeutic agent for diseases in which LPA takes part, for example, urinary diseases, central nervous diseases, inflammatory diseases, circulatory diseases, cancer, diabetes, immune system disorders and alimentary diseases.

摘要翻译： 提供高活性LPA及其筛选方法。 提供了一种筛选LPA参与的疾病的预防和/或治疗物质的方法，其特征在于由式（I），（II）和（III）中任何一种表示的化合物：[其中字符的含义 在描述中被描述]被使用。 通过本发明的筛选方法或筛选试剂盒获得的化合物，它们的盐，它们的溶剂合物和前体药物将调节人和其它哺乳动物中高活性LPA与LPA受体的结合，从而可以将其用作预防 和/或其中LPA参与的疾病的治疗剂，例如尿病，中枢神经疾病，炎性疾病，循环系统疾病，癌症，糖尿病，免疫系统疾病和消化性疾病。

公开(公告)号：US08269035B2

公开(公告)日：2012-09-18

申请号：US12747726

申请日：2008-12-16

申请人： Fumie Kurosaki ,  Masahito Toyama ,  Akio Hayashi

发明人： Fumie Kurosaki ,  Masahito Toyama ,  Akio Hayashi

IPC分类号： C07C69/74

CPC分类号： C07B59/00 ,  C07B59/001 ,  C07B2200/05 ,  C07C269/06 ,  C07C2601/04 ,  Y02P20/55 ,  C07C271/24

摘要： A process for production of a radioactive fluorine-labeled organic compound is provided which can improve the yield of radioactive fluorination. Provided is a process in which a compound represented by the following formula (1): (wherein R1 is a straight or branched alkyl chain with 1-10 carbon atoms or an aromatic substituent, R2 is a straight or branched haloalkylsulfonic acid substituent with 1-10 carbon atoms, a straight or branched alkylsulfonic acid substituent with 1-10 carbon atoms, a fluorosulfonic acid substituent or an aromatic sulfonic acid substituent, and R3 is a protective group) is heated under stirring in an inert organic solvent in a presence of a phase transfer catalyst, 18F ions and potassium ions, so as to effect labeling with a radioactive fluorine, wherein the heating temperature is 40-90° C., and the concentration of the phase transfer catalyst in the inert organic solvent is 70 mmol/L or more. Preferably, the molar ratio of the phase transfer catalyst is 0.7 or more relative to the compound of the formula (1), and the concentration of the compound of the formula (1) in the inert organic solvent is 50 mmol/L or more.

摘要翻译： 提供了可以提高放射性氟化产率的放射性氟标记的有机化合物的制造方法。 本发明提供下述式（1）表示的化合物：其中，R 1为碳原子数为1〜10的直链或支链烷基或芳香族取代基的化合物，R2为直链或支链的卤代烷基磺酸取代基， 10个碳原子，具有1-10个碳原子的直链或支链烷基磺酸取代基，氟磺酸取代基或芳族磺酸取代基，并且R 3是保护基））在搅拌下在惰性有机溶剂中，在 相转移催化剂，18F离子和钾离子，以便用放射性氟进行标记，其中加热温度为40-90℃，相转移催化剂在惰性有机溶剂中的浓度为70mmol / L 或者更多。 相对于式（1）化合物，相转移催化剂的摩尔比优选为0.7以上，惰性有机溶剂中式（1）化合物的浓度为50mmol / L以上。

公开(公告)号：US20100119448A1

公开(公告)日：2010-05-13

申请号：US12526667

申请日：2008-02-12

申请人： Daisaku Nakamura ,  Soichi Nakamura ,  Masahito Toyama ,  Akio Hayashi

发明人： Daisaku Nakamura ,  Soichi Nakamura ,  Masahito Toyama ,  Akio Hayashi

IPC分类号： A61K51/04

CPC分类号： C07C229/48 ,  A61K9/0019 ,  A61K47/26 ,  A61K51/0402 ,  A61K51/0406 ,  C07B59/001 ,  C07B63/04 ,  C07B2200/05 ,  C07C2601/04

摘要： A method for producing a radioactive diagnostic imaging agent which contains a radioactive halogen-labeled amino acid compound as an effective ingredient and has a composition that can inhibit radiolysis of the effective ingredient, thereby further improving stability, is provided. Disclosed is a method for producing a radioactive diagnostic imaging agent, comprising a solution preparation step of preparing a solution containing a radioactive halogen-labeled amino acid compound, and a dilution step of diluting the solution containing the radioactive fluorine-labeled organic compound in order to adjust radioactive concentration thereof, which further comprises an acid addition step of adding an acid to the solution containing the radioactive fluorine-labeled organic compound, after the solution preparation step and before the dilution step, wherein the acid is added in the acid addition step in an amount sufficient to adjust the pH of the solution resulting from the dilution step to 2.0-5.9, for example, in an amount corresponding to 0.40-2.8 mmol per 1 L of the solution resulting from the dilution step.

摘要翻译： 提供了含有放射性卤素标记的氨基酸化合物作为有效成分并具有能够抑制有效成分的放射线析出，从而进一步提高稳定性的组成的放射性诊断显像剂的制造方法。 本发明公开了一种放射性诊断显像剂的制造方法，其特征在于，包括：制备含有放射性卤素标记的氨基酸化合物的溶液的溶液制备工序，以及稀释含有放射性氟标记的有机化合物的溶液的稀释步骤， 调整其放射性浓度，其还包括在溶液制备步骤之后和稀释步骤之前在含有放射性氟标记的有机化合物的溶液中加入酸的酸添加步骤，其中在酸添加步骤中加入酸 足以将由稀释步骤得到的溶液的pH调节至2.0-5.9的量，例如，相对于每1L由稀释步骤得到的溶液为0.40-2.8mmol的量。

公开(公告)号：US20100016626A1

公开(公告)日：2010-01-21

申请号：US12448311

申请日：2007-12-17

申请人： Masahito Toyama ,  Akio Hayashi

发明人： Masahito Toyama ,  Akio Hayashi

IPC分类号： C07C69/74

CPC分类号： G21H5/02 ,  A61K51/0406 ,  C07B59/001 ,  C07B2200/09 ,  C07C303/28 ,  C07C303/44 ,  C07C2601/04 ,  Y02P20/55 ,  C07C309/73 ,  C07C309/65 ,  C07C309/66

摘要： A process is provided for producing a labeled precursor which is useful for production of a radioactive fluorine-labeled amino acid compound. In the reaction step for introducing a leaving group to a mixture of syn-form and anti-form of FACBC, a base is allowed to present in the reaction system to produce a syn-leaving group adduct, which is unreactive with the base and is highly stable, and an anti-leaving group adduct which can react with the base to form a water-soluble compound. By employing a purification method utilizing such a difference in solubility, the syn-leaving group adduct can be separated selectively. The base may be a linear- or branched-chain primary to tertiary alkylamine having 1 to 10 carbon atoms, a nitrogen-containing heterocyclic compound with 2 to 20 carbon atoms, and a nitrogen-containing hetero aromatic compound with 2 to 20 carbon atoms.

摘要翻译： 提供了一种制备可用于制备放射性氟标记的氨基酸化合物的标记前体的方法。 在用于将离去基团引入到FACBC的正构形式和抗体形式的混合物的反应步骤中，允许碱在反应体系中存在以产生与碱不反应的合成离去基团加合物，并且是 高度稳定的抗离析基加合物，其可以与碱反应形成水溶性化合物。 通过使用利用这种溶解度差异的纯化方法，可以选择性地分离出合成离去基加成物。 碱可以是具有1-10个碳原子的直链或支链伯 - 叔烷基胺，具有2-20个碳原子的含氮杂环化合物和具有2-20个碳原子的含氮杂芳族化合物。

公开(公告)号：US20090226884A1

公开(公告)日：2009-09-10

申请号：US12225158

申请日：2007-03-20

申请人： Kazuo Tsujimoto ,  Akio Hayashi ,  Takaaki Kawai ,  Hiroyuki Matsumoto

发明人： Kazuo Tsujimoto ,  Akio Hayashi ,  Takaaki Kawai ,  Hiroyuki Matsumoto

IPC分类号： C12Q1/00 ,  G01N33/68

CPC分类号： G01N33/6842

摘要： Oxidized proteins, which have undergone oxidative modifications, are labeled with labeling reagents and quantified by mass spectrometry. In this process, a first labeling reagent, which is capable of reacting with the oxidized proteins, and a second labeling reagent, which has the same chemical structure as the first labeling reagent and in which at least part of the component atoms is substituted by an isotope of the atom concerned, are employed as the labeling reagents. The oxidized proteins labeled with the first labeling reagent and the oxidized proteins labeled with the second labeling reagent are mixed together and subjected to mass spectrometry, with mixing ratios varied. As the labeling reagents, are raised here 2,4-dinitrophenylhydrazine and 2,4-dinitrophenylhydrazine in which a carbon atom on the phenyl group has been substituted by a stable isotope (13C), for example.

摘要翻译： 已经经过氧化修饰的氧化蛋白质用标记试剂标记并通过质谱法定量。 在该方法中，能够与氧化蛋白反应的第一标记试剂和与第一标记试剂具有相同化学结构的第二标记试剂，其中至少部分成分原子被 所用原子的同位素用作标记试剂。 用第一标记试剂标记的氧化蛋白质和用第二标记试剂标记的氧化蛋白质混合在一起，进行质谱分析，混合比例变化。 作为标记试剂，例如可以举出苯基中的碳原子被稳定的同位素（13C）代替的2,4-二硝基苯肼和2,4-二硝基苯肼。

公开(公告)号：US20080281121A1

公开(公告)日：2008-11-13

申请号：US12085679

申请日：2006-11-28

申请人： Osamu Ito ,  Akio Hayashi ,  Fumie Kurosaki ,  Masahito Toyama ,  Toshiyuki Shinmura ,  Arinori Harano

发明人： Osamu Ito ,  Akio Hayashi ,  Fumie Kurosaki ,  Masahito Toyama ,  Toshiyuki Shinmura ,  Arinori Harano

IPC分类号： C07C69/74

CPC分类号： A61K51/0402 ,  A61K51/0406 ,  C07B59/00 ,  C07B2200/05 ,  C07C67/307 ,  C07C309/65 ,  C07C2601/04 ,  Y02P20/55

摘要： It is intended to provide a novel amino acid organic compound which can be used as a labeling precursor compound for radioactive halogen-labeled amino acid compounds including [18F]FACBC, and which prevents methanol from remaining in the radioactive halogen-labeled amino acid compounds produced therefrom. The novel amino acid organic compound is a compound represented by the following formula: wherein n is an integer of 0 or of 1 to 4; R1 is an ethyl, 1-propyl or isopropyl substituent; X is a halogen substituent or a group represented by —OR2; R2 is a straight-chain or branched-chain haloalkylsulfonic acid substituent with one to 10 carbon atoms, trialkylstannyl substituent with 3 to 12 carbon atoms, fluorosulfonic acid substituent or aromatic sulfonic acid substituent; and R3 is a protective group.

摘要翻译： 旨在提供一种新的氨基酸有机化合物，其可用作用于放射性卤素标记的氨基酸化合物的标记前体化合物，包括[SUP 18 F] FACBC，并且其防止甲醇残留在 由其制备的放射性卤素标记的氨基酸化合物。 新型氨基酸有机化合物是下式表示的化合物：其中，n为0或1〜4的整数， R 1是乙基，1-丙基或异丙​​基取代基; X是卤素取代基或由-OR 2表示的基团。 R 2是具有1至10个碳原子的直链或支链卤代烷基磺酸取代基，具有3至12个碳原子的三烷基甲锡烷基取代基，氟代磺酸取代基或芳族磺酸取代基; R 3是保护基。

公开(公告)号：US20070256401A1

公开(公告)日：2007-11-08

申请号：US11790208

申请日：2007-04-24

申请人： Yoshihisa Hibi ,  Graeme Sidney Parris ,  Akio Hayashi

发明人： Yoshihisa Hibi ,  Graeme Sidney Parris ,  Akio Hayashi

IPC分类号： A01D75/28

CPC分类号： A01D34/824

摘要： A walk-behind lawn mower in a form that a handle arm is integrally provided toward an obliquely upper back in a rear of a machine, and a loop handle is provided at a rear end of the relevant handle arm with slightly tilting forward, and a driver performs drive operation while walking following the machine that travels by itself at a back of the machine, includes a throttle lever, the throttle lever being able to be drawn together with the handle by being operated by either of right and left hands grasping the handle, in addition, engine rotation frequency being able to be controlled using the amount of drawing, wherein the throttle lever is rotatably provided on the handle arm in an obliquely lower front or obliquely upper back of the handle.

摘要翻译： 把手臂一体地设置在机器后部的斜上背部的形式的步行式割草机，并且在稍后向前倾斜的相关把手臂的后端设置有环把手，并且 驾驶员在机器背后的机器行走时执行驾驶操作，包括节流杆，节气门杆能够通过由把手握住的左手和右手中的任一个操作而与手柄一起拉动 此外，能够使用拉伸量来控制发动机转速，其中节流杆可旋转地设置在手柄的手柄的倾斜下前方或斜后方。

公开(公告)号：US06706260B1

公开(公告)日：2004-03-16

申请号：US09743357

申请日：2001-01-05

申请人： Shinji Tanaka ,  Ken Suzuki ,  Kenshiro Shuto ,  Akio Hayashi ,  Nobuo Nakabayashi ,  Kazuhiko Ishihara

发明人： Shinji Tanaka ,  Ken Suzuki ,  Kenshiro Shuto ,  Akio Hayashi ,  Nobuo Nakabayashi ,  Kazuhiko Ishihara

IPC分类号： A61K3174

CPC分类号： C08F230/02 ,  A61L15/24 ,  A61L15/26 ,  A61L27/16 ,  C08F30/02 ,  C08L43/02 ,  C08F2220/1825 ,  C08F2222/108 ,  C08F2222/1013 ,  C08F2220/1858 ,  C08F2220/325 ,  C08L101/02

摘要： A wound-covering agent containing a polymer having a group represented by formula (I) (wherein R1, R2 and R3 are the same or different and each represents hydrogen atom or C1-4 alkyl, and m is an integer of 2 to 4); a wound-covering material containing the preparation; and a method of wound healing which comprises the step of covering the wound of a subject with the wound-covering material to protect the wound.

摘要翻译： 含有具有式（I）表示的基团的聚合物的伤口覆盖剂（其中R 1，R 2和R 3相同或不同，各自表示氢原子或C 1-4烷基， m为2〜4的整数）; 含有该制剂的伤口覆盖材料; 以及伤口愈合方法，其包括用伤口覆盖材料覆盖受试者的伤口以保护伤口的步骤。

公开(公告)号：US5889087A

公开(公告)日：1999-03-30

申请号：US842386

申请日：1997-04-23

申请人： Akio Hayashi ,  Katsuhiro Horita

发明人： Akio Hayashi ,  Katsuhiro Horita

IPC分类号： C08K3/00 ,  C08L23/00 ,  C08L23/08 ,  C08L31/04 ,  C08L33/04 ,  C08L33/08 ,  H01B3/44 ,  H01B7/295 ,  H02G15/00

CPC分类号： H01B3/441 ,  H01B3/447 ,  H01B3/448 ,  H01B7/295 ,  H02G15/003

摘要： A cable comprising one or more electrical conductors or communications media, or a core of two or electrical conductors or communications media, each electrical conductor, communications medium, or core being surrounded by a composition comprising:(A) about 40 to about 93 percent by weight of at least one resin selected from the group consisting of ethylene/vinyl acetate copolymer, ethylene/ethyl acrylate copolymer, and an ethylene/alpha-olefin copolymer having a density equal to or less than 0.915 gram per cubic centimeter.(B) about 5 to about 50 percent by weight of a linear ethylene/alpha-olefin copolymer produced by using a single-site metallocene catalyst and having a melt flow rate of about 0.5 to about 50 grams per 10 minutes; a density of 0.86 to 0.91 gram per cubic centimeter; and an Mw/Mn ratio equal to or less than about 3.0;(C) about 2 to about 40 percent by weight of an ethylenic resin modifiedwith a compound or compounds containing a functional group, andfor each 100 parts by weight of components (A), (B), and (C), combined,(D) about 50 to about 250 parts by weight of an inorganic flame retardant; and(E) about 0.05 to about 10 parts by weight of silicone oil.

摘要翻译： 一种电缆，包括一个或多个电导体或通信介质，或两个或电气导体或通信介质的核心，每个电导体，通信介质或核心被组合物包围，所述组合物包括：（A）约40至约93％ 选自乙烯/乙酸乙烯酯共聚物，乙烯/丙烯酸乙酯共聚物和密度等于或小于0.915克/立方厘米的乙烯/α-烯烃共聚物中的至少一种树脂的重量。 （B）约5至约50重量％的通过使用单位点金属茂催化剂制备的线性乙烯/α-烯烃共聚物，其熔体流动速率为约0.5至约50克/ 10分钟; 密度为0.86至0.91克/立方厘米; 和Mw / Mn比等于或小于约3.0; （C）约2〜约40重量％的用含有官能团的化合物或化合物改性的乙烯树脂，并且对于每100重量份的组分（A），（B）和（C）组合， （D）约50至约250重量份的无机阻燃剂; 和（E）约0.05至约10重量份的硅油。