公开(公告)号：US20050075393A1

公开(公告)日：2005-04-07

申请号：US10450816

申请日：2001-12-18

申请人： Tomoyuki Nishizaki ,  Akito Tanaka

发明人： Tomoyuki Nishizaki ,  Akito Tanaka

IPC分类号： A61K31/19 ,  A61K31/20 ,  A61P25/00 ,  A61P25/16 ,  A61P25/28 ,  C07C53/132 ,  C07C53/134 ,  C07C57/26 ,  C07C61/04 ,  C07C61/12 ,  C07C61/28 ,  C07C61/35 ,  A61K31/215

CPC分类号： C07C61/04 ,  C07C53/134 ,  C07C57/26 ,  C07C61/12 ,  C07C61/28 ,  C07C61/35

摘要： A carboxylic acid compound having cyclopropane ring(s) of the formula (I): wherein R is alkyl or alkenyl optionally having one or more 1,2-cyclopropylene in a carbon chain and/or optionally having cyclopropyl at the end of a chain, X is a single bond or alkylene, wherein the total number of carbon less the number of cyclopropane ring is 10-25, and a pharmaceutically acceptable salt thereof are provided. The compound (I) shows an LTP-like potentiation of synaptic transmission, allows slow metabolism in the living body, shows a stable LTP-like potentiation of synaptic transmission, and is useful as an agent for LTP-like potentiation of synaptic transmission, a cognition-enhancing drug or an agent for the prophylaxis and treatment of dementia, a learning and memory disorder and a neurotransmitter release disorder.

摘要翻译： 具有式（I）的环丙烷环的羧酸化合物：其中R是在碳链中任选具有一个或多个1,2-亚丙基的烷基或链烯基和/或在链末端任选具有环丙基的羧酸化合物， X是单键或亚烷基，其中提供环丙烷环数少于10-25的碳总数及其药学上可接受的盐。 化合物（I）显示突触传递的LTP样增强，允许活体中的代谢缓慢，表现出稳定的LTP样增强突触传递，并且可用作LTP样增强突触传递的药剂， 认知增强药物或预防和治疗痴呆，学习和记忆障碍和神经递质释放障碍的药剂。

公开(公告)号：US06225480B1

公开(公告)日：2001-05-01

申请号：US09331580

申请日：1999-06-30

申请人： Akito Tanaka ,  Hideo Tsutsumi

发明人： Akito Tanaka ,  Hideo Tsutsumi

IPC分类号： C07D31104

CPC分类号： C40B80/00 ,  C07C309/87 ,  C07D311/70 ,  C07D311/92 ,  C40B40/04 ,  C40B50/14 ,  Y02P20/55

摘要： The present invention relates to a linker shown by the following formula (I): X—SO2—R1—(A)m—R2  (I) wherein R1 is a group of the formula (A): [wherein R3, R4 and R5 are the same or different hydrogen, etc], etc, R2 is a group which can form a chemical bond to a resin which may be protected by a conventional protective group, A is lower alkylene, etc, X is a leaving group, and m is an integer of 0 or 1, with proviso that A is (C2-C6)alkylene, and m is an integer of 1, when R1 is a group of the formula (A).

摘要翻译： 本发明涉及由下式（I）表示的接头：其中R1是式（A）的基团：[其中R3，R4和R5是相同或不同的氢等]等，R2是 可以与常规保护基保护的树脂形成化学键的基团，A为低级亚烷基等，X为离去基团，m为0或1的整数，条件是A为（C2- C6）亚烷基，当R1是式（A）的基团时，m是1的整数。

公开(公告)号：US6093710A

公开(公告)日：2000-07-25

申请号：US147812

申请日：1999-03-12

申请人： Akito Tanaka ,  Hiroaki Mizuno ,  Minoru Sakurai

发明人： Akito Tanaka ,  Hiroaki Mizuno ,  Minoru Sakurai

IPC分类号： C07D333/24 ,  A61K31/343 ,  A61K31/381 ,  A61K31/542 ,  A61P9/00 ,  A61P15/18 ,  A61P19/02 ,  A61P19/10 ,  A61P27/02 ,  A61P35/00 ,  C07D307/82 ,  C07D307/85 ,  C07D333/70 ,  C07D333/80 ,  C07D513/04 ,  C07D493/04 ,  C07D495/04

CPC分类号： C07D513/04 ,  C07D307/85 ,  C07D333/70 ,  C07D333/80 ,  Y02P20/55

摘要： A compound of the formula ##STR1## in which R.sup.1 is hydrogen, lower alkyl, optionally substituted ar(lower)alkyl, cyclo(lower)alkyl(lower)alkyl, protected carboxy)lower)alkyl, carboxy)lower)alkyl, hydroxy(lower)alkyl, optionally substituted lower alkylcarbamoyl(lower)alkyl, lower alkylthio(lower)alkyl, carboxy(lower)alkanoyl, protected carboxy(lower)alkanoyl, aroyl, lower alkanoyl, or optionally substituted arylcarbamoyl(lower)alkyl,R.sup.2 is hydrogen, carboxy, protected carboxy, formyl or N-(lower)alkyl-N-(lower)alkoxycarbamoyl,R.sup.3 is hydrogen or amidino-protective group,A is lower alkylene or carbonyl,X is ##STR2## Y is --S-- or --SO.sub.2 --, Z is --S-- or --O--,or pharmaceutically acceptable salts thereofwhich is useful as a medicament.

摘要翻译： PCT No.PCT / JP97 / 03215 Sec。 371 1999年3月12日 102（e）1999年3月12日PCT PCT 1997年9月12日PCT公布。 出版物WO98 / 11089 日本公开的化合物，其中R 1为氢，低级烷基，任选取代的芳（低级）烷基，环（低级）烷基（低级）烷基，被保护的羧基）低级烷基，羧基）低级）烷基， 羟基（低级）烷基，任选取代的低级烷基氨基甲酰基（低级）烷基，低级烷硫基（低级）烷基，羧基（低级）烷酰基，受保护的羧基（低级）烷酰基，芳酰基，低级烷酰基或任选取代的芳基氨基甲酰基 （低级）烷基-N-（低级）烷氧基氨基甲酰基，R3是氢或脒基保护基，A是低级亚烷基或羰基，X是Y是-S-或-SO2 - ，Z是-S-或-O-，或其药学上可接受的盐，其可用作药物。

公开(公告)号：US5229386A

公开(公告)日：1993-07-20

申请号：US849179

申请日：1992-03-10

申请人： Hisashi Takasugi ,  Shigetaka Nishino ,  Akito Tanaka

发明人： Hisashi Takasugi ,  Shigetaka Nishino ,  Akito Tanaka

IPC分类号： C07D277/28 ,  C07D277/40 ,  C07D277/48 ,  C07D417/04 ,  C07D417/12 ,  C07D471/04

CPC分类号： C07D417/04 ,  C07D277/28 ,  C07D277/40 ,  C07D277/48 ,  C07D417/12 ,  C07D471/04

摘要： The invention relates to new thiazole compounds, of antithrombotic, vasodilating, antiallergic, antiinflammatory and 5-lipoxygenase inhibitory activity, of the formula: ##STR1##

摘要翻译： 本发明涉及新的噻唑化合物，抗血栓形成，血管扩张，抗过敏，抗炎和5-脂氧合酶抑制活性，其结构如下：

公开(公告)号：US5145860A

公开(公告)日：1992-09-08

申请号：US495622

申请日：1990-03-19

申请人： Hisashi Takasugi ,  Shigetaka Nishino ,  Akito Tanaka

发明人： Hisashi Takasugi ,  Shigetaka Nishino ,  Akito Tanaka

IPC分类号： C07D277/28 ,  C07D277/40 ,  C07D277/48 ,  C07D417/04 ,  C07D417/12 ,  C07D471/04

CPC分类号： C07D417/04 ,  C07D277/28 ,  C07D277/40 ,  C07D277/48 ,  C07D417/12 ,  C07D471/04

摘要： The invention relates to new thiazole compounds, of antithrombotic, vasodilating, antiallergic, antiinflammatory and 5-lipoxygenase inhibitory activity, of the formula: ##STR1## wherein A is lower alkylene or carbonyl; R.sup.1 and R.sup.2 are each halogen, lower alkyloxy, lower alkylthio or lower alkylsulfinyl;R.sup.3 is acyl derived from an aliphatic carboxylic or carbamic acid; andR.sup.4 is hydrogen, lower alkyl, amidino or acyl derived from an aliphatic carboxylic or carbamic acid, or the pharmaceutically acceptable salt thereof.

摘要翻译： 本发明涉及新的噻唑化合物，抗血栓形成，血管扩张，抗过敏，抗炎和5-脂氧合酶抑制活性，其结构式如下：其中A为低级亚烷基或羰基; R1和R2各自为卤素，低级烷氧基，低级烷硫基或低级烷基亚磺酰基; R3是衍生自脂族羧酸或氨基甲酸的酰基; R4为氢原子，低级烷基，脒基或衍生自脂族羧酸或氨基甲酸的酰基，或其药学上可接受的盐。

公开(公告)号：US09012500B2

公开(公告)日：2015-04-21

申请号：US13885751

申请日：2011-11-15

申请人： Tomoyuki Nishizaki ,  Akito Tanaka

发明人： Tomoyuki Nishizaki ,  Akito Tanaka

IPC分类号： A61K31/235 ,  C07C53/132

CPC分类号： C07C53/132 ,  A61K31/235 ,  C07B2200/07

摘要： The present invention aims to obtain an optical isomer of DCP-LA, which shows more superior activity and is suitable for clinical utilization, and provide an agent having a superior PKC-ε activation action, a prophylactic and/or therapeutic agent for neurotransmitter release disorders, and a prophylactic and/or therapeutic agent for neuropsychiatric diseases, which contain the isomer as an active ingredient.A compound represented by the following formula: or a pharmaceutically acceptable salt thereof, and a selective PKC-ε activator containing same as an active ingredient, and is the like.

摘要翻译： 本发明旨在获得DCP-LA的光学异构体，其具有更优异的活性并且适用于临床应用，并提供具有优异PKC- 活化作用，神经递质释放障碍的预防和/或治疗剂，以及含有异构体作为活性成分的神经精神疾病的预防和/或治疗剂。 由下式表示的化合物或其药学上可接受的盐和选择性PKC- 含有与活性成分相同的活化剂，等等。

公开(公告)号：US07923211B2

公开(公告)日：2011-04-12

申请号：US12543801

申请日：2009-08-19

申请人： Akito Tanaka ,  Akira Yamazaki

发明人： Akito Tanaka ,  Akira Yamazaki

IPC分类号： G01N33/53 ,  G01N33/543

CPC分类号： G01N33/54313 ,  G01N33/54393 ,  Y10S435/973 ,  Y10T436/10 ,  Y10T436/25375

摘要： A method to determine specificity of ligand binding includes comparing a solid phase carrier first extract obtained by pre-treating a sample with a ligand-immobilized solid phase carrier and a solid phase carrier second extract obtained by treating the pretreated sample again with a ligand-immobilized solid phase carrier in terms of the proteins contained therein, and identifying a protein whose content is remarkably decreased in the second extract compared to the first extract, in order to solve 1) the problem of the solubility of subject ligand, 2) the problem of the non-specific protein-denaturing effect of the subject ligand added, and the like, in antagonism experiments in target search using an affinity resin.

摘要翻译： 确定配体结合特异性的方法包括比较通过预处理样品与固定配体的固相载体获得的固相载体第一提取物和通过用配体固定化处理再次处理预处理的样品获得的固相载体第二提取物 固相载体与其中所含的蛋白质相比，并鉴定出与第一提取物相比，第二提取物中其含量显着降低的蛋白质，以解决1）本发明配体的溶解度问题，2） 使用亲和树脂进行目标检测的拮抗实验中加入的受试者配体的非特异性蛋白质变性效应等。

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。

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。

公开(公告)号：US06274619B1

公开(公告)日：2001-08-14

申请号：US09584136

申请日：2000-05-31

申请人： Akito Tanaka ,  Hiroaki Mizuno ,  Minoru Sakurai

发明人： Akito Tanaka ,  Hiroaki Mizuno ,  Minoru Sakurai

IPC分类号： C07D30785

CPC分类号： C07D513/04 ,  C07D307/85 ,  C07D333/70 ,  C07D333/80 ,  Y02P20/55

摘要： A compound of the formula: in which R1 is hydrogen, optionally substituted lower alkylcarbamoyl(lower)alkylidene, lower alkylidene, lower alkyl, optionally substituted ar(lower)alkyl, cyclo(lower)alkyl(lower)alkyl, protected carboxy(lower)alkyl, carboxy(lower)alkyl, hydroxy(lower)alkyl, optionally substituted lower alkylcarbamoyl(lower)alkyl, lower alkylthio(lower)alkyl, carboxy(lower)alkanoyl, protected carboxy(lower)alkanoyl, aroyl, lower alkanoyl, or optionally substituted arylcarbamoyl(lower)alkyl, R2 is hydrogen, carboxy, protected carboxy, formyl or N-(lower)alkyl-N-(lower)alkoxycarbamoyl, R3 is hydrogen or amidino-protective group, A is lower alkylene or carbonyl, X is Y is lower alkylene, —S— or —SO2—, Z is —S— or —O—, and the line: is a single bond or a double bond, or pharmaceutically acceptable salts thereof, which is useful as a medicament.

摘要翻译： 下式化合物：其中R 1为氢，任选取代的低级烷基氨基甲酰基（低级）亚烷基，低级亚烷基，低级烷基，任选取代的芳（低级）烷基，环（低级）烷基（低级）烷基，被保护的羧基 ，羧基（低级）烷基，羟基（低级）烷基，任选取代的低级烷基氨基甲酰基（低级）烷基，低级烷硫基（低级）烷基，羧基（低级）烷酰基，受保护羧基（低级）烷酰基，芳酰基，低级烷酰基或任选取代 芳基氨基甲酰基（低级）烷基，R2是氢，羧基，保护的羧基，甲酰基或N-（低级）烷基-N-（低级）烷氧基氨基甲酰基，R3是氢或脒基保护基，A是低级亚烷基或羰基，X是Y 低级亚烷基，-S-或-SO 2 - ，Z是-S-或-O-，并且行：是 单键或双键，或其药学上可接受的盐，其可用作药物。