公开(公告)号：US08664226B2

公开(公告)日：2014-03-04

申请号：US13263023

申请日：2010-04-16

Applicant: Toru Miura ,  Kazuhiro Onogi ,  Seiichi Sato ,  Junya Tagashira ,  Gen Watanabe ,  Ryohei Sekimoto ,  Rie Ishida ,  Hitomi Aoki ,  Tadaaki Ohgiya

Inventor： Toru Miura ,  Kazuhiro Onogi ,  Seiichi Sato ,  Junya Tagashira ,  Gen Watanabe ,  Ryohei Sekimoto ,  Rie Ishida ,  Hitomi Aoki ,  Tadaaki Ohgiya

IPC: C07D401/14 ,  A61K31/506

CPC classification number: C07D401/14 ,  C07D403/14 ,  C07D413/14 ,  C07D417/14

Abstract: Disclosed is a compound which has both an angiotensin-II receptor antagonistic activity and a PPARγ activation activity and is useful as a prophylactic and/or therapeutic agent for hypertension, heart diseases, angina pectoris, cerebrovascular disorders, cerebral circulatory disorders, ischemic peripheral circulatory disorders, renal diseases, arteriosclerosis, inflammatory diseases, type-2 diabetes, diabetic complications, insulin resistance syndrome, syndrome X, metabolic syndrome and hyperinsulinemia. [In the formula, A represents a 5- to 10-membered heteroaryl group; R1 and R2 independently represent a C1-6 alkyl group; and each of R3 to R5 is absent or represents H, a halogen atom, OH, NO2, a halo-C1-6 alkyl group, a (substituted) C1-6 alkoxy group, a (substituted) C3-6 cycloalkyloxy group, or a 5- to 10-membered heteroaryl group.]

Abstract translation: 公开了具有血管紧张素-II受体拮抗作用和PPARγ活化活性的化合物，可用作高血压，心脏病，心绞痛，脑血管障碍，脑循环障碍，缺血性外周循环障碍的预防和/或治疗剂 肾脏疾病，动脉硬化，炎性疾病，2型糖尿病，糖尿病并发症，胰岛素抵抗综合征，X综合征，代谢综合征和高胰岛素血症。 [式中，A表示5至10元杂芳基; R1和R2独立地表示C1-6烷基; 并且R 3至R 5不存在或表示H，卤素原子，OH，NO 2，卤代C 1-6烷基，（取代的）C 1-6烷氧基，（取代的）C 3-6环烷氧基或 5至10元杂芳基。]

公开(公告)号：US20140051876A1

公开(公告)日：2014-02-20

申请号：US14113498

申请日：2012-04-26

Applicant: Shinji Ina ,  Takahiro Yamazaki ,  Junichi Sakata ,  Koji Ezaki ,  Katsuhiro Sakamoto

Inventor： Shinji Ina ,  Takahiro Yamazaki ,  Junichi Sakata ,  Koji Ezaki ,  Katsuhiro Sakamoto

IPC: C07C51/09 ,  C07C57/03 ,  C07F9/40

CPC classification number: C07C51/09 ,  A61K9/4858 ,  A61K9/4866 ,  A61K9/4875 ,  A61K31/167 ,  A61K31/202 ,  A61K33/16 ,  A61K35/742 ,  A61K35/744 ,  A61K45/06 ,  C07C51/353 ,  C07C57/03 ,  C07C67/343 ,  C07F9/4015 ,  A61K2300/00 ,  C07C69/587

Abstract: Provided is a method of manufacturing a high quality phosphonocrotonic acid derivative.The present invention is a method of manufacturing a compound represented by the following Formula (3) by reacting a compound represented by the following Formula (1) with a compound represented by the following Formula (2), which comprises a treatment process using an acid or base.[in the formula, R1 represents a C1-6 linear or branched alkyl group that may be substituted by a C6-10 aryl group, a C2-6 linear or branched alkenyl group that may be substituted by a C6-10 aryl group, a C2-6 linear or branched alkynyl group that may be substituted by a C6-10 aryl group, or a C6-10 aryl group, R2 represents a hydrogen atom, or a C1-6 linear or branched alkyl group that may be substituted by a C6-10 aryl group, R3 represents a C1-6 linear or branched alkyl group, a C6-10 aryl group, or a halogen atom, and X represents a halogen atom, and multiple R1s may be the same or different].

Abstract translation: 提供制造高品质膦酸巴豆酸衍生物的方法。 本发明是通过使由下式（1）表示的化合物与下式（2）表示的化合物反应来制备由下式（3）表示的化合物的方法，该方法包括使用酸 或基地。 [式中，R 1表示可被C 6-10芳基取代的C 1-6直链或支链烷基，可被C 6-10芳基取代的C 2-6直链或支链烯基， 可被C 6-10芳基或C 6-10芳基取代的C 2-6直链或支链炔基，R 2表示氢原子，或可被C 1-6烷基取代的C 1-6直链或支链烷基 C6-10芳基，R3表示C1-6直链或支链烷基，C6-10芳基或卤素原子，X表示卤素原子，多个R1可以相同或不同]。

公开(公告)号：US20140039616A1

公开(公告)日：2014-02-06

申请号：US14002831

申请日：2012-03-23

Applicant: Asaki Suzaki

Inventor： Asaki Suzaki

IPC: A61F2/16 ,  G02C7/02

CPC classification number: A61F2/1637 ,  A61F2/1613 ,  A61F2240/001 ,  G02C7/027

Abstract: Provided is an intraocular lens having a novel structure with high utility which is easy to adapt to patients, and can improve quality of vision (QOV). In an intraocular lens, an optical characteristic is set rotationally symmetric around an optical axis, and a spherical aberration of a size corresponding to a coma aberration remaining in a patient's eye after extraction of a human lens of the eye is set.

Abstract translation: 本发明提供一种具有高效益的新型结构的眼内透镜，其易于适应患者，并且可以提高视力（QOV）。 在眼内透镜中，光学特性围绕光轴旋转对称设定，并且设置了在提取眼睛的人体眼镜后残留在患者眼睛中的彗差的大小的球面像差。

公开(公告)号：US20130309704A1

公开(公告)日：2013-11-21

申请号：US13981893

申请日：2012-01-26

Applicant: Katsuya Inada ,  Shigeatsu Endo ,  Taisuke Hirono ,  Takaharu Asano

Inventor： Katsuya Inada ,  Shigeatsu Endo ,  Taisuke Hirono ,  Takaharu Asano

IPC: G01N21/82

CPC classification number: G01N21/82 ,  G01N33/54313 ,  G01N33/54393 ,  G01N33/579

Abstract: The purpose of the present invention is to improve the measurement accuracy in the measurement of the concentration of a physiologically active biological substance in a sample by a stirring turbidimetry, a light scattering method or an AL-bound beads method, wherein the purpose can be achieved by preventing the occurrence of aggregation or gelation that is caused by the stirring of a mixed solution and is not associated with the physiologically active substance. AL is mixed with a sample containing a physiologically active biological substance, and the aggregation of a protein which is associated with the reaction between AL and the physiologically active substance in the mixed solution is detected while stirring the mixed solution, wherein the occurrence of the aggregation or gelation of a protein which is not associated with the reaction between AL and the physiologically active substance in the mixed solution can be prevented by adding a specific protein that has been heated in advance and/or a specific surfactant to the mixed solution.

Abstract translation: 本发明的目的是通过搅拌比浊法，光散射法或AL结合珠法提高测定生物活性生物物质浓度的测量精度，其目的是实现 通过防止混合溶液的搅拌引起的聚集或凝胶化的发生，与生理活性物质不相关。 将AL与含有生理活性生物物质的样品混合，并在搅拌混合溶液的同时检测与混合溶液中AL与生理活性物质之间的反应相关的蛋白质的聚集，其中发生聚集 或者与混合溶液中的AL与生理活性物质的反应无关的蛋白质的凝胶化可以通过将预先加热的特定蛋白质和/或特定的表面活性剂加入到混合溶液中来防止。

公开(公告)号：US20130225814A1

公开(公告)日：2013-08-29

申请号：US13700849

申请日：2011-06-03

Applicant: Tadaaki Ohgiya ,  Takeshi Murakami ,  Katsutoshi Miyosawa ,  Kimiyuki Shibuya ,  Koichi Yamazaki ,  Taichi Kusakabe

Inventor： Tadaaki Ohgiya ,  Takeshi Murakami ,  Katsutoshi Miyosawa ,  Kimiyuki Shibuya ,  Koichi Yamazaki ,  Taichi Kusakabe

IPC: C07D239/47

CPC classification number: C07D239/47

Abstract: Substantially optically pure (S)-trans-{4-[({2-[({1-[3,5-bis(trifluoromethyl)phenyl]ethyl}{5-[2-(methylsulfonyl)ethoxy]pyrimidin-2-yl}amino)methyl]-4-(trifluoromethyl)phenyl}(ethyl)amino)methyl]cyclohexyl}acetic acid, or a salt thereof, or a solvate thereof, which has actions of reducing amount of PCSK9 protein and increasing amount of LDL receptor.

Abstract translation: 基本上光学纯的（S） - 反 - {4 - [（{2 - [（{1- [3,5-双（三氟甲基）苯基]乙基} {5- [2-（甲基磺酰基）乙氧基] 吡啶-3-基}氨基）甲基] -4-（三氟甲基）苯基}（乙基）氨基）甲基]环己基}乙酸或其盐或其溶剂合物，其具有减少PCSK9蛋白量和增加LDL量的作用 受体。

公开(公告)号：US08309574B2

公开(公告)日：2012-11-13

申请号：US10590493

申请日：2005-02-24

Applicant: Takahide Kohro ,  Yoshikazu Shibasaki ,  Takao Hamakubo ,  Tatsuhiko Kodama

Inventor： Takahide Kohro ,  Yoshikazu Shibasaki ,  Takao Hamakubo ,  Tatsuhiko Kodama

IPC: A61K31/47

CPC classification number: G01N33/6872 ,  A61K31/51 ,  A61K45/06 ,  G01N2333/4719 ,  A61K2300/00

Abstract: A nuclear transfer promoter for Rac protein comprising an isoprenoid synthesis inhibitor and/or a geranylgeranyl transferase inhibitor such as an HMG-CoA synthase inhibitor, an HMG-CoA reductase inhibitor, an AMPK activator or a farnesyl pyrophosphoric acid synthase preparation; utilization thereof; a method therefor; a blood vessel remedy comprising the nuclear transfer promoter for Rac protein as the active ingredient; and a method of screening a blood vessel remedy which comprises assaying the ability of Rac protein to transfer into nucleus.

Abstract translation: 包含类异戊二烯合成抑制剂和/或香叶基香叶基转移酶抑制剂如HMG-CoA合成酶抑制剂，HMG-CoA还原酶抑制剂，AMPK激活剂或法呢基焦磷酸合成酶的Rac蛋白的核转移启动子; 使用; 一种方法; 包括用于Rac蛋白的核转移启动子作为活性成分的血管补救剂; 以及筛选血管补救的方法，其包括测定Rac蛋白转移入细胞核的能力。

公开(公告)号：US20120264753A1

公开(公告)日：2012-10-18

申请号：US13511876

申请日：2010-12-22

Applicant: Toru Miura ,  Hajime Yamada ,  Junya Tagashira ,  Gen Watanabe ,  Ryohei Sekimoto ,  Rie Ishida ,  Hitomi Aoki ,  Tadaaki Ohgiya

Inventor： Toru Miura ,  Hajime Yamada ,  Junya Tagashira ,  Gen Watanabe ,  Ryohei Sekimoto ,  Rie Ishida ,  Hitomi Aoki ,  Tadaaki Ohgiya

IPC: A61K31/4178 ,  A61K31/4245 ,  C07D413/14 ,  A61K31/506 ,  C07D403/14 ,  A61K31/5377 ,  C07D403/10 ,  A61P9/00 ,  A61P9/12 ,  A61P9/10 ,  A61P13/12 ,  A61P3/00 ,  A61P3/10 ,  A61P25/00 ,  C07D413/10

CPC classification number: C07D403/10 ,  C07D403/14 ,  C07D413/10 ,  C07D413/14

Abstract: Disclosed is a novel 1-(biphenyl-4-yl-methyl)-1H-imidazole derivative represented by general formula (I), which has both angiotensin II receptor antagonist activity and PPAR-γ activating activity and is useful as a prophylactic and/or therapeutic agent for cardiovascular diseases and metabolic diseases. Also disclosed is a pharmaceutical composition which contains the novel 1-(biphenyl-4-yl-methyl)-1H-imidazole derivative. In general formula (I), ring A represents a group represented by formula (II) or (III); R1 represents a C1-6 alkyl group; R2 represents a C1-6 alkyl group which may be substituted by a hydroxy group, or a group represented by formula —CO—R4 (wherein R4 represents a hydroxy group, a C1-6 alkoxy group, an amino group, a mono(C1-6 alkyl)amino group, a di(C1-6 alkyl)amino group, a morpholino group, a piperidino group or a pyrrolidino group); R3 represents a halogen atom or a C1-6 alkoxy group; and X and Y may be the same or different and each represents a nitrogen atom or CH.

Abstract translation: 公开了由通式（I）表示的新颖的1-（联苯-4-基 - 甲基）-1H-咪唑衍生物，其具有血管紧张素II受体拮抗剂活性和PPAR-γ活化活性，可用作预防和/ 或用于心血管疾病和代谢疾病的治疗剂。 还公开了含有新的1-（联苯-4-基 - 甲基）-1H-咪唑衍生物的药物组合物。 在通式（I）中，环A表示由式（II）或（III）表示的基团; R1表示C1-6烷基; R2表示可以被羟基取代的C1-6烷基或由式-CO-R4表示的基团（其中R4表示羟基，C1-6烷氧基，氨基，单（C1 -6烷基）氨基，二（C 1-6烷基）氨基，吗啉代基，哌啶子基或吡咯烷子基）。 R3表示卤素原子或C1-6烷氧基; X和Y可以相同或不同，各自表示氮原子或CH。

公开(公告)号：US08265398B2

公开(公告)日：2012-09-11

申请号：US12531123

申请日：2008-03-10

Applicant: Hiroshi Fujita ,  Toshiaki Nakagawa ,  Yoshinori Hayashi

Inventor： Hiroshi Fujita ,  Toshiaki Nakagawa ,  Yoshinori Hayashi

IPC: G06K9/00 ,  G01B11/30 ,  A61B3/14

CPC classification number: G06T7/593 ,  G06T2207/10012 ,  G06T2207/10024 ,  G06T2207/20012 ,  G06T2207/20021 ,  G06T2207/30041

Abstract: There is provided an image analysis system which captures image data of an arbitrary pair of a first image RI and a second image LI among images obtained by color-photographing a single object from different positions into an analysis computer, wherein the computer includes corresponding point extraction means for assigning a weighing factor to a pixel information value based on the contrast size of the pixel information value in each of a first local area ROI1 set around an arbitrary reference point in RI and second local areas ROI2s at which scanning is performed on LI, calculating the similarity between ROI1 and ROI2s, and extracting a corresponding point which corresponds to the reference point from a ROI2 having the highest similarity, and depth information calculating means for calculating depth information of the object based on coordinates of the reference point and the corresponding point.

Abstract translation: 提供了一种图像分析系统，其捕获通过将单个对象从不同位置彩色拍摄而获得的图像中的任意一对第一图像RI和第二图像LI的图像数据，其中所述计算机包括相应的点提取 用于基于在RI中的任意参考点周围设置的第一局部区域ROI1和对LI执行扫描的第二局部区域ROI2中的每一个中的像素信息值的对比度大小将像素信息值分配给像素信息值的装置， 计算ROI1和ROI2之间的相似度，以及从具有最高相似度的ROI2提取与参考点对应的对应点，以及深度信息计算装置，用于基于参考点和对应点的坐标来计算对象的深度信息 。

公开(公告)号：US08252781B2

公开(公告)日：2012-08-28

申请号：US12607650

申请日：2009-10-28

Applicant: Hisashi Nakashima ,  Takaaki Araki ,  Takahisa Ogamino ,  Noriaki Gomi ,  Yasushi Kaneko ,  Kazutoyo Abe ,  Tadaaki Ohgiya

Inventor： Hisashi Nakashima ,  Takaaki Araki ,  Takahisa Ogamino ,  Noriaki Gomi ,  Yasushi Kaneko ,  Kazutoyo Abe ,  Tadaaki Ohgiya

IPC: C07D229/00 ,  C07D409/04 ,  C07D405/12 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  A61K31/397 ,  A61K31/4427 ,  A61K31/498 ,  A61P9/12 ,  A61P3/10 ,  A61P3/04 ,  A61P3/06

CPC classification number: C07D229/00 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D405/04 ,  C07D405/06 ,  C07D409/04

Abstract: [Object]It is to provide a novel compound useful for preventing and/or treating diseases that involves 11β-hydroxysteroid dehydrogenase 1 (in particular diabetes, insulin resistance, diabetes complication, obesity, dyslipidemia, hypertension, fatty liver, or metabolic syndrome).[Means to Solve the Object]A 1,2-diazetidin-3-one derivative represented by the following general formula (1) or salt thereof, or their solvate.

Abstract translation: 提供一种可用于预防和/或治疗涉及11-羟基类固醇脱氢酶1（特别是糖尿病，胰岛素抵抗，糖尿病并发症，肥胖，血脂异常，高血压，脂肪肝或代谢综合征）的疾病的新化合物。 。 解决对象的方法由下述通式（1）表示的1,2-二氮杂环丁-3-酮衍生物或其盐或其溶剂化物。

公开(公告)号：US08252524B2

公开(公告)日：2012-08-28

申请号：US12548239

申请日：2009-08-26

Applicant: Takahide Kohro ,  Yoshikazu Shibasaki ,  Takao Hamakubo ,  Tatsuhiko Kodama

Inventor： Takahide Kohro ,  Yoshikazu Shibasaki ,  Takao Hamakubo ,  Tatsuhiko Kodama

IPC: C12Q1/00

CPC classification number: A61K45/06 ,  A61K31/51 ,  A61K2300/00

Abstract: A nuclear transfer promoter for Cdc42 protein comprising an isoprenoid synthesis inhibitor and/or a geranylgeranyl transferase inhibitor such as an HMG-CoA synthase inhibitor, an HMG-CoA reductase inhibitor, an AMPK activator or a farnesyl pyrophosphoric acid synthase preparation; utilization thereof; a method therefor; a blood vessel remedy comprising the nuclear transfer promoter for Cdc42 protein as the active ingredient; and a method of screening a blood vessel remedy which comprises assaying the ability of Cdc42 protein to transfer into nucleus.

Abstract translation: 包含类异戊二烯合成抑制剂和/或香叶基香叶基转移酶抑制剂如HMG-CoA合成酶抑制剂，HMG-CoA还原酶抑制剂，AMPK活化剂或法呢基焦磷酸合成酶的Cdc42蛋白的核转移启动子; 使用; 一种方法; 包括Cdc42蛋白的核转移启动子作为活性成分的血管补救剂; 以及筛选血管补救的方法，其包括测定Cdc42蛋白转移到细胞核中的能力。