公开(公告)号：US08601650B2

公开(公告)日：2013-12-10

申请号：US12864027

申请日：2009-01-21

申请人： Takayoshi Nakagawa

发明人： Takayoshi Nakagawa

IPC分类号： F16B2/20

CPC分类号： F16B21/086 ,  Y10T24/30 ,  Y10T24/309 ,  Y10T24/44026 ,  Y10T24/45105

摘要： An attachment structure for a clip including a mounting member, a retaining hole formed in the mounting member, and a rib. An elastic retaining piece of the clip, while elastically deformed, is inserted into the retaining hole from an outer side of the mounting member toward an inner side to be retained therein. The rib is disposed around the retaining hole and is formed integrally with the mounting member. The rib includes a first rib formed on the inner side of the mounting member and a second rib formed outside, and concentric to, the first rib. The first rib has a thickness such that a clip press-contacting piece abuts the outer side of the mounting member when the elastic retaining piece is inserted in the retaining hole and retained on the rib, and the second rib has a thickness larger than the thickness of the first rib.

摘要翻译： 一种用于夹子的附接结构，包括安装构件，形成在安装构件中的保持孔和肋。 夹子的弹性保持片弹性变形时，从安装部件的外侧向内侧插入保持孔，保持在内侧。 肋设置在保持孔周围并与安装构件一体地形成。 所述肋包括形成在所述安装构件的内侧上的第一肋和形成在所述第一肋之外并且与所述第一肋同心的第二肋。 第一肋具有这样的厚度，使得当弹性保持片插入保持孔并保持在肋上时，夹压接触件邻接安装构件的外侧，并且第二肋的厚度大于厚度 的第一个肋骨。

公开(公告)号：US6082103A

公开(公告)日：2000-07-04

申请号：US97494

申请日：1998-06-15

申请人： Shigeki Sugiura ,  Takayoshi Nakagawa ,  Yasuhiro Oi

发明人： Shigeki Sugiura ,  Takayoshi Nakagawa ,  Yasuhiro Oi

IPC分类号： F01N13/00 ,  F01N13/08 ,  F01N13/10 ,  F01N99/00 ,  F02D35/00 ,  F01N7/10

CPC分类号： F01N13/08 ,  F01N13/008 ,  F01N13/10

摘要： An exhaust manifold comprising a plurality of exhaust pipes and a merging portion applies exhaust gas from each cylinder uniformly to an oxygen sensor in a merging portion at low speed thereby improving the durability of the oxygen sensor. A downstream forward end of each exhaust pipe of the exhaust manifold, when connected to an inlet wall of a merging case having the oxygen sensor mounted on a side thereof, is formed in the shape of a bell mouth for leading the exhaust gas to the oxygen sensor. Each exhaust pipe is fixedly welded to the merging case at a position upstream of the forward end of the bell mouth. An angle formed by lines perpendicular to tangential lines at starting and ending points of a curved portion of the bell mouth at the forward end of the exhaust pipe is set in the range of 45.degree. to 75.degree.. As a result, the bell mouth spreads over the whole interior of the merging case and reduces a flow rate of the exhaust gas, and part of the exhaust gas flows toward the oxygen sensor. The oxygen sensor is thus more evenly exposed to the exhaust gas and has increased durability.

摘要翻译： 包括多个排气管和合流部的排气歧管以低速将来自每个气缸的排气均匀地施加到合流部中的氧传感器，从而提高氧传感器的耐久性。 当排气歧管的每个排气管的下游前端连接到具有安装在其一侧的氧传感器的合并壳体的入口壁上时，形成为将排气引导到氧气的喇叭口的形状 传感器。 每个排气管在喇叭口前端上游的一个位置固定地焊接到合并壳体上。 在排气管前端处的喇叭口的弯曲部分的起点和终点处垂直于切线的线形成的角度设定在45°至75°的范围内。 结果，喇叭口扩展在合并壳体的整个内部，并且降低了废气的流量，并且一部分排气朝向氧传感器流动。 因此，氧传感器更均匀地暴露于废气并且具有增加的耐久性。

公开(公告)号：US08748437B2

公开(公告)日：2014-06-10

申请号：US13700935

申请日：2011-05-31

申请人： Hiroyuki Hayashi ,  Takayoshi Nakagawa ,  Koichi Miyazaki

发明人： Hiroyuki Hayashi ,  Takayoshi Nakagawa ,  Koichi Miyazaki

IPC分类号： A61K31/519

CPC分类号： C07D495/04 ,  A61K31/519

摘要： The invention provides a crystal of 2-(3,4-dichlorobenzyl)-5-methyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidine-6-carboxylic acid (which has the chemical structure shown below) and a mixed crystal comprising such a crystal. The invention also provides methods of producing such crystals, pharmaceutical compositions comprising such crystals, and methods of modulating phosphodiesterase-9 activity and treating disorders such as overactive bladder syndrome by administration of an effective amount of the crystals.

摘要翻译： 本发明提供2-（3,4-二氯苄基）-5-甲基-4-氧代-3,4-二氢噻吩并[2,3-d]嘧啶-6-甲酸（其化学结构如下所示） ）和包含这种晶体的混合晶体。 本发明还提供了生产这种晶体的方法，包含这种晶体的药物组合物，以及通过施用有效量的晶体来调节磷酸二酯酶-9活性和治疗诸如膀胱过度活动症综合征的疾病的方法。

公开(公告)号：US08623909B2

公开(公告)日：2014-01-07

申请号：US12991155

申请日：2009-05-08

申请人： Hajime Nawata ,  Toshihiko Yanase ,  Takayoshi Nakagawa

发明人： Hajime Nawata ,  Toshihiko Yanase ,  Takayoshi Nakagawa

IPC分类号： C07D311/78 ,  A61K31/35

CPC分类号： A61K31/57 ,  A61K31/56 ,  G01N33/5044 ,  G01N33/689 ,  G01N33/6893 ,  G01N33/74 ,  G01N2800/02 ,  G01N2800/042 ,  G01N2800/044 ,  G01N2800/321

摘要： Disclosed is a method for screening a compound having an activity that selectively modulates an androgen receptor, comprising a step of measuring the mRNA expression level of prostate-specific antigen or the production level of prostate-specific antigen in prostate cancer cells by contacting a test substance with the prostate cancer cells, and a step of measuring the mRNA expression level of uncoupling protein 1 or the production level of uncoupling protein 1 in adipocytes by contacting a test substance with the adipocytes. Additionally disclosed is a selective androgen receptor modulator, comprising as an active ingredient thereof a compound represented by any of structural formulas (I) to (III), and a composition for preventing or treating a lifestyle-related disease, comprising as an active ingredient thereof said selective androgen receptor modulator.

摘要翻译： 公开了一种筛选具有选择性调节雄激素受体活性的化合物的方法，包括通过使测试物质接触测量前列腺癌细胞中前列腺特异性抗原的mRNA表达水平或前列腺特异性抗原的产生水平的步骤 与前列腺癌细胞，以及通过使测试物质与脂肪细胞接触来测量解偶联蛋白1的mRNA表达水平或脂肪细胞中解偶联蛋白1的产生水平的步骤。 另外公开了一种选择性雄激素受体调节剂，其包含作为其活性成分的由结构式（I）至（III）中任一项表示的化合物和用于预防或治疗与生活方式有关的疾病的组合物，其包含作为其活性成分 所述选择性雄激素受体调节剂。

公开(公告)号：US20130123279A1

公开(公告)日：2013-05-16

申请号：US13700935

申请日：2011-05-31

申请人： Hiroyuki Hayashi ,  Takayoshi Nakagawa ,  Koichi Miyazaki

发明人： Hiroyuki Hayashi ,  Takayoshi Nakagawa ,  Koichi Miyazaki

IPC分类号： A61K31/519 ,  C07D495/04

CPC分类号： C07D495/04 ,  A61K31/519

摘要： Crystals are obtained by heating an aqueous suspension of 2-(3,4-dichlorobenzyl)-5-methyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidine-6-carboxylic acid. Novel crystals are obtained by adjusting the heating temperature and/or duration.

摘要翻译： 通过加热2-（3,4-二氯苄基）-5-甲基-4-氧代-3,4-二氢噻吩并[2,3-d]嘧啶-6-甲酸的水悬浮液获得晶体。 通过调节加热温度和/或持续时间获得新的晶体。

公开(公告)号：US20100293762A1

公开(公告)日：2010-11-25

申请号：US12864027

申请日：2009-01-21

申请人： Takayoshi Nakagawa

发明人： Takayoshi Nakagawa

IPC分类号： F16B2/20

CPC分类号： F16B21/086 ,  Y10T24/30 ,  Y10T24/309 ,  Y10T24/44026 ,  Y10T24/45105

摘要： To provide an attachment structure of a clip in which merely by adding a simple construction to a wall body of a mounting member, deformation of that portion around a retaining hole is eliminated, and the clip can be attached in a stable condition. In the attachment structure of the clip (1) which is attached by inserting part thereof into the retaining hole (11) formed in the wall body (10) of the mounting member and by retaining it therein, and in the attachment structure of the clip including elastic retaining pieces (4, 4) which are elastically deformed and inserted into the retaining hole (11) to be retained in the retaining hole (11), a first rib (12) is formed integrally on the wall body (10) and is disposed around the retaining hole (11) in the wall body (10), and a second rib (13) is further formed on the wall body (10) in surrounding relation to the periphery of the elastic retaining pieces (4, 4).

摘要翻译： 为了提供夹子的附接结构，其中仅通过向安装构件的壁体添加简单的构造，消除了围绕保持孔的部分的变形，并且夹子可以在稳定的状态下被安装。 在夹子（1）的安装结构中，其通过将其插入到形成在安装构件的壁体（10）中的保持孔（11）中并通过将其保持在其中并在夹子的附接结构 包括弹性变形并插入到保持孔（11）中以保持在保持孔（11）中的弹性保持件（4,4），第一肋（12）一体形成在壁体（10）上，并且 围绕所述壁体（10）中的所述保持孔（11）设置，并且在所述壁体（10）上进一步形成围绕所述弹性保持片（4,4）的周边的第二肋（13） 。

公开(公告)号：US20110104066A1

公开(公告)日：2011-05-05

申请号：US12991155

申请日：2009-05-08

申请人： Hajime Nawata ,  Toshihiko Yanase ,  Takayoshi Nakagawa

发明人： Hajime Nawata ,  Toshihiko Yanase ,  Takayoshi Nakagawa

IPC分类号： A61K49/00 ,  C12Q1/68 ,  C07D311/78 ,  C07C49/563 ,  A61K31/573 ,  A61K31/585 ,  A61K31/352 ,  A61P3/04 ,  A61P3/10 ,  A61P3/06 ,  A61P9/12

CPC分类号： A61K31/57 ,  A61K31/56 ,  G01N33/5044 ,  G01N33/689 ,  G01N33/6893 ,  G01N33/74 ,  G01N2800/02 ,  G01N2800/042 ,  G01N2800/044 ,  G01N2800/321

摘要： Disclosed is a method for the screening of a compound having an activity to selectively modulate an androgen receptor. The method comprises the steps of: contacting a substance to be tested with a prostate cancer cell and measuring the level of expression of mRNA for a prostate-specific antigen or the level of production of the prostate-specific antigen in the prostate cancer cell; and contacting the substance with an adipocyte and measuring the level of expression of mRNA for uncoupling protein-1 or the level of production of uncoupling protein-1 in the adipocyte. Also disclosed is a selective androgen receptor modulator comprising a compound represented by any one formula selected from the structural formulae (I) to (III) as an active ingredient. Further disclosed is a composition for preventing or treating lifestyle-related diseases, which comprises the selective androgen receptor modulator.

摘要翻译： 披露了筛选具有选择性调节雄激素受体活性的化合物的方法。 该方法包括以下步骤：使待测物质与前列腺癌细胞接触，并测量前列腺特异性抗原mRNA表达水平或前列腺癌细胞中前列腺特异性抗原产生水平; 并将该物质与脂肪细胞接触并测量mRNA的表达水平以解偶联蛋白-1或脂肪细胞中解偶联蛋白-1的产生水平。 还公开了包含由选自结构式（I）至（III）的任何一种式表示的化合物作为活性成分的选择性雄激素受体调节剂。 进一步公开的是用于预防或治疗生活方式相关疾病的组合物，其包含选择性雄激素受体调节剂。

公开(公告)号：US20060189625A1

公开(公告)日：2006-08-24

申请号：US10558253

申请日：2004-05-07

申请人： Shigehiro Takegawa ,  Shigeki Iwashita ,  Makoto Okada ,  Takayoshi Nakagawa ,  Naoyuki Koizumi ,  Tomohito Fujii

发明人： Shigehiro Takegawa ,  Shigeki Iwashita ,  Makoto Okada ,  Takayoshi Nakagawa ,  Naoyuki Koizumi ,  Tomohito Fujii

IPC分类号： A61K31/496 ,  A61K31/495 ,  A61K31/445 ,  C07D211/54

CPC分类号： C07D211/32 ,  C07D211/14

摘要： This invention provides cyclicamino-phenyl sulfamate derivatives represented by a formula wherein each of R1 and R2 stands for hydrogen or lower alkyl; each of R3 and R4 stands for hydrogen, halogen, cyano or the like; A stands for nitrogen or CH; B stands for CH2, SO2, CO, optionally substituted phenyl or the like; and R5 stands for alkyl, phenyl, amino or the like, or salts thereof which exhibit excellent steroid sulfatase inhibitory activity and are useful for prevention or treatment of diseases associated with steroids such as estrogen, androgen and the like.

摘要翻译： 本发明提供由下式表示的环氨基 - 苯基氨基磺酸酯衍生物，其中R 1和R 2各自代表氢或低级烷基; R 3和R 4中的每一个代表氢，卤素，氰基等; A代表氮或CH; B代表CH 2，SO 2，CO，任选取代的苯基等; R 5表示烷基，苯基，氨基等，或其盐，其表现出优异的类固醇硫酸酯酶抑制活性，并且可用于预防或治疗与类固醇如雌激素，雄激素相关的疾病， 喜欢。

公开(公告)号：US06762205B1

公开(公告)日：2004-07-13

申请号：US10019693

申请日：2002-01-03

申请人： Naoyuki Koizumi ,  Makoto Okada ,  Shigeki Iwashita ,  Shigehiro Takegawa ,  Takayoshi Nakagawa ,  Hiroo Takahashi ,  Tomohito Fujii

发明人： Naoyuki Koizumi ,  Makoto Okada ,  Shigeki Iwashita ,  Shigehiro Takegawa ,  Takayoshi Nakagawa ,  Hiroo Takahashi ,  Tomohito Fujii

IPC分类号： A61K3118

CPC分类号： C07D213/30 ,  C07C307/02 ,  C07D213/74 ,  C07D213/82 ,  C07D231/12 ,  C07D233/56 ,  C07D239/42 ,  C07D241/20 ,  C07D249/08 ,  C07D277/24 ,  C07D333/20 ,  C07D333/38

摘要： Phenyl sulfamate derivatives represented by the following formula or salts thereof have a powerful inhibitory effect on steroid sulfatase and are hence useful for the prophylaxis or treatment of diseases associated with steroids such as estrogens, such as breast cancer, corpus uteri cancer, endometrial hyperplasia, infertility, endometriosis, adenomyosis uteri, autoimmune disease, dementia or Alzheimer's disease. wherein R1 and R2 each independently represent a hydrogen atom or a lower alkyl group; R3 represents a hydrogen atom, a halogen atom, a lower alkyl group, —OSO2NR1R2, a lower alkanoylamino group, a nitro group or a cyano group; and A represents a substituted or unsubstituted phenyl group, a group of the formula —X—NR4R5, or the like.

摘要翻译： 由下式表示的氨基磺酸苯酯衍生物或其盐对类固醇硫酸酯酶具有强大的抑制作用，因此可用于预防或治疗与类固醇相关的疾病，例如乳腺癌，子宫内膜增生症，子宫内膜增生症，不育症等雌激素 ，子宫内膜异位症，子宫腺肌症，自身免疫性疾病，痴呆或阿尔茨海默病。其中R 1和R 2各自独立地表示氢原子或低级烷基; R 3表示氢原子，卤素原子，低级烷基，-OSO 2 NR 1 R 2，低级烷酰基氨基，硝基或氰基; A表示取代或未取代的苯基，式-X-NR 4 R 5的基团等。

公开(公告)号：US07449466B2

公开(公告)日：2008-11-11

申请号：US10558253

申请日：2004-05-07

申请人： Shigehiro Takegawa ,  Shigeki Iwashita ,  Makoto Okada ,  Takayoshi Nakagawa ,  Naoyuki Koizumi ,  Tomohito Fujii

发明人： Shigehiro Takegawa ,  Shigeki Iwashita ,  Makoto Okada ,  Takayoshi Nakagawa ,  Naoyuki Koizumi ,  Tomohito Fujii

IPC分类号： A61K31/497 ,  A61K31/4965 ,  A61K31/445 ,  A01N43/40 ,  C07D401/00 ,  C07D241/04 ,  C07D295/00 ,  C07D211/40 ,  C07D211/54

CPC分类号： C07D211/32 ,  C07D211/14

摘要： This invention provides cyclicamino-phenyl sulfamate derivatives represented by a formula wherein each of R1 and R2 stands for hydrogen or lower alkyl; each of R3 and R4 stands for hydrogen, halogen, cyano or the like; A stands for nitrogen or CH; B stands for CH2, SO2, CO, optionally substituted phenyl or the like; and R5 stands for alkyl, phenyl, amino or the like, or salts thereof which exhibit excellent steroid sulfatase inhibitory activity and are useful for prevention or treatment of diseases associated with steroids such as estrogen, androgen and the like.

摘要翻译： 本发明提供由下式表示的环氨基 - 苯基氨基磺酸酯衍生物，其中R 1和R 2各自代表氢或低级烷基; R 3和R 4中的每一个代表氢，卤素，氰基等; A代表氮或CH; B代表CH 2，SO 2，CO，任选取代的苯基等; R 5表示烷基，苯基，氨基等，或其盐，其表现出优异的类固醇硫酸酯酶抑制活性，并且可用于预防或治疗与类固醇如雌激素，雄激素相关的疾病， 喜欢。