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1. 发明申请

US20120309754A1 PYRAZOLOPYRIMIDINE COMPOUNDS AND THEIR USE AS PDE10 INHIBITORS 有权
标题翻译：吡唑并嘧啶化合物及其作为PDE10抑制剂的用途
公开(公告)号：US20120309754A1
公开(公告)日：2012-12-06
申请号：US13579095
申请日：2011-02-25
申请人： Eiji Kawanishi , Mitsuya Hongu , Yoshihito Tanaka
发明人： Eiji Kawanishi , Mitsuya Hongu , Yoshihito Tanaka
IPC分类号： A61K31/519 , C07D487/04 , A61P25/00 , A61P25/22 , A61P25/30 , A61K31/5377 , A61P25/18
CPC分类号： C07D487/04
摘要： The present invention relates to a compound represented by formula [I]: wherein: R1 is hydrogen, halogen, lower alkyl or cyano; Ring A is an optionally substituted heterocyclic group; Ring B is an optionally substituted 3 to 6-membered monocyclic group; and Y is optionally substituted amino, optionally substituted cyclic amino, optionally substituted aliphatic 3 to 6-membered monocyclyloxy, optionally substituted lower alkyl or optionally substituted lower alkyl-O—, or a pharmaceutically acceptable salt thereof, and to their use as PDE10 inhibitor.
摘要翻译：本发明涉及由式[I]表示的化合物：其中：R 1是氢，卤素，低级烷基或氰基; 环A是任选取代的杂环基; 环B是任选取代的3至6元单环基团; 并且Y是任选取代的氨基，任选取代的环状氨基，任选取代的脂族3至6元单环氧基，任选取代的低级烷基或任选取代的低级烷基-O-或其药学上可接受的盐，以及它们作为PDE10抑制剂的用途。

2. 发明授权

US07935700B2 Morpholine compound 有权
标题翻译：吗啉化合物
公开(公告)号：US07935700B2
公开(公告)日：2011-05-03
申请号：US11662228
申请日：2005-09-08
申请人： Yoshihito Tanaka , Shuzo Takeda , Hidemitsu Higashi , Mamoru Matsuura , Fujio Kobayashi , Maiko Hamada , Minoru Tanaka
发明人： Yoshihito Tanaka , Shuzo Takeda , Hidemitsu Higashi , Mamoru Matsuura , Fujio Kobayashi , Maiko Hamada , Minoru Tanaka
IPC分类号： A61K31/535 , C07D417/12
CPC分类号： C07D265/30 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D495/04 , C07D513/04
摘要： A compound represented by the formula (1) wherein ring A is aryl optionally having substituent(s) and the like; ring B is arylene optionally having substituent(s) and the like; m=0-2; n=1-5; X is a bond and the like; Y is a bond and the like; and Z is hydrogen atom and the like or a pharmaceutically acceptable salt thereof, and a hydrate or solvate thereof have affinity for CCR3, and can be pharmaceutical products for the treatment and/or prophylaxis of immune or inflammatory diseases.
摘要翻译：由式（1）表示的化合物，其中环A为任选具有取代基的芳基等; 环B是任选具有取代基的亚芳基等; m = 0-2; n = 1-5; X是一个键等; Y是一个债券等; Z是氢原子等或其药学上可接受的盐，其水合物或溶剂化物对CCR3具有亲和性，可以是用于治疗和/或预防免疫或炎性疾病的药物。

3. 发明授权

US07790725B2 Thiazolidine derivatives and medicinal use thereof 有权
标题翻译：噻唑烷衍生物及其医药用途
公开(公告)号：US07790725B2
公开(公告)日：2010-09-07
申请号：US11774941
申请日：2007-07-09
申请人： Hiroshi Sakashita , Tomohiro Yoshida , Hiroshi Kitajima , Masahiro Takeuchi , Yoshihito Tanaka , Takuya Yoshimura , Fumihiko Akahoshi , Yoshiharu Hayashi
发明人： Hiroshi Sakashita , Tomohiro Yoshida , Hiroshi Kitajima , Masahiro Takeuchi , Yoshihito Tanaka , Takuya Yoshimura , Fumihiko Akahoshi , Yoshiharu Hayashi
IPC分类号： A61K31/435 , A61K31/496 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14
CPC分类号： C07D277/04
摘要： A thiazolidine derivative represented by the formula (I) wherein each symbol is as defined in the specification, and a pharmaceutically acceptable salt thereof exhibit a potent DPP-IV inhibitory activity, and can be provided as an agent for the prophylaxis or treatment of diabetes, an agent for the prophylaxis or treatment of obesity and the like.
摘要翻译：由式（I）表示的噻唑烷衍生物，其中每个符号如说明书中所定义，及其药学上可接受的盐显示出有效的DPP-IV抑制活性，并且可以作为预防或治疗糖尿病，用于预防或治疗肥胖症等的药剂。

4. 发明申请

US20070086988A1 Insulin expressing human pancreatic islet cell line capable of reversibly proliferating and use thereof 失效
标题翻译：胰岛素表达人胰岛细胞系，其能够可逆地增殖并使用
公开(公告)号：US20070086988A1
公开(公告)日：2007-04-19
申请号：US10578260
申请日：2003-11-10
申请人： Noriaki Tanaka , Naoya Kobayashi , Michiki Narushima , Yoshihito Tanaka
发明人： Noriaki Tanaka , Naoya Kobayashi , Michiki Narushima , Yoshihito Tanaka
IPC分类号： A61K48/00 , C12N5/08
CPC分类号： C12N5/0676 , A61K35/12 , C12N2510/04
摘要： A reversibly immortalized human pancreatic islet cell line containing an hTERT gene and an SV40T gene each interposed between a pair of LoxP sequences, characterized in that it is capable of producing insulin and enhancing expression of insulin after excising the hTERT gene and the SV40T gene, in particular, NAKT-13 (deposited with International Patent Organism Depository, National Institute of Advanced Industrial Science and Technology, address: AIST Tsukuba Central 6, 1-1, Higashi 1-Chome, Tsukuba-shi, Ibaraki-ken, 305-8566 Japan, deposited date: Sep. 4, 2003, accession number: FERM BP-08461) or a passage cell line thereof; a human pancreatic islet cell obtained by excising the hTERT gene and the SV40T gene from the reversibly immortalized human pancreatic islet cell line or passage cell line thereof; and use of these cells. By using the reversibly immortalized human pancreatic islet cell line of the invention insulin-producing cells can be easily and surely obtained in a number enough to meet the demand.
摘要翻译：一种含有hTERT基因和SV40T基因的可逆永生人胰岛细胞系，每个插入一对LoxP序列之间，其特征在于能够在切除hTERT基因和SV40T基因之后产生胰岛素并增强胰岛素的表达，特别是NAKT-13（保藏于国立先进工业科学与技术研究所国际专利生物保藏中心，地址：日本茨城市茨城市筑波市东1町1-1-1筑波中央6-1号日本305-8566 ，保藏日期：2003年9月4日，登录号：FERM BP-08461）或其传代细胞系; 通过从可逆永生化人胰岛细胞系或其传代细胞系中切除hTERT基因和SV40T基因获得的人胰岛细胞; 并使用这些细胞。通过使用本发明的可逆永生人胰岛细胞系，可以容易且可靠地获得足够数量的胰岛素产生细胞以满足需求。

5. 发明授权

US07115635B2 Benzylpiperidine compound 有权
标题翻译：苄基哌啶化合物
公开(公告)号：US07115635B2
公开(公告)日：2006-10-03
申请号：US10476149
申请日：2002-04-26
申请人： Masatoshi Kiuchi , Takanobu Kuroita , Hideo Tomozane , Shuuzou Takeda , Yoshihito Tanaka , Hidemitsu Higashi , Shigeki Kuwahara
发明人： Masatoshi Kiuchi , Takanobu Kuroita , Hideo Tomozane , Shuuzou Takeda , Yoshihito Tanaka , Hidemitsu Higashi , Shigeki Kuwahara
IPC分类号： A61K31/445 , C07D419/12
CPC分类号： C07D401/12 , A61K31/454 , A61K31/4545 , A61K31/4725 , A61K31/496 , A61K31/501 , A61K31/5377 , A61K31/55 , C07D413/12 , C07D417/12 , C07D417/14 , C07D491/10
摘要： The object of the present invention is to provide a compound having a treatment effect based on a chemokine inhibitory activity, which is satisfactory as a pharmaceutical product for oral administration.The present inventors have found that the following benzylpiperidine derivative (the formula (1)) has a chemokine inhibitory activity. Further intensive studies have resulted in successful enhancement of the chemokine inhibitory activity and stability in blood of the present compound, as well as the completion of the present invention. wherein each symbol is as defined in the specification.
摘要翻译：本发明的目的是提供一种具有基于趋化因子抑制活性的治疗效果的化合物，其作为用于口服给药的药物产品是令人满意的。本发明人发现以下苄基哌啶衍生物（式（1））具有趋化因子抑制活性。进一步的深入研究已经导致本发明化合物的趋化因子抑制活性和血液稳定性的成功增强以及本发明的完成。其中每个符号如说明书中所定义。

6. 发明授权

US4733465A Process for manufacturing electrical contact pin 失效
标题翻译：电接触针制造工艺
公开(公告)号：US4733465A
公开(公告)日：1988-03-29
申请号：US22783
申请日：1987-03-06
申请人： Yoshihito Tanaka
发明人： Yoshihito Tanaka
IPC分类号： H01R12/34 , H01R12/58 , H01R43/16
CPC分类号： H01R43/16 , H01R12/585 , Y10T29/49204
摘要： An electrical contact pin has a fixing part to be fitted into a through hole of a circuit board for fixing without using any solder. The fixing part has a substantially rectangular cross section. A pair of alternating recesses are provided on opposite sides of said rectangular section. A pair of corners closer to said recesses extend beyond said sides to form a pair of projected corners. A process for manufacturing such an electrical contact pin is characterized by the step of pressing a metal work having a substantially rectangular cross section to form said fixing part in a pair of metal dies. A pair of projections are provided on the bottoms of said dies to form said recesses. A pair of opposite sides of said dies are arranged so that there may be small spaces between said pair of sides and the opposite sides of said work before pressed. A part of said bottom of each die is made deeper than the rest of said bottom so as to form said projected corner when said work is squeezed.
摘要翻译：电接触销具有固定部分，以将其装配到电路板的通孔中，用于固定，而不使用任何焊料。固定部分具有大致矩形的截面。一对交替的凹槽设置在所述矩形部分的相对侧上。靠近所述凹部的一对角部延伸超过所述侧面以形成一对突出的角。用于制造这种电接触针的方法的特征在于：按压具有大致矩形横截面的金属制件以在一对金属模具中形成所述固定部分的步骤。在所述模具的底部设置有一对凸起以形成所述凹部。所述模具的一对相对侧被布置成使得在压制之前所述工件的所述一对侧面和相对侧之间可以具有小的空间。每个模具的所述底部的一部分比所述底部的其余部分更深，以便当所述工件被挤压时形成所述突出的角部。

7. 发明授权

US07629168B2 Insulin expressing human pancreatic islet cell line capable of reversibly proliferating and use thereof 失效
标题翻译：胰岛素表达人胰岛细胞系，其能够可逆地增殖并使用
公开(公告)号：US07629168B2
公开(公告)日：2009-12-08
申请号：US10578260
申请日：2003-11-10
申请人： Noriaki Tanaka , Naoya Kobayashi , Michiki Narushima , Yoshihito Tanaka
发明人： Noriaki Tanaka , Naoya Kobayashi , Michiki Narushima , Yoshihito Tanaka
IPC分类号： C12P5/06 , C12P21/06 , C12P21/04 , A61K48/00
CPC分类号： C12N5/0676 , A61K35/12 , C12N2510/04
摘要： A reversibly immortalized human pancreatic islet cell line containing an hTERT gene and an SV40T gene each interposed between a pair of LoxP sequences, characterized in that it is capable of producing insulin and enhancing expression of insulin after excising the hTERT gene and the SV40T gene, in particular, NAKT-13 (deposited with International Patent Organism Depository, National Institute of Advanced Industrial Science and Technology, address: AIST Tsukuba Central 6, 1-1, Higashi 1-Chome, Tsukuba-shi, Ibaraki-ken, 305-8566 Japan, deposited date: Sep. 4, 2003, accession number: FERM BP-08461) or a passage cell line thereof; a human pancreatic islet cell obtained by excising the hTERT gene and the SV40T gene from the reversibly immortalized human pancreatic islet cell line or passage cell line thereof; and use of these cells. By using the reversibly immortalized human pancreatic islet cell line of the invention insulin-producing cells can be easily and surely obtained in a number enough to meet the demand.
摘要翻译：一种含有hTERT基因和SV40T基因的可逆永生人胰岛细胞系，每个插入一对LoxP序列之间，其特征在于能够在切除hTERT基因和SV40T基因之后产生胰岛素并增强胰岛素的表达，特别是NAKT-13（保藏于国立先进工业科学与技术研究所国际专利生物保藏中心，地址：日本茨城市茨城市筑波市东1町1-1-1筑波中央6-1号日本305-8566 ，保藏日期：2003年9月4日，登录号：FERM BP-08461）或其传代细胞系; 通过从可逆永生化人胰岛细胞系或其传代细胞系中切除hTERT基因和SV40T基因获得的人胰岛细胞; 并使用这些细胞。通过使用本发明的可逆永生人胰岛细胞系，可以容易且可靠地获得足够数量的胰岛素产生细胞以满足需求。

8. 发明授权

US06633291B1 Method and apparatus for displaying an image 失效
标题翻译：用于显示图像的方法和装置
公开(公告)号：US06633291B1
公开(公告)日：2003-10-14
申请号：US09516208
申请日：2000-02-29
申请人： Hirofumi Sugitani , Yoshihito Tanaka , Masaaki Yoshikawa , Satoshi Ohtake , Noritsune Sekiguchi
发明人： Hirofumi Sugitani , Yoshihito Tanaka , Masaaki Yoshikawa , Satoshi Ohtake , Noritsune Sekiguchi
IPC分类号： G06T1510
CPC分类号： G06T15/10 , G06T17/00
摘要： A three-dimensional shape model indicating a first part is constructed and a three-dimensional shape that works as a transparent screen is disposed thereon continuously. A sight line direction is set and the three-dimensional shape model is displayed after rotated in accordance with the set sight line direction. A first two-dimensional image is constructed in accordance with the sight line direction, and a second two-dimensional image is constructed. The first two-dimensional image and the second two-dimensional image are combined with each other so as to construct a combined two-dimensional image. The combined two-dimensional image is assigned so that the part thereof corresponding to the first two-dimensional image agrees with the three-dimensional shape model, and the combined two-dimensional image is displayed visually.
摘要翻译：构成表示第一部分的三维形状模型，并且连续地设置作为透明屏幕的三维形状。设置视线方向，并且根据设定的视线方向旋转后显示三维形状模型。根据视线方向构造第一二维图像，构造第二二维图像。将第一二维图像和第二二维图像相互组合，以构成组合的二维图像。分配组合的二维图像，使得其对应于第一二维图像的部分与三维形状模型一致，并且组合的二维图像被目视显示。

9. 发明授权

US08030303B2 Salt of morpholine compound 有权
标题翻译：吗啉化合物盐
公开(公告)号：US08030303B2
公开(公告)日：2011-10-04
申请号：US12309196
申请日：2007-07-11
申请人： Katsuhiko Masuda , Shuzo Takeda , Yoshihito Tanaka
发明人： Katsuhiko Masuda , Shuzo Takeda , Yoshihito Tanaka
IPC分类号： A61K31/535 , C07D417/12
CPC分类号： C07D417/12
摘要： (2S)-[4-(Carboxymethyl)thiazol-2-ylthio]-N-{[4-(3,4-dichlorobenzyl)morpholin-2-yl]methyl}acetamide hydrobromide and a crystal thereof, which resist easy weight change caused by vapor sorption as compared to a free form, and are superior as drug substances of pharmaceutical products, and a production intermediate therefor are provided.
摘要翻译：（2S） - [4-（羧甲基）噻唑-2-基硫代] -N - {[4-（3,4-二氯苄基）吗啉-2-基]甲基}乙酰胺氢溴酸盐及其结晶，与游离形式相比，由蒸汽吸附引起，作为药物的药物，优选为其制造中间体。

10. 发明授权

US08969376B2 Pyrazolopyrimidine compounds and their use as PDE10 inhibitors 有权
标题翻译：吡唑并嘧啶化合物及其作为PDE10抑制剂的用途
公开(公告)号：US08969376B2
公开(公告)日：2015-03-03
申请号：US13579095
申请日：2011-02-25
申请人： Eiji Kawanishi , Mitsuya Hongu , Yoshihito Tanaka
发明人： Eiji Kawanishi , Mitsuya Hongu , Yoshihito Tanaka
IPC分类号： A61K31/415 , C07D293/00 , C07D487/00 , C07D487/04
CPC分类号： C07D487/04
摘要： The present invention relates to a compound represented by formula [I]: wherein: R1 is hydrogen, halogen, lower alkyl or cyano; Ring A is an optionally substituted heterocyclic group; Ring B is an optionally substituted 3 to 6-membered monocyclic group; and Y is optionally substituted amino, optionally substituted cyclic amino, optionally substituted aliphatic 3 to 6-membered monocyclyloxy, optionally substituted lower alkyl or optionally substituted lower alkyl-O—, or a pharmaceutically acceptable salt thereof, and to their use as PDE10 inhibitor.
摘要翻译：本发明涉及由式[I]表示的化合物：其中：R 1是氢，卤素，低级烷基或氰基; 环A是任选取代的杂环基; 环B是任选取代的3至6元单环基团; 并且Y是任选取代的氨基，任选取代的环状氨基，任选取代的脂族3至6元单环氧基，任选取代的低级烷基或任选取代的低级烷基-O-或其药学上可接受的盐，以及它们作为PDE10抑制剂的用途。

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