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1. 发明授权

US08772297B2 TGF-β signal transduction inhibitor 有权
标题翻译： TGF- 信号转导抑制剂
公开(公告)号：US08772297B2
公开(公告)日：2014-07-08
申请号：US13579843
申请日：2011-02-17
申请人： Hideaki Kakeya , Akira Hattori , Yasuaki Takasu , Nobutaka Fujii , Shinya Oishi , Soichi Kojima , Mitsuko Hara
发明人： Hideaki Kakeya , Akira Hattori , Yasuaki Takasu , Nobutaka Fujii , Shinya Oishi , Soichi Kojima , Mitsuko Hara
IPC分类号： A61K31/495 , C07D295/104
CPC分类号： C07D295/104 , C07D211/28 , C07D295/18 , C07D405/12
摘要： The present invention provides a compound represented by the following formula (I) or a physiologically acceptable salt thereof, and use thereof for the prophylaxis or treatment of TGF-β-related diseases: wherein Y is a hydrogen atom and the like; R2 is and the like; R3 is —NR8—R9— and the like; R4, R5, R6 and R7 are the same or different and each is a hydrogen atom and the like; and X is and the like.
摘要翻译：本发明提供由下式（I）表示的化合物或其生理学上可接受的盐，及其用于预防或治疗TGF-β相关疾病的用途：其中Y为氢原子等; R2是等等; R3是-NR8-R9-等; R4，R5，R6和R7相同或不同，各自为氢原子等; X等。

2. 发明申请

US20130045977A1 TGF-beta SIGNAL TRANSDUCTION INHIBITOR 有权
标题翻译： TGF-β信号转导抑制剂
公开(公告)号：US20130045977A1
公开(公告)日：2013-02-21
申请号：US13579843
申请日：2011-02-17
申请人： Hideaki Kakeya , Akira Hattori , Yasuaki Takasu , Nobutaka Fujii , Shinya Oishi , Soichi Kojima , Mitsuko Hara
发明人： Hideaki Kakeya , Akira Hattori , Yasuaki Takasu , Nobutaka Fujii , Shinya Oishi , Soichi Kojima , Mitsuko Hara
IPC分类号： A61K31/445 , C07D401/12 , A61P25/00 , C07D413/12 , A61K31/5377 , A61P35/00 , C07D211/32 , A61K31/4545
CPC分类号： C07D295/104 , C07D211/28 , C07D295/18 , C07D405/12
摘要： The present invention provides a compound represented by the following formula (I) or a physiologically acceptable salt thereof, and use thereof for the prophylaxis or treatment of TGF-β-related diseases: wherein Y is a hydrogen atom and the like; R2 is and the like; R3 is —NR8—R9— and the like; R4, R5, R6 and R7 are the same or different and each is a hydrogen atom and the like; and X is and the like.
摘要翻译：本发明提供由下式（I）表示的化合物或其生理学上可接受的盐，及其用于预防或治疗TGF-β相关疾病的用途：其中Y为氢原子等; R2是等等; R3是-NR8-R9-等; R4，R5，R6和R7相同或不同，各自为氢原子等; X等。

3. 发明授权

US08592379B2 Metastin derivative and use thereof 有权
标题翻译： Metastin衍生物及其用途
公开(公告)号：US08592379B2
公开(公告)日：2013-11-26
申请号：US12990161
申请日：2009-04-28
申请人： Nobutaka Fujii , Shinya Oishi , Kenji Tomita
发明人： Nobutaka Fujii , Shinya Oishi , Kenji Tomita
IPC分类号： A61K38/06 , A61K38/07 , A61K38/00 , A61P25/28 , A61P35/00 , C07K5/00 , C07K7/00 , C07K16/00 , C07K17/00
CPC分类号： C07K14/4703 , A61K38/00 , C07K7/02
摘要： The present invention provides a metastin derivative represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof, or a pharmaceutical composition containing it. The metastin derivative or a salt thereof is superior in blood stability, and has a cancer metastasis suppressive action or cancer growth suppressive action.
摘要翻译：本发明提供由式（I）表示的亚氨基衍生物：其中每个符号如说明书中所定义，或其盐或含有它的药物组合物。所述转氨酶衍生物或其盐具有优异的血液稳定性，具有癌转移抑制作用或癌生长抑制作用。

4. 发明授权

US08183212B2 Compound having GPR54 agonistic activity 有权
标题翻译：具有GPR54激动作用的化合物
公开(公告)号：US08183212B2
公开(公告)日：2012-05-22
申请号：US12298200
申请日：2006-10-24
申请人： Nobutaka Fujii , Shinya Oishi , Kenji Tomita , Ayumu Niida
发明人： Nobutaka Fujii , Shinya Oishi , Kenji Tomita , Ayumu Niida
IPC分类号： A61K38/08 , C07K5/00 , C07K7/00 , C07K16/00 , C07K17/00
CPC分类号： C07K5/0808 , A61K38/00 , C07K7/06
摘要： The present invention provides a compound represented by the following formula (1); wherein R1 is an aryl group etc.; R2 is —CO—NH— etc.; R3 is a methyl group having an aromatic group or a cycloalkyl group; R4 is a hydrogen atom etc.; R5 is a methyl group having an aromatic group; and R6 is an amino group or an N-alkyl substituted amino group, having a low-molecular weight and a superior GPR54 agonist activity, and a pharmaceutical composition containing the compound.
摘要翻译：本发明提供由下式（1）表示的化合物。其中R1是芳基等; R2是-CO-NH-等; R3是具有芳基或环烷基的甲基; R4是氢原子等。 R5是具有芳基的甲基; 和R6是具有低分子量和优异的GPR54激动剂活性的氨基或N-烷基取代的氨基，以及含有该化合物的药物组合物。

5. 发明申请

US20110039786A1 METASTIN DERIVATIVE AND USE THEREOF 有权
标题翻译：衍生物及其用途
公开(公告)号：US20110039786A1
公开(公告)日：2011-02-17
申请号：US12990161
申请日：2009-04-28
申请人： Nobutaka Fujii , Shinya Oishi , Kenji Tomita
发明人： Nobutaka Fujii , Shinya Oishi , Kenji Tomita
IPC分类号： A61K38/06 , C07K5/097 , A61P35/00 , A61P1/18 , A61P25/28 , A61P35/02
CPC分类号： C07K14/4703 , A61K38/00 , C07K7/02
摘要： The present invention provides a metastin derivative represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof, or a pharmaceutical composition containing it. The metastin derivative or a salt thereof is superior in blood stability, and has a cancer metastasis suppressive action or cancer growth suppressive action.
摘要翻译：本发明提供由式（I）表示的亚氨基衍生物：其中每个符号如说明书中所定义，或其盐或含有它的药物组合物。所述转氨酶衍生物或其盐具有优异的血液稳定性，具有癌转移抑制作用或癌生长抑制作用。

6. 发明授权

US06800611B2 Metastin derivatives and their use 有权
标题翻译： Metastin衍生物及其用途
公开(公告)号：US06800611B2
公开(公告)日：2004-10-05
申请号：US10337105
申请日：2003-01-06
申请人： Nobutaka Fujii , Ryuichiro Doi , Shinya Oishi
发明人： Nobutaka Fujii , Ryuichiro Doi , Shinya Oishi
IPC分类号： A61K3807
CPC分类号： C07K5/1016 , A61K38/00
摘要： The invention relates to metastin derivatives represented by the formula: X-AA1-AA2-AA3-AA4-Z (I), or a salt thereof, or a pro-drug thereof, which have cancer metastatis suppressing activity and cancer proliferation suppressing activity. The invention also relates to the use of these derivatives as drugs for preventing or treating cancers.
摘要翻译：本发明涉及具有癌症转移抑制活性和癌细胞增殖抑制活性的由式X-AA1-AA2-AA3-AA4-Z（I）表示的亚铁蛋白衍生物或其盐或其前体药物。本发明还涉及这些衍生物作为预防或治疗癌症的药物的用途。

7. 发明申请

US20110014649A1 METHOD FOR PRODUCTION OF N36-BINDING PEPTIDE 审中-公开
标题翻译：生产N36-结合肽的方法
公开(公告)号：US20110014649A1
公开(公告)日：2011-01-20
申请号：US12296805
申请日：2007-07-26
申请人： Hiroko Tsutsumi , Hiroki Ishida , Hiromoto Hisada , Makiko Mizumoto , Yoji Hata , Nobutaka Fujii , Masao Matsuoka , Eiichi Kodama , Shinya Oishi
发明人： Hiroko Tsutsumi , Hiroki Ishida , Hiromoto Hisada , Makiko Mizumoto , Yoji Hata , Nobutaka Fujii , Masao Matsuoka , Eiichi Kodama , Shinya Oishi
IPC分类号： C12P21/06 , C12N9/26
CPC分类号： C07K14/005 , A61K38/00 , C12N2740/15022 , C12N2740/16122
摘要： The present invention relates to the production of an N36-binding peptide at low cost and in a large quantity utilizing a microorganism. More specifically, the present invention relates to a method for producing an N36-binding peptide comprising introducing a recombinant vector into which a DNA molecule encoding an N36-binding peptide that binds to an N36 protein derived from a retrovirus that causes immunodeficiency in a mammal has been incorporated into E. coli as a host to produce a transformant.
摘要翻译：本发明涉及以低成本和大量利用微生物生产N36结合肽。更具体地说，本发明涉及一种N36-结合肽的制造方法，其特征在于，包括引入重组载体，其中编码与衍生自引起哺乳动物免疫缺陷的逆转录病毒的N36蛋白结合的N36结合肽的DNA分子作为宿主掺入大肠杆菌以产生转化体。

8. 发明申请

US20100160241A1 NOVEL COMPOUND HAVING GPR54 AGONISTIC ACTIVITY 有权
标题翻译：具有GPR54激活活性的新化合物
公开(公告)号：US20100160241A1
公开(公告)日：2010-06-24
申请号：US12298200
申请日：2006-10-24
申请人： Nobutaka Fujii , Shinya Oishi , Kenji Tomita , Ayumu Niida
发明人： Nobutaka Fujii , Shinya Oishi , Kenji Tomita , Ayumu Niida
IPC分类号： A61K38/08 , C07K5/103 , C07K7/06 , A61K38/07 , A61P35/00
CPC分类号： C07K5/0808 , A61K38/00 , C07K7/06
摘要： The present invention provides a compound represented by the following formula (1); wherein R1 is an aryl group etc.; R2 is —CO—NH— etc.; R3 is a methyl group having an aromatic group or a cycloalkyl group; R4 is a hydrogen atom etc.; R5 is a methyl group having an aromatic group; and R6 is an amino group or an N-alkyl substituted amino group, having a low-molecular weight and a superior GPR54 agonist activity, and a pharmaceutical composition containing the compound.
摘要翻译：本发明提供由下式（1）表示的化合物。其中R1是芳基等; R2是-CO-NH-等; R3是具有芳基或环烷基的甲基; R4是氢原子等。 R5是具有芳基的甲基; 和R6是具有低分子量和优异的GPR54激动剂活性的氨基或N-烷基取代的氨基，以及含有该化合物的药物组合物。

9. 发明授权

US08917452B2 Optical diffusion film 有权
标题翻译：光扩散膜
公开(公告)号：US08917452B2
公开(公告)日：2014-12-23
申请号：US13080822
申请日：2011-04-06
申请人： Yuki Ohashi , Tomoyuki Kitagawa , Naoto Niiya , Shinya Oishi
发明人： Yuki Ohashi , Tomoyuki Kitagawa , Naoto Niiya , Shinya Oishi
IPC分类号： G02B5/02 , G02F1/1335
CPC分类号： G02B5/0221 , G02B5/0205 , G02B5/0278 , G02F1/133504
摘要： Measurement reference lengths of length and width are set with respect to a convex structure, and an average of vertical distances between tip points and bottom points inside a measurement reference area is calculated as an average height. An average of horizontal distances between the tip points and bottom points is calculated as an average distance. A value obtained by dividing the average height by the average distance provides a gradient ratio. An inverse tangent of the gradient ratio provides an average gradient angle. When the average gradient angle ranges from 5 degrees to 15 degrees and a standard deviation of average gradient angle ranges from 30% to 40% of the average gradient angle, a regular reflectance at a regular reflection angle with respect to incident light of an angle of 30 degrees from a normal direction of the film surface is 1% or less.
摘要翻译：长度和宽度的测量参考长度相对于凸形结构设置，并且将测量参考区域内的尖点和底点之间的垂直距离的平均值计算为平均高度。平均距离计算出尖点和底点之间的水平距离的平均值。通过将平均高度除以平均距离而获得的值提供了梯度比。梯度比的反正切提供平均梯度角。当平均梯度角为5度至15度，平均梯度角的标准偏差范围为平均梯度角的30％至40％时，相对于角度为从膜表面的法线方向30度为1％以下。

10. 发明申请

US20080139456A1 Macrocyclic Sh2 Domain Binding Inhibitors 审中-公开
标题翻译：大环Sh2结构域结合抑制剂
公开(公告)号：US20080139456A1
公开(公告)日：2008-06-12
申请号：US11575723
申请日：2005-09-30
申请人： Terrence R. Burke , Zhen-Dan Shi , Shinya Oishi , Fa Liu
发明人： Terrence R. Burke , Zhen-Dan Shi , Shinya Oishi , Fa Liu
IPC分类号： A61K38/12 , C07K5/12
CPC分类号： C07K5/06113 , A61K38/00 , C07K5/06191 , C07K5/0812 , C07K5/0827
摘要： Disclosed are compounds for inhibiting the binding of an SH2 domain-containing protein, for example, a compound of formula (I): FORMULA (I) wherein R1 is a lipophile; R2, in combination with the phenyl ring, is a phenylphosphate mimic group or a protected phenylphosphate mimic group; R3 is, for example, hydrogen, azido, amino, oxalylamino, carboxy alkyl, alkoxycarbonyl alkyl, aminocarbonyl alkyl, or alkyl carbonylamino; R6 is a linker; AA is an amino acid; and n is 1 to 6; or a pharmaceutically acceptable salt, stereoisomer, solvate, or hydrate thereof. Also disclosed are pharmaceutical compositions and methods of use of such compounds.
摘要翻译：公开了用于抑制含SH2结构域的蛋白质，例如式（I）的化合物：式（I）的化合物：其中R1是亲油性物质; R2与苯环组合是苯基磷酸酯模拟基团或被保护的苯基磷酸酯模拟基团; R3是例如氢，叠氮基，氨基，草酰氨基，羧基烷基，烷氧基羰基烷基，氨基羰基烷基或烷基羰基氨基; R6是连接体; AA是氨基酸; n为1〜6; 或其药学上可接受的盐，立体异构体，溶剂合物或水合物。还公开了药物组合物和这些化合物的使用方法。

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