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1. 发明专利

IL261055A Tetrahydroisoquinoline derivatives 未知
公开(公告)号：IL261055A
公开(公告)日：2021-03-25
申请号：IL26105518
申请日：2018-08-08
申请人： ASTELLAS PHARMA INC , CYTOKINETICS INC , IPPEI SATO , TAKASHI KAMIKUBO , MASANORI MIURA , YUJI MATSUSHIMA , HIROAKI TANAKA , YASUHIRO SHIINA , SUSUMU YAMAKI , TOMOYUKI SAITO , HIROSHI KIYOHARA , MUNEMICHI OHE , KAYOKO MIHARA , BRADLEY PAUL MORGAN , FADY MALIK , SCOTT EMILE COLLIBEE , LUKE ASHCRAFT , PU PING LU , JEFFREY MICHAEL WARRINGTON , MARC GARARD
发明人： IPPEI SATO , TAKASHI KAMIKUBO , MASANORI MIURA , YUJI MATSUSHIMA , HIROAKI TANAKA , YASUHIRO SHIINA , SUSUMU YAMAKI , TOMOYUKI SAITO , HIROSHI KIYOHARA , MUNEMICHI OHE , KAYOKO MIHARA , BRADLEY PAUL MORGAN , FADY MALIK , SCOTT EMILE COLLIBEE , LUKE ASHCRAFT , PU-PING LU , JEFFREY MICHAEL WARRINGTON , MARC GARARD
IPC分类号： A61K31/47 , A61P21/00
摘要： Novel tetrahydroisoquinoline derivative compounds are disclosed herein that may be used as an active ingredient for a pharmaceutical composition, and in particular, for a pharmaceutical composition useful for preventing or treating a disease or condition responsive to modulation of the contractility of the skeletal sarcomere. This may be accomplished, for example, by modulation of the troponin complex of the fast skeletal muscle sarcomere through one or more of fast skeletal myosin, actin, tropomyosin, troponin C, troponin I, and troponin T, and fragments and isoforms thereof. The tetrahydroisoquinoline derivative compounds can thus be used as an agent for preventing or treating 1) neuromuscular disorders, 2) disorders of voluntary muscle, 3) CNS disorders in which muscle weakness, atrophy, and fatigue are prominent symptoms, 4) muscle symptoms stemming from systemic disorders, and 5) dysfunctions of pelvic floor and urethral/anal sphincter muscle.

2. 发明专利

IL261055D0 Tetrahydroisoquinoline derivatives 未知
公开(公告)号：IL261055D0
公开(公告)日：2018-10-31
申请号：IL26105518
申请日：2018-08-08
申请人： ASTELLAS PHARMA INC , CYTOKINETICS INC , IPPEI SATO , TAKASHI KAMIKUBO , MASANORI MIURA , YUJI MATSUSHIMA , HIROAKI TANAKA , YASUHIRO SHIINA , SUSUMU YAMAKI , TOMOYUKI SAITO , HIROSHI KIYOHARA , MUNEMICHI OHE , KAYOKO MIHARA , BRADLEY PAUL MORGAN , FADY MALIK , SCOTT EMILE COLLIBEE , LUKE ASHCRAFT , PU PING LU , JEFFREY MICHAEL WARRINGTON , MARC GARARD
发明人： IPPEI SATO , TAKASHI KAMIKUBO , MASANORI MIURA , YUJI MATSUSHIMA , HIROAKI TANAKA , YASUHIRO SHIINA , SUSUMU YAMAKI , TOMOYUKI SAITO , HIROSHI KIYOHARA , MUNEMICHI OHE , KAYOKO MIHARA , BRADLEY PAUL MORGAN , FADY MALIK , SCOTT EMILE COLLIBEE , LUKE ASHCRAFT , PU-PING LU , JEFFREY MICHAEL WARRINGTON , MARC GARARD
IPC分类号： C07D20060101
摘要： Novel tetrahydroisoquinoline derivative compounds are disclosed herein that may be used as an active ingredient for a pharmaceutical composition, and in particular, for a pharmaceutical composition useful for preventing or treating a disease or condition responsive to modulation of the contractility of the skeletal sarcomere. This may be accomplished, for example, by modulation of the troponin complex of the fast skeletal muscle sarcomere through one or more of fast skeletal myosin, actin, tropomyosin, troponin C, troponin I, and troponin T, and fragments and isoforms thereof. The tetrahydroisoquinoline derivative compounds can thus be used as an agent for preventing or treating 1) neuromuscular disorders, 2) disorders of voluntary muscle, 3) CNS disorders in which muscle weakness, atrophy, and fatigue are prominent symptoms, 4) muscle symptoms stemming from systemic disorders, and 5) dysfunctions of pelvic floor and urethral/anal sphincter muscle.

3. 发明申请

US20110082133A1 PYRIDONE COMPOUNDS 审中-公开
标题翻译：吡咯烷酮化合物
公开(公告)号：US20110082133A1
公开(公告)日：2011-04-07
申请号：US12999379
申请日：2009-06-16
申请人： Takashi Kamikubo , Masanori Miura , Takao Okuda , Keisuke Maki , Fukushi Hirayama , Ayako Moritomo , Yuriko Komiya , Keisuke Matsuura , Ryotaro Ibuka
发明人： Takashi Kamikubo , Masanori Miura , Takao Okuda , Keisuke Maki , Fukushi Hirayama , Ayako Moritomo , Yuriko Komiya , Keisuke Matsuura , Ryotaro Ibuka
IPC分类号： A61K31/5415 , A61K31/4725 , A61K31/4439 , A61K31/4412 , C07D417/06 , A61P9/10 , A61K31/444 , C07D417/12 , C07D401/06 , C07D211/72
CPC分类号： C07D401/06 , A61K31/13 , A61K31/4412 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/538 , A61K31/5415 , C07D213/64 , C07D213/69 , C07D213/79 , C07D409/12 , C07D413/06 , C07D413/10 , C07D413/14 , C07D417/06 , C07D417/12
摘要： [Problems] A useful compound which can be used as a pharmaceutical, in particular, an agent for treating peripheral arterial occlusive disease is provided.[Means for Solution] The present inventors have conducted extensive studies on EP4 receptor agonists, and as a result, have found that a novel pyridone compound, in which a group having an acidic group is substituted at the 1-position of the pyridone ring, the 6-position is bonded with an aromatic ring group via a linking part, and the linking part contains a nitrogen atom, has an excellent EP4 receptor agonistic action, thereby completing the present invention. Since the compound of the present invention has an excellent EP4 receptor agonistic action, it is useful as a pharmaceutical, in particular, as an agent for treating peripheral arterial occlusive disease.
摘要翻译： [问题]提供了可用作药物，特别是用于治疗外周动脉闭塞性疾病的药剂的有用化合物。 [解决方案]本发明人对EP4受体激动剂进行了广泛的研究，结果发现，其中具有酸性基团的基团在吡啶酮环的1位被取代的新的吡啶酮化合物， 6-位通过连接部分与芳环基团键合，并且连接部分含有氮原子，具有优异的EP4受体激动作用，从而完成了本发明。由于本发明的化合物具有优异的EP4受体激动作用，所以作为药物，特别是作为治疗外周动脉闭塞性疾病的药剂是有用的。

4. 发明申请

US20110068281A1 CHARGED PARTICLE BEAM DRAWING APPARATUS AND PROXIMITY EFFECT CORRECTION METHOD THEREOF 有权
标题翻译：充电粒子束绘图装置及其近似效应校正方法
公开(公告)号：US20110068281A1
公开(公告)日：2011-03-24
申请号：US12882713
申请日：2010-09-15
申请人： Shigehiro HARA , Shuichi Tamamushi , Takashi Kamikubo , Hitoshi Higurashi , Shinji Sakamoto , Yusuke Sakai , Yoshihiro Okamoto , Akihito Anpo
发明人： Shigehiro HARA , Shuichi Tamamushi , Takashi Kamikubo , Hitoshi Higurashi , Shinji Sakamoto , Yusuke Sakai , Yoshihiro Okamoto , Akihito Anpo
IPC分类号： G21K5/10 , G03F7/20
CPC分类号： H01J37/3174 , B82Y10/00 , B82Y40/00 , H01J37/304 , H01J2237/31769 , H01J2237/31776
摘要： A charged particle beam drawing apparatus forms a map having meshes, forms representative figures, area of each representative figure in each mesh being equal to gross area of figures in each mesh, and calculates a proximity effect correction dose of the charged particle beam in each mesh on the basis of area of each representative figure in each mesh. If it is necessary to change the proximity effect correction dose of the charged particle beam for drawing at least one pattern corresponding to at least one figure, the charged particle beam drawing apparatus changes area of the at least one figure before the representative figures are formed by a representative figure forming portion, and changes the proximity effect correction dose of the charged particle beam for drawing the at least one pattern corresponding to the at least one figure, calculated by a proximity effect correction dose calculating portion.
摘要翻译：带电粒子束描绘装置形成具有网格的图，形成代表性图，每个网格中每个代表图的面积等于每个网格中的图形的总面积，并计算每个网格中的带电粒子束的邻近效应校正剂量在每个网格中每个代表人物的面积的基础上。如果需要改变带电粒子束的接近效应校正剂量以绘制与至少一个图形相对应的至少一个图案，则带电粒子束描绘装置在代表性图形形成之前改变至少一个图形的面积，代表图形形成部分，并且改变用于绘制由邻近效应校正剂量计算部分计算的与至少一个图形相对应的至少一个图案的带电粒子束的邻近效应校正剂量。

5. 发明申请

US20100178611A1 Lithography method of electron beam 审中-公开
标题翻译：电子束光刻法
公开(公告)号：US20100178611A1
公开(公告)日：2010-07-15
申请号：US12659774
申请日：2010-03-22
申请人： Hirohito Anze , Takehiko Katsumata , Shuichi Tamamushi , Takashi Kamikubo , Rieko Nishimura , Makoto Hiramoto , Tomoo Motosugi , Takazuki Ohnishi
发明人： Hirohito Anze , Takehiko Katsumata , Shuichi Tamamushi , Takashi Kamikubo , Rieko Nishimura , Makoto Hiramoto , Tomoo Motosugi , Takazuki Ohnishi
IPC分类号： G03F7/20
CPC分类号： B82Y40/00 , B82Y10/00 , G03F1/78 , G03F7/0382 , G03F7/0392 , H01J37/3174
摘要： A charged particle beam writing method on a chemical amplification type resist, comprising: coating said chemical amplification type resist which contains an acid diffusion inhibitor, on a surface of a mask substrate, exposing charged particle beams to said chemical amplification type resist layer on said surface of the mask substrate, baking said chemical amplification type resist layer which said charged particle beams were exposed, and developing said chemical amplification type resist after the baking, wherein an exposure current density of said electron beams exposing ranges of 50˜5000 A/cm2, said photo acid generator is in an amount ranging from 0.1 to 30 weight percent (wt %) relative to all solid content of said chemical amplification type resist, and said acid diffusion inhibitor is composed of at least one material selected from the group consisting of tertiary amine class, benzyl-carbamate class, benzoin-carbamate class, o-carbamoyl-hydroxy-amine class, o-carbamoyl-oxime class, and dithio-calbamate-quaternary ammonium salt.
摘要翻译：一种化学放大型抗蚀剂的带电粒子束写入方法，包括：在掩模基板的表面上涂覆含有酸扩散抑制剂的所述化学放大型抗蚀剂，将带电粒子束暴露于所述表面上的所述化学放大型抗蚀剂层对所述带电粒子束进行曝光的所述化学放大型抗蚀剂层进行烘烤，烘烤后显影所述化学放大型抗蚀剂，其中所述电子束的曝光电流密度为50〜5000A / cm 2，所述光酸产生剂的量相对于所述化学增幅型抗蚀剂的全部固体含量为0.1〜30重量％（重量％），所述酸扩散抑制剂由选自三级胺类，氨基甲酸苄酯类，苯偶姻 - 氨基甲酸酯类，邻氨基甲酰基 - 羟基 - 胺类，邻氨基甲酰基肟屁股和二硫代氨基甲酸铵 - 季铵盐。

6. 发明申请

US20100113391A1 BICYCLIC HETEROCYCLIC COMPOUND 审中-公开
标题翻译：双相杂环化合物
公开(公告)号：US20100113391A1
公开(公告)日：2010-05-06
申请号：US12596643
申请日：2008-04-17
申请人： Yuji Koga , Takao Okuda , Takashi Kamikubo , Michihito Kageyama , Hiroyuki Moritomo
发明人： Yuji Koga , Takao Okuda , Takashi Kamikubo , Michihito Kageyama , Hiroyuki Moritomo
IPC分类号： A61K31/695 , C07D215/22 , C07D239/80 , C07F7/02 , C07D243/14 , A61K31/47 , A61K31/517 , A61K31/5513 , A61P7/02
CPC分类号： C07D217/24 , C07D239/96 , C07D243/14 , C07D401/06 , C07D403/12 , C07D405/04 , C07D405/06 , C07D413/06 , C07D417/06
摘要： [Problem]Provided is a compound, which exhibits a P2Y12 inhibitory action and is useful as a medical drug, particularly, as a platelet aggregation inhibitor.[Means for Solution]The inventors have eagerly investigated P2Y12 inhibitors. As a result, the inventors have found that a bicyclic heterocyclic compound such as quinazolinedione, isoquinolone, and the like having an amino group substituted with lower alkyl, cycloalkyl, or lower alkylene-cycloalkyl at the specific position exhibits an excellent platelet aggregation inhibitory action, thereby completing the present invention. Since the compound of the invention exhibits excellent P2Y12 inhibitory action and platelet aggregation inhibitory action, it is useful as a platelet aggregation inhibitor.
摘要翻译： [问题]提供了表现出P2Y12抑制作用的化合物，可用作医药，特别是作为血小板聚集抑制剂。解决方法本发明人急切地研究P2Y12抑制剂。结果发现，在具体位置具有被低级烷基，环烷基或低级亚烷基 - 环烷基取代的氨基的喹唑啉二酮，异喹诺酮等双环杂环化合物显示优异的血小板聚集抑制作用，从而完成了本发明。由于本发明化合物表现出优异的P2Y12抑制作用和血小板聚集抑制作用，因此作为血小板聚集抑制剂是有用的。

7. 发明申请

US20090014663A1 CHARGED-PARTICLE BEAM WRITING METHOD 有权
标题翻译：充电粒子束写法
公开(公告)号：US20090014663A1
公开(公告)日：2009-01-15
申请号：US12170874
申请日：2008-07-10
申请人： Rieko NISHIMURA , Takashi KAMIKUBO
发明人： Rieko NISHIMURA , Takashi KAMIKUBO
IPC分类号： H01J3/26
CPC分类号： H01J37/3045 , B82Y10/00 , B82Y40/00 , H01J37/3174 , H01J2237/2817 , H01J2237/30455 , H01J2237/30461 , H01J2237/30483
摘要： The present invention provides an electron beam writing method capable of suppressing a variation in position to be irradiated with an electron beam due to its drift and writing a predetermined pattern.A positional displacement amount near the center of each main deflection area of the charged-particle beam is determined. Correction values are determined from a plurality of the positional displacement amounts. A position irradiated with the charged-particle beam is corrected from the correction values. The neighborhood of the center of the main deflection area can be a sub deflection area including the center of the main deflection area. In this case, the positional displacement amount can be one for one arbitrary point in the sub deflection area. Alternatively, the Positional displacement amount can also be the average of positional displacement amounts at a plurality of arbitrary points in the sub deflection area.
摘要翻译：本发明提供一种电子束写入方法，其能够抑制由于其漂移并写入预定图案而被电子束照射的位置的变化。确定带电粒子束的每个主偏转区域的中心附近的位置偏移量。从多个位置偏移量确定校正值。从校正值校正用带电粒子束照射的位置。主偏转区域的中心附近可以是包括主偏转区域的中心的副偏转区域。在这种情况下，位移位移量可以是副偏转区域中的一个任意点的位移量。或者，位移位移量也可以是副偏转区域中的多个任意点处的位置偏移量的平均值。

8. 发明授权

US5698618A Coating composition 失效
标题翻译：涂料组成
公开(公告)号：US5698618A
公开(公告)日：1997-12-16
申请号：US683213
申请日：1996-07-18
申请人： Takashi Kamikubo , Tadashi Itabashi , Masami Kuwahara
发明人： Takashi Kamikubo , Tadashi Itabashi , Masami Kuwahara
IPC分类号： C09D7/45 , C09D167/08 , C09D201/06 , C08K5/42
CPC分类号： C09D167/08 , C09D201/06 , C09D7/02
摘要： A coating composition is formed from an acid-set coating varnish and a pigment composition. The pigment composition includes a specific organic dyestuff derivative and a specific basic-group-containing resin-type pigment dispersant. The coating composition excels in pigment dispersibility, nonflocculation properties, noncrystallizability and fluidity. When used as a coating, the coating composition has excellent color tone, gloss, hardness, weather resistance, and solvent resistance.
摘要翻译： PCT No.PCT / JP95 / 02355 Sec。 371日期：1996年7月18日 102（e）日期1996年7月18日PCT提交1995年11月17日PCT公布。出版物WO96 / 16130 日期：1996年5月30日涂料组合物由酸性涂料清漆和颜料组合物形成。颜料组合物包括特定的有机染料衍生物和特定的含碱性基团的树脂型颜料分散剂。涂料组合物的颜料分散性，非絮凝性，非结晶性和流动性优异。当用作涂层时，涂料组合物具有优异的色调，光泽度，硬度，耐候性和耐溶剂性。

9. 发明申请

US20120136025A1 QUINOLONE DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF 失效
标题翻译：喹诺酮衍生物或药物可接受的盐
公开(公告)号：US20120136025A1
公开(公告)日：2012-05-31
申请号：US13364815
申请日：2012-02-02
申请人： Yuji KOGA , Takao OKUDA , Susumu WATANUKI , Takashi KAMIKUBO , Fukushi HIRAYAMA , Hiroyuki MORITOMO , Jiro FUJIYASU , Michihito KAGEYAMA , Toshio UEMURA , Jun TAKASAKI
发明人： Yuji KOGA , Takao OKUDA , Susumu WATANUKI , Takashi KAMIKUBO , Fukushi HIRAYAMA , Hiroyuki MORITOMO , Jiro FUJIYASU , Michihito KAGEYAMA , Toshio UEMURA , Jun TAKASAKI
IPC分类号： A61K31/47 , A61P9/00 , A61P7/02 , C07D215/22
CPC分类号： C07D513/04 , C07D215/22 , C07D215/56 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/14 , C07D487/04 , C07F7/1804 , C07F9/60
摘要： Disclosed are quinolone derivatives characterized in that these have lower alkyl, cycloalkyl or the like at the 1-position; —N(R0)C(O)-lower alkylene-CO2R0, lower alkylene-CO2R0, lower alkenylene-CO2R0, —O-lower alkylene-CO2R0, —O-(lower alkylene which may be substituted with —CO2R0)-aryl or —O-lower alkenylene-CO2R0 (wherein R0 is H or lower alkyl) at the 3-position; halogen at the 6-position; and amino group substituted with a substituent group having a ring structure at the 7-position, respectively, or pharmaceutically acceptable salts thereof, has excellent P2Y12 inhibitory activity. The quinolone derivatives have excellent platelet aggregation inhibitory activity. A method of using the compounds is also disclosed.
摘要翻译：公开了喹诺酮衍生物，其特征在于它们在1-位具有低级烷基，环烷基等; -N（R 0）C（O） - 低级亚烷基-CO 2 R 0，低级亚烷基-CO 2 R 0，低级亚烯基-CO 2 R O，-O-低级亚烷基-CO 2 R O，-O-（可被-CO 2 R 0取代的低级亚烷基） - 芳基或 O-低级亚烯基-CO 2 R 0（其中R 0是H或低级烷基）在3-位; 6位卤素; 分别被具有7位具有环结构的取代基取代的氨基或其药学上可接受的盐具有优异的P2Y12抑制活性。喹诺酮衍生物具有优异的血小板聚集抑制活性。还公开了使用该化合物的方法。

10. 发明授权

US07585886B2 Pyrrolidine derivative or salt thereof 有权
标题翻译：吡咯烷衍生物或其盐
公开(公告)号：US07585886B2
公开(公告)日：2009-09-08
申请号：US11662539
申请日：2006-05-18
申请人： Shunichiro Hachiya , Makoto Oku , Hana Mukai , Takashi Shin , Keisuke Matsuura , Ryushi Seo , Takashi Kamikubo , Yoh Terada , Masanao Sanagi , Kousei Yoshihara , Taisuke Takahashi
发明人： Shunichiro Hachiya , Makoto Oku , Hana Mukai , Takashi Shin , Keisuke Matsuura , Ryushi Seo , Takashi Kamikubo , Yoh Terada , Masanao Sanagi , Kousei Yoshihara , Taisuke Takahashi
IPC分类号： C07D207/00 , A61K31/40
CPC分类号： C07D207/09 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/04 , C07D405/06 , C07D405/12 , C07D409/04 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/10 , C07D417/06 , C07D417/10
摘要： [Problem] To provide a compound which may be used in treating diseases in which a calcium sensing receptor (CaSR) is concerned, particularly hyperparathyroidism. [Means for Resolution] It was found that novel pyrrolidine derivatives which are characterized by the possession of aminomethyl group substituted with arylalkyl group or the like, or salts thereof, have excellent CaSR agonistic regulatory activity and also have excellent selectivity with CYP2D6 inhibitory activity having a possibility of causing drug interaction. Based on the above, these novel pyrrolidine derivatives are useful as therapeutic agents for treating diseases in which CaSR is concerned (hyperparathyroidism, renal osteodystrophy, hypercalcemia and the like).
摘要翻译： [问题]提供可用于治疗其中涉及钙感觉受体（CaSR）的疾病的化合物，特别是甲状旁腺机能亢进。 [解决方法]发现以芳基烷基等取代的氨甲基为特征的新型吡咯烷衍生物或其盐具有优异的CaSR激动调节活性，并且对于CYP2D6抑制活性也具有优异的选择性，具有引起药物相互作用的可能性。基于上述，这些新型吡咯烷衍生物可用作治疗涉及CaSR的疾病（甲状旁腺功能亢进，肾性骨营养不良，高钙血症等）的治疗剂。

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