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1. 发明授权

US06069176A Phenylethanolamine compounds useful as .beta. 3 agonists, process for producing the same, and intermediates in the production of the same 失效
标题翻译：可用作β3激动剂的苯乙醇胺化合物，其制备方法和在其生产中的中间体
公开(公告)号：US06069176A
公开(公告)日：2000-05-30
申请号：US65077
申请日：1998-04-24
申请人： Susumu Tsuchiya , Nobuyuki Yasuda , Toshifumi Matsumoto , Kozo Hiratsuka , Hiroyuki Iizuka , Atsusi Hukuzaki , Kouichi Matsunaga
发明人： Susumu Tsuchiya , Nobuyuki Yasuda , Toshifumi Matsumoto , Kozo Hiratsuka , Hiroyuki Iizuka , Atsusi Hukuzaki , Kouichi Matsunaga
IPC分类号： C07C215/42 , C07C217/74 , C07C219/24 , C07C235/36 , C07D235/08 , C07D295/185 , C07D317/46 , A61K31/135 , C07C49/255 , C07C49/753 , C07C213/02
CPC分类号： C07D295/185 , C07C215/42 , C07C217/74 , C07C219/24 , C07C235/36 , C07D235/08 , C07D317/46 , C07C2101/08 , C07C2101/14 , Y10S514/866 , Y10S514/909
摘要： The present invention relates to phenylethanolamine compounds represented by general formula [I]: ##STR1## (where R.sub.1 represents hydrogen or halogen; R.sub.2 represents hydrogen, hydroxy, lower alkoxy, lower alkoxy substituted with one or two lower alkoxycarbonyl or carboxy groups, lower alkoxy substituted with lower alkylaminocarbonyl which may be substituted with lower alkoxy, lower alkoxy substituted with cyclic aminocarbonyl of 4 to 6 carbon atoms, lower alkoxycarbonyl or carboxy; R.sub.3 represents hydrogen, hydroxy, lower alkoxy or lower alkoxy substituted with one or two lower alkoxycarbonyl or carboxy groups; R.sub.2 and R.sub.3 may be bonded to each other to form methylenedioxy substituted with carboxy or lower alkoxycarbonyl; and m and n are 0 or 1), and their pharmacologically acceptable salts, which have a potent .beta.3 adrenergic stimulating effect and high .beta.3 adrenergic receptor selectivity, as well as to processes for their production and intermediates in their production.
摘要翻译： PCT No.PCT / JP96 / 03097 Sec。 371日期：1998年4月24日 102（e）1998年4月24日PCT 1996年10月24日PCT公布。第WO97 / 15549号公报日期：1997年5月1日本发明涉及由通式[I]表示的苯乙醇胺化合物：其中R1表示氢或卤素; R2表示氢，羟基，低级烷氧基，被一个或两个低级烷氧基羰基或羧基取代的低级烷氧基，较低级被可被低级烷氧基取代的低级烷基氨基羰基取代的烷氧基，被4-6个碳原子的环状氨基羰基取代的低级烷氧基，低级烷氧基羰基或羧基; R3代表氢，羟基，低级烷氧基或被一个或两个低级烷氧基羰基取代的低级烷氧基，羧基; R2和R3可以彼此键合以形成被羧基或低级烷氧基羰基取代的亚甲二氧基; m和n为0或1），以及它们的药理学上可接受的盐，其具有强大的β3肾上腺素能刺激作用和高β 3肾上腺素能受体选择性，以及其生产过程及其生产中间体。

2. 发明授权

US07812178B2 Isoquinoline compound and pharmaceutical use thereof 有权
标题翻译：异喹啉化合物及其药物用途
公开(公告)号：US07812178B2
公开(公告)日：2010-10-12
申请号：US12263963
申请日：2008-11-03
申请人： Masakazu Fujio , Hiroyuki Satoh , Shinya Inoue , Toshifumi Matsumoto , Yasuhiro Egi
发明人： Masakazu Fujio , Hiroyuki Satoh , Shinya Inoue , Toshifumi Matsumoto , Yasuhiro Egi
IPC分类号： C07D405/00 , C07D207/00 , C07D207/40
CPC分类号： C07D401/04 , A61K31/4725 , C07D207/12 , C07D401/06 , C07D405/06
摘要： The present invention relates to an isoquinoline compound represented by the following formula (I), an optically active form thereof, a pharmaceutically acceptable salt thereof, a water adduct thereof, a hydrate thereof and a solvate thereof, as well as an agent for the prophylaxis and/or treatment of a disease caused by hyperreactivity of poly(ADP-ribose)polymerase, containing the compound, and a poly(ADP-ribose)polymerase inhibitor containing the compound. In addition, this compound is useful as an agent for the prophylaxis and/or treatment of cerebral infarction, particularly as an agent for the prophylaxis and/or treatment of acute cerebral infarction. Furthermore, this compound is useful as a prophylactic and/or therapeutic agent that improves neurological symptoms associated with cerebral infarction, particularly acute cerebral infarction. wherein the symbols are the same as defined in the description.
摘要翻译：本发明涉及由下式（I）表示的异喹啉化合物，其光学活性形式，其药学上可接受的盐，其水加合物，其水合物和溶剂化物，以及预防药物和/或治疗由含有该化合物的聚（ADP-核糖）聚合酶和含该化合物的聚（ADP-核糖）聚合酶抑制剂）的高反应性引起的疾病。此外，该化合物可用作预防和/或治疗脑梗塞的药剂，特别是作为预防和/或治疗急性脑梗死的药物。此外，该化合物可用作改善与脑梗死特别是急性脑梗死相关的神经症状的预防和/或治疗剂。其中符号与描述中定义的相同。

3. 发明授权

US07459465B2 Isoquinoline compound and pharmaceutical use thereof 有权
标题翻译：异喹啉化合物及其药物用途
公开(公告)号：US07459465B2
公开(公告)日：2008-12-02
申请号：US11688103
申请日：2007-03-19
申请人： Masakazu Fujio , Hiroyuki Satoh , Shinya Inoue , Toshifumi Matsumoto , Yasuhiro Egi
发明人： Masakazu Fujio , Hiroyuki Satoh , Shinya Inoue , Toshifumi Matsumoto , Yasuhiro Egi
IPC分类号： C07D403/02 , A61K31/47
CPC分类号： C07D401/04 , A61K31/4725 , C07D207/12 , C07D401/06 , C07D405/06
摘要： The present invention relates to an isoquinoline compound represented by the following formula (I), an optically active form thereof, a pharmaceutically acceptable salt thereof, a water adduct thereof, a hydrate thereof and a solvate thereof, as well as an agent for the prophylaxis and/or treatment of a disease caused by hyperreactivity of poly(ADP-ribose)polymerase, containing the compound, and a poly(ADP-ribose)polymerase inhibitor containing the compound. In addition, this compound is useful as an agent for the prophylaxis and/or treatment of cerebral infarction, particularly as an agent for the prophylaxis and/or treatment of acute cerebral infarction. Furthermore, this compound is useful as a prophylactic and/or therapeutic agent that improves neurological symptoms associated with cerebral infarction, particularly acute cerebral infarction. wherein the symbols are the same as defined in the description.
摘要翻译：本发明涉及由下式（I）表示的异喹啉化合物，其光学活性形式，其药学上可接受的盐，其水加合物，其水合物和溶剂化物，以及预防药物和/或治疗由含有该化合物的聚（ADP-核糖）聚合酶和含该化合物的聚（ADP-核糖）聚合酶抑制剂）的高反应性引起的疾病。此外，该化合物可用作预防和/或治疗脑梗塞的药剂，特别是作为预防和/或治疗急性脑梗死的药物。此外，该化合物可用作改善与脑梗死特别是急性脑梗死相关的神经症状的预防和/或治疗剂。其中符号与描述中定义的相同。

4. 发明申请

US20070161620A1 ISOQUINOLINE COMPOUND AND PHARMACEUTICAL USE THEREOF 有权
标题翻译：异喹啉化合物及其药物用途
公开(公告)号：US20070161620A1
公开(公告)日：2007-07-12
申请号：US11688103
申请日：2007-03-19
申请人： Masakazu Fujio , Hiroyuki Satoh , Shinya Inoue , Toshifumi Matsumoto , Yasuhiro Egi
发明人： Masakazu Fujio , Hiroyuki Satoh , Shinya Inoue , Toshifumi Matsumoto , Yasuhiro Egi
IPC分类号： A61K31/55 , A61K31/496 , A61K31/4709 , C07D401/02 , C07D403/02
CPC分类号： C07D401/04 , A61K31/4725 , C07D207/12 , C07D401/06 , C07D405/06
摘要： The present invention relates to an isoquinoline compound represented by the following formula (I), an optically active form thereof, a pharmaceutically acceptable salt thereof, a water adduct thereof, a hydrate thereof and a solvate thereof, as well as an agent for the prophylaxis and/or treatment of a disease caused by hyperreactivity of poly(ADP-ribose)polymerase, containing the compound, and a poly(ADP-ribose)polymerase inhibitor containing the compound. In addition, this compound is useful as an agent for the prophylaxis and/or treatment of cerebral infarction, particularly as an agent for the prophylaxis and/or treatment of acute cerebral infarction. Furthermore, this compound is useful as a prophylactic and/or therapeutic agent that improves neurological symptoms associated with cerebral infarction, particularly acute cerebral infarction. wherein the symbols are the same as defined in the description.
摘要翻译：本发明涉及由下式（I）表示的异喹啉化合物，其光学活性形式，其药学上可接受的盐，其水加合物，其水合物和溶剂化物，以及预防药物和/或治疗由含有该化合物的聚（ADP-核糖）聚合酶和含该化合物的聚（ADP-核糖）聚合酶抑制剂）的高反应性引起的疾病。此外，该化合物可用作预防和/或治疗脑梗塞的药剂，特别是作为预防和/或治疗急性脑梗死的药物。此外，该化合物可用作改善与脑梗死特别是急性脑梗死相关的神经症状的预防和/或治疗剂。其中符号与描述中定义的相同。

5. 发明授权

US07220759B2 Isoquinoline compound and pharmaceutical use thereof 有权
标题翻译：异喹啉化合物及其药物用途
公开(公告)号：US07220759B2
公开(公告)日：2007-05-22
申请号：US10836377
申请日：2004-04-30
申请人： Masakazu Fujio , Hiroyuki Satoh , Shinya Inoue , Toshifumi Matsumoto , Yasuhiro Egi
发明人： Masakazu Fujio , Hiroyuki Satoh , Shinya Inoue , Toshifumi Matsumoto , Yasuhiro Egi
IPC分类号： C07D217/22 , A61K31/47
CPC分类号： C07D401/04 , A61K31/4725 , C07D207/12 , C07D401/06 , C07D405/06
摘要： The present invention relates to an isoquinoline compound represented by the following formula (I), an optically active form thereof, a pharmaceutically acceptable salt thereof, a water adduct thereof, a hydrate thereof and a solvate thereof, as well as an agent for the prophylaxis and/or treatment of a disease caused by hyperreactivity of poly(ADP-ribose)polymerase, containing the compound, and a poly(ADP-ribose)polymerase inhibitor containing the compound. In addition, this compound is useful as an agent for the prophylaxis and/or treatment of cerebral infarction, particularly as an agent for the prophylaxis and/or treatment of acute cerebral infarction. Furthermore, this compound is useful as a prophylactic and/or therapeutic agent that improves neurological symptoms associated with cerebral infarction, particularly acute cerebral infarction. wherein the symbols are the same as defined in the description.
摘要翻译：本发明涉及由下式（I）表示的异喹啉化合物，其光学活性形式，其药学上可接受的盐，其水加合物，其水合物和溶剂化物，以及预防药物和/或治疗由含有该化合物的聚（ADP-核糖）聚合酶和含该化合物的聚（ADP-核糖）聚合酶抑制剂）的高反应性引起的疾病。此外，该化合物可用作预防和/或治疗脑梗塞的药剂，特别是作为预防和/或治疗急性脑梗死的药物。此外，该化合物可用作改善与脑梗死特别是急性脑梗死相关的神经症状的预防和/或治疗剂。其中符号与描述中定义的相同。

6. 发明授权

US07501412B2 Isoquinoline compounds and medicinal use thereof 有权
标题翻译：异喹啉化合物及其医药用途
公开(公告)号：US07501412B2
公开(公告)日：2009-03-10
申请号：US10536173
申请日：2003-11-21
申请人： Masakazu Fujio , Hiroyuki Satoh , Shinya Inoue , Toshifumi Matsumoto , Yasuhiro Egi , Taichi Takahashi
发明人： Masakazu Fujio , Hiroyuki Satoh , Shinya Inoue , Toshifumi Matsumoto , Yasuhiro Egi , Taichi Takahashi
IPC分类号： C07D403/02 , A61K31/47
CPC分类号： C07D471/04 , A61K31/472 , A61K31/4725 , A61K31/4745 , A61K31/496 , A61K31/5377 , C07D217/24 , C07D401/04 , C07D401/06 , C07D513/04
摘要： The present invention relates to an isoquinoline compound represented by the following formula (I) or (II), an optically active form thereof, a pharmaceutically acceptable salt thereof, a water adduct thereof, a hydrate thereof and a solvate thereof, as well as an agent for the prophylaxis and/or treatment of a disease caused by hyperreactivity of poly(ADP-ribose)polymerase, containing the compound, and a poly(ADP-ribose)polymerase inhibitor containing the compound. In addition, this compound is useful as an agent for the prophylaxis and/or treatment of cerebral infarction, particularly as an agent for the prophylaxis and/or treatment of acute cerebral infarction.
摘要翻译：本发明涉及由下式（I）或（II）表示的异喹啉化合物，其光学活性形式，其药学上可接受的盐，其水加合物，其水合物及其溶剂合物，以及用于预防和/或治疗由含有该化合物的聚（ADP-核糖）聚合酶的高反应性引起的疾病和含该化合物的聚（ADP-核糖）聚合酶抑制剂。此外，该化合物可用作预防和/或治疗脑梗塞的药剂，特别是作为预防和/或治疗急性脑梗死的药物。

7. 发明申请

US20060094743A1 Isoquinoline compounds and medicinal use thereof 有权
公开(公告)号：US20060094743A1
公开(公告)日：2006-05-04
申请号：US10536173
申请日：2003-11-21
申请人： Masakazu Fujio , Hiroyuki Satoh , Shinya Inoue , Toshifumi Matsumoto , Yasuhiro Egi , Taichi Takahashi
发明人： Masakazu Fujio , Hiroyuki Satoh , Shinya Inoue , Toshifumi Matsumoto , Yasuhiro Egi , Taichi Takahashi
IPC分类号： A61K31/4745 , A61K31/4709 , C07D471/02 , C07D403/02
CPC分类号： C07D471/04 , A61K31/472 , A61K31/4725 , A61K31/4745 , A61K31/496 , A61K31/5377 , C07D217/24 , C07D401/04 , C07D401/06 , C07D513/04
摘要： The present invention relates to an isoquinoline compound represented by the following formula (I) or (II), an optically active form thereof, a pharmaceutically acceptable salt thereof, a water adduct thereof, a hydrate thereof and a solvate thereof, as well as an agent for the prophylaxis and/or treatment of a disease caused by hyperreactivity of poly(ADP-ribose)polymerase, containing the compound, and a poly(ADP-ribose)polymerase inhibitor containing the compound. In addition, this compound is useful as an agent for the prophylaxis and/or treatment of cerebral infarction, particularly as an agent for the prophylaxis and/or treatment of acute cerebral infarction.

8. 发明授权

US06233499B1 Method and apparatus for designing molds using 3-dimensional CAD system 失效
标题翻译：使用三维CAD系统设计模具的方法和设备
公开(公告)号：US06233499B1
公开(公告)日：2001-05-15
申请号：US09097821
申请日：1998-06-16
申请人： Toshifumi Matsumoto
发明人： Toshifumi Matsumoto
IPC分类号： G06F1900
CPC分类号： B29C33/3835
摘要： A product solid (A) is generated on a CAD screen using a 3-dimensional CAD system, then thin film solids (B1 and B2) are added to the product solid so as to divide an object mold into parts or fill holes of the mold, and after this, the product solid (A) is united with the thin film solids (B1 and B2) into one, thereby to generate a thin film formed product solid. This thin film formed product solid is put in a rectangular solid, then the thin film formed product solid is removed from the rectangular solid, thereby to generate cavities in the rectangular solid. And, along these cavities, the mold is divided into a cavity solid and a core solid. In addition, the thickness (t) of each thin film solid is decided so as to prevent melted resin invasion. This method can thus divide a mold into a cavity and a core easily when product data is converted to solids for designing a mold using a 3-dimensional CAD system.
摘要翻译：在CAD屏幕上使用三维CAD系统产生产品固体（A），然后将薄膜固体（B1和B2）添加到产品固体中，以将目标模具分成模具的零件或填充孔，然后将产物固体（A）与薄膜固体（B1和B2）结合成一体，从而产生薄膜形成产物固体。将该薄膜形成的固体产品放入矩形固体中，然后从矩形固体中除去形成薄膜的产品固体，从而产生矩形固体的空腔。并且，沿着这些空腔，模具被分成腔体固体和芯部固体。此外，确定每个薄膜固体的厚度（t），以防止熔融的树脂侵入。因此，当使用三维CAD系统将产品数据转换为固体以设计模具时，该方法可以容易地将模具分成空腔和芯体。

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