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1. 发明申请

US20080318961A1 Drugs comprising chymase inhibitors and ACE inhibitors as effective ingredients 审中-公开
标题翻译：包含胃促胰酶抑制剂和ACE抑制剂作为有效成分的药物
公开(公告)号：US20080318961A1
公开(公告)日：2008-12-25
申请号：US12153897
申请日：2008-05-27
申请人： Hidenori Urata , Naoki Hase , Naoki Tsuchiya
发明人： Hidenori Urata , Naoki Hase , Naoki Tsuchiya
IPC分类号： A61K31/5025 , A61K31/506 , A61P9/00 , A61K31/4166
CPC分类号： A61K45/06
摘要： It is an object of the present invention to provide drugs which are effective for treatment of hypertension, cardiac disease (cardiac hypertrophy, cardiac failure, myocardial infarction, etc.), cerebral apoplexy, nephritis and the like. The invention also provides circulatory disease treatment agents in forms that allow combined use of chymase inhibitors and ACE inhibitors, and circulatory disease treatment methods which produce simultaneous chymase inhibition and ACE inhibition.
摘要翻译：本发明的目的是提供对治疗高血压，心脏病（心脏肥大，心力衰竭，心肌梗塞等），脑中风，肾炎等有效的药物。本发明还以允许组合使用胃促胰酶抑制剂和ACE抑制剂的形式提供循环系统疾病治疗剂，以及产生同时胃促胰酶抑制和ACE抑制的循环系统疾病治疗方法。

2. 发明申请

US20070032466A1 Drug containing chymase inhibitor as the active ingredient 审中-公开
标题翻译：药物含有胃促胰酶抑制剂作为活性成分
公开(公告)号：US20070032466A1
公开(公告)日：2007-02-08
申请号：US10568711
申请日：2004-08-20
申请人： Hidenori Urata , Naoki Hase , Naoki Tsuchiya
发明人： Hidenori Urata , Naoki Hase , Naoki Tsuchiya
IPC分类号： A61K31/513 , A61K31/4745 , A61K31/4184 , A61K31/4412 , A61K31/397 , A61K31/381
CPC分类号： A61K31/00 , A61K31/4184 , C07D413/12
摘要： The present invention provides drugs containing chymase inhibitors as active ingredients for improving glucose intolerance or preventing and/or treating diseases caused by glucose intolerance. The diseases caused by glucose intolerance are diabetes and/or diabetes complications, wherein the diabetes complications include diabetic nephropathy, diabetic retinopathy, diabetic peripheral neuropathy, hyperinsulinism, insulin resistance syndrome, arteriosclerosis, acute coronary syndrome, arteriosclerosis obliterans, angitis, stroke, hypertension, renal insufficiency, nephropathy, nephritis, renal artery aneurysm, renal infarction, obesity and the like.
摘要翻译：本发明提供含有胃促胰酶抑制剂作为改善葡萄糖耐受不良或预防和/或治疗由葡萄糖不耐受引起的疾病的活性成分的药物。由葡萄糖不耐受引起的疾病是糖尿病和/或糖尿病并发症，其中糖尿病并发症包括糖尿病性肾病，糖尿病性视网膜病变，糖尿病性周围神经病变，高胰岛素血症，胰岛素抵抗综合征，动脉硬化，急性冠状动脉综合征，闭塞性动脉硬化症，血管炎，中风，高血压，肾功能不全，肾病，肾炎，肾动脉瘤，肾梗死，肥胖等。

3. 发明授权

US06649656B1 Anthranilic acid derivatives 失效
标题翻译：邻氨基苯甲酸衍生物
公开(公告)号：US06649656B1
公开(公告)日：2003-11-18
申请号：US09744388
申请日：2001-04-04
申请人： Naoki Tsuchiya , Susumu Takeuchi , Takumi Takeyasu , Naoki Hase , Takao Yamori , Takashi Tsuruo
发明人： Naoki Tsuchiya , Susumu Takeuchi , Takumi Takeyasu , Naoki Hase , Takao Yamori , Takashi Tsuruo
IPC分类号： A61K31195
CPC分类号： C07D207/08 , C07C235/38 , C07C235/56 , C07C271/16 , C07C271/26 , C07C307/08 , C07C311/07 , C07C311/20 , C07C311/29 , C07C323/25 , C07C323/30 , C07C323/41 , C07C323/42 , C07C323/43 , C07C323/60 , C07C323/62 , C07C327/44 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2601/20 , C07C2602/28 , C07D211/02 , C07D211/46 , C07D213/30 , C07D213/64 , C07D213/643 , C07D213/70 , C07D213/82 , C07D213/89 , C07D295/088 , C07D295/185 , C07D307/42 , C07D307/58 , C07D309/10 , C07D405/12
摘要： The present invention relates to an anthranilic acid derivative expressed by the following formula (1) or the following formula (2), or its pharmacologically permissible salt or solvate.
摘要翻译：本发明涉及由下式（1）或下式（2）表示的邻氨基苯甲酸衍生物或其药理学上允许的盐或溶剂合物。

4. 发明授权

US5808144A Benzene derivatives 失效
标题翻译：苯衍生物
公开(公告)号：US5808144A
公开(公告)日：1998-09-15
申请号：US875284
申请日：1997-07-23
申请人： Masaichi Hasegawa , Takumi Takeyasu , Naoki Tsuchiya , Naoki Hase , Katsushi Takahashi , Takashi Kamimura
发明人： Masaichi Hasegawa , Takumi Takeyasu , Naoki Tsuchiya , Naoki Hase , Katsushi Takahashi , Takashi Kamimura
IPC分类号： C07C235/38 , C07C229/00 , C07C321/00
CPC分类号： C07C235/38 , C07C2101/14
摘要： Novel benzene derivatives of the formula (I) shown below, pharmacological salts thereof, pharmacological solvates of the above-mentioned benzene derivatives and salts, pharmaceutical compositions including, as active ingredients, the above-mentioned compounds, and especially, prophylactic or therapeutic medicines for allergic diseases. ##STR1## wherein R.sup.1 =H, C.sub.1 -C.sub.12 cyclic or straight or branched chain alkyl group (which may be substituted by one or more C.sub.6 -C.sub.10 aryloxy groups), C.sub.7 -C.sub.12 aralkyl group (of which the aryl group may be substituted one or more of halogen, methyl and methoxy, or C.sub.3 -C.sub.10 alkenyl which may be substituted by one or more phenyl groups; A=O, S or CH.sub.2 group, B=CO or CZ.sub.2 CO group (Z=H or F), R.sup.2 =H or C.sub.1 -C.sub.4 alkyl group, X=halogen or methyl group, and Y=H, NO.sub.2 or CN group.
摘要翻译： PCT No.PCT / JP96 / 03456 Sec。 371日期1997年7月23日 102（e）日期1997年7月23日PCT提交1995年11月27日PCT公布。第WO97 / 19910号公报日期：1997年5月6日下述式（I）的新型苯衍生物，其药理学盐，上述苯衍生物和盐的药理学溶剂化物，作为活性成分的上述化合物，特别是预防性或用于过敏性疾病的治疗药物。（I）其中R1 = H，C1-C12环状或直链或支链烷基（其可被一个或多个C 6 -C 10芳氧基取代），C 7 -C 12芳烷基（其芳基可以取代一个或多个卤素，甲基和甲氧基，或可被一个或多个苯基取代的C 3 -C 10链烯基; A = O，S或CH 2基团，B = CO或CZ 2 CO基团（Z = H或F），R2 = H或C1-C4烷基，X =卤素或甲基，Y = H，NO2或CN基团。

5. 发明授权

US06890932B2 Anthranilic acid derivative 失效
标题翻译：邻氨基苯甲酸衍生物
公开(公告)号：US06890932B2
公开(公告)日：2005-05-10
申请号：US10355125
申请日：2003-01-31
申请人： Naoki Tsuchiya , Susumu Takeuchi , Takumi Takeyasu , Naoki Hase , Takao Yamori , Takashi Tsuruo
发明人： Naoki Tsuchiya , Susumu Takeuchi , Takumi Takeyasu , Naoki Hase , Takao Yamori , Takashi Tsuruo
IPC分类号： C07C235/38 , C07C235/56 , C07C271/16 , C07C271/26 , C07C307/08 , C07C311/07 , C07C311/20 , C07C311/29 , C07C323/25 , C07C323/30 , C07C323/41 , C07C323/42 , C07C323/43 , C07C323/60 , C07C323/62 , C07C327/44 , C07D207/08 , C07D211/02 , C07D211/46 , C07D213/30 , C07D213/64 , C07D213/643 , C07D213/70 , C07D213/82 , C07D213/89 , C07D295/092 , C07D295/185 , C07D307/42 , C07D307/58 , C07D309/10 , C07D405/12 , A61K31/435 , A01N43/40 , C07D213/00 , C07D213/63
CPC分类号： C07D207/08 , C07C235/38 , C07C235/56 , C07C271/16 , C07C271/26 , C07C307/08 , C07C311/07 , C07C311/20 , C07C311/29 , C07C323/25 , C07C323/30 , C07C323/41 , C07C323/42 , C07C323/43 , C07C323/60 , C07C323/62 , C07C327/44 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2601/20 , C07C2602/28 , C07D211/02 , C07D211/46 , C07D213/30 , C07D213/64 , C07D213/643 , C07D213/70 , C07D213/82 , C07D213/89 , C07D295/088 , C07D295/185 , C07D307/42 , C07D307/58 , C07D309/10 , C07D405/12
摘要： The present invention relates to an anthranilic acid derivative expressed by the following formula (1) or the following formula (2), or its pharmacologically permissible salt or solvate.
摘要翻译：本发明涉及由下式（1）或下式（2）表示的邻氨基苯甲酸衍生物或其药理学上允许的盐或溶剂合物。

6. 发明申请

US20050267148A1 Benzimidazole derivative 审中-公开
标题翻译：苯并咪唑衍生物
公开(公告)号：US20050267148A1
公开(公告)日：2005-12-01
申请号：US11129508
申请日：2005-05-16
申请人： Naoki Tsuchiya , Tsuyoshi Mizuno , Hiroshi Saitou , Yoshiyuki Matsumoto , Susumu Takeuchi , Naoki Hase
发明人： Naoki Tsuchiya , Tsuyoshi Mizuno , Hiroshi Saitou , Yoshiyuki Matsumoto , Susumu Takeuchi , Naoki Hase
IPC分类号： A61K31/4184 , A61K31/4745 , C07D401/06 , C07D403/06 , C07D405/06 , C07D409/06 , C07D413/06 , C07D471/02
CPC分类号： C07D401/06 , C07D403/06 , C07D405/06 , C07D409/06 , C07D413/06
摘要： The present invention is a thiobenzimidazole derivative represented by the following formula (1) or a medically acceptable salt thereof wherein said thiobenzimidazole derivative and a medically acceptable salt thereof have a potent activity of inhibiting human chymase. Thus, they are potential preventive and/or therapeutic agents clinically applicable to various diseases in which human chymase is involved.
摘要翻译：本发明是由下式（1）表示的硫代苯并咪唑衍生物或其医学上可接受的盐，其中所述硫代苯并咪唑衍生物及其医学上可接受的盐具有抑制人胃促胰酶的有效活性。因此，它们是临床适用于涉及人胃促胰酶的各种疾病的潜在的预防和/或治疗剂。

7. 发明申请

US20080015240A1 Acid Salt of Benzimidazole Derivative and Crystal Thereof 审中-公开
标题翻译：苯并咪唑衍生物及其晶体的酸性盐
公开(公告)号：US20080015240A1
公开(公告)日：2008-01-17
申请号：US11667683
申请日：2005-11-14
申请人： Mitsuru Teramoto , Naoki Tsuchiya , Hiroshi Saitoh
发明人： Mitsuru Teramoto , Naoki Tsuchiya , Hiroshi Saitoh
IPC分类号： A61K31/4184 , A61P11/00 , A61P15/00 , A61P29/00 , A61P3/00 , C07D233/30
CPC分类号： C07D409/06
摘要： The present invention provides acid salts, such as sulfate, hydrochloride, and methanesulfonate, of 4-(1-((4-methylbenzothiophen-3-yl)methyl)benzimidazol-2-ylthio)butanoic acid and the crystals thereof. These benzimidazole derivatives and the crystals thereof have an in vivo chymase inhibitory activity and can be used as a preventive or therapeutic agent for inflammatory diseases, allergic diseases, respiratory diseases, circulatory diseases, or bone/cartilage metabolic diseases.
摘要翻译：本发明提供4-（1 - （（4-甲基苯并噻吩-3-基）甲基）苯并咪唑-2-基硫基）丁酸的酸式盐，如硫酸盐，盐酸盐和甲磺酸盐及其晶体。这些苯并咪唑衍生物及其结晶体具有体内糜酶抑制活性，可用作炎性疾病，过敏性疾病，呼吸系统疾病，循环系统疾病或骨/软骨代谢疾病的预防或治疗剂。

8. 发明授权

US07176320B2 Benzimidazole derivative 失效
标题翻译：苯并咪唑衍生物
公开(公告)号：US07176320B2
公开(公告)日：2007-02-13
申请号：US10777067
申请日：2004-02-13
申请人： Naoki Tsuchiya , Yoshiyuki Matsumoto , Hiroshi Saitou , Tsuyoshi Mizuno
发明人： Naoki Tsuchiya , Yoshiyuki Matsumoto , Hiroshi Saitou , Tsuyoshi Mizuno
IPC分类号： C07D403/12 , C07D409/12 , A61K31/4184
CPC分类号： C07D403/06 , C07D409/06
摘要： A benzimidazole derivative or its medically acceptable salt, represented by the following formula (1), that is a human chymase activity inhibitor capable of being applied clinically: wherein, R1 and R2 represent a hydrogen atom, an alkyl group or an alkoxy group, etc., A represents an alkylene group or an alkenylene group, E represents —COOR3, —SO3R3, —CONHR3 or —SO2NHR3, etc., G represents an alkylene group, M represents a single bond or —S(O)m—, J represents a heterocyclic group, and X represents —CH═ or a nitrogen atom.
摘要翻译：由下式（1）表示的苯并咪唑衍生物或其医学上可接受的盐，其是能够临床应用的人胃促胰酶抑制酶抑制剂：其中R 1和R 2， SUP>表示氢原子，烷基或烷氧基等，A表示亚烷基或亚烯基，E表示-COOR 3，-SO 3 R 3，-CONHR 3或-SO 2 NHR 3等，G表示亚烷基 M表示单键或-S（O）m - ，J表示杂环基，X表示-CH-或氮原子。

9. 发明申请

US20060195256A1 Systems, methods, and programs for updating map data 审中-公开
标题翻译：用于更新地图数据的系统，方法和程序
公开(公告)号：US20060195256A1
公开(公告)日：2006-08-31
申请号：US11299972
申请日：2005-12-13
申请人： Norihiro Nakamura , Naoki Tsuchiya , Seiji Takahata
发明人： Norihiro Nakamura , Naoki Tsuchiya , Seiji Takahata
IPC分类号： G01C21/32
CPC分类号： G09B29/10 , G01C21/32
摘要： Systems, methods, and programs for updating map data create differential data in a server by comparing an old version of map data stored in the server with a new version of map data and transmit the differential data from the server to a relay device. The systems, methods and programs create updated map data by combining the differential data received from the server with map data previously stored in the relay device. The relay device may then be connected to an updated data storing device that disconnectably connects to both the relay device and the navigation system. The systems, methods, and programs, may then transfer the updated map data from the relay device to the updated data storing device and from the updated data storing device to the navigation system.
摘要翻译：用于更新地图数据的系统，方法和程序通过将存储在服务器中的旧版本的地图数据与新版本的地图数据进行比较来创建服务器中的差异数据，并将差分数据从服务器传送到中继设备。系统，方法和程序通过将从服务器接收的差分数据与先前存储在中继设备中的地图数据组合来创建更新的地图数据。然后，中继设备可以连接到可断开地连接到中继设备和导航系统的更新的数据存储设备。然后，系统，方法和程序可以将更新的地图数据从中继设备传送到更新的数据存储设备，并从更新的数据存储设备传送到导航系统。

10. 发明授权

US06884896B2 Benzo[b]thiophene derivatives and process for preparing the same 失效
标题翻译：苯并[b]噻吩衍生物及其制备方法
公开(公告)号：US06884896B2
公开(公告)日：2005-04-26
申请号：US10258173
申请日：2002-02-22
申请人： Hiroshi Saitoh , Naoki Tsuchiya , Tsuyoshi Mizuno , Tomohide Ida , Yoshiyuki Sawai
发明人： Hiroshi Saitoh , Naoki Tsuchiya , Tsuyoshi Mizuno , Tomohide Ida , Yoshiyuki Sawai
IPC分类号： C07D333/54 , C07D333/56 , C07D333/64 , C07D235/24 , C07D333/52
CPC分类号： C07D333/54 , C07D333/56 , C07D333/64
摘要： The present invention is 3,4-disubstituted-benzo[b]thiophene derivatives represented by general formula (I) and processes for preparing compounds represented by general formula (V) from compounds represented by general formula (IV), preparing a mixture of compounds represented by the following formula (II) and the following formula (III) and preparing the benzo[b]thiophene derivatives represented by the above formula (I): wherein, R1 and R2 represent each a halogen atom, a trihalomethyl group, a C1-4 alkyl group or a C1-4 alkoxy group; X represents a hydroxy group or a halogen atom; R3 and R4 represent each a hydrogen or a halogen atom, a trihalomethyl group, a C1-4 alkyl group or a C1-4 alkoxy group; and R5 represents a C1-3 alkyl group or a trifluoromethyl group.
摘要翻译：本发明是由通式（I）表示的3,4-二取代 - 苯并[b]噻吩衍生物和由通式（Ⅳ）表示的化合物制备由通式（Ⅴ）表示的化合物的方法，制备化合物由下式（II）和下式（III）表示并制备由上式（I）表示的苯并[b]噻吩衍生物：其中R 1和R 2 代表卤素原子，三卤代甲基，C 1-4烷基或C 1-4烷氧基; X表示羟基或卤素原子; R 3和R 4各自表示氢或卤素原子，三卤代甲基，C 1-4烷基或C 1-4烷基， C 1-4烷氧基; R 5表示C 1-3烷基或三氟甲基。

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