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    Benzimidazole derivative
    2.
    发明授权
    Benzimidazole derivative 失效
    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。

    Benzene derivatives
    5.
    发明授权
    Benzene derivatives 失效
    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。

    Drugs comprising chymase inhibitors and ACE inhibitors as effective ingredients
    6.
    发明申请
    Drugs comprising chymase inhibitors and ACE inhibitors as effective ingredients 审中-公开
    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。

    Drug containing chymase inhibitor as the active ingredient
    7.
    发明申请
    Drug containing chymase inhibitor as the active ingredient 审中-公开
    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。

    Benzo[b]thiophene derivatives and process for preparing the same
    8.
    发明授权
    Benzo[b]thiophene derivatives and process for preparing the same 失效
    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。

    3-Hydroxymethylbenzo[b]thiophene derivatives and process for their preparation
    9.
    发明授权
    3-Hydroxymethylbenzo[b]thiophene derivatives and process for their preparation 失效
    3-羟甲基苯并[b]噻吩衍生物及其制备方法

    公开(公告)号：US06774245B2

    公开(公告)日：2004-08-10

    申请号：US10332079

    申请日：2003-01-02

    申请人： Hiroshi Saitoh ,  Tsuyoshi Mizuno ,  Naoki Tsuchiya

    发明人： Hiroshi Saitoh ,  Tsuyoshi Mizuno ,  Naoki Tsuchiya

    IPC分类号： C07D33356

    CPC分类号： C07D333/56

    摘要： The present invention is a method of producing a 3-hydroxymethyl-benzo[b]thiophene derivative without the possible concomitant formation of isomers, which comprises selectively cyclizing a sulfoxide having X shown in the reaction scheme below: wherein R1 to R3 are, same or independently, a hydrogen atom, an alkyl group having 1 to 4 carbons, a trihalomethyl group, an alkoxy group having 1 to 4 carbons, an alkylthio group having 1 to 4 carbons, or a trihalomethoxy group; R4 is an acyl group; X is a halogen atom, a hydroxy group, an amino group, a mercapto group, an alkylthio group having 1 to 9 carbons, an acyloxy group having 1 to 9 carbons, an acylamino group having 1 to 9 carbons, or a trihalomethoxy group.

    摘要翻译： 本发明是一种不含可能伴随形成异构体的3-羟甲基 - 苯并[b]噻吩衍生物的制备方法，该方法包括选择性环化下述反应方案中所示的具有X的亚砜：其中R1至R3相同或相同 独立地为氢原子，碳原子数1〜4的烷基，三卤代甲基，碳原子数1〜4的烷氧基，碳原子数1〜4的烷硫基或三卤甲氧基。 R4是酰基; X是卤素原子，羟基，氨基，巯基，碳原子数1〜9的烷硫基，碳原子数1〜9的酰氧基，碳原子数1〜9的酰氨基或三卤代甲氧基。