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    BENZIMIDAZOLE DERIVATIVES
    55.
    发明公开
    BENZIMIDAZOLE DERIVATIVES 失效
    BENZIMIDAZOLDERIVATE

    公开(公告)号：EP0882718A1

    公开(公告)日：1998-12-09

    申请号：EP96943331.7

    申请日：1996-12-27

    申请人： FUJISAWA PHARMACEUTICAL CO., LTD.

    发明人： YAMASAKI, Noritsugu ,  IMOTO, Takafumi ,  MURAI, Yoshiyuki ,  HIRAMURA, Takahiro ,  OKU, Teruo ,  SAWADA, Kouzou

    IPC分类号： C07D235/08 ,  C07D235/10 ,  C07D235/22 ,  C07D235/24 ,  C07D235/26 ,  C07D235/28 ,  C07D235/30 ,  C07D401/06 ,  C07D401/12 ,  C07D405/06 ,  C07D417/14

    CPC分类号： C07D401/06 ,  C07D209/08 ,  C07D235/08 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D417/06 ,  C07D417/10 ,  C07D417/12 ,  C07D417/14

    摘要： Novel benzimidazole derivatives represented by the formula (I):
    wherein R 3 is a carboxyl group, a esterified carboxyl group, an amidated carboxyl group, an amino group, an amido group, or a sulfonyl group, or their pharmaceutically acceptable salts. Because of their blood sugar-depressing effect or PDE5 inhibitory effect, these compounds or salts thereof are useful as medicines for treating impaired glucose tolerance, diabetes, diabetic complications, syndrome of insulin resistance, hyperlipidemia, atherosclerosis, cardiovascular disorders, hyperglycemia, or hypertension; or stenocardia, hypertension, pulmonary hypertension, congestive heart failure, glomerulopathy, tubulointerstitial disorders, renal failure, atherosclerosis, angiostenosis, distal angiopathy, cerebral apoplexy, chronic reversible obstructions, allergic rhinitis, urticaria, glaucoma, diseases characterized by enteromotility disorders, impotence, diabetic complications, nephritis, cancerous cachexia, or restenosis after PTCA.

    摘要翻译： 式（I）表示的新型苯并咪唑衍生物：其中R 3为羧基，酯化羧基，酰胺化羧基，氨基，酰胺基或磺酰基的或其药学上可接受的盐。 这些化合物或其盐由于其降糖作用或PDE5抑制作用，可用作治疗葡萄糖耐量异常，糖尿病，糖尿病并发症，胰岛素抵抗综合征，高脂血症，动脉粥样硬化，心血管疾病，高血糖或高血压的药物。 或心绞痛，高血压，肺动脉高压，充血性心力衰竭，肾小球病，肾小管间质性疾病，肾衰竭，动脉粥样硬化，血管狭窄症，远端血管病，脑中风，慢性可逆障碍，过敏性鼻炎，荨麻疹，青光眼，以肠蠕动障碍为特征的疾病，阳ence，糖尿病 并发症，肾炎，癌性恶病质，或PTCA后的再狭窄。

    Benzimidazole derivatives, their production and use and use as angiotensin II antagonists
    60.
    发明公开
    Benzimidazole derivatives, their production and use and use as angiotensin II antagonists 失效
    Benzimidazolderivate，ihre Herstellung und Verwendung als Angiotensin II-Antagonisten

    公开(公告)号：EP0720982A1

    公开(公告)日：1996-07-10

    申请号：EP95118796.2

    申请日：1991-04-19

    申请人： TAKEDA CHEMICAL INDUSTRIES, LTD.

    发明人： Naka, Takehiko ,  Nishikawa, Kohei ,  Kato, Takeshi

    IPC分类号： C07D235/26 ,  A61K31/415 ,  C07D235/28 ,  C07D235/30 ,  C07D403/10

    CPC分类号： C07D235/02 ,  C07D235/26 ,  C07D235/28 ,  C07D235/30 ,  C07D403/10 ,  C07D405/14

    摘要： Benzimidazole derivatives of the formula (I):

    wherein the ring A is a benzene ring which may optionally contain substitution in addition to the R' group and R 1 , R 2 , X, R', Y and n are defined as in claim 1; with the exclusion of 2-ethoxy-1-[[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl]-benzimidazole-7-carboxylic acid and 1-(cyclohexyloxycarbonyloxy)ethyl 2-ethoxy-1-[[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl]benzimidazole-7-carboxylate; and the pharmaceutically acceptable salts thereof, have potent angiotensin antagonistic activity and antihypertensive activity, thus being useful as therapeutic agents for treating circulatory system diseases such as hypertensive diseases, heart diseases (e.g. hypercardia, heart failure, cardiac infarction, etc.), strokes, cerebral apoplexy, nephritis, etc.

    摘要翻译： 式（I）的苯并咪唑衍生物：其中环A是可以任选地除R'基团和R 1，R 2，X，R'，Y之外的取代基的苯环，和 n如权利要求1所定义; 除了2-乙氧基-1-Ä2' - （1H-四唑-5-基）联苯-4-基甲基 - 苯并咪唑-7-羧酸和1-（环己基氧基羰基氧基）乙基2-乙氧基-1-Ä2'- （1H-四唑-5-基）联苯-4-基甲基苯并咪唑-7-羧酸酯; 和其药学上可接受的盐具有有效的血管紧张素@拮抗活性和抗高血压活性，因此可用作治疗循环系统疾病如高血压疾病，心脏病（例如高血压，心力衰竭，心肌梗塞等）的治疗剂， 脑卒中，脑中风，肾炎等