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    • 4. 发明申请
    • INDOLE DERIVATIVES
    • INDOLE DORIVATIVES
    • WO1998015530A1
    • 1998-04-16
    • PCT/JP1997003592
    • 1997-10-07
    • FUJISAWA PHARMACEUTICAL CO., LTD.YAMASAKI, NoritsuguIMOTO, TakafumiMURAI, YoshiyukiHIRAMURA, TakahiroONOMURA, OsamuNISHIKAWA, MasahiroOKU, TeruoSAWADA, KouzouKAYAKIRI, Hiroshi
    • FUJISAWA PHARMACEUTICAL CO., LTD.
    • C07D209/08
    • C07D401/06C07D209/08C07D401/12C07D403/06C07D403/12C07D405/06C07D405/12C07D417/06C07D417/10C07D417/12C07D417/14
    • Novel indole derivatives represented by general formula (V) or pharmaceutically acceptable salts thereof. Because of having hypoglycemic or PDE5-inhibitory activities, these compouds or salts thereof are useful as remedies for impaired glucose tolerance, diabetes, complication of diabetes, insulin resistant syndrome, hyperlipidemia, atherosclerosis, cardiovascular diseases, hyper glycemia, hypertension; diseases characterized by angina pectoris, high blood pressure, pulmonary hypertension, congestive heart failure, glomerular diseases, tubular interstitial diseases, renal insufficiency, atherosclerosis, angiostenosis, peripheral vascular diseases, cerebral stroke, chronic reversible obstructive diseases, allergic rhinitis, urticaria, glaucoma or intestinal motility disorders; sexual impotence, complication of diabetes, osteoporosis, nephritis, cancerous cachexia or post-PTCA reconstriction, wherein R13 to R15 represent each: 1) hydrogen, 2) lower alkyl, lower alkylthio or lower alkoxy-substituted lower alkyl, or 3) lower alkyl, hydroxy, hydroxylated lower alkyl, lower alkyloxy, etc. bonded to or substituted by aryl or a heterocycle; provided that R13 to R15 do not represent hydrogen at the same time; R16 represents: 1) hydrogen, or 2) lower alkyl; and R17 represents optionally esterified carboxy.
    • 由通式(V)表示的新型吲哚衍生物或其药学上可接受的盐。 由于具有低血糖或PDE5抑制活性,这些化合物或其盐可用作葡萄糖耐量降低,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,高血糖症,高血压症的补救措施; 特征为心绞痛,高血压,肺动脉高压,充血性心力衰竭,肾小球疾病,肾小管间质疾病,肾功能不全,动脉粥样硬化,血管狭窄症,外周血管疾病,脑中风,慢性可逆性阻塞性疾病,过敏性鼻炎,荨麻疹,青光眼或 肠蠕动障碍; 性功能障碍,糖尿病并发症,骨质疏松症,肾炎,癌性恶病质或PTCA后重建,其中R13至R15各自表示:1)氢,2)低级烷基,低级烷硫基或低级烷氧基取代的低级烷基,或3)低级烷基 ,羟基,羟基化的低级烷基,低级烷氧基等,与芳基或杂环结合或取代; 条件是R13至R15不同时代表氢; R16表示:1)氢,或2)低级烷基; R 17代表任意酯化的羧基。