首页> 外国专利> 2-ARYLBENZOTHIOPHENE DERIVATIVES OR PHARCEUTICALLY ACCEPTABLE SALTS THEREOF, PREPARATION METHOD THEREOF, AND PHARCEUTICAL COMPOSITION FOR THE DIAGNOSIS OR TREATMENT OF DEGENERATIVE BRAIN DISEASE CONTAINING THE SAME AS ACTIVE INGREDIENT

2-ARYLBENZOTHIOPHENE DERIVATIVES OR PHARCEUTICALLY ACCEPTABLE SALTS THEREOF, PREPARATION METHOD THEREOF, AND PHARCEUTICAL COMPOSITION FOR THE DIAGNOSIS OR TREATMENT OF DEGENERATIVE BRAIN DISEASE CONTAINING THE SAME AS ACTIVE INGREDIENT

机译:含2-芳基苯并噻吩衍生物或可药用盐,其制备方法以及用于诊断或治疗退行性脑病的药用成分,该成分与活性成分相同

摘要

2-arylbenzothiophene derivatives or pharmaceutically acceptable salts thereof, a preparation method thereof, and a pharmaceutical composition for the diagnosis or treatment of degenerative brain disease containing the same as an active ingredient. Since the 2-arylbenzothiophene derivatives of Formula 1 have a relatively high binding affinity for β-amyloid, they can be used as diagnostic reagents for diagnosing Alzheimer's disease at an early stage by non-invasive techniques when they are labeled with radioisotopes:; ;wherein R1-R4, V, W, X, Y and Z are as defined in the Detailed Descript of the specification. Further, when the pharmaceutical composition containing the 2-arylbenzothiophene derivative binds with a low-molecular weight β-amyloid peptide binding compound, generation of malignant high-molecular weight β-amyloid deposits is minimized. Accordingly, the pharmaceutical composition can be used as a therapeutic agent of degenerative brain disease such as Alzheimer's disease.
机译:含有2-芳基苯并噻吩衍生物或其药学上可接受的盐,其制备方法以及用于诊断或治疗变性性脑病的药物组合物,其包含其作为活性成分。由于式1的2-芳基苯并噻吩衍生物对β-淀粉样蛋白具有相对较高的结合亲和力,因此当它们被放射性同位素标记时,它们可用作早期通过无创技术诊断阿尔茨海默氏病的诊断试剂: ;其中R 1 -R 4 ,V,W,X,Y和Z如规范的详细描述中所定义。此外,当含有2-芳基苯并噻吩衍生物的药物组合物与低分子量β-淀粉样蛋白肽结合化合物结合时,恶性高分子量β-淀粉样蛋白沉积物的产生最小化。因此,该药物组合物可以用作变性性脑病例如阿尔茨海默氏病的治疗剂。

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