2-arylbenzothiophene derivatives or pharmaceutically acceptable salts thereof, preparation method thereof, and pharmaceutical composition for the diagnosis or treatment of degenerative brain disease containing the same as active ingredient
申请人:Chi Dae Yoon
公开号:US08497260B2
公开(公告)日:2013-07-30
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.
本发明涉及2-芳基苯并噻吩衍生物或其药学上可接受的盐,其制备方法以及含有其作为活性成分的用于诊断或治疗退行性脑病的制药组合物。由于式1中的2-芳基苯并噻吩衍生物具有相对较高的β-淀粉样蛋白结合亲和力,因此当它们被标记为放射性同位素时,它们可以用于非侵入性技术诊断早期阿尔茨海默病的诊断试剂。其中,R1-R4、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制药组合物与低分子量β-淀粉样肽结合化合物结合时,可以最小化致恶性高分子量β-淀粉样沉积物的产生。因此,该制药组合物可用作治疗退行性脑病,如阿尔茨海默病的治疗剂。