Alston & Bird LLP
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
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.
Industry-University Cooperation Foundation Sogang University
A A A A C C A
A61K A61K A61P A61K C07D C07D A61K
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Seung Jun Dae Hyuk Youjung Yu Jin Dae Yoon So Young Jae Seung Heejun Jin-Sook Yoo Jin Uthaiwan Byoung Se
Oh Moon Jung Bae Chi Chu Kim Kim Ryu Lim Sirion Lee