ARYL DERIVATIVES SUBSTITUTED WITH (3-FLUORO-2-HYDROXY) PROPYL GROUP OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION FOR THE DIAGNOSIS OR TREATMENT OF DEGENERATIVE BRAIN DISEASE CONTAINING THE SAME AS AN ACTIVE INGREDIENT
The present disclosure relates to an aryl derivative substituted with a (3-fluoro-2-hydroxy)propyl group or a pharmaceutically acceptable salt thereof, a method for preparing the same, and a pharmaceutical composition for the diagnosis or treatment of a degenerative brain disease containing the same as an active ingredient. With the (3-fluoro-2-hydroxy)propyl group introduced, the derivative according to the present disclosure has an increased polarity and thus can easily pass through the blood-brain barrier. Further, since it strongly binds to β-amyloid, it can be used as a diagnostic reagent for detecting Alzheimer’s disease early in a noninvasive manner after labeling with an isotope. In addition, since it binds with low molecular weight β-amyloid peptide aggregates and inhibits formation of malignant, high molecular weight β-amyloid plaques, it may be used as a therapeutic agent for a degenerative brain disease such as Alzheimer’s disease.本發明係關於一種取代為(3-氟-2-羥基)丙基之芳香基衍生物或其藥學可接受鹽類、其製備方法,以及包含其作為活性成分用於退化性腦疾病之診斷或治療之藥學組合物。有該導入之(3-氟-2-羥基)丙基,依據本發明之該衍生物具有增加之極性且因此能輕易地通過該血腦障壁。再者,因其強烈地結合至β-類澱粉,於同位素標誌後,可用作以非侵入方式偵測阿茲海默症之診斷試劑。此外,因其結合至低分子量的β-類澱粉胜肽集合體且抑制惡性、高分子量β-類澱粉斑塊之形成,本發明之該衍生物可作為用於治療腦退化性疾病(如:阿茲海默症)之治療藥劑。該圖為一數據圖故無元件代表符號。
