[EN] DIHYDROTHIAZINE AND DIHYDROOXAZINE DERIVATIVES HAVING BACE1 INHIBITORY ACTIVITY<br/>[FR] DÉRIVÉS DE DIHYDROTHIAZINE ET DE DIHYDROOXAZINE PRÉSENTANT UNE ACTIVITÉ INHIBITRICE DE BACE1
申请人:SHIONOGI & CO
公开号:WO2015156421A1
公开(公告)日:2015-10-15
The present invention provides a compound which has an effect of inhibiting amyloid β production, especially an effect of inhibiting BACE1, and which is useful as a therapeutic or phylactic agent for diseases induced by production, secretion and/or deposition of amyloid β proteins. A compound of the formula (I) wherein X is -S- or -O-, R3a is alkyl, haloalkyl or the like, R2a is H, halogen, alkyloxy, haloalkyloxy or the like, R2b is H or the like, R3b is H or alkyl, ring A and ring B is each independently a substituted or unsubstituted aromatic carbocycle, a substituted or unsubstituted aromatic heterocycle or the like, and R1 is substituted or unsubstituted alkyl or the like, or a pharmaceutically acceptable salt thereof.
本发明提供了一种具有抑制淀粉样蛋白β产生作用的化合物,特别是抑制BACE1的作用,并且作为治疗或预防通过淀粉样蛋白β蛋白的产生、分泌和/或沉积引起的疾病的药物或预防剂而有用。其中化合物的结构式(I)中,X为-S-或-O-,R3a为烷基、卤代烷基或类似物,R2a为H、卤素、烷氧基、卤代烷氧基或类似物,R2b为H或类似物,R3b为H或烷基,环A和环B分别独立地为取代或未取代的芳香环烃、取代或未取代的芳香杂环或类似物,R1为取代或未取代的烷基或类似物,或其药学上可接受的盐。