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DIHYDROTHIAZINE AND DIHYDROOXAZINE DERIVATIVES HAVING BACE1 INHIBITORY ACTIVITY
专利权人:
发明人:
KUSAKABE, KEN-ICHI,日下部兼一,日下部兼一,TADANO, GENTA,只野元太,只野元太,KOMANO, KAZUO,驹野和雄,駒野和雄,FUCHINO, KOUKI,渊野光记,淵野光記,NAKAHARA, KENJI,中原健二,中原健二
申请号:
TW104111465
公开号:
TW201623295A
申请日:
2015.04.09
申请国别(地区):
TW
年份:
2016
代理人:
摘要:
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 prophylactic 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, R1 is substituted or unsubstituted alkyl or the like, R5 is halogen or substituted or unsubstituted alkyl, and n is an integer of 0 to 2, or a pharmaceutically acceptable salt thereof.本發明提供一種化合物,其具有抑制澱粉狀蛋白β產生之效果,尤其為抑制BACE1之效果,且其適用作由澱粉狀蛋白β蛋白之產生、分泌及/或沈積所誘發之疾病的治療劑或預防劑。一種式(I)之化合物:其中X為-S-或-O-,R3a為烷基、鹵烷基或其類似基團,R2a為H、鹵素、烷氧基、鹵烷氧基或其類似基團,R2b為H或其類似基團,R3b為H或烷基,環A及環B各自獨立地為經取代或未經取代之芳族碳環、經取代或未經取代之芳族雜環或其類似基團,R1為經取代或未經取代之烷基或其類似基團,R5為鹵素或經取代或未經取代之烷基,且n為0至2之整數,或其醫藥學上可接受之鹽。
来源网站:
中国工程科技知识中心
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