[EN] FUSED AMINODIHYDROTHIAZINE DERIVATIVES<br/>[FR] DÉRIVÉS D'AMINODIHYDROTHIAZINE FUSIONNÉS
申请人:EISAI R&D MAN CO LTD
公开号:WO2012093148A1
公开(公告)日:2012-07-12
The present invention relates to a fused aminodihydrothiazine derivative of formula (I): wherein R is hydrogen or C1 -6 alkyl,optionally substituted by one to five halogen atoms; n is 0,1,2 or 3; Ar is phenyl or a 5-or 6-membered heteroaromatic group containing 1,2 or 3 N atoms,which Ar is optionally substituted by one to three substituents selected from hal, hydroxyl,-CN,C1-6alkyl,C2-3alkenyl,C2-3alkynyl,C-6alkoxy,C3-6cycloalkoxy and pyrazine,where C1-6alkyl and C1-6alkoxy are optionally substituted by one to three halogen atoms; and pharmaceutically acceptable salts thereof; which compound has an Aβ production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease1 caused by Aβ and typified by Alzheimer-type dementia.
本发明涉及一种公式(I)的融合氨基二氢噻唑衍生物:其中R是氢或C1-6烷基,可选地被一个至五个卤素原子取代;n是0、1、2或3;Ar是苯基或含1、2或3个N原子的5或6元杂芳基族,该Ar可选地被一个至三个选自卤素、羟基、-CN、C1-6烷基、C2-3烯基、C2-3炔基、C-6烷氧基、C3-6环烷氧基和吡嗪的取代基取代,其中C1-6烷基和C1-6烷氧基可选地被一个至三个卤素原子取代;以及药用可接受的盐;该化合物具有Aβ生成抑制效果或BACE1抑制效果,并且用作预防或治疗由Aβ引起的神经退行性疾病1的预防或治疗剂,该疾病以阿尔茨海默症型痴呆为典型。