发明名称 Fused aminodihydrothiazine derivatives
摘要 A compound represented by the general formula:; or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein Ring A is a C6-14 aryl group or the like, L is —NReCO— or the like (wherein Re is a hydrogen atom or the like), Ring B is a C6-14 aryl group or the like, X is a C1-3 alkylene group or the like, Y is a single bond or the like, Z is a C1-3 alkylene group or the like, R1 and R2 are each independently a hydrogen atom or the like, and R3, R4, R5 and R6 are independently a hydrogen atom, a halogen atom or the like, has an Aβ production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by Aβ and typified by Alzheimer-type dementia.
申请公布号 US8946210(B2) 申请公布日期 2015.02.03
申请号 US201113333238 申请日期 2011.12.21
申请人 Eisai R&D Management Co., Ltd. 发明人 Suzuki Yuichi;Motoki Takafumi;Kaneko Toshihiko;Takaishi Mamoru;Ishida Tasuku;Kita Yoichi;Takeda Kunitoshi;Yamamoto Noboru;Khan Afzal;Dimopoulos Paschalis
分类号 C07D239/14;A61K31/5415 主分类号 C07D239/14
代理机构 Fish & Richardson P.C. 代理人 Fish & Richardson P.C.
主权项 1. A compound represented by the formula (I):or a pharmaceutically acceptable salt thereof, wherein Ring A is a C6-14 aryl group which may have 1 to 3 substituents selected from Substituent Group α or a 5- to 6-membered heteroaryl group which may have 1 to 3 substituents selected from Substituent Group α, L is a single bond or a formula —NReCO— (wherein Re is a hydrogen atom or a C1-6 alkyl group which may have 1 to 3 substituents selected from Substituent Group α), Ring B is a C6-14 aryl group which may have 1 to 3 substituents selected from Substituent Group α or a 5- to 10-membered heterocyclic group which may have 1 to 3 substituents selected from Substituent Group α, X is a C1-3 alkylene group which may have 1 to 3 substituents selected from Substituent Group α, Y is a single bond, Z is a single bond or a C1-3 alkylene group which may have 1 to 3 substituents selected from Substituent Group α, R1 and R2 are hydrogen atoms, R3, R4, R5 and R6 are independently a hydrogen atom, a halogen atom, a hydroxy group, a C1-6 alkyl group which may have 1 to 3 substituents selected from Substituent Group α, a C1-6 alkoxy group which may have 1 to 3 substituents selected from Substituent Group α, or R4 and R6 together may form a ring represented by the formula (II):wherein Y, Z, R5 and R3 are the same as defined above and Q is an oxygen atom, a methylene group or an ethylene group, Substituent Group α is a halogen atom, a hydroxy group, a nitro group, a C1-6 alkylthio group, or a cyano group, a C1-6 alkoxy group which may have 1 to 3 substituents selected from Substituent Group β, or a C1-6 alkyl group which may have 1 to 3 substituents selected from Substituent Group β, and Substituent Group β is a halogen atom, a cyano group, a hydroxy group, or a C1-6 alkoxy group.
地址 Tokyo JP