发明名称 Tetrahydroimidazo(1,5-D)[1,4]oxazepine derivative
摘要 A compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof works as an mGluR2 antagonist, and is applicable as a therapeutic agent for neurological disorders related to glutamate dysfunction and diseases involving the mGluR2, such as Alzheimer's disease:;wherein R is a hydrogen atom, a C1-6 alkyl group or the like, R1 is a C1-6 alkyl group, a C1-6 alkoxy group or the like, R2 is a halogen atom, a C1-6 alkyl group, a C1-6 alkoxy group or the like, R3 is a hydrogen atom, a C1-6 alkyl group or the like, and R4 is a C1-6 alkyl group or the like.
申请公布号 US9458176(B2) 申请公布日期 2016.10.04
申请号 US201414190356 申请日期 2014.02.26
申请人 Eisai R&D Management Co., Ltd. 发明人 Takaishi Mamoru;Sato Nobuhiro;Shibuguchi Tomoyuki;Motoki Takafumi;Takahashi Yoshinori;Sasaki Takeo;Braunton Alan
分类号 A61K31/553;C07D498/04 主分类号 A61K31/553
代理机构 Fish & Richardson P.C. 代理人 Fish & Richardson P.C.
主权项 1. A compound represented by the following formula (I) or a pharmaceutically acceptable acid addition salt thereof: wherein R is a hydrogen atom or a C1-6 alkyl group optionally substituted with 1 to 3 fluorine atoms, wherein when R is a hydrogen atom, R1 is a chlorine atom, a bromine atom, a trifluoromethyl group, an ethyl group, a trifluoromethoxy group, a methoxy group substituted with a phenyl group, a methoxy group substituted with a C3-8 cycloalkyl group, an ethoxy group optionally substituted with 1 to 3 fluorine atoms, or C3-8 cycloalkyloxy group,R2 is a fluorine atom, a chlorine atom, a methyl group optionally substituted with 2 to 3 fluorine atoms, a methoxy group optionally substituted with 1 to 3 fluorine atoms, or an ethoxy group optionally substituted with 1 to 3 fluorine atoms,R3 is a hydrogen atom or a methyl group, andR4 is a fluorine atom or a methyl group optionally substituted with 1 to 3 fluorine atoms, or when R is a C1-6 alkyl group optionally substituted with 1 to 3 fluorine atoms, R1 is a hydrogen atom, a halogen atom, a C1-6 alkyl group optionally substituted with 1 to 3 fluorine atoms, a C1-6 alkoxy group optionally substituted with 1 to 3 substituents selected from a fluorine atom and a C3-8 cycloalkyl group, a C3-8 cycloalkyloxy group, or a 4- to 6-membered heterocycloalkyloxy group,R2 is a hydrogen atom, a cyano group, a halogen atom, a C1-6 alkyl group optionally substituted with 1 to 3 substituents selected from a fluorine atom and a hydroxyl group, or a C1-6 alkoxy group optionally substituted with 1 to 3 substituents selected from a fluorine atom, a C3-8 cycloalkyl group and a 4- to 6-membered heterocycloalkyl group,R3 is a hydrogen atom or a C1-6 alkyl group, andR4 is a C1-6 alkyl group optionally substituted with 1 to 3 substituents selected from a fluorine atom and a hydroxyl group, or a C1-6 alkoxy group.
地址 Tokyo JP