发明名称 4-OXO-3,4-DIHYDRO-1,2,3-BENZOTRIAZINE MODULATORS OF GPR139
摘要 The present invention provides a method for treating a disease, disorder or condition associated with GPR139 using compounds of formula 1:;;which are agonists of GPR139, certain compounds encompassed by formula 1, pharmaceutical compositions thereof, processes for making the compounds, and intermediates thereof.
申请公布号 US2016145218(A1) 申请公布日期 2016.05.26
申请号 US201514946194 申请日期 2015.11.19
申请人 Takeda Pharmaceutical Company Limited 发明人 Hitchcock Stephen;Lam Betty;Monenschein Holger;Reichard Holly
分类号 C07D253/08;A61K31/53 主分类号 C07D253/08
代理机构 代理人
主权项 1. A compound of formula 2: or a pharmaceutically acceptable salt thereof, wherein m is selected from 0, 1, and 2; n is selected from 0, 1, and 2; each R1 is independently selected from the group consisting of cyano, halo, hydroxy, amino, C1-4 alkyl, C1-4 alkoxy, trifluoromethyl, and trifluoromethoxy; each R4 is independently selected from the group consisting of cyano, halo, hydroxy, amino, C1-4 alkyl, C1-4 alkoxy, trifluoromethyl, fluoromethoxy, difluoromethoxy, and trifluoromethoxy; and R5 is selected from the group consisting of hydrogen, trifluoromethyl, and C1-4 alkyl, provided: (a) if R5 is hydrogen, methyl, n-propyl, i-propyl, or i-butyl, then m and n are not both 0;(b) if R5 is hydrogen, m is 0, and n is 1, then R4 is not chloro, methoxy, 3-trifluoromethyl, 4-trifluoromethyl, 4-methyl, 4-fluoro, 2-difluoromethoxy 3-difluoromethoxy, 2-trifluoromethoxy, 4-trifluoromethoxy, 4-trifluoroethoxy, or 2-(i-butoxy);(c) if R5 is methyl, m is 0, and n is 1, then R4 is not chloro, 2-fluoro, 4-fluoro, 2-bromo, 4-ethyl, 2-methyl, 4-(i-propyl), 4-(i-butyl), or 3-trifluoromethyl;(d) if R5 is ethyl, m is 0, and n is 1, then R4 is not 3-chloro, 4-chloro, 4-bromo, 4-methyl, 4-methoxy, or 2-difluoromethoxy;(e) if R5 is n-propyl, m is 0, and n is 1, then R4 is not 3-trifluoromethyl;(f) if R5 is i-propyl, m is 0, and n is 1, then R4 is not 4-fluoro or 4-methoxy;(g) if R5 is i-butyl, m is 0, and n is 1, then R4 is not 3-trifluoromethyl;(h) if R5 is hydrogen, m is 0, and n is 2, then R4 is not 2,6-difluoro, 2,4-dichloro, 3,5-dimethoxy, 3,4-dimethoxy, 4-methoxy-3-difluoromethoxy, 4-fluoro-2-trifluoromethyl, or 5-bromo-2-difluormethoxy; and(i) if R5 is methyl, m is 0, and n is 2, then R4 is not 3,4-dimethyl, 3,4-dichloro, 2,4-dichloro, 3-fluoro-4-methoxy, 3-bromo-4-methoxy, 3-methoxy-4-isopropyloxy, or 3-methoxy-4-isobutyloxy.
地址 Osaka JP