发明名称 Chemical compounds
摘要 The invention relates to a novel compound of formula (I) or a stereoisomer, or a racemate or a mixture or a pharmaceutically acceptable salt thereof: wherein: R is phenyl or a 5- or 6-membered heteroaryl ring containing 1 to 3 heteroatoms selected from S, N and O, such rings may be optionally substituted with n groups Q; Q is selected from a group consisting of: C1-C4 alkyl, halogen, halo C1-C4 alkyl, C1-C4 alkoxy, CN, SO2CH3 or a group —O[(CR1R2]pQ1; or Q may be a group Q2; Q1 is phenyl, which may be optionally substituted with n substituents selected from a group consisting of: C1-C4 alkyl, halogen, halo C1-C4 alkyl, C1-C4 alkoxy, CN, or a group Q2; or corresponds to 2,2-difluoro-benzo[d][1,3]dioxol-4-yl; Q2 is a 5- or 6-membered heteroaryl containing at least one nitrogen atom, which may optionally substituted with n substituents selected from a group consisting of: C1 C1-C4 alkyl, halogen, halo C1-C4 alkyl, C1-C4 alkoxy, CN; P is a 6-membered heteroaryl or a 8-1 1 membered bicyclic heteroaryl group, which may be substituted with n substituents selected from a group consisting of: C1-C4 alkyl, halogen, halo C1-C4 alkyl, C1-C4 alkoxy, CN; R1 is hydrogen or C1-C3 alkyl; R2 is hydrogen or C1-C3 alkyl; n is 1, 2 or 3; p is 0, 1 or 2; and with the proviso that when R corresponds to phenyl, P is substituted by at least one CF3; processes for the preparation of those compounds, pharmaceutical compositions containing one or more compounds of formula (I) and their use as dual antagonists of the Orexin 1 and Orexin 2 receptors.;
申请公布号 US9062033(B2) 申请公布日期 2015.06.23
申请号 US201214366743 申请日期 2012.12.20
申请人 Rottapharm Biotech S.R.L. 发明人 Stasi Luigi Piero;Rovati Lucio Claudio;Artusi Roberto;Colace Fabrizio;Mandelli Stefano;Perugini Lorenzo
分类号 C07D417/14;C07D403/14;C07D471/04;C07D401/12;C07D413/14;A61K31/505;A61K31/4439;A61K31/427;C07D401/14;C07D405/14 主分类号 C07D417/14
代理机构 Jones Day 代理人 Jones Day
主权项 1. A compound of formula (I) or a stereoisomer, a racemate, or a pharmaceutically acceptable salt thereof: wherein: R is phenyl or a 5- or 6-membered heteroaryl ring containing 1 to 3 heteroatoms selected from S, N, and O, such rings may be optionally substituted with n groups Q; Q is C1-C4 alkyl, halogen, halo C1-C4 alkyl, C1-C4 alkoxy, CN, SO2CH3 or —O[CR1R2)]pQ1; or Q may be a group Q2; Q1 is phenyl, which may be optionally substituted with n substituents selected from C1-C4 alkyl, halogen, halo C1-C4 alkyl, C1-C4 alkoxy, CN, or a group Q2; or Q1 corresponds to 2,2-difluorobenzo[d][1,3]dioxol-4-yl; Q2 is a 5- or 6-membered heteroaryl containing at least one nitrogen atom, which may be optionally substituted with n substituents selected from C1-C4 alkyl, halogen, halo C1-C4 alkyl, C1-C4 alkoxy, or CN; P is a 6-membered heteroaryl or a 8-11 membered bicylic heteroaryl group, which may be substituted with n substituents selected from C1-C4 alkyl, halogen, halo C1-C4 alkyl, C1-C4 alkoxy, or CN; R1 is hydrogen or C1-C3 alkyl; R2 is hydrogen or C1-C3 alkyl; n is 1, 2, or 3; p is 0, 1, or 2; and with the proviso that when R corresponds to phenyl, which may be optionally substituted, P is substituted by at least one CF3.
地址 Monza IT