发明名称 Substituted triazolyl piperazine and triazolyl piperidine derivatives as gamma secretase modulators
摘要 The present invention is concerned with novel substituted triazolyl piperazine and triazolyl piperidine derivatives of Formula (I); wherein R1, R2, R3, R4a, R4b, R5, X, Y1, Y2, L1, and L2 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
申请公布号 US8987276(B2) 申请公布日期 2015.03.24
申请号 US201214005598 申请日期 2012.03.22
申请人 Janssen Pharmaceuticals, Inc.;Cellzome Limited 发明人 Bischoff Francois Paul;Velter Adriana Ingrid;Van Brandt Sven Franciscus Anna;Berthelot Didier Jean-Claude
分类号 A61K31/496;A61K31/506;C07D249/14;C07D401/04;C07D401/14;C07D403/04;C07D249/10 主分类号 A61K31/496
代理机构 Baker & Hostetler LLP 代理人 Baker & Hostetler LLP
主权项 1. A compound of Formula (I)or a stereoisomeric form thereof, wherein R1 and R2 independently are selected from the group consisting of hydrogen, halo, C1-4 alkyl, C1-4 alkyloxy, C1-4 alkyl substituted with one or more halo substituents, and C1-4 alkyloxy substituted with one or more halo sub stituents; L1 is NR6, O, carbonyl or a covalent bond; wherein R6 is hydrogen or C1-4 alkyl; R3 represents C1-4 alkyl; R4a and R4b independently are selected from the group consisting of hydrogen and C1-4 alkyl; X is N or CH; L2 is O, CH2 or a covalent bond; provided that when L2 is O, then X is CH; R5 is hydrogen or C1-4 alkyl; Y1 is CH or N; Y2 is CR7 or N; wherein R7 represents H or C1-4 alkyloxy; or a pharmaceutically acceptable addition salt or a hydrate thereof.
地址 Titusville NJ US