发明公开
EP2723744A1 1-ARYL-4-METHYL-[1,2,4]TRIAZOLO[4,3-a]QUINOXALINE DERIVATIVES
有权
1-芳基-4-甲基 - [1,2,4]三唑并[4,3-A] -CHINOXALIN衍
- 专利标题: 1-ARYL-4-METHYL-[1,2,4]TRIAZOLO[4,3-a]QUINOXALINE DERIVATIVES
- 专利标题(中): 1-芳基-4-甲基 - [1,2,4]三唑并[4,3-A] -CHINOXALIN衍
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申请号: EP12729637.4申请日: 2012-06-26
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公开(公告)号: EP2723744A1公开(公告)日: 2014-04-30
- 发明人: ANDRÉS-GIL, José, Ignacio , ROMBOUTS, Frederik, Jan, Rita , TRABANCO-SUÁREZ, Andrés, Avelino , VANHOOF, Greta, Constantia, Peter , DE ANGELIS, Meri , BUIJNSTERS, Peter, Jacobus, Johannes, Antonius , GUILLEMONT, Jerôme, Emile, Georges , BORMANS, Guy, Maurits R. , CELEN, Sofie, Jeanne, Leopoldine , VLIEGEN, Maarten
- 申请人: Janssen Pharmaceutica, N.V.
- 申请人地址: Turnhoutseweg 30 2340 Beerse BE
- 专利权人: Janssen Pharmaceutica, N.V.
- 当前专利权人: Janssen Pharmaceutica, N.V.
- 当前专利权人地址: Turnhoutseweg 30 2340 Beerse BE
- 代理机构: Garcia Prieto, Maria
- 优先权: EP11171519 20110627
- 国际公布: WO2013000924 20130103
- 主分类号: C07D487/04
- IPC分类号: C07D487/04 ; A61K31/4985 ; A61P25/00
摘要:
The present invention relates to novel l-aryl-4-methyl-[l,2,4]triazolo[4,3-a]- quinoxaline derivatives as inhibitors of phosphodiesterase 2 (PDE2) and to a lesser extent of phosphodiesterase 10 (PDE10) or as inhibitors of both, phosphodiesterases 2 and 10. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which PDE2 is involved, or disorders in which both PDE2 and PDE10 are involved, such as neurological and psychiatric disorders, and endocrinological or metabolic diseases. The present invention also relates to radiolabeled compounds which may be useful for imaging and quantifying the PDE2 enzyme in tissues, using positron- emission tomography (PET). The invention is also directed to compositions comprising such compounds, to processes for preparing such compounds and compositions, to the use of such compounds and compositions for imaging a tissue, cells or a host, in vitro or in vivo and to precursors of said compounds.
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