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1-aryl-4-methyl-1,2,4triazolo4,3-aquinoxaline derivatives

机译:1-芳基-4-甲基-[1,2,4]三唑并[4,3-a]喹喔啉衍生物

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.
机译:本发明涉及新颖的1-芳基-4-甲基-[1,2,4]三唑并[4,3-a]-喹喔啉衍生物作为磷酸二酯酶2(PDE2)的抑制剂和较小程度的磷酸二酯酶10(PDE10)的抑制剂)或作为磷酸二酯酶2和10的抑制剂。本发明还涉及包含此类化合物的药物组合物,制备此类化合物和组合物的方法,以及此类化​​合物和组合物在预防和治疗疾病中的用途。 PDE2涉及哪些疾病,或PDE2和PDE10均涉及疾病,例如神经系统疾病和精神疾病以及内分泌或代谢疾病。本发明还涉及放射性标记的化合物,其可用于使用正电子发射断层扫描(PET)对组织中的PDE2酶进行成像和定量。本发明还涉及包含此类化合物的组合物,制备此类化合物和组合物的方法,此类化合物和组合物在体外或体内对组织,细胞或宿主成像的用途以及所述化合物的前体。

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