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NOVEL SUBSTITUTED-1H-QUINAZOLINE-2,4-DIONE DERIVATIVES, PREPARATION METHOD THEREOF AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME
NOVEL SUBSTITUTED-1H-QUINAZOLINE-2,4-DIONE DERIVATIVES, PREPARATION METHOD THEREOF AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME
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机译:新型取代的1H-喹唑啉-2,4-二酮衍生物,其制备方法和包含该衍生物的药物组合物
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摘要
Disclosed herein are novel substituted-1H-quinazoline-2,4-dione derivatives, a preparation method thereof, and a pharmaceutical composition containing the same. The novel substituted-1H-quinazoline-2,4-dione derivatives are excellent in binding affinity and selectivity for 5-HT6 receptors over other receptors, inhibit serotonin(5-HT)-stimulated cAMP accumulation, and disrupt apomorphine(2 mg/kg, i.p.)-induced hyperactivity in rats. Thanks to these effects, the derivatives are useful in the treatment of 5-HT6 receptor-related central nervous system diseases.
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机译:本文公开了新颖的取代的-1H-喹唑啉-2,4-二酮衍生物,其制备方法以及含有该衍生物的药物组合物。新型取代的1H-喹唑啉-2,4-二酮衍生物对5-HT6受体的结合亲和力和选择性优于其他受体,抑制5-羟色胺(5-HT)刺激的cAMP积累,并破坏阿扑吗啡(2 mg / kg ,ip)诱导的大鼠活动过度。由于这些作用,这些衍生物可用于治疗5-HT6受体相关的中枢神经系统疾病。
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