The present invention proposes a series of novel substituted quinoxaline 2,3-diones useful as neuroprotective agents. Also proposed are new intermediates, preparation methods and pharmaceutical compositions containing the compound. The compound is a glutamate antagonist and can be used in the treatment of stroke, cerebral ischemia, or cerebral infarction caused by thromboembolic or hemorrhagic stroke, cerebral vasospasm, hypoglycemia, cardiac arrest, status epilepticus, and peripartum asphyxia , hypoxia, Alzheimer's disease, Parkinson's disease and Huntington's disease.