NOVEL 1,4-DIHYDROQUINOXALINE-2,3-DIONES AND USES THEREFOR AS GLYCINE RECEPTOR ANTAGONISTS

摘要

Methods of treating or preventing neuronal loss associated with stroke,ischemia, CNS trauma, hypoglyemia and surgery, as well as treatingneurodegenerative diseases including Alzheimer's disease, amyotrophic lateralsclerosis, Huntington's disease and Down's syndrome, treating or preventingthe adverse consequences of hyperactivity of the excitatory amino acids,treating anxiety, chronic pain, convulsions, inducing anesthesia and psychosisby administering to an animal in need of such treatment a compound havinghigh affinity for the glycine binding site, lacking PCP side effects and whichcrosses the blood brain barrier of the animal. Novel 1,4-dihydroquinoxaline-2,3-diones having the Formula:or a tautomer thereof or a pharmaceutically acceptable salt thereof;wherein R1 is amino, hydroxylamino, acylamino, halo, haloalkyl, or nitro; R2is hydrogen, amino, hydroxylamino, acylamino, halo, haloalkyl, or nitro; R3 isamino, hydroxylamino, acylamino, halo, or haloalkyl; and R4 is hydrogen, andpharmaceutical compositions thereof and highly soluble ammonium saltsthereof are disclosed.