UK-315716/UK-240455. Pfizer.
Pfizer is developing the atropoisomeric quinoxalinediones, UK-315716 and UK-240255, from a series of NMDA/glycine antagonists for the potential treatment of stroke. Both are compounds are undergoing clinical trials. UK-315716 has improved aqueous solubility and in vivo efficacy over UK-240455, and a lower projected clinical dose of 200 mg compared to 500 mg with UK-240455.
Capelli
A M
AM
GlaxoSmithKline, Medicines Research Centre, Chemistry Dept, Verona, Italy.
Micheli
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F
D000818:Animals; D017321:Clinical Trials, Phase I as Topic; D006801:Humans; D018696:Neuroprotective Agents / Q000494:pharmacology* / Q000627:therapeutic use; D011810:Quinoxalines / Q000494:pharmacology* / Q000627:therapeutic use; D018009:Receptors, Glycine / Q000037:antagonists & inhibitors*; D016194:Receptors, N-Methyl-D-Aspartate / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
D018696:Neuroprotective Agents; D011810:Quinoxalines; D018009:Receptors, Glycine; D016194:Receptors, N-Methyl-D-Aspartate; C464530:UK240455; C464529:UK315716