Patent Number: 6,251,948

Title: Tri-and tetra-substituted guanidines and their use as excitatory amino acid antagonists

Abstract: Tri- and tetra-substituted guanidines which exhibit a high binding affinity to phencyclidine (PCP) receptors and, more preferably, low affinity to the brain sigma receptors. These guanidine derivatives act as non-competitive inhibitors of glutamate induced responses of the NMDA receptor by acting as blockers for the ion channel of the NMDA receptor-ion channel complex. These compounds thus exert neuroprotective activity and are useful in the therapeutic treatment of neuronal loss in hypoxia, hypoglycemia, brain or spinal cord ischemia, and brain or spinal chord trauma as well as being useful for the treatment of epilepsy, Alzheimer's disease, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, Down's Syndrome, Korsakoff's disease and other neurodegenerative disorders.

Inventors: Weber; Eckard (Laguna Beach, CA), Keana; John F. W. (Eugene, OR)

Assignee: State of Oregon, acting by and through the Oregon State Board of Higher Education, acting for and on behalf of the Oregon Health Sciences University and the University of Oregon

International Classification: A61K 31/155 (20060101); B41J 2/435 (20060101); B41J 2/47 (20060101); C07C 279/00 (20060101); C07C 279/18 (20060101); C07D 311/18 (20060101); C07D 311/00 (20060101); G03G 15/16 (20060101); A61K 031/155 (); A61K 031/35 (); A61K 031/44 (); A61K 031/33 ()

Expiration Date: 06/26/2018