Patent number: 6281211
Abstract: This invention is related to substituted semicarbazides represented by Formula (I) or a pharmaceutically acceptable salt or prodrug thereof, wherein: R1 and R2 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl; R3, R4, R5 and R6 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl, or R3 and R4 is defined as above, and R5 and R6 together with the nitrogen atom to which they are attached form a heterocycle, including piperidine, piperazine, morpholine; A1 and A2 are independently aryl, heteroaryl, saturated or partially unsaturated carbocycle or saturated or partially unsaturated heterocycle, any of which is optionally substituted; X is one of O, S, NR7, CH2, C(O), NR7C(O), C(O)NR7, SO, SO2 or a covalent bond; where R7 is hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl; n is
Type:
Grant
Filed:
September 21, 2000
Date of Patent:
August 28, 2001
Assignee:
Euro-Celtique S.A.
Inventors:
Sui Xiong Cai, Nancy C. Lan, Soo Hong-Bae
Patent number: 6218404
Abstract: The invention relates to subtype-selective NMDA receptor ligands and the use thereof for treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating neuro-degenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease and Down's syndrome, treating or preventing the adverse consequences of the overstimulation of the excitatory amino acids, treating anxiety, psychosis, convulsions, aminoglycoside antibiotics-induced hearing loss, migraine headache, chronic pain, Parkinson's disease, glaucoma, CMV retinitis, urinary incontinence, opioid tolerance or withdrawal, and inducing anesthesia, as well as for enhancing cognition.
Type:
Grant
Filed:
September 16, 1998
Date of Patent:
April 17, 2001
Assignees:
Warner-Lambert Co., Cocensys, Inc.
Inventors:
Christopher F. Bigge, Gian Luca Araldi, Sui Xiong Cai, Anthony P. Guzikowski, Donald Lamunyon, Nancy F. Lan, Zhang-Lin Zhou, John F. W. Keana
Patent number: 5863916
Abstract: Disclosed are compounds of the formula: ##STR1## or pharmaceutically acceptable salts thereof; wherein n is zero or 1; R.sup.4, R.sup.5, R.sup.6 are independently hydrogen, nitro, amino, halo, haloalkyl, cyano, alkyl, cycloalkyl, alkenyl, alkynyl, azido, acylamino, alkylsulfonyl, aryl, substituted aryl, heteroaryl, alkoxy, trialkylsilyl-substituted alkoxy, aryloxy, substituted aryloxy, heteroaryloxy, a heterocyclic group, a heterocyclicoxy group, aralkoxy, or haloalkoxy; and R.sup.c and R.sup.d are defined in the specification. These compounds have high binding to the glycine site of the NMDA receptor. Also disclosed are methods of treating pathophysiologic conditions associated with neuronal degeneration, convulsions, anxiety, chronic pain, pyschosis, opiate tolerance, and inducing anesthesia.
Type:
Grant
Filed:
February 4, 1997
Date of Patent:
January 26, 1999
Assignees:
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, The Regents of the University of California, Cocensys, Inc.
Inventors:
Sui Xiong Cai, John F. W. Keana, Eckard Weber