Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...
Patent
1993-06-03
1994-10-25
Springer, David B.
Organic compounds -- part of the class 532-570 series
Organic compounds
Heterocyclic carbon compounds containing a hetero ring...
548548, 548549, C07D207404, C07D207448
Patent
active
053590872
ABSTRACT:
The present invention provides bioactive compounds of the general formula: ##STR1## wherein R is H, (C.sub.1 -C.sub.4)alkyl, (C.sub.3 -C.sub.6)cycloalkyl, (C.sub.3 -C.sub.6)cycloalkyl(C.sub.1 -C.sub.4)alkyl, allyl, (C.sub.6 -C.sub.10)aryl or (C.sub.1 -C.sub.4)alkylCO.sub.2 Y; Y is H, (C.sub.1 -C.sub.4)alkyl or (C.sub.6 -C.sub.10)aryl; each X is individually H, (C.sub.1 -C.sub.4)alkyl, (C.sub.6 -C.sub.10)aryl, (C.sub.3 -C.sub.6)cycloalkyl(C.sub.1 -C.sub.4)alkyl, or (C.sub.3 -C.sub.6)cycloatkyl; the bond represented by--is present or is absent; and the pharmaceutically acceptable salts thereof, and methods for using said compounds to stimulate receptors in the mammalian nervous systems.
REFERENCES:
J. D. Davies et al., "Excitatory Amino Acid Receptors and Synaptic Excitation in the Mammalian Central Nervous System", J. Physiol., 75, 641-654 (1979).
T. Honore et al., "The Binding of [.sup.3 H]AMPA, a Structural Analogue of Glutamic Acid, to Rat Brain Membranes", J. Neurochem., 38, 173 (1982).
R. L. Johnson et al., "Excitatory Amino Acid Neurotransmission", J. Med. Chem., 31, 2057 (1988).
E. D. London, "Specific Binding of [.sup.3 H]Kainic Acid to Receptor Sites in Rat Brain", Mol. Pharmacol., 15, 492 (1979).
D. J. Monaghan et al., "The Excitatory Amino Acid Receptors: Their Classes, Pharmacology, and Distinct Properties in the Function of The Central Nervous System", Annu. Rev. Pharmacol. Toxicol., 29, 365 (1989).
M. Recasens et al., "A New Quisqualate Receptor Subtype (sAA.sub.2) Responsible for the Glutamate-Induced Inositol Phosphate Formation in Rat Brain Synaptoneurosomes", Neurochem. Int., 13, 463 (1988).
M. B. Robinson et al., "Exposure of Hippocampal Slices to Quisqualate Sensitizes Synaptic Responses to Phosphonate-Containing Analogues of Glutamate", Brain Res., 381, 187 (1986).
M. B. Robinson et al., "Hydrolysis of the Brain Dipeptide N-Acetyl-L-aspartyl-L-glutamate", J. Biol. Chem., 262, 14498 (1987).
D. D. Schoepp et al., "Excitatory Amino Acid Agonist-Antagonist Interactions at 2-Amino-4-Phosphonobutyric Acid-Sensitive Quisqualate Receptors Coupled to Phosphoinositide Hydrolysis in Slices of Rat Hippocampus", J. Neurochem., 50, 1605 (1988).
M. K. Schulte et al., "Structure-function Relationships for Analogues of L-2-Amino-4-phosphonobutanoic Acid on the Quisqualic Acid-Sensitive AP4 Receptor of the Rat Hippocampus", Brain Res., 582, 291 (1992).
M. J. Sheardown et al., "A New and Specific Non-NMDA Receptor Antagonist, FG 9065, Blocks L-AP4-evoked Depolarization in Rat Cerebral Cortex", Eur. J. Pharmacol., 148, 471 (1988).
E. R. Whittemore, "Novel Recognition Site for L-Quisqualate Sensitizes Neurons to Depolarization by L-2-amino-4-phosphonobutanoate (L-AP4)", Brain Res., 485, 146-156 (1989).
E. R. Whittemore et al., "Pre-exposure to L-homocysteinesulfinic Acid Blocks Quisqualate-induced Sensitization to L-2-amino-4-phosphonobutanoic Acid", Eur. J. Pharmacol., 192, 435 (1991).
R. Zaczek et al., "Characteristics of Chloride-Dependent Incorporation of Glutamate into Brain Membranes Argue Against a Receptor Binding Site", Neuropharmacol. 26, 281 (1987).
R. J. Roon et al., "Synthesis of Quisqualic Acid Analogues as Possible Selective Ligands at Quisqualic Acid Receptors", Soc. Neuroscience Abstracts, 18, 649, Abstract No. 277.16 (1992).
N. Subasinghe et al., "Synthesis of Quisaqualic Acid Analogues as Possible Selective Ligands at Quisqualic Acid Receptors", 23rd National Medicinal Chemistry Symposium, Buffalo N.Y., Abstract No. 12 (1992).
N. Subasinghe et al., "Quisqualic Acid Analogues: Synthesis of beta-Heterocyclic 2-Aminopropanoic Acid Derivatives and Their Activity at a Novel Quisqualate-Sensitized Site", J. Med. Chem., 35, 4602-2607 (1992).
Johnson Rodney L.
Koerner James F.
Subasinghe Nalin L.
Regents of the University of Minnesota
Springer David B.
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