Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1994-07-11
1996-09-24
Davis, Zinna Northington
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
5142352, 514253, 546155, 544128, 544363, C07D21548, A61K 3147
Patent
active
055591256
ABSTRACT:
A class of 4-hydroxy-2-(1H)-quinolone derivatives, substituted at the 3-position by an optionally substituted aryl substituent, are selective non-competitive antagonists of NMDA receptors and/or are antagonists of AMPA receptors, and are therefore of utility in the treatment of conditions, such as neurodegenerative disorders, convulsions or schizophrenia, which require the administration of an NMDA and/or AMPA receptor antagonist.
REFERENCES:
patent: 5348962 (1994-09-01), Kulagowski et al.
Dickenson and Aydar, "Antagonism at the glycine site on the NMDA receptor reduces spinal nociception in the rat", Neuroscience Letters, 121, 263-266 (1991).
Murray et al., "Neurokinin and NMDA antagonists (but not a kainic acid antagonist) are antinociceptive in the mouse formalin model", Pain, 44, 179-185 (1991).
Woolf and Thompson, "The induction and maintenance of central sensitization is dependent on N-methyl-D-aspartic acid receptor activation; implications for the treatment of post-injury pain hypersensitivity states", Pain, 44, 293-299 (1991).
Trullas and Skolnick, "Functional antagonists at the NMDA receptor complex exhibit antidepressant actions", European Journal of Pharmacology, 185, 1-10 (1990).
Kehne, et al., "NMDA receptor complex antagonists have potential anxiolytic effects as measured with separation-induced ultrasonic vocalizations", European Journal of Pharmacology, 193, 283-292 (1990).
Werling, et al., "Regulation of [3H] Dopamine Release from Guinea Pig Striatum by NMDA Receptor/Channel Activators and Inhibitors1", The Journal of Pharmacology and Experimental Therapeutics, 255, 1, 40-45 (1990).
Graham, et al., "Atypical Endogenous Opioid Systems in Mice in Relation to an Auto-Addiction Opioid Model of Anorexia Nervosa", Life Sciences, 47, 16, 1427-1435 (1990).
Turski, et al., "Protection of substantia nigra from MPP+ neurotoxicity by N-methyl-D-aspartate antagonists", Nature, 349, 414-418 (1991).
Lauritzen, et al., "XV-4. The Neuroprotective Effect on the NMDA Antagonist MK801 and Non-NMDA Antagonist NBQX is not Explained by an Effect on Anoxic Depolarization, and only MK801 Inhibits Spreading Depression", Journal of Cerebral Blood Flow and Metabolism, II, 2, Abstract S222 (1991).
Bagetta, et al., "Prevention by the NMDA receptor antagonist, MK801 of neuronal loss produced by tetanus toxin in the rat hippocampus", British Journal Pharmacology, 101, 776-780 (1990).
Lipton, et al., "AIDS Virus Coat Protein Sensitizes Neurons to NMDA Receptor-Mediated Toxicity", Society for Neuroscience Abstracts, 16, 1, 128.11 (1990).
van den Pol, et al., "Glutamate, the Dominant Excitatory Transmitter in Neuroendocrine Regulation", Science, 250, 1276-1278 (1990).
Urbanski, "A Role for N-Methyl-D-Aspartate Receptors in the Control of Seasonal Breeding", Endocrinology, 127, 5, 2223-2228 (1990).
Christie, et al., "An Excitant Amino Acid Projection from the Medial Prefrontal Cortex to the Anterior Part of Nucleus Accumbens in the Rat", Journal of Neurochemistry, 45, 2, 477-482 (1985).
Rudolph, et al., "L-Glutamic Acid, A Neuromodulator of Dopaminergic Transmission in the Rat Corpus Striatum", Neurochemistry International, 5, 479-486 (1983).
Arnt, "Hyperactivity Following Injection of a Glutamate Agonist and 6,7-ADTN into Rat Nucleus Accumbens and its Inhibition by THIP", Life Sciences, 28, 14, 1597-1603 (1981).
Yamaguchi, et al., "The Synthesis of Benzofuroquinolines, III. Two Dihydroxybenzofuroquinolinones", Journal of Heterocycl. Chemistry, 21, 737-739 (1984).
Nishimura, et al., "Synthesis of 4-Hydroxy-2(1H)-quinolone Derivatives", Yakugaku Zasshi, 90, 818-828 (1970) (English Translation).
Stadlbauer and Kappe, "Oxidative Hydroxylation of Heterocyclic B-Dicarbonyl Compounds", Monatshefte fur Chemie, 116, 1005-1015 (1985) (English Translation).
Kappe, et al., "Syntheses of Heterocycles, 131st Report: On the Reactions of Some Mesoxalyl Heterocycles and their Animals", Monatshefte fur Chemie, 100, 951-959 (1969) (English Translation).
Sterk and Ziegler, "Infrared Spectroscopic Studies of 4-hydroxycarbostyril and its Derivatives", Monatshefte fur Chemie, 98, 100-104 (1967) (English Translation).
Kawase, et al., "The Synthesis of Benzofuroquinolines. II. Two Benzofuroquinolinones and Some Benzofuroquinoline Derivatives", Bulletin Chemical Society. Japan, 53, 1057-1060 (1980).
Yamaguchi, et al., "The Synthesis of Benzofuroquinolines. IV. Some Halobenzofuro[2,3-b]-and [3,2-c]quinoline Derivatives", J. Heterocyclic Chemistry, 26, 281-284 (1989).
Walser, et al., "Nucleophilic Displacement of Aromatic Fluorine, Part III (1), Indoloquinolines and Benzofuranoquinolines", J. Heterocyclic Chemistry, 12, 351-358 (1975).
Kappe, et al., "Synthesis of Benzo-halogenated 4-Hydroxy-2((1H) quinolones", J. Heterocyclic Chemistry, 25, 857-862 (1988).
Stadlbauer and Kappe, "Syntheses of 3-Hydroxy-tetrahydroquinoline-2,4-diones)", Z. Naturforsch. 37b, 1196-1200 (1982) (English Translation).
Diesbach, et al., "128. On Some Derivatives of the Phenyl-hydroxy-quinolines", Helvetica Chimica Acta., 34, 1050-1060 (1951) (English Translation).
Grimwood, et al., "204P Modulation by Polyamines of [3H]L-689,560 Binding to the Glycine Site on the N-Methyl-D-Aspartate Receptor from Rat Cortex/Hippocampus Membranes", British Journal of Pharmacology Proceedings Supplement, 107, 204P (1992).
Wong, et al., "The anticonvulsant MK-801 is a potent N-methyl-D-aspartate antagonist", Proc Natl. Acad. Sci. U.S.A., 83, 7104-7108 (1986).
Kulagowski Janusz J.
Leeson Paul D.
Mawer Ian M.
Rowley Michael
Davis Zinna Northington
Merck Sharp & Dohme Limited
North Robert J.
Winokur Melvin
LandOfFree
Hydroxyquinolone derivatives does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Hydroxyquinolone derivatives, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Hydroxyquinolone derivatives will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-1928635