Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
2005-11-08
2005-11-08
Huang, Evelyn Mei (Department: 1625)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
C546S162000
Reexamination Certificate
active
06962930
ABSTRACT:
Compounds, composition and method for ameliorating alcohol or drug dependency withdrawal syndromes and withdrawal-induced brain damage are disclosed. In particular, a series of N-substituted-4-uredo-5,7-dihalo-2-carboxy quinoline compounds are disclosed having combined properties as antagonists of voltage-sensitive sodium channels (VSNaC) and as selective competitive antagonists at the strychnine-intensive glycine site of N-methyl-D-aspartate (NMDA) receptors. The disclosed compounds prevent or reduce the signs and symptoms of neurohyperexcitability and particularly the neurohyperexcitability associated with withdrawal syndrome manifested by patients upon withdrawal from chronic use of dependence inducing agents (e.g. ethanol, barbiturates, opiates etc.). The combined actions of the disclosed compound on VSNaC and NMDA receptors also impart properties to these compounds that are important in preventing and reducing excitotoxic neurodegeneration and reducing anxiety without the undesirable CNS depressant side-effects of agents hitherto employed for these purposes.
REFERENCES:
patent: 5026700 (1991-06-01), Harrison et al.
patent: 5135956 (1992-08-01), Borg et al.
patent: 5183807 (1993-02-01), della Valle et al.
patent: 5252584 (1993-10-01), Carling et al.
patent: 5270309 (1993-12-01), Leeson
patent: 5321012 (1994-06-01), Mayer et al.
patent: 5348962 (1994-09-01), Kulagowski et al.
patent: 5493027 (1996-02-01), Nichols et al.
patent: 5606063 (1997-02-01), Harrison et al.
patent: 5783700 (1998-07-01), Nichols
patent: 5914403 (1999-06-01), Nichols
Leeson et al. J. Med. Chem. 1994, 37(24):4053-4067.
Carling et al. J. Med. Chem. 1993, 36:3397-3408.
Ahern, K. von B., et al, “Enhancement of NMDA Toxicity and Calcium Responses by Chronic Exposure of Cultured Cortical Neurons to Ethanol,”Neuroscience Letters, 165, 211-214 (1994).
Brandao, F., et al., “Piracetam Impedes Hippocampal Neuronal Loss During Withdrawal After Chronic Alcohol Intake,”Alcohol, 12(3), 279-288 (1995).
Chandler, L., et al., “Chronic Ethanol Exposure Potentiates NMDA Excitotoxicity in Cerebral Cortical Neurons”,Journal of Neurochemistry, 60(4), 1578-1581 (1993).
Grant, K., et al., “Ethanol Withdrawal Seizures and the NMDA Receptor Complex,”European Journal of Pharmacology, 176, 289-296 (1990).
Hoffman, P., et al. “Glutamate Receptors in Alcohol Withdrawal-Induced Neurotoxicity”,Metabolic Brain Disease, (10),1, 73-79 (1995).
Iorio, K., et al., “Glutamate-Induced Neurotoxicity is Increased in Cerebellar Granule Cells Exposed Chronically to Ethanol”European Journal of Pharmacology-Environmental Toxicology and Pharmacology Section, 248, 209-212 (1993).
Iorio, K., et al., Chronic Exposure to Cerebellar Granule Cells to Ethanol Results in Increased N-Methyl-D-Aspartate Receptor Function,Molecular Pharmacology, 41, 1142-1148 (1992).
Khanna, J. M., et al., “Effect of NMDA Antagonists on Rapid and Chronic Tolerance to Ethanol: Importance of Intoxicated Practice,”Pharmacology Biochemistry and Behavior, 48(3), 755-763 (1994).
Lenzi M.D. G. L., et al., “Early Treatment of Stroke with Monosialoganglioside GM-1 Efficacy and Safety Results of the Early Stroke Trial”,Stroke, 25(8), 1552-1558 (1994).
Manev, H., et al., “Glutamate-Induced Neuronal Death in Primary Cultures of Cerebellar Granule Cells: Protection by Synthetic Derivatives of Endogenous Sphingolipids”,The Journal of Pharmacology and Experimental Therapeutics, 252(1), 419-427 (1990).
Manev, H., et al., “Abusive Stimulation of Excitatory Amino Acid Receptors: A Strategy to Limit Neurotoxicity” ,The FASEB Journal, 4, 2789-2797 (Jul., 1990).
Rabbani, M., et al., “Possible Involvement of NMDA Receptor-Mediated Transmission in Barbiturate Physical Dependence”,British Journal of Pharmacology, 111, 89-96, 1994).
Schneider, PhD, J., et al. “GM1 Ganglioside Treatment of Parkinson's Disease: An Open Pilot Study of Safety and Efficacy”,Neurology, 45, 1149-1154, (Jun., 1995).
Jaffee, J., “Drug Addiction and Drug Abuse”, Ch. 22 inGoodman and Gilman's The Pharmacological Basis of Therapeutics, (Gilman A.G., et al. eds.), 522-573, Pergamon Press, New York (8th Ed. 1990).
Rall, T., et al., “Hypnotics and sedatives: Ethanol,” Ch. 17 inGoodman and Gilman's The Pharmacological Basis of Therapeutics, (Goodman, A.G., et al., eds), 436-462, Pergamon Press, New York, (8th ed., 1990).
Ripley, T.L., et al., “Effects on Ethanol Withdrawal Hyperexcitability of Chronic Treatment with a Competitive N-Methyl-D-Aspartate Receptor Antagonist,”The Journal of Pharmacological and Experimental Therapeutics, 272(1), 112-118 (1995).
Szabó, G., et al. “The NMDA Receptor Antagonist Dizocilpine Differentially Affects Environment-Dependent and Environment-Independent Ethanol Tolerance,”Psychopharmacology, 113, 511-517 (1994).
Tabakoff, Boris., et al., “Biology of Tolerance and Dependence”,Medical and Social Aspects of Alcohol Abuse, (Tabakoff et al. eds.), 187-220, Plenum Press, New York, (1983).
Wallis, C., et al., “GM1 Ganglioside Reduces Ethanol Intoxication and the Development of Ethanol Dependence,”Alcohol, 12(6), 573-580, (1995).
Hoffman Paula L.
Snell Lawrence
Tabakoff Boris
Huang Evelyn Mei
Lohocla Research Corporation
Olson & Hierl Ltd.
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