Opioid compounds and methods for using same

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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A61K 31495, A61K 31445

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active

055524044

ABSTRACT:
Diarylmethyl piperazine compounds having utility as exogenous receptor combinant species for binding with receptors such as delta, mu, sigma, and/or kappa receptors are disclosed. Compounds of the invention may be employed as conjugates in agonist/antagonist pairs for transductional monitoring and assays of neurotransmitter function, and also variously exhibit therapeutic utility, including mediating analgesia, and possessing utility for the treatment of diarrhea, urinary incontinence, mental illness, drug and alcohol addiction/overdose, lung edema, depression, asthma, emphysema, cough, and apnea, respiratory depression, cognitive disorders, emesis and gastrointestinal disorders.

REFERENCES:
patent: 2630435 (1953-03-01), Baltzly et al.
patent: 4518711 (1985-05-01), Hruby et al.
patent: 4816586 (1989-03-01), Portoghese
Pakarinen, E. D., "Effects of Convulsant Agents on Learning and Memory in Squirrel Monkeys", Dissertation Abstracts International. 54(01B), 189 (Mar. 31, 1993--entered in the Louisiana State University online catalog).
Calderon, S. N., "Synthesis and Absolute Configuration of Optically Pure Enantiomers of (=)-BW373U86, A Nonpeptidic .delta.-Opioid Receptor Agonist", College on Problems of Drug Dependence, Inc., Fifty-fifth Annual Scientific Meeting. Toronto. Canada. Poster Presentation. (Jun. 12-17, 1993).
Selley, D. E., "BW373U86 A Non-peptide .delta. Opioid Agonist With Novel Receptor-G-Protein-Mediated Actions", Meeting of the International Narcotics Research Conference (INRC). Skoevde, Sweden, Abstract (Jul. 11-16, 1993).
Corner, S. D., "BW 373U86:Behavioral Pharmacology of a Putative Non-Peptide, Systemically-Active Delta Opiod Agonist", Disertation Abstracts International, 53(5B), 2578 (Jul. 1, 1992--entered in the University of Michigan online catalog).
Chang, K. -J., "Identification of a novel, potent and selective non-peptidic delta-selective agonist BW 373U86", Meeting of the International Narcotics Research Conference (INRC). Keystone, Colorado, Oral Presentation. (Jun. 23-27, 1992).
Comer, S. D., "BW 373U86: Delta-receptor-mediation of convulsions and refractoriness." Meeting of the International Narcotics Research Conference (INRC). Keystone, Colorado, Oral Presentation. (Jun. 23-27, 1992).
Dykstra, L., "Behavioral effects of a novel and selective opioid delta agonist in the monkey." Meeting of the International Narcotics Research Conference (INRC). Keystone. Colorado. Oral Presentation. (Jun. 23-27, 1992).
Porreca, F. "Multiple opioid delta receptors." Meeting of the International Narotics Research Conference (INRC). Keystone, Colorado. Oral Presentation. (Jun. 23-27).
Broadbent, J. et al., "Role of opioid receptor subtypes in the discriminative stimulus effects of cocaine." Meeting of the International Narcotics Research Conference (INRC), Keystone, Colorado. Abstract, (Jun. 23-27, 1992).
Dworkin, S. I. et al., "Effects of .delta.-opiate agonists and antagonists on cocaine and heroin self administration in rats." Meeting in the International Narcotics Research Conference (INRC). Keystone, Colorado, Abstract (Jun. 23-27, 1992).
Dykstra, L., et al. "Effects of a novel delta opioid agonist in squirrel monkeys responding under a schedule of shock tritration." Meeting of the International Narcotics Research Conference (INRC). Keystone, Colorado, Abstract (Jun. 23-27, 1992).
Lee, P. H. K., et al., "A non-peptide delta-opioid receptor agonist BW 373U86 suppresses naloxone-precipiated morphine abstience." Meeting of the International Narcotics Research Conference (INRC). Keystone, Colorado, Abstract (Jun. 23-27, 1992).
Porreca, F., et al., "Pharmacology of Multiple Opioid Delta Receptors", National Institute on Drug Abuse Research Monograph Series 132, Problems of Drug Dependence, 1992: Proceeding of the 54th Annual Scientific Meeting, 430-436 (1993).
Iwanoto, T. et a., "Calcium Antagonism by KB-2796, a New Diphenylpiperazine Analogue, in Dog Vascular Smooth Muscle", J. Pharm. Pharmacol., 43. 535-539 (1991).
Goenechea, V. S. et al., "Untersuchungen zur Biotransformation von Meclozin im menschlichen K oper", J. Clin. Chem. Clin. Biochem., 26. 105-115 (1988)--See Specification. p. 4, last paragraph and Chemical Abstracts 108: 215746g.
Iwamoto, T. et al., "Effects of KB-2796, a New Calcium Antagonist, and Other Diphenlpiperazines on [.sup.3 H]Nitrendipine Binding", Japan. J. Pharmacol., 48. 241-247 (1988).
Natsuka, K. et al., "Synthesis and Structure-Activity Relationships of 1-Substituted 4-(1,2-Diphenylethyl)piperazine Derivatives Having Narcotic Agonist and Antagonist Activity". J. Med. Chem., 30(10), 1779-1787 (1987).
Meuldermans, W. et al., "Plasma Levels, Biotransformation and Excretion of Oxatomide (R 35 443) in Rats, Dogs and Man", Xenobiotica. 14(6), 445-462 (1984).
Krishnamurthy, S., "A Highly Efficient and General N-Monomethylation of Functionalized Primary Amines Via Formylation--Borane: Methyl Sulfide Reduction". Tetrahedron Letters. 23(33), 3315-3318, (1982).
Lord. J. A. H. et al., "Endogenous Opioid Peptides: Multiple Agonists and Receptors", Nature. 267, 495-499 (1977).
Chang et al., "A Novel, Potent and Selective Nonpeptide Delta Opioid Receptor Agonist BW 373U86", J. Pharmacol. Exp. Ther., 267, 852-857 (1993).
Childers et al., "BW373U86: A Non-peptidic .delta.-Opioid Agonist With Novel Receptor-g Protein-mediated Actions in Rats Brain Membrane and Neuroblastoma Cells", Molec. Pharmacol., 44, 827-834 (1993).
Comer et al., "Convulsive Effects of Systemic Administration of the Delta Opioid Agonist BW373U86 in Mice", J. Pharmacol. Exp. Ther., 267, 888-895 (1993).
Comer et al., "Discriminative Stimulus Effects of BW373U86: A Non-peptide Ligand With Selectivity for Delta Opioid Receptors". J. Pharmacol. Exp. Ther., 267, 866-874 (1993).
Dykstra et al., "A Novel Delta Opioid Agonist, BW373U86, in Squirrel Monkeys Responding Under a Schedule of Shock Titration", J. Pharmacol. Exp. Ther., 267, 875-882 (1993).
Lee et al., "A Nonpeptidic Delta-opioid Receptor Agonist. BW373U86, Attenuates the Development and Expression of Morphine Abstinence Precipitated by Naloxone in Rat . . .". J. Pharmacol. Exp. Ther., 267, 883-887 (1993).
Negus et al., "Effects of Opioid Agonist Selective for Mu, Kappa and Delta Opioid Receptors on Schedule-controlled Responding in Rhesus Monkeys: Antagonism by Quadazocine", J. Pharmacol. Exp. Ther., 267, 896-903 (1993).
Wild et al., "Binding of 373U86, A Non-peptidic .delta.-Opioid Receptor Agonist is Not Regulated by Guanine Nucleotides and Sodium", Eur. J. Pharmacol.--Molec. Pharmacol., Section 246, 289-292 (1993).
Wild et al., "Antinociceptive Actions of BW373U86 in the Mouse", J. Pharmacol, Exp. Ther. 267, 858-865, 1993.
Xu et al., "Differential Binding of Opioid Peptides and Other Drugs to Two Subtypes of Opioid .delta..sub.ncx Binding Sites in Mouse Brian: Further Evidence of .delta. Receptor Heterogeneity", Peptides 14, 893-907 (1993).
"A General Route to 4-Substituted Imidazoles", J. Chem. Soc., Perkin Trans. I, 1989, pp. 1139-1145.
"The Synthesis of Secondary and Tertiary Amines by Borohydride Reduction", Department of Chemistry, Harvard University, Cambridge, Mass., Nov. 1963, pp. 3259-61.
"Diastereoselektive Synthese neuartiger Mannich-Basen.sup.1) mittels Titanderivaten.sup.2)", Helvetica Chimica Acta, vol. 67 (1984), pp. 1593-1597.
"Copper Salts Catalysis of N-Phenylation of Amines by Trivalent Organobismuth Compounds", Tetrahedron Letters, vol. 28, No. 8, pp. 887-890, 1987.
"Organic Chemistry of L-Tyrosine. 1. General Synthesis of Chiral Piperazines from Amino Acids", J. Org. Chem., 1985, 50, 4909-4913.
"Synthesis of Primary Amines via Alkylation of the Sodium Salt of Trifluoroacetamide: An Alternative to the Gabriel Synthesis", Communications, Department of Chemistry, University of Lancaster, Lancaster, Great Britain, pp. 941-944, 1985.
Review: "Iontophoretic Devices for Drug Delivery", Pharmaceutical Reserach, vol. 3, No. 6, 1986, pp. 318-326.

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