Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1998-10-02
2000-08-22
Gerstl, Robert
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
5462691, C07D41304, A61K 31454
Patent
active
06107313&
ABSTRACT:
This invention provides a novel class of oxadiazolyl piperidines which exhibit a high binding affinity for dopamine ligands. The compounds of the invention display selectivity for the dopamine D.sub.4 receptor over the dopamine D.sub.2 receptor. Preferably, these compounds act as dopamine antagonists, which are useful in the treatment of psychotic disorders.
REFERENCES:
patent: 5262427 (1993-11-01), Nilson
patent: 5559128 (1996-09-01), Chakravarty et al.
patent: 5686463 (1997-11-01), Baker
patent: 5854261 (1998-12-01), Bosmans
Boyfield et al., "Design and Synthesis of 2-Naphthoate Esters as Selective Dopamine D.sub.4 Antagonist", J. Med. Chem. 39:1946-1948 (1996).
Kulagowski et al., "Dopamine D4 Receptor Antagonist", Current Phamaceutical Design, 3:355-366 (1997).
Lahti et al., "Dopamine D.sub.4 versus D.sub.2 receptor selectivity of dopamine receptor antagonist: possible therapeutic implications", European Journal of Pharmacology, 236:483-486 (1983).
Liegeois et al., "Dopamine D.sub.4 Receptors: A New Opportunity for Research on Schizophrenia", Current Medicianal Chemistry, 5:77-100 (1998).
Rowley et al., "4-Heterocyclylpiperidines as Selective High-Affinity Ligands at the Human Dopamine D4 Receptor", J. Med. Chem., 40:2374-2385 (1997).
Rowley et al., "5-(4-Chlorophenyl)-4-methyl-3-(1-(2-phenylethyl)piperidin-4-yl)isoxazole: A Potent, Selective Antagonist at Human Cloned Dopamine D4 Receptors", 39:1943-1945 (1996).
Seeman et al., "Atypical Neuroleptics Have Low Affinity for Dopamine D.sub.2 Receptors or Are Selective for D.sub.4 Receptors", Neuropsychopharm, 16:2, 93-100 (1997).
Shaikh et al., "Dopamine D.sub.4 Receptors, Potential Therapeutic Implications in the Treatment of Schizophrenia", CNS Drugs, 8:1-11 (1997).
Andersen, et al., "Oxadiazoles as Bioisosteric Transformations of Carboxylic Functionalities. II", J. Med. Chem., 31:417-425 (1996).
Gupta, et al., "Quantitative Structure-Activity Relationship Studies on Some Nonbenzodiazepine Series of Compounds Acting at the Benzodiazepine Receptor", Bioorganic & Medicinal Chemical Chemistry, 6:2213-2218 (1998).
Street, et al., Synthesis and Biological Activity of 1,2,4-Oxadiazole Derivatives: Highly Potent and Efficacious Agonists for Cortical Muscarinic Receptors, J. Med. Chem., 33:10, 2690-2697 (1990).
Lavrador Karine
Williams John
CombiChem, Inc.
Dow Karen B.
Gerstl Robert
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