Organic compounds -- part of the class 532-570 series – Organic compounds – Four or more ring nitrogens in the bicyclo ring system
Reexamination Certificate
2006-01-03
2006-01-03
McKenzie, Thomas C. (Department: 1624)
Organic compounds -- part of the class 532-570 series
Organic compounds
Four or more ring nitrogens in the bicyclo ring system
C544S359000, C544S363000, C544S368000, C544S392000
Reexamination Certificate
active
06982332
ABSTRACT:
Compounds exhibiting CNS activity in mammalian species, having the structurewherein A is an optionally heterocyclic 5 or 6 membered aromatic ring system;R2is an organyl group substituent or two R2together may form a fused ring system,o is an integer from 0 to 4, the upper limit of o bounded by the num er of available substitutent sites on said optionally heterocyclic 5 or 6 membered aromatic ring structure;n is an integer from 0 to 2;R1is an organyl group;p is 1 to 4;wherein one (CH2)ngroup may be replaced by O or S;or a pharmaceutically acceptable derivative thereof;The compounds exhibit activity in dopamine transporter systems, and in p rticular a high differential activity between the D3 and D2 receptors.
REFERENCES:
patent: 2794804 (1957-06-01), Kushner et al.
patent: 6087346 (2000-07-01), Glennon et al.
patent: 6380224 (2002-04-01), Dax et al.
patent: WO 02/098367 (2002-12-01), None
Levant, Beth, Pharmacological Reviews, vol. 49, Issue 3, 231-252, Sep. 1997.
Pinter MM, Rutgers AW, Hebenstreit E., J. Neural Transm. 2000; 107(11):1307-23, Medline abstract PMID: 11145006.
Canon, J.G., Lee, T., Goldman, H.D., Costall, B., Naylor, R.J., “Cerebral Dopmine Agonist Properties of Some 2-aminotetralin Derivatives after Peripheral and Intracerebral Administration,” J. Med. Chem., 20, 1111-1116, 1977.
McDermed, J., McKenzie, G., Phillips, A., “Synthesis and Pharmacology of Some 2-aminotetralins Dopamine Receptor Agonists,” J. Med. Chem. 18, 362-367, 1975.
Levesque, D., Diaz, J., Pilon, C., Martres, M.-P., Giros, B., Souil, E., Schott, D., Morgat, J.-L., Schwartz, J.-C., Sokoloff, P., “Identification, Characterization, and Localization of the Dopamine D3Receptor in Rat Brain Using 7-[3H]hydroxy-N,N-di-n-propyl-2-aminotetralin,” Proc. Natl. Acad. Sci, U.S.A., 89, 8155-8159, 1992.
Alexander van Vliet, L., Tepper, P.G., Dijkstra, D., Damsma, G., Wikstrom, H. Pugsly, T.A., Akunne, H.C., Heffner, T.G., Glase, S.A., Wise, L.D., “Affinity for Dopamine D2, D3and D4Receptors of 2-aminotetralins, Relevance of D2Agonist Binding for Determination of Receptor Subtype Selectivity,” J. Med. Chem. 39, 4233-4237, 1996.
John Murray, P., et al., “A Novel Series of Arylpiperazines with High Affinity and Selectivity for the Dopamine D3Receptor,” Bioorg. Med. Chem. Lett., 5, 219-222, 1995.
Teran, C., et al., “Phenylpiperazine Derivatives with Strong Affinity for 5HT1a, D2A and D3 Receptors,” Bioorg. Med. Chem. Lett., 8, 3567-3570, 1998.
* Boyfield, I., et al., “A Novel Series of 2-aminotetralins with High Affinity and Selectivity for the Dopamine D3Receptor,” Bioorg. Med. Chem. Lett., 7, 1995-1998, 1997.
Yuan, J., et al., “NGB 2904 and NGB 2849: Two Highly Selective Dopamine D3Receptor Antagonist,” Bioorg. Med. Chem. Lett., 8, 2715-2718, 1998.
Homan, E.J., et al., “2-aminotetralin-derived Substituted Benzamide with Mixed Dopamine D2, D3, and Serotonin 5-HT1A Receptor Binding Properties: A Novel Class of Potential Atypical Antipsychotic Agents,” Bioorg. Med. Chem.
Avenell, K.Y., et al., Heterocyclic Analogues of 2-aminotetralins with High Affinity and Selectivity for Dopamine D3Receptor, Bioorg. Med. Chem. Lett., 9, 2715-2720, 1999.
Pugsley, T.A., et al., Pharmacol. Exp. Ther., 275, 1355-1366, 1995.
*Pilon, C., et al., Eur. J. Pharmacol., 268: 129-139, 1994.
Millan, M.J., et al., J. Pharmacol. Exp. Ther., 286, 1341-1355, 1998.
Ravina, E., et al., J. Med. Chem., 43, 4678-4693, 2000.
*Watts, V.J., et al., Eur. J. Pharmacol., 239, 271-273, 1993.
*Dutta, A.K., et al., Bioorg. Med. Chem. Lett., 12:4:619-6, 2002.
Kula, N.S., et al., Cell. Mol., Neurobiol., 14, 185-191, 1994.
Brooks & Kushman P.C.
Wayne State University
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