Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1997-07-25
2000-02-22
Seaman, D. Margaret
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
546239, A61K 3144, C07D21134
Patent
active
060280832
ABSTRACT:
The present invention is directed to esters of (+)-.alpha.-(2,3 Dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol, pharmaceutical formulations, methods of making and methods of using these esters. These compounds antagonize the effects of serotonin at the 5HT.sub.2A receptor and are useful in treating various conditions such as, for example, psychoses such as schizophrenia.
REFERENCES:
patent: 2833775 (1958-05-01), Sperber et al.
patent: 3058979 (1962-10-01), Ullyot et al.
patent: 3194733 (1965-07-01), Yale et al.
patent: 3394131 (1968-07-01), Yale et al.
patent: 3655676 (1972-04-01), Kaiser et al.
patent: 4569941 (1986-02-01), Suh et al.
patent: 4623728 (1986-11-01), Sarges
patent: 4632929 (1986-12-01), Suh et al.
patent: 4701461 (1987-10-01), Suh et al.
patent: 4762842 (1988-08-01), Cohen et al.
patent: 4783471 (1988-11-01), Carr
patent: 4804663 (1989-02-01), Kennis et al.
patent: 4810713 (1989-03-01), Yanni et al.
patent: 4877798 (1989-10-01), Sorensen
patent: 4895841 (1990-01-01), Sugimoto et al.
patent: 4908369 (1990-03-01), Schechter et al.
patent: 4912117 (1990-03-01), Carr
patent: 4921863 (1990-05-01), Sugimoto et al.
patent: 4950614 (1990-08-01), Yanni et al.
patent: 4950674 (1990-08-01), Yanni et al.
patent: 5021428 (1991-06-01), Carr
patent: 5064838 (1991-11-01), Carr et al.
patent: 5070087 (1991-12-01), Teng et al.
patent: 5100901 (1992-03-01), Sugimoto et al.
patent: 5106855 (1992-04-01), McLees et al.
patent: 5112978 (1992-05-01), Molinari
patent: 5116846 (1992-05-01), Cain et al.
patent: 5134149 (1992-07-01), Carr et al.
patent: 5158952 (1992-10-01), Janssen et al.
patent: 5169096 (1992-12-01), Carr et al.
patent: 5254556 (1993-10-01), Janssen et al.
patent: 5561144 (1996-10-01), Carr et al.
patent: 5618824 (1997-04-01), Schmidt et al.
patent: 5700812 (1997-12-01), Carr et al.
patent: 5700813 (1997-12-01), Carr et al.
patent: 5721247 (1998-02-01), Carr et al.
Tetrahedron: Asymmetry, vol. 4, No. 5 (pp. 943-946) (1993), King.
Tetrahedron: Asymmetry, vol. 1, No. 8 (pp. 535-536) (1990), Nieduzak.
Tetrahedron: Asymmetry, vol. 2, No. 2 (pp. 113-122) (1991), Nieduzak.
Nambu, Keiko et al., Biochemical Pharmacology, vol. 36, No. 10, pp. 1715-1722, 1987.
Dencker, Svan Jonas et al., Disease Management, CNS Drugs, 1996, Nov:6(5)367-381.
Remington's Pharmaceuticals Sciences, "Sustained-release drug delivery systems", pp. 1687-1688, 18th edition-1990.
Biopharmaceutics (1990), vol. 5, pp. 123-130, C.Hansch, et al., "Comprehensive Medicinal Chemistry." Pergamon Press, Oxford XP002105609.
Pharmazeutische Chemie (1982), pp. 14, 15 & 17, E. Schroeder et al. Georg Thieme Verlag, Stuttgart XP002105610.
Deconoate: International Clinical Psychopharmacology, No. 12 (pp. 255-261) (1997).
An electrophysiological investigation of the mechanism of action of the mechanism of action of the 5-ht2 antagonists ritanserin and mdl 28,133a on amphetamine induced slowing of a 1qO dopamine neurons, abstract of presentation at International Congress on Schizophrenic Research present in Tuscon Arizona on April 21-25, 1991, Sorensen.
Psychopharmacology (1989) 98:45-50: L. Ugedo wt al.
Drugs of the Future vol. 14, No. 5, 1989, pp. 489-490, Janssen.
Pharmacology and Toxicology Supplement 1, 1990, 5-7, E. Christensson et al.
Pharmacology and Toxicology Supplement 1, 1990, 12-17, B. Gustaffson et al.
Life Sciences, vol. 47, pp. 2401-2408, J. Frank Nash.
The Journal of Pharmacology and Experimental Therapeutics,vol. 253, No. 3, 1162-1170, Saller.
Journal of Neurochemistry, vol. 54, No. 3, 1990, 1062-1066, Nash et al.
The Journal of Pharmacology and Experimental Therapeutics, vol. 249, No. 3, 673-679, Goldstein et al.
Psychopharmacology (1989) vol. 99:S18-S27; H. Y. Meltzer.
The Journal of Pharmacology and Experimental Therapeutics, vol. 251:238-246, Meltzer et al.
4-Aroylpiperidines and Related Carbinols as Potent and Selective Inhibitors of Serotonin 5-HT2 Receptors with Antipsychotic Potential, Abstract of presentation at International Congress on Schizophrenic Research present in Tuscon Arizona on Apr. 21-25, 1991.
Carr Albert A.
Hijfte Luc Van
Kosley, Jr. Raymond W.
Hoechst Marion Roussel Inc.
Moon Carolyn D.
Seaman D. Margaret
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