Organic compounds -- part of the class 532-570 series – Organic compounds – Nitrogen attached directly or indirectly to the purine ring...
Reexamination Certificate
2007-10-02
2007-10-02
Bernhardt, Emily (Department: 1624)
Organic compounds -- part of the class 532-570 series
Organic compounds
Nitrogen attached directly or indirectly to the purine ring...
C514S253060
Reexamination Certificate
active
10835185
ABSTRACT:
Benzofuranyl- and benzothienyl-piperzinyl quinoline derivatives and compositions containing such compounds are disclosed. Methods of using benzofuranyl- and benzothienyl-piperzinyl quinoline derivatives and compositions containing such composition in the treatment and/or prevention of serotonin-related disorders, such as depression and anxiety, are also disclosed. In addition, processes for the preparation of benzofuranyl- and benzothienyl-piperzinyl quinoline derivatives are disclosed. Benzofuranyl- and benzothienyl-piperzinyl quinoline derivatives of Formula I are disclosed:
REFERENCES:
patent: 6313126 (2001-11-01), Mewshaw et al.
patent: 0 376 607 (1990-07-01), None
patent: 0 546 583 (1993-06-01), None
patent: 0 666 258 (1995-08-01), None
patent: 1 092 715 (2001-04-01), None
patent: WO99/51592 (1999-10-01), None
patent: WO99/55695 (1999-11-01), None
patent: WO99/67237 (1999-12-01), None
patent: WO 00/34263 (2000-06-01), None
patent: WO 00/40554 (2000-07-01), None
patent: WO 00/43382 (2000-07-01), None
patent: WO 01/14330 (2001-03-01), None
patent: WO 02/44170 (2002-06-01), None
Wolff, Manfred E. Burger's Medicinal Chemistry, 5thEd. Part 1, pp. 975-977 (1995).
Banker et al. “Modern Pharmaceutics”, 3rdEd. p. 596 (1996).
Arborelius, L. et al., “HT1Areceptor antagonists increase the activity of serotonergic cells in the dorsal raphe nucleus in rats treated acutely or chronically with citalopram,”Naunyn-Schmiedeberg's Arch. Pharmacol. 1995, 352: 157-165.
Invernizzi, R. et al., “Chronic treatment with citalopram facilitates the effect of a challenge dose on cortical serotonin output: role of presynaptic 5-HT1Areceptors,”Eur. J. Pharmacol. 1994, 260: 243-246.
Artigas, F. et al., “Acceleration of the effect of selected antidepressant drugs in major depression by 5-HT1Aantagonists,”Trends Neurosci. 1996, 19(9): 378-383.
Jean-Luc Malleron et al., “New Indole Derivatives as Potent and Selective Serotonin Uptake Inhibitors,”J. Med. Chem. 1993, 36: 1194-1202 [plus erratum: p. 2242].
Wustrow et al., “3-[[(4-Aryl-1-piperazinyl)alkyl]cyclohexyl]-1H-indoles as Dopamine D2 Partial Agonists and Autoreceptor Agonists,”J. Med. Chem. 1997, 40: 250-259.
Perez, V., et al., “Randomised double-blind, placebo-controlled trial of pindolol in combination with fluoxetine antidepressant treatment,”The Lancet, 1997, 349: 1594-1597.
Feiger, A., “A Double-Blind Comparison of Gepirone Extended Release, Imipramine, and Placebo in the Treatment of Outpatient Major Depression,”Psychopharmacol. Bull., 1996, 32(4): 659-665.
Wilcox, C. et al., “A Double-Blind Trial of Low- and High-Dose Ranges of Gepirone-ER Compared With Placebo in the Treatment of Depressed Outpatients,”Psychopharmacol. Bull., 1996, 32(3): 335-342.
Grof, P. et al., “An open study of oral flesinoxan, a 5-HT1Areceptor agonist, in treatment-resistant depression,”International Clinical Psychopharmacology, 1993, 8: 167-172.
Dimitriou, E. et al., “Buspirone Augmentation of Antidepressant Therapy,”J. Clinical Psychopharmacol., 1998, 18(6): 465-469.
Krogsgaard-Larsen, et al., (ed.), Design and Application of Prodrugs, Textbook of Drug Design and Development, Chapter 5, 113-191 (1991).
Bundgaard, H. et al., “Prodrugs as a means to improve the delivery of peptide drugs,”Advanced Drug Delivery Reviews, Elsevier Science Publishers, 8:1-38 (1992).
Bundgaard, J. et al., “Glycolamide Esters as Biolabile Prodrugs of Carboxylic Acid Agents: Synthesis, Stability, Bioconversion, and Physicochemical Properties,”Journal of Pharmaceutical Sciences, 77(4):285-298 (Apr. 1988).
Cheetham, S. C. et al., “[3H]Paroxetine Binding in Rat Frontal Cortex Strongly Correlates With [3H]5-HT Uptake: Effect of Administration of Various Antidepressant Treatments,”Neuropharmacol., 1993, 32: 737-743.
Cheng, Y-C. et al., “Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction,”Biochem. Pharmacol., 1973, 22: 3099-3108.
Hall, M. D. et al. “[3H]8-Hydroxy-2-(Di-n-Propylamino)Tetralin Binding to Pre- and Postsynaptic 5-Hydroxytryptamine Sites in Various Regions of the Rat Brain,”J. Neurochem., 1985, 44(6): 1685-1696.
Lazareno, S. and Birdsall, N.J.M., “Pharmacological characterization of acetylcholine-stimulated [35S]-GTPγS binding mediated by human muscarinic m1-m4 receptors: antagonist studies,”Br. J. Pharmacol., 1993, 109:1120-1127.
Burkamp, F. et al., “Preparation of 3-Aminoalkylbenzo[b]thiophenes,”Journal of Heterocyclic Chemistry, Nov.-Dec. 2002, 39(6): 1177-1187.
Orús, L. et al., “Synthesis and Molecular Modeling of New 1-Aryl-3-[4-arylpiperazin-1-yl]-1-propane Derivatives with High Affinity at the Serotonin Transporter and at 5-HT1AReceptors,”J Med Chem, 2002, 45(19): 4128-4139.
Asselin Magda
Dos Santos Osvaldo
Evrard Deborah A.
Grosu George Theodore
Meagher Kristin
Bernhardt Emily
Woodcock & Washburn LLP
Wyeth
LandOfFree
Benzofuranyl-and benzothienyl-piperazinyl quinolines and... does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Benzofuranyl-and benzothienyl-piperazinyl quinolines and..., we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Benzofuranyl-and benzothienyl-piperazinyl quinolines and... will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-3903215