5-hydroxytryptamine subtype 6 receptor modulators: a patent survey

Bibliography

• Kenakin T. Efficacy as a vector: the relative prevalence and paucity of inverse agonism. Mol Pharmacol 2004;65(1):2-11
   Google Scholar
• Dixon RA, Kobilka BK, Strader DJ, Cloning of the gene and cDNA for mammalian beta-adrenergic receptor and homology with rhodopsin. Nature 1986;321(6065):75-9
   Google Scholar
• Nathans J, Hogness DS. Isolation, sequence analysis, and intron-exon arrangement of the gene encoding bovine rhodopsin. Cell 1983;34(3):807-14
   Google Scholar
• Murray R, Keenan AK. The beta-adrenoceptor is precoupled to Gs in chicken erythrocyte membranes. Cell Signal 1989;1(2):173-9
   Google Scholar
• Freissmuth M, Selzer E, Marullo S, Expression of two human beta-adrenergic receptors in Escherichia coli: functional interaction with two forms of the stimulatory G protein. Proc Natl Acad Sci USA 1991;88(19):8548-52
   Google Scholar
• Adie EJ, Milligan G. Regulation of basal adenylate cyclase activity in neuroblastoma x glioma hybrid, NG108-15, cells transfected to express the human beta 2 adrenoceptor: evidence for empty receptor stimulation of the adenylate cyclase cascade. Biochem J 1994;303(Pt3):803-8
   Google Scholar
• Chidiac P, Hebert TE, Valiquette M, Inverse agonist activity of beta-adrenergic antagonists. Mol Pharmacol 1994;45(3):490-9
   Google Scholar
• Gotze K, Jakobs KH. Unoccupied beta-adrenoceptor-induced adenylyl cyclase stimulation in turkey erythrocyte membranes. Eur J Pharmacol 1994;268(2):151-8
   Google Scholar
• Costa T, Herz A. Antagonists with negative intrinsic activity at delta opioid receptors coupled to GTP-binding proteins. Proc Natl Acad Sci USA 1989;86(19):7321-5
   Google Scholar
• Westphal RS, Sanders-Bush E. Reciprocal binding properties of 5-hydroxytryptamine type 2C receptor agonists and inverse agonists. Mol Pharmacol 1994;46(5):937-42
   Google Scholar
• Leeb-Lundberg LM, Mathis SA, Herzig MC. Antagonists of bradykinin that stabilize a G-protein-uncoupled state of the B2 receptor act as inverse agonists in rat myometrial cells. J Biol Chem 1994;269(42):25970-3
   Google Scholar
• Ren Q, Kurose H, Lefkowitz RJ, Cotecchia S. Constitutively active mutants of the alpha 2-adrenergic receptor. J Biol Chem 1993;268(22):16483-7
   Google Scholar
• Hamm HE. The many faces of G protein signaling. J Biol Chem 1998;273(2):669-72
   Google Scholar
• Strader CD, Fong TM, Tota MR, Structure and function of G protein-coupled receptors. Annu Rev Biochem 1994;63:101-32
   PubMed Web of Science ®Google Scholar
• Ji TH, Grossmann M, Ji I. G protein-coupled receptors. I. Diversity of receptor-ligand interactions. J Biol Chem 1998;273(28):17299-302
   Google Scholar
• Bockaert J, Pin JP. Molecular tinkering of G protein-coupled receptors: an evolutionary success. EMBO J 1999;18(7):1723-9
   PubMed Web of Science ®Google Scholar
• Gether U. Uncovering molecular mechanisms involved in activation of G protein-coupled receptors. Endocr Rev 2000;21(1):90-113
   Google Scholar
• Drews J. Drug discovery: a historical perspective. Science 2000;287(5460):1960-4
   PubMed Web of Science ®Google Scholar
• Howard AD, McAllister G, Feighner SD, Orphan G-protein-coupled receptors and natural ligand discovery. Trends Pharmacol Sci 2001;22(3):132-40
   Google Scholar
• Barnes NM, Sharp T. A review of central 5-HT receptors and their function. Neuropharmacology 1999;38(8):1083-152
   Google Scholar
• Filip M, Frankowska M, Zaniewska M, The serotonergic system and its role in cocaine addiction. Pharmacol Rep 2005;57(6):685-700
   Google Scholar
• Hoyer D, Hannon JP, Martin GR. Molecular, pharmacological and functional diversity of 5-HT receptors. Pharmacol Biochem Behav 2002;71(4):533-54
   PubMed Web of Science ®Google Scholar
• Filip M, Bader M. Overview on 5-HT receptors and their role in physiology and pathology of the central nervous system. Pharmacol Rep 2009;61(5):761-77
   Google Scholar
• Johnson CN, Ahmed M, Miller ND. 5-HT6 receptor antagonists: prospects for the treatment of cognitive disorders including dementia. Curr Opin Drug Discov Devel 2008;11(5):642-54
   Google Scholar
• Kohen R, Fashingbauer LA, Heidmann DE, Cloning of the mouse 5-HT6 serotonin receptor and mutagenesis studies of the third cytoplasmic loop. Brain Res Mol Brain Res 2001;90(2):110-7
   Google Scholar
• Teitler M, Herrick-Davis K, Purohit A. Constitutive activity of G-protein coupled receptors: emphasis on serotonin receptors. Curr Top Med Chem 2002;2(6):529-38
   Google Scholar
• Reavill C, Rogers DC. The therapeutic potential of 5-HT6 receptor antagonists. Curr Opin Investig Drugs 2001;2(1):104-9
   Google Scholar
• Hoyer D, Martin GR. Classification and nomenclature of 5-HT receptors: a comment on current issues. Behav Brain Res 1996;73(1-2):263-8
   Google Scholar
• Woolley ML, Marsden CA, Fone KC. 5-HT6 receptors. Curr Drug Targets CNS Neurol Disord 2004;3(1):59-79
   Google Scholar
• Hannon J, Hoyer D. Molecular biology of 5-HT receptors. Behav Brain Res 2008;195(1):198-213
   Google Scholar
• Kennett GA. Serotonin receptors and their function. Smith-Kline Beecham Pharmaceuticals, Published by Tocris Cooksen, Inc.; 1997
   Google Scholar
• Fink KB, Göthert M. 5-HT receptor regulation of neurotransmitter release. Pharmacol Rev 2007;59(4):360-417
   Google Scholar
• Ruat M, Traiffort E, Arrang JM, A novel rat serotonin (5-HT6) receptor: molecular cloning, localization and stimulation of cAMP accumulation. Biochem Biophys Res Commun 1993;193(1):268-76
   Google Scholar
• Kohen R, Metcalf MA, Khan N, Cloning, characterization, and chromosomal localization of a human 5-HT6 serotonin receptor. J Neurochem 1996;66(1):47-56
   Google Scholar
• Monsma FJ Jr, Shen Y, Ward RP, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol Pharmacol 1993;43(3):320-7
   Google Scholar
• Ward RP, Hamblin MW, Lachowicz JE, Localization of serotonin subtype 6 receptor messenger RNA in the rat brain by in situ hybridization histochemistry. Neuroscience 1995;64(4):1105-11
   Google Scholar
• Fone KC, Topham IA. Alteration in 5-hydroxytryptamine agonist-induced behaviour following a corticosterone implant in adult rats. Pharmacol Biochem Behav 2002;71(4):815-23
   Google Scholar
• Roberts JC, Reavill C, East SZ, The distribution of 5-HT6 receptors in rat brain: an autoradiographic binding study using the radiolabelled 5-HT6 receptor antagonist [(125)I]SB-258585. Brain Res 2002;934(1):49-57
   Google Scholar
• Gerard C, Martres MP, Lefèvre K, Immuno-localization of serotonin 5-HT6 receptor-like material in the rat central nervous system. Brain Res 1997;746(1-2):207-19
   Google Scholar
• Hirst WD, Abrahamsen B, Blaney FE, Differences in the central nervous system distribution and pharmacology of the mouse 5-hydroxytryptamine-6 receptor compared with rat and human receptors investigated by radioligand binding, site-directed mutagenesis, and molecular modeling. Mol Pharmacol 2003;64(6):1295-308
   Google Scholar
• Setola V, Roth BL. Why mice are neither miniature humans nor small rats: a cautionary tale involving 5-hydroxytryptamine-6 serotonin receptor species variants. Mol Pharmacol 2003;64(6):1277-8
   Google Scholar
• Saudou F, Hen R. 5-Hydroxytryptamine receptor subtypes in vertebrates and invertebrates. Neurochem Int 1994;25(6):503-32
   Google Scholar
• Hamon M, Doucet E, Lefèvre K, Antibodies and antisense oligonucleotide for probing the distribution and putative functions of central 5-HT6 receptors. Neuropsychopharmacology 1999;21(2 Suppl):68S-76S
   Google Scholar
• East SZ, Burnet PW, Leslie RA, 5-HT6 receptor binding sites in schizophrenia and following antipsychotic drug administration: autoradiographic studies with [125I]SB-258585. Synapse 2002;45(3):191-9
   Google Scholar
• Marcos B, Gil-Bea FJ, Hirst WD, Lack of localization of 5-HT6 receptors on cholinergic neurons: implication of multiple neurotransmitter systems in 5-HT6 receptor-mediated acetylcholine release. Eur J Neurosci 2006;24(5):1299-306
   Google Scholar
• Jorgensen HS. Studies on the neuroendocrine role of serotonin. Dan Med Bull 2007;54(4):266-88
   Google Scholar
• Branchek TA, Blackburn TP. 5-HT6 receptors as emerging targets for drug discovery. Annu Rev Pharmacol Toxicol 2000;40:319-34
   PubMed Web of Science ®Google Scholar
• Slassi A. Recent advances in 5-HT1B/1D receptor antagonists and agonists and their potential therapeutic applications. Curr Top Med Chem 2002;2(6):559-74
   Google Scholar
• Unsworth CD, Molinoff PB. Characterization of a 5-hydroxytryptamine receptor in mouse neuroblastoma N18TG2 cells. J Pharmacol Exp Ther 1994;269(1):246-55
   Google Scholar
• Holenz J, Merce R, Diaz JL, Medicinal chemistry driven approaches toward novel and selective serotonin 5-HT6 receptor ligands. J Med Chem 2005;48(6):1781-95
   Google Scholar
• Trani G, Baddeley SM, Briggs MA, Tricyclic azepine derivatives as selective brain penetrant 5-HT6 receptor antagonists. Bioorg Med Chem Lett 2008;18(20):5698-700
   Google Scholar
• Heal DJ, Smith SL, Fisas A, Selective 5-HT6 receptor ligands: progress in the development of a novel pharmacological approach to the treatment of obesity and related metabolic disorders. Pharmacol Ther 2008;117(2):207-31
   Google Scholar
• Meltzer HY. An overview of the mechanism of action of clozapine. J Clin Psychiatry 1994;55(Suppl B):47-52
   Google Scholar
• Mitchell ES, Neumaier JF. 5-HT6 receptors: a novel target for cognitive enhancement. Pharmacol Ther 2005;108(3):320-33
   Google Scholar
• King MV, Marsden CA, Fone KC. A role for the 5-HT1A, 5-HT4 and 5-HT6 receptors in learning and memory. Trends Pharmacol Sci 2008;29(9):482-92
   PubMed Web of Science ®Google Scholar
• Geldenhuys WJ, Van der Schyf CJ. The serotonin 5-HT6 receptor: a viable drug target for treating cognitive deficits in Alzheimer's disease. Expert Rev Neurother 2009;9(7):1073-85
   Google Scholar
• Messina D, Annesi G, Serra P, Association of the 5-HT6 receptor gene polymorphism C267T with Parkinson's disease. Neurology 2002;58(5):828-9
   Google Scholar
• Wu J, Li Q, Bezprozvanny I. Evaluation of Dimebon in cellular model of Huntington's disease. Mol Neurodegener 2008;3:15
   PubMedGoogle Scholar
• Schaffhauser H, Mathiasen JR, Dicamillo A, Dimebolin is a 5-HT6 antagonist with acute cognition enhancing activities. Biochem Pharmacol 2009;78(8):1035-42
   Google Scholar
• Memory Pharmaceuticals Corp. Acyclic compounds having 5-HT6 receptor affinity. WO011546; 2010
   Google Scholar
• Memory Pharmaceuticals Corp. Pyrrolo-pyridine-3-yl-piperazine derivatives having 5-HT6 receptor affinity. WO008832; 2010
   Google Scholar
• Memory Pharmaceuticals Corp. Pyrrolidine-substituted azaindole compounds having 5-HT6 receptor affinity. WO002802; 2010
   Google Scholar
• Arena Pharmaceuticals, Inc. 5-HT6 receptor and modulators thereof for the treatment of insulin-related disorders. WO011305; 2010
   Google Scholar
• Janssen Pharmaceutical NV. Substituted 6-(1-piperazinyl)-pyridazines as 5-HT6 receptor antagonists. WO000456; 2010
   Google Scholar
• Geldenhuys WJ, Van der Schyf CJ. Serotonin 5-HT6 receptor antagonists for the treatment of Alzheimer's disease. Curr Top Med Chem 2008;8(12):1035-48
   Google Scholar
• Upton N, Chuang TT, Hunter AJ, Virley DJ. 5-HT6 receptor antagonists as novel cognitive enhancing agents for Alzheimer's disease. Neurotherapeutics 2008;5(3):458-69
   Google Scholar
• Sleight AJ, Boess FG, Bos M, Bourson A. The putative 5-HT6 receptor: localization and function. Ann NY Acad Sci 1998;861:91-6
   PubMed Web of Science ®Google Scholar
• Holenz J, Pauwels PJ, Diaz JL, Medicinal chemistry strategies to 5-HT6 receptor ligands as potential cognitive enhancers and antiobesity agents. Drug Discov Today 2006;11(7-8):283-99
   Google Scholar
• Vinogradova EV, Danusevich IK, Kost AN, Shadurskii KS. Antihistaminic activity of carboline derivates. Zdravookhr Beloruss 1963;85:38-41
   Google Scholar
• Shadurskiy KS, Danusevich IK, Vinogradova EV, Kost AN. Antihistaminic agent “Dimebon”. SU833156; 1963
   Google Scholar
• Zefirov NS, Afanas'ev AZ, Afanas'eva SV, US7071206; 2006
   Google Scholar
• Doody RS, Gavrilova SI, Sano M, Effect of dimebon on cognition, activities of daily living, behaviour, and global function in patients with mild-to-moderate Alzheimer's disease: a randomised, double-blind, placebo-controlled study. Lancet 2008;372(9634):207-15
   PubMed Web of Science ®Google Scholar
• Zefirov NS, Afanas'ev AZ, Afanas'eva SV, Agent for treating neurodegenerative disorders. Chem Abstr 1998;126:338861. WO9715225; 1997
   Google Scholar
• Galenko-Yaroshevskii PA, Cherednik IL, Bartashevich VV, Comparative characteristics of antiarrhythmic activity of phencarol and dimebone in neurogenic ventricular fibrillation. Bull Exp Biol Med 1997;124:691
   Google Scholar
• Hung D. Methods and compositions for treating amyotrophic lateral sclerosis (ALS). Chem Abstr 2008;148:394417. WO036410; 2008
   Google Scholar
• Bachurin S, Bukatina T, Lermontova N, Antihistamine agent dimebon as novel neuroprotector and cognition enhancer. Ann NY Acad Sci 2001;939:425
   PubMed Web of Science ®Google Scholar
• Pfizer and medivation announce. Results from two phase 3 studies in Dimebon (Latrepirdine) Alzheimer's Disease. Available from: http://investors.medivation.com/releasedetail.cfm?ReleaseID=448818
   Google Scholar
• Kieburtz K, McDermott MP, Voss TS, A randomized, placebo-controlled trial of latrepirdine in Huntington disease. Arch Neurol 2010;67(2):154-60
   Google Scholar
• Matveeva IA. About Dimebon action towards histamine receptors. Farmakol toksikol 1983;46:27
   Google Scholar
• Lermontova NN, Redkozubov AE, Shevtsova EF, Dimebon and tacrine inhibit neurotoxic action of beta-amyloid in culture and block L-type Ca2+ channels. Bull Exp Biol Med 2001;132(5):1079-83
   Google Scholar
• Grigorev VV, Dranyi OA, Bachurin SO. Comparative study of action mechanisms of dimebon and memantine on AMPA- and NMDA-subtypes glutamate receptors in rat cerebral neurons. Bull Exp Biol Med 2003;136(5):474-7
   Google Scholar
• Lermontova NN, Lukoyanov NV, Serkova TP, Dimebon improves learning in animals with experimental Alzheimer's disease. Bull Exp Biol Med 2000;129(6):544-6
   Google Scholar
• Bachurin SO, Shevtsova EP, Kireeva EG, Mitochondria as a target for neurotoxins and neuroprotective agents. Ann NY Acad Sci 2003;993:334-44
   PubMed Web of Science ®Google Scholar
• Hung D. Dimebon. 11th Int Conf Alzheimer's Dis Relat Disord (ICAD) [abstract S4-04-05]. 26 – 31 July 2008, Chicago.
   Google Scholar
• Tkachenko SE, Ivachtchenko AV, Khvat A, 1st International Conference on Drug Design and Discovery [abstract IL 187]. 2 – 6 February 2008, Dubai
   Google Scholar
• Roth BL, Sheffler DJ, Kroeze WK. Magic shotguns versus magic bullets: selectively non-selective drugs for mood disorders and schizophrenia. Nat Rev Drug Discov 2004;3(4):353-9
   PubMed Web of Science ®Google Scholar
• Cole DC, Stock JR, Lennox WJ, Discovery of N1-(6-chloroimidazo[2,1-b][1,3]thiazole-5-sulfonyl)tryptamine as a potent, selective, and orally active 5-HT6 receptor agonist. J Med Chem 2007;50(23):5535-8
   Google Scholar
• Ivachtchenko AV, Mitkin OD, Tkachenko SE, 8-Sulfonyl-substituted tetrahydro-1H-pyrido[4,3-b]indoles as 5-HT6 receptor antagonists. Eur J Med Chem 2010;45(2):782-9
   Google Scholar
• Okun I, Tkachenko ES, Khvat A, From Anti-allergic to Anti-Alzheimer's: molecular pharmacology of Dimebon. Curr Alzheimer Res 2010;7(2):97-112
   Google Scholar
• Ivachtchenko AV, Frolov EB, Mitkin OD, Synthesis and biological evaluation of novel gamma-carboline analogues of Dimebon as potent 5-HT6 receptor antagonists. Bioorg Med Chem Lett 2009;19(12):3183-7
   Google Scholar
• Dupuis DS, Mannoury la Cour C, Chaput C, Actions of novel agonists, antagonists and antipsychotic agents at recombinant rat 5-HT6 receptors: a comparative study of coupling to G alpha s. Eur J Pharmacol 2008;588(2-3):170-7
   Google Scholar
• Esteve. Substituted indole compounds and their use as 5-HT6 receptor modulators. WO024535; 2006
   Google Scholar
• Esteve. Substituted indazolyl sulfonamide and 2,3-dihydro-indolyl sulfonamide compounds, their preparation and use in medicaments. WO069809; 2006
   Google Scholar
• Suven Life Science. Thioether derivatives as functional 5-HT6 ligands. WO020653; 2007
   Google Scholar
• Suven Life Science. Orally administered small peptides synergize statin activity. WO020652; 2006
   Google Scholar
• Wyeth. Use of a 5-HT6 agonist for the treatment and prevention of neurodegenerative disorders. WO065710; 2006
   Google Scholar
• GlaxoSmithKline. Novel compounds. WO038006; 2006
   Google Scholar
• AstraZeneca. Chroman derivatives and their use as 5-HT6 receptor ligands. WO066746; 2006
   Google Scholar
• Hoffmann-LaRoche. Tetralin and indane derivatives and uses thereof as 5-HT6 antagonists. WO066748; 2006
   Google Scholar
• Hoffmann-LaRoche. Tetralin and indane derivatives and uses thereof. WO066790; 2006
   Google Scholar
• Biovitrum. Benzofuranyl derivatives as 5-HT6-receptor inhibitors. WO134150; 2006
   Google Scholar
• Wyeth. Substituted-3-sulfonylindazole derivatives as 5-hydroxytryptamine-6 ligands. US037802; 2007
   Google Scholar
• Wyeth. Process for the manufacture of benzylsulfonylarenes. US0054896; 2007
   Google Scholar
• Wyeth. Azinyl-3-sulfonylindazole derivatives as 5-hydroxytryptamine-6 ligands. WO032833; 2007
   Google Scholar
• Wyeth. Substituted-3-sulfonylindazole derivatives as 5-hydroxytryptamine-6 ligands. WO021711; 2007
   Google Scholar
• Bromidge SM, Brown AM, Clarke SE, 5-Chloro-N-(4-methoxy-3-piperazin-1-yl- phenyl)-3-methyl-2-benzothiophenesulfon- amide (SB-271046): a potent, selective, and orally bioavailable 5-HT6 receptor antagonist. J Med Chem 1999;42(2):202-5
   Google Scholar
• Glennon RA, Lee M, Rangisetty JB, 2-Substituted tryptamines: agents with selectivity for 5-HT6 serotonin receptors. J Med Chem 2000;43(5):1011-8
   Google Scholar
• Tsai Y, Dukat M, Slassi A, N1-(Benzenesulfonyl)tryptamines as novel 5-HT6 antagonists. Bioorg Med Chem Lett 2000;10(20):2295-9
   Google Scholar
• Pullagurla MR, Dukat M, Setola V, N1-benzenesulfonylgramine and N1-benzenesulfonylskatole: novel 5-HT6 receptor ligand templates. Bioorg Med Chem Lett 2003;13(19):3355-9
   Google Scholar
• Esteve. Nitro-substituted phenyl-piperazine compounds, their preparation and use in medicaments. WO069808; 2006
   Google Scholar
• Hoffmann-LaRoche. Chroman derivatives and uses thereof in the treatment of cns disorders. WO066756; 2006
   Google Scholar
• Glaxo. Radiolabelled quinoline-based ligands for the 5-HT6 receptor functionality. WO053785; 2006
   Google Scholar
• Hoffmann-LaRoche. 4-Aryloxy quinoline derivatives as 5-HT6 modulators. WO025798; 2007
   Google Scholar
• Biovitrum. New benzofuran derivatives and their use in the treatment of obesity, type ii diabetes and cns disorders. WO062481; 2006
   Google Scholar
• Hoffmann-LaRoche. Compositions and methods for treating cognitive disorders. WO037482; 2006
   Google Scholar
• Hoffmann-LaRoche. Dibenzoxazepinone derivatives. WO061126; 2006
   Google Scholar
• Korea Research Institute. N-substituted-1H-quinoline-2, 4-diones, preparation method thereof, and pharmaceutical composition containing the same. WO032572; 2007
   Google Scholar
• Hoffmann-LaRoche. Benzimidazole derivatives as 5-HT6, 5-HT2A. WO006677; 2007
   Google Scholar
• Hoffmann-LaRoche. Pyrazolopyrimidines and pyrazolotriazines with 5-HT6 receptor affinity. EP0941994; 1999
   Google Scholar
• Upton N, Chuang TT, Hunter AJ, Virley DJ. 5-HT6 receptor antagonists as novel cognitive enhancing agents for Alzheimer's disease. Neurotherapeutics 2008;5(3):458-69
   Google Scholar
• Martarello L, Parker C, Cunningham V, First evaluation in humans of (11C) GSK215083 as a probe to image the 5-HT6 receptors. J Nucl Med 2008;49(Suppl 1): abstract 313
   Google Scholar
• Zhao SH, Berger J, Clark RD, 3,4-Dihydro-2H-benzo[1,4]oxazine derivatives as 5-HT6 receptor antagonists. Bioorg Med Chem Lett 2007;17(12):3504-7
   Google Scholar
• Hoffmann-LaRoche. Benzoxazine and quinoxaline derivatives and uses. WO037481; 2006
   Google Scholar
• Gannon KS, Heal DJ, Cheetham SC, PRX-07034, a potent and selective 5-HT6 receptor antagonist, reduces food intake and body weight in rats. J Pharmacol Sci 2006;101(Suppl 1): abstract P2-17
   Google Scholar
• Tkachenko S, Ivachtchenko A, Okun I, Comparison of highly selective and non-selective 5-HT6 receptor antagonists in in vitro and in vivo neurodegenerative models. 12th Int Conf Alzheimer's Dis Relat Disord (ICAD) [abstract P4-212]. 11 – 16 July 2009, Vienna
   Google Scholar
• Tkachenko S, Ivachtchenko A, Khvat A, Discovery and preclinical studies of AVN-322 highly selective and potent 5-HT6 antagonist for cognition enhancement in treating neurodegerative diseases. 9th Int Conf Alzheimer Parkinson Dis (AD/PD). 11 – 15 March 2009, Prague
   Google Scholar
• Ramakrishna N, Kambhampati R, Shinde A, SUVN-502: A safe, potent, selective, brain penetrant and orally active 5-HT6 receptor antagonist - first in human clinical phase-1 study. 12th Int Conf Alzheimer's Dis Relat Disord (ICAD) [abstract P1-251]. 11 – 16 July 2009, Vienna
   Google Scholar
• Hoffmann-LaRoche. Benzimidazole derivatives as 5-HT6, 5-HT2A. WO006677; 2007
   Google Scholar
• Hoffmann-LaRoche. derives de benzoxazine et de quinoxaline et leurs utilisations. WO037481; 2006
   Google Scholar
• AstraZeneca. Novel 8-sulfonylamino-3 aminosubstituted chroman or tetrahydronaphtalene derivatives modulating the 5-HT6 receptor. WO126939; 2006
   Google Scholar
• AstraZeneca. Novel 8-sulfonylamino-3 aminosubstituted chroman or tetrahydronaphtalene derivatives modulating the 5HT6 receptor. WO126938; 2006
   Google Scholar
• AstraZeneca. New compounds, process for their preparation, intermediates, pharmaceutical compositions and their use in the treatment of 5-HT6 mediated disorders such as alzheimer's desease, cognitive disorders, cognitive impairment associated with schizophrenia, obesity and parkinson's disease. WO004960; 2007
   Google Scholar
• AstraZeneca. New compounds, process for their preparation, intermediates, pharmaceutical compositions and their use in the treatment of 5-HT6 mediated disorders such as alzheimer's desease, cognitive disorders, cognitive impairment associated with schizophrenia, obesity and parkinson's disease. WO004959; 2007
   Google Scholar
• Psychenomics. Multimediator 5-HT6 receptor antagonists, and uses related thereto. WO091703; 2006
   Google Scholar
• Korea Research Institute of Chemical Technology (Taejon [KR]). 3-Aryl-3-methyl-quinoline-2,4-diones, preparation method thereof and pharmaceutical composition containing same. US084676; 2006
   Google Scholar
• Korea Research Institute of Chemical Technology (Taejon [KR]). 3-Aryl-3-methyl-quinoline-2,4-diones, preparation method thereof and pharmaceutical composition containing same. EP1650190; 2006
   Google Scholar
• Laboratorios del Dr. Esteve, SA. 5-HT6-ligands such as sulfonamide derivatives in drug-induced weight-gain. WO013010; 2009
   Google Scholar
• Laboratorios del Dr. Esteve, SA. 5-HT6-ligands such as sulfonamide derivatives in drug-induced weight-gain. EP2018861; 2009
   Google Scholar
• Laboratorios del Dr. Esteve, SA. Active substance combination comprising a compound with NPY receptor affinity and a compound with 5-HT6 receptor affinity. US059364; 2007
   Google Scholar
• Laboratorios del Dr. Esteve, SA. Active substance combination comprising a compound with NPY receptor affinity and a compound with 5-HT6 receptor affinity. WO014000; 2005
   Google Scholar
• Laboratorios del Dr. Esteve, SA. Active substance combination comprising a compound with NPY receptor affinity and a compound with 5-HT6 receptor affinity. EP1648468; 2006
   Google Scholar
• Fisas A, Codony X, Romero G, Chronic 5-HT6 receptor modulation by E-6837 induces hypophagia and sustained weight loss in diet-induced obese rats. Br J Pharmacol 2006;148(7):973-83
   Google Scholar
• Eli Lilly. Piperazine substituted aryl benzodiazepines. US084643; 2006
   Google Scholar
• Eli Lilly. Piperazine substituted aryl benzodiazepines. WO014895; 2004
   Google Scholar
• Eli Lilly. Piperazine substituted aryl benzodiazepines. EP1546134; 2005
   Google Scholar
• Eli Lilly. Benzenesulfonic acid indol-5-yl esters as antagonists of the 5-HT6 receptor. WO060871; 2002
   Google Scholar
• Eli Lilly. Substituted piperazines of azepines, oxazepines, and thiazepines. US270656; 2006
   Google Scholar
• Eli Lilly. Piperazine substituted aryl benzodiazepines. WO4014895; 2004
   Google Scholar
• Eli Lilly. Piperazine substituted aryl benzodiazepines and their use as dopamine receptor antagonists for the treatment of psychotic disorders. US7214673; 2007
   Google Scholar
• Eli Lilly. N-(2-Arylethyl)benzylamines as antagonists of the 5-HT6 receptor. US132800; 2004
   Google Scholar
• Selena Pharmaceuticals, Inc. Agents for treating neurodegenerative disorders. RU118252; 1995
   Google Scholar
• Medivation, Inc. A drug demonstrating anxiolytic effect based on hydrogenated pyrido(4,3-b)indoles, its pharmacological compound and application method. WO005771; 2009
   Google Scholar
• Wyeth Pharmaceutical. Indolylalkylamine metabolites as 5-hydroxytrytamine-6 ligands. WO002125; 2006
   Google Scholar
• GlaxoSmithKline. Use of 5-HT6 antagonists. US094979; 2002
   Google Scholar
• Swedish Orphan Biovitrum AB. Aryl sulfonamides as serotonin antagonist for the treatment of obesity. SE2739; 2000
   Google Scholar
• Laboratorios del Dr. Esteve, SA. Combination of at least two 5-HT6-ligands. EP384032; 2007
   Google Scholar
• GlaxoSmithKline. Combinations comprising 3-phenylsulfonyl-8-piperazinyl-1yl-quinoline. GB24281; 2007
   Google Scholar
• GlaxoSmithKline. Radiolabelled quinoline-based ligands for the 5-HT6 receptor functionality. GB25548; 2004
   Google Scholar
• F. Hoffmann-La Roche AG. Benzoxazine derivatives as 5-HT6 modulators and uses thereof. US435732; 2003
   Google Scholar
• F. Hoffmann-La Roche AG. Dibenzoxazepinone derivatives. WO061126; 2006
   Google Scholar
• GlaxoSmithKline. Methods and compositions for treating schizophrenia using antipsychotic combination therapy. WO017836; 2009
   Google Scholar
• GlaxoSmithKline. Benzenesulfonamide derivatives as antipsychotic agents. GB24466; 2002
   Google Scholar
• Suven Life Sciences Ltd. Amino arylsulfonamide compounds and their use as 5-HT6 ligands field of invention. WO053997; 2009
   Google Scholar
• Epix Pharmaceuticals, Inc. Combinations comprising 5HT6 modulators and cholinesterase inhibitors. US816517; 2006
   Google Scholar
• Laboratorios del Dr. Esteve, SA. Process for the preparation of N-(phenylethyl)anilines salts and solvates thereof useful as serotonin 5-HT6 antagonists. EP384003; 2008
   Google Scholar
• Swedish Orphan Biovitrum AB. Benzofuranyl derivatives as 5-HT6-receptor inhibitors. SE1383; 2005
   Google Scholar
• Suven Life Sciences Ltd. Use of 5-HT6 antagonists to prevent relapse into addiction. WO087123; 2008
   Google Scholar
• Suven Life Sciences Ltd. N-Arylsulfonyl-3-substituted indoles having serotonin receptor affinity, process for their preparation and pharmaceutical composition containing them. IN884; 2002
   Google Scholar