Recent advances in histamine H₃ receptor antagonists/inverse agonists

Bibliography

• Arrang JM, Garbarg M, Schwartz JC. Autoinhibition of brain histamine release mediated by a novel class (H3) receptor of histamine. Nature 1983;302:832-7
   PubMed Web of Science ®Google Scholar
• Clapham J, Kilpatrick GJ. Histamine H3 receptors modulate the release of [3H]-acetylcholine from slices of rat entorhinal cortex: evidence for the possible existence of H3 receptor subtypes. Br J Pharmacol 1992;107:919-23
   Google Scholar
• Schlicker E, Malinowska B, Kathmann M, Gothert M. Modulation of neurotransmitter release via histamine H3 heteroreceptors. Fund Clin Pharmacol 1994;8:128-37
   PubMed Web of Science ®Google Scholar
• Lovenberg TW, Roland BL, Wilson SJ, Cloning and functional expression of the human histamine H3 receptor. Mol Pharmacol 1999;55:1101-7
   PubMed Web of Science ®Google Scholar
• Oda T, Morikawa N, Saito Y, Molecular cloning and charaterization of a new human histamine receptor preferentially expressed in leukocytes. J Biol Chem 2000;275:36781-6
   PubMed Web of Science ®Google Scholar
• Nakamura T, Itadani H, Hidaka Y, Molecular cloning and characterization of a new human histamine receptor, HH4R. Biochem Biophys Res Commun 2000;279:615-20
   PubMed Web of Science ®Google Scholar
• Liu C, Ma X-J, Jiang X, Cloning and pharmacological characerization of a fourth histamine receptor (H4) expressed in bone marrow. Mol Pharmacol 2001;59:420-6
   PubMed Web of Science ®Google Scholar
• Morse KL, Behan J, Laz TM, Cloning and pharmacological characterization of a novel human histamine receptor. J Pharmacol Exp Ther 2001;296:1058-66
   PubMed Web of Science ®Google Scholar
• Hough LB. Genomics meets histamine receptors: new subtypes, new receptors. Mol Pharmacol 2001;59:415-19
   PubMed Web of Science ®Google Scholar
• Hancock AA, Esbenshade TA, Krueger KM, Yao BB. Genetic aspects to pharmacological heterogeneity of histamine H3 receptors. Life Sci 2003;73:3043-72
   PubMed Web of Science ®Google Scholar
• Leurs R, Bakker RA, Timmerman H, de Esch IJP. The histamine H3 receptor: from gene cloning to H3 receptor drugs. Nat Rev Drug Discov 2005;4:107-18
   PubMed Web of Science ®Google Scholar
• Ireland-Denny L, Parihar AS, Miller TR, Species-related pharmacological heterogeneity of histamine H3 receptors. Eur J Pharmacol 2001;433:141-50
   PubMed Web of Science ®Google Scholar
• Bakker RA. Histamine H3-receptor isoforms. Inflamm Res 2004;53:509-16
   PubMed Web of Science ®Google Scholar
• Arrang JM, Morisset S, Gbahou F. Constitutive activity of the histamine H3 receptor. Trends Pharmacol Sci 2007;28:350-7
   PubMed Web of Science ®Google Scholar
• Gbahou F, Rouleau A, Morisset S, Protean agonism at histamine H3 receptors in vitro and in vivo. Proc Natl Acad Sci USA 2003;100:11086-91
   PubMed Web of Science ®Google Scholar
• Esbenshade TA, Estvander BR, Miller TR, Pharmacological classification of histamine H3 receptor agents across species is attributable to transmembrane 3 sequence differences. Inflamm Res 2007;56:S45-6
   Google Scholar
• Stark H, Kathmann M, Schlicker E, Medicinal chemical and pharmacological aspects of imidazole-containing histamine H3 receptor antagonists. Mini Rev Med Chem 2004;4:965-77
   PubMed Web of Science ®Google Scholar
• Stark H, Arrang JM, Ligneau X, The histamine H3 receptor and its ligands. Prog Med Chem 2001;38:279-308
   PubMedGoogle Scholar
• Stark H, Sippl W, Ligneau X, Different antagonist binding properties of human and rat histamine H3 receptors. Bioorg Med Chem Lett 2001;11:951-4
   PubMed Web of Science ®Google Scholar
• Yang R, Hey JA, Aslanian R, Rizzo CA. Coordination of histamine H3 receptor antagonists with human adrenal cytochrome P450 enzymes. Pharmacology 2002;66:128-3
   PubMed Web of Science ®Google Scholar
• Ganellin CR, Leurquin F, Piripitsi A, Synthesis of potent non-imidazole histamine H3 receptor antagonists. Arch Pharm Pharm Med Chem 1998;331:395-404
   PubMed Web of Science ®Google Scholar
• Esbenshade TA, Fox GB, Cowart MD. Histamine H3 receptor antagonists: preclinical promise for treating obesity and cognitive disorders. Mol Interv 2006;6:77-88
   PubMed Web of Science ®Google Scholar
• Berlin M, Boyce CW. Recent advances in the development of histamine H3 antagonists. Exp Opin Ther Patents 2007;17:675-87
   PubMed Web of Science ®Google Scholar
• Hudkins RL, Raddatz R. Recent advances in drug discovery of histamine H3 antagonists. Ann Rep Med Chem 2007;42:49-62
   Google Scholar
• Sander K, Kottke T, Stark H. Histamine H3 antagonists go to clinics. Biol Pharm Bull 2008;31:2163-81
   PubMed Web of Science ®Google Scholar
• Stocking EM, Letavic MA. Histamine H3 antagonists as wake-promoting and pro-cognitive agents. Curr Top Med Chem 2008;8:988-1002
   PubMed Web of Science ®Google Scholar
• Glemkow MJ, Davenport AJ, Harich S, The histamine H3 receptor as a therapeutic drug target for CNS disoders. Drug Discov Today 2009;14:509-15
   Google Scholar
• Wijtmans M, Leurs R, de Esch I. Histamine H3 receptor ligands break ground in a remarkable plethora of therapeutic areas. Exp Opin Invest Drugs 2007;16:967-85
   PubMed Web of Science ®Google Scholar
• Esbenshade TA, Browman KE, Bitner RS, The histamine H3 receptor: an atractive target for the treatment of cognitive disorders. Br J Pharmacol 2008;154:1166-81
   PubMed Web of Science ®Google Scholar
• Tiligada E, Zampeli E, Sander K, Stark H. Histamine H3 and H4 receptors as novel drug targets. Exp Opin Investig Drugs 2009;18:1519-31
   PubMed Web of Science ®Google Scholar
• Celanire S, Lebon F, Stark H. Drug discovery: from hits to clinical candidates. In: Vohora DS, editor, The third histamine H3 receptor: selective ligands as potential therapeutic agents in CNS disorders. Taylor & Francis CRC Press, Inc., Boca Raton, FL; 2009. p. 103-65
   Google Scholar
• Ito C. Histamine H3 receptor inverse agonists as novel antipsychotics. Cent Nerv Syst Agents Med Chem 2009;9:132-6
   PubMedGoogle Scholar
• Raddatz R, Tao M, Hudkins RL. Histamine H3 antagonists for treatment of cognitive deficits in CNS diseases. Curr Top Med Chem 2010;10:153-69
   PubMed Web of Science ®Google Scholar
• Efficacy and safety study for cognitive deficits in adult subjects with schizophrenia. NCT01077700; 26 February 2010. Available from: www.ClinicalTrials.gov [Last accessed 7 May 2010]
   Google Scholar
• Efficacy and safety study of ABT-288 in subjects with mild-to-moderate Alzheimer's disease. NCT01018875; 20 November 2009. Available from: www.ClinicalTrials.gov [Last accessed 7 May 2010]
   Google Scholar
• Single-dose safety study of APD916 in healthy volunteers. NCT01093508; 24 March 2010. Available from: www.ClinicalTrials.gov [Last accessed 7 May 2010]
   Google Scholar
• Efficacy and safety study of BF2.649 and BF2.649 add on modafinil on cataplexy in patients with narcolespy (Harmony II). NCT01067235; 9 February 2010. Available from: www.ClinicalTrials.gov [Last accessed 7 May 2010]
   Google Scholar
• Efficacy and safety study of BF2.649 in the treatment of excessive daytime sleepiness in narcolepsy (Harmony1). NCT01067222; 9 February 2010. Available from: www.ClinicalTrials.gov [Last accessed 7 May 2010]
   Google Scholar
• Efficacy and safety of BF2.649 in excessive daytime sleepiness (EDS) in Parkinson's disease (HARPS 1). NCT01036139; 11 December 2009. Available from: www.ClinicalTrials.gov [Last accessed 7 May 2010]
   Google Scholar
• Study to demonstrate cognitive enhancing effects of BF2.649. NCT00690274; 2 June 2008. Available from: www.ClinicalTrials.gov [Last accessed 7 May 2010]
   Google Scholar
• Available from: http://www.cephalon.com/our-science/pipeline.shtml [Last accessed 7 May 2010]
   Google Scholar
• A study of GSK189254 and duloxetine in the electrical hyperalgesia model of healthy volunteers (COMPLETED). NCT00387413; 11 October 2006. Available from: www.ClinicalTrials.gov [Last accessed 17 March 2010]
   Google Scholar
• Study to evaluate the efficacy and safety of GSK239512 in schizophrenia. NCT01009060; 5 November 2009. Available from: www.ClinicalTrials.gov [Last accessed 7 May 2010]
   Google Scholar
• Study to evaluate the efficacy and safety of GSK239512 in Alzheimer's disease. NCT01009255; 5 November 2009. Available from: www.ClinicalTrials.gov [Last accessed 7 May 2010]
   Google Scholar
• Allergen challenge chamber study with single dose oral GSK835726 compared with placebo (COMPLETED). NCT00851344; 24 February 2009. Available from: www.ClinicalTrials.gov [Last accessed 7 May 2010]
   Google Scholar
• 723/726 Proof of concept study in allergen challenge chamber in Hannover (COMPLETED). NCT00972504; 27 August 2009. Available from: www.ClinicalTrials.gov [Last accessed 7 May 2010]
   Google Scholar
• Allergen challenge chamber study with single dose intranasal GSK1004723 compared with placebo (COMPLETED). NCT00824356; 8 January 2009. Available from: www.ClinicalTrials.gov [Last accessed 7 May 2010]
   Google Scholar
• Available from: http://www.ttpharma.com/theraputicareas/metabolicdisease/obesity/HPP404/tabid/128/default.aspx [Last accessed 7 May 2010]
   Google Scholar
• A safety and effectiveness study of a single dose of JNJ-17216498 in patients with narcolepsy (COMPLETED). NCT00424931; 19 January 2007. Available from: www.ClinicalTrials.gov [Last accessed 7 May 2010]
   Google Scholar
• A safety and effectiveness study of JNJ-31001074 in adults with Attention-Deficit/Hyperactivity Disorder (COMPLETED). NCT00566449; 29 November 2007. Available from: www.ClinicalTrials.gov [Last accessed 7 May 2010]
   Google Scholar
• A study to evaluate 3 different doses of JNJ-31001074 in the treatment of adults with Attention-Deficit/Hyperactivity Disorder (ADHD) (COMPLETED). NCT00880217; 9 April 2009. Available from: www.ClinicalTrials.gov [Last accessed 7 May 2010]
   Google Scholar
• A study to evaluate pharmacokinetics, safety and tolerability after a single dose administration of JNJ-31001074 in children (6-11 Years) with Attention Deficit Hyperactivity Disorder (ADHD) (COMPLETED). NCT00890240; 27 April 2009. Available from: www.ClinicalTrials.gov [Last accessed 7 May 2010]
   Google Scholar
• A study to evaluate pharmacokinetics, safety and tolerability after a single dose administration of JNJ-31001074 in pediatric patients (12-17 years) with Attention Deficit Hyperactivity Disorder (ADHD) (COMPLETED). NCT00890292; 27 April 2009. Available from: www.ClinicalTrials.gov [Last accessed 7 May 2010]
   Google Scholar
• MK0249 for the treatment of cognitive impairment in patients with schizophrenia (COMPLETED). NCT00506077; 24 July 2007. Available from: www.ClinicalTrials.gov [Last accessed 7 May 2010]
   Google Scholar
• MK0249 for the symptomatic treatment of Alzheimer's disease (COMPLETED). NCT00420420; 9 January 2007. Available from: www.ClinicalTrials.gov [Last accessed 7 May 2010]
   Google Scholar
• A study to test the safety and efficacy of MK0249 in patients with ADHD (COMPLETED). NCT00475735; 17 May 2007. Available from: www.ClinicalTrials.gov [Last accessed 7 May 2010]
   Google Scholar
• BOLD functional magnetic resonance imaging (fMRI) and cerebral blood flow measurements as biomarkers for cognition enhancing drugs (COMPLETED). NCT00887601; 23 April 2009. Available from: www.ClinicalTrials.gov [Last accessed 7 May 2010]
   Google Scholar
• A study to evaluate the efficacy and safety of two doses of PF-03654746 in adults with Attention Deficit Hyperactivity Disorder (ADHD) (COMPLETED). NCT00531752; 18 September 2007. Available from: www.ClinicalTrials.gov [Last accessed 7 May 2010]
   Google Scholar
• A study to evaluate the safety, tolerability, and blood levels of PF-03654746 in subjects with mild to moderate Alzheimer's disease. NCT01028911; 7 December 2009. Available from: www.ClinicalTrials.gov [Last accessed 7 May 2010]
   Google Scholar
• A study of a novel compound for excessive daytime sleepiness associated with narcolepsy. NCT01006122; 29 October 2009. Available from: www.ClinicalTrials.gov [Last accessed 7 May 2010]
   Google Scholar
• A study to test a new decongestant in patients with allergic rhinitis following a nasal allergen challenge (COMPLETED). NCT00562120; 19 November 2007. Available from: www.ClinicalTrials.gov [Last accessed 7 May 2010]
   Google Scholar
• Available from: http://eu.sanofi-aventis.com/binaries/RD_2009-10-30_phase-I-II_EN_tcm28-24004.pdf [Last accessed 10 March 2010]
   Google Scholar
• Efficacy and safety trial to evaluate the effect of SCH 497079 on weight in obese and overweight subjects (Study P05483)(COMPLETED). NCT00642993; 21 March 2008. Available from: www.ClinicalTrials.gov [Last accessed 17 March 2010]
   Google Scholar
• Alavijeh MS, Palmer AM. Measurement of the pharmacokinetics and pharmacodynamics of neuroactive compounds. Neurobiol Dis 2010;37:38-47
   PubMed Web of Science ®Google Scholar
• Hancock AA. The challenge of drug discovery of a GPCR target: analysis of preclinical pharmacology of histamine H3 antagonists/inverse agonists. Biochem Pharmacol 2006;71:1103-13
   PubMed Web of Science ®Google Scholar
• Bonaventure P, Letavic M, Dugovic C, Histamine H3 receptor anatagonists: from target identification to drug leads. Biochem Pharmacol 2007;73:1084-96
   PubMed Web of Science ®Google Scholar
• Rodriguez Sarmiento RM, Nettekoven MH, Taylor S, Selective naphthalene H(3) receptor inverse agonists with reduced potential to induce phospholipidosis and their quinoline analogs. Bioorg Med Chem Lett 2009;19:4495-500
   PubMed Web of Science ®Google Scholar
• Hay T, Jones R, Beaumont K, Modulation of the partition coefficient between octanol and buffer at pH 7.4 and pKa to achieve the optimum balance of blood clearance and volume of distribution for a series of tetrahydropyran histamine type 3 receptor antagonists. Drug Metab Dispos 2009;37:1864-70
   PubMed Web of Science ®Google Scholar
• Black LA, Liu H, Diaz GJ, Minimization of potential hERG liability in histamine H3 receptor antagonists. Inflamm Res 2008;57(Suppl 1):S45-6
   Google Scholar
• Liu H, Altenbach RJ, Diaz GJ, In vitro studies on a class of quinoline containing histamine H3 antagonists. Bioorg Med Chem Lett 2010;20:3295-30
   Google Scholar
• Strakhova M, Esbenshade TA. Characterization of histaminergic receptors. Curr Protoc Pharmacol 2007;37(Suppl):1. 19.1-24
   Google Scholar
• Neurogen Corp. Dipiperazinyl ketones and related analogues. WO2007013506; 2007
   Google Scholar
• Miller TR, Baranowski JL, Estvander BR, A robust and high-capacity [(35)S]GTPgammaS binding assay for determining antagonist and inverse agonist pharmacological parameters of histamine H(3) receptor ligands. Assay Drug Dev Technol 2008;6:339-49
   Google Scholar
• Hew RW, Hodgkinson CR, Hill SJ. Characterization of histamine H3-receptors in guinea-pig ileum with H3-selective ligands. Br J Pharmacol 1990;101:621-4
   PubMedGoogle Scholar
• Sander K, von Coburg I, Camellin J-C, Acidic elements in histamine H3 receptor antagonists. Bioorg Med Chem Lett 2010;20:1581-4
   PubMed Web of Science ®Google Scholar
• Vanderbilt University. Unnatural dispyrin analogues, preparation and uses thereof. WO2009152071; 2009
   Google Scholar
• Kennedy JP, Conn PJ, Lindsley CW. A novel class of H3 antagonists derived from the natural product guide synthesis of unnatural analogs of the marine bromopyrrole alkaloid dispyrin. Biorg Med Chem Lett 2009;19:3204-8
   Google Scholar
• Kennedy JP, Brogan JT, Lindsley CW. Total synthesis and biological evaluation of the marine bromopyrrole alkaloid dispyrin: elucidation of discrete molecular targets with therapeutic potential. J Nat Prod 2008;71:1783-6
   Google Scholar
• Sanofi-Aventis. Substituted N-phenyl-pyrrolidinylmethylpyrrolidine amides and therapeutic use thereof as histamine H3 receptor modulators. WO2009052063; 2009
   Google Scholar
• UCB Pharma SA. Compounds comprising a cyclobutoxy group. WO2008128919; 2008
   Google Scholar
• Schering Corp. Phenoxypiperidines and analogs thereof useful as histamine H3 anatagonists. WO2007075629; 2007
   Google Scholar
• Schering Corp. Oxypiperidine derivatives and methods of use thereof. WO2009045313; 2009
   Google Scholar
• Taisho Pharmaceutical Co., Ltd. Pyrazole derivatives. WO2008072724; 2008
   Google Scholar
• Janssen Pharmaceutica (Johnson & Johnson). Subtituted phenylpropyl amines as histamine H3 receptor and serotonin transporter modulators. WO2008064036; 2008
   Google Scholar
• Stocking EM, Miller JM, Barbier AJ, Synthesis and biological evaluation of diamine-based histamine H3 antagonists with serotonin reuptake inhibitor activity. Bioorg Med Chem Lett 2007;17:3130-5
   Google Scholar
• Janssen Pharmaceutica (Johnson & Johnson). Butyl and butynyl amine compounds. WO2008002817; 2008
   Google Scholar
• Letavic MA, Stocking EM, Barbier AJ, Benzylamine histamine H3 antagonists and serotonin reuptake inhibitors. Bioorg Med Chem Lett 2007;17:4799-803
   PubMedGoogle Scholar
• Novo Nordisk, Inc. Novel aryl- and heteroarylpiperazines. US20090264435; 2009
   Google Scholar
• Evotec Neurosciences GMBH. Diazepanes as histamine H3 receptor antagonist. WO2009095394; 2009
   Google Scholar
• High Point Pharmaceuticals, LLC. Histamine H3 receptor ligands. WO2009126782; 2009
   Google Scholar
• Cephalon, Inc. Substituted pyridazinone derivatives as histamine-3 (H3) receptor ligands. WO2009142732; 2009
   Google Scholar
• Pfizer Products, Inc. Azabicyclic ether histamine-3 antagonists. WO2007138431; 2007
   Google Scholar
• Les Laboratoires Servier. Azabicyclic compounds, a process for their preparation and pharmaceutical composition containing them. US20090312389; 2009
   Google Scholar
• Les Laboratoires Servier. Novel azabicyclo derivatives, preparation methods thereof and pharmaceutical composition containing same. WO2005089747; 2005
   Google Scholar
• Wyeth. N-Substituted azacyclylamines as histamine-3 antagonists. WO2007108936; 2007
   Google Scholar
• Wyeth. N-Benzoyl- and N-benzylpyrrolidin-3-ylamines as histamine H3 antagonists. WO2007136668; 2007
   Google Scholar
• Wyeth. N-Substituted azacyclylamines as histamine-3 antagonists. WO2008045371; 2008
   Google Scholar
• Cole DC, Gross JL, Comery TA, Benzimidazole- and indole-substituted 1,3′-bipyrrolidine benzamides as histamine H3 receptor antagonists. Bioorg Med Chem Lett 2010;20:1237-40
   Google Scholar
• Wyeth. Azacyclylbenzamide derivatives as histamine-3 antagonist. WO2008147945; 2008
   Google Scholar
• Eli Lilly & Co. Histamine H3 receptor agents, preparation and therapeutic uses. WO2007005503; 2007
   Google Scholar
• Schering Corp. Piperidine derivatives useful as histamine H3 antagonists. WO2007001975; 2007
   Google Scholar
• Schering Corp. Substituted aniline derivatives useful as histamine H3 antagonists. WO2007075688; 2007
   Google Scholar
• Evotec Neurosciences GMBH. Azetidines and cyclobutanes as histamine H3 receptor antagonists. WO2009135842; 2009
   Google Scholar
• Janssen Pharmaceutica (Johnson & Johnson). Substituted aminomethyl benzamide compounds. WO2008002818; 2008
   Google Scholar
• Janssen Pharmaceutica (Johnson & Johnson). Substituted benzyl amine compounds. WO2008002820; 2008
   Google Scholar
• Janssen Pharmaceutica (Johnson & Johnson). Cyclopropyl amines as modulators of the histamine H3 receptor. WO2007035425; 2007
   Google Scholar
• Janssen Pharmaceutica (Johnson & Johnson). Substituted benzamide modulators of the histamine H3 receptor. WO2008002816; 2008
   Google Scholar
• Janssen Pharmaceutica (Johnson & Johnson). Cycloalkoxy and heterocycloalkyloxypyridine compounds as modulators of the histamine H3 receptor. WO2009067401; 2009
   Google Scholar
• Janssen Pharmaceutica (Johnson & Johnson). Substituted pyridyl amide compounds as modulators of the histamine H3 receptor. WO2007143422; 2007
   Google Scholar
• Janssen Pharmaceutica (Johnson & Johnson). Substituted pyridyl amide compounds as modulators of the histamine H3 receptor. WO2009067406; 2009
   Google Scholar
• Janssen Pharmaceutica (Johnson & Johnson). Substituted pyrazinyl amide compounds as modulators of the histamine H3 receptor. WO2009067405; 2009
   Google Scholar
• Janssen Pharmaceutica (Johnson & Johnson). Substituted pyrrolidine amides as modulators of the histamine H3 receptor. WO2009143153; 2009
   Google Scholar
• Stocking EM, Aluisio L, Atack JR, Novel substituted pyrrolidines are high affinity histamine H3 receptor antagonists. Bioorg Med Chem Lett 2010;20:2755-60
   Google Scholar
• AstraZeneca Pharmaceuticals LP. Cyclopropyl amide derivatives 978. WO2009024823; 2009
   Google Scholar
• Faghih R, Dwight W, Vasudevan A, Aminoalkoxybiphenylnitriles as histamine H3 receptor ligands. Bioorg Med Chem Lett 2002;12:3077-9
   PubMed Web of Science ®Google Scholar
• Faghih R, Dwight W, Pan JB, Synthesis and SAR of aminoalkoxy-biaryl-4-carboxamides: novel and selective histamine H3 receptor antagonists. Bioorg Med Chem Lett 2003;13:1325-8
   PubMed Web of Science ®Google Scholar
• Zhao C, Sun M, Bennani YL, Design of a new histamine H3 receptor antagonist chemotype: (3aR, 6aR)-5-alkyl-1-aryl-octahydropyrrolo[3,4-b]pyrroles, synthesis, structure–activity relationships. J Med Chem 2009;52:4640-9
   Google Scholar
• Abbott Laboratories. Octahydro-pyrrolo[3,4-b]pyrrole derivatives. WO2007100990; 2007
   Google Scholar
• Arena Pharmaceuticals. Modulators of the histamine H3-receptor useful for the treatment of disorders related thereto. WO2008005338; 2008
   Google Scholar
• Covel JA, Santora VJ, Smith JM, Design and evaluation of novel biphenyl sulfonamide derivatives with potent histamine H3 receptor inverse agonist activity, J Med Chem 2009;52:5603-11
   Google Scholar
• Arena Pharmaceuticals. Biphenyl derivatives as modulators of the histamine H3 receptor useful for the treatment of disorders related thereto. WO2009058300; 2009
   Google Scholar
• Arena Pharmaceuticals. Biphenyl sulfonyl and phenyl-heteroaryl sulfonyl modulators of the histamine H3 receptor useful for the treatment of disorders related thereto. WO2008048609; 2008
   Google Scholar
• Arena Pharmaceuticals. Modulators of the histamine H3 receptor useful for the treatment of disorders related thereto. WO2009105206; 2009
   Google Scholar
• High Point Pharmaceuticals. New heterocyclic H3 antagonists. WO2008154126; 2008
   Google Scholar
• Cephalon, Inc. Substituted pyridazine derivatives which have histamine H3 antagonist activity. WO2009097306; 2009
   Google Scholar
• Glaxo Group Ltd. Piperazinone derivatives useful as histamine H3 receptor antagonists and/or inverse agonists. WO2007009741; 2007
   Google Scholar
• Procopiou PA, Ancliff RA, Bamforg MJ, 4-Acyl-1-(4-aminoalkoxyphenyl)-ketopiperazines as a novel class of non-brain-penetrant histamine H3 receptor antagonists. J Med Chem 2007;50:6706-17
   PubMed Web of Science ®Google Scholar
• Wyeth. Aminoalkylazole derivatives as histamine-3 antagonists. WO2009012252; 2009
   Google Scholar
• Taisho Pharmaceutical Co., Ltd. Pyrazole derivatives. WO2008072724; 2008
   Google Scholar
• Athersys, Inc. Pyrazoles for the treatment of obesity and other CNS disorders. WO2007094962; 2007
   Google Scholar
• Novo Nordisk, Inc. Substituted homopiperidine, piperidine or pyrrolidine derivatives. US20080113995; 2008
   Google Scholar
• UCB Pharma SA. Fused oxazoles and thiazoles as histamine H3 receptor ligands. WO2008012010; 2008
   Google Scholar
• Abbott Laboratories. Cyclopropyl amine derivatives. WO2007150010; 2007
   Google Scholar
• Abbott Laboratories. Cyclopropylamine derivatives. WO2009079225; 2009
   Google Scholar
• Pfizer Products, Inc. Histamine H3 receptor antagonists. WO2007049123; 2007
   Google Scholar
• Athersys, Inc. Indole derivatives as histamine 3 receptor inhibitors for the treatment of cognitive and sleep disorders, obesity and other CNS disorders. WO2007047775; 2007
   Google Scholar
• Hoffmann-La Roche AG. 5-Aminoindole derivatives. WO2006077024; 2006
   Google Scholar
• Hoffmann-La Roche AG. Indole derivatives as histamine H3 receptor antagonists. WO2005123716; 2005
   Google Scholar
• Hoffmann-La Roche AG. 5-Amido-2-carboxyamide indoles. WO2007115938; 2007
   Google Scholar
• Hoffmann-La Roche AG. Aza-indole-2-carboxyamide derivatives. WO2007057329; 2007
   Google Scholar
• Hoffmann-La Roche AG. 5-Amido-(1H-indol-2-yl) piperazin-1-yl-methanone derivatives as histamine H3 receptor ligands. WO2008095823; 2008
   Google Scholar
• Pierson PD, Fettes A, Freichel C, 5-Hydroxyindole-2-carboxylic acid amides: novel histamine-3 receptor inverse agonists for the treatment of obesity. J Med Chem 2009;52:3855-68
   PubMed Web of Science ®Google Scholar
• Janssen Pharmaceutica (Johnson & Johnson). Indole and benzothiophene compounds as modulators of the histamine H3 receptor. WO2008109333; 2008
   Google Scholar
• Hoffmann-La Roche AG. Benzofuran- and benzo[b]thiophene-2-carboxylic acid amide derivatives and use thereof as histamine 3 receptor modulators. WO2009013195; 2009
   Google Scholar
• Pfizer Products, Inc. Benzimidazole antagonists of the H3 receptor. WO2007069053; 2007
   Google Scholar
• Neurogen Corp. Pyridynyl-substituted piperazinyl oxoethyl tetrahydro-pyrazolopyridines. WO2009100120; 2009
   Google Scholar
• Abbott Laboratories. Benzothiazole and benzoxazole derivatives and methods of use. WO2009085945; 2009
   Google Scholar
• Abbott Laboratories. Fused bicyclic-substituted amines as histamine-3 receptor ligands. US20080119520; 2008
   Google Scholar
• Abbott Laboratories. Benzothiazole cyclobutyl amine derivatives and their use as histamine-3 receptors. WO2007038074; 2007
   Google Scholar
• Pfizer Products, Inc. Chromane antagonists of the H3 receptor. WO2007088450; 2007
   Google Scholar
• Pfizer Products, Inc. Tetralines antagonists of the H-3 receptor. WO2007105053; 2007
   Google Scholar
• Pfizer Products, Inc. 1-Pyrrolidine indane derivatives as histamine-3 receptor antagonists. WO2007099423; 2007
   Google Scholar
• Abbott Laboratories. Bicyclic-substituted amines as histamine-3 receptor ligands. US2009054420; 2009
   Google Scholar
• Wyeth. Isoquinolinyl and isoindolinyl derivatives as histamine-3 antagonists. WO2009036144; 2009
   Google Scholar
• Wyeth. Azacyclylisoquinolinone and isoindolinone derivatives as histamine-3 antagonists. WO2009036117; 2009
   Google Scholar
• Janssen Pharmaceutica (Johnson & Johnson). Diaryl-substituted tetrahydroisoquinolines as histamine H3 receptor and serotonin transporter modulators. WO2008144305; 2008
   Google Scholar
• Janssen Pharmaceutica (Johnson & Johnson). Tetrahydroisoquinoline compounds as modulators of the histamine H3 receptor. WO2008109336; 2008
   Google Scholar
• Mizutani T, Nagase T, Ito S, Development of novel 2-[4-(aminoalkoxy)phenyl]-4(3H)-quinazolinone derivatives as potent and selective histamine H3 receptor inverse agonists. Bioorg Med Chem Lett 2008;1:6041-5
   Google Scholar
• Nagase T, Mizutani T, Ishikawa S, Synthesis, structure–activity relationships, and biological profiles of a quinazolinone class of histamine H3 receptor inverse agonists. J Med Chem 2008;51:4780-9
   PubMed Web of Science ®Google Scholar
• Nagase T, Mizutani T, Sekino E, Synthesis and evaluation of structurally constrained quinazolinone derivatives as potent and selective histamine H3 receptor inverse agonists. J Med Chem 2008;51:6889-901
   PubMed Web of Science ®Google Scholar
• Banyu Pharmaceutical. Fused ring 4-oxopyrimidine derivative. US20090209562; 2009
   Google Scholar
• Merck and Co., Inc. Crystal of 4(3H)-quinazoline derivative. US20080139589; 2008
   Google Scholar
• Pfizer, Inc. Tetrahydronaphthyridine derivatives. US20090258861; 2009
   Google Scholar
• Pfizer, Inc. Tetrahydronaphthyridine derivatives. US2005256135; 2005
   Google Scholar
• Evotec Neurosciences GMBH. Tetrahydronaphthyridines and aza derivatives thereof as histamine H3 receptor antagonists. WO2009121812; 2009
   Google Scholar
• Glaxo Group Ltd. 2-Substituted 4-benzylphthalazinone derivatives as histamine H1 and H3 antagonists. WO2007122156; 2007
   Google Scholar
• Glaxo Group Ltd. Pharmaceutical composition comprising a non-steroidal glucocorticoid receptor agonist in combination with a dual histamine antagonist. WO2009153296; 2009
   Google Scholar
• Glaxo Group Ltd. Histamine receptor antagonists comprising an azepin core. WO2007135081; 2007
   Google Scholar
• Neurogen Corp. Tetrahydropyrido [3,4-D]pyriminides and related analogues. WO2007146122; 2007
   Google Scholar
• Neurogen Corp. Piperazinyl oxoalkyl tetrahydro-beta-carbolines and related analogues. WO2009003003; 2009
   Google Scholar
• AstraZeneca AB. Spirocyclopropyl piperidine derivatives. WO2008147314; 2008
   Google Scholar
• Neurogen Corp. Substituted azaspiro derivatives. WO2007133561; 2007
   Google Scholar
• Neurogen Corp. Substituted aryl-fused spirocyclic amines. WO2009039431; 2009
   Google Scholar
• Cephalon, Inc. Substituted spirocyclic piperidine derivatives as histamine-3 (H3) receptor ligands. WO2009097309; 2009
   Google Scholar
• Cephalon, Inc. Substituted spirocyclic piperidine derivatives as histamine 3 (H3) receptor ligands. WO2009097567; 2009
   Google Scholar
• Pfizer Products, Inc. Spirocyclic amine histamine-3 receptor antagonists. WO2007063385; 2007
   Google Scholar
• Pfizer Products, Inc. Spirochromane antagonists of the H-3 receptor. WO2001088462; 2007
   Google Scholar
• Merck & Co.; Banyu Pharmaceutical. Aza-substituted spiro derivatives. WO2007055418; 2007
   Google Scholar
• Banyu Pharmaceutical. Novel piperidine derivatives. WO2006129826; 2006
   Google Scholar
• Ballon JS, Feifel D. A systematic review of modafinil: potential clinical uses and mechanisms of action. J Clin Psychiatry 2006;67:554-66
   PubMed Web of Science ®Google Scholar
• Bioprojet Soc Civ. Combination of modafinil and an antagonist or inverse agonist of the H3 receptor. WO2008009866; 2008
   Google Scholar
• Abbott Laboratories. Composition for treatment of cognitive disorders. WO2009082698; 2009
   Google Scholar
• Abbott Laboratories. Octahydro-pyrrolo[3,4-b]pyrole N-oxides. WO2009036132; 2009
   Google Scholar
• Arena Pharmaceuticals. (R)-1-{2-[4′-(3-Methoxy-propane-1-sulfonyl)-biphenyl-4-yl]-ethyl}-2-methyl-pyrrolidine. WO2008153958; 2008
   Google Scholar
• Glaxo Group Ltd. 6-(2,3,4,5-Tetrahydro-1H-benzo[d] azepi-7-yloxy)-nicotamide derivatives as radiolabelled ligands. WO2006072596; 2006
   Google Scholar
• Glaxo Group Ltd. 1-{4-[(1-Cyclobutyl-4-piperidinyl)oxy]phenyl]-4-{[-(methylsulfonyl)phenyl]carbonyl piperazin as histamine H3 antagonist. WO2006090142; 2006
   Google Scholar
• Glaxo Group Ltd. Piperazine derivative having affinity for the histamine H3 receptor. WO2009030716; 2009
   Google Scholar
• Novo Nordisk. 6-(4-Cyclopropylpiperazin-1-yl)-2′-methyl-[3,4′]-bipyridine and its use as a medicament. WO2007135111; 2007
   Google Scholar
• Novo Nordisk. 3-(1,3-Benzodioxol)-6- (4-cyclopropylpiperazin-1-yl)-pyridazine, its salts and solvates and its use as histamine H3 receptor antagonist. WO2007137968; 2007
   Google Scholar
• Pfizer, Inc. Tosylate salt of trans-N-isobutyl-3-fluoro-3- [3-fluoro-4-(pyrrolidin-1-yl-methyl)-phenyl]cyclobutanecarboxamide. WO2009071988; 2009
   Google Scholar
• Pfizer, Inc. Tetrahydronaphthyridine derivative. WO2007052124; 2007
   Google Scholar
• Schering Corp. 1-[[1-[(2-Amino-6-methyl-4-pyridinyl)methyl]-4-fluoro-4-piperidinyl]carbonyl]-4-[2-(2-pyridinyl)-3H-imidazo[4,5-b]pyridin-3-yl]piperidine useful as histamine H3 antagonist. WO2007035703; 2007
   Google Scholar
• Barbier AJ, Aluisio L, Lord B, Pharmacological characterization of JNJ-28583867, a histamine H3 receptor antagonist and serotonin reuptake inhibitor. Eur J Pharmacol 2007;576:43-54
   PubMed Web of Science ®Google Scholar
• Stocking EM, Letavic MA, Bonaventure P, Carruthers NI. Exploration of structure–activity relationship for dual serotonin transporter reuptake inhibitors-histamine H3 receptor antagonists. Curr Top Med Chem 2010;10:596-616
   Google Scholar
• Bembenek SD, Keith JM, Letavic MA, Lead identification of acetylcholinesterase inhibitors-histamine H3 receptor antagonists from molecular modeling. Bioorg Med Chem 2008;16:2968-73
   Google Scholar
• Medhurst SJ, Collins SD, Billinton A, Novel histamine H3 receptor antagonists GSK189254 and GSK334429 are efficacious in surgically-induced and virally-induced rat models of neuropathic pain. Pain 2008;138:61-9
   PubMed Web of Science ®Google Scholar