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Novel histamine H4 receptor ligands and their potential therapeutic applications: an update

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Bibliography

  • Kollmeier A, Francke K, Chen B, et al. The Histamine H4 receptor antagonist, JNJ 39758979, is effective in reducing histamine-induced pruritus in a randomized clinical study in healthy subjects. J Pharmacol Exp Ther 2014;350:181-7
  • Thurmond RL, Chen B, Dunford PJ, et al. Clinical and preclinical characterization of the histamine H(4) receptor antagonist JNJ-39758979. J Pharmacol Exp Ther 2014;349:176-84
  • Kiss R, Keserű GM. Histamine H4 receptor ligands and their potential therapeutic applications: an update. Expert Opin Ther Pat 2012;22:205-21
  • Clinical trial: a Study of JNJ-38518168 in symptomatic adult participants with uncontrolled, persistent asthma. 2014. Available from: http://clinicaltrials.gov/show/NCT01823016 [Last accessed 20 July 2014]
  • Clinical trial: a dose range finding study of JNJ-38518168 in patients with active rheumatoid arthritis in spite of treatment with methotrexate. 2014. Available from: http://clinicaltrials.gov/show/NCT01679951 [Last accessed 20 July 2014]
  • ZIARCO, histamine H4 receptor antagonist programme. 2014. Available from: http://ziarcopharma.com/h4.html [Last accessed 20 July 2014]
  • Kalypsys. 2014. Available from: http://www.kalypsys.com/home/home01.shtml [Last accessed 20 July 2014]
  • Draconis Pharma. 2014. Available from: http://draconispharma.com/index.php/en/history [Last accessed 20 July 2014]
  • Jemima EA, Prema A, Thangam EB. Functional characterization of histamine H4 receptor on human mast cells. Mol Immunol 2014;62:19-28
  • Neumann D, Seifert R. The therapeutic potential of histamine receptor ligands in inflammatory bowel disease. Biochem Pharmacol 2014;91(1):12-17
  • Mahapatra S, Albrecht M, Behrens B, et al. Delineating the role of histamine-1- and -4-receptors in a mouse model of Th2-dependent antigen-specific skin inflammation. PLoS One 2014;9:e87296
  • Czerner CP, Klos A, Seifert R, et al. Histamine induces chemotaxis and phagocytosis in murine bone marrow-derived macrophages and RAW 264.7 macrophage-like cells via histamine H4-receptor. Inflamm Res 2014;63:239-47
  • Cowden JM, Yu F, Banie H, et al. The histamine H4 receptor mediates inflammation and Th17 responses in preclinical models of arthritis. Ann Rheum Dis 2014;73:600-8
  • Cowden JM, Yu F, Challapalli M, et al. Antagonism of the histamine H4 receptor reduces LPS-induced TNF production in vivo. Inflamm Res 2013;62:599-607
  • Somma T, Cinci L, Formicola G, et al. A selective antagonist of histamine H4 receptors prevents antigen-induced airway inflammation and bronchoconstriction in guinea pigs: involvement of lipocortin-1. Br J Pharmacol 2013;170:200-13
  • Neumann D, Beermann S, Burhenne H, et al. The dual H3/4R antagonist thioperamide does not fully mimic the effects of the ’standard’ H4R antagonist JNJ 7777120 in experimental murine asthma. Naunyn Schmiedebergs Arch Pharmacol 2013;386:983-90
  • Ballerini C, Aldinucci A, Luccarini I, et al. Antagonism of histamine H4 receptors exacerbates clinical and pathological signs of experimental autoimmune encephalomyelitis. Br J Pharmacol 2013;170:67-77
  • Glatzer F, Gschwandtner M, Ehling S, et al. Histamine induces proliferation in keratinocytes from patients with atopic dermatitis through the histamine 4 receptor. J Allergy Clin Immunol 2013;132:1358-67
  • Suwa E, Yamaura K, Sato S, et al. Increased expression of the histamine H4 receptor following differentiation and mediation of the H4 receptor on interleukin-8 mRNA expression in HaCaT keratinocytes. Exp Dermatol 2014;23:138-40
  • Yu B, Shao Y, Zhang J, et al. Polymorphisms in human histamine receptor H4 gene are associated with atopic dermatitis. Br J Dermatol 2010;162:1038-43
  • Mommert S, Scherer R, Glatzer F, et al. Genetic variants in the promoter region of the human histamine H4 receptor gene are associated with psoriasis. J Invest Dermatol 2013;133:S134
  • Janssen. Use of a histamine H4 antagonist for the treatment of post-operative adhesions. US20130202685A1; 2013
  • Matsushita A, Seike M, Okawa H, et al. Advantages of histamine H4 receptor antagonist usage with H1 receptor antagonist for the treatment of murine allergic contact dermatitis. Exp Dermatol 2012;21:714-15
  • Ohsawa Y, Hirasawa N. The antagonism of histamine H1 and H4 receptors ameliorates chronic allergic dermatitis via anti-pruritic and anti-inflammatory effects in NC/Nga mice. Allergy 2012;67:1014-22
  • Deiteren A, De Man JG, Ruyssers NE, et al. Histamine H4 and H1 receptors contribute to postinflammatory visceral hypersensitivity. Gut 2014. [Epub ahead of print]
  • UCL Business Plc. Histamine 4 receptor partial agonists, inverse agonists or antagonists for use in treating non-autoimmune uveitis. WO20140033480; 2014
  • Terrasse G. Use of an h4 agonist molecule for treating cystic fibrosis. WO20130175116A1; 2013
  • Kaneko H, Ye F, Ijima R, et al. Histamine receptor h4 as a new therapeutic target for choroidal neovascularization in age-related macular degeneration. Br J Pharmacol 2014;171(15):3754-63
  • Aldi S, Takano K, Tomita K, et al. Histamine H4-receptors inhibit mast cell renin release in ischemia/reperfusion via protein kinase C ε-dependent aldehyde dehydrogenase type-2 activation. J Pharmacol Exp Ther 2014;349:508-17
  • Cai WK, Hu J, Li T, et al. Activation of histamine H4 receptors decreases epithelial-to-mesenchymal transition progress by inhibiting transforming growth factor-beta1 signalling pathway in non-small cell lung cancer. Eur J Cancer 2014;50:1195-206
  • Zhang C, Xiong Y, Li J, et al. Deletion and down-regulation of HRH4 gene in gastric carcinomas: a potential correlation with tumor progression. PLoS One 2012;7:e31207
  • Wersinger E, Gaboyard-Niay S, Travo C, et al. Symptomatic treatment of vestibular deficits: therapeutic potential of histamine H4 receptors. J Vestib Res 2013;23:153-9
  • Desmadryl G, Gaboyard-Niay S, Brugeaud A, et al. Histamine H4 receptor antagonists as potent modulators of mammalian vestibular primary neuron excitability. Br J Pharmacol 2012;167:905-16
  • Martinel Lamas DJ, Carabajal E, Prestifilippo JP, et al. Protection of radiation-induced damage to the hematopoietic system, small intestine and salivary glands in rats by JNJ7777120 compound, a histamine H4 ligand. PLoS One 2013;8:e69106
  • Galeotti N, Sanna MD, Ghelardini C. Pleiotropic effect of histamine H4 receptor modulation in the central nervous system. Neuropharmacology 2013;71:141-7
  • Adami M, Pozzoli C, Menozzi A, et al. Effects of histamine H4 receptor ligands in a mouse model of gastric ulceration. Pharmacology 2012;89:287-94
  • Sensorion. H4 receptor inhibitors for treating tinnitus. WO20130182711; 2013
  • PATENTSCOPE database of World Intellectual Property Organization. 2014. Available from: http://www.wipo.int/patentscope/search/en/structuredSearch.jsf [Last accessed 6 June 2014]
  • Geyer R, Kaske M, Baumeister P, et al. Synthesis and functional characterization of imbutamine analogues as histamine H3 and H4 receptor ligands. Arch Pharm (Weinheim) 2014;347:77-88
  • Janssen Pharmaceutica NV. Benzoimidazol-2-yl pyrimidines and pyrazines as modulators of the histamine H4 receptor. US20140038995; 2014
  • Janssen Pharmaceutica NV. Benzoimidazol-2-yl pyrimidines and pyrazines as modulators of the histamine H4 receptor. US20130072510; 2013
  • Bioprojet. Benzazole derivatives as histamine H4 receptor ligands. WO20120041860; 2012
  • Bioprojet. Benzazole derivatives as histamine H4 receptor ligands. EP2447263; 2012
  • Bioprojet. Benzazole derivatives as histamine H4 receptor ligands. CA2812686; 2012
  • Bioprojet. Benzazole derivatives as histamine H4 receptor ligands. US20130231329; 2013
  • Shionogi. Pharmaceutical composition containing fused hetero-ring derivative. US20120277238; 2012
  • Wagner E, Wittmann HJ, Elz S, et al. Pharmacological profile of astemizole-derived compounds at the histamine H1 and H4 receptor–H1/H4 receptor selectivity. Naunyn Schmiedebergs Arch Pharmacol 2014;387:235-50
  • Engelhardt H, de Esch IJ, Kuhn D, et al. Detailed structure-activity relationship of indolecarboxamides as H4 receptor ligands. Eur J Med Chem 2012;54:660-8
  • Lane CA, Hay D, Mowbray CE, et al. Synthesis of novel histamine H4 receptor antagonists. Bioorg Med Chem Lett 2012;22:1156-9
  • Incyte Corp. Substituted heterocyclic compounds. US20130296327; 2013
  • Incyte Corp. Substituted heterocyclic compounds. US20130244999; 2013
  • Janssen Pharmaceutica NV. 2-aminopyrimidine modulators of the histamine. H4 receptor. US20130158259; 2013
  • Janssen Pharmaceutica NV. 2-aminopyrimidine modulators of the histamine. H4 receptor. US20130158258; 2013
  • Janssen Pharmaceutica NV. 2-aminopyrimidine modulators of the histamine. H4 receptor. EP2599386; 2013
  • Janssen Pharmaceutica NV. Process for the preparation of substituted pyrimidine derivatives. US20140121374; 2014
  • Savall BM, Chavez F, Tays K, et al. Discovery and SAR of 6-alkyl-2,4-diaminopyrimidines as histamine H4 receptor antagonists. J Med Chem 2014;57:2429-39
  • Medicis Pharmaceutical Corp. Aminoalkylpyrimidine derivatives as histamine H4 receptor antagonists. US20130018031; 2013
  • Schreeb A, Walter M, Odadzic D, et al. Piperazine modification in 2,4,6-triaminopyrimidine derivatives as histamine H4 receptor ligands. Pharmazie 2013;68:521-5
  • Engelhardt H, Schultes S, de Graaf C, et al. Bispyrimidines as potent histamine H(4) receptor ligands: delineation of structure-activity relationships and detailed H(4) receptor binding mode. J Med Chem 2013;56:4264-76
  • Janssen Pharmaceutica NV. Thieno- and furo-pyrimidine modulators of the histamine H4 receptor. US20120270855; 2012
  • Janssen Pharmaceutica NV. Thieno- and furo-pyrimidine modulators of the histamine H4 receptor. US20120238544; 2012
  • Janssen Pharmaceutica NV. Thieno- and furo-pyrimidine modulators of the histamine H4 receptor. US20120208793; 2012
  • Andaloussi M, Lim HD, van der Meer T, et al. A novel series of histamine H4 receptor antagonists based on the pyrido[3,2-d]pyrimidine scaffold: comparison of hERG binding and target residence time with PF-3893787. Bioorg Med Chem Lett 2013;23:2663-70
  • Arena Pharmaceutical, Inc. Methods and compounds useful in treating pruritus, and methods for identifying such compounds. WO20130151982; 2013
  • Kalypsys, Inc. Heterocyclic inhibitors of histamine receptors for the treatment of disease. WO20110112766; 2011
  • Kalypsys, Inc. Heterocyclic inhibitors of histamine receptors for the treatment of disease. WO20130039785; 2013
  • Kalypsys, Inc. Heterocyclic inhibitors of histamine receptors for the treatment of disease. US20130245001; 2013
  • Bioprojet. New 6,11-dihydro-5H-benzo[d]imidazo[1,2-a]azepines derivatives as histamine H4 receptor ligands. US20130324506; 2013
  • Bioprojet. New 6,11-dihydro-5H-benzo[d]imidazo[1,2-a]azepines derivatives as histamine H4 receptor ligands. EP2671884; 2013
  • Terrasse G. Use of a new histamine H4 agonist for the treatment of acute leukemia. US20130303565; 2013
  • Loria E. Treatment of diseases modulated by a H4 receptor agonist. US20130059878; 2013
  • ChEMBL database. 2014. Available from: https://www.ebi.ac.uk/chembl/ [Last accessed 18 July 2014]
  • Mcule. 2014. Available from: https:\⊂\⊂mcule.com [Last accessed 18 July 2014]
  • Hopkins AL, Keserű GM, Leeson PD, et al. The role of ligand efficiency metrics in drug discovery. Nat Rev Drug Discov 2014;13:105-21
  • Tarcsay A, Nyíri K, Keserű GM. Impact of lipophilic efficiency on compound quality. J Med Chem 2012;55:1252-60
  • Wager TT, Chandrasekaran RY, Hou X, et al. Defining desirable central nervous system drug space through the alignment of molecular properties, in vitro ADME, and safety attributes. ACS Chem Neurosci 2010;1:420-34
  • Project information: UR-63325. 2014. Available from: http://www.histamineresearch.com/Reports/Palau_Pharma_H4.pdf [Last accessed 19 July 2014]
  • Hann MM, Leach AR, Harper G. Molecular complexity and its impact on the probability of finding leads for drug discovery. J Chem Inf Comput Sci 2001;41:856-64

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