Scaffold variations in amine warhead of histamine H3 receptor antagonists

Drug Discovery Today: Technologies

Volumn 10, Issue 4, 2013, Pages

  Wingen, Kerstin ^a   Stark, Holger ^a,b  

^a GOETHE UNIVERSITY   (Germany)

^b HEINRICH HEINE UNIVERSITY   (Germany)

Author keywords

[No Author keywords available]

Indexed keywords

5 (4 CYANOPHENYL) 2 [2 (2 METHYL 1 IMIDAZOLIDINYL)ETHYL]BENZOFURAN; 6 (3 CYCLOBUTYL 2,3,4,5 TETRAHYDRO 1H 3 BENZAZEPIN 7 YLOXY) N METHYLNICOTINAMIDE; A 331440; A 417022; AMINE; APLYSAMINE; BAVISANT; CIPROXIFAN; CLOBENPROPIT; CONESSINE; FUB 181; GSK 334429; HISTAMINE H3 RECEPTOR ANTAGONIST; HPP 404; IMIDAZOLE; IRDABISANT; JNJ 280566; JNJ 5207852; JNJ 7737782; MK 0249; NNC 0038 1202; PF 03654746; PIPERAZINE; PITOLISANT; S 36662 1; S 38761 1; THIADIAZOLE DERIVATIVE; THIOPERAMIDE; THIOUREA; UNCLASSIFIED DRUG; UNINDEXED DRUG;

ALLERGY; ALZHEIMER DISEASE; ARTICLE; ATTENTION DEFICIT DISORDER; BINDING AFFINITY; COGNITIVE DEFECT; DIABETES MELLITUS; DRUG BINDING; DRUG POTENCY; DRUG STRUCTURE; HUMAN; MOLECULE; NARCOLEPSY; NEUROPATHIC PAIN; NEUROTRANSMISSION; NONHUMAN; OBESITY; PHARMACOPHORE; PHASE 1 CLINICAL TRIAL (TOPIC); PHASE 2 CLINICAL TRIAL (TOPIC); PHASE 3 CLINICAL TRIAL (TOPIC); SCHIZOPHRENIA;

AMINES; ANIMALS; DRUG DESIGN; HISTAMINE H3 ANTAGONISTS;

EID: 84886294150     PISSN: None     EISSN: 17406749     Source Type: Journal    
DOI: 10.1016/j.ddtec.2013.07.001     Document Type: Review

References (32)

1. Available from: http://clinicaltrials.gov; Identifier: NCT00420420 (accessed 13.02.12)
2. Available from: http://clinicaltrials.gov; Identifier: NCT01540864 (accessed 13.02.12)
3. Available from: http://clinicaltrials.gov; Identifier: NCT00531752 (accessed 13.02.12)
4. Available from: http://clinicaltrials.gov; Identifier: NCT00366080 (accessed 13.02.12)
5. 3 receptor as a drug discovery target J. Med. Chem. 54 2011 26 53
6. T. Bonaventura Histamine H3 receptor antagonists: from target identification to drug leads Biochem. Pharmacol. 73 2007 1084 1096
7. S. Celanire Drug discovery: from hits to clinical candidates D. Vohora, The Third Histamine Receptor: Selective Ligands as Potential Therapeutic Agents in CNS Disorders 2009 CRC Press, Taylor & Francis CRC Press Inc. 103 165
8. 3 receptor antagonists in seasonal allergic rhinitis Int. Arch. Allergy Immunol. 158 2012 84 98
9. J. Diaz Cyclopropylmethanone derivatives, particularly (cyclopropyl)(phenyl)methanone drivatives, and their preparation and therapeutic use thereof 2005 patent WO2005037810 (04/28/2005)
10. T.A. Esbenshade Pharmacological and behavioral properties of A-349821, a selective and potent human histamine H3 receptor antagonist Biochem. Pharmacol. 68 2004 933 945
11. 3 receptor ligands. Part 2: Binding preference for d-amino acids motifs Bioorg. Med. Chem. Lett. 12 2002 2035 2037
12. 3 receptor antagonist, U.S. Patent 20120149728
13. R. Leurs En route to new blockbuster anti-histamines: surveying the offspring of the expanding histamine receptor family Trends Pharmacol. Sci. 32 2011 250 257
14. 3 receptor modulators, U.S. Patent 2012201625
15. 3 receptor model through structure-activity relationships for classical H3 antagonists Bioorg. Med. Chem. Lett. 13 2005 5647 5657
16. 3-receptor antagonists Eur. J. Pharm. Sci. 13 2001 249 259
17. H. Miko Novel nonimidazole histamine H3 receptor antagonists: 1-(4-(phenoxymethyl)benzyl)piperidines and related compounds J. Med. Chem. 46 2003 1523 1530
18. 3 receptor antagonist/inverse agonist with cognition-enhancing and wake-promoting activities J. Pharmacol. Exp. Ther. 340 2012 124 133
19. 3 receptor ligands Chem. Pharm. Bull. 58 2001 1353 1361
20. 3 receptor antagonists go to clinics Biol. Pharm. Bull. 31 2008 2163 2181
21. 3 receptor for ligand docking and pharmacophore-based screening J. Comput. Aided Mol. Des. 2007 437 453
22. Schwartz, J.-C. et al., 2006. Treatment of Parkinson's disease obstructive sleep apnea, dementia with Lewy bodies, vascular dementia with non-imidazole alkylamines histamine H3- receptor ligands, U.S. Patent EP1707203
23. H. Stark Recent advances in histamine H3/H4 receptor ligands Expert Opin. Ther. Patents 13 2003 851 865
24. H. Stark The histamine H3 receptor and its ligands F.D. King, A.W. Oxford, Prog. Med. Chem. 2001 Elsevier 279 308
25. H. Stark Medicinal chemical and pharmacological aspects of imidazole-containing histamine H3 receptor antagonists Mini-Rev. Med. Chem. 4 2004 965 977
26. J. Stephanos Drug-protein interactions: two-site binding of heterocyclic ligands to a monomeric hemoglobin J. Inorg. Biochem. 62 1996 155 169
27. Stranne, R. et al., 2011. Processes for making cyclopropyl amide derivatives and intermediates associated therewith, U.S. Patent WO 2011102794
28. 3 receptor antagonists Bioorg. Med. Chem. Lett. 16 2006 897 900
29. E. Tiligada Histamine H3and H4 receptors as novel drug targets Expert Opin. Ther. Patents 18 2009 851 865
30. E. Tiligada Histamine pharmacology and new CNS drug targets CNS Neurosci. Ther. 17 2011 620 628
31. M. Walter Histamine receptor subtypes: a century of rational drug design Front. Biosci. S4 2012 461 488
32. 3 receptor antagonists J. Med. Chem. 51 2008 5423 5430