414
Views
12
CrossRef citations to date
0
Altmetric
Reviews

β3-Adrenoceptor ligand development history through patent review

&
Pages 505-536 | Published online: 17 Mar 2011

Bibliography

  • Perrone MG, Scilimati A. beta3-Adrenoceptor agonists and (antagonists as) inverse agonists: history, perspective, constitutive activity, and stereospecific binding. Methods Enzymol 2010;484:197-230
  • Arch JRS, Kaufmann AJ. beta3 and atypical beta-adrenoceptors. Med Res Rev 1993;21:663-729
  • Moens AL, Yang R, Watts VL, Beta 3-adrenoreceptor regulation of nitric oxide in the cardiovascular system. J Mol Cell Cardiol 2010;48:1088-95
  • Boivin B, Lavoie C, Vaniotis G, Functional beta-adrenergic receptor signalling on nuclear membranes in adult rat and mouse ventricular cardiomyocytes. Cardiovasc Res 2006;71:69-78
  • Ghorbani M, Himms-Hagen J. Appearance of brown adipocytes in white adipose tissue during CL 316,243-induced reversal of obesity and diabetes in Zucker fa/fa rats. Int J Obes Relat Metab Disord 1997;21:465-75
  • Arch JRS. Perspectives from beta3-adrenoceptor agonists on pharmacology, physiology and obesity drug discovery. Naunyn Schmiedebergs Arch Pharmacol 2008;378:225-40
  • Barbe P, Millet L, Galitzky J, In situ assessment of the role of the beta1-, beta2- and beta3-adrenoceptors in the control of lipolysis and nutritive blood flow in human subcutaneous adipose tissue. Br J Pharmacol 1996;117:907-13
  • Rosenbaum M, Malbon CC, Hirsch J, Lack of beta3-adrenergic effect on lipolysis in human subcutaneous adipose tissue. J Clin Endocrinol Metab 1993;77:352-5
  • Ursino MG, Vasina V, Raschi E, The beta3-adrenoceptor as a therapeutic target: current perspectives. Pharmacol Res 2009;59:221-34
  • Geyer O, Bar-Ilan A, Nachman R, Beta 3-adrenergic relaxation of bovine iris sphincter. FEBS Lett 1998;429:356-8
  • Steinle JJ, Booz GW, Meininger CJ, Beta 3-adrenergic receptors regulate retinal endothelial cell migration and proliferation. J Biol Chem 2003;278:20681-6
  • Tagaya E, Tamaoki J, Takemura H, Atypical adrenoceptor-mediated relaxation of canine pulmonary artery through a cyclic adenosine monophosphate-dependent pathway. Lung 1999;177:321-32
  • Berlan M, Galitzky J, Bousquet-Melou A, Beta-3 adrenoceptor-mediated increase in cutaneous blood flow in the dog. JPET 1994;268:1444-51
  • Hom GJ, Forrest MJ, Bach TJ, Beta(3)-adrenoceptor agonist-induced increases in lipolysis, metabolic rate, facial flushing, and reflex tachycardia in anesthetized rhesus monkeys. JPET 2001;297:299-307
  • Trochu JN, Leblais V, Rautureau Y, Beta 3-adrenoceptor stimulation induces vasorelaxation mediated essentially by endothelium-derived nitric oxide in rat thoracic aorta. Br J Pharmacol 1999;128:69-76
  • Rautureau Y, Toumaniantz G, Serpillon S, Beta 3-adrenoceptor in rat aorta: molecular and biochemical characterization and signalling pathway. Br J Pharmacol 2002;137:153-61
  • Berlan M, Galitzky J, Montastruc JL. Beta3-adrenoceptors in the cardiovascular system. Fundam Clin Pharmacol 1995;9:234-9
  • Rozec B, Serpillon S, Toumaniantz G, Characterization of beta 3-adrenoceptors in human internal mammary artery and putative involvement in coronary artery bypass management. J Am Coll Cardiol 2005;46:351-9
  • Dessy C, Moniotte S, Ghisdal P, Endothelial beta 3-adrenoceptors mediate vasorelaxation of human coronary microarteries through nitric oxide and endothelium-dependent hyperpolarization. Circulation 2004;110:948-54
  • Summers RJ, Papaioannou M, Harris S, Expression of beta 3-adrenoceptor mRNA in rat brain. Br J Pharmacol 1995;116:2547-8
  • Castillo-Melendez M, McKinley MJ, Summers RJ. Intracerebroventricular administration of the beta(3)-adrenoceptor agonist CL 316243 causes Fos immunoreactivity in discrete regions of rat hypothalamus. Neurosci Lett 2000;290:161-4
  • Lenard NR, Gettys TW, Dunn AJ. Activation of beta2- and beta 3-adrenergic receptors increases brain tryptophan. JPET 2003;305:653-9
  • Howe R. beta3-adrenergic agonists. Drugs Future 1993;18:529-49
  • Simiand J, Keane PE, Guitard J, Antidepressant profile in rodents of SR 58611A, a new selective agonist for atypical beta-adrenoceptors. Eur J Pharmacol 1992;219:193-20
  • Glenmark Pharmaceuticals Ltd. Novel benzopyran compounds and process for their preparation and use. WO2003014113; 2003
  • Berkowitz DE, Nardone NA, Smiley RM, Distribution of beta3-adrenoceptor mRNA in human tissues. Eur J Pharmacol Mol Pharmacol 1995;289:223-8
  • Pang Z, Wu N, Zhang X, GPR40 is partially required for insulin secretion following activation of beta3-adrenergic receptors. Mol Cell Endocrinol 2010;325:18-25
  • Strosberg AD. The beta3-adrenoreceptor.Volume 5. Taylor & Francis, New York; 2000. p. 84-5
  • Houghten Pharmaceuticals. Use of a substituted 1,3-benzodioxole to reduce a wasting condition. US5597843; 1997
  • Kim YS, Sainz RD. Beta-adrenergic agonists and hypertrophy of skeletal muscles. Life Sci 1992;50:397-407
  • Tisdale MJ. Pathogenesis of cancer cachexia. J Support Oncol 2003;1:159-68
  • Candelore MR, Deng L, Tota L, Potent and selective human beta3-adrenergic receptor antagonists. JPET 1999;290:649-55
  • Perrone MG, Santandrea E, Bleve L, Stereospecific synthesis and bio-activity of novel beta3-adrenoceptor agonists and inverse agonists. Bioorg Med Chem 2008;16:2473-88
  • Univ. Degli Studi Di Bari. Beta-3 receptor ligands and their use in therapy. WO2008015558; 2008
  • Fedorov VV, Lozinsky IT. Is the beta 3-adrenergic receptor a new target for treatment of post-infarct ventricular tachyarrhythmias and prevention of sudden cardiac death? Heart Rhythm 2008;5:298-9
  • Rozec B, Gauthier C. Beta 3-adrenoceptors in the cardiovascular system: putative roles in human pathologies. Pharmacol Ther 2006;111:652-73
  • Bungaard H, Liu C-C, Garcia A, beta3 adrenergic stimulation of the cardiac Na+-K+ pump by reversal of an inhibitory oxidative modification. Circulation 2010;122:2699-708
  • Rasmussen HH, Figtree GA, Krum H, Use of beta3-adrenergic receptor agonists in the treatment of heart failure. Curr Opin Investig Drugs 2009;10:955-62
  • Gan RT, Li WM, Xiu CH, Chronic blocking of beta3-adrenoceptor ameliorates cardiac function in rat model of heart failure. Chin Med J (Eng) 2007;120:2250-5
  • Pott C, Brixius K, Bloch W, Beta3-adrenergic stimulation in the human heart: signal transduction, functional implications and therapeutic perspectives. Pharmazie 2006;61:255-60
  • Fujimura T, Tamura T, Tsutsumi T, Expression and possible functional role of the beta3-adrenoceptor in human and rat detrusor muscle. J Urol 1999;161:680-5
  • Kissei Pharmaceutical. 2-Methylpropionic acid derivatives and medicinal compositions containing the same. EP1072583; 2001
  • Otsuka A, Shinbo H, Matsumoto R, Expression and functional role of beta-adrenoceptors in the human urinary bladder. Naunyn Schmiedebergs Arch Pharmacol 2008;377:473-81
  • Takasu T, Ukai M, Sato S, Effect of (R)-2-(2-aminothiazol-4-yl)-4'-{2-[(2-hydroxy-2-phenylethyl)amino]ethyl} acetanilide (YM178), a novel selective beta3-adrenoceptor agonist, on bladder function. JPET 2007;321:642-7
  • Yamaguchi O, Chapple CR. beta3-Adrenoceptors in urinary bladder. Neurourol Urodyn 2007;26:752-6
  • Marcus JD. Emerging drugs for treatment of overactive bladder and detrusor overactivity. Expert Opin Emerg Drugs 2008;13:431-46
  • Michel MC, Ochodnicky P, Summers RJ. Tissue functions mediated by beta3-adrenoceptors – findings and challenges. Naunyn Schmiedebergs Arch Pharmacol 2010;382:103-8
  • Bianchetti A, Manara L. In vitro inhibition of intestinal motility by phenylethanolaminotetralines: evidence of atypical beta-adrenoceptors in rat colon. Br J Pharmacol 1990;100:831-9
  • De Ponti F, Gibelli G, Croci T, Functional evidence of atypical beta3-adrenoceptors in the human colon using the beta 3-selective adrenoceptor antagonist, SR 59230A. Br J Pharmacol 1996;117:1374-6
  • De Ponti F, Cosentino M, Costa A, Inhibitory effects of SR 58611A on canine colonic motility: evidence for a role of beta3-adrenoceptors. Br J Pharmacol 1995;114:1447-53
  • Bharucha AE, Camilleri M, Zinsmeister AR, Adrenergic modulation of human colonic motor and sensory function. Am J Physiol 1997;273:997-1006
  • Cellek S, Thangiah R, Bassil AK, Demonstration of functional neuronal beta(3)-adrenoceptors within the enteric nervous system. Gastroenterology 2007;133:175-83
  • Kuratani K, Kodama H, Yamaguchi I. Enhancement of gastric mucosal blood flow by beta-3 adrenergic agonists prevents indomethacin-induced antral ulcer in the rat. JPET 1994;270:559-65
  • Sevak R, Paul A, Goswami S, Gastroprotective effect of beta3 adrenoreceptor agonists ZD 7114 and CGP 12177A in rats. Pharmacol Res 2002;46:351-6
  • Vasina V, Abu-gharbieh E, Barbara G, The beta3-adrenoceptor agonist SR58611A ameliorates experimental colitis in rats. Neurogastroenterol Motil 2008;20:1030-41
  • Schemann M, Hafsi N, Michel K, The beta3-adrenoceptor agonist GW427353 (solabegron) decreases excitability of human enteric neurons via release of somatostatin. Gastroenterology 2010;138:266-74
  • Yasuhiko I, Naoki A, Yukio H. Beta3-adrenoceptor agonists: possible role in the treatment of overactive bladder. Korean J Urol 2010;51:811-18
  • Palm D, Lang K, Niggemann B, The norepinephrine-driven metastasis development of PC-3 human prostate cancer cells in BALB/c nude mice is inhibited by beta-blockers. Int J Cancer 2006;118:2744-9
  • Perrone MG, Notarnicola M, Caruso MG, Upregulation of beta3-adrenergic receptor mRNA in human colon cancer: a preliminary study. Oncology 2008;75:224-9
  • Bardou M, Rouget C, Breuiller-Fouche M, Is the beta3-adrenoceptor (ADRB3) a potential target for uterorelaxant drugs? BMC Pregnancy Childbirth 2007;7:S14
  • Dennedy MC, Friel AM, Gardeil F, Beta-3 versus beta-2 adrenergic agonists and preterm labour: in vitro uterine relaxation effects. Br J Obstet Gynaecol 2001;108:605-9
  • Rouget C, Bardou M, Breuiller-Fouche M, beta3-Adrenoceptor is the predominant beta-adrenoceptor subtype in human myometrium and its expression is up-regulated in pregnancy. J Clin Endocrinol Metab 2005;90:1644-50
  • Sanofi-Aventis. Novel therapeutic uses of beta-3 adrenergic receptor agonist derivatives in particular to modulate apoptosis. WO2009019607; 2009
  • Zhang Q, Paria BC. Importance of uterine cell death, renewal, and their hormonal regulation in hamsters that show progesterone-dependent implantation. Endocrinology 2006;147:2215-27
  • Smith SC, Baker PN. Increased placental apoptosis in intrauterine growth restriction. Am J Obstet Gynecol 1997;177:1395-401
  • Allaire AD, Ballenger KA, Wells SR, Placental apoptosis in preeclampsia. Obstet Gynecol 2000;96:271-6
  • Erel CT, Dane B, Calay Z, Apoptosis in the placenta of pregnancies complicated with IUGR. Int J Gynaecol Obstet 2001;73:229-35
  • lshihara N, Matsuo H, Murakoshi H, Increased apoptosis in the syncytiotrophoblast in human term placentas complicated by either preeclampsia or intrauterine growth retardation. Am J Obstet Gynecol 2002;186:158-66
  • Madazli R, Benian A, Ilvan S, Placental apoptosis and adhesion molecules expression in the placenta and the maternal placental bed of pregnancies complicated by fetal growth restriction with and without pre-eclampsia. J Obstet Gynaecol 2006;26:5-10
  • Callaghan WM, MacDorman MF, Rasmussen SA, The contribution of preterm birth to infant mortality rates in the United States. Pediatrics 2006;118:1566-73
  • Edwards RK. Chorioamnionitis and labor. Obstet Gynecol Clin North Am 2005;32:287-96
  • Charpigny G, Leroy M-J, Breuiller-Fouche M, A functional genomic study to identify differential gene expression in the preterm and term human myometrium. Biol Reprod 2003;68:2289-96
  • Danial NN, Korsmeyer SJ. Cell death: critical control point. Cell 2004;116:205-19
  • Sanofi Synthelabo. Cyclohexyl(alkyl)-propanolamines, preparation method and pharmaceutical compositions containing same. WO2002044139; 2002
  • Lirussi F, Rakotoniaina Z, Madani S, ADRB3 adrenergic receptor is a key regulator of human myometrial apoptosis and inflammation during chorioamnionitis. Biol Reprod 2008;78:497-05
  • Trebicka J, Hennenberg M, Probsting AS, Role of beta3-adrenoceptors for intrahepatic resistance and portal hypertension in liver cirrhosis. Hepatology 2009;50:1924-35
  • Stemmelin J, Cohen C, Terranova JP, Stimulation of the beta3-adrenoceptor as a novel treatment strategy for anxiety and depressive disorders. Neuropsychopharmacology 2008;33:574-87
  • Overstreet DH, Stemmelin J, Griebel G. Confirmation of antidepressant potential of the selective beta 3 adrenoceptor agonist amibegron in an animal model of depression. Pharmacol Biochem Behav 2008;89:623-6
  • Stemmelin J, Cohen C, Yalcin I, Implication of beta3-adrenoceptors in the antidepressant-like effects of amibegron using Adrb3 knockout mice in the chronic mild stress. Behav Brain Res 2010;206:310-12
  • Available from: www.clinicaltrials.gov
  • Strosberg AD. The beta3-adrenoreceptor. Taylor & Francis, London; 2000. p. 11
  • de Souza CJ, Burkey BF. Beta(3)-adrenoceptor agonists as anti-diabetic and anti-obesity drugs in humans. Curr Pharm Des 2001;7:1433-49
  • Perrone MG, Bleve L, Santandrea E, The tertiary amine nitrogen atom of piperazine sulfonamides as a novel determinant of potent and selective beta3-adrenoceptor agonists. Chem Med Chem 2009;4:2080-97
  • Brockunier LL, Candelore MR, Cascieri MA, Human beta3 adrenergic receptor agonists containing cyanoguanidine and nitroethylenediamine moieties. Bioorg Med Chem Lett 2001;11:379-82
  • Dow RL, Paight ES, Schneider SR, Potent and selective, sulfamide-based human beta3-adrenergic receptor agonists. Bioorg Med Chem Lett 2004;14:3235-40
  • Kashaw SK, Rathi L, Mishra P, Development of 3D-QSAR models in cyclic ureidobenzenesulfonamides: human beta3-adrenergic receptor agonist. Bioorg Med Chem Lett 2003;13:2481-4
  • Mizuno K, Sawa M, Harada H, Discovery of 1, 7-cyclized indoles as a new class of potent and highly selective human beta3-adrenergic receptor agonists with high cell permeability. Bioorg Med Chem 2005;13:855-68
  • Mizuno K, Sawa M, Harada H, Tryptamine-based human beta3-adrenergic receptor agonists. Part 1: SAR studies of the 7-position of the indole ring. Bioorg Med Chem Lett 2004;14:5959-62
  • Nakajima Y, Hamashima H, Washizuka K, Discovery of a novel, potent and selective human beta3-adrenergic receptor agonist. Bioorg Med Chem Lett 2005;15:251-4
  • Tanaka N, Tamai T, Mukaiyama H, Relationship between stereochemistry and the beta3-adrenoceptor agonistic activity of 4-hydroxynorephedrine derivative as an agent for treatment of frequent urination and urinary incontinence. J Med Chem 2003;46:105-12
  • Steffan R, Ashwell MA, Solvibile WR, Novel substituted 4-aminomethylpiperidines as potent and selective human beta3-agonists. Part 1: aryloxypropanolaminomethylpiperidines. Bioorg Med Chem Lett 2002;12:2957-61
  • Popp BD, Hutchinson DS, Evans BA, Stereoselectivity for interactions of agonists and antagonists at mouse, rat and human beta3-adrenoceptors. Eur J Pharm 2004;484:323-31
  • Peleg G, Ghanouni P, Kobilka BK, Singlemolecule spectroscopy of the beta(2) adrenergic receptor: observation of conformational substates in a membrane protein. Proc Natl Acad Sci USA 2001;98:8469-74
  • Salamon Z, Hruby VJ, Tollin G, Binding of agonists, antagonists, and inverse agonists to the human delta-opioid receptor produces distinctly different conformational states distinguishable by plasmon-waveguide resonance spectroscopy. J Pept Res 2002;60:322-8
  • Beecham Group PLC. Ethanamine derivatives, their preparation and use in pharmaceutical compositions. EP23385; 1981
  • Baker JG. The selectivity of beta-adrenoceptor agonists at human beta1-, beta2- and beta3-adrenoceptors. Br J Pharmacol 2010;160:1048-61
  • Mori A, Miwa T, Sakamoto K, Pharmacological evidence for the presence of functional beta 3-adrenoceptors in rat retinal blood vessels. Naunyn Schmiedebergs Arch Pharmacol 2010;382:119-26
  • American Cyanamid Co. Substituted 5-(2-((2-aryl-2-hydroxyethyl)amino)propyl)-1,3-benzodioxoles. US5061727; 1991
  • Microbial Chem Res F and Banyu Pharma Co. Ltd. N-Methylphenylserine alkyl ester derivatives and uses thereof. EP218440; 1987
  • Bristol-Myers Squibb Co. Thiazole and oxazole-based beta 3-adrenergic receptor agonists. US5321036; 1994
  • Merck & Co., IncSubstituted phenyl sulfonamides as selective beta3-agonists for the treatment of diabetes and obesityEP611003; 1994
  • Yamamoto H, Takakura S, Yamamoto T, FR149175, a beta3-adrenoceptor-selective agonist, is a possible therapeutic agent for non-insulin-dependent diabetes mellitus. Jpn J Pharmacol 1997;74:109-12
  • Harada H, Hirokawa Y, Suzuki K, Novel and potent human and rat beta3-adrenergic receptor agonists containing substituted 3-indolylalkylamines. Bioorg Med Chem Lett 2003;13:1301-5
  • Weyer C, deSouza CJ. Development of beta3-adrenoceptor agonists as antiobesity and antidiabetes drugs in humans: current status and future prospects. Drug Dev Res 2000;51:80-93
  • Strosberg AD. The beta3-adrenoreceptor. Taylor & Francis, London; 2000. p. 58
  • Strosberg AD. The beta3-adrenoreceptor. Taylor & Francis, London; 2000. p. 66
  • Strosberg AD. The beta3-adrenoreceptor. Taylor & Francis, London; 2000. p. 65
  • Hatakeyama Y, Sakata Y, Takakura S, Acute and chronic effects of FR-149175, a beta3-adrenergic receptor agonist, on energy expenditure in Zucker fatty rats. Am J Physiol Regul Integr Comp Physiol 2004;287:R336-41
  • Morita T, Iizuka H, Iwata T, Function and distribution of beta3-adrenoceptors in rat, rabbit and human urinary bladder and external urethral sphincter. Smooth Muscle Res 2000;36:21-32
  • Yanagisawa T, Sato T, Yamada H, Selectivity and potency of agonists for the three subtypes of cloned human beta-adrenoceptors expressed in Chinese hamster ovary cells. Tohoku J Exp Med 2000;192:181-93
  • Hieble JP. Recent advances in identification and characterization of beta-adrenoceptor agonists and antagonists. Curr Top Med Chem 2007;7:207-16
  • Strosberg AD. The beta3-adrenoreceptor. Taylor & Francis, London; 2000. p. 59
  • Mathvink RJ, Tolman JS, Chitty D, Potent, selective 3-pyridylethanolamine beta3-adrenergic receptor agonists possessing a thiazole benzenesulfonamide pharmacophore. Bioorg Med Chem Lett 2000;10:1971-3
  • Ok HO, Reigle LB, Candelore MR, Substituted oxazole benzenesulfonamides as potent human beta3-adrenergic receptor agonists. Bioorg Med Chem Lett 2000;10:1531-4
  • Hu B, Ellingboe J, Han S, (4-Piperidin-1-yl)phenyl amides: potent and selective human beta3-agonists. J Med Chem 2001;44:1456-66
  • Hu B, Ellingboe J, Gunawan I, 2,4-Thiazolidinediones as potent and selective human beta3-agonists. Bioorg Med Chem Lett 2001;11:757-60
  • Ashwell MA, Solvibile WR, Han S, 4-Aminopiperidine ureas as potent selective agonists of the human beta3-adrenergic receptor. Bioorg Med Chem Lett 2001;11:3123-7
  • Sawa M, Harada H. Recent developments in the design of orally bioavailable beta3-adrenergic receptor agonists. Curr Med Chem 2006;13:25-37
  • Harada H, Hirokawa Y, Suzuki K, Discovery of a novel and potent human and rat beta 3-adrenergic receptor agonist, [3-[(2R)-[[(2R)-(3-chlorophenyl)-2-hydroxyethyl]amino]propyl]-1H-indol-7-yloxy]acetic acid. Chem Parm Bull 2005;53:184-98
  • Arch JRS, Kaumannl AJ, Molenaarl P, Studies on a novel selective beta3-adrenoceptor agonist in human right atrial appendage and human white adipocytes. Br J Pharmacol 1999;126:100P
  • Merck & Co., Inc. Hydroxymethyl pyrrolidines as beta 3-adrenergic receptor agonists. WO2009124167; 2009
  • Strosberg AD. The beta3-adrenoreceptor. Taylor & Francis, London; 2000. p. 66
  • Hicks A, McCafferty GP, Riedel E, GW427353 (Solabegron), a novel, selective beta3-adrenergic receptor agonist, evokes bladder relaxation and increases micturition reflex threshold in the dog. JPET 2007;323:202-9
  • King FD. Progress in medicinal chemistry. Volume 41. Oxford AW; 2003. p. 188
  • van Baak MA, Hul GBJ, Toubro S, Acute effect of L-796568, a novel beta3-adrenergic receptor agonist, on energy expenditure in obese men. Clin Pharmacol Ther 2002;71:272-9
  • Kissei Pharmaceutical. Phenoxyacetic acid derivatives and medicinal compositions containing the same. WO2000002846; 2000
  • Kissei Pharmaceutical. Medicine for prevention or treatment of frequent urination or urinary incontinence. WO2005089742; 2005
  • Candelore MR, Deng L, Tota L, Potent and selective human beta(3)-adrenergic receptor antagonists. JPET 1999;290:649-55

  • American Home Prod. Transcriptional regulation of the human beta 3-adrenergic receptor gene. WO20000044901; 2000
  • American Home Prod. Phenyl-oxo-tetrahydroquinolin-3-yl beta-3 adrenergic receptor agonists. US2002068751; 2002
  • American Home Prod. 2-Substituted thiazolidinones as beta-3 adrenergic receptor agonists. WO2002006281; 2002
  • American Home Prod. N-(4-sulfonylaryl)cyclylamine-2-hydroxyethylamines as beta-3 adrenergic receptor agonists. WO2002006274; 2002
  • American Home Prod. Azolidines as beta-3 adrenergic receptor agonists. WO2002006258; 2002
  • American Home Prod. Substituted 2-(S)-hydroxy-3-(piperidin-4-yl-methylamino)-propyl ethers and substituted 2-aryl-2-(R)-hydroxy-1-(piperidin-4-yl-methyl)-ethylamine beta-3 adrenergic receptor agonists. WO2002006255; 2002
  • American Home Prod. Substituted arylsulfides, arylsulfoxides and arylsulfones as beta-3 adrenergic receptor agonists. WO2002006250; 2002
  • American Home Prod. Heterocyclic beta-3 adrenergic receptor agonists. WO2002006235; 2002
  • American Home Prod. Cyclic amine phenyl beta-3 adrenergic receptor agonists. WO2002006232; 2002
  • American Cyanamid Co. Treatment of glaucoma and ocular hypertension with beta 3-adrenergic agonists. US5578638; 2002
  • American Cyanamid Co. Beta 3-adrenergic agents and their use in pharmaceutical compositions. US5482971; 1996
  • American Cyanamid Co. Beta 3-adrenergic agents benzodioxole dicarboxylates and their use in pharmaceutical compositions. US5480908; 1996
  • American Cyanamid Co. Aminocycloalkanobenzodioxoles as beta-3 selective adrenergic agents. EP608568; 1996
  • Asahi Kasei Pharma Corp. Indazole compound. WO2010041568; 2010
  • Asahi Kasei Pharma Corp. Indazole compound. WO2010041569; 2010
  • Astellas Pharma, Inc. Aminoalcohol derivatives. WO20051109; 2005
  • Astellas Pharma, Inc. Aminoalcohol derivatives. AU2006202092; 2006
  • Bayer AG. 2,6-Substituted chroman derivatives useful as beta-3 adrenoreceptor agonists. WO2002085891; 2002
  • Bayer AG. Di-substituted aminomethyl chroman derivative beta-3 adrenoreceptor agonists. WO2002048134; 2002
  • Beth Israel Hospital. Transgenic animals deficient in endogenous beta 3-adrenergic receptor and uses thereof. WO9742309; 1997
  • Boehringer Ingelheim Int. Beta-3-agonist use for treating kidney and bladder troubles of a patient with spinal cord damages. WO2007036543; 2007
  • Bristol-Myers Squibb Co. Thiazole and oxazole-based beta 3 adrenergic receptor agonists. US5321036; 1994
  • Bristol-Myers Squibb Co. Catecholamine surrogates useful as beta 3 agonists. EP659737; 1995
  • Bristol-Myers Squibb Co. Sulfonic, phosphonic or phosphinic acid beta 3 agonist derivatives. US5491134; 1996
  • Bristol-Myers Squibb Co. Benzo 1,3-dioxole derivatives. US5488064; 1996
  • Bristol-Myers Squibb Co. Aryloxypropanolamine beta 3 adrenergic agonists. EP714883; 1996
  • Bristol-Myers Squibb Co. Catecholamine surrogates useful as beta 3 agonists. WO9737646; 1997
  • Bristol-Myers Squibb Co. Catecholamine surrogates useful as beta 3 agonists. US5770615 (1998)
  • Bristol-Myers Squibb Co. Aminoethylphenoxyacetic acid derivatives and drugs for pain remission and calculi removal promotion in urinary lithiasis. WO9905090; 2010
  • Bristol-Myers Squibb Co. 2-Hydroxy-3-(4-hydroxy-3-sulfonamidophenyl)-propylamines useful as beta 3 adrenergic agonists. US2002026065; 2002
  • Centre Nat Rech Scient. Method for producing adipocytes from non-differentiated fibroblasts and use of resulting adipocytes. WO2000037607; 2002
  • Centre Nat Rech Scient. Nucleotidic sequences coding for the murine adrenergic beta 3 receiver and applications thereof. WO9212246; 1992
  • Cedars Sinai Medical Center. Method for reducing the likelihood of the occurrence of cardiac arrhythmias. US2006019954; 2006
  • Chen Jian. Synthesis and uses of synephrine derivatives. US2005250944; 2005
  • Kadowaki T, Tobe K, Suzuki R. Compositions and methods for the amelioration of leptin resistance. US2004242485; 2004
  • Dainippon Pharmaceutical Co. New 2-akylamino-1-phenylethanol derivative. JP8165276; 1996
  • Dainippon Pharmaceutical Co. 2-(2-(Indol-3-ly)ethylamino)-1-phenylethanol derivative. JP6345731; 1994
  • Dainippon Pharmaceutical Co. Indole derivative. WO9616938; 1996
  • Dainippon Pharmaceutical Co. Benzothiophene derivative. JP8157470; 1996
  • Dainippon Pharmaceutical Co. 3,7-Disubstituted indole derivatives and medicinal compositions containing the same. WO2000044721; 2002
  • Dainippon Pharmaceutical Co. Heteroarylsulfonanilide derivative and medicinal composition containing the same. WO2004089936; 2004
  • Dainippon Pharmaceutical Co. Indole compound and pharmaceutical composition containing the same. WO2006078006; 2006
  • Dainippon Pharmaceutical Co. Method for synthesizing indoles and synthetic intermediate. JP2006169113; 2006
  • Dainippon Pharmaceutical Co. Sulfonyloxyindole derivative and medicinal composition containing the same. JP2006111553; 2006
  • Dainippon Pharmaceutical Co. Novel useful therapeutic agent for lower urinary tract symptom. WO2010053068; 2010
  • Eli Lilly & Co. Selective beta 3 adrenergic agonists. WO9809625; 1998
  • Eli Lilly & Co. Selective beta 3 adrenergic agonists. WO9929672; 1999
  • Eli Lilly & Co. Selective beta 3 adrenergic agonists. EP921120; 1999
  • Eli Lilly & Co. Crystalline salts of 2-(4-{2-[2-hydroxy-3-(2-thiophen-2-yl-phenoxy)-propylamino]-2-methyl-propyl}-phenoxy)-nicotinonitrile. WO2002094820; 2002
  • Eli Lilly & Co. 3-Substituted oxindole beta 3 agonists. WO2002038543; 2002
  • Eli Lilly & Co. 3-Substituted oxindole beta 3 agonists. WO2002038544; 2002
  • Eli Lilly & Co. Beta 3 adrenergic agonists. WO20020124; 2002
  • Eli Lilly & Co. 3-Substituted oxindole beta 3 agonists. WO2003044016; 2003
  • Eli Lilly & Co. Beta 3 adrenergic agonists. WO2003016307; 2003
  • Eli Lilly & Co. Beta 3 adrenergic agonists. WO2003044017; 2003
  • Eli Lilly & Co. 3-Substituted oxindole beta 3 agonists. WO2003016276; 2003
  • Fancl Corp. Oligosaccharide-esterified substance effective for obesity and diabetes. JP200616018; 2006
  • Fancl Corp. Lysophosphatidyl choline effective for obesity, diabetes, etc. JP200616018; 2006
  • Fujisawa Pharmaceutical Co. New pharmaceutical use of beta 3-adrenalin agonist. JP6293664; 1994
  • Fujisawa Pharmaceutical Co. New pharmaceutical use of beta 3-adrenalin agonist. JP7228543; 1995
  • Fujisawa Pharmaceutical Co. Aminoalcohol derivatives and their use as beta 3 adrenergic agonists. WO2000012462; 2000
  • Fujisawa Pharmaceutical Co. Aminoalcohol derivatives. WO2002094770; 2002
  • Fujisawa Pharmaceutical Co. Aminoalcohol derivatives and their use as beta 3 adrenergic agonists. WO2003076397; 2003
  • Fujisawa Pharmaceutical Co. Aminoalcohol derivatives and their use as beta 3 adrenergic agonists. WO2004045610; 2004
  • Fujisawa Pharmaceutical Co. Aminoalcohol derivatives. US2004106653; 2004
  • Fujisawa Pharmaceutical Co. Aminoalcohol derivatives. WO2004002939; 2004
  • Fujisawa Pharmaceutical Co., Astellas Pharma, Inc. Aminoalcohol derivatives. WO2005061433; 2005
  • Fujisawa Pharmaceutical Co. Astellas Pharma Inc. Aminoalcohol derivatives. US2005137236; 2005
  • Genaissance Pharmaceuticals. Haplotypes of the adrb3 gene. WO2002008425; 2002
  • Glaxo Group Ltd. Phenethanolamine derivatives and their use as atypical beta-adrenoceptor agonists. WO9533724; 1995
  • Glaxo Group Ltd. Arylethanolamine derivatives and their use as agonists of atypical beta-adrenoceptors. WO9721666; 1997
  • Glaxo Group Ltd. Naphthalenesulphonic or carboxylic acids and their use as atypical beta-adrenoceptor agonists. WO9843953; 1998
  • Glaxo Wellcome, Inc. Arylethanolamine derivatives and their use as agonists of atypical beta-adrenoceptors. US6048872; 1998
  • Glaxo Wellcome, Inc. Therapeutic biaryl derivatives. WO9965877; 1999
  • Glaxo Group Ltd. Beta-3 adrenoceptor agonists. WO0142217; 2001
  • Glaxo Group Ltd. Chemical compounds. WO02060885; 2002
  • Glaxo Group Ltd. Method for producing arylethanoldiamine useful as agonist of beta-adrenoceptor. JP2009137946; 2009
  • Glenmark Pharmaceuticals Ltd. Novel benzopyran compounds and process for their preparation and use. WO2003014113; 2003
  • Imperial Chemical Industries Plc.; Zeneca Ltd. 2-Hydroxy-2-phenylethylamine derivatives as beta-3-adrenoceptor agonists. EP516350; 1992
  • Kaneka Corp. Human beta 3-adrenalin receptor agonist agent. WO2006213657; 2006
  • Kaken Pharmaceut Co. Ltd. Phenylethanolamine derivative. JP7112958; 2000
  • Kissei Pharmaceutical. Preventive/remedy for frequent urination and urinary incontinence. WO9807445; 1998
  • Kissei Pharmaceutical. 2-Methylpropionic acid derivatives and medicinal compositions containing the same. WO9952856; 1999
  • Kissei Pharmaceutical. Phenylaminoalkylcarboxylic acid derivatives and medicinal compositions containing the same. WO9931045; 1999
  • Kissei Pharmaceutical. Aminoethylphenoxyacetic acid derivatives and drugs for pain remission and calculi removal promotion in urinary lithiasis. WO9905090; 1999
  • Kissei Pharmaceutical. Crystal polymorphism of aminoethylphenoxyacetic acid derivative dihydrate. JP2000212137; 2000
  • Kissei Pharmaceutical. Crystal polymorphism of aminoethylphenoxyacetic acid derivative dihydrate. JP2000212138; 2000
  • Kissei Pharmaceutical. Crystal polymorphism of aminoethylphenoxyacetic acid derivative. JP2000212139; 2000
  • Kissei Pharmaceutical. Crystal polymorphism of aminoethylphenoxyacetic acid derivative. WO2000043350; 2000
  • Kissei Pharmaceutical. Phenoxyacetic acid derivatives and medicinal compositions containing the same. WO2000002846; 2000
  • Kissei Pharmaceutical. Amino alcohol derivative, medicinal composition containing the same, and uses of these. WO2004108674; 2004
  • Kissei Pharmaceutical. Amino alcohol derivatives, pharmaceutical compositions containing the same, and use of both. WO2004106290; 2004
  • Kissei Pharmaceutical. Amino alcohol derivative, medicinal composition containing the same, and uses of these. WO2004106283; 2004
  • Kissei Pharmaceutical. Amino alcohol derivative, medicinal composition containing the same, and use of these. WO2005040093; 2005
  • Kissei Pharmaceutical. Method for producing aminoalcohol derivative having biphenyl group. WO2006123672; 2006
  • Kissei Pharmaceutical. Pharmaceutical composition for prevention or treatment of neurogenic pain. WO2007061114; 2007
  • Kissei Pharmaceutical. Preventive or therapeutic agent for disease caused by decrease in lacrimal fluid. WO2007026630; 2007
  • L'oreal. Use of alverine or one of its salts. WO2002080877; 2002
  • Malak JCEG. Chemical compounds derived from octopamine and their uses as beta 3-adrenergic agonists. WO2002081424; 2002
  • Medicinova, Inc. Method of treatment or prophylaxis of depression. WO2008024787; 2008
  • Merck & Co., Inc. Substituted phenyl sulfonamides as selective beta 3 agonists for the treatment of diabetes and obesity. EP611003; 1994
  • Merck & Co., Inc. Substituted sulfonamides as selective beta 3 agonists for the treatment of diabetes and obesity. US5561142; 1996
  • Merck & Co., Inc. Substituted sulfonamides as selective beta 3 agonists for the treatment of diabetes and obesity. US5541197; 1996
  • Merck & Co., Inc. Oxadiazole benzenesulfonamides as selective beta 3 agonists for the treatment of diabetes and obesity. WO9746556; 1997
  • Merck & Co., Inc. Selective B3 agonists for the treatment of diabetes and obesity. GB2305665; 1997
  • Merck & Co., Inc. Thiazole benzenesulfonamides as beta 3 agonists for the treatment of diabetes and obesity. WO9832753; 1998
  • Merck & Co., Inc. Combination therapy for the treatment of diabetes and obesity. WO9818481; 1998
  • Merck & Co., Inc. Substituted sulfonamides as selective beta -3 agonists for the treatment of diabetes and obesity. US5705515; 1998
  • Merck & Co., Inc. Fused piperidine substituted arylsulfonamides as beta 3-agonists. WO9944609; 1999
  • Merck & Co., Inc. Combination therapy for the treatment of urinary frequency, urinary urgency and urinary incontinence. WO2007044296; 2007
  • Merck & Co., Inc. Combination therapy for the treatment-of lower urinary tract symptoms. WO2008121268; 2008
  • Merck & Co. Inc. Hydroxymethyl pyrrolidines as beta 3 adrenergic receptor agonists. WO2009123870; 2009
  • Merck & Co. Inc. Hydroxymethyl pyrrolidines as beta 3 adrenergic receptor agonists. WO2009124166; 2009
  • Merck & Co. Inc. Hydroxymethyl pyrrolidines as beta 3 adrenergic receptor agonists. WO2009124167; 2009
  • Metabolic Pharm Ltd. Product and method for control of obesity. WO2002018436; 2002
  • Pfeizer, Inc. beta3-adrenoceptor agonists and antagonists for the treatment of intestinal motility disorders, depression, prostate disease and dyslipidemia. CA2158910; 1996
  • Pfeizer, Inc. Heterocyclic beta-adrenergic agonists. EP8021060; 1997
  • Pfeizer, Inc. Heterocyclic beta-adrenergic agonists. US5843972; 1998
  • Pfeizer, Inc. Sulfamide derivatives useful as beta3 agonists and pharmaceutical uses thereof. EP1236723; 2002
  • Pfeizer Products, Inc. Alpha-aryl ethanolamines and their use as beta-3 adrenergic receptor agonists. WO2002032897; 2002
  • Pfeizer, Inc. Combinations of beta 3 agonists and growth hormone secretagogues. US6657063; 2003
  • Pfeizer Products, Inc. Crystal forms of (R)-2-(2-(4-oxazol-4-yl-phenoxy)-ethylamino)-1-pyridin-3-yl-ethanol. WO2003072573; 2003
  • Pfeizer Products, Inc. Crystal forms of (R)-2-(2-(4-oxazol-4-yl-phenoxy)-ethylamino)-1-pyridin-3-yl-ethanol. WO2003072573; 2003
  • Pfeizer Products, Inc. Salt of a pyridyl ethanolamine derivative and its use as a beta-3-adrenergic receptor agonist. WO2003072571; 2003
  • Pfeizer, Inc. Beta 3 adrenergic receptor agonist crystal forms, processes for the production thereof, and uses thereof. US2003166686; 2003
  • Ricom Corp. Human beta3-adrenergic receptor ligand, and food or pharmaceutical product containing the same. WO2009151094; 2009
  • Sanofi SA; Midy SPA. Phenylethanol aminotetralines, process for their preparation and pharmaceutical compositions containing them. EP0211721; 1987
  • Sanofi SA; Midy SPA. Process for the preparation of phenylethanolaminotetralines. EP0303545; 1989
  • Sanofi SA; Midy SPA. Phenylethanolaminomethyltetralins, procedure for their preparation and pharmaceutical compositions containing same. EP0436435; 1991
  • Sanofi ELF; Midy SPA. Phenylethanolamino- and phenylethanolaminomethyltetralines, process for their preparation, intermediates of this process and pharmaceutical compositions containing them. EP0500443; 1992
  • Sanofi ELF; Midy SPA. (7S)-7-(2(3-chlorophenyl)-2-hydroxyethylamino-5,6,7,8-tetrahydro-naphthalen-2-yloxy acetic acid, their pharmaceutically acceptable salts with a beta-3-adrenergic agonist activity and pharmaceutical compositions containing them. EP0627407; 1994
  • Sanofi SA; Midy SPA. (7S)-7-(1R)-2-(3-chlorophenyl)-2-hydroxyethylamino-5,6,7,8-tetrahydronaphtalen-2-yloxy acetic acid, their pharmaceutically acceptable salts with a beta-3-adrenergic agonist activity and pharmaceutical compositions containing them. EP0626367; 1994
  • Sanofi SA. Use of agonists of adrenergic beta-3 receptors for preparing wound-healing medicines. WO9831357; 1998
  • Sanofi SA. Use of central cannabinoid receptor antagonists for regulating appetence. WO9832441; 1998
  • Sanofi SA. Phenoxypropanolamines having beta 3-adrenergic antagonist activity. WO9803485; 1998
  • Sanofi Synthelabo. Phenoxylpropanolamines, method for the production thereof and pharmaceutical compositions containing the same. WO9965895; 1999
  • Sanofi Synthelabo. Heteroaryloxy propanolamines, preparation method and pharmaceutical compositions containing same. WO0117989; 2001
  • Sanofi Synthelabo. Phenoxypropanolamines, method for producing them and pharmaceutical compositions containing them. WO2001043744; 2001
  • Sanofi Synthelabo. Phenoxypropanolamines, preparation and therapeutic use thereof. WO2001044227; 2001
  • Sanofi Synthelabo. Propanolaminotetralines, preparation thereof and compositions containing same. WO2001094307; 2001
  • Sanofi Synthelabo. Cyclohexyl(alkyl)-propanolamines, preparation method and pharmaceutical compositions containing same. WO2002044139; 2002
  • Sanofi Synthelabo. Propanolaminomethyltetralines, their preparation and pharmaceutical composition comprising same. FR2833010; 2003
  • Sanofi Synthelabo. Propanolaminomethyltetralines, their preparation and pharmaceutical composition comprising same. WO2003048117; 2003
  • Sanofi Synthelabo. Phenylcyclohexylpropanolamine derivatives, preparation and therapeutic application thereof. WO2003099772; 2003
  • Sanofi Synthelabo. Oxophenyl-cyclohexyl-propanolamine derivatives, production and use thereof in therapeutics. WO2003099819; 2003
  • Sanofi Aventis. Novel therapeutic uses of beta-3 adrenergic receptor agonist derivatives in particular to modulate apoptosis. WO2009019607; 2009
  • Sanofi Aventis. Beta adrenergic receptor ligand derivatives for modulating apoptosis. EP2011490; 2010
  • Smithkline Beecham PLC. Arylethanolamine derivatives and their use as beta-3-adrenoceptor agonists. WO9310074; 1993
  • Smithkline Beecham PLC. Arylethanolamine derivatives and their use in the treatment of obesity and hyperglycaemia. WO9424090; 1994
  • Smithkline Beecham PLC. Aryloxy andarycthio propanolamine derivatives useful as beta3-adrenoreceptor agonists and antagons of the beta1- and beta2-adrenoreceptors and pharmaceutical composition thereof. WO9604234; 1996
  • Smithkline Beecham PLC. Aryloxy and arylthiopropanolamine derivatives useful as beta 3-adrenoreceptor agonists and antagonists of the beta 1- and beta 2-adrenoreceptors and pharmaceutical composition thereof. WO9604233; 1996
  • Sumitomo Pharma. Cyclic amine and medicinal composition containing the same. WO2003106423; 2003
  • Sumitomo Pharma. Indole, indazole, and benzazole derivative. WO2003106418; 2003
  • Sawai Seiyaku Kk. Phenoxyacetic acid derivative. JP11035534; 1999
  • Tokyo Tanabe Co. Ltd. Tetrahydrobenzothiophene derivative. JP10152488; 1998
  • Toyo Shinyaku Co. Ltd. Enhancer of expression of beta 3-adrenergic receptor. WO2010010786; 2010
  • Univ Wayne State. Beta 3-adrenergic receptor protein and DNA encoding same. WO9402590; 1994
  • Univ Maryland. Genetic markers which identify individuals who improve their diabetes status with exercise. WO2000031297; 2000
  • Univ Johns Hopkins Med. Susceptibility gene for obesity and type ii diabetes mellitus. JP2006169113; 2006
  • Vetigen. Canine beta 2- and beta 3-adrenergic receptors and use thereof. WO9735973; 1997
  • Vetigen. Nucleotide sequences coding for the bovine beta 3-adrenergic receptor, and applications thereof. WO9424162; 1996
  • Virbac SA. Aryloxypropanolamine derivatives, method of preparation and applications thereof. WO9820005; 1998
  • 4SC AG. Aryloxypropanolamines, methods of preparation thereof and use of aryloxypropanolamines as medicaments. WO2008090140; 2008
  • Univ. degli Studi di Bari. Beta-3 receptor ligands and their use in therapy. WO2008015558; 2008
  • Univ. Reading. Beta adrenergic receptor pharmacophore. WO2007045893; 2007
  • Univ North Carolina. Methods and materials for determining pain sensitivity and predicting and treating related disorders. WO2007001324; 2007
  • Yamanouchi Pharmaceut Co. Ltd. New guanidine derivative or salt thereof. JP10158233; 1998

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.