198
Views
1
CrossRef citations to date
0
Altmetric
Patent Evaluations

Compound and compositions as TGR5 agonists: WO2012082947

Pages 531-536 | Published online: 15 Feb 2013

Bibliography

  • Shaw JE, Sicree RA, Zimmet PZ. Global estimates of the prevalence of diabetes for 2010 and 2030. Diabetes Res Clin Pract 2010;87:4-14
  • Nauck MA, Homberger E, Siegel EG, Incretin effects of increasing glucose loads in man calculated from venous insulin and C-peptide responses. J Clin Endocrinol Metab 1986;63:492-8
  • Toft-Nielsen MB, Damholt MB, Madsbad S, Determinants of the impaired secretion of glucagon-like peptide-1 in type 2 diabetic patients. J Clin Endocrinol Metab 2001;86:3717-23
  • Ihara H, Hirukawa K, Goto S, Togari A. ATP-stimulated interleukin-6 synthesis through P2Y receptors on human osteoblasts. Biochem Biophys Res Commun 2005;326:329-34
  • Thomas C, Pellicciari R, Pruzanski M, Targeting bile-acid signalling for metabolic diseases. Nat Rev Drug Discov 2008;7:678-93
  • Fiorucci S, Rizzo G, Donini A, Targeting farnesoid X receptor for liver and metabolic disorders. Trends Mol Med 2007;13:298-309
  • Modica S, Moschetta A. Nuclear bile acid receptor FXR as pharmacological target: are we there yet? FEBS Lett 2006;580:5492-9
  • Francis GA, Fayard E, Picard F, Auwerx J. Nuclear receptors and the control of metabolism. Annu Rev Physiol 2003;65:261-311
  • Maruyama T, Miyamoto Y, Nakamura T, Identification of membrane-type receptor for bile acids (M-BAR). Biochem Biophys Res Commun 2002;298:714-19
  • Kawamata Y, Fujii R, Hosoya M, A G protein-coupled receptor responsive to bile acids. J Biol Chem 2003;278:9435-40
  • Sato H, Macchiarulo A, Thomas C, Novel potent and selective bile acid derivatives as TGR5 agonists: biological screening, structure-activity relationships, and molecular modeling studies. J Med Chem 2008;51:1831-41
  • Groen AK. The emerging role of bile acids as integrators of intermediary metabolism. J Hepatol 2006;45:337-8
  • Watanabe M, Houten SM, Mataki C, Bile acids induce energy expenditure by promoting intracellular thyroid hormone activation. Nature 2006;439:484-9
  • Maruyama T, Tanaka K, Suzuki J, Targeted disruption of G protein-coupled bile acid receptor 1 (Gpbar1/M-Bar) in mice. J Endocrinol 2006;191:197-205
  • Pols TW, Nomura M, Harach T, TGR5 activation inhibits atherosclerosis by reducing macrophage inflammation and lipid loading. Cell Metab 2011;14:747-57
  • Pols TW, Noriega LG, Nomura M, The bile acid membrane receptor TGR5 as an emerging target in metabolism and inflammation. J Hepatol 2011;54:1263-72
  • Gioiello A, Rosatelli E, Nuti R, Patented TGR5 modulators: a review (2006 - present). Expert Opin Ther Patents 2012;22:1399-414
  • Hinuma S, Fujii R, Kawamata Y, Screening Method. WO2004043468; 2004
  • Qiu J, Webb RR, Unett DJ, Modulators of Human G Protein-Coupled Receptors for The Treatment of Hyperglycemia and Related Disorders. WO2005116653; 2005
  • Evans KA, Budzik BW, Ross SA, Discovery of 3-aryl-4-isoxazolecarboxamides as TGR5 receptor agonists. J Med Chem 2009;52:7962-5
  • Budzik BW, Evans KA, Wisnoski DD, Synthesis and structure-activity relationships of a series of 3-aryl-4-isoxazolecarboxamides as a new class of TGR5 agonists. Bioorg Med Chem Lett 2010;20:1363-7
  • Heterocyclic Modulators of TGR5. WO2008067222; 2008
  • Quinazolinone Modulators of TGR5. WO2008067219; 2008
  • Bollu V. Triazole and Imidazole Derivatives for use as TGR5 Agonists in The Treatment of Diabetes and Obesity. WO2010093845; 2010
  • Bollu V. TGR5 Agonists. WO2011071565; 2011
  • Bissantz C, Dehmlow H, Erickson SD, 3-Amino-Pyridines as GPBAR1 Agonists. WO2012117000; 2012
  • Duan H, Ning M, Chen X, Design, synthesis, and antidiabetic activity of 4-phenoxynicotinamide and 4-phenoxypyrimidine-5-carboxamide derivatives as potent and orally efficacious TGR5 agonists. J Med Chem 2012;55:10475-89
  • Robl JA. Novel Bicyclic Nitrogen Containing Heteroaryl TGR5 Receptor Modulators. WO2012149236; 2012
  • Futatsugi K, Bahnck KB, Brenner MB, Optimization of triazole-based TGR5 agonists towards orally available agents. Med Chem Comm 2013;4:205-10

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.