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Patent Evaluation

Inhibition of stearoyl-CoA desaturase by cyclic amine derivatives

Merck Frosst Canada: WO2007134457

&
Pages 457-460 | Published online: 07 Apr 2008

Bibliography

  • Ntambi JM, Miyazaki M. Regulation of stearoyl-CoA desaturases and role in metabolism. Prog Lipid Res 2004;43:91-104
  • Dobrzyn P, Dobrzyn A. Stearoyl-CoA desaturase: a new therapeutic target of liver steatosis. Drug Dev Res 2006;67: 643-650
  • Storlien LH, Jenkins AB, Chisholm DJ, et al. Influence of dietary fat composition on development of insulin resistance in rats Relationship to muscle triglyceride and omega-3 fatty acids in muscle phospholipid. Diabetes 1991;40:280-9
  • Jones BH, Maher MA, Banz WJ, et al. Adipose tissue stearoyl-CoA desaturase mRNA is increased by obesity and decreased by polyunsaturated fatty acids. Am J Physiol 1996;271:E44-9
  • Pan DA, Hulbert AJ, Storlein LH. Dietary fats, membrane phospholipids and obesity. J Nutr 1994;124:1555-65
  • Pettegrew JW, Panchalingam K, Hamilton RL, McClur RJ. Brain membrane phospholipid alterations in Alzheimer's disease. Neurochem Res 2001;26:771-82
  • Solans R, Motta C, Sola R, et al. Abnormalities of erythrocyte membrane fluidity, lipid composition, and lipid peroxidation in systemic sclerosis: evidence of free radical-mediated injury. Arthritis Rheum 2000;43:894-900
  • Agatha G, Hafer R, Zintl F. Fatty acid composition of lymphocyte membrane phospholipids in children with acute leukemia. Cancer Lett 2001;173:139-44
  • Dobrzyn P, Dobrzyn A. Stearoyl-CoA desaturase: a novel control point of lipid metabolism and insulin sensitivity. Eur J Lipid Sci Technol 2008;110:93-100
  • Ntambi JM, Buhrow SA, Kaestner KH, et al. Differentiation-induced gene expression in 3T3-L1 preadipocytes Characterization of a differentially expressed gene encoding stearoyl-CoA desaturase. J Biol Chem 1988;263:17291-300
  • Kaestner KH, Ntambi JM, Kelly TJ Jr, Lane MD. Differentiation-induced gene expression in 3T3-L1 preadipocytes A second differentially expressed gene encoding stearoyl-CoA desaturase. J Biol Chem 1989;264:14755-61
  • Zheng Y, Prouty SM, Harmon A, et al. Scd3: a novel gene of the stearoyl-CoA desaturase family with restricted expression in skin. Genomics 2001;71:182-91
  • Miyazaki M, Jacobson MJ, Man WC, et al. Identification and characterization of murine SCD4, a novel heart-specific stearoyl-CoA desaturase isoform regulated by leptin and dietary factors. J Biol Chem 2003;278:33904-11
  • Dobrzyn A, Dobrzyn P. Stearoyl-CoA desaturase: a new player in skeletal muscle metabolism regulation. J Physiol Pharmacol 2006;57:31-42
  • Zheng Y, Eilertsen KJ, Ge L, et al. SCD1 is expressed in sebaceous glands and is disrupted in the asebia mouse. Nat Genet 1999;23:268-70
  • Beiraghi S, Zhou M, Talmadge CB, et al. Identification and characterization of a novel gene disrupted by a pericentric inversion inv(4)(p13.1q21.1) in a family with cleft lip. Gene 2003;309:11-21
  • Miyazaki M, Dobrzyn A, Elias PM, Ntambi JM. Stearoyl-CoA desaturase-2 gene expression is required for lipid synthesis during early skin and liver development. Proc Natl Acad Sci USA 2005;102:12501-6
  • Dobrzyn A, Ntambi JM. The role of stearoyl-CoA desaturase in body weight regulation. Trends Cardiovasc Med 2004;14:77-81
  • Dobrzyn A, Ntambi JM. The role of stearoyl-CoA desaturase in the control of metabolism. Prostaglandins Leukot Essent Fatty Acids 2005;73:35-41
  • Dobrzyn A, Ntambi JM. Stearoyl-CoA desaturase as a new drug target for obesity treatment. Obes Rev 2005;6:169-74
  • Ntambi JM, Miyazaki M, Stoehr JP, et al. Loss of stearoyl-CoA desaturase-1 function protects mice against adiposity. Proc Natl Acad Sci USA 2002;99:11482-6
  • Miyazaki M, Kim YC, Gray-Keller MP, et al. The biosynthesis of hepatic cholesterol esters and triglycerides is impaired in mice with a disruption of the gene for stearoyl-CoA desaturase 1. J Biol Chem 2000;275:30132-8
  • Attie AD, Krauss MM, Gray-Keller MP, et al. Relationship between stearoyl-CoA desaturase activity and plasma triglycerides in human and mouse hypertriglyceridemia. J Lipid Res 2002;43:1899-907
  • Miyazaki M, Kim YC, Ntambi JM. A lipogenic diet in mice with a disruption of the stearoyl-CoA desaturase 1 gene reveals a stringent requirement of endogenous monounsaturated fatty acids for triglyceride synthesis. J Lipid Res 2001;42:1018-24
  • Cohen P, Miyazaki M, Socci ND, et al. Role for stearoyl-CoA desaturase-1 in leptin-mediated weight loss. Science 2002;297:240-3
  • Chen HC, Farese RV. Turning WAT into BAT gets rid of fat. Nat Med 2001;7:1102-3
  • Dobrzyn A, Dobrzyn P, Lee SH, et al. Stearoyl-CoA desaturase-1 deficiency reduces ceramide synthesis by downregulating serine palmitoyltransferase and increasing beta-oxidation in skeletal muscle. Am J Physiol Endocrinol Metab 2005;288:E599-607
  • Gomez FE, Bauman DE, Ntambi JM, Fox BG. Effects of sterculic acid on stearoyl-CoA desaturase in differentiating 3T3-L1 adipocytes. Biochem Biophys Res Commun 2003;300:316-26
  • Kamboj R, Zhang Z, Fu J, et al. Heterocyclic derivatives and their use as mediators of stearoyl-CoA desaturase. WO2006034338 (2006)
  • Kamboj R, Fu J, Kodumuru V, et al. Bicyclic heterocyclic derivatives and their use as inhibitors of stearoyl-CoA desaturase (SCD). WO2006034312 (2006)
  • Zhao H, Serby MD, Smith HT, et al. Discovery of 1-(4-phenoxypiperidin-1-yl)-2-arylaminoethanone stearoyl-CoA desaturase 1 inhibitors. Bioorg Med Chem Lett 2007;17:3388-91
  • Liu G, Lynch JK, Freeman J, et al. Discovery of potent, selective, orally bioavailable stearoyl-CoA desaturase 1 inhibitors. J Med Chem 2007;50:3086-100

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