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10
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84920336162
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submitted for publication
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Waddell, S. T.; Balkovec, J. M.; Graham, D.; Patel, G.; Dragovic, J.; LeGrand, C.; Mundt, S. S.; Shah, K.; Springer, M. S.; Tan, E. Y.; Thieringer, R.; Hermanovski-Vosatka, A.; Zokian, H. J. Bioorg. Med. Chem. Lett., submitted for publication.
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Waddell, S.T.1
Balkovec, J.M.2
Graham, D.3
Patel, G.4
Dragovic, J.5
Legrand, C.6
Mundt, S.S.7
Shah, K.8
Springer, M.S.9
Tan, E.Y.10
Thieringer, R.11
Hermanovski-Vosatka, A.12
Zokian, H.J.13
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11
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23944493717
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For a detailed summary of the in vitro and in vivo assays see: A. Hermanovski-Vosatka, J. Balkovec, K. Cheng, H.Y. Chen, M. Hernandez, G.C. Koo, C.B. Le Grand, Z. Li, J.M. Metzger, S.S. Mundt, H. Noonan, C.N. Nunes, S.H. Olson, B. Pikounis, N. Ren, N. Robertson, J.M. Schaeffer, K. Shah, M.S. Springer, A.M. Strack, M. Strowski, K. Wu, T.J. Wu, J. Xiao, B.B. Zhang, S.D. Wright, and R. Thieringer J. Exp. Med. 202 2005 517
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Hernandez, M.5
Koo, G.C.6
Le Grand, C.B.7
Li, Z.8
Metzger, J.M.9
Mundt, S.S.10
Noonan, H.11
Nunes, C.N.12
Olson, S.H.13
Pikounis, B.14
Ren, N.15
Robertson, N.16
Schaeffer, J.M.17
Shah, K.18
Springer, M.S.19
Strack, A.M.20
Strowski, M.21
Wu, K.22
Wu, T.J.23
Xiao, J.24
Zhang, B.B.25
Wright, S.D.26
Thieringer, R.27
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PK parameters were based on whole blood drug levels for mouse and plasma for all other species. All the compounds were dosed as a solution in 5-30% hydroxypropyl β-cyclodextrin vehicle
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PK parameters were based on whole blood drug levels for mouse and plasma for all other species. All the compounds were dosed as a solution in 5-30% hydroxypropyl β-cyclodextrin vehicle.
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X. Gu, C. LeGrand, J. Dragovic, K. Shah, S.S. Mundt, G.C. Koo, H.J. Zokian, R. Thieringer, A. Hermanowski-Vosatka, M. Springer, J.M. Balkovec, and S.T. Waddell Bioorg. Med. Chem. Lett. 15 2005 5266
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Zokian, H.J.7
Thieringer, R.8
Hermanowski-Vosatka, A.9
Springer, M.10
Balkovec, J.M.11
Waddell, S.T.12
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G. Koldobskii, S. Ivanova, I. Nikonova, A.R. Zhivich, and Ostrovskii Acta Chem. Scand. 48 1994 596
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Y. Zhu, S.H. Olson, A. Hermanowski-Vosatka, S.S. Mundt, K. Shah, J. Xiao, Y. Gao, M.S. Springer, R. Thieringer, S.D. Wright, H.J. Zokian, and J.M. Balkovec Bioorg. Med. Chem. Lett. 18 2008 3405
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Ismail, J.6
Hartley, D.7
Mosley, R.8
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79953287172
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PCT Int. Appl., WO 2004106294 A2
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Waddell, S. T.; Santorelli, G. M.; Maletic, M. M.; Leeman, A. H.; Gu, X.; Graham, D. W.; Balkovec, J. M.; Aster, S. D. PCT Int. Appl., WO 2004106294 A2, 2004, pp 46.
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Waddell, S.T.1
Santorelli, G.M.2
Maletic, M.M.3
Leeman, A.H.4
Gu, X.5
Graham, D.W.6
Balkovec, J.M.7
Aster, S.D.8
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18
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79953269099
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While mouse PK was not obtained on all the compounds described in this communication, plasma levels of compound were determined in mice following the PD studies. There was generally a good correlation between efficacy and compound levels in plasma for the compounds in Tables 4 and 5; compounds with decreased plasma exposures showed lowered efficacy in extended PD
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While mouse PK was not obtained on all the compounds described in this communication, plasma levels of compound were determined in mice following the PD studies. There was generally a good correlation between efficacy and compound levels in plasma for the compounds in Tables 4 and 5 ; compounds with decreased plasma exposures showed lowered efficacy in extended PD.
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19
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79953278032
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Steamboat Springs, CO, Mar 28-Apr 1, 2007; Poster 224; (b) Maletic, M.; Leeman, A.; Waddell, S. T.; Balkovec, J. 'Bicyclo[2.2.2]octyltriazole inhibitors of 11β-HSD type 1: Pharmacological agents for the treatment of metabolic syndrome' 231st ACS National Meeting, Atlanta, GA, Mar 26-30, 2006; MEDI-196
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Unpublished results; (a) Maletic, M.; Leeman, A.; Mundt, S.; Zokian, H.; Shah, K.; Dragovic, J.; Lyons, K.; Tan, E.; Thieringer, R.; Vosatka, A.; Springer, M.; Balkovec, J.; Waddell, S. T. 'Bicyclo[2.2.2]octyltriazole inhibitors of 11β-HSD type 1: Pharmacological agents for the treatment of metabolic syndrome' Metabolic Syndrome and Cardiovascular Risk Keystone Symposium, Steamboat Springs, CO, Mar 28-Apr 1, 2007; Poster 224; (b) Maletic, M.; Leeman, A.; Waddell, S. T.; Balkovec, J. 'Bicyclo[2.2.2]octyltriazole inhibitors of 11β-HSD type 1: Pharmacological agents for the treatment of metabolic syndrome' 231st ACS National Meeting, Atlanta, GA, Mar 26-30, 2006; MEDI-196.
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Bicyclo[2.2.2]octyltriazole Inhibitors of 11β-HSD Type 1: Pharmacological Agents for the Treatment of Metabolic Syndrome' Metabolic Syndrome and Cardiovascular Risk Keystone Symposium
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Maletic, M.1
Leeman, A.2
Mundt, S.3
Zokian, H.4
Shah, K.5
Dragovic, J.6
Lyons, K.7
Tan, E.8
Thieringer, R.9
Vosatka, A.10
Springer, M.11
Balkovec, J.12
Waddell, S.T.13
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