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38749114993
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C.A. Salvatore , J.C. Hershey , H.A. Corcoran , J.F. Fay , V.K. Johnston , E.L. Moore , S.D. Mosser , C.S. Burgey , D.V. Paone , A.W. Shaw , S.L. Graham , J.P. Vacca , T.M. Williams , K.S. Koblan , and S.A. Kane JPET 324 2008 416
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18
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79955483944
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-
For the details of these assays see: Bell, I. M.; Graham, S. L.; Williams, T. M.; Stump, C. A. WO 2004/087649
-
For the details of these assays see: Bell, I. M.; Graham, S. L.; Williams, T. M.; Stump, C. A. WO 2004/087649.
-
-
-
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19
-
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79955479805
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-
Aqueous solubilities at pH 7.4: telcagepant = 30 μg/mL; triazole 1 = 158 μg/mL
-
Aqueous solubilities at pH 7.4: telcagepant = 30 μg/mL; triazole 1 = 158 μg/mL.
-
-
-
-
20
-
-
79955477690
-
-
As a general trend, fused heterocycles in this series with low permeability resulted in low oral exposures
-
As a general trend, fused heterocycles in this series with low permeability resulted in low oral exposures.
-
-
-
-
22
-
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49649114639
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C.S. Burgey , D.V. Paone , A.W. Shaw , J.Z. Deng , D.N. Nguyen , C.M. Potteiger , S.L. Graham , J.P. Vacca , and T.M. Williams Org. Lett. 10 2008 3235
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Graham, S.L.7
Vacca, J.P.8
Williams, T.M.9
-
24
-
-
79955482106
-
-
For additional synthetic details, see: Burgey, C. S.; Paone, D. V.; Shaw, A. W.; Nguyen, D. N.; Deng, Z. J.; Vacca, J. P.; Selnick, H. G.; Williams, T. M.; Potteiger, C. WO 2006/044504 A2
-
For additional synthetic details, see: Burgey, C. S.; Paone, D. V.; Shaw, A. W.; Nguyen, D. N.; Deng, Z. J.; Vacca, J. P.; Selnick, H. G.; Williams, T. M.; Potteiger, C. WO 2006/044504 A2.
-
-
-
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25
-
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79955478606
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1H NMR, HRMS, and HPLC
-
1H NMR, HRMS, and HPLC.
-
-
-
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26
-
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32044444143
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C.E. Raab , J.W. Butcher , T.M. Connolly , J. Karczewski , N.X. Yu , S.J. Staskiewicz , N. Liverton , D.C. Dean , and D.G. Melillo Bioorg. Med. Chem. Lett. 16 2006 1692
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71049116463
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28
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13144251165
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J.C. Hershey , H.A. Corcoran , E.P. Baskin , C.A. Salvatore , S. Mosser , T.M. Williams , K.S. Koblan , R. Hargreaves , and S.A. Kane Regul. Pept. 127 2005 71
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Kane, S.A.9
-
29
-
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79955480580
-
-
-OH = (po normalized AUC 31 upon dosing of 30)/ (iv normalized AUC 31 upon dosing of 31)
-
-OH = (po normalized AUC 31 upon dosing of 30)/ (iv normalized AUC 31 upon dosing of 31).
-
-
-
-
30
-
-
79955471613
-
-
Additions of both amino alcohols and amino ketones to thioamides were rapid, typically complete in <10 min. Cyclization of the intermediate amidine to 38 required and additional 18 h
-
Additions of both amino alcohols and amino ketones to thioamides were rapid, typically complete in <10 min. Cyclization of the intermediate amidine to 38 required and additional 18 h.
-
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