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Nagarajan S.R., Lu H.-F., Gasiecki A.F., Khanna I.K., Parikh M.D., Desai B.N., Rogers T.E., Clare M., Chen B.B., Russell M.A., Keene J.L., Duffin T., Engleman V.W., Finn M.B., Freeman S.K., Klover J.A., Nickols G.A., Nickols M.A., Shannon K.E., Steininger C.A., Westlin W.F., Westlin M.M., and Williams M.L. Bioorg. Med. Chem. 15 (2007) 3390
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0037147775
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Urbahns K., Haerter M., Albers M., Schmidt D., Stelte-Ludwig B., Brueggemeier U., Vaupel A., and Gerdes C. Bioorg. Med. Chem. Lett. 12 (2002) 205
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Vaupel, A.7
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10
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35148863047
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The B-series analogs of 5 and 6 are examples 25 and 26 (Table 3).
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11
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0037463755
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Urbahns K., Haerter A., Vaupel M., Albers M., Schmidt D., Stelte-Ludwig B., Brueggemeier U., Gerdes C., and Tsujishita H. Bioorg. Med. Chem. Lett. 13 (2003) 1071
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12
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35148863465
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For details of the syntheses and the primary assay procedures see: Urbahns, K.; Haerter, M.; Albers, M.; Vaupel, A.; Schmidt, D.; Stelte-Ludwig, B.; Gerdes, C.; Lustig, K. WO 0035864, 2000; Chem. Abstr. 2000, 133, 43809.
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13
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14
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0034642520
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Use of imidazolines
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Use of imidazolines. Batt D.G., Petraitis J.J., Houghton G.C., Modi D.P., Cain G.A., Corjay M.H., Mousa S.A., Bouchard P.J., Forsythe M.S., Harlow P.P., Barbera F.A., Spitz S.M., Wexler R.R., and Jadhav P.K. J. Med. Chem. 43 (2000) 41
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15
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0034642555
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Pitts W.J., Wityak J., Smallheer J.M., Tobin A.E., Jetter J.W., Buynitsky J.S., Harlow P.P., Solomon K.A., Corjay M.H., Mousa S.A., Wexler R.R., and Jadhav P.K. J. Med. Chem. 43 (2000) 27
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16
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35148837554
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Squaric acid amides have been used as α4 integrin inhibitors before: Head, J. C.; Porter, J. R.; McKay, C.; WO 2002-010136.
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17
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35148833003
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Chem. Abstr. 2002, 136, 167287 and WO 2002-042264.
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18
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35148859270
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Chem. Abstr. 2002, 136, 401746 (Celltech).
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19
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0030971054
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note
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3 as described: Kumar, C. S.; James, I. E.; Wong, A.; Mwang, V.; Field, J. A.; Nuthulaganti, P.; Conner, J. R.; Eichman, C.; Ali, F.; Hwang, S. M.; Rieman, D. J.; Drake, F. H.; Gowen, M. J. Biol. Chem. 1997, 272, 16390.
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20
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0035803478
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The binding constant to human serum albumin (HSA) was determined by equilibrium dialysis
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The binding constant to human serum albumin (HSA) was determined by equilibrium dialysis. Loidl-Stahlhofen A., Schmitt J., Noller J., Hartmann T., Brodowsky H., Schmitt W., and Keldenich J. Adv. Mater. 13 (2001) 1829
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Schmitt, W.6
Keldenich, J.7
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21
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0344025397
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Sebille B., Zini R., Madjar C.V., Thuaud N., and Tillement J.P. J. Chromatogr. 51 (1990) 531
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22
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0035666579
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Membrane affinities were determined as described. Briefly, the reduction of compound concentration after incubation with liposomal egg yolk lecithin followed by ultracentrifugation was measured by HPLC:
-
Membrane affinities were determined as described. Briefly, the reduction of compound concentration after incubation with liposomal egg yolk lecithin followed by ultracentrifugation was measured by HPLC:. Loidl-Stahlhofen A., Hartmann T., Schottner M., Rohring C., Brodowsky H., Schmitt J., and Keldenich J. Pharm. Res. 18 (2001) 1782
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Schmitt, J.6
Keldenich, J.7
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23
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0344333422
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The prediction of hepatic clearance was performed according to
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The prediction of hepatic clearance was performed according to. Houston J.B., and Carlile D.J. Drug Metab. Rev. 29 (1997) 891
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Houston, J.B.1
Carlile, D.J.2
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24
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35148891174
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Briefly, compounds were incubated (1 μM, 37 °C) with 0.2 mg/ml rat microsomal protein. Samples were taken at 7 time points within 30 min to calculate half-lives and extrapolate clearance. Compound A showed an extrapolated clearance of 0.6 l/h/kg in this in vitro assay.
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25
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33845360094
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Recent review on arginine mimetics
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Recent review on arginine mimetics. Masic L.P. Curr. Med. Chem. 13 (2006) 3627
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