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1
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0027217067
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For a review of the topic:
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For a review of the topic:. Howe R. Drugs Fut. 18 (1993) 529
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Drugs Fut.
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Howe, R.1
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3
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0030950052
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Sher P.A., Mathur A., Fisher L.G., Wu G., Skwish S., Michel I.M., Seiler S.M., and Dickinson E.J. Bioorg. Med. Chem. Lett. 7 (1997) 1583
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Sher, P.A.1
Mathur, A.2
Fisher, L.G.3
Wu, G.4
Skwish, S.5
Michel, I.M.6
Seiler, S.M.7
Dickinson, E.J.8
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4
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0021363316
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Arch J.R.S., Ainsworth A.T., Cawthorne M.A., Piercy V., Sennitt M.V., Thody V.E., Wilson C., and Wilson S. Nature 309 (1984) 163
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Nature
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Arch, J.R.S.1
Ainsworth, A.T.2
Cawthorne, M.A.3
Piercy, V.4
Sennitt, M.V.5
Thody, V.E.6
Wilson, C.7
Wilson, S.8
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6
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0000386860
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2 agonists reported in the literature, see Ref. 5
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2 agonists reported in the literature, see Ref. 5. Weber A.E. Ann. Rep. Med. Chem. 33 (1998) 193
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(1998)
Ann. Rep. Med. Chem.
, vol.33
, pp. 193
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Weber, A.E.1
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7
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0033584163
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As described for: CP-331679 in Ref. 5 and for CL-316243 in
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As described for: CP-331679 in Ref. 5 and for CL-316243 in. Sum F.W., Gilbert A., Venkatesan A.M., Lim K., Wong V., O'Dell M., Francisco G., Chen Z., Grosu G., Baker J., Ellingboe J., Malamas M., Gunawan I., Primeau J., Largis E., and Steiner K. Bioorg. Med. Chem. Lett. 9 (1999) 1921
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Bioorg. Med. Chem. Lett.
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Sum, F.W.1
Gilbert, A.2
Venkatesan, A.M.3
Lim, K.4
Wong, V.5
O'Dell, M.6
Francisco, G.7
Chen, Z.8
Grosu, G.9
Baker, J.10
Ellingboe, J.11
Malamas, M.12
Gunawan, I.13
Primeau, J.14
Largis, E.15
Steiner, K.16
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8
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0034687253
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and references cited therein
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Mathvink R.J., Tolman J.S., Chitty D., Candelore M.R., Cascieri M.A., Colwell L.F., Deng L., Feeney W.P., Forrest M.J., Hom G.J., MacIntyre D.E., Miller R.R., Stearns R.A., Tota L., Wyvratt M.J., Fisher M.H., and Weber A.E. J. Med. Chem. 43 (2000) 3832 and references cited therein
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J. Med. Chem.
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, pp. 3832
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Mathvink, R.J.1
Tolman, J.S.2
Chitty, D.3
Candelore, M.R.4
Cascieri, M.A.5
Colwell, L.F.6
Deng, L.7
Feeney, W.P.8
Forrest, M.J.9
Hom, G.J.10
MacIntyre, D.E.11
Miller, R.R.12
Stearns, R.A.13
Tota, L.14
Wyvratt, M.J.15
Fisher, M.H.16
Weber, A.E.17
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9
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34547922950
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van Baak M.A., Hul G.B.J., Toubro S., Astrup A., Gottesdiener K.M., DeSmet M., and Saris W.H.M. Clin. Pharmacol. Ther. 76 (2002) 780
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(2002)
Clin. Pharmacol. Ther.
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van Baak, M.A.1
Hul, G.B.J.2
Toubro, S.3
Astrup, A.4
Gottesdiener, K.M.5
DeSmet, M.6
Saris, W.H.M.7
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10
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0035987890
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Stearns R.A., Miller R.R., Tang W., Kwei G.Y., Tang F.S., Mathvink R.J., Naylor E.M., Chitty D., Colandrea V.J., Weber A.E., Colleti A.E., Strauss J.R., Keohane C.A., Feeney W.P., Iliff S.A., and Chiu S.L. Drug Metab. Disp. 30 (2002) 771
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(2002)
Drug Metab. Disp.
, vol.30
, pp. 771
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-
Stearns, R.A.1
Miller, R.R.2
Tang, W.3
Kwei, G.Y.4
Tang, F.S.5
Mathvink, R.J.6
Naylor, E.M.7
Chitty, D.8
Colandrea, V.J.9
Weber, A.E.10
Colleti, A.E.11
Strauss, J.R.12
Keohane, C.A.13
Feeney, W.P.14
Iliff, S.A.15
Chiu, S.L.16
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13
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34547903385
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Lafontaine, J. A.; Morgan, B. P. PCT Int. Appl. WO 2003072572, 2003.
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14
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34547858283
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Dow, R. L.; Schneider, S. R. European Patent Application 1138685, 2001. (R)-Toluene-4-sulfonic acid 2-(6-chloropyridin-3-yl)-2-hydroxyethyl ester, described therein, was treated with 1 M NaOH in THF and water to afford epoxide 8 in 90% yield.
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15
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34547894867
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50 < 100 nM and IA > 50% was tested at least twice in functional assays. Similar potencies and intrinsic activities were observed in the assays.
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17
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34547855637
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Solubility measurements were made in pH 6.5 phosphate buffer.
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19
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34547887027
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note
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Animals were removed from general housing in the morning (7-7:30 am) and were deprived of food and water for the length of the oxygen consumption measurements. Animals were weighed (310-350 g), marked, and placed into individual activity-monitored chambers (17″ × 17″ × 5″). The system was calibrated and the run started (8:00-8:30 am). Oxygen consumption measurements were made every 10 min for 3 h, and then the animals were dosed with the test compound or vehicle. Oxygen consumption measurements were continued for 2 h. Oxygen consumption values associated with periods of high ambulatory activity (>100 counts/10 min) were excluded from all calculations, as were the first five values of the run and the first value after dosing.
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20
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34547912297
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note
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b is the dissociation equilibrium constant for a competitive antagonist (the concentration which would occupy 50% of the receptors at equilibrium).
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21
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0018575383
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For the preparation of 28, see:
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For the preparation of 28, see:. Ridge D.N., Hanifin J.W., Harten L.A., Johnson B.D., Menschik J., Nicolau G., Sloboda A.E., and Watts D.E. J. Med. Chem. 22 (1979) 1385
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(1979)
J. Med. Chem.
, vol.22
, pp. 1385
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Ridge, D.N.1
Hanifin, J.W.2
Harten, L.A.3
Johnson, B.D.4
Menschik, J.5
Nicolau, G.6
Sloboda, A.E.7
Watts, D.E.8
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22
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33645546372
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For a representative procedure, see:
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For a representative procedure, see:. Scott R.W., Neville S.N., Urbina A., Camp D., and Stankovic N. Org. Process Res. Dev. 10 (2006) 296
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(2006)
Org. Process Res. Dev.
, vol.10
, pp. 296
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-
Scott, R.W.1
Neville, S.N.2
Urbina, A.3
Camp, D.4
Stankovic, N.5
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23
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34547918618
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note
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Compound 31 was prepared in two steps from ethanolamine, which was first protected as the benzyl carbamate, and then converted to the mesylate, under standard conditions.
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24
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33748796698
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As in:
-
As in:. Finley D.R., Bell M.G., Borel A.G., Bloomquist W.E., Cohen M.L., Heiman M.L., Kriauciunas A., Matthews D.P., Miles T., Neel D.A., Rito C.J., Sall D.J., Shuker A.J., Stephens T.W., Tinsley F.C., Winter M.A., and Jesudason C.D. Bioorg. Med. Chem. Lett. 16 (2006) 5691
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(2006)
Bioorg. Med. Chem. Lett.
, vol.16
, pp. 5691
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Finley, D.R.1
Bell, M.G.2
Borel, A.G.3
Bloomquist, W.E.4
Cohen, M.L.5
Heiman, M.L.6
Kriauciunas, A.7
Matthews, D.P.8
Miles, T.9
Neel, D.A.10
Rito, C.J.11
Sall, D.J.12
Shuker, A.J.13
Stephens, T.W.14
Tinsley, F.C.15
Winter, M.A.16
Jesudason, C.D.17
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