-
2
-
-
0037831023
-
-
R.C. Keesler, P. Berglung, O. Demler, R. Jin, D. Loretz, K.R. Merikangas, A.J. Rush, E.E. Walters, and P.S. Wang J. Am. Med. Assoc. 289 2003 3095
-
(2003)
J. Am. Med. Assoc.
, vol.289
, pp. 3095
-
-
Keesler, R.C.1
Berglung, P.2
Demler, O.3
Jin, R.4
Loretz, D.5
Merikangas, K.R.6
Rush, A.J.7
Walters, E.E.8
Wang, P.S.9
-
4
-
-
36549069650
-
-
J.A. Blumenthal, A. Sherwood, S.D. Rogers, M.A. babyak, P.M. Doraiswamy, L. Watkins, B.M. Hoffman, C. O'Connell, J.J. Johnson, S.M. Patidar, R. Waugh, and A. Hinderlitter Clin. Trials 4 2007 548
-
(2007)
Clin. Trials
, vol.4
, pp. 548
-
-
Blumenthal, J.A.1
Sherwood, A.2
Rogers, S.D.3
Babyak, M.A.4
Doraiswamy, P.M.5
Watkins, L.6
Hoffman, B.M.7
O'Connell, C.8
Johnson, J.J.9
Patidar, S.M.10
Waugh, R.11
Hinderlitter, A.12
-
5
-
-
34548396844
-
-
S. Moussavi, E.M. Chatterji, A. Tandon, V. Patel, and B. Ustun Lancet 370 2007 851
-
(2007)
Lancet
, vol.370
, pp. 851
-
-
Moussavi, S.1
Chatterji, E.M.2
Tandon, A.3
Patel, V.4
Ustun, B.5
-
10
-
-
0037209183
-
-
C.J. Harmer, Z. Bhagwagar, B.A. Völlm, P.J. Cowen, and G.M. Goodwin Neuropsycopharmacology 28 2003 148
-
(2003)
Neuropsycopharmacology
, vol.28
, pp. 148
-
-
Harmer, C.J.1
Bhagwagar, Z.2
Völlm, B.A.3
Cowen, P.J.4
Goodwin, G.M.5
-
15
-
-
33748077457
-
-
P. Skolnick, P. Kreiter, J. Tizzano, A. Basile, P. Popik, P. Czobor, and A. Lippa CNS Drug Rev. 12 2006 123
-
(2006)
CNS Drug Rev.
, vol.12
, pp. 123
-
-
Skolnick, P.1
Kreiter, P.2
Tizzano, J.3
Basile, A.4
Popik, P.5
Czobor, P.6
Lippa, A.7
-
16
-
-
10744233215
-
-
L. Azford, J.R. Boot, T.M. Hotten, M. Keenan, F.M. Martin, S. Milutinovic, N.A. Moore, M.F. Oneil, F.M. Pullar, D.F. Tupper, K. Van Belle, and V. Vivien Bioorg. Med. Chem. Lett. 13 2003 3277
-
(2003)
Bioorg. Med. Chem. Lett.
, vol.13
, pp. 3277
-
-
Azford, L.1
Boot, J.R.2
Hotten, T.M.3
Keenan, M.4
Martin, F.M.5
Milutinovic, S.6
Moore, N.A.7
Oneil, M.F.8
Pullar, F.M.9
Tupper, D.F.10
Van Belle, K.11
Vivien, V.12
-
18
-
-
28944435199
-
-
M. Fava, A.J. Rush, M. Thase, A. Clayton, S.M. Stahl, J.F. Pradko, and J.A. Johnston J. Clin. Psychiatry 7 2005 106
-
(2005)
J. Clin. Psychiatry
, vol.7
, pp. 106
-
-
Fava, M.1
Rush, A.J.2
Thase, M.3
Clayton, A.4
Stahl, S.M.5
Pradko, J.F.6
Johnston, J.A.7
-
19
-
-
0037310632
-
-
C. Debattista, H.B. Solvanson, J. Poirier, E. Kendrick, and A.F. Schatzberg J. Clin. Psychopharmacol. 23 2003 27
-
(2003)
J. Clin. Psychopharmacol.
, vol.23
, pp. 27
-
-
Debattista, C.1
Solvanson, H.B.2
Poirier, J.3
Kendrick, E.4
Schatzberg, A.F.5
-
21
-
-
0030022134
-
-
A.L. Stoll, S.S. Pillay, L. Diamond, S.B. Workum, and J.O. Cole J. Clin. Psychiatry 57 1996 72
-
(1996)
J. Clin. Psychiatry
, vol.57
, pp. 72
-
-
Stoll, A.L.1
Pillay, S.S.2
Diamond, L.3
Workum, S.B.4
Cole, J.O.5
-
22
-
-
67651097819
-
-
M.C. Lucas, D.S. Carter, H. Cai, E.K. Lee, R.C. Schoenfeld, S.S. Steiner, Marzia. Villa, V. Weikert, R.J. Weikert, and P. Iyer Bioorg. Med. Chem. Lett. 19 2009 4630
-
(2009)
Bioorg. Med. Chem. Lett.
, vol.19
, pp. 4630
-
-
Lucas, M.C.1
Carter, D.S.2
Cai, H.3
Lee, E.K.4
Schoenfeld, R.C.5
Steiner, S.S.6
Villa, M.7
Weikert, V.8
Weikert, R.J.9
Iyer, P.10
-
23
-
-
77954310055
-
-
3H]-Vanoxerine, respectively. The specific details of this assay are reported in Carter, D. S.; Schoenfeld, R. C.; Weikert, R. J. WO 2008019971
-
3H]-Vanoxerine, respectively. The specific details of this assay are reported in Carter, D. S.; Schoenfeld, R. C.; Weikert, R. J. WO 2008019971.
-
-
-
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24
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77954310583
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-
MW = 305, Clog P = 3.68, PSA = 27
-
MW = 305, Clog P = 3.68, PSA = 27.
-
-
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26
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0036367835
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-
J.H. Meyer, V.S. Goulding, A.A. Wilson, D. Hussey, B.K. Christensen, and S. Houle Psychopharmacology 162 2002 102
-
(2002)
Psychopharmacology
, vol.162
, pp. 102
-
-
Meyer, J.H.1
Goulding, V.S.2
Wilson, A.A.3
Hussey, D.4
Christensen, B.K.5
Houle, S.6
-
27
-
-
67649408864
-
-
X. Liu, O. Vilenski, J. Kwan, S. Apparsundaram, and R. Weikert Drug Metab. Dispos. 37 2009 1548
-
(2009)
Drug Metab. Dispos.
, vol.37
, pp. 1548
-
-
Liu, X.1
Vilenski, O.2
Kwan, J.3
Apparsundaram, S.4
Weikert, R.5
-
28
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77954316464
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-
note
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i's >7.0) similar to DOV-216,303 and SERT selective based in buproprion augmentation trials.
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-
-
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32
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77954314992
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-
note
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3) δ 7.47 (d, J = 9.0 Hz, 1H), 7.27-7.17 (m, 4H), 7.13-7.07 (m, 2H), 7.16 (d, J = 3.1 Hz, 1H), 6.96 (dd, J = 9.0, 2.4 Hz, 1H), 6.56 (dd, J = 3.1, 0.8 Hz, 1H), 3.85-3.77 (m, 1H), 3.65-3.75 (br s, overlapping, 1H), 3.30-3.10 (m, 5H) 2.80-2.60 (br s, overlapping, 1H), 2.64-2.56 (m, 1H), 1.51 (br s, 9H), 0.93 (s, 9H), 0.63 (s, 3H), 0.60 (s, 3H).
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33
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77954310907
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Iyer, P.; Lucas, M. C.; Schoenfeld, R. C.; Villa, M.; Weikert, R. J. US 2007123527
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Iyer, P.; Lucas, M. C.; Schoenfeld, R. C.; Villa, M.; Weikert, R. J. US 2007123527.
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34
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77954310620
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-
note
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Clearance measured in HT format: total incubation volume 250 μL, 0.5 mg/mL human microsomal protein, reaction started by adding NADPH and performed at 37 °C with no shaking. 40 μL aliquots at four time points (0.1, 10, 20 and 30 min) were taken then the samples were transferred to 384 well plates for LC/MS analysis
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-
-
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35
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77954316510
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-
note
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Clearance measured in human liver microsomes (μL/min/mg): low stability >35, medium stability 35-6, high stability <6.5.
-
-
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37
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77954309205
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note
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The piperazine starting material (1-Boc-3-phenyl piperazine) for compound 17 was commercially available.
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38
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17744400080
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M. Berkheij, L. van der Sluis, C. Sewing, D.J. den Boer, J.W. Terpstra, H. Hiemstra, W.I.I. Bakker, A. van den Hoogenband, and J.H. van Maarseveen Tetrahedron Lett. 2005 2369
-
(2005)
Tetrahedron Lett.
, pp. 2369
-
-
Berkheij, M.1
Van Der Sluis, L.2
Sewing, C.3
Den Boer, D.J.4
Terpstra, J.W.5
Hiemstra, H.6
Bakker, W.I.I.7
Van Den Hoogenband, A.8
Van Maarseveen, J.H.9
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39
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77954312448
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-
note
-
CYP2D6 inhibition was measured in a fluorescence based assay where CYP marker substrates become fluorescent upon CYP metabolism.
-
-
-
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40
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77954316008
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note
-
(R)-2-Propylpiperazine and (S)-2-propylpiperazine were prepared from (R)-N-Boc-norvaline and (S)-N-Boc-norvaline, respectively by the method described in the following patent
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-
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41
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77954310309
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WO 03082877 A1
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WO 03082877 A1
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-
-
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42
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77954311862
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note
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(a) (R)-2-Propylpiperazine and (S)-2-propylpiperazine were prepared from (R)-N-Boc-norvaline and (S)-N-Boc-norvaline, respectively by the method described in the following patent; (b) WO 03082877 A1; (c) Both piperazines were Boc-protected and converted to the final compounds (S)-19 and (R)-19 by the method outlined in Scheme 1.
-
-
-
-
43
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77954310730
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-
note
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1/2 = 0.8 h, AUC = 182 ng-h/mL.
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-
-
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44
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77954313512
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-
note
-
The absolute configurations of (S)-19 and (R)-19 were tentatively assigned based on comparing data from (S)-19 and (R)-19.
-
-
-
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46
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16444377083
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S. Zhou, S.Y. Chan, B.C. Goh, E. Chan, W. Duan, M. Huang, and H.L. Mcleod Clin. Pharmacokinet. 44 2005 279
-
(2005)
Clin. Pharmacokinet.
, vol.44
, pp. 279
-
-
Zhou, S.1
Chan, S.Y.2
Goh, B.C.3
Chan, E.4
Duan, W.5
Huang, M.6
McLeod, H.L.7
-
48
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77954309243
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note
-
obs) and the data is plotted as a % of control (no inhibitor). In this manuscript 3A4 TDI is reported as a % of t = 12 min. Compounds with a greater rate of inactivation than verapamyl are categorized as high, while compounds with a rate less than ethynylestradiol are categorized as low.
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50
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77954311817
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Iyer, P.; Lin, C.; Lucas, M.; Lynch, S.; Madera, A. M.; Ozboya, K.; Schoenfeld, R.; Weikert, R. WO 2009153178
-
Iyer, P.; Lin, C.; Lucas, M.; Lynch, S.; Madera, A. M.; Ozboya, K.; Schoenfeld, R.; Weikert, R. WO 2009153178.
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