-
2
-
-
28444469759
-
-
For a recent review of new chemical entities, see
-
For a recent review of new chemical entities, see. Walter M.W. Drug Dev. Res. 65 (2005) 97
-
(2005)
Drug Dev. Res.
, vol.65
, pp. 97
-
-
Walter, M.W.1
-
4
-
-
1642293910
-
-
Hajos M., Fleishaker J.C., Filipiak-Reisner J.K., Brown M.T., and Wong E.H.F. CNS Drug Rev. 10 (2004) 23
-
(2004)
CNS Drug Rev.
, vol.10
, pp. 23
-
-
Hajos, M.1
Fleishaker, J.C.2
Filipiak-Reisner, J.K.3
Brown, M.T.4
Wong, E.H.F.5
-
5
-
-
33745727155
-
-
Fray M.J., Bish G., Brown A.D., Fish P.V., Stobie A., Wakenhut F., and Whitlock G.A. Bioorg. Med. Chem. Lett. 16 (2006) 4345
-
(2006)
Bioorg. Med. Chem. Lett.
, vol.16
, pp. 4345
-
-
Fray, M.J.1
Bish, G.2
Brown, A.D.3
Fish, P.V.4
Stobie, A.5
Wakenhut, F.6
Whitlock, G.A.7
-
6
-
-
33745781487
-
-
Fray M.J., Bish G., Fish P.V., Stobie A., Wakenhut F., and Whitlock G.A. Bioorg. Med. Chem. Lett. 16 (2006) 4349
-
(2006)
Bioorg. Med. Chem. Lett.
, vol.16
, pp. 4349
-
-
Fray, M.J.1
Bish, G.2
Fish, P.V.3
Stobie, A.4
Wakenhut, F.5
Whitlock, G.A.6
-
7
-
-
33847732615
-
-
Fish P.V., Fray M.J., Stobie A., Wakenhut F., and Whitlock G.A. Bioorg. Med. Chem. Lett. 17 (2007) 2022
-
(2007)
Bioorg. Med. Chem. Lett.
, vol.17
, pp. 2022
-
-
Fish, P.V.1
Fray, M.J.2
Stobie, A.3
Wakenhut, F.4
Whitlock, G.A.5
-
9
-
-
40749160241
-
-
Fish, P. V.; Mackenny, M. C.; Stobie, A.; Wakenhut, F.; Whitlock, G. A. WO Patent 105100, 2005.
-
Fish, P. V.; Mackenny, M. C.; Stobie, A.; Wakenhut, F.; Whitlock, G. A. WO Patent 105100, 2005.
-
-
-
-
10
-
-
40749105478
-
-
Adam, M. D.; Andrews, M. D.; Gymer, G. E.; Hepworth, D.; Howard, H. R., Jr.; Middleton, D. S.; Stobie, A. WO Patent 083643, 2002.
-
Adam, M. D.; Andrews, M. D.; Gymer, G. E.; Hepworth, D.; Howard, H. R., Jr.; Middleton, D. S.; Stobie, A. WO Patent 083643, 2002.
-
-
-
-
11
-
-
40749112514
-
-
Whitlock, G. A.; Fish, P. V.; Fray, M. J.; Stobie, A.; Wakenhut, F. Bioorg. Med. Chem. Lett., submitted for publication.
-
Whitlock, G. A.; Fish, P. V.; Fray, M. J.; Stobie, A.; Wakenhut, F. Bioorg. Med. Chem. Lett., submitted for publication.
-
-
-
-
13
-
-
40749115385
-
-
note
-
3 = OPh which was prepared as shown.{A figure is presented}
-
-
-
-
14
-
-
0036896304
-
-
Mahar Doan K.M., Humphreys J.E., Webster L.O., Wring S.A., Shampine L.J., Serabjit-Singh C.J., Adkison K.K., and Polli J.W. J. Pharmacol. Exp. Ther. 303 (2002) 1029
-
(2002)
J. Pharmacol. Exp. Ther.
, vol.303
, pp. 1029
-
-
Mahar Doan, K.M.1
Humphreys, J.E.2
Webster, L.O.3
Wring, S.A.4
Shampine, L.J.5
Serabjit-Singh, C.J.6
Adkison, K.K.7
Polli, J.W.8
-
15
-
-
33846363963
-
-
The Me group adjacent to the pyridine N atom was retained in all targets in order to reduce the liability of CYP450 inhibition. See
-
The Me group adjacent to the pyridine N atom was retained in all targets in order to reduce the liability of CYP450 inhibition. See. Blagg J. Annu. Rep. Med. Chem. 41 (2006) 353
-
(2006)
Annu. Rep. Med. Chem.
, vol.41
, pp. 353
-
-
Blagg, J.1
-
16
-
-
40749152063
-
-
note
-
3 (π): OMe (-0.02); OEt (0.38); Me (0.56); SMe (0.61); Cl (0.71); Et (1.02); i-Pr (1.53); n-Pr (1.55); OPh (2.08).
-
-
-
-
19
-
-
40749134333
-
-
Hughes, J. D.; Blagg, J.; Bailey, S.; De Crescenzo, G. A.; Dalvie, D.; Devraj, R. V.; Doubovetzky, M.; Ellsworth, E.; Fobian, Y. M.; Gibbs, M. E.; Gilles, R. W.; Grant, D.; Greene, N.; Huang, E.; Kreiger-Burke, T.; Lee, L.; Loesel, J.; Nahas, K.; Price, D. A.; Wager, T.; Whiteley, L.; Zhang, Y., Nat. Biotechnol., in press.
-
Hughes, J. D.; Blagg, J.; Bailey, S.; De Crescenzo, G. A.; Dalvie, D.; Devraj, R. V.; Doubovetzky, M.; Ellsworth, E.; Fobian, Y. M.; Gibbs, M. E.; Gilles, R. W.; Grant, D.; Greene, N.; Huang, E.; Kreiger-Burke, T.; Lee, L.; Loesel, J.; Nahas, K.; Price, D. A.; Wager, T.; Whiteley, L.; Zhang, Y., Nat. Biotechnol., in press.
-
-
-
-
20
-
-
40749137946
-
-
note
-
1/2 > 120 min.
-
-
-
-
21
-
-
33745958408
-
-
Deecher D.C., Beyer C.E., Johnston G., Bray J., Shah S., Abou-Gharbia M., and Andree T.H. J. Pharmacol. Exp. Ther. 318 (2006) 657
-
(2006)
J. Pharmacol. Exp. Ther.
, vol.318
, pp. 657
-
-
Deecher, D.C.1
Beyer, C.E.2
Johnston, G.3
Bray, J.4
Shah, S.5
Abou-Gharbia, M.6
Andree, T.H.7
-
22
-
-
40749127350
-
-
note
-
50 = 2.5 nM (n = 7).
-
-
-
-
23
-
-
40749111217
-
-
note
-
3H salt: mp 155 °C.
-
-
-
-
24
-
-
40749086963
-
-
note
-
There is a significant discrepancy between calculated c log P (4.4) and measured log P (3.2) values for 31. It is our hypothesis that 31 undergoes hydrophobic collapse to adopt a folded structure and so reduce the exposure of lipophilic faces.
-
-
-
|