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15
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65649120120
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P.J. Gilligan, T. Clarke, L. He, S. Lelas, Y.-W. Li, K. Heman, L. Fitzgerald, K. Miller, G. Zhang, A. Marshall, C. Krause, J.F. McElroy, K. Ward, K. Zeller, H. Wong, S. Bai, J. Saye, S. Grossman, R. Zaczek, P. Hartig, D. Robertson, and G. Trainor J. Med. Chem. 52 2009 3084
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Gilligan, P.J.1
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McElroy, J.F.12
Ward, K.13
Zeller, K.14
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Grossman, S.18
Zaczek, R.19
Hartig, P.20
Robertson, D.21
Trainor, G.22
more..
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16
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79953279095
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Gilligan, P. J. 4-(2-Butylamino)-2,7-dimethyl-8-(2-methyl-6-methoxypyrid- 3-yl)[1,5-a]-1,3,5-triazine, its enantiomers and pharmaceutically acceptable salts as a corticotropin releasing factor Receptor ligands, US 7157578 B2 (2007)
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Gilligan, P. J. 4-(2-Butylamino)-2,7-dimethyl-8-(2-methyl-6-methoxypyrid- 3-yl)[1,5-a]-1,3,5-triazine, its enantiomers and pharmaceutically acceptable salts as a corticotropin releasing factor Receptor ligands, US 7157578 B2 (2007).
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17
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79953283762
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2O (10%)/TFA (0.1%); starting% B, 0; final% B, 100; flow rate 5 mL/min; gradient time, 2 min; end time, 3 min.
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2O (10%)/TFA (0.1%); starting% B, 0; final% B, 100; flow rate 5 mL/min; gradient time, 2 min; end time, 3 min.
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19
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79953268191
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note
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125I-o-CRF (2200 Ci/mmol) was obtained from PerkinElmer Life Sciences, Inc. (Boston, MA).
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20
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79953274056
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note
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Shake-flask log D determination assay for lipophilicity: In a 250 mL separatory funnel were added 25 mM phosphate buffer (200 mL) and octanol (10 mL). The two-phase system was mixed well and let stand overnight to allow complete saturation and separation of both layers. A sample (1.0 mg) was dissolved in octanol (1 mL) and transferred to a volumetric flask, containing 50 mL of the phosphate buffer, saturated with octanol, as described above. The resulting mixture was shaken intensely for 30-40 min and was allowed to stand until two layers separated completely. A sample of each layer was analyzed by an HPLC method twice. The sample area counts were used to calculate the shake-flask log D.
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21
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79953280243
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note
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+).
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-
-
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22
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79953292773
-
-
note
-
2O (10%)/TFA (0.1%); starting% B, 30; final% B, 100; flow rate 25 mL/min; gradient time, 20 min; end time, 25 min.
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-
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23
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0007268871
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E.-L. Kämäräinen, T. Kyllönen, A. Airaksinen, C. Lundkvist, M. Yu, K. Ngren, J. Sandell, O. Langer, J. Vepsäläinen, J. Hiltunen, K. Bergström, S. Lötjönen, T. Jaakkola, and C. Halldin J. Labelled Compd. Radiopharm. 37 1995 55
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(1995)
J. Labelled Compd. Radiopharm.
, vol.37
, pp. 55
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Kämäräinen, E.-L.1
Kyllönen, T.2
Airaksinen, A.3
Lundkvist, C.4
Yu, M.5
Ngren, K.6
Sandell, J.7
Langer, O.8
Vepsäläinen, J.9
Hiltunen, J.10
Bergström, K.11
Lötjönen, S.12
Jaakkola, T.13
Halldin, C.14
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24
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79953286916
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The X-ray crystal structure of 18 was deposited with Cambridge Crystallographic Data Centre (deposition number - CCDC 810575)
-
The X-ray crystal structure of 18 was deposited with Cambridge Crystallographic Data Centre (deposition number - CCDC 810575).
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26
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79953275376
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The log D values of compounds 1-6 had not been reported and, therefore, were unavailable for comparison with the log D value of 7e
-
The log D values of compounds 1-6 had not been reported and, therefore, were unavailable for comparison with the log D value of 7e.
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