-
1
-
-
0030609068
-
-
Collo G., Neidhart S., Kawashima E., Kosco-Vibois M., North R.A., and Buell G. Neuropharmacology 36 (1997) 1277
-
(1997)
Neuropharmacology
, vol.36
, pp. 1277
-
-
Collo, G.1
Neidhart, S.2
Kawashima, E.3
Kosco-Vibois, M.4
North, R.A.5
Buell, G.6
-
5
-
-
33745737686
-
-
Gever J.R., Cockayne D.A., Dillon M.P., Burnstock G., and Ford A.P.D.W. Eur. J. Physiol. 452 (2006) 513
-
(2006)
Eur. J. Physiol.
, vol.452
, pp. 513
-
-
Gever, J.R.1
Cockayne, D.A.2
Dillon, M.P.3
Burnstock, G.4
Ford, A.P.D.W.5
-
7
-
-
43349107705
-
-
Romagnoli R., Baraldi P.G., Cruz-Lopez O., Lopez-Cara C., Preti D., Borea P.A., and Gessi S. Expert Opin. Ther. Targets 12 (2008) 647
-
(2008)
Expert Opin. Ther. Targets
, vol.12
, pp. 647
-
-
Romagnoli, R.1
Baraldi, P.G.2
Cruz-Lopez, O.3
Lopez-Cara, C.4
Preti, D.5
Borea, P.A.6
Gessi, S.7
-
8
-
-
66249138835
-
-
Guile S.D., Alcaraz L., Birkinshaw T.N., Bowers K.C., Ebden M.R., Furber M., and Stocks M.J. J. Med. Chem. 52 (2009) 3123
-
(2009)
J. Med. Chem.
, vol.52
, pp. 3123
-
-
Guile, S.D.1
Alcaraz, L.2
Birkinshaw, T.N.3
Bowers, K.C.4
Ebden, M.R.5
Furber, M.6
Stocks, M.J.7
-
9
-
-
0023796357
-
-
Buisman H.P., Steinberg T.H., Fischbarg J., Silverstein S.C., Vogelzang S.A., Ince C., Ypey D.L., and Leijh P.C. Proc. Natl. Acad. Sci. U.S.A. 85 (1988) 7988
-
(1988)
Proc. Natl. Acad. Sci. U.S.A.
, vol.85
, pp. 7988
-
-
Buisman, H.P.1
Steinberg, T.H.2
Fischbarg, J.3
Silverstein, S.C.4
Vogelzang, S.A.5
Ince, C.6
Ypey, D.L.7
Leijh, P.C.8
-
11
-
-
33646072818
-
-
Ferrari D., Pizzirani C., Adinolfi E., Lemoli R.M., Curti A., Idzko M., Panther E., and Di Virgilio F. J. Immunol. 176 (2006) 3877
-
(2006)
J. Immunol.
, vol.176
, pp. 3877
-
-
Ferrari, D.1
Pizzirani, C.2
Adinolfi, E.3
Lemoli, R.M.4
Curti, A.5
Idzko, M.6
Panther, E.7
Di Virgilio, F.8
-
13
-
-
0037440567
-
-
Duan S., Anderson C.M., Keung E.C., Chen Y., Chen Y., and Swanson R.A. J. Neurosci. 23 (2003) 1320
-
(2003)
J. Neurosci.
, vol.23
, pp. 1320
-
-
Duan, S.1
Anderson, C.M.2
Keung, E.C.3
Chen, Y.4
Chen, Y.5
Swanson, R.A.6
-
15
-
-
20144375454
-
-
Chessel I.P., Hatcher J.P., Bountra C., Michel A.D., Hughes J.P., Green P., Egerton J., Murfin M., Richardson J., Peck W.L., Grahames C.B.A., Casula M.A., Yiangou Y., Birch R., Anand P., and Buell G.N. Pain 114 (2005) 386
-
(2005)
Pain
, vol.114
, pp. 386
-
-
Chessel, I.P.1
Hatcher, J.P.2
Bountra, C.3
Michel, A.D.4
Hughes, J.P.5
Green, P.6
Egerton, J.7
Murfin, M.8
Richardson, J.9
Peck, W.L.10
Grahames, C.B.A.11
Casula, M.A.12
Yiangou, Y.13
Birch, R.14
Anand, P.15
Buell, G.N.16
-
16
-
-
33751165071
-
-
Honore P.M., Donnelly-Roberts D., Namovic M., Hsieh G., Zhu C., Mikusa J., Hernandez G., Zhong C., Gauvin D.M., Chandran P., Harris R., Medrano A.P., Carroll W., Marsh K., Sullivan J.P., Faltynek C.R., and Jarvis M.F. J. Pharmacol. Exp. Ther. 319 (2006) 1376
-
(2006)
J. Pharmacol. Exp. Ther.
, vol.319
, pp. 1376
-
-
Honore, P.M.1
Donnelly-Roberts, D.2
Namovic, M.3
Hsieh, G.4
Zhu, C.5
Mikusa, J.6
Hernandez, G.7
Zhong, C.8
Gauvin, D.M.9
Chandran, P.10
Harris, R.11
Medrano, A.P.12
Carroll, W.13
Marsh, K.14
Sullivan, J.P.15
Faltynek, C.R.16
Jarvis, M.F.17
-
17
-
-
57349085122
-
-
Broom D.C., Matson D.J., Bradshaw E., Buck M.E., Meade R., Coombs S., Matchett M., Ford K.K., Yu W., Yuan J., Sun S.H., Ochoa R., Krause J.E., Wustrow D.J., and Cortright D.N. J. Pharmacol. Exp. Ther. 327 (2008) 620
-
(2008)
J. Pharmacol. Exp. Ther.
, vol.327
, pp. 620
-
-
Broom, D.C.1
Matson, D.J.2
Bradshaw, E.3
Buck, M.E.4
Meade, R.5
Coombs, S.6
Matchett, M.7
Ford, K.K.8
Yu, W.9
Yuan, J.10
Sun, S.H.11
Ochoa, R.12
Krause, J.E.13
Wustrow, D.J.14
Cortright, D.N.15
-
18
-
-
66249113481
-
-
Perez-Medrano A., Donnelly-Roberts D.L., Honore P., Hsieh G.C., Namovic M.T., Peddi S., Shuai Q., Wang Y., Faltynek C.R., Jarvis M.F., and Carroll W.A. J. Med. Chem. 52 (2009) 3366
-
(2009)
J. Med. Chem.
, vol.52
, pp. 3366
-
-
Perez-Medrano, A.1
Donnelly-Roberts, D.L.2
Honore, P.3
Hsieh, G.C.4
Namovic, M.T.5
Peddi, S.6
Shuai, Q.7
Wang, Y.8
Faltynek, C.R.9
Jarvis, M.F.10
Carroll, W.A.11
-
19
-
-
33745142545
-
-
Nelson D.W., Gregg R.J., Kort M.E., Perez-Medrano A., Voight E.A., Wang Y., Grayson G., Namovic M.T., Donnelly-Roberts D.L., Niforatos W., Honore P., Jarvis M.F., Faltynek C.R., and Carroll W.A. J. Med. Chem. 49 (2006) 3659
-
(2006)
J. Med. Chem.
, vol.49
, pp. 3659
-
-
Nelson, D.W.1
Gregg, R.J.2
Kort, M.E.3
Perez-Medrano, A.4
Voight, E.A.5
Wang, Y.6
Grayson, G.7
Namovic, M.T.8
Donnelly-Roberts, D.L.9
Niforatos, W.10
Honore, P.11
Jarvis, M.F.12
Faltynek, C.R.13
Carroll, W.A.14
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77952108331
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Abst 2085
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McInnes, I. B.; Snell, N. J.; Perrett, J. H.; Parmar, H.; Wang, M. M.; Astbury, C. Arthritis Rheum [71st Annu Sci Meet Am Coll Rheumatol (Nov 6-11, Boston) 2007], 2007, 56 (9, Suppl.): Abst 2085.
-
Arthritis Rheum [71st Annu Sci Meet Am Coll Rheumatol (Nov 6-11, Boston) 2007], 2007, 56 (9, Suppl.)
-
-
McInnes, I.B.1
Snell, N.J.2
Perrett, J.H.3
Parmar, H.4
Wang, M.M.5
Astbury, C.6
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77952108399
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ClinicalTrial.gov Identifier: NCT00628095.
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ClinicalTrial.gov Identifier: NCT00628095.
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24
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67649962669
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The same concept was independently proposed by researchers at Pfizer and termed lipE:
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The same concept was independently proposed by researchers at Pfizer and termed lipE:. Ryckmans T., Edwards M.P., Horne V.A., Monica Correia A., Owen D.R., Thompson L.R., Tran I., Tutt M.F., and Young T. Bioorg. Med. Chem. Lett. 15 (2009) 4406
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(2009)
Bioorg. Med. Chem. Lett.
, vol.15
, pp. 4406
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-
Ryckmans, T.1
Edwards, M.P.2
Horne, V.A.3
Monica Correia, A.4
Owen, D.R.5
Thompson, L.R.6
Tran, I.7
Tutt, M.F.8
Young, T.9
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77952109618
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note
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max values of 100%. Full details of the assay protocol can be found in patent application WO 2007 141267 A1.
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26
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77952109415
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Compound 12 was prepared from commercial 3,5-dimethyl-1-phenyl-1H-pyrazole-4-carboxylic acid. Compound 13 was prepared from commercial [(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)methyl]amine. Compound 14 was prepared from commercial 3,5-dimethyl-1-phenyl-1H-pyrazol-4-amine. Compound 15 was prepared via cyclodehydration of an intermediate hydrazide.
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27
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77952105642
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note
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The preparation of compounds 16 and 17 is described in patent application WO 2008 138876 A1. Compound 18 was prepared via alkylation of commercial 3-phenyl-2,4-imidazolidinedione. Compounds 19-21 were prepared from commercially available acetic acids.
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77952103562
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The synthesis and optimisation of compound 22 will be described in a forthcoming publication.
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77952107173
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metasite v3.0, developed by Molecular Discovery, predicts metabolic transformations related to cytochrome-mediated reactions in phase I metabolism.
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31
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77952105715
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Calculated log D values were obtained using ACD Labs software v8.0.
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32
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77952106670
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All experiments were performed in accordance with the United Kingdom Animals (Scientific Procedures) Act, 1986 under Project Licence as well as under the review and approval of the GlaxoSmithKline Procedures Review Panel. GlaxoSmithKline safety regulations were adhered to at all times.
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