-
2
-
-
78649835003
-
-
Bhatt, H. G.; Agrawal, Y. K.; Raval, H. G.; Manna, K.; Desai, P. R. Mini-Rev. Med. Chem. 2010, 10, 1293;
-
(2010)
Mini-Rev. Med. Chem.
, vol.10
, pp. 1293
-
-
Bhatt, H.G.1
Agrawal, Y.K.2
Raval, H.G.3
Manna, K.4
Desai, P.R.5
-
3
-
-
70149117255
-
-
Engelhardt, H.; Smits, R. A.; Leurs, R.; Haaksma, E.; de Esch, I. J. P. Curr. Opin. Drug Discovery Dev. 2009, 12, 628.
-
(2009)
Curr. Opin. Drug Discovery Dev.
, vol.12
, pp. 628
-
-
Engelhardt, H.1
Smits, R.A.2
Leurs, R.3
Haaksma, E.4
De Esch, I.J.P.5
-
5
-
-
0141455895
-
-
Jablonowski, J. A.; Grice, C. A.; Chai, W.; Dvorak, C. A.; Venable, J. D.; Kwok, A. K.; Ly, K. S.; Wei, J.; Baker, S. M.; Desai, P. J.; Jiang, W.; Wilson, S. J.; Thurmond, R. L.; Karlsson, L.; Edwards, J. P.; Lovenberg, T. W.; Carruthers, N. I. J. Med. Chem. 2003, 46, 3957.
-
(2003)
J. Med. Chem.
, vol.46
, pp. 3957
-
-
Jablonowski, J.A.1
Grice, C.A.2
Chai, W.3
Dvorak, C.A.4
Venable, J.D.5
Kwok, A.K.6
Ly, K.S.7
Wei, J.8
Baker, S.M.9
Desai, P.J.10
Jiang, W.11
Wilson, S.J.12
Thurmond, R.L.13
Karlsson, L.14
Edwards, J.P.15
Lovenberg, T.W.16
Carruthers, N.I.17
-
6
-
-
33847712187
-
-
Zhang, M.; Thurmond, R. L.; Dunford, P. J. Pharmacol. Ther. 2007, 113, 594.
-
(2007)
J. Pharmacol. Ther.
, vol.113
, pp. 594
-
-
Zhang, M.1
Thurmond, R.L.2
Dunford, P.3
-
7
-
-
79953314978
-
-
Park, B. K.; Boobis, A.; Clarke, S.; Goldring, C. E. P.; Jones, D.; Kenna, J. G.; Lambert, C.; Laverty, H. G.; Naisbitt, D. J.; Nelson, S.; Nicoll-Griffith, D. A.; Obach, S.; Routledge, P.; Smith, D. A.; Tweedie, D. J.; Vermeulen, N.; Williams, D. P.; Wilson, I. D.; Baillie, T. A. Nat. Rev. Drug Disc. 2011, 10, 292.
-
(2011)
Nat. Rev. Drug Disc.
, vol.10
, pp. 292
-
-
Park, B.K.1
Boobis, A.2
Clarke, S.3
Goldring, C.E.P.4
Jones, D.5
Kenna, J.G.6
Lambert, C.7
Laverty, H.G.8
Naisbitt, D.J.9
Nelson, S.10
Nicoll-Griffith, D.A.11
Obach, S.12
Routledge, P.13
Smith, D.A.14
Tweedie, D.J.15
Vermeulen, N.16
Williams, D.P.17
Wilson, I.D.18
Baillie, T.A.19
-
8
-
-
1942453243
-
-
Hopkins, A. L.; Groom, C. R.; Alex, A. Drug Discovery Today 2004, 9, 430.
-
(2004)
Drug Discovery Today
, vol.9
, pp. 430
-
-
Hopkins, A.L.1
Groom, C.R.2
Alex, A.3
-
9
-
-
85030494263
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We first presented the work described in this paper at the Gordon Research Conference on Medicinal Chemistry at Colby-Sawyer College, New London, NH, USA, August 12, 2010 in a presentation by Charles E. Mowbray titled: 'The Discovery and Evaluation of PF-3893787: A Novel Histamine H4 Receptor Antagonist'. The compounds described in that presentation and this letter were first disclosed in patent applications
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We first presented the work described in this paper at the Gordon Research Conference on Medicinal Chemistry at Colby-Sawyer College, New London, NH, USA, August 12, 2010 in a presentation by Charles E. Mowbray titled: 'The Discovery and Evaluation of PF-3893787: A Novel Histamine H4 Receptor Antagonist'. The compounds described in that presentation and this letter were first disclosed in patent applications
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10
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85030488029
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Preparation of substituted 2,4- diaminopyrimidines as histamine H4 receptor ligands
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'Preparation of substituted 2,4- diaminopyrimidines as histamine H4 receptor ligands' Bell, A. S.; Lane, C. A. L.; Mowbray, C. E.; Selby, M. D.; Swain, N. A.; Williams, D. H. World Patent Application WO 2007072163
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World Patent Application WO 2007072163
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-
Bell, A.S.1
Lane, C.A.L.2
Mowbray, C.E.3
Selby, M.D.4
Swain, N.A.5
Williams, D.H.6
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11
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85030494378
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Preparation of octahydropyrrolo[3,4- c]pyrrole derivatives as histamine H4 receptor ligands, U.S. Patent Application US 2006111416. Since then a group from Johnson & Johnson has published an in vitro structure activity study 'Triamino pyrimidines and pyridines as histamine H4 receptor modulators'
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Preparation of octahydropyrrolo[3,4- c]pyrrole derivatives as histamine H4 receptor ligands' ane, C. A. L.; Price, D. A. U.S. Patent Application US 2006111416. Since then a group from Johnson & Johnson has published an in vitro structure activity study 'Triamino pyrimidines and pyridines as histamine H4 receptor modulators'
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Ane, C.A.L.1
Price, D.A.2
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12
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79955566558
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Meduna, S. P.; Savall, B. M; Cai, H.; Edwards, J. P.; Thurmond, R. L.; McGovern, P. M.; Bioorg. Med. Chem. Lett. 2011, 21, 3113.
-
(2011)
Bioorg. Med. Chem. Lett.
, vol.21
, pp. 3113
-
-
Meduna, S.P.1
Savall, B.M.2
Cai, H.3
Edwards, J.P.4
Thurmond, R.L.5
McGovern, P.M.6
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14
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85030496624
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Functional Ki values for antagonists were determined using HEK-293 cells expressing the full-length human H4R and a CRE-b-lactamase reporter gene. Antagonists reversed histamine inhibition of forskolin-stimulated cAMP. Detailed experimental details are provided in Ref. 7a
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Functional Ki values for antagonists were determined using HEK-293 cells expressing the full-length human H4R and a CRE-b-lactamase reporter gene. Antagonists reversed histamine inhibition of forskolin-stimulated cAMP. Detailed experimental details are provided in Ref. 7a.
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5344236080
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Other authors have independently explored the benzimidazole template
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Other authors have independently explored the benzimidazole template: (a) Terzioglu, N.; van Rijn, R. M.; Bakker, R. A.; De Esch, I. J. P.; Leurs, R. Bioorg. Med. Chem. Lett. 2004, 14, 5251;
-
(2004)
Bioorg. Med. Chem. Lett.
, vol.14
, pp. 5251
-
-
Terzioglu, N.1
Van Rijn, R.M.2
Bakker, R.A.3
De Esch, I.J.P.4
Leurs, R.5
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16
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29744441372
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Venable, J. D.; Cai, H.; Chai, W.; Dvorak, C. A.; Grice, C. A.; Jablonowski, J. A.; Shah, C. R.; Kwok, A. K.; Ly, K. S.; Pio, B.; Wei, J.; Desai, P. J.; Jiang, W.; Nguyen, S.; Ling, P.; Wilson, S. J.; Dunford, P. J.; Thurmond, R. L.; Lovenberg, T. W.; Karlsson, L.; Carruthers, N. I.; Edwards, J. P. J. Med. Chem. 2005, 48, 8289.
-
(2005)
J. Med. Chem.
, vol.48
, pp. 8289
-
-
Venable, J.D.1
Cai, H.2
Chai, W.3
Dvorak, C.A.4
Grice, C.A.5
Jablonowski, J.A.6
Shah, C.R.7
Kwok, A.K.8
Ly, K.S.9
Pio, B.10
Wei, J.11
Desai, P.J.12
Jiang, W.13
Nguyen, S.14
Ling, P.15
Wilson, S.J.16
Dunford, P.J.17
Thurmond, R.L.18
Lovenberg, T.W.19
Karlsson, L.20
Carruthers, N.I.21
Edwards, J.P.22
more..
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79959373790
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We have recently published further synthetic chemistry in this series: 'Synthesis of A Novel Octahydro Pyrrolo[3,4-c]Pyrrole Cyclic Amidine via 1,3- Dipolar Cycloaddition of Azomethine Ylides'
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We have recently published further synthetic chemistry in this series: 'Synthesis of A Novel Octahydro Pyrrolo[3,4-c]Pyrrole Cyclic Amidine via 1,3- Dipolar Cycloaddition of Azomethine Ylides' Paradowski, M.; Lane, C. AL.; Peakman, T. Synlett 2011, 1543.
-
Synlett
, vol.2011
, pp. 1543
-
-
Paradowski, M.1
Lane, C.A.L.2
Peakman, T.3
-
18
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-
0035953319
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(a) Van de Waterbeemd, H.; Smith, D. A.; Beaumont, K.; Walker, D. J. Med. Chem. 2001, 44, 1313;
-
(2001)
J. Med. Chem.
, vol.44
, pp. 1313
-
-
Van De Waterbeemd, H.1
Smith, D.A.2
Beaumont, K.3
Walker, D.4
-
19
-
-
0035289779
-
-
Lipinski, C. A.; Lombardo, F.; Dominy, B. W.; Feeney, P. J. Adv. Drug Delivery Rev. 2001, 46, 3.
-
(2001)
J. Adv. Drug Delivery Rev.
, vol.46
, pp. 3
-
-
Lipinski, C.A.1
Lombardo, F.2
Dominy, B.W.3
Feeney, P.4
-
20
-
-
68149160053
-
-
Price, D. A.; Blagg, J.; Jones, L.; Greene, N.; Wager, T. Expert Opin. Drug Metab. Toxicol. 2009, 5, 921;
-
(2009)
Expert Opin. Drug Metab. Toxicol.
, vol.5
, pp. 921
-
-
Price, D.A.1
Blagg, J.2
Jones, L.3
Greene, N.4
Wager, T.5
-
21
-
-
1842525842
-
-
Ploemen, J.-P. H. T. M.; Kelder, J.; Hafmans, T.; van de Sandt, H.; van Burgsteden, J. A.; Salemink, P. J. M.; van Esch, E. Exp. Toxicol. Pathol. 2004, 55, 347.
-
(2004)
Exp. Toxicol. Pathol.
, vol.55
, pp. 347
-
-
Ploemen, J.-P.H.T.M.1
Kelder, J.2
Hafmans, T.3
Van De Sandt, H.4
Van Burgsteden, J.A.5
Salemink, P.J.M.6
Van Esch, E.7
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85030493782
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A 7-day oral in vivo toleration study in rats achieved up to a free Cmax 197x projected human Cmin (10-15 nM) which represents 240x rat binding Ki. There was no evidence of toxicity. Similarly a 7-day oral in vivo toleration study in dogs achieved up to a free Cmax 187x the projected human Cmin (10-15 nM) which represents 1.7x dog binding Ki. There was no evidence of toxicit.y
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A 7-day oral in vivo toleration study in rats achieved up to a free Cmax 197x projected human Cmin (10-15 nM) which represents 240x rat binding Ki. There was no evidence of toxicity. Similarly a 7-day oral in vivo toleration study in dogs achieved up to a free Cmax 187x the projected human Cmin (10-15 nM) which represents 1.7x dog binding Ki. There was no evidence of toxicity.
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42049099229
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Barnard, R.; Barnard, A.; Salmon, G.; Liu, W.; Sreckovic, S. Cytometry 2008, 73A, 299.
-
(2008)
Cytometry
, vol.73 A
, pp. 299
-
-
Barnard, R.1
Barnard, A.2
Salmon, G.3
Liu, W.4
Sreckovic, S.5
-
25
-
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0034802259
-
-
Liu, C.; Wilson, S. J.; Kuei, C.; Lovenberg, T. W. J. Pharmacol. Exp. Ther. 2001, 299, 121.
-
(2001)
J. Pharmacol. Exp. Ther.
, vol.299
, pp. 121
-
-
Liu, C.1
Wilson, S.J.2
Kuei, C.3
Lovenberg, T.W.4
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77951033264
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Lim, H. D.; de Graaf, C.; Jiang, W.; Sadek, P.; McGovern, P. M.; Istyastono, E. P.; Bakker, R. A.; de Esch, I. J. P.; Thurmond, R. L.; Leurs, R. Mol. Pharmacol. 2010, 77, 734.
-
(2010)
Mol. Pharmacol.
, vol.77
, pp. 734
-
-
Lim, H.D.1
De Graaf, C.2
Jiang, W.3
Sadek, P.4
McGovern, P.M.5
Istyastono, E.P.6
Bakker, R.A.7
De Esch, I.J.P.8
Thurmond, R.L.9
Leurs, R.10
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27
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79953019023
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Seifert, R.; Schneider, E. H.; Dove, S.; Brunskole, I.; Neumann, D.; Strasser, A.; Buschauer, A. Mol. Pharmacol. 2011, 79, 631.
-
(2011)
Mol. Pharmacol.
, vol.79
, pp. 631
-
-
Seifert, R.1
Schneider, E.H.2
Dove, S.3
Brunskole, I.4
Neumann, D.5
Strasser, A.6
Buschauer, A.7
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78449298129
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H4 receptor agonists have recently been reviewed
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H4 receptor agonists have recently been reviewed: Igel, P.; Dove, S.; Buschauer, A. Bioorg. Med. Chem. Lett. 2010, 20, 7191;
-
(2010)
Bioorg. Med. Chem. Lett.
, vol.20
, pp. 7191
-
-
Igel, P.1
Dove, S.2
Buschauer, A.3
-
29
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79952977834
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'Molecular Determinants of Selective Agonist and Antagonist Binding to the Histamine H4 Receptor' have also recently been described
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'Molecular Determinants of Selective Agonist and Antagonist Binding to the Histamine H4 Receptor' have also recently been described: Istyastano, E. P.; de Graaf, C.; de Esch, I. J. P.; Leurs, R. Curr. Top. Med. Chem. 2011, 11, 661.
-
(2011)
Curr. Top. Med. Chem.
, vol.11
, pp. 661
-
-
Istyastano, E.P.1
De Graaf, C.2
De Esch, I.J.P.3
Leurs, R.4
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A recent report described benzimidazole oximes as H4R agonists
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A recent report described benzimidazole oximes as H4R agonists: Yu, F.; Wolin, R. L.; Wei, J.; Desai, P. J.; McGovern, P. M.; Dunford, P. J.; Karlsson, L.; Thurmond, R. L. J. Recept. Ligand Channel Res. 2010, 3, 37.
-
(2010)
J. Recept. Ligand Channel Res.
, vol.3
, pp. 37
-
-
Yu, F.1
Wolin, R.L.2
Wei, J.3
Desai, P.J.4
McGovern, P.M.5
Dunford, P.J.6
Karlsson, L.7
Thurmond, R.L.8
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