-
1
-
-
0035862329
-
2 selectively induces chemotaxis in T helper type 2 cells, eosinophils, and basophils via seven-transmembrane receptor CRTH2
-
2 selectively induces chemotaxis in T helper type 2 cells, eosinophils, and basophils via seven-transmembrane receptor CRTH2 J. Exp. Med. 2001, 193, 255-261
-
(2001)
J. Exp. Med.
, vol.193
, pp. 255-261
-
-
Hirai, H.1
Tanaka, K.2
Yoshie, O.3
Ogawa, K.4
Kenmotsu, K.5
Takamori, Y.6
Ichimasa, M.7
Sugamura, K.8
Nakamura, M.9
Takano, S.10
Nagata, K.11
-
3
-
-
77958503296
-
Novel CRTH2 antagonists: A review of patents from 2006 to 2009
-
Ulven, T.; Kostenis, E. Novel CRTH2 antagonists: A review of patents from 2006 to 2009 Expert Opin. Ther. Pat. 2010, 20, 1505-1530
-
(2010)
Expert Opin. Ther. Pat.
, vol.20
, pp. 1505-1530
-
-
Ulven, T.1
Kostenis, E.2
-
4
-
-
77954725559
-
2 receptor antagonists in development
-
2 receptor antagonists in development Expert Opin. Invest. Drugs 2010, 19, 947-961
-
(2010)
Expert Opin. Invest. Drugs
, vol.19
, pp. 947-961
-
-
Norman, P.1
-
5
-
-
79951633728
-
Prostaglandin D receptor CRTH2 antagonists for the treatment of inflammatory diseases
-
Chen, J. J.; Budelsky, A. L. Prostaglandin D receptor CRTH2 antagonists for the treatment of inflammatory diseases Prog. Med. Chem. 2011, 50, 49-107
-
(2011)
Prog. Med. Chem.
, vol.50
, pp. 49-107
-
-
Chen, J.J.1
Budelsky, A.L.2
-
6
-
-
0033083112
-
Selective expression of a novel surface molecule by human Th2 cells in vivo
-
Nagata, K.; Tanaka, K.; Ogawa, K.; Kemmotsu, K.; Imai, T.; Yoshie, O.; Abe, H.; Tada, K.; Nakamura, M.; Sugamura, K.; Takano, S. Selective expression of a novel surface molecule by human Th2 cells in vivo J. Immunol. 1999, 162, 1278-1286
-
(1999)
J. Immunol.
, vol.162
, pp. 1278-1286
-
-
Nagata, K.1
Tanaka, K.2
Ogawa, K.3
Kemmotsu, K.4
Imai, T.5
Yoshie, O.6
Abe, H.7
Tada, K.8
Nakamura, M.9
Sugamura, K.10
Takano, S.11
-
7
-
-
33750005155
-
A dominant role for chemoattractant receptor-homologous molecule expressed on T helper type 2 (Th2) cells (CRTH2) in mediating chemotaxis of CRTH2+ CD4+ Th2 lymphocytes in response to mast cell supernatants
-
Gyles, S. L.; Xue, L.; Townsend, E. R.; Wettey, F.; Pettipher, R. A dominant role for chemoattractant receptor-homologous molecule expressed on T helper type 2 (Th2) cells (CRTH2) in mediating chemotaxis of CRTH2+ CD4+ Th2 lymphocytes in response to mast cell supernatants Immunology 2006, 119, 362-368
-
(2006)
Immunology
, vol.119
, pp. 362-368
-
-
Gyles, S.L.1
Xue, L.2
Townsend, E.R.3
Wettey, F.4
Pettipher, R.5
-
8
-
-
61849171197
-
Interaction between prostaglandin D and chemoattractant receptor-homologous molecule expressed on Th2 cells mediates cytokine production by Th2 lymphocytes in response to activated mast cells
-
Xue, L.; Barrow, A.; Pettipher, R. Interaction between prostaglandin D and chemoattractant receptor-homologous molecule expressed on Th2 cells mediates cytokine production by Th2 lymphocytes in response to activated mast cells Clin. Exp. Immunol. 2009, 156, 126-133
-
(2009)
Clin. Exp. Immunol.
, vol.156
, pp. 126-133
-
-
Xue, L.1
Barrow, A.2
Pettipher, R.3
-
9
-
-
76249084143
-
2 released from IgE/anti-IgE treated nasal polyp tissue
-
2 released from IgE/anti-IgE treated nasal polyp tissue Allergy 2009, 65, 304-310
-
(2009)
Allergy
, vol.65
, pp. 304-310
-
-
Perez-Novo, C.A.1
Holtappels, G.2
Vinall, S.L.3
Xue, L.4
Zhang, N.5
Bachert, C.6
Pettipher, R.7
-
10
-
-
33746923091
-
2 plays an essential role in chronic allergic inflammation of the skin via CRTH2 receptor
-
2 plays an essential role in chronic allergic inflammation of the skin via CRTH2 receptor J. Immunol. 2006, 177, 2621-2629
-
(2006)
J. Immunol.
, vol.177
, pp. 2621-2629
-
-
Satoh, T.1
Moroi, R.2
Aritake, K.3
Urade, Y.4
Kanai, Y.5
Sumi, K.6
Yokozeki, H.7
Hirai, H.8
Nagata, K.9
Hara, T.10
Utsuyama, M.11
Hirokawa, K.12
Sugamura, K.13
Nishioka, K.14
Nakamura, M.15
-
11
-
-
45949101464
-
CRTH2 plays an essential role in the pathophysiology of Cry j 1-induced pollinosis in mice
-
Nomiya, R.; Okano, M.; Fujiwara, T.; Maeda, M.; Kimura, Y.; Kino, K.; Yokoyama, M.; Hirai, H.; Nagata, K.; Hara, T.; Nishizaki, K.; Nakamura, M. CRTH2 plays an essential role in the pathophysiology of Cry j 1-induced pollinosis in mice J. Immunol. 2008, 180, 5680-5688
-
(2008)
J. Immunol.
, vol.180
, pp. 5680-5688
-
-
Nomiya, R.1
Okano, M.2
Fujiwara, T.3
Maeda, M.4
Kimura, Y.5
Kino, K.6
Yokoyama, M.7
Hirai, H.8
Nagata, K.9
Hara, T.10
Nishizaki, K.11
Nakamura, M.12
-
12
-
-
69249240524
-
2 receptor CRTH2 attenuates asthma pathology in mouse eosinophilic airway inflammation
-
2 receptor CRTH2 attenuates asthma pathology in mouse eosinophilic airway inflammation Respir. Res. 2007, 8, 16
-
(2007)
Respir. Res.
, vol.8
, pp. 16
-
-
Uller, L.1
Mathiesen, J.M.2
Alenmyr, L.3
Korsgren, M.4
Ulven, T.5
Hogberg, T.6
Andersson, G.7
Persson, C.G.8
Kostenis, E.9
-
13
-
-
57049141701
-
CRTH2 antagonism significantly ameliorates airway hyperreactivity and downregulates inflammation-induced genes in a mouse model of airway inflammation
-
Lukacs, N. W.; Berlin, A. A.; Franz-Bacon, K.; Sasik, R.; Sprague, L. J.; Ly, T. W.; Hardiman, G.; Boehme, S. A.; Bacon, K. B. CRTH2 antagonism significantly ameliorates airway hyperreactivity and downregulates inflammation-induced genes in a mouse model of airway inflammation Am. J. Physiol. Lung Cell Mol. Physiol. 2008, 295, L767-L779
-
(2008)
Am. J. Physiol. Lung Cell Mol. Physiol.
, vol.295
-
-
Lukacs, N.W.1
Berlin, A.A.2
Franz-Bacon, K.3
Sasik, R.4
Sprague, L.J.5
Ly, T.W.6
Hardiman, G.7
Boehme, S.A.8
Bacon, K.B.9
-
14
-
-
40349108550
-
1 and CRTH2 in promoting allergic responses
-
1 and CRTH2 in promoting allergic responses Br. J. Pharmacol. 2008, 153 (Suppl 1) S191-S199
-
(2008)
Br. J. Pharmacol.
, vol.153
, Issue.SUPPL. 1
-
-
Pettipher, R.1
-
15
-
-
67649158208
-
Novel function of CRTH2 in preventing apoptosis of human Th2 cells through activation of the phosphatidylinositol 3-kinase pathway
-
Xue, L.; Barrow, A.; Pettipher, R. Novel function of CRTH2 in preventing apoptosis of human Th2 cells through activation of the phosphatidylinositol 3-kinase pathway J. Immunol. 2009, 182, 7580-7586
-
(2009)
J. Immunol.
, vol.182
, pp. 7580-7586
-
-
Xue, L.1
Barrow, A.2
Pettipher, R.3
-
16
-
-
84655167630
-
A randomized, double-blind, placebo-controlled study of the CRTH2 antagonist OC000459 in moderate persistent asthma
-
Barnes, N.; Pavord, I.; Chuchalin, A.; Bell, J.; Hunter, M.; Lewis, T.; Parker, D.; Payton, M.; Collins, L. P.; Pettipher, R.; Steiner, J.; Perkins, C. M. A randomized, double-blind, placebo-controlled study of the CRTH2 antagonist OC000459 in moderate persistent asthma Clin. Exp. Allergy 2012, 42, 38-48
-
(2012)
Clin. Exp. Allergy
, vol.42
, pp. 38-48
-
-
Barnes, N.1
Pavord, I.2
Chuchalin, A.3
Bell, J.4
Hunter, M.5
Lewis, T.6
Parker, D.7
Payton, M.8
Collins, L.P.9
Pettipher, R.10
Steiner, J.11
Perkins, C.M.12
-
17
-
-
13944263887
-
Minor structural modifications convert the dual TP/CRTH2 antagonist ramatroban into a highly selective and potent CRTH2 antagonist
-
Ulven, T.; Kostenis, E. Minor structural modifications convert the dual TP/CRTH2 antagonist ramatroban into a highly selective and potent CRTH2 antagonist J. Med. Chem. 2005, 48, 897-900
-
(2005)
J. Med. Chem.
, vol.48
, pp. 897-900
-
-
Ulven, T.1
Kostenis, E.2
-
19
-
-
34548830702
-
2 receptor CRTH2
-
2 receptor CRTH2 Bioorg. Med. Chem. Lett. 2007, 17, 5924-5927
-
(2007)
Bioorg. Med. Chem. Lett.
, vol.17
, pp. 5924-5927
-
-
Ulven, T.1
Gallen, M.J.2
Nielsen, M.C.3
Merten, N.4
Schmidt, C.5
Mohr, K.6
Trainkle, C.7
Kostenis, E.8
-
21
-
-
67651120073
-
2 with efficacy in a murine model of allergic rhinitis
-
2 with efficacy in a murine model of allergic rhinitis Bioorg. Med. Chem. Lett. 2009, 19, 4647-4651
-
(2009)
Bioorg. Med. Chem. Lett.
, vol.19
, pp. 4647-4651
-
-
Stearns, B.A.1
Baccei, C.2
Bain, G.3
Broadhead, A.4
Clark, R.C.5
Coate, H.6
Evans, J.F.7
Fagan, P.8
Hutchinson, J.H.9
King, C.10
Lee, C.11
Lorrain, D.S.12
Prasit, P.13
Prodanovich, P.14
Santini, A.15
Scott, J.M.16
Stock, N.S.17
Truong, Y.P.18
-
22
-
-
78651341515
-
Pharmacological characterization of MK-7246, a potent and selective CRTH2 (chemoattractant receptor-homologous molecule expressed on T-helper type 2 cells) antagonist
-
Gervais, F. G.; Sawyer, N.; Stocco, R.; Hamel, M.; Krawczyk, C.; Sillaots, S.; Denis, D.; Wong, E.; Wang, Z.; Gallant, M.; Abraham, W. M.; Slipetz, D.; Crackower, M. A.; O'Neill, G. P. Pharmacological characterization of MK-7246, a potent and selective CRTH2 (chemoattractant receptor-homologous molecule expressed on T-helper type 2 cells) antagonist Mol. Pharmacol. 2011, 79, 69-76
-
(2011)
Mol. Pharmacol.
, vol.79
, pp. 69-76
-
-
Gervais, F.G.1
Sawyer, N.2
Stocco, R.3
Hamel, M.4
Krawczyk, C.5
Sillaots, S.6
Denis, D.7
Wong, E.8
Wang, Z.9
Gallant, M.10
Abraham, W.M.11
Slipetz, D.12
Crackower, M.A.13
O'Neill, G.P.14
-
23
-
-
78650509769
-
Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases
-
Gallant, M.; Beaulieu, C.; Berthelette, C.; Colucci, J.; Crackower, M. A.; Dalton, C.; Denis, D.; Ducharme, Y.; Friesen, R. W.; Guay, D.; Gervais, F. G.; Hamel, M.; Houle, R.; Krawczyk, C. M.; Kosjek, B.; Lau, S.; Leblanc, Y.; Lee, E. E.; Levesque, J. F.; Mellon, C.; Molinaro, C.; Mullet, W.; O'Neill, G. P.; O'Shea, P.; Sawyer, N.; Sillaots, S.; Simard, D.; Slipetz, D.; Stocco, R.; Sorensen, D.; Truong, V. L.; Wong, E.; Wu, J.; Zaghdane, H.; Wang, Z. Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases Bioorg. Med. Chem. Lett. 2011, 21, 288-293
-
(2011)
Bioorg. Med. Chem. Lett.
, vol.21
, pp. 288-293
-
-
Gallant, M.1
Beaulieu, C.2
Berthelette, C.3
Colucci, J.4
Crackower, M.A.5
Dalton, C.6
Denis, D.7
Ducharme, Y.8
Friesen, R.W.9
Guay, D.10
Gervais, F.G.11
Hamel, M.12
Houle, R.13
Krawczyk, C.M.14
Kosjek, B.15
Lau, S.16
Leblanc, Y.17
Lee, E.E.18
Levesque, J.F.19
Mellon, C.20
Molinaro, C.21
Mullet, W.22
O'Neill, G.P.23
O'Shea, P.24
Sawyer, N.25
Sillaots, S.26
Simard, D.27
Slipetz, D.28
Stocco, R.29
Sorensen, D.30
Truong, V.L.31
Wong, E.32
Wu, J.33
Zaghdane, H.34
Wang, Z.35
more..
-
24
-
-
78649892557
-
Practical and efficient synthesis of N-fused tricyclic indoles
-
Koay, N.; Tonelli, D. L.; Truong, V. L. Practical and efficient synthesis of N-fused tricyclic indoles Tetrahedron Lett. 2011, 52, 122-124
-
(2011)
Tetrahedron Lett.
, vol.52
, pp. 122-124
-
-
Koay, N.1
Tonelli, D.L.2
Truong, V.L.3
-
25
-
-
79956159758
-
New indole amide derivatives as potent CRTH2 receptor antagonists
-
Zaghdane, H.; Boyd, M.; Colucci, J.; Simard, D.; Berthelette, C.; Leblanc, Y.; Wang, Z.; Houle, R.; Lévesque, J. F.; Molinaro, C.; Hamel, M.; Stocco, R.; Sawyer, N.; Sillaots, S.; Gervais, F.; Gallant, M. New indole amide derivatives as potent CRTH2 receptor antagonists Bioorg. Med. Chem. Lett. 2011, 21, 3471-3474
-
(2011)
Bioorg. Med. Chem. Lett.
, vol.21
, pp. 3471-3474
-
-
Zaghdane, H.1
Boyd, M.2
Colucci, J.3
Simard, D.4
Berthelette, C.5
Leblanc, Y.6
Wang, Z.7
Houle, R.8
Lévesque, J.F.9
Molinaro, C.10
Hamel, M.11
Stocco, R.12
Sawyer, N.13
Sillaots, S.14
Gervais, F.15
Gallant, M.16
-
26
-
-
34247893955
-
2 receptor 1 antagonists: Impacts of glutathione trapping and glucuronide conjugation on covalent binding
-
2 receptor 1 antagonists: Impacts of glutathione trapping and glucuronide conjugation on covalent binding Bioorg. Med. Chem. Lett. 2007, 17, 3038-3043
-
(2007)
Bioorg. Med. Chem. Lett.
, vol.17
, pp. 3038-3043
-
-
Lévesque, J.F.1
Day, S.H.2
Chauret, N.3
Seto, C.4
Trimble, L.5
Bateman, K.P.6
Silva, J.M.7
Berthelette, C.8
Lachance, N.9
Boyd, M.10
Li, L.11
Sturino, C.F.12
Wang, Z.13
Zamboni, R.14
Young, R.N.15
Nicoll-Griffith, D.A.16
-
27
-
-
78651233023
-
Azaindoles as potent CRTH2 receptor antagonists
-
Simard, D.; Leblanc, Y.; Berthelette, C.; Zaghdane, M. H.; Molinaro, C.; Wang, Z.; Gallant, M.; Lau, S.; Thao, T.; Hamel, M.; Stocco, R.; Sawyer, N.; Sillaots, S.; Gervais, F.; Houle, R.; Lévesque, J. F. Azaindoles as potent CRTH2 receptor antagonists Bioorg. Med. Chem. Lett. 2011, 21, 841-845
-
(2011)
Bioorg. Med. Chem. Lett.
, vol.21
, pp. 841-845
-
-
Simard, D.1
Leblanc, Y.2
Berthelette, C.3
Zaghdane, M.H.4
Molinaro, C.5
Wang, Z.6
Gallant, M.7
Lau, S.8
Thao, T.9
Hamel, M.10
Stocco, R.11
Sawyer, N.12
Sillaots, S.13
Gervais, F.14
Houle, R.15
Lévesque, J.F.16
-
29
-
-
77958469339
-
-
(Actelion). PCT Int. Appl. WO2006070325.
-
Fecher, A.; Fretz, H.; Riederer, M. (Actelion) 2,3,4,9- Tetrahydrocarbazole derivatives as CRTH2 receptor antagonists. PCT Int. Appl. WO2006070325, 2006.
-
(2006)
2,3,4,9-Tetrahydrocarbazole Derivatives As CRTH2 Receptor Antagonists
-
-
Fecher, A.1
Fretz, H.2
Riederer, M.3
-
30
-
-
84859797318
-
-
(Actelion). PCT Int. Appl. WO2008017989.
-
Fretz, H.; Fecher, A.; Pothier, J.; Risch, P. (Actelion) 3-Amino-1,2,3,4-tetrahydro-9H-carbazol-9-yl)acetic acid derivatives. PCT Int. Appl. WO2008017989, 2008.
-
(2008)
3-Amino-1,2,3,4-tetrahydro-9H-carbazol-9-yl)acetic Acid Derivatives
-
-
Fretz, H.1
Fecher, A.2
Pothier, J.3
Risch, P.4
-
31
-
-
0036467346
-
2 receptor, CRTH2
-
2 receptor, CRTH2 J. Immunol. 2002, 168, 981-985
-
(2002)
J. Immunol.
, vol.168
, pp. 981-985
-
-
Hirai, H.1
Tanaka, K.2
Takano, S.3
Ichimasa, M.4
Nakamura, M.5
Nagata, K.6
-
32
-
-
0036944934
-
2 receptor, CRTH2
-
2 receptor, CRTH2 Br. J. Pharmacol. 2002, 137, 1163-1172
-
(2002)
Br. J. Pharmacol.
, vol.137
, pp. 1163-1172
-
-
Sawyer, N.1
Cauchon, E.2
Chateauneuf, A.3
Cruz, R.P.4
Nicholson, D.W.5
Metters, K.M.6
O'Neill, G.P.7
Gervais, F.G.8
-
33
-
-
13844294096
-
2 is a potent and selective CRTH2 receptor agonist and causes activation of human eosinophils and Th2 lymphocytes
-
2 is a potent and selective CRTH2 receptor agonist and causes activation of human eosinophils and Th2 lymphocytes Prostaglandins Other Lipid Mediat. 2005, 75, 153-167
-
(2005)
Prostaglandins Other Lipid Mediat.
, vol.75
, pp. 153-167
-
-
Gazi, L.1
Gyles, S.2
Rose, J.3
Lees, S.4
Allan, C.5
Xue, L.6
Jassal, R.7
Speight, G.8
Gamble, V.9
Pettipher, R.10
-
35
-
-
26444568206
-
2 receptor CRTH2
-
2 receptor CRTH2 J. Med. Chem. 2005, 48, 6174-6177
-
(2005)
J. Med. Chem.
, vol.48
, pp. 6174-6177
-
-
Armer, R.E.1
Ashton, M.R.2
Boyd, E.A.3
Brennan, C.J.4
Brookfield, F.A.5
Gazi, L.6
Gyles, S.L.7
Hay, P.A.8
Hunter, M.G.9
Middlemiss, D.10
Whittaker, M.11
Xue, L.12
Pettipher, R.13
-
36
-
-
22944479010
-
A physiocogenetic method to assign ligand-binding relationships between 7TM receptors
-
Frimurer, T. M.; Ulven, T.; Elling, C. E.; Gerlach, L.-O.; Kostenis, E.; HoIgberg, T. A physiocogenetic method to assign ligand-binding relationships between 7TM receptors Bioorg. Med. Chem. Lett. 2005, 15, 3707-3712
-
(2005)
Bioorg. Med. Chem. Lett.
, vol.15
, pp. 3707-3712
-
-
Frimurer, T.M.1
Ulven, T.2
Elling, C.E.3
Gerlach, L.-O.4
Kostenis, E.5
Hoigberg, T.6
-
37
-
-
33745813184
-
2) receptor antagonists
-
2) receptor antagonists Bioorg. Med. Chem. Lett. 2006, 16, 4287-4290
-
(2006)
Bioorg. Med. Chem. Lett.
, vol.16
, pp. 4287-4290
-
-
Birkinshaw, T.N.1
Teague, S.J.2
Beech, C.3
Bonnert, R.V.4
Hill, S.5
Patel, A.6
Reakes, S.7
Sanganee, H.8
Dougall, I.G.9
Phillips, T.T.10
Salter, S.11
Schmidt, J.12
Arrowsmith, E.C.13
Carrillo, J.J.14
Bell, F.M.15
Paine, S.W.16
Weaver, R.17
-
38
-
-
80255125988
-
N-Arylation of a hindered indoline as a route to 2-(2-methyl-1-(4-oxo-3, 4-dihydrophthalazin-1-yl)-1H-indol-3-yl)acetic acid derivatives
-
Papaioannou, N.; Marathias, V.; Wan, Z.-K.; Kaila, N.; Ali, Z.; Saiah, E. N-Arylation of a hindered indoline as a route to 2-(2-methyl-1-(4-oxo-3,4- dihydrophthalazin-1-yl)-1H-indol-3-yl)acetic acid derivatives Tetrahedron Lett. 2011, 52, 6317-6320
-
(2011)
Tetrahedron Lett.
, vol.52
, pp. 6317-6320
-
-
Papaioannou, N.1
Marathias, V.2
Wan, Z.-K.3
Kaila, N.4
Ali, Z.5
Saiah, E.6
-
39
-
-
33746648806
-
-
(Oxagen). PCT Int. Appl. WO2005044260.
-
Middlemiss, D.; Ashton, M. R.; Boyd, E. A.; Brookfield, F. A.; Pettipher, E. R. (Oxagen) Use of CRTH2 antagonist compounds in therapy. PCT Int. Appl. WO2005044260, 2005.
-
(2005)
Use of CRTH2 Antagonist Compounds in Therapy
-
-
Middlemiss, D.1
Ashton, M.R.2
Boyd, E.A.3
Brookfield, F.A.4
Pettipher, E.R.5
-
42
-
-
80054786311
-
Substituted indole-1-acetic acids as potent and selective CRTh2 antagonists-discovery of AZD1981
-
Luker, T.; Bonnert, R.; Brough, S.; Cook, A. R.; Dickinson, M. R.; Dougall, I.; Logan, C.; Mohammed, R. T.; Paine, S.; Sanganee, H. J.; Sargent, C.; Schmidt, J. A.; Teague, S.; Thom, S. Substituted indole-1-acetic acids as potent and selective CRTh2 antagonists-discovery of AZD1981 Bioorg. Med. Chem. Lett. 2011, 21, 6288-6292
-
(2011)
Bioorg. Med. Chem. Lett.
, vol.21
, pp. 6288-6292
-
-
Luker, T.1
Bonnert, R.2
Brough, S.3
Cook, A.R.4
Dickinson, M.R.5
Dougall, I.6
Logan, C.7
Mohammed, R.T.8
Paine, S.9
Sanganee, H.J.10
Sargent, C.11
Schmidt, J.A.12
Teague, S.13
Thom, S.14
-
43
-
-
41849141562
-
2) receptor antagonists for the treatment of allergic inflammatory diseases
-
2) receptor antagonists for the treatment of allergic inflammatory diseases J. Med. Chem. 2008, 51, 2227-2243
-
(2008)
J. Med. Chem.
, vol.51
, pp. 2227-2243
-
-
Crosignani, S.1
Page, P.2
Missotten, M.3
Colovray, V.4
Cleva, C.5
Arrighi, J.F.6
Atherall, J.7
MacRitchie, J.8
Martin, T.9
Humbert, Y.10
Gaudet, M.11
Pupowicz, D.12
Maio, M.13
Pittet, P.A.14
Golzio, L.15
Giachetti, C.16
Rocha, C.17
Bernardinelli, G.18
Filinchuk, Y.19
Scheer, A.20
Schwarz, M.K.21
Chollet, A.22
more..
-
44
-
-
80051763689
-
2) receptor antagonists
-
2) receptor antagonists ACS Med. Chem. Lett. 2011, 2, 644-649
-
(2011)
ACS Med. Chem. Lett.
, vol.2
, pp. 644-649
-
-
Crosignani, S.1
Jorand-Lebrun, C.2
Page, P.3
Campbell, G.4
Colovray, V.5
Missotten, M.6
Humbert, Y.7
Cleva, C.8
Arrighi, J.-F.9
Gaudet, M.10
Johnson, Z.11
Ferro, P.12
Chollet, A.13
-
45
-
-
77953292659
-
3-Indolyl sultams as selective CRTh2 antagonists
-
Tumey, L. N.; Robarge, M. J.; Gleason, E.; Song, J.; Murphy, S. M.; Ekema, G.; Doucette, C.; Hanniford, D.; Palmer, M.; Pawlowski, G.; Danzig, J.; Loftus, M.; Hunady, K.; Sherf, B.; Mays, R. W.; Stricker-Krongrad, A.; Brunden, K. R.; Bennani, Y. L.; Harrington, J. J. 3-Indolyl sultams as selective CRTh2 antagonists Bioorg. Med. Chem. Lett. 2010, 20, 3287-3290
-
(2010)
Bioorg. Med. Chem. Lett.
, vol.20
, pp. 3287-3290
-
-
Tumey, L.N.1
Robarge, M.J.2
Gleason, E.3
Song, J.4
Murphy, S.M.5
Ekema, G.6
Doucette, C.7
Hanniford, D.8
Palmer, M.9
Pawlowski, G.10
Danzig, J.11
Loftus, M.12
Hunady, K.13
Sherf, B.14
Mays, R.W.15
Stricker-Krongrad, A.16
Brunden, K.R.17
Bennani, Y.L.18
Harrington, J.J.19
-
47
-
-
67651094080
-
7-Azaindole-3-acetic acid derivatives: Potent and selective CRTh2 receptor antagonists
-
Sandham, D. A.; Adcock, C.; Bala, K.; Barker, L.; Brown, Z.; Dubois, G.; Budd, D.; Cox, B.; Fairhurst, R. A.; Furegati, M.; Leblanc, C.; Manini, J.; Profit, R.; Reilly, J.; Stringer, R.; Schmidt, A.; Turner, K. L.; Watson, S. J.; Willis, J.; Williams, G.; Wilson, C. 7-Azaindole-3-acetic acid derivatives: potent and selective CRTh2 receptor antagonists Bioorg. Med. Chem. Lett. 2009, 19, 4794-4798
-
(2009)
Bioorg. Med. Chem. Lett.
, vol.19
, pp. 4794-4798
-
-
Sandham, D.A.1
Adcock, C.2
Bala, K.3
Barker, L.4
Brown, Z.5
Dubois, G.6
Budd, D.7
Cox, B.8
Fairhurst, R.A.9
Furegati, M.10
Leblanc, C.11
Manini, J.12
Profit, R.13
Reilly, J.14
Stringer, R.15
Schmidt, A.16
Turner, K.L.17
Watson, S.J.18
Willis, J.19
Williams, G.20
Wilson, C.21
more..
-
53
-
-
79952361716
-
Thienopyrrole acetic acids as antagonists of the CRTH2 receptor
-
Bonafoux, D.; Abibi, A.; Bettencourt, B.; Burchat, A.; Ericsson, A.; Harris, C. M.; Kebede, T.; Morytko, M.; McPherson, M.; Wallace, G.; Wu, X. Thienopyrrole acetic acids as antagonists of the CRTH2 receptor Bioorg. Med. Chem. Lett. 2011, 21, 1861-1864
-
(2011)
Bioorg. Med. Chem. Lett.
, vol.21
, pp. 1861-1864
-
-
Bonafoux, D.1
Abibi, A.2
Bettencourt, B.3
Burchat, A.4
Ericsson, A.5
Harris, C.M.6
Kebede, T.7
Morytko, M.8
McPherson, M.9
Wallace, G.10
Wu, X.11
-
54
-
-
33750978443
-
Novel selective orally active CRTH2 antagonists for allergic inflammation developed from in silico derived hits
-
Ulven, T.; Receveur, J. M.; Grimstrup, M.; Rist, O.; Frimurer, T. M.; Gerlach, L. O.; Mathiesen, J. M.; Kostenis, E.; Uller, L.; Hogberg, T. Novel selective orally active CRTH2 antagonists for allergic inflammation developed from in silico derived hits J. Med. Chem. 2006, 49, 6638-6641
-
(2006)
J. Med. Chem.
, vol.49
, pp. 6638-6641
-
-
Ulven, T.1
Receveur, J.M.2
Grimstrup, M.3
Rist, O.4
Frimurer, T.M.5
Gerlach, L.O.6
Mathiesen, J.M.7
Kostenis, E.8
Uller, L.9
Hogberg, T.10
-
55
-
-
34347371424
-
2-Cycloalkyl phenoxyacetic acid CRTh2 receptor antagonists
-
Sandham, D. A.; Aldcroft, C.; Baettig, U.; Barker, L.; Beer, D.; Bhalay, G.; Brown, Z.; Dubois, G.; Budd, D.; Bidlake, L.; Campbell, E.; Cox, B.; Everatt, B.; Harrison, D.; Leblanc, C. J.; Manini, J.; Profit, R.; Stringer, R.; Thompson, K. S.; Turner, K. L.; Tweed, M. F.; Walker, C.; Watson, S. J.; Whitebread, S.; Willis, J.; Williams, G.; Wilson, C. 2-Cycloalkyl phenoxyacetic acid CRTh2 receptor antagonists Bioorg. Med. Chem. Lett. 2007, 17, 4347-4350
-
(2007)
Bioorg. Med. Chem. Lett.
, vol.17
, pp. 4347-4350
-
-
Sandham, D.A.1
Aldcroft, C.2
Baettig, U.3
Barker, L.4
Beer, D.5
Bhalay, G.6
Brown, Z.7
Dubois, G.8
Budd, D.9
Bidlake, L.10
Campbell, E.11
Cox, B.12
Everatt, B.13
Harrison, D.14
Leblanc, C.J.15
Manini, J.16
Profit, R.17
Stringer, R.18
Thompson, K.S.19
Turner, K.L.20
Tweed, M.F.21
Walker, C.22
Watson, S.J.23
Whitebread, S.24
Willis, J.25
Williams, G.26
Wilson, C.27
more..
-
56
-
-
79957851179
-
Switching between agonists and antagonists at CRTh2 in a series of highly potent and selective biaryl phenoxyacetic acids
-
Luker, T.; Bonnert, R.; Schmidt, J.; Sargent, C.; Paine, S. W.; Thom, S.; Pairaudeau, G.; Patel, A.; Mohammed, R.; Akam, E.; Dougall, I.; Davis, A. M.; Abbott, P.; Brough, S.; Millichip, I.; McInally, T. Switching between agonists and antagonists at CRTh2 in a series of highly potent and selective biaryl phenoxyacetic acids Bioorg. Med. Chem. Lett. 2011, 21, 3616-3621
-
(2011)
Bioorg. Med. Chem. Lett.
, vol.21
, pp. 3616-3621
-
-
Luker, T.1
Bonnert, R.2
Schmidt, J.3
Sargent, C.4
Paine, S.W.5
Thom, S.6
Pairaudeau, G.7
Patel, A.8
Mohammed, R.9
Akam, E.10
Dougall, I.11
Davis, A.M.12
Abbott, P.13
Brough, S.14
Millichip, I.15
McInally, T.16
-
57
-
-
84859787573
-
-
pA2 online. See.
-
Sargent, C.; Stinson, S.; Schmidt, J.; Dougall, I.; Bonnert, R.; Paine, S.; Saunders, M.; Foster, M. Br. J. Pharmacol. 2009, 98, pA2 online. See https://bps.conference-services.net/resources/344/1686/pdf/JB2009-0098.pdf.
-
(2009)
Br. J. Pharmacol.
, vol.98
-
-
Sargent, C.1
Stinson, S.2
Schmidt, J.3
Dougall, I.4
Bonnert, R.5
Paine, S.6
Saunders, M.7
Foster, M.8
-
59
-
-
79952801932
-
Zwitterionic CRTh2 antagonists
-
Luker, T.; Bonnert, R.; Paine, S. W.; Schmidt, J.; Sargent, C.; Cook, A. R.; Cook, A.; Gardiner, P.; Hill, S.; Weyman-Jones, C.; Patel, A.; Thom, S.; Thorne, P. Zwitterionic CRTh2 antagonists J. Med. Chem. 2011, 54, 1779-1788
-
(2011)
J. Med. Chem.
, vol.54
, pp. 1779-1788
-
-
Luker, T.1
Bonnert, R.2
Paine, S.W.3
Schmidt, J.4
Sargent, C.5
Cook, A.R.6
Cook, A.7
Gardiner, P.8
Hill, S.9
Weyman-Jones, C.10
Patel, A.11
Thom, S.12
Thorne, P.13
-
60
-
-
80054959577
-
2) receptor antagonists for the treatment of allergic inflammatory diseases
-
2) receptor antagonists for the treatment of allergic inflammatory diseases J. Med. Chem. 2011, 54, 7299-7317
-
(2011)
J. Med. Chem.
, vol.54
, pp. 7299-7317
-
-
Crosignani, S.1
Pretre, A.2
Jorand-Lebrun, C.3
Fraboulet, G.4
Seenisamy, J.5
Augustine, J.K.6
Missotten, M.7
Humbert, Y.8
Cleva, C.9
Abla, N.10
Daff, H.11
Schott, O.12
Schneider, M.13
Burgat-Charvillon, F.14
Rivron, D.15
Hamernig, I.16
Arrighi, J.-F.17
Gaudet, M.18
Zimmerli, S.C.19
Juillard, P.20
Johnson, Z.21
more..
-
61
-
-
77958468653
-
-
(Amira). US Appl. US20090197959.
-
2 receptors. US Appl. US20090197959, 2009.
-
(2009)
2 Receptors
-
-
Hutchinson, J.H.1
Stearns, B.A.2
Scott, J.M.3
Truong, Y.P.4
Roppe, J.R.5
Stock, N.S.6
Arruda, J.M.7
Seiders, T.J.8
Wang, B.9
-
62
-
-
77249086270
-
2 receptor inhibits cigarette smoke-induced inflammation, mucus cell metaplasia, and epithelial hyperplasia in the mouse lung
-
2 receptor inhibits cigarette smoke-induced inflammation, mucus cell metaplasia, and epithelial hyperplasia in the mouse lung J. Pharmacol. Exp. Ther. 2010, 332, 764-775
-
(2010)
J. Pharmacol. Exp. Ther.
, vol.332
, pp. 764-775
-
-
Stebbins, K.J.1
Broadhead, A.R.2
Baccei, C.S.3
Scott, J.M.4
Truong, Y.P.5
Coate, H.6
Stock, N.S.7
Santini, A.M.8
Fagan, P.9
Prodanovich, P.10
Bain, G.11
Stearns, B.A.12
King, C.D.13
Hutchinson, J.H.14
Prasit, P.15
Evans, J.F.16
Lorrain, D.S.17
-
63
-
-
80054103321
-
2 antagonists with efficacy in a murine model of allergic rhinitis
-
2 antagonists with efficacy in a murine model of allergic rhinitis Bioorg. Med. Chem. Lett. 2011, 21, 6608-6612
-
(2011)
Bioorg. Med. Chem. Lett.
, vol.21
, pp. 6608-6612
-
-
Scott, J.M.1
Baccei, C.2
Bain, G.3
Broadhead, A.4
Evans, J.F.5
Fagan, P.6
Hutchinson, J.H.7
King, C.8
Lorrain, D.S.9
Lee, C.10
Prasit, P.11
Prodanovich, P.12
Santini, A.13
Stearns, B.A.14
-
64
-
-
79959497075
-
2 receptor type 2 antagonist that is active in animal models of allergic inflammation
-
2 receptor type 2 antagonist that is active in animal models of allergic inflammation J. Pharmacol. Exp. Ther. 2011, 338, 290-301
-
(2011)
J. Pharmacol. Exp. Ther.
, vol.338
, pp. 290-301
-
-
Bain, G.1
Lorrain, D.S.2
Stebbins, K.J.3
Broadhead, A.R.4
Santini, A.M.5
Prodanovich, P.6
Darlington, J.7
King, C.D.8
Lee, C.9
Baccei, C.10
Stearns, B.11
Troung, Y.12
Hutchinson, J.H.13
Prasit, P.14
Evans, J.F.15
-
67
-
-
81855162919
-
-
(Amira). PCT Int. Appl. WO2010003120.
-
Hutchinson, J. H.; Seiders, T. J.; Wang, B.; Arruda, J. M.; Stearns, B. A. (Amira) Antagonists of prostaglandin D2 receptors. PCT Int. Appl. WO2010003120, 2010.
-
(2010)
Antagonists of Prostaglandin D2 Receptors
-
-
Hutchinson, J.H.1
Seiders, T.J.2
Wang, B.3
Arruda, J.M.4
Stearns, B.A.5
-
68
-
-
78751649417
-
2 receptor antagonist
-
2 receptor antagonist Bioorg. Med. Chem. Lett. 2011, 21, 1036-1040
-
(2011)
Bioorg. Med. Chem. Lett.
, vol.21
, pp. 1036-1040
-
-
Stock, N.1
Volkots, D.2
Stebbins, K.3
Broadhead, A.4
Stearns, B.5
Roppe, J.6
Parr, T.7
Baccei, C.8
Bain, G.9
Chapman, C.10
Correa, L.11
Darlington, J.12
King, C.13
Lee, C.14
Lorrain, D.S.15
Prodanovich, P.16
Santini, A.17
Evans, J.F.18
Hutchinson, J.H.19
Prasit, P.20
more..
-
70
-
-
84976318191
-
Safety, PK and PD of ARRY-502, a CRTH2 antagonist, in healthy subjects with a history of seasonal allergies
-
Paper E3954 presented at the Barcelona, Spain, September
-
Bell, S.; Anderson, l.; Nugent, C.; Klopfenstein, N.; Carter, L.; Kass, C.; Rojas-Caro, S.; Burgess, L.; Bergstrom, B.; Miller S. Safety, PK and PD of ARRY-502, a CRTH2 antagonist, in healthy subjects with a history of seasonal allergies. Paper E3954 presented at the European Society Annual Congress, Barcelona, Spain, September 18 â̂ 22, 2010.
-
(2010)
European Society Annual Congress
, pp. 18-22
-
-
Bell, S.1
Anderson, I.2
Nugent, C.3
Klopfenstein, N.4
Carter, L.5
Kass, C.6
Rojas-Caro, S.7
Burgess, L.8
Bergstrom, B.9
Miller, S.10
-
71
-
-
71049187691
-
Discovery and optimization of CRTH2 and DP dual antagonists
-
Liu, J.; Fu, Z.; Wang, Y.; Schmitt, M.; Huang, A.; Marshall, D.; Tonn, G.; Seitz, L.; Sullivan, T.; Lucy, T. H.; Collins, T.; Medina, J. Discovery and optimization of CRTH2 and DP dual antagonists Bioorg. Med. Chem. Lett. 2009, 19, 6419-6423
-
(2009)
Bioorg. Med. Chem. Lett.
, vol.19
, pp. 6419-6423
-
-
Liu, J.1
Fu, Z.2
Wang, Y.3
Schmitt, M.4
Huang, A.5
Marshall, D.6
Tonn, G.7
Seitz, L.8
Sullivan, T.9
Lucy, T.H.10
Collins, T.11
Medina, J.12
-
72
-
-
79956066242
-
Discovery of AMG 853, a CRTH2 and DP Dual Antagonist
-
Liu, J.; Li, A.-R.; Wang, Y.; Johnson, M. G.; Su, Y.; Shen, W.; Wang, X.; Lively, S.; Brown, M.; Lai, S.; Lopez De Turiso, F. G.; Xu, Q.; Van Lengerich, B.; Schmitt, M.; Fu, Z.; Sun, Y.; Lawlis, S.; Seitz, L.; Danao, J.; Wait, J.; Ye, Q.; Tang, H. L.; Grillo, M.; Collins, T. L.; Sullivan, T. J.; Medina, J. C. Discovery of AMG 853, a CRTH2 and DP Dual Antagonist ACS Med. Chem. Lett. 2011, 2, 326-330
-
(2011)
ACS Med. Chem. Lett.
, vol.2
, pp. 326-330
-
-
Liu, J.1
Li, A.-R.2
Wang, Y.3
Johnson, M.G.4
Su, Y.5
Shen, W.6
Wang, X.7
Lively, S.8
Brown, M.9
Lai, S.10
Lopez De Turiso, F.G.11
Xu, Q.12
Van Lengerich, B.13
Schmitt, M.14
Fu, Z.15
Sun, Y.16
Lawlis, S.17
Seitz, L.18
Danao, J.19
Wait, J.20
Ye, Q.21
Tang, H.L.22
Grillo, M.23
Collins, T.L.24
Sullivan, T.J.25
Medina, J.C.26
more..
-
73
-
-
71749095907
-
1 antagonist laropiprant in asthma and allergic rhinitis
-
1 antagonist laropiprant in asthma and allergic rhinitis J. Allergy Clin. Immunol. 2009, 124, 942-948
-
(2009)
J. Allergy Clin. Immunol.
, vol.124
, pp. 942-948
-
-
Philip, G.1
Van Adelsberg, J.2
Loeys, T.3
Liu, N.4
Wong, P.5
Lai, E.6
Dass, S.B.7
Reiss, T.F.8
-
74
-
-
79960400846
-
Benzodiazepinone Derivatives as CRTH2 Antagonists
-
Liu, J.; Cheng, A. C.; Tang, H. L.; Medina, J. C. Benzodiazepinone Derivatives as CRTH2 Antagonists ACS Med. Chem. Lett. 2011, 2, 515-518
-
(2011)
ACS Med. Chem. Lett.
, vol.2
, pp. 515-518
-
-
Liu, J.1
Cheng, A.C.2
Tang, H.L.3
Medina, J.C.4
-
75
-
-
74049135437
-
Novel selective thiazoleacetic acids as CRTH2 antagonists developed from in silico derived hits. Part 1
-
Rist, O.; Grimstrup, M.; Receveur, J. M.; Frimurer, T. M.; Ulven, T.; Kostenis, E.; Hogberg, T. Novel selective thiazoleacetic acids as CRTH2 antagonists developed from in silico derived hits. Part 1 Bioorg. Med. Chem. Lett. 2010, 20, 1177-1180
-
(2010)
Bioorg. Med. Chem. Lett.
, vol.20
, pp. 1177-1180
-
-
Rist, O.1
Grimstrup, M.2
Receveur, J.M.3
Frimurer, T.M.4
Ulven, T.5
Kostenis, E.6
Hogberg, T.7
-
76
-
-
74049135437
-
Novel selective thiazoleacetic acids as CRTH2 antagonists developed from in silico derived hits. Part 2
-
Grimstrup, M.; Rist, O.; Receveur, J. M.; Frimurer, T. M.; Ulven, T.; Mathiesen, J. M.; Kostenis, E.; Hogberg, T. Novel selective thiazoleacetic acids as CRTH2 antagonists developed from in silico derived hits. Part 2 Bioorg. Med. Chem. Lett. 2010, 20, 1181-1185
-
(2010)
Bioorg. Med. Chem. Lett.
, vol.20
, pp. 1181-1185
-
-
Grimstrup, M.1
Rist, O.2
Receveur, J.M.3
Frimurer, T.M.4
Ulven, T.5
Mathiesen, J.M.6
Kostenis, E.7
Hogberg, T.8
-
77
-
-
76649106066
-
Exploration of SAR features by modifications of thiazoleacetic acids as CRTH2 antagonists
-
Grimstrup, M.; Receveur, J. M.; Rist, O.; Frimurer, T. M.; Nielsen, P. A.; Mathiesen, J. M.; Hogberg, T. Exploration of SAR features by modifications of thiazoleacetic acids as CRTH2 antagonists Bioorg. Med. Chem. Lett. 2010, 20, 1638-1641
-
(2010)
Bioorg. Med. Chem. Lett.
, vol.20
, pp. 1638-1641
-
-
Grimstrup, M.1
Receveur, J.M.2
Rist, O.3
Frimurer, T.M.4
Nielsen, P.A.5
Mathiesen, J.M.6
Hogberg, T.7
-
80
-
-
58049195679
-
A small molecule CRTH2 antagonist inhibits FITC-induced allergic cutaneous inflammation
-
Boehme, S. A.; Franz-Bacon, K.; Chen, E. P.; Sasik, R.; Sprague, L. J.; Ly, T. W.; Hardiman, G.; Bacon, K. B. A small molecule CRTH2 antagonist inhibits FITC-induced allergic cutaneous inflammation Int. Immunol. 2009, 21, 81-93
-
(2009)
Int. Immunol.
, vol.21
, pp. 81-93
-
-
Boehme, S.A.1
Franz-Bacon, K.2
Chen, E.P.3
Sasik, R.4
Sprague, L.J.5
Ly, T.W.6
Hardiman, G.7
Bacon, K.B.8
-
81
-
-
84859787578
-
-
(Boehringer Ingelheim). PCT Int. Appl. WO2011092140.
-
Oost, T.; Anderskewitz, R.; Hamprecht, D. W.; Hoenke, C.; Martyres, D.; Rist, W.; Seither, P. (Boehringer Ingelheim) Pyrazole compounds as CRTH2 antagonists. PCT Int. Appl. WO2011092140, 2011.
-
(2011)
Pyrazole Compounds As CRTH2 Antagonists
-
-
Oost, T.1
Anderskewitz, R.2
Hamprecht, D.W.3
Hoenke, C.4
Martyres, D.5
Rist, W.6
Seither, P.7
-
82
-
-
84859803564
-
-
(Roche). PCT Int. Appl. WO20100055004.
-
Chen, L.; Firooznia, F.; Gillespie, P.; He, Y.; Lin, T.-A.; Mertz, E.; So, S.-S.; Yun, H.; Zhang, Z. (Roche) Naphthylacetic acids. PCT Int. Appl. WO20100055004, 2010.
-
(2010)
Naphthylacetic Acids
-
-
Chen, L.1
Firooznia, F.2
Gillespie, P.3
He, Y.4
Lin, T.-A.5
Mertz, E.6
So, S.-S.7
Yun, H.8
Zhang, Z.9
-
83
-
-
84859803564
-
-
(Roche). PCT Int. Appl. WO2010055005.
-
Firooznia, F.; Gillespie, P.; Lin, T.-A.; Mertz, E.; Sidduri, A.; So, S.-S.; Jan, J.; Thakkar, K. C. (Roche) Naphthylacetic acids. PCT Int. Appl. WO2010055005, 2010.
-
(2010)
Naphthylacetic Acids
-
-
Firooznia, F.1
Gillespie, P.2
Lin, T.-A.3
Mertz, E.4
Sidduri, A.5
So, S.-S.6
Jan, J.7
Thakkar, K.C.8
-
84
-
-
84859803563
-
-
(Roche). PCT Int. Appl. WO2010055006.
-
Firooznia, F.; Lin, T.-A.; So, S.-S.; Wang, B.; Yun, H. (Roche) Naphthylacetic acids used as CRTH2 antagonists or partial agonists. PCT Int. Appl. WO2010055006, 2010.
-
(2010)
Naphthylacetic Acids Used As CRTH2 Antagonists or Partial Agonists
-
-
Firooznia, F.1
Lin, T.-A.2
So, S.-S.3
Wang, B.4
Yun, H.5
-
85
-
-
77958452409
-
-
(Argenta). PCT Int. Appl. WO2007036743.
-
Cramp, M. C.; Arienzo, R.; Hynd, G.; Crackett, P.; Griffon, Y.; Harrison, T. K.; Ray, N. C.; Finch, H.; Montana, J. G. (Argenta) Quinolines and their therapeutic use. PCT Int. Appl. WO2007036743, 2007.
-
(2007)
Quinolines and Their Therapeutic Use
-
-
Cramp, M.C.1
Arienzo, R.2
Hynd, G.3
Crackett, P.4
Griffon, Y.5
Harrison, T.K.6
Ray, N.C.7
Finch, H.8
Montana, J.G.9
-
86
-
-
77958457433
-
-
(Argenta). PCT Int. Appl. WO2007144625.
-
Hynd, G.; Harris, N. V.; Bull, R. J.; Gardan, S.; Handa, B. K. (Argenta) 2-Oxo-2 H -chromene compounds. PCT Int. Appl. WO2007144625, 2007.
-
(2007)
2-Oxo-2 H -chromene Compounds
-
-
Hynd, G.1
Harris, N.V.2
Bull, R.J.3
Gardan, S.4
Handa, B.K.5
-
87
-
-
77958509368
-
-
(Argenta). PCT Int. Appl. WO2008122784.
-
Montana, J. G.; Finch, H.; Hynd, G.; Cramp, M. C.; Arienzo, R.; Mclean, N. (Argenta) Quinolines and their therapeutic use. PCT Int. Appl. WO2008122784, 2008.
-
(2008)
Quinolines and Their Therapeutic Use
-
-
Montana, J.G.1
Finch, H.2
Hynd, G.3
Cramp, M.C.4
Arienzo, R.5
McLean, N.6
-
88
-
-
77958511228
-
-
(Argenta). PCT Int. Appl. WO2008119917.
-
Ray, N. C.; Finch, H.; Cramp, M. C.; Arienzo, R.; Hynd, G.; Crackett, P.; Griffon, Y.; Harrison, T. K.; Trevor, K.; Montana, J. G. (Argenta) Quinoline derivatives as CRTH2 receptor ligands. PCT Int. Appl. WO2008119917, 2008.
-
(2008)
Quinoline Derivatives As CRTH2 Receptor Ligands
-
-
Ray, N.C.1
Finch, H.2
Cramp, M.C.3
Arienzo, R.4
Hynd, G.5
Crackett, P.6
Griffon, Y.7
Harrison, T.K.8
Trevor, K.9
Montana, J.G.10
-
89
-
-
77958478525
-
-
(Argenta). PCT Int. Appl. WO2008074966.
-
Hynd, G.; Ray, N. C.; Finch, H.; Middlemiss, D.; Cramp, M. C.; Blaney, P. M.; Williams, K.; Griffon, Y.; Harrison, T. K.; Crackett, P. (Argenta) CRTH2 Antagonists. PCT Int. Appl. WO2008074966, 2008.
-
(2008)
CRTH2 Antagonists
-
-
Hynd, G.1
Ray, N.C.2
Finch, H.3
Middlemiss, D.4
Cramp, M.C.5
Blaney, P.M.6
Williams, K.7
Griffon, Y.8
Harrison, T.K.9
Crackett, P.10
-
90
-
-
84859803562
-
-
(Argenta). PCT Int. Appl. WO2010040989.
-
Hynd, G.; Montana, J. G.; Finch, H.; Cramp, M. C.; Ward, S. (Argenta) Quinolin-2-one compounds. PCT Int. Appl. WO2010040989, 2010.
-
(2010)
Quinolin-2-one Compounds
-
-
Hynd, G.1
Montana, J.G.2
Finch, H.3
Cramp, M.C.4
Ward, S.5
-
91
-
-
84859793109
-
-
(Array Biopharma). PCT Int. Appl. WO2009158426.
-
Burgess, L. E.; Clark, C. T.; Cook, A.; Corrette, C. P.; Delisle, R. K.; Doherty, G. A.; Hunt, K. W.; Romoff, T. (Array Biopharma) 6-Substituted phenoxychroman carboxylic acid derivatives. PCT Int. Appl. WO2009158426, 2009.
-
(2009)
6-Substituted Phenoxychroman Carboxylic Acid Derivatives
-
-
Burgess, L.E.1
Clark, C.T.2
Cook, A.3
Corrette, C.P.4
Delisle, R.K.5
Doherty, G.A.6
Hunt, K.W.7
Romoff, T.8
-
92
-
-
84859803560
-
-
(Array Biopharma). PCT Int. Appl. WO2010075200.
-
Cook, A.; Hunt, K. W.; Delisle, R. K.; Romoff, T.; Clark, C. T.; Kim, G.; Corrette, C. P.; Doherty, G. A.; Burgess, L. E. (Array Biopharma) 7-Phenoxychroman carboxylic acid derivatives. PCT Int. Appl. WO2010075200, 2010.
-
(2010)
7-Phenoxychroman Carboxylic Acid Derivatives
-
-
Cook, A.1
Hunt, K.W.2
Delisle, R.K.3
Romoff, T.4
Clark, C.T.5
Kim, G.6
Corrette, C.P.7
Doherty, G.A.8
Burgess, L.E.9
-
93
-
-
77955839741
-
-
(AstraZeneca). PCT Int. Appl. WO2007068894.
-
Bonnert, R. V.; Luker, T. J.; Mohammed, R. T.; Thom, S.; Cook, A. (AstraZeneca) Novel compounds. PCT Int. Appl. WO2007068894, 2007.
-
(2007)
Novel Compounds
-
-
Bonnert, R.V.1
Luker, T.J.2
Mohammed, R.T.3
Thom, S.4
Cook, A.5
-
95
-
-
33746639320
-
-
(Warner-Lambert). PCT Int. Appl. WO2004035543.
-
Awad, M. M. A.; Bazin, M.; Feru, F.; Goldstein, S. W.; Kuhn, C. F. (Warner-Lambert) Tetrahydroquinoline derivatives as CRTH2 antagonists. PCT Int. Appl. WO2004035543, 2004.
-
(2004)
Tetrahydroquinoline Derivatives As CRTH2 Antagonists
-
-
Awad, M.M.A.1
Bazin, M.2
Feru, F.3
Goldstein, S.W.4
Kuhn, C.F.5
-
96
-
-
23044463582
-
Inhibitory effect of the 4-aminotetrahydroquinoline derivatives, selective chemoattractant receptor-homologous molecule expressed on T helper 2 cell antagonists, on eosinophil migration induced by prostaglandin D2
-
Mimura, H.; Ikemura, T.; Kotera, O.; Sawada, M.; Tashiro, S.; Fuse, E.; Ueno, K.; Manabe, H.; Ohshima, E.; Karasawa, A.; Miyaji, H. Inhibitory effect of the 4-aminotetrahydroquinoline derivatives, selective chemoattractant receptor-homologous molecule expressed on T helper 2 cell antagonists, on eosinophil migration induced by prostaglandin D2 J. Pharmacol. Exp. Ther. 2005, 314, 244-251
-
(2005)
J. Pharmacol. Exp. Ther.
, vol.314
, pp. 244-251
-
-
Mimura, H.1
Ikemura, T.2
Kotera, O.3
Sawada, M.4
Tashiro, S.5
Fuse, E.6
Ueno, K.7
Manabe, H.8
Ohshima, E.9
Karasawa, A.10
Miyaji, H.11
-
97
-
-
71849102580
-
Tetrahydroquinoline derivatives as CRTH2 antagonists
-
Liu, J.; Wang, Y.; Sun, Y.; Marshall, D.; Miao, S.; Tonn, G.; Anders, P.; Tocker, J.; Tang, H. L.; Medina, J. Tetrahydroquinoline derivatives as CRTH2 antagonists Bioorg. Med. Chem. Lett. 2009, 19, 6840-6844
-
(2009)
Bioorg. Med. Chem. Lett.
, vol.19
, pp. 6840-6844
-
-
Liu, J.1
Wang, Y.2
Sun, Y.3
Marshall, D.4
Miao, S.5
Tonn, G.6
Anders, P.7
Tocker, J.8
Tang, H.L.9
Medina, J.10
-
99
-
-
77958450713
-
-
(Merck Serono). PCT Int. Appl. WO2006111560.
-
Page, P.; Schwarz, M.; Sebille, E.; Cleva, C.; Merlot, C.; Maio, M. (Merck Serono) 2,3-Substituted pyrazine sulfonamides as inhibitors of CRTH2. PCT Int. Appl. WO2006111560, 2006.
-
(2006)
2,3-Substituted Pyrazine Sulfonamides As Inhibitors of CRTH2
-
-
Page, P.1
Schwarz, M.2
Sebille, E.3
Cleva, C.4
Merlot, C.5
Maio, M.6
-
100
-
-
14944363741
-
Structural determinants of arylacetic acid nonsteroidal anti-inflammatory drugs necessary for binding and activation of the prostaglandin D2 receptor CRTH2
-
Hata, A. N.; Lybrand, T. P.; Marnett, L. J.; Breyer, R. M. Structural determinants of arylacetic acid nonsteroidal anti-inflammatory drugs necessary for binding and activation of the prostaglandin D2 receptor CRTH2 Mol. Pharmacol. 2005, 67, 640-647
-
(2005)
Mol. Pharmacol.
, vol.67
, pp. 640-647
-
-
Hata, A.N.1
Lybrand, T.P.2
Marnett, L.J.3
Breyer, R.M.4
-
101
-
-
25444451591
-
Identification of determinants of ligand binding affinity and selectivity in the prostaglandin D2 receptor CRTH2
-
Hata, A. N.; Lybrand, T. P.; Breyer, R. M. Identification of determinants of ligand binding affinity and selectivity in the prostaglandin D2 receptor CRTH2 J. Biol. Chem. 2005, 280, 32442-32451
-
(2005)
J. Biol. Chem.
, vol.280
, pp. 32442-32451
-
-
Hata, A.N.1
Lybrand, T.P.2
Breyer, R.M.3
-
102
-
-
0037422456
-
Acyl glucuronide reactivity in perspective: Biological consequences
-
Bailey, M.; Dickinson, R. G. Acyl glucuronide reactivity in perspective: Biological consequences Chem. Biol. Interact. 2003, 145, 117-137
-
(2003)
Chem. Biol. Interact.
, vol.145
, pp. 117-137
-
-
Bailey, M.1
Dickinson, R.G.2
-
103
-
-
78649495086
-
Acyl glucuronides: The good, the bad and the ugly
-
Regan, S. L.; Maggs, J. L.; Hammond, T. G.; Lambert, C.; Williams, D. P.; Park, B. K. Acyl glucuronides: the good, the bad and the ugly Biopharm. Drug Dispos. 2010, 31, 367-395
-
(2010)
Biopharm. Drug Dispos.
, vol.31
, pp. 367-395
-
-
Regan, S.L.1
Maggs, J.L.2
Hammond, T.G.3
Lambert, C.4
Williams, D.P.5
Park, B.K.6
-
104
-
-
44349171209
-
Metabolic activation of carboxylic acids
-
Skonberg, C.; Olsen, J.; Madsen, K. G.; Hansen, S. H.; Grillo, M. P. Metabolic activation of carboxylic acids Expert Opin. Drug Metab. Toxicol. 2008, 4, 425-438
-
(2008)
Expert Opin. Drug Metab. Toxicol.
, vol.4
, pp. 425-438
-
-
Skonberg, C.1
Olsen, J.2
Madsen, K.G.3
Hansen, S.H.4
Grillo, M.P.5
-
105
-
-
79953655654
-
Drug-S-acyl-glutathione thioesters: Synthesis, bioanalytical properties, chemical reactivity, biological formation and degradation
-
Grillo, M. P. Drug-S-acyl-glutathione thioesters: synthesis, bioanalytical properties, chemical reactivity, biological formation and degradation Curr. Drug Metab. 2011, 12, 229-244
-
(2011)
Curr. Drug Metab.
, vol.12
, pp. 229-244
-
-
Grillo, M.P.1
-
106
-
-
0027199712
-
Predictability of the covalent binding of acidic drugs in man
-
Benet, L. Z.; Spahn-Langguth, H.; Iwakawa, S.; Volland, C.; Mizuma, T.; Mayer, S.; Mutschler, E.; Lin, E. T. Predictability of the covalent binding of acidic drugs in man Life Sci. 1993, 53, PL141-PL146
-
(1993)
Life Sci.
, vol.53
-
-
Benet, L.Z.1
Spahn-Langguth, H.2
Iwakawa, S.3
Volland, C.4
Mizuma, T.5
Mayer, S.6
Mutschler, E.7
Lin, E.T.8
-
107
-
-
61849141666
-
Structure-activity relationships for degradation reaction of 1-beta-o-acyl glucuronides: Kinetic description and prediction of intrinsic electrophilic reactivity under physiological conditions
-
Baba, A.; Yoshioka, T. Structure-activity relationships for degradation reaction of 1-beta-o-acyl glucuronides: kinetic description and prediction of intrinsic electrophilic reactivity under physiological conditions Chem. Res. Toxicol. 2009, 22, 158-172
-
(2009)
Chem. Res. Toxicol.
, vol.22
, pp. 158-172
-
-
Baba, A.1
Yoshioka, T.2
-
108
-
-
78651490914
-
Development of specific drug-like property rules for carboxylate- containing oral drug candidates
-
BoIcker, A.; Bonneau, P. R.; Hucke, O.; Jakalian, A.; Edwards, P. J. Development of specific drug-like property rules for carboxylate-containing oral drug candidates ChemMedChem 2010, 5, 2102-2113
-
(2010)
ChemMedChem
, vol.5
, pp. 2102-2113
-
-
Boicker, A.1
Bonneau, P.R.2
Hucke, O.3
Jakalian, A.4
Edwards, P.J.5
-
109
-
-
1242337282
-
The high solubility definition of the current FDA Guidance on Biopharmaceutical Classification System may be too strict for acidic drugs
-
Yazdanian, M.; Briggs, K.; Jankovsky, C.; Hawi, A. The high solubility definition of the current FDA Guidance on Biopharmaceutical Classification System may be too strict for acidic drugs Pharm. Res. 2004, 21, 293-299
-
(2004)
Pharm. Res.
, vol.21
, pp. 293-299
-
-
Yazdanian, M.1
Briggs, K.2
Jankovsky, C.3
Hawi, A.4
-
110
-
-
78649706279
-
The effect of plasma protein binding on in vivo efficacy: Misconceptions in drug discovery
-
Smith, D. A.; Di, L; Kerns, E. H. The effect of plasma protein binding on in vivo efficacy: Misconceptions in drug discovery Nat. Rev. Drug Discovery 2010, 9, 929-939
-
(2010)
Nat. Rev. Drug Discovery
, vol.9
, pp. 929-939
-
-
Smith, D.A.1
Di, L.2
Kerns, E.H.3
-
111
-
-
0035147506
-
Prediction of a new drug's potential to cause idiosyncratic reactions
-
Uetrecht, J. Prediction of a new drug's potential to cause idiosyncratic reactions Curr. Opin. Drug Discovery Dev. 2001, 4, 55-59
-
(2001)
Curr. Opin. Drug Discovery Dev.
, vol.4
, pp. 55-59
-
-
Uetrecht, J.1
-
112
-
-
38949104743
-
Idiosyncratic drug reactions: Past, present, and future
-
Uetrecht, J. Idiosyncratic drug reactions: past, present, and future Chem. Res. Toxicol. 2008, 21, 84-92
-
(2008)
Chem. Res. Toxicol.
, vol.21
, pp. 84-92
-
-
Uetrecht, J.1
-
113
-
-
33748770143
-
Inhibitory effect of carboxylic acid group on hERG binding
-
Zhu, B.-Y.; Jia, Z.; Zhang, P.; Ting, S.; Huang, W.; Goldman, E.; Tumas, D.; Kadambi, V.; Eddy, P.; Sinha, U.; Scarborough, R. M.; Song, Y. Inhibitory effect of carboxylic acid group on hERG binding Bioorg. Med. Chem. Lett. 2006, 21, 5507-5512
-
(2006)
Bioorg. Med. Chem. Lett.
, vol.21
, pp. 5507-5512
-
-
Zhu, B.-Y.1
Jia, Z.2
Zhang, P.3
Ting, S.4
Huang, W.5
Goldman, E.6
Tumas, D.7
Kadambi, V.8
Eddy, P.9
Sinha, U.10
Scarborough, R.M.11
Song, Y.12
-
114
-
-
33847336843
-
A quantative assessment of hERG liability as a function of lipophilicity
-
Waring, M. J.; Johnstone, C. A quantative assessment of hERG liability as a function of lipophilicity Bioorg. Med. Chem. Lett. 2007, 17, 1759-1764
-
(2007)
Bioorg. Med. Chem. Lett.
, vol.17
, pp. 1759-1764
-
-
Waring, M.J.1
Johnstone, C.2
-
115
-
-
77958465654
-
-
(Oxagen). PCT Int. Appl. WO2009063215.
-
Hunter, M. G; Pettipher, E. R.; Perkins, C. M.; Payton, M. A.; Xue, L. (Oxagen) Use of CRTH2 antagonist compounds. PCT Int. Appl. WO2009063215, 2009.
-
(2009)
Use of CRTH2 Antagonist Compounds
-
-
Hunter, M.G.1
Pettipher, E.R.2
Perkins, C.M.3
Payton, M.A.4
Xue, L.5
-
116
-
-
61849086181
-
Mepolizumab and exacerbations of refractory eosinophilic asthma
-
Haldar, P.; Brightling, C. E.; Hargadon, B.; Gupta, S.; Monteiro, W.; Sousa, A.; Marshall, R. P.; Bradding, P.; Green, R. H.; Wardlaw, A. J.; Pavord, I. D. Mepolizumab and exacerbations of refractory eosinophilic asthma N. Engl. J. Med. 2009, 360, 973-984
-
(2009)
N. Engl. J. Med.
, vol.360
, pp. 973-984
-
-
Haldar, P.1
Brightling, C.E.2
Hargadon, B.3
Gupta, S.4
Monteiro, W.5
Sousa, A.6
Marshall, R.P.7
Bradding, P.8
Green, R.H.9
Wardlaw, A.J.10
Pavord, I.D.11
-
117
-
-
81455155725
-
Reslizumab for poorly controlled, eosinophilic asthma: A randomized, placebo-controlled study
-
Castro, M.; Mathur, S.; Hargreave, F.; Boulet, L. P.; Xie, F.; Young, J.; Wilkins, H. J.; Henkel, T.; Nair, P. Reslizumab for poorly controlled, eosinophilic asthma: a randomized, placebo-controlled study. Am. J. Respir. Crit. Care Med. 2011, 184, 1125-1132
-
(2011)
Am. J. Respir. Crit. Care Med.
, vol.184
, pp. 1125-1132
-
-
Castro, M.1
Mathur, S.2
Hargreave, F.3
Boulet, L.P.4
Xie, F.5
Young, J.6
Wilkins, H.J.7
Henkel, T.8
Nair, P.9
-
118
-
-
80053084755
-
Lebrikizumab treatment in adults with asthma
-
Corren, J.; Lemanske, R. F.; Hanania, N. A.; Korenblat, P. E.; Parsey, M. V.; Arron, J. R.; Harris, J. M.; Scheerens, H.; Wu, L. C.; Su, Z.; Mosesova, S.; Eisner, M. D.; Bohen, S. P.; Matthews, J. G. Lebrikizumab treatment in adults with asthma N. Engl. J. Med. 2011, 365, 1088-1098
-
(2011)
N. Engl. J. Med.
, vol.365
, pp. 1088-1098
-
-
Corren, J.1
Lemanske, R.F.2
Hanania, N.A.3
Korenblat, P.E.4
Parsey, M.V.5
Arron, J.R.6
Harris, J.M.7
Scheerens, H.8
Wu, L.C.9
Su, Z.10
Mosesova, S.11
Eisner, M.D.12
Bohen, S.P.13
Matthews, J.G.14
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