Indexed keywords
4 [(1H 1,2,4 TRIAZOL 1 YL)METHYL] 1 (2 CHLOROPHENYL) 5 (4 CHLOROPHENYL) N (CYCLOHEXYLMETHYL) 1H PYRAZOLE 3 CARBOXAMIDE;
4 [(1H 1,2,4 TRIAZOL 1 YL)METHYL] 1 (2 CHLOROPHENYL) 5 (4 CHLOROPHENYL) N CYCLOHEPTYL 1H PYRAZOLE 3 CARBOXAMIDE;
4 [(1H 1,2,4 TRIAZOL 1 YL)METHYL] 1 (2 CHLOROPHENYL) 5 (4 CHLOROPHENYL) N CYCLOHEXYL 1H PYRAZOLE 3 CARBOXAMIDE;
4 [(1H 1,2,4 TRIAZOL 1 YL)METHYL] 5 (4 BROMOPHENYL) 1 (2 CHLOROPHENYL) N CYCLOHEPTYL 1H PYRAZOLE 3 CARBOXAMIDE;
4 [(1H 1,2,4 TRIAZOL 1 YL)METHYL] 5 (4 BROMOPHENYL) 1 (2 CHLOROPHENYL) N CYCLOHEXYL 1H PYRAZOLE 3 CARBOXAMIDE;
4 [(1H 1,2,4 TRIAZOL 1 YL)METHYL] 5 (4 BROMOPHENYL) 1 (2,4 DICHLOROPHENYL) N (PIPERIDIN 1 YL) 1H PYRAZOLE 3 CARBOXAMIDE;
4 [(1H 1,2,4 TRIAZOL 1 YL)METHYL] 5 (4 BROMOPHENYL) N (CYCLOHEXYLMETHYL) 1 (2,4 DICHLOROPHENYL) 1H PYRAZOLE 3 CARBOXAMIDE;
4 [(1H 1,2,4 TRIAZOL 1 YL)METHYL] 5 (4 BROMOPHENYL) N [1 (4 BROMOPHENYL)ETHYL] 1 (2 CHLOROPHENYL) 1H PYRAZOLE 3 CARBOXAMIDE;
4 [(1H 1,2,4 TRIAZOL 1 YL)METHYL] 5 (4 BROMOPHENYL) N [1 (4 BROMOPHENYL)ETHYL] 1 (2,4 DICHLOROPHENYL) 1H PYRAZOLE 3 CARBOXAMIDE;
4 [(1H 1,2,4 TRIAZOL 1 YL)METHYL] 5 (4 BROMOPHENYL) N CYCLOHEPTYL 1 (2,4 DICHLOROPHENYL) 1H PYRAZOLE 3 CARBOXAMIDE;
4 [(1H 1,2,4 TRIAZOL 1 YL)METHYL] 5 (4 BROMOPHENYL) N CYCLOHEXYL 1 (2,4 DICHLOROPHENYL) 1H PYRAZOLE 3 CARBOXAMIDE;
4 [(1H 1,2,4 TRIAZOL 1 YL)METHYL] 5 (4 CHLOROPHENYL) 1 (2,4 DICHLOROPHENYL) N (2 METHYLCYCLOHEXYL) 1H PYRAZOLE 3 CARBOXAMIDE;
4 [(1H 1,2,4 TRIAZOL 1 YL)METHYL] 5 (4 CHLOROPHENYL) 1 (2,4 DICHLOROPHENYL) N (4 METHYLCYCLOHEXYL) 1H PYRAZOLE 3 CARBOXAMIDE;
4 [(1H 1,2,4 TRIAZOL 1 YL)METHYL] 5 (4 CHLOROPHENYL) 1 (2,4 DICHLOROPHENYL) N (PIPERIDIN 1 YL) 1H PYRAZOLE 3 CARBOXAMIDE;
4 [(1H 1,2,4 TRIAZOL 1 YL)METHYL] 5 (4 CHLOROPHENYL) N (CYCLOHEXYLMETHYL) 1 (2,4 DICHLOROPHENYL) 1H PYRAZOLE 3 CARBOXAMIDE;
4 [(1H 1,2,4 TRIAZOL 1 YL)METHYL] 5 (4 CHLOROPHENYL) N CYCLOHEPTYL 1 (2,4 DICHLOROPHENYL) 1H PYRAZOLE 3 CARBOXAMIDE;
4 [(1H 1,2,4 TRIAZOL 1 YL)METHYL] 5 (4 CHLOROPHENYL) N CYCLOHEXYL 1 (2,4 DICHLOROPHENYL) 1H PYRAZOLE 3 CARBOXAMIDE;
4 [(1H 1,2,4 TRIAZOL 1 YL)METHYL] 5 (4 CHLOROPHENYL) N CYCLOPENTYL 1 (2,4 DICHLOROPHENYL) 1H PYRAZOLE 3 CARBOXAMIDE;
4 [(1H1,2,4 TRIAZOL 1 YL)METHYL] 5 (4 CHLOROPHENYL) 1 (2,4 DICHLOROPHENYL) N (2,6 DIMETHYLPIPERIDIN 1 YL) 1H PYRAZOLE 3 CARBOXAMIDE;
[4 ((1H 1,2,4 TRIAZOL 1 YL)METHYL) 5 (4 CHLOROPHENYL) 1 (2,4 DICHLOROPHENYL) 1H PYRAZOL 3 YL)(4 (2,3 DIMETHYLPHENYL)PIPERAZIN 1 YL]METHANONE;
ANTIOBESITY AGENT;
CANNABINOID 1 RECEPTOR;
CANNABINOID 1 RECEPTOR ANTAGONIST;
CANNABINOID 2 RECEPTOR;
DRINABANT;
IBIPINABANT;
OTENABANT;
RIMONABANT;
SP 945598;
TARANABANT;
UNCLASSIFIED DRUG;
UNINDEXED DRUG;
ANIMAL EXPERIMENT;
ANIMAL MODEL;
ARTICLE;
BINDING AFFINITY;
CONTROLLED STUDY;
DRUG BINDING;
DRUG SELECTIVITY;
DRUG SYNTHESIS;
MALE;
MOUSE;
NONHUMAN;
OBESITY;
STRUCTURE ACTIVITY RELATION;
ANIMALS;
MALE;
MICE;
MICE, INBRED C57BL;
PROTEIN BINDING;
PYRAZOLES;
RATS;
RATS, SPRAGUE-DAWLEY;
RECEPTOR, CANNABINOID, CB1;
RECEPTOR, CANNABINOID, CB2;
STRUCTURE-ACTIVITY RELATIONSHIP;
TRIAZOLES;
6
68949216617
Lee J., Song K.-S., Kang J., Lee S.H., and Lee J. Curr. Top. Med. Chem. 9 (2009) 564
(2009)
Curr. Top. Med. Chem.
, vol.9
, pp. 564
Lee, J.1
Song, K.-S.2
Kang, J.3
Lee, S.H.4
Lee, J.5
12
75149172865
US patent 54,62,960
Barth, F.; Cassellas, P.; Congy, C.; Martinez, S.; Rinaldi, M. US patent 54,62,960, 1995.
(1995)
Barth, F.1
Cassellas, P.2
Congy, C.3
Martinez, S.4
Rinaldi, M.5
13
33845950577
Lin L.S., Lanza T.J., Jewell J.P., Liu P., Shah S.K., Qi H., Tong X., Wang J., Xu S., Fong T.M., Shen C.-P., Lao J., Chen J., Shearman L.P., Stribling D.S., Rosko K., Strack A., Marsh D.J., Feng Y., Kumar S., Samuel K., Yin W., Van der Ploeg L., Goulet M.T., and Hagman W.K. J. Med. Chem. 49 (2006) 7584
(2006)
J. Med. Chem.
, vol.49
, pp. 7584
Lin, L.S.1
Lanza, T.J.2
Jewell, J.P.3
Liu, P.4
Shah, S.K.5
Qi, H.6
Tong, X.7
Wang, J.8
Xu, S.9
Fong, T.M.10
Shen, C.-P.11
Lao, J.12
Chen, J.13
Shearman, L.P.14
Stribling, D.S.15
Rosko, K.16
Strack, A.17
Marsh, D.J.18
Feng, Y.19
Kumar, S.20
Samuel, K.21
Yin, W.22
Van der Ploeg, L.23
Goulet, M.T.24
Hagman, W.K.25
more..
14
34547560379
Chen C.-y., Frey L.F., Shultz S., Wallace D.J., Marcantonio K., Payack J.F., Vazquez E., Springfield S.A., Zhou G., Liu P., Kieczykowski G.R., Chen A.M., Phenix B.D., Singh U., Strine J., Izzo B., and Krska S.W. Org. Process Res. Dev. 11 (2007) 616
(2007)
Org. Process Res. Dev.
, vol.11
, pp. 616
Chen, C.-y.1
Frey, L.F.2
Shultz, S.3
Wallace, D.J.4
Marcantonio, K.5
Payack, J.F.6
Vazquez, E.7
Springfield, S.A.8
Zhou, G.9
Liu, P.10
Kieczykowski, G.R.11
Chen, A.M.12
Phenix, B.D.13
Singh, U.14
Strine, J.15
Izzo, B.16
Krska, S.W.17
15
41849121146
Lin L.S., Ha S., Ball R.G., Tsou N.N., Castonguay L.A., Doss G.A., Fong T.M., Shen C.P., Xiao J.C., Goulet M.T., and Hagmann W.K. J. Med. Chem. 51 (2008) 2108
(2008)
J. Med. Chem.
, vol.51
, pp. 2108
Lin, L.S.1
Ha, S.2
Ball, R.G.3
Tsou, N.N.4
Castonguay, L.A.5
Doss, G.A.6
Fong, T.M.7
Shen, C.P.8
Xiao, J.C.9
Goulet, M.T.10
Hagmann, W.K.11
16
60549088559
Griffith D.A., Hadcock J.R., Black S.C., Iredale P.A., Carpino P.A., DaSilva-Jardine P., Day R., DiBrino J., Dow R.L., Landis M.S., O'Connor R.E., and Scott D.O. J. Med. Chem. 52 (2009) 234
(2009)
J. Med. Chem.
, vol.52
, pp. 234
Griffith, D.A.1
Hadcock, J.R.2
Black, S.C.3
Iredale, P.A.4
Carpino, P.A.5
DaSilva-Jardine, P.6
Day, R.7
DiBrino, J.8
Dow, R.L.9
Landis, M.S.10
O'Connor, R.E.11
Scott, D.O.12
18
0037187367
Shim J.Y., Welsh W.J., Cartier E., Edwards J.L., and Howlett A.C. J. Med. Chem. 45 (2002) 1447-1459
(2002)
J. Med. Chem.
, vol.45
, pp. 1447-1459
Shim, J.Y.1
Welsh, W.J.2
Cartier, E.3
Edwards, J.L.4
Howlett, A.C.5
19
75149190009
Barth, F, Congy, C, Gueule, P, Rinaldi-Carmona, M, Van Brodeck, D. PCT Patent WO 2006/087480 A1, 2006
Barth, F.; Congy, C.; Gueule, P.; Rinaldi-Carmona, M.; Van Brodeck, D. PCT Patent WO 2006/087480 A1, 2006
20
75149180824
Moritani, Y. PCT Patent WO 2007/046550 A1, 2007
Moritani, Y. PCT Patent WO 2007/046550 A1, 2007.
21
56749107436
Lee S.H., Seo H.J., Lee S.-H., Jung M.E., Park J.-H., Park H.-J., Yoo J., Yun H., Na J., Kang S.Y., Song K.-S., Kim M.-a., Chang C.-H., Kim J., and Lee J. J. Med. Chem. 51 (2008) 7216
(2008)
J. Med. Chem.
, vol.51
, pp. 7216
Lee, S.H.1
Seo, H.J.2
Lee, S.-H.3
Jung, M.E.4
Park, J.-H.5
Park, H.-J.6
Yoo, J.7
Yun, H.8
Na, J.9
Kang, S.Y.10
Song, K.-S.11
Kim, M.-a.12
Chang, C.-H.13
Kim, J.14
Lee, J.15
22
61849137327
Lee S.H., Seo H.J., Kim M.J., Kang S.Y., Song K.-S., Lee S.-H., Jung M.E., Kim J., and Lee J. Bioorg. Med. Chem. Lett. 19 (2009) 1899
(2009)
Bioorg. Med. Chem. Lett.
, vol.19
, pp. 1899
Lee, S.H.1
Seo, H.J.2
Kim, M.J.3
Kang, S.Y.4
Song, K.-S.5
Lee, S.-H.6
Jung, M.E.7
Kim, J.8
Lee, J.9
23
71749115522
Seo H.J., Kim M.J., Song K.-S., Lee S.-H., Jung M.E., Kim M.-S., Park H.-J., Yoo J., Chang C.-H., Kim J., and Lee J. Future Med. Chem. 1 (2009) 947
(2009)
Future Med. Chem.
, vol.1
, pp. 947
Seo, H.J.1
Kim, M.J.2
Song, K.-S.3
Lee, S.-H.4
Jung, M.E.5
Kim, M.-S.6
Park, H.-J.7
Yoo, J.8
Chang, C.-H.9
Kim, J.10
Lee, J.11
24
71749089474
Lee S.H., Seo H.J., Kim M.J., Kang S.Y., Lee S.-H., Ahn K., Lee M., Han H.-K., Kim J., and Lee J. Bioorg. Med. Chem. Lett. 19 (2009) 6632
(2009)
Bioorg. Med. Chem. Lett.
, vol.19
, pp. 6632
Lee, S.H.1
Seo, H.J.2
Kim, M.J.3
Kang, S.Y.4
Lee, S.-H.5
Ahn, K.6
Lee, M.7
Han, H.-K.8
Kim, J.9
Lee, J.10
25
75149135962
US Patent 6028,084, 2000
(a) Barth, F.; Congy, C.; Martinez, S.; Rinaldi, M. US Patent 6028,084, 2000
Barth, F.1
Congy, C.2
Martinez, S.3
Rinaldi, M.4
26
75149157908
Amengual, R, Marsol, C, Mayeux, E, Sierra, M, Wagner, P. PCT Patent WO 2006/133926 A1, 2006
Amengual, R.; Marsol, C.; Mayeux, E.; Sierra, M.; Wagner, P. PCT Patent WO 2006/133926 A1, 2006.
27
33745854821
Nielsen F.E., Ebdrup S., Jensen A.F., Ynddal L., Bodvarsdottir T.B., Stidsen C., Worsaae A., Boonen H.C.M., Arkhammar P.O.G., Fremming T., Wahl P., Kornø H.T., and Hansen J.B. J. Med. Chem. 49 (2006) 4127
(2006)
J. Med. Chem.
, vol.49
, pp. 4127
Nielsen, F.E.1
Ebdrup, S.2
Jensen, A.F.3
Ynddal, L.4
Bodvarsdottir, T.B.5
Stidsen, C.6
Worsaae, A.7
Boonen, H.C.M.8
Arkhammar, P.O.G.9
Fremming, T.10
Wahl, P.11
Kornø, H.T.12
Hansen, J.B.13
28
0027379769
Kuster J.E., Stevenson J.I., Ward S.J., D'Ambra T.E., and Haycock D.A. J. Pharmacol. Exp. Ther. 264 (1993) 1352
(1993)
J. Pharmacol. Exp. Ther.
, vol.264
, pp. 1352
Kuster, J.E.1
Stevenson, J.I.2
Ward, S.J.3
D'Ambra, T.E.4
Haycock, D.A.5
30
68949135354
Dow R.L., Hadcock J.R., Scott D.O., Schneider S.R., Paight E.S., Iredale P.A., Carpino P.A., Griffith D.A., Hammond M., and DaSilva-Jardine P. Bioorg. Med. Chem. Lett. 19 (2009) 5351
(2009)
Bioorg. Med. Chem. Lett.
, vol.19
, pp. 5351
Dow, R.L.1
Hadcock, J.R.2
Scott, D.O.3
Schneider, S.R.4
Paight, E.S.5
Iredale, P.A.6
Carpino, P.A.7
Griffith, D.A.8
Hammond, M.9
DaSilva-Jardine, P.10
31
75149179924
Kang S.Y., Lee S.-H., Seo H.J., Jung M.E., Ahn K., Kim J., and Lee J. Bioorg. Med. Chem. Lett. 18 (2008) 2384
(2008)
Bioorg. Med. Chem. Lett.
, vol.18
, pp. 2384
Kang, S.Y.1
Lee, S.-H.2
Seo, H.J.3
Jung, M.E.4
Ahn, K.5
Kim, J.6
Lee, J.7
33
75149160848
note
50 = 5.0 ± 1.0 nM) in each different assay (>1800 compounds tested). Therefore, we believe that all SAR discussions in the manuscript in the manuscript are scientifically meaningful.
34
0030826705
Bouaboula M., Perrachon S., Milligan L., Canat X., Rinaldi-Carmona M., Potier M., Barth F., Calandra B., Pecceu F., Lupker J., Maffrand J.P., Le Fur G., and Casellas P. J. Biol. Chem. 272 (1997) 22330
(1997)
J. Biol. Chem.
, vol.272
, pp. 22330
Bouaboula, M.1
Perrachon, S.2
Milligan, L.3
Canat, X.4
Rinaldi-Carmona, M.5
Potier, M.6
Barth, F.7
Calandra, B.8
Pecceu, F.9
Lupker, J.10
Maffrand, J.P.11
Le Fur, G.12
Casellas, P.13
35
0032968566
Calandra B., Portier M., Kerneis A., Delpech M., Carillon C., Le Fur G., Ferrara P., and Shire D. Eur. J. Pharmacol. 374 (1999) 445
(1999)
Eur. J. Pharmacol.
, vol.374
, pp. 445
Calandra, B.1
Portier, M.2
Kerneis, A.3
Delpech, M.4
Carillon, C.5
Le Fur, G.6
Ferrara, P.7
Shire, D.8