-
5
-
-
79956067846
-
-
Atlanta, GA Poster 1119
-
Genovese, M. C.; Gao, L.; Yin, J.; Smith, S.; Weinblatt, M.; Smolen, J.; Wang, X.; Schieven, G.; Garcia-Meijide, J. A.; Latek, R.; Pasternak, R.; Kaul, S.; Roy, A.; Raymond, R., Thienel, U.; Wang, J. Presented at the American College of Rheumatology Scientific Meeting; Atlanta, GA, 2010; Poster 1119.
-
(2010)
Presented at the American College of Rheumatology Scientific Meeting
-
-
Genovese, M.C.1
Gao, L.2
Yin, J.3
Smith, S.4
Weinblatt, M.5
Smolen, J.6
Wang, X.7
Schieven, G.8
Garcia-Meijide, J.A.9
Latek, R.10
Pasternak, R.11
Kaul, S.12
Roy, A.13
Raymond, R.14
Thienel, U.15
Wang, J.16
-
6
-
-
54949126342
-
-
G. Schett, C. Stach, J. Zwerina, R. Voll, and B. Manger Arthritis Rheum. 58 2008 2936
-
(2008)
Arthritis Rheum.
, vol.58
, pp. 2936
-
-
Schett, G.1
Stach, C.2
Zwerina, J.3
Voll, R.4
Manger, B.5
-
9
-
-
57349130600
-
-
R.J. Hill, K. Dabbagh, D. Phippard, C. Li, R.T. Suttmann, M. Welch, E. Papp, K.W. Song, K.-C. Chang, D. Leaffer, Y.-N. Kim, R.T. Roberts, T.S. Zabka, D. Aud, J. Dal Porto, A.M. Manning, S.L. Peng, D.M. Goldstein, and B.R. Wong J. Pharmacol. Exp. Ther. 327 2008 610
-
(2008)
J. Pharmacol. Exp. Ther.
, vol.327
, pp. 610
-
-
Hill, R.J.1
Dabbagh, K.2
Phippard, D.3
Li, C.4
Suttmann, R.T.5
Welch, M.6
Papp, E.7
Song, K.W.8
Chang, K.-C.9
Leaffer, D.10
Kim, Y.-N.11
Roberts, R.T.12
Zabka, T.S.13
Aud, D.14
Dal Porto, J.15
Manning, A.M.16
Peng, S.L.17
Goldstein, D.M.18
Wong, B.R.19
-
10
-
-
59649114148
-
-
S.B. Cohen, T.T. Cheng, V. Chindalore, N. Damjanov, R. Burgos-Vargas, P. Delora, K. Zimany, H. Travers, and J.P. Caulfield Arthritis Rheum. 60 2009 335
-
(2009)
Arthritis Rheum.
, vol.60
, pp. 335
-
-
Cohen, S.B.1
Cheng, T.T.2
Chindalore, V.3
Damjanov, N.4
Burgos-Vargas, R.5
Delora, P.6
Zimany, K.7
Travers, H.8
Caulfield, J.P.9
-
11
-
-
75749115980
-
-
R.E. Alten, C. Zerbini, S. Jeka, F. Irazoque, F. Khatib, P. Emery, A. Bertasso, M. Rabbia, and J.P. Caulfield Ann. Rheum. Dis. 69 2010 364
-
(2010)
Ann. Rheum. Dis.
, vol.69
, pp. 364
-
-
Alten, R.E.1
Zerbini, C.2
Jeka, S.3
Irazoque, F.4
Khatib, F.5
Emery, P.6
Bertasso, A.7
Rabbia, M.8
Caulfield, J.P.9
-
12
-
-
79953795938
-
-
D.M. Goldstein, M.J. Soth, T. Gabriel, N. Dewdney, A. Kuglstatter, H. Arzeno, J. Chen, W. Bingenheimer, S.A. Dalrymple, J. Dunn, R. Farrell, S. Frauchiger, J. La Fargue, M. Ghate, B. Graves, R.J. Hill, F. Li, R. Litman, B. Loe, J. McIntosh, D. McWeeney, E. Papp, J. Park, H.F. Reese, R.T. Roberts, D. Rotstein, B. San Pablo, K. Sarma, M. Stahl, M. Sung, R.T. Suttman, E.B. Sjogren, Y. Tan, A. Trejo, M. Welch, P. Weller, B.R. Wong, and H. Zecic J. Med. Chem. 54 2011 2255
-
(2011)
J. Med. Chem.
, vol.54
, pp. 2255
-
-
Goldstein, D.M.1
Soth, M.J.2
Gabriel, T.3
Dewdney, N.4
Kuglstatter, A.5
Arzeno, H.6
Chen, J.7
Bingenheimer, W.8
Dalrymple, S.A.9
Dunn, J.10
Farrell, R.11
Frauchiger, S.12
La Fargue, J.13
Ghate, M.14
Graves, B.15
Hill, R.J.16
Li, F.17
Litman, R.18
Loe, B.19
McIntosh, J.20
McWeeney, D.21
Papp, E.22
Park, J.23
Reese, H.F.24
Roberts, R.T.25
Rotstein, D.26
San Pablo, B.27
Sarma, K.28
Stahl, M.29
Sung, M.30
Suttman, R.T.31
Sjogren, E.B.32
Tan, Y.33
Trejo, A.34
Welch, M.35
Weller, P.36
Wong, B.R.37
Zecic, H.38
more..
-
14
-
-
79956070010
-
-
Representative experimental procedures for compounds can be found in WO 2007/023110
-
Representative experimental procedures for compounds can be found in WO 2007/023110.
-
-
-
-
15
-
-
19744365702
-
-
M.A. Fabian, W.H. Biggs III, D.K. Treiber, C.E. Atteridge, M.D. Azimioara, M.G. Benedetti, T.A. Carter, P. Ciceri, P.T. Edeen, M. Floyd, J.M. Ford, M. Galvin, J.L. Gerlach, R.M. Grotzfeld, S. Herrgard, D.E. Insko, M.A. Insko, A.G. Lai, J.-M. Lelias, S.A. Mehta, Z.V. Milanov, A.M. Velasco, L.M. Wodicka, H.K. Patel, P.P. Zarrinkar, and D.J. Lockhart Nat. Biotechnol. 23 2005 329
-
(2005)
Nat. Biotechnol.
, vol.23
, pp. 329
-
-
Fabian, M.A.1
Iii, H.B.W.2
Treiber, D.K.3
Atteridge, C.E.4
Azimioara, M.D.5
Benedetti, M.G.6
Carter, T.A.7
Ciceri, P.8
Edeen, P.T.9
Floyd, M.10
Ford, J.M.11
Galvin, M.12
Gerlach, J.L.13
Grotzfeld, R.M.14
Herrgard, S.15
Insko, D.E.16
Insko, M.A.17
Lai, A.G.18
Lelias, J.-M.19
Mehta, S.A.20
Milanov, Z.V.21
Velasco, A.M.22
Wodicka, L.M.23
Patel, H.K.24
Zarrinkar, P.P.25
Lockhart, D.J.26
more..
-
16
-
-
84856076831
-
-
8 compound 23 at 10 μM displaces ligands for the following kinases at the percents indicated: p38α, p38β, JNK1, JNK2, and JNK3 (100%); CSNK1E (88%); GAK (87%); and STK36 (74%). Ambit Kd's were determined for p38α (1.2 nM), p38β (8.7 nM), JNK1 (110 nM), JNK2 (16 nM) and JNK3 (16 nM)
-
8 compound 23 at 10 μM displaces ligands for the following kinases at the percents indicated: p38α, p38β, JNK1, JNK2, and JNK3 (100%); CSNK1E (88%); GAK (87%); and STK36 (74%). Ambit Kd's were determined for p38α (1.2 nM), p38β (8.7 nM), JNK1 (110 nM), JNK2 (16 nM) and JNK3 (16 nM).
-
-
-
-
17
-
-
54549083435
-
-
B. Herberich, G-Q. Cao, P.P. Chakrabarti, J.R. Falsey, L. Pettus, R.M. Rzasa, A.B. Reed, A. Reichelt, K. Sham, M. Thaman, R.P. Wurz, S. Xu, D. Zhang, F. Hsieh, M.R. Lee, R. Syed, V. Li, D. Grosfeld, M.H. Plant, B. Henkle, L. Sherman, S. Middleton, L.M. Wong, and A.S. Tasker J. Med. Chem. 51 2008 6271
-
(2008)
J. Med. Chem.
, vol.51
, pp. 6271
-
-
Herberich, B.1
Cao, G.-Q.2
Chakrabarti, P.P.3
Falsey, J.R.4
Pettus, L.5
Rzasa, R.M.6
Reed, A.B.7
Reichelt, A.8
Sham, K.9
Thaman, M.10
Wurz, R.P.11
Xu, S.12
Zhang, D.13
Hsieh, F.14
Lee, M.R.15
Syed, R.16
Li, V.17
Grosfeld, D.18
Plant, M.H.19
Henkle, B.20
Sherman, L.21
Middleton, S.22
Wong, L.M.23
Tasker, A.S.24
more..
-
18
-
-
79956149738
-
-
note
-
3S) C, H, N. Specific rotation (MeOH)-34.000 °/g/100 mL.
-
-
-
-
19
-
-
79956131067
-
-
note
-
All animal procedures were approved by the Institutional Animal Care and Use Committee of Roche Palo Alto. Compound was administered (p.o.) to Hanover-Wistar rats 0.5 h prior to challenge with 50 μg/kg LPS (i.e., 0.9% saline). Serum was collected 1.5 h after LPS injection and analyzed for TNF-α levels (ELISA) and drug concentrations.
-
-
-
-
25
-
-
0142060917
-
-
A. Trejo, Humberto Arzeno, Michelle F. Browner, Sushmita Chanda, Soan Cheng, Daniel D. Comer, Stacie A. Dalrymple, Pete Dunten, JoAnn La Fargue, Brett Lovejoy, Jose Freire-Moar, Julie Lim, Joel McIntosh, Jennifer Miller, Eva Papp, Deborah Reuter, Rick Roberts, Florentino Sanpablo, John Saunders, Kyung Song, Armando Villasenor, Stephen D. Warren, Mary Welch, Paul Weller, Phyllis E. Whiteley, Lu Zeng, and David M. Goldstein J. Med. Chem. 46 2003 4702
-
(2003)
J. Med. Chem.
, vol.46
, pp. 4702
-
-
Trejo, A.1
Arzeno, H.2
Browner, M.F.3
Chanda, S.4
Cheng, S.5
Comer, D.D.6
Dalrymple, S.A.7
Dunten, P.8
La Fargue, J.9
Lovejoy, B.10
Freire-Moar, J.11
Lim, J.12
McIntosh, J.13
Miller, J.14
Papp, E.15
Reuter, D.16
Roberts, R.17
Sanpablo, F.18
Saunders, J.19
Song, K.20
Villasenor, A.21
Warren, S.D.22
Welch, M.23
Weller, P.24
Whiteley, P.E.25
Zeng, L.26
Goldstein, D.M.27
more..
|