-
1
-
-
2642559875
-
Targeting IL-1 in inflammatory disease: New opportunities for therapeutic intervention
-
Braddock, M.; Quinn, A. Targeting IL-1 in inflammatory disease: new opportunities for therapeutic intervention. Nat. Rev. Drug Discov. 2004, 3, 330-340.
-
(2004)
Nat. Rev. Drug Discov.
, vol.3
, pp. 330-340
-
-
Braddock, M.1
Quinn, A.2
-
2
-
-
0037289461
-
Anti-TNFalpha therapy for rheumatoid arthritis: An update
-
Taylor, P.C. Anti-TNFalpha therapy for rheumatoid arthritis: an update. Intern. Med. 2003, 42, 15-20.
-
(2003)
Intern. Med.
, vol.42
, pp. 15-20
-
-
Taylor, P.C.1
-
3
-
-
0142058174
-
Anti-TNF-α therapies: The next generation
-
Palladino, M.A.; Bahjat, F.R.; Theodorakis, E.A.; Moldawer, L.L. Anti-TNF-α therapies: the next generation. Nat. Rev. Drug Discov. 2003, 2, 736-746.
-
(2003)
Nat. Rev. Drug Discov.
, vol.2
, pp. 736-746
-
-
Palladino, M.A.1
Bahjat, F.R.2
Theodorakis, E.A.3
Moldawer, L.L.4
-
4
-
-
0035932519
-
Cytokine pathways and joint inflammation in rheumatoid arthritis
-
Choy, E.H.; Panayi, G.S. Cytokine pathways and joint inflammation in rheumatoid arthritis. N. Engl. J. Med. 2001, 344, 907-916.
-
(2001)
N. Engl. J. Med.
, vol.344
, pp. 907-916
-
-
Choy, E.H.1
Panayi, G.S.2
-
5
-
-
0028605318
-
A protein kinase involved in the regulation of inflammatory cytokine biosynthesis
-
Lee, J.C.; Laydon, J.T.; McDonnell, P.C.; Gallagher, T.F.; Kumar, S.; Green, D.; McNulty, D.; Blumenthal, M.J.; Heyes, J.R. A protein kinase involved in the regulation of inflammatory cytokine biosynthesis. Nat. (London) 1994, 372, 739-746.
-
(1994)
Nat. (London)
, vol.372
, pp. 739-746
-
-
Lee, J.C.1
Laydon, J.T.2
McDonnell, P.C.3
Gallagher, T.F.4
Kumar, S.5
Green, D.6
McNulty, D.7
Blumenthal, M.J.8
Heyes, J.R.9
-
6
-
-
0142026209
-
p38 MAP kinases: Key signalling molecules as therapeutic targets for inflammatory diseases
-
Kumar, S.; Boehm, J.; Lee, J.C. p38 MAP kinases: key signalling molecules as therapeutic targets for inflammatory diseases. Nat. Rev. Drug Discov. 2003, 2, 717-726.
-
(2003)
Nat. Rev. Drug Discov.
, vol.2
, pp. 717-726
-
-
Kumar, S.1
Boehm, J.2
Lee, J.C.3
-
7
-
-
0021350020
-
Antiinflammatory activity of 5,6-diaryl-2,3-dihydroimidazo[2,1-thiazoles. Isomeric 4-pyridyl and 4-substituted phenyl derivatives
-
Lantos, I.; Bender, P.E.; Razgaitis, K.A.; Sutton, B.M.; DiMartino, M.J.; Griswold, D.E.; Walz, D.T. Antiinflammatory activity of 5,6-diaryl-2,3-dihydroimidazo[2,1-#1b]thiazoles. Isomeric 4-pyridyl and 4-substituted phenyl derivatives. J. Med. Chem. 1984, 27, 72-75.
-
(1984)
J. Med. Chem.
, vol.27
, pp. 72-75
-
-
Lantos, I.1
Bender, P.E.2
Razgaitis, K.A.3
Sutton, B.M.4
DiMartino, M.J.5
Griswold, D.E.6
Walz, D.T.7
-
8
-
-
0033030207
-
p38 mitogen-activated protein kinase inhibitors - Mechanisms and therapeutic potentials
-
Lee, J.C.; Kassis, S.; Kumar, S.; Badger, A.; Adams, JL. p38 mitogen-activated protein kinase inhibitors - mechanisms and therapeutic potentials. Pharmacol. Therap. 1999, 82, 389-397.
-
(1999)
Pharmacol. Therap.
, vol.82
, pp. 389-397
-
-
Lee, J.C.1
Kassis, S.2
Kumar, S.3
Badger, A.4
Adams, J.L.5
-
10
-
-
0034513614
-
Potential of p38 inhibitors in the treatment of rheumatoid arthritis
-
Foster, M.L.; Halley, F.; Souness, J.E. Potential of p38 inhibitors in the treatment of rheumatoid arthritis. Drug News Perspect. 2000, 13, 488-497.
-
(2000)
Drug News Perspect.
, vol.13
, pp. 488-497
-
-
Foster, M.L.1
Halley, F.2
Souness, J.E.3
-
11
-
-
0034045949
-
Inhibition of p38 MAP kinase as a therapeutic strategy
-
Lee, J.C.; Kumar, S.; Griswold, D.E.; Underwood, D.C.; Votta, B.J.; Adams, J.L. Inhibition of p38 MAP kinase as a therapeutic strategy. Immunopharmacol. 2000, 47, 185-201.
-
(2000)
Immunopharmacol.
, vol.47
, pp. 185-201
-
-
Lee, J.C.1
Kumar, S.2
Griswold, D.E.3
Underwood, D.C.4
Votta, B.J.5
Adams, J.L.6
-
12
-
-
0036715931
-
Pyridinylimidazole based p38 MAP kinase inhibitors
-
Jackson, P.F.; Bullington, J.L. Pyridinylimidazole based p38 MAP kinase inhibitors. Curr. Top. Med. Chem. (Hilversum, Netherlands) 2002, 2, 1011-1020.
-
(2002)
Curr. Top. Med. Chem. (Hilversum, Netherlands)
, vol.2
, pp. 1011-1020
-
-
Jackson, P.F.1
Bullington, J.L.2
-
13
-
-
8044257704
-
A metalloproteinase disintegrin that releases tumour-necrosis factor- alpha from cells
-
Black, R.A.; Rauch, C.T.; Kozlosky, C.J.; Peschon, J.J.; Slack, J.L.; Wolfson, M.F.; Castner, B.J.; Stocking, K.L.; Reddy, P.; Srinivasan, S.; Nelson, N.; Boiani, N.; Schooley, K-A.; Gerhart, M.; Davis, R.; Fitzner, J.N.; Johnson, R.S.; Paxton, R.J.; March, C.J.; Cerretti, D.P. A metalloproteinase disintegrin that releases tumour-necrosis factor- alpha from cells. Nature 1997, 385, 729-33.
-
(1997)
Nature
, vol.385
, pp. 729-733
-
-
Black, R.A.1
Rauch, C.T.2
Kozlosky, C.J.3
Peschon, J.J.4
Slack, J.L.5
Wolfson, M.F.6
Castner, B.J.7
Stocking, K.L.8
Reddy, P.9
Srinivasan, S.10
Nelson, N.11
Boiani, N.12
Schooley, K.-A.13
Gerhart, M.14
Davis, R.15
Fitzner, J.N.16
Johnson, R.S.17
Paxton, R.J.18
March, C.J.19
Cerretti, D.P.20
more..
-
14
-
-
8044250278
-
Cloning of a disintegrin metalloproteinase that processes precursor tumour-necrosis factor-alpha
-
Moss, M.L.; Jin, S.L; Milla, M.E.; Bickett, D.M.; Burkhart, W.; Carter, H.L.; Chen, W.J.; Clay, W.C.; Didsbury, J.R.; Hassler, D.; Hoffman, C.R.; Kost, T.A.; Lambert, M.H.; Leesnitzer, M.A.; McCauley, P.; McGeehan, G.; Mitchell, J.; Moyer, M.; Pahel, G.; Rocque, W.; Overton, L.K.; Schoenen, F.; Seaton, T.; Su, J.L.; Becherer, J.D. Cloning of a disintegrin metalloproteinase that processes precursor tumour-necrosis factor-alpha. Nature 1997, 385, 733-736.
-
(1997)
Nature
, vol.385
, pp. 733-736
-
-
Moss, M.L.1
Jin, S.L.2
Milla, M.E.3
Bickett, D.M.4
Burkhart, W.5
Carter, H.L.6
Chen, W.J.7
Clay, W.C.8
Didsbury, J.R.9
Hassler, D.10
Hoffman, C.R.11
Kost, T.A.12
Lambert, M.H.13
Leesnitzer, M.A.14
McCauley, P.15
McGeehan, G.16
Mitchell, J.17
Moyer, M.18
Pahel, G.19
Rocque, W.20
Overton, L.K.21
Schoenen, F.22
Seaton, T.23
Su, J.L.24
Becherer, J.D.25
more..
-
15
-
-
0026507126
-
A novel heterodimeric cysteine protease is required for interleukin-1 beta processing in monocytes
-
Thornberry, N.A.; Bull, H.G.; Calaycay, J.R.; Chapman, K.T.; Howard, A.D.; Kostura, M.J.; Miller, D.K.; Molineaux, S.M.; Weidner, J.R.; Aunins, J. A novel heterodimeric cysteine protease is required for interleukin-1 beta processing in monocytes. Nature 1992, 356, 768-774.
-
(1992)
Nature
, vol.356
, pp. 768-774
-
-
Thornberry, N.A.1
Bull, H.G.2
Calaycay, J.R.3
Chapman, K.T.4
Howard, A.D.5
Kostura, M.J.6
Miller, D.K.7
Molineaux, S.M.8
Weidner, J.R.9
Aunins, J.10
-
16
-
-
0030954172
-
A highly specific inhibitor of human p38 MAP kinase binds in the ATP pocket
-
Tong, L.; Pav, S.; White, D.M.; Rogers, S.; Crane, K.M,; Cywin, C.L.; Brown, M.L.; Pargellis, C.A. A highly specific inhibitor of human p38 MAP kinase binds in the ATP pocket. Nat. Struct. Biol. 1997, 4, 311-316.
-
(1997)
Nat. Struct. Biol.
, vol.4
, pp. 311-316
-
-
Tong, L.1
Pav, S.2
White, D.M.3
Rogers, S.4
Crane, K.M.5
Cywin, C.L.6
Brown, M.L.7
Pargellis, C.A.8
-
17
-
-
12644277392
-
The structural basis for the specificity of pyridinylimidazole inhibitors of p38 MAP kinase
-
Wilson, K.P.; McCaffrey, P.G.; Hsiao, K.; Pazhinisamy, S.; Galullo, V.; Bemis, G.W.; Fitzgibbon, M.J.; Caron, P.R.; Murcko, M.A.; Su, M.S.S. The structural basis for the specificity of pyridinylimidazole inhibitors of p38 MAP kinase. Chem. Biol. 1997, 4, 423-431.
-
(1997)
Chem. Biol.
, vol.4
, pp. 423-431
-
-
Wilson, K.P.1
McCaffrey, P.G.2
Hsiao, K.3
Pazhinisamy, S.4
Galullo, V.5
Bemis, G.W.6
Fitzgibbon, M.J.7
Caron, P.R.8
Murcko, M.A.9
Su, M.S.S.10
-
18
-
-
0032530336
-
Structural basis of inhibitor selectivity in MAP kinases
-
Wang, Z.; Canagarajah, B.J.; Boehm, J.C.; Kassisa, S.; Cobb, M.H.; Young, P.R.; Abdel-Meguid, S.; Adams, J.L.; Goldsmith, E.J. Structural basis of inhibitor selectivity in MAP kinases. Structure 1998, 6, 1117-1128.
-
(1998)
Structure
, vol.6
, pp. 1117-1128
-
-
Wang, Z.1
Canagarajah, B.J.2
Boehm, J.C.3
Kassisa, S.4
Cobb, M.H.5
Young, P.R.6
Abdel-Meguid, S.7
Adams, J.L.8
Goldsmith, E.J.9
-
19
-
-
10744227768
-
Acquisition of sensitivity of stress-activated protein kinases to the p38 inhibitor, SB 203580, by alteration of one or more amino acids within the ATP binding pocket
-
Gum, R.J.; Mclaughlin, M.M.; Kumar, S.; Wang, Z.; Bower, M.J.; Lee, J.C.; Adams, J.L.; Livi, G.P.; Goldsmith, E.J.; Young, P.R. Acquisition of sensitivity of stress-activated protein kinases to the p38 inhibitor, SB 203580, by alteration of one or more amino acids within the ATP binding pocket. J. Biol. Chem. 1998, 273, 15605-15610.
-
(1998)
J. Biol. Chem.
, vol.273
, pp. 15605-15610
-
-
Gum, R.J.1
Mclaughlin, M.M.2
Kumar, S.3
Wang, Z.4
Bower, M.J.5
Lee, J.C.6
Adams, J.L.7
Livi, G.P.8
Goldsmith, E.J.9
Young, P.R.10
-
20
-
-
0032564311
-
Molecular basis for p38 protein kinase inhibitor specificity
-
Lisnock, J.; Tebben, A.; Frantz, B.; O'Neill, E.A.; Croft, G.; O'Keefe, S.J.; Li, B.; Hacker, C.; de Laszlo, S.; Smith, A.; Libby, B.; Liverton, N.; Hermes, J.; LoGrasso, P. Molecular basis for p38 protein kinase inhibitor specificity. Biochemistry 1998, 37, 16573-16581.
-
(1998)
Biochemistry
, vol.37
, pp. 16573-16581
-
-
Lisnock, J.1
Tebben, A.2
Frantz, B.3
O'Neill, E.A.4
Croft, G.5
O'Keefe, S.J.6
Li, B.7
Hacker, C.8
de Laszlo, S.9
Smith, A.10
Libby, B.11
Liverton, N.12
Hermes, J.13
LoGrasso, P.14
-
21
-
-
0030924833
-
Pyridinyl imidazole inhibitors of p38 mitogen-activated protein kinase bind in the ATP site
-
Young, P.R.; McLaughlin, M.M.; Kumar, S.; Kassis, S.; Doyle, M.L.; McNulty, D.; Gallagher, T.F.; Fisher, S.; McDonnell, P.C.; Carr, S.A.; Huddleston, M.J.; Seibel, G.; Porter, T.G.; Livi, G.P.; Adams, J.L.; Lee, J.C. Pyridinyl imidazole inhibitors of p38 mitogen-activated protein kinase bind in the ATP site. J. Biol. Chem. 1997, 272, 12116-12121.
-
(1997)
J. Biol. Chem.
, vol.272
, pp. 12116-12121
-
-
Young, P.R.1
McLaughlin, M.M.2
Kumar, S.3
Kassis, S.4
Doyle, M.L.5
McNulty, D.6
Gallagher, T.F.7
Fisher, S.8
McDonnell, P.C.9
Carr, S.A.10
Huddleston, M.J.11
Seibel, G.12
Porter, T.G.13
Livi, G.P.14
Adams, J.L.15
Lee, J.C.16
-
22
-
-
0032541986
-
Pyrimidinylimidazole inhibitors of CSBP/p38 kinase demonstrating decreased inhibition of hepatic cytochrome P450 enzymes
-
Adams, J.L.; Boehm, J.C.; Kassis, S.; Gorycki, P.D.; Webb, E.F.; Hall, R.; Sorenson, M.; Lee, J.C.; Ayrton, A.; Griswold, D.E.; Gallagher, T.F. Pyrimidinylimidazole inhibitors of CSBP/p38 kinase demonstrating decreased inhibition of hepatic cytochrome P450 enzymes. Bioorg. Med. Chem. Lett. 1998, 8, 3111-3116.
-
(1998)
Bioorg. Med. Chem. Lett.
, vol.8
, pp. 3111-3116
-
-
Adams, J.L.1
Boehm, J.C.2
Kassis, S.3
Gorycki, P.D.4
Webb, E.F.5
Hall, R.6
Sorenson, M.7
Lee, J.C.8
Ayrton, A.9
Griswold, D.E.10
Gallagher, T.F.11
-
23
-
-
0033578080
-
Design and synthesis of potent, selective, and orally bioavailable tetrasubstituted imidazole inhibitors of p38 mitogen-activated protein kinase
-
Liverton, N.J.; Butcher, J.W.; Claiborne, C.F. Claremon, D.A.; Libby, B.E.; Nguyen, K.T.; Pitzenberger, S.M.; Selnick, H.G.; Smith, G.R.; Tebben, A.; Vacca, J.P.; Varga, S.L.; Agarwal, L.; Dancheck, K.; Forsyth, A.J.; Fletcher, D.S.; Frantz, B.; Hanlon, W.A.; Harper, C.F.; Hofsess, S.J.; Kostura, M.; Lin, J.; Luell, S.; O'Neill, E.A.; Orevillo, C.J.; Pang, M.; Parsons, J.; Rolando, A.; Sahly, Y.; Visco, D.M.; O'Keefe, S.J. Design and synthesis of potent, selective, and orally bioavailable tetrasubstituted imidazole inhibitors of p38 mitogen-activated protein kinase. J. Med. Chem. 1999, 42, 2180-2190.
-
(1999)
J. Med. Chem.
, vol.42
, pp. 2180-2190
-
-
Liverton, N.J.1
Butcher, J.W.2
Claiborne, C.F.3
Claremon, D.A.4
Libby, B.E.5
Nguyen, K.T.6
Pitzenberger, S.M.7
Selnick, H.G.8
Smith, G.R.9
Tebben, A.10
Vacca, J.P.11
Varga, S.L.12
Agarwal, L.13
Dancheck, K.14
Forsyth, A.J.15
Fletcher, D.S.16
Frantz, B.17
Hanlon, W.A.18
Harper, C.F.19
Hofsess, S.J.20
Kostura, M.21
Lin, J.22
Luell, S.23
O'Neill, E.A.24
Orevillo, C.J.25
Pang, M.26
Parsons, J.27
Rolando, A.28
Sahly, Y.29
Visco, D.M.30
O'Keefe, S.J.31
more..
-
24
-
-
0038642267
-
Novel substituted pyridinyl imidazoles as potent anticytokine agents with low activity against hepatic cytochrome P450 enzymes
-
Laufer, S.A.; Wagner, G.K.; Kotschenreuther, D.A.; Albrecht, W. Novel substituted pyridinyl imidazoles as potent anticytokine agents with low activity against hepatic cytochrome P450 enzymes. J. Med. Chem. 2003, 46, 3230-3244.
-
(2003)
J. Med. Chem.
, vol.46
, pp. 3230-3244
-
-
Laufer, S.A.1
Wagner, G.K.2
Kotschenreuther, D.A.3
Albrecht, W.4
-
25
-
-
0029042823
-
2,4,5-Triarylimidazole inhibitors of IL-1 biosynthesis
-
Gallagher, T.F.; Fier-Thompson, S.M.; Garigipati, R.S.; Sorenson, M.E.; Smietana, J.M.; Lee, D.; Bender, P.E.; Lee, J.C.; Laydon, J.T. 2,4,5-Triarylimidazole inhibitors of IL-1 biosynthesis. Bioorg. Med. Chem. Lett. 1995, 5, 1171-1176.
-
(1995)
Bioorg. Med. Chem. Lett.
, vol.5
, pp. 1171-1176
-
-
Gallagher, T.F.1
Fier-Thompson, S.M.2
Garigipati, R.S.3
Sorenson, M.E.4
Smietana, J.M.5
Lee, D.6
Bender, P.E.7
Lee, J.C.8
Laydon, J.T.9
-
26
-
-
10144243335
-
1-substituted 4-aryl-5-pyridinylimidazoles: A new class of cytokine suppressive drugs with low 5-lipoxygenase and cyclooxygenase inhibitory potency
-
Boehm, J.C.; Smietana, J.M.; Sorenson, M.E.; Garigipati, R.S.; Gallagher, T.F.; Sheldrake, P.L.; Bradbeer, J.; Badger, A.M.; Laydon, J.T.; Lee, J.C.; Hillegass, L.M.; Griswold, D.E.; Breton, J.J.; Chabot-Fletcher, M.C.; Adams, J.L. 1-substituted 4-aryl-5-pyridinylimidazoles: a new class of cytokine suppressive drugs with low 5-lipoxygenase and cyclooxygenase inhibitory potency. J. Med. Chem. 1996, 39, 3929-3937.
-
(1996)
J. Med. Chem.
, vol.39
, pp. 3929-3937
-
-
Boehm, J.C.1
Smietana, J.M.2
Sorenson, M.E.3
Garigipati, R.S.4
Gallagher, T.F.5
Sheldrake, P.L.6
Bradbeer, J.7
Badger, A.M.8
Laydon, J.T.9
Lee, J.C.10
Hillegass, L.M.11
Griswold, D.E.12
Breton, J.J.13
Chabot-Fletcher, M.C.14
Adams, J.L.15
-
27
-
-
17644437502
-
Regulation of stress-induced cytokine production by pyridinylimidazoles; inhibition of CSBP kinase
-
Gallagher, T.F.; Seibel, G.L.; Kassis, S.; Laydon, J.T.; Blumenthal, M.J.; Lee, J.C.; Lee, D.; Boehm, J.C.; Fier-Thompson, S.M.; Abt, J.W.; Soreson, M.E.; Smietana, J.M.; Hall, R.F.; Garigipati, R.S.; Bender, P.E.; Erhard, K.F.; Krog, A.J.; Hofmann, G.A.; Sheldrake, P.L.; McDonnell, P.C.; Kumar, S.; Young, P.R.; Adams, J.L. Regulation of stress-induced cytokine production by pyridinylimidazoles; inhibition of CSBP kinase. Bioorg. Med. Chem, 1997, 5, 49-64.
-
(1997)
Bioorg. Med. Chem
, vol.5
, pp. 49-64
-
-
Gallagher, T.F.1
Seibel, G.L.2
Kassis, S.3
Laydon, J.T.4
Blumenthal, M.J.5
Lee, J.C.6
Lee, D.7
Boehm, J.C.8
Fier-Thompson, S.M.9
Abt, J.W.10
Soreson, M.E.11
Smietana, J.M.12
Hall, R.F.13
Garigipati, R.S.14
Bender, P.E.15
Erhard, K.F.16
Krog, A.J.17
Hofmann, G.A.18
Sheldrake, P.L.19
McDonnell, P.C.20
Kumar, S.21
Young, P.R.22
Adams, J.L.23
more..
-
28
-
-
0037136006
-
SAR of 2,6-diamino-3,5-difluoropyridinyl substituted heterocycles as novel p38 MAP kinase inhibitors
-
Revesz, L,; Di Padova, F.E.; Buhl, T.; Feifel, R.; Gram, H.; Hiestand, P.; Manning, U.; Wolf, R.; Zimmerlin, A.G. SAR of 2,6-diamino-3,5-difluoropyridinyl substituted heterocycles as novel p38 MAP kinase inhibitors. Bioorg. Med. Chem. Lett. 2002, 12, 2109-2112.
-
(2002)
Bioorg. Med. Chem. Lett.
, vol.12
, pp. 2109-2112
-
-
Revesz, L.1
Di Padova, F.E.2
Buhl, T.3
Feifel, R.4
Gram, H.5
Hiestand, P.6
Manning, U.7
Wolf, R.8
Zimmerlin, A.G.9
-
29
-
-
33646202755
-
Preparation of 1,5-disubstituted-3,4-dihydro-1H-pyrimido[4,5-d]pyrimidin-2-ones for treatment of CSBP/p38 kinase mediated diseases
-
Edited by Smithkline Beecham Corp. 2001-US6688[0164679], 102. WO. Ref Type: Patent
-
Adams, J.L.; Boehm, J.C.; Hall, R.F.; Taggart, J.J. Preparation of 1,5-disubstituted-3,4-dihydro-1H-pyrimido[4,5-d]pyrimidin-2-ones for treatment of CSBP/p38 kinase mediated diseases. Edited by Smithkline Beecham Corp. 2001-US6688[0164679], 102. 2001. WO. Ref Type: Patent
-
(2001)
-
-
Adams, J.L.1
Boehm, J.C.2
Hall, R.F.3
Taggart, J.J.4
-
30
-
-
0031714877
-
SB202190, a selective inhibitor of p38 mitogen-activated protein kinase, is a powerful regulator of LPS-induced mRNAs in monocytes
-
Manthey, C.L.; Wang, S.W.; Kinney, S.D.; Yao, Z. SB202190, a selective inhibitor of p38 mitogen-activated protein kinase, is a powerful regulator of LPS-induced mRNAs in monocytes. J. Leukoc. Biol. 1998, 64, 409-417.
-
(1998)
J. Leukoc. Biol.
, vol.64
, pp. 409-417
-
-
Manthey, C.L.1
Wang, S.W.2
Kinney, S.D.3
Yao, Z.4
-
31
-
-
0035086636
-
The discovery of RPR 200765A, a p38 MAP kinase inhibitor displaying a good oral anti-arthritic efficacy
-
Mclay, L.M.; Halley, F.; Souness, J.E.; McKenna, J.; Benning, V.; Birrell, M.; Burton, B.; Belvisi, M.; Collis, A.; Constan, A.; Foster, M.; Hele, D.; Jayyosi, Z.; Kelley, M.; Maslen, C.; Miller, G.; Ouldelhkim, M.C.; Page, K.; Phipps, S.; Pollock, K.; Porter, B.; Ratcliffe, A.J.; Redford, E.J.; Webber, S.; Slater, B.; Thybaud, V.; Wilsher, N. The discovery of RPR 200765A, a p38 MAP kinase inhibitor displaying a good oral anti-arthritic efficacy. Bioorg. Med. Chem. 2000, 9, 537-554.
-
(2000)
Bioorg. Med. Chem.
, vol.9
, pp. 537-554
-
-
Mclay, L.M.1
Halley, F.2
Souness, J.E.3
McKenna, J.4
Benning, V.5
Birrell, M.6
Burton, B.7
Belvisi, M.8
Collis, A.9
Constan, A.10
Foster, M.11
Hele, D.12
Jayyosi, Z.13
Kelley, M.14
Maslen, C.15
Miller, G.16
Ouldelhkim, M.C.17
Page, K.18
Phipps, S.19
Pollock, K.20
Porter, B.21
Ratcliffe, A.J.22
Redford, E.J.23
Webber, S.24
Slater, B.25
Thybaud, V.26
Wilsher, N.27
more..
-
32
-
-
0035848384
-
RPR203494 a pyrimidine analogue of the p38 inhibitor RPR200765A with an improved in vitro potency
-
Collis, A.J.; Foster, M.L.; Halley, F.; Maslen, C.; McLay, I.M.; Page, K.M.; Redford, E.J.; Souness, J.E.; Wilsher, N.E. RPR203494 a pyrimidine analogue of the p38 inhibitor RPR200765A with an improved in vitro potency. Bioorg. Med. Chem. Lett. 2001, 11, 693-696.
-
(2001)
Bioorg. Med. Chem. Lett.
, vol.11
, pp. 693-696
-
-
Collis, A.J.1
Foster, M.L.2
Halley, F.3
Maslen, C.4
McLay, I.M.5
Page, K.M.6
Redford, E.J.7
Souness, J.E.8
Wilsher, N.E.9
-
33
-
-
0034608331
-
SAR of 4-hydroxypiperidine and hydroxyalkyl substituted heterocycles as novel p38 map kinase inhibitors
-
Revesz, L.; Di Padova, F.E.; Buhl, T.; Feifel, R; Gram, H.; Hiestand, P.; Manning, U.; Zimmerlin, A.G. SAR of 4-hydroxypiperidine and hydroxyalkyl substituted heterocycles as novel p38 map kinase inhibitors. Bioorg. Med. Chem. Lett. 2000, 10, 1261-1264.
-
(2000)
Bioorg. Med. Chem. Lett.
, vol.10
, pp. 1261-1264
-
-
Revesz, L.1
Di Padova, F.E.2
Buhl, T.3
Feifel, R.4
Gram, H.5
Hiestand, P.6
Manning, U.7
Zimmerlin, A.G.8
-
34
-
-
27744452654
-
4(5)-Aryl-5(4)-pyridylimidazoles
-
Edited by (Ciba-Geigy A.-G.). 72-2221546[2221546], 57. DE. 3-5-1972. RefType: Patent
-
Fitzi, K. 4(5)-Aryl-5(4)-pyridylimidazoles. Edited by (Ciba-Geigy A.-G.). 72-2221546[2221546], 57. 1972. DE. 3-5-1972. RefType: Patent
-
(1972)
-
-
Fitzi, K.1
-
35
-
-
0027761036
-
Bicyclic imidazoles as a novel class of cytokine biosynthesis inhibitors
-
Lee, J.C.; Badger, A.M.; Griswold, D.E.; Dunnington, D.; Truneh, A.; Votta, B.; White, J.R.; Young, P.R.; Bender, P.E. Bicyclic imidazoles as a novel class of cytokine biosynthesis inhibitors. Ann. NY Acad. Sci. 1993, 696, 149-170.
-
(1993)
Ann. NY Acad. Sci.
, vol.696
, pp. 149-170
-
-
Lee, J.C.1
Badger, A.M.2
Griswold, D.E.3
Dunnington, D.4
Truneh, A.5
Votta, B.6
White, J.R.7
Young, P.R.8
Bender, P.E.9
-
36
-
-
18044405088
-
Pyrimidinylimidazole inhibitors of p38: Cyclic N-1 imidazole substituents enhance p38 kinase inhibition and oral activity
-
Adams, J.L.; Boehm, J.C.; Gallagher, T.F.; Kassis, S.; Webb, E.F.; Hal, R.; Sorenson, M.; Garigipati, R.; Griswold, D.E.; Lee, J.C. Pyrimidinylimidazole inhibitors of p38: cyclic N-1 imidazole substituents enhance p38 kinase inhibition and oral activity. Bioorg. Med. Chem. Lett. 2001, 11, 2867-2870.
-
(2001)
Bioorg. Med. Chem. Lett.
, vol.11
, pp. 2867-2870
-
-
Adams, J.L.1
Boehm, J.C.2
Gallagher, T.F.3
Kassis, S.4
Webb, E.F.5
Hal, R.6
Sorenson, M.7
Garigipati, R.8
Griswold, D.E.9
Lee, J.C.10
-
37
-
-
18044405088
-
Pyrimidinylimidazole inhibitors of p38: Cyclic N-1 imidazole substituents enhance p38 kinase inhibition and oral activity
-
Adams, J.L.; Boehm, J.C.; Gallagher, T.F.; Kassis, S.; Webb, E.F.; Hall, R.; Sorenson, M.; Garigipati, R.; Griswold, D.E.; Lee, J.C. Pyrimidinylimidazole inhibitors of p38: cyclic N-1 imidazole substituents enhance p38 kinase inhibition and oral activity. Bioorg. Med. Chem. Lett. 2001, 11, 2867-2870.
-
(2001)
Bioorg. Med. Chem. Lett.
, vol.11
, pp. 2867-2870
-
-
Adams, J.L.1
Boehm, J.C.2
Gallagher, T.F.3
Kassis, S.4
Webb, E.F.5
Hall, R.6
Sorenson, M.7
Garigipati, R.8
Griswold, D.E.9
Lee, J.C.10
-
38
-
-
0035820526
-
Phenoxypyrimidine inhibitors of p38.alpha. Kinase synthesis and statistical evaluation of the p38 inhibitory potencies of a series of 1-(piperidin-4-yl)4-(4-fluorophenyl)-5-(2-phenoxypyrimidin-4-yl) imidazoles
-
Boehm, J.C.; Bower; M.J.; Gallagher, T.F.; Kassis, S.; Johnson, S.R.; Adams, J.L. Phenoxypyrimidine inhibitors of p38.alpha. kinase synthesis and statistical evaluation of the p38 inhibitory potencies of a series of 1-(piperidin-4-yl)4-(4-fluorophenyl)-5-(2-phenoxypyrimidin-4-yl) imidazoles. Bioorg. Med. Chem. Lett. 2001, 11, 1123-1126.
-
(2001)
Bioorg. Med. Chem. Lett.
, vol.11
, pp. 1123-1126
-
-
Boehm, J.C.1
Bower, M.J.2
Gallagher, T.F.3
Kassis, S.4
Johnson, S.R.5
Adams, J.L.6
-
39
-
-
13844288120
-
SB 239063, a p38 MAPK inhibitor, reduces neutrophilia, inflammatory cytokines, MMP-9, and fibrosis in lung
-
Underwood, D.C.; Osborn, R.R.; Bochnowicz, S.; Webb, E.F.; Rieman, D.J.; Lee, J.C.; Romanic, A.M; Adams, J.L.; Hay, D.W.; Griswold, D.E. SB 239063, a p38 MAPK inhibitor, reduces neutrophilia, inflammatory cytokines, MMP-9, and fibrosis in lung. Am. J. Physiol. Lung Cell. Mol. Physiol. 2000, 279, 895-902.
-
(2000)
Am. J. Physiol. Lung Cell. Mol. Physiol.
, vol.279
, pp. 895-902
-
-
Underwood, D.C.1
Osborn, R.R.2
Bochnowicz, S.3
Webb, E.F.4
Rieman, D.J.5
Lee, J.C.6
Romanic, A.M.7
Adams, J.L.8
Hay, D.W.9
Griswold, D.E.10
-
40
-
-
18544406054
-
Griswold, D.E. SB 239063, a potent p38 MAP kinase inhibitor, reduces inflammatory cytokine production, airways eosinophil infiltration, and persistence
-
Underwood, D.C.; Osborn, R.R.; Kotzer, C.J.; Adams, J.L.; Lee, J.C.; Webb, E.F.; Carpenter, D.C.; Bochnowicz, S.; Thomas, H.C.; Hay, D.W.; Griswold, D.E. SB 239063, a potent p38 MAP kinase inhibitor, reduces inflammatory cytokine production, airways eosinophil infiltration, and persistence. J. PharmacoL Exp. Ther. 2000, 293, 281-288.
-
(2000)
J. PharmacoL Exp. Ther.
, vol.293
, pp. 281-288
-
-
Underwood, D.C.1
Osborn, R.R.2
Kotzer, C.J.3
Adams, J.L.4
Lee, J.C.5
Webb, E.F.6
Carpenter, D.C.7
Bochnowicz, S.8
Thomas, H.C.9
Hay, D.W.10
-
41
-
-
0034121690
-
Disease-modifying activity of SB 242235, a selective inhibitor of p38 mitogen-activated protein kinase, in rat adjuvant-induced arthritis
-
Badger, A.M.; Griswold, D.E.; Kapadia, R.; Blake, S.; Swift, B.A.; Hoffman, S.J.; Stroup, G.B.; Webb, E.; Rieman, D.J.; Gowen, M.; Boehm, J.C.; Adams, J.L.; Lee, J.C. Disease-modifying activity of SB 242235, a selective inhibitor of p38 mitogen-activated protein kinase, in rat adjuvant-induced arthritis. Arthritis Rheum. 2000, 43, 175-183.
-
(2000)
Arthritis Rheum.
, vol.43
, pp. 175-183
-
-
Badger, A.M.1
Griswold, D.E.2
Kapadia, R.3
Blake, S.4
Swift, B.A.5
Hoffman, S.J.6
Stroup, G.B.7
Webb, E.8
Rieman, D.J.9
Gowen, M.10
Boehm, J.C.11
Adams, J.L.12
Lee, J.C.13
-
42
-
-
0000458458
-
Suppression of ex vivo cytokine production by SB-242235, a selective inhibitor of p38 map kinase
-
Fullerton, T.; Sharma, A.; Prabhakar, U.; Tucci, M.; Boike, S.; Davis, H.; Jorkasky, D.; Williams, W. Suppression of ex vivo cytokine production by SB-242235, a selective inhibitor of p38 map kinase. Clin. Pharmacol. Therap. 2000, 67, 114.
-
(2000)
Clin. Pharmacol. Therap.
, vol.67
, pp. 114
-
-
Fullerton, T.1
Sharma, A.2
Prabhakar, U.3
Tucci, M.4
Boike, S.5
Davis, H.6
Jorkasky, D.7
Williams, W.8
-
43
-
-
18544406054
-
SB 239063, a potent p38 MAP kinase inhibitor, reduces inflammatory cytokine production, airways eosinophil infiltration, and persistence
-
Underwood, D.C.; Osborn, R.R.; Kotzer, C.J.; Adams, J.L.; Lee, J.C.; Webb, E.F.; Carpenter, D.C.; Bochnowicz, S.; Thomas, H.C.; Hay, D.W.P.; Griswold, D.E. SB 239063, a potent p38 MAP kinase inhibitor, reduces inflammatory cytokine production, airways eosinophil infiltration, and persistence. J. Pharmacol. Exp. Therap. 2000, 293, 281-288.
-
(2000)
J. Pharmacol. Exp. Therap.
, vol.293
, pp. 281-288
-
-
Underwood, D.C.1
Osborn, R.R.2
Kotzer, C.J.3
Adams, J.L.4
Lee, J.C.5
Webb, E.F.6
Carpenter, D.C.7
Bochnowicz, S.8
Thomas, H.C.9
Hay, D.W.P.10
Griswold, D.E.11
-
44
-
-
0030868682
-
Kinetic mechanism for p38 MAP kinase
-
LoGrasso, P.V.; Frantz, B.; Rolando, A.M.; O'Keefe, S.J.; Hermes, J.D.; O'Neill, E.A. Kinetic mechanism for p38 MAP kinase. Biochemistry 1997, 36, 10422-10427.
-
(1997)
Biochemistry
, vol.36
, pp. 10422-10427
-
-
LoGrasso, P.V.1
Frantz, B.2
Rolando, A.M.3
O'Keefe, S.J.4
Hermes, J.D.5
O'Neill, E.A.6
-
45
-
-
0032578559
-
The activation state of p38 mitogen-activated protein kinase determines the efficiency of ATP competition for pyridinylimidazole inhibitor binding
-
Frantz, B.; Klatt T.; Pang, M.; Parsons, J.; Rolando, A.; Williams, H.; Tocci, M.J.; O'Keefe, S.J.; O'Neill, E.A. The activation state of p38 mitogen-activated protein kinase determines the efficiency of ATP competition for pyridinylimidazole inhibitor binding. Biochemistry 1998, 37, 13846-13853.
-
(1998)
Biochemistry
, vol.37
, pp. 13846-13853
-
-
Frantz, B.1
Klatt, T.2
Pang, M.3
Parsons, J.4
Rolando, A.5
Williams, H.6
Tocci, M.J.7
O'Keefe, S.J.8
O'Neill, E.A.9
-
46
-
-
0035171919
-
Kinetics of small molecule inhibitor binding to p38 kinase
-
Thurmond, R.L.; Wadsworth, S.A.; Schafer, P.H.; Zivin, R.A.; Siekierka, J.J. Kinetics of small molecule inhibitor binding to p38 kinase. Eur. J. Biochem. 2001, 268, 5747-5754.
-
(2001)
Eur. J. Biochem.
, vol.268
, pp. 5747-5754
-
-
Thurmond, R.L.1
Wadsworth, S.A.2
Schafer, P.H.3
Zivin, R.A.4
Siekierka, J.J.5
-
47
-
-
0032745423
-
RWJ 67657, a potent, orally active inhibitor of p38 mitogen-activated protein kinase
-
Wadsworth, S.A.; Cavender, D.E.; Beers, S.A.; Lalan, P; Schafer, P.H.; Malloy, E.A.; Wu, W.; Fahmy, B.; Olini, G.C.; Davis, J.E.; Pellegrino-Gensey, J.L.; Wachter, M.P.; Siekierka, J.J. RWJ 67657, a potent, orally active inhibitor of p38 mitogen-activated protein kinase. J. Pharmacol Exp. Ther. 1999, 291, 680-687.
-
(1999)
J. Pharmacol Exp. Ther.
, vol.291
, pp. 680-687
-
-
Wadsworth, S.A.1
Cavender, D.E.2
Beers, S.A.3
Lalan, P.4
Schafer, P.H.5
Malloy, E.A.6
Wu, W.7
Fahmy, B.8
Olini, G.C.9
Davis, J.E.10
Pellegrino-Gensey, J.L.11
Wachter, M.P.12
Siekierka, J.J.13
-
48
-
-
2942560875
-
Novel p38 inhibitors with potent oral efficacy in several models of rheumatoid arthritis
-
Revesz, L.; Blum, E; Di Padova, F.E.; Buhl, T.; Feifel, R.; Gram, H.; Hiestand, P.; Manning, U.; Rucklin, G. Novel p38 inhibitors with potent oral efficacy in several models of rheumatoid arthritis. Bioorg. Med. Chem. Lett. 2004, 14, 3595-3599.
-
(2004)
Bioorg. Med. Chem. Lett.
, vol.14
, pp. 3595-3599
-
-
Revesz, L.1
Blum, E.2
Di Padova, F.E.3
Buhl, T.4
Feifel, R.5
Gram, H.6
Hiestand, P.7
Manning, U.8
Rucklin, G.9
-
49
-
-
0037057579
-
Imidazole inhibitors of cytokine release: Probing substituents in the 2 position
-
Laufer, S.A.; Striegel, H.; Wagner, G.K. Imidazole inhibitors of cytokine release: probing substituents in the 2 position. J. Med. Chem. 2002, 45, 4695-4705.
-
(2002)
J. Med. Chem.
, vol.45
, pp. 4695-4705
-
-
Laufer, S.A.1
Striegel, H.2
Wagner, G.K.3
-
50
-
-
33646195644
-
Preparation of 2-aralkylthioimidazoles and related compounds as antiinflammatories
-
Edited by (Merckle G.m.b.H. G. [0017192], 53. WO. RefType: Patent
-
Laufer, S.; Striegel, H-G.; Neher, K. Preparation of 2-aralkylthioimidazoles and related compounds as antiinflammatories. Edited by (Merckle G.m.b.H. G. [0017192], 53. 2000. WO. RefType: Patent
-
(2000)
-
-
Laufer, S.1
Striegel, H.-G.2
Neher, K.3
-
51
-
-
33646167168
-
Preparation of 2-substituted imidazoles useful in the treatment of inflammatory diseases
-
Edited by (Orto-McNeil Pharmaceutical IU. 98-US13419 [9903837], 55. WO. 29-6-1998. RefType: Patent
-
Wachter, M. Preparation of 2-substituted imidazoles useful in the treatment of inflammatory diseases. Edited by (Orto-McNeil Pharmaceutical IU. 98-US13419 [9903837], 55. 1999. WO. 29-6-1998. RefType: Patent
-
(1999)
-
-
Wachter, M.1
-
53
-
-
0032491233
-
Pyrroles and other heterocycles as inhibitors of p38 kinase
-
de Laszlo, S.E.; Visco, D.; Agarwal, L.; Chang, L.; Chin, J.; Croft, G.; Forsyth, A.; Fletcher, D.; Frantz, B.; Hacker, C.; Hanlon, W.; Harper, C.; Kostura, M.; Li, B.; Luell, S.; MacCoss, M.; Mantlo, N.; O'Neill, E.A.; Orevillo, C.; Pang, M.; Parsons, J.; Rolando, A.; Sahly, Y.; Sidler, K.; O'Keefe, S.J. Pyrroles and other heterocycles as inhibitors of p38 kinase. Bioorg. Med. Chem. Lett. 1998, 8, 2689-2694.
-
(1998)
Bioorg. Med. Chem. Lett.
, vol.8
, pp. 2689-2694
-
-
de Laszlo, S.E.1
Visco, D.2
Agarwal, L.3
Chang, L.4
Chin, J.5
Croft, G.6
Forsyth, A.7
Fletcher, D.8
Frantz, B.9
Hacker, C.10
Hanlon, W.11
Harper, C.12
Kostura, M.13
Li, B.14
Luell, S.15
MacCoss, M.16
Mantlo, N.17
O'Neill, E.A.18
Orevillo, C.19
Pang, M.20
Parsons, J.21
Rolando, A.22
Sahly, Y.23
Sidler, K.24
O'Keefe, S.J.25
more..
-
54
-
-
0038025786
-
The development of new triazole based inhibitors of tumor necrosis factor-alpha (TNF-alpha) production
-
Tullis, J.S.; VanRens, J.C.; Natchus, M.G.; Clark, M.P.; De, B.; Hsieh, L.C.; Janusz, M.J. The development of new triazole based inhibitors of tumor necrosis factor-alpha (TNF-alpha) production. Bioorg. Med. Chem. Lett. 2003, 13, 1665-1668.
-
(2003)
Bioorg. Med. Chem. Lett.
, vol.13
, pp. 1665-1668
-
-
Tullis, J.S.1
VanRens, J.C.2
Natchus, M.G.3
Clark, M.P.4
De, B.5
Hsieh, L.C.6
Janusz, M.J.7
-
55
-
-
0037025435
-
Synthesis and bioactivities of novel bicyclic thiophenes and 4,5,6,7-tetrahydrothieno[2,3-c]pyridines as inhibitors of tumor necrosis factor-alpha (TNF-alpha) production
-
Fujita, M.; Seki, T.; Ikeda, N. Synthesis and bioactivities of novel bicyclic thiophenes and 4,5,6,7-tetrahydrothieno[2,3-c]pyridines as inhibitors of tumor necrosis factor-alpha (TNF-alpha) production. Bioorg. Med. Chem. Lett. 2002, 12, 1897-1900.
-
(2002)
Bioorg. Med. Chem. Lett.
, vol.12
, pp. 1897-1900
-
-
Fujita, M.1
Seki, T.2
Ikeda, N.3
-
56
-
-
0037025435
-
Synthesis and bioactivities of novel bicyclic thiophenes and 4,5,6,7-tetrahydrothieno[2,3-c]pyridines as inhibitors of tumor necrosis factor-alpha (TNF-alpha) production
-
Fujita, M.; Seki, T.; Ikeda, N. Synthesis and bioactivities of novel bicyclic thiophenes and 4,5,6,7-tetrahydrothieno[2,3-c]pyridines as inhibitors of tumor necrosis factor-alpha (TNF-alpha) production. Bioorg. Med. Chem. Lett. 2002, 12, 1897-1900.
-
(2002)
Bioorg. Med. Chem. Lett.
, vol.12
, pp. 1897-1900
-
-
Fujita, M.1
Seki, T.2
Ikeda, N.3
-
57
-
-
0037142301
-
From imidazoles to pyrimidines: New inhibitors of cytokine release
-
Laufer, S.A.; Wagner, G.K. From imidazoles to pyrimidines: new inhibitors of cytokine release. J. Med. Chem. 2002, 45, 2733-2740.
-
(2002)
J. Med. Chem.
, vol.45
, pp. 2733-2740
-
-
Laufer, S.A.1
Wagner, G.K.2
-
58
-
-
0037169987
-
Pyridazine based inhibitors of p38 MAPK
-
McIntyre, C.J.; Ponticello, G.S.; Liverton, N.J.; O'Keefe, S.J.; O'Neill, E.A.; Pang, M.; Schwartz, C.D.; Claremon, D.A. Pyridazine based inhibitors of p38 MAPK. Bioorg. Med. Chem. Lett. 2002, 12, 689-692.
-
(2002)
Bioorg. Med. Chem. Lett.
, vol.12
, pp. 689-692
-
-
McIntyre, C.J.1
Ponticello, G.S.2
Liverton, N.J.3
O'Keefe, S.J.4
O'Neill, E.A.5
Pang, M.6
Schwartz, C.D.7
Claremon, D.A.8
-
59
-
-
0032401112
-
Potent inhibitors of the MAP kinase p38
-
Henry, J.R.; Rupert K.C.; Dodd, J.H.; Turchi, I.J.; Wadsworth, S.A.; Cavender, D.E.; Schafer, P.H.; Siekierka, J.J. Potent inhibitors of the MAP kinase p38. Bioorg. Med. Chem. Lett. 1998, 8, 3335-3340.
-
(1998)
Bioorg. Med. Chem. Lett.
, vol.8
, pp. 3335-3340
-
-
Henry, J.R.1
Rupert, K.C.2
Dodd, J.H.3
Turchi, I.J.4
Wadsworth, S.A.5
Cavender, D.E.6
Schafer, P.H.7
Siekierka, J.J.8
-
60
-
-
7844222102
-
6-Amino-2-(4-fluorophenyl)-4-methoxy-3- (4-pyridyl)-1H-pyrrolo[2,3-b]pyridine (RWJ 68354): A Potent and Selective p38 Kinase Inhibitor
-
Henry, J.R.; Rupert, K.C.; Dodd, J.H.; Turchi, I.J.; Wadsworth, S.A.; Cavender, D.E.; Fahmy, B.; Olini, G.C.; Davis, J.E.; Pellegrino-Gensey, J.L.; Schafer, P.H.; Siekierka, J.J. 6-Amino-2-(4-fluorophenyl)-4-methoxy-3- (4-pyridyl)-1H-pyrrolo[2,3-b]pyridine (RWJ 68354): A Potent and Selective p38 Kinase Inhibitor. J. Med. Chem. 1998, 41, 4196-4198.
-
(1998)
J. Med. Chem.
, vol.41
, pp. 4196-4198
-
-
Henry, J.R.1
Rupert, K.C.2
Dodd, J.H.3
Turchi, I.J.4
Wadsworth, S.A.5
Cavender, D.E.6
Fahmy, B.7
Olini, G.C.8
Davis, J.E.9
Pellegrino-Gensey, J.L.10
Schafer, P.H.11
Siekierka, J.J.12
-
61
-
-
0037330356
-
Imidazopyrimidines, potent inhibitors of p38 MAP kinase
-
Rupert, K.C.; Henry, J.R.; Dodd, J.H.; Wadsworth, S.A.; Cavender, D.E.; Olini, G.C.; Fahmy, B.; Siekierka, J.J. Imidazopyrimidines, potent inhibitors of p38 MAP kinase. Bioorg. Med. Chem. Lett. 2003, 13, 347-350.
-
(2003)
Bioorg. Med. Chem. Lett.
, vol.13
, pp. 347-350
-
-
Rupert, K.C.1
Henry, J.R.2
Dodd, J.H.3
Wadsworth, S.A.4
Cavender, D.E.5
Olini, G.C.6
Fahmy, B.7
Siekierka, J.J.8
-
62
-
-
2442716439
-
Development of orally bioavailable bicyclic pyrazolones as inhibitors of tumor necrosis factor-alpha production
-
Clark, M.P.; Laughlin, S.K.; Laufersweiler, M.J.; Bookland, R.G.; Brugel,T.A.; Golebiowski, A.; Sabat, M.P.; Townes, J.A.; VanRens, J.C.; Djung, J.F.; Natchus, M.G.; De, B.; Hsieh, L.C.; Xu, S.C.; Walter, R.L.; Mekel, M.J.; Heitmeyer, S.A.; Brown, K.K.; Juergens, K.; Taiwo, Y.O.; Janusz, M.J. Development of orally bioavailable bicyclic pyrazolones as inhibitors of tumor necrosis factor-alpha production. J. Med. Chem. 2004, 47, 2724-2727.
-
(2004)
J. Med. Chem.
, vol.47
, pp. 2724-2727
-
-
Clark, M.P.1
Laughlin, S.K.2
Laufersweiler, M.J.3
Bookland, R.G.4
Brugel, T.A.5
Golebiowski, A.6
Sabat, M.P.7
Townes, J.A.8
VanRens, J.C.9
Djung, J.F.10
Natchus, M.G.11
De, B.12
Hsieh, L.C.13
Xu, S.C.14
Walter, R.L.15
Mekel, M.J.16
Heitmeyer, S.A.17
Brown, K.K.18
Juergens, K.19
Taiwo, Y.O.20
Janusz, M.J.21
more..
-
63
-
-
0142060917
-
Design; and Synthesis of 4-Azaindoles as Inhibitors of p38 MAP Kinase
-
Trejo, A.; Arzeno, H.; Browner, M.; Chanda, S.; Cheng, S.; Comer, D.D.; Dalrymple, S.A.; Dunten, P.; Lafargue, J.; Lovejoy, B.; Freire-Moar, J.; Lim, J.; McIntosh, J.; Miller, J.; Papp, E.; Reuter, D.; Roberts, R.; Sanpablo, F.; Saunders, J.; Song, K.; Villasenor, A.; Warren, S.D.; Welch, M.; Weller, P.; Whiteley, P.E.; Zeng, L.; Goldstein,D.M. Design and Synthesis of 4-Azaindoles as Inhibitors of p38 MAP Kinase. J. Med. Chem. 2003, 46, 4702-4713.
-
(2003)
J. Med. Chem.
, vol.46
, pp. 4702-4713
-
-
Trejo, A.1
Arzeno, H.2
Browner, M.3
Chanda, S.4
Cheng, S.5
Comer, D.D.6
Dalrymple, S.A.7
Dunten, P.8
Lafargue, 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..
-
64
-
-
0036336136
-
Design, synthesis and bioactivities of novel diarylthiophenes: Inhibitors of turnor necrosis factor-alpha(TNF-alpha) production
-
Fujita, M.; Hirayama, T.; Ikeda, N. Design, synthesis and bioactivities of novel diarylthiophenes: inhibitors of turnor necrosis factor-alpha(TNF-alpha) production. Bioorg. Med. Chem. Leu. 2002, 10, 3113-3122.
-
(2002)
Bioorg. Med. Chem. Leu.
, vol.10
, pp. 3113-3122
-
-
Fujita, M.1
Hirayama, T.2
Ikeda, N.3
-
65
-
-
17344381323
-
p38 MAP kinase inhibitors. Part 1: Design and developmentof a new class of potent and highly selective inhibitors based on 3,4-dihydropyrido[3,2-d]pyrimidone scaffold
-
Natarajan, S.R.; Wisnoski, D.D.; Singh, S.B.; Stelmach, J.E.; O'Neill, E.A.; Schwartz, C.D.; Thompson, C.M.; Fitzgerald, C.E.; O'Keefe, S.J.; Kumar, S.; Hop, C.E.C.A.; Zaller, D.M.; Schmatz, D.M.; Doherty, J.B. p38 MAP kinase inhibitors. part 1: design and developmentof a new class of potent and highly selective inhibitors based on 3,4-dihydropyrido[3,2-d]pyrimidone scaffold. Bioorg. Med. Chem. Lett. 2003, 13, 273 -276.
-
(2003)
Bioorg. Med. Chem. Lett.
, vol.13
, pp. 273-276
-
-
Natarajan, S.R.1
Wisnoski, D.D.2
Singh, S.B.3
Stelmach, J.E.4
O'Neill, E.A.5
Schwartz, C.D.6
Thompson, C.M.7
Fitzgerald, C.E.8
O'Keefe, S.J.9
Kumar, S.10
Hop, C.E.C.A.11
Zaller, D.M.12
Schmatz, D.M.13
Doherty, J.B.14
-
66
-
-
0347990520
-
A novel Pd-catalyzed cyclization reaction of ureas for the synthesis of dihydroquinazolinone p38 kinase inhibitors
-
Schlapbach, A.; Heng, R.; Di, P.F. A novel Pd-catalyzed cyclization reaction of ureas for the synthesis of dihydroquinazolinone p38 kinase inhibitors. Bioorg. Med. Chem. Lett. 2004, 14, 357-360.
-
(2004)
Bioorg. Med. Chem. Lett.
, vol.14
, pp. 357-360
-
-
Schlapbach, A.1
Heng, R.2
Di, P.F.3
-
67
-
-
18744397820
-
Design and synthesis of potent, orally bioavailable dihydroquinazolinone inhibitors of p3 8 MAP kinase
-
Stelmach, J.E.; Liu, L.; Patel, S.B.; Pivnichny, J.V.; Scapin, G.; Singh, S.; Hop, C.E.C.A.; Wang, Z.; Strauss, JR.; Cameron, P.M.; Nichols,E.A.; O'Keefle, S.J.; O'Neill, E.A.; Schmatz, D.M.; Schwartz,C.D.; Thompson, C.M.; Zaller, D.M.; Doherty, J.B. Design and synthesis of potent, orally bioavailable dihydroquinazolinone inhibitors of p3 8 MAP kinase. Bioorg. Med. Chem. Lett. 2003, 13, 277-280.
-
(2003)
Bioorg. Med. Chem. Lett.
, vol.13
, pp. 277-280
-
-
Stelmach, J.E.1
Liu, L.2
Patel, S.B.3
Pivnichny, J.V.4
Scapin, G.5
Singh, S.6
Hop, C.E.C.A.7
Wang, Z.8
Strauss, J.R.9
Cameron, P.M.10
Nichols, E.A.11
O'Keefle, S.J.12
O'Neill, E.A.13
Schmatz, D.M.14
Schwartz, C.D.15
Thompson, C.M.16
Zaller, D.M.17
Doherty, J.B.18
-
68
-
-
0037330941
-
p38 Inhibitors: Piperidine-and 4-aminopiperidine-substitated naphthyridinones, quinolinones, and dihydroquinazolinones
-
Hunt, J.A.; Kallashi, F.; Ruzek, R.D.; Sinclair, P.J.; Ita, I.; McCormick, S.X.; Pivnichny, J.V.; Hop, C.E.C.A.; Kumar, S.; Wang, Z.; O'Keefe, S.J.; O'Neill, E.A.; Porter, G.; Thompson, J.E.; Woods, A.; Zaller, D.M.; Doherty, J.B. p38 Inhibitors: piperidine-and 4-aminopiperidine-substitated naphthyridinones, quinolinones, and dihydroquinazolinones. Bioorg. Med. Chem. Lett. 2003, 13, 467-470.
-
(2003)
Bioorg. Med. Chem. Lett.
, vol.13
, pp. 467-470
-
-
Hunt, J.A.1
Kallashi, F.2
Ruzek, R.D.3
Sinclair, P.J.4
Ita, I.5
McCormick, S.X.6
Pivnichny, J.V.7
Hop, C.E.C.A.8
Kumar, S.9
Wang, Z.10
O'Keefe, S.J.11
O'Neill, E.A.12
Porter, G.13
Thompson, J.E.14
Woods, A.15
Zaller, D.M.16
Doherty, J.B.17
-
69
-
-
0041318841
-
Structural basis for p38a MAP kinase quinazolinone and pyridol-pyrimidine inhibitor specificity
-
Fitzgerald, C.E.; Patel, S.B.; Becker, J.W.; Cameron, P.M.; Zaller, D.; Pikounis, V.B.; O'Keefe, S.J.; Scapin, G. Structural basis for p38a MAP kinase quinazolinone and pyridol-pyrimidine inhibitor specificity. Nat. Struct. Biol. 2003, 10, 764-769.
-
(2003)
Nat. Struct. Biol.
, vol.10
, pp. 764-769
-
-
Fitzgerald, C.E.1
Patel, S.B.2
Becker, J.W.3
Cameron, P.M.4
Zaller, D.5
Pikounis, V.B.6
O'Keefe, S.J.7
Scapin, G.8
-
70
-
-
0037472796
-
Hybrid-designed inhibitors of p38 MAP kinase utilizing N-arylpyridazinones
-
Colletti, S.L.; Frie, J.L.; Dixon, E.C.; Singh, S.B.; Choi, B.K.; Scapin, G.; Fitzgerald, C.E.; Kumar, S.; Nichols, E.A.; O'Keefe, S.J.; O'Neill, E.A.; Porter, G.; Samuel, K.; Schmatz, D.M.; Schwartz, C.D.; Shoop, W.L.; Thompson, C.M.; Thompson, J.E.; Wang, R.; Woods, A.; Zaller, D.M.; Doherty, J.B. Hybrid-designed inhibitors of p38 MAP kinase utilizing N-arylpyridazinones. J. Med. Chem. 2003,46,349-352.
-
(2003)
J. Med. Chem.
, vol.46
, pp. 349-352
-
-
Colletti, S.L.1
Frie, J.L.2
Dixon, E.C.3
Singh, S.B.4
Choi, B.K.5
Scapin, G.6
Fitzgerald, C.E.7
Kumar, S.8
Nichols, E.A.9
O'Keefe, S.J.10
O'Neill, E.A.11
Porter, G.12
Samuel, K.13
Schmatz, D.M.14
Schwartz, C.D.15
Shoop, W.L.16
Thompson, C.M.17
Thompson, J.E.18
Wang, R.19
Woods, A.20
Zaller, D.M.21
Doherty, J.B.22
more..
-
71
-
-
0037463762
-
N-Phenyl-N-purin-6-yl ureas: The design and synthesis of p38.alpha. MAP kinase inhibitors
-
Wan. Z.; Boehm, J.C.; Bower, M.J.; Kassis, S.; Lee, J.C.; Zhao, B.; Adams, J.L. N-Phenyl-N-purin-6-yl ureas: The design and synthesis of p38.alpha. MAP kinase inhibitors. Bioorg. Med. Chem. Lett. 2003,13,1191-1194.
-
(2003)
Bioorg. Med. Chem. Lett.
, vol.13
, pp. 1191-1194
-
-
Wan, Z.1
Boehm, J.C.2
Bower, M.J.3
Kassis, S.4
Lee, J.C.5
Zhao, B.6
Adams, J.L.7
-
72
-
-
33646196384
-
Preparation of 5-amino-4-aroyl-1-arylpyrazoles as p38 MAP kinase inhibitors
-
Edited by (F.Hoffmann-La Roche A.-G. S. 2000-EP8981[2001021591], 112. WO. 14-9-2000. Ref Type: Patent
-
Goldstein, D.M.; Labadie, S.S.; Rotstein, D.M.; Sjogren, E.B.; Talamas, F.X. Preparation of 5-amino-4-aroyl-1-arylpyrazoles as p38 MAP kinase inhibitors. Edited by (F.Hoffmann-La Roche A.-G. S. 2000-EP8981[2001021591], 112. 2001. WO. 14-9-2000. Ref Type: Patent
-
(2001)
-
-
Goldstein, D.M.1
Labadie, S.S.2
Rotstein, D.M.3
Sjogren, E.B.4
Talamas, F.X.5
-
73
-
-
0347627154
-
Synthesis and structure-activity relationship of aminobenzophenones. A novel class of p38 MAP kinase inhibitors with high antiinflammatory activity
-
Ottosen, E.R.; Sorensen, M.D.; Bjoerkling, F.; Skak-Nielsen, T.; Fjording, M.S.; Aaes, H.; Binderup, L. Synthesis and structure-activity relationship of aminobenzophenones. A novel class of p38 MAP kinase inhibitors with high antiinflammatory activity. J Med. Chem. 2003, 46, 5651-5662.
-
(2003)
J Med. Chem.
, vol.46
, pp. 5651-5662
-
-
Ottosen, E.R.1
Sorensen, M.D.2
Bjoerkling, F.3
Skak-Nielsen, T.4
Fjording, M.S.5
Aaes, H.6
Binderup, L.7
-
74
-
-
5344273921
-
A novel series of p38 MAP kinase inhibitors for the potential treatment of rheumatoid arthritis
-
Brown, D.S.; Belfield, A.J.; Brown, G.R.; Campbell, D.; Foubister, A.; Masters, D.J.; Pike, K.G.; Snelson, W.L.; Wells, S.L. A novel series of p38 MAP kinase inhibitors for the potential treatment of rheumatoid arthritis. Bioorg. Med. Chem. Lett. 2004, 14, 5383- 5387.
-
(2004)
Bioorg. Med. Chem. Lett.
, vol.14
, pp. 5383-5387
-
-
Brown, D.S.1
Belfield, A.J.2
Brown, G.R.3
Campbell, D.4
Foubister, A.5
Masters, D.J.6
Pike, K.G.7
Snelson, W.L.8
Wells, S.L.9
-
75
-
-
5444244504
-
Novel, potent and selective anilinoquinazoline and anilinopyrimidine inhibitors of p38 MAP kinase
-
Cumming, J.G.; McKenzie, C.L.; Bowden, S.G.; Campbell, D.; Masters, D.J.; Breed, J.; Jewsbury, P.J. Novel, potent and selective anilinoquinazoline and anilinopyrimidine inhibitors of p38 MAP kinase. Bloorg. Med. Chem. Lett. 2004, 14, 5389-5394.
-
(2004)
Bloorg. Med. Chem. Lett.
, vol.14
, pp. 5389-5394
-
-
Cumming, J.G.1
McKenzie, C.L.2
Bowden, S.G.3
Campbell, D.4
Masters, D.J.5
Breed, J.6
Jewsbury, P.J.7
-
76
-
-
0034642482
-
Binding mode of the 4-anilinoquinazoline class of protein kinase inhibitor: X-ray crystallographic studies of 4-anilinoquinazolines bound to cyclin-dependent kinase 2 and p38 kinase
-
Shewchuk, L.; Hassell, A.; Wisely, B.; Rocque, W.; Holmes, W.; Veal, J.; Kuyper, L.F. Binding mode of the 4-anilinoquinazoline class of protein kinase inhibitor: X-ray crystallographic studies of 4-anilinoquinazolines bound to cyclin-dependent kinase 2 and p38 kinase. J. Med. Chem. 2000, 43,133-138.
-
(2000)
J. Med. Chem.
, vol.43
, pp. 133-138
-
-
Shewchuk, L.1
Hassell, A.2
Wisely, B.3
Rocque, W.4
Holmes, W.5
Veal, J.6
Kuyper, L.F.7
-
77
-
-
9744269944
-
The discovery of orally active triaminotriazine aniline amides as inhibitors ofp38 MAP kinase
-
Leftheris, K.; Ahmed, G.; Chan, R.; Dyckman, A.J.; Hussain, Z.; Ho, K.; Hynes, J. Jr.; Letourneau, J.; Li, W.; Lin, S.; Metzger, A.; Moriarty, K.J.; Riviello, C.; Shimshock, Y.; Wen, J.; Wityak, J.; Wrobleski, S.T.; Wu, H.; Wu, J.; Desai, M.; Gillooly, K.M.; Lin, T.H.; Loo, D.; McIntyre, K.W.; Pitt, S.; Shen, D.R.; Shuster, D.J; Zhang, R.; Diller, D.; Doweyko, A; Sack, J.; Baldwin, J.; Barrish, J.; Dodd, J.; Henderson, I.; Kanner, S.; Schieven, G.L.; Webb, M. The discovery of orally active triaminotriazine aniline amides as inhibitors ofp38 MAP kinase. J. Med. Chem. 2004, 47, 6283-6291.
-
(2004)
J. Med. Chem.
, vol.47
, pp. 6283-6291
-
-
Leftheris, K.1
Ahmed, G.2
Chan, R.3
Dyckman, A.J.4
Hussain, Z.5
Ho, K.6
Hynes Jr., J.7
Letourneau, J.8
Li, W.9
Lin, S.10
Metzger, A.11
Moriarty, K.J.12
Riviello, C.13
Shimshock, Y.14
Wen, J.15
Wityak, J.16
Wrobleski, S.T.17
Wu, H.18
Wu, J.19
Desai, M.20
Gillooly, K.M.21
Lin, T.H.22
Loo, D.23
McIntyre, K.W.24
Pitt, S.25
Shen, D.R.26
Shuster, D.J.27
Zhang, R.28
Diller, D.29
Doweyko, A.30
Sack, J.31
Baldwin, J.32
Barrish, J.33
Dodd, J.34
Henderson, I.35
Kanner, S.36
Schieven, G.L.37
Webb, M.38
more..
-
78
-
-
33646198735
-
Preparation of pyridinylarylureas and related compounds as inhibitors of p38 kinase
-
Edited by (Vertex Pharmaceuticals Incorporated U. 99-US10291[9958502], 99. WO. 11-5-1999. Ref Type: Patent
-
Salituro, F.; Galullo, V.; Bellon, S.; Bemis, G.; Cochran, J. Preparation of pyridinylarylureas and related compounds as inhibitors of p38 kinase. Edited by (Vertex Pharmaceuticals Incorporated U. 99-US10291[9958502], 99. 1999. WO. 11-5-1999. Ref Type: Patent
-
(1999)
-
-
Salituro, F.1
Galullo, V.2
Bellon, S.3
Bemis, G.4
Cochran, J.5
-
79
-
-
33646184114
-
Preparation of urea derivatives as inhibitors of p38
-
Edited by (Vertex Pharmaceuticals Incorporated U. 98-US13496[9900357], 93. WO. 29-6-1998. Ref Type: Patent
-
Salituro, F.G.; Bemis, G. Preparation of urea derivatives as inhibitors of p38. Edited by (Vertex Pharmaceuticals Incorporated U. 98-US13496[9900357], 93. 1999. WO. 29-6-1998. Ref Type: Patent
-
(1999)
-
-
Salituro, F.G.1
Bemis, G.2
-
80
-
-
0033813234
-
Discovery of a new class of p38 kinase inhibitors
-
Dumas, J.; Sibley, R.; Riedl, B.; Monahan, M.K.; Lee, W.; Lowinger, T.B.; Redman, A.M.; Johnson, J.S.; Kingery-Wood, J.; Scott, W.J. Discovery of a new class of p38 kinase inhibitors. Bioorg. Med. Chem. Lett. 2000, 10, 2047-2050.
-
(2000)
Bioorg. Med. Chem. Lett.
, vol.10
, pp. 2047-2050
-
-
Dumas, J.1
Sibley, R.2
Riedl, B.3
Monahan, M.K.4
Lee, W.5
Lowinger, T.B.6
Redman, A.M.7
Johnson, J.S.8
Kingery-Wood, J.9
Scott, W.J.10
-
81
-
-
0037019275
-
Pyrazole Urea-Based Inhibitors of p38 MAP Kinase: From Lead Compound to Clinical Candidate
-
Regan, J.; Breitfelder, S.; Cirillo, P.; Gilmore, T.; Graham, A.G.; Hickey, E.; Klaus, B.; Madwed, J.; Moriak, M.; Moss, N.; Pargellis, C.; Pav, S.; Proto, A.; Swinamer, A.; Tong, L.; Torcellini, C. Pyrazole Urea-Based Inhibitors of p38 MAP Kinase: From Lead Compound to Clinical Candidate. J. Med. Chem. 2002, 45, 2994-3008.
-
(2002)
J. Med. Chem.
, vol.45
, pp. 2994-3008
-
-
Regan, J.1
Breitfelder, S.2
Cirillo, P.3
Gilmore, T.4
Graham, A.G.5
Hickey, E.6
Klaus, B.7
Madwed, J.8
Moriak, M.9
Moss, N.10
Pargellis, C.11
Pav, S.12
Proto, A.13
Swinamer, A.14
Tong, L.15
Torcellini, C.16
-
82
-
-
18344395134
-
Inhibition of p38 MAP kinase by utilizing a novel allosteric binding site
-
Pargellis, C.; Tong, L.; Churchill, L.; Cirillo, P.F.; Gilmore, T.; Graham, A.G.; Grob, P.M.; Hickey, E.R.; Moss, N.; Pav, S.; Regan, J. Inhibition of p38 MAP kinase by utilizing a novel allosteric binding site. Nat. Struct. Biol. 2002, 9, 268-272.
-
(2002)
Nat. Struct. Biol.
, vol.9
, pp. 268-272
-
-
Pargellis, C.1
Tong, L.2
Churchill, L.3
Cirillo, P.F.4
Gilmore, T.5
Graham, A.G.6
Grob, P.M.7
Hickey, E.R.8
Moss, N.9
Pav, S.10
Regan, J.11
-
83
-
-
0142028917
-
Structure-Activity Relationships of the p38.alpha. MAP Kinase Inhibitor 1-(5-tert-Butyl-2-p-tolyl-2H-pyrazol-3-yl) -3-[4-(2-morpholin-4-yl-ethoxy) naph- thalen-1-yl]urea (BIRB 796)
-
Regan, J.; Capolino, A.; Cirillo, P.F.; Gilmore, T.; Graham, A.G.; Hickey, E.; Kroe, R.R.; Madwed, J.; Moriak, M.; Nelson, R.; Pargellis, C.A.; Swinamer, A.; Torcellini, C.; Tsang, M.; Moss, N. Structure-Activity Relationships of the p38.alpha. MAP Kinase Inhibitor 1-(5-tert-Butyl-2-p-tolyl-2H-pyrazol-3-yl) -3-[4-(2-morpholin-4-yl-ethoxy) naph- thalen-1-yl]urea (BIRB 796). J. Med. Chem. 2003, 46, 4676-4686.
-
(2003)
J. Med. Chem.
, vol.46
, pp. 4676-4686
-
-
Regan, J.1
Capolino, A.2
Cirillo, P.F.3
Gilmore, T.4
Graham, A.G.5
Hickey, E.6
Kroe, R.R.7
Madwed, J.8
Moriak, M.9
Nelson, R.10
Pargellis, C.A.11
Swinamer, A.12
Torcellini, C.13
Tsang, M.14
Moss, N.15
-
84
-
-
0042020196
-
The kinetics of binding to p38 MAP kinase by analogues of BIRB 796
-
Regan, J.; Pargellis, C.A.; Cirillo, P.F.; Gilmore, T.; Hickey, E.R.; Peet, G.W.; Proto, A.; Swinamer, A.; Moss, N. The kinetics of binding to p38 MAP kinase by analogues of BIRB 796. Bioorg. Med Chem. Lett. 2003, 13, 3101-3104.
-
(2003)
Bioorg. Med Chem. Lett.
, vol.13
, pp. 3101-3104
-
-
Regan, J.1
Pargellis, C.A.2
Cirillo, P.F.3
Gilmore, T.4
Hickey, E.R.5
Peet, G.W.6
Proto, A.7
Swinamer, A.8
Moss, N.9
-
85
-
-
0035825364
-
p38 kinase inhibitors for the treatment of arthritis and osteoporosis: Thienyl, furyl, and pyrrolyl ureas
-
Redman, A.M.; Johnson, J.S.; Daily, R.; Swartz, S.; Wild, H.; Paulsen, H.; Caringal, Y.; Gunn, D.; Renick, J.; Osterhout, M.; Kingery-Wood, J.; Smith, R.A.; Lee, W.; Dumas, J.; Wilhelm, S.M.; Housley, T.J.; Bhargava, A.; Ranges, G.E.; Shrikbande, A.; Young, D.; Bombara, M.; Scott, W.J. p38 kinase inhibitors for the treatment of arthritis and osteoporosis: thienyl, furyl, and pyrrolyl ureas. Bioorg. Med. Chem. Lett. 2001, 11, 9-12.
-
(2001)
Bioorg. Med. Chem. Lett.
, vol.11
, pp. 9-12
-
-
Redman, A.M.1
Johnson, J.S.2
Daily, R.3
Swartz, S.4
Wild, H.5
Paulsen, H.6
Caringal, Y.7
Gunn, D.8
Renick, J.9
Osterhout, M.10
Kingery-Wood, J.11
Smith, R.A.12
Lee, W.13
Dumas, J.14
Wilhelm, S.M.15
Housley, T.J.16
Bhargava, A.17
Ranges, G.E.18
Shrikbande, A.19
Young, D.20
Bombara, M.21
Scott, W.J.22
more..
-
86
-
-
0033822467
-
1-Phenyl-5-pyrazolyl ureas: Potent and selective p38 kinase inhibitors
-
Dumas, J.; Hatoum-Mokdad, H.; Sibley, R.; Riedl, B.; Scott, W.J.; Monahan, M.K.; Lowinger, T.B.; Brennan, C.; Natero, R.; Turner, T. 1-Phenyl-5-pyrazolyl ureas: potent and selective p38 kinase inhibitors. Bioorg. Med. Chem. Lett. 2000,10, 2051-2054.
-
(2000)
Bioorg. Med. Chem. Lett.
, Issue.10
, pp. 2051-2054
-
-
Dumas, J.1
Hatoum-Mokdad, H.2
Sibley, R.3
Riedl, B.4
Scott, W.J.5
Monahan, M.K.6
Lowinger, T.B.7
Brennan, C.8
Natero, R.9
Turner, T.10
-
87
-
-
0037124174
-
Synthesis and pharmacological characterization of a potent; orally active p38 kinase inhibitor
-
Dumas, J.; Hatoum-Mokdad, H.; Sibley, R.N.; Smith, R.A.; Scott, W.J.; Khire, U.; Lee, W.; Wood, J.; Wolanin, D.; Cooley, J.; Bankston, D.; Redman, A.M.; Schoenleber, R.; Caringal, Y.; Gunn, D.; Romero, R.; Osterhout, M.; Paulsen, H.; Housley, T.J.; Wilhelm, S.M.; Pirro, J.; Chien, D.S.; Ranges, G.E.; Shrikhande, A.; Muzsi, A.; Bortolon, E.; Wakefield, J.; Gianpaolo Ostravage, C.; Bhargava, A.; Chau, T. Synthesis and pharmacological characterization of a potent; orally active p38 kinase inhibitor. Bioorg. Med Chem. Lett. 2002, 1Z 1559-1562.
-
(2002)
Bioorg. Med Chem. Lett.
, vol.12
, pp. 1559-1562
-
-
Dumas, J.1
Hatoum-Mokdad, H.2
Sibley, R.N.3
Smith, R.A.4
Scott, W.J.5
Khire, U.6
Lee, W.7
Wood, J.8
Wolanin, D.9
Cooley, J.10
Bankston, D.11
Redman, A.M.12
Schoenleber, R.13
Caringal, Y.14
Gunn, D.15
Romero, R.16
Osterhout, M.17
Paulsen, H.18
Housley, T.J.19
Wilhelm, S.M.20
Pirro, J.21
Chien, D.S.22
Ranges, G.E.23
Shrikhande, A.24
Muzsi, A.25
Bortolon, E.26
Wakefield, J.27
Gianpaolo Ostravage, C.28
Bhargava, A.29
Chau, T.30
more..
-
88
-
-
0142028929
-
Thermal Denaturation: A Method to Rank Slow Binding, High-Affinity P38a MAP Kinase Inhibitors
-
Kroe, R.R.; Regan, J.; Proto, A.; Peet, G.W.; Roy, T.; Landro, L.D.; Fuschetto, N.G.; Pargellis, C.A.; Ingraham, R.H. Thermal Denaturation: A Method to Rank Slow Binding, High-Affinity P38a MAP Kinase Inhibitors. J Med. Chem. 2003, 46, 4669-4675.
-
(2003)
J Med. Chem.
, vol.46
, pp. 4669-4675
-
-
Kroe, R.R.1
Regan, J.2
Proto, A.3
Peet, G.W.4
Roy, T.5
Landro, L.D.6
Fuschetto, N.G.7
Pargellis, C.A.8
Ingraham, R.H.9
-
89
-
-
19944434344
-
Identification of novel p38alpha MAP kinase inhibitors using fragment-based lead generation
-
Gill, A.L.; Frederickson, M.; Cleasby, A.; Woodhead, S.J.; Carr, M.G.; Woodhead, A.J.; Walker, M.T.; Congreve, M.S.; Devine, L.A.; Tisi, D.; O'Reilly, M.; Seavers, L.C.; Davis, D.J.; Curry, J.; Anthony, R.; Padova, A.; Murray, CW.; Carr, R.A.; Jhoti, H. Identification of novel p38alpha MAP kinase inhibitors using fragment-based lead generation. J. Med. Chem. 2005, 48, 414-426.
-
(2005)
J. Med. Chem.
, vol.48
, pp. 414-426
-
-
Gill, A.L.1
Frederickson, M.2
Cleasby, A.3
Woodhead, S.J.4
Carr, M.G.5
Woodhead, A.J.6
Walker, M.T.7
Congreve, M.S.8
Devine, L.A.9
Tisi, D.10
O'Reilly, M.11
Seavers, L.C.12
Davis, D.J.13
Curry, J.14
Anthony, R.15
Padova, A.16
Murray, C.W.17
Carr, R.A.18
Jhoti, H.19
-
90
-
-
21544434331
-
p38 MAP kinase inhibitors: Many are made, but few are chosen
-
Dominguez, C.; Powers, D.A. and Tamayo, N. p38 MAP kinase inhibitors: Many are made, but few are chosen. Curr. Opin. Drug Discov. Develop. 2005,8, 421-430.
-
(2005)
Curr. Opin. Drug Discov. Develop.
, vol.8
, pp. 421-430
-
-
Dominguez, C.1
Powers, D.A.2
Tamayo, N.3
-
91
-
-
8044250278
-
Cloning of a disintegrin metalloproteinase that processes precursor tumour-necrosis factor-alpha
-
Moss, M.L.; An, S.L.; Milla, M.E.; Bickett, D.M.; Burkhart, W.; Carter, H.L.; Chen, W.J.; Clay, W.C.; Didsbury, J.R.; Hassler, D.; Hoffman, C.R.; Kost, T.A.; Lambert, M.H.; Leesnitzer, M.A.; McCauley, P.; McGeehan, G.; Mitchell, J.; Moyer, M.; Pahel, G.; Rocque, W.; Overton, L.K.; Schoenen, F.; Seaton, T.; Su, J.L.; Becherer, J.D. Cloning of a disintegrin metalloproteinase that processes precursor tumour-necrosis factor-alpha. Nature 1997, 385, 733-736.
-
(1997)
Nature
, vol.385
, pp. 733-736
-
-
Moss, M.L.1
An, S.L.2
Milla, M.E.3
Bickett, D.M.4
Burkhart, W.5
Carter, H.L.6
Chen, W.J.7
Clay, W.C.8
Didsbury, J.R.9
Hassler, D.10
Hoffman, C.R.11
Kost, T.A.12
Lambert, M.H.13
Leesnitzer, M.A.14
McCauley, P.15
McGeehan, G.16
Mitchell, J.17
Moyer, M.18
Pahel, G.19
Rocque, W.20
Overton, L.K.21
Schoenen, F.22
Seaton, T.23
Su, J.L.24
Becherer, J.D.25
more..
-
92
-
-
0026507126
-
A novel heterodimeric cysteine protease is required for interleukin-1 beta processing in monocytes
-
Thomberry, N.A.; Bull, H.G.; Calaycay, J.R.; Chapman, K.T.; Howard, A.D.; Kostura, M.J.; Miller, D.K.; Molineaux, S.M.; Weidner, J.R.; Aunins, J. A novel heterodimeric cysteine protease is required for interleukin-1 beta processing in monocytes. Nature 1992,356, 768-774.
-
(1992)
Nature
, vol.356
, pp. 768-774
-
-
Thomberry, N.A.1
Bull, H.G.2
Calaycay, J.R.3
Chapman, K.T.4
Howard, A.D.5
Kostura, M.J.6
Miller, D.K.7
Molineaux, S.M.8
Weidner, J.R.9
Aunins, J.10
-
93
-
-
0033769803
-
Anti-interleukin-I and anti-tumor necrosis factor-.alpha. Synergistically inhibit adjuvant arthritis in Lewis rats
-
Feige, U.; Hu, Y.L.; Gasser, J.; Campagnuolo, G.; Munyakazi, L.; Bolon, B. Anti-interleukin-I and anti-tumor necrosis factor-.alpha. synergistically inhibit adjuvant arthritis in Lewis rats. Cell. Mol. Life Sci. 2000, 57, 1457-1470.
-
(2000)
Cell. Mol. Life Sci.
, vol.57
, pp. 1457-1470
-
-
Feige, U.1
Hu, Y.L.2
Gasser, J.3
Campagnuolo, G.4
Munyakazi, L.5
Bolon, B.6
|