메뉴 건너뛰기




Volumn 52, Issue 7, 2009, Pages 1994-2005

Novel tricyclic inhibitors of 1κB kinase

(30)  Kempson, James a,b   Spergel, Steven H a,b   Guo, Junqing a,b   Quesnelle, Claude a,b   Gill, Patrice a,b   Belanger, Dominique a,b   Dyckman, Alaric J a,b   Li, Tianle a,b   Watterson, Scott H a,b   Langevine, Charles M a,b   Das, Jagabandhu a,b   Moquin, Robert V a,b   Furch, Joseph A a,b   Marinier, Anne a,b   Dodier, Marco a,b   Martel, Alain a,b   Nirschl, David a,c   Van Kirk, Katy a,c   Burke, James R a,b   Pattoli, Mark A a,b   more..


Author keywords

[No Author keywords available]

Indexed keywords

1,4 DIMETHYL 7 METHYLAMINO 2 PHENYL 4H IMIDAZ[4,5 D]IMIDAZO[5,4 B]PYRIDINE; 2 (4 FLUOROPHENYL) 8 METHYL N [2 (1 PIPERIDINYL)ETHYL] 8H IMIDAZO[4,5 D]THIAZOLO[5,4 B]PYRIDINE 5 AMINE; 2 METHANESULFONYL 4 METHYL 7 METHYLAMINO 2 (METHYLTHIO) 4H IMIDAZO[4,5 D]THIAZOLO[5,4 B]PYRIDINE; 4 METHYL 7 METHYLAMINO 2 (AZEPAN 1 YL) 4H IMIDAZO[4,5 D]THIAZOLO[5,4 B]PYRIDINE; 4 METHYL 7 METHYLAMINO 2 (METHYLTHIO) 4H IMIDAZO[4,5 D]THIAZOLO[5,4 B]PYRIDINE; 4 METHYL 7 METHYLAMINO 2 [1,2,3,6 TETRAHYDROPYRIDINE] 4H IMIDAZO[4,5 D]THIAZOLO[5,4 B]PYRIDINE; 4 METHYL 7 METHYLAMINO 2 BENZYLAMINO 4H IMIDAZO[4,5 D]THIAZOLO[5,4 B]PYRIDINE; 4 METHYL 7 METHYLAMINO 2 CYCLOPENTYLAMIDO 4H IMIDAZO[4,5 D]THIAZOLO[5,4 B]PYRIDINE; 4 METHYL 7 METHYLAMINO 2 DIETHYLAMIDO 4H IMIDAZO[4,5 D]THIAZOLO[5,4 B]PYRIDINE; 4 METHYL 7 METHYLAMINO 2 ETHYLAMIDO 4H IMIDAZO[4,5 D]THIAZOLO[5,4 B]PYRIDINE; 4 METHYL 7 METHYLAMINO 2 HYDROXYETHYLAMINO 4H IMIDAZO[4,5 D]THIAZOLO[5,4 B]PYRIDINE; 4 METHYL 7 METHYLAMINO 2 METHYLAMIDO 4H IMIDAZO[4,5 D]THIAZOLO[5,4 B]PYRIDINE; 4 METHYL 7 METHYLAMINO 2 METHYLAMINO 4H IMIDAZO[4,5 D]THIAZOLO[5,4 B]PYRIDINE; 4 METHYL 7 METHYLAMINO 2 PHENYL 4H IMIDAZO[4,5 D]OXAZOLO[5,4 B]PYRIDINE; 4 METHYL 7 METHYLAMINO 2 PHENYL 4H IMIDAZO[4,5 D]THIAZOLO[5,4 B]PYRIDINE; 4 METHYL 7 METHYLAMINO 2 PIPERIDINE 4H IMIDAZO[4,5 D]THIAZOLO[5,4 B]PYRIDINE; 4 METHYL 7 METHYLAMINO 2 THIENYLAMIDO 4H IMIDAZO[4,5 D]THIAZOLO[5,4 B]PYRIDINE; 8 METHYL 2 (4 FLUOROPHENYL) 8 METHYL 8H IMIDAZO[4,5 D]THIAZOLO[5,4 B]PYRIDINE; I KAPPA B KINASE INHIBITOR; N [2 [[2 (4 FLUOROPHENYL) 8 METHYL 8H IMIDAZO[4,5 D]THIAZOLO[5,4 B]PYRIDINE 5 YL]AMINO]ETHYL]ACETAMIDE; N [2 [[2 (4 FLUOROPHENYL) 8 METHYL 8H IMIDAZO[4,5 D]THIAZOLO[5,4 B]PYRIDINE 5 YL]AMINO]ETHYL]ETHANOL; N [[2 FLUORO 5 (8 METHYL 5 METHYLAMINO 8H IMIDAZO[4,5 D]THIAZOLO[5,4 B]PYRIDINE 2 YL)PHENYL]METHYL]ACETAMIDE; N [[2 FLUORO 5 (8 METHYL 5 METHYLAMINO 8H IMIDAZO[4,5 D]THIAZOLO[5,4 B]PYRIDINE 2 YL)PHENYL]METHYL]METHANESULFONAMIDE; N [[3 [8 METHYL 5 (METHYLAMINO) 8H IMIDAZO[4,5 D]THIAZOLO[5,4 B]PYRIDINE 2 YL]PHENYL]METHYL]ACETAMIDE; N [[3 [8 METHYL 5 (METHYLAMINO) 8H IMIDAZO[4,5 D]THIAZOLO[5,4 B]PYRIDINE 2 YL]PHENYL]METHYL]ISOXAZOLE 5 AMIDE; N [[3 [8 METHYL 5 (METHYLAMINO) 8H IMIDAZO[4,5 D]THIAZOLO[5,4 B]PYRIDINE 2 YL]PHENYL]METHYL]METHANESULFONAMIDE; N ETHYL 2 (4 FLUOROPHENYL) 8 METHYL 8H IMIDAZO[4,5 D]THIAZOLO[5,4 B]PYRIDINE; N METHYL 2 (4 FLUOROPHENYL) 8 METHYL 8H IMIDAZO[4,5 D]THIAZOLO[5,4 B]PYRIDINE; UNCLASSIFIED DRUG;

EID: 64549109718     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm8015816     Document Type: Article
Times cited : (29)

References (23)
  • 1
    • 1942521356 scopus 로고    scopus 로고
    • Transcriptional profiling of IKK2/ NF-κB and p38 MAP kinase dependent gene expression in TNF-R stimulated primary human endothelial cells
    • (a) Viemann, D. Transcriptional profiling of IKK2/ NF-κB and p38 MAP kinase dependent gene expression in TNF-R stimulated primary human endothelial cells. Blood 2004, 103, 3365-3373.
    • (2004) Blood , vol.103 , pp. 3365-3373
    • Viemann, D.1
  • 2
    • 0031593664 scopus 로고    scopus 로고
    • Neurath, M. F. Role of NF-κB in immune and inflammatory responses in the gut. Gut 1998, 43, 856-860.
    • (b) Neurath, M. F. Role of NF-κB in immune and inflammatory responses in the gut. Gut 1998, 43, 856-860.
  • 3
    • 33645959483 scopus 로고    scopus 로고
    • Cho, M. L. STAT3 and NF-κB signal pathway is required for IL-23 mediated IL-17 production in spontaneous arthritis animal model IL-1 receptor antagonist-deficient mice. J. Immunol. 2006, 176, 5652-5661.
    • (c) Cho, M. L. STAT3 and NF-κB signal pathway is required for IL-23 mediated IL-17 production in spontaneous arthritis animal model IL-1 receptor antagonist-deficient mice. J. Immunol. 2006, 176, 5652-5661.
  • 4
    • 21644446281 scopus 로고    scopus 로고
    • Interleukin-1β and tumor necrosis factor-a upregulate interleukin-23 subunit p19 gene expression in human colonic subepithelial myofibroblasts
    • (d) Zhang, Z. Interleukin-1β and tumor necrosis factor-a upregulate interleukin-23 subunit p19 gene expression in human colonic subepithelial myofibroblasts. Int. J. Mol. Med. 2005, 15, 79-83.
    • (2005) Int. J. Mol. Med , vol.15 , pp. 79-83
    • Zhang, Z.1
  • 5
    • 0041967294 scopus 로고    scopus 로고
    • Essential role for IKKg/NEMO in TCR-induced IL-2 expression in Jurkat T cells
    • (e) He, K. L.; Ting, A. T. Essential role for IKKg/NEMO in TCR-induced IL-2 expression in Jurkat T cells. Eur. J. Immunol. 2003, 33, 1917-1924.
    • (2003) Eur. J. Immunol , vol.33 , pp. 1917-1924
    • He, K.L.1    Ting, A.T.2
  • 6
    • 0030048332 scopus 로고    scopus 로고
    • B cells from p50/NF-κB knockout mice have selective defects in proliferation, differentiation, germ-line CH transcription, and Ig class switching
    • (f) Snapper, C. M. B cells from p50/NF-κB knockout mice have selective defects in proliferation, differentiation, germ-line CH transcription, and Ig class switching. J. Immunol. 1996, 156, 183-191.
    • (1996) J. Immunol , vol.156 , pp. 183-191
    • Snapper, C.M.1
  • 7
    • 19344374949 scopus 로고    scopus 로고
    • IκB kinase (IKK)b, but not IKKa, is a critical mediator of osteoclast survival and is required for inflammation-induced bone loss
    • (g) Ruocco, M. G. IκB kinase (IKK)b, but not IKKa, is a critical mediator of osteoclast survival and is required for inflammation-induced bone loss. J. Exp. Med. 2005, 201, 1677-1687.
    • (2005) J. Exp. Med , vol.201 , pp. 1677-1687
    • Ruocco, M.G.1
  • 8
    • 25644459306 scopus 로고    scopus 로고
    • Collagen and aggrecan degradation is blocked in interleukin-1-treated cartlidge explants by an inhibitor of IκB kinase through suppression of metalloproteinase expression
    • (h) Pattoli, M. A. Collagen and aggrecan degradation is blocked in interleukin-1-treated cartlidge explants by an inhibitor of IκB kinase through suppression of metalloproteinase expression. J. Pharmacol. Exp. Ther. 2005, 315, 382-388.
    • (2005) J. Pharmacol. Exp. Ther , vol.315 , pp. 382-388
    • Pattoli, M.A.1
  • 9
    • 0031126395 scopus 로고    scopus 로고
    • IκB proteins: Structure function and regulation
    • Whiteside, S. T.; Israel, A. IκB proteins: structure function and regulation. Semin. Cancer Biol. 1997, 8, 75-82.
    • (1997) Semin. Cancer Biol , vol.8 , pp. 75-82
    • Whiteside, S.T.1    Israel, A.2
  • 10
    • 0036234459 scopus 로고    scopus 로고
    • Missing pieces in the NF-κB puzzle
    • Ghosh, S.; Karin, M. Missing pieces in the NF-κB puzzle. Cell 2002, 109, S81-S96.
    • (2002) Cell , vol.109
    • Ghosh, S.1    Karin, M.2
  • 11
    • 33847168466 scopus 로고    scopus 로고
    • IκB kinase inhibitors for treating autoimmune and inflammatory disorders: Potential and challenges
    • Strnad, J.; Burke, J. R. IκB kinase inhibitors for treating autoimmune and inflammatory disorders: potential and challenges. Trends Pharmacol. Sci. 2007, 28, 142-148.
    • (2007) Trends Pharmacol. Sci , vol.28 , pp. 142-148
    • Strnad, J.1    Burke, J.R.2
  • 12
    • 0036242607 scopus 로고    scopus 로고
    • Glucocorticoids: Do we know how they work?
    • Saklatvala, J. Glucocorticoids: do we know how they work? Arthritis Res. 2002, 4, 146-150.
    • (2002) Arthritis Res , vol.4 , pp. 146-150
    • Saklatvala, J.1
  • 13
    • 11844305963 scopus 로고    scopus 로고
    • Attenuation of murine collagen-induced arthritis by a novel, potent, selective small molecule inhibitor of IκB kinase 2, TPCA-1 (2-[(aminocarbonyl)amino]-5-(4-fluorophenyl)-3-thiophenecarboxamide), occurs via reduction of proinflammatory cytokines and antigen-induced T cell proliferation
    • (a) Podolin, P. L. Attenuation of murine collagen-induced arthritis by a novel, potent, selective small molecule inhibitor of IκB kinase 2, TPCA-1 (2-[(aminocarbonyl)amino]-5-(4-fluorophenyl)-3-thiophenecarboxamide), occurs via reduction of proinflammatory cytokines and antigen-induced T cell proliferation. J. Pharmacol. Exp. Ther. 2005, 312, 373-381.
    • (2005) J. Pharmacol. Exp. Ther , vol.312 , pp. 373-381
    • Podolin, P.L.1
  • 14
    • 0037449711 scopus 로고    scopus 로고
    • BMS-345541 is a highly selective inhibitor of IκB kinase that binds to an allosteric site of the enzyme and blocks NF-κB dependent transcription in mice
    • (b) Burke, J. R. BMS-345541 is a highly selective inhibitor of IκB kinase that binds to an allosteric site of the enzyme and blocks NF-κB dependent transcription in mice. J. Biol. Chem. 2003, 278, 1450-1456.
    • (2003) J. Biol. Chem , vol.278 , pp. 1450-1456
    • Burke, J.R.1
  • 15
    • 19944374141 scopus 로고    scopus 로고
    • A selective novel lowmolecular- weight inhibitor of IκB kinase- (IKK-) prevents pulmonary inflammation and shows broad anti-inflammatory activity
    • (c) Ziegelbauer, K. A selective novel lowmolecular- weight inhibitor of IκB kinase- (IKK-) prevents pulmonary inflammation and shows broad anti-inflammatory activity. Br. J. Pharmacol. 2005, 145, 178-192.
    • (2005) Br. J. Pharmacol , vol.145 , pp. 178-192
    • Ziegelbauer, K.1
  • 16
    • 33646767823 scopus 로고    scopus 로고
    • A selective small molecule IκB kinase β inhibitor blocks nuclear factor κB-mediated inflammatory responses in human fibroblast-like synovicocytes, chondrocytes, and mast cells
    • (d) Wen, D. A selective small molecule IκB kinase β inhibitor blocks nuclear factor κB-mediated inflammatory responses in human fibroblast-like synovicocytes, chondrocytes, and mast cells. J. Pharmacol. Exp. Ther. 2006, 317, 989-1001.
    • (2006) J. Pharmacol. Exp. Ther , vol.317 , pp. 989-1001
    • Wen, D.1
  • 18
    • 64549138278 scopus 로고    scopus 로고
    • Preparation of Pyrazolopurine-Based Tricyclic Compounds for the Treatment of Inflammatory and Immune Diseases
    • PCT Int. Appl. WO 2004075846
    • (f) Qiu, Y.; Belema, M.; Yang, X.; Zusi, F. C.; Pitts, W. J. Preparation of Pyrazolopurine-Based Tricyclic Compounds for the Treatment of Inflammatory and Immune Diseases. PCT Int. Appl. WO 2004075846, 2004.
    • (2004)
    • Qiu, Y.1    Belema, M.2    Yang, X.3    Zusi, F.C.4    Pitts, W.J.5
  • 20
    • 84986456135 scopus 로고
    • Chemistry of the phenoxathiins and isosterically related heterocycles. The synthesis of 2-azathianthrene and selected analogs
    • Lam, W. W.; Martin, G. E.; Lynch, V. M.; Simonsen, S. H.; Lindsay, C. M.; Smith, K. Chemistry of the phenoxathiins and isosterically related heterocycles. The synthesis of 2-azathianthrene and selected analogs. J. Heterocycl. Chem. 1986, 23, 785-791.
    • (1986) J. Heterocycl. Chem , vol.23 , pp. 785-791
    • Lam, W.W.1    Martin, G.E.2    Lynch, V.M.3    Simonsen, S.H.4    Lindsay, C.M.5    Smith, K.6
  • 21
    • 85162659176 scopus 로고
    • Nitrierungsprodukte des γ-aminopyridins
    • Koenigs, E.; Mields, M.; Gurlt, H. Nitrierungsprodukte des γ-aminopyridins. Chem. Ber. 1924, 57, 1179-1187.
    • (1924) Chem. Ber , vol.57 , pp. 1179-1187
    • Koenigs, E.1    Mields, M.2    Gurlt, H.3
  • 22
    • 3242778456 scopus 로고    scopus 로고
    • Whatever happened to cassette-dosing pharmacokinetics?
    • Manitpisitkul, P.; White, R. E. Whatever happened to cassette-dosing pharmacokinetics? Drug DiscoVery Today 2004, 15, 652-658.
    • (2004) Drug DiscoVery Today , vol.15 , pp. 652-658
    • Manitpisitkul, P.1    White, R.E.2
  • 23
    • 64549115224 scopus 로고    scopus 로고
    • The Alamar blue assay was conducted according to the protocol described in Zhi-Jun et al. (J. Immunol. Methods 1997, 210, 25) by using reagents obtained from Biosource International.
    • The Alamar blue assay was conducted according to the protocol described in Zhi-Jun et al. (J. Immunol. Methods 1997, 210, 25) by using reagents obtained from Biosource International.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.