메뉴 건너뛰기




Volumn 20, Issue 3, 2010, Pages 828-831

Design and synthesis of piperazine-indole p38α MAP kinase inhibitors with improved pharmacokinetic profiles

Author keywords

Inflammatory; Inhibitor; Kinase; MAP; p38

Indexed keywords

CARBENE; MITOGEN ACTIVATED PROTEIN KINASE P38 INHIBITOR; PIPERAZINE DERIVATIVE; SCIO 469; INDOLE DERIVATIVE; MITOGEN ACTIVATED PROTEIN KINASE 14; PIPERAZINE; PROTEIN BINDING; PROTEIN KINASE INHIBITOR;

EID: 74049110562     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.12.091     Document Type: Article
Times cited : (12)

References (20)
  • 14
    • 84925561840 scopus 로고    scopus 로고
    • note
    • http://www.accessmylibrary.com/article-1G1-70735265/scios-begin-phase-ib.html.
  • 15
    • 84925571364 scopus 로고    scopus 로고
    • note
    • http://clinicaltrials.gov/ct2/show/NCT00089921.
  • 16
    • 84925571363 scopus 로고    scopus 로고
    • Mavunkel, B. J.; Chakravarty, S.; Perumattam, J. J.; Dugar, S.; Lu, Q.; Liang, X. WO 2000/071535, 2000 ((d)-tartaric acid was used in the chiral resolution to obtain (2S,5R)-2,5-dimethyl-4-fluoro-benzyl piperazine tartaric salt).
    • Mavunkel, B. J.; Chakravarty, S.; Perumattam, J. J.; Dugar, S.; Lu, Q.; Liang, X. WO 2000/071535, 2000 ((d)-tartaric acid was used in the chiral resolution to obtain (2S,5R)-2,5-dimethyl-4-fluoro-benzyl piperazine tartaric salt).
  • 17
    • 84925571362 scopus 로고    scopus 로고
    • Baroudy, B. M.; Clader, J. W.; Josien, H. B.; Mccombie, S. W.; Mckittrick, B. A.; Miller, M. W.; Neustadt, B. R.; Palani, A.; Smith, E. M.; Steensma, R.; Tagat, J. R.; Vice, S. F.; Laughlin, M. A.; Gilbert, E.; Labroli, M. A. WO 2000/066558, 2000.
    • Baroudy, B. M.; Clader, J. W.; Josien, H. B.; Mccombie, S. W.; Mckittrick, B. A.; Miller, M. W.; Neustadt, B. R.; Palani, A.; Smith, E. M.; Steensma, R.; Tagat, J. R.; Vice, S. F.; Laughlin, M. A.; Gilbert, E.; Labroli, M. A. WO 2000/066558, 2000.
  • 18
    • 84925568216 scopus 로고    scopus 로고
    • note
    • (2R,5S)-Dimethyl-piperazine-1-carboxylic acid tert-butyl ester was synthesized using same procedure as for the synthesis of intermediate 5, except (l)-tartaric salt of chiral (2S,5R)-2,5-dimethyl-4-fluorobenzyl piperazine was used.
  • 19
    • 84925563316 scopus 로고    scopus 로고
    • Mavunkel, B. J.; Perumattam, J. J.; Tan, X.; Luedtke, G. R.; Lu, Q.; Lim, D.; Kizer, D.; Dugar, S.; Chakravarty, S.; Xu, Y.-j.; Jung, J.; Liclican, A.; Levy, D. E.; Tabora, J. Bioorg. Med. Chem. Lett., in press. doi:10.1016/j.bmcl.2009.12.031.
    • Mavunkel, B. J.; Perumattam, J. J.; Tan, X.; Luedtke, G. R.; Lu, Q.; Lim, D.; Kizer, D.; Dugar, S.; Chakravarty, S.; Xu, Y.-j.; Jung, J.; Liclican, A.; Levy, D. E.; Tabora, J. Bioorg. Med. Chem. Lett., in press. doi:10.1016/j.bmcl.2009.12.031.
  • 20
    • 84925568215 scopus 로고    scopus 로고
    • The LPS/TNFα Human Whole Blood Assay was run as described in: Mavunkel, B, Dugar, S, Luedtke, G, Tan, X, McEnroe, G. US Patent 6,696,443, 2004
    • The LPS/TNFα Human Whole Blood Assay was run as described in: Mavunkel, B.; Dugar, S.; Luedtke, G.; Tan, X.; McEnroe, G. US Patent 6,696,443, 2004.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.