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Volumn 20, Issue 17, 2010, Pages 5269-5273

Discovery of tetrahydroisoquinoline (THIQ) derivatives as potent and orally bioavailable LFA-1/ICAM-1 antagonists

Author keywords

Antagonist; Intercellular adhesion molecule 1 (ICAM 1); Leukocyte function associated antigen 1 (LFA 1); Tetrahydroisoquinoline (THIQ) derivative

Indexed keywords

INTERCELLULAR ADHESION MOLECULE 1; LYMPHOCYTE FUNCTION ASSOCIATED ANTIGEN 1; TETRAHYDROISOQUINOLINE DERIVATIVE; THIOGLYCOLIC ACID;

EID: 77955659802     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.06.145     Document Type: Article
Times cited : (13)

References (49)
  • 13
    • 77955657159 scopus 로고    scopus 로고
    • Post-market findings have shown that long term use of efalizumab causes severe side effects, including lymphoma, meningitis, progressive multifocal leukoencephalopathy (PML), and sepsis etc. Recently, Genentech, the manufacturer of the efalizumab, announced that it has begun a voluntary, phased withdrawal of the product from the US market. For more information, see
    • Post-market findings have shown that long term use of efalizumab causes severe side effects, including lymphoma, meningitis, progressive multifocal leukoencephalopathy (PML), and sepsis etc. Recently, Genentech, the manufacturer of the efalizumab, announced that it has begun a voluntary, phased withdrawal of the product from the US market. For more information, see http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm149561.htm.
  • 39
    • 77955661732 scopus 로고    scopus 로고
    • There were no LFA-1 antagonists derived from N-benzoyl amino acid advanced to clinical trials reported when we initiated this program in late 2002. SARCode, Inc. in-licensed Sunesis Pharmaceuticals, Inc.'s LFA-1 program in 2007 and has recently completed two Phase II clinical trials of SAR 1118 in patients with dry eyes and/or allergic conjunctivitis. For related press release, please see http://clinicaltrials.gov/ct2/results?term=SAR+1118
    • There were no LFA-1 antagonists derived from N-benzoyl amino acid advanced to clinical trials reported when we initiated this program in late 2002. SARCode, Inc. in-licensed Sunesis Pharmaceuticals, Inc.'s LFA-1 program in 2007 and has recently completed two Phase II clinical trials of SAR 1118 in patients with dry eyes and/or allergic conjunctivitis. For related press release, please see http://www.sarcode.com/news.html and for information on clinical trial status of SAR 1118, please see http://clinicaltrials.gov/ct2/ results?term=SAR+1118.
  • 40
    • 77955662503 scopus 로고    scopus 로고
    • WIPO Patent Appl. WO1999/49856
    • (a) Burdick, D. J. WIPO Patent Appl. WO1999/49856
    • Burdick, D.J.1
  • 47
    • 77955654551 scopus 로고    scopus 로고
    • Those active compounds in Hut-78 assay are also less potent in the presence of 10% fetal bovine serum (FBS). This suggests that the decrease of potency is possibly due to serum protein binding
    • Those active compounds in Hut-78 assay are also less potent in the presence of 10% fetal bovine serum (FBS). This suggests that the decrease of potency is possibly due to serum protein binding.
  • 48
    • 77955661864 scopus 로고    scopus 로고
    • -6 cm/s (A/B and B/A))
    • -6 cm/s (A/B and B/A)).


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.