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Journal Abstract Search

121 related items for PubMed ID: 19891440

  • 1. Discovery of trans-4-[1-[[2,5-Dichloro-4-(1-methyl-3-indolylcarboxamido)phenyl]acetyl]-(4S)-methoxy-(2S)-pyrrolidinylmethoxy]cyclohexanecarboxylic acid: an orally active, selective very late antigen-4 antagonist.
    Muro F, Iimura S, Sugimoto Y, Yoneda Y, Chiba J, Watanabe T, Setoguchi M, Iigou Y, Matsumoto K, Satoh A, Takayama G, Taira T, Yokoyama M, Takashi T, Nakayama A, Machinaga N.
    J Med Chem; 2009 Dec 24; 52(24):7974-92. PubMed ID: 19891440
    [Abstract] [Full Text] [Related]

  • 2. A novel and potent VLA-4 antagonist based on trans-4-substituted cyclohexanecarboxylic acid.
    Muro F, Iimura S, Yoneda Y, Chiba J, Watanabe T, Setoguchi M, Takayama G, Yokoyama M, Takashi T, Nakayama A, Machinaga N.
    Bioorg Med Chem; 2009 Feb 01; 17(3):1232-43. PubMed ID: 19124247
    [Abstract] [Full Text] [Related]

  • 3. A novel, potent, and orally active VLA-4 antagonist with good aqueous solubility: trans-4-[1-[[2-(5-Fluoro-2-methylphenylamino)-7-fluoro-6-benzoxazolyl]acetyl]-(5S)-[methoxy(methyl)amino]methyl-(2S)-pyrrolidinylmethoxy]cyclohexanecarboxylic acid.
    Setoguchi M, Iimura S, Sugimoto Y, Yoneda Y, Chiba J, Watanabe T, Muro F, Iigo Y, Takayama G, Yokoyama M, Taira T, Aonuma M, Takashi T, Nakayama A, Machinaga N.
    Bioorg Med Chem; 2013 Jan 01; 21(1):42-61. PubMed ID: 23218775
    [Abstract] [Full Text] [Related]

  • 4. Identification of trans-4-[1-[[7-fluoro-2-(1-methyl-3-indolyl)-6-benzoxazolyl]acetyl]-(4S)-fluoro-(2S)-pyrrolidinylmethoxy]cyclohexanecarboxylic acid as a potent, orally active VLA-4 antagonist.
    Setoguchi M, Iimura S, Sugimoto Y, Yoneda Y, Chiba J, Watanabe T, Muro F, Iigo Y, Takayama G, Yokoyama M, Taira T, Aonuma M, Takashi T, Nakayama A, Machinaga N.
    Bioorg Med Chem; 2012 Feb 01; 20(3):1201-12. PubMed ID: 22261021
    [Abstract] [Full Text] [Related]

  • 5. A concise synthesis of a very late antigen-4 antagonist trans-4-[1-[[2,5-dichloro-4-(1-methyl-3-indolylcarboxyamide)phenyl]acetyl]-(4S)-methoxy-(2S)-pyrrolidinylmethoxy]cyclohexanecarboxylic acid via reductive etherification.
    Chiba J, Muro F, Setoguchi M, Machinaga N.
    Chem Pharm Bull (Tokyo); 2012 Feb 01; 60(7):882-6. PubMed ID: 22790822
    [Abstract] [Full Text] [Related]

  • 6. A novel synthetic approach to very late antigen-4 antagonist trans-4-[1-[[2,5-dichloro-4-(1-methyl-3-indolylcarboxyamide)phenyl]acetyl]-(4S)-methoxy-(2S)-pyrrolidinylmethoxy]cyclohexanecarboxylic acid via tert-butyl trans-[(4S)-Methoxy-(2S)-pyrrolidinylmethoxy]cyclohexanecarboxylate as a key intermediate.
    Chiba J, Machinaga N.
    Chem Pharm Bull (Tokyo); 2011 Feb 01; 59(5):574-8. PubMed ID: 21532195
    [Abstract] [Full Text] [Related]

  • 7. Identification of 4-[1-[3-chloro-4-[N'-(5-fluoro-2-methylphenyl)ureido]phenylacetyl]-(4S)-fluoro-(2S)-pyrrolidinylmethoxy]benzoic acid as a potent, orally active VLA-4 antagonist.
    Muro F, Iimura S, Yoneda Y, Chiba J, Watanabe T, Setoguchi M, Iigou Y, Takayama G, Yokoyama M, Takashi T, Nakayama A, Machinaga N.
    Bioorg Med Chem; 2008 Dec 01; 16(23):9991-10000. PubMed ID: 18952443
    [Abstract] [Full Text] [Related]

  • 8. Improvement of pulmonary function by oral treatment with a VLA-4 antagonist in a mouse asthmatic model.
    Takayama G, Matsumoto K, Taira T, Aonuma M, Yokoyama M, Iigo Y, Takashi T.
    J Pharmacol Sci; 2013 Dec 01; 121(2):172-5. PubMed ID: 23419271
    [Abstract] [Full Text] [Related]

  • 9. Synthesis and biological evaluation of benzoic acid derivatives as potent, orally active VLA-4 antagonists.
    Chiba J, Iimura S, Yoneda Y, Watanabe T, Muro F, Tsubokawa M, Iigou Y, Satoh A, Takayama G, Yokoyama M, Takashi T, Nakayama A, Machinaga N.
    Bioorg Med Chem; 2007 Feb 15; 15(4):1679-93. PubMed ID: 17194595
    [Abstract] [Full Text] [Related]

  • 10. Discovery and development of the novel potent orally active thrombin inhibitor N-(9-hydroxy-9-fluorenecarboxy)prolyl trans-4-aminocyclohexylmethyl amide (L-372,460): coapplication of structure-based design and rapid multiple analogue synthesis on solid support.
    Brady SF, Stauffer KJ, Lumma WC, Smith GM, Ramjit HG, Lewis SD, Lucas BJ, Gardell SJ, Lyle EA, Appleby SD, Cook JJ, Holahan MA, Stranieri MT, Lynch JJ, Lin JH, Chen IW, Vastag K, Naylor-Olsen AM, Vacca JP.
    J Med Chem; 1998 Jan 29; 41(3):401-6. PubMed ID: 9464370
    [Abstract] [Full Text] [Related]

  • 11. (3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor.
    Ammirati MJ, Andrews KM, Boyer DD, Brodeur AM, Danley DE, Doran SD, Hulin B, Liu S, McPherson RK, Orena SJ, Parker JC, Polivkova J, Qiu X, Soglia CB, Treadway JL, VanVolkenburg MA, Wilder DC, Piotrowski DW.
    Bioorg Med Chem Lett; 2009 Apr 01; 19(7):1991-5. PubMed ID: 19275964
    [Abstract] [Full Text] [Related]

  • 12. Discovery of a thieno[2,3-d]pyrimidine-2,4-dione bearing a p-methoxyureidophenyl moiety at the 6-position: a highly potent and orally bioavailable non-peptide antagonist for the human luteinizing hormone-releasing hormone receptor.
    Sasaki S, Cho N, Nara Y, Harada M, Endo S, Suzuki N, Furuya S, Fujino M.
    J Med Chem; 2003 Jan 02; 46(1):113-24. PubMed ID: 12502365
    [Abstract] [Full Text] [Related]

  • 13. Identified a morpholinyl-4-piperidinylacetic acid derivative as a potent oral active VLA-4 antagonist.
    Chiba J, Machinaga N, Takashi T, Ejima A, Takayama G, Yokoyama M, Nakayama A, Baldwin JJ, McDonald E, Moriarty KJ, Sarko CR, Saionz KW, Swanson R, Hussain Z, Wong A.
    Bioorg Med Chem Lett; 2005 Jan 03; 15(1):41-5. PubMed ID: 15582407
    [Abstract] [Full Text] [Related]

  • 14. Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2.
    Xue CB, Wang A, Meloni D, Zhang K, Kong L, Feng H, Glenn J, Huang T, Zhang Y, Cao G, Anand R, Zheng C, Xia M, Han Q, Robinson DJ, Storace L, Shao L, Li M, Brodmerkel CM, Covington M, Scherle P, Diamond S, Yeleswaram S, Vaddi K, Newton R, Hollis G, Friedman S, Metcalf B.
    Bioorg Med Chem Lett; 2010 Dec 15; 20(24):7473-8. PubMed ID: 21036044
    [Abstract] [Full Text] [Related]

  • 15. Synthesis and serotonergic activity of 3-[2-(pyrrolidin-1-yl)ethyl]indoles: potent agonists for the h5-HT1D receptor with high selectivity over the h5-HT1B receptor.
    Sternfeld F, Guiblin AR, Jelley RA, Matassa VG, Reeve AJ, Hunt PA, Beer MS, Heald A, Stanton JA, Sohal B, Watt AP, Street LJ.
    J Med Chem; 1999 Feb 25; 42(4):677-90. PubMed ID: 10052975
    [Abstract] [Full Text] [Related]

  • 16. Pharmacology of (2S,4Z)-N-[(2S)-2-hydroxy-2-phenylethyl]-4-(methoxyimino) -1-[(2'-methyl[1,1'-biphenyl]-4-yl)carbonyl]-2-pyrrolidinecarboxamide, a new potent and selective nonpeptide antagonist of the oxytocin receptor.
    Cirillo R, Gillio Tos E, Schwarz MK, Quattropani A, Scheer A, Missotten M, Dorbais J, Nichols A, Borrelli F, Giachetti C, Golzio L, Marinelli P, Thomas RJ, Chevillard C, Laurent F, Portet K, Barberis C, Chollet A.
    J Pharmacol Exp Ther; 2003 Jul 25; 306(1):253-61. PubMed ID: 12660315
    [Abstract] [Full Text] [Related]

  • 17. A novel class of orally active non-peptide bradykinin B2 receptor antagonists. 4. Discovery of novel frameworks mimicking the active conformation.
    Abe Y, Kayakiri H, Satoh S, Inoue T, Sawada Y, Inamura N, Asano M, Aramori I, Hatori C, Sawai H, Oku T, Tanaka H.
    J Med Chem; 1998 Nov 05; 41(23):4587-98. PubMed ID: 9804698
    [Abstract] [Full Text] [Related]

  • 18. 3-[5-(3,4-Dichloro-phenyl)-1-(4-methoxy-phenyl)-1H-pyrazol-3-yl]-2-m-tolyl-propionate (JNJ-17156516), a novel, potent, and selective cholecystokinin 1 receptor antagonist: in vitro and in vivo pharmacological comparison with dexloxiglumide.
    Morton MF, Barrett TD, Yan W, Freedman JM, Lagaud G, Prendergast CE, Moreno V, Pyati J, Figueroa K, Li L, Wu X, Rizzolio M, Breitenbucher JG, McClure K, Shankley NP.
    J Pharmacol Exp Ther; 2007 Nov 05; 323(2):562-9. PubMed ID: 17684117
    [Abstract] [Full Text] [Related]

  • 19. Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate.
    Shen HC, Ding FX, Raghavan S, Deng Q, Luell S, Forrest MJ, Carballo-Jane E, Wilsie LC, Krsmanovic ML, Taggart AK, Wu KK, Wu TJ, Cheng K, Ren N, Cai TQ, Chen Q, Wang J, Wolff MS, Tong X, Holt TG, Waters MG, Hammond ML, Tata JR, Colletti SL.
    J Med Chem; 2010 Mar 25; 53(6):2666-70. PubMed ID: 20184326
    [Abstract] [Full Text] [Related]

  • 20. Discovery of N1-(6-chloroimidazo[2,1-b][1,3]thiazole-5-sulfonyl)tryptamine as a potent, selective, and orally active 5-HT(6) receptor agonist.
    Cole DC, Stock JR, Lennox WJ, Bernotas RC, Ellingboe JW, Boikess S, Coupet J, Smith DL, Leung L, Zhang GM, Feng X, Kelly MF, Galante R, Huang P, Dawson LA, Marquis K, Rosenzweig-Lipson S, Beyer CE, Schechter LE.
    J Med Chem; 2007 Nov 15; 50(23):5535-8. PubMed ID: 17948978
    [Abstract] [Full Text] [Related]

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