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Journal Abstract Search

173 related items for PubMed ID: 21036044

  • 1. 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]

  • 2. Pharmacological characterization of INCB3344, a small molecule antagonist of human CCR2.
    Shin N, Baribaud F, Wang K, Yang G, Wynn R, Covington MB, Feldman P, Gallagher KB, Leffet LM, Lo YY, Wang A, Xue CB, Newton RC, Scherle PA.
    Biochem Biophys Res Commun; 2009 Sep 18; 387(2):251-5. PubMed ID: 19576173
    [Abstract] [Full Text] [Related]

  • 3. Synthesis and biological evaluation of 3-aminopyrrolidine derivatives as CC chemokine receptor 2 antagonists.
    Lim JW, Oh Y, Kim JH, Oak MH, Na Y, Lee JO, Lee SW, Cho H, Park WK, Choi G, Kang J.
    Bioorg Med Chem Lett; 2010 Apr 01; 20(7):2099-102. PubMed ID: 20223662
    [Abstract] [Full Text] [Related]

  • 4. Discovery of trisubstituted cyclohexanes as potent CC chemokine receptor 2 (CCR2) antagonists.
    Cherney RJ, Brogan JB, Mo R, Lo YC, Yang G, Miller PB, Scherle PA, Molino BF, Carter PH, Decicco CP.
    Bioorg Med Chem Lett; 2009 Feb 01; 19(3):597-601. PubMed ID: 19131247
    [Abstract] [Full Text] [Related]

  • 5. Pharmacological profile of JNJ-27141491 [(S)-3-[3,4-difluorophenyl)-propyl]-5-isoxazol-5-yl-2-thioxo-2,3-dihydro-1H-imidazole-4-carboxyl acid methyl ester], as a noncompetitive and orally active antagonist of the human chemokine receptor CCR2.
    Buntinx M, Hermans B, Goossens J, Moechars D, Gilissen RA, Doyon J, Boeckx S, Coesemans E, Van Lommen G, Van Wauwe JP.
    J Pharmacol Exp Ther; 2008 Oct 01; 327(1):1-9. PubMed ID: 18599682
    [Abstract] [Full Text] [Related]

  • 6. Discovery and pharmacological characterization of a novel rodent-active CCR2 antagonist, INCB3344.
    Brodmerkel CM, Huber R, Covington M, Diamond S, Hall L, Collins R, Leffet L, Gallagher K, Feldman P, Collier P, Stow M, Gu X, Baribaud F, Shin N, Thomas B, Burn T, Hollis G, Yeleswaram S, Solomon K, Friedman S, Wang A, Xue CB, Newton RC, Scherle P, Vaddi K.
    J Immunol; 2005 Oct 15; 175(8):5370-8. PubMed ID: 16210643
    [Abstract] [Full Text] [Related]

  • 7. The discovery of novel cyclohexylamide CCR2 antagonists.
    Lanter JC, Markotan TP, Zhang X, Subasinghe N, Kang FA, Hou C, Singer M, Opas E, McKenney S, Crysler C, Johnson D, Molloy CJ, Sui Z.
    Bioorg Med Chem Lett; 2011 Dec 15; 21(24):7496-501. PubMed ID: 22061641
    [Abstract] [Full Text] [Related]

  • 8. Discovery of 3-piperidinyl-1-cyclopentanecarboxamide as a novel scaffold for highly potent CC chemokine receptor 2 antagonists.
    Yang L, Butora G, Jiao RX, Pasternak A, Zhou C, Parsons WH, Mills SG, Vicario PP, Ayala JM, Cascieri MA, MacCoss M.
    J Med Chem; 2007 May 31; 50(11):2609-11. PubMed ID: 17461566
    [Abstract] [Full Text] [Related]

  • 9. Potent antagonists of the CCR2b receptor. Part 3: SAR of the (R)-3-aminopyrrolidine series.
    Moree WJ, Kataoka K, Ramirez-Weinhouse MM, Shiota T, Imai M, Tsutsumi T, Sudo M, Endo N, Muroga Y, Hada T, Fanning D, Saunders J, Kato Y, Myers PL, Tarby CM.
    Bioorg Med Chem Lett; 2008 Mar 15; 18(6):1869-73. PubMed ID: 18313297
    [Abstract] [Full Text] [Related]

  • 10. Discovery of potent, orally bioavailable small-molecule inhibitors of the human CCR2 receptor.
    Doyon J, Coesemans E, Boeckx S, Buntinx M, Hermans B, Van Wauwe JP, Gilissen RA, De Groot AH, Corens D, Van Lommen G.
    ChemMedChem; 2008 Apr 15; 3(4):660-9. PubMed ID: 18188859
    [Abstract] [Full Text] [Related]

  • 11. Elucidation of binding sites of dual antagonists in the human chemokine receptors CCR2 and CCR5.
    Hall SE, Mao A, Nicolaidou V, Finelli M, Wise EL, Nedjai B, Kanjanapangka J, Harirchian P, Chen D, Selchau V, Ribeiro S, Schyler S, Pease JE, Horuk R, Vaidehi N.
    Mol Pharmacol; 2009 Jun 15; 75(6):1325-36. PubMed ID: 19297521
    [Abstract] [Full Text] [Related]

  • 12. Synthesis and evaluation of cis-3,4-disubstituted piperidines as potent CC chemokine receptor 2 (CCR2) antagonists.
    Cherney RJ, Nelson DJ, Lo YC, Yang G, Scherle PA, Jezak H, Solomon KA, Carter PH, Decicco CP.
    Bioorg Med Chem Lett; 2008 Sep 15; 18(18):5063-5. PubMed ID: 18722120
    [Abstract] [Full Text] [Related]

  • 13. CCR2 receptor antagonists: optimization of biaryl sulfonamides to increase activity in whole blood.
    Wang GZ, Haile PA, Daniel T, Belot B, Viet AQ, Goodman KB, Sha D, Dowdell SE, Varga N, Hong X, Chakravorty S, Webb C, Cornejo C, Olzinski A, Bernard R, Evans C, Emmons A, Briand J, Chung CW, Quek R, Lee D, Gough PJ, Sehon CA.
    Bioorg Med Chem Lett; 2011 Dec 15; 21(24):7291-4. PubMed ID: 22047688
    [Abstract] [Full Text] [Related]

  • 14. Discovery of disubstituted cyclohexanes as a new class of CC chemokine receptor 2 antagonists.
    Cherney RJ, Mo R, Meyer DT, Nelson DJ, Lo YC, Yang G, Scherle PA, Mandlekar S, Wasserman ZR, Jezak H, Solomon KA, Tebben AJ, Carter PH, Decicco CP.
    J Med Chem; 2008 Feb 28; 51(4):721-4. PubMed ID: 18232650
    [Abstract] [Full Text] [Related]

  • 15. Design, synthesis, and structure-activity relationship of novel CCR2 antagonists.
    Kothandaraman S, Donnely KL, Butora G, Jiao R, Pasternak A, Morriello GJ, Goble SD, Zhou C, Mills SG, Maccoss M, Vicario PP, Ayala JM, Demartino JA, Struthers M, Cascieri MA, Yang L.
    Bioorg Med Chem Lett; 2009 Mar 15; 19(6):1830-4. PubMed ID: 19237282
    [Abstract] [Full Text] [Related]

  • 16. Synthesis and biological evaluation of phenyl piperidine derivatives as CCR2 antagonists.
    Xia M, Hou C, Pollack S, Brackley J, DeMong D, Pan M, Singer M, Matheis M, Olini G, Cavender D, Wachter M.
    Bioorg Med Chem Lett; 2007 Nov 01; 17(21):5964-8. PubMed ID: 17869105
    [Abstract] [Full Text] [Related]

  • 17. Substituted dipiperidine alcohols as potent CCR2 antagonists.
    Xia M, Hou C, Demong D, Pollack S, Pan M, Brackley J, Singer M, Matheis M, Cavender D, Wachter M.
    Bioorg Med Chem Lett; 2008 Jun 15; 18(12):3562-4. PubMed ID: 18487045
    [Abstract] [Full Text] [Related]

  • 18. Discovery of an orally-bioavailable CC Chemokine Receptor 2 antagonist derived from an acyclic diaminoalcohol backbone.
    Carter PH, Brown GD, King SR, Voss ME, Tebben AJ, Cherney RJ, Mandlekar S, Lo YC, Yang G, Miller PB, Scherle PA, Zhao Q, Decicco CP.
    Bioorg Med Chem Lett; 2012 May 01; 22(9):3311-6. PubMed ID: 22475558
    [Abstract] [Full Text] [Related]

  • 19. Synthesis, structure-activity relationship and in vivo antiinflammatory efficacy of substituted dipiperidines as CCR2 antagonists.
    Xia M, Hou C, DeMong DE, Pollack SR, Pan M, Brackley JA, Jain N, Gerchak C, Singer M, Malaviya R, Matheis M, Olini G, Cavender D, Wachter M.
    J Med Chem; 2007 Nov 15; 50(23):5561-3. PubMed ID: 17929797
    [Abstract] [Full Text] [Related]

  • 20. Novel, orally bioavailable gamma-aminoamide CC chemokine receptor 2 (CCR2) antagonists.
    Pasternak A, Marino D, Vicario PP, Ayala JM, Cascierri MA, Parsons W, Mills SG, Maccoss M, Yang L.
    J Med Chem; 2006 Aug 10; 49(16):4801-4. PubMed ID: 16884289
    [Abstract] [Full Text] [Related]

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