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Discovery of S-[5-amino-1-(4-fluorophenyl)-1H-pyrazol-4-yl]-[3-(2,3-dihydroxypropoxy)phenyl]methanone (RO3201195), an orally bioavailable and highly selective inhibitor of p38 MAP kinase.
Goldstein DM, Alfredson T, Bertrand J, Browner MF, Clifford K, Dalrymple SA, Dunn J, Freire-Moar J, Harris S, Labadie SS, La Fargue J, Lapierre JM, Larrabee S, Li F, Papp E, McWeeney D, Ramesha C, Roberts R, Rotstein D, San Pablo B, Sjogren EB, So OY, Talamas FX, Tao W, Trejo A, Villasenor A, Welch M, Welch T, Weller P, Whiteley PE, Young K, Zipfel S. Goldstein DM, et al. Among authors: san pablo b. J Med Chem. 2006 Mar 9;49(5):1562-75. doi: 10.1021/jm050736c. J Med Chem. 2006. PMID: 16509574
Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally bioavailable and highly selective inhibitors of p38α mitogen-activated protein kinase.
Goldstein DM, Soth M, Gabriel T, Dewdney N, Kuglstatter A, Arzeno H, Chen J, Bingenheimer W, Dalrymple SA, Dunn J, Farrell R, Frauchiger S, La Fargue J, Ghate M, Graves B, Hill RJ, Li F, Litman R, Loe B, McIntosh J, McWeeney D, Papp E, Park J, Reese HF, Roberts RT, Rotstein D, San Pablo B, Sarma K, Stahl M, Sung ML, Suttman RT, Sjogren EB, Tan Y, Trejo A, Welch M, Weller P, Wong BR, Zecic H. Goldstein DM, et al. Among authors: san pablo b. J Med Chem. 2011 Apr 14;54(7):2255-65. doi: 10.1021/jm101423y. Epub 2011 Mar 4. J Med Chem. 2011. PMID: 21375264
Rational design of 6-methylsulfonylindoles as selective cyclooxygenase-2 inhibitors.
Campbell JA, Bordunov V, Broka CA, Browner MF, Kress JM, Mirzadegan T, Ramesha C, Sanpablo BF, Stabler R, Takahara P, Villasenor A, Walker KA, Wang JH, Welch M, Weller P. Campbell JA, et al. Bioorg Med Chem Lett. 2004 Sep 20;14(18):4741-5. doi: 10.1016/j.bmcl.2004.06.075. Bioorg Med Chem Lett. 2004. PMID: 15324899