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Page 1
Investigation of aminopyridiopyrazinones as PDE5 inhibitors: Evaluation of modifications to the central ring system.
Hughes RO, Walker JK, Cubbage JW, Fobian YM, Rogier DJ, Heasley SE, Blevis-Bal RM, Benson AG, Owen DR, Jacobsen EJ, Freskos JN, Molyneaux JM, Brown DL, Stallings WC, Acker BA, Maddux TM, Tollefson MB, Williams JM, Moon JB, Mischke BV, Rumsey JM, Zheng Y, Macinnes A, Bond BR, Yu Y. Hughes RO, et al. Among authors: brown dl. Bioorg Med Chem Lett. 2009 Aug 1;19(15):4092-6. doi: 10.1016/j.bmcl.2009.06.004. Epub 2009 Jun 6. Bioorg Med Chem Lett. 2009. PMID: 19539468
Design of potent inhibitors of human beta-secretase. Part 1.
Freskos JN, Fobian YM, Benson TE, Bienkowski MJ, Brown DL, Emmons TL, Heintz R, Laborde A, McDonald JJ, Mischke BV, Molyneaux JM, Moon JB, Mullins PB, Bryan Prince D, Paddock DJ, Tomasselli AG, Winterrowd G. Freskos JN, et al. Among authors: brown dl. Bioorg Med Chem Lett. 2007 Jan 1;17(1):73-7. doi: 10.1016/j.bmcl.2006.09.092. Epub 2006 Oct 4. Bioorg Med Chem Lett. 2007. PMID: 17046251
Design of potent inhibitors of human beta-secretase. Part 2.
Freskos JN, Fobian YM, Benson TE, Moon JB, Bienkowski MJ, Brown DL, Emmons TL, Heintz R, Laborde A, McDonald JJ, Mischke BV, Molyneaux JM, Mullins PB, Bryan Prince D, Paddock DJ, Tomasselli AG, Winterrowd G. Freskos JN, et al. Among authors: brown dl. Bioorg Med Chem Lett. 2007 Jan 1;17(1):78-81. doi: 10.1016/j.bmcl.2006.09.091. Epub 2006 Oct 4. Bioorg Med Chem Lett. 2007. PMID: 17049233
Identification, synthesis and SAR of amino substituted pyrido[3,2b]pyrazinones as potent and selective PDE5 inhibitors.
Owen DR, Walker JK, Jon Jacobsen E, Freskos JN, Hughes RO, Brown DL, Bell AS, Brown DG, Phillips C, Mischke BV, Molyneaux JM, Fobian YM, Heasley SE, Moon JB, Stallings WC, Joseph Rogier D, Fox DN, Palmer MJ, Ringer T, Rodriquez-Lens M, Cubbage JW, Blevis-Bal RM, Benson AG, Acker BA, Maddux TM, Tollefson MB, Bond BR, Macinnes A, Yu Y. Owen DR, et al. Among authors: brown dl, brown dg. Bioorg Med Chem Lett. 2009 Aug 1;19(15):4088-91. doi: 10.1016/j.bmcl.2009.06.012. Epub 2009 Jun 6. Bioorg Med Chem Lett. 2009. PMID: 19540112 Free article.
Optimization of the aminopyridopyrazinones class of PDE5 inhibitors: discovery of 3-[(trans-4-hydroxycyclohexyl)amino]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one.
Hughes RO, Walker JK, Rogier DJ, Heasley SE, Blevis-Bal RM, Benson AG, Jacobsen EJ, Cubbage JW, Fobian YM, Owen DR, Freskos JN, Molyneaux JM, Brown DL, Acker BA, Maddux TM, Tollefson MB, Moon JB, Mischke BV, Rumsey JM, Zheng Y, MacInnes A, Bond BR, Yu Y. Hughes RO, et al. Among authors: brown dl. Bioorg Med Chem Lett. 2009 Sep 1;19(17):5209-13. doi: 10.1016/j.bmcl.2009.07.019. Epub 2009 Jul 10. Bioorg Med Chem Lett. 2009. PMID: 19631533
Design, synthesis, and biological evaluation of 3-[4-(2-hydroxyethyl)piperazin-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one, a potent, orally active, brain penetrant inhibitor of phosphodiesterase 5 (PDE5).
Hughes RO, Rogier DJ, Jacobsen EJ, Walker JK, Macinnes A, Bond BR, Zhang LL, Yu Y, Zheng Y, Rumsey JM, Walgren JL, Curtiss SW, Fobian YM, Heasley SE, Cubbage JW, Moon JB, Brown DL, Acker BA, Maddux TM, Tollefson MB, Mischke BV, Owen DR, Freskos JN, Molyneaux JM, Benson AG, Blevis-Bal RM. Hughes RO, et al. Among authors: brown dl. J Med Chem. 2010 Mar 25;53(6):2656-60. doi: 10.1021/jm901781q. J Med Chem. 2010. PMID: 20196613
4,5-Diaryloxazole inhibitors of cyclooxygenase-2 (COX-2).
Talley JJ, Bertenshaw SR, Brown DL, Carter JS, Graneto MJ, Koboldt CM, Masferrer JL, Norman BH, Rogier DJ Jr, Zwwifel BS, Seibert K. Talley JJ, et al. Among authors: brown dl. Med Res Rev. 1999 May;19(3):199-208. doi: 10.1002/(sici)1098-1128(199905)19:3<199::aid-med1>3.0.co;2-7. Med Res Rev. 1999. PMID: 10232649 Review.
1,048 results