Discovery of INCB10820/PF-4178903, a potent, selective, and orally bioavailable dual CCR2 and CCR5 antagonist
Zheng, Changsheng, Cao, Ganfeng, Xia, Michael, Feng, Hao, Glenn, Joseph, Anand, Rajan, Zhang, Ke, Huang, Taisheng, Wang, Anlai, Kong, Ling, Li, Mei, Galya, Laurine, Hughes, Robert O., Devraj, Rajesh, Morton, Phillip A., Rogier, D. Joseph, Covington, Maryanne, Baribaud, Fred, Shin, Niu, Scherle, Peggy, Diamond, Sharon, Yeleswaram, Swamy, Vaddi, Kris, Newton, Robert, Hollis, Greg, Friedman, Steven, Metcalf, Brian, Xue, Chu-Biao
Published in Bioorganic & medicinal chemistry letters (01.03.2011)
Published in Bioorganic & medicinal chemistry letters (01.03.2011)
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Investigation of the pyrazinones as PDE5 inhibitors: Evaluation of regioisomeric projections into the solvent region
Hughes, Robert O., Maddux, Todd, Joseph Rogier, D., Lu, Sharon, Walker, John K., Jon Jacobsen, E., Rumsey, Jeanne M., Zheng, Yi, MacInnes, Alan, Bond, Brian R., Han, Seungil
Published in Bioorganic & medicinal chemistry letters (01.11.2011)
Published in Bioorganic & medicinal chemistry letters (01.11.2011)
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Design and synthesis of novel CCR2 antagonists: Investigation of non-aryl/heteroaryl binding motifs
Trujillo, John I., Huang, Wei, Hughes, Robert O., Joseph Rogier, D., Turner, Steven R., Devraj, Rajesh, Morton, Philip A., Xue, Chu-Biao, Chao, Ganfeng, Covington, Maryanne B., Newton, Robert C., Metcalf, Brian
Published in Bioorganic & medicinal chemistry letters (15.03.2011)
Published in Bioorganic & medicinal chemistry letters (15.03.2011)
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Identification, synthesis and SAR of amino substituted pyrido[3,2b]pyrazinones as potent and selective PDE5 inhibitors
Owen, Dafydd R., Walker, John K., Jon Jacobsen, E., Freskos, John N., Hughes, Robert O., Brown, David L., Bell, Andrew S., Brown, David G., Phillips, Christopher, Mischke, Brent V., Molyneaux, John M., Fobian, Yvette M., Heasley, Steve E., Moon, Joseph B., Stallings, William C., Joseph Rogier, D., Fox, David N.A., Palmer, Michael J., Ringer, Tracy, Rodriquez-Lens, Margarita, Cubbage, Jerry W., Blevis-Bal, Radhika M., Benson, Alan G., Acker, Brad A., Maddux, Todd M., Tollefson, Michael B., Bond, Brian R., MacInnes, Alan, Yu, Yung
Published in Bioorganic & medicinal chemistry letters (01.08.2009)
Published in Bioorganic & medicinal chemistry letters (01.08.2009)
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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(1 H)-one
Hughes, Robert O., Walker, John K., Joseph Rogier, D., Heasley, Steve E., Blevis-Bal, Rhadika M., Benson, Alan G., Jon Jacobsen, E., Cubbage, Jerry W., Fobian, Yvette M., Owen, Dafydd R., Freskos, John N., Molyneaux, John M., Brown, David L., Acker, Brad A., Maddux, Todd M., Tollefson, Mike B., Moon, Joseph B., Mischke, Brent V., Rumsey, Jeanne M., Zheng, Yi, MacInnes, Alan, Bond, Brian R., Yu, Ying
Published in Bioorganic & medicinal chemistry letters (01.09.2009)
Published in Bioorganic & medicinal chemistry letters (01.09.2009)
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Discovery of INCB8761/PF-4136309, a Potent, Selective, and Orally Bioavailable CCR2 Antagonist
Xue, Chu-Biao, Wang, Anlai, Han, Qi, Zhang, Yingxin, Cao, Ganfeng, Feng, Hao, Huang, Taisheng, Zheng, Changsheng, Xia, Michael, Zhang, Ke, Kong, Lingquan, Glenn, Joseph, Anand, Rajan, Meloni, David, Robinson, D. J, Shao, Lixin, Storace, Lou, Li, Mei, Hughes, Robert O, Devraj, Rajesh, Morton, Philip A, Rogier, D. Joseph, Covington, Maryanne, Scherle, Peggy, Diamond, Sharon, Emm, Tom, Yeleswaram, Swamy, Contel, Nancy, Vaddi, Kris, Newton, Robert, Hollis, Greg, Metcalf, Brian
Published in ACS medicinal chemistry letters (08.12.2011)
Published in ACS medicinal chemistry letters (08.12.2011)
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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, Robert O, Rogier, D. Joseph, Jacobsen, E. Jon, Walker, John K, MacInnes, Alan, Bond, Brian R, Zhang, Lena L, Yu, Ying, Zheng, Yi, Rumsey, Jeanne M, Walgren, Jennie L, Curtiss, Sandra W, Fobian, Yvette M, Heasley, Steven E, Cubbage, Jerry W, Moon, Joseph B, Brown, David L, Acker, Brad A, Maddux, Todd M, Tollefson, Mike B, Mischke, Brent V, Owen, Dafydd R, Freskos, John N, Molyneaux, John M, Benson, Alan G, Blevis-Bal, Rhadika M
Published in Journal of medicinal chemistry (25.03.2010)
Published in Journal of medicinal chemistry (25.03.2010)
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Investigation of aminopyridiopyrazinones as PDE5 inhibitors: Evaluation of modifications to the central ring system
Hughes, Robert O., Walker, John K., Cubbage, Jerry W., Fobian, Yvette M., Rogier, D. Joseph, Heasley, Steve E., Blevis-Bal, Rhadika M., Benson, Alan G., Owen, Dafydd R., Jacobsen, E. Jon, Freskos, John N., Molyneaux, John M., Brown, David L., Stallings, William C., Acker, Brad A., Maddux, Todd M., Tollefson, Mike B., Williams, Jennifer M., Moon, Joseph B., Mischke, Brent V., Rumsey, Jeanne M., Zheng, Yi, MacInnes, Alan, Bond, Brian R., Yu, Ying
Published in Bioorganic & medicinal chemistry letters (01.08.2009)
Published in Bioorganic & medicinal chemistry letters (01.08.2009)
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Journal Article
4,5-Diaryloxazole inhibitors of cyclooxygenase-2 (COX-2)
Talley, John J., Bertenshaw, Stephen R., Brown, David L., Carter, Jeffery S., Graneto, Mathew J., Koboldt, Carol M., Masferrer, Jaime L., Norman, Bryan H., Rogier Jr, D. Joseph, Zweifel, Ben S., Seibert, Karen
Published in Medicinal research reviews (01.05.1999)
Published in Medicinal research reviews (01.05.1999)
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Journal Article
Pyridine [3,4-b] pyrazinones
Hughes, Robert O, Bell, Andrew Simon, Brown, David Graham, Owen, Dafydd, Palmer, Michael John, Phillips, Christopher, Brown, David L, Fobian, Yvette M, Freskos, John N, Heasley, Steven E, Jacobsen, E. Jon, Maddux, Todd, Mischke, Brent, Molyneaux, John M, Moon, Joseph B, Rogier, Jr, D. Joseph, Tollefson, Michael B, Walker, John K
Year of Publication 08.03.2011
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Year of Publication 08.03.2011
Patent
Pyridine [3,4-b] pyrazinones
MOLYNEAUX JOHN M, FOBIAN YVETTE M, MOON JOSEPH B, HUGHES ROBERT O, BELL ANDREW SIMON, PHILLIPS CHRISTOPHER, BROWN DAVID L, JACOBSEN E. JON, WALKER JOHN K, HEASLEY STEVEN E, PALMER MICHAEL JOHN, MADDUX TODD, MISCHKE BRENT, OWEN DAFYDD, FRESKOS JOHN N, BROWN DAVID GRAHAM, ROGIER, JR. D. JOSEPH, TOLLEFSON MICHAEL B
Year of Publication 08.03.2011
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Year of Publication 08.03.2011
Patent