Zobrazeno 1 - 10
of 17
pro vyhledávání: '"D Joseph, Rogier"'
Autor:
Daniel P. Walker, D. Joseph Rogier
Publikováno v:
Synthesis. 45:2966-2970
Thiomorpholine and thiomorpholine 1,1-dioxide are important building blocks in medicinal chemistry research, and some analogues containing these moieties have entered human clinical trials. Analogues containing bridged bicyclic thiomorpholines have a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::1dcd1a13fff6bdd92c0566f5f052b564
https://doi.org/10.1055/s-0033-1338528
https://doi.org/10.1055/s-0033-1338528
Autor:
Brian R. Bond, D. Joseph Rogier, Yi Zheng, Maddux Todd Michael, Sharon Lu, Alan MacInnes, Jeanne M. Rumsey, John K. Walker, E. Jon Jacobsen, Robert Hughes, Seungil Han
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:6348-6352
We describe the design, synthesis and profiling of a novel series of PDE5 inhibitors. We take advantage of an alternate projection into the solvent region to identify compounds with excellent potency, selectivity and pharmacokinetic profiles.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5fa3656b2c0c95aea695fd40890798ca
https://doi.org/10.1016/j.bmcl.2011.08.106
https://doi.org/10.1016/j.bmcl.2011.08.106
Autor:
Brian Metcalf, Sharon Diamond, Taisheng Huang, Lixin Shao, Swamy Yeleswaram, D. Joseph Rogier, Greg Hollis, Michael Xia, Ke Zhang, Ganfeng Cao, Nancy Contel, Lingquan Kong, Peggy Scherle, Maryanne Covington, Tom Emm, Robert Hughes, Joseph Glenn, Robert C. Newton, Kris Vaddi, Changsheng Zheng, Lou Storace, Chu-Biao Xue, Rajan Anand, Hao Feng, Meloni David, Anlai Wang, Mei Li, Philip A. Morton, Robinson Darius J, Qi Han, Rajesh V. Devraj, Yingxin Zhang
Publikováno v:
ACS Medicinal Chemistry Letters. 2:913-918
We report the discovery of a new (S)-3-aminopyrrolidine series of CCR2 antagonists. Structure-activity relationship studies on this new series led to the identification of 17 (INCB8761/PF-4136309) that exhibited potent CCR2 antagonistic activity, hig
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3d2a792b5ba70daa3c854d4e609b3ad5
https://doi.org/10.1021/ml200199c
https://doi.org/10.1021/ml200199c
Autor:
Sandra W. Curtiss, D. Joseph Rogier, Alan MacInnes, Brown David L, Mike B. Tollefson, Brian R. Bond, Yvette M. Fobian, Maddux Todd Michael, Dafydd R. Owen, Jeanne M. Rumsey, Brent V. Mischke, Jerry W. Cubbage, Alan G. Benson, Robert Hughes, Lena L Zhang, E. Jon Jacobsen, Steven E. Heasley, Joseph B. Moon, Ying Yu, John M. Molyneaux, Yi Zheng, Brad A. Acker, Blevis-Bal Radhika M, John N. Freskos, John K. Walker, Jennie L. Walgren
Publikováno v:
Journal of Medicinal Chemistry. 53:2656-2660
We recently described a novel series of aminopyridopyrazinones as PDE5 inhibitors. Efforts toward optimization of this series culminated in the identification of 3-[4-(2-hydroxyethyl)piperazin-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::892c7788c8aa398973abd4f8bb5a78a5
https://doi.org/10.1021/jm901781q
https://doi.org/10.1021/jm901781q
Autor:
Maddux Todd Michael, Yvette M. Fobian, Alan G. Benson, Dafydd R. Owen, Brian R. Bond, Christopher Phillips, Brad A. Acker, E. Jon Jacobsen, Michael John Palmer, D. Joseph Rogier, John M. Molyneaux, Brent V. Mischke, John N. Freskos, Tracy J. Ringer, Andrew Simon Bell, Blevis-Bal Radhika M, Robert Hughes, David G. Brown, Steve E. Heasley, Joseph B. Moon, John K. Walker, Brown David L, William C. Stallings, Michael B. Tollefson, Alan MacInnes, Jerry W. Cubbage, Yung Yu, Margarita Rodriquez-Lens, Fox David Nathan Abraham
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:4088-4091
A new class of potent and selective PDE5 inhibitors is disclosed. Guided by X-ray crystallographic data, optimization of an HTS lead led to the discovery of a series of 2-aryl, (N8)-alkyl substituted-6-aminosubstituted pyrido[3,2b]pyrazinones which s
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5005db6742e606fdadbf520ea66a63a9
https://doi.org/10.1016/j.bmcl.2009.06.012
https://doi.org/10.1016/j.bmcl.2009.06.012
Autor:
Daniel P. Walker, D. Joseph Rogier
Publikováno v:
ChemInform. 45
Thiomorpholine and thiomorpholine 1,1-dioxide are important building blocks in medicinal chemistry research, and some analogues containing these moieties have entered human clinical trials. Analogues containing bridged bicyclic thiomorpholines have a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::3ad148e7e49392e56589db4f7a64a924
https://doi.org/10.1002/chin.201413187
https://doi.org/10.1002/chin.201413187
Autor:
Jeffery S. Carter, John J. Talley, Karen Seibert, Stephen R. Bertenshaw, D. Joseph Rogier, Carol M. Koboldt, Graneto Matthew J, David L. Brown, Ben S. Zweifel, Jaime L. Masferrer, Bryan H. Norman
Publikováno v:
Medicinal Research Reviews. 19:199-208
A series of methysulfonyl or sulfonamido substituted 4,5-diaryloxazole were prepared and evaluated for their ability to inhibit the inducible form of cyclooxygenase (COX-2) in vitro and in vivo. Several unique substitution patterns were identified th
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::efe6962fa7e482f1968255b75b942a14
https://doi.org/10.1002/(sici)1098-1128(199905)19:3<199::aid-med1>3.0.co
https://doi.org/10.1002/(sici)1098-1128(199905)19:3<199::aid-med1>3.0.co
Autor:
Philip A. Morton, D. Joseph Rogier, Ganfeng Chao, Brian Metcalf, Robert Hughes, Rajesh V. Devraj, Wei Huang, Maryanne Covington, Robert C. Newton, Turner Steven R, John I. Trujillo, Chu-Biao Xue
Publikováno v:
Bioorganicmedicinal chemistry letters. 21(6)
This report describes the design and synthesis of a series of CCR2 antagonists incorporating novel non-aryl/heteroaryl RHS (right hand side) motifs. Previous SAR in the area has suggested an aryl/heteroaryl substituent as a necessary structural featu
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bb32aaf54ef29dcf73b8bd08df7acc33
https://pubmed.ncbi.nlm.nih.gov/21316220
https://pubmed.ncbi.nlm.nih.gov/21316220
Autor:
Anlai Wang, Kris Vaddi, Robert Hughes, Sharon Diamond, Mei Li, Steven Friedman, D. Joseph Rogier, Greg Hollis, Joseph Glenn, Phillip A. Morton, Changsheng Zheng, Niu Shin, Ke Zhang, Ganfeng Cao, Peggy Scherle, Swamy Yeleswaram, Hao Feng, Taisheng Huang, Rajan Anand, Ling Kong, Brian Metcalf, Fred Baribaud, Rajesh V. Devraj, Laurine G. Galya, Maryanne Covington, Robert C. Newton, Chu-Biao Xue, Michael Xia
Publikováno v:
Bioorganicmedicinal chemistry letters. 21(5)
We report the discovery of a potent, selective, and orally bioavailable dual CCR2 and CCR5 antagonist (3S,4S)-N-[(1R,3S)-3-isopropyl-3-({4-[4-(trifluoromethyl)pyridin-2-yl]piperazin-1-yl}carbonyl)cyclopentyl]-3-methoxytetrahydro-2H-pyran-4-amine (19)
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8748c7ed89a54cd646a78460c292b1a0
https://pubmed.ncbi.nlm.nih.gov/21295478
https://pubmed.ncbi.nlm.nih.gov/21295478
Autor:
Robert O, Hughes, D Joseph, Rogier, E Jon, Jacobsen, John K, Walker, Alan, Macinnes, Brian R, Bond, Lena L, Zhang, Ying, Yu, Yi, Zheng, Jeanne M, Rumsey, Jennie L, Walgren, Sandra W, Curtiss, Yvette M, Fobian, Steven E, Heasley, Jerry W, Cubbage, Joseph B, Moon, David L, Brown, Brad A, Acker, Todd M, Maddux, Mike B, Tollefson, Brent V, Mischke, Dafydd R, Owen, John N, Freskos, John M, Molyneaux, Alan G, Benson, Rhadika M, Blevis-Bal
Publikováno v:
Journal of medicinal chemistry. 53(6)
We recently described a novel series of aminopyridopyrazinones as PDE5 inhibitors. Efforts toward optimization of this series culminated in the identification of 3-[4-(2-hydroxyethyl)piperazin-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::88c2de53db53a1f8525bbef66ae6a7e3
https://pubmed.ncbi.nlm.nih.gov/20196613
https://pubmed.ncbi.nlm.nih.gov/20196613