Zobrazeno 1 - 10
of 38
pro vyhledávání: '"Michael S. Dappen"'
Autor:
David F. Nakamura, Hing L. Sham, John-Michael Sauer, Dean R. Artis, Lany Ruslim, Ted Yednock, Michael A. Pleiss, Gary Probst, Marc Adler, Minghua Sun, Louis Brogley, Michael S. Dappen, Roy K. Hom, Michel Maillard, Nanhua Yao, Simeon Bowers, Andrei W. Konradi, Jay S. Tung, Raymond A. Ng, Andrea Gailunas, Wes Zmolek, Kevin P. Quinn, Fang Lawrence Y, Varghese John, R. Jeffrey Neitz, Michael P. Bova
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:4674-4679
The structure activity relationship of the prime region of conformationally restricted hydroxyethylamine (HEA) BACE inhibitors is described. Variation of the P1′ region provided selectivity over Cat-D with a series of 2,2-dioxo-isothiochromanes and
Autor:
John P. Anderson, Dean R. Artis, Hing L. Sham, Roy K. Hom, Michael S. Dappen, Andrei W. Konradi, Simeon Bowers, Hu Pan, Robert A. Galemmo, Marc Adler, Pearl Tanaka, May Lin, Jeanne Baker, Lany Ruslim, Donald J. Fauss, Zhao Ren, Yong L. Zhu, Anh P. Truong, Danny Tam, Marcelle Bergeron, Lee H. Latimer, Paul Beroza, Jacek Jagodzinski, Heather Zhang, Michael P. Bova, George Tonn, Linnea Diep, Ruth Motter, Kent Fitzgerald, Nanhua Yao, Wayman Chan, Jennifer K. Hoffman, R. Jeffrey Neitz, Danielle L. Aubele
Publikováno v:
ChemMedChem. 8:1295-1313
Polo-like kinase-2 (Plk-2) has been implicated as the dominant kinase involved in the phosphorylation of α-synuclein in Lewy bodies, which are one of the hallmarks of Parkinson's disease neuropathology. Potent, selective, brain-penetrant inhibitors
Autor:
Anna Liao, Gary Probst, Pamela S. Keim, Kang Hu, Roy K. Hom, David A. Quincy, Michael S. Dappen, Grace T. Kwong, Jenifer Smith, Martin L. Neitzel, Ying-zi Xu, Elizabeth F. Brigham, Kevin P. Quinn, Frédérique Bard, Minghua Sun, Jing Wu, John-Michael Sauer, Dora Kholodenko, Hongbin Zhang, William Wallace, Matthew N. Mattson, Patricia Sacayon, Jacek Jagodzinski, Hing L. Sham, Brian T. Peterson, Simeon Bowers, Jennifer Marugg, Guriqbal S. Basi, Lee H. Latimer, Susanna S. Hemphill, Darren B. Dressen, Karina Wong, Kevin Tanaka, Michael P. Bova, Pamela Santiago, Daniel K. Ness, Anh P. Truong, Wes Zmolek, Lany Ruslim, Christopher Willits, Michael K. Lee, Andrei W. Konradi, Xiaocong M. Ye, Lam Nguyen, Chris M. Semko, Ted A. Yednock, Ruth N. Motter, Albert W. Garofalo, Erich Goldbach, Pearl Tanaka, Danielle L. Aubele
Publikováno v:
Journal of Medicinal Chemistry. 56:5261-5274
Herein, we describe our strategy to design metabolically stable γ-secretase inhibitors which are selective for inhibition of Aβ generation over Notch. We highlight our synthetic strategy to incorporate diversity and chirality. Compounds 30 (ELND006
Autor:
Jennifer S. Smith, Michael A. Pleiss, Caroline Garrido, Ying-Zi Xu, Frank Stappenbeck, Elizabeth Messersmith, Frederique Bard, Bhushan Samant, Linda Mutter, Semko Christopher M, Brent Welch, Brian P. Stupi, Chris Vandervert, Mark Dreyer, Zhenmei Liao, Mike Krimm, Brian Wipke, Ian Gallager, Ted Yednock, Michael S. Dappen, Andrei W. Konradi, Lilibeth Dofiles
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:3070-3074
A series of (S)-2-(2-(diethylamino)-5-(N-alkyl-N-sulfonamido)pyrimidin-4-ylamino)-3-(4-(carbamoyloxy)phenyl)propanoic acid is discovered as orally available VLA-4 antagonists. Representative compounds 11b and 11p showed efficacy in multiple in vivo a
Autor:
Gergley Tóth, Hu Pan, Gary Probst, John-Michael Sauer, Dean R. Artis, Anh P. Truong, Michael P. Bova, Wes Zmolek, Ted Yednock, Jose Aquino, Michael S. Dappen, Kevin P. Quinn, Sukanto Sinha, Varghese John, Hing L. Sham, Michael A. Pleiss, Roy K. Hom, Lany Ruslim, Louis Brogley, Jennifer Sealy, Nanhua Yao, Larry Fang, Jay S. Tung, John A. Tucker, Eric Brecht, Andrei W. Konradi
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:4789-4794
Herein we describe further evolution of hydroxyethylamine inhibitors of BACE-1 with enhanced permeability characteristics necessary for CNS penetration. Variation at the P2' position of the inhibitor with more polar substituents led to compounds 19 a
Autor:
Gary, Probst, Danielle L, Aubele, Simeon, Bowers, Darren, Dressen, Albert W, Garofalo, Roy K, Hom, Andrei W, Konradi, Jennifer L, Marugg, Matthew N, Mattson, Martin L, Neitzel, Chris M, Semko, Hing L, Sham, Jenifer, Smith, Minghua, Sun, Anh P, Truong, Xiaocong M, Ye, Ying-Zi, Xu, Michael S, Dappen, Jacek J, Jagodzinski, Pamela S, Keim, Brian, Peterson, Lee H, Latimer, David, Quincy, Jing, Wu, Erich, Goldbach, Daniel K, Ness, Kevin P, Quinn, John-Michael, Sauer, Karina, Wong, Hongbin, Zhang, Wes, Zmolek, Elizabeth F, Brigham, Dora, Kholodenko, Kang, Hu, Grace T, Kwong, Michael, Lee, Anna, Liao, Ruth N, Motter, Patricia, Sacayon, Pamela, Santiago, Christopher, Willits, Frédérique, Bard, Michael P, Bova, Susanna S, Hemphill, Lam, Nguyen, Lany, Ruslim, Kevin, Tanaka, Pearl, Tanaka, William, Wallace, Ted A, Yednock, Guriqbal S, Basi
Publikováno v:
Journal of medicinal chemistry. 56(13)
Herein, we describe our strategy to design metabolically stable γ-secretase inhibitors which are selective for inhibition of Aβ generation over Notch. We highlight our synthetic strategy to incorporate diversity and chirality. Compounds 30 (ELND006
Autor:
Angie Wadsworth, Wenxian Mao, Stellanie Simmonds, Eric Peterson, Christopher Vandevert, F. Bong San Pablo, Ted Yednock, Ying-Zi Xu, David A. Quincy, Carlos Lorenzana, Andrei W. Konradi, Kassandra Inez Rossiter, Michael S. Dappen, Michael A. Pleiss, Frederique Bard, Elizabeth Messersmith, Brian Wipke, Caroline Garrido, Jenifer L. Smith, Christopher M. Semko, Jacek Jagodzinski, Lilibeth Dofiles
Publikováno v:
Bioorganicmedicinal chemistry letters. 23(14)
Mitsunobu reactions were employed to link t-butyl esters of α4 integrin inhibitors at each of the termini of a three-arm, 40 kDa, branched PEG. Cleavage of the t-butyl esters using HCO2H provided easily isolated PEG derivatives, which are potent α4
Autor:
Bhushan Samant, Mark Shoemaker, Michael Krimm, Elizabeth Messersmith, Brent Welch, John-Michael Sauer, Linda Chen, Michael S. Dappen, Wenxian Mao, Zhenmei Liao, Ted Yednock, Jenifer L. Smith, Carrol Henschel, Nancy G. Wehner, Lilibeth Dofiles, Ian Gallager, Linda Mutter, Michael A. Pleiss, Mark Dreyer, David A. Quincy, Andrei W. Konradi, Hongbin Zhang, Christopher M. Semko, Kassandra Inez Rossiter, Eric Petersen, George Shopp, Juri Y Fukuda, Brian Wipke, Christopher Vandevert, Frederique Bard, Judevin Lugar, Ying-Zi Xu
Publikováno v:
Bioorganicmedicinal chemistry letters. 23(15)
A series of potent α4β1/α4β7 integrin inhibitors is reported, including an inhibitor 12d with remarkable oral exposure and efficacy in rat models of rheumatoid arthritis and Crohn's disease.
Autor:
Paul Beroza, Michael P. Bova, Jennifer K. Hoffman, Jennifer Sealy, Heather Zhang, Marcelle Bergeron, Linnea Diep, Danny Tam, Ruth Motter, Zhao Ren, R. Jeffrey Neitz, Danielle L. Aubele, Kent Fitzgerald, Michael Ye, Wayman Chan, Pearl Tanaka, Deepal Pandya, Donald J. Fauss, Andrei W. Konradi, John P. Anderson, Roy K. Hom, Dean R. Artis, Hing L. Sham, Robert A. Galemmo, George Tonn, Jeanne Baker, Lany Ruslim, Yong L. Zhu, Anh P. Truong, Michael S. Dappen, Simeon Bowers
Publikováno v:
Bioorganicmedicinal chemistry letters. 23(9)
Polo-like kinase-2 (Plk-2) is a potential therapeutic target for Parkinson’s disease and this Letter describes the SAR of a series of dihydropteridinone based Plk-2 inhibitors. By optimizing both the N-8 substituent and the biaryl region of the inh
Autor:
Tadimeti S. Rao, Paul L. Wood, Alexis A. Cordi, Nancy M. Gray, Michael S. Dappen, M.R. Emmett, S. Iyengar, Joseph B. Monahan, Julie A. Cler, S.J. Mick
Publikováno v:
Neuropharmacology. 32:139-147
Recent in vitro receptor binding studies have indicated that indole-2-carboxylates with halogen substitutions at the position 5 or 6 are potent competitive antagonists of the NMDA (N- methyl- D -aspartate ) -associated strychnine-insensitive glycine