Discovery and Preclinical Profile of Saxagliptin (BMS-477118): A Highly Potent, Long-Acting, Orally Active Dipeptidyl Peptidase IV Inhibitor for the Treatment of Type 2 Diabetes
Augeri, David J, Robl, Jeffrey A, Betebenner, David A, Magnin, David R, Khanna, Ashish, Robertson, James G, Wang, Aiying, Simpkins, Ligaya M, Taunk, Prakash, Huang, Qi, Han, Song-Ping, Abboa-Offei, Benoni, Cap, Michael, Xin, Li, Tao, Li, Tozzo, Effie, Welzel, Gustav E, Egan, Donald M, Marcinkeviciene, Jovita, Chang, Shu Y, Biller, Scott A, Kirby, Mark S, Parker, Rex A, Hamann, Lawrence G
Published in Journal of medicinal chemistry (28.07.2005)
Published in Journal of medicinal chemistry (28.07.2005)
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Potent and selective biphenyl azole inhibitors of adipocyte fatty acid binding protein (aFABP)
Sulsky, Richard, Magnin, David R., Huang, Yanting, Simpkins, Ligaya, Taunk, Prakash, Patel, Manorama, Zhu, Yeheng, Stouch, Terry R., Bassolino-Klimas, Donna, Parker, Rex, Harrity, Thomas, Stoffel, Robert, Taylor, David S., Lavoie, Thomas B., Kish, Kevin, Jacobson, Bruce L., Sheriff, Steven, Adam, Leonard P., Ewing, William R., Robl, Jeffrey A.
Published in Bioorganic & medicinal chemistry letters (15.06.2007)
Published in Bioorganic & medicinal chemistry letters (15.06.2007)
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Journal Article
A Novel Series of Highly Potent Benzimidazole-Based Microsomal Triglyceride Transfer Protein Inhibitors
Robl, Jeffrey A, Sulsky, Richard, Sun, Chong-Qing, Simpkins, Ligaya M, Wang, Tammy, Dickson, John K, Chen, Ying, Magnin, David R, Taunk, Prakash, Slusarchyk, William A, Biller, Scott A, Lan, Shih-Jung, Connolly, Fergal, Kunselman, Lori K, Sabrah, Talal, Jamil, Haris, Gordon, David, Harrity, Thomas W, Wetterau, John R
Published in Journal of medicinal chemistry (15.03.2001)
Published in Journal of medicinal chemistry (15.03.2001)
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Journal Article
Synthesis of Novel Potent Dipeptidyl Peptidase IV Inhibitors with Enhanced Chemical Stability: Interplay between the N-Terminal Amino Acid Alkyl Side Chain and the Cyclopropyl Group of α-Aminoacyl-l-cis-4,5-methanoprolinenitrile-Based Inhibitors
Magnin, David R, Robl, Jeffrey A, Sulsky, Richard B, Augeri, David J, Huang, Yanting, Simpkins, Ligaya M, Taunk, Prakash C, Betebenner, David A, Robertson, James G, Abboa-Offei, Benoni E, Wang, Aiying, Cap, Michael, Xin, Li, Tao, Li, Sitkoff, Doree F, Malley, Mary F, Gougoutas, Jack Z, Khanna, Ashish, Huang, Qi, Han, Song-Ping, Parker, Rex A, Hamann, Lawrence G
Published in Journal of medicinal chemistry (06.05.2004)
Published in Journal of medicinal chemistry (06.05.2004)
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Journal Article
Regioselectivity and diastereoselectivity in free-radical macrocyclization
Porter, Ned A, Lacher, Brigitte, Chang, Vincent H. T, Magnin, David R
Published in Journal of the American Chemical Society (01.10.1989)
Published in Journal of the American Chemical Society (01.10.1989)
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Journal Article
Potent non-nitrile dipeptidic dipeptidyl peptidase IV inhibitors
Simpkins, Ligaya M., Bolton, Scott, Pi, Zulan, Sutton, James C., Kwon, Chet, Zhao, Guohua, Magnin, David R., Augeri, David J., Gungor, Timur, Rotella, David P., Sun, Zhong, Liu, Yajun, Slusarchyk, William S., Marcinkeviciene, Jovita, Robertson, James G., Wang, Aiying, Robl, Jeffrey A., Atwal, Karnail S., Zahler, Robert L., Parker, Rex A., Kirby, Mark S., Hamann, Lawrence G.
Published in Bioorganic & medicinal chemistry (01.12.2007)
Published in Bioorganic & medicinal chemistry (01.12.2007)
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Journal Article
Diprolyl nitriles as potent dipeptidyl peptidase IV inhibitors
Zhao, Guohua, Taunk, Prakash C., Magnin, David R., Simpkins, Ligaya M., Robl, Jeffrey A., Wang, Aiying, Robertson, James G., Marcinkeviciene, Jovita, Sitkoff, Doree F., Parker, Rex A., Kirby, Mark S., Hamann, Lawrence G.
Published in Bioorganic & medicinal chemistry letters (15.09.2005)
Published in Bioorganic & medicinal chemistry letters (15.09.2005)
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Journal Article
NMR Structure of a Potent Small Molecule Inhibitor Bound to Human Keratinocyte Fatty Acid-Binding Protein
McDonnell, Patricia A, Constantine, Keith L, Goldfarb, Valentina, Johnson, Stephen R, Sulsky, Richard, Magnin, David R, Robl, Jeffrey A, Caulfield, Thomas J, Parker, Rex A, Taylor, David S, Adam, Leonard P, Metzler, William J, Mueller, Luciano, Farmer, Bennett T
Published in Journal of medicinal chemistry (10.08.2006)
Published in Journal of medicinal chemistry (10.08.2006)
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Journal Article
Seco-prolinenitrile inhibitors of dipeptidyl peptidase IV define minimal pharmacophore requirements at P1
Magnin, David R., Taunk, Prakash C., Robertson, James G., Wang, Aiying, Marcinkeviciene, Jovita, Kirby, Mark S., Hamann, Lawrence G.
Published in Bioorganic & medicinal chemistry letters (15.03.2006)
Published in Bioorganic & medicinal chemistry letters (15.03.2006)
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Journal Article
Application of robotics to steady state enzyme kinetics: analysis of tight-binding inhibitors of dipeptidyl peptidase IV
Wang, Aiying, Huang, Yanting, Taunk, Prakash, Magnin, David R, Ghosh, Krishnendu, Robertson, James G
Published in Analytical biochemistry (15.10.2003)
Published in Analytical biochemistry (15.10.2003)
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Journal Article
Microsomal triglyceride transfer protein inhibitors: discovery and synthesis of alkyl phosphonates as potent MTP inhibitors and cholesterol lowering agents
Magnin, David R, Biller, Scott A, Wetterau, John, Robl, Jeffrey A, Dickson, John K, Taunk, Prakash, Harrity, Thomas W, Lawrence, R.Michael, Sun, C.-Q, Wang, Tammy, Logan, Janette, Fryszman, Olga, Connolly, Fergal, Jolibois, Kern, Kunselman, Lori
Published in Bioorganic & medicinal chemistry letters (07.04.2003)
Published in Bioorganic & medicinal chemistry letters (07.04.2003)
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Journal Article
Orally Active Squalene Synthase Inhibitors: Bis((acyloxy)alkyl) Prodrugs of the α-Phosphonosulfonic Acid Moiety
Dickson, John K, Biller, Scott A, Magnin, David R, Petrillo, Edward W, Hillyer, John W, Hsieh, Dolly C, Lan, Shih-Jung, Rinehart, J. Kent, Gregg, Richard E, Harrity, Thomas W, Jolibois, Kern G, Kalinowski, Stephen S, Kunselman, Lori K, Mookhtiar, Kasim A, Ciosek, Carl P
Published in Journal of medicinal chemistry (02.02.1996)
Published in Journal of medicinal chemistry (02.02.1996)
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Journal Article
Enantioselective Synthesis of α-Phosphono Sulfonate Squalene Synthase Inhibitors: Chiral Recognition in the Interactions of an α-Phosphono Sulfonate Inhibitor with Squalene Synthase
Lawrence, R. Michael, Biller, Scott A, Dickson, John K, Logan, Janette V. H, Magnin, David R, Sulsky, Richard B, DiMarco, John D, Gougoutas, Jack Z, Beyer, Barbara D, Taylor, Susan C, Lan, Shih-Jung, Ciosek, Carl P, Harrity, Thomas W, Jolibois, Kern G, Kunselman, Lori K, Slusarchyk, Dorothy A
Published in Journal of the American Chemical Society (20.11.1996)
Published in Journal of the American Chemical Society (20.11.1996)
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Journal Article
α-Phosphonosulfonic Acids: Potent and Selective Inhibitors of Squalene Synthase
Magnin, David R, Biller, Scott A, Chen, Ying, Dickson, John K, Fryszman, Olga M, Lawrence, R. Michael, Logan, Janette V. H, Sieber-McMaster, Ellen S, Sulsky, Richard B, Traeger, Sarah C, Hsieh, Dolly C, Lan, Shih-Jung, Rinehart, J. Kent, Harrity, Thomas W, Jolibois, Kern G, Kunselman, Lori K, Rich, Lois C, Slusarchyk, Dorothy A, Ciosek, Carl P
Published in Journal of medicinal chemistry (02.02.1996)
Published in Journal of medicinal chemistry (02.02.1996)
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Journal Article
1,1-Bisphosphonate Squalene Synthase Inhibitors: Interplay Between the Isoprenoid Subunit and the Diphosphate Surrogate
Magnin, David R, Dickson, John K, Logan, Janette V, Lawrence, R. Michael, Chen, Ying, Sulsky, Richard B, Ciosek, Carl P, Biller, Scott A, Harrity, Thomas W, Jolibois, Kern G, Kunselman, Lori K, Rich, Lois C, Slusarchyk, Dorothy A
Published in Journal of medicinal chemistry (01.07.1995)
Published in Journal of medicinal chemistry (01.07.1995)
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Journal Article
Free-radical macrocyclization-transannular cyclization
Porter, Ned A, Chang, Vincent H. T, Magnin, David R, Wright, Bruce T
Published in Journal of the American Chemical Society (01.05.1988)
Published in Journal of the American Chemical Society (01.05.1988)
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Journal Article
Free radical macrocyclization
Porter, Ned A, Magnin, David R, Wright, Bruce T
Published in Journal of the American Chemical Society (01.05.1986)
Published in Journal of the American Chemical Society (01.05.1986)
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Journal Article
An MTP Inhibitor that Normalizes Atherogenic Lipoprotein Levels in WHHL Rabbits
Wetterau, John R., Gregg, Richard E., Harrity, Thomas W., Arbeeny, Cynthia, Cap, Michael, Connolly, Fergal, Chu, Ching-Hsuen, George, Rocco J., Gordon, David A., Jamil, Haris, Jolibois, Kern G., Kunselman, Lori K., Lan, Shih-Jung, Maccagnan, Thomas J., Ricci, Beverly, Yan, Mujing, Young, Douglas, Chen, Ying, Fryszman, Olga M., Janette V. H. Logan, Musial, Christa L., Poss, Michael A., Robl, Jeffrey A., Simpkins, Ligaya M., Slusarchyk, William A., Sulsky, Richard, Taunk, Prakash, Magnin, David R., Tino, Joseph A., Lawrence, R. Michael, Dickson, John K., Biller, Scott A.
Published in Science (American Association for the Advancement of Science) (23.10.1998)
Published in Science (American Association for the Advancement of Science) (23.10.1998)
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