Search Results - "Sulsky, Richard"

Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2 by Makowski, Liza, Hotamisligil, Gökhan S, Tuncman, Gürol, Görgün, Cem Z, Fazio, Sergio, Parker, Rex A, Kono, Keita, Robl, Jeffrey A, Atsumi, Genichi, Sulsky, Richard, Babaev, Vladimir R, Furuhashi, Masato, Linton, MacRae F, Vaillancourt, Eric

“…Adipocyte fatty-acid-binding protein, aP2 (FABP4) is expressed in adipocytes and macrophages, and integrates inflammatory and metabolic responses. Studies in…”
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Potent and selective biphenyl azole inhibitors of adipocyte fatty acid binding protein (aFABP) by 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.

“…X-ray crystal structure of an FABP inhibitor bound to the active site of aFABP. Herein we report the first disclosure of biphenyl azoles that are nanomolar…”
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Reductions in log P Improved Protein Binding and Clearance Predictions Enabling the Prospective Design of Cannabinoid Receptor (CB1) Antagonists with Desired Pharmacokinetic Properties by Ellsworth, Bruce A, Sher, Philip M, Wu, Ximao, Wu, Gang, Sulsky, Richard B, Gu, Zhengxiang, Murugesan, Natesan, Zhu, Yeheng, Yu, Guixue, Sitkoff, Doree F, Carlson, Kenneth E, Kang, Liya, Yang, Yifan, Lee, Ning, Baska, Rose A, Keim, William J, Cullen, Mary Jane, Azzara, Anthony V, Zuvich, Eva, Thomas, Michael A, Rohrbach, Kenneth W, Devenny, James J, Godonis, Helen E, Harvey, Susan J, Murphy, Brian J, Everlof, Gerry G, Stetsko, Paul I, Gudmundsson, Olafur, Johnghar, Susan, Ranasinghe, Asoka, Behnia, Kamelia, Pelleymounter, Mary Ann, Ewing, William R

“…Several strategies have been employed to reduce the long in vivo half-life of our lead CB1 antagonist, triazolopyridazinone 3, to differentiate the…”
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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 by 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

“…A series of methanoprolinenitrile-containing dipeptide mimetics were synthesized and assayed as inhibitors of the N-terminal sequence-specific serine protease…”
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A Novel Series of Highly Potent Benzimidazole-Based Microsomal Triglyceride Transfer Protein Inhibitors by 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

“…A series of benzimidazole-based analogues of the potent MTP inhibitor BMS-201038 were discovered. Incorporation of an unsubstituted benzimidazole moiety in…”
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Conformational Switching and the Synthesis of Spiro[2H-indol]-3(1H)-ones by Radical Cyclization by Sulsky, Richard, Gougoutas, Jack Z, DiMarco, John, Biller, Scott A

“…Radical cyclization of 1-(2-bromophenylamino)cyclohexanecarbonitriles (3, X = CH) and 4-(2-bromophenylamino)-4-piperidinecarbonitriles (3, X = N) provide…”
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Enantioselective Synthesis of α-Phosphono Sulfonate Squalene Synthase Inhibitors:  Chiral Recognition in the Interactions of an α-Phosphono Sulfonate Inhibitor with Squalene Synthase by 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

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Discovery of a Partial Glucokinase Activator Clinical Candidate: Diethyl ((3-(3-((5-(Azetidine-1-carbonyl)pyrazin-2-yl)oxy)-5-isopropoxybenzamido)-1 H -pyrazol-1-yl)methyl)phosphonate (BMS-820132) by Shi, Yan, Wang, Ying, Meng, Wei, Brigance, Robert P, Ryono, Denis E, Bolton, Scott, Zhang, Hao, Chen, Sean, Smirk, Rebecca, Tao, Shiwei, Tino, Joseph A, Williams, Kristin N, Sulsky, Richard, Nielsen, Laura, Ellsworth, Bruce, Wong, Michael K Y, Sun, Jung-Hui, Leith, Leslie W, Sun, Dawn, Wu, Dauh-Rurng, Gupta, Anuradha, Rampulla, Richard, Mathur, Arvind, Chen, Bang-Chi, Wang, Aiying, Fuentes-Catanio, Helen G, Kunselman, Lori, Cap, Michael, Zalaznick, Jacob, Ma, Xiaohui, Liu, Heng, Taylor, Joseph R, Zebo, Rachel, Jones, Beverly, Kalinowski, Stephen, Swartz, Joann, Staal, Ada, O'Malley, Kevin, Kopcho, Lisa, Muckelbauer, Jodi K, Krystek, Jr, Stanley R, Spronk, Steven A, Marcinkeviciene, Jovita, Everlof, Gerry, Chen, Xue-Qing, Xu, Carrie, Li, Yi-Xin, Langish, Robert A, Yang, Yanou, Wang, Qi, Behnia, Kamelia, Fura, Aberra, Janovitz, Evan B, Pannacciulli, Nicola, Griffen, Steven, Zinker, Bradley A, Krupinski, John, Kirby, Mark, Whaley, Jean, Zahler, Robert, Barrish, Joel C, Robl, Jeffrey A, Cheng, Peter T W

“…Glucokinase (GK) is a key regulator of glucose homeostasis, and its small-molecule activators represent a promising opportunity for the treatment of type 2…”
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Discovery of a Partial Glucokinase Activator Clinical Candidate: Diethyl ((3-(3-((5-(Azetidine-1-carbonyl)pyrazin-2-yl)oxy)-5-isopropoxybenzamido)‑1H‑pyrazol-1-yl)methyl)phosphonate (BMS-820132) by Shi, Yan, Wang, Ying, Meng, Wei, Brigance, Robert P, Ryono, Denis E, Bolton, Scott, Zhang, Hao, Chen, Sean, Smirk, Rebecca, Tao, Shiwei, Tino, Joseph A, Williams, Kristin N, Sulsky, Richard, Nielsen, Laura, Ellsworth, Bruce, Wong, Michael K. Y, Sun, Jung-Hui, Leith, Leslie W, Sun, Dawn, Wu, Dauh-Rurng, Gupta, Anuradha, Rampulla, Richard, Mathur, Arvind, Chen, Bang-Chi, Wang, Aiying, Fuentes-Catanio, Helen G, Kunselman, Lori, Cap, Michael, Zalaznick, Jacob, Ma, Xiaohui, Liu, Heng, Taylor, Joseph R, Zebo, Rachel, Jones, Beverly, Kalinowski, Stephen, Swartz, Joann, Staal, Ada, O’Malley, Kevin, Kopcho, Lisa, Muckelbauer, Jodi K, Krystek, Stanley R, Spronk, Steven A, Marcinkeviciene, Jovita, Everlof, Gerry, Chen, Xue-Qing, Xu, Carrie, Li, Yi-Xin, Langish, Robert A, Yang, Yanou, Wang, Qi, Behnia, Kamelia, Fura, Aberra, Janovitz, Evan B, Pannacciulli, Nicola, Griffen, Steven, Zinker, Bradley A, Krupinski, John, Kirby, Mark, Whaley, Jean, Zahler, Robert, Barrish, Joel C, Robl, Jeffrey A, Cheng, Peter T. W

“…Glucokinase (GK) is a key regulator of glucose homeostasis, and its small-molecule activators represent a promising opportunity for the treatment of type 2…”
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α-Phosphonosulfonic Acids:  Potent and Selective Inhibitors of Squalene Synthase by 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

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1,1-Bisphosphonate Squalene Synthase Inhibitors: Interplay Between the Isoprenoid Subunit and the Diphosphate Surrogate by 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

“…Inhibitors of squalene synthase have the potential to be superior cholesterol-lowering agents. We previously disclosed that lipophilic 1,1-bisphosphonates I…”
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An MTP Inhibitor that Normalizes Atherogenic Lipoprotein Levels in WHHL Rabbits by 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.

“…Patients with abetalipoproteinemia, a disease caused by defects in the microsomal triglyceride transfer protein (MTP), do not produce apolipoprotein…”
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5-Carboxamido-1,3,2-dioxaphosphorinanes, potent inhibitors of MTP by Sulsky, Richard, Robl, Jeffrey A., Biller, Scott A., Harrity, Thomas W., Wetterau, John, Connolly, Fergal, Jolibois, Kern, Kunselman, Lori

“…[Display omitted] 5-Carboxamido-1,3,2-dioxaphosphorinanes have been identified as potent inhibitors of microsomal triglyceride-transfer protein. The…”
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NMR Structure of a Potent Small Molecule Inhibitor Bound to Human Keratinocyte Fatty Acid-Binding Protein by 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

“…The NMR structure is presented for compound 1 (BMS-480404) (K i = 33 (±2) nM) bound to keratinocyte fatty acid-binding protein. This article describes…”
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Vasopeptidase Inhibitors:  Incorporation of Geminal and Spirocyclic Substituted Azepinones in Mercaptoacyl Dipeptides by Robl, Jeffrey A, Sulsky, Richard, Sieber-McMaster, Ellen, Ryono, Denis E, Cimarusti, Maria P, Simpkins, Ligaya M, Karanewsky, Donald S, Chao, Sam, Asaad, Magdi M, Seymour, Andrea A, Fox, Maxine, Smith, Patricia L, Trippodo, Nick C

“…A series of 7-(di)alkyl and spirocyclic substituted azepinones were generated and incorporated as conformationally restricted dipeptide surrogates in…”
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Lipophilic 1,1-bisphosphonates are potent squalene synthase inhibitors and orally active cholesterol lowering agents in vivo by Ciosek, C P, Magnin, D R, Harrity, T W, Logan, J V, Dickson, J K, Gordon, E M, Hamilton, K A, Jolibois, K G, Kunselman, L K, Lawrence, R M

“…Squalene synthase catalyzes the reductive dimerization of two molecules of farnesyl diphosphate to form squalene at the final branchpoint of the cholesterol…”
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Synthetic routes for the generation of 7,7-dialkyl azepin-2-ones by Robl, Jeffrey A., Sieber-McMaster, Ellen, Sulsky, Richard

“…Three diverse synthetic routes to C-7 dialkylated and spiro-alkylated azepinones are described. Compounds of this type may be used as conformationally…”
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Preparation and alkylation of 1,5‐dihydro‐3 H ‐1,2,4‐thiadiazolo[3,4‐ b ]quinazolin‐5‐one 2,2‐dioxides by Demers, James P., Sulsky, Richard, Klaubert, Dieter H.

“…Abstract 1,5‐Dihydro‐3 H ‐1,2,4‐thiadiazolo[3,4‐ b ]quinazolin‐5‐one 2,2‐dioxides ( 3 ) are prepared by reaction of isatoic anhydrides with methyl N…”
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Preparation and alkylation of 1,5-dihydro-3H-1,2,4-thiadiazolo[3,4-b]quinazolin-5-one 2,2-dioxides by Demers, James P., Sulsky, Richard, Klaubert, Dieter H.

“…1,5‐Dihydro‐3H‐1,2,4‐thiadiazolo[3,4‐b]quinazolin‐5‐one 2,2‐dioxides (3) are prepared by reaction of isatoic anhydrides with methyl…”
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