Search Results - "Huebert, Norman D"

Structure-based design, synthesis, and biological evaluation of novel 1,4-diazepines as HDM2 antagonists by Raboisson, Pierre, Marugán, Juan José, Schubert, Carsten, Koblish, Holly K., Lu, Tianbao, Zhao, Shuyuan, Player, Mark R., Maroney, Anna C., Reed, Rolanda L., Huebert, Norman D., Lattanze, Jennifer, Parks, Daniel J., Cummings, Maxwell D.

“…Novel 1,4-diazepine-2,5-diones that act as antagonists of the HDM2–p53 interaction are reported. Crystallographic analysis of ligands bound to HDM2 suggested…”
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Design, synthesis and biological evaluation of (2S,3R,4R,5S,6R)-5-fluoro-6-(hydroxymethyl)-2-aryltetrahydro-2H-pyran-3,4-diols as potent and orally active SGLT dual inhibitors by Xu, Guozhang, Gaul, Michael D., Kuo, Gee-Hong, Du, Fuyong, Xu, June Zhi, Wallace, Nathaniel, Hinke, Simon, Kirchner, Thomas, Silva, Jose, Huebert, Norman D., Lee, Seunghun, Murray, William, Liang, Yin, Demarest, Keith

“…[Display omitted] •A new series of SGLT1 and SGLT2 dual inhibitors were disclosed.•Two methods were developed to efficiently synthesize C5-fluoro-lactones 3…”
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Improved pharmacokinetic and bioavailability support of drug discovery using serial blood sampling in mice by Peng, Sean X, Rockafellow, Beth A, Skedzielewski, Tina M, Huebert, Norman D, Hageman, William

“…Pharmacokinetic studies in mice traditionally require one animal per time point, resulting in dosing and euthanizing a large number of animals and producing…”
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Design and synthesis of polyethylene glycol-modified biphenylsulfonyl-thiophene-carboxamidine inhibitors of the complement component C1s by Subasinghe, Nalin L., Khalil, Ehab, Travins, Jeremy M., Ali, Farah, Ballentine, Shelley K., Hufnagel, Heather R., Pan, Wenxi, Leonard, Kristi, Bone, Roger F., Soll, Richard M., Crysler, Carl S., Ninan, Nisha, Kirkpatrick, Jennifer, Kolpak, Michael X., Diloreto, Karen A., Eisennagel, Stephen H., Huebert, Norman D., Molloy, Christopher J., Tomczuk, Bruce E., Gaul, Michael D.

“…Complement C1s protease inhibitors have potential utility in the treatment of diseases associated with activation of the classical complement pathway such as…”
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FcRn binding is not sufficient for achieving systemic therapeutic levels of immunoglobulin G after oral delivery of enteric‐coated capsules in cynomolgus macaques by Muzammil, Salman, Mabus, John R., Cooper, Philip R., Brezski, Randall J., Bement, Courtney B., Perkinson, Rob, Huebert, Norman D., Thompson, Suzanne, Levine, Dalia, Kliwinski, Connie, Bradley, Dino, Hornby, Pamela J.

“…Although much speculation has surrounded intestinally expressed FcRn as a means for systemic uptake of orally administered immunoglobulin G (IgG), this has not…”
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Isocratic high-performance liquid chromatographic method for the separation of testosterone metabolites by Sanwald, Patricia, Blankson, Evelyn A., Duléry, Bertrand D., Schoun, Josiane, Huebert, Norman D., Dow, James

“…An isocratic reversed-phase high-performance liquid chromatographic (HPLC) method using an Ultrasphere IP column has been developed for the determination of…”
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Orally efficacious thrombin inhibitors with cyanofluorophenylacetamide as the P2 motif by Kreutter, Kevin D., Lu, Tianbao, Lee, Lily, Giardino, Edward C., Patel, Sharmila, Huang, Hui, Xu, Guozhang, Fitzgerald, Mark, Haertlein, Barbara J., Mohan, Venkatraman, Crysler, Carl, Eisennagel, Stephen, Dasgupta, Malini, McMillan, Martin, Spurlino, John C., Huebert, Norman D., Maryanoff, Bruce E., Tomczuk, Bruce E., Damiano, Bruce P., Player, Mark R.

“…2-Cyano-6-fluorophenylacetamide was explored as a novel P2 scaffold in the design of thrombin inhibitors. Optimization around this structural motif culminated…”
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Discovery, SAR, and X-ray structure of novel biaryl-based dipeptidyl peptidase IV inhibitors by Qiao, Lei, Baumann, Christian A., Crysler, Carl S., Ninan, Nisha S., Abad, Marta C., Spurlino, John C., DesJarlais, Renee L., Kervinen, Jukka, Neeper, Mike P., Bayoumy, Shariff S., Williams, Robyn, Deckman, Ingrid C., Dasgupta, Malini, Reed, Rolanda L., Huebert, Norman D., Tomczuk, Bruce E., Moriarty, Kevin J.

“…The discovery, SAR, and X-ray crystal structure of novel biarylaminoacyl-( S)-2-cyano-pyrrolidines and biarylaminoacylthiazolidines as potent inhibitors of…”
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Pharmacokinetics of vigabatrin: implications of creatinine clearance by Haegele, K D, Huebert, N D, Ebel, M, Tell, G P, Schechter, P J

“…The pharmacokinetics of both enantiomers of vigabatrin after a single oral dose in healthy young subjects (mean creatinine clearance 120 ml/min) were compared…”
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Kinetics and metabolism of p-tyramine during monoamine oxidase inhibition by mofegiline by Huebert, N D, Dulery, B D, Schoun, J, Schwach, V, Hinze, C, Haegele, K D

“…The effects of monoamine oxidase B (MAO-B) inhibition by mofegiline on the pharmacokinetics of p-tyramine and its major metabolite, p-hydroxyphenylacetic acid,…”
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Using in vitro human tissues to predict pharmacokinetic properties by Huebert, Norman D, Dasgupta, Malini, Chen, Yanmin

“…Pressure on drug discovery teams to predict the success of drug candidates earlier in the drug discovery process has led to the development of in vitro assays…”
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The measurement of beta-phenylethylamine in human plasma and rat brain by Huebert, N D, Schuurmans Schwach, V, Richter, G, Zreika, M, Hinze, C, Haegele, K D

“…A sensitive and specific analytical method has been developed for the measurement of beta-phenylethylamine (PEA) in human plasma and rat brain extracts. The…”
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Longitudinal urinary trace amine excretion in a human male by Huebert, N D, Boulton, A A

“…The urinary excretion of a beta-phenylethylamine (PE), m-tyramine (mTA), p-tyramine (pTA) and tryptamine (TR) in their unconjugated (free) and conjugated…”
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