Search Results - "Feldman, Paul L."

Gut hormone pharmacology of a novel GPR119 agonist (GSK1292263), metformin, and sitagliptin in type 2 diabetes mellitus: results from two randomized studies by Nunez, Derek J, Bush, Mark A, Collins, David A, McMullen, Susan L, Gillmor, Dawn, Apseloff, Glen, Atiee, George, Corsino, Leonor, Morrow, Linda, Feldman, Paul L

“…GPR119 receptor agonists improve glucose metabolism and alter gut hormone profiles in animal models and healthy subjects. We therefore investigated the…”
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Discovery of a Highly Potent, Nonabsorbable Apical Sodium-Dependent Bile Acid Transporter Inhibitor (GSK2330672) for Treatment of Type 2 Diabetes by Wu, Yulin, Aquino, Christopher J, Cowan, David J, Anderson, Don L, Ambroso, Jeff L, Bishop, Michael J, Boros, Eric E, Chen, Lihong, Cunningham, Alan, Dobbins, Robert L, Feldman, Paul L, Harston, Lindsey T, Kaldor, Istvan W, Klein, Ryan, Liang, Xi, McIntyre, Maggie S, Merrill, Christine L, Patterson, Kristin M, Prescott, Judith S, Ray, John S, Roller, Shane G, Yao, Xiaozhou, Young, Andrew, Yuen, Josephine, Collins, Jon L

“…The apical sodium-dependent bile acid transporter (ASBT) transports bile salts from the lumen of the gastrointestinal (GI) tract to the liver via the portal…”
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Insights into the Chemical Discovery of Remifentanil by Feldman, Paul L.

“…Design, Synthesis, and Pharmacological Evaluation of Ultrashort- to Long-acting Opioid Analgetics. By Feldman PL, James MK, Brackeen MF, Bilotta JM, Schuster…”
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A 28-Day Toxicity Study of Tenofovir Alafenamide Hemifumarate by Subcutaneous Infusion in Rats and Dogs by Zane, Doris, Roller, Shane, Shelton, Josephine, Singh, Roshni, Jain, Rachna, Wang, Yan, Yang, Bing, Felx, Melanie, Alessi, Thomas, Feldman, Paul L

“…The toxicity of tenofovir alafenamide (TAF) hemifumarate (HF) was evaluated when administered by continuous subcutaneous (s.c.) infusion via an external…”
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Nitric Oxide: A New Paradigm for Second Messengers by Kerwin, James F, Lancaster, Jack R, Feldman, Paul L

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Development and Regulatory Challenges for Peptide Therapeutics by Zane, Doris, Feldman, Paul L., Sawyer, Tomi, Sobol, Zhanna, Hawes, Jessica

“…There has been an increased interest in and activity for the use of peptide therapeutics to treat a variety of human diseases. The number of peptide drugs…”
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Quality guidelines for oral drug candidates: dose, solubility and lipophilicity by Bayliss, Martin K., Butler, James, Feldman, Paul L., Green, Darren V.S., Leeson, Paul D., Palovich, Michael R., Taylor, Anthony J.

“…[Display omitted] •Experimental properties of GSK's oral portfolio were compared with marketed drugs.•Properties were dose, solubility and the property…”
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Potent, Selective, and Orally Efficacious Antagonists of Melanin-Concentrating Hormone Receptor 1 by Tavares, Francis X, Al-Barazanji, Kamal A, Bigham, Eric C, Bishop, Michael J, Britt, Christy S, Carlton, David L, Feldman, Paul L, Goetz, Aaron S, Grizzle, Mary K, Guo, Yu C, Handlon, Anthony L, Hertzog, Donald L, Ignar, Diane M, Lang, Daniel G, Ott, Ronda J, Peat, Andrew J, Zhou, Hui-Qiang

“…The high expression of MCH in the hypothalamus with the lean hypophagic phenotype coupled with increased resting metabolic rate and resistance to high fat…”
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Tenofovir Alafenamide for HIV Prevention: Review of the Proceedings from the Gates Foundation Long-Acting TAF Product Development Meeting by Romano, Joseph W, Baum, Marc M, Demkovich, Zach R, Diana, Frank, Dobard, Charles, Feldman, Paul L, Garcia-Lerma, J Gerardo, Grattoni, Alessandro, Gunawardana, Manjula, Ho, Duy-Khiet, Hope, Thomas J, Massud, Ivana, Milad, Mark, Moss, John A, Pons-Faudoa, Fernanda P, Roller, Shane, van der Straten, Ariane, Srinivasan, Selvi, Veazey, Ronald S, Zane, Doris

“…The ability to successfully develop a safe and effective vaccine for the prevention of HIV infection has proven challenging. Consequently, alternative…”
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CNS 7056: a novel ultra-short-acting Benzodiazepine by Kilpatrick, Gavin J, McIntyre, Margaret S, Cox, Richard F, Stafford, Jeffrey A, Pacofsky, Gregory J, Lovell, Gwyer G, Wiard, Robert P, Feldman, Paul L, Collins, Holly, Waszczak, Barbara L, Tilbrook, Gary S

“…A new benzodiazepine derivative, CNS 7056, has been developed to permit a superior sedative profile to current agents, i.e., more predictable fast onset, short…”
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A Novel One-Pot Synthesis of N-Substituted Thieno[3,2-d]pyrimidin-4(3H)-ones by J. Peat, Andrew, L. Feldman, Paul, Garrido, Dulce, C. Guo, Yu, L. Hertzog, Donald

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Synthesis of Ultra-Short-Acting Neuromuscular Blocker GW 0430:  A Remarkably Stereo- and Regioselective Synthesis of Mixed Tetrahydroisoquinolinium Chlorofumarates by Samano, Vicente, Ray, John A, Thompson, James B, Mook, Robert A, Jung, David K, Koble, Cecilia S, Martin, Michael T, Bigham, Eric C, Regitz, Craig S, Feldman, Paul L, Boros, Eric E

“…The stereo- and regioselective synthesis of ultra-short-acting nondepolarizing neuromuscular blocker GW 0430 (5a) is described. Key steps involved the…”
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Bis- and Mixed-Tetrahydroisoquinolinium Chlorofumarates:  New Ultra-Short-Acting Nondepolarizing Neuromuscular Blockers by Boros, Eric E, Bigham, Eric C, Boswell, G. Evan, Mook, Robert A, Patel, Sanjay S, Savarese, John J, Ray, John A, Thompson, James B, Hashim, Mir A, Wisowaty, James C, Feldman, Paul L, Samano, Vicente

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An efficient and practical total synthesis of (+)-vincamine from L-aspartic acid by Gmeiner, Peter, Feldman, Paul L, Chu-Moyer, Margaret Y, Rapoport, Henry

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Design and Synthesis of Conformationally Constrained Analogs of 4-(3-Butoxy-4-methoxybenzyl)imidazolidin-2-one (Ro 20-1724) as Potent Inhibitors of cAMP-Specific Phosphodiesterase by Brackeen, Marcus F, Stafford, Jeffrey A, Cowan, David J, Brown, Peter J, Domanico, Paul L, Feldman, Paul L, Rose, Dudley, Strickland, Alan B, Veal, James M, Verghese, Margrith

“…The synthesis and biological evaluation of cAMP-specific phosphodiesterase (PDE IV) inhibitors is described. The PDE IV inhibitor…”
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6-(4-Chlorophenyl)-3-substituted-thieno[3,2-d]pyrimidin-4(3H)-one-Based Melanin-Concentrating Hormone Receptor 1 Antagonist by Tavares, Francis X, Al-Barazanji, Kamal A, Bishop, Michael J, Britt, Christy S, Carlton, David L, Cooper, Joel P, Feldman, Paul L, Garrido, Dulce M, Goetz, Aaron S, Grizzle, Mary K, Hertzog, Donald L, Ignar, Diane M, Lang, Daniel G, McIntyre, Maggie S, Ott, Ronda J, Peat, Andrew J, Zhou, Hui-Qiang

“…Genetic manipulation studies in mice at both the MCH receptor 1 (MCHR1) as well as the MCH peptide levels have implicated MCHR1 as a key player in energy…”
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Degradative Rearrangements of N-(t-Butyloxycarbonyl)-O-methanesulfonyl-hydroxamic Acids:  A Novel, Reagent-Based Alternative to the Lossen Rearrangement1 by Stafford, Jeffrey A, Gonzales, Stephen S, Barrett, David G, Suh, Edward M, Feldman, Paul L

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Preclinical pharmacology of GW280430A (AV430A) in the rhesus monkey and in the cat: A comparison with mivacurium by SAVARESE, John J, BELMONT, Matthew R, SPITZER, Timothy, COHN, Douglas L, MORGAN, Philip, WASTILA, William B, HASHIM, Mir A, MOOK, Robert A, BOROS, Eric E, SAMANO, Vicente, PATEL, Sanjay S, FELDMAN, Paul L, SCHULTZ, Jan-Ake I, MCNULTY, Michael

“…No replacement for succinylcholine is yet available. GW280430A (AV430A) is a representative of a new class of nondepolarizing neuromuscular blocking drugs…”
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CNS 7056 by Kilpatrick, Gavin J., McIntyre, Margaret S., Cox, Richard F., Stafford, Jeffrey A., Pacofsky, Gregory J., Lovell, Gwyer G., Wiard, Robert P., Feldman, Paul L., Collins, Holly, Waszczak, Barbara L., Tilbrook, Gary S.

“…Abstract Background: A new benzodiazepine derivative, CNS 7056, has been developed to permit a superior sedative profile to current agents, i.e., more…”
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Identification and Structure–Activity Studies of Novel Ultrashort-Acting Benzodiazepine Receptor Agonists by Stafford, Jeffrey A., Pacofsky, Gregory J., Cox, Richard F., Cowan, Jill R., Dorsey, George F., Gonzales, Stephen S., Jung, David K., Koszalka, George W., McIntyre, Maggie S., Tidwell, Jeffrey H., Wiard, Robert P., Feldman, Paul L.

“…The synthesis and evaluation of novel ultrashort-acting benzodiazepine (USA BZD) agonists are described. A BZD scaffold was modified by incorporation of amino…”
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