Search Results - "Azzarano, Leonard"

Parenteral platforms for tunable, long-acting administration of a highly hydrophobic antiretroviral drug by Akhavein, Nima, Baum, Marc M., Gunawardana, Manjula, Moss, John A., Calvez, Sandrine, Remedios-Chan, Mariana, Fanter, Rob, Lenhard, Steve, Rusk, Samantha, Azzarano, Leonard, McCoy, Deborah, Jucker, Beat, Johns, Brian, Burke, Matt, Velthuisen, Emile

“…GSK2838232 (GSK8232) is a second-generation maturation inhibitor (MI) developed for the treatment of HIV with excellent broad-spectrum virological profiles…”
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Preclinical pharmacokinetic properties of the P-glycoprotein inhibitor GF120918A (HCl salt of GF120918, 9,10-dihydro-5-methoxy-9-oxo-N-[4-[2-(1,2,3,4-tetrahydro-6,7-dimethoxy-2-isoquinolinyl)ethyl]phenyl]-4-acridine-carboxamide) in the mouse, rat, dog, and monkey by Ward, Keith W, Azzarano, Leonard M

“…GF120918A, the HCl salt of GF120918 (9,10-dihydro-5-methoxy-9-oxo-N-[4-[2-(1,2,3,4-tetrahydro-6,7-dimethoxy-2-isoquinolinyl)…”
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Design and synthesis of orally bioavailable serum and glucocorticoid-regulated kinase 1 (SGK1) inhibitors by Hammond, Marlys, Washburn, David G., Hoang, Tram H., Manns, Sharada, Frazee, James S., Nakamura, Hiroko, Patterson, Jaclyn R., Trizna, Walter, Wu, Charlene, Azzarano, Leonard M., Nagilla, Rakesh, Nord, Melanie, Trejo, Rebecca, Head, Martha S., Zhao, Baoguang, Smallwood, Angela M., Hightower, Kendra, Laping, Nicholas J., Schnackenberg, Christine G., Thompson, Scott K.

“…SGK1 inhibitors 1 and 2 suffered from poor oral exposure that could be attributed to factors such as high clearance and formation of glucuronic acid…”
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Comparison of N, N′-diarylsquaramides and N, N′-diarylureas as antagonists of the CXCR2 chemokine receptor by McCleland, Brent W., Davis, Roderick S., Palovich, Michael R., Widdowson, Katherine L., Werner, Michelle L., Burman, Miriam, Foley, James J., Schmidt, Dulcie B., Sarau, Henry M., Rogers, Martin, Salyers, Kevin L., Gorycki, Peter D., Roethke, Theresa J., Stelman, Gary J., Azzarano, Leonard M., Ward, Keith W., Busch-Petersen, Jakob

“…N, N′-diarylsquaramides were prepared and evaluated as antagonists of CXCR2. The compounds were found to be potent and selective antagonists of CXCR2…”
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DEVELOPMENT OF AN IN VIVO PRECLINICAL SCREEN MODEL TO ESTIMATE ABSORPTION AND FIRST-PASS HEPATIC EXTRACTION OF XENOBIOTICS. II. USE OF KETOCONAZOLE TO IDENTIFY P-GLYCOPROTEIN/CYP3A-LIMITED BIOAVAILABILITY IN THE MONKEY by WARD, Keith W, STELMAN, Gary J, MORGAN, Jayme A, ZEIGLER, Kelli S, AZZARANO, Leonard M, KEHLER, Jonathan R, MCSURDY-FREED, Jeanelle E, PROKSCH, Joel W, SMITH, Brian R

“…The effect of P-glycoprotein (Pgp) and/or CYP3A on the disposition of xenobiotics has been extensively investigated and is often of interest during drug…”
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Improving the developability profile of pyrrolidine progesterone receptor partial agonists by Kallander, Lara S., Washburn, David G., Hoang, Tram H., Frazee, James S., Stoy, Patrick, Johnson, Latisha, Lu, Qing, Hammond, Marlys, Barton, Linda S., Patterson, Jaclyn R., Azzarano, Leonard M., Nagilla, Rakesh, Madauss, Kevin P., Williams, Shawn P., Stewart, Eugene L., Duraiswami, Chaya, Grygielko, Eugene T., Xu, Xiaoping, Laping, Nicholas J., Bray, Jeffrey D., Thompson, Scott K.

“…The previously reported pyrrolidine class of progesterone receptor partial agonists demonstrated excellent potency but suffered from serious liabilities…”
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Assessment of oral bioavailability enhancing approaches for SB-247083 using flow-through cell dissolution testing as one of the screens by Perng, Cherng-Yih, Kearney, Albert S, Palepu, Nagesh R, Smith, Brian R, Azzarano, Leonard M

“…SB-247083 is a potent, nonpeptidic, orally active, ETA-selective, endothelin receptor antagonist. The diacid form and three salts (monoarginine, diarginine and…”
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Phenylbutyrates as potent, orally bioavailable vitronectin receptor (integrin αvβ3) antagonists by Miller, William H, Manley, Peter J, Cousins, Russell D, Erhard, Karl F, Heerding, Dirk A, Kwon, Chet, Ross, Stephen T, Samanen, James M, Takata, Dennis T, Uzinskas, Irene N, Yuan, Catherine C.K, Haltiwanger, R.Curtis, Gress, Catherine J, Lark, Michael W, Hwang, Shing-Mei, James, Ian E, Rieman, David J, Willette, Robert N, Yue, Tian-Li, Azzarano, Leonard M, Salyers, Kevin L, Smith, Brian R, Ward, Keith W, Johanson, Kyung O, Huffman, William F

“…In our continuing efforts to identify small molecule vitronectin receptor antagonists, we have discovered a series of phenylbutyrate derivatives, exemplified…”
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Discovery of Orally Active Nonpeptide Vitronectin Receptor Antagonists Based on a 2-Benzazepine Gly-Asp Mimetic by Miller, William H, Alberts, Doreen P, Bhatnagar, Pradip K, Bondinell, William E, Callahan, James F, Calvo, Raul R, Cousins, Russell D, Erhard, Karl F, Heerding, Dirk A, Keenan, Richard M, Kwon, Chet, Manley, Peter J, Newlander, Kenneth A, Ross, Stephen T, Samanen, James M, Uzinskas, Irene N, Venslavsky, Joseph W, Yuan, Catherine C.-K, Haltiwanger, R. Curtis, Gowen, Maxine, Hwang, Shing-Mei, James, Ian E, Lark, Michael W, Rieman, David J, Stroup, George B, Azzarano, Leonard M, Salyers, Kevin L, Smith, Brian R, Ward, Keith W, Johanson, Kyung O, Huffman, William F

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Pharmacokinetics of SB-247083, a potent and selective endothelinA receptor antagonist, in the rat, dog, and monkey by Ward, Keith W., Azzarano, Leonard M., Morgan, Jayme A., Gould, Michael J., Perng, Cherng-Yih, Souder, Pamela R., Lundberg, David, Smith, Brian R.

“…The endothelins (ET) are among the most potent vasoconstrictors identified to date, and have been implicated in such diseases as renal failure, pulmonary…”
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Pharmacokinetics of SB-247083, a potent and selective endothelin(A) receptor antagonist, in the rat, dog, and monkey by Ward, Keith W, Azzarano, Leonard M, Morgan, Jayme A, Gould, Michael J, Perng, Cherng-Yih, Souder, Pamela R, Lundberg, David, Smith, Brian R

“…The endothelins (ET) are among the most potent vasoconstrictors identified to date, and have been implicated in such diseases as renal failure, pulmonary…”
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Preclinical Pharmacokinetics and Interspecies Scaling of a Novel Vitronectin Receptor Antagonist by WARD, K. W, AZZARANO, L. M, MUMAW, J. A, NEWLANDER, K. A, PIRHALLA, J. L, ROETHKE, T. J, SALYERS, K. L, SOUDER, P. R, STELMAN, G. J, SMITH, B. R, BONDINELL, W. E, COUSINS, R. D, HUFFMAN, W. F, JAKAS, D. R, KEENAN, R. M, KU, T. W, LUNDBERG, D, MILLER, W. H

“…Allometric scaling may be used in drug development to predict the pharmacokinetics of xenobiotics in humans from animal data. Although allometry may be…”
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SB-239063, a potent and selective inhibitor of p38 map kinase : Preclinical pharmacokinetics and species-specific reversible isomerization by WARD, Keith W, PROKSCH, Joel W, AZZARANO, Leonard M, SALYERS, Kevin L, MCSURDY-FREED, Jeanelle E, MOLNAR, Tina M, LEVY, Mark A, SMITH, Brian R

“…A series of studies was conducted to evaluate the preclinical pharmacokinetics of SB-239063…”
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Orally bioavailable nonpeptide vitronectin receptor antagonists with efficacy in an osteoporosis model by Miller, William H., Bondinell, William E., Cousins, Russell D., Erhard, Karl F., Jakas, Dalia R., Keenan, Richard M., Ku, Thomas W., Newlander, Kenneth A., Ross, Stephen T., Haltiwanger, R.Curtis, Bradbeer, Jeremy, Drake, Fred H., Gowen, Maxine, Hoffman, Sandra J., Hwang, Shing-Mei, James, Ian E., Lark, Michael W., Lechowska, Beata, Rieman, David J., Stroup, George B., Vasko-Moser, Janice A., Zembryki, Denise L., Azzarano, Leonard M., Adams, Paula C., Salyers, Kevin L., Smith, Brian R., Ward, Keith W., Johanson, Kyung O., Huffaman, William F.

“…A new series of potent nonpeptide vitronectin receptor antagonists, based on a novel carbocyclic Gly-Asp mimetic, has been discovered. A representative of this…”
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THE RELATIONSHIP OF VOCATIONAL MATURITY AND SELECTED STUDENT CHARACTERISTICS TO THE DROPOUT RATE OF BLACK URBAN INDUSTRIAL EDUCATIONAL STUDENTS by AZZARANO, LEONARD

“…The purpose of this study was to (1) examine the dropout rate of black industrial education students in terms of its relationship to vocational maturity and…”
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