Search Results - "Christ, David D"

Potent, Orally Bioavailable Delta Opioid Receptor Agonists for the Treatment of Pain: Discovery of N,N-Diethyl-4-(5-hydroxyspiro[chromene-2,4′-piperidine]-4-yl)benzamide (ADL5859) by Bourdonnec, Bertrand Le, Windh, Rolf T, Ajello, Christopher W, Leister, Lara K, Gu, Minghua, Chu, Guo-Hua, Tuthill, Paul A, Barker, William M, Koblish, Michael, Wiant, Daniel D, Graczyk, Thomas M, Belanger, Serge, Cassel, Joel A, Feschenko, Marina S, Brogdon, Bernice L, Smith, Steven A, Christ, David D, Derelanko, Michael J, Kutz, Steve, Little, Patrick J, DeHaven, Robert N, DeHaven-Hudkins, Diane L, Dolle, Roland E

“…Selective δ opioid receptor agonists are promising potential therapeutic agents for the treatment of various types of pain conditions. A spirocyclic derivative…”
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N-in-1 dosing pharmacokinetics in drug discovery: experience, theoretical and practical considerations by He, Kan, Qian, Mingxin, Wong, Harvey, Bai, Stephen A, He, Bing, Brogdon, Bernice, Grace, James E, Xin, Baomin, Wu, Jingtao, Ren, Shelly X, Zeng, Hang, Deng, Yuzhong, Graden, Danielle M, Olah, Timothy V, Unger, Steve E, Luettgen, Joseph M, Knabb, Robert M, Pinto, Donald J, Lam, Patrick Y S, Duan, James, Wexler, Ruth R, Decicco, Carl P, Christ, David D, Grossman, Scott J

“…N-in-1 (or cassette) dosing pharmacokinetics (PK) has been used in drug discovery for rapid assessment of PK properties of new chemical entities. However,…”
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The Species-Dependent Metabolism of Efavirenz Produces a Nephrotoxic Glutathione Conjugate in Rats by Mutlib, Abdul E., Gerson, Ronald J., Meunier, Paul C., Haley, Patrick J., Chen, Hao, Gan, Lawrence S., Davies, Marc H., Gemzik, Brian, Christ, David D., Krahn, David F., Markwalder, Jay A., Seitz, Steven P., Robertson, Richard T., Miwa, Gerald T.

“…Efavirenz, a potent nonnucleoside reverse transcriptase inhibitor widely prescribed for the treatment of HIV infection, produces renal tubular epithelial cell…”
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Potent, selective, orally bioavailable inhibitors of tumor necrosis factor-α converting enzyme (TACE): Discovery of indole, benzofuran, imidazopyridine and pyrazolopyridine P1′ substituents by Lu, Zhonghui, Ott, Gregory R., Anand, Rajan, Liu, Rui-Qin, Covington, Maryanne B., Vaddi, Krishna, Qian, Mingxin, Newton, Robert C., Christ, David D., Trzaskos, James, Duan, James J.-W.

“…Selective inhibitors of TNF-α converting enzyme (TACE) with novel P1′ substituents. Potent and selective inhibitors of tumor necrosis factor-α converting…”
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Interaction of Ritonavir on Tissue Distribution of a [14C]L-Valinamide, a Potent Human Immunodeficiency Virus-1 Protease Inhibitor, in Rats Using Quantitative Whole-Body Autoradiography by SOLON, Eric G, BALANI, Suresh K, LEE, Frank W, GANG LUO, YANG, Tian J, HAINES, Paula J, LIFEI WANG, DEMOND, Tonya, DIAMOND, Sharon, CHRIST, David D, GAN, Liang-Shang

“…N -[(3-fluorophenyl)methyl]glycyl- N -{3-[((3-aminophenyl)sulfonyl)- 2-(aminophenyl)amino]-(1 S ,2 S )-2-hydroxy-1-(phenylmethyl)propyl}- 3-methyl- l…”
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THE CHIMPANZEE (PAN TROGLODYTES) AS A PHARMACOKINETIC MODEL FOR SELECTION OF DRUG CANDIDATES: MODEL CHARACTERIZATION AND APPLICATION by WONG, Harvey, GROSSMAN, Scott J, BAI, Stephen A, DIAMOND, Sharon, WRIGHT, Matthew R, GRACE, James E, MINGXIN QIAN, KAN HE, YELESWARAM, Krishnaswamy, CHRIST, David D

“…The chimpanzee (CHP) was evaluated as a pharmacokinetic model for humans (HUMs) using propranolol, verapamil, theophylline, and 12 proprietary compounds…”
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Potent, exceptionally selective, orally bioavailable inhibitors of TNF-alpha Converting Enzyme (TACE): novel 2-substituted-1H-benzo[d]imidazol-1-yl)methyl)benzamide P1' substituents by Ott, Gregory R, Asakawa, Naoyuki, Lu, Zhonghui, Anand, Rajan, Liu, Rui-Qin, Covington, Maryanne B, Vaddi, Krishna, Qian, Mingxin, Newton, Robert C, Christ, David D, Trzaskos, James M, Duan, James J-W

“…Novel ((2-substituted-1H-benzo[d]imidazol-1-yl)methyl)benzamides were found to be excellent P1' substituents in conjunction with unique constrained beta-amino…”
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Discovery of γ-Lactam Hydroxamic Acids as Selective Inhibitors of Tumor Necrosis Factor α Converting Enzyme:  Design, Synthesis, and Structure−Activity Relationships by Duan, James J.-W, Chen, Lihua, Wasserman, Zelda R, Lu, Zhonghui, Liu, Rui-Qin, Covington, Maryanne B, Qian, Mingxin, Hardman, Karl D, Magolda, Ronald L, Newton, Robert C, Christ, David D, Wexler, Ruth R, Decicco, Carl P

“…New γ-lactam TACE inhibitors were designed from known MMP inhibitors. A homology model of TACE was built and examined to identify the S1‘ site as the key area…”
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α,β-Cyclic-β-benzamido hydroxamic acids: Novel templates for the design, synthesis, and evaluation of selective inhibitors of TNF-α converting enzyme (TACE) by Ott, Gregory R., Asakawa, Naoyuki, Lu, Zhonghui, Liu, Rui-Qin, Covington, Maryanne B., Vaddi, Krishna, Qian, Mingxin, Newton, Robert C., Christ, David D., Traskos, James M., Decicco, Carl P., Duan, James J.-W.

“…Selective inhibitors of TNF-α Converting Enzyme (TACE) based on novel α,β-cyclic-β-benzamido hydroxamic acids have been synthesized and evaluated. Selective…”
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Pharmacokinetics and pharmacodynamics of DPC 333 (2R)-2-((3R)-3 -amino -3{4 -[2 -methyl -4 -quinolinyl) methoxy] phenyl}-2-oxopyrrolidinyl -n -hydroxy -4 -methylpentanamide , a potent and selective inhibitor of tumor necrosis factor α-Converting enzyme in rodents, dogs, chimpanzees, and humans by MINGXIN QIAN, BAI, Stephen A, YUZHONG DENG, MADUSKUIE, Thomas, TRZASKOS, James, DUAN, James J.-W, DECICCO, Carl P, CHRIST, David D, BROGDON, Bernice, WU, Jing-Tao, LIU, Rui-Qin, COVINGTON, Maryanne B, VADDI, Kris, NEWTON, Robert C, FOSSLER, Michael J, GARNER, C. Edwin

“…DPC 333 ((2R)-2-((3R)-3-amino-3{4-[2-methyl-4-quinolinyl) methoxy] phenyl}-2-oxopyrrolidinyl)-N-hydroxy-4-methylpentanamide)) is a potent and selective…”
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Discovery of β-benzamido hydroxamic acids as potent, selective, and orally bioavailable TACE inhibitors by Duan, James J.-W., Chen, Lihua, Lu, Zhonghui, Xue, Chu-Biao, Liu, Rui-Qin, Covington, Maryanne B., Qian, Mingxin, Wasserman, Zelda R., Vaddi, Krishna, Christ, David D., Trzaskos, James M., Newton, Robert C., Decicco, Carl P.

“…β-Benzamido hydroxamic acids were discovered as potent TACE inhibitors. A computer model was constructed to help understanding the binding activities and…”
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α,β-Cyclic-β-benzamido hydroxamic acids: Novel oxaspiro[4.4]nonane templates for the discovery of potent, selective, orally bioavailable inhibitors of tumor necrosis factor-α converting enzyme (TACE) by Ott, Gregory R., Asakawa, Naoyuki, Liu, Rui-Qin, Covington, Maryanne B., Qian, Mingxin, Vaddi, Krishna, Newton, Robert C., Trzaskos, James M., Christ, David D., Galya, Laurine, Scholz, Thomas, Marshall, Will, Duan, James J.-W.

“…Selective inhibitors of TNF-α Converting Enzyme (TACE) based on novel oxaspiro[4.4]nonane β-benzamido hydroxamic scaffolds acids have been synthesized and…”
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Design, Synthesis, and Evaluation of Benzothiadiazepine Hydroxamates as Selective Tumor Necrosis Factor-α Converting Enzyme Inhibitors by Cherney, Robert J, Duan, James J.-W, Voss, Matthew E, Chen, Lihua, Wang, Li, Meyer, Dayton T, Wasserman, Zelda R, Hardman, Karl D, Liu, Rui-Qin, Covington, Maryanne B, Qian, Mingxin, Mandlekar, Sandhya, Christ, David D, Trzaskos, James M, Newton, Robert C, Magolda, Ronald L, Wexler, Ruth R, Decicco, Carl P

“…Elevated levels of tumor necrosis factor-α (TNF-α) have been associated with several inflammatory diseases, and therefore, strategies for its suppression have…”
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A new 4-(2-methylquinolin-4-ylmethyl)phenyl P1′ group for the β-amino hydroxamic acid derived TACE inhibitors by Chen, Xiao-Tao, Ghavimi, Bahman, Corbett, Ronald L., Xue, Chu-Biao, Liu, Rui-Qin, Covington, Maryanne B., Qian, Mingxin, Vaddi, Krishna G., Christ, David D., Hartman, Karl D., Ribadeneira, Maria D., Trzaskos, James M., Newton, Robert C., Decicco, Carl P., Duan, James J.-W.

“…A new P1′ group for TACE inhibitors was identified by eliminating the oxygen atom in the linker of the original 4-(2-methylquinolin-4-ylmethoxy)phenyl P1′…”
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CC chemokine receptor-3 (CCR3) antagonists: Improving the selectivity of DPC168 by reducing central ring lipophilicity by Pruitt, James R., Batt, Douglas G., Wacker, Dean A., Bostrom, Lori L., Booker, Shon K., McLaughlin, Erin, Houghton, Gregory C., Varnes, Jeffrey G., Christ, David D., Covington, Maryanne, Das, Anuk M., Davies, Paul, Graden, Danielle, Kariv, Ilona, Orlovsky, Yevgeniya, Stowell, Nicole C., Vaddi, Krishna G., Wadman, Eric A., Welch, Patricia K., Yeleswaram, Swamy, Solomon, Kimberly A., Newton, Robert C., Decicco, Carl P., Carter, Percy H., Ko, Soo S.

“…DPC168, a benzylpiperidine-substituted aryl urea CCR3 antagonist evaluated in clinical trials, was a relatively potent inhibitor of the 2D6 isoform of…”
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Sultam Hydroxamates as Novel Matrix Metalloproteinase Inhibitors by Cherney, Robert J, Mo, Ruowei, Meyer, Dayton T, Hardman, Karl D, Liu, Rui-Qin, Covington, Maryanne B, Qian, Mingxin, Wasserman, Zelda R, Christ, David D, Trzaskos, James M, Newton, Robert C, Decicco, Carl P

“…In this communication we describe the design, synthesis, and evaluation of novel sultam hydroxamates 4 as MMP-2, -9, and -13 inhibitors. Compound 26 was found…”
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Potent and selective aggrecanase inhibitors containing cyclic P1 substituents by Cherney, Robert J, Mo, Ruowei, Meyer, Dayton T, Wang, Li, Yao, Wenqing, Wasserman, Zelda R, Liu, Rui-Qin, Covington, Maryanne B, Tortorella, Micky D, Arner, Elizabeth C, Qian, Mingxin, Christ, David D, Trzaskos, James M, Newton, Robert C, Magolda, Ron L, Decicco, Carl P

“…Anti-succinate hydroxamates with cyclic P1 motifs were synthesized as aggrecanase inhibitors. The N-methanesulfonyl piperidine 23 and the N-trifluoroacetyl…”
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Rational design, synthesis and structure-activity relationships of a cyclic succinate series of TNF-α converting enzyme inhibitors. Part 2: Lead optimization by XUE, Chu-Biao, XIAOHUA HE, CHRIST, David D, NEWTON, Robert C, TRZASKOS, James M, MAGOLDA, Ronald L, WEXLER, Ruth R, DECICCO, Carl P, RODERICK, John, CORBETT, Ronald L, DUAN, James J.-W, LIU, Rui-Qin, COVINGTON, Maryanne B, MINGXIN QIAN, RIBADENEIRA, Maria D, VADDI, Krishna

“…Modifications of the lead TACE inhibitor 1 (N-hydroxy-trans-2-[[4-(4-quinolinyloxymethyl)anilinyl]carbonyl]-1-cyclohexanecarboxamide) at the cyclohexyl ring…”
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Development of a dog microdialysis model for determining synovial fluid pharmacokinetics of anti-arthritis compounds exemplified by methotrexate by MINGXIN QIAN, WEST, Wanda, WU, Jing-Tao, BING LU, CHRIST, David D

“…The purpose of this study was to develop and validate an animal model of drug disposition in synovial fluid (SF) by comparing microdialysis with arthrocentesis…”
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Human plasma protein binding of the angiotensin II receptor antagonist losartan potassium (DuP 753/MK 954) and its pharmacologically active metabolite EXP3174 by Christ, D D

“…The in vitro protein binding characteristics of the prototypical angiotensin II receptor antagonist losartan potassium (DuP 753/MK 954) and its…”
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