Search Results - "Stella H. Vincent"

Metabolism and excretion of the dipeptidyl peptidase 4 inhibitor [14C]sitagliptin in humans by VINCENT, Stella H, REED, James R, DILZER, Stacy, LASSETER, Kenneth, GOTTESDIENER, Keith, WAGNER, John A, HERMAN, Gary A, BERGMAN, Arthur J, ELMORE, Charles S, BING ZHU, SHIYAO XU, EBEL, David, LARSON, Patrick, WEI ZENG, LI CHEN

“…The metabolism and excretion of [(14)C]sitagliptin, an orally active, potent and selective dipeptidyl peptidase 4 inhibitor, were investigated in humans after…”
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Disposition of the Dipeptidyl Peptidase 4 Inhibitor Sitagliptin in Rats and Dogs by BECONI, Maria G, REED, James R, STEARNS, Ralph A, VINCENT, Stella H, TEFFERA, Yohannes, XIA, Yuan-Qing, KOCHANSKY, Christopher J, LIU, David Q, SHIYAO XU, ELMORE, Charles S, CICCOTTO, Suzanne, HORA, Donald F

“…The pharmacokinetics, metabolism, and excretion of sitagliptin [MK-0431; (2 R )-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3- a ]pyrazin-7(8 H…”
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Characterization of Two Cyclic Metabolites of Sitagliptin by LIU, David Q, ARISON, Byron H, STEARNS, Ralph A, KIM, Dooseop, VINCENT, Stella H

“…Two novel metabolites of the dipeptidyl peptidase inhibitor sitagliptin (MK-0431, (2 R )-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3- a…”
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Discovery of a Novel Glucagon Receptor Antagonist N-[(4-{(1S)-1-[3-(3, 5-Dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the Treatment of Type II Diabetes by Xiong, Yusheng, Guo, Jian, Candelore, Mari R, Liang, Rui, Miller, Corey, Dallas-Yang, Qing, Jiang, Guoqiang, McCann, Peggy E, Qureshi, Sajjad A, Tong, Xinchun, Xu, Shiyao Sherrie, Shang, Jackie, Vincent, Stella H, Tota, Laurie M, Wright, Michael J, Yang, Xiaodong, Zhang, Bei B, Tata, James R, Parmee, Emma R

“…A potent, selective glucagon receptor antagonist 9m,…”
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DIFFERENCES IN THE PHARMACOKINETICS OF PEROXISOME PROLIFERATOR-ACTIVATED RECEPTOR AGONISTS IN GENETICALLY OBESE ZUCKER AND SPRAGUE-DAWLEY RATS: IMPLICATIONS OF DECREASED GLUCURONIDATION IN OBESE ZUCKER RATS by KIM, Mi-Sook, SUI WANG, ZHONGZHOU SHEN, KOCHANSKY, Christopher J, STRAUSS, John R, FRANKLIN, Ronald B, VINCENT, Stella H

“…Genetically obese Zucker rats exhibit symptoms similar to those of obese patients with insulin-resistance or Type II diabetes; therefore, they have been used…”
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Mechanistic Studies on the Metabolic Scission of Thiazolidinedione Derivatives to Acyclic Thiols by Reddy, Vijay Bhasker G, Karanam, Bindhu V, Gruber, Wendy L, Wallace, Michael A, Vincent, Stella H, Franklin, Ronald B, Baillie, Thomas A

“…Thiazolidinedione (TZD) derivatives have been reported to undergo metabolic activation of the TZD ring to produce reactive intermediates. In the case of…”
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SPECIES DIFFERENCES IN THE ELIMINATION OF A PEROXISOME PROLIFERATOR-ACTIVATED RECEPTOR AGONIST HIGHLIGHTED BY OXIDATIVE METABOLISM OF ITS ACYL GLUCURONIDE by KOCHANSKY, Christopher J, XIA, Yuan-Qing, SUI WANG, CATO, Brian, CREIGHTON, Mellissa, VINCENT, Stella H, FRANKLIN, Ronald B, REED, James R

“…A species difference was observed in the excretion pathway of 2-[[5,7-dipropyl-3-(trifluoromethyl)-1,2-benzisoxazol-6-yl]oxy]-2-methylpropanoic acid (MRL-C),…”
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Absorption, Metabolism, and Excretion of [14C]MK-0767 (2-Methoxy-5-(2,4-dioxo-5-thiazolidinyl)-N-[[4-(trifluoromethyl)phenyl] methyl]benzamide) in Humans by KOCHANSKY, Christopher J, RIPPLEY, Ronda K, FRANKLIN, Ronald B, WAGNER, John, YAN, Kerri X, HENGCHANG SONG, WALLACE, Michael A, DEAN, Dennis, JONES, Allen N, LASSETER, Kenneth, SCHWARTZ, Jules, VINCENT, Stella H

“…MK-0767 (KRP-297; 2-methoxy-5-(2,4-dioxo-5-thiazolidinyl)- N -[[4-(trifluoromethyl)phenyl] methyl]benzamide) is a thiazolidinedione (TZD)-containing dual…”
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SPECIES DIFFERENCES IN METABOLISM AND PHARMACOKINETICS OF A SPHINGOSINE-1-PHOSPHATE RECEPTOR AGONIST IN RATS AND DOGS: FORMATION OF A UNIQUE GLUTATHIONE ADDUCT IN THE RAT by REZA ANARI, M, CREIGHTON, Mellissa D, COLEMAN, John B, VINCENT, Stella H, EVANS, David C, NGUI, Jason S, TSCHIRRET-GUTH, Richard A, TEFFERA, Yohannes, DOSS, George A, WEI TANG, YU, Nathan X, CICCOTTO, Suzanne L, HOBRA, Donald F

“…The pharmacokinetics and metabolism of 1-(4-((4-phenyl-5-trifluoromethyl-2-thienyl)methoxy)benzyl)azetidine-3-carboxylic acid (MRL-A), a selective agonist for…”
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Overcoming Mutagenicity and Ion Channel Activity: Optimization of Selective Spleen Tyrosine Kinase Inhibitors by Ellis, J. Michael, Altman, Michael D, Bass, Alan, Butcher, John W, Byford, Alan J, Donofrio, Anthony, Galloway, Sheila, Haidle, Andrew M, Jewell, James, Kelly, Nancy, Leccese, Erica K, Lee, Sandra, Maddess, Matthew, Miller, J. Richard, Moy, Lily Y, Osimboni, Ekundayo, Otte, Ryan D, Reddy, M. Vijay, Spencer, Kerrie, Sun, Binyuan, Vincent, Stella H, Ward, Gwendolyn J, Woo, Grace H. C, Yang, Chiming, Houshyar, Hani, Northrup, Alan B

“…Development of a series of highly kinome-selective spleen tyrosine kinase (Syk) inhibitors with favorable druglike properties is described. Early leads were…”
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INDUCTION OF HEPATIC PHASE II DRUG-METABOLIZING ENZYMES BY 1,7-PHENANTHROLINE IN RATS IS ACCOMPANIED BY INDUCTION OF MRP3 by Wang, Sui, Hartley, Dylan P, Ciccotto, Suzanne L, Vincent, Stella H, Franklin, Ronald B, Kim, Mi-Sook

“…The purpose of the present study was to evaluate the effect of 1,7-phenanthroline (PH), which has been proposed to be a selective phase II enzyme inducer, on…”
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Discovery of Orally Bioavailable and Liver-Targeted Hypoxia-Inducible Factor Prolyl Hydroxylase (HIF-PHD) Inhibitors for the Treatment of Anemia by Liu, Ping, Wang, Liping, DuBois, Byron G, Colandrea, Vincent J, Liu, Rongqiang, Cai, Jiaqiang, Du, Xiaoxing, Quan, Weiguo, Morris, William, Bai, Jianwu, Bishwokarma, Bimjhana, Cheng, Mangeng, Piesvaux, Jennifer, Ray, Kallol, Alpert, Carla, Chiu, Chi-Sung, Zielstorff, Mark, Metzger, Joseph M, Yang, Liming, Leung, Dennis, Alleyne, Candice, Vincent, Stella H, Pucci, Vincenzo, Li, Xiaofang, Crespo, Alejandro, Stickens, Dominique, Hale, Jeffrey J, Ujjainwalla, Feroze, Sinz, Christopher J

“…We report herein the design and synthesis of a series of orally active, liver-targeted hypoxia-inducible factor prolyl hydroxylase (HIF-PHD) inhibitors for the…”
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IDENTIFICATION AND METABOLISM OF A NOVEL DIHYDROHYDROXY-S-GLUTATHIONYL CONJUGATE OF A PEROXISOME PROLIFERATOR-ACTIVATED RECEPTOR AGONIST, MK-0767 [(±)-5-[(2,4-DIOXOTHIAZOLIDIN-5-YL)METHYL]-2-METHOXY-N-[[(4-TRIFLUOROMETHYL) PHENYL]METHYL]BENZAMIDE], IN RATS by REDDY, Vijay Bhasker G, DOSS, George A, CREIGHTON, Mellissa, KOCHANSKY, Christopher J, VINCENT, Stella H, FRANKLIN, Ronald B, KARANAM, Bindhu V

“…MK-0767 [(±)-5-[(2,4-dioxothiazolidin-5-yl)methyl]-2-methoxy- N -[[(4-trifluoromethyl)phenyl]methyl]benzamide] is a novel thiazolidinedione-containing…”
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Modification of the pyridine moiety of non-peptidyl indole GnRH receptor antagonists by Simeone, Joseph P, Bugianesi, Robert L, Ponpipom, Mitree M, Yang, Yi Tien, Lo, Jane-Ling, Yudkovitz, Joel B, Cui, Jisong, Mount, George R, Ren, Rena Ning, Creighton, Mellissa, Mao, An-Hua, Vincent, Stella H, Cheng, Kang, Goulet, Mark T

“…The synthesis of a number of indole GnRH antagonists is described. Oxidation of the pyridine ring nitrogen, combined with alkylation at the two position, led…”
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In vitro metabolism of MK-0767 [(±)-5-[(2,4-dioxothiazolidin-5-yl)methyl]-2-methoxy-N-[[(4-trifluoromethyl)-phe nyl] methyl]benzamide], a peroxisome proliferator-activated receptor α/γ agonist. II. Identification of metabolites by liquid chromatography-tandem mass spectrometry by LIU, David Q, KARANAM, Bindhu V, DOSS, George A, SIDLER, Rick R, VINCENT, Stella H, HOP, Cornelis E. C. A

“…The in vitro metabolism of MK-0767 [(+/-)-5-[(2,4-dioxothiazolidin-5-yl) methyl]-2-methoxy-N-[[(4-trifluoromethyl)-phenyl] methyl]benzamide], a novel…”
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In vitro metabolism of MK-0767 [(±)-5-[(2,4-dioxothiazolidin-5-yl)methyl]-2-methoxy-N-[[(4-trifluoromethyl) phenyl]methyl]benzamide], a peroxisome proliferator-activated receptor α/γ agonist. I. Role of cytochrome P450, methyltransferases, flavin monooxygenases, and esterases by KARANAM, Bindhu V, HOP, Cornelis E. C. A, LIU, David Q, WALLACE, Mike, DEAN, Dennis, SATOH, Hiroya, KOMURO, Masakatsu, AWANO, Katsuya, VINCENT, Stella H

“…The metabolism of MK-0767, (+/-)-5-[(2,4-dioxothiazolidin-5-yl)methyl]-2-methoxy-N-[[(4-trifluoromethyl) phenyl]methyl]benzamide, a thiazolidinedione…”
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Orally bioavailable, indole-based nonpeptide GnRH receptor antagonists with high potency and functional activity by Ashton, Wallace T., Sisco, Rosemary M., Kieczykowski, Gerard R., Yang, Yi Tien, Yudkovitz, Joel B., Cui, Jisong, Mount, George R., Ren, Rena Ning, Wu, Tsuei-Ju, Shen, Xiaolan, Lyons, Kathryn A., Mao, An-Hua, Carlin, Josephine R., Karanam, Bindhu V., Vincent, Stella H., Cheng, Kang, Goulet, Mark T.

“…Stereospecific introduction of a methyl group to the indole-3-side chain enhanced activity in our tryptamine-derived series of GnRH receptor antagonists…”
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2-Arylindoles as gonadotropin releasing hormone (GnRH) antagonists: optimization of the tryptamine side chain by Young, Jonathan R., Huang, Song X., Walsh, Thomas F., Wyvratt, Matthew J., Yang, Yi Tien, Yudkovitz, Joel B., Cui, Jisong, Mount, George R., Ren, Rena Ning, Wu, Tsuei-Ju, Shen, Xiaolan, Lyons, Kathryn A., Mao, An-Hua, Carlin, Josephine R., Karanam, Bindhu V., Vincent, Stella H., Cheng, Kang, Goulet, Mark T.

“…A series of 2-arylindoles containing novel heteroaromatic substituents on the tryptamine tether, based on compound 1, was prepared and evaluated for their…”
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Simultaneous determination of MK-0767 and seven metabolites in rat urine using liquid chromatography/tandem mass spectrometry by Shen, Zhongzhou, Kochansky, Christopher, Bakhtiar, Ray, Franklin, Ronald B., Vincent, Stella H.

“…MK‐0767, 5‐[2,4‐dioxothiazolidin‐5‐yl)methyl]‐2‐methoxy‐N‐[[(4‐trifluoromethyl)phenyl]methyl]benzamide (I, Table 1), is a dual peroxisome…”
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The role of drug metabolism in drug discovery: a case study in the selection of an oxytocin receptor antagonist for development by Chiu, S H, Thompson, K A, Vincent, S H, Alvaro, R F, Huskey, S W, Stearns, R A, Pettibone, D J

“…Drug discovery is a process involving multiple disciplines and interests. During the research phase of drug discovery, usually a large number of compounds are…”
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