Search Results - "LAGO, Michael"

Metabolism and Disposition of Dasatinib after Oral Administration to Humans by Lisa J. Christopher, Donghui Cui, Chiyuan Wu, Roger Luo, James A. Manning, Samuel J. Bonacorsi, Michael Lago, Alban Allentoff, Francis Y. F. Lee, Betty McCann, Susan Galbraith, Donald P. Reitberg, Kan He, Anthony Barros, Jr, Anne Blackwood-Chirchir, W. Griffith Humphreys, Ramaswamy A. Iyer

“…SPRYCEL (dasatinib, BMS-354825; Bristol-Myers Squibb, Princeton, NJ), a multiple kinase inhibitor, is currently approved to treat chronic myelogenous leukemia…”
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A validated LC–MS/MS assay for the simultaneous determination of the anti-leukemic agent dasatinib and two pharmacologically active metabolites in human plasma: Application to a clinical pharmacokinetic study by Furlong, Michael T., Agrawal, Shruti, Hawthorne, Dara, Lago, Michael, Unger, Steve, Krueger, Linda, Stouffer, Bruce

“…► Dasatinib and active metabolites LC–MS/MS assay validation. ► Application of the assay to a human pharmacokinetic study. ► Active metabolite exposure in…”
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Spinal cord injury triggers an intrinsic growth-promoting state in nociceptors by Bedi, Supinder S, Lago, Michael T, Masha, Luke I, Crook, Robyn J, Grill, Raymond J, Walters, Edgar T

“…Although most investigations of the mechanisms underlying chronic pain after spinal cord injury (SCI) have examined the central nervous system (CNS), recent…”
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Lacteal Secretion, Fetal and Maternal Tissue Distribution of Dasatinib in Rats by KAN HE, LAGO, Michael W, IYER, Ramaswamy A, SHYU, Wen-Chyi, HUMPHREYS, William G, CHRISTOPHER, Lisa J

“…Dasatinib [ N -(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-5-thiazolecarboxamide; BMS-354825] is a potent…”
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Biotransformation of [14C]Dasatinib: In Vitro Studies in Rat, Monkey, and Human and Disposition after Administration to Rats and Monkeys by Lisa J. Christopher, Donghui Cui, Wenying Li, Anthony Barros, Jr, Vinod K. Arora, Haiying Zhang, Lifei Wang, Donglu Zhang, James A. Manning, Kan He, Anthony M. Fletcher, Marc Ogan, Michael Lago, Samuel J. Bonacorsi, W. Griffith Humphreys, Ramaswamy A. Iyer

“…This study describes the in vitro metabolism of [ 14 C]dasatinib in liver tissue incubations from rat, monkey, and human and the in vivo metabolism in rat and…”
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The 14C, 13C, and 15N syntheses of a potent VEGFR-2 kinase inhibitor, Brivanib, and its prodrug, Brivanib Alaninate by Tran, Scott B., Lago, Michael W., Tian, Yuan, Gong, Sharon X., Batra, Indu, Allentoff, Alban J., Maxwell, Brad D., Bonacorsi, Samuel J., Ogan, Marc, Rinehart, J. Kent, Balasubramanian, Balu

“…The interruption of tyrosine kinase vascular endothelial growth factor receptor‐2 (VEGFR‐2) signaling by the binding of a small molecule inhibitor, for…”
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Synthesis of 14C-labeled and 13C-,15N-labeled dasatinib and its piperazine N-dealkyl metabolite by Allentoff, Alban J., Lago, Michael W., Ogan, Marc, Chen, Bang-Chi, Zhao, Rulin, Iyer, Ramaswarmy A., Christopher, Lisa J., Rinehart, J. Kent, Balasubramanian, Balu, Bonacorsi Jr, Samuel J.

“…Dasatinib (SPRYCEL®) is a multiple kinase inhibitor approved for the treatment of chronic myelogenous leukemia and Philadelphia chromosome‐positive acute…”
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Synthesis of 13C6-labeled Reyataz™ (BMS-232632) by Burrell, Richard C., Lago, Michael W., Luke, George M., Rinehart, J. Kent

“…An efficient synthesis of 13C6‐labeled Reyataz™ (BMS‐232632) is described. 13C6‐labeled Reyataz™ was synthesized in eight steps from commercially available…”
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Benzazepinone calcium channel blockers. 2. Structure activity and drug metabolism studies leading to potent antihypertensive agents. Comparison with benzothiazepinones by Floyd, David M, Kimball, S. David, Krapcho, John, Das, Jagabandhu, Turk, Chester F, Moquin, Robert V, Lago, Michael W, Duff, Keith J, Lee, Ving G

“…As part of a program to discover potent antihypertensive analogues of diltiazem (3a), we prepared 1-benzazepin-2-ones (4). Benzazepinones competitively…”
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Benzazepinone calcium channel blockers. 3. Synthesis and structure-activity studies of 3-alkylbenzazepinones by Das, Jagabandhu, Floyd, David M, Kimball, S. David, Duff, Keith J, Lago, Michael W, Moquin, Robert V, Lee, Ving G, Gougoutas, Jack Z, Vu Chi Truc

“…As part of a program aimed at identifying novel analogues of diltiazem, we developed several synthetic routes for 3-alkylbenzazepinones, both in racemic and…”
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The syntheses of [14C]BMS-823778 for use in a human ADME clinical study and of [13CD3 13CD2]BMT-094817, a stable-isotope labeled standard of a newly detected human metabolite by Maxwell, Brad D., Tran, Scott B., Lago, Michael, Li, Jun, Bonacorsi Jr, Samuel J.

“…Type 2 diabetes is a significant worldwide health problem. To support the development of BMS‐823778 as an inhibitor of 11β‐hydroxysteroid dehydrogenase type 1…”
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Metabolism and Disposition of [14 C]Brivanib Alaninate after Oral Administration to Rats, Monkeys, and Humans by JIACHANG GONG, JINPING GAN, TRAN, Scott B, LYER, Ramaswamy A, CACERES-CORTES, Janet, CHRISTOPHER, Lisa J, ARORA, Vinod, MASSON, Eric, WILLIAMS, Daphne, PURSLEY, Janice, ALLENTOFF, Alban, LAGO, Michael

“…Brivanib [(R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[1,2,4]triazin-6-yloxy)propan-2-ol, BMS-540215] is a potent and selective dual inhibitor…”
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Benzazepinone calcium channel blockers. 5. Effects on antihypertensive activity associated with N1 and aromatic substituents by Das, Jagabandhu, Floyd, David M, Kimball, S. David, Duff, Keith J, Lago, Michael W, Krapcho, John, White, Ronald E, Ridgewell, Richard E, Obermeier, Mary T

“…We have shown that the pyrrolidinylmethyl substituent on the lactam nitrogen (N1) of benzazepinone and benzothiazepinone calcium channel blocking agents is…”
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CYP3A4-Mediated Ester Cleavage as the Major Metabolic Pathway of the Oral Taxane 3'-tert-Butyl-3'-N-tert-butyloxycarbonyl-4-deacetyl-3'-dephenyl-3'-N-debenzoyl-4-O-methoxycarbonyl-paclitaxel (BMS-275183) by DONGLU ZHANG, LY, Van T, LAGO, Michael, YUAN TIAN, JINPING GAN, HUMPHREYS, W. Griffith, NILGÜN CÖMEZOGLU, S

“…3'-tert-Butyl-3'-N-tert-butyloxycarbonyl-4-deacetyl-3'-dephenyl-3'-N-debenzoyl-4-O-methoxycarbonyl-paclitaxel (BMS-275183) is an orally available taxane analog…”
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CYP3A4-Mediated Ester Cleavage as the Major Metabolic Pathway of the Oral Taxane 3′-tert-Butyl-3′-N-tert-butyloxycarbonyl-4-deacetyl-3′-dephenyl-3′-N-debenzoyl-4-O-methoxycarbonyl-paclitaxel (BMS-275183) by Donglu Zhang, Van T. Ly, Michael Lago, Yuan Tian, Jinping Gan, W. Griffith Humphreys, S. Nilgün Çömezoğlu

“…3′- tert -Butyl-3′- N - tert -butyloxycarbonyl-4-deacetyl-3′-dephenyl-3′- N -debenzoyl-4- O -methoxycarbonyl-paclitaxel (BMS-275183) is an orally…”
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Microsomal Triglyceride Transfer Protein by Jamil, Haris, Dickson, John K., Chu, Ching-Hsuen, Lago, Michael W., Rinehart, J.Kent, Biller, Scott A., Gregg, Richard E., Wetterau, John R.

“…Microsomal triglyceride transfer protein (MTP) is a lipid transfer protein that is required for the assembly and secretion of very low density lipoproteins by…”
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The 14 C, 13 C, and 15 N syntheses of a potent VEGFR‐2 kinase inhibitor, Brivanib, and its prodrug, Brivanib Alaninate by Tran, Scott B., Lago, Michael W., Tian, Yuan, Gong, Sharon X., Batra, Indu, Allentoff, Alban J., Maxwell, Brad D., Bonacorsi, Samuel J., Ogan, Marc, Rinehart, J. Kent, Balasubramanian, Balu

“…Abstract The interruption of tyrosine kinase vascular endothelial growth factor receptor‐2 (VEGFR‐2) signaling by the binding of a small molecule inhibitor,…”
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Synthesis of 14 C‐labeled and 13 C‐, 15 N‐labeled dasatinib and its piperazine N ‐dealkyl metabolite by Allentoff, Alban J., Lago, Michael W., Ogan, Marc, Chen, Bang‐Chi, Zhao, Rulin, Iyer, Ramaswarmy A., Christopher, Lisa J., Rinehart, J. Kent, Balasubramanian, Balu, Bonacorsi, Samuel J.

“…Abstract Dasatinib (SPRYCEL ® ) is a multiple kinase inhibitor approved for the treatment of chronic myelogenous leukemia and Philadelphia chromosome‐positive…”
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Synthesis of13C6-labeled Reyataz? (BMS-232632) by Burrell, Richard C., Lago, Michael W., Luke, George M., Rinehart, J. Kent

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1-Benzazepin-2-one calcium channel blockers--VI. Receptor-binding model and possible relationship to desmethoxyverapamil by Kimball, S D, Hunt, J T, Barrish, J C, Das, J, Floyd, D M, Lago, M W, Lee, V G, Spergel, S H, Moreland, S, Hedberg, S A

“…We have prepared a series of potent antihypertensive 1-benzazepin-2-one calcium channel blockers (CCBs) 1 that are structurally related to diltiazem 2…”
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