Search Results - "TRAN, Scott B"
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The synthesis of [1‐14C]2‐(1H‐tetrazol‐5‐yl)acetic acid
Published in Journal of labelled compounds & radiopharmaceuticals (01-01-2017)“…Tetrazoles are a common heterocyclic functionality in many biologically active molecules. [1‐14C]2‐(1H‐Tetrazol‐5‐yl)acetic acid was required as an…”
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The syntheses of isotopically labelled CB-1 antagonists for the treatment of obesity
Published in Journal of labelled compounds & radiopharmaceuticals (01-12-2016)“…BMS‐725519, BMS‐811064, and BMS‐812204 are potent and selective central cannabinoid receptor antagonists that have been investigated for the treatment of human…”
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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
Published in Journal of labelled compounds & radiopharmaceuticals (30-05-2016)“…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
Published in Drug metabolism and disposition (01-05-2011)“…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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The synthesis of 14C-labeled, 13CD2-labeled saxagliptin, and its 13CD2-labeled 5-hydroxy metabolite
Published in Journal of labelled compounds & radiopharmaceuticals (01-03-2014)“…14C‐labeled saxagliptin, 13CD2‐labeled saxagliptin, and its 13CD2‐labeled 5‐hydroxy metabolite were synthesized to further support development of the compound…”
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Disposition of [1'-14C]Stavudine after Oral Administration to Humans
Published in Drug metabolism and disposition (01-04-2010)“…The disposition of stavudine, a potent and orally active nucleoside reverse transcriptase inhibitor, was investigated in six healthy human subjects. Before…”
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An improved synthesis of [2-14C]2, 5-dichloropyrimidine
Published in Journal of labelled compounds & radiopharmaceuticals (30-06-2012)“…A previously described, five‐step synthesis of [2‐14C]2, 5‐dichloropyrimidine was based on condensation of [14C]urea with an acetal, followed by bromination,…”
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A novel synthesis of [2-14C]2,5-dichloropyrimidine
Published in Journal of labelled compounds & radiopharmaceuticals (01-11-2011)“…[2‐14 C]2,5‐dichloropyrimidine is a useful reagent for labeling biologically active compounds for use in hepatocyte transport studies, protein covalent…”
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Synthesis of [13C4]Baraclude® (entecavir)
Published in Journal of labelled compounds & radiopharmaceuticals (15-09-2009)“…Entecavir, labeled as 1H‐[13C4]purin‐6(9H)‐one, was prepared from commercially available [13C]guanidine HCl, 1 and diethyl [1,2,3‐13C3]malonate, 2. The…”
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The syntheses and in vitro biotransformation studies of [14C]apixaban, a highly potent, selective, efficacious and orally bioavailable inhibitor of blood coagulation Factor Xa
Published in Journal of labelled compounds & radiopharmaceuticals (30-06-2011)“…Apixaban is a potent inhibitor of blood coagulation Factor Xa in the late stages of development. [14C]apixaban was synthesized with the 14C label in the two…”
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Synthesis of lead LFA-1 antagonist [14C]spyrocyclic hydantoin
Published in Journal of labelled compounds & radiopharmaceuticals (30-05-2009)“…Radiolabelled drug lead candidate leukocyte function‐associated antigen 1 antagonist [14C]spyrocyclic hydantoin:…”
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The 14C, 13C, and 15N syntheses of a potent VEGFR-2 kinase inhibitor, Brivanib, and its prodrug, Brivanib Alaninate
Published in Journal of labelled compounds & radiopharmaceuticals (30-05-2011)“…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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The synthesis of (14)C-labeled, (13)CD2-labeled saxagliptin, and its (13)CD2-labeled 5-hydroxy metabolite
Published in Journal of labelled compounds & radiopharmaceuticals (01-03-2014)“…(14)C-labeled saxagliptin, (13) CD2-labeled saxagliptin, and its (13) CD2-labeled 5-hydroxy metabolite were synthesized to further support development of the…”
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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
Published in Journal of labelled compounds & radiopharmaceuticals (30-05-2011)“…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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