Search Results - "LAMBING, Joseph L"

Discovery of betrixaban (PRT054021), N-(5-chloropyridin-2-yl)-2-(4-( N, N-dimethylcarbamimidoyl)benzamido)-5-methoxybenzamide, a highly potent, selective, and orally efficacious factor Xa inhibitor by Zhang, Penglie, Huang, Wenrong, Wang, Lingyan, Bao, Liang, Jia, Zhaozhong J., Bauer, Shawn M., Goldman, Erick A., Probst, Gary D., Song, Yonghong, Su, Ting, Fan, Jingmei, Wu, Yanhong, Li, Wenhao, Woolfrey, John, Sinha, Uma, Wong, Paul W., Edwards, Susan T., Arfsten, Ann E., Clizbe, Lane A., Kanter, James, Pandey, Anjali, Park, Gary, Hutchaleelaha, Athiwat, Lambing, Joseph L., Hollenbach, Stanley J., Scarborough, Robert M., Zhu, Bing-Yan

“…Systematic SAR studies of in vitro factor Xa inhibitory activity around compound 1 were performed by modifying each of the three phenyl rings. A class of…”
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Identification of Orally Active, Potent, and Selective 4-Piperazinylquinazolines as Antagonists of the Platelet-Derived Growth Factor Receptor Tyrosine Kinase Family by Pandey, Anjali, Volkots, Deborah L, Seroogy, Joseph M, Rose, Jack W, Yu, Jin-Chen, Lambing, Joseph L, Hutchaleelaha, Athiwat, Hollenbach, Stanley J, Abe, Keith, Giese, Neill A, Scarborough, Robert M

“…We have previously found that the 4-[4-(N-substituted carbamoyl)-1-piperazinyl]-6,7-dimethoxyquinazolines can function as potent and selective inhibitors of…”
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ABSENCE OF QTC PROLONGATION WITH BETRIXABAN: A RANDOMIZED, DOUBLE-BLIND, PLACEBO- AND POSITIVE-CONTROLLED THOROUGH ECG STUDY by Sinha, Uma, Morganroth, Joel, Gretler, Daniel D, Hollenbach, Stanley J, Lambing, Joseph L

“…To evaluate the effects of betrixaban on individual heart rate-corrected QT duration (QTcl), 96 healthy adults were randomly assigned to single-dose betrixaban…”
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Absence of QTc prolongation with betrixaban: a randomized, double-blind, placebo- and positive-controlled thorough ECG study by Morganroth, Joel, Gretler, Daniel D, Hollenbach, Stanley J, Lambing, Joseph L, Sinha, Uma

“…To evaluate the effects of the anticoagulant betrixaban on individual heart rate-corrected QT (QTcI). Ninety-six healthy adults were randomly assigned to…”
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1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides as potent factor xa inhibitors. Part 3: Design, synthesis and sar of orally bioavailable benzamidine-P4 inhibitors by JIA, Zhaozhong J, YANHONG WU, HOLLENNBACH, Stanley J, LAMBING, Joseph L, SCARBOROUGH, Robert M, ZHU, Bing-Yan, WENRONG HUANG, PENGLIE ZHANG, YONGHONG SONG, WOOLFREY, John, SINHA, Uma, ARFSTEN, Ann E, EDWARDS, Susan T, HUTCHALEELAHA, Athiwat

“…Using N,N-dialkylated benzamidines as the novel P4 motifs, we have designed and synthesized a class of 1-(2-naphthyl)-1H-pyrazole-5-carboxylamides as highly…”
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Design, synthesis, and SAR of anthranilamide-based factor Xa inhibitors incorporating substituted biphenyl P4 motifs by PENGLIE ZHANG, LIANG BAO, LAMBING, Joseph L, HOLLENBACH, Stanley J, SCARBOROUGH, Robert M, ZHU, Bing-Yan, ZUCKETT, Jingmei F, GOLDMAN, Erick A, JIA, Zhaozhong J, ARFSTEN, Ann, EDWARDS, Susan, SINHA, Uma, HUTCHALEELAHA, Athiwat, PARK, Gary

“…Anthranilamides 4 and 5 were designed and synthesized as selective and orally bioavailable factor Xa inhibitors. Structural modifications aimed at lowering…”
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Design, synthesis, and SAR of anthranilamide-based factor Xa inhibitors with improved functional activity by PENGLIE ZHANG, LIANG BAO, HOLLENBACH, Stanley J, SCARBOROUGH, Robert M, ZHU, Bing-Yan, ZUCKETT, Jingmei F, JIA, Zhaozhong J, WOOLFREY, John, ARFSTEN, Ann, EDWARDS, Susan, SINHA, Uma, HUTCHALEELAHA, Athiwat, LAMBING, Joseph L

“…Compound 2 containing an aminomethylbenzoyl moiety as the S4 binding motif was synthesized in order to modulate hydrophlicity of anthranilamide-based factor Xa…”
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Discovery of Novel 2,8-Diazaspiro[4.5]decanes as Orally Active Glycoprotein IIb-IIIa Antagonists by Mehrotra, Mukund M., Heath, Julie A., Smyth, Mark S., Pandey, Anjali, Rose, Jack W., Seroogy, Joseph M., Volkots, Deborah L., Nannizzi-Alaimo, Lisa, Park, Gary L., Lambing, Joseph L., Hollenbach, Stanley J., Scarborough, Robert M.

“…In our efforts to develop orally active GPIIb-IIIa antagonists with improved pharmaceutical properties, we have utilized a novel 2,8-diazaspiro[4.5]decane…”
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N, N-Dialkylated 4-(4-arylsulfonylpiperazine-1-carbonyl)-benzamidines and 4-((4-arylsulfonyl)-2-oxo-piperazin-1-ylmethyl)-benzamidines as potent factor Xa inhibitors by JIA, Zhaozhong J, TING SU, WENRONG HUANG, WOOLFREY, John, SINHA, Uma, ARFSTEN, Ann E, HUTCHALEELAHA, Athiwat, HOLLENBACH, Stanley J, LAMBING, Joseph L, SCARBOROUGH, Robert M, ZHU, Bing-Yan, ZUCKETT, Jingmei F, YANHONG WU, GOLDMAN, Erick A, WENHAO LI, PENGLIE ZHANG, CLIZBE, Lane A, YONGHONG SONG, BAUER, Shawn M

“…A class of N,N-dialkylated 4-(4-arylsulfonylpiperazine-1-carbonyl)-benzamidines and 4-((4-arylsulfonyl)-2-oxo-piperazin-1-ylmethyl)-benzamidines has been…”
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1-(2-Naphthyl)-1 H -pyrazole-5-carboxylamides as potent factor Xa inhibitors. Part 3: Design, synthesis and SAR of orally bioavailable benzamidine-P4 inhibitors by Jia, Zhaozhong J., Wu, Yanhong, Huang, Wenrong, Zhang, Penglie, Song, Yonghong, Woolfrey, John, Sinha, Uma, Arfsten, Ann E., Edwards, Susan T., Hutchaleelaha, Athiwat, Hollennbach, Stanley J., Lambing, Joseph L., Scarborough, Robert M., Zhu, Bing-Yan

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Metabolism and Disposition of Betrixaban and Its Lack of Interaction with Major CYP Enzymes by Hutchaleelaha, Athiwat, Ye, Christine, Song, Yonghong, Lorenz, Todd, Gretler, Daniel, Lambing, Joseph L

“…Abstract 2266 Betrixaban is a once daily oral Factor Xa inhibitor being investigated in a Phase 3 clinical trial to prevent venous thromboembolism in acute…”
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Discovery of betrixaban (PRT054021), N-(5-chloropyridin-2-yl)-2-(4-(N,N-dimethylcarbamimidoyl)benzamido )-5-metho xybenzamide, a highly potent, selective, and orally efficacious factor Xa inhibitor by Zhang, Penglie, Huang, Wenrong, Wang, Lingyan, Bao, Liang, Jia, Zhaozhong J, Bauer, Shawn M, Goldman, Erick A, Probst, Gary D, Song, Yonghong, Su, Ting, Fan, Jingmei, Wu, Yanhong, Li, Wenhao, Woolfrey, John, Sinha, Uma, Wong, Paul W, Edwards, Susan T, Arfsten, Ann E, Clizbe, Lane A, Kanter, James, Pandey, Anjali, Park, Gary, Hutchaleelaha, Athiwat, Lambing, Joseph L, Hollenbach, Stanley J, Scarborough, Robert M, Zhu, Bing-Yan

“…Systematic SAR studies of in vitro factor Xa inhibitory activity around compound 1 were performed by modifying each of the three phenyl rings. A class of…”
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Buffers for the reconstitution of aspartate aminotransferase by Lambing, J L, Foster, L C, Kearney, D J, Barnes, M R, Tran, T T, Yang, B I

“…The cofactor activation of the apoenzyme of pig heart cytosolic aspartate aminotransferase was studied in various buffers. Cationic buffers are shown to allow…”
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