Zobrazeno 1 - 10
of 10
pro vyhledávání: '"Joseph L. Lambing"'
Autor:
Athiwat Hutchaleelaha, Robert M. Scarborough, Penglie Zhang, Susan Edwards, Yanhong Wu, Uma Sinha, Zhaozhong J. Jia, John Woolfrey, Wenrong Huang, Stanley J. Hollennbach, Joseph L. Lambing, Ann E. Arfsten, Yonghong Song, Bing-Yan Zhu
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:1229-1234
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 potent and selective fXa inhibitors with significantly improved hydrophilicity and in vitro a
Autor:
Joseph L. Lambing, Ann E. Arfsten, Bing-Yan Zhu, Gary Park, Stanley J. Hollenbach, Athiwat Hutchaleelaha, Erick A. Goldman, Susan Edwards, Robert M. Scarborough, Jingmei Zuckett, Zhaozhong J. Jia, Bao Liang, Uma Sinha, Penglie Zhang
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:983-987
Anthranilamides 4 and 5 were designed and synthesized as selective and orally bioavailable factor Xa inhibitors. Structural modifications aimed at lowering their lipophilicity were performed at the central phenyl ring and at the S4 binding biphenyl r
Publikováno v:
Journal of the American College of Cardiology. 61(10)
To evaluate the effects of the anticoagulant betrixaban on individual heart rate-corrected QT (QTcI).Ninety-six healthy adults were randomly assigned to single-dose betrixaban 80 and 140 mg (therapeutic and supratherapeutic doses, respectively), plac
Autor:
Lane A. Clizbe, Anjali Pandey, Robert M. Scarborough, Athiwat Hutchaleelaha, Zhaozhong J. Jia, Gary Park, Erick A. Goldman, James Kanter, Lingyan Wang, Yanhong Wu, Ting Su, Gary Probst, Wenhao Li, Susan Edwards, Jingmei Fan, Paul W. Wong, Stanley J. Hollenbach, Uma Sinha, Wenrong Huang, Bauer Shawn M, Joseph L. Lambing, Ann E. Arfsten, Yonghong Song, Penglie Zhang, Bing-Yan Zhu, Bao Liang, John Woolfrey
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(8)
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 highly potent, selective, efficacious and orally bioavailable direct factor Xa inhibitors was di
Autor:
Mukund Mehrotra, Robert M. Scarborough, Gary L. Park, Deborah Volkots, Jack W. Rose, Joseph L. Lambing, Anjali Pandey, Julie Anne Heath, Joseph M. Seroogy, Stanley J. Hollenbach, Mark S. Smyth, Lisa Nannizzi-Alaimo
Publikováno v:
Journal of medicinal chemistry. 47(8)
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 scaffold as a template. We describe here our investigation of a variety of templates including
Autor:
Uma Sinha, Penglie Zhang, Erick A. Goldman, John Woolfrey, Yanhong Wu, Ting Su, Jingmei Zuckett, Bauer Shawn M, Lane A. Clizbe, Wenhao Li, Athiwat Hutchaleelaha, Stanley J. Hollenbach, Wenrong Huang, Zhaozhong J. Jia, Robert M. Scarborough, Joseph L. Lambing, Ann E. Arfsten, Yonghong Song, Bing-Yan Zhu
Publikováno v:
Bioorganicmedicinal chemistry letters. 14(9)
A class of N,N-dialkylated 4-(4-arylsulfonylpiperazine-1-carbonyl)-benzamidines and 4-((4-arylsulfonyl)-2-oxo-piperazin-1-ylmethyl)-benzamidines has been discovered as potent factor Xa inhibitors with desirable in vitro and in vivo anticoagulant acti
Autor:
Jingmei Zuckett, Joseph L. Lambing, Ann E. Arfsten, Bing-Yan Zhu, John Woolfrey, Stanley J. Hollenbach, Bao Liang, Robert M. Scarborough, Athiwat Hutchaleelaha, Zhaozhong J. Jia, Susan Edwards, Uma Sinha, Penglie Zhang
Publikováno v:
Bioorganicmedicinal chemistry letters. 14(4)
Compound 2 containing an aminomethylbenzoyl moiety as the S4 binding motif was synthesized in order to modulate hydrophlicity of anthranilamide-based factor Xa inhibitors with substituted biphenyl P4 groups. Structure–activity relationship studies
Autor:
Jack W. Rose, Deborah Volkots, Athiwat Hutchaleelaha, Keith Abe, Anjali Pandey, Neill A. Giese, Joseph M. Seroogy, Stanley J. Hollenbach, Robert M. Scarborough, Joseph L. Lambing, Jin-Chen Yu
Publikováno v:
Journal of medicinal chemistry. 45(17)
We have previously found that the 4-[4-(N-substituted carbamoyl)-1-piperazinyl]-6,7-dimethoxyquinazolines can function as potent and selective inhibitors of platelet-derived growth factor receptor (PDGFR) phosphorylation. A series of highly potent, s
Autor:
Todd Lorenz, Christine Ye, Athiwat Hutchaleelaha, Daniel D. Gretler, Joseph L. Lambing, Yonghong Song
Publikováno v:
Blood. 120:2266-2266
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 medically ill patients (APEX Study). Mass balance, metabolite profile and interaction with maj
Autor:
Joseph L. Lambing, Lance C. Foster, Tuongvan T. Tran, Mark R. Barnes, Bob In-yu Yang, David J. Kearney
Publikováno v:
Biochemical and biophysical research communications. 151(2)
The cofactor activation of the apoenzyme of pig heart cytosolic aspartate aminotransferase was studied in various buffers. Cationic buffers are shown to allow maximal reconstitution in the pH range of 5.0 to 9.0. Anionic buffers made up of mono- and