219671-91-7Relevant academic research and scientific papers
HETEROARYL DERIVATIVES AND USES THEREOF
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Paragraph 0610; 0611, (2014/05/20)
The present invention relates to antimalarial compounds and their use against protozoa of the genus Plasmodium, including drug-resistant Plasmodia strains. This invention further relates to compositions containing such compounds and a process for making the compounds.
Efforts toward oral bioavailability in factor VIIa inhibitors
Vijaykumar, Dange,Rai, Roopa,Shaghafi, Michael,Ton, Tony,Torkelson, Steve,Leahy, Ellen M.,Riggs, Jennifer R.,Hu, Huiyong,Sprengeler, Paul A.,Shrader, William D.,O'Bryan, Colin,Cabuslay, Ronnell,Sanford, Ellen,Gjerstadt, Erik,Liu, Liang,Sukbuntherng, Juthamas,Young, Wendy B.
, p. 3829 - 3832 (2007/10/03)
Efforts toward developing orally bioavailable factor VIIa inhibitors starting from parenteral lead compound 1 are described. SAR resulted in improved physicochemical properties, leading to enhanced oral absorption in rat.
2-(2-HYDROXYBIPHENYL-3-YL)-1H-BENZOIMIDAZOLE-5-CARBOXAMIDINE DERIVATIVES AS FACTOR VIIA INHIBITORS
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Page 69, (2008/06/13)
The present invention relates to novel inhibitors of Factors VIIa, IXa, Xa, XIa, in particular Factor VIIa, pharmaceutical compositions comprising these inhibitors, and methods for using these inhibitors for treating or preventing thromboembolic disorders, cancer or rheumatoid arthritis. Processes for preparing these inhibitors are also disclosed.
2-'5-(5-CARBAMIMIDOYL-1H-HETEROARYL)-6-HYDROXYBIPHENYL-3-YL!- CARBOXYLIC ACID DERIVATIVES AS FACTOR VIIA INHIBITORS
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Page/Page column 26; 31, (2010/02/07)
The present invention relates to novel inhibitors of Factors VIIa, IXa, Xa, XIa, in particular Factor VIIa, pharmaceutical compositions comprising these inhibitors, and methods for using these inhibitors for treating or preventing thromboembolic disorders. Processes for preparing these inhibitors are also disclosed.
2- [5- (5-carbamimidoyl-1H-heteroaryl)-6-hydroxybiphenyl-3-yl]-succinic acid derivatives as factor viia inhibitors
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, (2008/06/13)
The present invention relates to novel inhibitors of Factors VIIa, IXa, Xa, XIa, in particular Factor VIIa, pharmaceutical compositions comprising these inhibitors, and methods for using these inhibitors for treating or preventing thromboembolic disorders. Processes for preparing these inhibitors are also disclosed.
Amido-(propyl and allyl)-hydroxybenzamidines: Development of achiral inhibitors of factor Xa
Gong, Yong,Pauls, Henry W.,Spada, Alfred P.,Czekaj, Mark,Liang, Guyan,Chu, Valeria,Colussi, Dennis J.,Brown, Karen D.,Gao, Jingbo
, p. 217 - 221 (2007/10/03)
The design, synthesis and SAR of amido-(propyl and allyl)-hydroxybenzamidine coagulation factor Xa inhibitors is described. These achiral inhibitors are selective for fXa vis a vis structurally related serine proteases and are readily prepared in 6-7 linear steps. The most potent member 9j (fXa K(i) = 0.75 nM) is selective (>1000-fold) and an effective anticoagulant in mammalian plasma. (C) 2000 Elsevier Science Ltd. All rights reserved.
