2-Aminomethylphenylamine as a novel scaffold for factor Xa inhibitor

We have been researching orally active factor Xa inhibitor for a long time. We explored the new diamine linker using effective ligands to obtain a new attractive original scaffold 2-aminomethylphenylamine derivative. Compound 1D showed very strong in vitro and in vivo factor Xa inhibitory activity,...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2011-03, Vol.19 (5), p.1623-1642
Hauptverfasser:	Mochizuki, Akiyoshi, Nagata, Tsutomu, Kanno, Hideyuki, Suzuki, Makoto, Ohta, Toshiharu
Format:	Artikel
Sprache:	eng
Schlagworte:	amines Aniline Compounds - chemical synthesis Aniline Compounds - chemistry Animals Anticoagulant Biological and medical sciences Blood Coagulation Factor Inhibitors - chemical synthesis Blood Coagulation Factor Inhibitors - chemistry Blood. Blood coagulation. Reticuloendothelial system chemistry Crystallography, X-Ray enzyme inhibitors Factor Xa Factor Xa inhibitor Factor Xa Inhibitors Haplorhini Humans in vitro studies in vivo studies Inhibitory Concentration 50 Ligands Medical sciences Molecular Structure monkeys New diamine linker Pharmacology. Drug treatments Rats
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Beschreibung
Zusammenfassung:	We have been researching orally active factor Xa inhibitor for a long time. We explored the new diamine linker using effective ligands to obtain a new attractive original scaffold 2-aminomethylphenylamine derivative. Compound 1D showed very strong in vitro and in vivo factor Xa inhibitory activity, as well as favorable PK profiles in po administration to monkeys.
ISSN:	0968-0896 1464-3391
DOI:	10.1016/j.bmc.2011.01.035