Details

Autor(en) / Beteiligte

• 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

Titel

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

Ist Teil von

• Bioorganic & medicinal chemistry letters, 2009-04, Vol.19 (8), p.2179-2185

Erscheinungsjahr

2009

Link zum Volltext

Quelle

Elsevier ScienceDirect Journals Complete

Beschreibungen/Notizen

• 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 discovered. These compounds were screened in hERG binding assays to examine the effects of substitution groups on the hERG channel affinity. From the leading compounds, betrixaban (compound 11, PRT054021) has been selected as the clinical candidate for development.