308845-92-3Relevant academic research and scientific papers
Design, synthesis, and biological evaluation of pyrazinones containing novel P1 needles as inhibitors of TF/VIIa
Trujillo, John I.,Huang, Horng-Chih,Neumann, William L.,Mahoney, Matthew W.,Long, Scott,Huang, Wei,Garland, Danny J.,Kusturin, Carrie,Abbas, Zaheer,South, Michael S.,Reitz, David B.
, p. 4568 - 4574 (2008/02/11)
Herein is described the design, synthesis, and enzymatic activity of a series of substituted pyrazinones as inhibitors of the TF/VIIa complex. These inhibitors were designed to explore replacement and variation of the P1 amidine described previously [J. Med. Chem. 2003, 46, 4050]. The P1 needle replacements were selected based upon their reduced basicity compared to the parent phenyl amidine (pKa ～ 12). A contributing factor towards the oral bioavailability of a compound is the ionization state of the compound in the intestinal tract. The desired outcome of the study was to identify an orally bioavailable TF-VIIa inhibitor.
Substituted polycyclic aryl and heteroaryl pyrazinones useful for selective inhibition of the coagulation cascade
-
, (2012/01/30)
The invention relates to substituted polycyclic aryl and heteroaryl pyrazinone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.
