368426-78-2Relevant articles and documents
FACTOR XIIa INHIBITORS
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Paragraph 00248-00249, (2019/11/19)
This invention relates to compounds of formula (I). The compounds of formula (I) are modulators of Factor XII, specifically Factor XIIa. The compounds are inhibitors of Factor XIIa and may be useful as anticoagulants. The compounds of formula (I) may be used in methods of treatment (or prevention) of blood disorders related to bleeding or coagulation.
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.
THROMBIN INHIBITORS
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, (2008/06/13)
Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: or a pharmaceutically acceptable salt thereof, wherein b is N Y 1 or O; c is CY 2 or N; d is CY 2; e is CY 1 or N; f is CY 1 or N; g is CY 1 or N; Y 1 is hydrogen, C 1-4 alkyl, or halogen; Y 2 is hydrogen, C 1-4 alkyl, C 3-7 cycloalkyl, halogen, NH 2, OH or C 1-4 alkoxy;A is and W, X, Z, R 3, R 4 and R 5 are defined in the specification.