293329-60-9Relevant academic research and scientific papers
Substituted polycyclic aryl and heteroaryl pyrimidinones useful for selective inhibition of the coagulation cascade
-
Page/Page column 109, (2010/01/31)
The invention relates to substituted polycyclic aryl and heteroaryl pyrimidinone 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.
1,3,4-oxadiazole derivatives and process for producing the same
-
, (2008/06/13)
Oxadiazole derivatives represented by formula (I): (wherein R1represents a hydrogen atom or an amino-protective group; R2, R3, and R4each independently represents an alkyl group, a cycloalkyl group, a phenyl gro
PYRIMIDINE DERIVATIVES AND PROCESS FOR THE PREPARATION THEREOF
-
, (2008/06/13)
Novel pyrimidine derivatives represented by formula (I): (wherein R1 represents a (in the group, R3 represents a leaving group), a hydroxycarbamoyl group, or an amino group; and R2 represents a group capable of converting
Improved synthesis of a new nonpeptidic inhibitor of human neutrophil elastase
Ohmoto,Yamamoto,Horiuchi,Kojima,Hachiya,Hashimoto,Kawamura,Nakai,Toda
, p. 299 - 301 (2007/10/03)
A practical method for the synthesis of ONO-6818 {2-(5-Amino-6-oxo-2-phenylhydropyrimidinyl)-N-[2-(5-tert-butyl-1,3,4-oxadiazo l-2-yl)-1-(methylethyl)-2-oxoethyl]acetamide} (1), the first clinical candidate for a nonpeptidic orally active inhibitor of hum
Nonpeptidic inhibitors of human leukocyte elastase. 5. Design, synthesis, and X-ray crystallography of a series of orally active 5-aminopyrimidin-6- one-containing trifluoromethyl ketones
Veale,Bernstein,Bryant,Ceccarelli,Damewood Jr.,Earley,Feeney,Gomes,Kosmider,Steelman,Thomas,Vacek,Williams,Wolanin,Woolson
, p. 98 - 108 (2007/10/02)
The effects of changes in substitution in a series of 5-amino-2- pyrimidin-6-ones on both in vitro activity and oral activity in an acute hemorrhage assay have been explored. These compounds contained either a trifluoromethyl ketone or a boronic acid moiety to bind covalently to the Ser-195 hydroxyl of human leukocyte elastase (HLE). Boronic acid-containing inhibitors were found to be more potent than the corresponding trifluoromethyl ketones in vitro but were less active upon oral administration. Compound 13b was found to offer the best combination of oral potency, duration of action, and enzyme selectivity and, as such, was selected for further biological testing. X-ray crystallography of a cocrystallized complex of compound 19m and porcine pancreatic elastase demonstrated that the inhibitor is bound to the enzyme in a manner similar to that found previously for a closely related series of pyridone-containing inhibitors of HLE.
