148747-59-5Relevant academic research and scientific papers
Syntheses of 5-amino-2-phenyl-4(3H)-pyrimidinone derivertives starting with glycine
Takahashi, Daisuke,Honda, Yutaka,Izawa, Kunisuke
experimental part, p. 1089 - 1103 (2012/08/07)
N-Cbz derivative of 5-amino-2-phenyl-4(3H)-pyrimidinone was prepared from sodium salt of methyl hydroxymethylene glycinate and benzamidine hydrochloride in good yield. However, the reaction with N-substituted benzamidine did not proceed to give the desired pyrimidinone. In contrast, the reaction of 4-ethoxymethylene-2-phenyl-5(4H)-oxazolone readily prepared from hippuric acid and N-substituted benzamidine proceeded nicely to give 5-(benzoylamino)-6-oxo-2- phenyl-1(6H)-pyrimidineacetic acid in high yield.
PROCESS FOR PRODUCING PYRIMIDINE COMPOUND
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Page/Page column 14, (2010/02/12)
Azlactone Compound (2) is reacted with Amidine Compound (3) to give Pyrimidine Compound (1) useful as an intermediate for enzyme inhibitors (e.g., elastase inhibitor, chymase inhibitor etc.): Pyrimidine Compound (1) Azlactone Compound (2) Amidine Compound (3) wherein each symbol is as defined in the specification.
1,3,4-oxadiazole derivatives and process for producing the same
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, (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
Substituted polycyclic aryl and heteroaryl pyrimidinones useful for selective inhibition of the coagulation cascade
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Page/Page column 109-110, (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.
Synthesis and in vitro studies of novel pyrimidinyl peptidomimetics as potential antimalarial therapeutic agents
Zhu, Shuren,Hudson, Thomas H.,Kyle, Dennis E.,Lin, Ai J.
, p. 3491 - 3496 (2007/10/03)
A class of new pyrimidinyl peptidomimetic agents (compounds 1-6) were synthesized, and their in vitro antimalarial activities against Plasmodium falciparum were evaluated. The core structure of the new agents consists of a substituted 5-aminopyrimidone ri
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
HETEROCYCLIC AMIDE COMPOUNDS AND PHARMACEUTICAL USE OF THE SAME
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, (2008/06/13)
Heterocyclic amide compounds of the formula (I) STR1 wherein each symbol is as defined in the specification, pharmacologically acceptable salts thereof, pharmaceutical compositions thereof and pharmaceutical use thereof. The heterocyclic amide compounds and pharmacologically acceptable salts thereof of the present invention have superior inhibitory activity against chymase groups in mammals inclusive of human, and can be administered orally or parenterally. Therefore, they are useful as chymase inhibitors and can be effective for the prophylaxis and treatment of various diseases caused by chymase, such as those caused by angiotensin II.
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.
