148747-75-5

Upstream product

• 161488-95-5 <5-<(benzyloxycarbonyl)amino>-2-(4-fluorophenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl>acetaldehyde dimethyl acetal 
• 161488-94-4 1-(2,2-dimethoxyethyl)-2-(4-fluorophenyl)pyrimidin-6(1H)-one-5-carboxylic acid 
• 149742-96-1 N-(2,2-dimethoxyethyl)-4-(fluorophenyl)carboxamidine 
• 149742-99-4 methyl 1-(2,2-dimethoxyethyl)-2-(4-fluorophenyl)pyrimidin-6(1H)-one-5-carboxylate 
• 1194-02-1 4-fluorobenzonitrile 

Downstream Products

• 148747-76-6 [5-[(benzyloxycarbonyl)amino]-6-oxo-2-(4-fluorophenyl)-1,6-dihydro-1-pyrimidinyl]acetic acid 
• 148747-80-2 2-[2-(4-fluorophenyl)-6-oxo-5-(pyridin-4-ylmethoxycarbonylamino)-1,6-dihydro-1-pyrimidinyl]-N-(2-tert-butyldimethylsilyloxy-3,3,3-trifluoro-1-isopropylpropyl)acetamide 
• 148747-82-4 2-[2-(4-Fluorophenyl)-6-oxo-5-(pyridin-2-ylmethoxycarbonylamino)-1,6-dihydro-1-pyrimidinyl]-N-(2-tert-butyldimethylsilyloxy-3,3,3-trifluoro-1-isopropylpropyl)acetamide 
• 148747-78-8 2-[5-benzyloxycarbonylamino-2-(4-fluorophenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl]-N-(2-tert-butyldimethylsilyloxy-3,3,3-trifluoro-1-isopropylpropyl)acetamide 
• 1025829-60-0 [1-{[2-(tert-Butyl-dimethyl-silanyloxy)-3,3,3-trifluoro-1-isopropyl-propylcarbamoyl]-methyl}-2-(4-fluoro-phenyl)-6-oxo-1,6-dihydro-pyrimidin-5-yl]-carbamic acid trichloromethyl ester 
• 148747-83-5 {2-(4-Fluoro-phenyl)-6-oxo-1-[(3,3,3-trifluoro-2-hydroxy-1-isopropyl-propylcarbamoyl)-methyl]-1,6-dihydro-pyrimidin-5-yl}-carbamic acid pyridin-2-ylmethyl ester 
• 148748-54-3 2-[2-(4-fluorophenyl)-5-(N-trifluoroacetyl-N-methylamino)-6-oxo-1,6-dihydro-1-pyrimidinyl]-N-(3,3,3,-trifluoro-1-isopropyl-2-oxopropyl)acetamide 
• 148747-81-3 {2-(4-Fluoro-phenyl)-6-oxo-1-[(3,3,3-trifluoro-2-hydroxy-1-isopropyl-propylcarbamoyl)-methyl]-1,6-dihydro-pyrimidin-5-yl}-carbamic acid pyridin-4-ylmethyl ester 
• 148747-77-7 2-<5-<(benzyloxycarbonyl)amino>-6-oxo-2-(4-fluorophenyl)-1,6-dihydro-1-pyrimidinyl>-N-(3,3,3-trifluoro-2-hydroxy-1-isopropylpropyl)acetamide 
• 148746-64-9 2-[5-Trifluoroacetylamino-2-(4-fluorophenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl]-N-(3,3,3-trifluoro-1-isopropyl-2-oxopropyl)acetamide 
• 148747-79-9 2-<5-amino-2-(4-fluorophenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl>-N-<2<(tert-butyldimethylsilyl)oxy>-3,3,3-trifluoro-1-isopropylpropyl>acetamide 
• 154753-61-4 2-[5-benzyloxycarbonylamino-2-(4-fluorophenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl]-N-(3,3,3-trifluoro-1-isopropyl-2-oxopropyl)acetamide 
• 154753-62-5 {2-(4-Fluoro-phenyl)-6-oxo-1-[(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-methyl]-1,6-dihydro-pyrimidin-5-yl}-carbamic acid methyl ester 
• 154753-63-6 2-[5-amino-2-(4-fluorophenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl]-N-(3,3,3-trifluoro-1-isopropyl-2-oxopropyl)acetamide 

Relevant academic research and scientific papers

HETEROCYCLIC AMIDE COMPOUNDS AND PHARMACEUTICAL USE OF THE SAME

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

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.