Back to results
US 6,294,542 B1Granted
Pyrimidinone compounds, pharmaceutical compositions containing the compounds and the process for preparing the same
AssigneeBoryung Pharmaceutical Co., Ltd.
InventorsJae-hyoung Lee, Kyung-jin Jang, Byoung-wug Yoo, Ji-han Kim, Jae-seog Kang, Sang-lin Kim
Life of this patent
Estimating the term…
Abstract
The present invention relates to a novel pyrimidinone compounds and the pharmaceutical acceptable salts thereof having remarkable antagonistic action against angiotensin II receptor, thereby, being useful in treating cardiovascular disease caused by binding angiotensin II to its receptor.
Claims12
A pyrimidinone compound of formula (I) or pharmaceutically acceptable salts thereof:
- wherein:
- R1 is C1˜C4 normal or side chain alkyl, cycloalkyl, and C1-C4 alkylalkoxy or C1˜C4 alkylmercapto;
- R2 is H, halogen, C1˜C4 alkl, or arylalkyl;
- R3, R4 is same or different H, C1˜C4 normal or side chain alkyl, cycloalkyl, carbocyclic aryl, arylalkyl, arylcarbonyl, C1˜C4 alkoxycarbonyl, or aminocarbonyl, being optionally substituted by H, halogen, hydroxy, C1˜C4 alkoxy, amino, alkylamino or dialkylamino (each alkyl having C1˜C5), C1˜C4 alkoxycarbonyl or carboxy;
- R3 and R4 are together with N atom forming 4 to 8 membered heterocyclic ring, which can be further substituted with one or two substituents selected from the group consisting of cycloalkyl, carbocyclic aryl or arylalkyl, halogen, hydroxy, C1˜C4 alkoxy, amino alkylamino or dialkylamnino (each alkyl residue having C1˜C5), C1˜C4 alkoxycarbonyl, carboxy or aminocarbonly, and C1˜C4 normal or side chain alkyl being optionally substituted by H, wherein said heterocyclic ring can further include —O—, —S—, —SO—, —SO2— or >N—R5;
- R5 is H, C1C4 alkyl, carbocyclic aryl, arylalkyl, substituted alkenyl, pyridyl, pyrimidyl, C1˜C4 alkyl or arylcarbonyl, C1˜C4 alkyl or arylcarbonyl, C1˜C4 alkoxy carbonyl, aminocarbonyl, CN or SO2NR3R4;
- X is S or >N—R5;
- and
- Z is CN, COOR3, SO2NR3R4 or tetrazol-5-yl radical having the formula:
- wherein R6 is H, t-butyl or triplifenylmethyl;
- m is 1 or 2;
- and
- n is 1, 2, 3, 4, 5, and 6.
10 more elements
Dependencies are inferred from the claim text.