Patent ID: 6294542
Filing Date: 2001-09-25
Classification: A61P,C07D

Abstract:
A pyrimidinone compound of formula (I) or pharmaceutically acceptable salts thereof: ##STR5##wherein:R.sup.1 is C.sub.1.about.C.sub.4 normal or side chain alkyl, cycloalkyl, and C.sub.1 -C.sub.4 alkylalkoxy or C.sub.1.about.C.sub.4 alkylmercapto;R.sup.2 is H, halogen, C.sub.1.about.C.sub.4 alkl, or arylalkyl;R.sup.3, R.sup.4 is same or different H, C.sub.1.about.C.sub.4 normal or side chain alkyl, cycloalkyl, carbocyclic aryl, arylalkyl, arylcarbonyl, C.sub.1.about.C.sub.4 alkoxycarbonyl, or aminocarbonyl, being optionally substituted by H, halogen, hydroxy, C.sub.1.about.C.sub.4 alkoxy, amino, alkylamino or dialkylamino (each alkyl having C.sub.1.about.C.sub.5), C.sub.1.about.C.sub.4 alkoxycarbonyl or carboxy;R.sup.3 and R.sup.4 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, C.sub.1.about.C.sub.4 alkoxy, amino alkylamino or dialkylamnino (each alkyl residue having C.sub.1.about.C.sub.5), C.sub.1.about.C.sub.4 alkoxycarbonyl, carboxy or aminocarbonly, and C.sub.1.about.C.sub.4 normal or side chain alkyl being optionally substituted by H, wherein said heterocyclic ring can further include --O--, --S--, --SO--, --SO.sub.2 -- or >N--R.sup.5 ;R.sup.5 is H, C.sub.1 C.sub.4 alkyl, carbocyclic aryl, arylalkyl, substituted alkenyl, pyridyl, pyrimidyl, C.sub.1.about.C.sub.4 alkyl or arylcarbonyl, C.sub.1.about.C.sub.4 alkyl or arylcarbonyl, C.sub.1.about.C.sub.4 alkoxy carbonyl, aminocarbonyl, CN or SO.sub.2 NR.sup.3 R.sup.4 ;X is S or >N--R.sup.5 ; andZ is CN, COOR.sup.3, SO.sub.2 NR.sup.3 R.sup.4 or tetrazol-5-yl radical having the formula: ##STR6##wherein R.sup.6 is H, t-butyl or triplifenylmethyl;m is 1 or 2; andn is 1, 2, 3, 4, 5, and 6.