PYRIMIDINONE DERIVATIVE AND METHOD FOR PREPARATION THEREOF

摘要

PURPOSE: Provided are novel pyrimidinone derivatives represented by the formula(1) which inhibits vascular expansion and their pharmaceutically acceptable salt . CONSTITUTION: The novel pyrimidinone derivative is represented by the formula(1), wherein R1 is C1-C4 alkyl or C1-C4 alkoxy or C1-C4 alkylmercapto; R2 is halogen, C1-C4 alkyl; Y is NR3R4 wherein R3 and R4 are the same or different and represent hydrogen, C1-C4 alkoxy, amino, alkylamino, dialkylamino(the carbon number of each alkyl residue is 1-5), C1-C4 alkoxycarbonyl or aminocarbonyl substituted C1-C4 alkyl, cyclo alkyl, aryl, arylalkyl, C1-C4 alkyl, C1-C4 alkoxycarbonyl or aminocarbonyl; or R3 and R4 form C4-C8 cyclic ring together with a nitrogen atom which bins to them, the ring can be substituted by 1-2 of substituents selected from hydrogen, C1-C4 alkoxy, amino, C1-C4 alkoxycarbonyl or aminocarbonyl substituted C1-C4 alkyl, cycloalkyl, aryl, arylalkyl, C1-C4 alkoxy or amino and contains -O-, -S-, N-R5 as ring source;, wherein R5 is C1-C4 alkyl, aryl, arylalkyl, alkenyl, pyridyl, arylcarbonyl, C1-C4 alkoxycarbonyl, or aminocarbonyl; Z is CN, COOR3 or tetrazole-5-yl group, wherein R6 is hydrogen, t-butyl or triphenylmethyl; m is 1 or 2; and n is 1 to 6.