[EN] FUSED-RING PYRIMIDIN-4(3H)-ONE DERIVATIVES, PROCESSES FOR THE PREPARATION AND USES THEREOF<br/>[FR] DERIVES DE LA PYRIMIDIN-4(3H)-ONE A CYCLES FUSIONNES, SPN PROCEDE DE PREPARATION ET SES UTILISATIONS
申请人：SANKYO CO
公开号：WO2003106435A1
公开（公告）日：2003-12-24
AbstractNovel compounds of the following formula (I) and pharmacologically acceptable
salt and esters thereof can modulate LXR function and as a result show excellent
anti-arteriosclerotic and anti-inflammatory activity:wherein:A represents
aryl or heteroaryl;R1, R2 and R3 are the same or
different and each represents hydrogen, hydroxyl, nitro, cyano, amino, halogen,
carboxy, carbamoyl, mercapto, alkyl, haloalkyl, alkylcarbonyloxy, alkoxy,
alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, dialkylamino, alkylcarbonylamino,
N-(alkylcarbonyl)-N-(alkyl)amino, alkoxycarbonylamino, N-(alkoxycarbonyl)-N-(alkyl)amino,
alkylsulfonylamino, N-(alkylsulfonyl)-N-(alkyl)amino, haloalkylsulfonylamino,
N-(haloalkylsulfonyl)-N-(alkyl)amino, alkylcarbonyl, alkoxycarbonyl,
alkylaminocarbonyl or dialkylaminocarbonyl group, or R1 and R2
together are alkylenedioxy;R4 and R5 are the same or different
and each represents hydrogen, hydroxyl, amino, halogen, mercapto, alkyl, haloalkyl,
alkoxy, alkoxycarbonyl or alkylthio;X represents hydrogen, hydroxyl, halogen,
alkoxy or haloalkoxy; andY represents an optionally substituted alkyl, cycloalkyl,
heterocyclyl, aryl, cycloalkylalkyl, heterocyclylalkyl or aralkyl group.
新化合物具有以下式（I）的结构，其药学上可接受的盐和酯可以调节LXR功能，从而表现出优秀的抗动脉粥样硬化和抗炎活性：其中：A代表芳基或杂环芳基；R1、R2和R3相同或不同，每个代表氢、羟基、硝基、氰基、氨基、卤素、羧基、氨基甲酰基、巯基、烷基、卤代烷基、烷基羰氧基、烷氧基、烷硫基、烷磺基、烷基氨基、二烷基氨基、烷基羰基氨基、N-（烷基羰基）-N-（烷基）氨基、烷氧羰基氨基、N-（烷氧羰基）-N-（烷基）氨基、烷磺酰氨基、N-（烷磺酰基）-N-（烷基）氨基、卤代烷基磺酰氨基、N-（卤代烷基磺酰基）-N-（烷基）氨基、烷基羰基、烷氧羰基、烷基氨基羰基或二烷基氨基羰基，或R1和R2一起是亚烷二氧基；R4和R5相同或不同，每个代表氢、羟基、氨基、卤素、巯基、烷基、卤代烷基、烷氧基、烷氧羰基或烷硫基；X代表氢、羟基、卤素、烷氧基或卤代烷氧基；Y代表可选择取代的烷基、环烷基、杂环烷基、芳基、环烷基烷基、杂环烷基烷基或芳基烷基。
