会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 8. 发明申请
    • FUSED-RING PYRIMIDIN-4(3H)-ONE DERIVATIVES, PROCESSES FOR THE PREPARATION AND USES THEREOF
    • 熔融吡啶二酮-4(3H) - 酮衍生物,其制备方法及其用途
    • WO2003106435A1
    • 2003-12-24
    • PCT/JP2003/007677
    • 2003-06-17
    • SANKYO COMPANY, LIMITEDX-CEPTOR THERAPEUTICS, INC.KANEKO, SatoruWATANABE, TsuyoshiODA, KozoMOHAN, RajuSCHWEIGER, Edwin, J.MARTIN, Richard
    • KANEKO, SatoruWATANABE, TsuyoshiODA, KozoMOHAN, RajuSCHWEIGER, Edwin, J.MARTIN, Richard
    • C07D239/91
    • C07D401/06C07D239/70C07D239/91C07D403/06C07D409/06C07D417/06C07D471/04C07D495/04
    • 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;R 1 , R 2 and R 3 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 R 1 and R 2 together are alkylenedioxy;R 4 and R 5 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.
    • 摘要新的下式(I)化合物及其药理学上可接受的盐和酯可以调节LXR功能,结果显示出优异的抗动脉硬化和抗炎活性:其中:A代表芳基或杂芳基; R1,R2和R3是 烷基,卤代烷基,烷基羰基氧基,烷氧基,烷硫基,烷基亚磺酰基,烷基磺酰基,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,烷氧基羰基氨基,N-(烷氧基羰基)-N-(烷基)氨基,烷基磺酰基氨基,N-(烷基磺酰基)-N-(烷基)氨基,卤代烷基磺酰基氨基,N-(卤代烷基磺酰基) 氨基,烷基羰基,烷氧基羰基,烷基氨基羰基或二烷基氨基羰基,或R 1和R 2一起是亚烷基二氧基; R 4和R 5相同或不同,各自表示氢,羟基,氨基,卤素,巯基,烷基,卤代烷基,烷氧基, 或烷硫基; X表示氢,羟基,卤素,烷氧基或卤代烷氧基; 并且Y表示任选取代的烷基,环烷基,杂环基,芳基,环烷基烷基,杂环基烷基或芳烷基。