Cyclobutene derivatives
    50.
    发明公开
    Cyclobutene derivatives 审中-公开
    环丁烯衍生物

    公开(公告)号:EP1070703A1

    公开(公告)日:2001-01-24

    申请号:EP00306202.3

    申请日:2000-07-20

    摘要: Compounds of formula (I):
    {in which: R 1 and R 2 each represents a variety of organic groups; R 3 and R 4 each represents hydrogen or a variety of organic groups; A represents a group of formula (A-1):
       [in which: R 5 represents hydrogen, hydroxy or alkyl, R 6 represents hydroxy, alkoxy, alkylthio or an amine residue, X and Y each represents oxygen or sulphur, and Z represents a direct single bond between the nitrogen atom shown and the benzene ring shown in formula (I), or an alkylene group],
    G represents a single bond, alkylene or substituted alkylene; the broken line represents a single or double bond; when the broken line represents a double bond, D represents a carbon atom; and E represents an =N-O- group; when the broken line represents a single bond, D represents a CH group or a nitrogen atom, and E represents an oxygen atom, a sulphur atom, an -NH- group or a -CO- group}; and pharmaceutically acceptable salts, esters or other derivatives thereof have the ability to inhibit an ileal bile transporter and so may be used to treat or prevent hypercholesterolaemia.

    摘要翻译: 式(I)化合物:其中:R1和R2各自代表多种有机基团; R3和R4各自代表氢或各种有机基团; A代表式(A-1)的基团:[其中:R5代表氢,羟基或烷基,R6代表羟基,烷氧基,烷硫基或胺残基,X和Y各自代表氧或硫,Z代表直接 所示的氮原子与式(I)中所示的苯环或亚烷基之间的单键],G表示单键,亚烷基或取代的亚烷基; 虚线表示单键或双键; 当虚线表示双键时,D表示碳原子; E表示= N-O-基团; 当虚线表示单键时,D表示CH基团或氮原子,并且E表示氧原子,硫原子,-NH-基团或-CO-基团}。 及其药学上可接受的盐,酯或其它衍生物具有抑制回肠胆汁转运蛋白的能力,因此可用于治疗或预防高胆固醇血症。