Substituted 1,8-naphthyridines and their use in medicaments
    10.
    发明授权
    Substituted 1,8-naphthyridines and their use in medicaments 失效
    取代的1,8-萘啶并用于药物

    公开(公告)号:US5034399A

    公开(公告)日:1991-07-23

    申请号:US496757

    申请日:1990-03-21

    CPC分类号: C07D471/04

    摘要: Inhibitors of 3-hydrooxy-3-methyl-glutarylcoenzyme A reductase which are 1,8-naphthyridines of the formula ##STR1## in which Arepresents a 3- to 7-membered heterocycle which is optionally substituted, or aryl which is optionally substituted,Brepresents cycloalkyl or alkyl which is optionally substituted, aryl which is optionally substituted,D and E are identical or different andrepresents hydrogen, halogen, mercapto, hydroxyl, alkoxy, alkyl which is optionally substituted, or a group of the formula --NR.sup.1 R.sup.2, aryl, aryloxy or arylthio having 6 to 10 carbon atoms, which is optionally substituted,Yrepresents a group of the formula ##STR2## in which Jdenotes hydrogen, hydroxyl, mercapto or halogen, or alkyl, alkoxy or alkylthio which are optionally substituted, aryloxy, benzyloxy or arylthio or a group of the formula --NR.sup.1 R.sup.2,Zdenotes oxygen or sulphur,Gdenotes hydrogen, alkyl or alkenyl which is optionally substituted,Xrepresents a group of the formula --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--,andRrepresents a group of the formula ##STR3## in which R.sup.5denotes hydrogen or alkyl, andR.sup.6denotes hydrogen or alkyl, which may be substituted by phenyl, ordenotes aryl or a cation,and their salts.

    摘要翻译: 作为式“IMAGE”的1,8-萘啶的3-羟基-3-氧代-3-甲基 - 戊二酰辅酶A还原酶的抑制剂,其中A表示任选取代的3-至7-元杂环,或任选取代的芳基, B代表任选取代的环烷基或烷基,任选取代的芳基,D和E相同或不同,代表氢,卤素,巯基,羟基,烷氧基,任选被取代的烷基,或式-NR1R2的基团, 芳基,芳氧基或具有6至10个碳原子的芳硫基,其任选被取代,Y表示下式的基团,其中J表示氢,羟基,巯基或卤素,或任选被取代的烷基,烷氧基或烷硫基, 芳氧基,苄氧基或芳硫基或式-NR1R2的基团,Z表示氧或硫,G表示氢,任选被取代的烷基或烯基,X表示式-CH 2 -CH 2 - 或-CH = CH- ,和R 表示式为“IMAGE”的基团,其中R5表示氢或烷基,R6表示氢或可被苯基取代的烷基,或表示芳基或阳离子及其盐。