5-AMINO-4-HYDROXY-7-(1H-INDOLMETHYL)-8-METHYLNONAMIDE DERIVATIVES AS RENIN INHIBITORS FOR THE TREATMENT OF HYPERTENSION
    21.
    发明申请
    5-AMINO-4-HYDROXY-7-(1H-INDOLMETHYL)-8-METHYLNONAMIDE DERIVATIVES AS RENIN INHIBITORS FOR THE TREATMENT OF HYPERTENSION 审中-公开
    作为治疗高血压的RININ抑制剂的5-氨基-4-羟基-7-(1H-吲哚基甲基)-8-甲基壬酰胺衍生物

    公开(公告)号:WO2005090305A1

    公开(公告)日:2005-09-29

    申请号:PCT/EP2005/051244

    申请日:2005-03-17

    IPC分类号: C07D209/20

    摘要: The application relatés to novel alkanamides of the general formula (I) where X is -CH 2 - or >CH-OH; (A) R 1 is e.g. an optionally substituted heterocyclyl radical or an optionally substituted polycyclic, unsaturated hydrocarbon radical where X is hydroxymethylene; R 2 is C 1 -C 6 -alkyl or C 3 -C 6 -cydoalkyl; R 3 are each independently H, C 1 -C 6 -alkyl, C 1-6 -alkoxycarbonyl or C 1 -C 6 -alkanoyl; R 4 is C 1 -C 6 -alkyl, C 3 -C 6 -cycloalkyl, C 2 -C 6 -alkenyl or unsubstituted or substituted aryl­C 1 -C 6 -alkyl; R 5 is C l -C 6 -alkyl, C 1 -C 6 -hydroxyalkyl, C 1 -C 6 -alkoxy-C 1 -C 6 -alkyl, C 1 -C 6 -alkanoyloxy­ C 1 -C 6 -alkyl, C 1 -C 6 -aminoalkyl, C 1 -C 6 -alkylamino-C 1 -C 6 -alkyl, C 1 -C 6 -dialkylamino-C l -C 6 -alkyl, C 1 -C 6 -alkanoylamido-C 1 -C 6 -alkyl, HO(O)C-C 1 -C 6 -alkyl, C 1 -C 6 -alkyl-O-(O)C-C 1 -C 6 -alkyl, H 2 N-C(O)-C 1 -C 6 -alkyl, C 1 -C 6 -alkyl-HN-C(O)-C 1 -C 6 -alkyl, (C 1 ,-C 6 -alkyl) 2 N-C(O)-C 1 -C 6 -alkyl, C 2 -C 8 -alkenyl, C 2 -C 8 -alkynyl, cyano-C 1 -C 6 -alkyl, halo-C l -C 6 -alkyl, optionally substituted aryl-­C o -C 6 -alkyl, optionally substituted C 3 -C 8 -cycloalkyl-C o -C 6 -alkyl or optionally substituted heterocydyl-C o -C 6 -alkyl; to a process for their preparation and to the use of these compounds as medicines, especially as renin inhibitors for the treatment of hypertension.

    摘要翻译: 本发明涉及通式(I)的新型烷酰胺,其中X为-CH 2 - 或> CH-OH; (A)R 1是例如。 任选取代的杂环基或任选取代的多环不饱和烃基,其中X是羟基亚甲基; R 2是C 1 -C 6 - 烷基或C 3 -C 6 - 环烷基; R 3各自独立地为H,C 1 -C 6 - 烷基,C 1-6 - 烷氧基羰基或C 1 -C 6 - 烷酰基; R 4是C 1 -C 6 - 烷基,C 3 -C 6 - 环烷基,C 2 -C 6 - 烯基或未取代或取代的芳基C 1 -C 6烷基; R 5是C 1 -C 6烷基,C 1 -C 6羟基烷基,C 1 -C 6烷氧基-C 1 -C 6烷基,C 1 -C 6烷酰氧基C 1 -C 6烷基,C 1 -C 6氨基烷基,C 1 -C 6 - 烷基氨基-C 1 -C 6 - 烷基,C 1 -C 6 - 二烷基氨基-C 1 -C 6 - 烷基,C 1 -C 6 - 烷酰基氨基-C 1 -C 6烷基,HO(O)C 1 -C 6 - (O)C 1 -C 6烷基,H 2 N-C(O)-C 1 -C 6 - 烷基,C 1 -C 6烷基-NH-C(O)-C 1 -C 6 - 烷基,(C 1 -C 6) - 烷基)N 2 -C(O)-C 1 -C 6 - 烷基,C 2 -C 8 - 烯基,C 2 -C 8 - 炔基,氰基-C 1 -C 6烷基,卤代-C 1 -C 6烷基,任选取代的芳基-Co- C 6 - 烷基,任选取代的C 3 -C 8 - 环烷基-C 0 -C 6 - 烷基或任选取代的杂环-Co-C 6 - 烷基; 其制备方法和这些化合物作为药物的使用,特别是用作治疗高血压的肾素抑制剂。