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    5-amino 4-hydroxy-7-(1H-indolmethyl)-8-methylnonamide derivatives as renin inhibitors for the treatment of hypertension
    4.
    发明授权
    5-amino 4-hydroxy-7-(1H-indolmethyl)-8-methylnonamide derivatives as renin inhibitors for the treatment of hypertension 失效
    5-氨基-4-羟基-7-（1H-吲哚甲基）-8-甲基壬酰胺衍生物作为治疗高血压的肾素抑制剂

    公开(公告)号：US07851634B2

    公开(公告)日：2010-12-14

    申请号：US10593460

    申请日：2005-03-17

    申请人： Peter Herold ,  Stefan Stutz ,  Robert Mah ,  Vincenzo Tschinke ,  Aleksandar Stojanovic ,  Nathalie Jotterand ,  Michael Quirmbach ,  Dirk Behnke ,  Christiane Marti

    发明人： Peter Herold ,  Stefan Stutz ,  Robert Mah ,  Vincenzo Tschinke ,  Aleksandar Stojanovic ,  Nathalie Jotterand ,  Michael Quirmbach ,  Dirk Behnke ,  Christiane Marti

    IPC分类号： C07D405/02 ,  A61K31/44

    CPC分类号： C07C237/06 ,  C07C237/22 ,  C07D209/12 ,  C07D231/56 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12

    摘要： The application relates to novel alkanamides of the general formula (I) where X is —CH2— or >CH—OH; (A) R1 is e.g. an optionally substituted heterocyclyl radical or an optionally substituted polycyclic, unsaturated hydrocarbon radical where X is hydroxymethylene; R2 is C1-C6-alkyl or C3-C6-cydoalkyl; R3 are each independently H, C1-C6-alkyl, C1-6-alkoxycarbonyl or C1-C6-alkanoyl; R4 is C1-C6-alkyl, C3-C6-cycloalkyl, C2-C6-alkenyl or unsubstituted or substituted arylC1-C6-alkyl; R5 is C1-C6-alkyl, C1-C6-hydroxyalkyl, C1-C6-alkoxy-C1-C6-alkyl, C1-C6-alkanoyloxy C1-C6-alkyl, C1-C6-aminoalkyl, C1-C6-alkylamino-C1-C6-alkyl, C1-C6-dialkylamino-C1-C6-alkyl, C1-C6-alkanoylamido-C1-C6-alkyl, HO(O)C—C1-C6-alkyl, C1-C6-alkyl-O—(O)C—C1-C6-alkyl, H2N—C(O)—C1-C6-alkyl, C1-C6-alkyl-HN—C(O)—C1-C6-alkyl, (C1,-C6-alkyl)2N—C(O)—C1-C6-alkyl, C2-C8-alkenyl, C2-C8-alkynyl, cyano-C1-C6-alkyl, halo-C1-C6-alkyl, optionally substituted aryl-Co-C6-alkyl, optionally substituted C3-C8-cycloalkyl-Co-C6-alkyl or optionally substituted heterocydyl-Co-C6-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： 本申请涉及通式（I）的新型烷酰胺，其中X为-CH 2 - 或> CH-OH; （A）R1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; R2是C1-C6-烷基或C3-C6-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; R4是C1-C6-烷基，C3-C6-环烷基，C2-C6-烯基或未取代或取代的芳基C1-C6-烷基; R5是C1-C6-烷基，C1-C6-羟基烷基，C1-C6-烷氧基-C1-C6-烷基，C1-C6-烷酰氧基C1-C6-烷基，C1-C6-氨基烷基，C1-C6烷基氨基-C1 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 - 烷基，C 1 -C 6烷基-O-（ 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） 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-C 0 -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。