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    • 17. 发明授权
    • 5-amino 4-hydroxy-7-(1H-indolmethyl)-8-methylnonamide derivatives as renin inhibitors for the treatment of hypertension
    • 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
    • US07851634B2
    • 2010-12-14
    • US10593460
    • 2005-03-17
    • Peter HeroldStefan StutzRobert MahVincenzo TschinkeAleksandar StojanovicNathalie JotterandMichael QuirmbachDirk BehnkeChristiane Marti
    • Peter HeroldStefan StutzRobert MahVincenzo TschinkeAleksandar StojanovicNathalie JotterandMichael QuirmbachDirk BehnkeChristiane Marti
    • C07D405/02A61K31/44
    • C07C237/06C07C237/22C07D209/12C07D231/56C07D401/12C07D403/12C07D405/12C07D409/12C07D417/12
    • 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.
    • 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。