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    5-amino-4-hydroxy-7-(imidazo [1,2-A] pyridin-6-ylmethyl)-8-methyl-nonamide derivatives and related compounds as renin inhibitors for the treatment of hypertension
    4.
    发明授权
    5-amino-4-hydroxy-7-(imidazo [1,2-A] pyridin-6-ylmethyl)-8-methyl-nonamide derivatives and related compounds as renin inhibitors for the treatment of hypertension 失效
    5-氨基-4-羟基-7-（咪唑并[1,2-A]吡啶-6-基甲基）-8-甲基 - 非酰胺衍生物和相关化合物作为治疗高血压的肾素抑制剂

    公开(公告)号：US08071651B2

    公开(公告)日：2011-12-06

    申请号：US11992132

    申请日：2006-09-14

    申请人： Peter Herold ,  Robert Mah ,  Vincenzo Tschinke ,  Stefan Stutz ,  Aleksandar Stojanovic ,  Christiane Marti ,  Dirk Behnke ,  Stjepan Jelakovic

    发明人： Peter Herold ,  Robert Mah ,  Vincenzo Tschinke ,  Stefan Stutz ,  Aleksandar Stojanovic ,  Christiane Marti ,  Dirk Behnke ,  Stjepan Jelakovic

    IPC分类号： A01N43/42 ,  A01N43/40 ,  A01N43/58 ,  A01N43/00 ,  A01N43/64 ,  A01N37/18 ,  A01N35/00 ,  A01N33/18 ,  A01N33/24 ,  C07C233/00 ,  C07C235/00 ,  C07C237/00 ,  C07C239/00 ,  A61K31/16 ,  A61K31/12

    CPC分类号： C07D405/12 ,  C07D471/04

    摘要： Compounds of the general formula (I) or its salt or a compound in which one or more atoms are replaced by their stable, nonradio-active isotopes, in particular its pharmaceutically acceptable salt; in which X is —CH2—; R is a mono- to tetra-substituted, mono- or bicyclic, unsaturated heterocyclic radical having 1 to 4 nitrogen atoms, R2 is C1-6alkyl or C3-6cycloalkyl; R3 is independently of one another H, C1-6alkyl, C1-6alkoxycarbonyl or C1-6alkanoyl; R4 is C2-6alkenyl, C1-6alkyl, unsubstituted or substituted aryl-C1-6alkyl or C3-8cycloalkyl; R5 is -Lm-R6; L is C1-6alkylene which is optionally substituted by 1-4 halogen, or a linker: formula (II) n=0, 1 or 2; m=0 or 1; R6 is a radical composed of 2 cyclic systems selected from bicyclo[x.y.z]alkyl, spiro[o.p]alkyl, mono- or bioxabicyclo[x.y.z]alkyl or mono- or bioxaspiro[o.p]alkyl, all of which may be substituted by 1-3 substituents selected from C1-6alkyl, C1-6alkoxy, cyano, halogen, C1-6alkoxy-C1-6alkyl, hydroxy-C1-6alkyl or dialkylamino, or if m=0: is also saturated C3-8heterocyclyl which comprises 1-2 oxygen atoms, substituted by 1-3 substituents selected from C1-6alkyl, C1-6alkoxy, cyano, halogen, C1-6alkoxy-C1-6alkyl, hydroxy-C1-6alkyl or dialkylamino, or if m=1: is also saturated C3-8heterocyclyl which comprises 1-2 oxygen atoms, optionally substituted by 1-3 substituents selected from C1-6alkyl, C1-6alkoxy, cyano, halogen, C1-6-alkoxy-C1-6alkyl, hydroxy-C1-6alkyl or dialkylamino; have renin-inhibiting properties and can be used as medicines for the treatment of hypertension.

    摘要翻译： 通式（I）的化合物或其盐或其中一个或多个原子被其稳定的非放射性活性同位素替代的化合物，特别是其药学上可接受的盐; 其中X是-CH 2 - ; R是具有1至4个氮原子的单 - 四取代的单 - 或双环不饱和杂环基，R 2是C 1-6烷基或C 3-6环烷基; R 3彼此独立地为H，C 1-6烷基，C 1-6烷氧基羰基或C 1-6烷酰基; R 4是C 2-6烯基，C 1-6烷基，未取代或取代的芳基-C 1-6烷基或C 3-8环烷基; R5是-Lm-R6; L是任选被1-4个卤素取代的C 1-6亚烷基或连接基：式（II）n = 0,1或2; m = 0或1; R6是由选自双环[xyz]烷基，螺[op]烷基，单或生双环[xyz]烷基或单 - 或生物密封[op]烷基的2个环状体组成的基团，所有这些可以被1- 选自C 1-6烷基，C 1-6烷氧基，氰基，卤素，C 1-6烷氧基-C 1-6烷基，羟基-C 1-6烷基或二烷基氨基的3个取代基，或者如果m = 0：也是饱和的C 3-8杂环基，其包含1-2个氧 原子被1-3个选自C 1-6烷基，C 1-6烷氧基，氰基，卤素，C 1-6烷氧基-C 1-6烷基，羟基-C 1-6烷基或二烷基氨基取代的取代基取代，或者如果m = 1：也是饱和的C 3-8杂环基 其包含1-2个氧原子，任选被1-3个选自C 1-6烷基，C 1-6烷氧基，氰基，卤素，C 1-6 - 烷氧基-C 1-6烷基，羟基-C 1-6烷基或二烷基氨基的取代基取代; 具有肾素抑制性质，可用作治疗高血压的药物。

    5-amino 4-hydroxy-7-(1H-indolmethyl)-8-methylnonamide derivatives as renin inhibitors for the treatment of hypertension
    10.
    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。