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    ALTERNATIVE SYNTHESIS OF RENIN INHIBITORS AND INTERMEDIATES THEREOF
    1.
    发明申请
    ALTERNATIVE SYNTHESIS OF RENIN INHIBITORS AND INTERMEDIATES THEREOF 失效
    瑞宁抑制剂及其中间体的替代合成

    公开(公告)号：US20110137044A1

    公开(公告)日：2011-06-09

    申请号：US13022243

    申请日：2011-02-07

    申请人： Gottfried Sedelmeier ,  Stuart John Mickel ,  Heinrich Rueeger

    发明人： Gottfried Sedelmeier ,  Stuart John Mickel ,  Heinrich Rueeger

    IPC分类号： C07D498/04

    CPC分类号： C07D207/26 ,  C07C271/16 ,  C07C271/22 ,  C07D211/76 ,  C07D307/33

    摘要： The present invention relates to synthetic routes to prepare a compound of the formula wherein R1 is halogen, C1-6halogenalkyl, C1-6alkoxy-C1-6alkyloxy or C1-6alkoxy-C1-6alkyl; R2 is halogen, C1-4alkyl or C1-4alkoxy; R3 and R4 are independently branched C3-6alkyl; and R5 is cycloalkyl, C1-6alkyl, C1-6hydroxyalkyl, C1-6alkoxy-C1-6alkyl, C1-6alkanoyloxy-C1-6alkyl, C1-6aminoalkyl, C1-6alkylamino-C1-6alkyl, C1-6dialkylamino-C1-6alkyl, C1-6alkanoylamino-C1-6alkyl, HO(O)C-C1-6alkyl, C1-6alkyl-O—(O)C—C1-6alkyl, H2N—C(O)—C1-6alkyl, C1-6alkyl-HN—C(O)—C1-6alkyl or (C1-6alkyl)2N—C(O)—C1-6alkyl; or a pharmaceutically acceptable salt thereof as well as key intermediates obtained when following these routes as well as their preparation.

    摘要翻译： 本发明涉及制备下式化合物的合成路线：其中R 1是卤素，C 1-6卤代烷基，C 1-6烷氧基-C 1-6烷氧基或C 1-6烷氧基-C 1-6烷基; R2是卤素，C1-4烷基或C1-4烷氧基; R3和R4独立地是支链的C 3-6烷基; 和R 5是环烷基，C 1-6烷基，C 1-6羟基烷基，C 1-6烷氧基-C 1-6烷基，C 1-6烷酰氧基-C 1-6烷基，C 1-6氨基烷基，C 1-6烷基氨基-C 1-6烷基，C 1-6二烷基氨基-C 1-6烷基，C 1 （O）C 1-6烷基，C 1-6烷基-O-（O）C 1-6烷基，H 2 N-C（O）-C 1-6烷基，C 1-6烷基-NH- C （O）-C 1-6烷基或（C 1-6烷基）2 N -C（O）-C 1-6烷基; 或其药学上可接受的盐以及按照这些途径获得的关键中间体及其制备方法。

    Synthesis of Renin Inhibitors Involving a Cycloaddition Reaction
    2.
    发明申请
    Synthesis of Renin Inhibitors Involving a Cycloaddition Reaction 失效
    涉及环加成反应的肾素抑制剂的合成

    公开(公告)号：US20080255369A1

    公开(公告)日：2008-10-16

    申请号：US12067055

    申请日：2006-09-26

    申请人： Stuart John Mickel ,  Wolfgang Marterer

    发明人： Stuart John Mickel ,  Wolfgang Marterer

    IPC分类号： C07D207/16 ,  C07C227/18 ,  C07C237/20 ,  C07C229/34

    CPC分类号： C07C251/24 ,  C07C231/12 ,  C07D207/08 ,  C07D207/16 ,  C07C237/22

    摘要： The invention related to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially renin inhibitors, such as Aliskiren. Inter alia, the invention relates to a process for the manufacture of a compound of the formula III, wherein R, R1, and R′ are as defined in the specification, or a salt thereof, and a compound of formula IV wherein R, R1, R2 and R′ are as defined in the specification, and processes of manufacturing these.

    摘要翻译： 本发明涉及可用于合成药物活性化合物，特别是肾素抑制剂如阿利吉仑的新方法，新工艺步骤和新型中间体。 特别地，本发明涉及制备式III化合物的方法，其中R 1，R 1和R'如说明书中所定义，或其盐，和 式IV的化合物，其中R 1，R 2，R 2和R'如说明书中所定义，以及制备它们的方法。

    Alternative synthesis of renin inhibitors and intermediates thereof
    3.
    发明授权
    Alternative synthesis of renin inhibitors and intermediates thereof 失效
    肾素抑制剂及其中间体的替代合成

    公开(公告)号：US07910774B2

    公开(公告)日：2011-03-22

    申请号：US11573790

    申请日：2005-08-30

    申请人： Gottfried Sedelmeier ,  Stuart John Mickel ,  Heinrich Rueeger

    发明人： Gottfried Sedelmeier ,  Stuart John Mickel ,  Heinrich Rueeger

    IPC分类号： C07C233/65

    CPC分类号： C07D207/26 ,  C07C271/16 ,  C07C271/22 ,  C07D211/76 ,  C07D307/33

    摘要： The present invention relates to synthetic routes to prepare a compound of the formula wherein R1 is halogen, C1-6halogenalkyl, C1-6alkoxy-C1-6alkyloxy or C1-6alkoxy-C1-6alkyl; R2 is halogen, C1-4alkyl or C1-4alkoxy; R3 and R4 are independently branched C3-6alkyl; and R5 is cycloalkyl, C1-6alkyl, C1-6hydroxyalkyl, C1-6alkoxy-C1-6alkyl, C1-6alkanoyloxy-C1-6alkyl, C1-6aminoalkyl, C1-6alkylamino-C1-6alkyl, C1-6dialkylamino-C1-6alkyl, C1-6alkanoylamino-C1-6alkyl, HO(O)C—C1-6alkyl, C1-6alkyl-O—(O)C—C1-6alkyl, H2N—C(O)—C1-6alkyl, C1-6alkyl-HN—C(O)—C1-6alkyl or (C1-6alkyl)2N—C(O)—C1-6alkyl; or a pharmaceutically acceptable salt thereof as well as key intermediates obtained when following these routes as well as their preparation.

    摘要翻译： 本发明涉及制备下式化合物的合成路线：其中R 1是卤素，C 1-6卤代烷基，C 1-6烷氧基-C 1-6烷氧基或C 1-6烷氧基-C 1-6烷基; R2是卤素，C1-4烷基或C1-4烷氧基; R3和R4独立地是支链的C 3-6烷基; 和R 5是环烷基，C 1-6烷基，C 1-6羟基烷基，C 1-6烷氧基-C 1-6烷基，C 1-6烷酰氧基-C 1-6烷基，C 1-6氨基烷基，C 1-6烷基氨基-C 1-6烷基，C 1-6二烷基氨基-C 1-6烷基，C 1 （O）C 1-6烷基，C 1-6烷基-O-（O）C 1-6烷基，H 2 N-C（O）-C 1-6烷基，C 1-6烷基-NH- C （O）-C 1-6烷基或（C 1-6烷基）2 N -C（O）-C 1-6烷基; 或其药学上可接受的盐以及按照这些途径获得的关键中间体及其制备方法。

    Alternative synthesis of renin inhibitors and intermediates thereof
    4.
    发明授权
    Alternative synthesis of renin inhibitors and intermediates thereof 失效
    肾素抑制剂及其中间体的替代合成

    公开(公告)号：US08143416B2

    公开(公告)日：2012-03-27

    申请号：US13022243

    申请日：2011-02-07

    申请人： Gottfried Sedelmeier ,  Stuart John Mickel ,  Heinrich Rueeger

    发明人： Gottfried Sedelmeier ,  Stuart John Mickel ,  Heinrich Rueeger

    IPC分类号： C07D263/52

    CPC分类号： C07D207/26 ,  C07C271/16 ,  C07C271/22 ,  C07D211/76 ,  C07D307/33

    摘要： The present invention relates to synthetic routes to prepare a compound of the formula wherein R1 is halogen, C1-6halogenalkyl, C1-6alkoxy-C1-6alkyloxy or C1-6alkoxy-C1-6alkyl; R2 is halogen, C1-4alkyl or C1-4alkoxy; R3 and R4 are independently branched C3-6alkyl; and R5 is cycloalkyl, C1-6alkyl, C1-6hydroxyalkyl, C1-6alkoxy-C1-6alkyl, C1-6alkanoyloxy-C1-6alkyl, C1-6aminoalkyl, C1-6alkylamino-C1-6alkyl, C1-6dialkylamino-C1-6alkyl, C1-6alkanoylamino-C1-6alkyl, HO(O)C—C1-6alkyl, C1-6alkyl-O—(O)C—C1-6alkyl, H2N—C(O)—C1-6alkyl, C1-6alkyl-HN—C(O)—C1-6alkyl or (C1-6alkyl)2N—C(O)—C1-6alkyl; or a pharmaceutically acceptable salt thereof as well as key intermediates obtained when following these routes as well as their preparation.

    摘要翻译： 本发明涉及制备下式化合物的合成路线：其中R 1是卤素，C 1-6卤代烷基，C 1-6烷氧基-C 1-6烷氧基或C 1-6烷氧基-C 1-6烷基; R2是卤素，C1-4烷基或C1-4烷氧基; R3和R4独立地是支链的C 3-6烷基; 和R 5是环烷基，C 1-6烷基，C 1-6羟基烷基，C 1-6烷氧基-C 1-6烷基，C 1-6烷酰氧基-C 1-6烷基，C 1-6氨基烷基，C 1-6烷基氨基-C 1-6烷基，C 1-6二烷基氨基-C 1-6烷基，C 1 （O）C 1-6烷基，C 1-6烷基-O-（O）C 1-6烷基，H 2 N-C（O）-C 1-6烷基，C 1-6烷基-NH- C （O）-C 1-6烷基或（C 1-6烷基）2 N -C（O）-C 1-6烷基; 或其药学上可接受的盐以及按照这些途径获得的关键中间体及其制备方法。

    SYNTHESIS OF RENIN INHIBITORS INVOLVING A CYCLOADDITION REACTION
    6.
    发明申请
    SYNTHESIS OF RENIN INHIBITORS INVOLVING A CYCLOADDITION REACTION 审中-公开
    涉及环孢菌素反应的瑞宁抑制剂的合成

    公开(公告)号：US20110230665A1

    公开(公告)日：2011-09-22

    申请号：US13116349

    申请日：2011-05-26

    申请人： Stuart John Mickel ,  Wolfgang Marterer

    发明人： Stuart John Mickel ,  Wolfgang Marterer

    IPC分类号： C07D207/09 ,  C07C68/06

    CPC分类号： C07C251/24 ,  C07C231/12 ,  C07D207/08 ,  C07D207/16 ,  C07C237/22

    摘要： The invention related to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially renin inhibitors, such as Aliskiren. Inter alia, the invention relates to a process for the manufacture of a compound of the formula III, wherein R, R1, and R′ are as defined in the specification, or a salt thereof, and a compound of formula IV wherein R, R1, R2 and R′ are as defined in the specification, and processes of manufacturing these.

    摘要翻译： 本发明涉及可用于合成药物活性化合物，特别是肾素抑制剂如阿利吉仑的新方法，新工艺步骤和新型中间体。 特别地，本发明涉及制备式III化合物的方法，其中R，R 1和R'如本说明书中所定义，或其盐和式IV化合物，其中R，R 1 ，R2和R'如说明书中所定义，以及制造这些的方法。