利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

13 条记录 (耗时 0.019 秒)

    PROCESS FOR THE PREPARATION OF PROLINE DERIVATIVES
    8.
    发明申请
    PROCESS FOR THE PREPARATION OF PROLINE DERIVATIVES 有权
    制备衍生物的方法

    公开(公告)号：US20130123512A1

    公开(公告)日：2013-05-16

    申请号：US13671586

    申请日：2012-11-08

    申请人： Hoffmann-La Roche Inc.

    发明人： Bjoern Bartels ,  Fritz Bliss ,  Philipp Cueni ,  Christophe Pfleger ,  Ulrich Zutter

    IPC分类号： C07D207/09

    CPC分类号： C07D207/09 ,  C07D207/16

    摘要： The present invention relates in part to a process for the preparation of a proline derivative of formula I wherein, R1 is C1-7-alkyl or wherein R4 is selected from the group consisting of C1-7-alkyl, halogen-C1-7-alkyl and phenyl optionally substituted by halogen; R2 is halogen or halogen-C1-7-alkyl; and R3 is selected from the group consisting of hydrogen, halogen, halogen-C1-7-alkyl, C1-7-alkoxy, halogen-C1-7-alkoxy and a 5- or 6-membered heterocyclic ring containing one or two nitrogen atoms, said ring being optionally substituted by C1-7-alkyl or halogen. The proline derivatives of the formula I are preferential inhibitors of the cysteine protease Cathepsin S and are therefore useful to treat metabolic diseases like diabetes, atherosclerosis, abdominal aortic aneurysm, peripheral arterial disease and diabetic nephropathy.

    摘要翻译： 本发明部分涉及制备式I的脯氨酸衍生物的方法，其中R 1是C 1-7 - 烷基或其中R 4选自C 1-7 - 烷基，卤素-C 1-7 - 烷基和任选被卤素取代的苯基; R2是卤素或卤素-C1-7-烷基; 并且R 3选自氢，卤素，卤素-C 1-7 - 烷基，C 1-7 - 烷氧基，卤素-C 1-7 - 烷氧基和含有一个或两个氮原子的5-或6-元杂环 所述环任选被C 1-7 - 烷基或卤素取代。 式I的脯氨酸衍生物是半胱氨酸蛋白酶组织蛋白酶S的优先抑制剂，因此可用于治疗糖尿病，动脉粥样硬化，腹主动脉瘤，外周动脉疾病和糖尿病肾病等代谢疾病。