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    3-AMINO-INDAZOLE OR 3-AMINO-4,5,6,7-TETRAHYDRO-INDAZOLE DERIVATIVES
    9.
    发明公开
    3-AMINO-INDAZOLE OR 3-AMINO-4,5,6,7-TETRAHYDRO-INDAZOLE DERIVATIVES 有权
    3-氨基 - 吲唑或3-氨基-4,5,6,7-四氢 - 吲唑衍生物

    公开(公告)号：EP2346834A1

    公开(公告)日：2011-07-27

    申请号：EP09783046.7

    申请日：2009-09-15

    申请人： F.Hoffmann-La Roche AG

    发明人： BENSON, Gregory, Martin ,  BLEICHER, Konrad ,  FENG, Song ,  GRETHER, Uwe ,  KUHN, Bernd ,  MARTIN, Rainer, E. ,  PLANCHER, Jean-Marc ,  RICHTER, Hans ,  RUDOLPH, Markus ,  TAYLOR, Sven

    IPC分类号： C07D231/56 ,  A61K31/416 ,  A61P3/06 ,  A61P3/10 ,  C07D401/12 ,  C07D407/12

    CPC分类号： C07D231/56 ,  C07D401/12 ,  C07D407/12

    摘要： This invention relates to novel indazole derivatives of formula (I), wherein R
    1 to R
    7 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are FXR modulators and can be use as medicaments. The compounds are selective modulators of the farnesoid-X-receptor, preferably agonists u j[ιe farnesoid-X-receptor (FXR) is a member of the nuclear hormone receptor superfamily of transcription factors. Diseases which are affected by FXR modulators include increased lipid and cholesterol levels, particularly high LDL-cholesterol, high triglycerides, low HDL-cholesterol, dyslipidemia, diseases of cholesterol absorption, atherosclerotic disease, peripheral occlusive disease, ischemic, stroke, diabetes, particularly non-insulin dependent diabetes mellitus, metabolic syndrome, diabetic nephropathy, obesity, cholesterol gallstone disease, cholestasis/fibrosis of the liver, non alcoholic steatohepatitis (NASH), non-alcoholic fatty liver disease (NAFLD), psoriasis, cancer, particularly gastrointestinal cancer, osteoporosis, Parkinson's disease and Alzheimer's disease. Preferred diseases (and conditions) which are affected by FXR modulators are prevention or treatment of high LDL cholesterol levels high triglycerides, dyslipidemia, cholesterol gallstone disease, cancer, non-insulin dependent diabetes mellitus and metabolic syndrome. Particularly preferred diseases which arc affected by FXR modulators arc high LDL cholesterol, high triglyceride levels and dyslipidemia.

    摘要翻译： 本发明涉及式（I）的新型吲唑衍生物，其中R 1至R 7如说明书和权利要求书中所定义，及其生理上可接受的盐。 这些化合物是FXR调节剂，可用作药物。 该化合物是法尼醇-X-受体的选择性调节剂，优选激动剂，其中法尼醇-X-受体（FXR）是转录因子核激素受体超家族的成员。 受FXR调节剂影响的疾病包括增加的脂质和胆固醇水平，特别是高LDL-胆固醇，高甘油三酯，低HDL-胆固醇，血脂异常，胆固醇吸收疾病，动脉粥样硬化疾病，外周阻塞病，局部缺血，中风，糖尿病，特别是非 胰岛素依赖性糖尿病，代谢综合征，糖尿病肾病，肥胖症，胆固醇胆结石病，肝胆汁淤积/纤维化，非酒精性脂肪性肝炎（NASH），非酒精性脂肪肝病（NAFLD），牛皮癣，癌症，特别是胃肠癌， 骨质疏松症，帕金森病和阿尔茨海默病。 受FXR调节剂影响的优选疾病（和条件）是预防或治疗高LDL胆固醇水平高甘油三酯，血脂异常，胆固醇胆石病，癌症，非胰岛素依赖型糖尿病和代谢综合征。 特别优选的受FXR调节剂影响的疾病是高LDL胆固醇，高甘油三酯水平和血脂异常。