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    3-AMINO-INDAZOLE OR 3-AMINO-4,5,6,7-TETRAHYDRO-INDAZOLE DERIVATIVES
    1.
    发明申请
    3-AMINO-INDAZOLE OR 3-AMINO-4,5,6,7-TETRAHYDRO-INDAZOLE DERIVATIVES 审中-公开
    3-氨基吲哚或3-氨基-4,5,6,7-四氢吲哚衍生物

    公开(公告)号：WO2010034657A1

    公开(公告)日：2010-04-01

    申请号：PCT/EP2009/061966

    申请日：2009-09-15

    Applicant: F. HOFFMANN-LA ROCHE AG ,  BENSON, Gregory, Martin ,  BLEICHER, Konrad ,  FENG, Song ,  GRETHER, Uwe ,  KUHN, Bernd ,  MARTIN, Rainer, E. ,  PLANCHER, Jean-Marc ,  RICHTER, Hans ,  MARKUS, Rudolph ,  TAYLOR, Sven

    Inventor： BENSON, Gregory, Martin ,  BLEICHER, Konrad ,  FENG, Song ,  GRETHER, Uwe ,  KUHN, Bernd ,  MARTIN, Rainer, E. ,  PLANCHER, Jean-Marc ,  RICHTER, Hans ,  MARKUS, Rudolph ,  TAYLOR, Sven

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

    CPC classification number: C07D231/56 ,  C07D401/12 ,  C07D407/12

    Abstract: 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.

    Abstract translation: 本发明涉及式（I）的新的吲唑衍生物，其中R 1至R 7如说明书和权利要求书中所定义，以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。 这些化合物是法呢基-X-受体的选择性调节剂，优选激动剂uj [法新颖-X-受体（FXR）是转录因子的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脂质和胆固醇水平，特别是高LDL-胆固醇，高甘油三酸酯，低HDL-胆固醇，血脂异常，胆固醇吸收疾病，动脉粥样硬化疾病，外周性闭塞性疾病，缺血性，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，胆固醇胆结石疾病，肝脏胆汁郁积/纤维化，非酒精性脂肪性肝炎（NASH），非酒精性脂肪性肝病（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调节剂影响的首选疾病（和病症）是预防或治疗高LDL胆固醇水平高甘油三酯，血脂异常，胆固醇胆结石疾病，癌症，非胰岛素依赖性糖尿病和代谢综合征。 受FXR调节剂影响的特别优选的疾病具有高LDL胆固醇，高甘油三酯水平和血脂异常。

    2,3-SUBSTITUTED INDAZOLE OR 4,5,6,7-TETRAHYDRO-INDAZOLES AS FXR MODULATORS AGAINST DYSLIPIDEMIA AND RELATED DISEASES
    4.
    发明申请
    2,3-SUBSTITUTED INDAZOLE OR 4,5,6,7-TETRAHYDRO-INDAZOLES AS FXR MODULATORS AGAINST DYSLIPIDEMIA AND RELATED DISEASES 审中-公开
    2,3-取代的吲唑或4,5,6,7-四氢-1H-吲唑作为抗逆转录酶和相关疾病的FXR调节剂

    公开(公告)号：WO2010034649A1

    公开(公告)日：2010-04-01

    申请号：PCT/EP2009/061912

    申请日：2009-09-15

    Applicant: F. HOFFMANN-LA ROCHE AG ,  BENSON, Gregory Martin ,  BLEICHER, Konrad ,  GRETHER, Uwe ,  KUHN, Bernd ,  RICHTER, Hans ,  TAYLOR, Sven

    Inventor： BENSON, Gregory Martin ,  BLEICHER, Konrad ,  GRETHER, Uwe ,  KUHN, Bernd ,  RICHTER, Hans ,  TAYLOR, Sven

    IPC: C07D231/56 ,  C07D401/12 ,  C07D403/12 ,  A61P3/06 ,  A61P3/10 ,  A61K31/416

    CPC classification number: C07D231/56 ,  C07D401/12 ,  C07D403/12

    Abstract: This invention relates to novel indazole or 4,5,6,7-tetrahydro-indazole derivatives of formula (I) wherein R 1 to R 8 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 used as medicaments. The compounds are selective modulators of the farnesoid-X-receptor, preferably agonists. The 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.

    Abstract translation: 本发明涉及式（I）的新的吲唑或4,5,6,7-四氢 - 吲唑衍生物，其中R 1至R 8如说明书和权利要求书中所定义，以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。 化合物是法呢基-X受体的选择性调节剂，优选激动剂。 法尼基-X受体（FXR）是转录因子的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，外周闭塞疾病，缺血性卒中，糖尿病， 胰岛素依赖性糖尿病，代谢综合征，糖尿病肾病，肥胖症，胆固醇胆结石疾病，胆汁淤积/肝纤维化，非酒精性脂肪性肝炎（NASH），非酒精性脂肪性肝病（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调节剂影响的首选疾病（和病症）是预防或治疗高LDL胆固醇水平，高甘油三酯，血脂异常，胆固醇胆结石疾病，癌症，非胰岛素依赖性糖尿病和代谢综合征。 受FXR调节剂影响的特别优选的疾病具有高LDL胆固醇，高甘油三酯水平和血脂异常。

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