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    Organic Compounds
    2.
    发明申请
    Organic Compounds 审中-公开
    有机化合物

    公开(公告)号：US20090281161A1

    公开(公告)日：2009-11-12

    申请号：US12304425

    申请日：2007-06-11

    申请人： Juergen Klaus Maibaum ,  Edwige Liliane Jeanne Lorthiois

    发明人： Juergen Klaus Maibaum ,  Edwige Liliane Jeanne Lorthiois

    IPC分类号： A61K31/4025 ,  A61K31/40 ,  C07D207/14 ,  C07D405/12

    CPC分类号： C07D405/12 ,  C07D207/14

    摘要： Novel 3,4-di-, 3,3,4-di-, 3,4,4,-tri- and 3,3,4,4-tetra-substituted pyrrolidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on inappropriate activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on inappropriate activity of renin; the use of a compound of that class in the treatment of a disease that depends on inappropriate activity of renin; pharmaceutical formulations comprising a said substituted pyrrolidine compound, and/or a method of treatment comprising administering a said substituted pyrrolidine compound, a method for the manufacture of said substituted pyrrolidine compounds, and novel intermediates and partial steps for their synthesis are described. The substituted pyrrolidine compounds are especially of the formula (I) wherein the substituents are as described in the specification.

    摘要翻译： 新型3,4-二，3,3,4-二，3,4,4， - 和 - 3,3,4,4-四取代的吡咯烷化合物，用于诊断和治疗 治疗温血动物，特别是治疗依赖于肾素不适当活动的疾病（=病症）; 使用该类化合物制备用于治疗依赖于肾素不适当活性的疾病的药物制剂; 使用该类化合物治疗依赖肾素不适当活动的疾病; 包括所述取代的吡咯烷化合物的药物制剂和/或包括施用所述取代的吡咯烷化合物的方法，制备所述取代的吡咯烷化合物的方法和新的中间体及其合成的部分步骤。 取代的吡咯烷化合物特别是式（I），其中取代基如说明书中所述。

    4-phenylpiperidine derivatives as renin inhibitors
    7.
    发明授权
    4-phenylpiperidine derivatives as renin inhibitors 失效
    4-苯基哌啶衍生物作为肾素抑制剂

    公开(公告)号：US08362040B2

    公开(公告)日：2013-01-29

    申请号：US12789892

    申请日：2010-05-28

    申请人： Richard Sedrani ,  Juergen Klaus Maibaum ,  Werner Breitenstein ,  Holger Sellner ,  Claus Ehrhardt ,  Nils Ostermann

    发明人： Richard Sedrani ,  Juergen Klaus Maibaum ,  Werner Breitenstein ,  Holger Sellner ,  Claus Ehrhardt ,  Nils Ostermann

    IPC分类号： A01N43/40 ,  A61K31/445 ,  C07D211/40 ,  C07D211/54

    CPC分类号： C07D401/10 ,  C07D211/42 ,  C07D405/04 ,  C07D409/10

    摘要： Compounds of the present invention having the formula exhibit inhibitory activity on the natural enzyme renin. Thus, compounds of formula (I) may be employed for the treatment of hypertension, atherosclerosis, unstable coronary syndrome, congestive heart failure, cardiac hypertrophy, cardiac fibrosis, cardiomyopathy postinfarction, unstable coronary syndrome, diastolic dysfunction, chronic kidney disease, hepatic fibrosis, complications resulting from diabetes, such as nephropathy, vasculopathy and neuropathy, diseases of the coronary vessels, restenosis following angioplasty, raised intra-ocular pressure, glaucoma, abnormal vascular growth, hyperaldosteronism, cognitive impairment, alzheimers, dementia, anxiety states and cognitive disorders.

    摘要翻译： 具有下式的本发明化合物对天然酶肾素表现出抑制活性。 因此，式（I）化合物可用于治疗高血压，动脉粥样硬化，不稳定冠状动脉综合征，充血性心力衰竭，心脏肥大，心脏纤维化，心肌梗塞后梗死，冠状动脉综合征不稳定，舒张功能障碍，慢性肾脏疾病，肝纤维化， 糖尿病引起的并发症如肾病，血管病变和神经病变，冠状血管疾病，血管成形术后再狭窄，眼内压升高，青光眼，异常血管生长，醛固酮增多症，认知障碍，阿尔茨海默病，痴呆，焦虑状态和认知障碍。

    4-Phenylpiperidine derivatives as renin inhibitors
    9.
    发明申请
    4-Phenylpiperidine derivatives as renin inhibitors 审中-公开
    4-苯基哌啶衍生物作为肾素抑制剂

    公开(公告)号：US20070078164A1

    公开(公告)日：2007-04-05

    申请号：US10580296

    申请日：2004-11-25

    申请人： Richard Sedrani ,  Juergen-Klaus Maibaum ,  Werner Breitenstein ,  Holger Sellner ,  Claus Ehrhardt ,  Nils Ostermann

    发明人： Richard Sedrani ,  Juergen-Klaus Maibaum ,  Werner Breitenstein ,  Holger Sellner ,  Claus Ehrhardt ,  Nils Ostermann

    IPC分类号： A61K31/454 ,  C07D401/02

    CPC分类号： C07D401/10 ,  C07D211/42 ,  C07D405/04 ,  C07D409/10

    摘要： Compounds of the present invention having the formula exhibit inhibitory activity on the natural enzyme renin. Thus, compounds of formula (I) may be employed for the treatment of hypertension, atherosclerosis, unstable coronary syndrome, congestive heart failure, cardiac hypertrophy, cardiac fibrosis, cardiomyopathy postinfarction, unstable coronary syndrome, diastolic dysfunction, chronic kidney disease, hepatic fibrosis, complications resulting from diabetes, such as nephropathy, vasculopathy and neuropathy, diseases of the coronary vessels, restenosis following angioplasty, raised intra-ocular pressure, glaucoma, abnormal vascular growth, hyperaldosteronism, cognitive impairment, alzheimers, dementia, anxiety states and cognitive disorders.

    摘要翻译： 具有下式的本发明化合物对天然酶肾素表现出抑制活性。 因此，式（I）化合物可用于治疗高血压，动脉粥样硬化，不稳定冠状动脉综合征，充血性心力衰竭，心脏肥大，心脏纤维化，心肌梗塞后梗死，冠状动脉综合征不稳定，舒张功能障碍，慢性肾脏疾病，肝纤维化， 糖尿病引起的并发症如肾病，血管病变和神经病变，冠状血管疾病，血管成形术后再狭窄，眼内压升高，青光眼，异常血管生长，醛固酮增多症，认知障碍，阿尔茨海默病，痴呆，焦虑状态和认知障碍。