Agent for treatment of liver diseases containing pyrazolopyrimidinone derivative
    5.
    发明授权
    Agent for treatment of liver diseases containing pyrazolopyrimidinone derivative 有权
    用于治疗含有吡唑嘧啶酮衍生物的肝病的药剂

    公开(公告)号:US08796286B2

    公开(公告)日:2014-08-05

    申请号:US11916752

    申请日:2005-10-21

    CPC分类号: A61K31/519 C07D487/04

    摘要: The present invention relates to the pharmaceutical composition for prevention and treatment of liver diseases containing pyrazolopyrimidine derivative as an active ingredient. According to the present invention, pyrazolopyrimidine derivative has an excellent effect on inhibiting collagen synthesis in hepatic stellate cells and acts directly on the portal vein. Particularly, it may increase the diameter and the amount of blood flow of the portal vein, and finally decrease the pressure thereof. Therefore, pyrazolopyrimidine derivative can be used advantageously for prevention and treatment of hepatic fibrosis, liver cirrhosis caused by hepatic fibrosis, portal hypertension and various complications caused by portal hypertension. In addition, pyrazolopyrimidine derivative according to the present invention can reduce dosing frequency because of its long half-life, and therefore, has an advantage to improve the drug compliance of patients suffering from chronical liver diseases.

    摘要翻译: 本发明涉及用于预防和治疗含有吡唑并嘧啶衍生物作为活性成分的肝病的药物组合物。 根据本发明,吡唑并嘧啶衍生物对抑制肝星状细胞中的胶原合成具有优异的作用,直接作用于门静脉。 特别地,可能增加门静脉的直径和血流量,最终降低其压力。 因此,吡唑并嘧啶衍生物可有利地用于预防和治疗肝纤维化,肝纤维化引起的肝硬化,门静脉高压以及门静脉高压引起的各种并发症。 此外,根据本发明的吡唑并嘧啶衍生物由于其半衰期长而能降低给药频率,因此具有改善患有慢性肝病的患者的药物依从性的优点。

    Agent for the prevention and treatment of prostatic hyperplasia comprising pyrazolopyrimidinone compound
    6.
    发明授权
    Agent for the prevention and treatment of prostatic hyperplasia comprising pyrazolopyrimidinone compound 有权
    用于预防和治疗包含吡唑并嘧啶酮化合物的前列腺增生的药剂

    公开(公告)号:US08148386B2

    公开(公告)日:2012-04-03

    申请号:US12244432

    申请日:2008-11-24

    IPC分类号: A01N43/90

    CPC分类号: A61K31/519

    摘要: The present invention relates to an agent for preventing and treating benign prostatic hyperplasia (BPH) and lower urinary tract symptoms (LUTS) associated with BPH and a relaxant for relaxing urethral smooth muscle or prostatic smooth muscle comprising a pyrazolopyrimidinone compound as an effective ingredient. The agent in accordance with the present invention can provide nitric oxides by inhibiting the activity of PDE-5 that decomposes c-GMP, and the provided nitric oxides relax the urethral smooth muscle or the prostatic smooth muscle to lower the intraurethral pressure (IUP), thus treating BPH and LUTS associated with BPH. Furthermore, the time required for reaching a maximum blood concentration is shorter and the half-life is longer than the other PDE-5 inhibitors, thus reducing the frequency of administration. Moreover, the agent of the invention causing few side effects can be efficiently used as a safe drug.

    摘要翻译: 本发明涉及用于预防和治疗与BPH相关的良性前列腺增生症(BPH)和下尿路症状(LUTS)的药剂和用于缓解包含吡唑嘧啶酮化合物作为有效成分的尿道平滑肌或前列腺平滑肌的松弛剂。 根据本发明的药剂可以通过抑制分解c-GMP的PDE-5的活性来提供一氧化氮,并且所提供的一氧化氮使尿道平滑肌或前列腺平滑肌松弛以降低尿道内压(IUP), 从而治疗与BPH相关的BPH和LUTS。 此外,达到最大血液浓度所需的时间更短,半衰期比其他PDE-5抑制剂长,从而降低给药频率。 此外,本发明的副作用少的药剂可以有效地用作安全药物。

    7-carboxymethyloxy-3′,4′,5-trimethoxy flavone monohydrate, the preparation method and uses thereof
    8.
    发明授权
    7-carboxymethyloxy-3′,4′,5-trimethoxy flavone monohydrate, the preparation method and uses thereof 失效
    7-羧甲氧基-3',4',5-三甲氧基黄酮一水合物,其制备方法和用途

    公开(公告)号:US07371775B2

    公开(公告)日:2008-05-13

    申请号:US10564128

    申请日:2004-09-04

    IPC分类号: A61K31/353 C07D311/30

    摘要: The present invention relates to 7-carboxymethyloxy-3′,4′,5-trimethoxy flavone.monohydrate which is a non hygroscopic product suitable for the preparation of metered dose of 7-carboxymethyloxy-3′,4′,5-trimethoxy flavone having protective activity for gastrointestinal tract including the colon, and a preparation method and uses thereof. 7-carboxymethyloxy-3′,4′,5-trimethoxy flavone.monohydrate of the present invention has advantages such as mucus protecting activity for gastrointestinal tract including the colon, convenience for handling and storage under ordinary humidity owing to its non-hygroscopicity, and ability to contain an active compound consistently for the formulation production of a medicine. In addition, the preparation method of 7-carboxymethyloxy-3′,4′,5-trimethoxy flavone.monohydrate of the present invention reduces long steps of total synthesis and requires mild conditions for the production of a compound because autoclave condition is not necessary for methylation in this case, and makes mass-production possible without any purification process such as recrystallization or column chromatography.

    摘要翻译: 本发明涉及7-羧甲氧基-3',4',5-三甲氧基黄酮一水合物,它是适用于制备计量剂量的7-羧甲氧基-3',4',5-三甲氧基黄酮的非吸湿产品,其具有 包括结肠在内的胃肠道的保护活性及其制备方法和用途。 本发明的7-羧甲氧基-3',4',5-三甲氧基黄酮一水合物具有诸如包括结肠在内的胃肠道的粘液保护活性,由于其不吸湿性而在常湿下容易处理和储存的优点,以及 能够一致地含有活性化合物来制备药物。 此外,本发明的7-羧甲氧基-3',4',5-三甲氧基黄酮一水合物的制备方法减少了总合成的长步骤,并且由于不需要高压灭菌条件,因此对于化合物的制备需要温和的条件 在这种情况下甲基化,并且可以在没有任何纯化方法如重结晶或柱色谱法的情况下批量生产。

    7-Carboxymethyloxy-3',4',5-trimethoxy flavone monohydrate, the preparation method and uses thereof
    9.
    发明申请
    7-Carboxymethyloxy-3',4',5-trimethoxy flavone monohydrate, the preparation method and uses thereof 失效
    7-羧甲氧基-3',4',5-三甲氧基黄酮一水合物,其制备方法和用途

    公开(公告)号:US20060178428A1

    公开(公告)日:2006-08-10

    申请号:US10564128

    申请日:2004-09-04

    IPC分类号: A61K31/353 C07D311/74

    摘要: The present invention relates to 7-carboxymethyloxy-3′, 4′, 5-trimethoxy flavone.monohydrate which is a non hygroscopic product suitable for the preparation of metered dose of 7-carboxymethyloxy-3′, 4′, 5-trimethoxy flavone having protective activity for gastrointestinal tract including the colon, and a preparation method and uses thereof. 7-carboxymethyloxy-3′, 4′, 5-trimethoxy flavone.monohydrate of the present invention has advantages such as mucus protecting activity for gastrointestinal tract including the colon, convenience for handling and storage under ordinary humidity owing to its non-hygroscopicity, and ability to contain an active compound consistently for the formulation production of a medicine. In addition, the preparation method of 7-carboxymethyloxy-3′, 4′, 5-trimethoxy flavone.monohydrate of the present invention reduces long steps of total synthesis and requires mild conditions for the production of a compound because autoclave condition is not necessary for methylation in this case, and makes mass-production possible without any purification process such as recrystallization or column chromatography.

    摘要翻译: 本发明涉及7-羧甲氧基-3',4',5-三甲氧基黄酮一水合物,它是适用于制备计量剂量的7-羧甲氧基-3',4',5-三甲氧基黄酮的非吸湿产品,其具有 包括结肠在内的胃肠道的保护活性及其制备方法和用途。 本发明的7-羧甲氧基-3',4',5-三甲氧基黄酮一水合物具有诸如包括结肠在内的胃肠道的粘液保护活性,由于其不吸湿性而在常湿下容易处理和储存的优点,以及 能够一致地含有活性化合物来制备药物。 此外,本发明的7-羧甲氧基-3',4',5-三甲氧基黄酮一水合物的制备方法减少了总合成的长步骤,并且由于不需要高压灭菌条件,因此对于化合物的制备需要温和的条件 在这种情况下甲基化,并且可以在没有任何纯化方法如重结晶或柱色谱法的情况下批量生产。