利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

10 条记录 (耗时 0.018 秒)

    PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT OF CHRONIC HEART FAILURE COMPRISING PYRAZOLOPYRIMIDINONE DERIVATIVE COMPOUND
    1.
    发明申请
    PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT OF CHRONIC HEART FAILURE COMPRISING PYRAZOLOPYRIMIDINONE DERIVATIVE COMPOUND 审中-公开
    用于治疗包含吡唑并吡啶酮衍生化合物的慢性心力衰竭的药物组合物

    公开(公告)号：US20100173915A1

    公开(公告)日：2010-07-08

    申请号：US12602847

    申请日：2008-06-03

    申请人： Jee-Hyun Shin ,  Gook-Jun Ahn ,  Kyung-Koo Kang ,  Byoung-Ok Ahn ,  Moo-Hi Yoo

    发明人： Jee-Hyun Shin ,  Gook-Jun Ahn ,  Kyung-Koo Kang ,  Byoung-Ok Ahn ,  Moo-Hi Yoo

    IPC分类号： A61K31/519 ,  A61P9/00 ,  C07D487/04 ,  A61P9/04

    CPC分类号： A61K31/519 ,  A61K9/2059 ,  A61K9/4866

    摘要： Disclosed herein is a therapeutic agent for chronic heart failure comprising, as an effective ingredient, 5-[2-propyloxy-5-(1-methyl-2-pyrrolidinyl-ethylamidosulfonyl)phenyl]-1-methyl-propyl-1,6-dihydro-7H-pyrazolo(4,3-d)pyrimidine-7-one. The compound inhibits phosphodiesterase-5 (PDE-5), which catalyzes the intracellular degradation of cyclic guanosine monophosphatase (cGMP), thereby mitigating several signs of chronic heart failure, that is, thereby preventing left ventricular dilatation, decreasing ventricular wall thinning, lowering elevated cardiac and circulating levels of atrial natriuretic peptide (ANP), and inhibiting ventricular fibrosis. Also, the compound has advantages in that it reaches the maximal plasma level in a short time, has an in vivo half-life longer than conventional PDE-5 inhibitors, allowing decreased administration frequency, and has fewer side effects, thus ensuring safety. Thus, the compound is useful as a therapeutic agent for chronic heart failure.

    摘要翻译： 本文公开了一种用于慢性心力衰竭的治疗剂，其包含作为有效成分的5- [2-丙氧基-5-（1-甲基-2-吡咯烷基 - 乙基氨基磺酰基）苯基] -1-甲基 - 丙基-1,6- 二氢-7H-吡唑并（4,3-d）嘧啶-7-酮。 该化合物抑制磷酸二酯酶-5（PDE-5），其催化环鸟苷酸单磷酸酶（cGMP）的细胞内降解，从而减轻慢性心力衰竭的几个迹象，从而预防左心室扩张，降低心室壁变薄，降低升高 心脏和循环水平的心房钠尿肽（ANP），并抑制心室纤维化。 此外，该化合物具有在短时间内达到最大血浆水平的优点，具有比常规PDE-5抑制剂更长的体内半衰期，允许降低给药频率，并且具有较少的副作用，从而确保安全性。 因此，该化合物可用作慢性心力衰竭的治疗剂。

    AGENT FOR THE PREVENTION AND TREATMENT OF PROSTATIC HYPERPLASIA COMPRISING PYRAZOLOPYRIMIDINONE COMPOUND
    3.
    发明申请
    AGENT FOR THE PREVENTION AND TREATMENT OF PROSTATIC HYPERPLASIA COMPRISING PYRAZOLOPYRIMIDINONE COMPOUND 有权
    预防和治疗包含吡唑并嘧啶酮化合物的预防性高血压药物

    公开(公告)号：US20090099357A1

    公开(公告)日：2009-04-16

    申请号：US12244432

    申请日：2008-11-24

    申请人： Jae Young YU ,  Seul Min CHOI ,  Kyung Koo KANG ,  Byoung Ok AHN ,  Moohi YOO

    发明人： Jae Young YU ,  Seul Min CHOI ,  Kyung Koo KANG ,  Byoung Ok AHN ,  Moohi YOO

    IPC分类号： C07D487/04 ,  A61P43/00

    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。

    Agent for the prevention and treatment of prostatic hyperplasia comprising pyrazolopyrimidinone compound
    5.
    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

    申请人： Jae Young Yu ,  Seul Min Choi ,  Kyung Koo Kang ,  Byoung Ok Ahn ,  Moohi Yoo

    发明人： Jae Young Yu ,  Seul Min Choi ,  Kyung Koo Kang ,  Byoung Ok Ahn ,  Moohi Yoo

    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。