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    • 1. 发明申请
    • PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT OF CHRONIC HEART FAILURE COMPRISING PYRAZOLOPYRIMIDINONE DERIVATIVE COMPOUND
    • 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
    • US20100173915A1
    • 2010-07-08
    • US12602847
    • 2008-06-03
    • Jee-Hyun ShinGook-Jun AhnKyung-Koo KangByoung-Ok AhnMoo-Hi Yoo
    • Jee-Hyun ShinGook-Jun AhnKyung-Koo KangByoung-Ok AhnMoo-Hi Yoo
    • A61K31/519A61P9/00C07D487/04A61P9/04
    • A61K31/519A61K9/2059A61K9/4866
    • 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.
    • 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。