首页> 外国专利> A prophylactic and therapeutic agent for benign prostatic hyperplasia comprising a pyrazolopyrimidinone compound as an active ingredient

A prophylactic and therapeutic agent for benign prostatic hyperplasia comprising a pyrazolopyrimidinone compound as an active ingredient

机译：吡唑并嘧啶酮化合物作为有效成分的前列腺增生的预防和治疗剂

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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.

机译：本发明涉及一种预防和治疗与前列腺增生相关的良性前列腺增生（BPH）和下尿路症状（LUTS）的药物，以及一种用于松弛尿道平滑肌或前列腺平滑肌的松弛剂，其包含吡唑并吡咯烷二酮化合物作为有效成分。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可以放松尿道平滑肌或前列腺平滑肌，从而降低尿道内压（IUP），从而治疗BPH和与BPH相关的LUTS。此外，与其他PDE-5抑制剂相比，达到最大血药浓度所需的时间更短，半衰期更长，因此降低了给药频率。此外，引起副作用少的本发明的试剂可以有效地用作安全药物。

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公开/公告号JP2009532463A

专利类型
公开/公告日2009-09-10

原文格式PDF
申请/专利权人ドン・ア・ファーム・カンパニー・リミテッド;
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申请/专利号JP20090504098
发明设计人ユ;ジェヤング;チョイ;スルミン;カン;キュンクー;アーン;ビョンオク;ヨー;ムーヒ;
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申请日2006-04-04
分类号A61K31/519;A61P13/02;A61P13/08;A61P43;C07D487/04;
国家 JP
入库时间 2022-08-21 19:43:07

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1. A comparative study of thulium laser resection of the prostate-Tangerine technique and transurethral re-section of the prostate for the treatment of benign prostatic hyperplasia [J] . 卓见中国医学文摘：外科学分册英文版 . 2007,第002期

2. The Self-Administered International Prostate Symptoms Score (IPSS) Questionnaire of Kosovo Men with Benign Prostatic Hyperplasia [J] . Musa Oruqi, Elvana Podvorica, Jeton Islamaj 泌尿学期刊（英文） . 2021,第010期

3. Correlation between Prostatic Calculi and Benign Prostatic Hyperplasia [J] . Ruipeng Tang, Chuan Xiao 内分泌系统研究(英文) . 2020,第001期

4. Telfairia occidentalis Leaf and Seed Extracts asPossible Preventive and Therapeutic Agents forInduced Benign Prostatic Hyperplasia [J] . Rotimi Sunday Ajani, Akinsola Raphael Akinyemi European Journal of Medicinal Plants . 2015,第1期

5. Evaluation of the therapeutic effect against benign prostatic hyperplasia and the active constituents from Epilobium angustifolium L. [J] . Deng Liqing, Zong Wei, Tao Xueying, Journal of Ethnopharmacology: An Interdisciplinary Journal Devoted to Bioscientific Research on Indigenous Drugs . 2019,第期

6. Potential repositioning of GV1001 as a therapeutic agent for testosterone-induced benign prostatic hyperplasia [J] . Kim Kyeong Seok, Yang Hun Yong, Chang Seung-Cheol, International journal of molecular medicine . 2018,第4期

7. Analysis of glycoforms of urinary prostate-specific antigen of prostate cancer and benign prostate hyperplasia samples [C] . Chun-Jen Hsiao, Tzong-Shin Tzai, Chein-Hung Chen, ASMS Conference on Mass Spectrometry and Allied Topics . 2015

8. The Feasibility of Fourier Transform Infrared Imaging Spectroscopy in Discriminating Benign Prostatic Hyperplasia From Prostate Cancer in Blood Serum Samples [D] . Monjardez, Geraldine. 2013

9. Serum antibodies against genitourinary infectious agents in prostate cancer and benign prostate hyperplasia patients: a case-control study [O] . Jan Hrbacek, Michael Urban, Eva Hamsikova, 2011

10. Poster session 2Morphogenetic mechanisms290MiR-133 regulates retinoic acid pathway during early cardiac chamber specification291Bmp2 regulates atrial differentiation through miR-130 during early heart looping formationDevelopmental genetics294Association of deletion allele of insertion/deletion polymorphism in alpha 2B adrenoceptor gene and hypertension with or without type 2 diabetes mellitus295Association of G1359A polymorphism of the endocannabinoid type 1 receptor (CNR1) with coronary artery disease (CAD) with type 2 diabetes mellitusCell growth, differentiation and stem cells - Vascular298Gamma-secretase inhibitor prevents proliferation and migration of ductus arteriosus smooth muscle cells: a role of Notch signaling in postnatal closure of ductus arteriosus299Mesenchymal stromal-like cells (MLCs) derived from induced pluripotent stem (iPS) cells: a promising therapeutic option to promote neovascularization300Sonic Hedgehog promotes mesenchymal stem cell differentiation to vascular smooth muscle cells in cardiovacsular disease301Proinflammatory cytokine secretion and epigenetic modification in endothelial cells treated LPS-GinfivalisCell death and apoptosis - Vascular304Mitophagy acts as a safeguard mechanism against human vascular smooth muscle cell apoptosis induced by atherogenic lipidsTranscriptional control and RNA species - Vascular307MicroRNA-34a role in vascular calcification308Local delivery of a miR-146a inhibitor utilizing a clinically applicable approach attenuates neointima formation after vascular injury309Long noncoding RNA landscape of hypoxic endothelial cells310Specific circulating microRNAs levels associate with hypertension, hyperglycemia and dysfunctional HDL in acute coronary syndrome patientsCytokines and cellular inflammation - Vascular313Phosphodiesterase5A up-regulation in vascular endothelium under pro-inflammatory conditions: a newly disclosed anti-inflammatory activity for the omega-3polyunsaturated aatty acid docosahexaenoic acid314Cardiovascular risk modifying with extra-low dose anticytokine drugs in rhematoid arthritis315Conversion of human M-CSF macrophages into foam cells reduces their proinflammatory responses to classical M1-polarizing activation316Lymphocytic myocarditis coincides with increased plaque inflammation and plaque hemorrhage in coronary arteries, facilitating myocardial infarction317Serum osteoprotegerin level predictsdeclined numerous of circulating endothelial- derived and mononuclear-derived progenitor cells in patients with metabolic syndromeGrowth factors and neurohormones - Vascular320Effect of gastrin-releasing peptide (GRP) on vascular inflammationSignal transduction - Heart323A new synthetic peptide regulates hypertrophy in vitro through means of the inhibition of nfkb324Inducible fibroblast-specific knockout of p38 alpha map kinase is cardioprotective in a mouse model of isoproterenol-induced cardiac hypertrophy325Regulation of beta-adrenoceptor-evoked inotropic responses by inhibitory G protein, adenylyl cyclase isoforms 5 and 6 and phosphodiesterases326Binding to RGS3 and stimulation of M2 muscarinic acetylcholine receptors modulates the substrate specificity of p190RhoGAP in cardiac myocytes327Cardiac regulation of post-translational modifications, parylation and deacetylation in LMNA dilated cardiomyopathy mouse model328Beta-adrenergic regulation of the b56delta/pp2a holoenzyme in cardiac myocytes through b56delta phosphorylation at serine 573Nitric oxide and reactive oxygen species - Vascular331Oxidative stress-induced miR-200c disrupts the regulatory loop among SIRT1, FOXO1 and eNOS332Antioxidant therapy prevents oxidative stress-induced endothelial dysfunction and Enhances Wound Healing333Morphological and biochemical characterization of red blood cell in coronary artery diseaseCytoskeleton and mechanotransduction - Heart336Novel myosin activator, JSH compounds, increased myocardial contractility without chronotropic effect in ratsExtracellular matrix and fibrosis - Vascular339Ablation of Toll-like receptor 9 causes cardiac rupture after myocardial infarction by attenuating proliferation and differentiation of cardiac fibroblasts340Altered vascular remodeling in the mouse hind limb ischemia model in Factor VII activating protease (FSAP) deficiencyVasculogenesis, angiogenesis and arteriogenesis343Pro-angiogenic effects of proly-hydroxylase inhibitors and their potential for use in a novel strategy of therapeutic angiogenesis for coronary total occlusion344Nrf2 drives angiogenesis in transcription-independent manner: new function of the master regulator of oxidative stress response345Angiogenic gene therapy, despite efficient vascular growth, is not able to improve muscle function in normoxic or chronically ischemic rabbit hindlimbs -role of capillary arterialization and shunting346Effect of PAR-1 inhibition on collateral vessel growth in the murine hind limb model347Quaking is a key regulator of endothelial cell differentiation, neovascularization and angiogenesis348"Emerging angiogenesis" in the chick chorioallantoic membrane (CAM). 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V Garcia-Martinez, C Lopez Sanchez, W Hamed, 2016

1. Serum testosterone and prostate-specific antigen levels are major risk factors for prostatic volume increase among benign prostatic hyperplasia patients [J] . Gede Wirya Kusuma Duarsa ,Yudit Anastasia Sari ,Anak Agung Gde Oka . 亚洲泌尿外科杂志(英文) . 2021,第3期

2. Expression and significance of clusterin in normal prostate, benign prostate hyperplasia and prostate cancer [J] . 周利群 . 外科研究与新技术 . 2003,第2期

3. 1-苯基-3-甲基吡唑并4,3-e-1,2,4-三唑并2,3-a嘧啶-4-酮及衍生物的合成与生物活性 [C] . 刘莹 ,任军 ,付煜 . 第八届全国有机合成学术会议 . 2000

4. 新型吡唑并四嗪酮类及吡唑并嘧啶二酮类化合物的设计、合成及生物活性的研究 [A] . 吴超 . 2005