sildenafil hydrochloride | 252920-86-8

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: sildenafil hydrochloride
• 英文别名: 1-[[3-(4,7-dihydro-1-methyl-7-oxo-3-propyl-1H-pyrazolo[4,3-d]pyrimidin-5-yl)-4-ethoxyphenyl]sulphonyl]-4-methylpiperazine hydrochloride；5-(2-Ethoxy-5-((4-methylpiperazin-1-yl)sulfonyl)phenyl)-1-methyl-3-propyl-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-one hydrochloride；5-[2-ethoxy-5-(4-methylpiperazin-1-yl)sulfonylphenyl]-1-methyl-3-propyl-6H-pyrazolo[4,3-d]pyrimidin-7-one;hydrochloride
• CAS: 252920-86-8
• 化学式: C₂₂H₃₀N₆O₄S*ClH
• 分子量: 511.045
• InChiKey: SYUVUKKQXAXKHL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.03
• 重原子数：
  34
• 可旋转键数：
  7
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  118
• 氢给体数：
  2
• 氢受体数：
  8

反应信息

• 作为反应物：
  描述：

  维A酸 、 sildenafil hydrochloride 在 sodium hydroxide 作用下， 以 乙醇 、 水 为溶剂， 反应 1.0h， 生成 sildenafil-retinoic acid complex salt
  参考文献：
  名称：

  PROCESSES FOR PREPARING AMINE SALTS OF SILDENAFIL-ANALOGUES AND USE THEREOF

  摘要：

  提供了一系列包括公式(I)和公式(III)结构的胺盐。在公式I或公式(III)中，R1、Ra和RX如说明书中所定义。本发明公开的胺络合盐具有前药活性形式和多种药理功能。

  公开号：

  US20120108604A1
• 作为产物：
  描述：

  西地那非 在 盐酸 作用下， 以 乙醚 为溶剂， 反应 4.0h， 以99%的产率得到sildenafil hydrochloride
  参考文献：
  名称：

  [EN] LIQUID FILLED FORMULATIONS OF PDE5 INHIBITORS
  [FR] FORMULATIONS REMPLIES LIQUIDES D'INHIBITEURS DE PDE5

  摘要：

  即时披露提供了一种包括胶囊和填充配方的组合物，用于PDE5抑制剂的疏水性盐。填充配方的实施例包含一种液体、脂质载体，在其中活性成分被溶解并以相对较高的量存在。

  公开号：

  WO2019081451A1

文献信息

• [EN] NEW PHARMACEUTICAL FORMS OF SILDENAFIL<br/>[FR] NOUVELLES FORMES PHARMACEUTIQUES DU SILDÉNAFIL
  申请人：N4 PHARMA UK LTD

  公开号：WO2017168174A1

  公开（公告）日：2017-10-05

  The invention provides a pharmaceutical composition comprising sildenafil or a pharmaceutically acceptable salt thereof admixed with excipients in a multicomponent pharmaceutical composition, wherein a first component is adapted to deliver sildenafil rapidly to promote fast onset of action, and a further component is adapted to deliver the sildenafil from dose to dose, wherein the sildenafil is delivered from dose to dose within the therapeutic window.

  这项发明提供了一种药物组合物，包括硝苯地平或其药用可接受的盐与赋形剂混合在一个多成分的药物组合物中，其中第一个成分被设计用于快速释放硝苯地平以促进快速起效，另一个成分被设计用于从一剂到另一剂地释放硝苯地平，硝苯地平在治疗窗口内从一剂到另一剂被释放。
• SAA Derivative Compound Restores eNOS And Inhibits Oxidative Stress-Induced A Diseases In Hypoxia
  申请人：JANSFAT BIOTECHNOLOGY CO., LTD.

  公开号：US20150306107A1

  公开（公告）日：2015-10-29

  The Substituted Amine Analogs (SAA) derivative compounds and SAA complex compounds disclosed in the present invention are characterized as compositions having the functions of inhibiting disorders caused by oxidative stress, and more particularly to those SAA derivative compounds capable of inhibiting disorders caused by oxidative stress because of neurodegenerative diseases, lung diseases, oxidative stress-induced heart disease and carvenosus dysfunction.

  本发明揭示的取代胺类似物（SAA）衍生物化合物和SAA复合物化合物的特征是具有抑制氧化应激引起的疾病的功能，更特别地，是那些能够抑制由于神经退行性疾病、肺部疾病、氧化应激引起的心脏疾病和海绵体功能障碍引起的疾病的SAA衍生物化合物。
• Phosphodiesterase inhibitors and nitric oxide donors, compositions and methods of use
  申请人：——

  公开号：US20040087591A1

  公开（公告）日：2004-05-06

  The invention describes novel compositions containing at least one phosphodiesterase inhibitor, and at least one compound that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents. The invention also provides methods for treating or preventing sexual dysfunctions in males and females, for enhancing sexual responses in males and females, and for treating or preventing diseases induced by the increased metabolism of cyclic guanosine 3′,5′-monophosphate (cGMP), such as hypertension, pulmonary hypertension, congestive heart failure, renal failure, myocardial infraction, stable, unstable and variant (Prinzmetal) angina, atherosclerosis, cardiac edema, renal insufficiency, nephrotic edema, hepatic edema, stroke, asthma, bronchitis, chronic obstructive pulmonary disease (COPD), cystic fibrosis, dementia, immunodeficiency, premature labor, dysmenorrhoea, benign prostatic hyperplasis (BPH), bladder outlet obstruction, incontinence, conditions of reduced blood vessel patency, e.g., postpercutaneous transluminal coronary angioplasty (post-PTCA), peripheral vascular disease, allergic rhinitis, glucoma, and diseases characterized by disorders of gut motility, e.g., irritable bowel syndrome (IBS).

  该发明描述了一种新型组合物，其中包含至少一种磷酸二酯酶抑制剂，以及至少一种捐赠、转移或释放一氧化氮、提高内皮源性松弛因子内源水平、刺激内源性一氧化氮合成或是一氧化氮合酶底物和/或一种或多种血管活性剂的化合物。该发明还提供了治疗或预防男性和女性性功能障碍、增强男性和女性性反应以及治疗或预防由环磷鸟苷3′，5′-单磷酸（cGMP）代谢增加引起的疾病的方法，如高血压、肺动脉高压、充血性心力衰竭、肾功能衰竭、心肌梗塞、稳定、不稳定和变异性（普林兹梅塔尔）心绞痛、动脉粥样硬化、心脏水肿、肾功能不全、肾病性水肿、肝性水肿、中风、哮喘、支气管炎、慢性阻塞性肺疾病（COPD）、囊性纤维化、痴呆、免疫缺陷、早产、痛经、良性前列腺增生（BPH）、膀胱出口梗阻、失禁、血管通畅度降低的疾病，例如经皮冠状动脉成形术后（post-PTCA）、外周血管疾病、变应性鼻炎、青光眼以及肠道运动障碍等疾病的特征性障碍。
• Nitrosated and nitrosylated phosphodiesterase inhibitors, compositions and methods of use
  申请人：——

  公开号：US20030023087A1

  公开（公告）日：2003-01-30

  The present invention describes novel nitrosated and/or nitrosylated phosphodiesterase inhibitors, and novel compositions containing at least one nitrosated and/or nitrosylated phosphodiesterase inhibitor, and, optionally, one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents. The present invention also provides novel compositions containing at least one phosphodiesterase inhibitor, and one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents. The present invention also provides methods for treating or preventing sexual dysfunctions in males and females, for enhancing sexual responses in males and females, and for treating or preventing diseases induced by the increased metabolism of cyclic guanosine 3′,5′-monophosphate (cGMP), such as hypertension, pulmonary hypertension, congestive heart failure, renal failure, myocardial infraction, stable, unstable and variant (Prinzmetal) angina, atherosclerosis, cardiac edema, renal insufficiency, nephrotic edema, hepatic edema, stroke, asthma, bronchitis, chronic obstructive pulmonary disease (COPD), cystic fibrosis, dementia, immunodeficiency, premature labor, dysmenorrhoea, benign prostatic hyperplasis (BPH), bladder outlet obstruction, incontinence, conditions of reduced blood vessel patency, e.g., postpercutaneous transluminal coronary angioplasty (post-PTCA), peripheral vascular disease, allergic rhinitis, glucoma, and diseases characterized by disorders of gut motility, e.g., irritable bowel syndrome (IBS).

  本发明描述了新型的亚硝酸化和/或亚硝基化的磷酸二酯酶抑制剂，以及含有至少一种亚硝酸化和/或亚硝基化的磷酸二酯酶抑制剂和，可选地，一种或多种捐赠、转移或释放一氧化氮、提高内皮源性松弛因子内源水平、刺激内源性一氧化氮合成或是一氧化氮合酶底物和/或一种或多种血管活性剂的化合物的新型组合物。本发明还提供了含有至少一种磷酸二酯酶抑制剂和一种或多种捐赠、转移或释放一氧化氮、提高内皮源性松弛因子内源水平、刺激内源性一氧化氮合成或是一氧化氮合酶底物和/或一种或多种血管活性剂的化合物的新型组合物。本发明还提供了治疗或预防男女性性功能障碍、增强男女性反应、以及治疗或预防由环磷酸鸟苷3',5'-单磷酸（cGMP）代谢增加引起的疾病的方法，如高血压、肺动脉高压、充血性心力衰竭、肾衰竭、心肌梗塞、稳定性、不稳定性和变异性（普林兹梅塔尔）心绞痛、动脉粥样硬化、心脏水肿、肾功能不全、肾病性水肿、肝性水肿、中风、哮喘、支气管炎、慢性阻塞性肺疾病（COPD）、囊性纤维化、痴呆、免疫缺陷、早产、痛经、良性前列腺增生（BPH）、膀胱出口梗阻、失禁、血管通透性降低的疾病，例如经皮冠状动脉成形术后（post-PTCA）、周围血管疾病、过敏性鼻炎、青光眼以及以肠道动力障碍为特征的疾病，例如肠易激综合征（IBS）。
• Processes for preparing amine salts of sildenafil-analogues and use thereof
  申请人：Chen Ing-Jun

  公开号：US08497370B2

  公开（公告）日：2013-07-30

  A series of amine salts including a structure of formula (I) and formula (III) have provided. In formula I or formula (III), R1, Ra and RX are as defined in the specification. The amine complex salts disclosed in the present invention are characterized in a pro-drug active form and various pharmaceutical function.

  一系列胺盐包括公式（I）和公式（III）的结构已经提供。在公式I或公式（III）中，R1、Ra和RX如规范中所定义。本发明披露的胺络合盐具有前药活性形式和各种药物功能的特点。