Pyr-Phe-OH | 16947-06-1

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: Pyr-Phe-OH
• 英文别名: N-(2-Oxopropanoyl)-L-phenylalanine；(2S)-2-(2-oxopropanoylamino)-3-phenylpropanoic acid
• CAS: 16947-06-1
• 化学式: C₁₂H₁₃NO₄
• 分子量: 235.24
• InChiKey: YEALFOYYKCROFR-JTQLQIEISA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.5
• 重原子数：
  17
• 可旋转键数：
  5
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  83.5
• 氢给体数：
  2
• 氢受体数：
  4

文献信息

• Nitric Oxide Releasing Pyruvate Compounds, Compositions and Methods of Use
  申请人：Garvey David S.

  公开号：US20080287407A1

  公开（公告）日：2008-11-20

  The invention describes novel nitrosated and/or nitrosylated pyruvate compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated pyruvate compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one pyruvate compound and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one pyruvate compound, that is optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating diseases resulting from oxidative stress, diabetes, reperfusion injury following ischemia, preservation of tissues, organs, organ parts and/or limbs.

  该发明描述了新颖的硝化和/或亚硝化丙酮酸盐及其药用可接受盐，以及包含至少一种硝化和/或亚硝化丙酮酸化合物的新型组合物，以及可选地，至少一种捐赠、转移或释放一氧化氮、刺激内源性一氧化氮合成、提高内源性内皮源性舒张因子水平或是一氧化氮合酶底物的化合物，和/或至少一种治疗剂。该发明还提供了包含至少一种丙酮酸化合物和至少一种捐赠、转移或释放一氧化氮、提高内源性内皮源性舒张因子水平、刺激内源性一氧化氮合成或是一氧化氮合酶底物和/或至少一种治疗剂的新型组合物。该发明还提供了包含至少一种丙酮酸化合物的新型试剂盒，该丙酮酸化合物可选地硝化和/或亚硝化，以及可选地至少一种一氧化氮供体和/或至少一种治疗剂。该发明还提供了治疗由氧化应激、糖尿病、缺血后再灌注损伤、组织、器官、器官部分和/或肢体保护引起的疾病的方法。
• Peptidomimetic protease inhibitors
  申请人：VERTEX PHARMACEUTICALS INCORPORATED

  公开号：EP2371839A1

  公开（公告）日：2011-10-05

  The present invention relates to peptidomimetic compounds useful as protease inhibitors (1), particularly as serine protease inhibitors and more particularly as hepatitis C NS3 protease inhibitors; intermediates thereto; their preparation including novel steroselective processes to intermediates. The invention is also directed to pharmaceutical compositions and to methods for using the compounds for inhibiting HCV protease or treating a patient suffering from an HCV infection or physiological condition related to the infection. Also provided are pharmaceutical combinations comprising, in addition to one or more HCV serine protease inhibitors, one or more interferons exhibiting anti-HCV activity and/or one or more compounds having anti HCV activity and a pharmaceutically acceptable carrier, and methods for treating or preventing a HCV infection in a patient using the compositions. The present invention is also directed to a kit or pharmaceutical pack for treating or preventing HCV infection in a patient.

  本发明涉及肽类似物化合物，可用作蛋白酶抑制剂（1），特别是丝氨酸蛋白酶抑制剂，更特别是丙型肝炎NS3蛋白酶抑制剂；中间体；它们的制备，包括用于中间体的新型立体选择性过程。本发明还涉及制药组合物以及使用这些化合物抑制HCV蛋白酶或治疗患有HCV感染或与感染相关的生理状况的患者的方法。还提供了药物组合物，其中除了一个或多个HCV丝氨酸蛋白酶抑制剂外，还包括一个或多个表现出抗HCV活性的干扰素和/或一个或多个具有抗HCV活性的化合物和药学可接受的载体，并使用这些组合物治疗或预防患者的HCV感染的方法。本发明还涉及用于治疗或预防患者HCV感染的工具包或药品包。
• Compositions and methods for the treatment and prevention of chronic hypoxemia and dyspnea
  申请人：Martin Alain

  公开号：US10813893B2

  公开（公告）日：2020-10-27

  The present invention has shown that not all salts of pyruvic acid enhance lung functions or enhance the synthesis of lung surfactants and that certain salts of pyruvic acid with the correct concentrations of calcium, phosphate and magnesium, are synergistic in their ability to enhance the synthesis of lung surfactants that will enhance lung alveoli functions, while decreasing coughing and lung tightness, and increasing oxygen saturation values to prevent hypoxemia. This patent demonstrates that the sodium pyruvate formula with calcium, phosphate and magnesium was superior over standard sodium pyruvate formula in saline alone in the removal of mucus, reduction of lung or sinus infections, and in reducing drug side effects and congestion. The use of this formula clearly demonstrated that it can be used to produce better efficacy in patients with hypoxemia, with lung and sinus diseases including, asthma, COPD, cystic fibrosis, interstitial lung disease, allergic rhinitis, sinusitis, Alzheimer's, disease, Parkinson's disease, brain trauma, nicotine addiction, sleep apnea, autism, migraine headaches, sleep disorders, lung and sinus infections, cancer therapy with cancer drugs, nicotine addiction, and medications that cause a decrease in lung surfactants.

  本发明表明，并非所有丙酮酸盐都能增强肺功能或促进肺表面活性物质的合成，某些丙酮酸盐与正确浓度的钙、磷酸盐和镁协同作用，能够促进肺表面活性物质的合成，从而增强肺泡功能，同时减少咳嗽和肺部紧绷感，提高血氧饱和度值，防止低氧血症。本专利证明，在清除粘液、减少肺部或鼻窦感染、减轻药物副作用和充血方面，含钙、磷酸盐和镁的丙酮酸钠配方优于仅在生理盐水中添加的标准丙酮酸钠配方。病、帕金森病、脑外伤、尼古丁上瘾、睡眠呼吸暂停、自闭症、偏头痛、睡眠障碍、肺部和鼻窦感染、使用抗癌药物进行癌症治疗、尼古丁上瘾以及导致肺表面活性物质减少的药物。
• Synergistic compositions to stimulate the synthesis of human lung and sinus surfactants to decrease coughing, increase FEV-1/FVC ratios, decrease lung fibrosis, by increasing apoptosis of myofibroblasts
  申请人：Martin Alain

  公开号：US11311505B2

  公开（公告）日：2022-04-26

  Methods for the treatment of patients with both Chronic Obstructive Pulmonary Disease (COPD) and pulmonary fibrosis, and of patients with idiopathic pulmonary fibrosis without COPD, by stimulating the synthesis of human and animal patient lung and sinus surfactants to increase lung functions, inhibiting fibrosis and reducing coughing and nasal erythema, include the following steps: A) analyzing and diagnosing a patient with a lung ailment selected from the group consisting of i) both COPD and pulmonary fibrosis; and ii) idiopathic pulmonary fibrosis without COPD; and, B) treating the patient to raise the patient's lung functions including FEV1/FVC ratio by contacting mammalian cells with a [therapeutically effective amount of a treatment] composition that includes: a) a pyruvate salt; b) a phosphate; c) a salt of calcium; and d) a salt of magnesium, in an aqueous carrier, containing no more than 2.2 grams of said pyruvate salt per liter.

  治疗慢性阻塞性肺病（COPD）和肺纤维化患者以及无慢性阻塞性肺病的特发性肺纤维化患者的方法，通过刺激人和动物患者肺和窦表面活性物质的合成来增加肺功能、抑制肺纤维化并减少咳嗽和鼻部红斑，包括以下步骤：A）分析和诊断一名肺部疾病患者，该患者选自以下组别：i）慢性阻塞性肺病和肺纤维化；ii）无慢性阻塞性肺病的特发性肺纤维化；B）通过将哺乳动物细胞与[治疗有效量的治疗]组合物接触，对患者进行治疗，以提高患者的肺功能，包括 FEV1/FVC 比率，该组合物包括：a) 丙酮酸盐；b) 磷酸盐；c) 钙盐；d) 镁盐。2 克的丙酮酸盐。
• Methods and compositions for enhancing synthesis secretion and transport of collagen to increase wound strength
  申请人：Martin Alain

  公开号：US11458114B2

  公开（公告）日：2022-10-04

  A method for, and medicinal composition for, treatment of mammalian cells for enhancing synthesis, secretion and transport of collagen to increase wound strength, that includes magnesium pyruvate; calcium pyruvate; L proline; citrulline: and a liquid carrier.

  一种治疗哺乳动物细胞的方法和药物组合物，用于增强胶原蛋白的合成、分泌和运输，以提高伤口强度，其中包括丙酮酸镁、丙酮酸钙、L-脯氨酸、瓜氨酸和液体载体。