(2S,5R,6R)-6-[[(2R)-2-amino-2-(4-hydroxyphenyl)acetyl]amino]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid;(2S,5R,6R)-6-[[(2R)-2-amino-2-phenylacetyl]amino]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid | 156839-56-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 内酰胺类
• 英文名称: (2S,5R,6R)-6-[[(2R)-2-amino-2-(4-hydroxyphenyl)acetyl]amino]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid;(2S,5R,6R)-6-[[(2R)-2-amino-2-phenylacetyl]amino]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid
• CAS: 156839-56-4
• 化学式: C32H38N6O9S2
• 分子量: 714.8
• InChiKey: OSLJNGILIBLERD-TUQWAVKASA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.34
• 重原子数：
  49
• 可旋转键数：
  8
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.44
• 拓扑面积：
  296
• 氢给体数：
  7
• 氢受体数：
  13

文献信息

• CHRYSOPHAENTIN ANALOGS THAT INHIBIT FTSZ PROTEIN
  申请人：Bewley Carole A.

  公开号：US20130331460A1

  公开（公告）日：2013-12-12

  Embodiments of antimicrobial chrysophaentin compounds, pharmaceutical compositions including the chrysophaentin compounds, methods for using the chrysophaentin compounds, and methods for synthesizing the chrysophaentin compounds are disclosed. Certain embodiments of the chrysophaentin compounds inhibit FtsZ protein, thereby inhibiting the growth of clinically relevant bacteria, including drug-resistant strains.

  本文揭示了抗微生物药物Chrysophaentin化合物的实施例，包括该化合物的制药组合物，使用该化合物的方法以及合成该化合物的方法。某些实施例的Chrysophaentin化合物抑制FtsZ蛋白，从而抑制临床相关细菌的生长，包括耐药菌株。
• Beta-lactamases with improved properties for therapy
  申请人：Synthetic Biologics, Inc.

  公开号：US10011824B2

  公开（公告）日：2018-07-03

  This invention relates to, in part, compositions of beta-lactamases and methods of using these enzymes in, for example, gastrointestinal tract (GI tract) disorders such as C. difficile infection (CDI).

  本发明部分涉及β-内酰胺酶组合物以及将这些酶用于例如艰难梭菌感染（CDI）等胃肠道疾病的方法。
• Modified beta-lactamases and methods and uses related thereto
  申请人：Synthetic Biologics, Inc.

  公开号：US10041056B2

  公开（公告）日：2018-08-07

  The present invention relates to pharmaceuticals and modified beta-lactamases. Specifically, the invention relates to novel recombinant beta-lactamases and pharmaceutical compositions comprising the beta-lactamases. Also, the present invention relates to methods for modifying a beta-lactamase, producing the beta-lactamase and treating or preventing beta-lactam antibiotic induced adverse effects. Furthermore, the present invention relates to the beta-lactamase for use as a medicament and to the use of the beta-lactamase in the manufacture of a medicament for treating or preventing beta-lactam antibiotics induced adverse effects. Still further, the invention relates to a polynucleotide and a host cell comprising the polynucleotide.

  本发明涉及药物和改良β-内酰胺酶。具体而言，本发明涉及新型重组β-内酰胺酶和包含β-内酰胺酶的药物组合物。 此外，本发明还涉及改造β-内酰胺酶、生产β-内酰胺酶和治疗或预防β-内酰胺类抗生素诱导的不良反应的方法。此外，本发明还涉及作为药物使用的β-内酰胺酶，以及在生产治疗或预防β-内酰胺类抗生素诱发的不良反应的药物中使用β-内酰胺酶。 此外，本发明还涉及一种多核苷酸和包含该多核苷酸的宿主细胞。
• 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。