羟氯喹-d4O-硫酸盐 | 103152-84-7

• 物质功能分类: 有机原料 - 羧酸类化合物及衍生物
• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 中文名称: 羟氯喹-d4O-硫酸盐
• 中文别名: 羟氯喹邻硫酸盐
• 英文名称: Hydroxychloroquine O-Sulfate
• 英文别名: 2-[4-[(7-chloroquinolin-4-yl)amino]pentyl-ethylamino]ethyl hydrogen sulfate
• CAS: 103152-84-7
• 化学式: C₁₈H₂₆ClN₃O₄S
• 分子量: 415.9
• InChiKey: HDHZUDNKLODXFR-UHFFFAOYSA-N

物化性质

• 密度：
  1.329±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.9
• 重原子数：
  27
• 可旋转键数：
  11
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  100
• 氢给体数：
  2
• 氢受体数：
  7

文献信息

• AEROSOLIZATION OF HCQ OR ITS METABOLITES FOR THE TREATMENT OF LUNG INFECTIONS
  申请人：INSERM (Institut National de la Santé et de la Recherche Médicale)

  公开号：EP3892275A1

  公开（公告）日：2021-10-13

  Coronaviruses cause severe diseases mainly of the respiratory and gastrointestinal tract. The infection of humans with coronaviruses have been known since the sixties to be associated with respiratory tract i.e. common cold-like diseases. Severe Acute Respiratory Syndrome-Corona Virus (SARS-CoV) is a highly aggressive in humans with often fatal outcome. The inventors aim at developing a new prophylactic or preventive therapeutic approach as well as a curative therapeutic approach based on the local delivery of hydroxychloroquine (HCQ) or its metabolite (e.g. Desethylhydroxychloroquine (DHCQ)) into the lung by aerosolization. The present invention relates to a method of treating Severe Acute Respiratory Syndrome-Corona Virus (SARS-CoV) in a patient in need thereof comprising administering to the patient's lungs a therapeutically effective amount of hydroxychloroquine (HCQ) and/or Desethylhydroxychloroquine (DHCQ) by aerosolization.

  冠状病毒主要引起呼吸道和胃肠道的严重疾病。自六十年代以来，人们就知道冠状病毒感染人类会引起呼吸道疾病，即类似普通感冒的疾病。严重急性呼吸系统综合症--冠状病毒（SARS-CoV）对人类的侵袭性很强，往往会导致死亡。本发明者旨在开发一种新的预防性治疗方法，以及一种基于羟基氯喹（HCQ）或其代谢物（如去乙基羟基氯喹（DHCQ））通过气溶胶局部输送到肺部的治疗方法。本发明涉及一种治疗严重急性呼吸系统综合症-科罗纳病毒（SARS-CoV）的方法，该方法包括通过气溶胶化给患者肺部注射治疗有效量的羟氯喹（HCQ）和/或去乙基羟氯喹（DHCQ）。
• A MIXTURE FOR TRANSDERMAL DELIVERY OF LOW AND HIGH MOLECULAR WEIGHT COMPOUNDS
  申请人：ORYXE

  公开号：EP1765310B1

  公开（公告）日：2015-10-28
• USE OF LOW DOSES OF HYDROXYCHLOROQUINE FOR THE TREATMENT OF LIPIN-1 DEFICIENCY
  申请人：Institut National de la Santé et de la Recherche Médicale (INSERM)

  公开号：EP4100011A1

  公开（公告）日：2022-12-14
• [EN] USE OF LOW DOSES OF HYDROXYCHLOROQUINE FOR THE TREATMENT OF LIPIN-1 DEFICIENCY<br/>[FR] UTILISATION DE FAIBLES DOSES D'HYDROXYCHLOROQUINE POUR LE TRAITEMENT DE LA DÉFICIENCE EN LIPIN-1
  申请人：INST NAT SANTE RECH MED

  公开号：WO2021156369A1

  公开（公告）日：2021-08-12

  Lipin-1 deficiency is a rare, life-threatening condition that causes severe rhabdomyolysis episodes (RM) triggered by febrile illness and effort. Now, the inventors treated 10 patients with LPIN1 mutations with hydroxychloroquine (HCQ) in an off open-label use phases 1 and 2 study, to assess safety, clinical, and biological effects of the drug. A first inclusion group of patients were treated with oral HCQ at a dose of 6.5 mg/Kg/day in one intake, not exceeding 400 mg/day. Five patients have not presented any new acute RM under treatment, except for 2 patients experimented one and two episodes of RM respectively despite HCQ in a context of gastroenteritis. Plasma levels of HCQ were in the range of 400 ng/ml except in the two patients who experimented RM, in whom the plasma HCQ levels were higher (1000 ng/ml). With a therapeutic adjustment, in order to maintain plasma levels of HCQ under 700 ng/ml, in a new group of patients, two patients did not suffer from new acute RM under treatment. HCQ had not seem to have benefit effect for one patient.Thus, the inventors describe the first human experience with HCQ for Lipin-1 disease. The results allow the inventors to propose low doses of HCQ as a long-term treatment to prevent further relapses in this severe disease.
• [EN] AEROSOLIZATION OF HDL FOR THE TREATMENT OF LUNG INFECTIONS<br/>[FR] AÉROSOLISATION DE HDL POUR TRAITER DES INFECTIONS PULMONAIRES
  申请人：INST NAT SANTE RECH MED

  公开号：WO2021191266A1

  公开（公告）日：2021-09-30

  Lung infections remain a substantial concern, even in wealthy countries. For instance, the emergence of a new betacoronavirus SARS-CoV-2 has led to a major health-related crisis associated with a significant mortality in intensive care units, due to the pulmonary complications of COVID-19. The inventors aim at developing a new therapeutic approach based on the local delivery of apolipoprotein A1 nanoparticles into the lung by aerosolization. These particles may display antiviral properties that could be improved by loading them with small interference RNAs specifically targeting SARS-CoV2 genome and antiviral drugs (such as the hydrophobic chloroquine). Their preliminary results have shown in preclinical mouse models that aerosolization allowed apoA1 nanoparticle uptake and persistence (up to 72h) in pulmonary cells. In addition to the potential intrinsic antiviral activity of apoA1, these particle display important anti-inflammatory effects that may limit the excessive immuno-inflammatory host response that is deleterious for the lung. Thus, the present invention relates to aerosolization of HDL for the treatment of lung infections.