N,N-dimethyl-carbamoylmethyl p-(p-guanidinobenzoyloxy)phenylacetate acetate

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 缩酚酸和缩酚酸环醚类
• 英文名称: N,N-dimethyl-carbamoylmethyl p-(p-guanidinobenzoyloxy)phenylacetate acetate
• 英文别名: Acetic acid;[4-[2-[2-(dimethylamino)-2-oxoethoxy]-2-oxoethyl]phenyl] 4-(diaminomethylideneamino)benzoate
• 化学式: C₂H₄O₂*C₂₀H₂₂N₄O₅
• 分子量: 458.471
• InChiKey: PXZSCOICDHBRHM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.08
• 重原子数：
  33
• 可旋转键数：
  9
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.23
• 拓扑面积：
  175
• 氢给体数：
  3
• 氢受体数：
  8

反应信息

• 作为产物：
  描述：

  溶剂黄146 、 卡莫司他 以 水 、 异丙醇 为溶剂， 以89.5%的产率得到N,N-dimethyl-carbamoylmethyl p-(p-guanidinobenzoyloxy)phenylacetate acetate
  参考文献：
  名称：

  WO2006/108643

  摘要：

  公开号：

文献信息

• Organic compounds
  申请人：Novartis AG

  公开号：EP2253612A1

  公开（公告）日：2010-11-24

  The invention describes novel pharmaceutically acceptable salt forms of camostat, processes for lyophilisation, taste-masked formulations, nebulised formulations and the use of each of the fore-going in the treatment of respiratory diseases, particularly cystic fibrosis and chronic obstructive pulmonary disease (COPD).

  本发明描述了卡莫司他的新型药学可接受盐形式、冻干工艺、掩味制剂、雾化制剂以及上述每种制剂在治疗呼吸系统疾病，特别是囊性纤维化和慢性阻塞性肺病（COPD）中的应用。
• ORGANIC COMPOUNDS
  申请人：Novartis AG

  公开号：EP1874726A2

  公开（公告）日：2008-01-09
• Organic Compounds
  申请人：Danahay Henry Luke

  公开号：US20120208882A1

  公开（公告）日：2012-08-16

  The invention describes novel pharmaceutically acceptable salt forms of camostat, processes for lyophilisation, taste-masked formulations, nebulised formulations and the use of each of the fore-going in the treatment of respiratory diseases, particularly cystic fibrosis and chronic obstructive pulmonary disease (COPD).
• [EN] ORGANIC COMPOUNDS<br/>[FR] COMPOSES ORGANIQUES
  申请人：NOVARTIS AG

  公开号：WO2006108643A2

  公开（公告）日：2006-10-19

  [EN] The invention describes novel pharmaceutically acceptable salt forms of camostat, processes for lyophilisation, taste-masked formulations, nebulised formulations and the use of each of the fore-going in the treatment of respiratory diseases, particularly cystic fibrosis and chronic obstructive pulmonary disease (COPD).
  [FR] L'invention se rapporte à de nouvelles formes salines pharmaceutiquement acceptables du camostat, à des procédés de lyophilisation, à des formulations dont le goût est masqué, à des formulations nébulisées et à l'utilisation de ces nouvelles formes salines pour le traitement des maladies respiratoires, notamment de la mucovisidose et des broncho-pneumopathies chroniques obstructives (BPCO).
• [EN] A PHARMACEUTICAL COMBINATION COMPRISING AN ANTI-VIRAL PROTONOPHORE AND A SERINE PROTEASE INHIBITOR<br/>[FR] COMBINAISON PHARMACEUTIQUE COMPRENANT UN PROTONOPHORE ANTIVIRAL ET UN INHIBITEUR DE SÉRINE PROTÉASE
  申请人：UNIV BERLIN CHARITE

  公开号：WO2021255218A1

  公开（公告）日：2021-12-23

  The invention relates to a pharmaceutical combination, comprising a therapeutically effective amount of an anti-viral protonophore, and a therapeutically effective amount of a serine protease inhibitor. In preferred embodiments the invention relates to a combination of niclosamide and camostat mesylate. The invention further relates to a pharmaceutical composition comprising the combination, and use of the combination or composition in a treatment and/or prevention of a viral infection in a subject and/or a medical condition associated with a viral infection. In preferred embodiments the invention relates to the treatment and/or prevention of a SARS-CoV virus, preferably SARS-CoV-2.