8-hydroxy-5-[(1R)-1-hydroxy-2-[1-(4-methoxyphenyl)propan-2-ylamino]ethyl]-1H-quinolin-2-one

• 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
• 英文名称: 8-hydroxy-5-[(1R)-1-hydroxy-2-[1-(4-methoxyphenyl)propan-2-ylamino]ethyl]-1H-quinolin-2-one
• 化学式: C₂₁H₂₄N₂O₄
• 分子量: 368.4
• InChiKey: IHOXNOQMRZISPV-YFKXAPIDSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.1
• 重原子数：
  27
• 可旋转键数：
  7
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  90.8
• 氢给体数：
  4
• 氢受体数：
  5

文献信息

• PRESSURISED METERED DOSE INHALERS CONTAINING SOLUTIONS OF BETA-2 AGONISTS
  申请人：CHIESI FARMACEUTICI S.p.A.

  公开号：EP1480617A2

  公开（公告）日：2004-12-01
• STABLE PHARMACEUTICAL SOLUTION FORMULATION FOR PRESSURIZED METERED DOSE INHALERS
  申请人：CHIESI FARMACEUTICI S.p.A.

  公开号：EP1715849A1

  公开（公告）日：2006-11-02
• [EN] PRESSURISED METERED DOSE INHALERS CONTAINING SOLUTIONS OF BETA-2 AGONISTS<br/>[FR] FORMULATIONS HFA DE BETA 2-AGONISTES A ACTION PROLONGEE DE DERIVES DE 2(1H)-QIUNOLINONE
  申请人：CHIESI FARMA SPA

  公开号：WO2003074025A2

  公开（公告）日：2003-09-12

  The present invention relates to a pharmaceutical formulation for use in the administration of 2(1H)-quinolinone derivatives long-acting β2-agonists by inhalation. In particular this invention relates to a chemically stable highly efficient TA 2005 HFA solution formulation to be administered by pressurised metered dose inhalers (pMDIs) characterized by a deep lung penetration. The invention also relates to methods for the preparation of said formulation and to its use in respiratory diseases such as asthma and chronic obstructive pulmonary disease (COPD).
• [EN] STABLE PHARMACEUTICAL SOLUTION FORMULATIONS FOR PRESSURIZED METERED DOSE INHALERS<br/>[FR] FORMULATIONS DE SOLUTIONS PHARMACEUTIQUES STABLES POUR AEROSOLS-DOSEURS PRESSURISES
  申请人：CHIESI FARMA SPA

  公开号：WO2005084640A1

  公开（公告）日：2005-09-15

  Aerosol solution formulations for use in an aerosol inhaler which comprise 8-hydroxy-5-[(1R)-1-hydroxy-2-[[(1R)-2-(4-methoxyphenyl)-1-methylethyl]amino] ethyl]-2(1H)-quinolinone or a salt thereof, in particular the hydrochloride salt (TA 2005), as an active ingredient, a propellant containing a hydrofluoroalkane, and a cosolvent, stabilized by addition of a specific small amount of a high concentrated phosphoric acid and optionally by the use of a suitable can having part or all of its internal metallic surfaces lined with an inert organic coating.