卡莫特罗 | 147568-66-9

• 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: 卡莫特罗
• 英文名称: Carmoterol
• 英文别名: 8-hydroxy-5-[(1R)-1-hydroxy-2-[[(1R)-2-(4-methoxyphenyl)-1-methylethyl]amino]ethyl]-2(1H)-quinolinone；8-hydroxy-5-{(1R)-1-hydroxy-2-[N-((1R)-2-(p-methoxyphenyl)-1-methylethyl)-amino]ethyl}carbostyril；8-hydroxy-5-[(1R)-1-hydroxy-2-[N-[(1R)-2-(p-methoxyphenyl)-1-methylethyl]amino]ethyl]-2(1H)-quinolinone；5-[(1R)-1-hydroxy-2-[[(2R)-1-(4-methoxyphenyl)propan-2-yl]azaniumyl]ethyl]-2-oxo-1H-quinolin-8-olate
• CAS: 147568-66-9
• 化学式: C₂₁H₂₄N₂O₄
• 分子量: 368.433
• InChiKey: IHOXNOQMRZISPV-YJYMSZOUSA-N

物化性质

• 沸点：
  649.1±55.0 °C(Predicted)
• 密度：
  1.248

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

反应信息

• 作为反应物：
  描述：

  富马酸 、 卡莫特罗 以 乙醇 为溶剂， 以58.3%的产率得到8-hydroxy-5-[(1R)-1-hydroxy-2-[[(1R)-2-(4-methoxyphenyl)-1-methylethyl]amino]ethyl]-2(1H)-quinolinone hemi-fumarate
  参考文献：
  名称：

  WO2011/15289

  摘要：

  公开号：
• 作为产物：
  描述：

  8-benzyloxy-5-{(1R)-1-hydroxy-2-[N-((1R)-2-(p-methoxyphenyl)-1-methylethyl)amino]ethyl}carbostyril 生成 卡莫特罗
  参考文献：
  名称：

  Bronchodilating

  摘要：

  一种新型喹诺酮衍生物，其化学式为：##STR1##或其药学上可接受的酸加成盐，以及制备该化合物的方法。化合物(I)显示出强效的支气管扩张活性，并可作为支气管扩张剂使用。

  公开号：

  US04579854A1

文献信息

• Process for the preparation of 8-hydroxy-5-[(1R)-1-hydroxy-2[[(1R)-2-(4-methoxyphenyl)-1-methylethyl]amino]ethyl]-2(1H)-quinolinone monohydrochloride
  申请人：CHIESI FARMACEUTICI S.p.A.

  公开号：EP1953143A1

  公开（公告）日：2008-08-06

  The invention relates to a process for the preparation of 8-hydroxy-5-[(1R)-1-hydroxy-2 [[(1R)-2-(4-methoxyphenyl)-1-methylethyl]amino]ethyl]-2(1H)-quinolinone monohydrochloride of formula (I). Useful intermediates in the process are also disclosed.

  本发明涉及一种制备式为(I)的8-羟基-5-[(1R)-1-羟基-2[[(1R)-2-(4-甲氧基苯基)-1-甲基乙基]氨基]乙基]-2(1H)-喹啉酮单盐酸盐的方法。本方法还揭示了有用的中间体。
• MEDICAMENTS FOR INHALATION COMPRISING AN ANTICHOLINERGIC AND A BETAMIMETIC
  申请人：Meade Christopher John Montague

  公开号：US20090155185A1

  公开（公告）日：2009-06-18

  A pharmaceutical composition comprising an anticholinergic and a betamimetic of formula 2 optionally together with a pharmaceutically acceptable excipient, the anticholinergic and the betamimetic optionally in the form of their enantiomers, mixtures of their enantiomers, their racemates, their solvates, or their hydrates, processes for preparing them, and their use in the treatment of asthma, COPD, or other inflammatory or obstructive respiratory complaints.

  一种药物组合物，包括抗胆碱能药和公式2的β-肾上腺素受体激动剂，可选地与药学上可接受的赋形剂一起使用，抗胆碱能药和β-肾上腺素受体激动剂可以是其对映体形式、对映体混合物、拉克酸盐、溶剂化物或水合物形式，以及用于治疗哮喘、COPD或其他炎症或阻塞性呼吸道疾病的用途，以及其制备方法。
• [EN] 8-HYDROXY-5-[(-HYDROXY-2-[[ (1R)-2-(4-METHOXYPHENYL)-1-METHYLETHYL] AMINO ][ETHYL] -2(1H)-QUINOLINONE MONOHYDROCHLORIDE IN CRYSTALLINE FORM AND THE PROCESS FOR ITS PREPARATION<br/>[FR] MONOHYDROCHLORURE DE 8-HYDROXY-5-[(1R)-1-HYDROXY-2-[[(1R)-2-(4-METHOXYPHENYL)-1-METHYLETHYL]AMINO]ETHYL]-2(1H)-QUINOLINONE SOUS FORME CRISTALLINE ET PROCEDE DE PREPARATION ASSOCIE
  申请人：CHIESI FARMA SPA

  公开号：WO2005089760A1

  公开（公告）日：2005-09-29

  The invention relates to 8-hydroxy-5- [(1 R)-1-hydroxy-2­[[(1R)-2-(4-methoxyphenyl)-1-methyl ethyl] amino] ethyl] -2 (1 H)-quinolinone monohydrochloride of formula (I) in crystalline form, provided with suitable characteristics in order to be used for the preparation of pharrmaceutical compositions for inhalation in combination with suitable carriers or vehicles and the process for its preparation.

  本发明涉及具有适当特性的晶体形式的8-羟基-5-[(1R)-1-羟基-2-[[(1R)-2-(4-甲氧基苯基)-1-甲基乙基]氨基]乙基]-2(1H)-喹啉酮单盐酸盐(I)的制备方法，该晶体形式可与适当的载体或车辆结合用于制备吸入用药物组合物。
• Stable pharmaceutical solution formulations for pressurised metered dose inhalers
  申请人：CHIESI FARMACEUTICI S.p.A.

  公开号：EP1157689A1

  公开（公告）日：2001-11-28

  An aerosol solution composition for use in an aerosol inhaler comprises an active material, a propellant containing a hydrofluoroalkane, a cosolvent and optionally a low volatility component to increase the mass median aerodynamic diameter (MMAD) of the aerosol particles on actuation of the inhaler. The composition is stabilized by using a small amount of mineral acid and a suitable can having part or all of its internal metallic surfaces made of stainless steel, anodized aluminium or lined with an inert organic coating.

  一种用于气溶胶吸入器的气溶胶溶液组合物包括一种活性材料、一种含氢氟烷烃的推进剂、一种共溶剂和一种可选的低挥发性成分，以增加吸入器启动时气溶胶粒子的质量中值空气动力学直径（MMAD）。 使用少量矿物酸和一个合适的罐子来稳定这种成分，罐子的部分或全部内金属表面由不锈钢、阳极氧化铝或惰性有机涂层制成。
• Novel medicament combination of a highly potent long-lasting beta2-agonist and a corticosteroid
  申请人：CHIESI FARMACEUTICI S.p.A.

  公开号：EP1452179A1

  公开（公告）日：2004-09-01

  The present invention relates to the use of a bronchodilator in combination with an anti-inflammatory corticosteroid or an anticholinergic atropine-like derivative for the treatment of respiratory disorders and especially asthma and chronic obstructive pulmonary disease (COPD), and to pharmaceutical compositions containing the two active ingredients. In particular, the invention relates to the use of the long-acting β2-agonist 8-hydroxy-5-[(1R)-1-hydroxy-2-[[(1R)-2-(4-methoxyphenyl)-1-methylethyl]amino]ethyl-2(1H)-quinolinone and/or physiologically acceptable salts and/or solvates thereof in combination with a corticosteroid.

  本发明涉及支气管扩张剂与抗炎皮质类固醇或抗胆碱能阿托品样衍生物联合用于治疗呼吸系统疾病，特别是哮喘和慢性阻塞性肺病（COPD），以及含有这两种活性成分的药物组合物。特别是，本发明涉及长效β2-受体激动剂8-羟基-5-[(1R)-1-羟基-2-[[(1R)-2-(4-甲氧基苯基)-1-甲基乙基]氨基]乙基-2(1H)-喹啉酮和/或其生理上可接受的盐和/或溶液与皮质类固醇联合使用。