8-hydroxy-5-{1-hydroxy-2-[N-(2-(p-methoxyphenyl)-1-methylethyl)amino]ethyl}carbostyril dihydrochloride

• 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-{1-hydroxy-2-[N-(2-(p-methoxyphenyl)-1-methylethyl)amino]ethyl}carbostyril dihydrochloride
• 英文别名: hydron;8-hydroxy-5-[1-hydroxy-2-[1-(4-methoxyphenyl)propan-2-ylamino]ethyl]-1H-quinolin-2-one;chloride
• 化学式: C₂₁H₂₄N₂O₄*2ClH
• 分子量: 441.354
• InChiKey: SYCWERNQGSKYAG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.92
• 重原子数：
  28
• 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：
  5
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  8-benzyloxy-5-{1-oxo-2-[N-(2-(p-methoxyphenyl)-1-methylethyl)amino]ethyl}carbostyril hydrochloride 生成 8-hydroxy-5-{1-hydroxy-2-[N-(2-(p-methoxyphenyl)-1-methylethyl)amino]ethyl}carbostyril dihydrochloride
  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

• [EN] BRONCHORELAXING COMPOUNDS<br/>[FR] COMPOSES BRONCHO-RELACHANTS
  申请人：RESPIRATORIUS AB

  公开号：WO2005070887A1

  公开（公告）日：2005-08-04

  A compound of the general formula (I) including its pharmaceutically acceptable acid addition salts formula (I) wherein A is CHR9, wherein R9 is H, C1-C6 alkyl;n is 1-3; B is CHR10, wherein R10 is H, C1-C6 alkyl; m is 1 or 2; D is O or S; E is CR11R12 or NR13, wherein R11 and R12 are, independent of each other, H or C1-C6 alkyl, R13 is H or C1-C6 alkyl; F is C1-C18 alkyl or R4-R7 cycloalkyl, which may be mono- or di-unsaturated and/or substituted, is useful in treating and preventing pulmonary disease characterized by bronchoconstriction; also disclosed is a pharmaceutical composition comprising the compound of formula (I), a pharmaceutical carrier and, optionally, an anti-asthmatic, a method for its manufacture, and a method for treating or preventing such disease.

  通式（I）的化合物及其药学上可接受的酸加合盐，其中A为CHR9，其中R9为H，C1-C6烷基；n为1-3；B为CHR10，其中R10为H，C1-C6烷基；m为1或2；D为O或S；E为CR11R12或NR13，其中R11和R12独立地为H或C1-C6烷基，R13为H或C1-C6烷基；F为C1-C18烷基或R4-R7环烷基，可以是单烯或双烯和/或取代的，用于治疗和预防以支气管收缩为特征的肺部疾病；还公开了包含通式（I）的药物组合物、药物载体和可选的抗哮喘药、其制造方法以及治疗或预防该疾病的方法。
• Bronchorelaxing compounds
  申请人：Skogvall Staffan

  公开号：US20060040919A1

  公开（公告）日：2006-02-23

  A compound of the general formula (I) including its pharmaceutically acceptable acid addition salts wherein A is CHR 9 , wherein R 9 is H, C 1 -C 6 alkyl; n is 1-3; B is CHR 10 , wherein R 10 is H, C 1 -C 6 alkyl; m is 1 or 2; D is O or S; E is CR 11 R 12 or NR 13 , wherein R 11 and R 12 are, independent of each other, H or C 1 -C 6 alkyl, R 13 is H or C 1 -C 6 alkyl; F is C 1 -C 18 alkyl or R 4 -R 7 cycloalkyl, which may be mono- or di-unsaturated and/or substituted, is useful in treating and preventing pulmonary disease characterized by bronchoconstriction; also disclosed is a pharmaceutical composition comprising the compound of formula (I), a pharmaceutical carrier and, optionally, an anti-asthmatic, a method for its manufacture, and a method for treating or preventing such disease.

  化合物的一般式(I)及其药学上可接受的酸盐包括其中，其中A为CHR9，其中R9为H，C1-C6烷基；n为1-3；B为CHR10，其中R10为H，C1-C6烷基；m为1或2；D为O或S；E为CR11R12或NR13，其中R11和R12独立地为H或C1-C6烷基，R13为H或C1-C6烷基；F为C1-C18烷基或R4-R7环烷基，可以是单烯或双烯和/或取代的，用于治疗和预防以支气管收缩为特征的肺部疾病；还公开了包括式(I)化合物的药物组合物、药物载体和可选的抗哮喘药、其制造方法以及治疗或预防该疾病的方法。
• Crystal form 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：EP2116536A1

  公开（公告）日：2009-11-11

  The present invention relates to a novel crystal form of 8-hydroxy-5-[(1R)-1-hydroxy-2-[[(1R)-2-(4-methoxyphenyl)-1-methylethyl]amino]ethyl]-2(1H)-quinolinone monohydrochloride. The invention also relates to processes for its preparation, pharmaceutical compositions thereof, and to its use as a medicament.

  本发明涉及一种 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)-喹啉酮单盐酸盐的新型晶体形式。 本发明还涉及其制备工艺、药物组合物及其作为药物的用途。
• INHALANT FORMULATION CONTAINING CYCLODEXTRIN AND CORTICOSTEROID
  申请人：CyDex Pharmaceuticals, Inc.

  公开号：EP3238708A1

  公开（公告）日：2017-11-01

  An inhalable formulation comprising SAE-CD and corticosteroid is provided. The formulation is adapted for administration to a subject by nebulization with any known nebulizer. The formulation can be included in a kit. The formulation is administered as an aqueous solution, however, it can be stored as a dry powder, ready-to-use solution, or concentrated composition. The formulation is employed in an improved nebulization system for administering corticosteroid by inhalation. SAE-CD present in the formulation significantly enhances the chemical stability of budesonide. A method of administering the formulation by inhalation is provided. The formulation can also be administered by conventional nasal delivery apparatus.

  提供了一种由 SAE-CD 和皮质类固醇组成的可吸入制剂。该制剂可通过任何已知的雾化器雾化给药。该制剂可包含在试剂盒中。该制剂以水溶液形式给药，但也可以干粉、即用溶液或浓缩组合物的形式储存。该制剂可用于改进的雾化系统，通过吸入给药皮质类固醇。制剂中的 SAE-CD 可显著提高布地奈德的化学稳定性。该制剂还提供了一种吸入给药方法。该制剂也可通过传统的鼻腔给药装置给药。
• Pharmaceutical compositions
  申请人：CIPLA Limited

  公开号：US11077124B2

  公开（公告）日：2021-08-03

  A pharmaceutical composition for inhalation comprising R (+) budesonide and one or more bronchodilators, and, optionally, one or more pharmaceutically acceptable excipients is described.

  本文描述了一种吸入用药物组合物，它包含 R (+) 布地奈德和一种或多种支气管扩张剂，以及一种或多种药学上可接受的赋形剂。