carvedilol hydrobromide | 374779-42-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: carvedilol hydrobromide
• 英文别名: 1-carbazol-4-yloxy-3-[[2-(o-methoxyphenoxy)ethyl]amino]-2-propanol hydrobromide；1-(9H-carbazol-4-yloxy)-3-[2-(2-methoxyphenoxy)ethylamino]propan-2-ol;hydron;bromide
• CAS: 374779-42-7
• 化学式: BrH*C₂₄H₂₆N₂O₄
• 分子量: 487.393
• InChiKey: QHXINFRYDYEWAU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.32
• 重原子数：
  31
• 可旋转键数：
  10
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  75.7
• 氢给体数：
  4
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  卡维地洛 在 氢溴酸 作用下， 以 乙腈 为溶剂， 生成 carvedilol hydrobromide
  参考文献：
  名称：

  [EN] CARVEDILOL HYDOBROMIDE
  [FR] HYDOBROMURE DE CARVEDILOL

  摘要：

  本发明涉及卡维地洛的盐，包含这种卡维地洛盐或其对应溶剂的组合物，以及/或使用上述化合物在哺乳动物，特别是人类的某些疾病状态的治疗方法。本发明还涉及卡维地洛羟溴酸盐的新结晶形式，该羟溴酸盐是1-(咔唑基氧基)-3-[[2-(对甲氧基苯氧基)乙基]氨基]-2-丙醇的羟溴酸盐，以及/或其他卡维地洛溶剂，含有卡维地洛羟溴酸盐或其溶剂的组合物，以及使用上述化合物治疗高血压、充血性心力衰竭、心绞痛等的方法。

  公开号：

  WO2004002472A1

文献信息

• [EN] STABLE AMORPHOUS FORM OF CARVEDILOL DIHYDROGEN PHOSPHATE WITH STABILIZER<br/>[FR] FORME AMORPHE STABLE DE DIHYDROGÈNE PHOSPHATE DE CARVEDILOL AVEC AGENT STABILISANT
  申请人：LUPIN LTD

  公开号：WO2009024997A1

  公开（公告）日：2009-02-26

  The present invention provides a novel stable amorphous form of carvedilol dihydrogen phosphate and the process for its preparation that involves reaction of carvedilol base with ortho phosphoric acid in the presence of stabilizer in a suitable solvent or mixture of solvents followed by concentration and isolation. An alternate process for preparation of stable amorphous form of carvedilol dihydrogen phosphate involves addition of stabiliser to the solution of stable amorphous or crystalline carvedilol dihydrogen phosphate in a suitable solvent or mixture of solvents followed by concentration and isolation. The novel stable amorphous form of carvedilol dihydrogen phosphate is highly stable.

  本发明提供了一种新型稳定的非晶态卡维地洛双氢磷酸盐形式以及其制备过程，该过程涉及将卡维地洛碱与邻磷酸在适当溶剂或溶剂混合物中的稳定剂存在下反应，然后进行浓缩和分离。另一种制备稳定的非晶态卡维地洛双氢磷酸盐形式的方法涉及向稳定的非晶态或结晶卡维地洛双氢磷酸盐的溶液中加入稳定剂，然后进行浓缩和分离。这种新型稳定的非晶态卡维地洛双氢磷酸盐形式非常稳定。
• [EN] CARVEDILOL SALTS, CORRESPONDING COMPOSITIONS, METHODS OF DELIVERY AND/OR TREATMENT<br/>[FR] SELS DE CARVEDILOL, COMPOSITIONS CORRESPONDANTES, PROCEDES D'ADMINISTRATION ET/OU DE TRAITEMENT
  申请人：SB PHARMCO INC

  公开号：WO2005051383A1

  公开（公告）日：2005-06-09

  The present invention relates to a salt of carvedilol and/or corresponding solvates thereof, compositions containing such carvedilol and/or corresponding solvates thereof, and/or methods of using the aforementioned compound(s) in the treatment of certain disease states in mammals, in particular man. The present invention further relates to carvedilol phosphate salts, and/or solvates thereof, which include a novel crystalline form of carvedilol dihydrogen phosphate (i.e., which is the dihydrogen phosphate salt of 1­(carbazol-4-yloxy-3-[[2-(o-methoxyphenoxy) ethyl]amino]-2-propanol) and/or carvedilol hydrogen phosphate,etc.) and/or other corresponding solvates thereof, compositions containing these carvedilol phosphate salts and/or solvates, and methods of using the aforementioned salts and/or solvates to treat hypertension, congestive heart failure and angina, etc.

  本发明涉及卡维地洛盐及/或其对应的溶剂合物、含有该卡维地洛及/或其对应的溶剂合物的组合物，以及使用上述化合物在哺乳动物（尤其是人类）特定疾病状态的治疗中的方法。本发明还涉及卡维地洛磷酸盐及/或其溶剂合物，其中包括一种新型结晶形式的卡维地洛二氢磷酸盐（即，1-(氨基)-2-丙醇）和/或卡维地洛氢磷酸盐等）及/或其他对应的溶剂合物，含有这些卡维地洛磷酸盐及/或其溶剂合物的组合物，以及使用上述盐和/或溶剂治疗高血压、充血性心力衰竭和心绞痛等的方法。
• Carvedilol salts, corresponding compositions, methods of delivery and/or treatment
  申请人：Brook S. Christopher

  公开号：US20050277689A1

  公开（公告）日：2005-12-15

  The present invention relates to a salt of carvedilol and/or corresponding solvates thereof, compositions containing such carvedilol and/or corresponding solvates thereof, and/or methods of using the aforementioned compound(s) in the treatment of certain disease states in mammals, in particular man. The present invention further relates to carvedilol phosphate salts, and/or solvates thereof, which include a novel crystalline form of carvedilol dihydrogen phosphate (i.e., which is the dihydrogen phosphate salt of 1-(carbazol-4-yloxy-3-[[2-(o-methoxyphenoxy) ethyl]amino]-2-propanol) and/or carvedilol hydrogen phosphate, etc.) and/or other corresponding solvates thereof, compositions containing these carvedilol phosphate salts and/or solvates, and methods of using the aforementioned salts and/or solvates to treat hypertension, congestive heart failure and angina, etc.

  本发明涉及卡维地洛尔盐和/或相应的溶剂化物，包含此类卡维地洛尔和/或其相应溶剂化物的组合物，并且/或使用上述化合物在哺乳动物，特别是人类的某些疾病状态的治疗方法。本发明还涉及卡维地洛磷酸盐和/或其溶剂化物，其中包括卡维地洛双氢磷酸盐的新晶体形式（即1-（咔唑-4-氧基）-3-[[2-（o-甲氧基苯氧基）乙基]氨基]-2-丙醇的双氢磷酸盐和/或卡维地洛氢磷酸盐等），以及其他相应的溶剂化物，包含这些卡维地洛磷酸盐和/或溶剂化物的组合物，以及使用上述盐和/或溶剂化物治疗高血压、充血性心力衰竭和心绞痛等方法。
• Carvedilol free base, salts, anhydrous forms or solvates thereof, corresponding pharmaceutical compositions, controlled release formulations, and treatment or delivery methods
  申请人：Burke D. Matthew

  公开号：US20050169994A1

  公开（公告）日：2005-08-04

  The present invention also relates to carvedilol free base, salts, anhydrous forms, or solvates thereof, corresponding pharmaceutical compositions or controlled release formulations, and methods delivery of carvedilol forms to the lower gastrointestingal tract or methods to treat cardiovascular diseases, which may include, but are not limited to hypertension, congestive heart failure, and angina. The present invention relates to control release formulations, which comprise various cavedilol forms, which may include, but are not limited to carvedilol free base and corresponding carvedilol salts, anhydrous forms or solvates thereof.

  本发明还涉及卡维地洛自由基、盐、无水形式或其溶剂化物，相应的药物组合物或控制释放制剂，以及将卡维地洛形式传递到下消化道的方法或治疗心血管疾病的方法，其中可能包括但不限于高血压、充血性心力衰竭和心绞痛。本发明涉及控制释放制剂，其包括各种卡维地洛形式，可能包括但不限于卡维地洛自由基和相应的卡维地洛盐、无水形式或其溶剂化物。
• Carvedilol hydrobromide
  申请人：SmithKline Beechman Cork Limited

  公开号：US07649010B2

  公开（公告）日：2010-01-19

  The present invention relates to a salt of carvedilol, corresponding compositions containing such a carvedilol salt or corresponding solvates thereof, and/or methods of using the aforementioned compound(s) in the treatment of certain disease states in mammals, in particular man. The present invention further relates to a novel crystalline form of carvedilol hydrobromide, which is the hydrobromide salt of 1-(carbazol-4-yloxy-3-[[2-(o-methoxyphenoxy)ethyl]amino]-2-propanol, and/or other carvedilol solvates thereof, compositions containing salts or solvates of carvedilol hydrobromide, and methods of using the aforementioned compound(s) to treat hypertension, congestive heart failure, and angina, etc.

  本发明涉及卡维地洛尔的一种盐，包含该卡维地洛尔盐或其相应溶剂化物的对应组合物，以及/或使用上述化合物治疗哺乳动物特别是人类的某些疾病状态的方法。本发明还涉及一种新的卡维地洛尔羟溴酸盐的晶体形式，该晶体形式是1-(咔唑-4-氧基)-3-[[2-(邻甲氧基苯氧基)乙基]氨基]-2-丙醇的羟溴酸盐，和/或其他卡维地洛尔溶剂化物，包含卡维地洛尔羟溴酸盐的盐或溶剂化物的组合物，以及使用上述化合物治疗高血压、充血性心力衰竭和心绞痛等方法。