carvedilol methanesulfonate | 340269-63-8

• 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 methanesulfonate
• 英文别名: carvedilol mesylate；1-(9H-carbazol-4-yloxy)-3-[2-(2-methoxyphenoxy)ethylamino]propan-2-ol;methanesulfonic acid
• CAS: 340269-63-8
• 化学式: CH₄O₃S*C₂₄H₂₆N₂O₄
• 分子量: 502.588
• InChiKey: POFJUNNSHGGHIG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.24
• 重原子数：
  35
• 可旋转键数：
  10
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.28
• 拓扑面积：
  139
• 氢给体数：
  4
• 氢受体数：
  8

文献信息

• [EN] COMBINATION OF (S)-AMLODIPINE AND A BETA-BLOCKER, AND METHODS FOR REDUCING HYPERTENSION<br/>[FR] COMBINAISON DE (S)-AMLODIPINE ET D'UN BETABLOQUANT, ET PROCEDES POUR LA REDUCTION DE L'HYPERTENSION
  申请人：SEPRACOR INC

  公开号：WO2005099699A1

  公开（公告）日：2005-10-27

  One aspect of the present invention relates to pharmaceutical compositions comprising optically pure (S)-amlodipine and a beta-blocker. In a preferred embodiment, the beta-blocker is atenolol or bisprolol. Another aspect of the present invention relates to pharmaceutical compositions consisting essentially of at least one pharmaceutically acceptable carrier, optically pure (S)-amlodipine and a beta-blocker. In a preferred embodiment, the beta-blocker is atenolol or bisoprolol. The pharmaceutical compositions of the invention are useful, e.g., in the treatment of hypertension. In addition, the present invention also relates to a method of treating a patient suffering from hypertension or a related cardiac disorder, comprising co-administering to a patient in need thereof a therapeutically effective amount of optically pure (S)-amlodipine and a beta-blocker. In certain embodiments of the compositions and methods, said optically pure (S)-amlodipine is optically pure (S)-amlodipine malate, or a polymorph, pseudopolymorph or solvate thereof.

  本发明的一个方面涉及包含光学纯（S）-氨氯地平和β受体阻断剂的制药组合物。在一个首选实施例中，β受体阻断剂为阿托伐他汀或比索洛尔。本发明的另一个方面涉及基本上由至少一种药用载体、光学纯（S）-氨氯地平和β受体阻断剂组成的制药组合物。在一个首选实施例中，β受体阻断剂为阿托伐他汀或比索洛尔。本发明的制药组合物可用于治疗高血压等疾病。此外，本发明还涉及一种治疗患有高血压或相关心脏疾病的患者的方法，包括向需要的患者共同给予光学纯（S）-氨氯地平和β受体阻断剂的治疗有效量。在某些组合物和方法的实施例中，所述的光学纯（S）-氨氯地平为光学纯（S）-氨氯地平苹果酸盐，或其多晶形、伪多晶形或溶剂化合物。
• [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。
• CONTROLLED RELEASE FORMULATION OF CARVEDILOL
  申请人：TSH Biopharm Corporation Ltd.

  公开号：EP2471519A1

  公开（公告）日：2012-07-04

  A controlled release carvedilol formulation for less frequent, preferably once daily administration is described. The controlled release formulation comprises a therapeutically effective amount of carvedilol or a pharmaceutically acceptable salt thereof, a matrix forming polymer, a solubility enhancer and a pharmaceutically acceptable carrier. In one embodiment, a controlled release formulation having a therapeutically effective amount of carvedilol is contained in two or more subunits having different release profiles. The controlled release formulation is usable in the treatment and/or prophylaxis of one or more conditions such as cardiovascular disorders.

  本文描述了一种控释卡维地洛制剂，可减少给药次数，最好每天给药一次。控释制剂包括治疗有效量的卡维地洛或其药学上可接受的盐、基质形成聚合物、溶解度增强剂和药学上可接受的载体。在一个实施方案中，具有治疗有效量卡维地洛的控释制剂包含在两个或多个具有不同释放曲线的亚基中。控释制剂可用于治疗和/或预防一种或多种疾病，如心血管疾病。