盐酸多沙唑嗪 | 70918-01-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 中文名称: 盐酸多沙唑嗪
• 中文别名: 1-(4-氨基-6,7-二甲氧基-2-喹唑啉基)-4-(1,4-苯并二恶烷-2-甲酰基)哌嗪盐酸盐
• 英文名称: Doxazosin hydrochloride
• 英文别名: 4-amino-2-[4-(1,4-benzodioxan-2-carbonyl)piperazin-1-yl]-6,7-dimethoxyquinazoline hydrochloride；[2-[4-(2,3-dihydro-1,4-benzodioxine-3-carbonyl)piperazin-1-yl]-6,7-dimethoxyquinazolin-4-yl]azanium;chloride
• CAS: 70918-01-3
• 化学式: C₂₃H₂₅N₅O₅*ClH
• 分子量: 487.943
• InChiKey: AQAZIYFEPYHLHC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.14
• 重原子数：
  34
• 可旋转键数：
  4
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.35
• 拓扑面积：
  112
• 氢给体数：
  2
• 氢受体数：
  9

反应信息

• 作为反应物：
  描述：

  盐酸多沙唑嗪 、 sodium hydroxide 在 二氯甲烷 、 硫酸酯 作用下， 以to obtain 4.61 grams of white Doxazosin solid的产率得到多沙唑嗪
  参考文献：
  名称：

  Preparation of amides and quinazoline derivatives

  摘要：

  本发明涉及一种制备酰胺的方法，包括在硅胺的存在下将胺与羧酸反应。本发明还涉及一种制备喹唑啉衍生物的方法，包括在硅胺的存在下将胺与羧酸反应以获得酰胺，并将所得的酰胺与喹唑啉接触。

  公开号：

  US06313293B1
• 作为产物：
  描述：

  1,4-苯并二氧六环-2-甲酸乙酯 以 正丁醇 为溶剂， 反应 11.0h， 生成 盐酸多沙唑嗪
  参考文献：
  名称：

  A RELIABLE MULTIGRAM SYNTHESIS OF (±) DOXAZOSIN

  摘要：

  DOI：

  10.1080/00304940309355360

文献信息

• Hydroxylated nebivolol metabolites
  申请人：O'Donnell P. John

  公开号：US20070014733A1

  公开（公告）日：2007-01-18

  Hydroxylated nebivolol metabolites increase NO release from human endothelial cell preparations in a concentration dependent fashion following acute administration. In addition, hydroxylated nebivolol metabolites, including but not limited to 4-hydroxy-6,6′difluoro-, 4-hydroxy-5-phenol-6,6′difluoro-, and 4-hydroxy-8-pheno-6,6′difluoro-, have the ability to increase the capacity for NO release in human endothelial cells following chronic administration. This invention provides hydroxylated nebivolol metabolites and compositions comprising nebivolol and/or at least one hydroxylated metabolite of nebivolol and/or at least one additional compound used to treat cardiovascular diseases or a pharmaceutically acceptable salt thereof. In addition, this invention provides methods of treating and/or preventing vascular diseases by administering at least one hydroxylated metabolite of nebivolol that is capable of releasing a therapeutically effective amount of nitric oxide to a targeted site affected by the vascular disease. Also, this invention is directed to the treatment and/or prevention of migraine headaches administering at least one hydroxylated metabolite of nebivolol. This invention may also be used in conjunction with or as a single treatment of metabolic syndrome disorders.

  羟基化奈必洛尔代谢物在急性给药后以浓度依赖性方式增加人内皮细胞制剂的一氧化氮释放。此外，羟基化奈必洛尔代谢物，包括但不限于4-羟基-6,6'-二氟代-、4-羟基-5-苯酚-6,6'-二氟代-和4-羟基-8-苯并-6,6'-二氟代-，在慢性给药后能够增加人内皮细胞的一氧化氮释放能力。本发明提供了羟基化奈必洛尔代谢物和包含奈必洛尔和/或至少一种羟基化奈必洛尔代谢物和/或至少一种用于治疗心血管疾病的附加化合物的组合物，以及可药用的盐。此外，本发明还提供了通过给药至少一种能够释放治疗有效量的一氧化氮到受血管疾病影响的靶向部位的羟基化奈必洛尔代谢物来治疗和/或预防血管疾病的方法。本发明还涉及通过给药至少一种羟基化奈必洛尔代谢物来治疗和/或预防偏头痛。本发明还可以与治疗代谢综合征障碍的其他治疗联合使用，或作为单一治疗。
• Process for the Preparation of Doxazosin and Salts Thereof
  申请人：Rao Dharmaraj Ramachandra

  公开号：US20120041199A1

  公开（公告）日：2012-02-16

  The present invention relates to a process for the preparation of doxazosin or salts thereof.

  本发明涉及一种制备多沙唑嗪或其盐的方法。
• Antihypertensive 4-amino-2-[4-(1,4-benzodioxan-2-carbonyl)
  申请人：Pfizer Inc.

  公开号：US04188390A1

  公开（公告）日：1980-02-12

  Compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof wherein R represents 6,7-di(lower alkoxy) or 6,7,8-tri(lower alkoxy); m is 1 or 2, X is --CHR.sup.1 -- or --CH.sub.2 CH.sub.2 --; each R.sup.1 and R.sup.0 may be the same or different and is hydrogen or lower alkyl; each of R.sup.2 and R.sup.3 is hydrogen, lower alkoxy, lower alkyl, halogen, lower alkanoyl, lower alkoxycarbonyl, --CONR.sup.4 R.sup.5 or --SO.sub.2 NR.sup.4 R.sup.5 wherein each of R.sup.4 and R.sup.5 is hydrogen or lower alkyl; processes for their preparation; and their use as regulators of the cardiovascular system, and particularly in the treatment of hypertension.

  具有以下公式的化合物##STR1##及其药用可接受的盐，其中R代表6,7-二(较低烷氧基)或6,7,8-三(较低烷氧基)；m为1或2，X为--CHR.sup.1 --或--CH.sub.2 CH.sub.2 --；每个R.sup.1和R.sup.0可以相同也可以不同，是氢或较低烷基；每个R.sup.2和R.sup.3是氢、较低烷氧基、较低烷基、卤素、较低烷酰基、较低烷氧羰基、--CONR.sup.4 R.sup.5或--SO.sub.2 NR.sup.4 R.sup.5，其中每个R.sup.4和R.sup.5是氢或较低烷基；它们的制备方法；以及它们作为心血管系统调节剂的用途，尤其是在治疗高血压方面。
• Glucuronidated nebivolol metabolites
  申请人：O'Donnell P. John

  公开号：US20070014734A1

  公开（公告）日：2007-01-18

  This invention provides glucuronidated nebivolol metabolites and pharmaceutical compositions of glucuronidated nebivolol metabolites for treatment of cardiovascular diseases. In addition, this invention also provides compositions comprising nebivolol and/or at least one glucuronidated metabolite of nebivolol and/or at least one other active compound in a pharmaceutically acceptable carrier. This invention also provides methods of treating and/or preventing vascular diseases, by administering at least one glucuronidated metabolite of nebivolol that is capable of releasing a therapeutically effective amount of nitric oxide to a targeted site affected by the vascular disease. Also, this invention is directed to the treatment and/or prevention of migraine headaches administering at least one glucuronidated metabolite of nebivolol. This invention may also be used in conjunction with or as a single treatment of metabolic syndrome disorders.

  这项发明提供了葡萄糖醛酸化的尼布ivolol代谢物以及用于治疗心血管疾病的葡萄糖醛酸化的尼布ivolol代谢物的制药组合物。此外，该发明还提供了包含尼布ivolol和/或至少一种尼布ivolol的葡萄糖醛酸化代谢物和/或至少一种其他活性化合物的药用可接受载体的组合物。该发明还提供了通过向受影响血管疾病的靶位点投与至少一种能释放治疗有效量一氧化氮的尼布ivolol的葡萄糖醛酸化代谢物来治疗和/或预防血管疾病的方法。此外，该发明旨在通过投与至少一种尼布ivolol的葡萄糖醛酸化代谢物来治疗和/或预防偏头痛。该发明还可与代谢综合征紊乱的单一治疗或联合治疗一起使用。
• COMPOSITIONS COMPRISING LIPOPHILIC ACTIVE COMPOUNDS AND METHOD FOR THEIR PREPARATION
  申请人：Temtsin Krayz Galia

  公开号：US20090098200A1

  公开（公告）日：2009-04-16

  Compositions are provided comprising a lipophilic active compound, e.g., a human or veterinary drug or a nutraceutical, interwoven with a polymeric matrix formed by two or more polymers, wherein one of the polymers is an amphiphilic polymer and the other polymer is either an amphiphilic polymer with a different hydrophobic-hydrophilic balance or a hydrophilic polymer, and the active lipophilic compound has modified physicochemical properties. The composition forms colloidal nanodispersion upon contact with aqueous media.

  提供了一种组合物，其中包括一个亲脂性活性化合物，例如人类或兽医药物或营养保健品，与由两种或更多聚合物形成的聚合物基质交织在一起，其中一种聚合物是一种两性聚合物，另一种聚合物是具有不同疏水-亲水平衡的两性聚合物或亲水性聚合物，且活性亲脂性化合物具有改性的物理化学性质。该组合物在接触水性介质时形成胶体纳米分散体。