环庚醇,2,2-二乙氧基-,(+)-(9CI) | 24359-22-6

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 中文名称: 环庚醇,2,2-二乙氧基-,(+)-(9CI)
• 中文别名: 4-(9,10-二氢-4H-苯并[4,5]环庚并[1,2-b]噻吩-4-亚基)-1-甲基哌啶鎓马来酸氢盐；马来酸苯噻啶
• 英文名称: Pizotifen maleate
• 英文别名: (Z)-but-2-enedioic acid;1-methyl-4-(6-thiatricyclo[8.4.0.03,7]tetradeca-1(14),3(7),4,10,12-pentaen-2-ylidene)piperidine
• CAS: 24359-22-6
• 化学式: C23H25NO4S
• 分子量: 411.5
• InChiKey: GGYSHFFKUHGBIK-BTJKTKAUSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.33
• 重原子数：
  29
• 可旋转键数：
  1
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  110
• 氢给体数：
  2
• 氢受体数：
  5

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。
• 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。
• HYDROXYLATED NEBIVOLOL METABOLITES
  申请人：O'Donnell John P.

  公开号：US20110065783A1

  公开（公告）日：2011-03-17

  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.

  羟基化的内比洛尔代谢物在急性给药后以浓度依赖的方式增加人类内皮细胞制备的一氧化氮释放。此外，羟基化的内比洛尔代谢物，包括但不限于4-羟基-6,6′-二氟-、4-羟基-5-酚-6,6′-二氟-和4-羟基-8-苯基-6,6′-二氟-，具有在慢性给药后增加人类内皮细胞释放一氧化氮能力的能力。本发明提供了羟基化的内比洛尔代谢物和包含内比洛尔和/或至少一种内比洛尔羟基化代谢物和/或至少一种用于治疗心血管疾病的其他化合物或其药学上可接受的盐的组合物。此外，本发明提供了通过给靶向受影响的血管疾病的部位至少给予一种能够释放治疗有效量一氧化氮的内比洛尔羟基化代谢物的方法来治疗和/或预防血管疾病的方法。此外，本发明还涉及通过至少给予一种内比洛尔羟基化代谢物来治疗和/或预防偏头痛。此发明还可与代谢综合征疾病的单个治疗或联合治疗一起使用。
• Meropenem Derivatives and Uses Thereof
  申请人：KALA PHARMACEUTICALS, INC.

  公开号：US20160039823A1

  公开（公告）日：2016-02-11

  The present invention provides novel derivative of β-lactam antibiotics, such as meropenem. The inventive compounds include compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrugs thereof. Also provided are particles (e.g., nanoparticles) and pharmaceutical compositions thereof that are mucus penetrating. The inventive particles and pharmaceutical compositions may be useful in delivering an inventive compound to the respiratory tract of a subject. The invention further provides methods of using and kits including the inventive compounds, particles thereof, and/or pharmaceutical compositions thereof for treating and/or preventing a pulmonary disease (e.g., a respiratory tract infection).

  本发明提供了新型的β-内酰胺类抗生素衍生物，例如美罗培南。该发明化合物包括公式（I）的化合物，以及其药学上可接受的盐、溶剂化物、水合物、多晶型、共晶体、互变异构体、立体异构体、同位素标记衍生物和前药。还提供了粒子（例如纳米粒子）和药物组合物，其具有黏液穿透性。这些发明的粒子和药物组合物可用于将发明化合物输送到受试者的呼吸道。本发明还提供了使用发明化合物、其粒子和/或药物组合物治疗和/或预防肺部疾病（例如呼吸道感染）的方法和包含发明化合物、其粒子和/或药物组合物的工具包。