DE(methyl)-alvameline | 221549-70-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: DE(methyl)-alvameline
• 英文别名: 5-(2-ethyltetrazol-5-yl)-1,2,3,6-tetrahydropyridine
• CAS: 221549-70-8
• 化学式: C₈H₁₃N₅
• 分子量: 179.22
• InChiKey: KWCDFRUNFDIIQT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.2
• 重原子数：
  13
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.62
• 拓扑面积：
  55.6
• 氢给体数：
  1
• 氢受体数：
  4

ADMET

代谢

5-(2-乙基-2H-四唑-5-基)-1,2,3,6-四氢吡啶是Alvameline的人类已知代谢物。

5-(2-Ethyl-2H-tetrazol-5-yl)-1,2,3,6-tetrahydro-pyridine is a known human metabolite of Alvameline.

来源:NORMAN Suspect List Exchange

文献信息

• Pharmaceutical compositions containing oxybutynin
  申请人：——

  公开号：US20030185882A1

  公开（公告）日：2003-10-02

  A pharmaceutical composition and dosage form for the treatment of incontinence with oxybutynin and a second drug is provided. The second drug can be darifenacin or tolterodine. Depending upon the route of administration, the dosage form used, and the second drug used, the dosage form may independently include therapeutic or sub-therapeutic amounts of the oxybutynin and the second drug. Particular embodiments include a dosage form that provides a controlled release of oxybutynin and the second drug to maintain therapeutically effective levels oxybutynin and/or the second in a mammal for an extended period of time. An osmotic device containing a bi-layered core is provided. The osmotic device provides a dual controlled release of both drugs from the core. A method of treating urinary (stress or urge) incontinence with the pharmaceutical composition and dosage form is provided. Together, oxybutynin and the second drug provide an overall improved therapeutic benefit over either agent alone when administered at approximately the same dose.

  提供了一种含有奥克西布丁和第二种药物的药物组合物和剂型，用于治疗失禁。第二种药物可以是达瑞那新或托吡酯。根据给药途径、使用的剂型和第二种药物，剂量形式可以独立地包括治疗或亚治疗量的奥克西布丁和第二种药物。特定实施例包括提供一种剂量形式，该剂量形式提供奥克西布丁和第二种药物的控释，以维持哺乳动物体内的治疗有效水平，持续一段时间。提供一种含有双层核心的渗透设备。渗透设备从核心中提供两种药物的双重控制释放。提供使用药物组合物和剂型治疗尿失禁（压力性或切勿性）的方法。奥克西布丁和第二种药物一起，在大约相同的剂量下，提供了总体上比任何一种药物单独使用更好的治疗效果。
• Dual controlled release osmotic device
  申请人：Vergez A. Juan

  公开号：US20060177510A1

  公开（公告）日：2006-08-10

  A pharmaceutical composition and dosage form for the treatment of incontinence with oxybutynin and a second drug is provided. The second drug can be darifenacin or tolterodine. Depending upon the route of administration, the dosage form used, and the second drug used, the dosage form may independently include therapeutic or sub-therapeutic amounts of the oxybutynin and the second drug. Particular embodiments include a dosage form that provides a controlled release of oxybutynin and the second drug to maintain therapeutically effective levels oxybutynin and/or the second in a mammal for an extended period of time. An osmotic device containing a bi-layered core is provided. The osmotic device provides a dual controlled release of both drugs from the core. A method of treating urinary (stress or urge) incontinence with the pharmaceutical composition and dosage form is provided. Together, oxybutynin and the second drug provide an overall improved therapeutic benefit over either agent alone when administered at approximately the same dose.

  提供了一种用奥昔布宁和第二种药物治疗尿失禁的药物组合物和剂型。第二种药物可以是达非那新或托特罗定。根据给药途径、使用的剂型和第二种药物的不同，剂型可独立包含治疗量或亚治疗量的奥昔布宁和第二种药物。具体的实施方案包括提供奥昔布宁和第二种药物的控制释放的剂型，以在哺乳动物体内长时间维持治疗有效水平的奥昔布宁和/或第二种药物。提供了一种含有双层核心的渗透装置。该渗透装置可从芯中双重控制释放两种药物。提供了一种用药物组合物和剂型治疗尿失禁（压力性或急迫性）的方法。在给药剂量大致相同的情况下，奥昔布宁和第二种药物共同提供的整体治疗效果优于单独使用其中一种药物。
• Dual controlled release dosage form
  申请人：Vergez A. Juan

  公开号：US20060204578A1

  公开（公告）日：2006-09-14

  A dosage form that provides a controlled release of at least two different active agents is provided. Particular embodiments include a dosage form that provides therapeutically effective levels of a first active agent and a second active agent in a mammal for an extended period of time following oral administration. An osmotic device containing a bi-layered core is provided. The osmotic device provides a dual controlled release of both drugs from the core. The layers of the core are in stacked, substantially concentric or substantially eccentric arrangement.

  本发明提供了一种可控制释放至少两种不同活性剂的剂型。具体的实施方案包括一种剂型，可在哺乳动物口服后的较长时间内提供治疗有效水平的第一种活性剂和第二种活性剂。提供了一种含有双层核心的渗透装置。该渗透装置可从芯中双重控制释放两种药物。药芯的各层呈堆叠、基本同心或基本偏心排列。
• Heterocyclic compounds
  申请人：H. LUNDBECK A/S

  公开号：EP0296721B1

  公开（公告）日：1993-06-23
• NEUROGENESIS BY MUSCARINIC RECEPTOR MODULATION
  申请人：Barlow Carrolee

  公开号：US20110319386A1

  公开（公告）日：2011-12-29

  The instant disclosure describes methods for treating diseases and conditions of the central and peripheral nervous system by stimulating or increasing neurogenesis. The disclosure includes compositions and methods based on muscarinic receptor modulation, such as via inhibition of acetylcholine esterase (AChE) activity, alone or in combination with another neurogenic agent to stimulate or activate the formation of new nerve cells.