(R)-Desisopropyl Tolterodine

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: (R)-Desisopropyl Tolterodine
• 英文别名: 4-methyl-2-[(1R)-1-phenyl-3-(propan-2-ylamino)propyl]phenol
• 化学式: C₁₉H₂₅NO
• 分子量: 283.4
• InChiKey: CPLYUIYTJCFQJD-QGZVFWFLSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.4
• 重原子数：
  21
• 可旋转键数：
  6
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.37
• 拓扑面积：
  32.3
• 氢给体数：
  2
• 氢受体数：
  2

ADMET

代谢

N-去烷基托特罗定是托特罗定的人类已知代谢物。

N-Dealkylated tolterodine is a known human metabolite of tolterodine.

来源:NORMAN Suspect List Exchange

文献信息

• Smooth muscle spasmolytic agents
  申请人：——

  公开号：US20040248987A1

  公开（公告）日：2004-12-09

  The present invention relates to smooth muscle spasmolytic agents, pharmaceutical compositions containing them and method of using said compounds and compositions for the treatment of urinary incontinence, and other smooth muscle contractility conditions. More particularly, the present invention relates to certain metabolically stabilized secondary amines having smooth muscle relaxing properties while avoiding, on administration to a mammal, adverse side effects such as prominent antimuscarinic, arrhythmogenic and cardiodepressive effects.

  本发明涉及平滑肌松弛剂，含有它们的制药组合物及使用这些化合物和组合物治疗尿失禁和其他平滑肌收缩症状的方法。更具体地说，本发明涉及某些代谢稳定的次级胺，具有平滑肌松弛作用，同时在哺乳动物使用时避免了不良的副作用，如突出的抗胆碱能、心律不齐和心脏抑制作用。
• Tolterodine metabolites
  申请人：——

  公开号：US20030027856A1

  公开（公告）日：2003-02-06

  Methods for treating smooth muscle hyperactivity, including urinary incontinence, while avoiding concomitant liability of adverse effects associated with tolterodine and the racemic version thereof are disclosed. The methods comprise administering a therapeutically effective amount of a mono-isopropyl metabolite or a parahydroxymethyl metabolite or a parahydroxymethyl mono-isopropyl metabolite of tolterodine or racemic versions thereof or a pharmaceutically acceptable salt of either metabolite. Pharmaceutical compositions in the form of tablets and transdermal devices comprising said compounds and acceptable carriers are also disclosed.

  本发明公开了治疗平滑肌亢进症（包括尿失禁）的方法，同时避免了与托特罗定及其外消旋体相关的不良反应。这些方法包括施用治疗有效量的托特罗定的单异丙基代谢物或对羟甲基代谢物或对羟甲基单异丙基代谢物或其外消旋体或这两种代谢物的药学上可接受的盐。还公开了包含上述化合物和可接受载体的片剂和透皮装置形式的药物组合物。
• TOLTERODINE METABOLITES
  申请人：Bridge Pharma, Inc.

  公开号：EP1434574A2

  公开（公告）日：2004-07-07
• SMOOTH MUSCLE SPASMOLYTIC AGENTS
  申请人：Bridge Pharma, Inc.

  公开号：EP1633695A2

  公开（公告）日：2006-03-15
• EP1633695A4
  申请人：——

  公开号：EP1633695A4

  公开（公告）日：2007-12-12