4-(4-piperidyliden)-9-oxo-9,10-dihydro-4H-benzo[4,5]cyclohepta[1,2-b]thiophen | 61017-81-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 环七噻吩
• 英文名称: 4-(4-piperidyliden)-9-oxo-9,10-dihydro-4H-benzo[4,5]cyclohepta[1,2-b]thiophen
• 英文别名: 2-Piperidin-4-ylidene-6-thiatricyclo[8.4.0.03,7]tetradeca-1(14),3(7),4,10,12-pentaen-9-one
• CAS: 61017-81-0
• 化学式: C₁₈H₁₇NOS
• 分子量: 295.405
• InChiKey: LJRKFCOGIJPEHN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  21
• 可旋转键数：
  0
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.28
• 拓扑面积：
  57.3
• 氢给体数：
  1
• 氢受体数：
  3

文献信息

• Piperidylidene derivatives, their production and pharmaceutical compositions containing them
  申请人：SANDOZ AG

  公开号：EP0047226A2

  公开（公告）日：1982-03-10

  Piperidylidene derivatives of formula wherein n is 2 or 3, R1 comptises a tricyclic nucleus and R2 is hydrogen or an acid residue, useful in the treatment and prophylaxis of asthmatic conditions.

  式中的亚哌啶衍生物 其中 n 为 2 或 3，R1 为三环核，R2 为氢或酸残基，可用于治疗和预防哮喘。
• BENZOCYCLOHEPTATHIOPHENE COMPOUNDS
  申请人：Bridge Pharma, Inc.

  公开号：EP0977568B1

  公开（公告）日：2006-03-08
• Treatment xerophthalmia with norketotifen
  申请人：Aberg A.K. Gunnar

  公开号：US20100105734A1

  公开（公告）日：2010-04-29

  Methods of using a cycloheptathiophene compound for the treatment of xerophthalmia are described, as are formulations and compositions for such treatment.
• OCULAR FORMULATIONS OF NORKETOTIFEN
  申请人：Aberg A.K. Gunnar

  公开号：US20100130550A1

  公开（公告）日：2010-05-27

  Ophthalmic compositions containing norketotifen and methods of making the same and the use thereof are disclosed. The methods also comprise administering to the eyes of a mammal in need thereof topical ophthalmic compositions containing norketotifen.
• Formulations and Methods for Treating High Intraocular Pressure
  申请人：Bridge Pharma, Inc.

  公开号：US20170105987A1

  公开（公告）日：2017-04-20

  Disclosed herein are methods of treating a mammal in need of a reduction in intraocular pressure by administering an intraocular formulation including a therapeutically effective amount of norketotifen for the reduction of intraocular pressure to the eye of the mammal in need thereof, wherein the intraocular formulation includes about 0.02 wt % to about 1.0 wt % norketotifen or a salt or an isomer thereof, calculated as the norketotifen free base. In certain aspects, the intraocular formulation is free from any added preservative and the intraocular formulation is self-preserving. Also included herein is a method of treating a human in need of a reduction in intraocular pressure by administering an intranasal formulation that includes a therapeutically effective amount of norketotifen for the reduction of intraocular pressure to the eye of the human in need thereof. Also, the beneficial effects of known drugs for high IOP are improved by co-administration with norketotifen.