6-Fluoro-3-isopropylamino-4H-1,2,4-benzothiadiazine 1,1-dioxide

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 噻二嗪
• 英文名称: 6-Fluoro-3-isopropylamino-4H-1,2,4-benzothiadiazine 1,1-dioxide
• 英文别名: 6-fluoro-1,1-dioxo-N-propan-2-yl-4H-1λ6,2,4-benzothiadiazin-3-imine
• 化学式: C₁₀H₁₂FN₃O₂S
• 分子量: 257.289
• InChiKey: DVDYAMJMNJUZLO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.1
• 重原子数：
  17
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  78.9
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  异硫氰酸异丙酯 、 2-氨基-4-氟苯磺酰胺 在 乙酸乙酯 作用下， 以 乙酸乙酯 为溶剂， 反应 2.83h， 以to give 355 mg (14%) of the title compound的产率得到6-Fluoro-3-isopropylamino-4H-1,2,4-benzothiadiazine 1,1-dioxide
  参考文献：
  名称：

  1,2,4-benzothiadiazine derivatives, their preparation and use

  摘要：

  本文描述了由公式表示的1,2,4-苯并噻二嗪衍生物，其中D、R1、R2、R3、R4、R5、R12、R13、R14、R15在描述中有定义，以及它们的组成和制备方法。这些化合物在治疗中枢神经系统、心血管系统、肺系统、胃肠系统和内分泌系统的疾病中有用。

  公开号：

  US06242443B1

文献信息

• Therapeutics for the treatment of glaucoma
  申请人：MAYO FOUNDATION FOR MEDICAL EDUCATION AND RESEARCH

  公开号：US10981951B2

  公开（公告）日：2021-04-20

  The present invention provides benzothiadiazine and chroman derivatives and particularly diazoxide and cromakalim derivatives for use in treating glaucoma, retinopathy, treating age related macular degeneration, treating, stabilizing and/or inhibiting blood and lymph vascularization, and reducing intraocular pressure by administering a pharmaceutically effective amount of a prodrug disposed in an ophthalmically acceptable carrier to the eye, wherein the prodrug specifically modulates a KATP channel to reduce an intraocular pressure.

  本发明提供苯并噻二嗪和色苷衍生物，特别是用于治疗青光眼、视网膜病变、治疗年龄相关性黄斑变性、治疗、稳定和/或抑制血液和淋巴血管生成，并通过向眼睛内给予药学有效量的前药，其中前药特异性调节KATP通道以降低眼内压力。
• NOVEL THERAPEUTICS FOR THE TREATMENT OF GLAUCOMA
  申请人：Mayo Foundation for Medical Education and Research

  公开号：EP3099304A1

  公开（公告）日：2016-12-07
• THERAPEUTICS FOR THE TREATMENT OF GLAUCOMA
  申请人：Mayo Foundation for Medical Education and Research

  公开号：US20210040148A1

  公开（公告）日：2021-02-11

  The present invention provides benzothiadiazine and chroman derivatives and particularly diazoxide and cromakalim derivatives for use in treating glaucoma, retinopathy, treating age related macular degeneration, treating, stabilizing and/or inhibiting blood and lymph vascularization, and reducing intraocular pressure by administering a pharmaceutically effective amount of a prodrug disposed in an ophthalmically acceptable carrier to the eye, wherein the prodrug specifically modulates a K ATP channel to reduce an intraocular pressure.
• US6242443B1
  申请人：——

  公开号：US6242443B1

  公开（公告）日：2001-06-05
• [EN] NOVEL THERAPEUTICS FOR THE TREATMENT OF GLAUCOMA<br/>[FR] NOUVEAUX AGENTS THÉRAPEUTIQUES POUR LE TRAITEMENT DU GLAUCOME
  申请人：MAYO FOUNDATION

  公开号：WO2015117024A1

  公开（公告）日：2015-08-06

  The present invention provides benzothiadiazine and chroman derivatives and particularly diazoxide and cromakalim derivatives for use in treating glaucoma, retinopathy, treating age related macular degeneration, treating, stabilizing and/or inhibiting blood and lymph vascularization, and reducing intraocular pressure by administering a pharmaceutically effective amount of a prodrug disposed in an ophthalmically acceptable carrier to the eye, wherein the prodrug specifically modulates a KATP channel to reduce an intraocular pressure.