cyclohexyl-(4-methyl-1,1-dioxo-1,4-dihydro-1λ⁶-benzo[1,2,4]thiadiazin-3-yl)-amine

• 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: cyclohexyl-(4-methyl-1,1-dioxo-1,4-dihydro-1λ⁶-benzo[1,2,4]thiadiazin-3-yl)-amine
• 英文别名: 3-Cyclohexylamin-4-methyl-1,2,4-benzothiadiazin-1,1-dioxid；N-cyclohexyl-4-methyl-1,1-dioxo-1lambda6,2,4-benzothiadiazin-3-imine；N-cyclohexyl-4-methyl-1,1-dioxo-1λ6,2,4-benzothiadiazin-3-imine
• 化学式: C₁₄H₁₉N₃O₂S
• 分子量: 293.39
• InChiKey: IZMRKEOWLDUVHE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  20
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  70.2
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  硫酸二甲酯 、 3-(cyclohexylamino)-4H-benzo[e][1,2,4]thiadiazine 1,1-dioxide 生成 cyclohexyl-(4-methyl-1,1-dioxo-1,4-dihydro-1λ⁶-benzo[1,2,4]thiadiazin-3-yl)-amine
  参考文献：
  名称：

  Raffa; Melegari; Vampa, Farmaco, Edizione Scientifica, 1972, vol. 27, # 6, p. 509 - 516

  摘要：

  DOI：

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。
• 1,2,4-BENZOTHIADIAZINE DERIVATIVES, THEIR PREPARATION AND USE
  申请人：Université de Liège

  公开号：EP0906297B1

  公开（公告）日：2004-02-25
• 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
• USE OF DIAZOXIDE FOR SUPPRESSING THE PLASMA INSULIN LEVEL IN A MAMMAL
  申请人：De Boer Johannes Mathijs Maria

  公开号：US20100234362A1

  公开（公告）日：2010-09-16

  The present invention relates to the use of a potassium channel activator in the manufacture of a medicament for suppressing the fasting plasma insulin level and/or postabsorptive insulin level in a mammal in need thereof, wherein the fasting and/or postabsorptive plasma insulin level is reduced to about 5 mU/l or less. The present invention also relates to the use of a potassium channel activator in the manufacture of a medicament for suppressing the fasting plasma insulin level and/or postabsorptive insulin level in a mammal in need thereof for treating or preventing obesity, obesity related disorders and conditions and other disorders and conditions related to weight gain in a mammal in need thereof, said method comprising orally administering to said mammal in need thereof a daily dosage of about 5 mg to about 1200 mg, calculated on a Diazoxide active weight basis.
• USE OF A COMBINATION OF DIAZOXIDE AND METFORMIN FOR TREATING OBESITY OR OBESITY RELATED DISORDERS
  申请人：De Boer Johannes Marthijs Maria

  公开号：US20120053172A1

  公开（公告）日：2012-03-01

  The present invention relates to a method for suppressing the fasting plasma insulin level and/or postabsorptive insulin level in a mammal in need thereof, said method comprising administering to said mammal a pharmaceutically effective amount of a combination of a potassium channel activator and an anti-diabetic drug. The present invention also relates to a method for treating or preventing obesity, obesity related disorders and conditions and other disorders and conditions related to weight gain in a mammal in need thereof, said method comprising administering to said mammal a pharmaceutically effective amount of a combination of a potassium channel activator and an anti-diabetic drug.