CKLP1 | 1802655-72-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并吡喃
• 英文名称: CKLP1
• 英文别名: QLS-101；Foslevcromakalim；[(3S,4R)-6-cyano-2,2-dimethyl-4-(2-oxopyrrolidin-1-yl)-3,4-dihydrochromen-3-yl] dihydrogen phosphate
• CAS: 1802655-72-6
• 化学式: C₁₆H₁₉N₂O₆P
• 分子量: 366.31
• InChiKey: JRUHOGHWZXTUMZ-CABCVRRESA-N

物化性质

• 沸点：
  599.6±60.0 °C(Predicted)
• 密度：
  1.48±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -0.3
• 重原子数：
  25
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  120
• 氢给体数：
  2
• 氢受体数：
  7

制备方法与用途

foslevcromakalim（QLS-101）是一种ATP敏感性钾通道开启剂，主要用于眼部降压作用。

反应信息

• 作为反应物：
  描述：

  CKLP1 、 三乙二醇 在 吡啶 、 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 作用下， 反应 16.0h， 以22 mg的产率得到[(3S,4R)-6-cyano-2,2-dimethyl-4-(2-oxopyrrolidin-1-yl)-3,4-dihydrochromen-3-yl] 2-[2-[2-[[(3S,4R)-6-cyano-2,2-dimethyl-4-(2-oxopyrrolidin-1-yl)-3,4-dihydrochromen-3-yl]oxy-hydroxyphosphoryl]oxyethoxy]ethoxy]ethyl hydrogen phosphate
  参考文献：
  名称：

  [EN] CONTROLLED-DELIVERY CROMAKALIM PRODRUGS
  [FR] PROMÉDICAMENTS DE CROMAKALIM À LIBÉRATION CONTRÔLÉE

  摘要：

  本发明提供了克罗马卡利姆前药、组合物及其用于调节ATP敏感性钾（KATP）通道以用于治疗目的的方法。

  公开号：

  WO2021119503A1

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：US20170002040A1

  公开（公告）日：2017-01-05

  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.
• 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.
• CONTROLLED-DELIVERY CROMAKALIM PRODRUGS
  申请人：Qlaris Bio, Inc.

  公开号：US20220324890A1

  公开（公告）日：2022-10-13

  The present invention provides cromakalim prodrugs, compositions, and their use for the modulation of ATP-sensitive potassium (K ATP ) channels for therapeutic purposes.
• [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.