Cerapp_42116

• 分子结构分类: 有机化合物 - 核苷、核苷酸和类似物 - （5'->5'）-二核苷酸
• 英文名称: Cerapp_42116
• 英文别名: [[5-(2,4-dioxopyrimidin-1-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl] [[[5-(2,4-dioxopyrimidin-1-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-hydroxyphosphoryl] hydrogen phosphate
• 化学式: C₁₈H₂₆N₄O₂₃P₄
• 分子量: 790.3
• InChiKey: NMLMACJWHPHKGR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -9.1
• 重原子数：
  49
• 可旋转键数：
  14
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.56
• 拓扑面积：
  394
• 氢给体数：
  10
• 氢受体数：
  23

文献信息

• OPHTHALMIC COMPOSITION COMPRISING DIQUAFOSOL AND CATIONIC POLYMER
  申请人：Santen Pharmaceutical Co., Ltd.

  公开号：EP3760207A1

  公开（公告）日：2021-01-06

  Provided is an ophthalmic composition comprising diquafosol or a salt thereof and a cationic polymer, the cationic polymer being at least one selected from the group consisting of chitosan, a chitosan derivative, a cationic (meth)acrylate copolymer, a cationic silicone polymer, a diallyl quaternary ammonium salt-acrylamide copolymer, cationic hydrolyzed keratin, cationic hydrolyzed silk, cationic hydrolyzed collagen, cationic hydrolyzed casein, cationic hydrolyzed soy protein, a cationic vinylpyrrolidone copolymer, polyvinylpyrrolidone, a dimethyldiacrylammonium chloride homopolymer, an adipic acid-dimethylaminohydroxypropyldiethylenetriamine copolymer, an adipic acid-epoxypropyldiethylenetriamine copolymer and an acrylamide-β-methacryloyloxyethyltrimethylammoniummethyl sulfate copolymer.

  阳离子水解胶原蛋白、阳离子水解酪蛋白、阳离子水解大豆蛋白、阳离子乙烯基吡咯烷酮共聚物、聚乙烯吡咯烷酮、二甲基二丙烯酰胺氯化物均聚物、己二酸-二甲氨基羟丙基二乙烯三胺共聚物、己二酸-环氧丙基二乙烯三胺共聚物和丙烯酰胺-β-甲基丙烯酰氧乙基三甲基硫酸铵共聚物。
• Aqueous ophthalmic solution
  申请人：SANTEN PHARMACEUTICAL CO., LTD.

  公开号：US10278985B2

  公开（公告）日：2019-05-07

  Provided is an aqueous ophthalmic solution comprising diquafosol or a salt thereof at a concentration of 0.1% to 10% (w/v) and a chlorhexidine at a concentration of 0.0001% to 0.1% (w/v).

  本发明提供了一种眼科水溶液，其中包含浓度为 0.1% 至 10%（体积分数）的敌克松或其盐，以及浓度为 0.0001% 至 0.1%（体积分数）的洗必泰。
• Ophthalmic solution comprising diquafosol
  申请人：Santen Pharmaceutical Co., Ltd.

  公开号：US10632139B2

  公开（公告）日：2020-04-28

  Regarding Diquafosol ophthalmic solution comprising a chelating agent at a concentration of 0.0001 to 1% (w/v), formation of insoluble precipitates found in Diquafosol ophthalmic solution during storage of the solution, as well as deterioration of the filtration performance in the course of production (course of filtration sterilization), have been inhibited. Further, in Diquafosol ophthalmic solution comprising a chelating agent, reduction of eye irritation and enhancement of the preservative effectiveness have been confirmed, in comparison to Diquafosol ophthalmic solution comprising no chelating agent. Accordingly, the present invention has been confirmed to provide physicochemical properties that are stable during the courses of production and distribution as well as the course of storage by a patient, and also reduce eye irritation and enhance preservative effectiveness.

  关于含有浓度为 0.0001 至 1%（w/v）螯合剂的 Diquafosol 眼科溶液，在溶液储存过程中发现的 Diquafosol 眼科溶液中不溶性沉淀物的形成以及生产过程（过滤消毒过程）中过滤性能的恶化均已得到抑制。此外，在含有螯合剂的 Diquafosol 眼科溶液中，与不含螯合剂的 Diquafosol 眼科溶液相比，已证实减少了对眼睛的刺激并提高了防腐效果。因此，已证实本发明可提供在生产和分销过程中以及患者储存过程中稳定的理化特性，并可减少对眼睛的刺激和提高防腐剂的效果。
• Therapeutic agent for dry eye characterized by being applied to eye of dry eye patient wearing soft contact lens
  申请人：SANTEN PHARMACEUTICAL CO., LTD.

  公开号：US10729712B2

  公开（公告）日：2020-08-04

  An ophthalmic solution, which comprises diquafosol tetrasodium salt and is free from benzalkonium chloride, treats onset and/or exacerbation of dry eye symptom caused by wearing soft contact lenses.

  一种眼科溶液，由双唑磷四钠盐组成，不含苯扎氯铵，可治疗因配戴软性隐形眼镜而引起的干眼症状发作和/或加重。
• Ophthalmic solution comprising Diquafosol
  申请人：Santen Pharmaceutical Co., Ltd.

  公开号：US11166974B2

  公开（公告）日：2021-11-09

  Regarding Diquafosol ophthalmic solution comprising a chelating agent at a concentration of 0.0001 to 1% (w/v), formation of insoluble precipitates found in Diquafosol ophthalmic solution during storage of the solution, as well as deterioration of the filtration performance in the course of production (course of filtration sterilization), have been inhibited. Further, in Diquafosol ophthalmic solution comprising a chelating agent, reduction of eye irritation and enhancement of the preservative effectiveness have been confirmed, in comparison to Diquafosol ophthalmic solution comprising no chelating agent. Accordingly, the present invention has been confirmed to provide physicochemical properties that are stable during the courses of production and distribution as well as the course of storage by a patient, and also reduce eye irritation and enhance preservative effectiveness.

  关于含有浓度为 0.0001 至 1%（w/v）螯合剂的 Diquafosol 眼科溶液，在溶液储存过程中发现的 Diquafosol 眼科溶液中不溶性沉淀物的形成以及生产过程（过滤消毒过程）中过滤性能的恶化均已得到抑制。此外，在含有螯合剂的 Diquafosol 眼科溶液中，与不含螯合剂的 Diquafosol 眼科溶液相比，已证实减少了对眼睛的刺激并提高了防腐效果。因此，已证实本发明可提供在生产和分销过程中以及在患者储存过程中稳定的理化特性，并可减少对眼睛的刺激和提高防腐剂的效果。