Propan-2-yl 2-[[6-[1-amino-2-(4-pyrazol-1-ylphenyl)-1-pyridin-3-ylsulfonylethyl]pyridin-2-yl]amino]acetate

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: Propan-2-yl 2-[[6-[1-amino-2-(4-pyrazol-1-ylphenyl)-1-pyridin-3-ylsulfonylethyl]pyridin-2-yl]amino]acetate
• 英文别名: propan-2-yl 2-[[6-[1-amino-2-(4-pyrazol-1-ylphenyl)-1-pyridin-3-ylsulfonylethyl]pyridin-2-yl]amino]acetate
• 化学式: C₂₆H₂₈N₆O₄S
• 分子量: 520.6
• InChiKey: LWQVOQGHZCZWNI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  37
• 可旋转键数：
  11
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.23
• 拓扑面积：
  151
• 氢给体数：
  2
• 氢受体数：
  9

文献信息

• PHARMACEUTICAL PREPARATION INCLUDING PYRIDYLAMINO ACETIC ACID COMPOUND
  申请人：Santen Pharmaceutical Co., Ltd

  公开号：EP3424503A1

  公开（公告）日：2019-01-09

  An object of the present invention is to find which of an enormous number of pyridylaminoacetic acid compounds has a particularly excellent intraocular pressure lowering effect and may be used as a therapeutic or preventive agent for glaucoma or ocular hypertension or an intraocular pressure lowering agent, and to find how the found compound is used and/or what dose of the compound is instilled to a patient (mainly, a human) in order to achieve an effective therapeutic or preventive effect. Provided is a pharmaceutical preparation for treatment or prevention of glaucoma or ocular hypertension, comprising 0.0003 to 0.01% (w/v) of isopropyl (6-[4-(pyrazol-1-yl)benzyl] (pyridin-3-ylsulfonyl)aminomethyl}pyridin-2-ylamino) acetate, or a salt thereof.

  本发明的目的是在大量的吡啶基氨基乙酸化合物中找出哪一种具有特别优异的降低眼压效果，可用作青光眼或眼压过高的治疗或预防剂或眼压降低剂，并找出如何使用所发现的化合物和/或向患者（主要是人）灌注多大剂量的化合物才能达到有效的治疗或预防效果。 本发明提供了一种用于治疗或预防青光眼或眼压过高的药物制剂，其中包含 0.0003% 至 0.01% (w/v) 的 (6-[4-(吡唑-1-基)苄基](吡啶-3-基磺酰基)氨基甲基}吡啶-2-基氨基) 乙酸异丙酯或其盐。
• PHARMACEUTICAL FORMULATIONS COMPRISING A PYRIDYLAMINOACETIC ACID COMPOUND
  申请人：SANTEN PHARMACEUTICAL CO., LTD.

  公开号：US20160324838A1

  公开（公告）日：2016-11-10

  Provided is a pharmaceutical preparation for treatment or prevention of glaucoma or ocular hypertension, comprising 0.0003 to 0.01% (w/v) of isopropyl (6-[4-(pyrazol-1-yl)benzyl] (pyridin-3-ylsulfonyl)aminomethyl}pyridin-2-ylamino) acetate, or a salt thereof. The pharmaceutical preparation has an excellent intraocular pressure lowering effect and may be used as a therapeutic or preventive agent for glaucoma or ocular hypertension or an intraocular pressure lowering agent.
• US9943510B2
  申请人：——

  公开号：US9943510B2

  公开（公告）日：2018-04-17
• USRE48183E1
  申请人：——

  公开号：USRE48183E1

  公开（公告）日：2020-09-01