2-Methyl-2-[4-[(2,4,6-trichlorophenyl)carbamoylamino]phenoxy]propanoic acid

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 2-Methyl-2-[4-[(2,4,6-trichlorophenyl)carbamoylamino]phenoxy]propanoic acid
• 化学式: C₁₇H₁₅Cl₃N₂O₄
• 分子量: 417.7
• InChiKey: BJINMEROLLOVGH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.5
• 重原子数：
  26
• 可旋转键数：
  5
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.18
• 拓扑面积：
  87.7
• 氢给体数：
  3
• 氢受体数：
  4

文献信息

• Ophthalmic formulation for the prevention and treatment of ocular conditions
  申请人：Chakshu Research, Inc.

  公开号：EP1972344A1

  公开（公告）日：2008-09-24

  An ophthalmic formulation is provided for the prevention and treatment of adverse ocular conditions, including presbyopia, arcus senilis, age-related macular degeneration, and other conditions associated with aging. The formulation is also useful in the prevention and treatment of other adverse ocular conditions such as those associated with oxidative and/or free radical damage within the eye; these conditions can involve a condition, disease, or disorder of the cornea, retina, lens, sclera, anterior segment, or posterior segment of the eye. In one embodiment, the formulation contains at least 0.6 wt.% of a biocompatible chelating agent, an effective permeation enhancing amount of an ophthalmic permeation enhancer such as methylsulfonylmethane (MSM), an anti-AGE agent, i.e., a compound that serves to reduce the presence of advanced glycation endproducts (AGEs) in the eye, and a pharmaceutically acceptable ophthalmic carrier suited to the particular formulation type (e.g., eye drops or ointments). Preferred components of the formulation are multifunctional and naturally occurring.

  本制剂是一种眼科制剂，用于预防和治疗眼部不良症状，包括老花眼、老年性角膜病、老年性黄斑变性以及其他与衰老相关的症状。该制剂还可用于预防和治疗其他眼部不良症状，如与眼内氧化和/或自由基损伤有关的症状；这些症状可能涉及角膜、视网膜、晶状体、巩膜、眼前节或眼后节的状况、疾病或紊乱。在一个实施方案中，制剂含有至少 0.6 重量百分比的生物相容性螯合剂、有效渗透量的眼科渗透促进剂（如甲基磺酰基甲烷 (MSM)）、抗衰老剂（即：一种可减少眼内自由基含量的化合物）、一种可减少眼内高级糖化终产物（AGEs）的化合物，以及一种适合特定制剂类型（如滴眼液或软膏）的药学上可接受的眼科载体。制剂的首选成分是多功能的天然成分。
• Ophthalmic formulation for the prevention and treatment of adverse ocular conditions, particularly those associated with the aging eye
  申请人：——

  公开号：US20040137068A1

  公开（公告）日：2004-07-15

  An ophthalmic formulation is provided for the prevention and treatment of adverse ocular conditions, including presbyopia, arcus senilis, age-related macular degeneration, and other conditions associated with aging. The formulation is also useful in the prevention and treatment of other adverse ocular conditions such as those associated with oxidative and/or free radical damage within the eye; these conditions can involve a condition, disease, or disorder of the cornea, retina, lens, sclera, anterior segment, or posterior segment of the eye. In one embodiment, the formulation contains at least 0.6 wt. % of a biocompatible chelating agent, an effective permeation enhancing amount of an ophthalmic permeation enhancer such as methylsulfonylmethane (MSM), an anti-AGE agent, i.e., a compound that serves to reduce the presence of advanced glycation endproducts (AGEs) in the eye, and a pharmaceutically acceptable ophthalmic carrier suited to the particular formulation type (e.g., eye drops or ointments). Preferred components of the formulation are multifunctional and naturally occurring.

  本制剂是一种眼科制剂，用于预防和治疗眼部不良症状，包括老花眼、老年性角膜病、老年性黄斑变性以及其他与衰老相关的症状。该制剂还可用于预防和治疗其他眼部不良症状，如与眼内氧化和/或自由基损伤有关的症状；这些症状可能涉及角膜、视网膜、晶状体、巩膜、眼前节或眼后节的状况、疾病或紊乱。在一个实施方案中，制剂含有至少 0.6 重量百分比的生物相容性螯合剂、有效渗透量的眼科渗透促进剂（如甲基磺酰基甲烷 (MSM)）、抗衰老剂（即：一种可减少眼内自由基含量的化合物）、一种可减少眼内高级糖化终产物（AGEs）的化合物，以及一种适合特定制剂类型（如滴眼液或软膏）的药学上可接受的眼科载体。制剂的首选成分是多功能的天然成分。
• Treatment of conditions associated with the presence of macromolecular aggregates, particularly ophthalmic disorders
  申请人：Bhushan Rajiv

  公开号：US20060166879A1

  公开（公告）日：2006-07-27

  A method and formulation are provided for the treatment of medical conditions associated with the formation and/or deposition of macromolecular aggregates, particularly those associated with adverse ocular conditions. The formulation contains a non-cytotoxic chelating agent containing at least three negatively charged chelating atoms and a charge-masking agent containing at least one polar group and having a molecular weight of less than about 250, wherein the polar group contains at least one and preferably at least two heteroatoms having a Pauling electronegativity greater than about 3.00, and further wherein the molar ratio of the charge-masking agent to the chelating agent is sufficient to ensure that substantially all negatively charged chelating atoms are associated with a heteroatom on the charge-masking agent.

  本发明提供了一种方法和制剂，用于治疗与大分子聚集体的形成和/或沉积有关的病症，特别是与眼部不良状况有关的病症。该制剂含有至少三个带负电荷的螯合原子的无细胞毒性螯合剂和含有至少一个极性基团且分子量小于约 250 的电荷掩蔽剂，其中极性基团含有至少一个，最好是至少两个保灵电负性大于约 3 的杂原子。00，其中电荷掩蔽剂与螯合剂的摩尔比足以确保基本上所有带负电荷的螯合原子都与电荷掩蔽剂上的杂原子相连。
• Formulation and method for administration of ophthalmologically active agents
  申请人：Bhushan Rajiv

  公开号：US20060172972A1

  公开（公告）日：2006-08-03

  A method and formulation are provided for the administration of ophthalmologically active agents. In one embodiment, the method and formulation provided are for the treatment of medical conditions associated with the formation and/or deposition of macromolecular aggregates, particularly those associated with adverse ocular conditions. In another embodiment, the method and formulation provided are for the treatment of ocular conditions and disorders associated with aging.

  本发明提供了一种施用眼科活性制剂的方法和制剂。在一个实施方案中，所提供的方法和制剂用于治疗与大分子聚集体的形成和/或沉积有关的病症，特别是与眼部不良状况有关的病症。在另一个实施方案中，所提供的方法和制剂用于治疗与衰老相关的眼部疾病和失调。
• NOVEL INHIBITORS OF FORMATION OF ADVANCED GLYCATION ENDPRODUCTS (AGE'S)
  申请人：City of Hope

  公开号：EP1165064A2

  公开（公告）日：2002-01-02