2-[[5-[2-[(E)-[phenyl(pyridin-3-yl)methylidene]amino]oxyethyl]-7,8-dihydronaphthalen-1-yl]oxy]acetic 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-[[5-[2-[(E)-[phenyl(pyridin-3-yl)methylidene]amino]oxyethyl]-7,8-dihydronaphthalen-1-yl]oxy]acetic acid
• 化学式: C₂₆H₂₄N₂O₄
• 分子量: 428.5
• InChiKey: WBBLIRPKRKYMTD-BYCLXTJYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.9
• 重原子数：
  32
• 可旋转键数：
  9
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.19
• 拓扑面积：
  81
• 氢给体数：
  1
• 氢受体数：
  6

文献信息

• ANTIPRURITICS
  申请人：TAISHO PHARMACEUTICAL CO., LTD

  公开号：EP1477170A1

  公开（公告）日：2004-11-17

  The pharmaceutical preparation of the invention, which comprises a prostaglandin or a pharmaceutically acceptable salt thereof as an effective ingredient, has an antipruritic effect with fewer side effects. It is particularly effective in controlling the itch sensation accompanying atopic symptoms.

  本发明的药物制剂由前列腺素或其药学上可接受的盐作为有效成分，具有较少副作用的止痒效果。它对控制伴随特应性症状的瘙痒感特别有效。
• ENDOGENOUS REPAIR FACTOR PRODUCTION PROMOTERS
  申请人：ONO PHARMACEUTICAL CO., LTD.

  公开号：EP1563846A1

  公开（公告）日：2005-08-17

  It relates to an endogenous repair factor production accelerator which comprises one or at least two selected from prostaglandin (PG) 12 agonist, EP2 agonist and EP4 agonist. Since prostaglandin (PG) 12 agonist, EP2 agonist or EP4 agonist has various endogenous repair factor production accelerating action, angiogenesis acceleration action and stem cell differentiation induction action, it is useful as preventive and/or therapeutic agents for ischemic organ diseases (e.g., arteriosclerosis obliterans, Buerger disease, Raynaud disease, myocardial infarction, angina pectoris, diabetic neuropathy, spinal canal stenosis, cerebrovascular accidents, cerebral infarction, pulmonary hypertension, bone fracture, Alzheimer disease, etc.) and various cell and organ diseases.

  它涉及一种内源性修复因子生成促进剂，它包括前列腺素（PG）12 激动剂、EP2 激动剂和 EP4 激动剂中的一种或至少两种。由于前列腺素（PG）12 促效剂、EP2 促效剂或 EP4 促效剂具有各种内源性修复因子生成加速作用、血管生成加速作用和干细胞分化诱导作用，因此可用作缺血性器官疾病（如动脉硬化闭塞症）的预防和/或治疗药物、动脉硬化闭塞症、布格病、雷诺病、心肌梗塞、心绞痛、糖尿病神经病变、椎管狭窄、脑血管意外、脑梗塞、肺动脉高压、骨折、老年痴呆症等）以及各种细胞和器官疾病的预防和/或治疗药物。
• SUSTAINED RELEASE PREPARATION FOR TISSUE REGENERATION THERAPY
  申请人：ONO Pharmaceutical Co., Ltd.

  公开号：EP2087890A1

  公开（公告）日：2009-08-12

  The object of the present invention is to provide a microsphere which has a slow-release period of from about two weeks to about four weeks following administration, enables a higher content of a drug to be included, suppresses an initial burst of the drug, and enables the drug to be maintained at an optimal, effective blood concentration during the slow-release period. In a microsphere containing a drug and PLGA, the above problems can be resolved by setting: (1) the amount of lactic acid/glycolic acid copolymer per part by weight of the drug to from about 3 to about 10 parts by weight; (2) the microsphere to an average particle size of from about 20 to about 50 µm; and (3) the lactic acid/glycolic acid copolymer to a weight-average molecular weight of from about 10,000 to about 50,000 and to a lactic acid/glycolic acid compositional ratio of from about 75/25 to about 50/50. In addition, the microsphere, by promoting the production of various endogenous repair factors, is useful against various tissue disorders.

  本发明的目的是提供一种微球，该微球在给药后具有约两周到四周的缓释期，能够包含较高含量的药物，抑制药物的初始迸发，并使药物在缓释期保持在最佳的有效血药浓度。 在含有药物和 PLGA 的微球中，可以通过设置以下条件来解决上述问题：(1) 每份药物重量的乳酸/乙醇酸共聚物的量为约 3 至约 10 份重量；(2) 微球的平均粒径为约 20 至约 50 微米；(3) 乳酸/乙醇酸共聚物的重量平均分子量为约 10,000 至约 50,000 和乳酸/乙醇酸的组成比例为约 75/25 至约 50/50。 此外，微球通过促进各种内源性修复因子的产生，可用于防治各种组织疾病。
• Microspheres comprising ONO-1301
  申请人：ONO Pharmaceutical Co., Ltd.

  公开号：EP2465537A1

  公开（公告）日：2012-06-20

  It relates to an endogenous repair factor production accelerator which comprises one or at least two selected from prostaglandin (PG) 12 agonist, EP2 agonist and EP4 agonist. Since prostaglandin (PG) I2 agonist, EP2 agonist or EP4 agonist has various endogenous repair factor production accelerating action, angiogenesis acceleration action and stem cell differentiation induction action, it is useful as preventive and/or therapeutic agents for ischemic organ diseases (e.g., arteriosclerosis obliterans, Buerger disease, Raynaud disease, myocardial infarction, angina pectoris, diabetic neuropathy, spinal canal stenosis, cerebrovascular accidents, cerebral infarction, pulmonary hypertension, bone fracture, Alzheimer disease, etc.) and various cell and organ diseases.

  它涉及一种内源性修复因子生成促进剂，它包括前列腺素（PG）12 激动剂、EP2 激动剂和 EP4 激动剂中的一种或至少两种。由于前列腺素（PG）I2 激动剂、EP2 激动剂或 EP4 激动剂具有各种内源性修复因子生成加速作用、血管生成加速作用和干细胞分化诱导作用，因此可作为缺血性器官疾病（如动脉硬化闭塞症）的预防和/或治疗药物、动脉硬化闭塞症、布格病、雷诺病、心肌梗塞、心绞痛、糖尿病神经病变、椎管狭窄、脑血管意外、脑梗塞、肺动脉高压、骨折、老年痴呆症等）以及各种细胞和器官疾病的预防和/或治疗药物。
• ADVANCED HEART FAILURE TREATMENT MATERIAL AS MYOCARDIAL/CARDIOVASCULAR REGENERATION DEVICE
  申请人：Osaka University

  公开号：EP2898902A1

  公开（公告）日：2015-07-29

  Provided is an advanced heart failure treatment material, as a myocardial/cardiovascular regeneration device, that self-assembles, which can improve the universality and be used in an emergency by commercialization with no need of cell-culturing (cell-free) by controlling stem cells, and has a high therapeutic effect on the fundamental treatment of intractable cardiovascular diseases, in particular, advanced heart failure, in which not only the saving of lives but also improving the patient's quality of life (QOL) are urgent issues. The advanced heart failure treatment material of the present invention includes a pharmaceutical agent, an agent holding for the pharmaceutical agent, and a myocardial support device.

  本发明提供了一种作为心肌/心血管再生装置的晚期心力衰竭治疗材料，该材料可自我组装，通过控制干细胞，无需细胞培养（无细胞）即可提高通用性，并可通过商业化在紧急情况下使用，对于从根本上治疗难治性心血管疾病，尤其是晚期心力衰竭具有很高的治疗效果，在晚期心力衰竭中，不仅挽救生命，而且提高患者的生活质量（QOL）也是亟待解决的问题。本发明的晚期心力衰竭治疗材料包括药剂、药剂容纳器和心肌支持装置。