布洛芬二乙基氨基乙基酯 | 64622-41-9

• 分子结构分类: 有机化合物 - 脂质和类脂质分子 - 异戊烯醇脂质
• 中文名称: 布洛芬二乙基氨基乙基酯
• 英文名称: diethylaminoethyl 2-(p-isobutyl-phenyl)propionate
• 英文别名: diethylaminoethyl 2-(p-isobutylphenyl)propionate；diethylaminoethyl-2-(p-isobutylphenyl)propanoate；Ibuprofen diethylaminoethyl ester；2-(diethylamino)ethyl 2-[4-(2-methylpropyl)phenyl]propanoate
• CAS: 64622-41-9
• 化学式: C₁₉H₃₁NO₂
• 分子量: 305.461
• InChiKey: LMNZWAJFILAFEC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.6
• 重原子数：
  22
• 可旋转键数：
  10
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.63
• 拓扑面积：
  29.5
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  布洛芬 在 氯化亚砜 作用下， 以 四氢呋喃 、 甲苯 为溶剂， 反应 2.0h， 生成 布洛芬二乙基氨基乙基酯
  参考文献：
  名称：

  布洛芬和萘普生的酯和酰胺前药：合成，抗炎活性和胃肠道毒性。

  摘要：

  合成了布洛芬（1）和萘普生（16）的酯和酰胺前药，并评估其抗炎活性和胃肠道毒性。前药的化学结构在亲脂性和对水解的反应性方面有所不同。小鼠中乙酸诱导的扭体的抑制表明前药7、15、19和20表现出比母体化合物明显更好的活性（p小于0.01）。确定大鼠口服1和16以及前药5、18、21和22后在胃粘膜中形成的平均溃疡数。除甘氨酸酰胺21外，所有前药对胃粘膜的刺激​​性均显着低于1或16。

  DOI：

  10.1002/jps.2600810210

文献信息

• [EN] NOVEL HIGH PENETRATION DRUGS AND THEIR COMPOSITIONS THEREOF FOR TREATMENT OF PARKINSON DISEASES<br/>[FR] NOUVEAUX MÉDICAMENTS À PÉNÉTRATION ÉLEVÉE ET LEURS COMPOSITIONS POUR LE TRAITEMENT DE MALADIES DE PARKINSON
  申请人：TECHFIELDS PHARMA CO LTD

  公开号：WO2014139161A1

  公开（公告）日：2014-09-18

  One aspect of the invention provides a composition of novel high penetration compositions (HPC) or a high penetration prodrug (HPP) for treatment of Parkinson's disease. The HPCs/HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPCs/HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.

  本发明的方面之一提供了用于治疗帕金森病的新型高渗透组合物（HPC）或高渗透前药（HPP）。HPCs/HPPs能够穿过生物屏障后转化为母药活性药物或药物代谢物，因此能够对母药或代谢物能够治疗的疾病进行治疗。此外，HPPs能够到达母药可能无法进入的区域或在目标区域达到足够的浓度，从而实现新的治疗方法。HPCs/HPPs可以通过各种给药途径给药给受试者，例如，局部施用于具有高浓度的疾病作用部位，或者系统性地给药给生物受试者，并以更快的速率进入全身循环。
• HIGH PENETRATION COMPOSITIONS AND USES THEREOF
  申请人：Yu Chongxi

  公开号：US20090238763A1

  公开（公告）日：2009-09-24

  The present invention relates to compositions and uses of novel high penetration compositions or high penetration prodrugs (HPP), in particular HPPs for non-steroidal anti-inflammatory agents (NSAIAs), which are capable of crossing biological barriers with high penetration efficiency. The HPPs herein are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, due to the ability of penetrating biological barriers, the HPPs herein are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPPs herein can be administered to a subject through various administration routes. For example, the HPPs can be locally delivered to an action site of a condition with a high concentration due to their ability of penetrating biological barriers and thus obviate the need for a systematic administration. For another example, the HPPs herein can be systematically administer to a biological subject and enter the general circulation with a faster rate.

  本发明涉及新型高渗透性组合物或高渗透性前药（HPP）的组成和用途，特别是用于非甾体抗炎药（NSAIAs）的HPP，其能够高效地穿过生物屏障。这里的HPP能够在穿过生物屏障后转化为父活性药物或药物代谢物，从而可以治疗与父药物或代谢物相关的疾病。此外，由于能够穿过生物屏障，这里的HPP能够到达父药物可能无法进入或无法在目标区域产生足够浓度的区域，从而提供新的治疗方法。这里的HPP可以通过各种给药途径给予受试者。例如，由于其穿透生物屏障的能力，HPP可以在局部给药到疾病作用部位并以高浓度存在，从而避免系统性给药的需要。另一个例子是，这里的HPP可以被系统性地给药到生物体内，并以更快的速率进入循环系统。
• NOVEL HIGH PENETRATION DRUGS AND THEIR COMPOSITIONS THEREOF FOR TREATMENT OF PARKINSON DISEASES
  申请人：SUZHOU TECHFIELDS MEDICAL LTD.

  公开号：US20160002157A1

  公开（公告）日：2016-01-07

  One aspect of the invention provides a composition of novel high penetration compositions (HPC) or a high penetration prodrug (HPP) for treatment of Parkinson's disease. The HPCs/HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPCs/HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.

  发明的一个方面提供了一种用于治疗帕金森病的新型高穿透力组合物（HPC）或高穿透力前药（HPP）。 HPC / HPP能够在穿过生物屏障后转化为活性药物或药物代谢物，从而可以治疗父药物或代谢物可以治疗的疾病。此外，HPP能够到达父药物可能无法访问或在目标区域提供足够浓度的区域，从而提供新的治疗方法。 HPC / HPP可以通过各种给药途径给予受试者，例如局部给药到具有高浓度的病变部位或系统给药到生物学受体并以更快的速度进入全身循环。
• STABLE PHARMACEUTICAL COMPOSITION CONTAINING NON-STEROIDAL ANTI-INFLAMMATORY DRUG DERIVATIVE
  申请人：Zhejiang Yuejia Pharmaceuticals Co., Ltd

  公开号：EP3701937A1

  公开（公告）日：2020-09-02

  A stable pharmaceutical composition containing a non-steroidal anti-inflammatory drug derivative, at least comprising a separated solid part and liquid part, the solid part comprising a therapeutically effective dose of non-steroidal anti-inflammatory drug derivative and the liquid part being a pharmaceutically acceptable solvent.

  一种含有非甾体抗炎药物衍生物的稳定药物组合物，至少包括分离的固体部分和液体部分，固体部分含有治疗有效剂量的非甾体抗炎药物衍生物，液体部分为药学上可接受的溶剂。
• High penetration drugs and their compositions thereof for treatment of Parkinson diseases
  申请人：Techfields Pharma Co., Ltd.

  公开号：US11084813B2

  公开（公告）日：2021-08-10

  One aspect of the invention provides a composition of novel high penetration compositions (HPC) or a high penetration prodrug (HPP) for treatment of Parkinson's disease. The HPCs/HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPCs/HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.

  本发明的一个方面提供了一种用于治疗帕金森病的新型高渗透组合物（HPC）或高渗透原药（HPP）。HPCs/HPPs 在穿过生物屏障后能够转化为母体活性药物或药物代谢物，因此能够对母体药物或代谢物所能治疗的病症进行治疗。此外，HPPs 还能到达母体药物可能无法到达的区域，或在目标区域产生足够的浓度，从而提供新的治疗方法。HPCs/HPPs 可通过各种给药途径给受试者用药，例如，以高浓度局部给药到疾病的作用部位，或系统地给生物受试者用药，并以更快的速度进入血液循环。