N-methoxy-N-methyl-N'-[5-oxo-2-(trifluoromethyl)-5H-chromeno[2,3-b]pyridin-3-yl]urea

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并吡喃
• 英文名称: N-methoxy-N-methyl-N'-[5-oxo-2-(trifluoromethyl)-5H-chromeno[2,3-b]pyridin-3-yl]urea
• 英文别名: 1-methoxy-1-methyl-3-[5-oxo-2-(trifluoromethyl)chromeno[2,3-b]pyridin-3-yl]urea
• 化学式: C₁₆H₁₂F₃N₃O₄
• 分子量: 367.28
• InChiKey: UELKUTDTCQRAKX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  26
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.19
• 拓扑面积：
  80.8
• 氢给体数：
  1
• 氢受体数：
  8

文献信息

• TARGETED NITROXIDE AGENTS
  申请人：Wipf Peter

  公开号：US20100035869A1

  公开（公告）日：2010-02-11

  Provided herein are compositions and related methods useful for free radical scavenging, with particular selectivity for mitochondria. The compounds comprise a nitroxide-containing group attached to a mitochondria-targeting group. The compounds can be cross-linked into dimers without loss of activity. Also provided herein are methods, for preventing, mitigating and treating damage caused by radiation. The method comprises delivering a compound, as described herein, to a patient in an amount and dosage regimen effective to prevent, mitigate or treat damage caused by radiation.

  本文提供了一种对自由基清除有用的组合物和相关方法，具有特定选择性作用于线粒体。这些化合物包括一个连接到线粒体靶向基团的亚硝基含有基团。这些化合物可以交联成二聚体而不丧失活性。本文还提供了一种用于预防、缓解和治疗辐射引起的损伤的方法。该方法包括向患者输送一种如本文所述的化合物，以有效地预防、缓解或治疗辐射引起的损伤。
• INTRAESOPHAGEAL ADMINISTRATION OF TARGETED NITROXIDE AGENTS FOR PROTECTION AGAINST IONIZING IRRADIATION-INDUCED ESOPHAGITIS
  申请人：University of Pittsburgh - Of the Commonwealth System of Higher Education

  公开号：US20190210969A1

  公开（公告）日：2019-07-11

  Provided herein are compositions and related methods useful for prevention or mitigation of ionizing radiation-induced esophagitis. The compositions comprise compounds comprising a nitroxide-containing group attached to a mitochondria-targeting group. The compounds can be cross-linked into dimers without loss of activity. The method comprises delivering a compound, as described herein, to a patient in an amount and dosage regimen effective to prevent or mitigate esophageal damage caused by radiation.

  本文提供了一种用于预防或缓解电离辐射诱导的食管炎的组合物和相关方法。这些组合物包括含有与线粒体靶向基团相连的亚硝基含有基团的化合物。这些化合物可以交联成二聚体而不丧失活性。该方法包括向患者输送本文所述的化合物，以有效预防或缓解由辐射引起的食道损伤。
• TOPICAL FORMULATIONS OF TARGETED NITROXIDE AGENTS
  申请人：Falo, JR. Louis D.

  公开号：US20120207687A1

  公开（公告）日：2012-08-16

  A method for preventing or treating skin damage in a radiotherapy subject, comprising topically administering to the subject a composition that includes a therapeutically effective amount at least one targeted nitroxide agent and at least one additional ingredient.

  一种用于预防或治疗放疗受试者皮肤损伤的方法，包括将至少一种靶向亚硝酰胺试剂和至少一种其他成分的治疗有效剂量的组合物局部施用于受试者的皮肤。
• USE OF TARGETED NITROXIDE AGENTS IN PREVENTING, MITIGATING AND TREATING RADIATION INJURY
  申请人：Wipf Peter

  公开号：US20110172214A1

  公开（公告）日：2011-07-14

  Provided herein are compositions and related methods useful for free radical scavenging, with particular selectivity for mitochondria. The compounds comprise a nitroxide-containing group attached to a mitochondria-targeting group. The compounds can be cross-linked into dimers without loss of activity. Also provided herein are methods, for preventing, mitigating and treating damage caused by radiation. The method comprises delivering a compound, as described herein, to a patient in an amount and dosage regimen effective to prevent, mitigate or treat damage caused by radiation.

  本文提供了一种有用于自由基清除的组合物和相关方法，特别是对线粒体的选择性。该化合物包括连接到线粒体靶向基团的亚硝基含有基团。该化合物可以交联成二聚体而不失去活性。本文还提供了一种方法，用于预防、缓解和治疗放射性损伤。该方法包括将上述所述的化合物以有效的剂量和用药方案输送给患者，以预防、缓解或治疗放射性损伤。
• Compounds for the treatment of pathologies associated with aging and degenerative disorders
  申请人：University of Pittsburgh—of the Commonwealth System of Higher Education

  公开号：US10751273B2

  公开（公告）日：2020-08-25

  The present invention relates to methods of inhibiting one or more signs of aging and/or degenerative disorder in a subject in need of such treatment, which comprise administering, to the subject, an effective amount of one or more of the compounds as set forth herein. “Inhibiting a sign of aging or degenerative disorder” means reducing the risk of occurrence, delaying the onset, slowing the progression, and/or reducing the severity and/or manifestation, of a sign of aging or degenerative disorder, and includes, but is not limited to, preventing the occurrence, development or progression of a sign of aging or degenerative disorder.

  本发明涉及在需要治疗的受试者中抑制一种或多种衰老和/或退行性失调迹象的方法，其中包括向受试者施用有效量的一种或多种本文所述化合物。"抑制衰老或退行性病变的征兆 "是指降低衰老或退行性病变征兆的发生风险、延迟发病、减缓进展和/或降低严重程度和/或表现，并包括但不限于预防衰老或退行性病变征兆的发生、发展或进展。