Necrostatin-7; 5-[[3-(4-氟苯基)-1H-吡唑-4-基]亚甲基]-2-亚氨基-3-(2-噻唑基)-4-噻唑烷酮 | 351062-08-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 中文名称: Necrostatin-7; 5-[[3-(4-氟苯基)-1H-吡唑-4-基]亚甲基]-2-亚氨基-3-(2-噻唑基)-4-噻唑烷酮
• 中文别名: 5-[[3-(4-氟苯基)-1H-吡唑-4-基]亚甲基]-2-亚氨基-3-(2-噻唑基)-4-噻唑烷酮；（Z）-5-（（3-（4-氟苯基）-1H-吡唑-4-基）亚甲基）-2-亚氨基-3-（噻唑-2-基）噻唑烷-4-酮
• 英文名称: Necrostatin-7
• 英文别名: (5Z)-5-[[5-(4-fluorophenyl)-1H-pyrazol-4-yl]methylidene]-2-imino-3-(1,3-thiazol-2-yl)-1,3-thiazolidin-4-one
• CAS: 351062-08-3
• 化学式: C₁₆H₁₀FN₅OS₂
• 分子量: 371.4
• InChiKey: SMJGLNVGTJLIRV-KBEFMPHXSA-N

物化性质

• 沸点：
  613.4±65.0 °C(Predicted)
• 密度：
  1.63±0.1 g/cm3(Predicted)
• 溶解度：
  DMSO：>10mg/mL（加温）

计算性质

• 辛醇/水分配系数(LogP)：
  3.4
• 重原子数：
  25
• 可旋转键数：
  3
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  139
• 氢给体数：
  2
• 氢受体数：
  7

文献信息

• [EN] UNSATURATED HETEROCYCLIC INHIBITORS OF NECROPTOSIS<br/>[FR] INHIBITEURS HÉTÉROCYCLIQUES INSATURÉS DE LA NÉCROPTOSE
  申请人：HARVARD COLLEGE

  公开号：WO2010075290A1

  公开（公告）日：2010-07-01

  The invention features new small molecule inhibitors of necroptosis. The compounds of the invention are described by Formulas (I) and (II). The invention also features pharmaceutical compositions that include compounds of Formula (I) and (II). The compounds and compositions of the invention are also featured in kits and in methods of treatment of conditions that include neurodegenerative diseases, ischemic brain and heart injuries, and head trauma.

  这项发明涉及新型的坏死凋亡小分子抑制剂。该发明的化合物由化学式(I)和(II)描述。该发明还涉及包括化合物(I)和(II)的药物组合物。该发明的化合物和组合物还出现在试剂盒中，并用于治疗包括神经退行性疾病、缺血性脑部和心脏损伤以及头部创伤在内的疾病的治疗方法中。
• Methods for treating spinal cord injury
  申请人：Massachusetts Eye and Ear Infirmary

  公开号：US10022419B2

  公开（公告）日：2018-07-17

  Provided are methods for promoting axon regeneration of a Central Nervous System (CNS) neuron and promoting nerve function following injury to a CNS neuron, for example, brain and/or spinal cord injury. Axon regeneration in a CNS neuron or nerve function following injury to a CNS neuron can be promoted by administering a necrosis inhibitor either alone or in combination with an apoptosis inhibitor to a subject suffering from a CNS disorder, wherein a symptom of the CNS disorder is axon degeneration.

  本文提供了促进中枢神经系统（CNS）神经元轴突再生和促进中枢神经系统神经元损伤后神经功能的方法，例如脑和/或脊髓损伤。中枢神经系统神经元的轴突再生或中枢神经系统神经元损伤后的神经功能可通过向患有中枢神经系统疾病的受试者单独施用坏死抑制剂或与凋亡抑制剂联合施用来促进，其中中枢神经系统疾病的症状是轴突变性。
• Methods and compositions for preserving retinal ganglion cells
  申请人：Massachusetts Eye and Ear Infirmary

  公开号：US10617735B2

  公开（公告）日：2020-04-14

  Provided are methods and compositions for maintaining the viability of retinal ganglion cells in a subject with an ocular disorder including, for example, glaucoma and optic nerve injury. The viability of the retinal ganglion cells can be preserved by administering a necrosis inhibitor either alone or in combination with an apoptosis inhibitor to a subject having an eye with the ocular condition. The compositions, when administered, maintain the viability of the cells and/or promote axon regeneration, thereby minimizing the loss of vision or visual function associated with the ocular disorder.

  本发明提供了维持患有眼部疾病（例如青光眼和视神经损伤）的患者视网膜神经节细胞活力的方法和组合物。通过向患有眼部疾病的患者单独施用坏死抑制剂或与凋亡抑制剂联合施用，可保持视网膜神经节细胞的活力。给药后，组合物可维持细胞的活力和/或促进轴突再生，从而最大程度地减少与眼部疾病相关的视力或视觉功能的丧失。
• Compositions for preserving photoreceptor cells, retinal pigment epithelial cells, or visual function
  申请人：Massachusetts Eye and Ear Infirmary

  公开号：US10639345B2

  公开（公告）日：2020-05-05

  Provided are methods and compositions for maintaining the viability of photoreceptor cells and/or retinal pigment epithelial cells in a subject with an ocular disorder including, for example, age-related macular degeneration (AMD) (e.g., dry or neovascular AMD), retinitis pigmentosa (RP), or a retinal detachment. The viability of the photoreceptor cells and/or the retinal pigment epithelial cells can be preserved by administering a necrosis inhibitor either alone or in combination with an apoptosis inhibitor to a subject having an eye with the ocular condition. The compositions, when administered, maintain the viability of the cells, thereby minimizing the loss of vision or visual function associated with the ocular disorder.

  本发明提供的方法和组合物用于维持患有眼部疾病（例如老年性黄斑变性（AMD）（如干性或新生血管性AMD）、视网膜色素变性（RP）或视网膜脱离）的受试者的感光细胞和/或视网膜色素上皮细胞的活力。对患有眼部疾病的患者单独施用坏死抑制剂或与凋亡抑制剂联合施用，可保持感光细胞和/或视网膜色素上皮细胞的活力。这些组合物在给药后可保持细胞的活力，从而最大程度地减少与眼部疾病相关的视力或视觉功能的丧失。
• Methods for treating diabetic neurotherapy
  申请人：Massachusetts Eye and Ear Infirmary

  公开号：US10799552B2

  公开（公告）日：2020-10-13

  Provided are methods for promoting axon regeneration of a Central Nervous System (CNS) neuron and promoting nerve function following injury to a CNS neuron, for example, brain and/or spinal cord injury. Axon regeneration in a CNS neuron or nerve function following injury to a CNS neuron can be promoted by administering a necrosis inhibitor either alone or in combination with an apoptosis inhibitor to a subject suffering from a CNS disorder, wherein a symptom of the CNS disorder is axon degeneration.

  本文提供了促进中枢神经系统（CNS）神经元轴突再生和促进中枢神经系统神经元损伤后神经功能的方法，例如脑和/或脊髓损伤。中枢神经系统神经元的轴突再生或中枢神经系统神经元损伤后的神经功能可通过向患有中枢神经系统疾病的受试者单独施用坏死抑制剂或与凋亡抑制剂联合施用来促进，其中中枢神经系统疾病的症状是轴突变性。