3-Methoxytraxoprodil | 178457-09-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: 3-Methoxytraxoprodil
• 英文别名: 1-[(1S,2S)-1-hydroxy-1-(4-hydroxy-3-methoxyphenyl)propan-2-yl]-4-phenylpiperidin-4-ol
• CAS: 178457-09-5
• 化学式: C₂₁H₂₇NO₄
• 分子量: 357.4
• InChiKey: CAGLIAGCBUSTQI-MGPUTAFESA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  26
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.43
• 拓扑面积：
  73.2
• 氢给体数：
  3
• 氢受体数：
  5

文献信息

• PAK INHIBITORS FOR THE TREATMENT OF CELL PROLIFERATIVE DISORDERS
  申请人：AFRAXIS, INC.

  公开号：US20130116263A1

  公开（公告）日：2013-05-09

  Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of cell proliferative disorders and/or CNS disorders.

  本文提供了PAK抑制剂以及利用PAK抑制剂治疗细胞增殖性疾病和/或中枢神经系统疾病的方法。
• Pharmaceutical combinations for the treatment of stroke and traumatic brain injury
  申请人：——

  公开号：US20020045656A1

  公开（公告）日：2002-04-18

  This invention relates to methods of treating traumatic brain injury (TBI) or hypoxic or ischemic stroke, comprising administering to a patient in need of such treatment an NR2B subtype selective N-methyl-D-aspartate (NMDA) receptor antagonist in combination with either: (a) a neutrophil inhibitory factor (NIF); (b) a sodium channel antagonist; (c) a nitric oxide synthase (NOS) inhibitor; (d) a glycine site antagonist; (e) a potassium channel opener; (f) an AMPA/kainate receptor antagonist; (g) a calcium channel antagonist; (h) a GABA-A receptor modulator (e.g., a GABA-A receptor agonist); or (i) an antiinflammatory agent.

  本发明涉及治疗创伤性脑损伤（TBI）或缺氧性或缺血性中风的方法，包括向需要此类治疗的患者注射NR2B亚型选择性N-甲基-D-天门冬氨酸（NMDA）受体拮抗剂，与以下任一组合：（a）中性粒细胞抑制因子（NIF）；（b）钠通道拮抗剂；（c）一氧化氮合酶（NOS）抑制剂；（d）甘氨酸位点拮抗剂；（e）钾通道开放剂；（f）AMPA / kainate受体拮抗剂；（g）钙通道拮抗剂；（h）GABA-A受体调节剂（例如，GABA-A受体激动剂）；或（i）抗炎药物。
• Prophylactic use of N-methyl-D-aspartate (NMDA) antagonists
  申请人：——

  公开号：US20020072485A1

  公开（公告）日：2002-06-13

  This invention provides a method of inhibiting in a mammal neurological damage resulting from impairment of glucose and/or oxygen supply to the brain, which method comprises administering to the mammal prior to the impairment of glucose and/or oxygen supply to the brain an amount of an NR2B subunit selective NMDA antagonist, which amount is effective in inhibiting neurological damage. This invention also provides a method of preventing primary hyperalgesia, secondary hyperalgesia, primary allodynia, secondary allodynia, or other pain caused by central sensitization, in a mammal, which method comprises administering to the mammal, prior to affliction with said pain, an amount of an NR2B subunit selective NMDA antagonist, which amount is effective in preventing said pain.

  该发明提供了一种抑制哺乳动物神经系统损伤的方法，该损伤是由于葡萄糖和/或氧气供应不足引起的，该方法包括在葡萄糖和/或氧气供应不足之前向哺乳动物注射一定量的NR2B亚单位选择性NMDA拮抗剂，该量足以抑制神经系统损伤。该发明还提供了一种预防哺乳动物发生由中枢敏化引起的原发性疼痛、继发性疼痛、原发性触发痛、继发性触发痛或其他疼痛的方法，该方法包括在哺乳动物患有该疼痛之前向其注射一定量的NR2B亚单位选择性NMDA拮抗剂，该量足以预防该疼痛。
• NMDA NR2B antagonists for treatment
  申请人：——

  公开号：US20020072538A1

  公开（公告）日：2002-06-13

  The invention provides new methods for treating certain disorders resulting from neurodegeneration and for treating depression which comprise administration of NR2B subunit selective NMDA antagonists. The disorders that can be treating by the invention include hearing loss, vision loss, neurodegeneration caused by epileptic seizures, neurotoxin poisoning, Restless Leg Syndrome, multi-system atrophy, non-vascular headache, and depression.

  本发明提供了一种治疗神经退行性疾病引起的某些疾病和治疗抑郁症的新方法，包括给予NR2B亚单位选择性NMDA拮抗剂。该发明可用于治疗的疾病包括听力丧失、视力丧失、由癫痫发作引起的神经退行性疾病、神经毒素中毒、不宁腿综合症、多系统萎缩、非血管性头痛和抑郁症。
• Modulators of CDC2-like kinases (CLKS) and methods of use thereof
  申请人：Milne Jill

  公开号：US20070248590A1

  公开（公告）日：2007-10-25

  Provided herein are methods for using Cdc2-like kinase (Clk) modulators for treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, ocular disorders, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a Clk modulating compound in combination with another therapeutic agent.

  本文提供了使用Cdc2-like kinase (Clk)调节剂治疗和/或预防各种疾病和障碍的方法，包括与衰老或压力有关的疾病或障碍、糖尿病、肥胖症、神经退行性疾病、心血管疾病、血液凝结障碍、炎症、癌症、眼部疾病和/或潮红，以及需要增加线粒体活动的疾病或障碍。此外，提供了包含Clk调节化合物与另一种治疗剂联合使用的组合物。