7-benzyloxy-3,3-dibromochromanone | 403820-87-1

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 3,4-二氢香豆素
• 英文名称: 7-benzyloxy-3,3-dibromochromanone
• 英文别名: 3,3-dibromo-7-phenylmethoxy-4H-chromen-2-one
• CAS: 403820-87-1
• 化学式: C₁₆H₁₂Br₂O₃
• 分子量: 412.077
• InChiKey: AAGXQJIDHYJVEG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.7
• 重原子数：
  21
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.19
• 拓扑面积：
  35.5
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  3,4-dihydro-7-(phenylmethoxy)-2H-1-benzopyran-2-one 在 氮气 、 溴 作用下， 以 四氯化碳 、 乙酸乙酯 为溶剂， 以15.73 g (76%)的产率得到7-benzyloxy-3,3-dibromochromanone
  参考文献：
  名称：

  Neuroprotective compounds

  摘要：

  3R*4S*3-\x9b4-(4-氟苯基)-4-羟基哌啶-1-基!-茜草酮-4,7-二酚及其对映体和药学上可接受的盐是治疗对NMDA阻滞药敏感的疾病和病况的有效口服药物。

  公开号：

  US05744483A1

文献信息

• METHOD OF TREATING ACUTE, CHRONIC AND/OR NEUROPATHIC PAIN
  申请人：——

  公开号：US20010007872A1

  公开（公告）日：2001-07-12

  This invention relates to a method of treating acute, chronic and/or neuropathic pain in which a mammal suffering from acute, chronic and/or neuropathic pain is treated with an effective amount of an NR2B selective NMDA antagonist having a ratio of NR2B receptor activity to &agr; 1 -adrenergic receptor activity of at least about 3:1.

  本发明涉及一种治疗急性、慢性和/或神经病理性疼痛的方法，其中使用具有NR2B选择性NMDA拮抗剂的有效量来治疗患有急性、慢性和/或神经病理性疼痛的哺乳动物，所述NR2B选择性NMDA拮抗剂的NR2B受体活性与α1肾上腺素能受体活性的比率至少为约3:1。
• 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。
• Pharmaceutical combinations, for the treatment of stroke and traumatic brain injury, containing a neutrophil inhibiting factor and an selective NMDA-NR2B receptor antagonist
  申请人：Pfizer Products Inc.

  公开号：EP1186303A2

  公开（公告）日：2002-03-13

  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)或缺氧或缺血性中风的方法，包括向需要此类治疗的患者施用NR2B亚型选择性N-甲基-D-天冬氨酸(NMDA)受体拮抗剂，并与以下任一种结合使用：(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（如钙通道拮抗剂g.,(i) 抗炎剂。