替占帕奈 | 154652-83-2

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 中文名称: 替占帕奈
• 英文名称: (3S,4aR,6R,8aR)-6-[2-(1H-tatrazol-5-yl)ethyl]decahydroisoquinoline-3-carboxylic acid
• 英文别名: LY293558；LY326325；(-)(3S,4aR,6R,8aR)-6-(2-(1(2)H-tetrazole-5-yl)ethyl)-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline-3-carboxylic acid monohydrate；(3S,4aR,6R,8aR)-6-(2-(1H-Tetrazol-5-yl)ethyl)-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline-3-carboxylic acid；Tezampanel；(3S,4aR,6R,8aR)-6-[2-(2H-tetrazol-5-yl)ethyl]-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline-3-carboxylic acid
• CAS: 154652-83-2
• 化学式: C₁₃H₂₁N₅O₂
• 分子量: 279.342
• InChiKey: ZXFRFPSZAKNPQQ-YTWAJWBKSA-N

物化性质

• 沸点：
  527.3±56.0 °C(Predicted)
• 密度：
  1.252±0.06 g/cm3(Predicted)
• 溶解度：
  溶于二甲基亚砜

计算性质

• 辛醇/水分配系数(LogP)：
  -0.8
• 重原子数：
  20
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.85
• 拓扑面积：
  104
• 氢给体数：
  3
• 氢受体数：
  6

制备方法与用途

Tezampanel (LY 293558, NGX 424) is a competitive antagonist that targets both AMPA and kainate receptors, showing particular selectivity for the GluR5 subtype of the kainate receptor.

反应信息

• 作为反应物：
  描述：

  替占帕奈 在 4-二甲氨基吡啶 、 palladium 10% on activated carbon 、 氢气 、 N,N'-二环己基碳二亚胺 、 sodium hydroxide 作用下， 以 四氢呋喃 、 二氯甲烷 、 水 、 异丙醇 为溶剂， 生成
  参考文献：
  名称：

  WO2023/130008

  摘要：

  公开号：
• 作为产物：
  描述：

  ethyl (3S,4aR,8aR)-6-oxo-2-(methoxycarbonyl)-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline-3-carboxylate 在 sodium hydroxide 、 dimethyl sulfide borane 、 双氧水 、 sodium hexamethyldisilazane 作用下， 以 四氢呋喃 为溶剂， 生成 替占帕奈
  参考文献：
  名称：

  Synthesis and Characterization of Phosphonic Acid-Substituted Amino Acids as Excitatory Amino Acid Receptor Antagonists

  摘要：

  DOI：

  10.1080/10426509608545152

文献信息

• [EN] ESTER DERIVATIVES OF A DECAHYDROISOQUINOLINE-3-CARBOXYLIC ACID AS ANALGESTICS<br/>[FR] DERIVES ESTER D'UN ACIDE DECAHYDROISOQUINOLINE-3 CARBOXYLIQUE UTILES EN TANT QU'ANALGESIQUES
  申请人：LILLY CO ELI

  公开号：WO2003091243A1

  公开（公告）日：2003-11-06

  Thus, the present invention provides compounds of formula (I) The present invention further provides the use of a compound of formula (I) for the manufacture of a medicament for the treatment of a neurological disorder. The present invention further provides the use of a compound of formula (I) for the manufacture of a medicament for the treatment of pain or migraine.

  因此，本发明提供了化合物的公式（I）。本发明进一步提供了利用公式（I）化合物制造用于治疗神经系统疾病的药物的用途。本发明还提供了利用公式（I）化合物制造用于治疗疼痛或偏头痛的药物的用途。
• AMPA antagonists for the treatment of dyskinesias associated with dopamine agonist therapy
  申请人：Pfizer Products Inc.

  公开号：EP0900568A2

  公开（公告）日：1999-03-10

  The invention relates to a method of treating dyskinesias associated with dopamine agonist therapy in a mammal which comprises administering to said mammal a compound, as defined herein, which is an antagonist of the AMPA receptor. Dopamine agonist therapy, as referred to in the present invention, is generally used in the treatment of a central nervous system disorder such as Parkinson's disease.

  本发明涉及一种治疗哺乳动物多巴胺激动剂治疗相关运动障碍的方法，该方法包括向所述哺乳动物施用本文所定义的化合物，该化合物是 AMPA 受体的拮抗剂。本发明所述的多巴胺激动剂疗法通常用于治疗帕金森病等中枢神经系统疾病。
• A method for treating tension-type headache
  申请人：HEADEXPLORER ApS

  公开号：EP1829539A2

  公开（公告）日：2007-09-05

  Tension-type headache is treated by interacting with neuronal transmission in relation to pain in connection with headache in a way which prevents or decreases sensitization of second order nociceptive neurons. In particular, treatment is performed by administration of an effective amount of a substance which prevents or decreases central sensitization. Important examples of such substances are substances which interact with glutamate neurotransmission, such as glutamate receptor antagonists, such as NMDA receptor antagonists, such as MK-801 or Amitriptylline or Imipramine or Desipramine or Mirtazaprine or Venlafaxine. Other examples are substances which interact with nitric oxide, such as nitric oxide synthase (NOS) inhibitors, such as L-NMMA or L-NAME or L-NIO or L-NNA. According to a broader aspect of the invention tension-type headache is treated by administration of substances which are effective in preventing or decreasing pain in connection with tension-type headache, such as the substances mentioned above. An additional aspect of the invention relates to treatment of tension-type headache by administration of substances which substantially inhibit the activity of nitric oxide synthase (NOS), such as NOS inhibitors, such as L-NMMA or L-NAME or L-NIO or L-NNA.

  治疗紧张型头痛的方法是，与头痛有关的疼痛神经元传递相互作用，防止或减少二阶痛觉神经元的敏化。具体来说，治疗方法是通过施用有效量的物质来防止或减少中枢敏化。这类物质的重要例子是与谷氨酸神经递质相互作用的物质，如谷氨酸受体拮抗剂，如NMDA受体拮抗剂，如MK-801或阿米替林或丙咪嗪或地西普胺或米氮平或文拉法辛。其他例子包括与一氧化氮相互作用的物质，如一氧化氮合酶（NOS）抑制剂，如L-NMMA或L-NAME或L-NIO或L-NNA。根据本发明更广泛的一个方面，治疗紧张型头痛的方法是施用能有效预防或减轻紧张型头痛相关疼痛的物质，如上述物质。本发明的另一个方面涉及通过施用实质上抑制一氧化氮合酶（NOS）活性的物质，如NOS抑制剂，如L-NMMA或L-NAME或L-NIO或L-NNA，来治疗紧张型头痛。
• Administration of noncompetitive AMPA receptor antagonist for neuroprotection after traumatic brain injury
  申请人：——

  公开号：US20030073683A1

  公开（公告）日：2003-04-17

  The invention provides compositions and methods for treating traumatic brain injury by the administration of a noncompetitive AMPA receptor antagonist. In certain embodiments, the noncompetitive AMPA receptor antagonist is a 2,3-benzodiazepine derivative. Illustrative 2,3-benzodiazepine derivatives useful according to the invention include (R)-7-acetyl-5(4-aminophenyl)-8,9-dihydro-8-methyl-7H-1,3-dioxolo[4,5-h][2,3]benzodiazepine.

  本发明提供了通过施用非竞争性 AMPA 受体拮抗剂治疗创伤性脑损伤的组合物和方法。在某些实施方案中，非竞争性 AMPA 受体拮抗剂是 2,3-苯并二氮杂卓衍生物。根据本发明有用的说明性2,3-苯并二氮杂卓衍生物包括(R)-7-乙酰基-5(4-氨基苯基)-8,9-二氢-8-甲基-7H-1,3-二恶茂[4,5-h][2,3]苯并二氮杂卓。
• Methods and compositions for treating inflammatory disorders of the airways
  申请人：——

  公开号：US20040152694A1

  公开（公告）日：2004-08-05

  The present invention provides compositions and methods for treating inflammatory disorders of the airways by the administration of a therapeutically effective amount of a modulator according to the invention. More specifically, the invention relates to the treatment of airway inflammations including asthma or an asthma-related pathologies.

  本发明提供了通过施用治疗有效量的根据本发明的调节剂来治疗气道炎症性疾病的组合物和方法。更具体地说，本发明涉及气道炎症的治疗，包括哮喘或与哮喘相关的病症。