(6R)-6-[[[(4-氯苯基)磺酰基]氨基]-5,6,7,8-四氢-2-甲基-1-萘丙酸 | 165538-40-9

• 物质功能分类: 生物化工 - 生化试剂 - 激动剂抑制剂
• 分子结构分类: 有机化合物 - 苯类化合物 - 四氢化萘
• 中文名称: (6R)-6-[[[(4-氯苯基)磺酰基]氨基]-5,6,7,8-四氢-2-甲基-1-萘丙酸
• 中文别名: (R)-3-(6-(4--氯苯基磺胺基)-2-甲基-5,6,7,8-四氢萘-1-基)丙酸
• 英文名称: Terutroban
• 英文别名: S-18886；S18886；3-{6-[(4-chlorophenylsulphonyl)amino]-2-methyl-5,6,7,8-tetrahydronaphth-1-yl}propionic acid；3-[(6R)-6-[(4-chlorophenyl)sulfonylamino]-2-methyl-5,6,7,8-tetrahydronaphthalen-1-yl]propanoic acid
• CAS: 165538-40-9
• 化学式: C₂₀H₂₂ClNO₄S
• 分子量: 407.918
• InChiKey: HWEOXFSBSQIWSY-MRXNPFEDSA-N

物化性质

• 熔点：
  189 - 192°C
• 沸点：
  591.8±60.0 °C(Predicted)
• 密度：
  1.38±0.1 g/cm3(Predicted)
• 溶解度：
  氯仿（轻微溶解，超声处理）、DMSO（轻微溶解）、甲醇（轻微溶解，超声处理）

计算性质

• 辛醇/水分配系数(LogP)：
  4.1
• 重原子数：
  27
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.35
• 拓扑面积：
  91.8
• 氢给体数：
  2
• 氢受体数：
  5

安全信息

• 危险性防范说明：
  P261,P264,P271,P280,P302+P352,P304+P340+P312,P305+P351+P338,P332+P313,P337+P313,P362,P403+P233,P405,P501
• 危险性描述：
  H315,H319,H335
• 储存条件：
  2-8℃

制备方法与用途

用途

特鲁曲班可作为缺血性中风或短暂性脑缺血发作患者的抗血小板疗法，并在抗凝药物防治脑卒中的研究过程中发挥作用。

生物活性

Terutroban是一种血栓素-前列腺素受体拮抗剂。

文献信息

• Novel Thromboxane A2 (TP) Receptor Antagonists
  申请人：The Trustees of the University of Pennsylvania

  公开号：US20130165488A1

  公开（公告）日：2013-06-27

  The present invention relates to novel TP receptor antagonists, which optionally cross the blood-brain barrier of a mammal. The invention also provides methods for treating a disorder related to activation of TP receptor utilizing the compounds of the invention.

  本发明涉及一种新型的TP受体拮抗剂，该拮抗剂可以选择性地穿越哺乳动物的血脑屏障。该发明还提供了使用该发明化合物治疗与TP受体激活相关的疾病的方法。
• Novel Tetrahydronaphalene Antagonists to the Thromboxane A2 (TP) Receptor
  申请人：Trojanowski John Q.

  公开号：US20130190370A1

  公开（公告）日：2013-07-25

  The present invention relates to TP receptor antagonists, which have the ability to bind to TP receptor and optionally cross the blood brain barrier. The invention also provides compositions and methods for treating a disorder wherein activation of TP receptor is detrimental.

  本发明涉及TP受体拮抗剂，其具有结合TP受体的能力，并可选择性地穿越血脑屏障。本发明还提供了治疗激活TP受体有害的疾病的组合物和方法。
• TXA2 inhibitor as stimulator or inducer of MHC Class I cross-presentation
  申请人：INSTITUT PASTEUR

  公开号：EP3037106A1

  公开（公告）日：2016-06-29

  The application relates to a thromboxane A2 (TXA2) inhibitor. The application also relates to an Antigen Presenting Cell (APC), in the cytosol of which said TXA2 inhibitor is contained. Said TXA2 inhibitor can e.g., be a Non-Steroidal Anti-Inflammatory Drug (NSAID). More particularly, the application relates to means, such as preparations, compositions, and methods, which comprise or involve said TXA2 inhibitor or APC. Said TXA2 inhibitor or APC can notably be used as stimulator or inducer of the immune response, more particularly of MHC Class I cross-presentation.

  本申请涉及一种血栓素 A2（TXA2）抑制剂。本申请还涉及一种抗原呈递细胞（APC），其细胞液中含有所述 TXA2 抑制剂。所述 TXA2 抑制剂可以是非类固醇消炎药 (NSAID)。 更具体地说，本申请涉及包含或涉及所述 TXA2 抑制剂或 APC 的手段，如制剂、组合物和方法。 所述TXA2抑制剂或APC可显著用作免疫反应的刺激剂或诱导剂，尤其是MHC I类交叉呈递的刺激剂或诱导剂。
• Association between an anti-atherothrombotic and an angiotensin-converting enzyme inhibitor
  申请人：Verbeuren Tony

  公开号：US20090075976A1

  公开（公告）日：2009-03-19

  The present invention relates to the association of an anti-atherothrombotic and an angiotensin-converting enzyme inhibitor (ACEI), and also to pharmaceutical compositions containing them, and to methods of treating vascular complications associated with diabetes, with atherothrombotic diseases, with hyperlipidaemia, with hypertension, with chronic venous diseases, with inflammation, with metabolic syndrome associated with obesity, or with cancer, with such association.
• US8927586B2
  申请人：——

  公开号：US8927586B2

  公开（公告）日：2015-01-06