N-{(1S)-1-[({(4R)-1-[(4-fluorophenyl)suIfonyI]-3-oxohexahydro-1H-azepin-4-yl}amino)carbonyI]-3-methyIbutyl}-1-benzothiophene-2-carboxamide | 281216-61-3

• 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
• 英文名称: N-{(1S)-1-[({(4R)-1-[(4-fluorophenyl)suIfonyI]-3-oxohexahydro-1H-azepin-4-yl}amino)carbonyI]-3-methyIbutyl}-1-benzothiophene-2-carboxamide
• 英文别名: N-[(2S)-1-[[(4R)-1-(4-fluorophenyl)sulfonyl-3-oxoazepan-4-yl]amino]-4-methyl-1-oxopentan-2-yl]-1-benzothiophene-2-carboxamide
• CAS: 281216-61-3
• 化学式: C₂₇H₃₀FN₃O₅S₂
• 分子量: 559.683
• InChiKey: IPVHTBGJYIHNQK-YADHBBJMSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5
• 重原子数：
  38
• 可旋转键数：
  8
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.37
• 拓扑面积：
  149
• 氢给体数：
  2
• 氢受体数：
  8

反应信息

• 作为产物：
  描述：

  (S)-2-(2-benzo[b]thiophene-2-carboxylic acid)-4-methyl-pentanoic acid [3-hydroxy-1-(4-fluorobenzenesulfonyl)-azepan-4-yl]-amide 在 戴斯-马丁氧化剂 作用下， 以 二氯甲烷 为溶剂， 反应 0.5h， 生成 N-{(1S)-1-[({(4R)-1-[(4-fluorophenyl)suIfonyI]-3-oxohexahydro-1H-azepin-4-yl}amino)carbonyI]-3-methyIbutyl}-1-benzothiophene-2-carboxamide 、
  参考文献：
  名称：

  [EN] METHOD FOR ACTIVATING TRPV4 CHANNEL RECEPTORS BY AGONISTS
  [FR] PROCÉDÉ D'ACTIVATION DES RÉCEPTEURS-CANAUX TRPV4 PAR DES AGONISTES

  摘要：

  公开号：

  WO2006029209A3

文献信息

• Method for Activating Trpv4 Channel Receptors by Agonists
  申请人：Kumar Sanjay

  公开号：US20070259856A1

  公开（公告）日：2007-11-08

  This invention relates to methods for activating a TRPV4 channel receptor, thereby reducing the production and/or release of matrix degrading enzymes by a cell expressing a TRPV4 channel receptor, thereby reducing the breakdown of an extra-cellular matrix. Also contemplated within the scope of the invention are methods of attenuating the inhibition of matrix production.

  本发明涉及激活TRPV4通道受体的方法，从而减少表达TRPV4通道受体的细胞产生和/或释放基质降解酶，从而减少细胞外基质的分解。本发明还考虑了减轻基质生产抑制的方法。
• CATIONIC DRY POWDERS COMPRISING MAGNESIUM SALT
  申请人：Pulmatrix Operating Company, Inc.

  公开号：EP3470057A1

  公开（公告）日：2019-04-17

  The invention relates to respirable dry particles that contain one or more divalent metal cations, such as calcium, in an amount of less than 3% by weight, and to dry powders that contain the respirable particles. The dry particles can further contain an active agent, or can be used as carrier particles to deliver an active agent.

  本发明涉及含有一种或多种二价金属阳离子（如钙）且含量小于 3% （按重量计）的可吸入干颗粒，以及含有这种可吸入颗粒的干粉。干粉颗粒可进一步含有活性剂，或用作输送活性剂的载体颗粒。
• Monovalent metal cation dry powders for inhalation
  申请人：Pulmatrix Operating Company, Inc.

  公开号：US10376465B2

  公开（公告）日：2019-08-13

  The present invention is directed toward respirable dry powders and particles for systemic delivery of pharmaceutically active agents or delivery to the respiratory tract. The dry powders contain one or more monovalent metal cations (such as Na+), are small and dispersible.

  本发明针对的是用于全身给药或呼吸道给药的可吸入干粉和颗粒。干粉含有一种或多种单价金属阳离子（如 Na+），体积小且可分散。
• Methods for producing respirable dry powders
  申请人：Pulmatrix Operating Company, Inc.

  公开号：US10589039B2

  公开（公告）日：2020-03-17

  The invention related to dry powders that contain a therapeutic agent. The dry powders have characteristics, e.g., they are processable and/or dense in therapeutic agent that provide advantages for formulating and delivering therapeutic agents to patients.

  本发明涉及含有治疗剂的干粉。干粉具有可加工和/或富含治疗剂等特点，这些特点为配制治疗剂和向患者提供治疗剂提供了优势。
• Inhalable dry powders
  申请人：Pulmatrix Operating Company, Inc.

  公开号：US10806871B2

  公开（公告）日：2020-10-20

  The invention related to dry powders that contain a therapeutic agent. The dry powders have characteristics, e.g., they are processable and/or dense in therapeutic agent that provide advantages for formulating and delivering therapeutic agents to patients.

  本发明涉及含有治疗剂的干粉。干粉具有可加工和/或富含治疗剂等特点，这些特点为配制治疗剂和向患者提供治疗剂提供了优势。