3,4-二氢-6,7-二甲氧基-alpha-苯基-N,N-二[2-(2,3,4-三甲氧基苯基)乙基]-1-异喹啉乙酰胺 | 149759-26-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 异喹啉及其衍生物
• 中文名称: 3,4-二氢-6,7-二甲氧基-alpha-苯基-N,N-二[2-(2,3,4-三甲氧基苯基)乙基]-1-异喹啉乙酰胺
• 英文名称: Pinokalant
• 英文别名: 2-(6,7-dimethoxy-3,4-dihydroisoquinolin-1-yl)-2-phenyl-N,N-bis[2-(2,3,4-trimethoxyphenyl)ethyl]acetamide
• CAS: 149759-26-2
• 化学式: C₄₁H₄₈N₂O₉
• 分子量: 712.8
• InChiKey: PYWYBTRACMRUQV-UHFFFAOYSA-N

物化性质

• 沸点：
  803.7±65.0 °C(Predicted)
• 密度：
  1.17±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  6.6
• 重原子数：
  52
• 可旋转键数：
  17
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.37
• 拓扑面积：
  107
• 氢给体数：
  0
• 氢受体数：
  10

文献信息

• Verwendung von kondensierte Dihydropyridine zur Behandlung von chronisch inflammatorische Prozesse
  申请人：BOEHRINGER INGELHEIM KG

  公开号：EP0781556A1

  公开（公告）日：1997-07-02

  Die Erfindung betrifft die Verwendung von carbocyclisch und heterocyclisch anellierten Dihydropyridinen der Formel sowie deren tautomere Formen der Formel II worin A für die anellierten Ringsysteme steht und X für OR1, NHR2 oder NR3R4, für die Herstellung von Mitteln für die Behandlung chronisch inflammatorischer Prozesse.

  本发明涉及如下式的碳环和杂环融合二氢吡啶及其同分异构体的用途 及其式 II 的同分异构体的用途 其中 A 代表熔合环系统 X 代表 OR1、NHR2 或 NR3R4，用于制备治疗慢性炎症过程的制剂。
• SUR1 inhibitors for therapy
  申请人：University of Maryland, Baltimore

  公开号：EP2719380A2

  公开（公告）日：2014-04-16

  The present invention provides An NCca-ATP inhibitor for use in a method for treating and/or preventing: (i) colitis or inflammatory bowel disease in an individual; or (ii) subarachnoid hemorrhage or an inflammation related medical condition that is arthritis, eczema, psoriasis, atopic dermatitis, psoriatic arthropathy, asthma, autoimmune diseases, chronic inflammation, chronic prostatitis, glomerulonephritis, hypersensitivities, pelvic inflammatory disease, reperfusion injury, vasculitis, allergies, shoulder tendinitis, myocarditis, nephritis, bursitis or myopathy in an individual.

  本发明提供一种 NCca-ATP 抑制剂，用于治疗和/或预防以下疾病的方法中： (i) 结肠炎或炎症性肠病；或 (ii) 蛛网膜下腔出血或与炎症相关的病症，如关节炎、湿疹、银屑病、特应性皮炎、银屑病关节病、哮喘、自身免疫性疾病、慢性炎症、慢性前列腺炎、肾小球肾炎、过敏性疾病、盆腔炎、再灌注损伤、血管炎、过敏症、肩腱炎、心肌炎、肾炎、滑囊炎或肌病。
• TARGETTING NCCA-ATP CHANNEL FOR ORGAN PROTECTION FOLLOWING ISCHEMIC EPISODE
  申请人：University of Maryland, Baltimore

  公开号：EP3103451A1

  公开（公告）日：2016-12-14

  The present invention provides a pharmaceutical composition comprising an inhibitor of an NCCa-ATP channel and a pharmaceutically acceptable carrier for use in a method of preventing or reducing ischemic damage in one or more organs or tissues selected from kidney, wherein the inhibitor is administered as a loading dose followed by a constant infusion, or the inhibitor is delivered in a dosage of less than 3.5 mg per day, or the inhibitor is delivered at a dosage of less than 0.8 mg/kg body weight within a 24 hour period.

  本发明提供了一种药物组合物，该组合物包含一种 NCCa-ATP 通道抑制剂和一种药学上可接受的载体，用于预防或减轻选自肾脏的一种或多种器官或组织的缺血性损伤的方法，其中 抑制剂以负荷剂量给药，然后持续输注，或 抑制剂的给药剂量低于每天 3.5 毫克，或 抑制剂在 24 小时内的剂量小于 0.8 毫克/千克体重。
• Treatment of alzheimer's disease using compounds that reduce the activity of non-selective CA++ activated ATP-sensitive cation channels regulated by SUR1 channels
  申请人：Biogen Chesapeake LLC

  公开号：US10004703B2

  公开（公告）日：2018-06-26

  NSC antagonists are disclosed as useful in the treatment of dementia, in delaying the onset of dementia, and in the prevention of dementia. Dementia so treated may be, for example, Alzheimer's Disease (AD). NSC antagonists for treating dementia such as AD may be administered alone, a) in combination with other drugs used for treating dementia, b) in combination with drugs that stabilize or increase blood plasma glucose levels, or with both a) and b). Pharmaceutical compositions, dosage forms, and methods for using the same are disclosed, which include NSC antagonists, NSC antagonists combined with dementia drugs, NSC antagonists combined with glucose-level stabilizing or enhancing drugs, or combinations of these. Dosage forms may be designed to provide stable plasma levels for extended periods of time. Exemplary pharmaceutical compositions include compositions including glibenclamide and memantine; glibenclamide and donepezil; tolbutamide and memantine; tolbutamide and donepezil; and these compositions further including glucagon and/or glucose.

  NSC拮抗剂可用于治疗痴呆症、延缓痴呆症的发病和预防痴呆症。所治疗的痴呆症可以是阿尔茨海默病（AD）等。治疗痴呆症（如阿氏痴呆症）的 NSC 拮抗剂可单独使用，a) 与其他治疗痴呆症的药物联合使用，b) 与稳定或提高血浆葡萄糖水平的药物联合使用，或同时使用 a) 和 b)。已公开的药物组合物、剂型和使用方法包括 NSC 拮抗剂、NSC 拮抗剂与痴呆症药物的组合、NSC 拮抗剂与稳定或提高血糖水平的药物的组合或这些药物的组合。剂型可设计成能在较长时间内提供稳定的血浆水平。示例性药物组合物包括格列本脲和美金刚；格列本脲和多奈哌齐；托布他胺和美金刚；托布他胺和多奈哌齐；这些组合物还包括胰高血糖素和/或葡萄糖。
• Targeting NCCA-ATP channel for organ protection following ischemic episode
  申请人：University of Maryland, Baltimore

  公开号：US10166244B2

  公开（公告）日：2019-01-01

  The present invention concerns protection of an organ or tissue outside of the central nervous system following an ischemic episode. In particular aspects, the invention concerns organ preservation for transplantation, angina pectoris, kidney reperfusion injury, and so forth. In specific embodiments, the organ is subjected to an inhibitor of an NCCa-ATP channel that is regulated by SUR1. Exemplary inhibitors include sulfonylurea compounds, such as glibenclamide, for example.

  本发明涉及在缺血发作后保护中枢神经系统以外的器官或组织。在特定方面，本发明涉及用于移植、心绞痛、肾脏再灌注损伤等的器官保护。在具体的实施方案中，器官受到由 SUR1 调节的 NCCa-ATP 通道抑制剂的作用。 示例的抑制剂包括磺酰脲化合物，例如格列本脲。