2-[4-(4-Methyl-2-oxochromen-7-yl)piperazin-1-yl]ethyl 1-phenylcyclohexane-1-carboxylate

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 英文名称: 2-[4-(4-Methyl-2-oxochromen-7-yl)piperazin-1-yl]ethyl 1-phenylcyclohexane-1-carboxylate
• 英文别名: 2-[4-(4-methyl-2-oxochromen-7-yl)piperazin-1-yl]ethyl 1-phenylcyclohexane-1-carboxylate
• 化学式: C₂₉H₃₄N₂O₄
• 分子量: 474.6
• InChiKey: NMZZQIDFNAXHMT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.2
• 重原子数：
  35
• 可旋转键数：
  7
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.45
• 拓扑面积：
  59.1
• 氢给体数：
  0
• 氢受体数：
  6

文献信息

• Sigma receptor ligands and methods of modulating cellular protein homeostasis using same
  申请人：DREXEL UNIVERSITY

  公开号：US10314795B2

  公开（公告）日：2019-06-11

  The present invention includes compounds useful in preventing, treating or ameliorating Sigma-related disorders or diseases. The compounds of the invention may modulate cellular protein homeostasis, which includes: translation initiation, folding, processing, transport, and degradation (including ubiquitin selective autophagy) of proteins. The present invention also includes methods of preventing, treating or ameliorating a Sigma-related disorder or disease in a subject in need thereof, the method comprising administering to the subject an effective amount of a Sigma-modulating compound. The present invention also includes methods of preventing, treating or ameliorating a Sigma-related disorder or disease in a subject in need thereof, the method comprising administering to the subject an effective amount of a Sigma-modulating compound, further comprising administering an effective amount of a compound that inhibits the ubiquitin proteasome system (UPS) and/or autophagic survival pathways.

  本发明包括可用于预防、治疗或改善西格玛相关紊乱或疾病的化合物。本发明的化合物可调节细胞蛋白质的平衡，其中包括：蛋白质的翻译起始、折叠、加工、运输和降解（包括泛素选择性自噬）。本发明还包括预防、治疗或改善有需要的受试者与 Sigma 相关的失调或疾病的方法，该方法包括向受试者施用有效量的 Sigma 调节化合物。本发明还包括预防、治疗或改善有需要的受试者的西格玛相关紊乱或疾病的方法，该方法包括向受试者施用有效量的西格玛调节化合物，进一步包括施用有效量的抑制泛素蛋白酶体系统（UPS）和/或自噬存活途径的化合物。
• NOVEL SIGMA RECEPTOR LIGANDS AND METHODS OF MODULATING CELLULAR PROTEIN HOMEOSTASIS USING SAME
  申请人：Drexel University

  公开号：EP2874997A2

  公开（公告）日：2015-05-27
• US9388126B2
  申请人：——

  公开号：US9388126B2

  公开（公告）日：2016-07-12
• US9889102B2
  申请人：——

  公开号：US9889102B2

  公开（公告）日：2018-02-13
• [EN] NOVEL SIGMA RECEPTOR LIGANDS AND METHODS OF MODULATING CELLULAR PROTEIN HOMEOSTASIS USING SAME<br/>[FR] NOUVEAUX LIGANDS DU RÉCEPTEUR SIGMA ET PROCÉDÉS DE MODULATION DE L'HOMÉOSTASE DE PROTÉINE CELLULAIRE À L'AIDE DE CEUX-CI
  申请人：PHILADELPHIA HEALTH & EDUCATIO

  公开号：WO2014015157A2

  公开（公告）日：2014-01-23

  The present invention includes compounds useful in preventing, treating or ameliorating Sigma-related disorders or diseases. The compounds of the invention may modulate cellular protein homeostasis, which includes: translation initiation, folding, processing, transport, and degradation (including ubiquitin selective autophagy) of proteins. The present invention also includes methods of preventing, treating or ameliorating a Sigma-related disorder or disease in a subject in need thereof, the method comprising administering to the subject an effective amount of a Sigma-modulating compound. The present invention also includes methods of preventing, treating or ameliorating a Sigma-related disorder or disease in a subject in need thereof, the method comprising administering to the subject an effective amount of a Sigma-modulating compound, further comprising administering an effective amount of a compound that inhibits the ubiquitin proteasome system (UPS) and/or autophagic survival pathways.