6-Methylheptane-1,2,3,4,5-pentol

• 分子结构分类: 有机化合物 - 脂质和类脂质分子 - 脂肪酰基
• 英文名称: 6-Methylheptane-1,2,3,4,5-pentol
• 化学式: C₈H₁₈O₅
• 分子量: 194.23
• InChiKey: VVDQVGVVCXMMBN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.1
• 重原子数：
  13
• 可旋转键数：
  5
• 环数：
  0.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  101
• 氢给体数：
  5
• 氢受体数：
  5

文献信息

• CLASS- AND ISOFORM-SPECIFIC HDAC INHIBITORS AND USES THEREOF
  申请人：President and Fellows of Harvard College

  公开号：US20150307444A1

  公开（公告）日：2015-10-29

  HDAC inhibitors of the general formula (I) and (II) and pharmaceutically acceptable salts thereof, as described herein, are useful as inhibitors of histone deacetylases or other deacetylases, and thus are useful for the treatment of various diseases and disorders associated with acetylase/deacetylase activity as described herein (e.g., cancer). In certain embodiments, the compounds of the invention selectively target either a class or isoform of the HDAC family. Another aspect of the invention provides an assay for determining the inhibitory effect of a test compound on an HDAC protein comprising: incubating the HDAC protein with a substrate of general formula (IIIc) in the presence of a test compound; and determining the activity of the HDAC protein.

  本发明提供的通式（I）和（II）的HDAC抑制剂及其药学上可接受的盐，作为组蛋白去乙酰化酶或其他去乙酰化酶的抑制剂，因此可用于治疗与去乙酰化酶活性相关的各种疾病和障碍，如本文所述（例如癌症）。在某些实施例中，本发明的化合物有选择性地靶向HDAC家族的某个类别或亚型。本发明的另一方面提供了一种用于确定试验化合物对HDAC蛋白的抑制作用的测定方法，包括：在试验化合物的存在下，将HDAC蛋白与通式（IIIc）的底物孵育，并确定HDAC蛋白的活性。
• Non-systemic TGR5 agonists
  申请人：Venenum Biodesign, LLC

  公开号：US11236055B2

  公开（公告）日：2022-02-01

  The present invention relates to sulfonamide compounds of formula (I) and formula (II), or a pharmaceutically acceptable salt thereof. The present sulfonamide compounds are useful non-systemic TGR5 agonists that can be used to treat diabetic diseases in human. The present invention provides a pharmaceutical composition containing sulfonamide compounds of formula (I) and formula (II) and a method of making as well as a method of using same in treating patients inflicted with metabolic disorders by administering same. The compounds of the present invention may be used in combination with additional anti-diabetic drugs.

  本发明涉及式（I）和式（II）的磺酰胺化合物或其药学上可接受的盐。本发明的磺酰胺化合物是有用的非全身性 TGR5 激动剂，可用于治疗人类糖尿病疾病。本发明提供了一种含有式（I）和式（II）磺酰胺化合物的药物组合物及其制造方法，以及一种通过给药治疗代谢紊乱患者的方法。本发明的化合物可与其他抗糖尿病药物联合使用。
• LUMINESCENT LANTHANIDE LABELLING REAGENTS AND THEIR USE
  申请人：Abacus Diagnostica OY

  公开号：EP2052252B1

  公开（公告）日：2010-11-10
• Prodrugs of Succinic Acid for Increasing ATP Production
  申请人：NEUROVIVE PHARMACEUTICAL AB

  公开号：US20170105960A1

  公开（公告）日：2017-04-20

  The present invention provides novel cell-permeable succinates and cell permeable precursors of succinate aimed at increasing ATP-production in mitochondria. The main part of ATP produced and utilized in the eukaryotic cell originates from mitochondrial oxidative phosphorylation, a process to which high-energy electrons are provided by the Kreb's cycle. Not all Kreb's cycle intermediates are readily permeable to the cellular membrane, one of them being succinate. The provision of the novel cell permeable succinates is envisaged to allow passage over the cellular membrane and thus the cell permeable succinates can be used to enhance mitochondrial ATP-output.
• Novel Cell-Permeable Succinate Compounds
  申请人：NEUROVIVE PHARMACEUTICAL AB

  公开号：US20170105961A1

  公开（公告）日：2017-04-20

  The present invention provides novel cell-permeable succinates and cell permeable precursors of succinateaimed at increasing ATP-production in mitochondria. The main part of ATP produced and utilized in the eukaryotic cell originates from mitochondrial oxidative phosphorylation, a process to which high-energy electrons are provided by the Kreb's cycle. Not all Kreb's cycle intermediates are readily permeable to the cellular membrane, one of them being succinate. The provision of the novel cell permeable succinates is envisaged to allow passage over the cellular membrane and thus the cell permeable succinates can be used to enhance mitochondrial ATP-output.