(5E,8E,11E,14E,17E)-1-[4-(pyridine-3-carbonyl)piperazin-1-yl]icosa-5,8,11,14,17-pentaen-1-one

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: (5E,8E,11E,14E,17E)-1-[4-(pyridine-3-carbonyl)piperazin-1-yl]icosa-5,8,11,14,17-pentaen-1-one
• 化学式: C₃₀H₄₁N₃O₂
• 分子量: 475.7
• InChiKey: YZNNXSLWXVXCHV-RCHUDCCISA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.4
• 重原子数：
  35
• 可旋转键数：
  14
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.43
• 拓扑面积：
  53.5
• 氢给体数：
  0
• 氢受体数：
  3

文献信息

• METHODS OF LOWERING PROPROTEIN CONVERTASE SUBTILISIN/KEXIN TYPE 9 (PCSK9)
  申请人：Catabasis Pharmacauticals, Iinc.

  公开号：US20150344430A1

  公开（公告）日：2015-12-03

  The invention relates to new methods of modulating cholesterol by inhibiting proprotein convertase subtilisin/kexin type 9 (PCSK9) with fatty acid derivatives; and new methods for treating or preventing a metabolic disease comprising the administration of an effective amount of a fatty acid derivative. The present invention is also directed to fatty acid bioative derivatives and their use in the treatment of metabolic diseases.

  本发明涉及使用脂肪酸衍生物抑制前蛋白酶转化酶亚精氨酸/酶切割酶9 (PCSK9)来调节胆固醇的新方法；以及通过给予有效量的脂肪酸衍生物来治疗或预防代谢性疾病的新方法。本发明还涉及脂肪酸生物活性衍生物及其在治疗代谢性疾病中的应用。
• USE OF INTRACELLULAR ENZYMES FOR THE RELEASE OF COVALENTLY LINKED BIOACTIVES
  申请人：Catabasis Pharmaceuticals, Inc.

  公开号：EP2949344A2

  公开（公告）日：2015-12-02

  The present invention relates to targeting an intracellular enzyme for release of covalently linked bioactives which results in a synergistic effect between the bioactives. The present invention relates to the use of bioactives that are directly connected covalently or through a covalent molecular linker which have increased therapeutic activity when released as the free bioactives by intracellular enzymes as compared to when the bioactives are administered individually (i.e. not covalendy linked). Further, methods are described of administering to patients in need thereof, bioactives as linked bioactives having increased therapeutic activity. Accordingly, this invention also relates to methods of treating patients for certain diseases.

  本发明涉及靶向细胞内酶释放共价连接的生物活性物质，从而使生物活性物质之间产生协同效应。本发明涉及直接共价连接或通过共价分子连接体连接的生物活性物质的使用，与单独施用生物活性物质（即未共价连接）相比，这些生物活性物质在作为游离生物活性物质被细胞内酶释放时具有更高的治疗活性。此外，本发明还描述了向有需要的患者施用生物活性物的方法，这些生物活性物作为连接的生物活性物具有更高的治疗活性。因此，本发明还涉及治疗患者某些疾病的方法。
• FATTY ACID NIACIN CONJUGATES
  申请人：CATABASIS PHARMACEUTICALS, INC.

  公开号：US20160287712A1

  公开（公告）日：2016-10-06

  The invention provides fatty acid niacin conjugates; pharmaceutical compositions comprising an effective amount of the fatty acid niacin conjugate; and methods for treating or preventing a metabolic disease comprising the administration of an effective amount of the fatty acid niacin conjugate.
• [EN] METHODS OF LOWERING PROPROTEIN CONVERTASE SUBTILISIN/KEXIN TYPE 9 (PCSK9)<br/>[FR] MÉTHODES DE DIMINUTION DE LA PROPROTÉINE CONVERTASE SUBTILISINE/KEXINE DE TYPE 9 (PCSK9)
  申请人：CATABASIS PHARMACEUTICALS INC

  公开号：WO2013177536A2

  公开（公告）日：2013-11-28

  The invention relates to new methods of modulating cholesterol by inhibiting proprotein convertase subtilisin/kexin type 9 (PCSK9) with fatty acid derivatives; and new methods for treating or preventing a metabolic disease comprising the administration of an effective amount of a fatty acid derivative. The present invention is also directed to fatty acid bioative derivatives and their use in the treatment of metabolic diseases.