2H-Pyran-2-one, 6-(bromomethylene)tetrahydro-3-(1-naphthalenyl)- | 144298-62-4

• 分子结构分类: 有机化合物 - 苯类化合物 - 萘
• 英文名称: 2H-Pyran-2-one, 6-(bromomethylene)tetrahydro-3-(1-naphthalenyl)-
• 英文别名: 6-(bromomethylidene)-3-naphthalen-1-yloxan-2-one
• CAS: 144298-62-4
• 化学式: C₁₆H₁₃BrO₂
• 分子量: 317.18
• InChiKey: BYUCSFWXCMTYOI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.2
• 重原子数：
  19
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.19
• 拓扑面积：
  26.3
• 氢给体数：
  0
• 氢受体数：
  2

文献信息

• NOVEL LIPASE INHIBITORS, REPORTER SUBSTRATES AND USES THEREOF
  申请人：Northeastern University

  公开号：US20150099800A1

  公开（公告）日：2015-04-09

  The invention provides for novel lipase inhibitors, and compositions and devices comprising the same. The invention further provides for methods for treatment of disorders comprising administration of novel diacylglycerol lipase inhibitors, and compositions and devices comprising said inhibitors. In some embodiments, the disorders are pancreatitis, obesity, shock or pancreatic necrosis. The invention further provides for novel ether lipid reporter compounds and methods of assaying enzymatic activity comprising contacting a compound with a novel ether lipid reporter compound.

  本发明提供了新型脂肪酶抑制剂，以及包含它们的组合物和装置。本发明还提供了治疗疾病的方法，包括给予新型二酰基甘油脂肪酶抑制剂、含有该抑制剂的组合物和装置。在某些实施例中，这些疾病包括胰腺炎、肥胖症、休克或胰腺坏死。本发明还提供了新型醚脂质报告化合物和测定酶活性的方法，其中将化合物与新型醚脂质报告化合物接触。
• Protection of neurons against glutamate-induced damage in glaucoma and other conditions
  申请人：——

  公开号：US20020077322A1

  公开（公告）日：2002-06-20

  The present invention is directed to a method of protecting cells of the nervous system from glutamate-induced cytotoxicity , such as the type that is mimicked by administration of N-methyl-D-aspartate (NMDA), and which is associated with conditions such as ischemia or glaucoma. In general, the method comprises increasing the activity of a cannabinoid agonist that binds specifically to an endogenous cannabinoid receptor, such as the endogenous cannabinoid receptors CB 1 or CB 2 , to protect the cells against glutamate-induced neurotoxicity. This can be done either by the administration of a cannabinoid agonist such as a physiologically acceptable salt of R(+)-[2,3-dihydro-5-methyl3-[(morpholinyl)methyl]pyrrolo [1,2,3-de]-1,4-benzoxazinyl]-( 1 -naphthalenyl) methanone, preferably the mesylate salt, or by blocking degradation of naturally-occurring endogenous cannabinoid agonists in the cells, such as by inhibition of anandamide amidohydrolase. Administration can be performed by one of several routes, such as enterally, transdermally, or transmucosally.

  本发明涉及一种保护神经系统细胞免受谷氨酸诱导的细胞毒性的方法，例如通过施用 N-甲基-D-天冬氨酸（NMDA）模拟的细胞毒性，这种细胞毒性与缺血或青光眼等病症有关。一般来说，该方法包括提高与内源性大麻素受体（如内源性大麻素受体 CB 1 或 CB 2 等内源性大麻素受体结合的大麻素激动剂的活性，以保护细胞免受谷氨酸诱导的神经毒性的影响。这可以通过施用大麻素激动剂来实现，例如 R(+)-[2,3-二氢-5-甲基-3-[（吗啉基）甲基]吡咯[1,2,3-脱]-1,4-苯并恶嗪基]-(+)的生理上可接受的盐。 1 -萘基）甲酮，最好是甲磺酸盐，或通过阻断细胞中天然存在的内源性大麻素激动剂的降解，例如通过抑制安乃近酰胺酰胺水解酶。给药可通过多种途径之一进行，如肠内、经皮或经口。
• Methods of treating mental diseases, inflammation and pain
  申请人：——

  公开号：US20030134894A1

  公开（公告）日：2003-07-17

  Methods are disclosed for treating or preventing disorders such as mental diseases, inflammation and pain by inhibiting the enzyme anandamide amidohydrolase. A therapeutically effective level of an anandamide amidohydrolase inhibitor is administered such as a therapeutically effective level of a haloenol lactone. Preferably, the haloenol lactone is of the formula: 1 wherein R is hydrogen, R 1 is a halogen, and R 2 is selected from the group consisting of aryl, aryloxy, and heteroaryl radicals, derivatives of said haloenol lactones, and mixtures thereof. The haloenol lactone, E-6-(bromomethylene)tetrahydro-3-(1-naphthalenyl)-2H-pyrane-2-one, is most preferred.

  本发明公开了通过抑制酰胺酶来治疗或预防精神疾病、炎症和疼痛等疾病的方法。施用治疗有效水平的酰胺水解酶抑制剂，如治疗有效水平的卤烯醇内酯。优选地，卤烯醇内酯的化学式为 1 其中 R 为氢、R 1 是卤素，R 2 选自由芳基、芳氧基和杂芳基、所述卤代烯醇内酯的衍生物及其混合物组成的组。最优选的卤代烯醇内酯是 E-6-（溴亚甲基）四氢-3-（1-萘基）-2H-庚-2-酮。
• Calcium-independent phospholipase A2 induces ischemic ventricular arrhythmias and decreases infarction size
  申请人：——

  公开号：US20040185519A1

  公开（公告）日：2004-09-23

  A method for evaluating a compound to determine the relative or absolute therapeutic capability of a compound to pharmacologically inhibit ischemia induced activation of iPLA 2 &bgr; in an intact myocardium which comprises treating intact myocardium with a compound, inducing ischemia in the myocardium tissue and determining if there has been a change in expression of iPLA 2 &bgr;, its activity or in the iPLA 2 &bgr; regulating network and determining if there has been a change then that the compound is an anti-arrhythmia or myocardial salvage drug.

  一种评估化合物的方法，用于确定化合物在药理上抑制缺血诱导的 iPLA2 激活的相对或绝对治疗能力。 2 &bgr;在完整心肌中的相对或绝对治疗能力，该方法包括用化合物处理完整心肌，诱导心肌组织缺血，并确定 iPLA 2 &bgr;的表达、其活性或 iPLA 2 &bgr;调节网络的表达是否发生变化，如果发生变化，则确定该化合物是抗心律失常或心肌救治药物。
• Process for preparing purified s-bel and r-bel and compositions thereof
  申请人：Gross W Richard

  公开号：US20050181496A1

  公开（公告）日：2005-08-18

  A process for resolution of racemic BEL into its individual enantiomeric constituents by chiral HPLC. A method for determining the role of specific isoforms of iPLA 2 in biologic processes.

  一种通过手性高效液相色谱法将外消旋 BEL 分解为单个对映体成分的工艺。一种确定 iPLA 特定异构体作用的方法 2 在生物过程中的作用的方法。